Search

Estudo retrospectivo de 647 mulheres com idade340 anos, atendidas no Hospital-Escola da FMTM, Uberaba-MG. As três sorologias para a doença de Chagas foram negativas nas controles (n = 285) e positivas nas chagásicas (n = 362), que foram classificadas nas formas indeterminada (n = 125), megas (n = 58) e cardíaca (n = 179). Diabetes mellitus foi definido por duas glicemias em jejum3140mg/dl e hiperglicemia por glicemia em jejum > 110mg/dl. Os grupos foram comparados pelos testes do c2, análise de variância, "t" de Student, Kruskal-Wallis e Mann-Whitney, considerando-se significativo p < 0,05. chagásicas e controles estavam pareadas quanto à idade, o índice de massa corporal e a cor. Diabetes mellitus foi mais freqüente na forma cardíaca (15,1%), comparada com as controles (7,4%), megas (7,4%) e assintomáticas (5,6%), o mesmo ocorrendo com a hiperglicemia (37,4%, 26,7%, 25,9% e 27,2%, respectivamente), achados que estão de acordo com possível desnervação parassimpática causada pelo Trypanosoma cruzi e conseqüente predomínio da atividade simpática.

Leishmaniasis is a group of diseases caused by protozoa of the genus Leishmania. They are considered neglected diseases and are endemic to tropical and subtropical regions, affecting thousands of people annually. Leishmaniasis has a wide global distribution, present on four continents. Various drugs have been used to control leishmaniasis; however, obstacles such as high toxicity to patients and the occurrence of resistance have led to the search for alternatives. Chalcones are α, β-unsaturated ketones that can occur in the secondary metabolism of plants or can be obtained through organic synthesis. In this study, 21 chalcones brominated were synthesized via the Claisen-Schmidt condensation synthesis and characterized by UHRMS and NMR. The biological activity was evaluated for antiprotozoal potential against Leishmania amazonensis and cytotoxicity against L929 fibroblasts. Eighteen chalcones showed viability inhibition rates above 80 % at a concentration of 50 µM. Six chalcones demonstrated IC50 values ranging from 6.33 ± 0.70 µM to 23.95 ± 2.94 µM and maintained 70 % viability in L929 fibroblasts at 50 µM. The (E)-1-(4-bromophenyl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one, with a trimethoxylation at positions 2, 4, and 5 of ring B and a bromine substituent at position 4 of ring A, exhibited the lowest IC50 value (6.33 µM). These results indicate that these brominated chalcones have potential for studies aiming at the development of new drugs for leishmaniasis control., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024. Published by Elsevier Ltd.)

Chalcone (E)-1,3-diphenyl-prop-2-en-1-one and a series of 14 methoxylated derivatives have been synthesized via Claisen-Schmidt aldol condensation and characterized by FTIR, CG/MS/DIC, 1D ( 1 H and 13 C), 2D (COSY, HSQC, and HMBC) NMR, and EMAR techniques. All molecules were tested at 1 mM concentration for antifungal (Sclerotium sp., Macrophomina phaesolina and Colletotrichum gloeosporioides), antibacterial (Acidovorax citrulli two strains), and antiprotozoal (Phytomonas serpens) activities. Unmodified chalcone (CH0) and derivatives CH1, CH2, CH8 stood out in terms of antifungal activity. CH0 presented IC 50 values of 47.3 μM (9.8 μg/mL) for the fungus C. gloeosporioides. In addition, fluorescence microscopy indicated that CH0 promoted loss of hyphal cell membrane integrity. The CH1 and CH2 derivatives promoted the inhibition of Sclerotium sp. with IC 50 of 127.5 μM (32.9 μg/mL) and 110.4 μM (29.6 μg/mL), respectively. All molecules showed high activity against the phytoparasite P. serpens with IC 50 values of 0.98, 2.40, 10.25, and 3.11 μM for the derivatives CH2, CH3, CH5 and CH14 respectively. The results demonstrated that derivatives methoxylated in both rings (CH2) as well as derivatives with a furan ring associated with the methoxy group in ring A, as well as unmodified chalcone can be promising agricultural fungicides for controlling the fungi studied., (© 2024 Wiley-VHCA AG, Zurich, Switzerland.)

The mixture of pesticides is widely employed in cattle farming to combat ectoparasite resistance, such as ticks. The commercial formulation COLOSSO FC30, which contains three active ingredients (Cypermethrin, Chlorpyrifos, and Fenthion), stands out due to its efficiency. However, animals exposed to this product may become vectors of potentially toxic molecules, possibly causing contamination in aquatic and terrestrial ecosystems. In light of this, this study evaluated the eco(geno)toxic potential of the commercial formulation COLOSSO FC30, using plants (Allium cepa L., Lactuca sativa L., Raphanus sativus L., Pennisetum glaucum L., and Triticum aestivum L.) and Artemia salina L. as model organisms. In the phytotoxicity test, the species were ranked in order of sensitivity to the commercial formulation as follows: P. glaucum > L. sativa > T. aestivum > R. sativus. The most sensitive parameters were root length (RL) and shoot length (SL) of seedlings. In the cytogenotoxicity test with A. cepa, cell division was decreased at concentrations from 0.351 mL L -1 in the meristematic region and root F1. Chromosomal aberrations and micronucleus were observed at all concentrations. In the test with A. salina, the IC 50 after 24 h of exposure was 0.01207 mL L -1 of the commercial formulation. The results highlight the need for further research and regulations to understand and minimize the potential environmental impacts of COLOSSO FC30., (© 2024. The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.)

Chalcone is a molecule with known biological activities. Based on this, a series of chalcone derivatives bearing methyl, phenyl or furanyl substituents at different positions of A and B rings were synthesised, characterised, and evaluated regarding antiprotozoal activity. Molecules were synthesised via base catalyzed Claisen-Schmidt condensation and characterised by IR and NMR spectral data. Antiprotozoal activity against Phytomonas serpens , Leishmania amazonensis and Acanthamoeba polyphaga was performed. All compounds inhibited more than 50% of the growth of P. serpens while five had this effect on L. amazonensis and all of them no more than 35% of inhibition on A. polyphaga . Remarkably interesting antiprotozoal effects were recorded with compound 5, with IC 50 of 1.59 µM for P. serpens and 11.49 µM for L. amazonensis . The addition of a naphthyl group to the B ring can be postulated to be the cause of the 10 times increase observed in its trypanocidal activity.

Phytomonas serpens is a trypanosomatid phytoparasite, found in a great variety of species, including tomato plants. It is a significant problem for agriculture, causing high economic loss. In order to reduce the vegetal infections, different strategies have been used. The biological activity of molecules obtained from natural sources has been widely investigated to treat trypanosomatids infections. Among these compounds, chalcones have been shown to have anti-parasitic and anti-inflammatory effects, being described as having a remarkable activity on trypanosomatids, especially in Leishmania species. Here, we evaluated the antiprotozoal activity of the chalcone derivative (NaF) on P. serpens promastigotes, while also assessing its mechanism of action. The results showed that treatment with the derivative NaF for 24 h promotes an important reduction in the parasite proliferation (IC 50 /24 h = 23.6 ± 4.6 µM). At IC 50 /24 h concentration, the compound induced an increase in reactive oxygen species (ROS) production and a shortening of the unique flagellum of the parasites. Electron microscopy evaluation reinforced the flagellar phenotype in treated promastigotes, and a dilated flagellar pocket was frequently observed. The treatment also promoted a prominent autophagic phenotype. An increased number of autophagosomes were detected, presenting different levels of cargo degradation, endoplasmic reticulum profiles surrounding different cellular structures, and the presence of concentric membranar structures inside the mitochondrion. Chalcone derivatives may present an opportunity to develop a treatment for the P. serpens infection, as they are easy to synthesize and are low in cost. In order to develop a new product, further studies are still necessary.