Paenidigyamycin g: 1-acetyl-2,4-dimethyl-3-phenethyl-1H-imidazol-3-ium

Gilbert Mawuli Tetevi, Samuel Kwain, Thomas Mensah, Anil Sazak Camas, Mustafa Camas, Aboagye Kwarteng Dofuor, Faustus Akankperiwen Azerigyik, Emmanuel Oluwabusola, Hai Deng, Marcel Jaspars, Kwaku Kyeremeh*

*Corresponding author for this work

Research output: Contribution to journalComment/debatepeer-review

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Abstract

The Ghanaian Paenibacillus sp. DE2SH (GenBank Accession Number: MH091697) is a prolific producer of potent antiparasitic alkaloids. Further detailed study of the culture broth of this strain produced the compound Paenidigyamycin G (1), which is a derivative of the known antiparasitic compound Paenidigyamycin A (2). Compound (1) was isolated on HPLC at tR ≈ 37.5 min and its structure determined by IR, UV, MS, 1D, and 2D-NMR data. Compound 1 produced weak to moderate antileishmanial and antitrypanosomal activity when tested against Leishmania donovani (Laveran and Mesnil) Ross (D10) and Trypanosoma brucei subsp. brucei strain GUTat 3.1 with IC50 = 115.41 and 28.75 µM, respectively. This result is interesting since the parent compound 2 is known to possess consistent and potent antiparasitic activity. However, 1 displayed a promising selectivity profile towards T. brucei subsp. brucei due to its relatively low toxicity against normal mouse macrophages RAW 264.7 cells (SI = 8.70). Given that compound 1 is also the main metabolite found in the hexane fraction of all extracts produced by Paenibacillus sp. DE2SH when it is co-cultured with other bacteria strains, it must possess some unique biological functions which should make it an excellent candidate for further biological activity screening in other bioassays.

Original languageEnglish
Article numberM1094
Number of pages9
JournalMolBank
Volume2019
Issue number4
DOIs
Publication statusPublished - 21 Nov 2019

Keywords

  • Alkaloid
  • Antileishmanials
  • Antitrypanosomals
  • Imidazole
  • Leishmaniasis
  • Paenibacillus
  • Trypanosomiasis

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