来自青花的 Hirsutinolide 型倍半萜类化合物具有抗前列腺癌活性。
Hirsutinolide-type sesquiterpenoids with anti-prostate cancer activity from Cyanthillium cinereum.
发表日期:2023 Oct 06
作者:
Song Ang, Chun Liu, Peng Hong, Lei Yang, Gui'e Hu, Xi Zheng, Jingwei Jin, Rihui Wu, Wing-Leung Wong, Kun Zhang, Lishe Gan, Dongli Li
来源:
PHYTOCHEMISTRY
摘要:
从 Cyanthillium cinereum 的地上部分分离出四种先前未描述的 hirsutinolide 型倍半萜类化合物,cyanolides A-D (1-4),以及十二种已知的类似物 (5-16)。通过NMR、HRESIMS和ECD谱的综合分析确定了它们的结构。化合物1是一种罕见的1,4-醚环破裂且含有氯原子的多毛内酯型倍半萜类化合物,化合物13-16为首次从该植物中报道。测试了所有化合物对前列腺癌细胞的抑制作用。结果,化合物1、3和8-14对PC-3和LNCaP细胞表现出显着的抗前列腺癌活性,IC50值范围为2.2±0.4至8.5±0.7μM和3.0±0.7至10.5±1.1μM,分别。讨论了初步的构效关系。进一步研究表明,化合物 1 诱导 PC-3 细胞凋亡。版权所有 © 2023。由 Elsevier Ltd 出版。
Four previously undescribed hirsutinolide-type sesquiterpenoids, cyanolides A-D (1-4), along with twelve known analogues (5-16), were isolated from the aerial parts of Cyanthillium cinereum. Their structures were determined by comprehensive analysis of NMR, HRESIMS, and ECD spectra. Compound 1 is a rarely occurring hirsutinolide-type sesquiterpenoid with 1,4-ether ring ruptured and containing a chlorine atom, and compounds 13-16 were reported from this plant for the first time. All compounds were tested for their inhibiting effects on prostate cancer cells. As a result, compounds 1, 3, and 8-14 exhibited significant anti-prostate cancer activity against PC-3 and LNCaP cells with IC50 values ranging from 2.2 ± 0.4 to 8.5 ± 0.7 μM and 3.0 ± 0.7 to 10.5 ± 1.1 μM, respectively. The preliminary structure-activity relationship was discussed. Further investigation showed that compound 1 induced apoptosis in PC-3 cells.Copyright © 2023. Published by Elsevier Ltd.