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Antihyperglycemic agents from Ammannia multiflora

机译:百日草的降血糖药

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The serial chromatographic separation of chloroform and n-butanol fractions of Ammannia multiflora resulted in the isolation and characterization of 4- hydroxy-α-tetralone (1) and 3,3'-(2 R,5R)-tetrahydrofuran-2,5-diyldiphenol (ammaniol, 2). Compound 1 was chemically modified into six semi-synthetic acyl and aryl derivatives (1A - 1F). The isolated compounds 1 and 2 along with semi-synthetic derivatives 1A - 1F were evaluated for in vitro antihyperglycemic activity employing 2-deoxyglucose uptake by L-6 rat muscle cell lines. The results indicated that both the isolates, as well as derivatives (1A - 1F), have the property to stimulate glucose uptake. Ammaniol (2) increased glucose uptake significantly (64.8%), while one of the aryl derivatives of 1, 4-O-(3,4,5- trimethoxybenzoyl)-α-tetralone (1D), showed potent antihyperglycemic activity and increased glucose uptake by 94.6%, even more than rosiglitazone (88.8%). Further, since 1D possesses better antihyperglycemic activity than rosiglitazone (standard), this might be a new safer antidiabetic drug of herbal origin.
机译:多花Ammannia的氯仿和正丁醇馏份的连续色谱分离导致4-羟基-α-四氢萘酮(1)和3,3'-(2 R,5R)-四氢呋喃-2,5-的表征二基二酚(苯甲醇,2)。将化合物1化学修饰为六个半合成的酰基和芳基衍生物(1A-1F)。利用L-6大鼠肌肉细胞系对2-脱氧葡萄糖的摄取,对分离的化合物1和2以及半合成衍生物1A-1F进行了体外抗高血糖活性的评价。结果表明,分离物和衍生物(1A-1F)均具有刺激葡萄糖吸收的特性。 Ammaniol(2)显着提高了葡萄糖摄取(64.8%),而1,4-O-(3,4,5-三甲氧基苯甲酰基)-α-四氢萘酮(1D)的芳基衍生物之一显示出强效的降血糖活性并增加了葡萄糖吸收率为94.6%,甚至超过罗格列酮(88.8%)。此外,由于1D具有比罗格列酮(标准品)更好的降血糖活性,因此这可能是一种更安全的草药来源的抗糖尿病药物。

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