Anti-Trichophyton Activity of Protocatechuates and Their Synergism with Fluconazole
Dermatophytosis and superficial mycosis are a major global public health problem that affects 20–25% of the world’s population. The increase in fungal resistance to the commercially available antifungal agents, in conjunction with the limited spectrum of action of such drugs, emphasises the need to...
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| Veröffentlicht in: | Evidence-based complementary and alternative medicine 2014-01, Vol.2014 (2014), p.1-9 |
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| creator | Souza, Patrícia Fernanda Silva, Dulce Helena Siqueira Mendes-Giannini, Maria José Soares Fusco-Almeida, Ana Marisa Regasini, Luis Octávio Scorzoni, Liliana Sangalli-Leite, Fernanda Costa-Orlandi, Caroline Barcelos Pitangui, Nayla S. Sardi, Janaina C. O. Gullo, Fernanda P. Soares, Luciana A. Petrônio, Maicon Segalla |
| description | Dermatophytosis and superficial mycosis are a major global public health problem that affects 20–25% of the world’s population. The increase in fungal resistance to the commercially available antifungal agents, in conjunction with the limited spectrum of action of such drugs, emphasises the need to develop new antifungal agents. Natural products are attractive prototypes for antifungal agents due to their broad spectrum of biological activities. This study aimed to verify the antifungal activity of protocatechuic acid, 3,4-diacetoxybenzoic, and fourteen alkyl protocatechuates (3,4-dihydroxybenzoates) against Trichophyton rubrum and Trichophyton mentagrophytes and to further assess their activities when combined with fluconazole. Susceptibility and synergism assays were conducted as described in M38-A2 (CLSI), with modifications. Three strains of Trichophyton rubrum and three strains of Trichophyton mentagrophytes were used in this work. The pentyl, hexyl, heptyl, octyl, nonyl, and decyl protocatechuates showed great fungicidal effects, with minimum inhibitory concentration (MIC) values ranging from 0.97 to 7.8 mg/L. Heptyl showed a synergistic activity (FIC index = 0.49 ), reducing the MIC of fluconazole by fourfold. All substances tested were safe, especially the hexyl, heptyl, octyl, and nonyl compounds, all of which showed a high selectivity index, particularly in combination with fluconazole. These ester associations with fluconazole may represent a promising source of prototypes in the search for anti-Trichophyton therapeutic agents. |
| doi_str_mv | 10.1155/2014/957860 |
| format | Article |
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O. ; Gullo, Fernanda P. ; Soares, Luciana A. ; Petrônio, Maicon Segalla</creator><contributor>Sulaiman, Mohd Roslan ; Mohd Roslan Sulaiman</contributor><creatorcontrib>Souza, Patrícia Fernanda ; Silva, Dulce Helena Siqueira ; Mendes-Giannini, Maria José Soares ; Fusco-Almeida, Ana Marisa ; Regasini, Luis Octávio ; Scorzoni, Liliana ; Sangalli-Leite, Fernanda ; Costa-Orlandi, Caroline Barcelos ; Pitangui, Nayla S. ; Sardi, Janaina C. O. ; Gullo, Fernanda P. ; Soares, Luciana A. ; Petrônio, Maicon Segalla ; Sulaiman, Mohd Roslan ; Mohd Roslan Sulaiman</creatorcontrib><description>Dermatophytosis and superficial mycosis are a major global public health problem that affects 20–25% of the world’s population. The increase in fungal resistance to the commercially available antifungal agents, in conjunction with the limited spectrum of action of such drugs, emphasises the need to develop new antifungal agents. Natural products are attractive prototypes for antifungal agents due to their broad spectrum of biological activities. This study aimed to verify the antifungal activity of protocatechuic acid, 3,4-diacetoxybenzoic, and fourteen alkyl protocatechuates (3,4-dihydroxybenzoates) against Trichophyton rubrum and Trichophyton mentagrophytes and to further assess their activities when combined with fluconazole. Susceptibility and synergism assays were conducted as described in M38-A2 (CLSI), with modifications. Three strains of Trichophyton rubrum and three strains of Trichophyton mentagrophytes were used in this work. The pentyl, hexyl, heptyl, octyl, nonyl, and decyl protocatechuates showed great fungicidal effects, with minimum inhibitory concentration (MIC) values ranging from 0.97 to 7.8 mg/L. Heptyl showed a synergistic activity (FIC index = 0.49 ), reducing the MIC of fluconazole by fourfold. All substances tested were safe, especially the hexyl, heptyl, octyl, and nonyl compounds, all of which showed a high selectivity index, particularly in combination with fluconazole. These ester associations with fluconazole may represent a promising source of prototypes in the search for anti-Trichophyton therapeutic agents.</description><identifier>ISSN: 1741-427X</identifier><identifier>EISSN: 1741-4288</identifier><identifier>DOI: 10.1155/2014/957860</identifier><identifier>PMID: 25136374</identifier><language>eng</language><publisher>Cairo, Egypt: Hindawi Publishing Corporation</publisher><subject>Acids ; Alternative medicine ; Antibiotics ; Antifungal activity ; Antifungal agents ; Chemical compounds ; Dermatomycosis ; Fluconazole ; Fungal infections ; Fungicides ; Laboratories ; Microorganisms ; Minimum inhibitory concentration ; Mycosis ; Natural products ; Protocatechuic acid ; Prototypes ; Public health ; Synergism ; Trichophyton mentagrophytes ; Trichophyton rubrum</subject><ispartof>Evidence-based complementary and alternative medicine, 2014-01, Vol.2014 (2014), p.1-9</ispartof><rights>Copyright © 2014 Luciana Arantes Soares et al.</rights><rights>Copyright © 2014 Luciana Arantes Soares et al. This is an open access article distributed under the Creative Commons Attribution License (the “License”), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License. https://creativecommons.org/licenses/by/4.0</rights><rights>Copyright © 2014 Luciana Arantes Soares et al. 2014</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c467t-ba155e3d9daf1bdcdeec70e2501bec59e10ec78e742badd0d799f130b902233b3</citedby><cites>FETCH-LOGICAL-c467t-ba155e3d9daf1bdcdeec70e2501bec59e10ec78e742badd0d799f130b902233b3</cites><orcidid>0000-0002-2115-8988 ; 0000-0001-6560-4049 ; 0000-0003-3248-5180</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4086519/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4086519/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,314,723,776,780,881,27901,27902,53766,53768</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/25136374$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><contributor>Sulaiman, Mohd Roslan</contributor><contributor>Mohd Roslan Sulaiman</contributor><creatorcontrib>Souza, Patrícia Fernanda</creatorcontrib><creatorcontrib>Silva, Dulce Helena Siqueira</creatorcontrib><creatorcontrib>Mendes-Giannini, Maria José Soares</creatorcontrib><creatorcontrib>Fusco-Almeida, Ana Marisa</creatorcontrib><creatorcontrib>Regasini, Luis Octávio</creatorcontrib><creatorcontrib>Scorzoni, Liliana</creatorcontrib><creatorcontrib>Sangalli-Leite, Fernanda</creatorcontrib><creatorcontrib>Costa-Orlandi, Caroline Barcelos</creatorcontrib><creatorcontrib>Pitangui, Nayla S.</creatorcontrib><creatorcontrib>Sardi, Janaina C. 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Natural products are attractive prototypes for antifungal agents due to their broad spectrum of biological activities. This study aimed to verify the antifungal activity of protocatechuic acid, 3,4-diacetoxybenzoic, and fourteen alkyl protocatechuates (3,4-dihydroxybenzoates) against Trichophyton rubrum and Trichophyton mentagrophytes and to further assess their activities when combined with fluconazole. Susceptibility and synergism assays were conducted as described in M38-A2 (CLSI), with modifications. Three strains of Trichophyton rubrum and three strains of Trichophyton mentagrophytes were used in this work. The pentyl, hexyl, heptyl, octyl, nonyl, and decyl protocatechuates showed great fungicidal effects, with minimum inhibitory concentration (MIC) values ranging from 0.97 to 7.8 mg/L. Heptyl showed a synergistic activity (FIC index = 0.49 ), reducing the MIC of fluconazole by fourfold. 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| identifier | ISSN: 1741-427X |
| ispartof | Evidence-based complementary and alternative medicine, 2014-01, Vol.2014 (2014), p.1-9 |
| issn | 1741-427X 1741-4288 |
| language | eng |
| recordid | cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_4086519 |
| source | Wiley Online Library Open Access; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; PubMed Central; Alma/SFX Local Collection; PubMed Central Open Access |
| subjects | Acids Alternative medicine Antibiotics Antifungal activity Antifungal agents Chemical compounds Dermatomycosis Fluconazole Fungal infections Fungicides Laboratories Microorganisms Minimum inhibitory concentration Mycosis Natural products Protocatechuic acid Prototypes Public health Synergism Trichophyton mentagrophytes Trichophyton rubrum |
| title | Anti-Trichophyton Activity of Protocatechuates and Their Synergism with Fluconazole |
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