查尔酮
化学
诺金
取代基
体外
C2C12型
变形链球菌
细胞毒性
立体化学
生物化学
骨形态发生蛋白
生物
细菌
遗传学
肌发生
基因
作者
Daheui Choi,Jin Chan Park,Ha Na Lee,Ji-Hoi Moon,Hyo-Won Ahn,Kwangyong Park,Jinkee Hong
标识
DOI:10.1021/acs.molpharmaceut.8b00288
摘要
Chalcone derivatives have been investigated as therapeutic agents for the anticancer, antioxidant, and anti-inflammatory fields. In this study, we have synthesized four different types of chalcone derivatives and demonstrated in vitro bioactivities. We divided these derivatives into two groups of chalcones on the basis of similar substituents on the aromatic rings, and we tested cell viability and proliferation potentials, which indicated that the methoxy substituent on the A ring could enhance cytotoxicity and antiproliferation potential depending on the chalcone concentration. We also investigated osteogenic differentiation of C2C12 cells by ALP staining, the early marker for osteogenesis, which demonstrated that the chalcones could not only induce activity of BMP-2 but also inhibit the activity of noggin, a BMP antagonist. In addition, chalcone bearing hydroxyl groups at the 2-, 4-, and 6-position on the A ring inhibited treptococcus mutans growth, a major causative agent of dental caries. Therefore, we concluded that the chalcone derivatives synthesized in this research can be good candidates for therapeutic agents promoting bone differentiation, with an expectation of inhibiting S. mutans, in dentistry.
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