PMID- 26929585 OWN - NLM STAT- PubMed-not-MEDLINE DCOM- 20160301 LR - 20200929 IS - 0973-1296 (Print) IS - 0976-4062 (Electronic) IS - 0973-1296 (Linking) VI - 11 IP - Suppl 3 DP - 2015 Oct TI - Selective Cytotoxicity and Pro-apoptotic Activity of Stem Bark of Wrightia tinctoria (Roxb.) R. Br. in Cancerous Cells. PG - S481-7 LID - 10.4103/0973-1296.168976 [doi] AB - BACKGROUND: Wrightia tinctoria (Roxb.) R. Br. is a widely available shrub in India used traditionally in various ailments, including cancer. However, the anticancer activity of the bioactive fractions has not been validated scientifically. OBJECTIVE: To investigate the anticancer potential of stem bark of W. tinctoria and establish its phytochemical basis. MATERIALS AND METHODS: The ethanol extract and subsequent fractions, petroleum ether, ethyl acetate, n-butanol, and aqueous were prepared by standard methods. In vitro cytotoxicity was determined in MCF-7 (breast) and HeLa (cervical) adenocarcinoma cells, and V79 (nontumor fibroblast) cells and apoptogenic activity in MCF-7 cells by acridine orange (AO)/ethidium bromide (EB) staining. Additionally, the antioxidant potential was evaluated using suitable methods. High-performance thin layer chromatography (HPTLC) analysis was performed for identification of active phytoconstituents. RESULTS: Petroleum ether and ethyl acetate fractions were most potent with IC50 values of 37.78 and 29.69 mug/ml in HeLa and 31.56 and 32.63 mug/ml in MCF-7 cells respectively in the sulforhodamine B assay. Comparable results were obtained in HeLa cells in 3-(4,5-dimethylthiazolyl-2-yl)-2,5-diphenyl tetrazolium bromide assay and interestingly, the fractions were found to be safe to noncancerous fibroblast cells. Both fractions induced significant (P < 0.05) apoptotic morphological changes observed by AO/EB staining. Moreover, extract/fractions exhibited excellent inhibition of lipid peroxidation with the ethyl acetate fraction being most active (IC50:23.40 mug/ml). HPTLC confirmed the presence of two anti-cancer triterpenoids, lupeol, and beta-sitosterol in active fractions. CONCLUSION: Extract/fractions of W. tinctoria exhibit selective cytotoxicity against cancerous cells that is mediated by apoptosis. Fractions are less toxic to noncancerous cells; hence, they can be developed as safer chemopreventive agents. SUMMARY: Petroleum ether and ethyl acetate fractions were most active and exhibited dose-dependent cytotoxicity in HeLa and MCF-7 cells.Fractions were relatively less toxic to non-tumor fibroblast cells demonstrating its selectivity to cancer cells.Fractions exhibited pro-apoptotic activity in MCF-7 cells in AO/EB staining.Lupeol and beta-sitosterol were identified as anticancer constituents by HPTLC. FAU - Chaudhary, Shilpee AU - Chaudhary S AD - Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka, India. FAU - Devkar, Raviraj Anand AU - Devkar RA AD - Department of Pharmacognosy, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka, India. FAU - Bhere, Deepak AU - Bhere D AD - Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka, India; Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Boston, MA 02114, USA. FAU - Setty, Manganahalli Manjunath AU - Setty MM AD - Department of Pharmacognosy, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka, India. FAU - Pai, Karkala Sreedhara Ranganath AU - Pai KS AD - Department of Pharmacognosy, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka, India. LA - eng PT - Journal Article PL - United States TA - Pharmacogn Mag JT - Pharmacognosy magazine JID - 101300403 PMC - PMC4745221 OTO - NOTNLM OT - anticancer OT - chemoprevention OT - high-performance thin layer chromatography OT - lupeol OT - beta-sitosterol EDAT- 2016/03/02 06:00 MHDA- 2016/03/02 06:01 PMCR- 2015/10/01 CRDT- 2016/03/02 06:00 PHST- 2016/03/02 06:00 [entrez] PHST- 2016/03/02 06:00 [pubmed] PHST- 2016/03/02 06:01 [medline] PHST- 2015/10/01 00:00 [pmc-release] AID - PM-11-481 [pii] AID - 10.4103/0973-1296.168976 [doi] PST - ppublish SO - Pharmacogn Mag. 2015 Oct;11(Suppl 3):S481-7. doi: 10.4103/0973-1296.168976.