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Mar. Drugs 2015, 13(7), 4505-4519; doi:10.3390/md13074505

Evaluation of Potential Thrombin Inhibitors from the White Mangrove (Laguncularia racemosa (L.) C.F. Gaertn.)

1
Universidade Estadual Paulista Julio de Mesquita Filho, UNESP, Praça Infante Dom Henrique, s/n, 11330-900 São Vicente, SP, Brazil
2
Departamento de Botânica, Instituto de Biociências, Universidade de São Paulo, Rua do Matão, 277, 05508-090 São Paulo, SP, Brazil
3
Unicastelo—Universidade Camilo Castelo Branco, Campus São Paulo, Rua Carolina Fonseca, 584 Itaquera São Paulo-SP, 08230-030 São Paulo, SP, Brazil
*
Author to whom correspondence should be addressed.
Academic Editor: Orazio Taglialatela-Scafati
Received: 10 April 2015 / Revised: 9 July 2015 / Accepted: 10 July 2015 / Published: 21 July 2015
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Abstract

The aim of this work was to verify the effects of methanol (MeOH) and hydroalcoholic (HA) extracts and their respective partition phases obtained from white mangrove (Laguncularia racemosa (L.) C.F. Gaertn.) leaves on human thrombin activity. Among the extracts and phases tested, only the ethyl acetate and butanolic partitions significantly inhibited human thrombin activity and the coagulation of plasma in the presence of this enzyme. Chromatographic analyses of the thrombin samples incubated with these phases revealed that different compounds were able to interact with thrombin. The butanolic phase of the MeOH extract had the most potent inhibitory effects, reducing enzymatic activity and thrombin-induced plasma coagulation. Two glycosylated flavonoids in this partition were identified as the most potent inhibitors of human thrombin activity, namely quercetin-3-O-arabinoside (QAra) and quercetin-3-O-rhamnoside (Qn). Chromatographic analyses of thrombin samples incubated with these flavonoids demonstrated the chemical modification of this enzyme, suggesting that the MeOH extract contained other compounds that both induced structural changes in thrombin and diminished its activity. In this article, we show that despite the near absence of the medical use of mangrove compounds, this plant contains natural compounds with potential therapeutic applications. View Full-Text
Keywords: thrombin; Laguncularia racemosa; flavonoids; plasma coagulation thrombin; Laguncularia racemosa; flavonoids; plasma coagulation
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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MDPI and ACS Style

Rodrigues, C.F.B.; Gaeta, H.H.; Belchor, M.N.; Ferreira, M.J.P.; Pinho, M.V.T.; Toyama, D.O.; Toyama, M.H. Evaluation of Potential Thrombin Inhibitors from the White Mangrove (Laguncularia racemosa (L.) C.F. Gaertn.). Mar. Drugs 2015, 13, 4505-4519.

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