0000000000020169
AUTHOR
Yu-jie Fu
Aqueous enzymatic process assisted by microwave extraction of oil from yellow horn (Xanthoceras sorbifolia Bunge.) seed kernels and its quality evaluation.
Abstract In this study, aqueous enzymatic process (AEP) assisted by microwave extraction (ME) of oil from yellow horn ( Xanthoceras sorbifolia Bunge.) seed kernel was investigated. Central composite design (CCD) and response surface methodology (RSM) were used to optimise an enzyme cocktail (cellulase, hemicellulase, pectinase) for AEP. The main factors of ME were also studied. A maximal oil extraction yield of 55.8% was achieved under optimal conditions. Moreover, scanning electron microscope (SEM) was applied to characterise the extraction process. Analysing chemical composition of the extracted oil by GC–MS showed that the content of unsaturated fatty acids by this emerging method (91.18…
Negative pressure cavitation extraction and antioxidant activity of genistein and genistin from the roots of pigeon pea [Cajanus cajan (L.) Millsp.]
Abstract A new method—negative pressure cavitation extraction (NPCE) was proposed and investigated for the extraction of the main isoflavonoids, namely genistein and genistin from pigeon pea roots. The effects of extraction time and particle size on the extraction yields were firstly optimized, then a central composite design (CCD) combined with response surface methodology (RSM) was used to study the effects of negative pressure, ethanol concentration and liquid/solid ratio on the extraction yields. The maximum extraction yields of genistein and genistin reached 0.418 and 0.398 mg/g, respectively, under the optimal conditions: extraction time 45 min, particle size 50 mesh, negative pressur…
Euonymus maackii Rupr. Seed oil as a new potential non-edible feedstock for biodiesel
Abstract In this study, Euonymus maackii Seed oil (EMSO) was exploited and evaluated for the first time as a new non-edible oil feedstock for preparation of biodiesel. The EMSO yield was 41.06 ± 2.68 wt%. The fatty acid compositions of EMSO involved palmitoleic acid (2.01%), palmitic acid (14.5%), stearic acid (3.1%), oleic acid (49.8%), linoleic acid (29.3%), 11-Eicosenoic acid (0.1%) and arachidic acid (0.07%). Microwave-assisted transesterification with methanol provided a high conversion yield in short duration under low temperature. The 2.0 wt% of catalyst amount, 10:1 of methanol/oil molar ratio, 40 min of reaction time and 60 °C of temperature were found to be the optimum process condi…
Cajanol, a novel anticancer agent from Pigeonpea [Cajanus cajan (L.) Millsp.] roots, induces apoptosis in human breast cancer cells through a ROS-mediated mitochondrial pathway.
Cajanol (5-hydroxy-3-(4-hydroxy-2-methoxyphenyl)-7-methoxychroman-4-one) is an isoflavanone from Pigeonpea [Cajanus cajan (L.) Millsp.] roots. As the most effective phytoalexin in pigeonpea, the cytotoxic activity of cajanol towards cancer cells has not been report as yet. In the present study, the anticancer activity of cajanol towards MCF-7 human breast cancer cells was investigated. In order to explore the underlying mechanism of cell growth inhibition of cajanol, cell cycle distribution, DNA fragmentation assay and morphological assessment of nuclear change, ROS generation, mitochondrial membrane potential (DeltaPsim) disruption, and expression of caspase-3 and caspase-9, Bax, Bcl-2, PA…
Cryptochlorogenic acid attenuates LPS-induced inflammatory response and oxidative stress via upregulation of the Nrf2/HO-1 signaling pathway in RAW 264.7 macrophages.
Phenolic acids are found in natural plants, such as caffeic acid, rosmarinic acid, and chlorogenic acid. They have long been used as pharmacological actives, owing to their anti-inflammatory and antioxidant activities. Cryptochlorogenic acid (CCGA) is a special isomer of chlorogenic acid; the pharmacological effects and related molecular mechanisms of CCGA have been poorly reported. In the present study, the antioxidant and anti-inflammatory effects of CCGA in RAW 264.7 macrophages and the underlying mechanisms were investigated. The results revealed that CCGA dose-dependently inhibited LPS-induced production of NO, TNF-α, and IL-6 and blocked iNOS, COX-2, TNF-α, and IL-6 expressions. CCGA …
Cajaninstilbene acid (CSA) exerts cytoprotective effects against oxidative stress through the Nrf2-dependent antioxidant pathway.
Cajaninstilbene acid (CSA), an active compound separated from pigeon pea leaves, possesses the highly efficient antioxidant activities. Transcription factor nuclear factor-erythroid 2-related factor 2 (Nrf2) is an important regulator of cellular oxidative stress. This study examined the role of Nrf2 in CSA-mediated antioxidant effects on human hepatocarcinoma (HepG2) cell line. The generation of reactive oxygen species (ROS) upon H2O2 and CSA treatment was lower than that of H2O2 alone. CSA activated Nrf2 as evaluated by Western blotting. A luciferase reporter assay also demonstrated that CSA-activated signaling resulted in the increased transcriptional activity of Nrf2 through binding to t…
Application of integrative cloud point extraction and concentration for the analysis of polyphenols and alkaloids in mulberry leaves
Abstract A simple and efficient method based on cloud point extraction and concentration combined with high performance liquid chromatography was developed for the simultaneous separation and determination of five target compounds (deoxynojirimycin, chlorogenic acid, rutin, isoquercitrin and astragalin) in mulberry leaves samples. Firstly, to obtain a high extraction rate, the ultrasound assisted extraction was developed on acid modified Triton X-114 system. Under the optimal conditions, the total maximum extraction yields of five target compounds reached 20.80 mg/g, which was superior to conventional solvent extraction. After the cloud point extraction and concentration, the HPLC analysis …
Enzymatic water extraction of taxifolin from wood sawdust of Larix gmelini (Rupr.) Rupr. and evaluation of its antioxidant activity
Abstract An enzyme incubation–water extraction (EI–WE) method was developed and optimised for the extraction of the natural antioxidant taxifolin and of the total flavonoids from wood sawdust of Larix gmelini ( Rupr. ) Rupr. A factorial design and a central composite design approach were used for method optimisation. Optimal conditions were 0.5 mg/ml cellulase and 0.5 mg/ml pectinase, a pH of 5.0, a temperature of 32 °C and 18 h incubation time. The flavonoids and taxifolin were extracted in hot water at 50 °C for 30 min, with a solid to liquid ratio of 1:20. Under optimised conditions, the yields of taxifolin and total flavonoids increased from 1.06 ± 0.08 to 1.35 ± 0.04 mg/g and 4.13 ± 0.…
Pinolenic acid ameliorates oleic acid-induced lipogenesis and oxidative stress via AMPK/SIRT1 signaling pathway in HepG2 cells
Pinolenic acid (PLA), a natural compound isolated from pine nut oil, has been reported to exert bioactivity against lipid anabolism. Nonetheless, the underlying mechanisms still poorly elucidated. The aim of this study is to comprehensively demonstrate the effects of PLA on oleic acid (OA)-induced non-alcoholic fatty liver disease (NAFLD) and their relationship with the lipid metabolic regulation. The results demonstrated that treatment with PLA dramatically inhibited lipid accumulation, oxidative stress as well as inflammatory responses induced by oleic acid in HepG2 cells. PLA also obviously decreased the levels of cellular triglyceride (TG), total cholesterol (TC), malondialdehyde (MDA),…
Activity of the antiestrogenic cajanin stilbene acid towards breast cancer
Antiestrogenic therapy is a mainstay for estrogen receptor (ERα)-positive breast cancer. Due to the development of resistance to established antihormones such as tamoxifen, novel compounds are required. The low abundant cajanin stilbene acid (CSA) recently isolated by us from Pigeon Pea (Cajanus cajan) has structural similarities with estrogen. We analyzed the cytotoxic and anticancer activity of CSA in ERα-positive and -negative human breast cancer cells in vitro, in vivo and in silico. CSA exerts anticancer and antiestrogenic activities towards ERα-positive breast cancer, and it showed cytotoxicity towards tamoxifen-resistant MCF-7 cells, implying that CSA may be active against tamoxifen-…
In Vitro Antioxidant and Antimicrobial Activity of Extracts from Morus alba L. Leaves, Stems and Fruits
In this study, the aqueous and ethanolic extracts (leaves, stems and fruits) from Morus alba L., a traditional Chinese medicine, were evaluated for their antioxidant and antimicrobial properties. Ethanolic extracts showed higher contents of both total phenolics and flavonoids than aqueous extracts. The total phenolic content was in the order of: leaf extracts > fruit extracts > stem extracts, whereas the total flavonoids was: leaf extracts > stem extracts > fruit extracts. Using DPPH assays, the concentrations providing 50% inhibition (IC50) values of aqueous extracts from leaves, stems and fruits were 7.11 ± 1.45 mg/ml, 86.78 ± 3.21 mg/ml and 14.38 ± 2.83 mg/ml, respectively, …
Dryofragin, a phloroglucinol derivative, induces apoptosis in human breast cancer MCF-7 cells through ROS-mediated mitochondrial pathway
Dryofragin is a phloroglucinol derivative extracted from Dryopteris fragrans (L.) Schott. In this study, the anticancer activity of dryofragin on human breast cancer MCF-7 cells was investigated. Dryofragin inhibited the growth of MCF-7 cells in a time and concentration-dependent manner. The cell viability was measured using MTT assay. After treatment with dryofragin for 72, 48 and 24 h, the IC₅₀ values were 27.26, 37.51 and 76.10 μM, respectively. Further analyses of DNA fragmentation and Annexin V-PI double-labeling indicated an induction of apoptosis. Dryofragin-treatment MCF-7 cells had a significantly accumulation of reactive oxygen species (ROS), as well as an increased percentage of …
Aspidin PB, a phloroglucinol derivative, induces apoptosis in human hepatocarcinoma HepG2 cells by modulating PI3K/Akt/GSK3β pathway.
Aspidin PB, a phloroglucinol derivative isolated from Dryopteris fragrans (L.) Schott, has been previously reported to exert high biological activities. In the present study, we analyzed the apoptotic mechanisms of aspidin PB on human hepatoma cell line, HepG2. Initially, aspidin PB was shown to inhibit the growth of HepG2 cells in a time and dose-dependent manner. After treatment with aspidin PB for 72 h, 48 h and 24 h using MTT assay, the IC(50) values were 10.59 μM, 20.86 μM and 46.59 μM, respectively. Aspidin PB was capable to induce apoptosis, as measured by mitochondrial membrane potential (ΔΨm), acridine orange (AO) staining and propidium iodide (PI)/annexin V-FITC double staining. T…
Catalytic transesterification of Pistacia chinensis seed oil using HPW immobilized on magnetic composite graphene oxide/cellulose microspheres
Abstract In the present study, magnetic composite graphene oxide/cellulose (GO/CM@Fe3O4) microspheres were prepared as support material, which are cost-efficient, non-toxic and environmental friendly. The microspheres with higher adsorption capacity were further modified using triethylene tetramine (TETA), and H3PW12O40 (HPW) was immobilized to form GO/CM-NH2@Fe3O4-HPW microspheres as heterogeneous catalyst for biodiesel production. The novel heterogeneous catalyst was characterized by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), Brunauer-Emmett-Teller (BET) and X-ray diffractometry (XRD). For the first time, GO/CM-NH2@Fe3O4--HPW was applied in the tr…
Dihydroquercetin (DHQ) induced HO-1 and NQO1 expression against oxidative stress through the Nrf2-dependent antioxidant pathway.
Dihydroquercetin (DHQ) is a well-known antioxidant agent. In the present investigation, we reported for the first time that DHQ stimulates the expression of phase II detoxifying enzymes through the Nrf2-dependent signaling pathway. The IC50 values of DHQ for reduction of 2,2-diphenyl-1-picrylhydrazol (DPPH), reducing power assay, lipid peroxidation assay, and xanthine oxidase inhibition were 5.96, 4.31, 2.03, and 13.24 μM, respectively. DHQ possessed considerable protective activity from oxidative DNA damage. A luciferase reporter assay also demonstrated that DHQ-activated signaling resulted in the increased transcriptional activity of Nrf2 through binding to the ARE (antioxidant response e…
Resin adsorption as a means to enrich rare stilbenes and coumarin from pigeon pea leaves extracts
Abstract In this study, resin adsorption as a means to enrich rare stilbenes cajaninstilbene acid (CSA) and longistyline C (LLC), and coumarin cajanuslactone (CL) from pigeon pea leaves was investigated. Among widely used twenty macroporous adsorption resins, NKA-9 resin presented higher adsorption capacity and desorption ratio in static tests. The adsorption kinetic model fitted better depended on types of compounds and pH values. The experimental adsorption data were better fitted to Langmuir isotherm (R2 0.921–0.991) than Freundlich isotherm (R2 0.753–0.988). In order to optimize the operating parameters for separating CSA, LLC and CL, dynamic adsorption and desorption tests were carried…
Molecular docking and pharmacogenomics of vinca alkaloids and their monomeric precursors, vindoline and catharanthine.
International audience; Vinblastine and vincristine are dimeric indole alkaloids derived from (formerly: ). Their monomeric precursor molecules are vindoline and catharanthine. While vinblastine and vincristine are well-known mitotic spindle poisons, not much is known about vindoline and catharanthine. Vindoline and catharanthine showed weak cytotoxicity, while vinblastine, vincristine, and the semisynthetic vindesine and vinorelbine revealed high cytotoxicity towards cancer cells. This may reflect a general biological principle of poisonous plants. Highly toxic compounds are not only active towards predators, but also towards plant tissues. Hence, plants need mechanisms to protect themselv…
Negative-pressure cavitation extraction of cajaninstilbene acid and pinostrobin from pigeon pea [Cajanus cajan (L.) Millsp.] leaves and evaluation of antioxidant activity
Abstract In this study, an efficient negative-pressure cavitation extraction (NPCE) technique was developed to extract cajaninstilbene acid (CSA) and pinostrobin (PI) from pigeon pea [Cajanus cajan (L.) Millsp.] leaves. The operating parameters were optimised using single-factor experiment and central composite design combined with response surface methodology. Well-fitting models for the extraction of CSA and PI were successfully established. From the economic perspective, the selected operating parameters were: extraction pressure −0.075 MPa, extraction temperature 45 °C, material size 40 mesh, ethanol concentration 80%, extraction time 30 min, liquid/solid ratio 30:1 and 4 extraction cyc…
Variation in contents of main active components and antioxidant activity in leaves of different pigeon pea cultivars during growth.
Pigeon pea is an important and multiuse grain legume crop, and its leaves are a very valuable natural resource. To obtain a high-quality biological resource, it is necessary to choose the excellent cultivar and determine the appropriate harvest time. In this study, the variation in contents of main active components and antioxidant activity in leaves of six pigeon pea cultivars during growth were investigated. The level of each individual active component significantly varied during growth, but with a different pattern, and this variation was different among cultivars. Flavonoid glycosides orientin, vitexin, and apigenin-6,8-di-C-α-L-arabinopyranoside showed two peak values at mid-late and …
Negative pressure cavitation-microwave assisted preparation of extract of Pyrola incarnata Fisch. rich in hyperin, 2'-O-galloylhyperin and chimaphilin and evaluation of its antioxidant activity.
Abstract A novel and effective extraction method, namely negative pressure cavitation-microwave assisted extraction technique (NMAE), was developed for the preparation of extracts of Pyrola incarnata Fisch., which are rich in the main constituents hyperin, 2′-O-galloylhyperin and chimaphilin. Single factor experiments and Box–Behnken design (BBD) were combined with a response surface methodology to examine factors affecting extraction. Maximum extraction yields of hyperin, 2′-O-galloylhyperin and chimaphilin (1.339 ± 0.029, 4.831 ± 0.117 and 0.329 ± 0.011 mg/g, respectively) were achieved under the following optimised conditions: 700 W microwave power, 50 °C extraction temperature, 30:1 mL/…
Enzyme pretreatment and negative pressure cavitation extraction of genistein and apigenin from the roots of pigeon pea [Cajanus cajan (L.) Millsp.] and the evaluation of antioxidant activity
Abstract An enzyme pretreatment and negative-pressure cavitation extraction (E-NPCE) method was investigated for extraction genistein and apigenin from pigeon pea roots. The important parameters involved in E-NPCE process were optimized by single-factor experiments and then critical parameters were investigated by a 2 3 full factorial central composite design (CCD) to optimize extract conditions. Under optimal conditions, the yields of genistein and apigenin were 0.628 mg/g and 0.359 mg/g, which represented an increase of 44.70% and 53.05%, respectively, compared to standard NPCE. Furthermore, from DPPH scavenging activity test the extract of E-NPCE showed better antioxidant activity than t…
Optimization of fermentation parameters with magnetically immobilized Bacillus natto on Ginkgo seeds and evaluation of bioactivity and safety
Abstract In this study, magnetically immobilized Bacillus natto fermentation approach was developed on Ginkgo seeds. Some parameters potentially influencing the fibrinolytic activity of fermented Ginkgo seeds were systematically investigated and optimized by Plackett-Burman and Box-Behnken designs, and the optimum fermentation conditions obtained were 60 mesh particle size, 150 rpm stirring rate, fermentation pH 6.5, 43.0 h fermentation time, 36.4 °C temperature, 16.4 mL/g liquid-solid ratio and 1.0 g/g beads-solid ratio. After fermentation, the satisfactory fibrinolytic activity of Ginkgo seeds was 3175 ± 43 IU/g. The total flavonoid contents were reached to 2.6 ± 0.2 mg rutin equivalent/g…
An effective negative pressure cavitation-microwave assisted extraction for determination of phenolic compounds in P. calliantha H. Andr.
A novel negative pressure and microwave assisted extraction technique (NMAE) was first proposed and applied for extraction of phenolic compounds from pyrola. [C₄MIM]BF₄ aqueous solution was selected as extraction solvent. Optimal extraction conditions were microwave power 700 W, negative pressure -0.07 MPa, temperature 40 °C, liquid-solid ratio 20 : 1, ionic liquid (IL) concentration 0.5 M, extraction time 15 min. The predominance of NMAE was investigated by comparing with microwave-assisted extraction (MAE) and negative pressure cavitation extraction (NPCE) using a first-order kinetics equation. The C∞ values of the target compounds by NMAE were from 0.406 to 5.977 mg g⁻¹ higher than these…
Efficient extraction and preparative separation of four main isoflavonoids from Dalbergia odorifera T. Chen leaves by deep eutectic solvents-based negative pressure cavitation extraction followed by macroporous resin column chromatography
In this study, green and efficient deep eutectic solvent-based negative pressure cavitation-assisted extraction (DES-NPCE) followed by macroporous resin column chromatography was developed to extract and separate four main isoflavonoids, i.e. prunetin, tectorigenin, genistein and biochanin A from Dalbergia odorifera T. Chen leaves. The extraction procedure was optimized systematically by single-factor experiments and a Box-Behnken experimental design combined with response surface methodology. The maximum extraction yields of prunetin, tectorigenin, genistein and biochanin A reached 1.204, 1.057, 0.911 and 2.448mg/g dry weight, respectively. Moreover, the direct enrichment and separation of…
Improvement of resveratrol production from waste residue of grape seed by biotransformation of edible immobilized Aspergillus oryzae cells and negative pressure cavitation bioreactor using biphasic ionic liquid aqueous system pretreatment
Abstract A biotransformation method of producing resveratrol with immobilized Aspergillus oryzae negative pressure cavitation bioreactor (ICNPCB) with biphasic ionic liquid aqueous system pretreatment was investigated. Subsequently, the biotransformation conditions were optimized for the resveratrol production under types of ILs [C4MIM]Br, concentration of ILs 0.75 M, temperature 31 °C, ratios of solid to liquid 1:15 (mg/L), time 60 h and pH 6.0, the yield of resveratrol reached 224.61 ± 0.35 μg/g, which increased 4.36-fold to that of untreated one. The conversion rate of piceid reached 85.21%. The residual activity of immobilized microorganism was 82.26% after used for 15 runs. The develop…
Enhanced extraction of astragalosides from Radix Astragali by negative pressure cavitation-accelerated enzyme pretreatment.
The optimal conditions for extraction of astragalosides III and IV (AGs III and IV) in Radix Astragali by negative pressure cavitation-accelerated enzyme pretreatment were studied on the basis of a Box-Behnken design and response surface methodology. Experimental results showed that negative pressure, amount of enzyme and incubation temperature were the main factors governing the enzyme pretreatment of Radix Astragali. The optimum parameters were obtained as follows: negative pressure -0.08 Mpa, amount of enzyme 1.48% (w/w of materials) and incubation temperature 45 degrees C. Under the optimal conditions, the maximal extraction yields of AGs III and IV were 0.103 and 0.325 mg/g, which were…
Cytochrome P450 reaction phenotyping and inhibition and induction studies of pinostrobin in human liver microsomes and hepatocytes
Pinostrobin (PI, 5-hydroxy-7-methoxyflavanone) is a natural flavonoid known for its rich pharmacological activities. The objective of this study was to identify the human liver cytochrome P450 (CYP450) isoenzymes involved in the metabolism of PI. A single hydoxylated metabolite was obtained from PI after an incubation with pooled human liver microsomes (HLMs). The relative contributions of different CYP450s were evaluated using CYP450-selective inhibitors in HLMs and recombinant human CYP450 enzymes, and the results revealed the major involvement of CYP1A2, CYP2C9 and CYP2E1 in PI metabolism. We also evaluated the ability of PI to inhibit and induce human cytochrome P450 enzymes in vitro. H…
Enhanced extraction of isoflavonoids from Radix Astragali by incubation pretreatment combined with negative pressure cavitation and its antioxidant activity
Abstract Incubation pretreatment with the function of endogenous enzyme combined with negative-pressure cavitation extraction (IP-NPCE) was established to extract calycosin and formononetin from Radix Astragali. Significant factors involved in the process were selected using Plackett–Burman factorial design (PBD) and then were optimized by central composite design (CCD). The optimum experimental conditions were incubation at 35 °C, 60 min, pH 4.0 and extraction at negative pressure − 0.080 MPa, ethanol concentration 60%, 60 mesh, 30 min, solid-to-liquid ratio 1:25 and two cycles. Under the optimal conditions, the extraction yields of calycosin and formononetin were 0.650 ± 0.015 and 0.307 ±…
Supercritical carbon dioxide extraction of seed oil from yellow horn (Xanthoceras sorbifolia Bunge.) and its anti-oxidant activity
Supercritical fluid carbon dioxide (SF-CO(2)) extraction (SFE) of seed oil from yellow horn and its anti-oxidant activity were investigated. The effects of CO(2) flow rate and particle size were firstly optimized, and a central composite design (CCD) combined with response surface methodology was used to study the effects of extraction pressure, temperature and time on the extraction yields. A maximal extraction yield of 61.28% was achieved under optimal conditions of extraction pressure 30 MPa at 45.68 degrees C, 2.08 h and CO(2) flow rate 12 kg/h with 0.5mm particle size. By analyzing the chemical composition of the seed oil, we found that the content of unsaturated fatty acids was approx…
UV-Induced Changes of Active Components and Antioxidant Activity in Postharvest Pigeon Pea [Cajanus cajan (L.) Millsp.] Leaves
In this study, the effect of UV irradiation (UV-A, UV-B, and UV-C) on phytochemicals, total phenolics, and antioxidant activity of postharvest pigeon pea leaves was evaluated. The response of pigeon pea leaves to UV irradiation was phytochemical specific. UV-B and UV-C induced higher levels of phytochemicals, total phenolics, and antioxidant activity in pigeon pea leaves compared with UV-A. Furthermore, UV-B irradiation proved to possess a long-lasting effect on the levels of phenolics and antioxidant activity. After adapting for 48 h at 4 °C following 4 h UV-B irradiation, total phenolics and antioxidant activity were approximately 1.5-fold and 2.2-fold increased from 39.4 mg GAE/g DM and …
Antioxidant properties, superoxide dismutase and glutathione reductase activities in HepG2 cells with a fungal endophyte producing apigenin from pigeon pea [Cajanus cajan (L.) Millsp.]
Abstract A fungal endophyte MD89 with obvious antioxidant activities was isolated from pigeon pea and identified as Chaetomium globosum by ITS sequence. Different fractions from MD89 culture were compared and evaluated by total phenol (TP) content, total flavonoid (TFL) content, DPPH radical scavenging, reducing power and lipid peroxidation assays, respectively. Results showed that EtOAc extracts had high content of TP and TFL, and strong antioxidant activities (IC 50 value was 6.87, 15.19, 16.78 μg/mL, respectively). Furthermore, the EtOAc extracts were analyzed by LC–MS/MS and a good antioxidant compound, apigenin, was found. The activities of superoxide dismutase (SOD) and glutathione re…
2′-O-Galloylhyperin Isolated From Pyrola incarnata Fisch. Attenuates LPS-Induced Inflammatory Response by Activation of SIRT1/Nrf2 and Inhibition of the NF-κB Pathways in Vitro and Vivo
2'-O-galloylhyperin, a major compound of Pyrola incarnata Fisch., possesses a variety of biological and pharmacological activities, including anti-oxidative and anti-inflammatory activities. Nevertheless, the underlying molecular mechanisms of 2'-O-GH in microbial infection and sepsis are not clear. In this study, we investigated the anti-inflammatory effects of 2'-O-GH. We found that 2'-O-GH significantly reduced the production of TNF-α, IL-6, and nitric oxide (NO), suppressed the expression levels of iNOS, blocked the translocation of NF-κB from the cytosol to nucleus, and decreased the MAPK activation in LPS-activated RAW 264.7 cells. 2'-O-GH also enhanced the nuclear translocation of Nr…
Negative-pressure cavitation coupled with aqueous two-phase extraction and enrichment of flavonoids and stilbenes from the pigeon pea leaves and the evaluation of antioxidant activities
Abstract An efficient extraction method, negative-pressure cavitation coupled with aqueous two-phase extraction (NPC-ATPE), was developed to simultaneously extract and enrich flavonoids and stilbenes from pigeon pea leaves. The main bioactive compounds, cajaninstilbene acid (CSA), longistyline C (LLC), pinostrobin (PI) and pinostrobin chalcone (PIC) were chosen as target compounds. The extraction conditions were optimized using central composite design combined with response surface methodology. The optimized conditions were: concentration of (NH 4 ) 2 SO 4 21% (w/w), concentration of ethanol 23% (w/w) and temperature 30 °C, negative pressure −0.06 MPa, extraction time 30 min and the liquid…
Synthesis and Anti-Tumor Activity of Novel Aminomethylated Derivatives of Isoliquiritigenin
A series of new aminomethylated derivatives of isoliquiritigenin was synthesized. The structures of the compounds were confirmed by IR, MS, NMR, 13C-NMR and elemental analyses. Cytotoxic activities of these derivatives towards the human prostatic cell line PC-3, human mammary cancer cell line MCF-7 and human oophoroma cell line HO-8910 in vitro were tested. The IC50 values showed cytotoxic activities of some of these new derivatives were relatively strong. Furthermore, tumor growth inhibition in vivo of aminomethylated derivatives of isoliquiritigenin 15 was superior to that of isoliquritigenin and reached inhibition rates of 71.68%. The detailed synthesis, spectroscopic data, biological an…
Cell cycle arrest and induction of apoptosis by cajanin stilbene acid from Cajanus cajan in breast cancer cells
Abstract Background: The low abundant cajanin stilbene acid (CSA) from Pigeon Pea ( Cajanus cajan ) has been shown to kill estrogen receptor α positive cancer cells in vitro and in vivo . Downstream effects such as cell cycle and apoptosis-related mechanisms have not been analyzed yet. Material and methods: We analyzed the activity of CSA by means of flow cytometry (cell cycle distribution, mitochondrial membrane potential, MMP), confocal laser scanning microscopy (MMP), DNA fragmentation assay (apoptosis), Western blotting (Bax and Bcl-2 expression, caspase-3 activation) as well as mRNA microarray hybridization and Ingenuity pathway analysis. Results: CSA induced G2/M arrest and apoptosis …
Preparation and antioxidant activity of Radix Astragali residues extracts rich in calycosin and formononetin
Abstract Radix Astragali is considered an excellent source of Traditional Chinese Medicine and a kind of famous restorative food. To make full usage of Radix Astragali, calycosin and formononetin were enriched through various macroporous resins from its residues, HPD500 resin, compared with other resins, offered the best effectiveness for the enrichment and separation of compounds. 35 °C was selected for its highest adoption capacity during static adsorption process, which can be obtained from adsorption isotherms. And then dynamic adsorption and desorption tests were carried out to optimize the operating parameters. After one run treatment with HPD500 resin, the contents of calycosin and f…
Activity investigation of pinostrobin towards herpes simplex virus-1 as determined by atomic force microscopy
In the present study, the antiviral activity of pinostrobin towards herpes simplex virus-1 (HSV-1) was investigated by MTT assay and atomic force microscopy. Pinostrobin can inhibit HSV-1 replication with 50% effective concentration (EC(50)) of 22.71 ± 1.72 μg/ml. MTT assay showed HSV-1 was significantly inhibited when pretreated with pinostrobin, with the inhibition of 85.69 ± 2.59%. Significant changes in morphology and size of HSV-1 were observed by atomic force microscopy (AFM) in response to pinostrobin treatment. AFM topography and phase images showed that with increasing time, the envelope was shedded and damaged, finally leading to virus inactivation. With increasing concentration, …
Negative pressure cavitation accelerated processing for extraction of main bioactive flavonoids from Radix Scutellariae
Abstract To enhance the extraction efficiency and reduce the energy consumption, an emerging technology named negative pressure cavitation extraction (NPCE) has been shown to be a feasible option for the extraction of bioactive compounds in agricultural crops and medicinal plants. Meanwhile, it can be applied at the pilot scale as a manufacturing process for edible and medicinal plants. Currently, NPCE was proposed for extraction of baicalin, wogonoside, baicalein and wogonin from Radix Scutellariae on the basis of a central composite design (CCD) and response surface methodology (RSM). With proper optimization (80 mesh of particle size, 40 mL/g of liquid/solid ratio, 75% aqueous ethanol as…
Plasma pharmacokinetics and tissue distribution study of cajaninstilbene acid in rats by liquid chromatography with tandem mass spectrometry
Cajaninstilbene acid (CSA; 3-hydroxy-4-prenyl-5-methoxystilbene-2-carboxylic acid) is a major active constituent of pigeonpea leaves, has been proven to be effective in clinical treatment of diabetes, hepatitis, measles and dysentery. A rapid and sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) method was developed and validated for the determination of CSA in rat plasma and various tissues (brain, heart, lung, liver, spleen, small intestine and kidney) of rat for the first time. Rat plasma and tissue distribution pre-treated by protein precipitation with acetoacetate was analyzed using LC-MS/MS with an electrospray ionization (ESI) interface, and isoliquiritigenin was us…
Efficient Production of Isoflavonoids by Astragalus membranaceus Hairy Root Cultures and Evaluation of Antioxidant Activities of Extracts
In this study, Astragalus membranaceus hairy root cultures (AMHRCs) were established as an attractive alternative source for the efficient production of isoflavonoids (IF). A. membranaceus hairy root line II was screened as the most efficient line and was confirmed by PCR amplification of rolB, rolC and aux1 genes. Culture parameters of AMHRCs were systematically optimized, and five main IF constituents were quali-quantitatively determined by LC-MS/MS. Under optimal conditions, the total IF accumulation of 34 day old AMHRCs was 234.77 μg/g dry weight (DW). This yield was significantly higher compared to that of 3 year old field grown roots (187.38 μg/g DW). Additionally, in vitro antioxidan…
In vitro antioxidant properties, DNA damage protective activity, and xanthine oxidase inhibitory effect of cajaninstilbene acid, a stilbene compound derived from pigeon pea [Cajanus cajan (L.) Millsp.] leaves.
The antioxidant properties, DNA damage protective activities, and xanthine oxidase (XOD) inhibitory effect of cajaninstilbene acid (CSA) derived from pigeon pea leaves were studied in the present work. Compared with resveratrol, CSA showed stronger antioxidant properties, DNA damage protective activity, and XOD inhibition activity. The IC(50) values of CSA for superoxide radical scavenging, hydroxyl radical scavenging, nitric oxide scavenging, reducing power, lipid peroxidation, and XOD inhibition were 19.03, 6.36, 39.65, 20.41, 20.58, and 3.62 μM, respectively. CSA possessed good protective activity from oxidative DNA damage. Furthermore, molecular docking indicated that CSA was more poten…
2′O-galloylhyperin attenuates LPS-induced acute lung injury via up-regulation antioxidation and inhibition of inflammatory responses in vivo
2'O-galloylhyperin, an active flavonol glycoside compound with remarkable anti-immune activity, was isolated from Pyrola [P. incarnata Fisch.]. However, the evidence of anti-inflammatory activity in pulmonary diseases was still not convincing. The aim of the present study was (1) to investigate the effect of 2'O-galloylhyperin on LPS-induced acute lung injury in mice, and (2) to identify the mechanisms of attenuation of inflammatory responses. The results demonstrated that 2'O-galloylhyperin significantly reduced LPS-induced inflammation damage in a dose-dependent manner. After LPS challenge, treatment with 2'O-galloylhyperin reduced the production of pro-inflammatory cytokines and chemokin…
Cytotoxicity of natural products and derivatives toward MCF-7 cell monolayers and cancer stem-like mammospheres
Abstract Although cancer stem-like cells (CSCs) are rare, they can enter a non-proliferative or dormant state and resist therapy. Furthermore, quiescent CSCs are responsible for metastases that can appear after curative surgical treatment of a primary tumor. Because of drug resistance of CSCs, the development of novel therapies is urgently required that specifically target CSCs. Purpose The aim of the present study was to investigate the potential of a panel of natural products and derivatives to inhibit CSC-enriched mammospheres of MCF-7 breast cancer cells. Methods CD44high/CD24low cells were identified by flow cytometry and maintained as mammospheres. As a control, we used two clinically…
Free radical scavenging capability, antioxidant activity and chemical constituents of Pyrola incarnata Fisch. leaves
Abstract In the present study, the crude extract and its four fractions of petroleum ether, ethyl acetate, n-butanol, water from Pyrola incarnata Fisch. leaves were prepared and their antioxidant activities were investigated by using four antioxidant assays in vitro. The ethyl acetate fraction showed remarkably strong antioxidant activities on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, ABTS radical scavenging, reducing power and β-carotene-linoleic acid bleaching, which were almost comparable to capacities of the positive controls (VC and BHT). The ethyl acetate fraction had the highest total phenolic and total flavonoid contents. Furthermore, Pearson correlation analysis was …