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目的:利用植物悬浮细胞体系对莪二酮进行结构改造研究。方法:采用生物转化技术和天然药物化学手段,分离转化产物单体,并利用波谱学手段对转化产物进行结构鉴定,并利用MTT法对转化产物的抗肿瘤活性进行了评价。结果:分离并鉴定了5个转化产物,分别为1β,10α-环氧基莪二酮(2),3α-羟基-莪二酮(3),3β-羟基-莪二酮(4),1α,10β-环氧基-11-羟基莪二酮(5)和2β-羟基-莪二酮(6)。结论:桔梗悬浮细胞对于莪二酮具有良好的转化能力,可以利用其作为植物反应器对莪二酮进行结构改造,以获得水溶性更好或活性更佳的衍生物。
OBJECTIVE: To study the structural modification of curdione by plant suspension cell system. Methods: The biotransformation technology and natural medicine chemistry were used to separate the monomers of the transformation products. The structures of the transformed products were identified by spectroscopic methods. The antitumor activity of the transformed products was evaluated by MTT assay. RESULTS: Five transformation products were isolated and identified as 1β, 10α-epoxydimorphine (2), 3α-hydroxy-radadione (3), 3β- , 10β-epoxy-11-hydroxyfetadione (5) and 2β-hydroxy-didorphone (6). CONCLUSION: Platycodon grandiflorum suspension cells have good transformation ability for meso-dione, and they can be used as plant reactor for structural modification of meso-dione to obtain better water-soluble or more active derivatives.