Anticancer cytotoxic activity of pentane-2, 4-dione extracted from the leaves of Cordia sebestena Ragunathan Adhithya, Ravi Lokesh, Krishnan Kannabiran* Department of Biomedical Sciences, School Biosciences and Technology, VIT University, Vellore, Tamil Nadu, India *Corresponding Author E-mail: kkb@vit.ac.in
Online published on 24 August, 2018. Abstract Cervical cancer is a menace to women in the under developed and developing countries. With the population on the rise and with the cervical cancer incidence ever increasing, there is a commensurate need to develop more and more potential anticancer compounds. The aim of the present study was to isolate and to identify the anticancer cytotoxic lead compound from Cordia sebestena leaves. Aqueous, petroleum ether and ethyl acetate extracts prepared from the Cordia sebestena leaves were assessed for their anti-proliferative activity on cervical cancer cells (HeLa) using MTT assay. The active lead present in the petroleum ether extract was separated using preparatory TLC. The structure of the active compound was elucidated by spectroscopic studies using GC-MS, NMR and FT-IR. Docking studies were also performed with the lead compound and cancer target protein using Auto Dock 4.2. Anti-inflammatory of the lead was also performed by LPS induced nitric oxide inhibition assay. Petroleum ether extract showed the IC50 value of 250μg/ml in HeLa cells. Pure compound was identified as pentane-2, 4-dione. Pentane-2, 4-dione demonstratedan IC50 value of 10μg/ml on HeLa cells. In-Silico molecular docking studies demonstrated that Pentane-2, 4-dione showed high-affinity interaction with Kras protein with the least binding energy of-5.15Kcal/mol and 124.37μM as inhibition constant. Pentane-2, 4-Dione (10μg/ml) showed a 47% reduction in nitric oxide production in LPS induced raw macrophages. Based on results, it can be concluded that the anticancer cytotoxic activity of the lead compound pentane-2, 4-dione from C. sebestena is due to its inhibition of Kras protein. Top Keywords Cervical cancer, Cordia sebestena, HeLa Cells, Kras protein, Pentane-2, 4-dione. Top |