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天山堇菜中的黄酮醇苷及其他酚类化合物及其抗补体活性。

Flavonol glycosides and other phenolic compounds from Viola tianshanica and their anti-complement activities.

作者信息

Qin Yan, Wen Quan, Cao Jie, Yin Chengle, Chen Daofeng, Cheng Zhihong

机构信息

a Department of Pharmacognosy , School of Pharmacy, Fudan University , Shanghai , China and.

b Zhongshan Hospital, Fudan University , Shanghai , China.

出版信息

Pharm Biol. 2016 Jul;54(7):1140-7. doi: 10.3109/13880209.2015.1055635. Epub 2015 Jun 17.

Abstract

CONTEXT

Viola tianshanica Maxim. (Violaceae) is a perennial herb distributed in Central Asia, especially in the Xinjiang Uygur Autonomous Region (XUAR) of China. Preliminary study showed that the ethanol extract of the herb exhibited the anti-complement activity against the classical pathway, but the active components responsible for this capacity remain unknown and are yet to be studied.

OBJECTIVE

The objective of this study was the isolation and identification of the anti-complement constituents of V. tianshanica.

MATERIALS AND METHODS

The ethyl acetate and n-butanol fractions from the ethanol extract of V. tianshanica were purified. The structures of the isolates were identified by spectroscopic methods, and comparing their spectral data with those reported in the literature. All the isolates (0.02-2.50 mg/mL) were evaluated for their anti-complement activity against the classical and alternative pathways.

RESULTS

Twenty-one phenolic compounds including 15 flavonol O-glycosides (1-15), one flavone 6,8-di-C-glycoside (16), one flavone aglycone (17), and four phenolic acid derivatives (18-21) were isolated and identified. Bioassay showed that 11 compounds inhibited the classical pathway and the alternative pathway with CH50 and AP50 values of 0.113-1.210 mM and 0.120-1.579 mM, respectively. Preliminary mechanistic study using complement-depleted sera demonstrated that 1 acted on C1q, C2, C4, and C9 components, 16 on C1q, C4, and C5, and 21 on C1q, C3, C4, and C9.

CONCLUSION

All isolated compounds except 1 and 10 were reported for the first time from V. tianshanica. Compound 16 is the first flavone C-glycoside isolated from the herb. Flavonol O-glycosides and phenolic acids contributed the anti-complement activity of the herb.

摘要

背景

天山堇菜(堇菜科)是一种多年生草本植物,分布于中亚地区,尤其是中国新疆维吾尔自治区。初步研究表明,该草药的乙醇提取物对经典途径具有抗补体活性,但其负责此活性的成分仍不清楚,有待进一步研究。

目的

本研究旨在分离和鉴定天山堇菜的抗补体成分。

材料与方法

对天山堇菜乙醇提取物的乙酸乙酯和正丁醇部位进行纯化。通过光谱方法鉴定分离物的结构,并将其光谱数据与文献报道的数据进行比较。评估所有分离物(0.02 - 2.50 mg/mL)对经典途径和替代途径的抗补体活性。

结果

分离并鉴定了21种酚类化合物,包括15种黄酮醇O-糖苷(1 - 15)、1种黄酮6,8-二-C-糖苷(16)、1种黄酮苷元(17)和4种酚酸衍生物(18 - 21)。生物活性测定表明,11种化合物抑制经典途径和替代途径,其CH50和AP50值分别为0.113 - 1.210 mM和0.120 - 1.579 mM。使用补体缺失血清进行的初步机制研究表明,化合物1作用于C1q、C2、C4和C9成分,化合物16作用于C1q、C4和C5,化合物21作用于C1q、C3、C4和C9。

结论

除化合物1和10外,所有分离得到的化合物均为首次从天山堇菜中报道。化合物16是首次从该草药中分离得到的黄酮C-糖苷。黄酮醇O-糖苷和酚酸是该草药抗补体活性的主要成分。

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