ent-Kaurane Diterpenoids from Croton tonkinensis Stimulate Osteoblast Differentiation

ent-Kaurane Diterpenoids from Croton tonkinensis Stimulate Osteoblast Differentiation
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DOI:
10.1021/np200667f
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发表时间:
2011-12-01
影响因子:
5.1
通讯作者:
Oh, Won-Keun
Oh, Won-Keun
中科院分区:
生物学2区
文献类型:
--
作者:
Dao, Trong-Tuan;Lee, Kwang-Youl;Oh, Won-Keun

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采用体外成骨细胞分化实验,通过活性导向分离,从越南巴豆叶中分离得到4个新的对映贝壳杉烷型二萜化合物(1-4)。它们的结构经鉴定为ent-11 beta-acetoxykaur-16-en-18-ol(1)、ent-11 alpha-hydroxy-18-acetoxykaur-16-ene(2)、ent-14 beta-hydroxy-18-acetoxykaur-16-ene(3)和ent-7 alpha-hydroxy-18-acetoxykaur-16-ene(4)。化合物1-4显著增加碱性磷酸酶活性和成骨基因启动子活性。化合物1-3还以剂量依赖性方式增加C2 C12细胞中ALP和I型胶原α mRNA的水平。这些结果表明,C.结论:越南楝素对成骨细胞的分化有直接的促进作用,可能成为治疗骨质疏松症等骨疾病的潜在分子。
Four new ent-kaurane diterpenoids (1-4) were isolated from the leaves of Croton tonkinensis by bioactivity-guided fractionation using an in vitro osteoblast differentiation assay. Their structures were identified as ent-11 beta-acetoxykaur-16-en-18-ol (1), ent-11 alpha-hydroxy-18-acetoxykaur-16-ene (2), ent-14 beta-hydroxy-18-acetoxykaur-16-ene (3), and ent-7 alpha-hydroxy-18-acetoxykaur-16-ene (4). Compounds 1-4 significantly increased alkaline phosphatase activity and osteoblastic gene promoter activity. Compounds 1-3 also increased the levels of ALP and collagen type I alpha mRNA in C2C12 cells in a dose-dependent manner. These results suggest that ent-kaurane diterpenoids from C. tonkinensis have a direct stimulatory effect on osteoblast differentiation and may be potential therapeutic molecules against bone diseases such as osteoporosis.