Chemopreventive Potential of Calotropis gigantea Root Fraction on MCF-7 Cells: In Vitro and In Silico Study
Abstract
Cancer remains a major global health issue due to its high mortality rate. Chemotherapy, though commonly used, often causes severe side effects by damaging both cancerous and healthy cells. Therefore, safer and more selective chemopreventive agents from natural sources are needed. This study aims to evaluate the chemopreventive potential of the ethanol fraction of biduri root (EFBR, Calotropis gigantea L.) through in vitro and in silico approaches. Phytochemical screening was used to identify bioactive compounds. Molecular docking using AutoDock Vina assessed calotropin’s interaction with Bcl-2 and HER-2 proteins. Antioxidant activity was measured by the DPPH method, and cytotoxic activity was tested on MCF-7 breast cancer cells and normal Vero cells using the MTT assay. EFBR was found to contain cardiac glycosides, flavonoids, terpenoids, saponins, and tannins. Docking results showed strong binding of calotropin to Bcl-2 (-9.3 kcal/mol) and HER-2 (-8.1 kcal/mol). EFBR showed weak antioxidant activity (IC₅₀: 518.93 μg/mL) but moderate cytotoxicity against MCF-7 (IC₅₀: 159.80 μg/mL), with low toxicity on Vero cells (IC₅₀: 2703.61 μg/mL) and a high selectivity index (SI: 16.91). These results indicate that EFBR has potential as a selective chemopreventive agent against breast cancer.
Keywords: Calotropis gigantea L., molecular docking, MTT assay, DPPH, MCF-7.
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Adams, J.M. and Cory, S., 2007, The Bcl-2 apoptotic switch in cancer development and therapy, Oncogene, 26(9), 1324–1337.
Andarina, R. and Djauhari, T., 2017, Antioksidan dalam Dermatologi, Jurnal Kedokteran dan Kesehatan, 4(1), 39–48.
Chandrawat, P. and Sharma, R.A., 2016, The Genus Calotropis : An Overview on Bioactive Principles and their Bioefficacy, Research Journal of Recent Sciences, 5(1), 61–70.
Depamede, S.N. and Rosyidi, A., 2009, Penghambatan Proliferasi Limfosit Mencit Balb/c oleh Ekstrak Testis Sapi Bali: Peran TGF-β, Media Peternakan, 32(2), 318–103.
Doyle, A. and Griffiths, J.B., 2000, Cell dan Tissue Culture for Medical Research, John Willey & Sons LTD.
Faradilla, M. and Maysarah, H., 2019, Potensi Biduri (Calotropis gigantea (L.) WT Aiton) sebagai Tanaman Obat (Prospect of Biduri (Calotropis gigantea (L.) WT Aiton) as Medicinal Plant), Ilmu Kefarmasian Indonesia, 17(2), 246–250.
Febriansah, R. and Dewayanti, I.A., 2021, Chemopreventive Activity of Clinacanthus nutans L. Ethyl Acetate Fraction on Breast Cancer Cells Line, Proceedings of the 4th International Conference on Sustainable Innovation 2020–Health Science and Nursing (ICoSIHSN 2020), 33, 520–527.
Globocan, 2022, Number of cases in 2022. https:// gco.iarc.fr/today/data/factsheets/popula-tions/360-indonesia-fact-sheets.pdf
Li, Y., Yao, J., Han, C., Yang, J., Chaudhry, M.T., Wang, S., et al., 2016, Quercetin, inflammation and immunity, Nutrients, 8(3), 167.
Loibl, S. and Gianni, L., 2017, HER2-positive breast cancer, The Lancet, 389(10087), 2415–2429.
Moasser, M.M., 2007, The oncogene HER2: its signaling and transforming functions and its role in human cancer pathogenesis, Oncogene, 26, 6469–6487.
Nussbaumer, S., Bonnabry, P., Veuthey, J-L., and Fleury-Souverain, S., 2011, Analysis of anticancer drugs : A review, Talanta, 85(5), 2265–2289.
Pai, V.V, Shukla, P., and Kikkeri, N.N., 2014, Antioxidants in dermatology, Indian Dermatology Online Journal, 5(2), 210-214.
Rafiqah, R., Mastura, M., and Hasibuan, M.P., 2019, Uji Toksisitas Fraksi Etanol Tanaman Obat yang Digunakan Masyarakat Menggunakan Metode Brine Shrimp Lethality Test, Katalis: Jurnal Penelitian Kimia dan Pendidikan Kimia, 2(1), 14–20.
Remesh, A., 2012, Toxicities of anticancer drugs and its management, International Journal of Basic & Clinical Pharmacology, 1(1), 2-12.
Sirait, P.S., Setyaningsih, I., and Tarman, K., 2019, Aktivitas Antikanker Ekstrak Sprirulina yang Dikultur Pada Media Walne dan Media Organik, Jurnal Pengolahan Hasil Perikanan Indonesia, 22(1), 50–59.
Siregarr, F. and Hadijono, B.S., 2000, Uji Sitotoksisitas Dengan Esei MTT, Jurnal Kedokteran Gigi, 7, 28–32.
Siswarni, M.Z., Putri, Y.I., and Rinda, R., 2017, Ekstaksi Kuersetin Dari Kulit Terong Belanda (Solanum betaceum Cav.) Menggunakan Pelarut Etanol Dengan Metode Maserasi dan Soxhletasi, Jurnal Teknik Kimia USU, 6(1), 36-42.
Tian, L., Xie, X.H., and Zhu, Z.H., 2018, Calotropin regulates the apoptosis of non-small cell cancer by regulating the cytotoxic T-lymphocyte associated antigen 4-mediated TGF-β/ERK signaling pathway, Molecular Medicine Reports, 17(6), 7683–7691.
Tristantini, D., Ismawati, A., Pradana, B.T., and Gabriel, J., 2016, Pengujian Aktivitas Antioksidan Menggunakan Metode DPPH pada Daun Tanjung Proofread 46 (Mimusops elengi L), Universitas Indonesia, 2.
Vajrabhaya, L-O., and Korsuwannawong, S., 2018, Cytotoxicity evaluation of a Thai herb us¬ing tetrazolium (MTT) and sulforhodamine B (SRB) assays, Journal of Analytical Science and Technology, 9, 15.
Wijaya, C.A. and Muchtaridi, M., 2017, Pengobatan Kanker Melalui Metode Gen Terapi, Farmaka, 15(1), 53–68.
Yip, K.W., and Reed, J.C., 2008, Bcl-2 family proteins and cancer, Oncogene, 27, 6398–6406.
Zhou, L., Cai, L., Guo, Y., Zhang, H., Wang, P., Yi, G., and Huang, Y., 2019, Calotropin activates YAP through downregulation of LATS1 in colorectal cancer cells, OncoTargets and Therapy, 12, 4047–4054.
DOI: http://dx.doi.org/10.14499/indonesianjcanchemoprev16iss2pp93-106
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