-
Journal of Infection and Public Health Apr 2021This work is development of new molecules of isoniazid derivatives as dealing with potential of antimicrobial activity against clinical pathogens causing infectious...
BACKGROUND
This work is development of new molecules of isoniazid derivatives as dealing with potential of antimicrobial activity against clinical pathogens causing infectious disease. Antimicrobial of novel Mannich base derivatives can be achieved via one-pot synthesis in green chemistry approach. This method offers efficient, mild reaction conditions and high yields. In this study, totally 12 compounds (1a-l) was prepared and screened for cytotoxic and antimicrobial activities.
MATERIALS AND METHODS
Newly synthesised compounds were conformed via FT- IR, H, and C NMR (Nuclear Magnetic Resonance), and mass spectra analysis. All compounds were checked antibacterial activity against gram-positive bacteria of Enterococcus faecalis, Staphylococcus aureus and gram-negative bacteria of Pseudomonas aeruginosa, Klebsiella pneumoniae and Escherichia coli. All compounds were checked against antifungal activity against Aspergillus fumigatus, Candida albicans, Cryptococcus neoformans, Aspergillus niger, and Microsporum audouinii. All compounds were screened for cytotoxic activity against the MCF-7 (Michigan Cancer Foundation-7) cancer cell line.
RESULT
The compound 1g was highly (MIC: 0.25 μg/mL) active against gram-negative bacterial of P. aeruginosa, whereas other compounds 1e and 1h were more active (MIC: 2 μg/mL) in K. pneumoniae and also 1g (MIC: 2 μg/mL) was more active in E. faecalis than standard ciprofloxacin. Antifungal screening, the compound 1b was highly active (MIC: 0.25 μg/mL) against C. albicance,1g (MIC: 2 μg/mL) and 1h (MIC: 4 μg/mL) was significant of active against A. fumigatus, and the compound 1c (MIC: 4 μg/mL) was extremely active in M. audouinii than clotrimazole. Compound 1g (GI = 0.01 μM) exhibited high activity against the MCF-7 cell line, while 1b (GI = 0.02 μM) was equipotent active compared with standard doxorubicin.
CONCLUSION
A novel set of isoniazid derivatives (1a-l) and 1h were synthesized and screened for antimicrobial and cytotoxic activities. We found some highly active molecules, which are evidencing to be a potential treatment of bacterial and fungal infection candidates.
Topics: Anti-Infective Agents; Communicable Diseases; Fungi; Gram-Negative Bacteria; Gram-Positive Bacteria; Humans; Isoniazid; Menthol; Microbial Sensitivity Tests; Microsporum; Structure-Activity Relationship
PubMed: 33744741
DOI: 10.1016/j.jiph.2020.12.033 -
Saudi Journal of Biological Sciences Sep 2015Dermatophytes are a scientific label for a group of three genera (Microsporum, Epidermophyton and Trichophyton) of fungus that causes skin disease in animals and humans....
BACKGROUND
Dermatophytes are a scientific label for a group of three genera (Microsporum, Epidermophyton and Trichophyton) of fungus that causes skin disease in animals and humans. Conventional methods for identification of these fungi are rapid and simple but are not accurate comparing to molecular methods.
OBJECTIVE
This study aimed to isolate human pathogenic dermatophytes which cause dermatophytosis in Riyadh City, Saudi Arabia and to identify these fungi by using conventional and molecular methods.
METHODS
The study was conducted in Medical Complex, Riyadh and King Saud University. Samples of infected skin, hairs and nails were collected from 112 patients. Diagnosis of skin infections, direct microscopic test, isolation and identification of dermatophytes by conventional and molecular methods were carried out.
RESULTS
The results indicated that the tinea capitis infection had the highest prevalence among the patients (22.3%) while Tinea barbae had the lowest. In this study the identified dermatophyte isolates belong to nine species as Trichophyton violaceum, Trichophyton verrucosum, Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton schoenleinii, Trichophyton concentricum, Microsporum canis, Microsporum audouinii and Epidermophyton floccosum which cause skin infections were isolated during this study. Non dermatophyte isolates included 5 isolates from Aspergillus spp. 4 isolates from Acremonium potronii and 15 isolates from Candida spp. M. canis were the most common species (25% of isolated dermatophytes). Out of the 52 dermatophyte isolates identified by conventional methods, there were 45 isolates identified by the molecular method.
CONCLUSIONS
The results concluded that approximately M. canis caused a quarter of dermatophyte cases, tinea capitis infection was prevalent and the molecular method was more accurate than conventional methods.
PubMed: 26288566
DOI: 10.1016/j.sjbs.2014.12.006 -
Journal of Clinical Microbiology Oct 2007Species of dermatophytes are classified into three anamorphic (asexual) genera, Epidermophyton, Microsporum, and Trichophyton. Conventional methods used to identify...
Species of dermatophytes are classified into three anamorphic (asexual) genera, Epidermophyton, Microsporum, and Trichophyton. Conventional methods used to identify dermatophytes are often lengthy and may be inconclusive because of atypical microscopic or colony morphology. Based on the internal transcribed spacer 1 (ITS-1) and ITS-2 sequences of the rRNA genes, an oligonucleotide array was developed to identify 17 dermatophyte species. The method consisted of PCR amplification of the ITS regions using universal primers, followed by hybridization of the digoxigenin-labeled PCR products to an array of oligonucleotides (17- to 30-mers) immobilized on a nylon membrane. Of 198 dermatophyte strains and 90 nontarget strains tested, the sensitivity and specificity of the array were 99.5% and 97.8%, respectively. The only strain not identified (Microsporum audouinii LMA 597) was found to have a nucleotide insertion at the ITS-2 region where the probe was designed. Two nontarget strains, Microsporum equinum LMA 40396666 and Trichophyton gourvilii var. intermedium CBS 170.65, were misidentified as Microsporum canis and Trichophyton soudanense, respectively. Sequence analysis of the ITS regions revealed that the two misidentified strains displayed high sequence homology with the probes designed for M. canis and T. soudanense, respectively. The present method can be used as a reliable alternative to conventional identification methods and can be completed with isolated colonies within 24 h.
Topics: Arthrodermataceae; DNA, Ribosomal Spacer; Humans; Oligonucleotide Array Sequence Analysis; Oligonucleotide Probes; Sensitivity and Specificity
PubMed: 17687010
DOI: 10.1128/JCM.00829-07 -
Indian Journal of Dermatology 2018The incidence of dermatophytosis is increasing over the last few years and there are many cases which are recurrent and chronic.
BACKGROUND
The incidence of dermatophytosis is increasing over the last few years and there are many cases which are recurrent and chronic.
AIM
The aim was to study the host and pathogen factors in dermatophytosis, to identify the species responsible, and to study the histopathological features of chronic dermatophytosis.
MATERIALS AND METHODS
It was a descriptive study conducted in the Department of Dermatology for a period of 1 year and all patients who were clinically diagnosed as dermatophytosis were included. Isolated hair, and nail involvement were excluded from the study. Epidemiological parameters and treatment history were analyzed, scrapings, and fungal culture were done in all patients. Histopathological examination was done in patients with chronic dermatophytosis who had applied topical steroids.
RESULTS
Chronic dermatophytosis was seen in 68%; tinea corporis was the most common presentation; topical steroid application was seen in 63%; azoles were the most common antifungals used; varied morphologies such as follicular and nonfollicular papules, arciform lesions, pseudoimbricata were seen in steroid modified tinea. and were the most common species isolated in culture, but rare species such as , , , and were also isolated from chronic cases. Histopathology showed perifolliculitis in steroid modified tinea. Minimal inhibitory concentration was lowest for itraconazole in susceptibility studies.
CONCLUSION
Chronicity in dermatophytosis is due to various factors such as topical steroid application, noncompliance, and change in predominant species.
PubMed: 30504978
DOI: 10.4103/ijd.IJD_177_18 -
Brazilian Journal of Microbiology :... Dec 2020Species identification of dermatophytes by conventional mycological methods based on macro- and microscopy analysis is time-consuming and has a lot of limitations such...
Species identification of dermatophytes by conventional mycological methods based on macro- and microscopy analysis is time-consuming and has a lot of limitations such as slow fungal growth or low specificity. Thus, there is a need for the development of molecular methods that would provide reliable and prompt identification of this group of medically important fungi. The are many reports in the literature concerning PCR identification of dermatophyte species, but still, there are not many PCR assays for the separate detection of members of the genera Microsporum, especially Microsporum canis (zoophilic species) and Microsporum audouinii (anthropophilic species). The correct distinction of these species is important to determine the source of infection to implement the appropriate action to eliminate the path of infection transmission. In this paper, we present such a PCR-based method targeting velB gene that uses a set of two primers-Mc-VelB-F (5'-CTTCCCCACCCGCAACATC-3') and Mc-VelB-R (5'-TGTGGCTGCACCTGAGAGTGG-3'). The amplified fragment is specific due to the presence of (CAGCAC) microsatellite sequence only in the velB gene of M. canis. DNA from 153 fungal samples was used in PCR assay followed by electrophoretic analysis. The specificity of the designed set of primers was also confirmed using the online BLAST-Primer tool. The positive results were observed only in the case of M. canis isolates, and no positive results were obtained neither for other dermatophytes and non-dermatophyte fungi nor for other Eukaryotes, including the human genome sequence, as well as the representatives of bacterial and viral taxa. The developed PCR assay using the proposed Mc-VelB-F and Mc-velB-R primers can be included in the algorithm of M. canis detection in animals and humans.
Topics: Animals; DNA, Fungal; Dermatomycoses; Fungal Proteins; Humans; Microsporum; Polymerase Chain Reaction; Sensitivity and Specificity
PubMed: 32696419
DOI: 10.1007/s42770-020-00340-y -
Drug Design, Development and Therapy 2020A new series of tetrazole derivatives, which are renowned antimicrobials possessing a five-membered aromatic heterocyclic group, are synthesized herein and subjected to...
PURPOSE
A new series of tetrazole derivatives, which are renowned antimicrobials possessing a five-membered aromatic heterocyclic group, are synthesized herein and subjected to antimicrobial and cytotoxicity screening.
METHODS
The tetrazole derivatives were synthesized via ultrasonication using Mannich base condensation. Structural verification of the products was performed using IR, H NMR, and C NMR spectroscopy, as well as mass spectroscopic and elemental analyses. The compounds were then screened for antimicrobial and cytotoxic activity against HepG2 (liver), MCF-7 (breast), and HeLa (cervical) cell lines. Inter- and intra-molecular binding interactions were determined using molecular docking studies. The exact binding mode between the most active tetrazole derivatives (ie, 1b, 2a, and 2b) and the proteins (ie, 4OR7, 1AI9, and 4FM9) was established using Autodock Vina 1.1.2 software and compared to the binding mode of the reference compounds (ie, cefazolin, clotrimazole, and fluorouracil).
RESULTS
Compound 1b was extremely active against relative to the positive control cefazolin. Compounds 1b and 1e were active against and compared to the positive control clotrimazole in antifungal screening. The HepG2 (liver) and MCF-7 (breast) cancer cell lines were particularly susceptible to the synthesized compounds. Compared to the control compound fluorouracil, 2a and 2b were extremely active against all three cancer cell lines. Molecular docking studies showed that 2b exhibited higher binding affinity (-7.8 kcal/mol) to the 4OR7 protein than the control cefazolin (-7.2 kcal/mol).
CONCLUSION
Generally, 1b, 2a, and 2b exhibited impressive inhibitory capabilities in antibacterial, antifungal, and cytotoxic screenings relative to the reference compounds. The results of the molecular docking studies and both the microbial and anticancer screenings indicate that these novel derivatives could be developed into potential therapeutic agents for medical applications.
Topics: Anti-Bacterial Agents; Antifungal Agents; Antineoplastic Agents; Bacteria; Cell Line, Tumor; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Fungi; Humans; Mannich Bases; Microbial Sensitivity Tests; Molecular Docking Simulation; Molecular Structure; Structure-Activity Relationship; Tetrazoles
PubMed: 33122891
DOI: 10.2147/DDDT.S270896 -
Journal of Clinical Microbiology Dec 2006This report describes application of PCR fingerprinting to identify common species of dermatophytes using the microsatellite primers M13, (GACA)4, and (GTG)5. The...
This report describes application of PCR fingerprinting to identify common species of dermatophytes using the microsatellite primers M13, (GACA)4, and (GTG)5. The initial PCR analysis rendered a specific DNA fragment for Microsporum audouinii, which was cloned and sequenced. Based on the sequencing data of this fragment, forward (MA_1F) and reverse (MA_1R) primers were designed and verified by PCR to establish their reliability in the diagnosis of M. audouinii. These primers produced a singular PCR band of 431 bp specific only to strains and isolates of M. audouinii, based on a global test of 182 strains/isolates belonging to 11 species of dermatophytes. These findings indicate these primers are reliable for diagnostic purposes, and we recommend their use in laboratory analysis.
Topics: Adolescent; Adult; DNA Primers; DNA, Fungal; Dermatomycoses; Female; Hair; Humans; Male; Microsatellite Repeats; Microsporum; Middle Aged; Nails; Polymerase Chain Reaction; Sensitivity and Specificity; Sequence Analysis, DNA; Skin; Tinea Capitis
PubMed: 17005755
DOI: 10.1128/JCM.00759-06 -
The Journal of Investigative Dermatology Apr 1957
Topics: Animals; Dog Diseases; Dogs; Microsporum; Tinea
PubMed: 13439223
DOI: 10.1038/jid.1957.39 -
Journal of Infection and Public Health Dec 2020This work is development of new hydantoin molecules as treatment of potential antibacterial and antifungal activity against clinical pathogens causing infectious...
Antimicrobial activity of novel 5-benzylidene-3-(3-phenylallylideneamino)imidazolidine-2,4-dione derivatives causing clinical pathogens: Synthesis and molecular docking studies.
BACKGROUND
This work is development of new hydantoin molecules as treatment of potential antibacterial and antifungal activity against clinical pathogens causing infectious disease. Synthesized compounds were evaluated in molecular docking studies, the most effective compound is used to dock against the targets of 1U1Z, and 1AI9 kinases, to evaluate its binding affinity, hoping to rationalize and obtain potent of antibacterial, antifungal agents.
MATERIAL AND METHOD
The FTIR, H &C NMR, and mass spectra were used to conform new molecules and their evaluation of antimicrobial activity. Gram-negative bacteria of Pseudomonas aeruginosa (ATCC-27853), Klebsiella pneumoniae (recultured) and Escherichia coli (ATCC-25922), and gram-positive bacteria of Enterococcus faecalis (recultured) and Staphylococcus aureus (ATCC-25923) were evaluated for all compounds. The in vitro antifungal activity was evaluated against Cryptococcus neoformans (recultured), Candida albicans (recultured), Aspergillus niger, Microsporum audouinii (recultured) and Aspergillus fumigatus (recultured) for all synthesized compounds.
RESULT
Antibacterial screening, we identified highly active antimicrobial agents for this study for example; gram-negative bacterial screening of 3g was highly (MIC: 0.25 μg/mL) active in contradiction of P. aeruginosa, whereas bacterial screening of 3e and 3h were more active (MIC: 2 μg/mL) in contradiction of K. pneumoniae and also 3g was more (MIC: 2 μg/mL) active in contradiction of E. faecalis than standard ciprofloxacin. Antifungal activity, the 3b was more active (MIC: 0.25 μg/mL) against C. albicance,3g (MIC: 2 μg/mL) and 3h (MIC: 4 μg/mL) were more potential of A. funigatus, and the compound 3c was highly (MIC: 4 μg/mL) active on M. audouinii than clotrimazole. Molecular docking studies also supported the new finding of potent antimicrobial agents, the compound 3g, 3b, and controls Ciprofloxacin, Clotrimazole were checked again proteins 1U1Z and 1AI9 by Autodock Vina program. The compound 3g was highest binding affinity (-8.4 kcal/mol) than ciprofloxacin (-8.2 kcal/mol) in 1U1Z protein and the compound 3b was highest binding affinity (-8.8 kcal/mol) than clotrimazole (-6.8 kcal/mol) in 1AI9 protein respectively.
CONCLUSION
A novel set of imidazolidine-2,4-dione compounds 3a-h have synthesized and characterized successfully. The screening of antimicrobial activity shows that all compounds possess antimicrobial activities. In addition, the objective of the study was succeeded with a few of the promising molecules, which are proving to be a potential treatment of bacterial infection candidates.
Topics: Anti-Bacterial Agents; Anti-Infective Agents; Antifungal Agents; Humans; Hydantoins; Imidazolidines; Microbial Sensitivity Tests; Microsporum; Molecular Docking Simulation; Molecular Structure
PubMed: 33289644
DOI: 10.1016/j.jiph.2020.09.017 -
Medical Mycology Journal 2013[corrected] Dermatophytes are common in both developed and developing countries, the species involved and the resulting clinical entities vary geographically.
BACKGROUND
[corrected] Dermatophytes are common in both developed and developing countries, the species involved and the resulting clinical entities vary geographically.
AIM OF STUDY
To determine public health importance of dermatophytes with special regard to the distribution of the zoophilic species among the examined human cases.
METHODS
Patient specimens (dermatophytosis-like lesions) were mycologically examined using direct microscopic and cultural examinations.
RESULTS
The overall dermatophyte infection rates among the examined patients (260) were 81.5% and 61.9% by direct microscopic and cultural examinations, respectively. A total of 161 dermatophyte isolates were obtained from culturally positive human specimens. The most common isolated species were Trichophyton violaceum (60, 37.3%) and Microsporum canis (46, 28.6%), followed by Trichophyton rubrum (20, 12.4%), Trichophyton tonsurans (16, 9.9%) and Trichophyton mentagrophytes (11, 6.8%). The less frequently isolated species were Trichophyton verrucosum (3, 1.9%), Epidermophyton floccosum (3, 1.9%), Microsporum gypseum (1, 0.6%) and Microsporum audouinii (1, 0.6%). The current study further revealed that out of 161 culturally positive patients, 61 (37.9%) had contact with pet animals, 6 (3.7%) had contact with farm animals, 7 (4.3%) had a history of rodent presence in or around their home and 87 (54%) had no contact with animals.
CONCLUSIONS AND RECOMMENDATIONS
Although the anthropophilic species dominated the aetiology of human dermatophytosis in present study, the zoophilic species represented nearly one third of the totally obtained isolates, with the most important organisms being M. canis, T.mentagrophytes var. mentagrophytes and T. verrucosum. These findings indicate the necessity of human beings taking appropriate control measures when they are in contact with animals.
Topics: Adolescent; Adult; Animals; Arthrodermataceae; Child; Egypt; Female; Humans; Male; Middle Aged; Tinea; Trichophyton; Zoonoses
PubMed: 23760076
DOI: 10.3314/mmj.54.123