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

Abstract

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.

OECD-407 Driven 28-day-repeated-dose non-clinical safety evaluation of Tinospora cordifolia (Giloy) stem aqueous extract in Sprague-Dawley rats under GLP compliance

“…Magnoflorine, besides being one of the marker phytocompounds of T. cordifolia , is associated with anti-nephro ( Gupta and Sharma, 2011 ) and anti-hepatotoxic ( Sharma and Dabur, 2015 ) effects. Likewise, β-ecdysone, along with remarkable anti-osteoporotic and bone-protective properties, is reported to be cytologically safe ( Abiramasundari et al, 2018 ). Therefore, the phytoconstitutional integrity and traceability of TCWE safety was established through UHPLC with the marker compounds, magnoflorine and β-ecdysone.…”

Identification, Validation and Standardization of Bioactive Molecules Using UPLC/MS-QToF, UHPLC and HPTLC in Divya-Denguenil-Vati: A Penta-Herbal Formulation for Dengue Fever

“…The wide-spectrum therapeutic activities of T. cordiofolia are due to the presence of numerous key bioactive compounds. T. cordiofolia was shown to be responsible for five phyto-constituents out of ten in the current investigation, these are gallic acid, magnoflorine, rutin, β-ecdysone and rosmarinic acid [ 22 – 24 ]. Aloe barbadensis or Aloe vera, has been classically used for skin disorders.…”

Giloy Ghanvati (Tinospora cordifolia (Willd.) Hook. f. and Thomson) Reversed SARS-CoV-2 Viral Spike-Protein Induced Disease Phenotype in the Xenotransplant Model of Humanized Zebrafish

“…Phytoecdysteoids have been identified in more than 100 plant families and plants are capable of biosynthesis of these from mevalonic acid, unlike insects ( Adler and Grebenok, 1995 ). The most commonly found phytoecdysteroid is 20-hydroxyecdysone (beta-ecdysone) and has also been identified in T. cordifolia ( Abiramasundari et al, 2018 ) and has been demonstrated to induce osteogenic transformation. They have been shown to have immunomodulatory activity wherein the concentration of antibody forming B cells in the spleen of mice immunized with sheep RBC was higher (Sakhibov et al, 1989).…”