《生命科学》 2022, 34(7): 821-829
五环三萜齐墩果烷型天然产物抗肿瘤活性研究进展
摘 要：
癌症是全球主要死因之一，也是阻碍人类期望寿命延长的重要因素，严重威胁了人类健康。五环三萜类化合物是具有多种生物活性的天然产物，分为齐墩果烷型、羽扇豆烷型、乌苏烷型。齐墩果烷型五环三萜已被证实具有多种生理活性，其中，抗癌和抗炎活性研究最多，该领域的广泛研究表明其抗癌作用由多种机制介导，因为它们调节多种分子靶点和信号通路，参与癌细胞增殖和存活。考虑到这类化合物的抗癌潜力，已经合成了许多半合成衍生物，旨在提高它们的治疗活性和药代动力学特性，并降低它们的毒性。该文总结了齐墩果烷型中齐墩果酸、甘草次酸、山楂酸等三种化合物对癌症的抑制作用、其衍生物的抗肿瘤活性以及与其他药物联用的作用机制，并对目前研究的不足做出展望，以期该类化合物在未来抗肿瘤治疗中发挥更大的作用。
通讯作者：伍春莲 , Email:wcl_xj@163.com
Abstract:
Cancer is one of the main causes of death in the world and is also an important factor hindering the extension of life expectancy, which poses a serious threat to human health. Pentacyclic triterpenoids as natural products, include oleanane-type, lupane-type, and ursane-type, and they all possess various biological activities. Oleanolane-type pentacyclic triterpenoids (OPT) have been confirmed to have a variety of physiological activities, mainly the anti-cancer and anti-inflammatory activities. The anti-cancer effects of OPT are mediated by multiple mechanisms including regulating molecular targets and signaling pathways and involving in cancer cell proliferation and survival. Therefore, considering the anti-cancer potential of these compounds, many semisynthetic derivatives have been synthesized, aiming at enhancing their therapeutic activity and pharmacokinetic properties, at the same time reducing their toxicity. The anti-cancer effects of oleanolic acid, glycyrrhizic acid, and maslinic acid, antitumor activities of their derivatives, and the mechanism in combination with other drugs were summarized, and the shortcomings of current research were presented. It is expected that these compounds will play a maximum role in anti-tumor therapy in the future.
Communication Author：WU Chun-Lian , Email:wcl_xj@163.com
