PMID: 8588874Jan 1, 1996Paper

Selective inhibition of cyclic AMP-dependent protein kinase by amphiphilic triterpenoids and related compounds

Phytochemistry
B H Wang, G M Polya

Abstract

A set of plant- and animal-derived amphiphilic triterpenoids have been shown to be potent and selective inhibitors of the catalytic subunit of rat liver cyclic AMP-dependent protein kinase (cAK). Thus plant-derived 18 alpha- and 18 beta-glycyrrhetinic acid, ursolic acid, oleanolic acid and betulin and animal-derived lithocholic acid, 5-cholenic acid and lithocholic acid methyl ester are inhibitors of cAK with IC50 values (concentrations for 50% inhibition) in the range 4-20 microM. These compounds are ineffective or relatively ineffective as inhibitors of various other eukaryote signal-regulated protein kinases namely wheat embryo Ca(2+)-dependent protein kinase (CDPK), avian calmodulin-dependent myosin light chain kinase (MLCK) and rat brain Ca(2+)- and phospholipid-dependent protein kinase C (PKC). These naturally occurring triterpenoids have a common structural motif involving polar residues located at opposite ends of an otherwise non-polar triterpenoid nucleus. A variety of triterpenoids not possessing this structural motif are relatively inactive as inhibitors of cAK and of CDPK, PKC and MLCK. The terpenoid amphiphilic compound crocetin is also a potent and relatively selective inhibitor of cAK (IC50 value for cAK 3.0 mic...Continue Reading

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Citations

May 13, 2011·Journal of Natural Products·Mayuko TakemuraAkira Hara
Nov 23, 2006·Natural Product Reports·Pavel A Krasutsky
Jul 26, 2006·Journal of Asian Natural Products Research·X-C ShenZ-Y Qian
Sep 11, 2010·Critical Reviews in Food Science and Nutrition·S Zahra Bathaie, S Zeinab Mousavi
Jun 1, 1996·Biological Chemistry Hoppe-Seyler·Z X LuG M Polya
Jun 1, 1996·Phytochemistry·M Hasmeda, G M Polya
Mar 22, 2012·Journal of Dietary Supplements·Catherine UlbrichtMinney Varghese
Jul 12, 2005·Expert Opinion on Investigational Drugs·Donglei YuKuo-Hsiung Lee
Aug 5, 2006·Medicinal Research Reviews·Donglei YuKuo-Hsiung Lee
Mar 1, 2006·Journal der Deutschen Dermatologischen Gesellschaft = Journal of the German Society of Dermatology : JDDG·Constance HuykeChristoph M Schempp
Jul 18, 2012·Asian Pacific Journal of Cancer Prevention : APJCP·Lim Yang MooiYeo Chew Chieng
Apr 14, 2015·BioMed Research International·Sylwia Katarzyna KrólAndrzej Stepulak
Aug 18, 2012·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·Thangaiyan RadhigaKodukkur Viswanathan Pugalendi
Jan 1, 2007·Toxicology Mechanisms and Methods·S SenthilK V Pugalendi

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