scholarly journals Antifungal effects of 3-(4-Phenyl-thiazol-2-yl)-2-thioxo-2, 3-dihydro-1H-quinazolin-4-one against Aspergillus Species

2018 ◽  
Author(s):  
Desh D. Singh ◽  
V. K. Tiwari ◽  
Rambir Singh ◽  
G L Sharam ◽  
Rajesh Dabur

AbstractAspergillus infections have become an important health problem with the increasing number of patients. Available antifungal drugs are lack with their spectrum, toxic or immunosuppressive in nature, so that need to develop new compound with high efficacy. To evaluate antifungal efficacy of synthesized compound and to identify the protein profile of Aspergillus fumigatus treated with antifungal. Clinical isolates of A. fumigatus, A. flavus and A. niger were cultured and efficacy of compound were conducted by Disc Diffusion Assay (DDA), Microbroth Dilution Assay (MDA). Percent of spore germination inhibition assay (PSGI), Time kill analysis and toxicity assay. The culture filtrate containing secretory proteins was collected after 24 h growth and expression of downregulated proteins were identified. We developed a new and useful quinazoline derivatives expected to antifungal activity. The result of anti-Aspergillus evolution revealed that one of the 3-(4-Phenyl-thiazol-2-yl)-2-thioxo-2, 3-dihydro-1H-quinazolin-4-one (DDVKT4Q) exhibited appreciable activity. The potency of compound was found concentration of 3.125 µg/disc by disc diffusion assay (DDA) and 15.625 µg/ml. by Microbroth Dilution Assay (MDA). The compound was nontoxic up to concentration 625 µg/ml and its lysed only 35.9% of human erythrocytes, at the highest dose tested. It’s observed that the treatment of pathogen with DDVKT-4Q targeted the expression of four proteins having molecular weights 18 kDa 37 KDa and 43 KDa proteins was completely inhibited or down regulated by the compound the extra cellular. The novel compound DDVKT-4Q, having antifungal activity Can be exploited further to develop new ideal antimycotic drugs.

2018 ◽  
Vol 102 (12) ◽  
pp. 1629-1633 ◽  
Author(s):  
Bhupesh Bagga ◽  
Savitri Sharma ◽  
Sai Jeevan Madhuri Guda ◽  
Ritu Nagpal ◽  
Joveeta Joseph ◽  
...  

BackgroundPythium insidiosum is a parafungus that causes keratitis resembling fungal keratitis. This study compares outcome in a large cohort of patients with P insidiosum keratitis treated with antifungal drugs, to a pilot group treated with antibacterial antibiotics.MethodsBetween January 2014 and December 2016, 114 patients with culture positive P insidiosum keratitis were included in the study. A subset of culture isolates was tested in vitro for response to nine antibacterial antibiotics by disc diffusion and E test. Patients were treated with topical natamycin in 2014, 2015 and up until mid 2016. Thereafter, the patients received a combination of topical linezolid and topical and oral azithromycin. Therapeutic penetrating keratoplasty (TPK) was done for patients not responding to medical therapy.ResultsIn vitro disc diffusion assay showed linezolid to be most effective. The rate of TPK was significantly higher in 2015 compared with 2016 (43/45, 95.6% vs 22/32, 68.8%; p=0.002). Eighteen patients were treated with antibacterial and 14 were treated with antifungal antibiotic in 2016. One patient was lost to follow-up in each group. The rate of TPK was higher and proportion of healed ulcers was lower (p=0.21, Fisher’s exact test) in the group on antifungal therapy (TPK—11/13, 84.6%; Healed—2/13, 15.3%) compared with the group on antibacterial therapy (TPK—11/17, 64.7%; Healed—6/17, 35.2%).ConclusionsWe report favourable but not statistically significant response of P insidiosum keratitis to antibacterial agents in a pilot series of patients. Further evaluation of this strategy in larger number of patients is recommended.


2020 ◽  
Vol 32 (7) ◽  
pp. 1788-1792
Author(s):  
Thurdpong Sribuhom ◽  
Yordhathai Thongsri ◽  
Chavi Yenjai

Chemical investigation of Dalbergia cultrata Grah. stems growing in Thailand resulted in the isolation and characterization of 14 known compounds, including tectorigenin (1), calycosin (2), pratensein (3), afromosin (4), irilin D (5), biochanin A (6), daidzein (7), formononetin (8), 8-O-methylretusin (9), 7,3′-dihydroxy-5′-methoxyisoflavone (10), (3S)-sativanone (11), (3S)-violanone (12), erycibenin D (13) and isoliquiritigenin (14). Their structures were established mainly based on NMR spectroscopic techniques and physical properties. The isolated compounds were evaluated for antifungal activity against Pythium insidiosum using disc diffusion assay. Antifungal drugs available now are not effective to treat this microorganism. It was found that compound 1 exhibited stronger antifungal activity than amphotericin-B standard with an MIC value of 10 μg/disc.


Author(s):  
Mrridula Dangi Narwal ◽  
Meenakshi Balhara ◽  
Renu Chaudhary ◽  
Anil Kumar Chhillar

Objective: The prevalence of invasive mycoses is increased in the immunocompromised patients with an increase in resistance developed againstcurrent antifungal drugs. This has led to the need for discovering novel combinations of the antifungal drugs to combat against resistant pathogenic spp.This study mainly targets to evaluate the antifungal activity of ibuprofen (IBU) alone and in combination with the standard antifungal drugs (polyenesand azoles) against eight isolates of Aspergillus fumigatus, Aspergillus flavus, and Aspergillus niger.Methods: The study was performed using the disc diffusion assay (DDA), microbroth dilution assay and spore germination inhibition assay. Moreover,cytotoxicity was checked by heamolytic assay.Results: Minimum inhibitory concentration (MIC) of IBU against A. fumigatus and A. flavus using DDA is found to be in the range of 250-275 μg/disc while for A. niger isolates, the range was 500-575 μg/disc. Likewise, by broth microdilution assay and spore germination inhibitory assay, MICdetermined, were in the range of 500-750 μg/ml against A. fumigatus and A. flavus while for A. niger, it was 1000-1500 μg/ml.Conclusion: IBU demonstrated its antimycotic potential against all the eight isolates of Aspergillus spp. Moreover, preliminary combinatorialevaluation of IBU with the standard antifungal drugs reported by DDA revealed an increase in zone of inhibition as compared to the drugs alone.Further research regarding the confirmation of synergistic interaction between the selected drugs is in progress.


Author(s):  
Nilofer Noorie M. ◽  
Chenthamarai G.

Background: In this study objectives were to evaluate the antifungal activity in increasing concentrations of ethanolic extract and aqueous extract of Carica papaya against Candida albicans and to assess the synergistic activity of ethanolic extract of Caricia papaya with flucanazole as a potential antifungal.Methods: The aim of the study was to evaluate the antifungal activity in increasing concentrations, 500 µl/ml, 750 µl/ml and 1000 µl/ml of ethanolic extract and aqueous extract of caricia papaya against Candida albicans and the synergistic activity with Fluconazole was assessed by observing the zone of inhibition in agar disc diffusion assay and by observing the turbidity in minimum inhibitory concentration (MIC) assay.Results: It was observed that ethanolic extract of Carica papaya leaf showed significant antifungal activity in higher concentration of 1000µg/ml with zone diameter of 11.97±0.15 mm in disc diffusion assay and MIC of 350 µg/ml. The ethanolic extract of Carica papaya leaf with fluconazole showed synergistic activity with zone diameter of 13.6±0.45 mm in disc diffusion assay and MIC was 125µg/ml, whereas the standard drug Fluconazole’s zone of inhibiton was 12.83±0.9 in disc diffusion and MIC was 500 µg/ml.Conclusions: From this study, we can safely conclude that the Carica papaya leaf extract has a significant antifungal property and exhibit synergistic effect when used with fluconazole.


2021 ◽  
Vol 22 (14) ◽  
pp. 7715
Author(s):  
Grzegorz Czernel ◽  
Dominika Bloch ◽  
Arkadiusz Matwijczuk ◽  
Jolanta Cieśla ◽  
Monika Kędzierska-Matysek ◽  
...  

Silver nanoparticles (AgNPs) were synthesized using aqueous honey solutions with a concentration of 2%, 10%, and 20%—AgNPs-H2, AgNPs-H10, and AgNPs-H20. The reaction was conducted at 35 °C and 70 °C. Additionally, nanoparticles obtained with the citrate method (AgNPs-C), while amphotericin B (AmB) and fluconazole were used as controls. The presence and physicochemical properties of AgNPs was affirmed by analyzing the sample with ultraviolet–visible (UV–Vis) and fluorescence spectroscopy, scanning electron microscopy (SEM), and dynamic light scattering (DLS). The 20% honey solution caused an inhibition of the synthesis of nanoparticles at 35 °C. The antifungal activity of the AgNPs was evaluated using opportunistic human fungal pathogens Candida albicans and Candida parapsilosis. The antifungal effect was determined by the minimum inhibitory concentration (MIC) and disc diffusion assay. The highest activity in the MIC tests was observed in the AgNPs-H2 variant. AgNPs-H10 and AgNPs-H20 showed no activity or even stimulated fungal growth. The results of the Kirby–Bauer disc diffusion susceptibility test for C. parapsilosis strains indicated stronger antifungal activity of AgNPs-H than fluconazole. The study demonstrated that the antifungal activity of AgNPs is closely related to the concentration of honey used for the synthesis thereof.


2019 ◽  
Vol 2019 ◽  
pp. 1-10
Author(s):  
Mashooq Ahmad Bhat ◽  
Mohamed A. Al-Omar ◽  
Ahmed M. Naglah ◽  
Abdul Arif Khan

A series of pyrazoles derived from the substituted enaminones were synthesized and were evaluated for antimicrobial activity. All the compounds were characterized by the spectral data and elemental analysis. The synthesized compounds were initially screened for their antimicrobial activity against ATCC 6538, NCTC 10400, NCTC 10418, and ATCC 27853. During initial screening, compounds (P1, P6, and P11) presented significant antimicrobial activity through disc diffusion assay. These compounds were further evaluated for antimicrobial activity at different time points against Gram-positive and Gram-negative bacteria and presented significant activity for 6 hours. The activity was found to be greater against Gram-positive bacteria. In contrast at 24 hours, the activity was found only against Gram-positive bacteria except compound (P11), showing activity against both types of bacteria. Compound (P11) was found to have highest activity against both Gram-positive and Gram-negative bacteria.


2007 ◽  
Vol 61 (1) ◽  
pp. 135-138 ◽  
Author(s):  
E. Canton ◽  
J. Peman ◽  
A. Espinel-Ingroff ◽  
E. Martin-Mazuelos ◽  
A. Carrillo-Munoz ◽  
...  

2011 ◽  
Vol 24 (1) ◽  
pp. 7-13 ◽  
Author(s):  
Sukolrat Boonyayatra ◽  
Lawrence K. Fox ◽  
John M. Gay ◽  
Ashish Sawant ◽  
Thomas E. Besser

Microbiological culture of milk samples has been used as a standard diagnosis for Mycoplasma mastitis. This technique is effective in isolating mollicutes that are Mycoplasma-like; however, isolates may be misinterpreted as Acholeplasma species, which are indistinguishable from Mycoplasma species by culture. A study to contrast the abilities of 2 culture-based tests, digitonin and nisin disc diffusion assays and a conventional polymerase chain reaction (PCR) technique, to discriminate between Mycoplasma and Acholeplasma was performed using 16S ribosomal RNA gene partial sequencing as the gold standard of comparison. A total of 288 bovine mollicute field isolates (248 from milk and 40 from other organ sites) and 13 reference strains were tested. Results obtained from the digitonin disc diffusion assay when it was performed with all field isolates were 92.7% and 99.0% in agreement with the gold standard using 5 mm and 3 mm of zone of growth inhibition as thresholds, respectively. Considering only milk isolates, agreements between the digitonin disc diffusion assay with the gold standard were 97.2% and 100% using 5 mm and 3 mm of zone of growth inhibition as thresholds, respectively. Culture identification using the nisin disc diffusion assay and the PCR was in a 100% agreement with the gold standard. Comparable results using culture-based nisin and digitonin disc diffusion assays, and PCR, to distinguish Mycoplasma and Acholeplasma species was found, especially for isolates from bovine milk.


Author(s):  
Okoro, Chisom Augusta ◽  
Onaebi, Chiemeka Nwakaego

Aim: Soil-borne diseases are difficult to control because they are caused by pathogens that can survive for long periods in the absence of the normal crop host and often have a wide host range including weeds. This present study was design to assess the antifungal assay dependent effect of methanolic extracts of Hyptis suaveolens and Moringa oleifera on Phytophthora colocasiae and Fusarium oxysporum. Methods: The presence of biologically active ingredients (alkaloid, saponin, tannins, flavonoid, terpenoids, tannins, steroids, hydrogen cyanides, phenols and glycoside) in the leaf extracts was investigated using standard procedures. The antifungal activities of the plant extract were tested against Phytophthora colocasiae and Fusarium oxysporum using disc and well diffusion assays. Results: The results of the phytochemical evaluated showed that H. suaveolens, contained significantly higher alkaloids, saponins, hydrogen cyanide, flavonoids and phenols than M. oleifera, while on the other hand, M. oleifera contained significantly higher terpenoids, tannins, steroids and glycosides. Consequently, H. suaveolens extract similarly recorded significantly (P < 0.05) higher inhibition on the organisms as compared to M. oleifera. The disc diffusion assay method was more sensitive than the well diffusion assay. H. suaveolens at 100 mg/ml using disc diffusion assay method showed higher inhibition on both P. colocasiae and F. oxysporum. While M. oleifera recorded higher inhibition on F. oxysporum at 50 mg/ml and P. colocasiae at 100 mg/ml using the disc diffusion assay method. MIC was lowest with H. suaveolens (12.5 mg/ml) against F. oxysporum. Conclusion: These results promote the identification of actives substances from these plants for use as lead molecules in the development of new fungicides for the control of Phytophthora colocasiae and Fusarium oxysporum.


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