Cardiovascular, antihyperlipidemic and antioxidant effects of oleanolic and ursolic acids in experimental hypertension
Cardiovascular, antihyperlipidemic and antioxidant effects of oleanolic and ursolic acids in experimental hypertension
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DOI：
10.1078/094471103321659807
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发表时间：
2003-03-01
期刊：
影响因子：
7.9
通讯作者：
Shode, FO
中科院分区：
文献类型：
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作者：
Somova, LO;Nadar, A;Shode, FO
在Dahl盐敏感（DSS）和胰岛素抵抗（IR）的遗传性高血压大鼠模型上研究了98%纯油酸（OA）和熊果酸（UA）的心血管（收缩压、舒张压、心率）、抗高血压（甘油三酯、总胆固醇和脂蛋白组分）、抗氧化（谷胱甘肽过氧化物酶- GPx和超氧化物歧化酶- SOD）、利尿/利尿和降血糖活性。OA和UA均表现出低毒性，LC_（50）分别为0.10和0.95 mg/ml。尽管两种三萜类化合物均无直接消肿作用，但以每日剂量60 mg/kg b.w.给药6周后，腹腔注射，他们阻止了严重高血压的发展。抗高血压作用归因于其强效利尿-利钠-利钠活性;直接心脏效应（心率分别下降34%和32%）;抗高血压（LDL和甘油三酯降低两倍以上）;抗氧化剂（GPx分别提高12%和10%; SOD分别升高12%和22%）和降血糖（血糖分别降低20%和50%）作用。除抗高血压作用外，上述OA和UA的其他体内抗高血压作用均为首次报道，其潜在机制目前正在研究中。
Cardiovascular (systolic and diastolic blood pressure, heart rate), antihyperlipidemic (tryglycerides, total cholesterol and lipoprotein fractions), antioxidant (glutathione peroxidase - GPx, and superoxide dismutase - SOD), diuretic/saluretic and hypoglycemic activity of 98% pure oleanolic (OA) and ursolic (UA) acid were studied in Dahl salt-sensitive (DSS), insulin resistant rat model of genetic hypertension. Both OA and UA displayed low toxicity, with LC50 0.10 and 0.95 mg/ml, respectively. Although both triterpenoids did not have direct hypotensive effect, after 6-week application in a daily dose 60 mg/kg b.w., i.p., they prevented the development of severe hypertension. The antihypertensive effect was attributed to their potent diuretic-natriuretic-saluretic activity; direct cardiac effect (heart rate decrease by 34% and 32%, respectively); antihyperlipidemic (more than two times decrease of LDL and triglycerides); antioxidant (GPx increase by 12% and 10%, respectively; SOD increase by 12% and 22%, respectively), and hypoglycemic (blood glucose decrease by 20% and 50%, respectively) effects on the DSS rats. Except for the antihyperlipidemic effects, the other described above in vivo antihypertensive effects of OA and UA are reported for the first time and the underlying mechanisms are currently under investigation.