Davies-Bolorunduro Olabisi Flora, Adeleye Isaac Adeyemi, Akinleye Moshood Olushola, Wang Peng George
Department of Microbiology, University of Lagos, Akoka, Lagos, Nigeria.
Department of Chemistry, Georgia State University, Atlanta, GA, United States.
J Pharm Anal. 2019 Jun;9(3):201-208. doi: 10.1016/j.jpha.2019.03.004. Epub 2019 Mar 14.
Thirty-two actinomycetes strains were isolated from sediment samples from 12 different sites at Lagos Lagoon and identified using standard physiological and biochemical procedures as well as 16S rDNA gene sequence analysis. Secondary metabolites were extracted from the strains and their anticancer activity on the K562 (Human acute myelocytic leukemia), HeLa (cervical carcinoma), AGS (Human gastric), MCF-7 (breast adenocarcinoma) and HL-60 (Human acute promyelocytic leukemia) cell lines was determined. The metabolic extracts exhibited cytotoxicity with IC values ranging from 0.030 mg/mL to 4.4 mg/mL. The ULS14 extract was cytotoxic against all the cell lines tested. The bioactivity-guided extraction and purification of the metabolic extracts from this strain yielded two purified anticancer compounds: ULDF4 and ULDF5. The structures of the extracted compounds were determined using spectroscopic analyses, including electrospray ionization mass spectrophotometer and nuclear magnetic resonance (1 Dimensional and 2 Dimensional), and were shown to be structurally similar to staurosporine and kigamicin. The IC of ULDF4 and ULDF5 against the HeLa cell line was 0.034 μg/mL and 0.075 μg/mL, respectively. This study is the first to reveal the anticancer potential of actinomycetes from Lagos Lagoon, which could be exploited for therapeutic purposes.
从拉各斯泻湖12个不同地点的沉积物样本中分离出32株放线菌菌株,并使用标准的生理生化程序以及16S rDNA基因序列分析进行鉴定。从这些菌株中提取次生代谢产物,并测定其对K562(人急性髓细胞白血病)、HeLa(宫颈癌)、AGS(人胃癌)、MCF-7(乳腺腺癌)和HL-60(人急性早幼粒细胞白血病)细胞系的抗癌活性。代谢提取物表现出细胞毒性,IC值范围为0.030 mg/mL至4.4 mg/mL。ULS14提取物对所有测试的细胞系均具有细胞毒性。对该菌株代谢提取物进行生物活性导向的提取和纯化,得到两种纯化的抗癌化合物:ULDF4和ULDF5。使用光谱分析(包括电喷雾电离质谱仪和核磁共振(一维和二维))确定提取化合物的结构,结果表明其结构与星形孢菌素和奇卡霉素相似。ULDF4和ULDF5对HeLa细胞系的IC值分别为0.034 μg/mL和0.075 μg/mL。本研究首次揭示了拉各斯泻湖放线菌的抗癌潜力,可用于治疗目的。