Potent In Vitro Antifungal Activities of Naturally Occurring Acetylenic Acids
| العنوان: | Potent In Vitro Antifungal Activities of Naturally Occurring Acetylenic Acids |
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| المؤلفون: | Alice M. Clark, Susan P. Manly, Xing-Cong Li, Shabana I. Khan, M. Khalid Ashfaq, Ameeta K. Agarwal, K. Suresh Babu, Hala N. ElSohly, Melissa R. Jacob |
| المصدر: | Antimicrobial Agents and Chemotherapy. 52:2442-2448 |
| بيانات النشر: | American Society for Microbiology, 2008. |
| سنة النشر: | 2008 |
| مصطلحات موضوعية: | Antifungal Agents, Rubiaceae, Aspergillus flavus, Microbial Sensitivity Tests, Candida parapsilosis, Cell Line, Aspergillus fumigatus, Microbiology, Candida tropicalis, Mice, Trichophyton, Candida krusei, Candida albicans, medicine, Animals, Humans, Pharmacology (medical), Pharmacology, Plants, Medicinal, Molecular Structure, biology, Candida glabrata, Fungi, biology.organism_classification, Infectious Diseases, Biochemistry, Susceptibility, Alkynes, Undecylenic acid, Fatty Acids, Unsaturated, medicine.drug |
| الوصف: | Our continuing effort in antifungal natural product discovery has led to the identification of five 6-acetylenic acids with chain lengths from C 16 to C 20 : 6-hexadecynoic acid (compound 1), 6-heptadecynoic acid (compound 2), 6-octadecynoic acid (compound 3), 6-nonadecynoic acid (compound 4), and 6-icosynoic acid (compound 5) from the plant Sommera sabiceoides . Compounds 2 and 5 represent newly isolated fatty acids. The five acetylenic acids were evaluated for their in vitro antifungal activities against Candida albicans, Candida glabrata, Candida krusei, Candida tropicalis, Candida parapsilosis, Cryptococcus neoformans, Aspergillus fumigatus, Aspergillus flavus, Aspergillus niger, Trichophyton mentagrophytes , and Trichophyton rubrum by comparison with the positive control drugs amphotericin B, fluconazole, ketoconazole, caspofungin, terbinafine, and undecylenic acid. The compounds showed various degrees of antifungal activity against the 21 tested strains. Compound 4 was the most active, in particular against the dermatophytes T. mentagrophytes and T. rubrum and the opportunistic pathogens C. albicans and A. fumigatus , with MICs comparable to several control drugs. Inclusion of two commercially available acetylenic acids, 9-octadecynoic acid (compound 6) and 5,8,11,14-eicosatetraynoic acid (compound 7), in the in vitro antifungal testing further demonstrated that the antifungal activities of the acetylenic acids were associated with their chain lengths and positional triple bonds. In vitro toxicity testing against mammalian cell lines indicated that compounds 1 to 5 were not toxic at concentrations up to 32 μM. Furthermore, compounds 3 and 4 did not produce obvious toxic effects in mice at a dose of 34 μmol/kg of body weight when administered intraperitoneally. Taking into account the low in vitro and in vivo toxicities and significant antifungal potencies, these 6-acetylenic acids may be excellent leads for further preclinical studies. |
| تدمد: | 1098-6596 0066-4804 |
| DOI: | 10.1128/aac.01297-07 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57303734c28d844c113ae89fe0b675c0 https://doi.org/10.1128/aac.01297-07 |
| Rights: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....57303734c28d844c113ae89fe0b675c0 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 10986596 00664804 |
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| DOI: | 10.1128/aac.01297-07 |