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巨花马兜铃(Scheff.)Boerl 果实水提物在体内和体外增强 LDL 受体和 PCSK9 的表达。

Phaleria macrocarpa (Scheff.) Boerl fruit aqueous extract enhances LDL receptor and PCSK9 expression in vivo and in vitro.

机构信息

Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, University Putra Malaysia, 43400 UPM, Serdang, Selangor, Malaysia.

出版信息

J Ethnopharmacol. 2011 Sep 1;137(1):817-27. doi: 10.1016/j.jep.2011.06.041. Epub 2011 Jul 5.

DOI:10.1016/j.jep.2011.06.041
PMID:21763412
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Phaleria macrocarpa (Scheff.) Boerl (Pm) has been shown to reduce cholesterol level in vitro and in vivo experiment.

AIM OF THE STUDY

This study investigated the effects of Pm fruit on weight control and mechanistic basis of its anti-hypercholesterolemic effect in both in vivo and in vitro.

MATERIALS AND METHOD

In the in vivo study, thirty six male Sprague Dawley were randomized to six groups. Five groups were induced into hypercholesterolemia by giving 3% cholesterol enriched-diet for 52 days while one group acted as control. The rats were then treated with Pm extract (0, 20, 30 and 40 mg/ml) or simvastatin for 84 days. The following parameters were determined: (1) body weight, (2) blood lipid profile (total cholesterol, triglyceride, HDL and LDL) and (3) hepatic LDL receptor (160 kDa and 120 kDa) and PCSK9 proteins. In the in vitro study, HepG2 cells were cultured in serum-free RPMI supplemented with 0.2% BSA with or without LDL and in the presence of Pm extract (0, 0.1, 2, 40 and 1,000 μg/ml) or simvastatin (4.60 μg/ml) for 24h. The abundance of both LDL receptor and PCSK9 proteins and mRNA were investigated.

RESULTS

Pm extract significantly (P<0.05) reduced body weight gain, total cholesterol, triglycerides, HDL LDL levels and upregulated hepatic LDL receptor as well as PCSK9 proteins of hypercholesterolemic rats. These results were supported by studies in HepG2 cells whereby Pm extract also significantly upregulated both LDL receptor and PCSK9 at protein and mRNA levels.

CONCLUSION

This study enhances the potential usage of Pm fruit for controlling the body weight of obese people and for treating hypercholesterolemia.

摘要

植物学相关性

已证实 Phaleria macrocarpa(Scheff.)Boerl(Pm)具有降低胆固醇水平的体外和体内实验作用。

研究目的

本研究旨在调查 Pm 果实对体重控制的影响及其在体内和体外抗高胆固醇血症作用的机制基础。

材料与方法

在体内研究中,将 36 只雄性 Sprague Dawley 大鼠随机分为六组。五组给予富含 3%胆固醇的饮食 52 天,诱导产生高胆固醇血症,一组作为对照。然后,这些大鼠用 Pm 提取物(0、20、30 和 40mg/ml)或辛伐他汀治疗 84 天。测定以下参数:(1)体重,(2)血脂谱(总胆固醇、甘油三酯、HDL 和 LDL)和(3)肝 LDL 受体(160kDa 和 120kDa)和 PCSK9 蛋白。在体外研究中,将 HepG2 细胞在无血清 RPMI 中培养,添加 0.2%BSA,有或无 LDL,并存在 Pm 提取物(0、0.1、2、40 和 1000μg/ml)或辛伐他汀(4.60μg/ml)24 小时。研究了 LDL 受体和 PCSK9 蛋白和 mRNA 的丰度。

结果

Pm 提取物显著(P<0.05)降低了高胆固醇血症大鼠的体重增加、总胆固醇、甘油三酯、HDL 和 LDL 水平,并上调了肝 LDL 受体和 PCSK9 蛋白。HepG2 细胞的研究结果也支持了这一点,Pm 提取物也显著上调了 LDL 受体和 PCSK9 蛋白和 mRNA 的水平。

结论

本研究增强了 Pm 果实控制肥胖人群体重和治疗高胆固醇血症的潜在用途。

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