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A new indole glycoside from Kitasatospora sp. MG372-hF19 carrying a 6-deoxy-α-L-talopyranose moiety.
The Journal of Antibiotics ( IF 2.1 ) Pub Date : 2019-11-18 , DOI: 10.1038/s41429-019-0258-9
Yasuko Kohda 1 , Shuichi Sakamoto 1 , Yasunari Otsuka 1 , Ryuichi Sawa 2 , Yumiko Kubota 2 , Masayuki Igarashi 2 , Hideyuki Muramatsu 2 , Masatomi Iijima 1 , Manabu Kawada 1, 2
Affiliation  

Small cell lung cancer (SCLC) is a severe malignancy with early and widespread metastasis, and novel therapeutic drugs are needed. To identify cytotoxic natural compounds against SCLC, we screened libraries of microbial fermentation broths using several lung cancer cell lines. We found that the actinomycete strain MG372-hF19 produces a compound that has not been isolated from natural sources but previously chemically synthesized, 6-chloro-1H-indole-3-carboxaldehyde (1), and an entirely new compound, named 6-deoxy-α-L-talopyranose 1-(6-chloro-1H-indole-3-carboxylate) (2), together with leptomycins. The molecular formulas of the compounds were established as C9H6ClNO and C15H16ClNO6, respectively, via high-resolution electrospray ionization mass spectrometry, and their structures were determined using detailed NMR. Absolute configurational analysis of the sugar unit of compound 2 revealed that the compound incorporates the rare deoxyhexose 6-deoxy-α-L-talopyranose. Both compounds exhibited weak growth-inhibiting activities against human lung cancer cell lines.

中文翻译:

Kitasatospora sp。的一种新的吲哚苷。带有6-脱氧-α-L-塔拉吡喃糖部分的MG372-hF19。

小细胞肺癌(SCLC)是一种严重的恶性肿瘤,具有早期和广泛的转移灶,因此需要新型治疗药物。为了鉴定针对SCLC的细胞毒性天然化合物,我们使用几种肺癌细胞系筛选了微生物发酵液文库。我们发现放线菌菌株MG372-hF19产生的化合物不是从天然来源中分离出来的,而是以前化学合成的6-氯-1H-吲哚-3-羧甲醛(1)和一种全新的化合物,称为6-脱氧-α-L-塔拉吡喃糖1-(6-氯-1H-吲哚-3-羧酸酯)(2),与细霉素一起。通过高分辨率电喷雾电离质谱法分别将化合物的分子式确定为C9H6ClNO和C15H16ClNO6,并使用详细的NMR确定其结构。化合物2的糖单元的绝对构型分析表明该化合物结合了稀有的脱氧己糖6-脱氧-α-L-塔拉吡喃糖。两种化合物对人肺癌细胞系均显示出弱的生长抑制活性。
更新日期:2020-01-17
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