School of Pharmacy, Tongji Medical College of Huazhong University of Science and Technology, Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, Wuhan, People's Republic of China.
Planta Med. 2020 Sep;86(13-14):976-982. doi: 10.1055/a-1091-8831. Epub 2020 Feb 4.
Three new (alterchothecenes A - C, 1: -3: ) and 3 known (4: -6: ) trichothecenes, along with 9 known compounds (7: -15: ), were isolated from the culture of sp. sb23, an endophytic fungus separated from the root of Rehd. et Wils. Their structures were elucidated by spectroscopic analyses, and the absolute configurations of 1: -3: were determined through comparison of the experimental electronic circular dichroism (ECD) spectra and optical rotations with similar analogues. cytotoxicity tests of compounds 1: -6: against human HT-29 colon carcinoma and human MCF-7 breast cancer cell lines indicated that 4: -6: exhibited significant cytotoxic effects, with IC values ranging from 0.89 to 9.38 µM. And the potential of compounds 1: -6: as tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) sensitizers in HT-29 cells was evaluated. The results revealed that combination treatment of TRAIL with compounds 1: -6: synergistically decreased cell viability compared with the sole treatment with those compounds.
从内生真菌 sb23 的培养物中分离得到了 3 种新的(alterchothecenes A - C, 1: -3: )和 3 种已知的(4: -6: )曲菌素,以及 9 种已知的化合物(7: -15: )。通过光谱分析阐明了它们的结构,通过比较实验电子圆二色性(ECD)光谱和与类似物的旋光度,确定了 1: -3: 的绝对构型。对化合物 1: -6: 对人 HT-29 结肠癌细胞和人 MCF-7 乳腺癌细胞系的细胞毒性试验表明,化合物 4: -6: 具有显著的细胞毒性作用,IC 值范围为 0.89 至 9.38 μM。还评估了化合物 1: -6: 作为 TRAIL 敏感剂在 HT-29 细胞中诱导肿瘤坏死因子(TNF)-相关凋亡诱导配体(TRAIL)的潜力。结果表明,与单独使用这些化合物相比,TRAIL 与化合物 1: -6: 的联合治疗可协同降低细胞活力。