摘要
环烯醚萜苷在传统中药中分布广泛,具有抗炎等多种生物活性,也是中药中重要的一类质控成分。中药中常见的环烯醚萜苷分为九碳骨架环烯醚萜苷、十碳骨架环烯醚萜苷及裂环环烯醚萜苷3类。以3类环烯醚萜苷中15个受到广泛关注的代表性成分,包括京尼平苷、梓醇、龙胆苦苷等为对象,概括了近5年其抗炎功效及可能的相关机制,以期总结不同类型环烯醚萜苷成分的抗炎作用特点。通过对比结构和作用特点分析,发现这些环烯醚萜苷的抗炎作用多与核转录因子-κB(NF-κB)通路和丝裂原活化蛋白激酶(MAPK)通路相关,对肿瘤坏死因子-α(TNF-α)、白细胞介素-6(IL-6)、IL-1β这几个炎症因子均有明显的抑制效果。另外,少数具有降低诱导型一氧化氮合酶(i NOS)和环氧合酶-2(COX-2)的表达,通过NLRP3、Nrf2/HO-1、PI3K等通路发挥作用的特点。从构效关系来看,环烯醚萜苷中环戊烷上的双键、C-11取代基、开环后的成键方式均对其抗炎活性存在重要影响。
Iridoid glycosides are widely distributed in Chinese materia medica(CMM) with various biological activities such as anti-inflammation. They are also used as quality control constituents in some Chinese medicines. Iridoid glycosides are usually divided into nine-carbon skeleton iridoid glycoside type, ten-carbon skeleton iridoid glycoside type, and secoiridoid glycoside type. In this paper, 15 representative iridoid glycosides from three types which are received extensive attention(including geniposide, catalpol, gentiopicroside, etc) have been selected. Their anti-inflammatory effects and possible related mechanisms are summarized to find out the acting feature of different types. Through comparing the structures and function characteristics, it was concluded that the anti-inflammatory effects of iridoid glycosides were mostly related to NF-κB pathway and MAPK pathway. They have obvious inhibitory effects on TNF-α, IL-6, and IL-1β inflammatory factors, some of which could play a role by reducing the expression of i NOS and COX-2 in NLRP3, Nrf2/HO-1, PI3 K, and other pathways. From the structure-activity relationship, the double bond on the cyclopentane, the C-11 substituent and the bond formation after ring opening in iridoid glycosides all have important effects on its anti-inflammatory activities.
作者
毛高慧
张刘强
钱菲
陈凯先
许锦文
李医明
MAO Gao-hui;ZHANG Liu-qiang;QIAN Fei;CHEN Kai-xian;XU Jin-wen;LI Yi-ming(School of Pharmacy,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China;Institute of Interdisciplinary Integrative Medicine Research,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China)
出处
《中草药》
CAS
CSCD
北大核心
2019年第1期225-233,共9页
Chinese Traditional and Herbal Drugs
基金
上海市优秀学术带头人项目(16XD1403500)
国家自然科学基金项目(81673570)
上海市"中药药效物质"E-研究院项目
上海中医药大学预算内项目(2016YSN07)
