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Volumn 20, Issue 2, 2010, Pages 513-515

Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa

Author keywords

Hedyotis diffusa; Human neutrophil elastase; Iridoid glycosides

Indexed keywords

6 O 4 COUMAROYL SCANDOSIDE METHYL ESTER; 6 O 4 FERULOYL SCANDOSIDE METHYL ESTER; 6 O 4 METHOXYCINNAMOYL SCANDOSIDE METHYL ESTER; EPIGALLOCATECHIN GALLATE; HEDYOTIS DIFFUSA EXTRACT; IRIDOID; LEUKOCYTE ELASTASE; LEUKOCYTE ELASTASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 72249085972     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.11.109     Document Type: Article
Times cited : (47)

References (25)
  • 16
    • 72249118303 scopus 로고    scopus 로고
    • note
    • R, 33 min, 40 mg), respectively.
  • 20
    • 72249084038 scopus 로고    scopus 로고
    • note
    • -.
  • 23
    • 34547726120 scopus 로고    scopus 로고
    • note
    • HNE inhibitory activity was evaluated according to previously described procedure (Benedek, B.; Kopp, B.; Melzig, M. F. J. Ethnopharmacol. 2007, 113, 312.). Briefly, 125 μL of substrate solution [1.4 mM N-methoxysuccinyl-ala-ala-pro-val-p-nitroanilide, in Tris-HCl buffer (pH 7.5)], 60 μL of test solution [stock solutions of the test compounds were dissolved in 500 μL DMSO and diluted with Tris-HCl buffer to give the final sample concentrations] and 390 μL of Tris-HCl buffer were mixed and vortexed. After addition of 25 μL enzyme solution (approx. 0.18 U elastase from human neutrophils, EC 3.4.21.37, from Serva, Heidelberg, Germany) the samples were incubated for 1 h at 37 °C. After the reaction was stopped by addition of 500 μL soybean trypsin inhibitor [Sigma, Germany; 0.2 mg/mL Tris-HCl buffer (pH 7.5)], absorbance was immediately measured at 405 nm. Epigallocatechin gallate (EGCG) (Sigma, Germany) was used as a positive control.
  • 24
    • 72249111203 scopus 로고    scopus 로고
    • note
    • To build a structural model for the HNE in complex with compound 1, compound 1 was docked into the HNE (PDB code: 1HNE) by cdocker program in the software Discovery Studio 2.1 (Accelrys). Ten initial random conformations were taken and 10 initial poses were chosen for final refinement. CHARMm forcefield was employed for molecular dynamics and dynamics steps and target temperature were set to be 1000 and 1000 K, respectively. Figures were drawn by using the software Discovery Studio 2.1.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.