基于“病证-效应-生物样本分析”方法的桑寄生补肝肾强筋骨功效物质及归经研究

A Research of Effective Chemicals of Taxillus Chinensis Danser on Osteoporosis and Channel Tropism Based on Disease-Effect-Bioanalysis

目的:建立与桑寄生功效相对应的骨质疏松模型,观察桑寄生补肝肾强筋骨功效物质及其在大鼠体内分布与归经的关系。方法:采用维甲酸制造骨质疏松模型大鼠模型,观察桑寄生水煎液药效。同时以萹蓄苷、槲皮苷、芦丁为指标成分,对含药组织进行分析检测,观察其体内分布及代谢时间,研究功效相关物质的组织分布与归经的关系。结果:桑寄生水煎液能明显提高骨质疏松模型大鼠左股骨骨重、骨重/骨长、骨重/骨直径等指标,且能降低大鼠血清中骨钙素(OT)、碱性磷酸酶(ALP)含量。大鼠体内桑寄生指标成分的分析结果显示,芦丁仅在胃中有少量分布,萹蓄苷在组织中AUC0?t大小顺序为胃>肾>脑>小肠>大肠>肝>肺,体内维持时间长短顺序为肾=胃>脑>大肠>小肠=脾>肝>心>肺>血清。槲皮苷在组织中AUC0?t大小顺序为肾>胃>肝>心>肺>脾>小肠>大肠>脑,体内维持时间长短顺序为肾=胃=脑=肺=肝=脾=心>大肠>血清>小肠。结论:桑寄生水煎液可对抗维甲酸致大鼠骨质疏松,具有补肝肾、强筋骨作用;萹蓄苷、槲皮苷为桑寄生补肝肾、强筋骨代表成分;萹蓄苷、槲皮苷在大鼠体内分布与桑寄生归肾经的传统认识一致。

This study aimed to observe the effect of Taxillus on osteoporotic rats and investigate effective chemicals of Taxillus, in order to find out the relationships between their body distribution and the channel tropism of Taxillus. The osteoporotic rat models were established through retinoic acid administration to observe the efficacy of the water solution of Taxillus. Besides, taking rutin, avicularin and quercetin as indexes, organs of all rats were prepared to measure their distributions and metabolism before analyzing the correlation between body distribution of effective chemicals and channel tropism of Taxillus. It was found that Taxillus solution significantly improved weight（W）, W / length（L） and W / diameter（D） of osteoporotic rats, and reduced the contents of osteocalcin（OT） and alkaline phosphatase（ALP）. Rutin, one of the indexes in this study, was seldom in the stomach. AUC0-t of avicularin showed its distribution in stomach, kidney, brain, small intestine, large intestine, liver, lung from most to least in content. The metabolism results showed that avicularin stayed longer time in stomach and kidney than that in brain, large intestine, small intestine and spleen, liver, heart, lung, and plasma. And AUC0-t of quercetin showed its distribution in kidney, stomach, liver, heart, lung, spleen, small intestine, large intestine and brain from most to least in content. Quercetin kept longer time in kidney, stomach, liver, heart, spleen and brain than that in large intestine, plasma and small intestine. In conclusion, water solution of Taxillus was effective in the treatment of osteoporotic rats. Avicularin and quercetin, as the main substance of Taxillus, functioned in nourishing liver and kidney. Their distributions in rats were consistent with the channel tropism of Taxillus.