大黄药材两种化学型对金葡菌生长代谢热动力学变化的影响  

Antimicrobial activity and chemical differences between the two chemotypes of rhubarbs

作　　者：张学儒[1,2] 王伽伯[1] 肖小河[1] 刘塔斯[2] 楚笑辉[1,2] 周灿平[1,2] 金城[1] 

机构地区：[1]解放军中药研究所解放军第302医院,北京100039 [2]湖南中医药大学药学院,湖南长沙410208

出　　处：《药学学报》2010年第9期1144-1148,共5页Acta Pharmaceutica Sinica

基　　金："重大新药创制"科技重大专项资助项目(2009ZX09502-022);国家自然科学基金资助项目(30973947);国家公益性行业科研专项基金资助项目(200807020)

摘　　要：大黄药材可根据酸水解后所含大黄酸和大黄酚在总蒽醌中所占比例高低分为大黄酸型和大黄酚型两种化学型。为了确证大黄药材两种可能的化学型是否具有生物活性或药效学差异, 本文采用微量量热法比较了两种化学型大黄药材对金葡菌的抑制作用。通过调整加样量, 使所有药材作用于金葡菌的总蒽醌量相等, 以凸显大黄药材不同化学型抑菌活性的差异性。结果显示, 金葡菌在大黄酸型药材作用下第一指数生长期速率常数 (k1) 显著低于大黄酚型药材, 提示大黄酸型药材对金葡菌的抑制作用明显强于大黄酚型药材。但大黄酸型药材的抑菌活性与大黄酸含量之间未发现明显相关性, 提示大黄药材对金葡菌的抑制作用除与化学型有关外, 可能还受到其他未知特征成分的影响, 且该成分在大黄药材中的积累规律可能与大黄酸相似。本文采用微量量热法证明了两种化学型大黄药材的抑菌活性存在客观差异, 佐证了大黄药材可根据大黄酸和大黄酚的比例关系区分化学型的合理性, 亦为从化学角度制订大黄药材的商品规格标准提供了参考。Through our pre-investigation and literature analysis, it was found that rhubarb could be categorized into two types, chrysophanol-type and rhein-type, based on the proportion of the two constituents in the total content of anthraquinones after acid hydrolysis. In this paper, the antimicrobial activities of chrysophanol-type and rhein-type rhubarbs against Staphylococcus aureus were compared with microcalorimetric analysis, in order to illustrate the bioactive differentiability between the two chemotypes. For the aim to display the distinction of chrysophanol and rhein percentage in total anthraquinones, the sampling volume was regulated to make the total anthraquinones equivalent, thus, the antimicrobial difference was only attributed to the difference of chemotypes. The results indicated that the antimicrobial difference between the two chemotypes was confirmable labeled at the biothermokinetic parameters of S. aureus growth affected by the rhubarb samples. The growth rate constant （k1） of the first exponential phase for the growth of S. aureus affected by the rhein-type rhubarb was significantly lower than that of chrysophanol-type （P 0.01）, which suggested stronger antimicrobial activity of rhein-type rhubarb than that of chrysophanol-type. However, the antimicrobial activities of rhein-type rhubarbs were not positively correlated to the contents of rhein. It suggested that the antimicrobial activity of rhubarb might be related to some unknown components which were of same accumulating pattern of rhein. The findings in present study provided some experimental evidence on categorizing rhubarb into two chemotypes through the difference of antimicrobial activity on S. aureus by microcalorimetric analysis and, further, offered references to revision of the commercial specification of rhubarb from chemical view.

关 键 词：大黄药材 化学型 抑菌 微量量热法 

分 类 号：R932[医药卫生—生药学]