3-氧代-γ-土木香酸的真菌转化产生具有体外肿瘤抑制活性的桉烷倍半萜。
3-Oxo-γ-costic acid fungal-transformation generates eudesmane sesquiterpenes with in vitro tumor-inhibitory activity.
作者信息
Hegazy Mohamed-Elamir F, El-Beih Ahmed A, Hamed Ahmed R, Abd El Aty Abeer A, Mohamed Naglaa S, Paré Paul W
机构信息
Phytochemistry Department, National Research Centre, El-Tahrir Street, Dokki, Giza 12622, Egypt.
Chemistry of Natural & Microbial Products, National Research Centre, El-Tahrir Street, Dokki, Giza 12622, Egypt.
出版信息
Bioorg Med Chem Lett. 2017 Aug 15;27(16):3825-3828. doi: 10.1016/j.bmcl.2017.06.057. Epub 2017 Jun 23.
While select eudesmane sesquiterpenes exhibit anti-neoplastic activity, tumor-inhibition for costic-acids has not been established. Here biological activity of 3-oxo-γ-costic acid (1), previously isolated from Chiliadenus montanus, as well as new sesquiterpenes (2-5) and the known derivative, 3-oxoeudesma-1,4,11(13)-trien-7-1061αH-l2-oic acid (6), all produced from 1 by the fungus Athelia rolfsii, are reported. Structures were elucidated using MS and NMR spectroscopy with activity-screening utilizing human colon- and lung-tumor lines, Caco-2 and A549 respectively. Compound 1 exhibited anti-proliferative activity against Caco-2 (IC 39µM) and 2 was active against A549 (IC 74µM) suggesting therapeutic potential for the original substrate and a bio-transformed product.
虽然某些桉烷倍半萜具有抗肿瘤活性，但肋酸的肿瘤抑制作用尚未得到证实。本文报道了先前从山地辣薄荷中分离出的3-氧代-γ-肋酸（1）以及新的倍半萜（2-5）和已知衍生物3-氧代桉叶-1,4,11(13)-三烯-7-1061αH-12-酸（6）的生物活性，所有这些化合物均由真菌罗尔夫丝核菌从1产生。通过质谱和核磁共振光谱对结构进行了阐明，并分别利用人结肠肿瘤细胞系Caco-2和肺肿瘤细胞系A549进行活性筛选。化合物1对Caco-2表现出抗增殖活性（IC 39µM），化合物2对A549有活性（IC 74µM），这表明原始底物和生物转化产物具有治疗潜力。
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