CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology, Southern Marine Science and Engineering Guangdong Laboratory (Guangzhou), Guangdong Key Laboratory of Marine Materia Medica, RNAM Center for Marine Microbiology, South China Sea Institute of Oceanology, Chinese Academy of Sciences, 164 West Xingang Road, Guangzhou 510301, China.
University of Chinese Academy of Sciences, 19 Yuquan Road, Beijing 100049, China.
Mar Drugs. 2022 Feb 18;20(2):150. doi: 10.3390/md20020150.
Three new metabolites, including a cyclic tetrapeptide asperhiratide (), an ecdysteroid derivative asperhiratine (), and a sesquiterpene lactone asperhiratone (), were isolated and identified from the soft coral-derived fungus SCSIO 5Bn003, together with 10 known compounds. Their structures were elucidated via spectroscopic analysis, X-ray diffraction analysis, and electronic circular dichroism calculations. In addition, the absolute configuration of was determined by Marfey's technique and an analysis of the acid hydrolysates using a chiral phase HPLC column. Among all the compounds, and showed medium cytotoxic activities against four tumor cell lines (SF-268, HepG-2, MCF-7, and A549), with IC values ranging from 31.03 ± 3.04 to 50.25 ± 0.54 µM. Meanwhile, they strongly inhibited α-glucosidase activities, with IC values of 35.73 ± 3.94 and 22.00 ± 2.45 µM, which were close to and even stronger than the positive control acarbose (IC = 32.92 ± 1.03 µM). Compounds - showed significant antibacterial activities against , with MIC values of 10.26 ± 0.76 µM, 17.00 ± 1.25 µM, and 5.30 ± 0.29 µM, respectively. Compounds and exhibited potent radical scavenging activities against DPPH, with IC values of 12.23 ± 0.78 µM and 7.38 ± 1.16 µM. In addition, asperhiratide () was evaluated for anti-angiogenic activities in the in vivo zebrafish model, which showed a weak inhibitory effect on intersegmental vessel (ISV) formation.
从软珊瑚来源的真菌 SCSIO 5Bn003 中分离鉴定了 3 个新代谢物，包括环四肽asperhiratide()、蜕皮甾酮衍生物 asperhiratine()和倍半萜内酯 asperhiratone()，以及 10 个已知化合物。通过光谱分析、X 射线衍射分析和电子圆二色性计算确定了它们的结构。此外，通过 Marfey 技术和手性相 HPLC 柱分析酸水解产物确定了的绝对构型。在所有化合物中，和对 4 种肿瘤细胞系（SF-268、HepG-2、MCF-7 和 A549）表现出中等细胞毒性活性，IC 值范围为 31.03±3.04 至 50.25±0.54µM。同时，它们强烈抑制α-葡萄糖苷酶活性，IC 值分别为 35.73±3.94 和 22.00±2.45µM，接近甚至强于阳性对照阿卡波糖（IC=32.92±1.03µM）。化合物-对表现出显著的抗菌活性，对的 MIC 值分别为 10.26±0.76µM、17.00±1.25µM 和 5.30±0.29µM。化合物和表现出强烈的清除 DPPH 自由基的活性，IC 值分别为 12.23±0.78µM 和 7.38±1.16µM。此外，asperhiratide()在体内斑马鱼模型中评估了抗血管生成活性，结果显示对节间血管（ISV）形成有较弱的抑制作用。
