Posted by admin on Nov 30, 2018 in |
Plasmodium falciparum and multidrug resistant bacteria such as Mycobacterium avium, Staphylococcus aureus and Escherichia coli are among the top causes of morbidity and mortality especially in developing countries. These pathogens are responsible for the reported antibiotic resistance incidents globally. Due to the increase in antibiotic resistance worldwide, there is an urgent need for new bioactive compounds. This study aimed at determining the antiplasmodial and antimicrobial activity of secondary metabolites produced by soil actinomycetes. Soil samples were collected from Kavango and Hardap regions and cultured on various media to isolate and identify actinomycetes. Secondary metabolites produced were extracted using different solvents. The antimicrobial activity of different isolated secondary metabolites was determined against M. avium, S. aureus and E. coli. Antiplasmodial activity of four bioactive fractions with potent antibacterial activity was further determined against a chloroquine resistant (D10) P. falciparum strain at various concentrations. Bioactive compounds from two isolates displayed activity against M. avium, whilst another two showed activity against E. coli. None of the secondary metabolites displayed activity against S....
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Posted by admin on Nov 30, 2018 in |
The biologically active compounds in plants reckoned their application in medicines from ancient times. Among the biologically active compounds enzymes have evolved as a potential therapeutic agent. L-asparaginase a therapeutic protein is extensively employed in medical sector to diagnose and treat leukemia. Bacteria, fungi, yeast and plants have been identified as potential sources of L-asparaginase. The side effects associated with microbial L-asparaginase restricted their utilization in treatment of leukemia and bought medicinal plants as source into focus. In the present study, different species of Phyllanthus genera have been screened for presence of L-asparaginase in different seasons. The leaves of Phyllanthus emblica with highest enzyme activity (20.3 IU/ml) and specific activity (5.2 IU/mg) emerged out as potential source for L-asparaginase production. Phyllanthus amarus and Phyllanthus niruri also contained appreciable amount of L-asparaginase. This is the first report of identifying presence of L-asparaginase in Phyllanthus genera. L-asparaginase from Phyllanthus emblica was further purified to homogeneity and the molecular mass of enzyme was found to approximately 85kDa. The yield of purified enzyme...
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Posted by admin on Nov 30, 2018 in |
Background: It has been developed a new combination of Palladium catalyzed Buchwald-Hartwig type reaction for the synthesis of N–tert– Butyl- 3- {[5- methyl- 2- (arylamino)pyrimidin- 4- yl]amino}benzene-sulfonamides 5 by the treatment of N–tert-butyl-3-[(2-chloro-5-methyl pyrimidin-4-yl)-amino]benzene sulfonamide 4 with various aromatic amines in the presence of Cs2CO3 and in DMF under microwave conditions. Method: All the eight compounds 5a-h were screened in-vitro for their antibacterial Gram-positive bacteria namely, Bacillus subtilis, Bacillus sphaericus and Staphylococcus aureus and three Gram-negative bacteria Pseudomonas aeruginosa, Klebsiella aerogenes, Chromobacterium violaceum. All the synthesized compounds were tested for their antifungal activity against five test organisms, Aspergillus niger, Chrysosporium tropicum, Rhizopus oryzae, Fusarium moniliforme and Curvularia lunata. Results: Among the title compounds 5d and 5e exhibited potent activity towards both gram positive and gram negative bacteria. Compounds 5e and 5f showed good antifungal activity. Conclusion: A new efficient catalyst/ligand combination was developed for the synthesis of title compounds 5a-5h under microwave conditions. The microwave procedure is slightly superior to the conventional method in terms of reduced time period...
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Posted by admin on Nov 30, 2018 in |
Efavirenz (EFA) solid binary systems were prepared with β-CD by co-grinding and microwave irradiation methods. Detection of inclusion complexation was done in solution state by means of phase solubility analysis and in solid state by FTIR, DSC and in-vitro Dissolution studies. Apparent stability constant revealed EFA with β-CD at 1:1 M produces stiochometric complex with AL type phase solubility profile. A true inclusion of EFA with β-CD at 1:2 M in solid state was confirmed by FTIR and DSC. Dissolution properties of EFA- β-CD binary systems were superior when compared to physical mixture and pure drug. Overall the rank order of improvement in dissolution properties of Efavirenz with ratios is 1:2M > 1:1M and methods MW > CG > PM > pure drug. One way ANOVA suggest the DP60 and DE60 values were significantly higher (P<0.01) in solid binary systems prepared by microwave irradiation method when compared to co-grinding and its corresponding physical mixtures and pure...
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Posted by admin on Nov 30, 2018 in |
As in the cases of non-communicable but chronic and autoimmune disorders like diabetes, cancer, anemia and rheumatoid arthritis are growing threat to humans. They depend on the genetic information and the genome sequence of the patients and other factors like environmental factors. In most of the cases, the pattern of the disease, i.e. pathogenesis is different for every individual, though phenotypic expression is same. Hence, there is a greater risk for the patient having the genes which are likely to cause above mentioned diseases and side effects or adverse drug reactions due to the therapy available. This occurs due to only one reason that every individual will not react to a drug in a same way. For minimizing these unwanted side effects or adverse reactions which are disease related and for giving patients a better and a bit healthy life, personalizing the medication is essential. This personalization involves the study of phenotypic and genotypic information of the patient and then planning the 3D’s i.e. choice of drug, dose and...
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