acid-phosphatase and tanshinone

Novel diazirine or biotin-labeled tanshinone probes were synthesized and evaluated for TRAP inhibitory activity against RANKL-induced osteoclastogenesis in RAW264.7 cells. We found that diazirine-labeled derivatives (18 and 20) are potent inhibitors of RANKL-induced osteoclastogenesis. IC50 values were 18.02 and 15.00 microM, respectively. These probes will be useful reagents for investigating tanshinone-proteins interactions.

Topics: Abietanes; Acid Phosphatase; Animals; Carrier Proteins; Cell Line; Cell Proliferation; Hydrogen; Isoenzymes; Membrane Glycoproteins; Mice; Molecular Structure; Osteoclasts; Osteogenesis; Phenanthrenes; Proteins; RANK Ligand; Receptor Activator of Nuclear Factor-kappa B; Tartrate-Resistant Acid Phosphatase

In isoprenaline-induced myocardial infarction in rabbits, the circulating neutrophils (neu) were in an activated state. tanshinone (tan, ig) suppressed the neu functions (acid-phosphatase release, adhesiveness, and phagocytosis) dose-dependently and reduced myocardial necrosis concomitantly. There was a positive correlation between neu functions and myocardial necrosis. In addition, tan caused an obvious decrease in content of lipoperoxide malondialdehyde in serum and myocardium, an increase in superoxide dismutase activity, an inhibition of leukocytic infiltration, and a production of prostaglandin E2 in myocardium. These effects were also related closely to the suppression of neu functions. Anti-inflammatory drug dexamethasone was used as control and had similar effects on Neu functions and myocardial infarction. It is suggested that the prophylactic effects of tan on myocardial infarction may result from the inhibition of circulating neu functions.

Topics: Abietanes; Acid Phosphatase; Adhesiveness; Animals; Dose-Response Relationship, Drug; Female; Male; Myocardial Infarction; Myocardium; Neutrophils; Phagocytosis; Phenanthrenes; Rabbits