ANTINEOPLASTIC EFFICACY OF SMILAX WIGHTII A.DC. (SMILACACEAE) AND ITS STEROIDAL SAPOGENINS: IN VITRO TO IN SILICO APPROACHES
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Smilax wightii, Cytotoxicity, Sarsasapogenin, Diosgenin, HSP-90 alpha, LXR-alphaAbstract
. Competency of plant metabolites and derivatives as antineoplastic drugs has been validated by modern medicine and the screening of flora for anticancer agents is crucial in drug discovery. Smilax wightii A.DC. (Smilacaceae) is an ethnomedicinal plant endemic to Western Ghats of India. The methanolic extract of various plant parts were subjected to investigation of antiproliferative potential. Dalton’s lymphoma Ascites (DLA), Ehrlich-Lettre ascites carcinoma (EAC), rat spleen, mouse fibroblast (L929) and human lung cancer (A549) cell lines were employed in the analysis. Stem extract exhibited high inhibitory property at 200 µg/mL on both DLA and EAC cell lines with 92.43±0.176 and 90.42±0.272% cell death respectively. In the spleen cell line root extract recorded the lowest cytotoxicity. The leaf and root extracts were subjected to MTT assay in human lung cancer (A549) and mouse Fibroblast (L929) cell lines to determine their anticancer property. Root recorded better apoptotic effect on the mouse fibroblast cell line and lung cancer cell line when compared to leaf extract. Molecular docking of the compounds Sarsasapogenin and Diosgenin present in in the plant to potential anticancer target proteins viz HSP-90 alpha and LXR-alpha verified their anticancer potential. Sarsasapogenin could bind to the active site of HSP-90 alpha with the low binding energy of -9.33Kcal/Mol and Diosgenin interacted with the active site of LXR-alpha with low binding energy of -6.52Kcal/Mol. These molecules are among the many bioactive principles that are ground to the anticancer activity of the crude extract and are eligible to be prospective antineoplastic drugs.
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