金花茶叶醇提物通过调节胆固醇逆向转运关键蛋白的表达抑制动脉粥样硬化  

Ethanol extracts fromCamellia chrysantha(Hu)Tuyama leaves attenuated atherosclerosis via regulating the expressions of key proteins during cholesterol reverse transport

作　　者：农微[1] 陆宏浩 韦金锐 陈柏承 覃子洺 许思敏 卫智权[1] NONG Wei;LU Hong-hao;WEI Jin-rui;CHEN Bo-cheng;QIN Zi-ming;XU Si-min;WEI Zhi-quan(Guangxi University of Chinese Medicine,Guangxi Nanning 530200,China;Airport Campus of Affiliated Ruikang Hospital,Guangxi University of Chinese Medicine,Fusui County Hospital of Chinese Medicine,Guangxi Fusui 532100,China)

机构地区：[1]广西中医药大学,广西南宁530200 [2]广西中医药大学附属瑞康医院空港院区,扶绥县中医医院,广西扶绥532100

出　　处：《中国医院药学杂志》2021年第24期2519-2525,共7页Chinese Journal of Hospital Pharmacy

基　　金：广西自然科学基金青年基金项目(编号:2018GXNSFBA281207);广西中医基础研究重点实验室自主课题(编号:20-065-53-02)。

摘　　要：目的:探讨金花茶叶醇提物调节胆固醇逆向转运(RCT)关键蛋白细胞质膜微囊蛋白-1(caveolin-1)、清道夫受体B1(SR-B1)、A1型三磷酸腺苷结合盒转运体(ABCA1)、蛋白激酶A(PKA)的表达而抑制巨噬细胞向泡沫细胞衍变、拮抗动脉粥样硬化(AS)的潜在药理作用机制。方法:乙醇回流提取获得金花茶叶醇提物,制备金花茶叶醇提物含药大鼠血清。体外测试金花茶叶醇提物含药血清对巨噬细胞经典活化、吞噬氧化低密度脂蛋白(ox-LDL)并衍变为泡沫细胞以及caveolin-1、SR-B1、ABCA1、PKA表达的调节作用。高脂饲喂雄性ApoE-/-小鼠建立AS小鼠模型,体内测试金花茶叶醇提物对小鼠主动脉弓AS斑块形成以及内膜caveolin-1、SR-B1、ABCA1、PKA表达的调节作用。结果:10%金花茶叶醇提物含药血清显著抑制巨噬细胞经典活化,阻止其衍变为泡沫细胞,上调caveolin-1、SR-B1、ABCA1、PKA表达。金花茶叶醇提物显著上调AS小鼠主动脉内膜caveolin-1、SR-B1、ABCA1、PKA表达,抑制AS斑块形成。结论:金花茶叶醇提物可阻止巨噬细胞向泡沫细胞衍变,抑制AS斑块形成,可能与其上调RCT关键蛋白caveolin-1、SR-B1、ABCA1、PKA表达有关。OBJECTIVE To explore the regulation of ethanol extracts fromCamellia chrysantha(Hu)Tuyama leaves on the expressions of key proteins during reverse cholesterol transport(RCT),i.e.plasma membrane microcapsule protein-1(caveolin-1),scavenger receptor B1(SR-B1),type A1 adenosine triphosphate binding box transporter(ABCA1)and protein kinase A(PKA),as a potential pharmacological mechanism by which foam cell evolvement from macrophage and atherosclerosis(AS)would be attenuated.METHODS Ethanol extracts fromCamellia chrysantha(Hu)Tuyama leaves were purified by ethanol reflux.Ethanol extracts fromCamellia chrysantha(Hu)Tuyama leaves-containing rat sera was prepared.The regulations of ethanol extracts fromCamellia chrysantha(Hu)Tuyama leaves-containing rat serum on classical macrophage activation,foam cell evolvement after phagocytizing ox-LDL and expressions of caveolin-1,SR-B1,ABCA1,PKA were measured in vitro.The animal model of AS was established by male ApoE-/-mice with high-fat feeding.The regulatory effects of ethanol extracts fromCamellia chrysantha(Hu)Tuyama leaves on AS plaque formation and the expressions of caveolin-1,SR-B1,ABCA1,PKA in murine intima were detected in vivo.RESULTS The drug-contain sera not only significantly inhibited classical macrophage activation,but also prevented macrophages from evolving into foam cells.Also an up-regulation of caveolin-1,SR-B1,ABCA1 and PKA was observed.Ethanol extracts from Camellia chrysantha(Hu)Tuyama leaves demonstrated a marked up-regulation of caveolin-1,SR-B1,ABCA1 and PKA in aortic arch endomembrane of AS mice and attenuated AS plaque formation.CONCLUSION Ethanol extracts from Camellia chrysantha(Hu)Tuyama leaves can prevent macrophages from evolving into foam cells and attenuate AS plaque formation.It may be correlated with an up-regulation of caveolin-1,SR-B1,ABCA1 and PKA as the key proteins during RCT.

关 键 词：金花茶叶醇提物 胆固醇逆向转运 动脉粥样硬化 巨噬细胞 泡沫细胞 

分 类 号：R285[医药卫生—中药学]