Osteoblast differentiation stimulating activity of biflavonoids from Cephalotaxus koreana.

Abstract

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.

• Authors: Mi Kyeong Lee, Song Won Lim, Hyekyung Yang, Sang Hyun Sung, Heum-Sook Lee, Mi Jung Park, Young Choong Kim
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 16 Issue 11 Pg. 2850-4 (Jun 01 2006) ISSN: 0960-894X [Print] England
• PMID: 16574412 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Biflavonoids
• Collagen

Topics

• Animals
• Biflavonoids (chemistry, pharmacology)
• Cell Differentiation (drug effects)
• Cells, Cultured
• Cephalotaxus (chemistry)
• Collagen (metabolism)
• Mice
• Molecular Structure
• Osteoblasts (cytology, drug effects, metabolism)
• Plant Leaves (chemistry)
• Plant Stems (chemistry)
• Structure-Activity Relationship