School of Pharmaceutical Sciences, South-Central University for Nationalities, Wuhan 430074, People's Republic of China.
School of Pharmaceutical Sciences, South-Central University for Nationalities, Wuhan 430074, People's Republic of China; The Modernization Engineering Technology Research Center of Ethnic Minority Medicine of Hubei Province, School of Pharmaceutical Sciences, South-Central University for Nationalities, Wuhan 430074, People's Republic of China.
Bioorg Chem. 2021 Jun;111:104874. doi: 10.1016/j.bioorg.2021.104874. Epub 2021 Apr 5.
Seven previously undescribed trichothecenes, named trichothecrotocins M-S (1-7), along with five known compounds, were isolated from rice cultures of the potato-associated fungus Trichothecium crotocinigenum. Their structures and absolute configurations were determined through spectroscopic methods, single-crystal X-ray diffraction, and quantum chemistry calculations on ECD. Compound 1 possesses a rare 6,11-epoxy moiety in the trichothecene family. Compound 6 exhibited strong cytotoxic activity against MCF-7 cancer cell lines with an IC value of 2.34 ± 0.45 μM. It promoted apoptosis induction in MCF-7 cells. Moreover, cell cycle analysis showed cell cycle arrest caused by compound 6 at the G2/M phase which resulted to cell proliferation inhibition and pro-apoptotic activity. Further quantitative real-time PCR (qRT-PCR) analysis confirmed that the G2/M arrest was accompanied by upregulation of p21 and down regulation of cyclins B1 in 6-treated MCF-7 cells.
从与土豆相关的真菌——长枝木霉的大米培养物中分离到了 7 种以前未被描述过的曲霉菌毒素，分别命名为曲霉菌毒素 M-S（1-7），以及 5 种已知化合物。通过光谱方法、单晶 X 射线衍射和 ECD 上的量子化学计算确定了它们的结构和绝对构型。化合物 1 在曲霉菌毒素家族中具有罕见的 6,11-环氧部分。化合物 6 对 MCF-7 癌细胞系表现出强烈的细胞毒性，IC 值为 2.34±0.45μM。它能促进 MCF-7 细胞的凋亡诱导。此外，细胞周期分析显示，化合物 6 可使细胞周期阻滞在 G2/M 期，从而抑制细胞增殖并诱导细胞凋亡。进一步的实时定量 PCR（qRT-PCR）分析证实，G2/M 期阻滞伴随着 6 处理的 MCF-7 细胞中 p21 的上调和细胞周期蛋白 B1 的下调。
