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- 衍生的二萜倍半萜类化合物抑制破骨细胞分化。

-Derived Drimane Sesquiterpenoids That Inhibit Osteoclast Differentiation.

机构信息

Natural Product Informatics Research Center , Korea Institute of Science and Technology (KIST) Gangneung Institute , Gangneung 25451 , Republic of Korea.

Herbal Medicine Resources Research Center , Korea Institute of Oriental Medicine , Naju 58245 , Republic of Korea.

出版信息

J Nat Prod. 2019 Oct 25;82(10):2835-2841. doi: 10.1021/acs.jnatprod.9b00559. Epub 2019 Oct 10.

DOI:10.1021/acs.jnatprod.9b00559
PMID:31599157
Abstract

The presence of excessive osteoclasts is a major factor in skeletal diseases. The present study aimed to discover osteoclast differentiation inhibitors from the basidiomycete . Seven new drimane sesquiterpenoids (-) and 7-ketoisodrimenin-5-ene () were obtained and characterized by various spectroscopic methods. The isolated compounds were evaluated for their inhibitory effects against receptor activator of nuclear factor-kappa-B ligand-induced osteoclastogenesis in mouse bone marrow macrophages. Compounds , , and showed potent activities with IC values of 1.6, 0.9, and 2.1 μM, respectively, while , , and exhibited relatively weak activities with IC values of 10.7, 10.1, and 8.5 μM, respectively.

摘要

破骨细胞的过度存在是骨骼疾病的一个主要因素。本研究旨在从担子菌中发现破骨细胞分化抑制剂。通过各种光谱方法获得了 7 个新的倍半萜(-)和 7-酮异二氢紫堇宁-5-烯()。对分离得到的化合物进行了受体激活因子核因子-κB 配体诱导的小鼠骨髓巨噬细胞破骨细胞生成抑制活性评价。化合物、和表现出较强的活性,IC 值分别为 1.6、0.9 和 2.1 μM,而、和表现出较弱的活性,IC 值分别为 10.7、10.1 和 8.5 μM。

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