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1.
Pak J Pharm Sci ; 36(3(Special)): 927-934, 2023 May.
Article in English | MEDLINE | ID: mdl-37587700

ABSTRACT

Aspergillus fumigatus is a green echinulate with greenish phialides and 2.5-3 mm conidia. The diverse biological functions of A. fumigatus secondary metabolites make them interesting. The ethyl acetate extract of A. fumigatus was tested for antibacterial activity. Culture media, temperature, incubation and pH were optimized for A. fumigatus growth. Continuous 150rpm agitation incubated the fungus at 28°C for 10 days. Potato Dextrose Broth at 28°C in shaking incubator at pH 04 produced the most biomass and secondary metabolites. Metabolite antibacterial activity was tested. Salmonella flexneri had the greatest zone of inhibition at 100µl (25.66mm) while Staphylococcus aureus had the least (16.33mm). At 75µg/mL, S. flexneri showed 23.66mm activity and S. typhi 14.66mm. At 50µg/mL, S. flexneri was 21.33mm and S. typhi 12.33mmMBC was 0.01µg/µl and MIC50 varied. At 100µg/mL, the metabolites showed antifungal efficacy against Penicillium chrysogenum (26.33mm) but not A. flavus (21.33mm). A. oryzae was significantly inhibited at 75µg/mL (26.33mm) and 50µg/mL (20.33mm). 1000µl demonstrated 100% phytotoxicity, 100µl 60% and 10µl 50%. Bactrocera cucurbitae, Sitotroga cerealella and Callosobruchus maculatus were killed at 150, 100 and 75µl. Metabolites and antibiotics synergized well. Metabolites have alkanes, esters and ethers in their infrared spectra.


Subject(s)
Alkanes , Aspergillus fumigatus , Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Biomass
2.
Pak J Pharm Sci ; 36(3(Special)): 969-972, 2023 May.
Article in English | MEDLINE | ID: mdl-37587706

ABSTRACT

Probiotic bacteria have capacity to bind with heavy metals. The present study was planned to assess the bioremediation potential of probiotic Lactobacillus species isolated from yogurt samples. L. acidophilus and L. plantarum were tested for acidic pH tolerance, bile salt resistance and gastric juice tolerance. The antibiotic susceptibility and antimicrobial activity was also checked. These Lactobacillus species were also evaluated for degradation of lead (Pb) and cadmium (Cd) metals. The results indicated that L. acidophilus and L. plantarum were able to tolerate high acidic pH: 3. both showed significant growth after exposure to stimulated gastric juice from 0 to 24 hours. The significant plate count was observed at different bile salt concentrations (0.1%, 0.3%). The isolates showed resistance for all the tested antibiotics except L. acidophilus showed susceptibility for gentamicin and co-amoxiclave. The isolates depicted no antimicrobial activity against the indicator bacteria. L. acidophilus and L. plantarum were capable of tolerating Cd and Pb. Maximum tolerance and removal were observed for Pb by both Lactobacillus spp. The Cd removal was 11.50 and 3.50% while Pb removal was 42.70 and 35.50% for L. plantarum and L. acidophilus, respectively. In conclusion, L. acidophilus and L. Plantarum have potential for bioremediation of heavy metals.


Subject(s)
Cadmium , Probiotics , Biodegradation, Environmental , Lead , Yogurt , Lactobacillus acidophilus , Lactobacillus , Anti-Bacterial Agents/pharmacology , Bile Acids and Salts
3.
Heliyon ; 7(3): e06464, 2021 Mar.
Article in English | MEDLINE | ID: mdl-33842699

ABSTRACT

Drug design is an integrated and developing system that portends an era of a novel and safe tailored drugs. It involves studying the effects of biologically active synthetic, semi-synthetic, and natural compounds based on molecular interactions in terms of molecular structure with activated functional groups or its unique physicochemical properties involved. The title compound, N-(2-aminophenyl)-2-(4-bromophenoxy) acetamide (c), was synthesized in a good yield and characterized by different spectroscopic techniques (1H, 13CNMR, and LC-MS) and finally, the structure was confirmed by X-ray diffraction (XRD) studies. The XRD data confirms that the cryatal structure is orthorhombic with space group of Pca2 1 . The intermolecular interactions (N-H … O and N-H … Cg) inside the molecule stabilizes the crystal structure. The existence of this intermolecular interactions are computed by the Hirshfeld surfaces (HS) and two-dimensional (2D) fingerprints plot analysis. In addition to this, Energy frame work analysis is performed to quantify the interaction energies between the molecular pairs in a crystal by incorporating new version of CrystalExplorer17 using the energy model of HF/3-21G. Also to calculate the HOMO and LUMO energies, DFT calculations were carried out.

4.
Microb Pathog ; 123: 275-284, 2018 Oct.
Article in English | MEDLINE | ID: mdl-30041001

ABSTRACT

Bacterial adhesion is a threshold event in the formation of biofilms which leads to serious bacterial diseases. This shows that the underlining the problem is interesting and need to solve the problem of biofilm-related complications. To support this, in the present study, we first time initiated to understand the role of methicillin-resistant Staphylococcus aureus (MRSA) biofilm using previously developed benzodioxane midst piperazine decorated chitosan silver nanoparticles (BP*C@AgNPs). The BP*C@AgNPs studied for antimicrobial, anti-biofilm, biofilm adherence inhibition, the role of ions in biofilm, and an antibiotic cocktail in the treatment of biofilm was assessed. The results showed that, the significant biocidal role of BP*C@AgNPs in controlling the MRSA biofilm and interaction of biofilm protein to calcium ions were significantly decreased. This confirms that calcium ion involved in the biofilm formation and for the treatment of BP*C@AgNPs, cocktail of enzyme and antibiotic have the promising therapeutic value was observed. In future the locking of biofilm protein and its expression in presence of calcium ion was interesting, and greater application related to biofilm infection was warrantable.


Subject(s)
Biofilms/drug effects , Metal Nanoparticles/chemistry , Methicillin-Resistant Staphylococcus aureus/drug effects , Silver/pharmacology , Amino Acid Sequence , Anti-Bacterial Agents/pharmacology , Anti-Infective Agents/pharmacology , Bacterial Adhesion/drug effects , Benzodioxoles , Binding Sites , Calcium/metabolism , Chitosan , Drug Combinations , Endopeptidase K/pharmacology , Heterocyclic Compounds, 2-Ring/chemistry , Heterocyclic Compounds, 2-Ring/pharmacology , Microbial Sensitivity Tests , Staphylococcal Infections/microbiology , Virulence/drug effects
5.
Biomed Pharmacother ; 95: 375-386, 2017 Nov.
Article in English | MEDLINE | ID: mdl-28858736

ABSTRACT

Neoplastic metastasis is a major process where tumor cells migrate from the primary tumor and colonize at other parts of our body to form secondary tumor. Cancer incidences are rising and novel anti-neoplastic compounds with new mechanism of actions are essential for preventing cancer related deaths. In the current examination, a novel series of pyridazine analogues 6a-l was synthesized and evaluated against metastatic neoplastic cells. Experimental data postulated compound 6j has potential cytotoxic efficacy with prolonged activity against various cancer cells, including A549, HepG2, A498, CaSki and SiHa cells. Moreover, compound 6j arrests the A549 migration and invasions markedly by counteracting matrix metalloproteinase (MMP)-2 and MMP-9 expressions. Also, compound 6j proved its potentiality against Dalton's solid lymphoma progression in-vivo by abridging MVD and MMP expressions. Compound 6j interacts with MMP-2 and MMP-9 by H- bond in-silico, thereby down regulates the MMPs action in tumourigenesis. Altogether, we concluded that compound 6j down regulates MMP-2 and MMP-9 and thereby impairs metastatic cancer cell migration and invasions which can be translated into a potent anti-neoplastic agent.


Subject(s)
Carcinogenesis/pathology , Hydrazines/chemical synthesis , Hydrazines/therapeutic use , Matrix Metalloproteinases/metabolism , Phenoxyacetates/chemistry , Pyridazines/chemical synthesis , Pyridazines/therapeutic use , Animals , Cell Line, Tumor , Cell Movement/drug effects , Computer Simulation , Down-Regulation/drug effects , Humans , Hydrazines/chemistry , Hydrazines/pharmacology , Inhibitory Concentration 50 , Male , Mice , Microvessels/drug effects , Microvessels/pathology , Models, Molecular , NIH 3T3 Cells , Neoplasm Invasiveness , Pyridazines/chemistry , Pyridazines/pharmacology , Structure-Activity Relationship
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