Department of Biochemistry, CCB, Federal University of Santa Catarina, Florianópolis, SC, Brazil.
Planta Med. 2011 Sep;77(14):1569-74. doi: 10.1055/s-0030-1270956. Epub 2011 Apr 6.
This study evaluated the hypolipidemic and antiobesity effects of phloroacetophenone (2',4',6'-trihydroxyacetophenone, THA) isolated from Myrcia multiflora and their relationship with triglyceride (TG) intestinal absorption and pancreatic lipase activity inhibition. The hypolipidemic effect of THA was evaluated by acute (Triton WR-1339 treatment) and chronic assay (high-fat diet treatment), the antiobesity effect was evaluated by chronic assay (high-fat diet treatment), while the inhibition of enzymatic activity of pancreatic lipase was measured in the intestinal tissue of mice treated with high olive oil concentration. In the acute assay, THA caused greater total cholesterol (37 %) and triglyceride (46 %) serum level reduction than lovastatin (32 and 1 %), a HMG-CoA reductase inhibitor or orlistat (26 and 34 %), a gastrointestinal lipase inhibitor. In addition, in the chronic assay with a high-fat diet, THA reduced cholesterol and triglyceride levels (32 and 61 %, respectively) while lovastatin showed a decrease of 35 and 49 %, respectively. THA also caused a reduction in weight gain very similar to orlistat (40 and 38 %, respectively) when the animals were submitted to a high-fat diet. Moreover, THA showed a stronger and continuous pancreatic lipase inhibitory activity when compared with orlistat, causing inhibition of this enzyme during 6 hours associated to a significant reduction of triglyceride serum levels. The IN VIVO antiobesity and hypolipidemic effects of THA may be partly mediated by delaying the intestinal absorption of dietary fat by inhibiting pancreatic lipase activity.
本研究评估了从桃金娘科植物中分离得到的对羟基苯乙酮(2',4',6'-三羟基苯乙酮,THA)的降血脂和抗肥胖作用及其与甘油三酯(TG)肠道吸收和胰腺脂肪酶活性抑制的关系。THA 的降脂作用通过急性(曲前列环素 WR-1339 处理)和慢性测定(高脂肪饮食处理)进行评估,抗肥胖作用通过慢性测定(高脂肪饮食处理)进行评估,而胰腺脂肪酶的酶活性抑制作用则在高橄榄油浓度处理的小鼠肠组织中进行测量。在急性测定中,THA 引起的血清总胆固醇(37%)和甘油三酯(46%)水平降低比洛伐他汀(32%和 1%),即 HMG-CoA 还原酶抑制剂或奥利司他(26%和 34%),一种胃肠道脂肪酶抑制剂更大。此外,在高脂肪饮食的慢性测定中,THA 降低胆固醇和甘油三酯水平(分别为 32%和 61%),而洛伐他汀分别降低 35%和 49%。当动物接受高脂肪饮食时,THA 还导致体重增加减少,与奥利司他非常相似(分别为 40%和 38%)。此外,与奥利司他相比,THA 表现出更强且持续的胰腺脂肪酶抑制活性,在 6 小时内抑制该酶,同时显著降低血清甘油三酯水平。THA 的体内抗肥胖和降血脂作用可能部分通过抑制胰腺脂肪酶活性来延迟膳食脂肪的肠道吸收来介导。