Planta Med 2000; 66(4): 324-328
DOI: 10.1055/s-2000-8549
Original Paper
Georg Thieme Verlag Stuttgart · New York

Effects of Some Iridoids from Plant Origin on Arachidonic Acid Metabolism in Cellular Systems

Paulina  Bermejo Benito1,*, Ana  María Díaz Lanza2 , Ana  Maria Silván Sen1 , Javier  De Santos Galindez2 , Lidia  Fernandez Matellano2 , Aurora  Sanz Gómez1 , María  José Abad Martínez1
  • 1 Department of Pharmacology, Faculty of Pharmacy, University Complutense, Madrid, Spain
  • 2 Department of Pharmacology, Faculty of Pharmacy, University Alcala, Madrid, Spain
Further Information

Publication History

Publication Date:
31 December 2000 (online)


Seven iridoid glycosides isolated from different extracts of Scrophularia scorodonia L., namely bartsioside, aucubin, harpagide, harpagoside, 8-acetylharpagide, scorodioside and scropolioside B, had been evaluated for their in vitro anti-inflammatory activity in cellular systems generating COX and LOX metabolites. Structure-activity relationships obtained from in vitro screening results were discussed. Most compounds assayed did not exhibit any significant effect on PGE2- and LTC4-release from calcium ionophore-stimulated mouse peritoneal macrophages. In the LTC4-assay, only aucubin showed a significant effect, with an IC50 value of 72 μM. Harpagoside and harpagide also inhibited release of LTC4, but neither effect reached statistical significance. The release of PGE2 by mouse peritoneal macrophages stimulated with calcium ionophore was inhibited by harpagoside and 8-acetylharpagide, but this effect is not statistically significant. However, most iridoids assayed showed a significant effect on TXB2-release from calcium ionophore-stimulated human platelets, with inhibition percentages slightly lower than the reference drug ibuprofen. Only harpagide, scorodioside and scropolioside B had no significant effect on TXB2-release. Our results indicate that selective inhibition of the TX-synthase enzyme may be the primary target of action of most of these iridoids, and one of the mechanisms through which they exert their anti-inflammatory effects.


COX:cyclooxygenase5-LOX:5-lipoxygenaseAA:arachidonic acidPGs:prostaglandinsTXs:thromboxanesLTs:leukotrienesNSAIDs:non-steroidal anti-inflammatory drugsHETEs:hydroxy-eicosatetraenoic acidsNDGA:nordihydroguaiaretic acidDMSO:dimethyl sulfoxideEDTA:ethylenediaminotetraacetic acidMTT:3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromideELISA:enzyme-linked immunosorbent assayPBS:Dulbecco's phosphate-buffered salineDMEM:Dulbecco's modified Eagle's mediumFCS:fetal calf serumPMA:phorbol myristate acetatePKC:protein kinase C


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Paulina Bermejo Benito

Department of Pharmacology Faculty of Pharmacy University Complutense

28040 Madrid



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