A Novel Triterpene From Erica Miranjiana with Potential Anti-Tubercular Activity
摘要
The research aims to isolate a plant-based anti-TB agent from the dried leaves of Ericae miranjiana, an endemic medicinal plant of Mulanje Mountain, that may be more effective and safer, thus providing an adjunct or alternative treatment to existing medications to treat multidrug-resistant tuberculosis.
MethodologyColumn chromatography was used to isolate the compound of interest from 80% methanol crude extract, followed by characterization by infrared spectroscopy (IR), high-resolution mass spectrometry (HRMS), and nuclear magnetic resonance (NMR) spectroscopic methods. Anti-TB activity of the compound was determined using the Resazurin Microtiter Assay (REMA) Plate method, while synergy with first-line TB drugs was determined using the Fractional Inhibitory Concentration Index (FICI). Its toxicity and drug likeness were determined using several online servers. The biosynthetic pathway of the compound was predicted using the AI-based Biosynthesis Navigator for Natural Products platform.
ResultsThe research identified a compound, 27-hydroxymethyl-3β,28-dihydroxylup-14,20-diene, showing possible activity against TB (MIC of 32 µg/ml) and synergistic effects when tested with rifampicin, isoniazid, and ethambutol. The compound showed a good ADMET profile, but the potential hepatotoxicity leads to additional caution. Its good gastrointestinal absorption and bioavailability score (0.55) indicate it has promising pharmacokinetic properties.
ConclusionThese results suggest that the E. miranjiana derived triterpene can be a very effective lead substance for developing novel anti-TB medications. It is necessary to conduct additional research to confirm tuberculosis (TB) efficacy and investigate its other medicinal properties.
Graphical Abstract