中国中药杂志

2015, v.40(12) 2420-2427

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分子烙印-活性筛选结合评价桂枝茯苓胶囊主要成分活性贡献度研究
Study on contribution of main components in Guizhi Fuling capsule based on molecular imprinting technique and activity screening

曹泽彧;丁玥;苏真真;李娜;曹亮;丁岗;王振中;萧伟;
CAO Ze-yu;DING Yue;SU Zhen-zhen;LI Na;CAO Liang;DING Gang;WANG Zhen-zhong;XIAO Wei;Jiangsu Kanion Pharmarceutical Co. ,Ltd.;State Key Laboratory of New-tech for Chinese Medicine Pharmaceutical Process;

摘要(Abstract):

为了明确桂枝茯苓胶囊治疗原发性痛经、盆腔炎和子宫肌瘤的主要药效成分,该研究基于分子烙印技术将桂枝茯苓胶囊中主要成分梯度敲除(分别敲除10%,30%,50%,70%,90%,100%)后,分别在离体子宫收缩、LPS诱导RAW264.7释放TNF-α、小鼠脾淋巴细胞(SPL)增殖及子宫肌瘤细胞增殖模型上考察桂枝茯苓胶囊活性的变化情况。结果表明,1梯度敲除芍药苷、丹皮酚和苦杏仁苷,桂枝茯苓胶囊抑制离体子宫收缩作用逐步减弱;2梯度敲除没食子酸、桂皮醛、五没食子酰葡萄糖和茯苓多糖,桂枝茯苓胶囊抑制TNF-α释放作用逐步减弱;3梯度敲除没食子酸、芍药苷、桂皮醛、槲皮素和茯苓多糖,桂枝茯苓胶囊促SPL细胞增殖作用逐渐减弱;4梯度敲除芍药苷、丹皮酚、五没食子酰葡萄糖和白芍苷,桂枝茯苓胶囊制剂体外抑制子宫肌瘤细胞的作用逐渐减弱。该研究提示,上述成分可能是桂枝茯苓胶囊发挥治疗原发性痛经、盆腔炎和子宫肌瘤作用的重要活性基础。
To clarify the active components in Guizhi Fuling capsule in treatment of intrinsic dysmenorrhea,pelvic inflammation and hysteromyoma,main components were gradually knocked out from the capsules,the effects of knockout capsules on uterine contraction,TNF-α secretion,murine splenocytes( SPL) and hysteromyoma cells proliferation were evaluated,respectively. The inhibition of capsules on uterine contraction was weakened by gradient knockout of paeoniflorin,paeonol,and amygdalin. The suppression of capsulte on TNF-α secretion was reduced by gradient knockout of gallic acid,cinnamaldehyde,pentagalloylglucose,and pachyman. The promotion of SPL cells proliferation was reversed by gradient knockout of gallic acid,paeoniflorin,cinnamaldehyde,quercetin,and pachyman. The depression of capsules on hysteromyoma cells proliferation was attenuated by gradient knockout of paeoniflorin,paeonol,pentagalloylglucose,and albiflorin. In conclusion,the compounds mentioned-above could be the key active basis of Guizhi Fuling capsule in treatment of intrinsic dysmenorrhea,pelvic inflammation and hysteromyoma.

关键词(KeyWords): 桂枝茯苓胶囊;分子烙印技术;子宫收缩;TNF-α;SPL细胞;子宫肌瘤细胞
Guizhi Fuling capsule;molecular imprinting technique;uterine contraction;TNF-α;SPL cells;hysteromyoma cells

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Keywords:

基金项目(Foundation): 国家“重大新药创制”科技重大专项(2013ZX09402203)

作者(Author): 曹泽彧;丁玥;苏真真;李娜;曹亮;丁岗;王振中;萧伟;
CAO Ze-yu;DING Yue;SU Zhen-zhen;LI Na;CAO Liang;DING Gang;WANG Zhen-zhong;XIAO Wei;Jiangsu Kanion Pharmarceutical Co. ,Ltd.;State Key Laboratory of New-tech for Chinese Medicine Pharmaceutical Process;

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