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五环三萜类共前药的结构与活性。 综述。

Structure and Activity of Pentacyclic Triterpenes Codrugs. A Review.

机构信息

Department of Organic Chemistry, Pharmaceutical Faculty, Poznan University of Medical Sciences, Grunwaldzka 6, 60-780 Poznan, Poland.

出版信息

Mini Rev Med Chem. 2021;21(12):1509-1526. doi: 10.2174/1389557521666210105110848.

DOI:10.2174/1389557521666210105110848
PMID:33402080
Abstract

Triterpenes are a wide and important group of compounds that have several promising pharmacological properties, such as hepatoprotective, anti-inflammatory, anti-HIV, antioxidant, or anticancer activities. Such potent substances can be successfully incorporated in more complex chemical systems e.g. codrugs or pro-drugs that have a better pharmacological profile. The codrug is connected with a drug formation pathway to chemically cohere at least two drug molecules to improve positive therapeutic efficiency or decrease side effects. The codrug can be cleaved in the organism to generate effective compounds previously used as substrates. This article presents an overview of codrugs that consist of pentacyclic triterpene moiety that is chosen as a basic codrug moiety due to their wide range of vital activities and another drug molecule fragment. It was found that triterpenoid codrugs are characterized by a wide range of biological activities. However, most of them have anticancer potency.

摘要

三萜类化合物是一类广泛而重要的化合物,具有多种有前途的药理学特性,如保肝、抗炎、抗 HIV、抗氧化或抗癌活性。这些有效物质可以成功地整合到更复杂的化学系统中,例如前药或前药,它们具有更好的药理学特性。前药与药物形成途径相连,通过化学结合至少两种药物分子来提高积极的治疗效果或降低副作用。前药可以在体内裂解,生成以前用作底物的有效化合物。本文概述了由五环三萜部分组成的前药,由于其广泛的生命活动和另一种药物分子片段,五环三萜部分被选为基本前药部分。研究发现,三萜类前药具有广泛的生物学活性。然而,它们中的大多数具有抗癌活性。

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