AI Article Synopsis
- Researchers studied extracts from the cyanobacterium Anabaena compacta and isolated two compounds: spumigin J (1) and the known thrombin inhibitor spumigin A (2).
- Both compounds were effective at inhibiting thrombin, with EC(50) values of 4.9 μM for spumigin J and 2.1 μM for spumigin A.
- Advanced methods indicated that spumigin A, particularly with a 2S-4-methylproline configuration, was a stronger inhibitor of thrombin compared to other tested compounds.
Article Abstract
Bioassay-guided investigation of the cyanobacterium Anabaena compacta extracts afforded spumigin J (1) and the known thrombin inhibitor spumigin A (2). The absolute configuration of 1 was analyzed by advanced Marfey's methodology. Compounds 1 and 2 inhibited thrombin with EC(50) values of 4.9 and 2.1 μM, and 0.7 and 0.2 μM in the cathepsin B inhibitory assay, respectively. The MM-GBSA methodology predicted spumigin A with 2S-4-methylproline as the better thrombin inhibitor.
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| http://dx.doi.org/10.1021/np300282a | DOI Listing |
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