卵叶槲寄生化学成分体外抗HIV活性的初步研究  

Anti-HIV activities of chemical constituents from V. album L.var. meridianum Danser

作　　者：刘武青[1,2] 李晓莉[3] 王睿睿[1] 李阳[3,2] 杨柳萌[1] 杨永平[3] 郑永唐[1] 

机构地区：[1]中国科学院昆明动物研究所中国科学院和云南省动物模型与人类疾病机理重点实验室,昆明650223 [2]中国科学院研究生院,北京100039 [3]中国科学院昆明植物研究所民族植物学实验室,昆明650204

出　　处：《中国新药杂志》2010年第12期1017-1021,1025,共6页Chinese Journal of New Drugs

基　　金：国家重大新药创制科技重大专项(2009ZX09501-029);国家重点基础研究发展计划(973)(2009CB522306);国家科技重大专项“十一五”计划(2008ZX10005-005);中国科学院知识创新工程重要方向(KSCX1-YW-R-24,KSCX2-YW-R-185);云南省科技计划(2007BC006)资助课题;中国科学院人才培养计划“西部博士资助项目”

摘　　要：目的:探讨卵叶槲寄生化学成分的体外抗人免疫缺陷病毒(HIV)活性。方法:采用四甲基偶氮唑蓝法测定化合物的细胞毒性;细胞病变法检测化合物对HIV急性感染的抑制活性;HIV-1p24抗原ELISA方法检测化合物对慢性感染细胞中HIV复制的影响。计算化合物的抑制率和半数抑制浓度(EC50)。结果:多种卵叶槲寄生的化学成分具有体外抑制HIV复制的作用,特别是3,5,7,4′-四羟基-3′-甲氧基黄烷酮和圣草酚。3,5,7,4′-四羟基-3′-甲氧基黄烷酮在2～3μg·mL-1的浓度范围内对HIV-1和HIV-2复制的抑制率均≥50%,而对C8166细胞的半数细胞毒性浓度(CC50)>200μg·mL-1。圣草酚在低浓度(1.5～2.5μg·mL-1)时,对HIV-1和HIV-2复制的抑制率达50%,其对C8166细胞的CC50为43.40μg·mL-1。结论:卵叶槲寄生化学成分3,5,7,4′-四羟基-3′-甲氧基黄烷酮和圣草酚对HIV-1和HIV-2的体外复制均有不同程度的抑制作用。Objective：To investigate the activities of anti-HIV of chemical constituents from V.album L.var. meridianum Danser and provid the references for the further studies and development.Methods：MTT assay was used to determine the cytotoxicity of compounds. The anti-HIV activities on acute infection of chemical constituents were evaluated by cytopathic effect（CPE） assay. The inhibition of HIV-1 replication in chronically infected cells was evaluated by p24 antigen expression（ELISA method）. Results：Several compounds from V. album var. meridianum showed potent inhibition HIV replication. 3,5,7,4＇-tetrahydroxy-3＇-methoxyflavanone and eriodictyol had the potent anti-HIV-1 and HIV-2 activities with EC50 of 2-3 μg·mL^-1 and 1.5-2.5 μg·mL^-1,respectively. Meantime,no significant cytotoxicy was obtained on T lymphocytes cell lines C8166. Conclusion：Compounds 3,5,7,4＇-tetrahydroxy-3＇-methoxyflavanone and eriodictyol extracted from V. album L.var. meridianum have anti-HIV-1 and HIV-2 activities.

关 键 词：3 5 7 4′-四羟基-3′-甲氧基黄烷酮 圣草酚 卵叶槲寄生 抗HIV活性 

分 类 号：R965.1[医药卫生—药理学] R373[医药卫生—药学]