原人参二醇型皂苷活性代谢物Compound K药理活性的研究进展  

Progress in pharmacological actions of ginsenoside compound K,an active metabolite of protopanaxadiol type saponins

作　　者：李相鹏[1] 王鹏[1] 李英霞[2] 

机构地区：[1]中国海洋大学医药学院合成药物化学实验室,山东青岛266003 [2]复旦大学药学院药物化学系,上海201203

出　　处：《中国药理学与毒理学杂志》2011年第1期97-101,共5页Chinese Journal of Pharmacology and Toxicology

基　　金：国家自然科学基金资助项目(30701046)~~

摘　　要：人参皂苷Compound K〔20-O-β-D-葡萄糖基-20(S)-原人参二醇,CK〕是原人参二醇型人参皂苷在人体内主要吸收形式和药效实体。近年来,CK的药理活性研究又有了新进展:①CK可通过活化胱天蛋白酶8直接或通过线粒体途径间接地激活胱天蛋白酶3,诱导肿瘤细胞凋亡;下调基质金属蛋白酶9基因的表达,抑制肿瘤细胞的转移;②可通过下调多种炎症因子如白细胞介素-4(IL-4),IL-6,肿瘤坏死因子α等及环氧合酶2与一氧化氮合酶的表达而发挥抗炎、抗过敏和神经保护作用;③可阻断ATP敏感性K+离子通道,促进胰岛素分泌,增强组织胰岛素敏感性,抑制糖异生,促进糖酵解,对胰岛素依赖性糖尿病表现出良好的疗效;④可上调核苷切除修复相关蛋白基因的表达,减少紫外线引起的DNA损伤,防止皮肤老化等。本文重点对近几年有关CK的药理活性及其作用机制研究新进展进行综述。Ginsenoside compound K（CK）,20-O-β-（D-glucopyranosyl）-20（S）-protopanaxadiol,is a major form of protopanaxadiol type saponins absorbed by the human body after oral administration,and a real component that mediates pharmacologic actions.Recently,new progress has been made in studies on pharmacological actions：① CK can activate caspase 8,which plays a key role in CK-stimulated apoptosis via activation of caspase 3 directly or indirectly through mitochondria pathway and can regulate the metastasis and invasiveness of tumor cells by down-regulating metalloproteinase 9 gene expression;② CK can reduce expression levels of NO synthase and cyclooxygenase-2 and inhibit secretion of some pro-inflammatory cytokines like interleukin 4（IL-4）,IL-6 or tumor necrosis factor-α,which are responsible for its anti-inflammatory,anti-allergic,and neuro-protective activities;③ CK can enhance the insulin secretion by blocking the ATP sensitive K＋ channel,improve insulin sensitivity,and shift glucose metabolisim from hepatic glucose production to hepatic glucose utilization in the liver,suggesting that CK be a therapeutic reagent for type 2 diabetic patients;④ CK can prevent the ultraviolet radiation induced skin damage by up-regulating nucleotide excision repair gene expression.

关 键 词：原人参二醇皂苷 COMPOUND K 药理学活性 

分 类 号：R962[医药卫生—药理学]