scholarly journals EVALUATION OF ANTIFUNGAL AND ANTIBACTERIAL ACTIVITY OF SOME NEW BENZIMIDAZOLE DERIVATIVES

2018 ◽  
Vol 48 (2) ◽  
pp. 125-129
Author(s):  
K. ZOMORODIAN ◽  
S. KHABNADIDEH ◽  
L. ZAMANI ◽  
K. PAKSHIR ◽  
M. TAJADDOD
Keyword(s):  
Antifungal Activity ◽  
Fungal Infections ◽  
Antimicrobial Activities ◽  
Antifungal Drugs ◽  
In Vivo Studies ◽  
Benzimidazole Derivatives ◽  
Dilution Method ◽  
Gram Positive ◽  
Meta Position

The extensive use of antifungal drugs and their resistance against fungal infections have led to discover new antimicrobial compounds. We previously described synthesis of some new derivatives of 2-methylbenzimidazole (1a-5a) and 5,6dimethylbenzimidazol (1b-5b). Here we evaluated the antimicrobial activities of these compounds against different species of micro organisms including gram positive and gram negative bacteria as well as fungi. Broth micro-dilution method as recommended by clinical and laboratory standard institute (CLSI) was used for this purpose. The results show compounds 2-Methyl-1-(3-methylbenzyl)-1H-benzo [d]imidazole (5a) and 5,6-Dimethyl-1-(3-methyl benzyl)-1H-benzo[d]imidazole (5b) had the best antifungal activity against the examined fungi and gram positive bacteria. Moreover these two compounds inhibited the growth of azole resistant strains. By comparison the relationship between the structures and activities of the tested compounds revealed that the presence of methyl residue in meta position of benzyl group enhance the antifungal activity. Regarding a broad spectrum antifungal activities of some of the tested compounds, they might be a good candidate for further in vivo studies to evaluate their pharmacological activity and toxicity as a novel antifungal agents.

scholarly journals Non-toxic Cobalt(III) Schiff Base Complexes with Broad Spectrum Antifungal Activity

2020 ◽  
Author(s):  
Angelo Frei ◽  
A. Paden King ◽  
Gabrielle J. Lowe ◽  
Amy K. Cain ◽  
Francesca L. Short ◽  
...  
Keyword(s):  
Schiff Base ◽  
Antifungal Activity ◽  
Broad Spectrum ◽  
Bacterial Infections ◽  
Fungal Infections ◽  
Antifungal Drugs ◽  
New Drugs ◽  
Schiff Base Complexes ◽  
In Vivo Studies

Resistance to currently available antifungal drugs has quietly been on the rise but overshadowed by the alarming spread of antibacterial resistance. There is a striking lack of attention to the threat of drug resistant fungal infections, with only a handful of new drugs currently in development. Given that metal complexes have proven to be useful new chemotypes in the fight against diseases such as cancer, malaria, and bacterial infections, it stands to reason to explore their possible utility in treating fungal infections. Herein we report a series of cobalt(III) Schiff base complexes with broad spectrum antifungal activity. Some of these complexes (1-3) show minimum inhibitory concentrations (MIC) in the low micro- to nanomolar range against a series of Candida and Cryptococcus yeasts. Additionally, we demonstrate that these compounds show no cytotoxicity against both bacterial and human cells. Finally, we report first in vivo toxicity data on these compounds in Galleria mellonella, showing that doses as high as 266 mg/kg are tolerated without adverse effects, paving the way for further in vivo studies of these complexes. <br>

scholarly journals Non-toxic Cobalt(III) Schiff Base Complexes with Broad Spectrum Antifungal Activity

2020 ◽  
Author(s):  
Angelo Frei ◽  
A. Paden King ◽  
Gabrielle J. Lowe ◽  
Amy K. Cain ◽  
Francesca L. Short ◽  
...  
Keyword(s):  
Schiff Base ◽  
Antifungal Activity ◽  
Broad Spectrum ◽  
Bacterial Infections ◽  
Fungal Infections ◽  
Antifungal Drugs ◽  
New Drugs ◽  
Schiff Base Complexes ◽  
In Vivo Studies

Resistance to currently available antifungal drugs has quietly been on the rise but overshadowed by the alarming spread of antibacterial resistance. There is a striking lack of attention to the threat of drug resistant fungal infections, with only a handful of new drugs currently in development. Given that metal complexes have proven to be useful new chemotypes in the fight against diseases such as cancer, malaria, and bacterial infections, it stands to reason to explore their possible utility in treating fungal infections. Herein we report a series of cobalt(III) Schiff base complexes with broad spectrum antifungal activity. Some of these complexes (1-3) show minimum inhibitory concentrations (MIC) in the low micro- to nanomolar range against a series of Candida and Cryptococcus yeasts. Additionally, we demonstrate that these compounds show no cytotoxicity against both bacterial and human cells. Finally, we report first in vivo toxicity data on these compounds in Galleria mellonella, showing that doses as high as 266 mg/kg are tolerated without adverse effects, paving the way for further in vivo studies of these complexes. <br>

GROWTH INHIBITORY ACTIVITIES OF THE RHIZOME CRUDE EXTRACT OF Curcuma longa ON THE HUMAN PATHOGENIC FUNGUS Mucor circinelloides

2020 ◽  
Vol 65 (10) ◽  
pp. 82-91
Author(s):  
Phuong Nguyen Anh ◽  
Mai Le Thi Tuyet ◽  
Trung Trieu Anh
Keyword(s):  
Antifungal Activity ◽  
Crude Extract ◽  
Fungal Infections ◽  
Early Stage ◽  
Curcuma Longa ◽  
Pathogenic Fungus ◽  
Mucor Circinelloides ◽  
Antifungal Drugs ◽  
Diffusion Method ◽  
Dilution Method

Mucormycosis is an uncommon but life-threatening invasive fungal infection, mostly occurs in immunocompromised patients. Lacking the appropriate antifungal drugs is one of the reasons that lead to difficulties in the management of mucormycosis. Curcuma longa has been used traditionally and widely to treat various diseases, including fungal infections. In the search for novel antifungal compounds from natural resources, we evaluated the effect of rhizome crude extract of C. longa on Mucor circinelloides – a causal agent of mucormycosis. The results of screening, using broth dilution method and agar-well diffusion method, showed that the C. longa extract exhibited promising antifungal activity against the fungus M. circinelloides. In liquid medium, C. longa extract decreased the ability of spore germination and the speed of hyphae formation of M. circinelloides decreased by up to approximately 70% and 90%, respectively. Besides, in a solid medium, the crude extract presented similar activity with amphotericin B (400 μg\mL) in decreasing the growth of M. circinelloides by nearly 77%. Moreover, the extract of C. longa also likely to induce the yeast-like type of growth of the dimorphic M. circinelloides in the early stage. These results suggest the plant could be a potential source for further study on biochemical components and the mechanism of its antifungal activity.

Synthesis and Antimicrobial Activity of Some New N-(1H-benzimidazol-2- yl)-2-mercaptoacetamide Derivatives

2018 ◽  
Vol 15 (2) ◽  
pp. 154-159
Author(s):  
Asaf Evrim Evren ◽  
Sinem Tekinkoca ◽  
Leyla Yurttas
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Bacterial Resistance ◽  
Fungal Infections ◽  
Antimicrobial Activities ◽  
Benzimidazole Derivatives ◽  
Standard Drug ◽  
E Coli ◽  
Pharmacological Significance ◽  
Anti Fungal

Background: Due to multi-drug, extended-drug, and pandrug resistance phenotypes, bacterial resistance to antibiotics and fungal infections are a general health issue. Particulary, increase of fungal infections due to secondary cause of human diseases have been observed. An extensive variety of benzimidazole derivatives have been characterized for their chemotherapeutic significance. Benzimidazole derivatives have received important attention because of pharmacological significance during current years, especially antimicrobial, anti-fungal, antitubercular, antioxidant, anti-Alzheimer's disease and antihypertension activities. Methods: Some N-(1H-benzimidazol-2-yl)-2-mercaptoacetamide derivatives (2a-h) were synthesised and evaluated for their antimicrobial activity. The title compounds were gained by reacting N-(1H-benzimidazol-2-yl)-2-chloroacetamide with some substituted 2-mercapto heterocyclic rings. The synthesised compounds were investigated for their antimicrobial activities against C. albicans (ATCC 24433), C. krusei (ATCC 6258), C. glabrata (ATCC90030), C. parapsilosis (ATCC 22019), E. coli (ATCC 25922), E. coli (ATCC 35218), E. feacalis (ATCC 51299), E. feacalis (ATCC 29212), S. aureus (ATCC 25923), K. pneumoniae (ATCC 700603), P. aeruginosa (ATCC 27853). Results: The compounds showed high antifungal activity when compared with standard drug ketoconazole. In addition, all compounds (MIC 100 µg/mL) showed inhibitor activity against P. aeruginosa at two fold concentration of chloramphenicol (MIC 50 µg/mL). Also, compounds 2a, 2c and 2e (MIC: 50 µg/mL) have equal effect against E. coli (ATCC 35218) and more effective than other compounds (MIC of chloramphenicol: 100 µg/mL). Conclusıon: All compounds showed notable activity. Compounds have determined to possess higher antifungal activity than antibacterial activity. Additionally, compounds 2a with 1-methyltetrazole, 2c with benzothiazole and 2e with 6-chlorobenzothiazole moieties were found as the most active compounds.

Preparation, characterizations and evaluation of antifungal activity of eugenol-linalool emulgel against anthrophilic dermatophytic trichophyton rubrum

2021 ◽  
pp. 1-15
Author(s):  
Abdullah Akram ◽  
Muhammad Khalid Khan ◽  
Barkat Ali Khan
Keyword(s):  
Antifungal Activity ◽  
Skin Infection ◽  
Trichophyton Rubrum ◽  
Sem Analysis ◽  
Antifungal Drugs ◽  
In Vivo Studies ◽  
Stability Studies ◽  
Antifungal Activities

Trichophyton rubrum (T. Rubrum) is responsible for chronic cases of dermatophytosis which have high rates of resistance to antifungal drugs worldwide. The aim of this study was to formulate an emulgel of Eugenol-Linalool for the treatment of T. Rubrum infections. The emulgel was prepared by slow emulsification method and characterized for physical examination, pH analysis, swelling index, stability studies, spreading coefficient, SEM analysis, thermal analysis and PXRD studies. In-vitro antifungal activities were performed by growing T. rubrum on specialized media in petri dishes. In-vivo antifungal activity was performed in rabbits by inducing the skin infection by application of fungal strain. Results indicated that the emulgel formulation is highly stable and the physical properties of the emulgel remained quite feasible. No deterioration was observed in the formulation and the pH remained the same as the pH of skin. The viscosity and spreadability of the emulgel remained highly compatible. The results of in vitro and in vivo studies indicated that the Eugenol and Linalool both inhibited the growth of T. rubrum. Eugenol was more effective in inhibition of zone (38±0.01 mm) of T. rubrum as compared to Linalool (32.9±0.03 mm). Similarly it was observed that when the combination of both Linalool and Eugenol was used, the growth of T. rubrum (42±0.01 mm) was significantly (P <  0.05) inhibited. It is hence concluded that the emulgel containing Eugenol and Linalool possess strong in vitro and in vivo antifungal activities against the commercial strains of anthrophilic dermophytic T. Rubrum.

Carvacrol essential oil stimulates growth performance, immune response, and tolerance of Nile tilapia to Cryptococcus uniguttulatus infection

2020 ◽  
Vol 141 ◽  
pp. 1-14 ◽  
Author(s):  
HH Mahboub ◽  
YH Tartor
Keyword(s):  
Antifungal Activity ◽  
Growth Performance ◽  
Nile Tilapia ◽  
Fungal Infections ◽  
Antifungal Drugs ◽  
Fish Growth ◽  
Immunological Parameters ◽  
Species Production

This study investigated the antifungal activity of 5 essential oils (EOs) towards yeasts recovered from diseased fishes; and focused on the efficacy of one EO (carvacrol) on growth performance, non-specific immunity, and disease resistance of Nile tilapia Oreochromis niloticus against Cryptococcus uniguttulatus challenge. Thymoquinone, thymol, carvacrol, eugenol, and cinnamon were first tested in vitro against 20 clinical yeast strains in comparison with antifungal drugs (fluconazole, ketoconazole, itraconazole, amphotericin B, nystatin, and clotrimazole) using disc diffusion and broth microdilution methods. For the in vivo challenge, fish (n = 150) were divided into 5 groups (carvacrol prophylaxis, carvacrol treatment, itraconazole treatment, unchallenged control, and positive control; 30 fish group-1) with 3 replicates. Phagocytic activity, reactive oxygen species production, reactive nitrogen species production, myeloperoxidase, lysozyme activity, and total immunoglobulins were tested before and after challenge. Relative percent survival (RPS) and mortality percent were determined as indicators for functional immunity. EOs displayed divergent degrees of antifungal activity, and carvacrol was the most effective against the tested yeasts. The dietary additive of carvacrol significantly enhanced growth performance, all immunological parameters, and the RPS values (90%) compared to other treatments. This unique experimental model indicates that carvacrol seems promising not only for enhancing immunity and promoting fish growth, but also for controlling emerging fungal infections. Future studies should investigate different concentrations of carvacrol as well as its antifungal activity in different fish species.

scholarly journals IN VITRO AND IN VIVO ANTIFUNGAL ACTIVITY OF ALKALOID 3,5-bis(4,4’’-dimethoxy- [1,1’:2’,1’’-terphenyl]-4’-yl)-4H-pyrazole-4,4-diol FROM DERRIS INDICA (LAM) BENNETT SEEDS

2021 ◽  
pp. 133-140
Author(s):  
NUZHAT TABASSUM ◽  
VIDYASAGAR G. M. ◽  
RAGHUNANDAN D ◽  
SHIVAKUMAR I
Keyword(s):  
Antifungal Activity ◽  
Fungal Pathogens ◽  
Antifungal Drugs ◽  
Hexane Extract ◽  
In Vivo Studies ◽  
Antifungal Compound ◽  
In Vivo Evaluation ◽  
Derris Indica

Objectives: The aim of the present study is to isolate an antifungal compound from Derris indica (Lam) Bennett seed oil with various solvents and evaluation of its antifungal activity against the clinical species of Candida. Methods: D. indica seed hexane extract was tested against Trichophyton rubrum, Trichophyton tonsurans and Candida albicans. Hexane extract was fractioned using different solvents through column chromatography (CC). Isolated compound D1 was identified and characterized using ultraviolet, Fourier-transform infrared, 1HNMR, and mass spectroscopy. In vitro evaluation of D1 carried out against 12 Candida strains. In vivo evaluation of D1 carried out against T. rubrum, T. tonsurans, and C. albicans using an excision wound healing model on male Wistar rats. Results: Different concentrations of hexane extract showed antimicrobial activity against tested microorganism with varying minimum inhibitory concentration values. On fractionation with hexane-petroleum ether through CC, it yielded a crystalline fraction. Compound D1 characterized as a 3,5-bis (4,4’’-dimethoxy-[1,1’: 2’,1’’-terphenyl]-4’-yl)-4H-pyrazole-4,4-diol. A novel alkaloid compound from D. indica is a new report and proved to be inhibitory against C. albicans MTCC 3017 (14.83±0.28), MTCC 1637 (16.0±0.0), Candida glabrata MTCC 3814 (16.83±0.28) and MTCC 3014 (16.66±0.57), Candida tropicalis MTCC 230 (20.0±0.0), MTCC 1406 (12.33±0.57). C. glabrata MTCC 3981 was found to be resistant to the compound. In vivo studies showed no visual symptoms at the end of treatment indicating the therapeutic property of the compound. Conclusion: The D1 was found to be effective against human fungal pathogens and can be used as a base molecule in designing new antifungal drugs.

scholarly journals Antifungal Activity of Linear and Disulfide-Cyclized Ultrashort Cationic Lipopeptides Alone and in Combination with Fluconazole against Vulvovaginal Candida spp.

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1589
Author(s):  
Paulina Czechowicz ◽  
Damian Neubauer ◽  
Joanna Nowicka ◽  
Wojciech Kamysz ◽  
Grażyna Gościniak
Keyword(s):  
Antifungal Activity ◽  
Synergistic Effect ◽  
Antimicrobial Activities ◽  
The Other ◽  
In Vivo Studies ◽  
Antifungal Compounds ◽  
Candida Spp ◽  
Anticandidal Activity ◽  
Toxic Concentrations

Vulvovaginal candidiasis (VVC) occurs in over 75% of women at least once during their lifetime and is an infection that significantly affects their health. Candida strains resistant to standard azole antifungal therapy and relapses of VVC are more and more common. Hypothetically, biofilm is one of the main reasons of relapses and failure of the therapy. Ultrashort cationic lipopeptides (USCLs) exhibit high antimicrobial activities. Our previous study on USCLs revealed that disulfide cyclization can result in selective antifungal compounds. Therefore, four USCL were selected and their antifungal activity were studied on 62 clinical strains isolated from VVC. The results confirmed previous premises that cyclic analogs have increased selectivity between fungal cells and keratinocytes and improved anticandidal activity compared to their linear analogs against both planktonic and biofilm cultures. On the other hand, linear lipopeptides in combination with fluconazole showed a synergistic effect. It was found that the minimum inhibitory concentrations of the tested compounds in combination with fluconazole were at least four times lower than when used separately. Our results indicate that combination therapy of VVC with USCLs and fluconazole at low non-toxic concentrations can be beneficial owing to the synergistic effect. However, further in vivo studies are needed to confirm this hypothesis.

scholarly journals Prospects of honey in fighting against COVID-19: pharmacological insights and therapeutic promises

2020 ◽  
Author(s):  
Khandkar Shaharina Hossain ◽  
Md. Golzar Hossain ◽  
Akhi Moni ◽  
Mahbubur Rahman ◽  
Umma Habiba Rahman ◽  
...  
Keyword(s):  
Immune System ◽  
Chronic Diseases ◽  
Fungal Infections ◽  
Antimicrobial Activities ◽  
In Vivo Studies ◽  
Therapeutic Effects ◽  
Host Immune System ◽  
Varicella Zoster

Honey and its various ingredients have been in limelight as an effective natural therapy capable of normalizing the situation by attenuating acute inflammation through encouraging immune response. Several studies have proved its potential healing capability against numerous chronic diseases/conditions, including pulmonary disorders, cardiac disorders, diabetes, hypertension, autophagy dysfunction, bacterial and fungal infections. More importantly, honey showed its virucidal effect on several enveloped viruses such as HIV, influenza virus, herpes simplex, and varicella zoster virus. Honey may be beneficial for patients with COVID-19 caused by an enveloped virus SARS-CoV-2 through simultaneously boosting the host immune system, improving comorbid conditions and antiviral activities. Moreover, a clinical trial of honey on COVID-19 patients has been undergoing. In this review, we summarized the potential benefits of honey and its ingredients in the context of antimicrobial activities, numerous chronic diseases, and host immune system and thereby tried to establish a relationship with honey for the treatment of COVID-19. This review will be helpful to reconsider the insights into the possible potential therapeutic effects of honey in the context of COVID-19 pandemic. However, the effects of honey on SARS-CoV-2 replication and/or host immune system need to be further investigated by in vitro and in vivo studies.

Efficacy of Novel Schiff base Derivatives as Antifungal Compounds in Combination with Approved Drugs Against Candida Albicans

2019 ◽  
Vol 15 (6) ◽  
pp. 648-658 ◽  
Author(s):  
Manzoor Ahmad Malik ◽  
Shabir Ahmad Lone ◽  
Parveez Gull ◽  
Ovas Ahmad Dar ◽  
Mohmmad Younus Wani ◽  
...  
Keyword(s):  
Schiff Base ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Fungal Infections ◽  
Total Sterol ◽  
Antifungal Drugs ◽  
New Drugs ◽  
Ergosterol Biosynthesis ◽  
Dependent Manner ◽  
Schiff Base Derivatives

Background: The increasing incidence of fungal infections, especially caused by Candida albicans, and their increasing drug resistance has drastically increased in recent years. Therefore, not only new drugs but also alternative treatment strategies are promptly required. Methods: We previously reported on the synergistic interaction of some azole and non-azole compounds with fluconazole for combination antifungal therapy. In this study, we synthesized some non-azole Schiff-base derivatives and evaluated their antifungal activity profile alone and in combination with the most commonly used antifungal drugs- fluconazole (FLC) and amphotericin B (AmB) against four drug susceptible, three FLC resistant and three AmB resistant clinically isolated Candida albicans strains. To further analyze the mechanism of antifungal action of these compounds, we quantified total sterol contents in FLC-susceptible and resistant C. albicans isolates. Results: A pyrimidine ring-containing derivative SB5 showed the most potent antifungal activity against all the tested strains. After combining these compounds with FLC and AmB, 76% combinations were either synergistic or additive while as the rest of the combinations were indifferent. Interestingly, none of the combinations was antagonistic, either with FLC or AmB. Results interpreted from fractional inhibitory concentration index (FICI) and isobolograms revealed 4-10-fold reduction in MIC values for synergistic combinations. These compounds also inhibit ergosterol biosynthesis in a concentration-dependent manner, supported by the results from docking studies. Conclusion: The results of the studies conducted advocate the potential of these compounds as new antifungal drugs. However, further studies are required to understand the other mechanisms and in vivo efficacy and toxicity of these compounds.

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