Ortho-nitrobenzyl derivatives as potential anti-schistosomal agents

ABSTRACT In the search for new anti-schistosomal agents, a series of fifteen ortho-nitrobenzyl derivatives was assayed in vitro against both the schistosomulum (somule) and adult forms of Schistosoma mansoni. Compounds 8 and 12 showed significant activity against somules at low micromolar concentrations, but none was active against adults. The SAR demonstrated that the compounds most active against the parasite were mutagenic to the human cell line RKO-AS45-1 only at concentrations 10- to 40-fold higher than the worm-killing dose. Given their electrophilicity, compounds were also screened as inhibitors of the S. mansoni cysteine protease (cathepsin B1) in vitro. Amides 5 and 15 exhibited a modest inhibition activity with values of 55.7 and 50.6 % at 100 µM, respectively. The nitrobenzyl compounds evaluated in this work can be regarded as hits in the search for more active and safe anti-schistosomal agents.

Investigation the Consumption of Aromatic Hydrocarbons by Anoxybacillus rupeinsis Ir3 (JQ912241) using FTIR and HPLC Analyses.

Aims: To confirm the ability of Anoxybacillus rupiensis strain Ir3 (JQ912241) to utilize the aromatic compounds using FTIR and HPLC analyses. Study Design: Experimental study. Place and Duration of Study: Department of Biotechnology, College of Science, Al-Nahrain University. Baghdad, Iraq, between December 2012 and April 2013. Methodology: Anoxybacillus rupiensis strain Ir3 (JQ912241), a newly thermophilic bacterium, isolated from hydrocarbon contaminated soil in Iraq, was used. Analytical experiments include HPLC (High performance liquid chromatography) and FTIR (Fourier transform infrared) were used to determine the ability of this strain to utilize the aromatic compounds. Results: The quantitative analysis (HPLC) indicated that this bacterium showed as much as 99.62% consumption of carbazole, 99.4% of ρ-nitrophenole, 97.73% of nitrobenzene and 98.89% of naphthalene. Qualitative analysis of FTIR spectra showed that A. rupiensis strain Ir3 (JQ912241) has the ability to convert carbazole to anthranilic acid, indicating the presence of the meta cleavage enzyme, this also confirmed by using 2, 3-dihydroxybiphenyl through converting the colony color on Luria-Bertani (LB) and minimal agar plates to brown. Conclusion: The good ability of A. rupiensis strain Ir3 to utilize the studied aromatic hydrocarbons make it a good candidate as biocatalist. Its ability to convert carbazole to anthranilic acid and to oxidize catechol to 2-hydroxymuconic semialdehyde is through the meta cleavage enzyme.

Degradation of 2,4,6-trinitrotoluene by P. aeruginosa and characterization of some metabolites

Degradation of 2,4,6-trinitrotoluene (TNT), a nitroaromatic explosive found in the soil and ground water, was investigated using Pseudomonas aeruginosa in in vitro experiments. Biodegradable abilitiy of this bacteria was performed with 50 and 75 mg L−1 TNT concentrations in a defined liquid medium for 96 h time period. Treatment of TNT in supernatant samples taken at 0, 6, 12, 24, 48, 72 and 96 h from agitated vessels was followed by reverse-phase high-performance liquid chromatography (HPLC). In cultures supplemented with 50 and 75 mgL−1 TNT, after 96 h of incubation 46% and 59% reduction were detected respectively. Two metabolites as degradation intermediates with nitrite release into the medium, 2,4-dinitrotoluene (2,4-DNT) and 4-aminodinitrotoluene (4-ADNT), were elucidated by thin layer chromatography (TLC) and gas chromatography-mass spectrometry (GC-MS). These findings clearly indicate that Pseudomonas aeruginosa can be used in bioremediation of TNT contaminated sites.

The activity of a metronidazole analogue and its β-cyclodextrin complex against Trypanosoma cruzi

In this study we prepared an inclusion complex between an iodide analogue of metronidazole (MTZ-I) and cyclodextrin (CD) to develop a safer and more effective method of treating Trypanosoma cruzi infections. According to our results, MTZ-I and MTZ-I:β-CD were 10 times more active than MTZ, demonstrating that the presence of an iodine atom on the side chain increased the trypanocidal activity while maintaining its cytotoxicity. The selective index shows that MTZ-I was 10 times more active against T. cruzi than it was against mammalian cells. The modification of MTZ side chains provides a promising avenue for the development of new drugs.