Osteoblast differentiation stimulating activity of biflavonoids from Cephalotaxus koreana.
Six amentoflavone-type biflavonoids, bilobetin (1), ginkgetin (2), 4',7''-di-O-methyl-amentoflavone (3), 7-O-methyl-isoginkgetin (4), sciadopitysin (5), and 7,4',7'',4'''-O-methyl-amentoflavone (6), were isolated from the EtOAc fraction of Cephalotaxus koreana Nakai (Cephalotaxaceae) by bioactivity-guided fractionation technique using primary cultures of mouse osteoblasts as an in vitro assay system. Among the six biflavonoids isolated, bilobetin (1), sciadopitysin (5), and 7,4',7'',4'''-O-methyl-amentoflavone (6) significantly increased osteoblast differentiation as assessed by alkaline phosphatase activity, collagen synthesis, and mineralization. Considering structure-activity relationship, methoxyl groups at 4' and 4''' in the B rings in amentoflavone-type biflavonoid might be important in osteoblast differentiation. Taken together, our present study suggests therapeutic potential of biflavonoids against bone diseases such as osteoporosis.
College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University, Seoul 151-742, Republic of Korea.
Mi Kyeong
MK
Lee
Song Won
SW
Lim
Hyekyung
H
Yang
Sang Hyun
SH
Sung
Heum-Sook
HS
Lee
Mi Jung
MJ
Park
Young Choong
YC
Kim
D000818:Animals; D044946:Biflavonoids / Q000737:chemistry* / Q000494:pharmacology*; D002454:Cell Differentiation / Q000187:drug effects*; D002478:Cells, Cultured; D032483:Cephalotaxus / Q000737:chemistry*; D003094:Collagen / Q000378:metabolism; D051379:Mice; D015394:Molecular Structure; D010006:Osteoblasts / Q000166:cytology* / Q000187:drug effects* / Q000378:metabolism; D018515:Plant Leaves / Q000737:chemistry; D018547:Plant Stems / Q000737:chemistry; D013329:Structure-Activity Relationship
D044946:Biflavonoids; D003094:Collagen