摘要
蛋白质二硫键异构酶既能抑制肿瘤细胞凋亡,又能促进肿瘤细胞浸润转移,在肿瘤的发展进程中具有关键作用。为了研究中药莲子心是否对该酶活性有影响,该文首先对莲子心的化学成分进行了提取分离,得到12个单体化合物,其中N-甲基乌药碱、山柰酚、金圣草素-7-O-新橘皮糖苷和甘露醇为首次从该药材中分离得到。随后该文研究了莲子心中主要的生物碱成分N-甲基乌药碱、莲心碱、异莲心碱和甲基莲心碱对蛋白质二硫键异构酶活性的影响,首次发现它们均具有抑制蛋白二硫键异构酶活性的作用,其中N-甲基乌药碱活性最强(IC501.4μmol·L^(-1))。
Increasing evidence suggested that protein disulfide isomerase supported the survival and progression of several cancers. Nelumbinis Plumula is a Chinese traditional herb which showed antitumor activity. To find if the Nelumbinis Plumula affect protein di- sulfide isomerase activity, we studied its chemical constituents, and 12 monomeric compounds were isolated by means of solvent extrac- tion, silica gel column chromatography, preparative HPLC and recrystallization. Among them, N-methylcoclaurine, kaempferol, chry- soeriol-7-O-neohesperidoside and mannitol were obtained for the first time. Following, we tested the compounds inhibitory activity on protein disulfide isomerase. The results showed that N-methylcoclaurine, neferine, liensinine and isoliensinine could inhibit the activity of protein disulfide isomerase in vitro, their IC50values were 1.4, 2. 9, 4. 0 and 5.4 μmol · L-1 , respectively.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2017年第15期3004-3010,共7页
China Journal of Chinese Materia Medica
关键词
莲子心
生物碱
蛋白二硫键异构酶
抗肿瘤
Nelumbinis Plumula
alkaloid
protein disulfide isomerase
anti-tumor
