Cytotoxicity and molecular docking studies on Phytosterols isolated from Polygonum hydropiper L

Publication date: Available online 13 November 2018Source: SteroidsAuthor(s): Muhammad Ayaz, Abdul Sadiq, Abdul Wadood, Muhammad Junaid, Farhat Ullah, Nadir Zaman KhanAbstractBased on our previous studies on cytotoxic potentials of Polygonum hydropiper L, two steroidal compounds beta-sitosterol and stigmasterol were isolated from the most active fraction and were subjected to cell lines cytotoxicity. Isolated compounds were tested against HeLa, MCF-7 and NIH/3T3 cell lines following MTT assay. Furthermore, the compounds were also docked against tyrosine kinase enzyme to predict the binding mode of phytosterols in the active sites of the enzyme. Beta-sitosterol exhibited considerable cytotoxicity against NIH/3T3, HeLa and MCF-7 cell with 67.05 ±2.08, 79.63 ±2.34 and 71.50 ±1.57 % lethality respectively at 1 mg/ml concentration. Median inhibitory concentrations calculated from dose response curve against NIH/3T3, HeLa and MCF-7 cells were 440, 170 and 200 µg/ml respectively. Stigmasterol was more effective against MCF-7 and NIH/3T3 cells by killing 87.50 and 81.45 % cancerous cells respectively at 1mg/ml concentration. Stigmasterol showed 77.25% cyctotoxicity against HeLA cells at 1mg/ml concentration in MTT assay. The IC50 values for HeLA, MCF-7 and NIH/3T3 cells were 170, 60 and 140 µg/ml respectively. In docking studies, the docking score for beta-sitosterol and stigmasterol were -7.266 and -4.89 respectively. The binding energies for beta-sitosterol and stigmasterol we...
Source: Steroids - Category: Drugs & Pharmacology Source Type: research