Abstract:
:An anti-fibrotic compound produced by Streptomycesn xiamenensis, found in mangrove sediments, was investigated for possible therapeutic effects against fibrosis. The compound, N-[[3,4-dihydro-3S-hydroxy-2S-methyl-2-(4'R-methyl-3'S-pentenyl)-2H-1-benzopyran-6-yl]carbonyl]-threonine (1), was isolated from crude extracts and its structure, including the absolute configuration was determined by extensive spectroscopic data analyses, Mosher's method, Marfey's reagent and quantum mechanical calculations. In terms of biological effects, this compound inhibits the proliferation of human lung fibroblasts (WI26), blocks adhesion of human acute monocytic leukemia cells (THP-1) to a monolayer of WI26 cells, and reduces the contractile capacity of WI26 cells in three-dimensional free-floating collagen gels. Altogether, these data indicate that we have identified a bioactive alkaloid (1) with multiple inhibitory biological effects on lung excessive fibrotic characteristics, that are likely involved in fibrosis, suggesting that this molecule might indeed have therapeutic potential against fibrosis.
journal_name
Mar Drugsjournal_title
Marine drugsauthors
Xu MJ,Liu XJ,Zhao YL,Liu D,Xu ZH,Lang XM,Ao P,Lin WH,Yang SL,Zhang ZG,Xu Jdoi
10.3390/md10030639subject
Has Abstractpub_date
2012-03-01 00:00:00pages
639-54issue
3issn
1660-3397pii
marinedrugs-10-00639journal_volume
10pub_type
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