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穿心莲内酯:一种用于生成结构和生物多样性二萜的天然产物模板。

Andrographolide: A natural product template for the generation of structurally and biologically diverse diterpenes.

机构信息

Department of Chemistry, Sri Sathya Sai Institute of Higher Learning, Prasanthi Nilayam, 515134, Puttaparthi, A.P., India.

Department of Chemistry, Sri Sathya Sai Institute of Higher Learning, Prasanthi Nilayam, 515134, Puttaparthi, A.P., India.

出版信息

Eur J Med Chem. 2019 Aug 15;176:513-533. doi: 10.1016/j.ejmech.2019.05.022. Epub 2019 May 11.

Abstract

From times immemorial, natural products have played an important role in the management of human health. Andrographis paniculata, belonging to the family Acanthaceae and its constituents are reported to possess a wide range of biological properties such as anti-cancer, anti-diabetic, anti-inflammatory, anti-bacterial, anti-malarial, anti-hepatitis, anti-HIV, anti-atherosclerosis, hepatoprotective, FXR antagonist, and α-glucosidase inhibition. Andrographolide (1), is identified as the major bioactive constituent of the plant. Promising biological properties of the major constituent Andrographolide (1) along with structural amenability for facile semi-synthetic modifications have led to the generation of structurally diverse bioactive labdane diterpenes by several research groups. The promising biological activities exhibited by these semi-synthetic derivatives have further kindled interest and the continued research is evidenced through publications, patents and could possibly lead to the development of Andrographolide based medicines in future. The present review aims at compiling and discussing various semi-synthetic derivatives of Andrographolide in relation to their biological properties and their mechanisms of action.

摘要

自古以来,天然产物在人类健康管理中发挥了重要作用。穿心莲属于爵床科,其成分据报道具有广泛的生物活性,如抗癌、抗糖尿病、抗炎、抗菌、抗疟疾、抗肝炎、抗 HIV、抗动脉粥样硬化、保肝、FXR 拮抗剂和α-葡萄糖苷酶抑制作用。穿心莲内酯(1)被确定为该植物的主要生物活性成分。主要成分穿心莲内酯(1)具有有前途的生物学特性,并且结构适合进行易于进行的半合成修饰,这导致了几个研究小组生成了结构多样的生物活性贝壳杉烷二萜。这些半合成衍生物表现出有前途的生物学活性,进一步激发了人们的兴趣,并通过出版物和专利得到了持续的研究,这有可能导致未来基于穿心莲内酯的药物的开发。本综述旨在编译和讨论穿心莲内酯的各种半合成衍生物与其生物活性及其作用机制的关系。

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