epimedin-a and Osteoporosis

Osteoporosis is the most common disease involving bone degeneration. As the age of the population increases, the prevalence of the disease is expected to rise. However, current treatment methods do not provide a desirable solution for the restoration of the function of degenerated bones in patients with osteoporosis. This led to emergence of controlled delivery systems to increase drug bioavailability and efficacy specifically at the bone regeneration. In this study, an epimedin A (EA) complex drug system was prepared by solution blending method. In vitro cell-based experiments showed that the EA complex drug could significantly promote the differentiation and proliferation of osteoblasts and increase the alkaline phosphatase activity, calcium nodule formation, and the expression of osteogenesis-related genes and proteins. In vivo experiments further demonstrated that this novel drugs remarkably enhanced bone regeneration. These results suggest that EA may be used for the treatment of osteoporosis.

Topics: Animals; Bone Density; Cell Differentiation; Cells, Cultured; Delayed-Action Preparations; Disease Models, Animal; Drug Carriers; Drug Liberation; Female; Flavonoids; Macromolecular Substances; Mice; Osteoblasts; Osteogenesis; Osteoporosis; Ovariectomy; Polysaccharides, Bacterial; Sulfhydryl Compounds

This article firstly established a new efficient method for screening anti-osteoporosis ingredients, which used two-dimensional zebrafish model combined with hyphenated chromatographic techniques to evaluate anti-osteoporosis activities of epimedin A and its metabolite baohuoside I. Adult zebrafish was used for metabolism of epimedin A in 0.5% DMSO, and LC-MS was used for analysis of the metabolite, which was captured by HPLC, and prednisolone-induced osteoporosis model of zebrafish was used to evaluate the anti-osteoporotic activities of trace amounts of epimedin A and baohuoside I. The results indicated that epimedin A and baohuoside I can prevent prednisolone-induced osteoporosis in zebrafish. The developed method in this paper enables the separation, enrichment and analysis of micro-amount metabolite of epimedin A, and anti-osteoporosis activities in vivo of epimedin A and baohuoside I was simple and efficient screening resorting to zebrafish osteoporosis mode. This paper would provide new ideas and methods for a rapid and early discovery of anti-osteoporosis activities of micro-ingredients and its metabolite of traditional Chinese medicine.

Topics: Animals; Chromatography, High Pressure Liquid; Chromatography, Liquid; Drug Evaluation, Preclinical; Drugs, Chinese Herbal; Flavonoids; Mass Spectrometry; Osteoporosis; Zebrafish