Kornsakulkarn Jittra, Palasarn Somporn, Choowong Wilunda, Thongpanchang Tienthong, Boonyuen Nattawut, Choeyklin Rattaket, Boonpratuang Thitiya, Isaka Masahiko, Thongpanchang Chawanee
National Center for Genetic Engineering and Biotechnology (BIOTEC), Thailand Science Park, 113 Phaholyothin Road, Klong Luang, Pathumthani 12120, Thailand.
Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Mahidol University, Bangkok 10400, Thailand.
J Nat Prod. 2020 Apr 24;83(4):905-917. doi: 10.1021/acs.jnatprod.9b00647. Epub 2020 Mar 20.
Fourteen new compounds, oudemansins -, oudemansinols -, favolasins -, favolasinin (), polyketides -, and (,)-2,4-dimethyl-5-phenyl-4-pentene-2,3-diol (), together with nine known compounds were isolated from the basidiomycete fungus sp. BCC 18686. Two new compounds, favolasin E () and 9-oxostrobilurin E (), were isolated from the closely related organism BCC 36684 along with nine β-methoxyacrylate-type derivatives. Compounds in the class of oudemansins and strobilurins exhibited moderate to strong antimalarial activity with relatively low cytotoxicity against Vero cells (African green monkey kidney fibroblasts). Potent antimalarial activity was demonstrated for 9-methoxystrobilurins G, K, and E (IC values 0.061, 0.089, and 0.14 μM, respectively). The structure-activity relationships (SAR) for antimalarial activity is proposed on the basis of the activity of the new and several known β-methoxyacrylate derivatives in combination with the data from previously isolated compounds. Furthermore, several compounds showed specific cytotoxicity against NCI-187 cells (human small-cell lung cancer), although the SAR was different from that for antimalarial activity.
从担子菌纲真菌 sp. BCC 18686中分离出14种新化合物，分别为奥德曼菌素-、奥德曼醇-、密环菌素-、密环菌素（）、聚酮化合物-和（，）-2,4-二甲基-5-苯基-4-戊烯-2,3-二醇（），以及9种已知化合物。从密切相关的生物体 BCC 36684中分离出2种新化合物，密环菌素E（）和9-氧代嗜球果伞素E（），以及9种β-甲氧基丙烯酸酯类衍生物。奥德曼菌素类和嗜球果伞素类化合物表现出中度至强的抗疟活性，对Vero细胞（非洲绿猴肾成纤维细胞）的细胞毒性相对较低。9-甲氧基嗜球果伞素G、K和E表现出强效抗疟活性（IC值分别为0.061、0.089和0.14 μM）。基于新的和几种已知的β-甲氧基丙烯酸酯衍生物的活性，并结合先前分离化合物的数据，提出了抗疟活性的构效关系（SAR）。此外，几种化合物对NCI-1-H7细胞（人小细胞肺癌）表现出特异性细胞毒性，尽管其构效关系与抗疟活性不同。
