The Effect Of Curculigoside On Bone Cells Estrogen Receptor Expression And Its Preliminary Pharmacokinetic Study

Curculigo orchioides is the rhizome of Curculigo orchioides Gaertn (Family: Amaryllidaceae), and has been included in the Chinese traditional literature for a long history. Modern medicine study found that alcohol extracts of curculigo can inhibit bone resorption and increase in serum phosphorus, calcium levels to prevent bone loss of castration rats. And the main ingredients in30%alcohol extract of curculigo are phenolic glycosides. This suggests that the phenolic glycosides are active ingredients in curculigo orchioides to anti-osteoporosis. Based on the above research, this research focuses on the following two aspects:1) Based on the early stage of the research confirmed that the phenolic glycosides curculigo anti osteoporosis effect in the whole animal experiment, we study the effect of curculigoside on bone cells and the influence of estrogen receptor protein expression.2)Study the preliminary pharmacokinetic of curculigoside in rats. We observe the effects of curculigo phenolic glycosides on UMR-106, OB and OC cells in proliferation, differentiation and the difference of estrogen receptors ER alpha, ER beta protein expression under the action of ICI182780in the above four cells. Then we selected SD rats to study the pharmacokinetics and tissue distribution of curculigoside, LC-MS method for testing the content of curculigoside in plasma and tissue samples was established, the characteristic of curculigoside in SD rats in vivo pharmacokinetic and tissue distribution was explored. The results show that curculigoside can promote osteoblast proliferation and ALP activity, and inhibit TRAP activity and bone absorption of osteoclast, The pharmacokinetic parameters indicate curculigoside enter the blood stream quickly, the time to high concentration is short, up to the peak concentration is high, and need a long time to eliminate in the blood, and its absolute bioavailability is low. Curculigoside is widely distributed in the organizations, while the absolute bioavailability of curculigoside is low.