摘要
目的研究姜黄素甲氧基水解及酚羟基酯化后的结构修饰物调血脂、抗脂质过氧化作用和对脂代谢相关酶类活性的影响,初步比较其构效关系,以期寻找到结构比姜黄素更适配的化合物,用于调血脂。方法用盐酸水解姜黄素甲氧基获得姜黄素水解物(HCur);用丁二酸酐酯化姜黄素酚羟基获得姜黄素酯化物(ECur);高脂膳食喂饲Wistar大鼠,建立食饵性高脂血症模型,用姜黄素(curcumin)、HCur和ECur进行实验性治疗,给药3周后处死动物,测定血清和肝脏总胆固醇(total cholester-ol,TC)、甘油三酯(triglyceride,TG)和血清高密度脂蛋白(high density lipoprotein cholesterol,HDL-C)含量,计算低密度脂蛋白(low density lipoprotein cholesterol LDL-C)含量,同时测定肝素化血浆总脂解酶(post heparin total activity,PHTA)、脂蛋白脂酶(lipoprotein lipase,LPL)和肝脂酶(hepatic lipase,HL)的活性及血清丙二醛(malondialdehyde,MDA)含量。结果①姜黄素能降低血清和肝脏TC、TG、LDL-C和MDA含量,升高血清HDL-C含量,提高PHTA活性。②HCur能降低TC、LDL-C、TG和MDA含量,能显著提高PHTA与LPL活性。③ECur仅具降LDL-C作用。结论HCur可降低肝脏和血清脂质及血清MDA含量,尤其能提高TG代谢相关酶活性,而ECur仅能降低LDL-C含量,其他活性均不显著,提示姜黄素结构上的酚羟基在降血脂中起重要作用。
OBJECTIVE To study the effects of the modified curcumin derivatives on regulating serum level of lipids and anti-lipid peroxidation,and their relationship between structures and activities. METHODS Hydrolyzed curcumin （HCur） was obtained by hydrolyzing the methoxyl from curcumin. Esterfied curcumin （ECur） was obtained by esterfying the phenolic hydroxyl of curcumin. The hyperlipidemic rat models were established by feeding Wistar rats with high lipid dieL Curcumin, HCur and ECur were then admin- istrated to the rats for experimental treatment. The levels of total cholesterol （TC） ,triglyceride （TG） and HDL-C in serum and liver were all determined after 3 weeks. The level of LDL-C was calculated. The activities of post heparin total activity （PHTA） ,lipoprotein lipase （ LPL）, hepatic lipase （HL） and malondialdehyde （MDA） were all measured. RESULTS ①Curcumin decreased the levels of TC,TG and LDL-C in serum and liver,increased the level of HDL-C and the activity of PHTA. ②HCur decreased the levels of TC, LDL-C,TG and MDA in serum,increased the activity of PHTA. ③ECur only decreased the level of LDL-C. CONCLUSION The resuits indicate that HCur obviously decrease the lipid in serum and liver and increase the activity of lipase involved in TG metabolization,while ECur could only decrease the level of LDL-C. It indicates that the phenolic hydroxyls played an important role in decreasing lipids.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2007年第10期737-739,共3页
Chinese Pharmaceutical Journal
基金
浙江省自然科学基金资助项目(202015)
关键词
萎黄素结构修饰物
脂蛋白脂酶
肝脂酶
高血脂大鼠
the modified curcumin derivatives
lipoprotein lipase （LPL）
hepatic lipase （HL）
hyperlipidemic rats
