Study of Endothelial Protective Activity of Phenol-Derived Thrombin and Arginase-2 Inhibitors KUD-259 and KUD-974

M V Pokrovskii; M V Korokin; K V Kudryavtsev; T G Pokrovskaya; O S Gudyrev; V V Gureev; L V Korokina; S V Povetkin

doi:10.1007/s10517-017-3822-y

Study of Endothelial Protective Activity of Phenol-Derived Thrombin and Arginase-2 Inhibitors KUD-259 and KUD-974

Bull Exp Biol Med. 2017 Aug;163(4):436-438. doi: 10.1007/s10517-017-3822-y. Epub 2017 Aug 29.

Authors

M V Pokrovskii¹, M V Korokin², K V Kudryavtsev¹, T G Pokrovskaya¹, O S Gudyrev¹, V V Gureev¹, L V Korokina¹, S V Povetkin¹

Affiliations

¹ Department of Pharmacology, Medical School, Belgorod State University, Belgorod, Russia.
² Department of Pharmacology, Medical School, Belgorod State University, Belgorod, Russia. mkorokin@mail.ru.

PMID: 28853095
DOI: 10.1007/s10517-017-3822-y

Abstract

We performed correction of endothelial dysfunction with phenol derivatives KUD-259 and KUD-974 containing heteroatomic and heterocyclic structures. Pharmacological activity of KUD-259 and KUD-974 surpassed that of L-norvaline, a non-selective arginase inhibitor.

Keywords: L-NAME; L-norvaline; arginase; modeled endothelial dysfunction; nitric oxide.

MeSH terms

Animals
Arginase / antagonists & inhibitors*
Endothelium, Vascular / drug effects
Endothelium, Vascular / metabolism
Male
NG-Nitroarginine Methyl Ester / pharmacology
Nitric Oxide / pharmacology
Phenol / chemistry*
Rats
Rats, Wistar
Signal Transduction / drug effects
Thrombin / chemistry*
Valine / analogs & derivatives
Valine / pharmacology

Substances

Nitric Oxide
Phenol
norvaline
Thrombin
Arginase
Valine
NG-Nitroarginine Methyl Ester