0000000000020988

AUTHOR

José-luis Ríos

Apoptotic Activities of Mediterranean Plant Species

Abstract Throughout the Mediterranean region, medicinal plants are widely used to improve health and avoid disease. Various epidemiological studies indicate that some of these plants reduce the incidence of inflammatory diseases and cancer by inducing programmed cell death, thus arresting proliferation. Several of these plant species, including saffron, capsicum, garlic, and onion, are employed for many purposes, while others, such as mistletoe, myrtle, French lavender, and rue, have more selective uses. For example, saffron exerts a chemopreventive effect by inhibiting cell proliferation and inducing apoptosis, and garlic inhibits cancer cell growth by promoting early mitotic arrest and ap…

research product

A taxonomical study of the subtribe leontodontinae based on the distribution of phenolic compounds

Abstract Evaluation of the phenolic constituents of five species belonging to the subtribe Leontodontinae (family Asteraceae) allowed the identification of ten flavonoid and eight phenolic acids by means of HPLC and other standard methods. The role of these compounds in relation to the morphological characteristics in the systematics of the subtribe is discussed.

research product

Screening of some rare endemic Italian plants for inhibitory activity on 5-lipoxygenase

Abstract The extracts of four rare plants found on the islands of Sicily, Vulcano and Marettimo, Southern Italy, were screened for their inhibitory effect on the production of leukotriene B 4 by 5-lipoxygenase in intact cells. The methanol extracts of pods of Cytisus aeolicus and aerial parts of Thymus richardii were the most active extracts, inhibiting almost completely the leukotriene B 4 production at 200 and 50 μg/ml, respectively.

research product

Medicinal plants and antimicrobial activity.

In the present paper, we analyze the past, present and future of medicinal plants, both as potential antimicrobial crude drugs as well as a source for natural compounds that act as new anti-infection agents. In the past few decades, the search for new anti-infection agents has occupied many research groups in the field of ethnopharmacology. When we reviewed the number of articles published on the antimicrobial activity of medicinal plants in PubMed during the period between 1966 and 1994, we found 115; however, in the following decade between 1995 and 2004, this number more than doubled to 307. In the studies themselves one finds a wide range of criteria. Many focus on determining the antim…

research product

Effect of triterpenoids on the inflammation induced by protein kinase C activators, neuronally acting irritants and other agents.

In order to establish the mode of the anti-inflammatory activity of triterpenoids, 11 naturally occurring compounds were assayed on mouse ear oedema induced by the protein kinase C activators, mezerein, 12-O-tetradecanoylphorbol-13-acetate (TPA), two 12-deoxyphorbol-13-monoesters (13-tetradecanoate (DPT) and 13-phenylacetate (DPP)) and bryostatin 1, and by resiniferatoxin, xylene and arachidonic acid. The effects on bradykinin-induced paw oedema and on the rat skin inflammation caused by hydrogen peroxide were also examined. The oedema induced by mezerein and DPT was reduced to different extents by the triterpenoids administered epicutaneously (0.5 mg per ear). Against DPT-induced oedema, l…

research product

Antimicrobial activity of selected plants employed in the Spanish mediterranean area. Part II

The antimicrobial properties of 59 plants used in folk medicine to treat general infectious diseases were studied. The in vitro antimicrobial activity of chloroform and methanol plant extracts were assayed using the agar-streak method and 38 of them showed activity against some of the microorganisms tested. Bioautography established the probable active compounds. Inhibition bands were identified as containing terpenoids and polyphenolic compounds.

research product

On the anti-inflammatory and anti-phospholipase A2 activity of extracts from lanostane-rich species

Abstract We have studied extracts from three species rich in lanostane triterpenes for their activity against different in vivo models of inflammation induced by TPA, EPP and PLA2. The inhibitory effect against PLA2 in vitro was also studied. When the Poria cocos extract was tested against PLA2-induced mouse paw edema, it was active by the oral and parenteral routes. Its effect was greater in both magnitude and duration than that of Pistacia terebinthus and Ganoderma lucidum extracts. P. terebinthus was effective against chronic and acute inflammation, and according to a preliminary chromatographic analysis, its seems to be a good source of lanostane anti-inflammatory agents. G. lucidum was…

research product

An Update Review of Saffron and its Active Constituents

This paper reviews the literature on recent research on the chemical composition and pharmacological activities of saffron (Crocus sativus) and its active constituents, mainly as antitumoral, hypolipidemic and tissue oxygenation enhancement agents.

research product

Cardioprotection and natural polyphenols: An update of clinical and experimental studies

Myocardial ischemia is the leading cause of death worldwide. Despite better outcomes with early coronary artery reperfusion strategies, morbidity and mortality remain significant. The principal myocardial hallmark of myocardial ischemia is cell death and the associated impairment of cardiac contractility. In this way, the use of extracts from medicinal plants versus synthetic drugs to mitigate post-ischemic damage constitutes an alternative. Despite their proven beneficial effects in cardiovascular disorders, the use of many plants is questioned. Our aim is to update the clinical and experimental studies about the actions of medicinal plants and polyphenol-enriched extracts against ischemia…

research product

Bcl-2 is a negative regulator of interleukin-1β secretion in murine macrophages in pharmacological-induced apoptosis

BACKGROUND AND PURPOSE Cucurbitacin R, a natural anti-inflammatory product, has been shown to exhibit activity against both adjuvant-induced arthritis and delayed-type hypersensitivity reactions induced by various agents. Previous studies have demonstrated that the effects of cucurbitacin R stem from its inhibition of both cytokine production and lymphocyte proliferation. EXPERIMENTAL APPROACHES Effects of cucurbitacin R were investigated on lipopolysaccharide-stimulated RAW 264.7 cells. Cell cycle evolution was analysed by flow cytometry, detection of apoptosis by DNA ladder, Bcl-2, p21, p53, Bax, cleaved caspase-1 (p10), caspase-9, and caspase-3, cleaved caspase (p17) and interleukin-1β d…

research product

Essential Oils

Abstract Essential oils are aromatic, volatile liquids obtained from plant material through steam distillation and named after the plant from which they are derived. Essential oils can be defined as either products or mixtures of fragrant substances or as mixtures of fragrant and odorless substances. These fragrant substances are chemically pure compounds that are volatile under normal conditions. Essential oils vary greatly, sometimes due to genetic causes, but also because of climate, rainfall, or geographic origin. They are composed principally of lipophilic and highly volatile secondary plant metabolites, principally mono- and sesquiterpenes, but other types of compounds such as allyl a…

research product

Phenolic Substances from Phagnalon rupestre Protect against 2,4,6-Trinitrochlorobenzene-Induced Contact Hypersensitivity

2-isoprenylhydroquinone-1-glucoside (1), 3,5-dicaffeoylquinic acid (2), and 3,5-dicaffeoylquinic acid methyl ester (3), isolated from Phagnalon rupestre, improved the contact hypersensitivity response to 2,4,6-trinitrochlorobenzene in mice. These phenolics reduced ear swelling and IL-1β content by 50% 24 h after challenge; in addition, 2 inhibited tumor necrosis factor-α by 53%. All three compounds also reduced interleukin-2 content by 50% 72 h after challenge. Both 2 and 3 inhibited metalloproteinase-9 levels in the skin lesions by 66% and 41%, respectively, and lowered cyclooxygenase-2 expression by 44% and 49%, respectively, at 24 h. Moreover, 2 was effective against atopic dermatitis in…

research product

Dual inhibition of cyclooxygenase-1 and 5-lipoxygenase by aerial part of Bupleurum fruticescens methanol extract

The effect of the methanol extract from aerial parts of Bupleurum fruticescens on the release of eicosanoids and hydrolytic enzymes was determined on in vitro cell systems. The extract had a significant effect on 5-lipoxygenase (5-LOX) activity, inhibiting both LTB4 and 5(S)-HETE production with IC50 values of 112 microg/ml and 95 microg/ml, respectively. At concentrations of 200 microg/ml, the extract also inhibited cyclooxygenase-1 (90%) and elastase activities (54%). The 12-LOX activity in intact platelets was not affected; a fact, which suggests that phospholipase A2 (PLA2) activity, is not modified by the extract.

research product

A Pharmacological Update of Ellagic Acid.

Este artículo se encuentra disponible en la página web de la revista en la siguiente URL: https://www.thieme-connect.com/products/ejournals/pdf/10.1055/a-0633-9492.pdf This is a pre-print of an article published in Ríos, JL., Giner, RM., Marín, M. and Recio, MC. (2018). A pharmacological update of ellagic acid. Planta Medica, vol. 84, n. 15, pp. 1068-1093. The final authenticated version is available online at: https://doi.org/10.1055/a-0633-9492 Este es el pre-print del siguiente artículo Ríos, JL., Giner, RM., Marín, M. and Recio, MC. (2018). A pharmacological update of ellagic acid. Planta Medica, vol. 84, n. 15, pp. 1068-1093 que se ha publicado de forma definitiva en https://doi.org/10…

research product

A new dual inhibitor of arachidonate metabolism isolated from Helichrysum italicum.

Six acetophenones (1-6) and one gamma-pyrone (7), previously isolated from Helichrysum italicum, were tested for their ability to inhibit enzymatic and non-enzymatic lipid peroxidation, the stable 1,1-diphenyl-2-pycryl-hydrazyl free radical, superoxide scavenging and arachidonic acid metabolism. In addition, they were studied in different experimental models such as the chronic inflammation induced by 12-O-tetradecanoylphorbol 13-acetate (TPA), the phospholipase A(2)-induced mouse paw oedema test, the carrageenan-induced mouse paw oedema test, and the writhing induced by acetic acid in the mouse. Of the assayed compounds, only 1 inhibited enzymatic lipid peroxidation but had no effect on no…

research product

In vitro and in vivo effects of Ranunculus peltatus subsp. baudotii methanol extract on models of eicosanoid production and contact dermatitis

Ranunculus (Crowfoot) species are numerous and they are all reputed to be counter-irritants and are used in several topical conditions. In order to study the pharmacological mechanisms of action underlying this popular use, a methanol extract of Ranunculus peltatus was tested in vitro in various assays involving eicosanoid and human elastase release by intact cells as well as in vivo, with models of delayed-type hypersensitivity (DTH) contact dermatitis. The extract proved to be a selective inhibitor of the cyclooxygenase-1 pathway, producing the total inhibition of 12-(S)-HHTrE release at 200 microg/mL, while leaving both 5-lipoxygenase and 12-lipoxygenase activities unaffected at the same…

research product

Oleuropein protects against dextran sodium sulfate-induced chronic colitis in mice.

The anti-inflammatory effect of oleuropein (1), the major phenolic secoiridoid in Olea europaea, was evaluated in an experimental model of chronic colitis in mice. Animals were exposed to four repeated cycles of dextran sodium sulfate in drinking water followed by a 7-day rest period. Animals receiving a standard diet supplemented with 0.25% of 1 (equivalent to 500 mg/kg/day) for 56 days exhibited a decrease of inflammatory symptoms, as reflected by improvement of disease activity index and histopathological changes. It was found that 1 decreased inflammatory cell recruitment and the release of inflammatory cytokines interleukin (IL)-1β and IL-6 with increased IL-10 levels in colon tissue. …

research product

On the activity of trifluoperazine and palmitoylcarnitine in mice: Delayed hypersensitivity models

Abstract The effect of pre- and post-challenge treatments with trifluoperazine and palmitoylcarnitine, two protein kinase C (PKC) inhibitors characterised by their interaction with the phospholipid enzyme cofactor, on the inflammation caused by delayed hypersensitivity (DTH) to dinitrofluorobenzene (DNFB) and sheep red blood cells (SRBC) in mice is reported. The activity of dexamethasone and two immunosupressors, azathioprine and methotrexate, is also evaluated. The effectiveness of pre-treatment with each of the test drugs diminished when the DNFB challenge dose increased, whereas trifluoperazine and azathioprine were more active when administered after the challenge at the high DNFB dose.…

research product

CNS depressant effects, anti-inflammatory activity and anti-cholinergic actions ofSantolina chamaecyparissus extracts

The pharmacological activity of several extracts together with the lyophilized infusion of S. chamaecyparissus ssp. squarrosa were investigated. The lethal dose 50% (LD50), effect on animal metabolism, mechanical and thermic analgesia and spontaneous, anti-inflammatory, and anti-ulcer activity have been determined. Studies on isolated organs (rat duodenum and rat uterus) were also carried out. The hexanic and chloroformic extracts were potent antagonists of the thermic analgesia test; the former extract was also active in the mechanical analgesia test. The chloroformic extract and, to a lesser extent, the ethyl acetate extract and lyophilized infusion demonstrated noteworthy activity as ant…

research product

A chematoxonomic review of the subtribe crepidinase based on its phenol constituents

Abstract The chemotaxonomical significance of flavonoids, phenolic acids and coumarins from 20 species, belonging to eight genera of the subtribe Crepidinae (family Compositae), is discussed. The content in phenolic compounds of three species of Lactuca (L. tenerrima, L. virosa and L. muralis ) is reported for the first time.

research product

Inhibition of c-MYC with involvement of ERK/JNK/MAPK and AKT pathways as a novel mechanism for shikonin and its derivatives in killing leukemia cells

Leukemia remains life-threatening despite remarkable advances in chemotherapy. The poor prognosis and drug resistance are challenging treatment. Novel drugs are urgently needed. Shikonin, a natural naphthoquinone, has been previously shown by us to be particularly effective towards various leukemia cell lines compared to solid tumors. However, the underlying mechanisms are still poorly understood. Here, we investigated shikonin and 14 derivatives on U937 leukemia cells. Four derivatives (isobutyrylshikonin, 2-methylbutyrylshikonin, isovalerylshikonin and β,β-dimethylacrylshikonin) were more active than shikonin. AnnexinV-PI analysis revealed that shikonins induced apoptosis. Cell cycle G1/S…

research product

Topical anti-inflammatory activity of some Asian medicinal plants used in dermatological disorders.

The topical anti-inflammatory activity of extracts from Cassia angustifolia, Rheum palmatum, Coptis chinensis, Phellodendron amurense and Scutellaria baicalensis, plants used in traditional East Asian medicine against different skin disorders, was studied. Though in different degree, all the extracts significantly inhibited the edema induced by 12-O-tetradecanoylphorbol-13-acetate (TPA), in both single or multiple application, oxazolone, and arachidonic acid (AA). None of the extracts inhibited in vitro the activity of phospholipase A(2) (PLA(2)) from Naja naja.

research product

Inhibition of Trypanosoma cruzi by plant extracts used in Chinese medicine.

In this work, we assessed the effect of extracts obtained from 17 plants used in traditional Chinese medicine. These extracts were tested in vitro with the epimastigote form of Trypanosoma cruzi, clone Bra C(15) C(2), at 27 degrees C in F-29 medium at a concentration of 100 microg/ml in axenic cultures. Allopurinol was used as reference drug. Seven plant extracts showed inhibitory activities lower than 25%. Pueraria lobata, Mahonia beaei, Dictamus dasycarpus, Kochia scoparia, Sophora flavescens and Ligustrum lucidum showed effects with inhibition values between 25% and 60%, whereas Lithospermum erythrorhizon, Saussurea lappa, Melia toosendan and Cinnamomum cassia showed the greatest inhibit…

research product

Structural considerations on the iridoids as anti-inflammatory agents.

Abstract Twelve iridoid glycosides have been evaluated for their anti-inflammatory activity on two models: the carrageenan-induced mouse paw edema and the TPA-induced mouse ear edema. Loganic acid was the most active (44.4% edema inhibition) on the former test, whereas the catalpol derivative mixture isolated from Scrophularia, aucubin, verbenalin, and loganin, showed the highest activity (from 72.0 to 80.0% edema inhibition) on the latter. The results allowed us to establish the relationship between the structure and anti-inflammatory activity on the basis of the different patterns of substitution, particularly hydroxylation, unsaturation, and acylation.

research product

In vivo anti-inflammatory activity of saponins from Bupleurum rotundifolium

Seven oleanane-type triterpene saponins were isolated from the methanolic extract of the aerial parts of Bupleurum rotundifolium. They were identified on the basis of their spectral data as 3-O-[alpha-L-rhamnopyranosyl (1--2)-beta-D-glucopyranosyl (1--2)-beta-D-glucopyranosyl]-28-O-[beta-D-glucopyranosyl (1--2)-beta-D-glucopyranosyl] echinocystic acid (saponin 1), 3-O-[alpha-L-rhamnopyranosyl (1--2)-beta-D-glucopyranosyl (1--2)-beta-D-fucopyranosyl] 11-methoxy-primulagenin A (saponin 2), rotundioside E (saponin 3), rotundioside F (saponin 4), 3beta-sulfate, 28-O-[beta-D-glucopyranosyl (1--6)-beta-D-glucopyranosyl (1--2)-beta-D-glucopyranosyl (1--2)-beta-D-glucopyranosyl] ester of primulagen…

research product

Dihydrocucurbitacin B Inhibits Delayed Type Hypersensitivity Reactions by Suppressing Lymphocyte Proliferation

We have studied the effects of dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, on different models of delayed type hypersensitivity (DTH) in mice, as well as on T-lymphocyte proliferation and the mediators involved. In experiments with mice, dihydrocucurbitacin B inhibited the inflammatory reactions induced by oxazolone, dinitrofluorobenzene, and sheep red blood cells, reducing both the edema and cell infiltration. Moreover, the analysis of inflamed tissues showed that dihydrocucurbitacin B reduced the presence of the most relevant cytokines implicated in these processes, including interleukin-1 beta, interleukin-4, and tumor necrosis factor-alpha. Dihydrocucurbita…

research product

Demethylnobiletin inhibits delayed-type hypersensitivity reactions, human lymphocyte proliferation and cytokine production

Background and purpose: Our aim was to examine the effect of demethylnobiletin on various experimental models of delayed-type hypersensitivity (DTH) reactions and to determine its influence on the mediators and enzymes involved in these reactions. Experimental approach: DTH was induced in mice by oxazolone, dinitrofluorobenzene (DNFB) and sheep red blood cells (SRBC). The effect of demethylnobiletin on the ensuing DTH was studied, especially in relation to oedema formation, cell infiltration and tissue damage. Its activity on different mediators implicated in DTH reactions was also determined and its effect on nitric oxide synthase (NOS)-2 analysed. Finally, its influence on T lymphocyte pr…

research product

Effects of naturally occurring dihydroflavonols from Inula viscosa on inflammation and enzymes involved in the arachidonic acid metabolism

Abstract The anti-inflammatory properties of three flavanones isolated from Inula viscosa , sakuranetin, 7- O -methylaromadendrin, and 3-acetyl-7- O -methylaromadendrin, have been tested both in vitro and in vivo. Acute inflammation in vivo was induced by means of topical application of 12- O -tetradecanoylphorbol 13-acetate (TPA) to mouse ears or by subcutaneous injection of phospholipase A 2 (PLA 2 ) into mouse paws. The test compounds were evaluated in vitro for their effect on both the metabolism of arachidonic acid and on the release and/or activity of enzymes involved in the inflammatory response such as elastase, myeloperoxidase (MPO), and protein kinase C (PKC). The most active comp…

research product

New prenylhydroquinone glycosides from Phagnalon rupestre.

Three new hydroquinone glycosides were isolated from the MeOH extract of the aerial parts of Phagnalon rupestre. Their structures were elucidated as 1-O-beta-glucopyranosyl-1,4-dihydroxy-2-(3',3'-dimethylallyl)benzene (1), 1-O-beta-glucopyranosyl-1,4-dihydroxy-2-(3'-hydroxymethyl-3'-methylallyl)benzene (2), and 1-O-(4' '-O-caffeoyl)-beta-glucopyranosyl-1,4-dihydroxy-2-(3',3'-dimethylallyl)benzene (3) by spectroscopic methods.

research product

Assessment of the anti-inflammatory activity and free radical scavenger activity of tiliroside

Three flavonoids, gnaphaliin, pinocembrin and tiliroside, isolated from Helichrysum italicum, were studied in vitro for their antioxidant and/or scavenger properties and in vivo in different models of inflammation. In vitro tests included lipid peroxidation in rat liver microsomes, superoxide radical generation in the xanthine/xanthine oxidase system and the reduction of the stable radical 1,1-diphenyl-2-pycryl-hydrazyl (DPPH). Acute inflammation was induced by application of 12-O-tetradecanoylphorbol 13-acetate (TPA) to the mouse ear or by subcutaneous injection of phospholipase A(2) or serotonin in the mouse paw. Eczema provoked on the mouse ear by repeated administration of TPA was selec…

research product

Cacao extract enriched in polyphenols prevents insulin-resistance and dyslipemia in a rat model

research product

Shikonin reduces the tumour formation and IL-17 in a model of colorectal cancer associated to chronic colitis in C57BL/6 mice

research product

Investigations on the Steroidal Anti-Inflammatory Activity of Triterpenoids fromDiospyros leucomelas*

Three triterpenes were isolated from Diospyros leucomelas and identified as betulin, betulinic acid, and ursolic acid. They showed anti-inflammatory activity in the carrageenan and serotonin paw edema tests and TPA and EPP ear edema tests. The blockade of their effects by progesterone, actinomycin D, and cycloheximide has served to determine the mechanism of action in relationship with that of glucocorticoids. Betulinic acid was the most affected and therefore a mode of action similar to these drugs may be postulated for it.

research product

Anti-inflammatory glycoterpenoids from Scrophularia auriculata.

The activity of the four glycoterpenoids: two saponins, verbascosaponin A and verbascosaponin, and two iridoids, scropolioside A and scrovalentinoside, isolated from Scrophularia auriculata ssp. pseudoauriculata, were studied in different models of acute and chronic inflammation. Both saponins significantly inhibited the mouse paw edema induced by carrageenan and ear edema induced by single and multiple doses of 12-O-tetradecanoylphorbol 13-acetate (TPA). Verbascosaponin A showed a potency twice as high as that of indomethacin in the acute TPA model. Verbascosaponin A and scropolioside A were active after a long latency period against ethyl phenylpropiolate edema, as are glucocorticoids. Wh…

research product

Natural Triterpenoids as Anti-Inflammatory Agents

Abstract This chapter reviews the natural triterpenes with anti-inflammatory activity, including the traditional ones and the new compounds isolated over the last six years. Triterpenes are widely distributed in plants, and in many cases are the principles responsible for their anti-inflammatory effects. Many of these compounds are active in different in vivo experimental models such as hind paw edema induced by carrageenan, serotonin and phospholipase A2; ear edema induced by phorbol and daphnane esters, ethylphenylpropiolate, arachidonic acid and capsaicin; adjuvant arthritis and experimental models of allergy. Other effects have been studied in vitro, and some triterpenes are active agai…

research product

Cocoa polyphenols and their potential benefits for human health.

This paper compiles the beneficial effects of cocoa polyphenols on human health, especially with regard to cardiovascular and inflammatory diseases, metabolic disorders, and cancer prevention. Their antioxidant properties may be responsible for many of their pharmacological effects, including the inhibition of lipid peroxidation and the protection of LDL-cholesterol against oxidation, and increase resistance to oxidative stress. The phenolics from cocoa also modify the glycemic response and the lipid profile, decreasing platelet function and inflammation along with diastolic and systolic arterial pressures, which, taken together, may reduce the risk of cardiovascular mortality. Cocoa polyph…

research product

Effects of plant alkylphenols on cytokine production, tyrosine nitration and inflammatory damage in the efferent phase of contact hypersensitivity

Background and purpose: The phenolic compounds isoprenylhydroquinone glucoside (IHG), 3,5-dicaffeoylquinic acid (DCA), and its methyl ester (DCE) have previously been shown to inhibit both contact hypersensitivity (CHS) and peroxynitrite reactivity. The present work seeks to establish a relationship between the anti-inflammatory effect and the release of cytokines and tyrosine nitration in skin. Experimental approach: Murine CHS was developed by means of sensitization and challenge with dinitrofluorobenzene (DNFB) or oxazolone. Ear swelling was measured 24 and 96 h after challenge. Interleukin (IL)-1b, IL-4, and tumour necrosis factor (TNF)-a were measured by ELISA; and the expression of in…

research product

Lanostanoids from Fungi as Potential Medicinal Agents

research product

Isolation and identification of an antiinflammatory principle from santolina chamaecyparissus

The chloroform extract from Santolina chamaecyparissus squarrosa exhibited a potent anti-inflammatory effect on carrageenan-induced oedema in the rat hind paw. β-Sytosteryl 3-β-D-glucoside, isolated by fractionating this extract, was anti-inflammatory in the above test, with intraperitoneal and oral ED50 values of 70 and 146 mg/kg, respectively.

research product

Inhibition of Transcription Factors by Plant-Derived Compounds and their Implications in Inflammation and Cancer

Inflammation is a general term used to describe various pathological processes with diverse causes that can include infection, trauma, or an autoimmune response. Due to its many causes, the inflammatory response involves multiple and varied mediators, including vasoactive amines, free radicals, and both lipidic and peptidic mediators. Medicinal plants and the compounds derived from them are a good source of new and specific inhibitors of the inflammatory process. The past decade has witnessed many important discoveries in this field, with new findings challenging the more traditional views of pharmacologists. Various studies, for example, have demonstrated the positive effects of plant-deri…

research product

Anti-Inflammatory Activity of Unusual Lupane Saponins fromBupleurum fruticescens

Extracts from Bupleurum fruticescens were examined for oral and topical anti-inflammatory activities. The BuOH extract proved to be active against carrageenan and tetradecanoylphorbol acetate acute edemas and allowed the isolation of three saponins identified by spectroscopic techniques as 3 beta-O-(O-alpha-L-rhamnopyranosyl-(1-->4)-O-[beta-D-glucopyranosyl- (1-->6)]-O-beta-D-glucopyranosyl)lup-20(29)-ene-23,28-dioic acid (fruticesaponin A), 3 beta-O-(O-alpha-L-rhamnopyranosyl-(1-->4)-O-beta-D-glucopyranosyl) lup-20(29)-ene-23,28-dioic acid 28-O-beta-D-glucopyranosyl ester (fruticesaponin B), and 3 beta-O-(O-alpha-L-rhamnopyranosyl-(1-->4)-O-[beta-D-glucopyranosyl- (1-->6)]-O-beta-D-glucopy…

research product

Zanhasaponins A and B, Antiphospholipase A2 Saponins from an Antiinflammatory Extract of Zanha africana Root Bark

A MeOH extract from Z. africana was examined for topical antiinflammatory activity and proved to be active against arachidonic acid (AA) acute edema, 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced chronic inflammation, and oxazolone delayed-type hypersensitivity in mice. The extract also showed significant inhibitory activity of Naja naja phospholipase A2 when a polarographic method was used. Two oleanane-type triterpene saponins, zanhasaponins A (1) and B (2), and the cyclitol pinitol (4), isolated from the extract, were active as inhibitors of PLA2. A further saponin, zanhasaponin C (3) was inactive in this assay.

research product

Anti-inflammatory Effects of South American Tanacetum vulgare

Abstract In recent years the role of phenolic compounds and sesquiterpene lactones, particularly parthenolide, in the anti-migraine and anti-inflammatory effects of Tanacetum parthenium (Asteraceae) has attracted much attention. However, the closely-related cosmopolitan species T. vulgare has remained outside the mainstream of research in this field. After treating the aerial parts of T. vulgare with dichloromethane and methanol, and applying conventional column and thin-layer chromatographic techniques, it was possible to isolate from the moderately lipophilic fractions the principles responsible for the anti-inflammatory activity of this plant against the mouse-ear oedema induced by 12-O-…

research product

Screening of tropical medicinal plants for antiinflammatory activity

The antiinflammatory activity of different extracts from 16 tropical plant species belonging to 15 different families has been determined. They were administered topically on TPA-induced mouse ear oedema and orally on carrageenan-induced mouse paw oedema. In the latter, extracts from Diospyros leucomelas, Erythrospermum monticolumn, Ficus polita, Heteromorpha trifoliata, Hypericum lalandii, Kirkia acuminata, Pterocarpus angolensis and Zanha africana significantly reduced the oedema 3 h after carrageenan injection. All the extracts were considerably active when assayed topically with only three exceptions.

research product

Isoprenylhydroquinone glucoside: a new non-antioxidant inhibitor of peroxynitrite-mediated tyrosine nitration

Abstract Three hydroquinone glucosides and four caffeoylquinic esters were examined for their effect on tyrosine nitration, as well as on the oxidation of dihydrorhodamine (DHR) 123 and cytochrome c 2+ induced by peroxynitrite. All these phenolics, which had previously been characterized as the active principles of the plant Phagnalon rupestre , were fairly active in preventing the oxidation of DHR 123, though inefficient in the cytochrome c test. While their antioxidant potency is associated with the presence of a caffeoyl moiety, not so an obvious chemical character was correlated to a greater activity against nitration of tyrosine. Here, the highest potency corresponded to 2-isoprenylhyd…

research product

Phenolics of Reichardia and their taxonomic implications

Abstract Fifteen compounds have been detected in Reichardia tingitana and R. picroides (nine flavonoids, four cinnamic derivatives and two unidentified non-phenolic compounds). The present study examines the taxonomic implications of these compounds in relation to the morphological and karyological characteristics.

research product

Pharmacological approach to the pro- and anti-inflammatory effects of Ranunculus sceleratus L.

Ranunculus sceleratus is a widespread species with unique toxicological and pharmacological activities. The present study seeks to assess this species' ability, both in vitro and in vivo, to modulate processes involved in inflammations. To this end, different extracts from the aerial parts of the plant were tested in several models of acute inflammation induced by tetradecanoylphorbol acetate (TPA), arachidonic acid (AA), and carrageenan, as well as in two models of delayed hypersensitivity induced by oxazolone and dinitrofluorobencene (DNFB). The extracts were also assayed in models of eicosanoid and elastase release by intact cells. When tested in vivo, all of the extracts showed anti-inf…

research product

Anti-Inflammatory Activity of Flavonol Glycosides fromErythrospermum monticolumDepending on Single or Repeated Local TPA Administration

Two anti-inflammatory principles were isolated from the methanol extract of the leaves of Erythrospermum monticolum (Flacourtiaceae). The isolation was based on a guided bioassay of the inhibitory activity on TPA-induced ear edema in mice. These compounds were identified as quercetin 3-O-xylosyl(1-->2) rhamnoside and quercetin 3-O-rhamnoside. In addition, their effects on a chronic topic inflammation model were evaluated.

research product

Two fungal lanostane derivatives as phospholipase A2 inhibitors.

The hydroalcoholic extract of Poria cocos and two lanostane derivatives isolated from it, pachymic acid (1) and dehydrotumulosic acid (2), were active as inhibitors of phospholipase A2 from snake venom when a polarographic method was used. Dehydrotumulosic acid exhibited an IC50 of 0.845 mM. These two compounds are structurally related to certain triterpenoids from Ganoderma and Schinus that have previously been described as competitive inhibitors of phospholipase A2. These comprise a new group of natural potential antiinflammatory agents due to their interaction with that enzyme.

research product

In vivo activity of pseudoguaianolide sesquiterpene lactones in acute and chronic inflammation.

The pseudoguaianolide sesquiterpene lactones 4-alpha-O-acetyl-pseudoguaian-6beta-olide (1), hymenin (2), ambrosanolide (3), tetraneurin A (4), parthenin (5), hysterin (6) and confertdiolide (7) were evaluated for their ability to affect the inflammation responses induced by different agents. All the compounds showed activity against the 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced mouse ear edema. The ethyl phenylpropiolate (EPP)-induced mouse ear edema was inhibited by compounds 3, 5 and 7. However, when sesquiterpene-lactones were assayed on the arachidonic acid (AA)-induced mouse ear edema, none of them were active. The only sesquiterpene lactone orally active against the paw mouse…

research product

In Vivo Studies on the Anti-Inflammatory Activity of Pachymic and Dehydrotumulosic Acids

Pachymic and dehydrotumulosic acids were studied in different models of acute and chronic inflammation. They proved to be active in most of the methods applied. None of them were active against arachidonic acid-induced ear edema. Dehydrotumulosic acid significantly diminished the mouse ear edema induced by ethyl phenylpropiolate, while pachymic acid was ineffective. When the putative corticoid-like mechanism of both compounds was explored, pachymic acid activity was partially abolished by the glucocorticoid receptor antagonist progesterone, but dehydrotumulosic acid activity was not affected. In vivo experiments demonstrated the inhibition by both principles of the phospholipase A2 (PLA2)-i…

research product

Isolation of two triterpenoids and a biflavanone with anti-Inflammatory activity from Schinus molle fruits.

Three compounds with anti-inflammatory activity were isolated from Schinus molle fruits. Two of the compounds were identified as 3- epi-isomasticadienolalic acid ( 1), isomasticadienonalic acid ( 2) and chamaejasmin ( 3). Triterpenes 1 and 2, and biflavanone 3 were tested on two models of mice paw inflammation: one of acute inflammation, induced by subcutaneous injection of either phospholipase A (2) (PLA (2)) or carrageenan in the paws of mice, and one of chronic inflammation in the form of eczema, provoked by repeated administration of TPA to the ears of mice. On the PLA (2)-induced mouse paw oedema, only 2 was active (30 mg/kg, 66 % inhibition at 60 min), whereas all compounds reduced th…

research product

Essential Oil from Sideritis funkiana

research product

Anti-phospholipase A2 and anti-inflammatory activity of Santolina chamaecyparissus

The activity of the Santolina chamaecyparissus methanol extract was tested against the phospholipase A2 (PLA2)-induced mouse paw edema and in vitro inhibition of PLA2 activity. After fractionation, only the dichloromethane extract was active against the PLA2 in vitro test. In addition, it reduced the edema induced by arachidonic acid, and by 12-O-tetradecanoylphorbol-13-acetate in a multidose test. After chromatography on silicagel and gel filtration on Sephadex, and using an in vitro anti-PLA2 assay-guided process, we have isolated and identified from the dichloromethane extract the flavone nepetin and four sesquiterpenes.

research product

Shikonin promotes intestinal wound healing in vitro via induction of TGF-β release in IEC-18 cells

The intestinal barrier is a complex system with a dynamic structure that is designed for the maintenance of homeostasis in healthy individuals. Ulcerative colitis, one of the main manifestations of inflammatory bowel disease, is characterized by an inadequate and delayed wound healing. Shikonin, the active principle in the root of Lithospermum erythrorhizon, has demonstrated its ability to attenuate dextran sulfate sodium-induced ulcerative colitis in mice. Moreover, the root of L. erythrorhizon has been used in traditional Chinese medicine for treatment of burns, anal ulcers, hemorrhoids and skin wounds. However, the effect of shikonin on intestinal wound healing is unknown. Using an in vi…

research product

On the Occurrence of Caffeoyltartronic Acid and Other Phenolics in Chondrilla juncea

Abstract Caffeoyltartronic acid and other eleven phenolic com pounds were identified in the MeOH extract of Chondrilla juncea: the flavonoids luteolin, luteolin-7-glucoside, luteolin-7-galactosylglucuronide and quercetin-3-galactoside; the phenolic acids protocatechuic, caffeic, chlorogenic, isochlorogenic and isoferulic and the coumarins cichoriin and aesculetin. The taxonomic im plications of these com pounds have been discussed.

research product

Effects of triterpenes on the immune system.

Ethnopharmacological relevance: Triterpenes, which comprise a broad chemical group of active principles, are implicated in the mechanisms of action and pharmacological effects of many medicinal plants used in folk medicine against diseases in which the immune system is implicated. They have been described as anti-inflammatory, antiviral, antimicrobial, and antitumoral agents, as well as being immunomodulator compounds. Several of them are implicated in the resolution of immune diseases, although their effects have not always been clearly correlated. Aim of the review: The aim of this review is to compile relevant data on the mechanisms of action of triterpenes isolated from active ethnomedi…

research product

Intestinal anti-inflammatory activity of ellagic acid in the acute and chronic dextrane sulfate sodium models of mice colitis.

Abstract Ethnopharmacological relevance Pomegranate (Punica granatum L.; Lythraceae) has traditionally been used for the treatment of various inflammatory diseases, including ulcerative colitis (UC). Because its fruits and extracts are rich in ellagitannins, which release ellagic acid when hydrolyzed, consumption of pomegranate products is currently being widely promoted for their potential health effects, including the prevention of inflammatory diseases and cancer. To evaluate the anti-inflammatory effects of ellagic acid on dextran sulfate sodium (DSS)-induced acute and chronic experimental colitis in two different strains of mice and to elucidate its possible mechanisms of action. Mater…

research product

Isolation and identification of the antibacterial compounds from Helichrysum stoechas.

Fractionation of the dicholoromethane extract of the aerial parts of Helichrysum stoechas yielded seven isolates (1-7), which exhibited varying antimicrobial activity against Gram-positive bacteria. Pure compounds 1-3 have been previously reported in the same species and 4 and 5 were identified as italipyrone and plicatipyrone, previously isolated from H. italicum and H. plicatum. The two other isolates are helipyrone (6) and homoarenol (7) mixed with related substances. Compound 6c (4,4'-dihydroxy-5,6,5',6'-tetramethyl-3,3'-methylen-di-pyr-2-one) and 6b helipyrone with one methyl substitution, have not been previously reported in other species.

research product

Shikonin reduces oedema induced by phorbol ester by interfering with IκBα degradation thus inhibiting translocation of NF-κB to the nucleus

Background and purpose In the present paper we studied the effect of shikonin on ear oedema induced by 12-O-tetradecanoylphorbol-13-acetate (TPA), and determined the mechanisms through which shikonin might exert its topical anti-inflammatory action. Experimental approach Acute ear oedema was induced in mice by topical application of TPA. The in vitro assays used macrophages RAW 264.7 cells stimulated with lipopolysaccharide. Cyclooxygenase-2, inducible nitric oxide synthase, protein kinase Calpha, extracellular signal-regulated protein kinase (ERK), phosphorylated ERK (pERK), c-Jun N-terminal kinase (JNK), pJNK, p38, p-p38, p65, p-p65, inhibitor protein of nuclear factor-kappaB (NF-kappaB) …

research product

Inhibition of Trypanosoma cruzi growth by medical plant extracts

This study describes the screening of extracts obtained from 18 plants and two fungi used in the Chinese and Mediterranean traditional medicines on epimastigote forms of Trypanosoma cruzi. The extracts were tested against epimastigote of T. cruzi Bra C15C2 clone in vitro at 27 degrees C and at a concentration of 250 microg/ml in axenic culture. Angelica dahurica, A. pubescens, A. sinensis, Astragalus membranaceus, Coptis chinensis, Haplophyllum hispanicum, Phellodendron amurense, Poria cocos, Ranunculus sceleratus and Scutellaria baicalensis showed significant effects against the parasite with a percentage of growth inhibition between 20 and 100%. C. chinensis and R. sceleratus showed the g…

research product

Anti-inflammatory and antioxidant properties of Helichrysum italicum.

Abstract The anti-inflammatory and antioxidant activities of the aerial part of Helichrysum italicum extracts have been established in various in-vivo and in-vitro experimental models. The results obtained on the acute oedemas induced by 12-O-tetradecanoylphorbol 13-acetate (TPA) and ethyl phenylpropiolate in the mouse ear, by serotonin and phospholipase A2 (PLA2) in the mouse paw, on chronic inflammation induced by repeated application of TPA in the mouse ear and on the delayed-type hypersensitivity induced by sheep red blood cells suggest that said anti-inflammatory activity is due to the effects of compounds expressed via a corticoid-like mechanism. In addition, the antioxidant activity …

research product

Inhibition of pro-inflammatory enzymes by inuviscolide, a sesquiterpene lactone from Inula viscosa

Abstract This work concerns the pharmacological activity of inuviscolide, a sesquiterpenoid from Inula viscosa. It exerts inhibitory effects on elastase, cyclooxygenase 1 and secretory phospholipase A2. Furthermore, it reduces the skin leukocyte infiltration in a murine model of dermatitis induced by repeated application of 12-O-tetradecanoylphorbol 13-acetate.

research product

Dihydrocucurbitacin B, isolated from Cayaponia tayuya, reduces damage in adjuvant-induced arthritis

23,24-Dihydrocucurbitacin B, from the anti-rheumatic plant Cayaponia tayuya, was tested on arthritis induced by adjuvant to corroborate the anti-inflammatory properties of this plant. Arthritis was induced in Lewis rats; the resulting arthritic rats were then treated with dihydrocucurbitacin B (1 mg/kg orally, daily, 1 week). The effect of dihydrocucurbitacin B on the synthesis, release, and activity of pro-inflammatory enzymes (elastase, cyclooxygenase-2, and nitric oxide synthase-2) as well as its effect on different mediators (tumor necrosis factor-alpha and interleukin-1beta) were determined. Dihydrocucurbitacin B modified the evolution of the clinical symptoms, reducing the swelling an…

research product

Anti-inflammatory activity of two cucurbitacins isolated from Cayaponia tayuya roots.

Fractionation of an anti-inflammatory extract from Cayaponia tayuya roots yielded two active compounds, identified as 23,24-dihydrocucurbitacin B (1) and cucurbitacin R (2). Both were evaluated for their anti-inflammatory activity on several experimental models of pain and inflammation. In addition, their cytotoxicity and effects on leukotriene B 4 (LTB 4 ) formation were evaluated in rat polymorphonuclear leukocytes. Both compounds showed activity in the following models: carrageenan-induced mouse paw oedema (1, 4 mg/kg p.o., 46% inhibition at 3 h), phospholipase A 2 -induced mouse paw oedema (2, 3 mg/kg i.p., 61% inhibition at 60 min), serotonin-induced mouse paw oedema (1 and 2, 0.5 mg/k…

research product

A chemotaxonomic survey of Sonchus subgenus Sonchus

Abstract Five species of Sonchus subgenus Sonchus were surveyed for their phenolic constituents. Seven flavonoids were identified: luteolin, luteolin-7-glucoside, apigenin, apigenin-3-glucoside, quercetin, quercetin-3-glucoside and quercetin-3-galactoside; three were phenolic acids; caffeic, chlorogenic and isochlorogenic; and two were coumarins: aesculetin and cichoriin. Their systematic significance for this genus is discussed.

research product

Influence of traditional Chinese anti-inflammatory medicinal plants on leukocyte and platelet functions.

Abstract The enzymes 5-lipoxygenase and elastase are therapeutic targets in dermatological disorders such as psoriasis. Fifteen extracts from traditional Chinese medicinal plants used to treat topical inflammations were screened for their inhibitory effect on lipoxygenase, cyclooxygenase and elastase activity in intact leukocytes and platelets. Astragalus membranaceus, Forsythia suspensa and Poria cocos inhibited 5-lipoxygenase, with IC50 values of 141, 80 and 141 μg mL−1, respectively. The latter two species, along with Angelica dahurica and Angelica pubescens, also inhibited elastase (IC50 values of 80, 123, 68 and 93 μg mL−1, respectively), while A. pubescens, Atractylodes macrocephala, …

research product

Modulation of protein tyrosine nitration and inflammatory mediators by isoprenylhydroquinone glucoside.

The nitration of tyrosine caused by peroxynitrite and other reactive nitrogen species is clearly detrimental for some physiological processes; however, its signalling role is still open to controversy. Among the natural phenolics known for their ability to oppose free tyrosine nitration, isoprenylhydroquinone glucoside is investigated due to its unusual structure, which contains a simple hydroxybenzene alkylated by a hemiterpenoid moiety. This hydroquinone was shown to be an effective inhibitor of peroxynitrite-induced protein tyrosine nitration in 3T3 fibroblasts. When tested on bovine seroalbumin nitration, however, the potency was reduced by half and the effect was almost abolished in th…

research product

Lanostanoids from fungi: a group of potential anticancer compounds.

Lanostanes are a group of tetracyclic triterpenoids derived from lanosterol. They have relevant biological and pharmacological properties, such as their cytotoxic effects via induction of apoptosis. This review compiles the most relevant lanostanoids studied from 2000 to 2011, principally those isolated from Ganoderma lucidum and other related fungi, such as Poria cocos, Laetiporus sulphureus, Inonotus obliquus, Antrodia camphorata, Daedalea dickinsii, and Elfvingia applanata, which have great potential as anticancer agents because of their cytotoxic or apoptotic effects. The compounds were selected on the basis of their proapoptotic mechanisms, through their ability to modify transcription…

research product

Screening of antiinflammatory medicinal plants used in traditional medicine against skin diseases

The antiinflammatory activity of twelve medicinal plants used against skin disorders were tested in different experimental models of topical inflammation and one in vitro inhibitory test against phospholipase A2 (PLA2) from Naja naja venom. Forsythia suspensa was the most active species on the arachidonic acid (AA) topical test. This last species together with Astragalus membranaceus and Ranunculus sceleratus were the most active on the 12-O-tetradecanoylphorbol-13-acetate (TPA) acute ear oedema test. Scrophularia auriculata was the most active on multiple topical applications of TPA and on the oxazolone-induced delayed type hypersensitivity (DTH). Santolina chamaecyparissus was the only sp…

research product

Antioxidant activity of anti-inflammatory plant extracts

The antioxidant properties of twenty medical herbs used in the traditional Mediterranean and Chinese medicine were studied. Extracts from Forsythia suspensa, Helichrysum italicum, Scrophularia auriculata, Inula viscosa, Coptis chinensis, Poria cocos and Scutellaria baicalensis had previously shown anti-inflammatory activity in different experimental models. Using free radical-generating systems H. italicum. I. viscosa and F. suspensa protected against enzymatic and non-enzymatic lipid peroxidation in model membranes and also showed scavenging property on the superoxide radical. All extracts were assayed at a concentration of 100 microg/ml. Most of the extracts were weak scavengers of the hy…

research product

Cucurbitacins as inducers of cell death and a rich source of potential anticancer compounds.

Triterpenes have been reported to induce cell death. One relevant group of this family of compounds is cucurbitacins, which have been studied as inducers of apoptosis in various cancer cell lines. The most significant mechanisms with regard to the apoptotic effects of cucurbitacins are their ability to modify transcriptional activities via nuclear factors or genes and their capability to activate or inhibit pro- or anti-apoptotic proteins. Still, while the majority of studies on these compounds have dealt with their apoptotic effects on cancer cell lines, several research groups have also explored their anti-inflammatory activities. In general, cucurbitacins are considered to be selective i…

research product

An Aqueous Extract of Ilex paraguariensis Reduces Carrageenan-Induced Edema and Inhibits the Expression of Cyclooxygenase-2 and Inducible Nitric Oxide Synthase in Animal Models of Inflammation

Mate (Ilex paraguariensis) is a highly popular herbal beverage in South America due to its high content of caffeine. Its hypolipidemic and antioxidant properties are of increasing interest in the treatment of cardiovascular disorders and for weight control. In the present study, we show for the first time both the local and systemic anti-inflammatory effects of an aqueous extract of mate in three classic in vivo models, namely acute and chronic 12-O-tetradecanoylphorbol 13-acetate-induced mouse ear edema and acute carrageenan-induced mouse paw edema. Caffeine, rutin, chlorogenic acid, 3,5-dicafeoyl quinic acid, and 4,5-dicafeoyl quinic acid, accompanied by a complex mixture of other simple …

research product

Anti-inflammatory profile of dehydrocostic acid, a novel sesquiterpene acid with a pharmacophoric conjugated diene

Sesquiterpene acids are natural products that, in contrast with the thoroughly studied sesquiterpene lactones, have received little pharmacological attention. A good source of this class of compounds is Inula viscosa (Asteraceae), a plant with documented anti-inflammatory effects. The present paper gives the results of our investigations on the biochemical mechanisms involved in the anti-inflammatory activity of one such compound, dehydrocostic acid. The most salient findings were that in vitro dehydrocostic acid inhibits leukotriene B(4) production (IC(50)=22 microM), elastase activity (IC(50)=43 microM) and bee venom phospholipase A(2) activity (IC(50)=17 microM). Furthermore, this sesqui…

research product

Phenolics as GABA-A receptor ligands:an updated review

Natural products can act as potential GABA modulators, avoiding the undesirable effects of traditional pharmacology used for the inhibition of the central nervous system such as benzodiazepines (BZD). Phenolics, especially flavonoids and phlorotannins, have been considered as modulators of the BZD-site of GABAA receptors (GABAARs), with sedative, anxiolytic or anticonvulsant effects. However, the wide chemical structural variability of flavonoids shows their potential action at more than one additional binding site on GABAARs, which may act either negatively, positively, by neutralizing GABAARs, or directly as allosteric agonists. Therefore, the aim of the present review is to compile and d…

research product

Medicinal Plants and Natural Products as Potential Sources for Antiparkinson Drugs

Parkinsonʼs disease is a progressive neurodegenerative dysfunction characterized by the loss of pigmented dopaminergic neurons of the nigrostriatal system with a consequent dopamine decrease. The reduction of dopamine levels produces neuronal damage, depigmentation of the substantia nigra, and the presence of intracellular inclusions in dopaminergic neurons. Treatments for Parkinsonʼs disease aim for improving these motor symptoms by increasing the dopaminergic signal in the striatum with levodopa in combination with enzyme inhibitors or anticholinergic drugs. Nevertheless, natural products can act as neuroprotective agents by reducing the progression of the disease and the inflammatory pro…

research product

A review of some antimicrobial compounds isolated from medicinal plants reported in the literature 1978–1988

This paper reviews the literature on recent antimicrobial plant products (1978–1988) and medicinal plants used for the treatment of infectious diseases. The review includes accounts of extracts, essential oils and other active principles isolated from plants that have been used in folk medicine as antimicrobial agents. The name and part of the plants studied, the spectrum of activity, type of active compounds and methods used are discussed, as are their mechanisms of action.

research product

Protective effect of apocynin in a mouse model of chemically-induced colitis.

Apocynin, a constituent of Picrorhiza kurroa, successfully inhibits NADPH oxidase and shows promise as an anti-inflammatory drug. Now, we report anti-inflammatory effects of apocynin in an experimental colitis model induced by dextran sulfate sodium as well as the effects on the mediators involved in this process. Apocynin reduced the colitis induced in mice by administration of 5 % dextran sulfate sodium during 7 days. Mice were fed a control diet or a diet supplemented with 2 % of apocynin or 2 % of rutin. Sulfasalazine (50 mg/kg, p. o.) was used as a positive control. Treatment with apocynin and rutin ameliorated the course of colonic inflammation with results similar to those of the ref…

research product

Apoptotic activities of Mediterranean plants

Medicinal plants from the Mediterranean region show great potential in the improvement of health and in the prevention of disease. Epidemiological studies indicate that some of these plants reduce the incidence of inflammatory diseases and cancer by inducing programmed cell death, thus arresting proliferation. These medicinal properties are related to the presence of compounds such as phenolics with antioxidant properties or nonphenolic compounds, including essential oils, terpenoids, or saponins. Our aim is to review role of different medicinal plants and phytochemicals in apoptosis and disease prevention and the mechanism of action implicated in these beneficial effects. Sin financiación …

research product

Topical Anti-Inflammatory Lignans from Haplophyllum hispanicum Haplophyllum hispanicum

The present paper reports the results of the methanol extract of Haplophyllum hispanicum Spach on single or repeated local 12-O-tetradecanoylphorbol acetate (TPA) administration and in the oxazolone-induced contact-delayed hypersensitivity mouse ear edemas. Two topical anti-inflammatory aryl naphthalide lignans were isolated from the active fractions of the methanol extract. They were identified by spectroscopic methods, including 13C NMR and heteronuclear multiple bond correlation (HMBC), as diphyllin acetyl apioside and tuberculatin. The former was the most active on acute TPA edema with a ID50 of 0.27 μmol/ear

research product

Anti-inflammatory and antiallergic activity in vivo of lipophilic Isatis tinctoria extracts and tryptanthrin.

The effects of a supercritical CO2 (SFE) extract, a dichloromethane (DCM) extract from Isatis tinctoria leaf and the alkaloidal constituent tryptanthrin were studied in acute and subchronic experimental models of inflammation. The SFE and DCM extracts showed anti-inflammatory activity in the carrageenan-induced acute mouse paw oedema (ED50 values of 78 mg/kg and 165 mg/kg P. O., respectively) and in the acute tetradecanoylphorbol acetate (TPA)-induced mouse ear oedema in oral (62% and 32% oedema reduction at 100 and 125 mg/kg, respectively) and topical application (37% and 33% reduction of oedema at 0.5 mg/ear). In contrast, tryptanthrin showed no significant anti-inflammatory effect. The D…

research product

Effect of selected triterpenoids on chronic dermal inflammation.

The activity of four natural triterpenoids on a 12-O-tetradecanoylphorbol-13-acetate multiple-dose model of skin chronic inflammation was studied. Erythrodiol and ursolic acid were significantly effective. The most important features concerning structure-activity relationship and previous data on the effect of these triterpenoids on other inflammatory conditions are discussed.

research product

New acetophenone glucosides isolated from extracts of Helichrysum italicum with antiinflammatory activity.

Three new acetophenone glucosides (4-6), three known aglycons (1-3), and a benzo-gamma-pyrone glucoside (7) were isolated from the CH(2)Cl(2), EtOAc, and BuOH extracts from the aerial parts of Helichrysum italicum. All the compounds tested showed antiinflammatory activity in a 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced mouse ear edema test, and the ID(50) value of compound 2, the most active compound, was determined.

research product

Chemical Constituents and Pharmacological Properties ofPoria cocos

Poria cocos (Polyporaceae) is a saprophytic fungus that grows in diverse species of Pinus. Its sclerotium, called fu-ling or hoelen, is used in traditional Chinese and Japanese medicine for its diuretic, sedative, and tonic effects. Various studies of this fungus have demonstrated its marked anti-inflammatory activity in different experimental models of acute and chronic inflammation. It is widely used as a constituent of many preparations in Asian medicine, but the number of research papers on its clinical properties is insufficient for establishing its efficacy and safety from a scientific point of view. In this review, we have compiled all the published data concerning the chemistry, pha…

research product

Pharmacological Study of Santolina chamaecyparissus. I. Acute Toxicity, Antiinflammatory and Antiulcer Activity

research product

Anti-arthritic activity of a lipophilic woad (Isatis tinctoria) extract

A dichloromethane extract of Isatis tinctoria was tested in the adjuvant-induced arthritis model in rats. The extract (150 mg/kg p. o.) leads to a significant reduction of paw oedema. Radiographic, histological and clinical assessment confirmed reduced damage of cartilage and signs of inflammatory response in comparison to untreated control. No significant differences were observed in the tissular levels of cyclooxygenases 1 and -2, and of inducible nitric oxide synthase in Isatis treated and untreated animals. High dose treatment with Isatis extract for two weeks did not result in macroscopic lesions of the gastric mucosa.

research product