Isolation and Difference in Anti-Staphylococcus aureus Bioactivity of Curvularin Derivates from Fungus Eupenicillium sp. |
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Authors: | Lian Wu Xie Yong Chang Ouyang Kun Zou Guang Hua Wang Min Jie Chen Hui Min Sun Shi Kun Dai and Xiang Li |
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Institution: | (1) Key Laboratory of Marine Bio-resources Sustainable Utilization (LMB-CAS), Guangdong Key Laboratory of Marine Materia Medica (LMM-GD), South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou, 510301, People’s Republic of China;(2) Central South University of Forestry & Technology, Changsha, 410004, People’s Republic of China;(3) Medical Science College of China Three Gorges University, Yichang, 443002, People’s Republic of China; |
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Abstract: | With the anti-microbial and anti-tumor composite screening model, bioassay-guided fractionation led to the isolation of two
structurally related bioactive compounds, curvularin and αβ-dehydrocurvularin, from ethyl acetate extract of Eupenicillium sp. associated with marine sponge Axinella sp. Further study on the structure–activity relationship demonstrated that both compounds exhibited differences in bioactive
profiles which are highly associated with their minor structural differences. Both curvularin and αβ-dehydrocurvularin have
similar level of anti-fungal and anti-tumorous activity, while αβ-dehydrocurvularin is active against Staphylococcus aureus with a minimal inhibitory concentration of 375 μg/ml but curvularin does not. No detectable activity against Gram-negative
bacteria such as Escherichia coli and Pseudomonas aeruginosa exists for both compounds. It is suggested that the partial planar backbone structure, due to the conjugation of π electrons
in the presence of a 3,4-double bond and the carbonyl group at position C-2 in αβ-dehydrocurvularin, acts as a key factor
for the inhibition of S. aureus, a Gram-positive low G + C bacteria that are often the hospital-acquired and/or community-acquired pathogen. |
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