Development of epimedin A complex drugs for treating the osteoporosis

Abstract

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.

Epimedium‐Curculigo herb pair enhances bone repair with infected bone defects and regulates osteoblasts through LncRNA MALAT1/miR‐34a‐5p/SMAD2 axis

“…Notably, Epimedin A/B and Icariin have been considered to be the hallmark compounds of the Epimedium brevicornum maxim , which have good antiosteoporotic activities through stimulating osteogenic differentiation and then accelerating the process of bone repair. 35 , 36 , 37 Meanwhile, Baohuoside I is one of the metabolites of Icariin in vivo and also one of the main active flavonoid components of the Epimedium brevicornum maxim . 38 Previous studies have shown that Curculigoside, the effective substance of Curculigo orchioides, could attenuate wear particle‐induced periprosthetic osteolysis by promoting osteoblastic MC3T3‐E1 cell differentiation and inhibiting osteoclast BMSC formation.…”

“…Six components were detected in ECP‐CS, including Curculigoside, Baohuoside I, Epimedin A/B, Icariin and Orcinol glucoside. Notably, Epimedin A/B and Icariin have been considered to be the hallmark compounds of the Epimedium brevicornum maxim , which have good antiosteoporotic activities through stimulating osteogenic differentiation and then accelerating the process of bone repair 35–37 . Meanwhile, Baohuoside I is one of the metabolites of Icariin in vivo and also one of the main active flavonoid components of the Epimedium brevicornum maxim 38 .…”

Advancements in the Biotransformation and Biosynthesis of the Primary Active Flavonoids Derived from Epimedium

“…However, similar to the major flavonoids described above, icariside I, epimedin A, and epimedin B also exhibit anti-osteoporosis, neuroprotective, and anti-cancer effects. Epimedin A has shown excellent efficacy against senile osteoporosis [8], and in vitro and in vivo experiments demonstrated that a complex epimedin A drug significantly enhances bone regeneration [81]. In addition, epimedin A could ameliorate 2,4-dinitrofluorobenzene (DNFB)-induced allergic contact dermatitis in mice, due to its ability to suppress the NF-κB/NLRP3 pathway, enhance the Nrf2 pathway, and modulate local inflammation [82].…”

Constituent Analysis and Quality Evaluation of Epimedii Folium from Different Species

“…In some samples, the content of epimedin C and sagittatoside A was higher than that of icariin. Also, the above constituents have been proved to have obvious pharmacological efects [39][40][41]. Terefore, in the future research and application, the composition determination may be considered as new quality control indexes of EF.…”