Pueraria lobata ( Wild. ) Ohwi ( Ye-Ge in Chinese ) is a perennial herb ofthe genus Pueraria, which belongs to the Leguminosae family. It is commonly employed to relievefever and dysentery, promote the production of b...Pueraria lobata ( Wild. ) Ohwi ( Ye-Ge in Chinese ) is a perennial herb ofthe genus Pueraria, which belongs to the Leguminosae family. It is commonly employed to relievefever and dysentery, promote the production of body fluid, reduce stiffness and pain of the nape,and for the treatment of cardiovascular diseases, e. g. hypertension, myocardial infarction, andarrhythmia. Previous phytochemical studies on P. lobata reported a number of bioactive isoflavones,e. g. daidzein, daidzin, and puerarin. Further investigation of its root has led to isolation offourteen compounds and their structures were identified as daidzein, ononin, daidzin, 3'' -methoxypuerarin, puerarin, pueroside B, daidzein-8-C-apiosyl- (1-6)-glucoside, 3''-hydroxy-puerarin,puerarinxyloside, daidzein-7, 4'' -O-glucoside, puerarin-4''-O-glucoside, mirificin-4''-O-glucoside,sissotorin, and pueroside C. Compounds 11 and 13 were isolated from the root of P. lobata for thefirst time.展开更多
Aim To study chemical constituents from Ampelopsis grossedentata. Methods Separation and purification were performed by using silica gel, polyamide, reverse-phase silica gel, Sephadex LH-20 column chromatographic tech...Aim To study chemical constituents from Ampelopsis grossedentata. Methods Separation and purification were performed by using silica gel, polyamide, reverse-phase silica gel, Sephadex LH-20 column chromatographic techniques and silica gel PTLC. Structures were determined by means of physicochemical properties and spectral analysis. Results Four flavonoids were separated and identified from Ampelopsis grossedentata including dihydromyricetin (1), myricetin (2), myricitrin (3), and myricetin-3-O-β-D-galactopy...展开更多
In addition to six known flavonoids quercitrin, hyperoside, avicularin, rutin, quercetin and kaemferol, a new flavonol glycoside named 6″_O_acetyl quercetin 3_O_β_ D _alloside (1) was isolated from the aerial par...In addition to six known flavonoids quercitrin, hyperoside, avicularin, rutin, quercetin and kaemferol, a new flavonol glycoside named 6″_O_acetyl quercetin 3_O_β_ D _alloside (1) was isolated from the aerial parts of Hypericum perforatum L. The structures were determined on the basis of spectroscopic methods (UV, IR, FAB_MS, 1H_NMR and 13 C NMR). Antifungal assay of all compounds showed that metabolite 1, quercitrin and quercetin were inhibitory to the growth of phytopathogenic fungus Helminthosporium sativum Pamel King et Bakke with minimum inhibitory concentrations (MICs) of 25, 50 and 50 μg/mL, respectively. Moreover, glycoside 1 and quercitrin were also shown to be able to inhibit the growth of Fusarium graminearum Schw. with MIC of 100 μg/mL. The MICs of ketoconazole used as control against the test fungi were 0.5 μg/mL in our assay.展开更多
Aim To study the chemical constituents of the root and rhizome of Rheum tanguticum Maxim. ex Balf. Methods Chemical constituents were isolated and purified by many chromatographic methods, and their structures were el...Aim To study the chemical constituents of the root and rhizome of Rheum tanguticum Maxim. ex Balf. Methods Chemical constituents were isolated and purified by many chromatographic methods, and their structures were elucidated by MS, NMR, and others. Results Twenty compounds were isolated and their structures were identified as β-sitosterol, chrysophanol, aloe-emodin, physcion, rhein, emodin, etc. Conclusion Among these compounds, 4-(4′-hydroxyphenyl)-2-butanone, 4-(4′-hydroxyphenyl)-2-butanone-4′-O-β-D-(2″-...展开更多
A method for the quantification of quercetin-3’-O-glucoside in rat plasma by high-performance liquid chromatography-tandem mass spectrometry（HPLC-MS/MS） was developed and validated.Along with internal standard（car...A method for the quantification of quercetin-3’-O-glucoside in rat plasma by high-performance liquid chromatography-tandem mass spectrometry（HPLC-MS/MS） was developed and validated.Along with internal standard（carbamazepine）,quercetin-3’-O-glucoside was extracted from plasma samples by simple liquid-liquid extraction with ethyl acetate.The mass spectrometry detection was set in multiple reaction monitoring（MRM） mode via positive electrospray ionization（ESI）.The chromatographic run time was 3.5 min per sample.The calibration curves were linear（r^2 = 0.9992） with a lower limit of quantification（LLOQ） of 10.625 ng/mL,and the limit of detection（LOD） was 4.25 ng/mL.The intra-and inter-day precision and accuracy,in terms of relative standard deviation（RSD）,were all lower than 10.44%.The recovery rate of the analyte and internal standard were higher than 66.80%.After intravenous administration of 10 mg/kg quercetin-3’-O-glucoside,the t1/2 and AUC were（0.02±0.01） h and（1.22±0.28）×10^4 μg/L·h.The method is accurate,stable and sensitive,which is suitable for the pharmacokinetic study of quercetin-3’-O-glucoside in rats.展开更多
Wogonin possesses potent inhibitory activities against cancer cell growth in vitro and in vivo and has attractive safety profiles.A highly sensitive liquid chromatography coupled with tandem mass spectrometry method w...Wogonin possesses potent inhibitory activities against cancer cell growth in vitro and in vivo and has attractive safety profiles.A highly sensitive liquid chromatography coupled with tandem mass spectrometry method was developed for the identification of major metabolites in mice liver after intravenous administration of wogonin.Five metabolites were identified and biotransformation pathways were elucidated as well.Furthermore,a method was developed and validated for the simultaneous quantitatively determination of wogonin and wogonin-7-O-glucuronide in mice liver.After liquid-liquid extraction by ethyl acetate,the analytes were separated on a C_（18）column with a mobile phase of methanol-10 mM ammonium acetate water （80：20,v/v）.The detection was operated with negative selected reaction monitoring mode using electrospray ionization technique. The linear response range was 0.2-40μg/g for both wogonin and wogonin-7-O-glucuronide in mice liver.The developed quantification method was suitable for distribution study after intravenous infusion of wogonin injection in animals.展开更多
Mangiferin is a natural plant polyphenol with a structure of xanthone C-glycoside and it displays a wide spectrum of pharmacological activities. Investigation of the metabolites of mangiferin is valuable in studying t...Mangiferin is a natural plant polyphenol with a structure of xanthone C-glycoside and it displays a wide spectrum of pharmacological activities. Investigation of the metabolites of mangiferin is valuable in studying the mechanisms of its various pharmacological properties and developing novel drugs from the mangiferin derivatives. Among the metabolites of mangiferin, mangiferin-7-O-β-D-glucuronide has been reported as the phase Ⅱ metabolite of mangiferin. Herein we described the first semi-synthesis of mangiferin-7-O-β-D-glucuronide with the natural product mangiferin as the starting material. In this work, we adopted several regioselective protection procedures to distinguish the different hydroxyl groups in the structure of mangiferin, and we accomplished the glycosylation under the phase-transfer catalysis conditions. In this method, we efficiently synthesized the glucuronide derivative of mangiferin in 10 steps with highly regioselective protection.展开更多
文摘Pueraria lobata ( Wild. ) Ohwi ( Ye-Ge in Chinese ) is a perennial herb ofthe genus Pueraria, which belongs to the Leguminosae family. It is commonly employed to relievefever and dysentery, promote the production of body fluid, reduce stiffness and pain of the nape,and for the treatment of cardiovascular diseases, e. g. hypertension, myocardial infarction, andarrhythmia. Previous phytochemical studies on P. lobata reported a number of bioactive isoflavones,e. g. daidzein, daidzin, and puerarin. Further investigation of its root has led to isolation offourteen compounds and their structures were identified as daidzein, ononin, daidzin, 3'' -methoxypuerarin, puerarin, pueroside B, daidzein-8-C-apiosyl- (1-6)-glucoside, 3''-hydroxy-puerarin,puerarinxyloside, daidzein-7, 4'' -O-glucoside, puerarin-4''-O-glucoside, mirificin-4''-O-glucoside,sissotorin, and pueroside C. Compounds 11 and 13 were isolated from the root of P. lobata for thefirst time.
文摘Aim To study chemical constituents from Ampelopsis grossedentata. Methods Separation and purification were performed by using silica gel, polyamide, reverse-phase silica gel, Sephadex LH-20 column chromatographic techniques and silica gel PTLC. Structures were determined by means of physicochemical properties and spectral analysis. Results Four flavonoids were separated and identified from Ampelopsis grossedentata including dihydromyricetin (1), myricetin (2), myricitrin (3), and myricetin-3-O-β-D-galactopy...
文摘In addition to six known flavonoids quercitrin, hyperoside, avicularin, rutin, quercetin and kaemferol, a new flavonol glycoside named 6″_O_acetyl quercetin 3_O_β_ D _alloside (1) was isolated from the aerial parts of Hypericum perforatum L. The structures were determined on the basis of spectroscopic methods (UV, IR, FAB_MS, 1H_NMR and 13 C NMR). Antifungal assay of all compounds showed that metabolite 1, quercitrin and quercetin were inhibitory to the growth of phytopathogenic fungus Helminthosporium sativum Pamel King et Bakke with minimum inhibitory concentrations (MICs) of 25, 50 and 50 μg/mL, respectively. Moreover, glycoside 1 and quercitrin were also shown to be able to inhibit the growth of Fusarium graminearum Schw. with MIC of 100 μg/mL. The MICs of ketoconazole used as control against the test fungi were 0.5 μg/mL in our assay.
基金Natural Research Foundation of Qinghai Province( No. 2004-N-103-02)
文摘Aim To study the chemical constituents of the root and rhizome of Rheum tanguticum Maxim. ex Balf. Methods Chemical constituents were isolated and purified by many chromatographic methods, and their structures were elucidated by MS, NMR, and others. Results Twenty compounds were isolated and their structures were identified as β-sitosterol, chrysophanol, aloe-emodin, physcion, rhein, emodin, etc. Conclusion Among these compounds, 4-(4′-hydroxyphenyl)-2-butanone, 4-(4′-hydroxyphenyl)-2-butanone-4′-O-β-D-(2″-...
基金National Natural Science Foundation of China (Grant No. 30960494)Jiangxi Province NSFC (Grant No. 2009 GZY0099)
文摘A method for the quantification of quercetin-3’-O-glucoside in rat plasma by high-performance liquid chromatography-tandem mass spectrometry（HPLC-MS/MS） was developed and validated.Along with internal standard（carbamazepine）,quercetin-3’-O-glucoside was extracted from plasma samples by simple liquid-liquid extraction with ethyl acetate.The mass spectrometry detection was set in multiple reaction monitoring（MRM） mode via positive electrospray ionization（ESI）.The chromatographic run time was 3.5 min per sample.The calibration curves were linear（r^2 = 0.9992） with a lower limit of quantification（LLOQ） of 10.625 ng/mL,and the limit of detection（LOD） was 4.25 ng/mL.The intra-and inter-day precision and accuracy,in terms of relative standard deviation（RSD）,were all lower than 10.44%.The recovery rate of the analyte and internal standard were higher than 66.80%.After intravenous administration of 10 mg/kg quercetin-3’-O-glucoside,the t1/2 and AUC were（0.02±0.01） h and（1.22±0.28）×10^4 μg/L·h.The method is accurate,stable and sensitive,which is suitable for the pharmacokinetic study of quercetin-3’-O-glucoside in rats.
基金China National Key Hi-Tech Innovation Project for the R&D of Novel Drugs(Grant No.2009zx09102-032).
文摘Wogonin possesses potent inhibitory activities against cancer cell growth in vitro and in vivo and has attractive safety profiles.A highly sensitive liquid chromatography coupled with tandem mass spectrometry method was developed for the identification of major metabolites in mice liver after intravenous administration of wogonin.Five metabolites were identified and biotransformation pathways were elucidated as well.Furthermore,a method was developed and validated for the simultaneous quantitatively determination of wogonin and wogonin-7-O-glucuronide in mice liver.After liquid-liquid extraction by ethyl acetate,the analytes were separated on a C_（18）column with a mobile phase of methanol-10 mM ammonium acetate water （80：20,v/v）.The detection was operated with negative selected reaction monitoring mode using electrospray ionization technique. The linear response range was 0.2-40μg/g for both wogonin and wogonin-7-O-glucuronide in mice liver.The developed quantification method was suitable for distribution study after intravenous infusion of wogonin injection in animals.
基金The National Research Foundation for the Doctoral Program of Higher Education of China(Grant No.20130001110058)
文摘Mangiferin is a natural plant polyphenol with a structure of xanthone C-glycoside and it displays a wide spectrum of pharmacological activities. Investigation of the metabolites of mangiferin is valuable in studying the mechanisms of its various pharmacological properties and developing novel drugs from the mangiferin derivatives. Among the metabolites of mangiferin, mangiferin-7-O-β-D-glucuronide has been reported as the phase Ⅱ metabolite of mangiferin. Herein we described the first semi-synthesis of mangiferin-7-O-β-D-glucuronide with the natural product mangiferin as the starting material. In this work, we adopted several regioselective protection procedures to distinguish the different hydroxyl groups in the structure of mangiferin, and we accomplished the glycosylation under the phase-transfer catalysis conditions. In this method, we efficiently synthesized the glucuronide derivative of mangiferin in 10 steps with highly regioselective protection.
