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1.
J Pak Med Assoc ; 69(1): 18-23, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30623906

RESUMO

OBJECTIVE: To attempt discovering new bioactive metabolites from fungal sources. METHODS: The exploratory study was conducted at the Department of Microbiology, Federal Urdu University for Arts, Science and Technology, Karachi from January 2016 to November 2017and comprised of soil samples collected from rhizosphere region of different garden plants from the city. Fungi were screened for production of antibiotics by testing cell-free culture filtrates obtained by Shake-flask fermentation technique. Agar-Well diffusion assay method was used to evaluate antagonistic activity against pathogenic microorganisms. RESULTS: Bioactive compounds extracted by ethyl acetate and thin layer chromatography revealed mixture of compounds in the crude extract. AspergillusterreusMK-1 showed significant inhibition of medically important test pathogens namely Staphylococcus aureus, Pseudomonas aeruginosa, Escherichiacoli, Salmonella typhi, Micrococcus luteus, Streptococcus epidermidis, Bacillus subtilis, Candida albicans and Aspergillusniger. The best biological activity of crude ethyl acetate extract was observed against Pseudomonas aeruginosa (63mm). CONCLUSIONS: Newly isolated AspergillusterreusMK-1 emerged as a potent candidate for the production of antimicrobial compounds.


Assuntos
Anti-Infecciosos/farmacologia , Aspergillus/fisiologia , Composição de Medicamentos/métodos , Descoberta de Drogas/métodos , Fungos , Microbiologia do Solo , Aspergillus/isolamento & purificação , Bactérias/classificação , Bactérias/isolamento & purificação , Biofarmácia/métodos , Cromatografia/métodos , Fungos/classificação , Fungos/isolamento & purificação , Humanos
2.
Chem Biodivers ; 14(10)2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28672060

RESUMO

Evaluation of phytochemical constituents and antioxidant and antimicrobial activities of hexane (PELH), dichloromethane (PELDCM), ethyl acetate (PELEA), and MeOH (PELM) extracts of young leaves of Pseudocalymma elegans have been carried out. Moreover, extracts have also been explored for the presence of sulphur containing compounds, 1,2-dithiolane (33), diallyl disulfide (35), 3-vinyl-1,2-dithiacyclohex-5-ene (37), and diallyl trisulfide (38) responsible for the garlic like smell of P. elegans. All the extracts were found to be antioxidant and showed potent inhibition with IC50 values of 0.168 ± 0.001, 0.128 ± 0.002, 0.221 ± 0.011, and 0.054 ± 0.001, respectively, as compared to standard drugs ascorbic acid (AA) and butylated hydroxytoluene (BHT). The ethyl acetate extract (PELE) showed excellent activities against few Gram-positive and Gram-negative bacteria and some fungi as compared with standard drug ceftriaxone (3rd generation cephalosporin) and nystatin, respectively. Chemical constituents of hexane, dichloromethane, and ethyl acetate extracts were identified by gas chromatography-mass spectrometry and mass spectral library search. Over all 55 chemical constituents were first time identified from the leaves which included branched and n-hydrocarbons, fatty acids, fatty acid methyl esters, fatty alcohols, terpenes, alkaloid, vitamins, glycosides, aromatic compounds, and sulfur containing compounds. Two known chemical constituents, ursolic acid (1) and ß-amyrin (2), were also purified for the first time from the MeOH extract. To elucidate the structures of these compounds, UV, IR, EI-MS, 1 H- and 13 C-NMR spectroscopy were used.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antioxidantes/farmacologia , Magnoliopsida/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antifúngicos/química , Antifúngicos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Relação Dose-Resposta a Droga , Fungos/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Conformação Molecular , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Relação Estrutura-Atividade
3.
Med Chem ; 2016 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-27917708

RESUMO

: Background: Pathogenic microbial diseases are now the key virulence in our daily life. Significant research has been carried out in order to trigger the bacterial infections. Amongst the organic molecules, oxazolone and derivatives were found to have excellent bioactivities including antimicrobial activities. METHODS: By keeping in mind the considerable antimicrobial activities of class benzoxazolones, a series of benzoxazolone derivatives 3-16 have been synthesized. Out of which five compounds 10, 11, 14, 15, and 16 were new synthetic derivatives whereas compounds 9, 12, and 13 were already known compounds. These compounds have been synthesized by refluxing of amino phenol and 1,1-carbonyldiimidazole1 (C3H3N2)2CO) (CDI) in a dry THF and then treated with commercially available acid chloride. The structures of the compounds were elucidated on the basis of 1H-NMR, EIMS and elemental analysis. All the compounds were screened for their antibacterial activities and tested by agar well diffusion method. RESULTS: Compounds 14 and 16 showed good activity against S. aureus. Compound 5 showed good while 14 and 16 were found to be most active against E. coli using cefuroxime as a standard. Antifungal activities were carried out by using standard drug nystatin and compounds 4, 5, 9, 11 and compound 12 were found to be active against C. albicans. Compounds 4, 5, 9 and compound 10 showed good while 7, 11, and compound 13 showed excellent activities against Chrysosporium sp. Compounds 6, 7 and compound 12 were found to be most active against A niger and A. flavus, respectively. CONCLUSION: A number of derivatives were identified to have potent antimicrobial activities and may serve as lead compounds for future research.

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