Selective Estrogen Receptor Modulator and prostimulatory effects of phytoestrogen β-ecdysone in Tinospora cordifolia on osteoblast cells

Background: Indian ethnomedicine acclaims Tinospora cordifolia 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 Methods: The 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. Keywords: ß-ecdysone, Tinospora cordifolia, SERM, Phytoestrogens, Osteoblasts, Osteoporosi