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Mar. Drugs 2017, 15(9), 275; doi:10.3390/md15090275

FVIIa-sTF and Thrombin Inhibitory Activities of Compounds Isolated from Microcystis aeruginosa K-139

1
Faculty of Pharmacy, Meijo University, Tempaku, Nagoya 468-8503, Japan
2
College of Agriculture, Ibaraki University, Ami, Ibaraki 300-0393, Japan
3
Graduate School of Environmental and Human Sciences, Meijo University, Tempaku, Nagoya 468-8503, Japan
*
Authors to whom correspondence should be addressed.
Received: 8 July 2017 / Revised: 11 August 2017 / Accepted: 25 August 2017 / Published: 30 August 2017
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Abstract

The rise of bleeding and bleeding complications caused by oral anticoagulant use are serious problems nowadays. Strategies that block the initiation step in blood coagulation involving activated factor VII-tissue factor (fVIIa-TF) have been considered. This study explores toxic Microcystis aeruginosa K-139, from Lake Kasumigaura, Ibaraki, Japan, as a promising cyanobacterium for isolation of fVIIa-sTF inhibitors. M. aeruginosa K-139 underwent reversed-phase solid-phase extraction (ODS-SPE) from 20% MeOH to MeOH elution with 40%-MeOH increments, which afforded aeruginosin K-139 in the 60% MeOH fraction; micropeptin K-139 and microviridin B in the MeOH fraction. Aeruginosin K-139 displayed an fVIIa-sTF inhibitory activity of ~166 µM, within a 95% confidence interval. Micropeptin K-139 inhibited fVIIa-sTF with EC50 10.62 µM, which was more efficient than thrombin inhibition of EC50 26.94 µM. The thrombin/fVIIa-sTF ratio of 2.54 in micropeptin K-139 is higher than those in 4-amidinophenylmethane sulfonyl fluoride (APMSF) and leupeptin, when used as positive controls. This study proves that M. aeruginosa K-139 is a new source of fVIIa-sTF inhibitors. It also opens a new avenue for micropeptin K-139 and related depsipeptides as fVIIa-sTF inhibitors. View Full-Text
Keywords: fVIIa-sTF inhibitors; Microcystis; blood coagulation cascade; LC-MS; aeruginosin K-139; thrombin; micropeptin K-139; microviridin B fVIIa-sTF inhibitors; Microcystis; blood coagulation cascade; LC-MS; aeruginosin K-139; thrombin; micropeptin K-139; microviridin B
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Anas, A.R.J.; Mori, A.; Tone, M.; Naruse, C.; Nakajima, A.; Asukabe, H.; Takaya, Y.; Imanishi, S.Y.; Nishizawa, T.; Shirai, M.; Harada, K.-I. FVIIa-sTF and Thrombin Inhibitory Activities of Compounds Isolated from Microcystis aeruginosa K-139. Mar. Drugs 2017, 15, 275.

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