来源于半夏块茎内生曲霉的细胞毒次级环二肽生物碱。
Cytotoxic seco-cytochalasins from an endophytic Aspergillus sp. harbored in Pinellia ternata tubers.
机构信息
State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China.
State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China.
出版信息
Fitoterapia. 2019 Jan;132:53-59. doi: 10.1016/j.fitote.2018.11.010. Epub 2018 Nov 26.
Six new seco-cytochalasins A-F (1-6), two new asperlactones G-H (7-8) along with three known cytochalasins (9-11) were isolated from the solid cultures of an endophytic fungus Aspergillus sp. Their structures were elucidated by comprehensive spectral analysis, and their absolute configurations were determined through Mo(OCOCH)-induced electronic circular dichroism (ECD) spectra and Rh(OCOCF)-induced ECD experiment. Compounds 5 and 6 were rare seco-cytochalasins possessing an α, β-unsaturated furanone structure in their side-chains. These isolates exhibited cytotoxicity against human lung cancer A-549 cell line with IC values ranging from 7.8 to 70.2 μM. At the concentration of 16 μM, compound 4 also exerted a 3-fold enhancement of doxorubicin susceptibility on doxorubicin-resistant human breast cancer (MCF-7/DOX) cell line.
从一株内生真菌 Aspergillus sp 的固体培养物中分离得到了 6 种新的 secocytochalasins A-F（1-6）、2 种新的 asperlactones G-H（7-8）以及 3 种已知的 cytochalasins（9-11）。通过综合光谱分析阐明了它们的结构，并通过 Mo(OCOCH)诱导的电子圆二色性（ECD）光谱和 Rh(OCOCF)诱导的 ECD 实验确定了它们的绝对构型。化合物 5 和 6 是罕见的 secocytochalasins，其侧链中具有α，β-不饱和呋喃酮结构。这些分离物对人肺癌 A-549 细胞系表现出细胞毒性，IC 值范围为 7.8 至 70.2 μM。在 16 μM 的浓度下，化合物 4 还对多柔比星耐药的人乳腺癌（MCF-7/DOX）细胞系表现出 3 倍增强的多柔比星敏感性。
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