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O-葡萄糖醛酸苷的生物合成研究进展 被引量:3
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作者 王梅玲 夏杨柳 +5 位作者 杨梦丽 吴大畅 刘丽坤 葛广波 杨凌 侯洁 《中草药》 CAS CSCD 北大核心 2015年第7期1065-1073,共9页
葡萄糖醛酸结合反应是机体内重要的一类代谢反应,其中O-葡萄糖醛酸结合是最常见的反应类型。O-葡萄糖醛酸苷的制备对于准确评估葡萄糖醛酸代谢产物的药理活性及安全性、药物代谢和药动学定量分析等研究至关重要。利用尿苷二磷酸葡萄糖... 葡萄糖醛酸结合反应是机体内重要的一类代谢反应,其中O-葡萄糖醛酸结合是最常见的反应类型。O-葡萄糖醛酸苷的制备对于准确评估葡萄糖醛酸代谢产物的药理活性及安全性、药物代谢和药动学定量分析等研究至关重要。利用尿苷二磷酸葡萄糖醛酸转移酶(UGT)生物合成目标代谢物是制备葡萄糖醛酸苷的重要手段之一。综述了近年来利用生物转化技术制备O-葡萄糖醛酸苷的研究进展,包括利用植物、微生物、动物来源及人重组UGT酶等不同方法制备O-葡萄糖醛酸苷的最新进展,同时还综述了近年来国内外通过对生物反应体系和转化工艺的改进与优化,实现葡萄糖醛酸苷高效制备的相关技术和工艺特点。 展开更多
关键词 o-葡萄糖醛酸苷 葡萄糖转移酶 植物生物合成 动物UGT酶 微生物发酵
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Metabolite identification and the development of a simultaneous quantification method for wogonin and wogonin-7-O-glucuronide:application to a distribution study in mice liver 被引量:1
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作者 柳文媛 杨晓静 +1 位作者 冯锋 徐晓珍 《Journal of Chinese Pharmaceutical Sciences》 CAS 2011年第3期282-289,共8页
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
关键词 WOGONIN Wogonin-7-o-glucuronide Metabolite identification Liquid chromatography-tandem mass spectrometry
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Semi-synthesis of mangiferin-7-O-β-D-glucuronide 被引量:1
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作者 杨博威 梁丹琳 +2 位作者 魏雄 孟祥豹 李中军 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2017年第8期556-565,共10页
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
关键词 Mangiferin-7-o-β-D-glucuronide Semi-synthesis Regioselective protection Glycosylation
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