title: Identification of MMP-1 and MMP-9 inhibitors from the roots of Eleutherococcus divaricatus, and the PAMPA test.
abstract: The purpose of this study was the isolation of metalloproteinases MMP-1 and MMP-9 inhibitors from the chloroform extract of the Eleutherococcus divaricatus roots. Using GC-MS, (1)H and (13)C NMR, HMQC, HMBC, COSY and DEPT, (+)-sesamin has been identified as a new anti-MMP inhibitor. We report for the first time that (+)-sesamin inhibited MMP-1 and MMP-9 activity in 40% and 17%, respectively. The high inhibitory potential has been shown by ursolic acid (90.9% and 89.8% for MMP-1 and MMP-9). In the PAMPA test, the Pe value for sesamin was established as 17.4 × 10(-6) cm/s, that for ursolic acid as 30.0 × 10(- 6) cm/s. Verapamil and theophylline were used as a positive and negative control (Pe 42.1 and 2.9 × 10(-6) cm/s). To our best knowledge, no information was available on this activity of sesamin and other compounds. These studies provide a biochemical basis for the regulation of MMP-1 and MMP-9 by E. divaricatus compounds.
authors.affiliation: a Department of Pharmacognosy , Jagiellonian University, Collegium Medicum , 9 Medyczna Street, 30 - 688 Cracow , Poland.
authors.forename: Daniel
authors.initials: D
authors.lastname: Załuski
authors.affiliation: b Department of Chemistry , Analytical Laboratory, UMCS , M. Curie Skłodowska Sq, Lublin , Poland.
authors.forename: Ewaryst
authors.initials: E
authors.lastname: Mendyk
authors.affiliation: c Chair and Department of Pharmaceutical Botany , Medical University of Lublin , 1 Chodźki Street, 20-093 Lublin , Poland.
authors.forename: Helena D
authors.initials: HD
authors.lastname: Smolarz
mesh_terms: D004149:Dioxoles / Q000302:isolation & purification / Q000494:pharmacology*; D028001:Eleutherococcus / Q000737:chemistry*; D008401:Gas Chromatography-Mass Spectrometry; D017705:Lignans / Q000302:isolation & purification / Q000494:pharmacology*; D020781:Matrix Metalloproteinase 1 / Q000187:drug effects*; D020780:Matrix Metalloproteinase 9 / Q000187:drug effects*; D061965:Matrix Metalloproteinase Inhibitors / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry; D012995:Solubility; D013806:Theophylline / Q000494:pharmacology; D014315:Triterpenes / Q000494:pharmacology; D014700:Verapamil / Q000494:pharmacology; D000097245:Ursolic Acid
chemical_list: D004149:Dioxoles; D017705:Lignans; D020781:Matrix Metalloproteinase 1; D020780:Matrix Metalloproteinase 9; D061965:Matrix Metalloproteinase Inhibitors; D013806:Theophylline; D014315:Triterpenes; D014700:Verapamil; D000097245:Ursolic Acid; C054125:sesamin
keywords: (+)-sesamin; Eleutherococcus divaricatus; MMPs; NMR; PAMPA test; inhibitor