Synthesis of Novel Triazine-Based Chalcones and 8,9-dihydro-7H-pyrimido[4,5-b][1,4]diazepines as Potential Leads in the Search of Anticancer, Antibacterial and Antifungal Agents.

This study presents the synthesis of four series of novel hybrid chalcones (20,21)a-g and (23,24)a-g and six series of 1,3,5-triazine-based pyrimido[4,5-b][1,4]diazepines (28-33)a-g and the evaluation of their anticancer, antibacterial, antifungal, and cytotoxic properties. Chalcones 20b,d, 21a,b,d, 23a,d-g, 24a-g and the pyrimido[4,5-b][1,4]diazepines 29e,g, 30g, 31a,b,e-g, 33a,b,e-g exhibited outstanding anticancer activity against a panel of 60 cancer cell lines with GI50 values between 0.01 and 100 µM and LC50 values in the range of 4.09 µM to >100 µM, several of such derivatives showing higher activity than the standard drug 5-fluorouracil (5-FU). On the other hand, among the synthesized compounds, the best antibacterial properties against N. gonorrhoeae, S. aureus (ATCC 43300), and M. tuberculosis were exhibited by the pyrimido[4,5-b][1,4]diazepines (MICs: 0.25-62.5 µg/mL). The antifungal activity studies showed that triazinylamino-chalcone 29e and triazinyloxy-chalcone 31g were the most active compounds against T. rubrum and T. mentagrophytes and A. fumigatus, respectively (MICs = 62.5 µg/mL). Hemolytic activity studies and in silico toxicity analysis demonstrated that most of the compounds are safe.

New pyridine-based chalcones and pyrazolines with anticancer, antibacterial, and antiplasmodial activities.

New pyridine-based chalcones 4a-h and pyrazolines 5a-h (N-acetyl), 6a-h (N-phenyl), and 7a-h (N-4-chlorophenyl) were synthesized and evaluated by the National Cancer Institute (NCI) against 60 different human cancer cell lines. Pyrazolines 6a, 6c-h, and 7a-h satisfied the pre-determined threshold inhibition criteria, obtaining that compounds 6c and 6f exhibited high antiproliferative activity, reaching submicromolar GI50 values from 0.38 to 0.45 µM, respectively. Moreover, compound 7g (4-CH3) exhibited the highest cytostatic activity of these series against different cancer cell lines from leukemia, nonsmall cell lung, colon, ovarian, renal, and prostate cancer, with LC50 values ranging from 5.41 to 8.35 µM, showing better cytotoxic activity than doxorubicin. Furthermore, the compounds were tested for antibacterial and antiplasmodial activities. Chalcone 4c was the most active with minimal inhibitory concentration (MIC) = 2 µg/mL against methicillin-resistant Staphylococcus aureus (MRSA), while the pyrazoline 6h showed a MIC = 8 µg/mL against Neisseria gonorrhoeae. For anti-Plasmodium falciparum activity, the chalcones display higher activity with EC50 values ranging from 10.26 to 10.94 µg/mL. Docking studies were conducted against relevant proteins from P. falciparum, exhibiting the minimum binding energy with plasmepsin II. In vivo toxicity assay in Galleria mellonella suggests that most compounds are low or nontoxic.

Gynandromorphs in mosquitoes (Diptera: Culicidae) from Valle del Cauca, Colombia.

Gynandromorphs of Culex nigripalpus Theobald (2), Cx. pedroi Sirivanakarn and Belkin (1) and Aedes albopictus (Skuse) (2) are described. Two individuals of the latter species were reared in the laboratory, while the remaining three specimens were wild-caught with different traps in rural areas in Valle del Cauca department, southwestern Colombia. All of the individuals were mounted on microscopic slides with Canada balsam. From each mosquito, main morphological characteristics are described and illustrated. Due to the paucity of information about this subject, these findings as well as other relevant cases are discussed.

Gynandromorphs in mosquitoes (Diptera: Culicidae) from Valle del Cauca, Colombia / Ginandromorfos en mosquitos (Diptera: Culicidae) del Valle del Cauca, Colombia

Se describen ginandromorfos de Culex nigripalpus Theobald (2), Cx. pedroi Sirivanakarn and Belkin (1) y Aedes albopictus (Skuse) (2). Los dos ejemplares de la última especie fueron criados en el laboratorio, mientras que los otros tres fueron capturados con distintas trampas en áreas rurales del departamento del Valle del Cauca, al suroeste de Colombia. Todos los ejemplares se montaron en láminas con bálsamo de Canadá. Se describen e ilustran las principales características morfológicas de cada mosquito. Por la escasez de informes sobre el tema, se discuten estos hallazgos y otros casos relevantes.

Gynandromorphs of Culex nigripalpus Theobald (2), Cx. pedroi Sirivanakarn and Belkin (1) and Aedes albopictus (Skuse) (2) are described. Two individuals of the latter species were reared in the laboratory, while the remaining three specimens were wild-caught with different traps in rural areas in Valle del Cauca department, southwestern Colombia. All of the individuals were mounted on microscopic slides with Canada balsam. From each mosquito, main morphological characteristics are described and illustrated. Due to the paucity of information about this subject, these findings as well as other relevant cases are discussed.

Human and mosquito infections by dengue viruses during and after epidemics in a dengue-endemic region of Colombia.

We conducted a study in a dengue-endemic area of Colombia to evaluate the dynamics of transmission of dengue viruses during and after epidemics. Information was simultaneously gathered about occurrence of infection in humans and mosquitoes every three months in four cities with endemic transmission. Viral isolation was confirmed in 6.7% of the persons and most were asymptomatic. Adult mosquito and larvae house indexes were not found associated with increased burden of disease. The only entomologic indicator related to dengue infection in humans was the pooled infection rate of mosquitoes. Aedes aegypti infection rates showed significant differences between the epidemic (10.68, 95% confidence interval [CI] = 7.04-15.62) and after epidemic periods of the study (6.15, 95% CI = 3.46-10.19). In addition, Ae. albopictus were also infected with dengue viruses. Increases in mosquito infection rates were associated with increases in human infection rates in the following trimester.

The bee mite Melittiphis alvearius (Berlese) (Acari: Laelapidae) in Colombia, South America / O ácaro Melittiphis alvearius (Berlese) (Acari: Laelapidae) na Colômbia, América do Sul

O total de 21 fêmeas do ácaro Melittiphis alvearius (Berlese) foi coletado sobre adultos de abelhas melíferas (Apis mellifera L.) em 12 colméias no departamento de Nariño, Colômbia. Este é o primeiro registro do ácaro na América do Sul.

A total of 21 females Melittiphis alvearius (Berlese) were found on adult honey bees (Apis mellifera L.) from 12 beehives in Nariño department, Colombia. This mite has not been previously reported in South America.