3-beta-o-acetylursolic-acid has been researched along with Osteoporosis* in 1 studies
1 other study(ies) available for 3-beta-o-acetylursolic-acid and Osteoporosis
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Tryptophan hydroxylase 1 (Tph-1)-targeted bone anabolic agents for osteoporosis.
Tryptophan hydroxylase 1 (Tph-1), the principal enzyme for peripheral serotonin biosynthesis, provides a novel target to design anabolic agents for osteoporosis. Here, we present a design, synthesis of a novel series of ursolic acid derivatives under the guidance of docking technique, and bioevaluation of the derivatives using RBL2H3 cells and ovariectomized (OVX) rats. Of the compounds, 9a showed a potent inhibitory activity on serotonin biosynthesis. Further investigations revealed that 9a, as an efficient Tph-1 binder identified by SPR (estimated KD: 6.82 μM), suppressed the protein and mRNA expressions of Tph-1 and lowered serotonin contents in serum and gut without influence on brain serotonin. Moreover, oral administration of 9a elevated serum level of N-terminal propeptide of procollagen type 1 (P1NP), a bone formation marker, and improved bone microarchitecture without estrogenic side effects in ovariectomized rats. Collectively, 9a may serve as a new candidate for bone anabolic drug discovery. Topics: Anabolic Agents; Animals; Bone and Bones; Brain; Cell Line; Female; Gastrointestinal Tract; Humans; Molecular Docking Simulation; Osteoporosis; Ovariectomy; Protein Binding; Quinoxalines; Rats; RNA, Messenger; Serotonin; Structure-Activity Relationship; Surface Plasmon Resonance; Triterpenes; Tryptophan Hydroxylase; Ursolic Acid | 2014 |