Inhibitors of bone resorption from Halenia corniculata.
Eleven xanthones (1-11), three flavonoids (12-14) and three secoiridoids (15-17) were isolated from the aerial parts of Halenia corniculata. Among those compounds, 1-hydroxy-2,3,4,5-tetramethoxyxanthone (1), 1-hydroxy-2,3,4,7-tetramethoxyxanthone (2), 1-hydroxy-2,3,4,5,7-pentamethoxyxanthone (3), 1-hydroxy-2,3,5-trimethoxyxanthone (4), 1,8-dihydroxy-3,5-dimethoxyxanthone (7), and luteolin (12), at the concentration of 1 microg/mL, effectively inhibited the osteoclast differentiation in a co-culture system with mouse osteoblastic calvarial cells and bone marrow cells. Notably, compounds 1, 3, and 4 exhibited, in a dose-dependent manner, significant inhibition of osteoclast differentiation even at a low concentration (0.01 microg/mL). All the inhibitory compounds, except for compound 7, significantly reduced the pit formation on the dentine slice compared with the control group. For the survival of the mature osteoclasts, compounds 1-4 and 12 (1 microg/mL), significantly decreased the survival number through induction of cell apoptosis, and compound 4 exhibited a significant inhibitory effect on osteoclast survival even at the low concentration of 0.1 microg/mL.
Zhang
Jin
J
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, Korea.
Ahn
Mi-Jeong
MJ
Sun
Qi Shi
QS
Kim
Ki-Yoon
KY
Hwang
Yun Ha
YH
Ryu
Jei Man
JM
Kim
Jinwoong
J
D000818:Animals; D001862:Bone Resorption / Q000188:drug therapy* / Q000473:pathology; D002470:Cell Survival; D002478:Cells, Cultured; D002851:Chromatography, High Pressure Liquid; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology; D029965:Gentianaceae / Q000737:chemistry*; D039823:Iridoids / Q000302:isolation & purification / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008813:Mice, Inbred ICR; D010010:Osteoclasts / Q000187:drug effects; D010936:Plant Extracts / Q000737:chemistry; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet; D044004:Xanthones / Q000302:isolation & purification / Q000494:pharmacology
D005419:Flavonoids; D039823:Iridoids; D010936:Plant Extracts; D044004:Xanthones