Study on the effect and mechanism of taxifolin on ameliorating cisplatin-induced acute kidney injury in mice through peroxisome proliferator-activated receptor γ coactivator-1α-mediated antioxidant pathway / 中华肾脏病杂志

Objective:To explore the effect and mechanism of taxifolin (TAX) on ameliorating cisplatin-induced renal oxidative damage.Methods:(1) Forty male C57BL/6 mice were divided into 4 groups: control group ( n=10), TAX group ( n=10), cisplatin group ( n=10) and cisplatin+TAX group ( n=10). The weight of mice in each group was measured. The level of serum creatinine (Scr) and blood urea nitrogen (BUN) was analyzed. Kidney histopathological change in mice was analyzed by HE staining. The pro-inflammatory cytokines levels of interleukin-6 (IL-6) and tumor necrosis factor alpha (TNF-α) were measured by enzyme linked immunosorbent assay. The levels of reactive oxygen species (ROS), malondialdehyde (MDA), superoxide dismutase (SOD), catalase (CAT) and glutathione (GSH) were measured by multifunctional microplate reader. The expression of inflammatory factors, antioxidant genes, and peroxisome proliferator-activated receptor γ coactivator-1α ( PGC- 1) mRNA were measured by real-time PCR. Evaluation of mitochondrial function by measuring ATP level and mtDNA content. Determination of AMP-activated protein kinase (AMPK) and phosphorylated AMPK protein expression by Western blotting. (2) Evaluate the effect of taxifolin on chemotherapy of cisplatin by establishing Lewis lung cancer transplantation tumor C57BL/6 mice model. Results:Compared with the control group, the weight of the mice in the TAX group was not significantly reduced ( P>0.05), and there was no obvious kidney damage ( P>0.05), indicating that oral TAX had good safety. Compared with the cisplatin group, TAX could significantly delay cisplatin-induced the weight loss of mice, reduce the levels of Scr and BUN, and alleviate the pathological changes of kidney tissue (all P<0.05). TAX could reduce the levels of serum inflammatory factors IL-6 and TNF-α and the expression of renal inflammatory factors IL- 6, TNF- α and IL- 1β mRNA induced by cisplatin in mice (all P<0.05). TAX could significantly reduce the levels of ROS and MDA, and increase the activities of SOD, CAT and GSH in cisplatin-induced acute kidney injury mice (all P<0.01). Meanwhile, TAX could up-regulate the mRNA expression of UCP2, SOD2, CAT antioxidant genes and PGC- 1α in the kidneys of mice with acute kidney injury induced by cisplatin, and increase the levels of ATP and mtDNA in cisplatin-induced acute kidney injury mice (all P<0.01). Western blotting results showed that TAX significantly promoted the expression of phosphorylated AMPK protein in cisplatin-induced acute kidney injury mice ( P<0.01). In addition, through the establishment of Lewis lung cancer transplantation tumor C57BL/6 mice model, it was found that TAX had no significant effect on the anti-tumor efficacy of cisplatin. Conclusions:TAX can ameliorate cisplatin-induced renal oxidative damage, and its mechanism may be related to the activation of AMPK/PGC-1α pathway.

Taxifolin attenuates inflammation via suppressing MAPK signal pathway in vitro and in silico analysis / 中草药·英文版

Objective: Taxifolin is a natural flavonoid compound that can be isolated from onions, grapes, oranges and grapefruit. It also acts as a medicine food homology with extraordinary antioxidant and anti-inflammatory activity. This study aims to explain the protective effects and potential mechanisms of taxifolin against inflammatory reaction. Methods: Levels of interleukin (IL)-6, IL-1β and intracellular reactive oxygen species (ROS) were assessed in different time after the treatment of taxifolin in RAW264.7 cells induced by lipopolysaccharide (LPS). Subsequently, the mRNA and protein levels of inducible nitric oxide synthase (iNOS), vascular endothelial growth factor (VEGF), cyclooxygenase (COX)-2, tumor necrosis factor (TNF)-α and the phosphorylation expression levels of the MAPK signal pathway were also evaluated. A silico analysis was used to explain the binding situation for the investigation of taxifolin and MAPK signal pathway. And then MAPK inhibitors were used to reveal the expression level of iNOS, VEGF, COX-2 and TNF-α in RAW264.7 cells. Results: It was demonstrated that cell inflammatory damage induced by LPS was significantly alleviated after the treatment of taxifolin. Then, the mRNA and protein levels of iNOS, VEGF, COX-2 and TNF-α were reduced and the phosphorylation expression levels of the MAPK signal pathway were down-regulated remarkably as well. In silico analysis, taxifolin could form a relatively stable combination with MAPK signal pathway. MAPK inhibitors showed increasing or decreasing effect in the mRNA levels of iNOS, VEGF, COX-2 and TNF-α, which suggesting that taxifolin down-regulated iNOS, VEGF, COX-2 and TNF-α expressions were not entirely through the MAPK pathway. Conclusion: This finding demonstrated that taxifolin improved the inflammatory responses that partly involved in the phosphorylation expression level of MAPK signal pathway in RAW264.7 cells exposed to acute stress.

Effect of taxifolin on methotrexate-induced oxidative and inflammatory oral mucositis in rats: biochemical and histopathological evaluation

Abstract The role of oxidative stress, as well as inflammation in the pathogenesis of methotrexate (MTX)-induced oral mucositis, is a known fact. The anti-inflammatory, antitumor, antimicrobial, and antioxidant properties of taxifolin—the effect we tested against MTX-induced oral mucosal damage—are well known. Objective Evaluating biochemically and histopathologically the effects of taxifolin on methotrexate-induced oral mucosal damage in rats. Methodology In the taxifolin+MTX (TMTX) group, 50 mg/kg taxifolin was orally administered to rats by gavage. In the MTX and healthy (HG) groups, normal saline was applied to rats as solvent by the same method. One hour after administration of taxifolin and solvent, 5 mg/kg MTX was orally administered to rats in the MTX and TMTX groups. Taxifolin and methotrexate were administered once a day for 30 days. Macroscopic, biochemical, and histopathological evaluations were performed on the inner cheek and tongue tissues of rats. These parts were removed after rats were killed with a high-dose anesthesia. Results Taxifolin with MTX prevented the increase in oxidant and pro-inflammatory parameters, such as malondialdehyde (MDA), tumor necrosis factor alpha (TNF-α), interleukin 1 beta (IL-1β), interleukin 6 (IL-6), on the inner cheek and tongue tissues of rats. Moreover, taxifolin antagonized the decrease in total glutathione (tGSH). Taxifolin decreased MTX-induced histopathological damage. Conclusion These findings suggest that taxifolin may be useful to treat MTX-associated oral mucositis.

Quality standards of Gleditsiae Spina and its decoction pieces / 中国中药杂志

In view of the current inadequate standards for Gleditsiae Spina in the Chinese Pharmacopoeia, this study put forward some new items of the quality standards of Gleditsiae Spina. Thin-layer chromatography(TLC) was performed for identification with the reference substance of taxifolin and the reference material of Gleditsiae Spina as the control. According to the general principles of the Chinese Pharmacopoeia(2020 edition, Vol. 4), the moisture, total ash content, and alcohol-soluble extract of medicinal materials and decoction pieces of Gleditsiae Spina were determined. The content determination method for medicinal materials and decoction pieces of Gleditsiae Spina was established using high-performance liquid chromatography(HPLC), with taxifolin as the quality control index. Based on the determination results of 30 batches of samples of Gleditsiae Spina from different habitats, the draft quality standards of Gleditsiae Spina were developed, which provided suggestions for the revision of the quality standards of Gleditsiae Spina in the Chinese Pharmacopoeia.

Mechanism of Wuling Powder in treatment of chronic heart failure based on network pharmacology / 中草药

Objective: To explore the mechanism of Wuling Powder in the treatment of chronic heart failure (CHF) based on network pharmacology. Methods: Traditional Chinese Medicine Systems Pharmacology Database (TCMSP) and literature mining were used to search the chemical components and targets of Wuling Powder, and a single drug-active ingredients-target network was established. The related targets of chronic heart failure were collected through Genecards and OMIM databases, the network model of active components-CHF-targets was constructed and analyzed by Cytoscape 3.7.1 software. The protein-protein interaction (PPI) network was constructed by STRING database platform, and the gene oesthetics (GO) function annotation and Kyoto Encyclopedin of Genes and Genomes (KEGG) signal pathway enrichment analysis were performed by DAVID online tools. The molecular docking was performed using Surflex software. Results: Fifty components, 29 potential targets, 8 243 targets related to chronic heart failure, and 27 targets of Wuling Powder-CHF were obtained. The network analysis results showed that the key targets of Wuling Powder in the treatment of chronic heart failure included CASP3, RELA, AR, ESR1, CHRM1 and CASP8, etc. Biological processes mainly involved signal transduction, nervous system development, transcription initiation from RNA polymerase II promoter in response to estradiol, synaptic transmission, cholinergic synaptic transmission, etc. KEGG enrichment involved neuroactive ligand-receptor interaction, PI3K-Akt signaling pathway, cholinergic synapse, etc. The molecular docking results showed that (+)-catechin, taxifolin and other key compounds in Wuling Powder had better binding ability with key targets such as CASP8, CHRM1, and NR3C1. Conclusion: The material basis and mechanism of Wuling Powder in the treatment of chronic heart failure were revealed based on network pharmacology, which provided a certain theoretical basis for the clinical application of Wuling Powder.

Identification of flavonoids 3-hydroxylase from Silybum marianum (L.) Gaertn and its application in enhanced production of taxifolin / 生物工程学报

(2S)-taxifolin is an important flavonoid that has anti-inflammatory and anti-oxidation effects. It is widely used in pharmaceutical and nutraceutical industries. Flavone 3-hydroxylase (F3H) can catalyze the synthesis of (2S)-taxifolin and other 3-hydroxylated flavonoids from (2S)-eriodictyol. Due to the low catalytic efficiency of F3H, the titer of many 3-hydroxyflavones, such as taxifolin, synthesized by microbial method is relatively low. In this study, a SmF3H was identified from the transcriptome of Silybum marianum (L.) Gaertn. The results of fermentation showed that SmF3H can catalyze the flavone 3-hydroxylation reaction, and its catalytic efficiency was significantly higher than that of commonly used SlF3H from Solanum lycopersicum. Six promoters with different transcription strength were selected to optimize the synthesis pathway from the flavonoid precursor (2S)-naringenin to (2S)-taxifolin. The results showed that the highest titer of (2S)-taxifolin (695.90 mg/L in shake flask) could be obtained when the P(GAL7) promoter was used to control the expression of SmF3H. The titer of (2S)-taxifolin was further improved to 3.54 g/L in a 5-L fermenter, which is the highest titer according to current available literatures.

Effect of taxifolin on oxidative gastric injury induced by celiac artery ligation in rats

Abstract Purpose: To examine the effect of taxifolin on I/R induced gastric injury in rats using biochemical and histopatholohical methods. Methods: Eighteen albino Wistar male rats equally grouped as; gastric I/R (I/R), 50 mg/kg taxifolin + gastric I/R (TAX+ I/R) and sham operation applied (SHAM). Ischemia induced for 1 hour, and reperfusion induced for 3 hours. Results: Oxidant parameters like, Malondialdehyde (MDA) and Hydroxyguanine (8-OHdG) were higher, whereas total glutathione (tGSH) was lower in the I/R group according to SHAM group, histopathological findings such as marked destruction, edema, and proliferated dilated congested blood vessels were observed severely in the I/R group, whereas there was not any pathological finding except mild dilated congested blood vessels in the TAX+ I/R group. Conclusion: The taxifolin can be clinically beneficial in the treatment of gastric injury due to I/R procedure.

Chemical constituents from Achyrocline satureioides (I) / 中草药

Objective To study the chemical constituents from Achyrocline satureioides. Methods Chemical constituents from A. satureioides were separated and purified by a variety of chromatographic techniques, and their structures were identified by various spectroscopic methods. Results Twenty-one compounds were isolated from ethyl acetate fraction of the plant, which were α-amyrin (1), ergosta-4,6,8,22-tetraene-3-one (2), (R)-24-ethylcholest-4-en-3,6-dione (3), clovandiol (4), caryolane-1,9β-diol (5), lepidissipyrone (6), 5,7-dihydroxy-3,6-dimethoxyflavone (7), quercetin-7-O-β-D-glucoside (8), pinocembrin (9), (2R,3R)-taxifolin (10), quercetin-4’-O-β-D-glucoside (11), helichrysetin (12), 3-[5,7-dihydroxy-2,2-dimethyl-8-(2-(S)-methyl-butanoyl)-2H-chromen-6- yl-methyl]-6-ethyl-4-hydroxy-5-methyl-pyran-2-one (13), quercetin (14), protocatechuic acid (15), (+)-(3R)-3-hydroxyl-4,4- dimethyl-4-butyrolactone (16), (4S,5R)-5-(4’-methyl-3’-pentenyl)-4-hydroxy-5-methyldihydrofuran-2-one (17), genkwanin (18), quercetin-3-methyl ether (19), galangin (20), and neosakuranin (21). Conclusion Compounds 1, 4, 5, 16, 17, and 21 are obtained from the genus for the first time, and compounds 1-12, 16-18, and 21 are obtained from the plant for the first time.

Study on flavonoids from green walnut husks of Juglans mandshurica / 中草药

Objective: To study the chemical constituents from the green walnut husks of Juglans mandshurica. Methods: The chemical constituents from the green walnut husks of J. mandshurica were isolated and purified by repeated silica gel, Sephadex LH-20 column chromatography and ODS column chromatography, and their structures were identified by NMR spectral analysis. Results: A total of 14 compounds were isolated from the green walnut husks of J. mandshurica, and identified as apigenin (1), tricin (2), eupatilin (3), 3,7,8,3’-tetrahydroxy-4’-methoxyflavone (4), 3,5-dihydroxy-7-methoxy-3’,4-methylenedioxyflavone (5), taxifolin (6), quercetin-3-O-(6″-galloyl)-β-D-galactopyranoside (7), quercetin-3-O-(4″-O-acetyl)-α-L-rhamnopyranoside (8), engeletin (9), isoengeletin (10), kaempferol-3-O-β-D-glucopyranoside (11), quercetin-3-O-β-D-glucuronide (12), quercetin-3-O-β-D- glucopyranoside (13), and myricetin-3-O-β-D-glucuronide (14). Conclusion: Compounds 1-10, 12, and 14 are isolated from the green walnut husks of J. mandshurica for the first time.

Isolation and content determination of taxifolin, orobol and quercetin in Cudrania tricuspidata / 国际中医中药杂志

Objective To isolate and identify 3 flavonoids (taxifolin, orobol and quercetin) from Cudrania tricuspidata, and develop a method for determining 3 flavonoid constituents in Cudrania tricuspidata. Methods Three flavonoids was isolated from ethanol extract of Cudrania tricuspidata by chromatography, and its structure was identified by nuclear magnetic resonance. The analysis was conducted on an Aglient C18 column (4.6 mm ×250 mm, 5 μm) eluted with 1％ acetic acid and methanol as mobile phases in gradient mode. The flow rate was 1 ml/min and the detection wavelength was set at 310 nm. The column temperature was 25 ℃. Results Taxifolin, orobol and quercetin were isolated from ethanol extract of Cudrania tricuspidata by chromatography. The content of taxifolin, orobol and quercetin were 0.850 mg/g, 0.518 mg/g, 0.103 mg/g. Conclusion The method can be used for the quality control of Cudrania tricuspidata as a reference.

Protective effect of taxifolin on H2O2-induced H9C2 cell pyroptosis / 中南大学学报(医学版)

Objective:To explore the effect of taxifolin on H2O2-induced pyroptosis in H9C2 cells and the possible mechanisms.Methods:The H9C2 cells was divided into 3 groups:a control group,a hydrogen peroxide (H2O2) group and a taxifolin group.The morphology of H9C2 cells was observed by inverted phase contrast microscope.The mitochondrial membrane potential was measured by JC-1 staining and flow cytometry.The alteration of the level of reactive oxygen species (ROS) was detected by specific mitochondrial probe.The protein levels of cysteinyl aspartate specific proteinase-1 (caspase-1) was determined by Western blot.The mRNA levels of interleukin-18 (IL-18),interleukin-1a (IL-1a),interleukin-1b (IL-1b),absent in melanoma 2 (AIM2),apoptosis-associated apeck-like protein (ASC),nucleotide-binding oligomerization domain-like receptor protein 3 (NLRP3)and nucleotide-binding oligomerization domain-like receptor family caspase recruitment domaincontaining protein 4 (NLRC4) were determined by reverse transcription-polymerase chain reaction (RT-PCR).Results:Compared with the control group,the morphology of H9C2 cells obviously changed in the H2O2-treated group,which was guadually improved in the presence of taxifolin.Compared with the control group,the mitochondrial membrane potential was markedly decreased in the H2O2-treated cells,accompanied by the increase of ROS (both P＜0.05).Compared with the H2O2 group,the mitochondrial membrane potential changes in the taxifolin group was increased while the ROS was decreased,with significant difference (both P＜0.05).Compared with the control group,the protein level of caspase-1 and the mRNA levels of IL-18,IL-1a,IL-1b,AIM2,ASC,NLRP3 and NLRC4 in the H2O2-treated group were significantly increased (all P＜0.05),which were attenuated in the presence of taxifolin (all P＜0.05).Conclusion:Taxifolin can protect H9C2 cells from oxidative injury,and it is able to suppress the H2O2-induced H9C2 cell pyroptosis through inhibition of AIM2,NLRP3 and NLRC4 in flammasome.

Optimization of Extraction and Purification Technology of Total Flavonoids from Engelhardia roxburghi-ana and Content Determination of 3 Kinds of Effective Components / 中国药房

OBJECTIVE:To optimize the extraction and purification technology of total flavonoids from Engelhardia roxburghi-ana,and to establish the method for the content determination of 3 kinds of effective components. METHODS:Using the extrac-tion transfer rate of astilbin as index,single factor test was used to investigate extraction solvent,extraction method,volume frac-tion of percolation solvent ethanol,percolation material-liquid ration,soaking time before percolation and percolation rate of extrac-tion technology,and volume fraction of eluant ethanol in AB-8 resin purification technology. The contents of 3 effective compo-nents as astilbin,texifolin and engelitin in total flavonoids from E. roxburghiana were determined by HPLC. RESULTS:The opti-mal extraction technology was using 70% ethanol as extraction and percolation solvent,percolation extraction,soaking for 8 h be-fore percolation,percolation material-liquid ratio of 1∶16(g/ml),percolation rate of 30 ml/(min·kg). The purification technology was diluting the solution to 0.5 g (crude drug)/ml with water,ethyl acetate extraction,dissolved extract with 50% ethanol after evaporated to dryness,AB-8 resin for sampling,eluted with 50% ethanol,concentrating and drying. In verification test,extraction transfer rate of astilbin was more than 80%(RSD=0.42%,n=3). The contents of astilbin,taxifolin and engeletin in total flavo-noids from E. roxburghiana by purified were 57.94%,3.72% and 2.83%,respectively;the contents of 3 components accounted for 64.00% of total flavonoids. CONCLUSIONS:The extraction and purification technology is stable,rational and reliable;the content determination method of 3 effective components in total flavonoids of E. roxburghiana is accurate,simple and producible.

Chemical constituents from Tetracera asiatica / 中草药

Objective: To study the chemical constituents in the aerial parts of Tetracera asiatica. Methods: Silica gel, ODS, Sephadex LH-20 gel column chromatographies, and HPLC were used to isolate and purify the compounds. And the structures of the obtained compounds were identified by their physical properties and spectroscopic data. Results: Twelve compounds were separated and purified from the alcoholic extract of T. asiatica. They were identified to be rhamnocitrin (1), isorhamnetin (2), naringenin (3), rhamnetin (4), kaempferol (5), taxifolin (6), quercetin (7), tiliroside (8), quercetin-3-O-α-L-rhamnopyranoside (9), (-)-epicatechin 3-(3-O-methyl) gallate (10), epicatechin-3-O-gallate (11), and (-)-epicatechin (12). Conclusion: Compounds 1-12 are obtained from this plant for the first time.

Chemical constituents from barks of Quercus mongolica / 中草药

Objective: To study the chemical constituents from the barks of Quercus mongolica. Methods: The chemical constituents were isolated and purified on the base of silica gel column chromatography and HPLC method. The structural elucidation was performed according to the physicochemical properties and spectral analysis. Results: Twenty compounds were isolated and identified as taraxerone (1), taraxerol (2), 20β-hydroxydammara-23-en-3-one (3), 20 (S), 24 (S)-dihydroxydammara-26-en-3-one (4), ursotic acid acetate (5), lupeol (6), β-sitosterone (7), isofouquierol (8), gallic acid (9), 5, 6, 7, 4'-tetrahydroxyflavanone (10), taxifolin (11), scopoletin (12), kaempferol (13), β-sitosterol (14), secoisolariciresinol (15), erythrodiol (16), (-)-epicatechin (17), daucosterol (18), (-)-epipinoresinol (19), and salicylic acid (20). Conclusion: Compounds 1, 2, 5, 6, and 11 are isolated from this plant for the first time, and compounds 4, 7, and 8 are isolated from the plants of Quercus L. for the first time.

Taxifolin Glycoside Blocks Human ether-a-go-go Related Gene K+ Channels

Taxifolin glycoside is a new drug candidate for the treatment of atopic dermatitis (AD). Many drugs cause side effects such as long QT syndrome by blocking the human ether-a-go-go related gene (hERG) K+ channels. To determine whether taxifolin glycoside would block hERG K+ channels, we recorded hERG K+ currents using a whole-cell patch clamp technique. We found that taxifolin glycoside directly blocked hERG K+ current in a concentration-dependent manner (EC50=9.6+/-0.7 microM). The activation curve of hERG K+ channels was negatively shifted by taxifolin glycoside. In addition, taxifolin glycoside accelerated the activation time constant and reduced the onset of the inactivation time constant. These results suggest that taxifolin glycoside blocks hERG K+ channels that function by facilitating activation and inactivation process.

Molecular docking based inhibition of Trypanothione reductase activity by Taxifolin novel target for antileishmanial activity.

The theoretical docking study, conducted on a sample of previously reported for anti-inflammatory and antioxidant activities of Taxifolin at the binding site of Leishmania infantum trypanothione reductase (Try R) examine interaction energy. Taxifolin is widely used in the traditional medicine have been investigated for their putative chemo preventive and antileishmanial properties for the last few decades. A theoretical docking study, the evaluation of Taxifolin as inhibitor of trypanothione reductase a validated drug target enzyme of the Leishmania parasite. Taxifolin was found to bind at active site of L. infantum TryR with lowest binding energy and RMSD values to be -8.82 Kcal/Mol and 2.0 Å respectively. Docking analysis of TryR with ligand enabled us to identify specific residues viz. Ser-14, Ala-47, Ser-162, Thr-336 and Arg-286, within the TryR binding pocket to play an important role in ligand binding affinity. The availability of TryR built model, together with insights gained from docking analysis will promote the rational design of potent and selective TryR inhibitor as antileishmanial therapeutic. The study contributes towards understanding mechanism of antileshmanial effect of the Taxifolin. This compound has shown promising biological activity in preliminary studies by targeting multiple signaling pathways. Thus on the basis of our in silico studies we hypothesize that this compound into Taxifolin can be inhibitory effect on against leishmaniasis.

Molecular construction of NADH-cytochrome b5 reductase inhibition by flavonoids and chemical basis of difference in inhibition potential: Molecular dynamics simulation study.

NADH-cytochrome b5 reductase, a flavoprotein, plays a central role in many diverse metabolic reactions. NADH-cytochrome b5 reductase has been shown to be responsible for the generation of free radicals from heterocyclic amines. Flavonoids compounds share remarkable similarity in structure but showed differences in their cytochrome b5 reductase inhibition pattern. Our molecular dynamics simulation studies revealed that the difference in substitution at C3 position of ring C may lead to difference in interaction with enzyme. Absence of hydroxyl group substitution at C3 in luteolin facilitates the strong cation-π interaction between Lys185 and ring A, and C and π-π between Phe92 and ring A, and C along with h-bonding between Lys185 and oxo group. Ring B of luteolin showed strong π-π interaction with FAD. These interactions were found absent in quercetin and taxifolin. These results suggest that absence of hydroxyl group substitution at C3 increases the potency of flavonoid inhibitors for cytochrome b5 reductase.

Taxifolin acts as type I inhibitor for VEGFR-2 kinase: Stability evaluation by molecular dynamic simulation.

The VEGFR-2 kinase specific intracellular signalling cascades leading to proliferation, migration, survival of endothelial cells and increased permeability of vessels which contributes to angiogenesis. ATP is essentially required by VEGFR-2 to perform phosphorylation of specific proteins and to maintain cascade downstream. Taxifolin (plant polyphenol) inhibit the VEGFR-2 kinase by binding at ATP-binding pocket revealed by molecular docking study. Further, stability of VEGFR-2 kinase-taxifolin complex is validated by molecular dynamic simulation. RMSD analysis for 3800 ps confirmed the stability of complex. Furthermore, thermodynamic stability was evidenced by stable total energy, potential energy, and, temperature and pressure profile. After MD simulation taxifolin was found to stably interact with pocket residues Cys 917 and Lys 1053 along with water molecules. These results suggest that therapeutic inhibition of VEGFR-2 by taxifolin as a type I inhibitor may be a promising ways to retard signaling cascade of specific proteins which play crucial role in cancer proliferation and also in development of second generation type II inhibitors.

Chemical constituents in Guizhi Fuling Capsula (I) / 中草药

Objective: To investigate the chemical constituents of the chloroform extraction from Guizhi Fuling Capsula. Methods: The compounds were separated with column chromatography and their chemical structures were identified by physiochemical and spectral methods, respectively. Results: Fifteen compounds were isolated from the Capsula. They were identified as paeonol (1), benzoic acid (2), β-stigmasterol (3), trans-cinnamic acid (4), betulinic acid (5), 2,5-dihydroxy-4-methylacetophenone (6), oleanolic acid (7), pachymic acid (8), taxifolin (9), amygdalin (10), mannitol (11), 3,3′-di-O-methyl ether ellagic acid (12), hederagenin (13), gallic acid (14), and daucosterol (15). Conclusion: Compounds 1-15 are isolated from the Capsula for the first time.

HPLC Fingerprint of Fructus Polygoni Orientalis / 中成药

AIM:In order to ensure the quality stability of Fructus Polygoni Orientalis,to study the determination method of the fingerprint of Fruetus Polygoni Orientalis and to establish the fingerprint of Fructus Polygoni Orientalis.METHODS:The HPLC assay was used to establish the fingerprint of Fructus Polygoni Orienlalis and 28 pieces of goods were compared.RESULTS:The fingerprint of Fructus Polygoni Orientalis with 7 common peaks was established.The relative retention time and the ranges of relative area of the common peaks were determined.CONCLUSION:The established fingerprint can be used for the quality control of Fructus Polygoni Orientalis.