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Discovery and characterization of berberine derivatives as stimulators of osteoblast differentiation

International Journal of Oral Biology 2019년 44권 4호 p.165 ~ 172
 ( Han Youn-Ho ) - Wonkwang University College of Dentistry Department of Oral Pharmacology

박원종 ( Park Won-Jong ) - Wonkwang University College of Dentistry Department of Oral and Maxillofacial Surgery

Abstract


Berberine has been used clinically for more than a decade to treat various diseases, has been shown to be effective in osteoblast differentiation, and is a potential treatment option for osteoporosis. However, compared with existing osteoporosis drugs, berberine is somewhat less effective. This study aimed to identify a new compound with efficacy superior to that of berberine. The osteogenic activities of various berberine derivatives were evaluated via cell differentiation in C2C12 preosteoblast cell lines. Alkaline phosphatase (ALP) staining assay and structure? activity relationship demonstrated that compound 2b had a potent osteogenic effect. Furthermore, compound 2b dose dependently increased ALP activity and showed no toxicity at the effective concentration, indicating its efficacy. Additionally, compound 2b upregulated BMP2-induced transcriptional activity in a promoter activity assay using ALP, BSP, and OC promoters.

키워드

Berberine; Derivative; Osteoblast
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