Anti-osteoporotic effects of 5,6-dehydrokawain and it's synthetic analogs

DOI

Bibliographic Information

Other Title
  • 月桃由来5,6-dehydrokawainの骨粗鬆症予防効果とその作用機序解明に向けた構造活性相関研究

Description

<p>Bone homeostasis is maintained by balancing bone formation and bone resorption, but an imbalance between them is associated with various bone-related diseases such as osteoporosis and rheumatoid arthritis. We found that 5,6-dehydrokawain (DK) and dihydro-5,6-dehydrokawain (DDK), which were isolated as promising compounds from Alpinia zerumbet rhizomes, promote differentiation of osteoblastic MC3T3-E1 cells. DK exerts larger effects than DDK. To confirm anti-osteoporosis effects of DK in vivo, we conducted animal experiments using ovariectomized (Ovx)-rat. DK was able to prevent Ovx-induced fat accumulation and body weight gain, and DK enhanced relative weight of bone mineral content. In these results, we considered DK may have clinical potential for treating osteoporosis and could be considered as a potential anabolic therapeutic agent. </p><p>Next, we examined the structure-activity relationships to understand action mode of DK and to obtain more active agents. We synthesized 28 analogs and evaluated stimulating activities of osteoblastogenesis. Some analogues were found to be more potent than DK. Moreover, we found that the analogs having hydrophobic groups at the para position on the aromatic ring indicated the strong activity. This result is important for the probe design because the direct substitution of a functional moiety onto the aromatic ring resulted in loss of the activity. </p>

Journal

Details 詳細情報について

  • CRID
    1390001277364062080
  • NII Article ID
    130007722932
  • DOI
    10.24496/tennenyuki.58.0_poster38
  • ISSN
    24331856
  • Text Lang
    ja
  • Data Source
    • JaLC
    • CiNii Articles
  • Abstract License Flag
    Disallowed

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