Show simple item record

dc.contributor.authorHochfellner, C.
dc.contributor.authorEvangelopoulos, D.
dc.contributor.authorZloh, Mire
dc.contributor.authorWube, A.
dc.contributor.authorGuzman, J. D.
dc.contributor.authorMchugh, T. D.
dc.contributor.authorKunert, O.
dc.contributor.authorBhakta, S.
dc.contributor.authorBucar, F.
dc.date.accessioned2016-04-06T08:56:28Z
dc.date.available2016-04-06T08:56:28Z
dc.date.issued2015-04-01
dc.identifier.citationHochfellner , C , Evangelopoulos , D , Zloh , M , Wube , A , Guzman , J D , Mchugh , T D , Kunert , O , Bhakta , S & Bucar , F 2015 , ' Antagonistic effects of indoloquinazoline alkaloids on antimycobacterial activity of evocarpine ' , Journal of Applied Microbiology , vol. 118 , no. 4 , pp. 864-872 . https://doi.org/10.1111/jam.12753
dc.identifier.issn1364-5072
dc.identifier.otherPURE: 9507724
dc.identifier.otherPURE UUID: a5c0306a-f495-4a04-91ac-09e2082959fd
dc.identifier.otherScopus: 84924914257
dc.identifier.urihttp://hdl.handle.net/2299/16967
dc.description.abstractThe interaction of quinolone and indoloquinazoline alkaloids concerning their antimycobacterial activity was studied. Methods and Results: The antimycobacterial and modulating activity of evodiamine (1), rutaecarpine (2) and evocarpine (3) was tested on mycobacteria including three multidrug-resistant (MDR) clinical isolates of Mycobacterium tuberculosis. Antagonistic effects were concluded from fractional inhibitory concentration (FICI) values. Interaction energies of the compounds were calculated using GLUE docking module implemented in GRID. 1 and 2 exhibited weak inhibition of rapidly growing mycobacteria, however, 1 was active against Myco. tuberculosis H37Rv (MIC = 10 mg l<sup>-1</sup>) while 2 was inactive. Both 1 and 2 showed a marked antagonistic effect on the susceptibility of different mycobacterial strains to 3 giving FICI values between 5 and 9. The interaction energies between compounds 1 and 2 with compound 3 suggested the possibility of complex formation in solution. Conclusions: Indoloquinazoline alkaloids markedly reduce the antimycobacterial effect of the quinolone alkaloid evocarpine. Complex formation may play a role in the attenuation of its antimycobacterial activity. Significance and Impact of the Study: This study gives a striking example of antagonism between compounds present in the same plant extract which should be considered in natural product based screening projects. Copyrighten
dc.format.extent9
dc.language.isoeng
dc.relation.ispartofJournal of Applied Microbiology
dc.subjectEuodia
dc.subjectAntagonism
dc.subjectEvocarpine
dc.subjectEvodiamine
dc.subjectModelling
dc.subjectMycobacteria
dc.subjectRutaecarpine
dc.subjectApplied Microbiology and Biotechnology
dc.subjectBiotechnology
dc.titleAntagonistic effects of indoloquinazoline alkaloids on antimycobacterial activity of evocarpineen
dc.contributor.institutionSchool of Life and Medical Sciences
dc.contributor.institutionHealth & Human Sciences Research Institute
dc.contributor.institutionDepartment of Pharmacy
dc.contributor.institutionMedicinal and Analytical Chemistry
dc.description.statusPeer reviewed
rioxxterms.versionofrecordhttps://doi.org/10.1111/jam.12753
rioxxterms.typeJournal Article/Review
herts.preservation.rarelyaccessedtrue


Files in this item

FilesSizeFormatView

There are no files associated with this item.

This item appears in the following Collection(s)

Show simple item record