来自海洋真菌Nq45的珠鸡菌素：晶体结构与多种生物活性研究
Meleagrin from marine fungus Nq45: crystal structure and diverse biological activity studies.
作者信息
Hamed Abdelaaty, Abdel-Razek Ahmed S, Araby Mariam, Abu-Elghait Mohammed, El-Hosari Doaa G, Frese Marcel, Soliman Hesham S M, Stammler Hans Georg, Sewald Norbert, Shaaban Mohamed
机构信息
Faculty of Chemistry, Organic and Bioorganic Chemistry, Bielefeld University, Bielefeld, Germany.
Faculty of Science, Department of Chemistry, Al-Azhar University, Cairo, Egypt.
出版信息
Nat Prod Res. 2021 Nov;35(21):3830-3838. doi: 10.1080/14786419.2020.1741583. Epub 2020 Mar 19.
The crystal structure and unambiguous absolute configuration of meleagrin () isolated from fungus Nq45 is reported herein to first time on the bases of single crystal X-ray diffraction. Together with , haenamindole (), isorugulosuvine (), secalonic acid D (), ergosterol () and cerebroside A () were obtained and their structures were determined by ESI MS and NMR data analysis. Diverse biological activity of meleagrin () was investigated. Compound pronounced potent cytotoxicity against the human cervix carcinoma cell line KB-3-1 and its multidrug resistant sub-clone KB-V1 of IC 3.07 and 6.07 µM, respectively, in comparison with the reference (+) - griseofulvin (IC 19, 19.5 µM). Based on the antibiofilm activity, compound displayed as well potent activity against with an MIC of 0.25 mg/mL. Isolation of the producing fungus and taxonomical characterization is stated as well.
本文首次基于单晶X射线衍射报道了从真菌Nq45中分离得到的麦角灵（）的晶体结构和明确的绝对构型。与麦角灵一起，还获得了海纳明哚（）、异鲁格苏文（）、黑麦角环肽D（）、麦角甾醇（）和脑苷脂A（），并通过电喷雾质谱（ESI MS）和核磁共振（NMR）数据分析确定了它们的结构。对麦角灵（）的多种生物活性进行了研究。与参考药物（+） - 灰黄霉素（IC分别为19、19.5 μM）相比，该化合物对人子宫颈癌细胞系KB - 3 - 1及其多药耐药亚克隆KB - V1表现出显著的细胞毒性，IC分别为3.07和6.07 μM。基于抗生物膜活性，该化合物对也表现出强效活性，最低抑菌浓度（MIC）为0.25 mg/mL。还阐述了产生该化合物的真菌的分离及分类学特征。
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