基于血清药物化学研究两色金鸡菊活性部位的降血脂活性成分

颜仁杰1,乐心逸1,于安伟2,孔德云1,吴 彤1*

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主办:上海医药工业研究院
   中国药学会
   中国化学制药工业协会
ISSN 1001-8255   CN 31-1243/R   ZYGZEA
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中国医药工业杂志 ›› 2016, Vol. 47 ›› Issue (11) : 1383. DOI: 10.16522/j.cnki.cjph.2016.11.010
中药与天然药物 Traditional Chinese Medicine & Natural Drug

基于血清药物化学研究两色金鸡菊活性部位的降血脂活性成分

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Anti-hyperlipidemic Components from Coreopsis tinctoria Based on Serum Pharmacochemistry Analysis

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摘要

以小鼠高血脂症为模型,筛选两色金鸡菊提取物,得到能显著降低血清中甘油三酯(TG) 和低密度脂蛋白(LDL-C)浓度的活性部位。对该活性部位进行血清药物化学研究,通过分析比较活性部位和含药血清样品,检测到含药血清中有12 个入血成分,其中6 个为代谢产物,6 个为原型成分。主要入血原型成分为异奥卡宁-7-O-β-D- 吡喃葡萄糖苷(1)、(Z)-6,7,3',4'- 四羟基橙酮-6-O-β-D- 吡喃葡萄糖苷(3) 和马里苷(4)。经金黄地鼠高血脂模型筛选,结果显示1 能显著降低动物血清中的TG、总胆固醇(CHOL) 和LDL-C 含量,4 能显著提升高密度脂蛋白(HDL-C) 水平。研究表明二氢黄酮类和查尔酮类化合物是两色金鸡菊中的降血脂活性成分。

Abstract

A hyperlipid diet-induced hyperlipidemic mice model was used to investigate the effects of Coreopsis tinctoria extract (CTE) on hyperlipidemia. It was observed that CTE could significantly decrease the triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C) levels. The chemical analysis of CTE and medicated serum samples, which were obtained from the rats administered with the bioactive component extract orally, was carried out in a HPLC system. Twelve transitional constituents (6 metabolites and 6 prototype constituents) into blood were detected and the main prototype constituents with anti-hyperlipidemic effects were isookanin-7-O-β-D-glucopyranoside (1), (Z)-6-O-β-D-glucopyranosyl-6,7,3',4'-tetrahydroxyaurone (3) and marein (4). After screening in hyperlipidemic golden hamster model, the results showed that compound 1 could significantly decrease the TG, serum total cholesterol (CHOL) and LDL-C levels in golden hamster serum, while compound 4 could significantly increase the high-density lipoprotein cholesterol (HDL-C) level. These findings suggested that flavanone and chalcone compounds were the antihyperlipidemic bioactive components of CTE.

关键词

两色金鸡菊 / 高血脂症 / 血清药物化学 / 活性成分

Key words

Coreopsis tinctoria / hyperlipidemia / serum pharmacochemistry / bioactive component

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颜仁杰1,乐心逸1,于安伟2,孔德云1,吴 彤1*. 基于血清药物化学研究两色金鸡菊活性部位的降血脂活性成分. 中国医药工业杂志. 2016, 47(11): 1383 https://doi.org/10.16522/j.cnki.cjph.2016.11.010
YAN Renjie1, LE Xinyi1, YU Anwei2, KONG Deyun1, WU Tong1*. Anti-hyperlipidemic Components from Coreopsis tinctoria Based on Serum Pharmacochemistry Analysis. Chinese Journal of Pharmaceuticals. 2016, 47(11): 1383 https://doi.org/10.16522/j.cnki.cjph.2016.11.010

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