Document Detail


Wound healing activity and docking of glycogen-synthase-kinase-3-beta-protein with isolated triterpenoid lupeol in rats.
MedLine Citation:
PMID:  18222664     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A triterpene compound lupeol isolated from petroleum ether extract of leaves of Celastrus paniculatus was screened for wound healing activity (8 mg/ml of 0.2% sodium alginate gel) by excision, incision and dead space wound models on Swiss Albino rats (175-225 g). In lupeol treated groups wound healing activity was more significant (17.83+/-0.48) than the standard skin ointment nitrofurazone (18.33+/-0.42). Epithelialization of the incision wound was faster with a high rate of wound contraction (571.50+/-5.07) as compared with the control group. In dead space wound model also the weight of the granulation tissue of the lupeol treated animal was increased indicating increase of collagenation and absence of monocytes. The comparative docking of isolated lupeol molecule and standard drug nitrofurazone to glycogen synthase kinase 3-beta protein by Wnt signaling pathway also supported the wound healing property of lupeol. The activation domain of GSK3-beta consisted of Tyr216, with residues Asn64, Gly65, Ser66, Phe67, Gly68, Val70, Lys85, Leu132, Val135, Asp181 in the active pocket docked with lupeol at the torsional degree of freedom 0.5 units with Lamarckian genetic algorithm showed the inhibition constant of 1.38 x 10(-7). The inhibition constant of nitrofurazone was only 1.35 x 10(-4).
Authors:
B G Harish; V Krishna; H S Santosh Kumar; B M Khadeer Ahamed; R Sharath; H M Kumara Swamy
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Publication Detail:
Type:  Journal Article     Date:  2008-01-28
Journal Detail:
Title:  Phytomedicine : international journal of phytotherapy and phytopharmacology     Volume:  15     ISSN:  1618-095X     ISO Abbreviation:  Phytomedicine     Publication Date:  2008 Sep 
Date Detail:
Created Date:  2008-08-11     Completed Date:  2008-10-16     Revised Date:  2011-11-02    
Medline Journal Info:
Nlm Unique ID:  9438794     Medline TA:  Phytomedicine     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  763-7     Citation Subset:  IM    
Affiliation:
Department of Biotechnology and Bioinformatics, Kuvempu University, Shimoga 577451, Karnataka, India.
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MeSH Terms
Descriptor/Qualifier:
Animals
Binding Sites
Enzyme Inhibitors / metabolism,  pharmacology*
Glycogen Synthase Kinase 3 / antagonists & inhibitors*,  metabolism
Pentacyclic Triterpenes
Rats
Triterpenes / metabolism,  pharmacology*
Wound Healing / drug effects*
Chemical
Reg. No./Substance:
0/Enzyme Inhibitors; 0/Pentacyclic Triterpenes; 0/Triterpenes; 545-47-1/lupeol; EC 2.7.11.1/glycogen synthase kinase 3 beta; EC 2.7.11.26/Glycogen Synthase Kinase 3

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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