Kumar C Ganesh, Mongolla Poornima, Sujitha Pombala, Joseph Joveeta, Babu K Suresh, Suresh Gangi, Ramakrishna Kallaganti Venkata Siva, Purushotham Uppula, Sastry G Narahari, Kamal Ahmed
Chemical Biology Laboratory, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad, Andhra Pradesh 500007 India.
Springerplus. 2013 Dec;2(1):122. doi: 10.1186/2193-1801-2-122. Epub 2013 Mar 21.
In an ongoing survey for bioactive potential of microorganisms from different biosphere zones of India, a new Chrysosporium lobatum strain BK-3 was isolated from soil sample collected from a biodiversity hotspot, Kaziranga National Park, Assam, India. Bioactivity-guided purification resulted in the isolation of two bioactive compounds whose chemical structures were elucidated by (1)H and (13)C Nuclear Magnetic Resonance (NMR), 2D-NMR, Fourier Transform Infra-red (FT-IR) and mass spectroscopic techniques, and were identified as α, β-dehydrocurvularin and curvularin. Only curvularin exhibited 80% acetylcholinesterase (AChE) inhibitory activity. Detailed ligand receptor binding interactions were studied for curvularin by molecular docking studies. Further, both curvularin and α, β-dehydrocurvularin had similar level of cytotoxicity against different human tumour cell lines like A549, HeLa, MDA-MB-231 and MCF-7, while α, β-dehydrocurvularin was active against COLO 205 with a IC50 of 7.9 μM, but curvularin was inactive. α, β-Dehydrocurvularin also showed good superoxide anion scavenging activity with an EC50 value of 16.71 μg ml(-1). Hence, both these compounds exhibited differences in bioactive profiles and this was probably associated with their minor structural differences. This is a first report on bioactive compounds exhibiting AChE inhibitory, cytotoxicity and antioxidant activities from Chrysosporium lobatum strain BK-3.
在一项对来自印度不同生物圈区域微生物生物活性潜力的持续调查中,从印度阿萨姆邦卡齐兰加国家公园(一个生物多样性热点地区)采集的土壤样本中分离出了一种新的裂褶菌菌株BK - 3。通过生物活性导向的纯化方法,分离出了两种生物活性化合物,其化学结构通过(1)H和(13)C核磁共振(NMR)、二维NMR、傅里叶变换红外(FT - IR)和质谱技术得以阐明,并被鉴定为α,β - 脱氢弯孢霉菌素和弯孢霉菌素。只有弯孢霉菌素表现出80%的乙酰胆碱酯酶(AChE)抑制活性。通过分子对接研究对弯孢霉菌素的详细配体 - 受体结合相互作用进行了研究。此外,弯孢霉菌素和α,β - 脱氢弯孢霉菌素对不同的人类肿瘤细胞系如A549、HeLa、MDA - MB - 231和MCF - 7具有相似水平的细胞毒性,而α,β - 脱氢弯孢霉菌素对COLO 205有活性,IC50为7.9 μM,但弯孢霉菌素无活性。α,β - 脱氢弯孢霉菌素还表现出良好的超氧阴离子清除活性,EC50值为16.71 μg ml(-1)。因此,这两种化合物在生物活性谱方面存在差异,这可能与它们微小的结构差异有关。这是关于裂褶菌菌株BK - 3中表现出AChE抑制、细胞毒性和抗氧化活性的生物活性化合物的首次报道。