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Depside derivatives with anti-hepatic fibrosis and anti-diabetic activities from Impatiens balsamina L. flowers

机译:凤仙花的具有抗肝纤维化和抗糖尿病活性的Depside衍生物

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Eighteen compounds (1-18), seven new (3-9) and eleven previously reported (1, 2, and 10-18), were isolated from the flowers of Impatiens balsamina (Linn). The structures of the isolated compounds were elucidated using different spectroscopic methods, including NMR (1D and 2D), UV, IR, and HR-ESI-MS. Analysis of the bioassay results showed the compounds had notable anti-hepatic fibrosis activity against murine Hepatic Stellate Cells (t-HSC/CI-6) and anti-diabetics activity against a-glucosidase. Specifically, new compounds 7, 8, 9 showed significant inhibitory activity on t-HSC/CI-6 cells with IC50 values of 42.12, 109.2, and 34.04 mu g/mL respectively, while the IC50 values of positive control Silymarin and Fufang Biejia Ruangan Plan were 202.34 and 231.56 mu g/mL, respectively. In addition, compounds 2, 4, 7, 8, 10, 11, 17, and 18 exhibited excellent a-glucosidase inhibitory activity. Among these compounds, 7 exhibited the highest activity with an IC50 value of 0.72 mu g/mL, while the IC50 value of the positive control acarbose was 336 mu g/mL. This is the first study evaluating the anti-hepatic fibrosis and anti-diabetic activities of compounds isolated from the flowers of I. balsamina. (C) 2015 Elsevier B.V. All rights reserved.
机译:从凤仙花(Linn)的花中分离出十八种化合物(1-18),七种新化合物(3-9)和十一种先前报道的化合物(1、2和10-18)。使用不同的光谱方法,包括NMR(1D和2D),UV,IR和HR-ESI-MS,阐明了分离出的化合物的结构。生物测定结果的分析表明,该化合物对鼠肝星状细胞(t-HSC / CI-6)具有显着的抗肝纤维化活性,对α-葡萄糖苷酶具有抗糖尿病活性。具体而言,新化合物7、8、9对t-HSC / CI-6细胞显示出显着的抑制活性,IC50值分别为42.12、109.2和34.04μg / mL,而阳性对照Silymarin和Fufang Biejia Ruangan的IC50值计划分别为202.34和231.56μg / mL。另外,化合物2、4、7、8、10、11、17和18显示出优异的α-葡萄糖苷酶抑制活性。在这些化合物中,有7种表现出最高的活性,IC50值为0.72μg / mL,而阳性对照阿卡波糖的IC50值为336μg / mL。这是第一项评估从苦瓜I. balsina花中分离的化合物的抗肝纤维化和抗糖尿病活性的研究。 (C)2015 Elsevier B.V.保留所有权利。

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