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BackgroundIndian ethnomedicine acclaims Tinosporacordifolia as a bone strengthening agent and prescribes it for the treatment of bone fractures, gout and other inflammatory diseases of the bone.Objective(a) To understand the potential of T. cordifolia to act as a Selective Estrogen Receptor Modulator (SERM) on in vitro models. (b) To understand the toxic effects (if any) of T. cordifolia in vivo. (c) To understand the effects of β-ecdysone (proposed osteoprotective principle of T. cordifolia) on the growth of human osteoblast-like cells MG-63 and rat primary culture of osteoblasts. (d) To conduct phytochemical analysis on T. cordifolia extract to confirm the presence of β-ecdysone.Materials and MethodsThe role of T. cordifolia as SERM was analyzed by investigating the effect of the extract on the growth of MCF-7 and HeLa cells. The effects of T. cordifolia in vivo was studied by biochemical (Liver function and renal function tests) and histopathological (Hematoxylin/Eosin staining) analysis. Phytochemical analysis of T.cordifolia was carried out by performing FT-IR and LC-ESI-MS analysis.Results(a) T. cordifolia extract exerted non-estrogenic effects on MCF-7 and HeLa cells implicating its role as SERM. (b) High doses of T. cordifolia extract (750 and 1000 mg/kg body wt.) showed impairment of hepatic and renal function, induced pathological alterations in hepatic and renal architecture in albino rats. (c) β-ecdysone an ecdysteroid proposed as the osteoprotective principle of T. cordifolia exhibited significant prostimulatory effects on osteoblast cells and rat primary osteoblasts. (d) Phytochemical analysis confirmed the presence of β-ecdysone in alcoholic extract of T. cordifolia extract substantiating its role as the osteoprotective principle of T. cordifolia.Conclusion(a) T. cordifolia could function as SERM and can have applications in the therapy of osteoporosis. (b) β-ecdysone is the osteoprotective principle of T. cordifolia.

Tamoxifen therapy for the treatment of hormone responsive breast cancer has limitations due to acquired resistance in the case of recurrences. Embelin, a known inhibitor of X-linked inhibitor of apoptosis protein (XIAP) was also reported to exhibit strong antiestrogenic effects in animal models. Dual role of embelin as a proapoptotic and antiestrogenic agent may have potential benefits in the therapy of breast cancer. In this study, the effects of embelin treatment on estrogen receptor positive Human breast adenocarcinoma (MCF-7) cells was investigated to primarily understand if embelin being an antiestrogen and XIAP inhibitor could be a potential alternative to tamoxifen therapy. Results revealed that, embelin at a concentration of 65 lg/ml attenuated proliferation, inhibited metastatic migration, modulated the expression of Bcl2, Caspases and induced apoptosis in MCF-7 cells which was found to be p53 mediated. Hence, chemotherapy with embelin could be a promising strategy to be experimented in hormone responsive breast cancers.