Abstract

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.

Highlights

  • Hypercholesterolemia is defined as a condition where the cholesterol level in human blood is higher than mg/dL

  • The in vivo study proved the effect of EMD at 0.5 g/kgbw dosage in reducing total cholesterol levels by

  • 224.9% and increasing the High-density lipoprotein (HDL) cholesterol level by 157% compared to a cholesterol group after days of treatment

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Summary

Introduction

Hypercholesterolemia is defined as a condition where the cholesterol level in human blood is higher than mg/dL. The role of SR-BI is crucial in order to allow HDL to remain functional to transport the plasma cholesterol away from the blood vessels to the liver to be metabolized [2,5,6]. Previous studies have reported the anticancer activity of P. macrocarpa leaves against HeLa [8] and myeloma cells [9]. To reduce cholesterol levels (hypocholesterolemia) and the mechanism of action of this activity remains uninvestigated, an in vitro study was done to evaluate the mechanism of action of. P. macrocarpa leaves extract on reducing cholesterol levels (hypocholesterolemia) by looking at the expression of SR-BI. The SGOT/SGPT activity and histology profiles of the liver were explored in this study to investigate the toxicity of the extract

Cytotoxicity Property
In Vitro Study
Total Cholesterol Levels
The HDL Cholesterol Level
SGOT and SGPT Activity
Histological Analysis
Experimental Section
Isolation and Structure Elucidation
Cytotoxicity Study by MTT Assay
Transfection of the Chimeric Reporter Plasmid into the HepG2 Cell Line
Treatment of the Transfected Cells with Sample
In Vivo Study
Statistical Analysis
Conclusions

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