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Cytotoxic triterpenoids from Antrodia camphorata as sensitizers of paclitaxel
Organic Chemistry Frontiers ( IF 4.6 ) Pub Date : 2020/02/11 , DOI: 10.1039/c9qo01516g
Bin Li, Yi Kuang, Meng Zhang, Jun-Bin He, Lu-Lu Xu, Chung-Hang Leung, Dik-Lung Ma, Jen-Yu Lo, Xue Qiao, Min Ye

In an attempt to discover anticancer triterpenoids from the medicinal fungus Antrodia camphorata, a total of 60 triterpenoids (1–60) including 18 new ones (antcamphins M–X, 1–18) were isolated from its dish cultures. The structures of the new compounds were elucidated by extensive NMR and HRESIMS data analyses. The absolute configurations were established by the modified Mosher's method, chemical transformation, or X-ray crystallographic data analysis. The cytotoxic activities of 1–60, together with previously reported compounds 61–81, were evaluated using four human cancer cell lines (HL60, U251, SW480, and MCF-7 cells). Compound 57 exhibited potent activities against all the four cell lines with IC50 values of 2.6, 8.2, 2.5, and 4.6 μM, respectively. Moreover, the combination of 10 and 69 (20 μM) could remarkably enhance their cytotoxic activities against the HL60 cells of paclitaxel (10 nM), with inhibition rates increasing from 19.6% to 58.2% and 70.6%, respectively.

中文翻译:

樟芝樟脑细胞毒性三萜作为紫杉醇的敏化剂

为了从药用真菌樟芝樟脑中发现抗癌三萜类化合物,从其培养皿中分离出总共60种三萜类化合物(1–60),其中包括18种新的三萜类化合物(antcamphins M–X,1–18)。通过广泛的NMR和HRESIMS数据分析阐明了新化合物的结构。绝对构型是通过改良的Mosher方法,化学转化或X射线晶体学数据分析建立的。使用四种人类癌细胞系(HL60,U251,SW480和MCF-7细胞)评估了1-60以及先前报道的化合物61-81的细胞毒活性。化合物57表现出对所有四个细胞系的有效活性,IC 50值分别为2.6、8.2、2.5和4.6μM。此外,1069(20μM)的组合可以显着增强其对紫杉醇(10 nM)HL60细胞的细胞毒活性,抑制率分别从19.6%增至58.2%和70.6%。
更新日期:2020-03-03
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