STUDI INDUKSI EKSTRAK PHYLLANTHUS NIRURI L. TERHADAP METABOLISME NEVIRAPINE PADA MIKROSOMAL HATI TIKUS WISTAR JANTAN

• Main Author: Rukmi Harumi, Anindita
• Format: Final Project
• Language: Indonesia
• Online Access: https://digilib.itb.ac.id/gdl/view/70330
• Institution: Institut Teknologi Bandung

Herbal therapies grow increasingly in the world. Consequently, herb-drug interactions may potentially occur. Meniran extracts have immunostimulant effects and antiviral activity in HIV-1 RT inhibition that can be used by HIV patients. This study was to evaluate induction effects of meniran extracts on nevirapine metabolism, an antiretroviral metabolized by cytochrome P450 enzymes (CYP450). Induction study of meniran extracts was performed using 3 groups of male wistar rats. Group I was control and did not received the extracts. Group II (n=3) dan Group II (n=3) received the extracts equivalent to human doses of 50 mg/day and 150 mg/day for 9 days. Liver was isolated followed by isolation of microsomes using differential centrifuge. In vitro incubation of microsomes and nevirapine 0.9; 1.88; 9.39; 18.78; 28.16; 37.55; 56.33; 75.10 ?M was performed for 5 min and remaining parent compounds were analyzed by HPLC. Km and Vmax values were calculated. Km and Vmax values for control were 207.4 ?M dan 6997 ?M.mg-1 protein.hr-1, respectively. Whereas, those values for induction groups decreased; 67.59 ?M dan 2128 ?M.mg-1 protein.hr-1 for Group II, respectively; and 26.5 ?M and 566.4 ?M.mg-1 protein.hr-1 for Group III, respectively. The decrease of Km and Vmax values indicated uncompetitive inhibition. In vitro study of meniran extracts did not show induction but rather un-competitive inhibition to enzymes metabolizing of nevirapine.