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本文对小檗碱及其5个类似物对体外缺糖缺氧再灌注PC12细胞的保护作用及其对COX-2的抑制作用进行了实验观察,并就它们的构效关系进行了分析。造模方法为缺糖缺氧4小时复灌24小时。以MTT法检测小檗碱及其类似物对细胞的保护作用。以实时定量PCR和Western blot方法检测COX-2的mRNA和蛋白的表达。结果表明,小檗碱及其类似物均能够对抗缺糖缺氧再灌所引起的细胞损伤、抑制COX-2的表达。小檗碱和小檗红碱作用最强,其最大有效剂量为0.31μg/mL,其最小有效剂量分别为0.02和0.04μg/mL。巴马汀作用较弱。R2和R3位的亚甲二氧基是小檗碱及其类似物的活性基团。而且R2,R3,R9和R10位的亚甲二氧基影响小檗碱及其类似物对COX-2的亲和力。R9位的羟基取代不影响其活性。
In this paper, berberine and its five analogues on the protective effect of hypoxic-reperfusion in vitro PC12 cells and its inhibitory effect on COX-2 were observed and their structure-activity relationship were analyzed. Modeling method for the lack of sugar 4 hours hypoxia reperfusion 24 hours. The protective effect of berberine and its analogues on the cells was detected by MTT assay. The mRNA and protein expression of COX-2 were detected by real-time PCR and Western blot. The results show that berberine and its analogues are able to fight cell injury caused by hypoxia and hypoxia and reperfusion and inhibit the expression of COX-2. Berberine and berberine the strongest role, the maximum effective dose of 0.31μg / mL, the minimum effective dose were 0.02 and 0.04μg / mL. Palmatine is weak. Methylenedioxy at the R2 and R3 positions is an active group of berberine and its analogs. Moreover, methylenedioxy groups at positions R2, R3, R9 and R10 affect the affinity of berberine and its analogs for COX-2. The hydroxyl substitution at position R9 does not affect its activity.