Trichomoniasis is a great public health burden worldwide and the increase in treatment failures has led to a need for finding alternative molecules to treat this disease. In this study, we present in ...vitro and in silico analyses of two 2,8-bis(trifluoromethyl) quinolines (QDA-1 and QDA-2) against
Trichomonas vaginalis
. For in vitro trichomonacidal activity, up to seven different concentrations of these drugs were tested. Molecular docking, biochemical, and cytotoxicity analyses were performed to evaluate the selectivity profile. QDA-1 displayed a significant effect, completely reducing trophozoites viability at 160 µM, with an IC
50
of 113.8 µM, while QDA-2 at the highest concentration reduced viability by 76.9%. QDA-1 completely inhibited
T. vaginalis
growth and increased reactive oxygen species production and lipid peroxidation after 24 h of treatment, but nitric oxide accumulation was not observed. In addition, molecular docking studies showed that QDA-1 has a favorable binding mode in the active site of the
T. vaginalis
enzymes purine nucleoside phosphorylase, lactate dehydrogenase, triosephosphate isomerase, and thioredoxin reductase. Moreover, QDA-1 presented a level of cytotoxicity by reducing 36.7% of Vero cells’ viability at 200 µM with a CC
50
of 247.4 µM and a modest selectivity index. In summary, the results revealed that QDA-1 had a significant anti-
T. vaginalis
activity. Although QDA-1 had detectable cytotoxicity, the concentration needed to eliminate
T. vaginalis
trophozoites is lower than the CC
50
encouraging further studies of this compound as a trichomonacidal agent.
The objectives of this study were to estimate the rate of infection by Treponema pallidum and co-infection with Human Immunodeficiency Virus (HIV) in individuals attending the General Hospital of ...Benguela (GHB), Angola, to verify the Rapid Plasma Reagin (RPR) test performance for its diagnosis when compared with other RPR tests, and to compare a rapid treponemal test with the Treponema pallidum hemagglutination assay (TPHA).
This is a cross-sectional study carried out between August 2016 and January 2017, at the GHB, 546 individuals attending the emergency room, the outpatient service or hospitalized at the GHB were included. All the samples were tested at the GHB with the routine hospital RPR test and a rapid treponemal test. The samples were then transported to the Institute of Hygiene and Tropical Medicine (IHMT) where RPR testing and TPHA testing were performed.
The rate of T. pallidum active infection, demonstrated by a reactive RPR and TPHA result, was 2.9%, of which 81.2% corresponded to indeterminate latent syphilis and 18.8% to secondary syphilis. HIV co-infection was detected in 62.5% of individuals diagnosed with syphilis. Past infection, defined as a non-reactive RPR and reactive TPHA test, was diagnosed in 4.1% of individuals.
The high rate of syphilis/HIV co-infection emphasizes the urgent requirement for adequate sexually transmitted infections (STIs) screening, prevention and treatment programs. In addition, implementation of quality control measures within RPR testing protocols at GHB are needed, including training for laboratory personnel, adequate equipment and introduction of other rapid testing.
Most studies of Brazilian red propolis have explored the composition and biological properties of its ethanolic extracts. In this work, we chemically extracted and characterized the essential oil of ...Brazilian red propolis (EOP) and assessed its adjuvant, antiparasitic and cytotoxic activities. The chemical composition of EOP was analyzed using gas chromatography with mass spectrometry (GC-MS). EOP was tested for in vitro activity against Trichomonas vaginalis (ATCC 30236 isolate); trophozoites were treated with different concentrations of EOP (ranging from 25 to 500 μg/mL) in order to establish the MIC and IC50 values. A cytotoxicity assay was performed in CHO-K1 cells submitted to different EOP concentrations. BALB/c mice were used to test the adjuvant effect of EOP. The animals were divided in 3 groups and inoculated as follows: 0.4 ng/kg BW EOP (G1); 50 μg of rCP40 protein (G2); or a combination of 0.4 ng/kg BW EOP and 50 μg of rCP40 (G3). Total IgG, IgG1 and IgG2a levels were assessed by ELISA. The major constituent compounds of EOP were methyl eugenol (13.1%), (E)-β-farnesene (2.50%), and δ-amorphene (2.3%). Exposure to EOP inhibited the growth of T. vaginalis, with an IC50 value of 100 μg/mL of EOP. An EOP concentration of 500 μg/mL was able to kill 100% of the T. vaginalis trophozoites. The EOP kinetic growth curve showed a 36% decrease in trophozoite growth after a 12 h exposure to 500 μg/mL of EOP, while complete parasite death was induced at 24 h. With regard to CHO-K1 cells, the CC50 was 266 μg/mL, and 92% cytotoxicity was observed after exposure to 500 μg/mL of EOP. Otherwise, a concentration of 200 μg/mL of EOP was able to reduce parasite proliferation by 70% and was not cytotoxic to CHO-K1 cells. As an adjuvant, a synergistic effect was observed when EOP was combined with the rCP40 protein (G3) in comparison to the administration of each component alone (G1 and G2), resulting in higher concentrations of IgG, IgG1 and IgG2a. EOP is constituted by biologically active components with promising antiparasitic and immunostimulatory activities and can be investigated for the formulation of new vaccines or trichomonacidal drugs.
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•Curcumin monocarbonyl analogues were synthesized in good yields by easy protocols.•Three analogues inhibited Trichomonas vaginalis growth similarly to metronidazole.•Curcumin ...analogues eradicated T. vaginalis growth within 24 hrs.•Analogue 3e did not induce any level of cytotoxicity on VERO cells.•The analogues reported are worth exploring as potential anti-T. vaginalis agents.
Trichomoniasis is a parasitic infection caused by Trichomonas vaginalis and it is considered to be the most common non-viral sexually transmitted infection in the world. Since the 1960s, nitroimidazoles such as metronidazole are the drugs of choice for the treatment of trichomoniasis, but many adverse effects and allergic reactions may result from their use. Reports of metronidazole-resistant infections also highlight the importance for the search of new anti-T. vaginalis agents. Considering this, herein we report the anti-T. vaginalis evaluation of 21 synthetic monocarbonyl analogues of curcumin, which itself has been reported to possess antiparasitic potential. From the in vitro analysis of the synthetic molecules, untreated trophozoites, and metronidazole at 100 μM, it was observed that three curcumin analogues (3a, 3e, and 5e) exhibited anti-T. vaginalis activity comparable to metronidazole (no significant statistical difference). Optimal antiparasitic concentrations were determined to be 80 μM and 90 μM for propanone derivatives 3a and 3e, respectively, and 200 μM for cyclohexanone derivative 5e. Kinetic growth curves showed that, after 24 h, the trophozoites were completely inhibited. At the tested concentrations, natural curcumin did not significantly inhibit the growth of trophozoites, therefore demonstrating that the designed synthetic molecules not only have better chemical stability, but also higher anti-T. vaginalis potential. Cytotoxicity analysis, performed on VERO cells, demonstrated low, moderate and high cytotoxic effects for analogues 3e, 5e and 3a, respectively. This study suggests that these analogues possess chemical features of interest to be further explored as alternatives for the treatment of trichomoniasis.
Men who have sex with men (MSM) are at greater risk for sexually transmitted infections (STIs). Data on MSM chlamydia and gonorrhea prevalence estimates and associated risk factors are scarce. To our ...knowledge, this is the first study to describe the prevalence and the determinants of both chlamydia and gonorrhea infections in MSM in Portugal. We conducted a cross-sectional study using data from 1832 visits to CheckpointLX, a community-based center for screening blood-borne viruses and other STIs in MSM. Overall prevalence of chlamydia or gonorrhea in our sample was 16.05%, with 14.23% coinfection and 40.73% asymptomatic presentation among those testing positive. Anorectal infection was most common for chlamydia (67.26%), followed by urethral (24.78%) and oral (19.47%) infection. Oral infection was most common for gonorrhea (55.63%), followed by anal (51.25%) and urethral (17.50%) infection. In multivariate analyses, young age (U = 94684, p = 0.014), being foreign-born (χ2 = 11.724, p = 0.003), reporting STI symptoms (χ2 = 5.316, p = 0.021), inhaled drug use (χ2 = 4.278, p = 0.039) and having a higher number of concurrent (χ2 = 18.769, p < 0.001) or total (χ2 = 5.988, p = 0.050) sexual partners were each associated with higher rates of chlamydia or gonorrhea infection. Young and migrant MSM are a vulnerable population to STIs, as are those who use inhaled drugs and those with a higher number of concurrent or total sexual partners. Although Portugal has no guidelines on chlamydia and gonorrhea screening, our results point toward a need for greater awareness about the importance of high-frequency screening for those at increased risk (i.e., every three to six months).
Annona coriacea
Mart. is a native tree to the savannas of Brazil that produces fruits that have economic, ecological, and dietary potential for use by local communities and the food industry. The ...conservation and pre-breeding of natural populations of
A. coriacea
depend on genetic divergence studies and require knowledge about its characterization and the possible identification of superior genotypes. Therefore, the objective of this study was to quantify genetic divergence in a native population of
A. coriacea
genotypes based on morphological and physicochemical characteristics, estimate the efficiency of descriptors used in the discrimination of the genotypes, and indicate the essential descriptors for the characterization activities. A total of 34 quantitative descriptors were used to describe this diversity, and the data were subjected to multivariate analysis and clustering analysis. The relative importance of the descriptors was measured using the Singh method. The pulp and fruit weight and potassium concentration were the most important descriptors that contributed to the genetic divergence of the populations. The grouping methods (UPGMA and Tocher) allocated to the heterogeneous groups presented high genetic variability, enabling the selection of individuals for hybridization programs with F1 generation gains. The evaluated populations had high phenotypic variability in fruits and seeds. This study identified genotypes that could be introduced into the food and cosmetic industries. These native populations have the potential to be used in breeding programs.
Lima bean (
Phaseolus lunatus
L.) have high genetic diversity, especially in Brazil, which has been maintained both on farms and in germplasm banks. Knowledge of the genetic diversity of germplasm in ...landraces is important for the development of breeding programs. We investigated the genetic diversity of lima bean landraces accessed in the
Phaseolus
Germplasm Bank of the Federal University of Piauí (PGB-UFPI, Brazil), using agro-morphological and microsatellite markers (SSRs). We analyzed 26 qualitative and 11 quantitative traits, following the Bioversity International descriptors. Furthermore, 15 SSRs were used to determine the genetic polymorphism and genetic differentiation among genotypes. The agro-morphological traits and SSR markers were reliable and effective for determining the genetic diversity of the accessions. Cluster analysis revealed a considerable phenotypic diversity among the accessions for some characters related to agronomic performance, such as the number of pods per plant, number of seeds per pod, and weight of 100 seeds. At the molecular level, ten loci showed polymorphism; the number of alleles per locus varied from two to seven, with mean polymorphism information content of 0.282 per locus. Loci GATS91 and PVat001 were highly informative and are indicated for further studies of lima bean. The accessions constitute an important gene pool for future breeding programs, especially accession UFPI-262. Accessions UFPI-262 and UFPI-252 can be used in crosses, as they are genetically distant and complementary in their characteristics.
•Neisseria gonorrhoeae isolates were susceptible to ceftriaxone.•Some isolates showed intermediate resistance to azithromycin.•Intermediately resistant and fully resistant isolates presented ...mutations in resistance genes.•The expedient development of new therapeutic options is essential.
To analyze the susceptibility of Neisseria gonorrhoeae isolates to penicillin (Pen), cefixime (Cfm), ceftriaxone (Cro), tetracycline (Tet), ciprofloxacin (Cip), azithromycin (Azm), and spectinomycin (Spt), and to verify the presence of mutations in resistance genes.
Antibiotic susceptibility testing was performed by Etest method on 30 N. gonorrhoeae isolates collected from the MSM (men who have sex with men) population. PCR and DNA sequencing were performed to identify mutations within the penA, mtrR, gyrA, and parC genes in intermediately resistant and fully resistant isolates.
N. gonorrhoeae isolates showed intermediate or full resistance to Pen (73%), Cfm (3%), Tet (60%), Cip (37%), and Azm (13%). One isolate with resistance to Cfm presented a penicillin-binding protein 2 (PBP2) mosaic XXXIV. All isolates with intermediate or full resistance to Pen (except at PBP2 mosaic) presented a D345a in PBP2. All Cip-resistant isolates had an S91F in the gyrA gene together with mutations in the parC gene. All intermediate or fully resistant isolates to substrates of the MtrCDE efflux pump had an A39T or G45D mutation in the mtrR gene or an adenine deletion within the mtrR promoter. One isolate presented a Neisseria meningitidis-like mtrR promoter sequence.
The results of this study are consistent with the findings of other studies and reinforce the importance of the expedient development of new therapeutic options.
Biodiversity underlies ecosystem functioning. While aboveground biodiversity is often well studied, the belowground microbiome, in particular protists, remains largely unknown. Indeed, holistic ...insights into soil microbiome structures in natural soils, especially in hyperdiverse biomes such as the Brazilian Cerrado, remain unexplored. Here, we study the soil microbiome across four major vegetation zones of the Cerrado, ranging from grass-dominated to tree-dominated vegetation with a focus on protists. We show that protist taxon richness increases towards the tree-dominated climax vegetation. Early successional habitats consisting of primary grass vegetation host most potential plant pathogens and least animal parasites. Using network analyses combining protist with prokaryotic and fungal sequences, we show that microbiome complexity increases towards climax vegetation. Together, this suggests that protists are key microbiome components and that vegetation succession towards climax vegetation is stimulated by higher loads of animal and plant pathogens. At the same time, an increase in microbiome complexity towards climax vegetation might enhance system stability.
ABSTRACT Some germplasm collections have a high number of accessions, which makes it difficult to explore the genetic variability present in the germplasm bank due to the redundancy and the ...difficulty of detailed analysis of all conserved accessions. Therefore, our study aimed to analyze the genetic diversity of 153 lima bean (Phaseolus lunatus) accessions for the purpose of constructing a core collection. Eleven SSRs were used for this purpose. The 153 lima bean accessions can be represented by low redundancy using a minimum of 34 accessions, thus representing 22 % of the size of the entire germplasm bank. The core collection had a higher Shannon diversity index and expected heterozygosity (1.906 and 0.811, respectively) than those presented by the entire germplasm bank (1.605 and 0.713, respectively), indicating a higher polymorphism of the representative cultivars in relation to the entire collection. The accessions selected for the core collection may be used in future studies of genome association as well as in genetic crosses in breeding programs aimed at developing improved cultivars with high genetic diversity which can meet current and future market needs.
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