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肾茶的化学成分及其抑制α-葡萄糖苷酶活性研究

Chemical Constituents of Clerodendranthus spicatus and Inhibitory Activity againstα-Glucosidase
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摘要 目的:对肾茶Clerodendranthus spicatus(Thunb.)C.Y.Wu ex H.W.Li地上部分的化学成分进行分离鉴定并测定其抑制α-葡萄糖苷酶的活性。方法:运用硅胶柱色谱、Sephadex LH-20凝胶柱色谱、ODS反相柱色谱和半制备液相色谱进行分离纯化,根据波谱学数据对化合物进行结构鉴定。通过4-硝基苯-β-D-吡喃葡萄糖苷法测定各化合物抑制α-葡萄糖苷酶的活性。结果:从肾茶中分离得到24个化合物,分别是外消旋顺式-2,3-二羟基-3-(3,4-二羟基苯基)-丙酸(1)、木犀草素(2)、3-(3,4-二羟基苯基)-丙烯酸-1-(3,4-二羟基苯基)-2-甲氧基羰基乙酯(3)、迷迭香酸甲酯(4)、迷迭香酸(5)、山地香茶菜素A(6)、肾茶酸A(7)、山柰酚-3-O-(2″-O-β-D-吡喃葡萄糖基)-β-D-吡喃葡萄糖苷(8)、鼠尾草素(9)、熊果酸(10)、齐墩果酸(11)、2,6-二甲氧基对苯醌(12)、2-O-去乙酰肾茶二萜醇J(13)、新肾茶二萜醇B(14)、肾茶二萜醇N(15)、斯塔醇C(16)、苯甲酸(17)、5,3′-二羟基-7,4′-二甲氧基黄酮(18)、半齿泽兰素(19)、委陵菜酸(20)、藜芦酸(21)、3-吲哚甲醛(22)、(6R,7E,9S)-9-羟基-4,7-巨豆二烯-3-酮(23)、肾茶二萜酮A(24)。结论:其中化合物1、8、12、22、23为首次从该植物中分离得到,化合物2~4、21、22对α-葡萄糖苷酶具有良好的抑制活性,半数抑制浓度分别为(45.76±0.01)、(51.09±0.01)、(41.08±0.03)、(66.96±0.72)、(116.80±0.33)μg·mL–1。 Objective:The chemical constituents of Clerodendranthus spicatus(Thunb.)C.Y.Wu ex H.W.Li were isolated,and their inhibitory activities againstα-glucosidase were studied.Methods:The compounds were isolated and purified by silica gel chromatography,Sephadex LH-20 gel chromatography,ODS reversed-phase chromatography,and semipreparative liquid chromatography,and their structures were identified on the basis of the spectral data.At the same time,the inhibitory activity of the compounds againstα-glucosidase was tested by 4-nitrophenyl-β-D-glucopyranoside(PNPG)method.Results:Twenty-four compounds were isolated and identified,namely asracsyn-2,3-dihydroxy-3-(3,4-dihydroxyphenyl)-propionicacid(1),luteolin(2),3-(3,4-dihydroxyphenyl)-acrylicacid-1-(3,4-dihydroxyphenyl)-2-methoxycarbonylethylester(3),methylrosmarinate(4),rosmarinicacid(5),oresbiusin A(6),orthosiphoicacid A(7),kaempferol-3-O-(2″-O-β-D-glycopyranosyl)-β-D-glucopyranoside(8),carnosic acid(9),ursolicacid(10),oleanolicacid(11),2,6-dimethoxy-p-benzoquinone(12),2-O-deacetylorthosiphol J(13),neoorthosiphol B(14),orthosiphol N(15),staminol C(16),benzoic acid(17),5,3′-dihydroxy-7,4′-dimethoxyflavone(18),eupatilin(19),valeric acid(20),veratric acid(21),3-indolecarboxaldehyde(22),(6R,7E,9S)-9-hydroxy-4,7-megastigmadiene-3-one(23),and orthosiphonone A(24).Conclusion:Among them,compounds 1,8,12,22,and 23 were isolated from this plant for the first time.Compounds 2-4,21,and 22 had potentα-glucosidase inhibition,and their IC50 were(45.76±0.01),(51.09±0.01),(41.08±0.03),(66.96±0.72),and(116.80±0.33)μg·mL–1,respectively.
作者 陈鑫 顾永哲 舒积成 梁永红 谭婷 罗云 CHEN Xin;GU Yongzhe;SHU Jicheng;LIANG Yonghong;TAN Ting;LUO Yun(Key Laboratory of Modern Preparation of Traditional Chinese Medicine,Ministry of Education,Jiangxi University of Chinese Medicine,Nanchang 330004,China;School of Pharmacy,Jiangxi University of Chinese Medicine,Nanchang 330004,China;The National Pharmaceutical Engineering Center(NPEC)for Solid Preparation in Chinese Herbal Medicine,Jiangxi University of Chinese Medicine,Nanchang 330006,China)
出处 《中国现代中药》 2025年第7期1245-1254,共10页 Modern Chinese Medicine
基金 国家自然科学基金项目(81760711,82160824,82260751) 江西省中医药中青年骨干人才培养计划项目(1242100903) 江西中医药大学重点领域科技创新团队计划项目(CXTD22006)。
关键词 肾茶 化学成分 提取分离 结构鉴定 Α-葡萄糖苷酶 Clerodendranthus spicatus(Thunb.)C.Y.Wu ex H.W.Li chemical constituent extraction separation structural identification α-glucosidase
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