Evaluation of the effect of 1,3-bis-(4-phenyl-[1,2,3] triazole-1-il)2-propanol in comparison with metronidazole in an in vitro culture of Blastocystis in samples of patients with irritable bowel syndrome.

Metronidazole is the most-used pharmaceutical for the treatment of infection by Blastocystis. However, studies have reported resistance of the microorganism towards this pharmaceutical. In Mexico, studies concerning the prevalence of this parasite and its relationship to Irritable Bowel Syndrome have been carried out. To evaluate the in vitro effect of metronidazole and the compound 1,3-bis-(4-phenyl-[1,2,3] triazole-1-il)2-propanol over Blastocystis, as well as the prevalence of Blastocystis in patients with Irritable Bowel Syndrome. A prospective, transversal design study (April 2016-April 2017) of 51 samples of patients with Irritable Bowel Syndrome, obtained from the ISSEMyM Medical Center in Toluca, Mexico. For the identification of Blastocystis was done in three serial stool samples through direct microscopic examination and the Ritchie technique. The in vitro susceptibility test towards metronidazole and the triazolic compound was done through a microculture in concentrations of 1 to 1000 µg/mL, each one in triplicate. A 31.3% prevalence of Blastocystis was observed in the population, with greater prevalence in women (30.2%) than in men (25%). In the susceptibility test, a CL50 of 64 µg/mL was obtained for metronidazole, in comparison to the CL50 of 250 µg/mL for 1,3-bis-(4-phenyl-[1,2,3] triazole-1-il)2-propanol. This molecule in development has an effect for the treatment of infection by Blastocystis in vitro in patients with IBS and therefore, more studies should be performed.

Indole-3-acetic acid biosynthesis is deficient in Gluconacetobacter diazotrophicus strains with mutations in cytochrome c biogenesis genes.

Gluconacetobacter diazotrophicus is an endophyte of sugarcane frequently found in plants grown in agricultural areas where nitrogen fertilizer input is low. Recent results from this laboratory, using mutant strains of G. diazotrophicus unable to fix nitrogen, suggested that there are two beneficial effects of G. diazotrophicus on sugarcane growth: one dependent and one not dependent on nitrogen fixation. A plant growth-promoting substance, such as indole-3-acetic acid (IAA), known to be produced by G. diazotrophicus, could be a nitrogen fixation-independent factor. One strain, MAd10, isolated by screening a library of Tn5 mutants, released only approximately 6% of the amount of IAA excreted by the parent strain in liquid culture. The mutation causing the IAA(-) phenotype was not linked to Tn5. A pLAFR3 cosmid clone that complemented the IAA deficiency was isolated. Sequence analysis of a complementing subclone indicated the presence of genes involved in cytochrome c biogenesis (ccm, for cytochrome c maturation). The G. diazotrophicus ccm operon was sequenced; the individual ccm gene products were 37 to 52% identical to ccm gene products of Escherichia coli and equivalent cyc genes of Bradyrhizobium japonicum. Although several ccm mutant phenotypes have been described in the literature, there are no reports of ccm gene products being involved in IAA production. Spectral analysis, heme-associated peroxidase activities, and respiratory activities of the cell membranes revealed that the ccm genes of G. diazotrophicus are involved in cytochrome c biogenesis.

A novel radiopharmaceutical for detection of malignant melanoma, based on melanin formation: 3-iodo-4-hydroxyphenyl-L-cysteine.

The aim of this study was to develop a new artificial amino acid radiopharmaceutical labelled with radioiodine for detection of malignant melanoma, based on melanin formation. By considering the affinity for tyrosinase, a starting enzyme on the branching point to melanin biosynthesis, 3-[125I]iodo-4-hydroxyphenyl-L-cysteine (125I-L-PC) was synthesized and evaluated biologically. Labelling of 125I-L-PC using the chloramine-T method was carried out conveniently and efficiently in a short period of time, with high specific activity. In a biodistribution study, 125I-L-PC showed a low accumulation in normal tissue and relative retention in B16 melanoma. A high contrast image of peripheral tumour was obtained during autoradiography. During an in vitro accumulation study, inhibition of 125I-L-PC with a tyrosinase inhibitor suggested interaction of this tracer with tyrosinase. It indicates that the uptake mechanism of 125I-L-PC to melanoma tissue was dependent on high tyrosinase activity in melanoma cells. Thus, 125I-L-PC appears to be a promising radioiodinated amino acid radiopharmaceutical for imaging malignant melanoma in relation to melanin formation, namely specific metabolism with high tyrosinase activity.