Search results for "flavonoids"

Natural products as inhibitors of recombinant cathepsin L of Leishmania mexicana.

2015

Cysteine proteinases (cathepsins) from Leishmania spp. are promising molecular targets against leishmaniasis. Leishmania mexicana cathepsin L is essential in the parasite life cycle and a pivotal in virulence factor in mammals. Natural products that have been shown to display antileishmanial activity were screened as part of our ongoing efforts to design inhibitors against the L. mexicana cathepsin L-like rCPB2.8. Among them, agathisflavone (1), tetrahydrorobustaflavone (2), 3-oxo-urs-12-en-28-oic acid (3), and quercetin (4) showed significant inhibitory activity on rCPB2.8 with IC50 values ranging from 0.43 to 18.03 µM. The mechanisms of inhibition for compounds 1–3, which showed Ki values…

New neuroprotective effect of lemon integropectin on neuronal cellular model

2021

Lemon IntegroPectin obtained via hydrodynamic cavitation of organic lemon processing waste in water shows significant neuroprotective activity in vitro, as first reported in this study investigating the effects of both lemon IntegroPectin and commercial citrus pectin on cell viability, cell morphology, reactive oxygen species (ROS) production, and mitochondria perturbation induced by treatment of neuronal SH-SY5Y human cells with H2O2. Mediated by ROS, including H2O2 and its derivatives, oxidative stress alters numerous cellular processes, such as mitochondrial regulation and cell signaling, propagating cellular injury that leads to incurable neurodegenerative diseases. These results, and t…

Synthesis and pharmacological evaluation of 2'-hydroxychalcones and flavones as inhibitors of inflammatory mediators generation.

1995

2'-Hydroxy-3,4-dimethoxy-3',4'-dimethylchalcone (3a), 2'-hydroxy-3',4',3,4-tetramethoxychalcone (3b), and their corresponding flavones, 3',4'-dimethoxy-7,8-dimethylflavone (4a) and 3',4',7,8-tetramethoxyflavone (4b), were prepared from 3,4-dimethoxycinnamic acid and the respective phenol. The four compounds inhibited enzymic lipid peroxidation and showed weak peroxyl scavenging activity. They also reduced LTB 4 release from human neutrophils stimulated by A23187. The chalcone 3b was the only compound able to inhibit in a concentration-dependent way, synovial human recombinant phospholipase A 2 activity, human platelet TXB 2 generation, and human neutrophil degranulation. This chalcone exert…

Cissampeloflavone, a chalcone-flavone dimer from Cissampelos pareira

2003

From the aerial parts of Cissampelos pareira L. (Menispermaceae), a chalcone-flavone dimer has been isolated which, mainly from NMR spectroscopic and MS data, was proved to be 2-(4-hydroxy-3-methoxyphenyl)-7-(4-methoxyphenyl)-6-(2-hydroxy-4,6-dimethoxybenzoyl)-furano[3,2-g]benzopyran-4-one. This has been assigned the trivial name cissampeloflavone. The compound has good activity against Trypanosoma cruzi and T. brucei rhodesiense and has a low toxicity to the human KB cell line.

Cytotoxicity of two naturally occurring flavonoids (dorsmanin F and poinsettifolin B) towards multi-factorial drug-resistant cancer cells.

2015

Abstract Introduction The expression of diverse resistance mechanisms in cancer cells is one of the major barriers to successful cancer chemotherapy. Methods In the present study, we assessed the cytotoxicity of two naturally occurring flavonoids dorsmanin F ( 1 , a flavanone) and poinsettifolin B ( 2 , a chalcone) against 9 drug-sensitive and multidrug-resistant (MDR) cancer cell lines. The resazurin reduction assay was used to evaluate the cytotoxicity of these compounds, whilst caspase-Glo assay was used to detect caspase activation. Cell cycle, mitochondrial membrane potential (MMP) and levels of reactive oxygen species (ROS) were all analysed via flow cytometry. Results Compounds 1 and…

Cytotoxicity and modes of action of 4'-hydroxy-2',6'-dimethoxychalcone and other flavonoids toward drug-sensitive and multidrug-resistant cancer cell…

2014

Abstract Introduction Resistance of cancer to chemotherapy is a main cause in treatment failure. Naturally occurring chalcones possess a wide range of biological activities including anti-cancer effects. In this work, we evaluated the antiproliferative activity of three chalcones [4′-hydroxy-2′,6′-dimethoxychalcone ( 1 ), cardamomin ( 2 ), 2′,4′-dihydroxy-3′,6′-dimethoxychalcone ( 3 )], and four flavanones [( S )-(–)-pinostrobin ( 4 ), ( S )-(–)-onysilin ( 5 ) and alpinetin ( 6 )] toward nine cancer cell lines amongst which were multidrug resistant (MDR) types. Methods The resazurin reduction assay was used to detect the antiproliferative activity of the studied samples whilst flow cytometr…

Hypolaetin-8-O-Glucoside, An Anti-inflammatory Flavonoid from Sideritis mugronensis.

1985

The Orange Peel: An Outstanding Source of Chemical Resources

2021

Citrus sinensis (L.) Osbeck is a very common cultivar belonging to the Rutaceae family. It is largely diffused in several areas of the world characterized by mild to warm climate conditions. Its abundant worldwide production (up to 107 Tons. per year) and consumption both as the edible part of the fruit and as several types of derivative products imply the production of a huge amount of waste, such as the fruit pomace. Several ways of recycling this material have been developed in recent years: employment as fertilizer, fodder ingredient, and even cloth material. However, the chemical added value of Citrus sinensis peel has been underestimated despite the diversified and significant content…

Secondary metabolites from the aerial parts of Cytisus villosus Pourr

2017

Phytochemical investigation of the aerial parts of Cytisus villosus Pourr. resulted in the isolation and characterization of a new isoflavan, (3S, 4S)-2′,4′-dihydroxy-3′-methoxy-6,7-methylenedioxyisoflavan- 4-ol (1), and a new monoterpene, (4R,6S)-4-hydroxy-2,2,6-trimethyl-9-oxabicyclo [4.2.1] non-1(8)-en-7-one (2), together with four known flavonoids: geinstein (3), chrysin (4), chrysin -7-O-β-D-glucopyranoside (5) and 2″-O-α-L-rhamnosylorientin (6). The structures of the new compounds were elucidated on the basis of extensive spectroscopic analysis, including 1D, 2D NMR ((1)H, (13)C, COSY, TOCSY, HMBC and HSQC) and HRESIMS. The absolute configurations of 1 and 2 were established by the co…

Influence of orange cultivar and mandarin postharvest storage on polyphenols, ascorbic acid and antioxidant activity during gastrointestinal digestio…

2017

Polyphenols, ascorbic acid content and antioxidant activity of two sweet oranges (Navel-N and Cara Cara-CC) and mandarin (Clementine-M) as well as their bioaccessibilities were evaluated in pulps and compared to those in fresh juice. Thus, pulps of oranges and mandarins displayed higher hesperidin (HES), narirutin (NAR), total flavonoids (TF), total phenols (TP) and antioxidant activity (AAC) than their corresponding juices. Also, CC products presented higher bioactive compounds content than N ones. Bioaccessibility of bioactive compounds and AAC were higher in pulps of both oranges and mandarin than in their corresponding juices. Oranges (N and CC) pulps and juices presented higher bioacce…