首页|苦参中钠-葡萄糖协同转运蛋白2抑制活性成分的研究

苦参中钠-葡萄糖协同转运蛋白2抑制活性成分的研究

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对一个含400种中草药和民族药的组分库进行活性筛选,结果显示苦参的甲醇提取物具有良好的抑制钠-葡萄糖协同转运蛋白2(SGLT2)的活性.在生物活性导向的分离纯化策略下,运用中压柱色谱和半制备高效制备液相色谱对苦参甲醇提取物的活性成分进行分离纯化,根据理化性质和波谱数据鉴定所分离化合物的结构,并对所得到的化合物进行抑制SGLT2活性测试.从苦参的甲醇提取物中分离得到7个黄酮苷类化合物,鉴定为芒柄花素-7-O-β-D-吡喃木糖基-(1→6)-β-D-吡喃葡萄糖苷(1)、芒柄花素-7-O-β-D-呋喃芹糖基-(1→6)-β-D-吡喃葡萄糖苷(2)、三叶豆紫檀苷(3)、(-)-高丽槐素-3-O-β-D-吡喃半乳糖苷(4)、6'-乙酰三叶豆紫檀苷(5)、罗思菌素(6)、芒柄花苷(7).除化合物3外,其他化合物均为首次从苦参中分离得到.7个化合物均有抑制SGLT2的活性,其中具有高丽槐素苷元结构的苷类成分3~5具有较好的抑制SGLT2的活性,对SGLT2的抑制活性的IC50范围为2.61~ 4.47 μmol/L.
Sodium-dependent glucose cotransporter 2 (SGLT2)inhibitors from Sophora flavescens
To discover new bioactive Sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors from the traditional Chinese medicine:" Kushen" (roots of Sophoraflavescens),the bioassay-guided purification of an active methanolic fraction was performed.Seven known flavonoid glycosides were isolated and determined.Their structures were elucidated as formononetin 7-O-β-D-xylopyranosyl-(1→6)-β-D-glucopyranoside (1),formononetin 7-O-β-D-apiofuranosyl-(1 →6)-β-D-glucopyranoside (2),trifolirhizin (3),(-)-maackiain 3-O-β-D-galactopyranoside (4),trifolirhizin 6'-monoacetate (5),rothindin (6) and ononin (7).All compounds were isolated from this plant for the first time except compound 3.All seven compounds exhibited inhibitory activity against SGLT2.Among them,compounds 3-5 with the maackiain skeleton showed the most potential inhibitory activity against SGLT2 with the IC50 value ranging between 2.61 and 4.47μmol/L.

Sophora flavescenschemical constituentsflavonoid glycosidesSGLT2 inhibitors

杨新洲、杨静、汪超、万近福、袁经权、任永申

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中南民族大学药学院,湖北武汉430074

云南白药集团股份有限公司研究院,云南昆明650032

广西药用植物园,广西南宁530023

苦参 化学成分 黄酮苷 SGLT2抑制剂

人事部留学人员科技活动项目择优资助项目国家自然科学基金武汉市青年科技晨光计划项目

BZY12006811027982013070104010028

2014

云南大学学报(自然科学版)
云南大学

云南大学学报(自然科学版)

CSTPCDCSCD北大核心
影响因子:0.663
ISSN:0258-7971
年,卷(期):2014.36(2)
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