虎尾轮根化学成分及其体外抗肾间质纤维化活性

Chemical constituents from Uraria crinita and their anti⁃renal interstitial fibrosis activity in vitro

目的研究虎尾轮根Uraria crinita(L.)Desv.ex DC的化学成分及其体外抗肾间质纤维化活性。方法虎尾轮根乙醇提取物采用硅胶、Sephadex LH⁃20进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。采用MTT法进行体外抗肾间质纤维化活性筛选。结果从中分离得到16个化合物,分别鉴定为divaricataester A(1)、pyrrolezanthine⁃6⁃ethyl ether(2)、5,7⁃二羟基⁃2′⁃甲氧基⁃3′,4′⁃亚甲基二氧异黄酮(3)、dehydroespeleton(4)、pleuchiol(5)、1,6⁃desoxypipoxide(6)、p⁃coumaroyl⁃β⁃phenethylamine(7)、isolugrandoside(8)、紫苜蓿烷(9)、二氢木豆异黄酮(10)、8⁃O⁃4⁃dehydrodiferulic acid(11)、8,9⁃dehydropellitorine(12)、6⁃O⁃(E)⁃肉桂酰基⁃α/β⁃D⁃吡喃葡萄糖苷(13)、trans⁃3′,4′⁃diacetylkhellacton(14)、3⁃甲氧基⁃4⁃O⁃β⁃D⁃吡喃葡萄糖基苯甲酸甲酯(15)、euparone(16)。化合物5、8对胶原纤维Ⅳ、Ⅲ型前胶原蛋白、层粘连蛋白;化合物11、14对胶原纤维Ⅳ、Ⅲ型前胶原蛋白;化合物2、7对Ⅲ型前胶原蛋白;化合物4、12对胶原纤维Ⅳ、层粘连蛋白均具有体外抑制作用。结论除化合物3外,所有化合物均为首次从该植物中分离得到,化合物2、4~5、7~8、11~12、14对肾间质纤维化指标有不同程度的抑制作用。

AIM To study the chemical constituents from Uraria crinita(L.)Desv.ex DC and their anti⁃renal interstitial fibrosis activity in vitro.METHODS The ethanol extract from U.crinita was isolated and purified by silica column,Sephadex LH⁃20,then the structures of obtained compounds were identified by physicochemical properties and spectral data.Their anti⁃renal interstitial fibrosis activity in vitro was evaluated by MTT method.RESULTS Sixteen compounds were isolated and identified as divaricataester A(1),pyrrolezanthine⁃6⁃ethyl ether(2),5,7⁃dihydroxy⁃2′⁃methoxy⁃3′,4′⁃methylene dioxy isoflavone(3),dehydroespeleton(4),pleuchiol(5),1,6⁃desoxypipoxide(6),p⁃coumaroyl⁃β⁃phenethylamine(7),isolugrandoside(8),sativan(9),dihydrocajanin(10),8⁃O⁃4⁃dehydrodiferulic acid(11),8,9⁃dehydropellito⁃rine(12),6⁃O⁃(E)⁃cinnamoyl⁃α/β⁃D⁃glucopyranoside(13),trans⁃3′,4′⁃diacetylkhellacton(14),3⁃methoxyl⁃4⁃O⁃β⁃D⁃glucopyranosyloxybenzoic acid methyl ester(15),euparone(16).Compounds 5,8 of collagen fiberⅣ,typeⅢcollagen,lamininm,compounds 11,14 on collagen fiberⅣ,typeⅢcollagen;compounds 2,7 on typeⅢcollagen;compounds 4,12 on collagen fiberⅣ,laminin have inhibition in vitro.CONCLUSION Except compound 3,all the compounds are isolated from this plant for the first time.Compounds 2,4-5,7-8,11-12 and 14 show different degrees of inhibition on renal interstitial fibrosis indexes.