title: Evaluation of Potential Thrombin Inhibitors from the White Mangrove (Laguncularia racemosa (L.) C.F. Gaertn.).
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.
authors.affiliation: Universidade Estadual Paulista Julio de Mesquita Filho, UNESP, Praça Infante Dom Henrique, s/n, 11330-900 São Vicente, SP, Brazil. cfabri3@gmail.com.
authors.forename: Caroline Fabri Bittencourt
authors.initials: CF
authors.lastname: Rodrigues
authors.affiliation: Universidade Estadual Paulista Julio de Mesquita Filho, UNESP, Praça Infante Dom Henrique, s/n, 11330-900 São Vicente, SP, Brazil. henriquehg@gmail.com.
authors.forename: Henrique Hessel
authors.initials: HH
authors.lastname: Gaeta
authors.affiliation: Universidade Estadual Paulista Julio de Mesquita Filho, UNESP, Praça Infante Dom Henrique, s/n, 11330-900 São Vicente, SP, Brazil. belchor.mariana@gmail.com.
authors.forename: Mariana Novo
authors.initials: MN
authors.lastname: Belchor
authors.affiliation: Departamento de Botânica, Instituto de Biociências, Universidade de São Paulo, Rua do Matão, 277, 05508-090 São Paulo, SP, Brazil. marcelopena@ib.usp.br.
authors.forename: Marcelo José Pena
authors.initials: MJ
authors.lastname: Ferreira
authors.affiliation: Universidade Estadual Paulista Julio de Mesquita Filho, UNESP, Praça Infante Dom Henrique, s/n, 11330-900 São Vicente, SP, Brazil. mvpinho@gmail.com.
authors.forename: Marcus Vinícius Terashima
authors.initials: MV
authors.lastname: Pinho
authors.affiliation: Unicastelo-Universidade Camilo Castelo Branco, Campus São Paulo, Rua Carolina Fonseca, 584 Itaquera São Paulo-SP, 08230-030 São Paulo, SP, Brazil. gaveira@yahoo.com.br.
authors.forename: Daniela de Oliveira
authors.initials: Dde O
authors.lastname: Toyama
authors.affiliation: Universidade Estadual Paulista Julio de Mesquita Filho, UNESP, Praça Infante Dom Henrique, s/n, 11330-900 São Vicente, SP, Brazil. marcoshikaritoyama@gmail.com.
authors.forename: Marcos Hikari
authors.initials: MH
authors.lastname: Toyama
mesh_terms: D001777:Blood Coagulation / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D029764:Combretaceae / Q000737:chemistry*; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology*; D018515:Plant Leaves / Q000737:chemistry*; D013917:Thrombin / Q000037:antagonists & inhibitors*
chemical_list: D005419:Flavonoids; D010936:Plant Extracts; D013917:Thrombin
keywords: Laguncularia racemosa; flavonoids; plasma coagulation; thrombin