Antimycotic Activity Research Articles

Synthesis and antimycotic activity of new derivatives of imidazo[1,2-a]pyrimidines.

The heterocyclic core of imidazo[1,2-a]pyrimidine was formed in satisfactory yields as a result of the interaction of the readily available 2-aminoimidazole with N-substituted maleimides or N-arylitaconimides. The mechanism of the studied processes was postulated basing on experimental data, HPLC-MS analysis of reaction mixtures, and quantum chemical calculations. Molecular docking results of the obtained imidazo[1,2-a]pyrimidines, when compared with voriconazole, a drug already in clinical use, suggest that they may possess antifungal activity against Candida albicans.

Antimycotic Activity of in silico Validation of Bioactive Compounds of Roccella montagnei Bel. against Clinically Isolated Onychomycosis Fungus Trichophyton mentagrophytes

Antimycotic Activity of in silico Validation of Bioactive Compounds of Roccella montagnei Bel. against Clinically Isolated Onychomycosis Fungus Trichophyton mentagrophytes

Antifungal activity’s study of the of new derivatives of pyrrolo[3,4-c]pyrazol-3-ones and pyrazol-3- carboxamides in the biofilm model of Candida spp.

The search for new antifungal drugs is current interest due to the wide spread of fungal infections. To simulate the antifungal effect of new promising compounds with high antifungal activity in planktonic culture in clinical practice, it is necessary to study their effect on the biofilm of micromycetes.Aim: To study the antifungal activity of new promising representatives of silver salts of pyrazoles and their condensed systems under conditions of biofilm formation.Material and Methods. To study the antifungal activity of silver salts I and II, the micromethod of two-fold serial dilutions was used. Activity against a typical and 14 clinical highly virulent isolates of C. albicans was studied. The study of the antimycotic activity of substances under biofilm conditions was carried out using resazurin to quantify the degree of biofilm formation. The minimum inhibitory concentrations for biofilms were calculated (sMIC50 - the concentration of the antifungal substance at which a 50% decrease in fluorescence is observed compared to the positive control).Results and Discussion. It was shown that the antifungal effect of the studied compounds in biofilm culture of clinical strains of Candida spp. is significantly lower than in planktonic culture. High antifungal activity of the silver salt of pyrazole-3- carboxamide in planktonic and biofilm cultures of resistant strains of Candida albicans, exceeding the effect of the reference drug fluconazole by 2.8–11.2 times, was revealed.Conclusion. A promising pyrazole-3-carboxamide derivative has been identified that effectively inhibits the growth of Candida albicans biofilms, which can be recommended for further study.

Aspergillus versicolor mediated biofabrication of zinc phosphate nanosheets for exploring their antimycotic activity and development of alginate-based nanocomposite for enhanced dye degradation

The production of novel, suitable, and cost-effective nanocomposites are highly required for its prospective application in the remediation of environmental pollutants and as antimycotic agents. Zinc phosphate nanosheets (ZP-ns) were fabricated by harnessing the exometabolites of Aspergillus versicolor and then incorporated within an alginate biopolymer (ZP-ns@Alg) to improve the biosorptive removal of the methyl orange (MthO) dye from its aqueous solution. For the very first time, the antimycotic activity of the green synthesized ZP-ns was unveiled. The mycelial growth inhibition was obtained in a dose-dependent manner with significant (P < 0.05) behavior compared to the control plates. The biosorption conditions using ZP-ns@Alg microbeads were optimized using the response surface methodology-based central composite design (RSM-CCD) to maximize the biosorption efficiency. The highest biosorptive efficiency was achieved at pH 4.0, biosorption dosage 0.07 g, contact time 50 min, dye concentration 100 mg/l, and shaking speed 100 rpm. The equilibrium data were more tailored to the pseudo-second order (PS) model with an R2 of 0.9955 and a Langmuir isotherm (R2 = 0.9945) with a maximum biosorptive capacity (qmax) of 166.95 mg/g and an average RL value of 0.0003, indicating favorable biosorption. The removal capacity was reduced to ∼90 % after the 6th cycle, which is a robust signal that the developed biosorbent microbeads could be recycled and regenerated for a prolonged time. These results marked the application of ZP-ns as a novel antimycotic agent with excellent activities. Microbeads, made from low-cost biopolymers, can be applied to remediating environmental pollutants from wastewater.

Adenocalymma alliaceum: An Overview

Adenocalymma alliaceum, commonly known as Garlic Vine or Lahsun bel, is an herbal shrub belonging to the family Bignoniaceae. It is native to northern Brazil and the Amazon rainforest, and certain species can also be found in the Chhattisgarh, Kerala states of India. This evergreen plant is highly valued for its ornamental qualities, with bright green leaves and tri-colored blooms that emit a distinct garlic-like fragrance. It grows up to 6-8 feet in height and is popular for landscaping purposes. The plant has various pharmacological activities that have been studied particularly in the management of diabetes mellitus. The bark, leaves, stems, and roots of Adenocalymma alliaceum contain a range of bioactive compounds that have been used to treat different diseases and disorders. Phytoconstituents such as diallyl disulfide and diallyl trisulfide are major chemical constituents of the plant, exhibiting antimicrobial, antihyperlipidemic, antifungal, and antimycotic activities. These properties make Adenocalymma alliaceum a promising source for the development of allopathic drugs. While the plant has traditional and cultural significance, it has also gained attention for its potential therapeutic properties. However, it is important to note that although it is used as a folk medicine in local communities, it is not extensively mentioned in published books or literature. In summary, Adenocalymma alliaceum is an intriguing natural resource with a rich cultural heritage and significant pharmacological potential. Further research and exploration of this plant may uncover additional therapeutic benefits and contribute to the development of novel drugs and treatments.

Vaginal Ovule Loaded with Bismuth Lipophilic Nanoparticles and Cetylpyridinium Chloride Inhibits Human Cervical Carcinoma and Candida albicans Growth.

Bismuth lipophilic nanoparticles (BisBAL NPs) and cetylpyridinium chloride (CPC) are antineoplastic and antimicrobial in vitro. As a next pre-clinical step, a clinically viable dosage form for vaginal application was developed. Compendial pharmacopeial tests (mass uniformity, disintegration, and compressive mechanics) and inductively coupled plasma optical emission spectroscopy were conducted on in-house developed glycerinated gelatin (60:15 v/w) vaginal ovules containing BisBAL NP-CPC. The antimycotic activity of BisBAL NP-CPC vaginal ovules was analyzed using disk diffusion and cell viability XTT assays. The antitumor properties of BisBAL NP-CPC vaginal ovules were assessed by cell viability MTT tests. BisBAL NP-CPC and drug-free vaginal ovules deposited into ex vivo porcine vaginas disaggregated without signs of adverse cytotoxicity within the timespan of clinical efficacy. BisBAL NP-CPC vaginal ovules demonstrated antifungal efficacy comparable to miconazole: C. albicans growth inhibition haloes in diffusion tests were 23 ± 0.968 mm (n = 3) for BisBAL NP-CPC and 20.35 ± 0.899 mm (n = 3) for miconazole. Likewise, BisBAL NP-CPC vaginal ovules reduced HeLa cell growth by 81%, outperforming the clinical reference of 500 μM 5-fluouracil, which induced a 70% growth inhibition. BisBAL NP-CPC incorporated into glycerinated gelatin vaginal ovules constitute an innovative drug delivery system for topical antimycotic and anti-cervical carcinoma treatments.

Formulation and Antimycotic Evaluation of Colloidal Itraconazole-Loaded Metered Dose Sprays for Treating Superficial Mycoses.

Commercial topical formulations containing itraconazole (poorly water soluble), for mycotic infections, have poor penetration to infection sites beneath the nails and skin thereby necessitating oral administration. To improve penetration, colloidal solutions of itraconazole (G1-G4) containing Poloxamer 188, tween 80, ethanol, and propylene glycol were prepared and incorporated into HFA-134-containing sprays. Formulations were characterized using particle size, drug content, and Fourier-transform infrared spectroscopy (FTIR). In vitro permeation studies were performed using Franz diffusion cells for 8h. Antimycotic activity on Candida albicans and Trichophyton rubrum was performed using broth micro-dilution and flow cytometry, while cytotoxicity was tested on HaCaT cell lines. Particle size ranged from 39.35-116.80nm. FTIR and drug content revealed that G1 was the most stable formulation (optimized formulation). In vitro release over 2h was 45% for G1 and 34% for the cream. There was a twofold increase in skin permeation, fivefold intradermal retention, and a sevenfold increase in nail penetration of G1 over the cream. Minimum fungicidal concentrations (MFC) against C. albicans were 0.156 and 0.313µg/mL for G1 and cream, respectively. The formulations showed optimum killing kinetics after 48h. MFC values against T. rubrum were 0.312 and 0.625µg/mL for the G1 and cream, respectively. Transmission electron microscopy revealed organelle destruction and cell leakage for G1 in both organisms and penetration of keratin layers to destroy T. rubrum. Cytotoxicity evaluation of G1 showed relative safety for skin cells. The G1 formulation showed superior skin permeation, nail penetration, and fungicidal activity compared with the cream formulation.

Penetration Profiles of Four Topical Antifungals in Mycotic Human Toenails Quantified by Matrix-Assisted Laser Desorption Ionization-Fourier Transform Ion Cyclotron Resonance Imaging.

Onychomycosis is a fungal infection of the nails that can be challenging to treat. Here, matrix-assisted laser desorption ionization-Fourier transform ion cyclotron resonance (MALDI-FTICR) imaging was applied to the quantitative analysis of the penetration profile of the antifungal compound, amorolfine, in human mycotic toenails. The amorolfine profile was compared with those of three other antifungals, ciclopirox, naftifine, and tioconazole. Antifungal compounds (amorolfine 5% lacquer, ciclopirox 8% lacquer, naftifine 1% solution, and tioconazole 28% solution) were applied to mycotic nails (n = 42). Nail sections were prepared, and MALDI-FTICR analysis was performed on the sections at a spatial resolution of 70 μm to compare the distribution profiles. Based on the minimum inhibitory concentrations of the four test compounds needed to kill 90% (MIC90) of the fungal organism, Trichophyton rubrum, the fold differences between the MIC90 and the antifungal concentrations in the nails (termed the multiplicity of the MIC90) were calculated for each. The penetration profiles indicated higher concentrations of amorolfine and ciclopirox in the deeper layers of the nails 3h after treatment, compared with naftifine and tioconazole. The mean concentrations across the entire nail sections at 3h were significantly different among the four antifungals: amorolfine, 2.46mM; ciclopirox, 0.95mM; naftifine, 0.63mM; and tioconazole, 1.36mM (p = 0.016; n = 8 per compound). The median multiplicity of the MIC90 at 3h was 191-fold for amorolfine, tenfold for ciclopirox, 52-fold for naftifine, and 208-fold for tioconazole. In this study, MALDI-FTICR was successfully applied to the quantitative analysis of antifungal distribution in human mycotic nails. The findings suggest that amorolfine penetrates deeper layers of the nail and accumulates at concentrations far exceeding the MIC needed to exert antimycotic activity.

Production, optimization and characterization of partially purified anti-mycotic compound from marine soil derived streptomycetes originating at unexplored region of Bay of Bengal, India

Sixty-eight morphologically distinct isolates of marine actinomycetes were derived from seashore, mangrove, and saltpan ecosystems located between the Palk Strait and Gulf of Mannar region, Bay of Bengal, Tamilnadu. Twenty-five (36.8%) isolates exhibited anti-mycotic activity against Candida albicans and Cryptococcus neoformans in preliminary screening, and 4 isolates with prominent activity were identified and designated at the genus level as Streptomyces sp. VPTS3-I, Streptomyces sp. VPTS3-2, Streptomyces sp. VPTSA1-4 and Streptomyces sp. VPTSA1-8. All the potential antagonistic isolates were further characterized with phenotypic and genotypic properties including 16S rRNA gene sequencing and identified species level as Streptomyces afghaniensis VPTS3-1, S. matensis VPTS3-2, S. tuirus VPTSA1-4 and S. griseus VPTSA1-8. In addition, the active fractions from the potential antagonistic streptomycetes were extracted with organic solvents by shake flask culture method and the anti-mycotic efficacies were evaluated. The optimization parameters for the production of the anti-mycotic compound were found to be pH between 7 and 8, the temperature at 30ᵒC, the salinity of 2%, incubation of 9 days, and starch and KNO3 as the suitable carbon and nitrogen sources respectively in starch casein medium.

Sertaconazole-PLGA nanoparticles for management of ocular keratitis

Ocular fungal infections can pose severe health conditions that may develop into vision impairment and blindness. Sertaconazole (STZ) is a widely used antifungal; however, its low aqueous solubility restricts its topical application for managing ocular keratitis. This investigation aimed to develop polymeric nanoparticles as delivery carriers to improve the ophthalmic availability of STZ for treating fungal keratitis. The impact of STZ solid dispersion incorporation within polymeric nanoparticles for in vitro drug release enhancement was also evaluated. STZ-laden PLGA NPs were formulated via nanoprecipitation technology, using a 24-full factorial layout to optimize the formulation. The formed nanoparticles were assessed for encapsulation efficiency percentage, hydrodynamic size, surface charge, and polydispersity index. The selected formula exhibited a particle size of 305.9 ± 4.36 nm, an entrapment efficiency (EE%) of 98.8 ± 0.008%, a surface charge of 22.57 ± 0.23 mV, and a low polydispersity index, indicating a uniform size distribution. Incorporating STZ in a solid dispersion form with PEG 2000 at a 1:3 w/w drug-to-carrier ratio increased the hydrodynamic size of the PLGA NPs. However, no significant variation in the entrapment efficiency percentage was recorded. The developed STZ-solid dispersion-loaded PLGA NPs have round-shaped structures. DSC and FTIR spectroscopy data indicated drug amorphization with successful loading within the PLGA matrix. Introducing the drug as a solid dispersion within PLGA NPs resulted in enhancing the rate of drug dissolution at initial time intervals, followed by a controlled drug release over 24 h. STZ-PEG2000-laden PLGA NPs enhanced permeability through rabbits’ corneas (Papp), 2.5-fold higher versus STZ-loaded PLGA NPs. The antimycotic activity of the developed formulation was tested against Candida albicans, and a 4-fold reduction in the MIC value was detected upon applying the nanoparticles’ formulation embedding STZ solid dispersion versus that containing the free drug. In conclusion, the formulation of solid dispersions of STZ loaded in PLGA nanoparticles may serve as a starting point for an efficient approach to the ocular delivery of hydrophobic medications and a viable setup for the upcoming research in animal models of fungal keratitis.

In Vitro Antimycotic Activity and Structural Damage against Canine Malassezia pachydermatis Strains Caused by Mexican Stingless Bee Propolis.

This work describes the antimycotic activity of propolis from the stingless bees Scaptotrigona mexicana and Tetragonisca angustula, collected from two Mexican regions (Veracruz and Chiapas, respectively), against three clinical isolates and the reference strain ATCC 14522 of Malassezia pachydermatis, the causative agent of canine otitis. The chemical components of the ethanolic extracts of propolis were determined by gas chromatography coupled with mass spectrometry (GC-MS), and sesquiterpenes were the predominant compounds. The antimycotic activity was evaluated by plate microdilution. The induced changes in the yeasts were evaluated by fluorescence microscopy and staining with calcofluor white and propidium iodide. The minimum inhibitory concentration (MIC) was 7.11 mg/mL, and the minimum fungicidal concentration was 21.33 mg/mL for both extracts. The EPPs of Scaptotrigona mexicana and Tetragonisca angustula caused substantial damage to yeast morphology, where the propidium iodide staining of the yeasts treated with both EEPs revealed the penetration of this marker, which indicates the destruction of the cell wall and plasma membrane of the fungi. This result suggests that these types of propolis could be used as alternative treatments for canine external otitis. To the best of our knowledge, this seems to be the first scientific report that has demonstrated structural damage in Malassezia pachydermatis by Mexican stingless bee propolis.

Study of the effect of bifonazole concentration on the antifungal activity of vaginal suppositories

The analysis of the current state of pharmacotherapy for vulvovaginal candidiasis reveals that there is a contemporary need for the development of soft dosage forms for the local treatment of infectious diseases affecting the vulva and vagina. This should be based on azole derivatives that, despite possessing a well-established wide spectrum of antifungal and antibacterial effects, have not been utilized for vaginal administration in domestic formulations. The successful realization of this project would enable the field of domestic dermatology to provide effective, compliant, and affordable drugs for gynecological practice to the general population of Ukraine. Additionally, it would establish a viable alternative to imported pharmacotherapeutic agents. Aim. The purpose of this work is the scientific substantiation of the concentration of bifonazole in suppository compositions for vaginal use. Materials and methods. Research was conducted to investigate the influence of bifonazole concentration ranging from 1 % to 15 % in soft dosage forms for vaginal use. Model compositions were formulated on a polyethylene oxide carrier, considering its solubility. The antifungal activity of the experimental suppository compositions was chosen as the optimization parameter and assessed using the diffusion method in agar against Candida albicans ATCC 885-653. Variance analysis of the results revealed a significant impact of bifonazole concentration on the antimycotic activity of the suppository compositions based on the model polyethylene oxide. Results. The research results show that increasing the concentration of the active pharmaceutical ingredient in suppository masses above 10 % does not lead to a statistically significant increase in their antimycotic activity. Conclusions. As a result of the conducted study on the antifungal effect of suppository masses with bifonazole on a model polyethylene oxide basis, it was found that the concentration of the active pharmaceutical ingredient has a statistically significant effect on the effectiveness of the soft dosage form. It was established that a ten percent concentration of bifonazole, equivalent to 0.3 g of the biologically active substance in vaginal suppositories, provides the optimal level of their antifungal effect.

Synthesis of novel benzylamine antimycotics and evaluation of their antimycotic potency.

A series of 23 novel benzylamines was synthesized by reductive amination from halogen-substituted 3- and 4-benzyloxybenzaldehyde derivatives and 6-methylhept-2-yl amine or n-octylamine. The antimycotic activity of the resulting amines was evaluated in a microdilution assay against the apathogenic yeast Yarrowia lipolytica as test microorganism. Promising compounds were also tested against human pathogenic Candida species. The influence of halogen substituents at the benzyl ether side chain was studied in this screening, as well as the influence of the branched side chain of (±)-6-methylhept-2-yl amine in comparison with the n-octyl side chain.

Nanosponge hydrogel of octadecyl 3-(3,5-di-tert-butyl-4-hydroxyphenyl) propanoate of Alcaligenes faecalis

Octadecyl 3-(3,5-di-tert-butyl-4-hydroxyphenyl) propanoate (ODHP) was extracted in a previous study from the culture broth of soil isolate Alcaligenes faecalis MT332429 and showed a promising antimycotic activity. This study was aimed to formulate ODHP loaded β-cyclodextrins (CD) nanosponge (NS) hydrogel (HG) to control skin fungal ailments since nanosponges augment the retention of tested agents in the skin. Box-Behnken design was used to produce the optimized NS formulation, where entrapment efficiency percent (EE%), polydispersity index (PDI), and particle size (PS) were assigned as dependent parameters, while the independent process parameters were polyvinyl alcohol % (w/v %), polymer-linker ratio, homogenization time, and speed. The carbopol 940 hydrogel was then created by incorporating the nanosponges. The hydrogel fit Higuchi’s kinetic release model the best, according to in vitro drug release. Stability and photodegradation studies revealed that the NS-HG remained stable under tested conditions. The formulation also showed higher in vitro antifungal activity against Candida albicans compared to the control fluconazole. In vivo study showed that ODHP-NS-HG increased survival rates, wound contraction, and healing of wound gap and inhibited the inflammation process compared to the other control groups. The histopathological examinations and Masson’s trichrome staining showed improved healing and higher records of collagen deposition. Moreover, the permeability of ODHP-NS-HG was higher through rats’ skin by 1.5-folds compared to the control isoconazole 1%. Therefore, based on these results, NS-HG formulation is a potential carrier for enhanced and improved topical delivery of ODHP. Our study is a pioneering research on the development of a formulation for ODHP produced naturally from soil bacteria.Key points• Octadecyl 3-(3,5-di-tert-butyl-4-hydroxyphenyl) propanoate was successfully formulated as a nanosponge hydrogel and statistically optimized.• The new formula exhibited in vitro good stability, drug release, and higher antifungal activity against C. albicans as compared to the fluconazole.• Ex vivo showed enhanced skin permeability, and in vivo analysis showed high antifungal activity as evidenced by measurement of various biochemical parameters and histopathological examination.

Fungal-mediated synthesis of silver nanoparticles: a novel strategy for plant disease management.

Various traditional management techniques are employed to control plant diseases caused by bacteria and fungi. However, due to their drawbacks and adverse environmental effects, there is a shift toward employing more eco-friendly methods that are less harmful to the environment and human health. The main aim of the study was to biosynthesize silver Nanoparticles (AgNPs) from Rhizoctonia solani and Cladosporium cladosporioides using a green approach and to test the antimycotic activity of these biosynthesized AgNPs against a variety of pathogenic fungi. The characterization of samples was done by using UV-visible spectroscopy, SEM (scanning electron microscopy), FTIR (fourier transmission infrared spectroscopy), and XRD (X-ray diffractometry). During the study, the presence of strong plasmon absorbance bands at 420 and 450 nm confirmed the AgNPs biosynthesis by the fungi Rhizoctonia solani and Cladosporium cladosporioides. The biosynthesized AgNPs were 80-100 nm in size, asymmetrical in shape and became spherical to sub-spherical when aggregated. Assessment of the antifungal activity of the silver nanoparticles against various plant pathogenic fungi was carried out by agar well diffusion assay. Different concentration of AgNPs, 5 mg/mL 10 mg/mL and 15 mg/mL were tested to know the inhibitory effect of fungal plant pathogens viz. Aspergillus flavus, Penicillium citrinum, Fusarium oxysporum, Fusarium metavorans, and Aspergillus aflatoxiformans. However, 15 mg/mL concentration of the AgNPs showed excellent inhibitory activity against all tested fungal pathogens. Thus, the obtained results clearly suggest that silver nanoparticles may have important applications in controlling various plant diseases caused by fungi.

Subterranean termites raise the alarm when their anti-fungal weapon falters.

Termicin is an anti-fungal defensin that is disseminated from termite salivary glands. The peptide appears to be critical for the elimination with mutual grooming (allogrooming) of pathogenic spores (conidia) that have attached to the insect cuticle. There has been a recent selective sweep for an advantageous variant of this peptide in the subterranean termite Reticulitermes flavipes. We tested the anti-mycotic activity of a recombinant termicin corresponding with this variant against the conidia of different Metarhizium fungal isolates from soil close to foraging R. flavipes workers. Termicin was most effective against isolates that had previously been shown to elicit a relatively weak alarm response, as indicated by brief bouts of rapid longitudinal oscillatory movement (LOM). These isolates that elicited weak alarm were also the deadliest apparently because the survival of termites exposed to the fungus depends on a strong social immune response (LOMs and allogrooming). The selective pressure for a single termicin variant may have been driven by the most dangerous isolates that elicit a weak behavioral response. The correlation between termicin anti-fungal activity and LOM suggests that pathogen-associated molecular patterns that affect termite recognition of conidial contamination and the onset of elevated allogrooming also affect the vulnerability of conidia to the disruption of their cell membranes by termicin.

ANTIMYCOTIC ACTIVITY OF THE ISOLATES OF LACTOBACTERIA FROM WA-TER AND MUSSELS OF BLACK SEA

Aim. Determination of the presence of antimycotic activity and its level in thirteen lactobacteria isolates from Black Sea water and mussels. Methods. Antimycotic activity of lactic acid bacteria (LAB) isolates was tested by agar diffusion method in 24-well plates. To determine character of action the plates were incubated for 7 days at 25 °C. Results. For the first time antimycotic activity of marine LAB from Odesa coast was estimated. The majority of the tested isolates of lactobateria exhibited antimycotic activity of high level completely inhibiting (in 100%) as mycelium growth as well as spore formation of Penicillium expansum UKM F-575 and Aspergillus niger UKM F-16706 on second day of the study. Four isolates (M.5.1, M.5.2, M.7.1, M.7.2) showed lower antimycotic activity (from 0 to 75%). Eight LAB isolates from seawater (W.1.1, W.1.2, W.1.3, W.1.4, W.1.5, W.1.дк, W.2.3, W.2.4) and one isolate from mussel liquor (M4.1) completely inhibited mycelial growth and sporulation of P. expansum UКМ F-575 and A. niger UКМ F-16706 even within seven days indicating fungicidal character of action. Conclusions. The most of tested LAB isolates from Black Sea exhibited high antimycotic activity against P. expansum UКМ F-575 and A. niger UКМ F-16706 indicator strains. The most active lactobacteria isolates were W.1.1, W.1.2, W.1.3, W.1.4, W.1.5, W.1.дк, W.2.3, W.2.4 isolated from Black Sea water and M4.1 – from mussel liquor. The character of the revealed antimycotic activity was determined as fungicidal.

A new stability indicating HPLC and LC-APCI-MS methods for the estimation of Flucytosine in pharmaceutical dosage forms

Flucytosine is an anti-fungal agent which acts against mycotic infections. The anti-mycotic activity of Flucytosine is due to its conversion in to 5-fluoro uracil. In the present study the authors have proposed a new stability indicating isocratic RP-HPLC as well as LC-APCI-MS methods for the estimation of Flucytosine and the methods are validated as per ICH guidelines. Thermo scientific - TSQ Quantis with Vanquish HPLC coupled with MS was employed for the study with Simpack C18 (250 mm x 4.6 mm x 5µm) column. A triple quadrupole mass spectrometer with atmospheric pressure chemical ionization (APCI) source, running in the positive mode (as well as negative mode) was used for the detection. A mixture of 0.1% Acetic acid: Methanol was used as mobile phase (50:50, v/v) (UV detection at 235 nm). A wide linearity concentration range 1.0-120 μg/ml was observed and the method is found to be precise and accurate and can be used for the estimation of marketed formulations. Stress degradation studies were performed and the method is found to be selective and specific.

Efficacy of topical forms of sertaconazole in treatment of mycoses of skin

Published research results indicate the high effectiveness of sertaconazole in the treatment of mycoses of the skin. According to a number of studies, it is superior to other antifungal agents in terms of cure rate and speed of action, and also has anti-inflammatory and antipruritic activity.Material and methods. The aim of the observational study was to evaluate the effectiveness of Zalain cream (sertaconazole 2%) in patients with mycosis of the smooth skin of the groin area. We observed 21 patients (13 men and 8 women) aged from 37 to 72 years with a verified diagnosis of mycosis of smooth skin, confirmed by microscopic and cultural methods. In patients, during a cultural study, a mixed fungal-bacterial infection was isolated in various combinations: 14 (66.7%) – Trichophyton rubrum and Staphylococcus, 7 (33.3%) – Candida albicans and Staphylococcus. Of the concomitant pathologies, the following diseases were most often diagnosed: hypertension (52.4%), obesity (BMI &gt; 30) (47.6%), type 2 diabetes mellitus (42.9%), gastrointestinal diseases (23.8%), diseases of the hepatobiliary system (19.1%). The effectiveness was assessed taking into account the VAS index (erythema, infiltration, desquamation, cracks, itching, burning) and special methods (microscopic and cultural) of the study at control points B1 (before therapy) and B2 (after 4 weeks of therapy). Long-term results of observations (disease relapse) were assessed after 6 months.Results. The total VAS at control point B 2 decreased by 94.9% (p &lt; 0.01). After therapy (4 weeks), in 18 (85.7%) patients, pathogenic fungi (Trichophyton rubrum, Trichophyton mentagrophytes var. interdigitale) were not sown during cultural examination. Patients with no laboratory cure were recommended to continue therapy with sertaconazole for 2–4 weeks until complete eradication of pathogenic fungi. Long-term results of observations (6 months) showed relapse of the disease in 28.6% of patients with concomitant metabolic syndrome and type 2 diabetes mellitus. Also, among patients with relapses, males predominated – 66.7%.Conclusions. Sertaconazole has a wide spectrum of antimycotic activity, which makes it possible to quickly achieve clinical and mycological recovery in patients with mycosis of smooth skin in the groin area.

Selected N-Terpenyl Organoselenium Compounds Possess Antimycotic Activity In Vitro and in a Mouse Model of Vulvovaginal Candidiasis.

In the present work, a series of N-terpenyl organoselenium compounds (CHB1-6) were evaluated for antimycotic activity by determining the minimum inhibitory concentration (MIC) for each compound in fluconazole (FLU)-sensitive (S1) and FLU-resistant (S2) strains of Candida albicans (C. albicans). The most active compounds in the MIC screen were CHB4 and CHB6, which were then evaluated for cytotoxicity in human cervical cancer cells (KB-3-1) and found to be selective for fungi. Next, CHB4 and CHB6 were investigated for skin irritation using a reconstructed 3D human epidermis and both compounds were considered safe to the epidermis. Using a mouse model of vulvovaginal candidiasis (VVC), CHB4 and CHB6 both exhibited antimycotic efficacy by reducing yeast colonization of the vaginal tract, alleviating injury to the vaginal mucosa, and decreasing the abundance of myeloperoxidase (MPO) expression in the tissue, indicating a reduced inflammatory response. In conclusion, CHB4 and CHB6 demonstrate antifungal activity in vitro and in the mouse model of VVC and represent two new promising antifungal agents.