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.
References
Adhikari, B.S., Babu, M.M., Saklani, P.L. and Rawat, G.S. (2010): Medicinal plants diversity and their conservation status in Wildlife Institute of India (WII) campus, Dehradun. Ethnobotanical Leaflets, 2010(1):46-83.
Devi, V.A., Arumugasamy, K.A., Shalimol, A., Kumar, R.N., Udhayasankar, M.R., Kokilavani, R. (2014): Anti-Inflammatory Activity of Smilax wightii fruit, Endemic A.DC.(Smilacaceaea) -An Endangered Medicinal Plant from the Nilgiris. J. Pharm. Bio. Res. 2(2):136-138.
Maheswari, P.U., Shalimol, A., Arumugasamy, K. (2014a): Free Radical Scavenging Activity of Smilax wightii A. DC. (Smilacaceae), an Endemic Medicinal Plant from Western Ghats. Int J Herb Med. 2(2):106–108.
Maheswari, P.U., Shalimol, A., Arumugasamy, K., Udhayasankar, U., Punitha, D. (2014b): Effect of methanolic extract of Smilax wightii A.Dc. on serum protein profile in streptozotocin induced diabetic rats. Int J Pharm Tech Res. 6(5):1870–1874.
Florento, L., Matias, R., Tuaño, E., Santiago, K., dela Cruz, F., Tuazon, A. (2012): Comparison of cytotoxic activity of anticancer drugs against various human tumor cell lines using in vitro cell-based approach. Int J Biomed Sci. 8(1): 76-80.
Walter, T.M., Justinraj, S., Swathi, K., Nandhini, V.S., Devi, S.G., Sanjana, G., Merish, S. (2017): Phytochemical analysis and Invitro Anticancer study of a Siddha formulation KKPN against Cervical Cancer. Siddha Papers. 12(3): 2-8.
Alami, N., Paterson, J., Belanger, S., Juste, S., Grieshaber, C.K., Leyland-Jones, B. (2007): Comparative analysis of xanafide cytotoxicity in breast cancer cell lines. British journal of cancer. 97(1): 58-64.
Imbert, T.F. (1998): Discovery of podophyllotoxins. Biochimie. 80(3): 207-222.
Moudi, M., Go, R., Yien, C.Y.S., Nazre, M. (2013): Vinca alkaloids. International journal of preventive medicine. 4(11):1231.
Wall, M.E., Wani, M.C., Cook, C.E., Palmer, K.H., McPhail, A.A., Sim, G.A. (1966): Plant antitumor agents. I. The isolation and structure of camptothecin, a novel alkaloidal leukemia and tumor inhibitor from camptotheca acuminata. Journal of the American Chemical Society. 88(16): 3888-3890.
Wani, M.C., Taylor, H.L., Wall, M.E., Coggon, P. and McPhail, A.T. (1971): Plant antitumor agents. VI. Isolation and structure of taxol, a novel antileukemic and antitumor agent from Taxus brevifolia. Journal of the American Chemical Society. 93(9): 2325-2327.
Pérard-Viret, J., Quteishat, L., Alsalim, R., Royer, J., Dumas, F. (2017): Cephalotaxus Alkaloids. In: Alkaloids: Chemistry and Biology. Elsevier Ltd, Academic Press.78: 205–352.
Kamal, A., Boehm, M.F., Burrows, F.J. (2004): Therapeutic and diagnostic implications of Hsp90 activation. Trends in molecular medicine. 10(6): 3-290.
Mahalingam, D., Swords, R., Carew, J.S., Nawrocki, S.T., Bhalla, K., Giles, F.J. (2009): Targeting HSP90 for cancer therapy. British journal of cancer. 100(10): 1523-1529.
Li, Y., Zhang, T., Schwartz, S.J., Sun, D. (2009): New developments in Hsp90 inhibitors as anti-cancer therapeutics: mechanisms, clinical perspective and more potential. Drug Resist Updat. 12(1-2): 17-27.
Chuu, C.P., Kokontis, J.M., Hiipakka, R.A., Liao, S. (2007): Modulation of liver X receptor signaling as novel therapy for prostate cancer. Journal of Biomedical science. 14(5): 543-553.
Fukuchi, J., Kokontis, J.M., Hiipakka, R.A., Chuu, C.P., Liao, S. (2004): Antiproliferative effect of liver X receptor agonists on LNCaP human prostate cancer cells. Cancer research. 64(21): 7686-7689.
Vedin, L.L., Lewandowski, S.A., Parini, P., Gustafsson, J.Å., Steffensen, K.R. (2009): The oxysterol receptor LXR inhibits proliferation of human breast cancer cells. Carcinogenesis. 30(4): 575-579.
Vigushin, D.M., Dong, Y., Inman, L., Peyvandi, N., Alao, J.P., Sun, C., Ali, S., Niesor, E.J., Bentzen, C.L., Coombes, R.C. (2004): The nuclear oxysterol receptor LXRα is expressed in the normal human breast and in breast cancer. Medical Oncology. 21(2): 123-131.
Lin, C.Y., Vedin, L.L., Steffensen, K.R. (2016): The emerging roles of liver X receptors and their ligands in cancer. Expert opinion on therapeutic targets. 20(1): 61-71.
Ju, X., Huang, P., Chen, M., Wang, Q. (2017): Liver X receptors as potential targets for cancer therapeutics. Oncology letters. 14(6): 7676-7680.
Gong, H., Guo, P., Zhai, Y., Zhou, J., Uppal, H., Jarzynka, M.J., Song, W.C., Cheng, S.Y., Xie, W. (2007): Estrogen deprivation and inhibition of breast cancer growth in vivo through activation of the orphan nuclear receptor liver X receptor. Molecular Endocrinology. 21(8): 1781-1790.
Christopherson II, K.W., Landay, A. (2009): Liver X receptor α (LXRα) as a therapeutic target in chronic lymphocytic leukemia (CLL). Journal of leukocyte biology. 86(5): 1019.
Matsui, Y., Yamaguchi, T., Yamazaki, T., Yoshida, M., Arai, M., Terasaka, N., Honzumi, S., Wakabayashi, K., Hayashi, S., Nakai, D., Hanzawa, H. (2015): Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl) benzoates as liver X receptor agonists. Bioorganic & medicinal chemistry letters. 25(18): 3914-3920.
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