来自海洋海绵共生体的抗多药耐药病原体的细胞毒性和抗菌物质：桔霉素，一种青霉菌的次生代谢产物
Cytotoxic and antibacterial substances against multi-drug resistant pathogens from marine sponge symbiont: Citrinin, a secondary metabolite of Penicillium sp.
作者信息
Subramani Ramesh, Kumar Rohitesh, Prasad Pritesh, Aalbersberg William, Retheesh S T
机构信息
Centre for Drug Discovery and Conservation, Institute of Applied Sciences, The University of the South Pacific, Laucala Campus, Suva, Fiji Islands.
出版信息
Asian Pac J Trop Biomed. 2013 Apr;3(4):291-6. doi: 10.1016/S2221-1691(13)60065-9.
OBJECTIVE
To Isolate, purify, characterize, and evaluate the bioactive compounds from the sponge-derived fungus Penicillium sp. FF001 and to elucidate its structure.
METHODS
The fungal strain FF001 with an interesting bioactivity profile was isolated from a marine Fijian sponge Melophlus sp. Based on conidiophores aggregation, conidia development and mycelia morphological characteristics, the isolate FF001 was classically identified as a Penicillium sp. The bioactive compound was identified using various spectral analysis of UV, high resolution electrospray ionization mass spectra, 1H and 13C NMR spectral data. Further minimum inhibitory concentrations (MICs) assay and brine shrimp cytotoxicity assay were also carried out to evaluate the biological properties of the purified compound.
RESULTS
Bioassay guided fractionation of the EtOAc extract of a static culture of this Penicillium sp. by different chromatographic methods led the isolation of an antibacterial, anticryptococcal and cytotoxic active compound, which was identified as citrinin (1). Further, citrinin (1) is reported for its potent antibacterial activity against methicillin-resistant Staphylococcus aureus (S. aureus), rifampicin-resistant S. aureus, wild type S. aureus and vancomycin-resistant Enterococcus faecium showed MICs of 3.90, 0.97, 1.95 and 7.81 µg/mL, respectively. Further citrinin (1) displayed significant activity against the pathogenic yeast Cryptococcus neoformans (MIC 3.90 µg/mL), and exhibited cytotoxicity against brine shrimp larvae LD50 of 96 µg/mL.
CONCLUSIONS
Citrinin (1) is reported from sponge associated Penicillium sp. from this study and for its strong antibacterial activity against multi-drug resistant human pathogens including cytotoxicity against brine shrimp larvae, which indicated that sponge associated Penicillium spp. are promising sources of natural bioactive metabolites.
目的
从海绵来源的青霉菌Penicillium sp. FF001中分离、纯化、鉴定并评估其生物活性化合物，并阐明其结构。
方法
从斐济海洋海绵Melophlus sp.中分离出具有有趣生物活性谱的真菌菌株FF001。根据分生孢子梗聚集、分生孢子发育和菌丝体形态特征，经典地将分离株FF001鉴定为青霉菌。使用紫外光谱、高分辨率电喷雾电离质谱、1H和13C NMR光谱数据的各种光谱分析来鉴定生物活性化合物。还进行了进一步的最低抑菌浓度（MIC）测定和卤虫细胞毒性测定，以评估纯化化合物的生物学特性。
结果
通过不同色谱方法对该青霉菌静态培养物的乙酸乙酯提取物进行生物测定导向分级分离，得到一种具有抗菌、抗隐球菌和细胞毒性活性的化合物，鉴定为桔霉素（1）。此外，据报道桔霉素（1）对耐甲氧西林金黄色葡萄球菌、耐利福平金黄色葡萄球菌、野生型金黄色葡萄球菌和耐万古霉素粪肠球菌具有强效抗菌活性，其MIC分别为3.90、0.97、1.95和7.81 μg/mL。此外，桔霉素（1）对致病性酵母新型隐球菌显示出显著活性（MIC 3.90 μg/mL），对卤虫幼虫的细胞毒性LD50为96 μg/mL。
结论
本研究报道了来自海绵相关青霉菌的桔霉素（1）及其对包括卤虫幼虫细胞毒性在内的多药耐药人类病原体的强抗菌活性，这表明海绵相关青霉菌是天然生物活性代谢物的有前途来源。
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