Paenidigyamycin G: 1-Acetyl-2,4-dimethyl-3-phenethyl-1H-imidazol-3-ium
Date
2019-11-21
Journal Title
Journal ISSN
Volume Title
Publisher
molbank
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 PaenidigyamycinA(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 M, 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.
Description
Research Article
Keywords
Paenibacillus, alkaloid, imidazole, antileishmanials, leishmaniasis, antitrypanosomals, trypanosomiasis