In vitro activity of propyl gallate-azole drug combination against fluconazole- and itraconazole-resistant Candida albicans strains

D’Auria, Felicia Diodata; Tecca, M.; Strippoli, Raffaele; Simonetti, N

doi:10.1046/j.1472-765x.2001.00893.x

Cited by 16 publications

(13 citation statements)

References 17 publications

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“…It has been shown to possess antifungal, 241 to water and oxygen, but a small portion is also utilized in the production of tyrosyl radicals. 111 Phenolic acids, including gallates, exhibit a strong MO inhibition.…”

Section: Other Therapeutically Benecial Activitiesmentioning

confidence: 99%

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Gallic acid: a versatile antioxidant with promising therapeutic and industrial applications

2015

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Oxidative stress, a result of an overproduction and accumulation of free radicals, is the leading cause of several degenerative diseases such as cancer, atherosclerosis, cardiovascular diseases, ageing and inflammatory diseases. Polyphenols form an important class of naturally occurring antioxidants, having innumerable biological activities such as anticancer, antifungal, antibacterial, antiviral, antiulcer and anticholesterol, to name a few. Among various polyphenols, gallic acid (3,4,5-trihydroxybenzoic acid), a naturally occurring low molecular weight triphenolic compound, has emerged as a strong antioxidant and an efficient apoptosis inducing agent. Starting from the bioavailability and the biosynthetic pathway of gallic acid, this review includes various in vitro, in vivo and in silico studies providing the mode of action, radical scavenging activity, ability to inhibit lipid peroxidation, maintenance of endogenous defense systems and metal ion chelation by this triphenolic molecule, along with a comprehensive overview of factors responsible for its high antioxidant activity. Gallic acid derivatives have also been found in a number of phytomedicines with diverse biological and pharmacological activities, including radical scavenging, interfering with the cell signaling pathways and apoptosis of cancer cells. The diverse range of applications of this simple polyphenol is due to a fine amalgam between its antioxidant and prooxidant potential. The existing literature on this dual behavior of gallic acid and its derivatives is reviewed here. This is followed by an account of their potential clinical and industrial applications.

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Section: Other Therapeutically Benecial Activitiesmentioning

confidence: 99%

“…Derivatives of GA have also been shown to display fungicidal and bactericidal properties. 241,244,245 Oxadiazole derivatives for example are known to possess antimicrobial, 257,279 antiparasitic 280 and antitubercular activities. [257][258][259] 4.2.3 Antimelanogenic.…”

Section: Other Therapeutically Benecial Activitiesmentioning

confidence: 99%

Gallic acid: a versatile antioxidant with promising therapeutic and industrial applications

2015

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“…However, contradictory results of either synergic or antagonistic actions in various antifungal combinations have been reported (8,11,16,27). As for fluconazoleresistant C. albicans, few data are available about the synergism of fluconazole with other antifungal agents (1,4,25).Berberine, a bioactive herbal ingredient, was demonstrated to have weak activity against C. albicans and C. glabrata (17,21,26). Recently, berberine was combined with amphotericin B to treat disseminated candidiasis in mice (10).…”

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confidence: 99%

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confidence: 99%

Potent In Vitro Synergism of Fluconazole and Berberine Chloride against Clinical Isolates of Candida albicans Resistant to Fluconazole

Quan

Cao

et al. 2006

Antimicrob Agents Chemother

139

136

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In vitro interaction of fluconazole and berberine chloride was investigated against 40 fluconazole-resistant clinical isolates of Candida albicans. Synergism in fungistatic activity was found with the checkerboard microdilution assay. The findings of agar diffusion tests and time-kill curves confirmed the synergistic interaction, but no antagonistic action was observed.Candida albicans is the most common candidal pathogen, causing mucosal and invasive infections (7,9,23,29). With the increasing clinical use of fluconazole, a choice for the treatment of C. albicans infections (3, 5, 12), fluconazole-resistant isolates are occurring more frequently (2,19,28). Attempts have been made to cope with treatment failures by using combination therapy (14). However, contradictory results of either synergic or antagonistic actions in various antifungal combinations have been reported (8,11,16,27). As for fluconazoleresistant C. albicans, few data are available about the synergism of fluconazole with other antifungal agents (1,4,25).Berberine, a bioactive herbal ingredient, was demonstrated to have weak activity against C. albicans and C. glabrata (17,21,26). Recently, berberine was combined with amphotericin B to treat disseminated candidiasis in mice (10). To seek a novel combination therapy, we investigated the in vitro interaction of fluconazole and berberine chloride (BBR) against fluconazoleresistant clinical isolates of C. albicans.Strains and agents. Forty clinical isolates of fluconazoleresistant C. albicans were used in this study, and C. albicans ATCC 90028 was used as a quality control. Drugs prepared in dimethyl sulfoxide (DMSO) included fluconazole (PfizerRoerig Pharmaceuticals, New York, NY) and BBR (SigmaAldrich, St. Louis, MO).Checkerboard microdilution assay. Assays were performed on all 40 isolates according to methods of the CLSI (formerly NCCLS) (M27-A) (6, 18). The initial concentration of fungal suspension in RPMI 1640 medium was 10 3 CFU/ml, and the final concentrations ranged from 0.125 to 64 g/ml for fluconazole and 1 to 32 g/ml for BBR. Plates were incubated at 35°C for 24 h. Optical density was measured at 630 nm, and background optical densities were subtracted from that of each well. Each isolate was tested in triplicate. MIC 80 and MIC 50 were determined as the lowest concentration of the drugs (alone or in combination) that inhibited growth by 80% or 50%, respectively, compared with that of drug-free wells. The fractional inhibitory concentration (FIC) index is defined as the sum of the MIC of each drug when used in combination divided by the MIC of the drug used alone. Synergy and antagonism were defined by FIC indices of Յ0.5 and Ͼ4, respectively. An FIC index result of Ͼ0.5 but Յ4 was considered indifferent (20).Agar diffusion test. C. albicans 0304103 (one fluconazole-resistant isolate with a MIC of Ͼ32 g/ml for BBR) was tested by agar diffusion assay. A 100-l aliquot of 10 6 -CFU/ml suspension was spread uniformly onto the yeast extract-peptone-dextrose agar plate with or without 64 g/ml ...

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“…Numerous attempts have been made to cope with clinical treatment failures resulting from drug resistance, such as developing novel antifungal compounds [18][19][20][21] and exploring combination therapies [22][23][24][25][26][27][28][29] . Small molecule approaches for gene regulation could bypass the need for delivery strategies.…”

Section: Introductionmentioning

confidence: 99%

A novel polyamide SL-A92 as a potential fungal resistance blocker: synthesis and bioactivities in Candida albicans

et al. 2010

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Aim: To synthesize a novel polyamide SL-A92 and evaluate its bioactivity against drug resistance in Candida albicans. Methods: SL-A92 was synthesized using N-hydroxybenzotriazole (HOBT)/N,N'-dicyclohexylcarbodiimide (DCC) in solution phase. Its antifungal activities and effects on strain growth were tested using the micro-broth dilution method and growth curves, respectively. Induced drug resistance in the C. albicans collection strain SC5314 was obtained by incubation with fluconazole (12 μg/mL) for 21 passages. Meanwhile, incubations with SL-A92 plus fluconazole were also carried out in SC5314 strains, and the MIC 80 s were used to evaluate the inhibitory effects of SL-A92 on drug resistance during the induction process. Real time RT-PCR was performed to investigate the CDR1 and CDR2 mRNA levels in induced SC5314 strains. Results: SC5314 strain induced by the combination of fluconazole and SL-A92 (200 μg/mL) did not develop drug resistance. On day 24, the CDR1 and CDR2 mRNA levels in SC5314 strain co-treated with fluconazole and SL-A92 relative to fluconazole alone were 26% and 24%, respectively, and on day 30 the CDR1 and CDR2 mRNA levels were 43% and 31%, respectively. Conclusion: SL-A92 can block the development of drug resistance during the fluconazole induction process, which partially results from the down-regulation of CDR1 and CDR2.

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In vitro activity of propyl gallate-azole drug combination against fluconazole- and itraconazole-resistant Candida albicans strains

Cited by 16 publications

References 17 publications

Gallic acid: a versatile antioxidant with promising therapeutic and industrial applications

Gallic acid: a versatile antioxidant with promising therapeutic and industrial applications

Potent In Vitro Synergism of Fluconazole and Berberine Chloride against Clinical Isolates of Candida albicans Resistant to Fluconazole

A novel polyamide SL-A92 as a potential fungal resistance blocker: synthesis and bioactivities in Candida albicans

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