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In Vitro Antifungal and Antibacterial Activities of Pentacycloundecane Tetra‐Amines
Author(s) -
Onajole Oluseye K.,
Coovadia Yacoob,
Govender Thavendran,
Kruger Hendrik G.,
Maguire Glenn E. M.,
Naidu Dianithi,
Singh Nisha,
Govender Patrick
Publication year - 2011
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2011.01055.x
Subject(s) - broth microdilution , antimicrobial , microbiology and biotechnology , minimum inhibitory concentration , candida albicans , antibacterial activity , chemistry , fluconazole , amphotericin b , escherichia coli , bacteria , biology , antifungal , biochemistry , genetics , gene
The antifungal and antimicrobial activities of three pentacycloundecane (PCU) tetra‐amine derivatives are reported herein. The in vitro activity of these PCU derivatives against yeasts ( Candida albicans and non‐ albicans species) and filamentous fungi was evaluated using the Clinical and Laboratory Standards Institute (CLSI) M27‐A2 and M38‐A2 guidelines and the 2H‐tetrazolium salt, (MTS) colorimetric method. The minimum inhibitory concentration against most of the tested clinical fungal strains for GKM8 and GKM9 derivatives ranges from 15.6 to 62.5 μg/mL while GKM11 ranged from 3.9 to 7.8 μg/mL. The GKM11 derivative was also active against fluconazole‐resistant strains of fungi. The GKM11 derivative also exhibited promising activity against filamentous fungi in that it was 2.5 times more active than amphotericin B against Sporothrix schenckii . Antibacterial activity was determined using the broth microdilution method (BMM) and the iodonitrotetrazolium chloride (INT) colorimetric method. The GKM11 derivative was mainly active against Gram‐positive bacteria with MIC ranging from 3.9 to 7.8 μg/mL. Activity against Gram‐negative bacteria tested was limited to Escherichia coli and Elizabethkingia meningoseptica (MIC of 31 μg/mL).