大黄的降血脂生物活性成分及作用机制研究进展

Research progress on the hypolipidemic bioactive components and mechanism of action of Rheum

中文关键词:  大黄  生物活性成分  降血脂  蒽酮类  芪类  机制

英文关键词:Rheum  bioactive components  hypolipidemic  anthraquinones  stilbenes  mechanism of action

中文摘要:

      大黄(Rheum)是蓼科(Polygonaceae)多年生草本植物, 是我国医药学领域应用最广泛的草药之一。越来越多的研究表明大黄中的蒽醌类、蒽酮类、芪类、糖类、鞣质类、黄酮类和苯丁酮苷类等可能是预防或治疗高脂血症及其并发症的有效生物活性成分。本文综述了大黄中主要化合物及其降血脂作用的机制, 主要从实验模型、剂量、作用和机制以及基本结构等对各种活性成分进行系统阐述。大黄中的主要降血脂生物活性成分可以分为蒽醌类、芪类、多糖和其他类等4类, 这些成分集中在抑制外源性脂类吸收、抑制内源性脂类合成、调控脂质的转运和代谢以及调节肠道菌群等方面上发挥降血脂作用, 主要涉及腺苷酸活化蛋白激酶(adenosine monophosphate-activated protein kinase, AMPK)、过氧化物酶体增殖物激活型受体(peroxisome proliferator activated receptor, PPAR)、胆固醇-7α-羟化酶(cholesterol-7α-hydroxylase, CYP7A1)、甾醇调节元件结合蛋白(sterol-regulatory element binding protein, SREBP)、低密度脂蛋白受体(low-density lipoprotein receptor, LDLR)、ATP结合盒转运体A1 (ATP-binding cassette protein A1, ABCA1)、人前蛋白转化酶枯草溶菌素9 (recombinant proprotein convertase subtilisin/kexin type 9, PCSK9)、尼曼—匹克C1型类似蛋白1 (niemann-pick type C1 Like 1, NPC1L1)等重要的降血脂作用靶点。本综述将为大黄的降血脂生物活性研究提供新的思路、借鉴与方法, 为开发安全、有效的降血脂功能性产品提供一定的理论基础和科学依据。

英文摘要:

      Rheum, a perennial plant of the Polygonaceae family, is one of the most widely used herbs in Chinese medicine. There is a growing body of research suggesting that anthraquinones, anthrone, stilbenes, sugars, tannins, flavonoids and phenylbutazones in Rheum may be effective bioactive components in preventing or treating hyperlipidemia and its complications. This review focused on main bioactive components of Rheum and their mechanisms of hypolipidemic effects. For each bioactive component, this paper summarized an overview of the experimental model, dosage, effects, and mechanisms, as well as the underlying chemical monomer structure. The main hypolipidemic bioactive components in Rheum can be divided into 4 categories: Anthraquinones, stilbenes, polysaccharides and others. The mechanisms of these components focus on effects such as inhibition of exogenous lipid absorption and of endogenous lipid synthesis, regulation of lipid transport and metabolism, and of intestinal flora to exert hypolipidemic effects. These mechanisms mainly involve important hypolipidemic targets of adenosine monophosphate-activated protein kinase (AMPK), peroxisome proliferator activated receptor (PPAR), cholesterol-7α-hydroxylase (CYP7A1), sterol-regulatory element binding protein (SREBP), low-density lipoprotein receptor (LDLR), ATP-binding cassette protein A1 (ABCA1), recombinant proprotein convertase subtilisin/kexin type 9 (PCSK9), and niemann-pick type C1 Like 1 (NPC1L1). This review will provide new ideas, references and methods for the study of hypolipidemic biological activity of Rheum, and provide theoretical and scientific basis for the development of safe and effective hypolipidemic functional products.