Evaluation of herbal extracts for alpha glucosidase inhibition and cytochrome P450 3A4 modulation.

Diabetes mellitus (DM) is one of the chronic non-communicable diseases and has been rapidly increasing globally. Alpha glucosidase is an important enzyme that hydrolyzes polysaccharides into monosaccharides before being absorbed into the bloodstream. The alpha glucosidase inhibitors, such as acarbose are expensive and have several adverse effects. The use of herbal products to prevent or treatment of disease is becoming popular. There are many herbal products that can reduce blood sugar levels. However, taking herbal products with anti-DM medicines may cause herb-drug interactions that affect either the pharmacokinetics or pharmacodynamics of the drugs, leading to adverse effects or ineffective treatment. The aim of this study is to examine the effect of herbal extracts on alpha-glucosidase activity and the level of cytochrome P450 3A4 (CYP3A4) by using HepaRG as a model. Three herbs that reported blood glucose-lowering activity were selected including Moringa oleifera, Momordica charantia, and Morus alba. All herbs were extracted with 95% ethanol and tested for their in vitro alpha glucosidase inhibitory activity. The results showed that M. alba extract exhibits the highest activity (IC50= 83.75 µg/mL). Then, the extracts were evaluated for their cytotoxicity on the HepaRG cell line. All extracts showed no cytotoxicity at concentrations up to 250 µg/mL. The sub-cytotoxic concentration of each extract was selected to test for the effect on the CYP3A4 enzyme. The results showed that only M. alba extract elevated the level of CYP3A4, while the others slightly reduce the level of CYP3A4. However, this is a preliminary study that the major compounds of each extract must be isolated and evaluated in the future. [ABSTRACT FROM AUTHOR]