CONTROLE DE Monosporascus cannonballus POR TIAZOLIDINA-2,4-DIONA E EFEITO SOBRE O AGENTE DE CONTROLE BIOLÓGICO Trichoderma spp

The objective of this study was to evaluate the effect of the synthetic compound Thiazolidines-2,4- dione on the ¿in vitro¿ development of Monosporascus cannonballus, the causal agent of the melon sudden wilt (vine decline) and Trichoderma sp., the biocontroller agent of the referred pathogen. The work was done through two experiments. In the first experiment the following concentrations of the composition were used: 0, 25, 50, 75, 100, 125, 150, 175 ìg.mL-1, combined with four isolates of M. cannonballus. The evaluated variables were mycelial growth inhibition (MGI), mycelial growth rate (MGR) and area below mycelial growth curve (ABMGC). In the second experiment the effect of the same concentrations of the synthetic compound were analyzed regarding a Trichoderma sp isolate. In the first experiment, there was a significant interaction between concentrations andisolates. High correlation coefficients confirmed the agreement of combination among the variables. The progress curves of the variables, according to compound concentrations, were adjusted by polynomial models. The most efficient concentration was 75 ìg.mL-1,, for inhibiting the mycelia growth until the experiment end, except for the Mc4 that showed TCM of 5.07. Regarding other isolates, Mc 3 was the least resistant, as with concentration of 50 g.mL- 1showed TCM of 2.36, while Mc1, Mc2 and Mc4 presented a higher growth rate, being 8.48; 8.08 and 8.97, respectively. The recommended dosage of the compound for the inhibition of M. cannonballus development when measured in vitro is 153 ug.mL .Neither concentrations influenced the mycelial development of Trichoderma sp.,as it didn¿t differ from control (P=0,05), demonstrating the potential of this synthetic compound as a complementary form of Monosporascus cannonballus control, together to the Trichoderma spp

Antinociceptive Effect of the Essential Oil Obtained from the Leaves of Croton cordiifolius Baill. (Euphorbiaceae) in Mice

Croton cordiifolius Baill. is a shrub known as “quebra-faca” and is used to treat inflammation, pain, wounds, and gastrointestinal disturbances in the semiarid region in the northeast of Brazil. In an ethnobotanical survey in the state of Pernambuco, “quebra-faca” use was cited in 33% of the interviews. Thus, we decided to evaluate the antinociceptive effects of the essential oil from C. cordiifolius (CcEO). Chemical analysis by gas chromatography-mass spectrometry revealed 1,8-cineole (25.09%) and α-phellandrene (15.43%) as major constituents. Antinociceptive activity was evaluated using murine models of chemically induced pain (writhing induced by acetic acid, formalin, capsaicin, and glutamate tests). Opioid and central nervous systems (CNS) involvement were also investigated. Regarding antinociceptive activity, CcEO (50 and 100 mg/kg) reduced the number of writhing responses induced by acetic acid and decreased the licking times in both phases of the formalin test. CcEO also was evaluated in capsaicin- and glutamate-induced nociception. While no effect was observed in the capsaicin test, CcEO (100 mg/kg) was effective in the glutamate test. Naloxone, an opioid antagonist, did not affect the antinociceptive activity of CcEO in writhing test. In conclusion, the antinociceptive effect of CcEO could be explained, at least in part, by inhibition of the glutamatergic system

Synthesis and Antimicrobial Activities of 5-Arylidene-thiazolidine-2,4-dione Derivatives

Antibiotic resistance is considered one of the world's major public health concerns. The main cause of bacterial resistance is the improper and repeated use of antibiotics. To alleviate this problem, new chemical substances against microorganisms are being synthesized and tested. Thiazolidines are compounds having many pharmacological activities including antimicrobial activities. For this purpose some thiazolidine derivatives substituted at position 5 in the thiazolidine nucleus were synthesized and tested against several microorganisms. Using a disc diffusion method, antimicrobial activity was verified against Gram-positive, Gram-negative, and alcohol acid resistant bacteria and yeast. The minimum inhibition concentrations (MIC) and minimum bactericidal concentrations (MBC) were determined. All derivatives showed antimicrobial activity mainly against Gram-positive bacteria, with MIC values ranging from 2 to 16 µg/mL

Biological Evaluation of Arylsemicarbazone Derivatives as Potential Anticancer Agents

International audienceFourteen arylsemicarbazone derivatives were synthesized and evaluated in order to find agents with potential anticancer activity. Cytotoxic screening was performed against K562, HL-60, MOLT-4, HEp-2, NCI-H292, HT-29 and MCF-7 tumor cell lines. Compounds 3c and 4a were active against the tested cancer cell lines, being more cytotoxic for the HL-60 cell line with IC50 values of 13.08 μM and 11.38 μM, respectively. Regarding the protein kinase inhibition assay, 3c inhibited seven different kinases and 4a strongly inhibited the CK1δ/ε kinase. The studied kinases are involved in several cellular functions such as proliferation, migration, cell death and cell cycle progression. Additional analysis by flow cytometry revealed that 3c and 4a caused depolarization of the mitochondrial membrane, suggesting apoptosis mediated by the intrinsic pathway. Compound 3c induced arrest in G1 phase of the cell cycle on HL-60 cells, and in the annexin V assay approximately 50% of cells were in apoptosis at the highest concentration tested (26 μM). Compound 4a inhibited cell cycle by accumulation of abnormal postmitotic cells at G1 phase and induced DNA fragmentation at the highest concentration (22 μM)