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Antimalarial 9-Methoxystrobilurins, Oudemansins, and Related Polyketides from Cultures of Basidiomycete Favolaschia Species.
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-03-20 , DOI: 10.1021/acs.jnatprod.9b00647 Jittra Kornsakulkarn 1 , Somporn Palasarn 1 , Wilunda Choowong 1 , Tienthong Thongpanchang 2 , Nattawut Boonyuen 1, 3 , Rattaket Choeyklin 1, 3 , Thitiya Boonpratuang 1, 3 , Masahiko Isaka 1 , Chawanee Thongpanchang 1
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-03-20 , DOI: 10.1021/acs.jnatprod.9b00647 Jittra Kornsakulkarn 1 , Somporn Palasarn 1 , Wilunda Choowong 1 , Tienthong Thongpanchang 2 , Nattawut Boonyuen 1, 3 , Rattaket Choeyklin 1, 3 , Thitiya Boonpratuang 1, 3 , Masahiko Isaka 1 , Chawanee Thongpanchang 1
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Fourteen new compounds, oudemansins 1-4, oudemansinols 5-7, favolasins 8-10, favolasinin (12), polyketides 13-15, and (R,E)-2,4-dimethyl-5-phenyl-4-pentene-2,3-diol (16), together with nine known compounds were isolated from the basidiomycete fungus Favolaschia sp. BCC 18686. Two new compounds, favolasin E (11) and 9-oxostrobilurin E (17), were isolated from the closely related organism Favolaschia calocera 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 (IC50 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.
中文翻译：
来自Basidiomycete Favolaschia物种培养物中的抗疟疾9-甲氧基间苯二酚，Oudemansins和相关的聚酮化合物。
十四种新化合物，oudemansins 1-4，oudemansinols 5-7，favolasins 8-10，favolasinin（12），聚酮化合物13-15和（R，E）-2,4-二甲基-5-苯基-4-戊烯-从担子菌真菌Favolaschia sp。分离了2，3-二醇（16）以及九种已知化合物。BCC18686。从密切相关的生物Favolaschia calocera BCC 36684中分离了两种新化合物，favolasin E（11）和9-oxostrobilurin E（17）以及九种β-甲氧基丙烯酸酯型衍生物。oudemansins和strobilururins类别的化合物表现出中等至强的抗疟活性，并且对Vero细胞（非洲绿猴肾成纤维细胞）的细胞毒性相对较低。证明了对9-甲氧基星形比林激素G，K和E的有效抗疟疾活性（IC50值分别为0.061、0.089和0.14μM）。基于新的和几种已知的β-甲氧基丙烯酸酯衍生物的活性，再结合先前分离出的化合物的数据，提出了抗疟活性的构效关系（SAR）。此外，尽管SAR与抗疟疾活性不同，但几种化合物对NCI-187细胞（人小细胞肺癌）显示出特定的细胞毒性。
更新日期：2020-03-20
中文翻译：
来自Basidiomycete Favolaschia物种培养物中的抗疟疾9-甲氧基间苯二酚，Oudemansins和相关的聚酮化合物。
十四种新化合物，oudemansins 1-4，oudemansinols 5-7，favolasins 8-10，favolasinin（12），聚酮化合物13-15和（R，E）-2,4-二甲基-5-苯基-4-戊烯-从担子菌真菌Favolaschia sp。分离了2，3-二醇（16）以及九种已知化合物。BCC18686。从密切相关的生物Favolaschia calocera BCC 36684中分离了两种新化合物，favolasin E（11）和9-oxostrobilurin E（17）以及九种β-甲氧基丙烯酸酯型衍生物。oudemansins和strobilururins类别的化合物表现出中等至强的抗疟活性，并且对Vero细胞（非洲绿猴肾成纤维细胞）的细胞毒性相对较低。证明了对9-甲氧基星形比林激素G，K和E的有效抗疟疾活性（IC50值分别为0.061、0.089和0.14μM）。基于新的和几种已知的β-甲氧基丙烯酸酯衍生物的活性，再结合先前分离出的化合物的数据，提出了抗疟活性的构效关系（SAR）。此外，尽管SAR与抗疟疾活性不同，但几种化合物对NCI-187细胞（人小细胞肺癌）显示出特定的细胞毒性。
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