Andriani Yosie, Tengku-Muhammad Tengku Sifzizul, Mohamad Habsah, Saidin Jasnizat, Syamsumir Desy Fitrya, Chew Guat-Siew, Abdul Wahid Mohd Effendy
Institute of Marine Biotechnology, University of Malaysia Terengganu, Kuala Terengganu 21030, Terengganu, Malaysia.
Chemistry Department, Faculty of Mathematics and Natural Sciences, Universitas Bengkulu (UNIB), Bengkulu 38371, Indonesia.
Molecules. 2015 Mar 9;20(3):4410-29. doi: 10.3390/molecules20034410.
In vitro and in vivo studies of the activity of Phaleria macrocarpa Boerl (Thymelaeaceae) leaves against the therapeutic target for hypercholesterolemia were done using the HDL receptor (SR-BI) and hypercholesterolemia-induced Sprague Dawley rats. The in vitro study showed that the active fraction (CF6) obtained from the ethyl acetate extract (EMD) and its component 2',6',4-trihydroxy-4'-methoxybenzophenone increased the SR-BI expression by 95% and 60%, respectively. The in vivo study has proven the effect of EMD at 0.5 g/kgbw dosage in reducing the total cholesterol level by 224.9% and increasing the HDL cholesterol level by 157% compared to the cholesterol group. In the toxicity study, serum glutamate oxalate transaminase (SGOT) and serum glutamate pyruvate transaminase (SGPT) activity were observed to be at normal levels. The liver histology also proved no toxicity and abnormalities in any of the treatment groups, so it can be categorized as non-toxic to the rat liver. The findings taken together show that P. macrocarpa leaves are safe and suitable as an alternative control and prevention treatment for hypercholesterolemia in Sprague Dawley rats.
利用高密度脂蛋白受体（SR-BI）和高胆固醇血症诱导的斯普拉格-道利大鼠，对大果木竹子（瑞香科）叶针对高胆固醇血症治疗靶点的活性进行了体外和体内研究。体外研究表明，从乙酸乙酯提取物（EMD）中获得的活性组分（CF6）及其成分2',6',4-三羟基-4'-甲氧基二苯甲酮分别使SR-BI表达增加了95%和60%。体内研究证明，与胆固醇组相比，剂量为0.5 g/kgbw的EMD可使总胆固醇水平降低224.9%，高密度脂蛋白胆固醇水平升高157%。在毒性研究中，观察到血清谷氨酸草酰乙酸转氨酶（SGOT）和血清谷氨酸丙酮酸转氨酶（SGPT）活性处于正常水平。肝脏组织学也证明任何治疗组均无毒性和异常，因此可归类为对大鼠肝脏无毒。综合研究结果表明，大果木竹子叶作为斯普拉格-道利大鼠高胆固醇血症的替代控制和预防治疗方法是安全且合适的。
