DOCSLIB.ORG

Antifungal Activity of Melaleuca Alternifolia Essential Oil (TTO) and Its Synergy with Itraconazole Or Ketoconazole Against Trichophyton Rubrum

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Antifungal Activity of Melaleuca Alternifolia Essential Oil (TTO) and Its Synergy with Itraconazole Or Ketoconazole Against Trichophyton Rubrum molecules Article Antifungal Activity of Melaleuca alternifolia Essential Oil (TTO) and Its Synergy with Itraconazole or Ketoconazole against Trichophyton rubrum Janira Roana 1 , Narcisa Mandras 1, Daniela Scalas 2, Paolo Campagna 3 and Vivian Tullio 1,* 1 Department of Public Health and Pediatrics, Microbiology Division, University of Turin, via Santena 9, 10126 Turin, Italy; [email protected] (J.R.); [email protected] (N.M.) 2 Department of Veterinary Sciences, University of Turin, Grugliasco, 10095 Turin, Italy; [email protected] 3 Società Italiana per la Ricerca Sugli Oli Essenziali, 00161 Rome, Italy; [email protected] * Correspondence: [email protected]; Tel.: +39-011-670-5637 Abstract: Over the past 20–30 years, Trichophyton rubrum represented the most widespread der- matophyte with a prevalence accounting for 70% of dermatophytosis. The treatment for cutaneous infections caused by Trichophyton spp. are imidazoles (ketoconazole (KTZ)) and triazoles (itraconazole (ITZ)). T. rubrum can develop resistance to azoles after prolonged exposure to subinhibitory concen- trations resulting in therapeutic failures and chronic infections. These problems have stimulated the search for therapeutic alternatives, including essential oils, and their potential use in combination with conventional antifungals. The purpose of this study was to evaluate the antifungal activity of tea tree oil (TTO) (Melaleuca alternifolia essential oil) and the main components against T. rubrum and to assess whether TTO in association with KTZ/ITZ as reference drugs improves the antifungal activity of these drugs. We used a terpinen-4-ol chemotype (35.88%) TTO, and its antifungal properties were evaluated by minimum inhibitory and minimum fungicidal concentrations in accordance with the Citation: Roana, J.; Mandras, N.; Scalas, D.; Campagna, P.; CLSI guidelines. The interaction between TTO and azoles was evaluated through the checkerboard Tullio, V. Antifungal Activity of and isobologram methods. The results demonstrated both the fungicide activity of TTO on T. rubrum Melaleuca alternifolia Essential Oil and the synergism when it was used in combination with azoles. Therefore, this mixture may reduce (TTO) and Its Synergy with the minimum effective dose of azole required and minimize the side effects of the therapy. Synergy Itraconazole or Ketoconazole against activity offered a promise for combination topical treatment for superficial mycoses. Trichophyton rubrum. Molecules 2021, 26, 461. https://doi.org/10.3390/ Keywords: Trichophyton rubrum; essential oils; tea tree oil; Melaleuca alternifolia; azoles; checker- molecules26020461 board; synergism Academic Editor: Francesca Mancianti Received: 30 December 2020 Accepted: 13 January 2021 1. Introduction Published: 17 January 2021 Dermatophytes are the most common fungal agents leading to superficial skin in- Publisher’s Note: MDPI stays neu- fections. During the last century, their spread changed under the influence of several tral with regard to jurisdictional clai- elements, such as socioeconomic factors, practices bound to life-style, increasing travel, ms in published maps and institutio- and migration from southern to northern countries and vice versa [1]. Trichophyton rubrum, nal affiliations. frequently causing tinea pedis, tinea unguium, and tinea corporis, has increased steadily over this period and became the main agent isolated worldwide [2–4]. Over the past 20–30 years, T. rubrum has represented the most widespread dermatophyte in Central and North Europe with a prevalence accounting for about 70% of dermatophytosis. This species is often the Copyright: © 2021 by the authors. Li- key etiological agent of chronic infections with a slow progression, suggesting that the censee MDPI, Basel, Switzerland. fungus has adapted to the human host [5]. Sometimes it is responsible for a deeper and This article is an open access article disseminated infection, particularly in immunocompromised patients [3]. distributed under the terms and con- Azoles and allylamines (such as terbinafine) (Figure1) are the most important oral and ditions of the Creative Commons At- topical antifungal drugs used to treat dermatophytosis: they interfere with the ergosterol tribution (CC BY) license (https:// creativecommons.org/licenses/by/ biosynthesis pathway causing structural modifications in the lipid membrane. 4.0/). Molecules 2021, 26, 461. https://doi.org/10.3390/molecules26020461 https://www.mdpi.com/journal/molecules Molecules 2020, 25, x; doi: FOR PEER REVIEW 2 of 10 sponsible for a deeper and disseminated infection, particularly in immunocompromised patients [3]. Azoles and allylamines (such as terbinafine) (Figure 1) are the most important oral Molecules 2021, 26, 461 2 of 10 and topical antifungal drugs used to treat dermatophytosis: they interfere with the er- gosterol biosynthesis pathway causing structural modifications in the lipid membrane. FigureFigure 1.1. Chemical structures of of azoles azoles (itraconazole, (itraconazole, ketoconazole) ketoconazole) and and terbinafine. terbinafine. The preferred treatment for cutaneous infections caused by Trichophyton spp. are The preferred treatment for cutaneous infections caused by Trichophyton spp. are imidazoles, such as ketoconazole (KTZ), and triazoles, such as itraconazole (ITZ), often imidazoles, such as ketoconazole (KTZ), and triazoles, such as itraconazole (ITZ), often resulting in a complete clearance of the lesions. However, inappropriate prescribing, and resulting in a complete clearance of the lesions. However, inappropriate prescribing, and the increased use of systemic antifungal agents in recent years are the main factors leading the increased use of systemic antifungal agents in recent years are the main factors lead- toing the to emergence the emergence of resistance of resistance to antifungal to antifungal drugs drugs (i.e., azoles) (i.e., azoles) [6]. In [6]. fact, In if notfact, properly if not treated,properly dermatophytosis treated, dermatophytosis may become may chronic, become requiringchronic, requiring oral antifungal oral antifungal drugs, which drugs, are oftenwhich associated are often associated with side effectswith side such effects as hepatotoxicity. such as hepatotoxicity.T. rubrum T.can rubrum develop can develop resistance toresistance azoles after to azoles prolonged after exposureprolonged to exposure subinhibitory to subinhibitory concentrations concentrations of these drugs of leadingthese todrugs therapeutic leading failuresto therapeutic and to thefailures persistence and to andthe persistence chronicity ofand the chronicity infections. of Furthermore, the infec- complicationstions. Furthermore, like bacterial complications superinfections like bacterial can superinfections occur [7]. can occur [7]. TheseThese problems have stimulated the the search search for for therapeutic therapeutic alternatives, alternatives, including including naturalnatural compoundscompounds suchsuch as as essential essential oils, oils which, which have have been been increasingly increasingly used used in recent in recent years foryears their for biologicaltheir biological and antimicrobial and antimicrobial activities. activities. Furthermore, Furthermore, a recent a recent focus focus of research of re- onsearch essential on essential oils is oils to investigate is to investigate their potentialtheir potential use inuse combination in combination with with conventional conven- antimicrobialtional antimicrobial drugs drugs [8,9]. [8,9]. In fact, In fact, essential essential oils oils are are one one of theof the most most evident evident promising prom- sourcesising sources for pharmacological for pharmacologic researchal research and theand development the development of new of new natural natural antimicrobial antimi- agentscrobial againstagents against many microbialmany microbial pathogens pathogens such assuch bacteria, as bacteria, yeasts, yeasts, filamentous filamentous fungi, includingfungi, including dermatophytes, dermatophytes, and viruses and viruses [10]. Among [10]. Among the best the known best known oils, teaoils, tree tea oiltree (TTO), oil the(TTO), essential the essential oil of Melaleuca oil of Melaleuca alternifolia alternifolia(Myrtaceae), (Myrtaceae), often used often as used an antiseptic as an antiseptic to treat skinto infections,treat skin infections, has recently has received recently much received attention much forattention its antifungal for its antifungal properties. properties Because. of itsBecause lipophilic of its nature, lipophilic which nature, facilitates which skin facilitates penetration, skin itpenetration is used as, ait local is used formulation as a local for dermatologicalformulation for disordersdermatological [11]. disorders [11]. Hence,Hence, thethe purposepurpose ofof thisthis studystudy waswas toto evaluateevaluate thethe antifungalantifungal activityactivity ofof TTOTTO and and its mainits main components components against againstT. rubrum T. rubrumand assessand assess for the for first the timefirst whethertime whether TTO inTTO association in as- withsociation ITZ orwith KTZ ITZ improves or KTZ the improves antifungal the activityantifungal of these activity drugs of againstthese drugsT. rubrum against. T. rubrum. 2. Results 2.1. TTO Composition The phytochemical composition of TTO used for this study was determined by GC-MS, and the results are reported in Table1. Molecules 2020, 25, x; doi: FOR PEER REVIEW 3 of 10 2. Results 2.1. TTO Composition Molecules
Load more

Recommended publications
  • Antibiofilm Efficacy of Tea Tree Oil and of Its Main Component Terpinen-4-Ol Against Candida Albicans
    ORIGINAL RESEARCH Periodontics Antibiofilm efficacy of tea tree oil and of its main component terpinen-4-ol against Candida albicans Renata Serignoli Abstract: Candida infection is an important cause of morbidity FRANCISCONI(a) and mortality in immunocompromised patients. The increase in its Patricia Milagros Maquera incidence has been associated with resistance to antimicrobial therapy HUACHO(a) and biofilm formation. The aim of this study was to evaluate the Caroline Coradi TONON(a) efficacy of tea tree oil (TTO) and its main component – terpinen-4-ol – Ester Alves Ferreira BORDINI(a) against resistant Candida albicans strains (genotypes A and B) identified by molecular typing and against C. albicans ATCC 90028 and SC 5314 Marília Ferreira CORREIA(a) reference strains in planktonic and biofilm cultures. The minimum Janaína de Cássia Orlandi inhibitory concentration, minimum fungicidal concentration, and SARDI(b) rate of biofilm development were used to evaluate antifungal activity. Denise Madalena Palomari Results were obtained from analysis of the biofilm using the cell (a) SPOLIDORIO proliferation assay 2,3-Bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H- tetrazolium-5-carboxanilide (XTT) and confocal laser scanning (a) Universidade Estadual Paulista – Unesp, microscopy (CLSM). Terpinen-4-ol and TTO inhibited C. albicans School of Dentistry of Araraquara, Department of Physiology and Pathology, growth. CLSM confirmed that 17.92 mg/mL of TTO and 8.86 mg/mL Araraquara, SP, Brazil of terpinen-4-ol applied for 60 s (rinse simulation) interfered with (b) Universidade Estadual de Campinas – biofilm formation. Hence, this in vitro study revealed that natural Unicamp, School of Dentistry of Piracicaba, substances such as TTO and terpinen-4-ol present promising results Department of Physiological Sciences, for the treatment of oral candidiasis.
    [Show full text]
  • New Insights Into the Effect of Amorolfine Nail Lacquer
    Review article New insights into the effect of amorolfine nail lacquer C. Flagothier, C. Pie´ rard-Franchimont and G. E. Pie´ rard Department of Dermatopathology, University Hospital of Lie`ge, Lie`ge, Belgium Summary Despite improvements in antifungal strategies, the outcome of treating onychomycoses often remains uncertain. Several factors account for treatment failure, of which the pharmacokinetics and pharmacodynamics of the antifungal are of importance. The taxonomic nature and ungual location of the fungus cannot be neglected, besides the type of nail and its growth rate. In addition, the biological cycle of the fungus and the metabolic activity of the pathogen likely play a marked influence in drug response. The presence of natural antimicrobial peptides in the nail is also probably a key feature controlling the cure rates. There are many outstanding publications that cover the full spectrum of the field. The purpose of this review is to put in perspective some facets of activity of the topical treatment using amorolfine nail laquer. The antifungal activity of the drug is likely less pronounced in onychomycosis than that expected from conventional in vitro studies. However, the nail laquer formulation should reduce the propensity to form antifungal-resistant spores and limit the risk of reinfection. Key words: amorolfine, antifungal, fungus, onychomycosis, spore. Topical treatments are often considered to be less Introduction efficacious than current oral treatments. However, some During the last 2 decades, the efficacy of treating topical formulations may provide effects that cannot be onychomycoses has been considerably improved by achieved by other treatments. In discussing the treat- the introduction of new generations of potent antifun- ment of onychomycosis, it should not be forgotten that gals.
    [Show full text]
  • The Management of Common Skin Conditions in General Practice
    Management of Common Skin Conditions In General Practice including the “red rash made easy” © Arroll, Fishman & Oakley, Department of General Practice and Primary Health Care University of Auckland, Tamaki Campus Reviewed by Hon A/Prof Amanda Oakley - 2019 http://www.dermnetnz.org Management of Common Skin Conditions In General Practice Contents Page Derm Map 3 Classic location: infants & children 4 Classic location: adults 5 Dermatology terminology 6 Common red rashes 7 Other common skin conditions 12 Common viral infections 14 Common bacterial infections 16 Common fungal infections 17 Arthropods 19 Eczema/dermatitis 20 Benign skin lesions 23 Skin cancers 26 Emergency dermatology 28 Clinical diagnosis of melanoma 31 Principles of diagnosis and treatment 32 Principles of treatment of eczema 33 Treatment sequence for psoriasis 34 Topical corticosteroids 35 Combination topical steroid + antimicrobial 36 Safety with topical corticosteroids 36 Emollients 37 Antipruritics 38 For further information, refer to: http://www.dermnetnz.org And http://www.derm-master.com 2 © Arroll, Fishman & Oakley, Department of General Practice and Primary Health Care, University of Auckland, Tamaki Campus. Management of Common Skin Conditions In General Practice DERM MAP Start Is the patient sick ? Yes Rash could be an infection or a drug eruption? No Insect Bites – Crop of grouped papules with a central blister or scab. Is the patient in pain or the rash Yes Infection: cellulitis / erysipelas, impetigo, boil is swelling, oozing or crusting? / folliculitis, herpes simplex / zoster. Urticaria – Smooth skin surface with weals that evolve in minutes to hours. No Is the rash in a classic location? Yes See our classic location chart .
    [Show full text]
  • Voriconazole
    Drug and Biologic Coverage Policy Effective Date ............................................ 6/1/2020 Next Review Date… ..................................... 6/1/2021 Coverage Policy Number .................................. 4004 Voriconazole Table of Contents Related Coverage Resources Coverage Policy ................................................... 1 FDA Approved Indications ................................... 2 Recommended Dosing ........................................ 2 General Background ............................................ 2 Coding/Billing Information .................................... 4 References .......................................................... 4 INSTRUCTIONS FOR USE The following Coverage Policy applies to health benefit plans administered by Cigna Companies. Certain Cigna Companies and/or lines of business only provide utilization review services to clients and do not make coverage determinations. References to standard benefit plan language and coverage determinations do not apply to those clients. Coverage Policies are intended to provide guidance in interpreting certain standard benefit plans administered by Cigna Companies. Please note, the terms of a customer’s particular benefit plan document [Group Service Agreement, Evidence of Coverage, Certificate of Coverage, Summary Plan Description (SPD) or similar plan document] may differ significantly from the standard benefit plans upon which these Coverage Policies are based. For example, a customer’s benefit plan document may contain a specific exclusion
    [Show full text]
  • Antifungal Agents in Agriculture: Friends and Foes of Public Health
    biomolecules Review Antifungal Agents in Agriculture: Friends and Foes of Public Health Veronica Soares Brauer 1, Caroline Patini Rezende 1, Andre Moreira Pessoni 1, Renato Graciano De Paula 2 , Kanchugarakoppal S. Rangappa 3, Siddaiah Chandra Nayaka 4, Vijai Kumar Gupta 5,* and Fausto Almeida 1,* 1 Department of Biochemistry and Immunology, Ribeirao Preto Medical School, University of Sao Paulo, Ribeirao Preto, SP 14049-900, Brazil; [email protected] (V.S.B.); [email protected] (C.P.R.); [email protected] (A.M.P.) 2 Department of Physiological Sciences, Health Sciences Centre, Federal University of Espirito Santo, Vitoria, ES 29047-105, Brazil; [email protected] 3 Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570006, India; [email protected] 4 Department of Studies in Biotechnology, University of Mysore, Manasagangotri, Mysore 570006, India; [email protected] 5 Department of Chemistry and Biotechnology, ERA Chair of Green Chemistry, Tallinn University of Technology, 12618 Tallinn, Estonia * Correspondence: [email protected] (V.K.G.); [email protected] (F.A.) Received: 7 July 2019; Accepted: 19 September 2019; Published: 23 September 2019 Abstract: Fungal diseases have been underestimated worldwide but constitute a substantial threat to several plant and animal species as well as to public health. The increase in the global population has entailed an increase in the demand for agriculture in recent decades. Accordingly, there has been worldwide pressure to find means to improve the quality and productivity of agricultural crops. Antifungal agents have been widely used as an alternative for managing fungal diseases affecting several crops. However, the unregulated use of antifungals can jeopardize public health.
    [Show full text]
  • Antimicrobial Resistance Benchmark 2020 Antimicrobial Resistance Benchmark 2020
    First independent framework for assessing pharmaceutical company action Antimicrobial Resistance Benchmark 2020 Antimicrobial Resistance Benchmark 2020 ACKNOWLEDGEMENTS The Access to Medicine Foundation would like to thank the following people and organisations for their contributions to this report.1 FUNDERS The Antimicrobial Resistance Benchmark research programme is made possible with financial support from UK AID and the Dutch Ministry of Health, Welfare and Sport. Expert Review Committee Research Team Reviewers Hans Hogerzeil - Chair Gabrielle Breugelmans Christine Årdal Gregory Frank Fatema Rafiqi Karen Gallant Nina Grundmann Adrián Alonso Ruiz Hans Hogerzeil Magdalena Kettis Ruth Baron Hitesh Hurkchand Joakim Larsson Dulce Calçada Joakim Larsson Marc Mendelson Moska Hellamand Marc Mendelson Margareth Ndomondo-Sigonda Kevin Outterson Katarina Nedog Sarah Paulin (Observer) Editorial Team Andrew Singer Anna Massey Deirdre Cogan ACCESS TO MEDICINE FOUNDATION Rachel Jones The Access to Medicine Foundation is an independent Emma Ross non-profit organisation based in the Netherlands. It aims to advance access to medicine in low- and middle-income Additional contributors countries by stimulating and guiding the pharmaceutical Thomas Collin-Lefebvre industry to play a greater role in improving access to Alex Kong medicine. Nestor Papanikolaou Address Contact Naritaweg 227-A For more information about this publication, please contact 1043 CB, Amsterdam Jayasree K. Iyer, Executive Director The Netherlands [email protected] +31 (0) 20 215 35 35 www.amrbenchmark.org 1 This acknowledgement is not intended to imply that the individuals and institutions referred to above endorse About the cover: Young woman from the Antimicrobial Resistance Benchmark methodology, Brazil, where 40%-60% of infections are analyses or results.
    [Show full text]
  • Diagnosis and Treatment of Tinea Versicolor Ronald Savin, MD New Haven, Connecticut
    ■ CLINICAL REVIEW Diagnosis and Treatment of Tinea Versicolor Ronald Savin, MD New Haven, Connecticut Tinea versicolor (pityriasis versicolor) is a common imidazole, has been used for years both orally and top­ superficial fungal infection of the stratum corneum. ically with great success, although it has not been Caused by the fungus Malassezia furfur, this chronical­ approved by the Food and Drug Administration for the ly recurring disease is most prevalent in the tropics but indication of tinea versicolor. Newer derivatives, such is also common in temperate climates. Treatments are as fluconazole and itraconazole, have recently been available and cure rates are high, although recurrences introduced. Side effects associated with these triazoles are common. Traditional topical agents such as seleni­ tend to be minor and low in incidence. Except for keto­ um sulfide are effective, but recurrence following treat­ conazole, oral antifungals carry a low risk of hepato- ment with these agents is likely and often rapid. toxicity. Currently, therapeutic interest is focused on synthetic Key Words: Tinea versicolor; pityriasis versicolor; anti­ “-azole” antifungal drugs, which interfere with the sterol fungal agents. metabolism of the infectious agent. Ketoconazole, an (J Fam Pract 1996; 43:127-132) ormal skin flora includes two morpho­ than formerly thought. In one study, children under logically discrete lipophilic yeasts: a age 14 represented nearly 5% of confirmed cases spherical form, Pityrosporum orbicu- of the disease.3 In many of these cases, the face lare, and an ovoid form, Pityrosporum was involved, a rare manifestation of the disease in ovale. Whether these are separate enti­ adults.1 The condition is most prevalent in tropical tiesN or different morphologic forms in the cell and semitropical areas, where up to 40% of some cycle of the same organism remains unclear.: In the populations are affected.
    [Show full text]
  • Systemic Antifungal Drug Use in Belgium—
    Received: 7 October 2018 | Revised: 28 March 2019 | Accepted: 14 March 2019 DOI: 10.1111/myc.12912 ORIGINAL ARTICLE Systemic antifungal drug use in Belgium—One of the biggest antifungal consumers in Europe Berdieke Goemaere1 | Katrien Lagrou2,3* | Isabel Spriet4,5 | Marijke Hendrickx1 | Eline Vandael6 | Pierre Becker1 | Boudewijn Catry6,7 1BCCM/IHEM Fungal Collection, Service of Mycology and Aerobiology, Sciensano, Summary Brussels, Belgium Background: Reports on the consumption of systemic antifungal drugs on a national 2 Department of Microbiology and level are scarce although of high interest to compare trends and the associated epi- Immunology, KU Leuven, Leuven, Belgium 3Clinical Department of Laboratory demiology in other countries and to assess the need for antifungal stewardship Medicine, National Reference Centre for programmes. Mycosis, University Hospitals Leuven, Leuven, Belgium Objectives: To estimate patterns of Belgian inpatient and outpatient antifungal use 4Department of Pharmaceutical and and provide reference data for other countries. Pharmacological Sciences, KU Leuven, Methods: Consumption records of antifungals were collected in Belgian hospitals Leuven, Belgium between 2003 and 2016. Primary healthcare data were available for the azoles for 5Pharmacy Department, University Hospitals Leuven, Leuven, Belgium the period 2010-2016. 6 Healthcare‐Associated Infections and Results: The majority of the antifungal consumption resulted from prescriptions of Antimicrobial Resistance, Sciensano, Brussels, Belgium fluconazole and itraconazole in the ambulatory care while hospitals were responsible 7Faculty of Medicine, Université Libre de for only 6.4% of the total national consumption and echinocandin use was limited. Bruxelles (ULB), Brussels, Belgium The annual average antifungal consumption in hospitals decreased significantly by Correspondence nearly 25% between 2003 and 2016, due to a decrease solely in non-university hos- Berdieke Goemaere, Sciensano, Mycology pitals.
    [Show full text]
  • Therapeutic Class Overview Antifungals, Topical
    Therapeutic Class Overview Antifungals, Topical INTRODUCTION The topical antifungals are available in multiple dosage forms and are indicated for a number of fungal infections and related conditions. In general, these agents are Food and Drug Administration (FDA)-approved for the treatment of cutaneous candidiasis, onychomycosis, seborrheic dermatitis, tinea corporis, tinea cruris, tinea pedis, and tinea versicolor (Clinical Pharmacology 2018). The antifungals may be further classified into the following categories based upon their chemical structures: allylamines (naftifine, terbinafine [only available over the counter (OTC)]), azoles (clotrimazole, econazole, efinaconazole, ketoconazole, luliconazole, miconazole, oxiconazole, sertaconazole, sulconazole), benzylamines (butenafine), hydroxypyridones (ciclopirox), oxaborole (tavaborole), polyenes (nystatin), thiocarbamates (tolnaftate [no FDA-approved formulations]), and miscellaneous (undecylenic acid [no FDA-approved formulations]) (Micromedex 2018). The topical antifungals are available as single entity and/or combination products. Two combination products, nystatin/triamcinolone and Lotrisone (clotrimazole/betamethasone), contain an antifungal and a corticosteroid preparation. The corticosteroid helps to decrease inflammation and indirectly hasten healing time. The other combination product, Vusion (miconazole/zinc oxide/white petrolatum), contains an antifungal and zinc oxide. Zinc oxide acts as a skin protectant and mild astringent with weak antiseptic properties and helps to
    [Show full text]
  • Table 1Fatty Acid Compostion of Salvia Species*
    ORIGINAL ARTICLE Org. Commun. 7:4 (2014) 114-122 Some new azole type heterocyclic compounds as antifungal agents Mohammad Russell*1 and Mohammad Ikthair Hossain Soiket2 1Department of Textile Engineering, Bangladesh University of Business and Technology, Mirpur-2, Dhaka-1216, Bangladesh 2Department of Mechanical Engineering, Bangladesh University of Engineering and Technology, Polashi, Dhaka-1000, Bangladesh (Received July 2, 2013; Revised December 3, 2014; Accepted December 12, 2014) Abstract:Schiff’s base1-[(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)]ethanone thiosemicarbazone (compound 1A) wasprepared by condensation of 1-(2,4-difluorophenyl)-2- [1 (H)-1,2,4-triazol-1-yl]ethanone (1)with thiosemicarbazide. The compound 1A, on reaction with α-halogenoketones yielded 1-(2, 4-difluorophenyl)-2- [(1H)-1,2,4-triazol-1-yl] ethanone [2-[4-halogenophenyl] thiazolyl]hydrazone.Anti-fungal activity of all the compounds has been tested against four fungal organism:C. albicans, Colletotrichum spp., A. nigar and Fusarium spp. commonly responsible for fungal infections in Bangladesh. Keywords: Schiff’s bases; compound 1A; 1-(2,4-difluorophenyl)-2- [1 (H)-1,2,4-triazol-1-yl] ethanone (1); α- halogenoketones; 1-(2,4-difluorophenyl)-2-[(1H)-1,2,4-triazol-1-yl] ethanone [2-[4-halogenophenyl] thiazolyl] hydrazone;Anti-fungal activity.© 2014 ACG Publications. All rights reserved. 1. Introduction Triazole compounds are gettingincreasingattention because oftheir extensive medicinal applications as antimicrobial agents particularly in antifungal therapy, and a large number of predominant triazole drugs have been successfully developed and prevalently used for the treatment of various microbial infections for many years1-3. Azoles like fluconazole, itraconazole, voriconazole, and posaconazole are important antifungal drugs for the treatment of IFIs (invasive fungal infections), which continues to be a major cause ofmorbidity and mortality in immune compromised or in severely ill patients4.
    [Show full text]
  • Stability of Two Antifungal Agents, Fluconazole and Miconazole, Compounded in HUMCO RECURA Topical Cream to Determine Beyond-Use Date
    PEER REVIEWED Stability of Two Antifungal Agents, Fluconazole and Miconazole, Compounded in HUMCO RECURA Topical Cream to Determine Beyond-use Date ABSTRACT Pradeep Gautam, MS Chemistry A novel compounding vehicle (RECURA) has previously been proven to Bob Light, BS, RPh penetrate the nail bed when compounded with the antifungal agent miconazole or fluconazole, providing for an effective treatment for onychomycosis. In this Troy Purvis, PhD study, miconazole and fluconazole were compounded separately in RECURA compounding cream, and they were tested at different time points (0, 7, 14, 28, 45, 60, 90, and 180 days), determining the beyond-use date of those INTRODUCTION formulations. The beyond-use date testing of both formulations (10% Onychomycosis is a fungal infection of miconazole in RECURA and 10% fluconazole in RECURA) proved them to be the nail bed in the fingers, or more com- physically, chemically, and microbiologically stable under International monly the toes, which affects an estimated Conference of Harmonisation controlled room temperature (25°C ± 2°C/60% 1 10% of the world’s population. Trichophy- RH ±5%) for at least 180 days from the date of compounding. Stability- ton is the typical fungal genus that causes indicating analytical method validation was completed for the simultaneous these infections in Western countries, while determination of miconazole and fluconazole in RECURA base using high- those living tropical regions experience Candida, Aspergillus, or Scytaldium infec- performance liquid chromatography coupled with photodiode array detector tion,2 but the symptoms of these infections prior to the study. are similar across the board. Minor infec- tion causes a yellow or black thickening of the nail bed, while further progression can 48% cure rate),1 yet concern about long- These medications must be in direct contact result in the nail chipping away and leaving term dosing and severe side-effects due to with the fungus in order to kill it.5 The FDA- an open sore, leading to secondary infec- oral administration exists.
    [Show full text]
  • Oral Antifungals Month/Year of Review: July 2015 Date of Last
    © Copyright 2012 Oregon State University. All Rights Reserved Drug Use Research & Management Program Oregon State University, 500 Summer Street NE, E35 Salem, Oregon 97301-1079 Phone 503-947-5220 | Fax 503-947-1119 Class Update with New Drug Evaluation: Oral Antifungals Month/Year of Review: July 2015 Date of Last Review: March 2013 New Drug: isavuconazole (a.k.a. isavunconazonium sulfate) Brand Name (Manufacturer): Cresemba™ (Astellas Pharma US, Inc.) Current Status of PDL Class: See Appendix 1. Dossier Received: Yes1 Research Questions: Is there any new evidence of effectiveness or safety for oral antifungals since the last review that would change current PDL or prior authorization recommendations? Is there evidence of superior clinical cure rates or morbidity rates for invasive aspergillosis and invasive mucormycosis for isavuconazole over currently available oral antifungals? Is there evidence of superior safety or tolerability of isavuconazole over currently available oral antifungals? • Is there evidence of superior effectiveness or safety of isavuconazole for invasive aspergillosis and invasive mucormycosis in specific subpopulations? Conclusions: There is low level evidence that griseofulvin has lower mycological cure rates and higher relapse rates than terbinafine and itraconazole for adult 1 onychomycosis.2 There is high level evidence that terbinafine has more complete cure rates than itraconazole (55% vs. 26%) for adult onychomycosis caused by dermatophyte with similar discontinuation rates for both drugs.2 There is low
    [Show full text]