目的:探讨紫苏粗提物体外对酶抑制剂的作用,初步阐明其对代谢综合征的药效物质基础.方法:测定紫苏粗提物中黄酮及酚酸含量,探明与酶抑制有关的活性成分.通过体外实验,以抑制率为指标,测定紫苏粗提物对不同酶活性的抑制作用,以IC50为指标评价抑制活性.结果:紫苏粗提物中黄酮含量0.3098(mg/mg),总酚酸含量58.59(mg/g).紫苏对α-淀粉酶抑制的IC50值为0.273(mg/mL),对黄嘌呤氧化酶的IC50值为0.244(mg/mL),对胰脂肪酶的IC50值为0.347(mg/mL),对乙酰胆碱酯酶的IC50值为0.018(mg/mL).结论:紫苏粗提取对四种酶都有一定的抑制活性,且呈现剂量-效应关系.初步阐明其治疗代谢综合征的药效物质基础为黄酮.可将紫苏中黄酮类化合物进一步开发利用.

Objective: The research is to explore the enzyme inhibition of Perilla crude extract, and to preliminarily elucidate the pharmacological substance basis of them on hyperglycemia, hyperuric acid and hyperlipidemia. Methods: The content of flavonoids and phenolic acid in UV extract was determined and showed the active components associated with enzyme inhibition. In vitro experiments, the inhibition of Perilla extracts on different enzyme activity was determined and the inhibitory activity was evaluated by IC50. Molecular docking was used to predict the targets of Perilla crude extract on pancreatic lipase and amylase inhibition. Results: Flavone content in the crude UV extract was 0.309 8 mg/mg, and the total phenolic acid content was 58.59 mg/g. The IC50 values of Perilla crude extractd for α-amylase, xanthine oxidase, pancreatic lipase and acetylcholinesterase were 0.273, 0.244, 0.347 and 0.018 mg/mL, respectively.Apigenin-5-O-β-D-glucosine, xyrhinin-7-diglucosotide, apigenin-7-glucosine, cannol-3-O-ruassin, rosemary acid, rutin and others were the effective active components of perilla crude extracts. Conclusion: The Perilla crude extracts all have certain inhibitory activities on four enzymes, and presents a dose-effect relationship.

Aim To explore the effects of Clausena-mide(Clau) on hippocampus cyclooxygenase-2 (COX-2) mRNA and protein expressions in diabetic rats. Methods The diabetic rat model was produced by injecting streptozotocin (STZ,48 mg·kg-1). After 3 months,the COX-2 gene and protein expressions in hippocampus of diabetic rats were detected by RT-PCR and immunohistochemistry respectively. Results ① The results of RT-PCR showed that the expression of COX-2 mRNA in hippocampus of diabetic group rats increased significantly (P0.01),however,the expression of COX-2 mRNA in the hippocampus of the rats in clau treatment groups (50,25 mg·kg-1) decreased significantly (P0.01).② The results of immunohistochemistry showed that the protein expression of COX-2 in hippocampus of diabetic group rats increased significantly (P0.01),but Clau could inhibit the expressions of COX-2(P0.01).Conclusion Clausenamide can significantly inhibit COX-2 mRNA and protein expressions in hippocampus,which may account for the protective effects.