Do fall armyworm's Metaflumizone resistante populations affect the activity of Trichogramma pretiosum? / Populações da lagarta-do-cartucho resistentes à Metaflumizona afetam a atividade de Trichogramma pretiosum?

Abstract The possible interference of resistant pest's populations to insecticides in natural enemies in the action thas not been clarified yet. Thus, this study aimed to evaluate Trichogramma pretiosum Riley (Hymenoptera: Trichogrammatidae) performance on Spodoptera frugiperda (J. E. Smith) (Lepidoptera: Noctuidae) eggs with resistance frequency to the Metaflumizone over six generations of product exposure. Egg cards (2.0 x 7.0 cm) containing eggs from two populations of S. frugiperda, (resistant to Metaflumizone and the other susceptible), were exposed to T. pretiosum females for 24 hours in free-choice and no-choice testing in three generations (G1, G4, and G6). A completely randomized experimental design was used with 25 replications, each consisting of an egg card (experimental unit) containing 20 eggs. The parameters evaluated were: parasitism (%), emergence (%), sex ratio, number of emerged parasitoids per egg and males/females longevity. ANOVA and Tukey test (P≤ 0.05) were applied on the results. Results showed a reduction in parasitism [41.0% (G1) and 28.4% (G4)], egg emergence (17.5%) and parasitoids/egg [16.2 (G4) and 17.2 (G6)] in eggs originating from the population with resistance frequency. Females emerging from G6 populations eggs without exposure to Metaflumizone had greater longevity (3.5 days more) than the resistant population. The sex ratio and male longevity were not affected. The results indicate a reduction in T. pretiosum activity if S. frugiperda populations have some frequency of resistance to Metaflumizone.

Resumo A possível interferência de populações de pragas resistentes na ação de inimigos naturais ainda não foi esclarecida. Assim, este trabalho teve como objetivo avaliar o desempenho de Trichogramma pretiosum Riley (Hymenoptera: Trichogrammatidae) em ovos de Spodoptera frugiperda (J. E. Smith) (Lepidoptera: Noctuidae) com frequência de resistência à Metaflumizona ao longo de seis gerações de exposição ao produto. Cartelas (2,0 x 7,0 cm) com ovos de duas populações de S. frugiperda, (resistente à Metaflumizona e outra suscetível), foram expostas às fêmeas de T. pretiosum por 24 horas em condições de livre escolha e sem chance de escolha por três gerações (G1, G4 e G6). O delineamento experimental foi inteiramente casualizado com 25 repetições, sendo cada repetição composta por uma cartela (unidade experimental) contendo 20 ovos. Os parâmetros avaliados foram: parasitismo (%), emergência (%), razão sexual, número de parasitoides emergidos por ovo e longevidade de machos e fêmeas. ANOVA e teste de Tukey (P≤ 0,05) foram aplicados aos dados coletados. Os resultados mostraram redução do parasitismo [41,0% (G1) e 28,4% (G4)], emergência de ovos (17,5%) e parasitoides/ovo [16,2 (G4) e 17,2 (G6)] em ovos oriundos da população com frequência de resistência. As fêmeas emergidas de ovos da população G6 sem exposição à Metaflumizona, tiveram maior longevidade (3,5 dias a mais) do que a população exposta ao inseticida. A razão sexual e a longevidade de machos não foram afetadas. Os resultados indicam uma redução na atividade de T. pretiosum se as populações de S. frugiperda apresentarem alguma frequência de resistência à Metaflumizona.

The antimicrobial activity of lapachol and its thiosemicarbazone and semicarbazone derivatives

Lapachol was chemically modified to obtain its thiosemicarbazone and semicarbazone derivatives. These compounds were tested for antimicrobial activity against several bacteria and fungi by the broth microdilution method. The thiosemicarbazone and semicarbazone derivatives of lapachol exhibited antimicrobial activity against the bacteria Enterococcus faecalis and Staphylococcus aureus with minimal inhibitory concentrations (MICs) of 0.05 and 0.10 µmol/mL, respectively. The thiosemicarbazone and semicarbazone derivatives were also active against the pathogenic yeast Cryptococcus gattii (MICs of 0.10 and 0.20 µmol/mL, respectively). In addition, the lapachol thiosemicarbazone derivative was active against 11 clinical isolates of Paracoccidioides brasiliensis, with MICs ranging from 0.01-0.10 µmol/mL. The lapachol-derived thiosemicarbazone was not cytotoxic to normal cells at the concentrations that were active against fungi and bacteria. We synthesised, for the first time, thiosemicarbazone and semicarbazone derivatives of lapachol. The MICs for the lapachol-derived thiosemicarbazone against S. aureus, E. faecalis, C. gattii and several isolates of P. brasiliensis indicated that this compound has the potential to be developed into novel drugs to treat infections caused these microbes.

Hepatoprotective effect of acetone semicarbazone on Ehrlich ascites carcinoma induced carcinogenesis in experimental mice

<p><b>OBJECTIVE</b>To determine the hepatoprotective effect of acetone semicarbazone (ASC) in vivo in normal and Ehrlich ascites carcinoma (EAC) bearing male Swiss albino mice.</p><p><b>METHODS</b>Drug-induced changes in biochemical and behavioral parameters at dose of 2.0 mg/kg body weight for 14 d and nullifying the toxicity induced by EAC cells were studied. The histopathology studies of the protective effects of ASC on vital organs were also assessed.</p><p><b>RESULTS</b>The administration of ASC made insignificant changes in body weight and behavioral (salivation, diarrhea, muscular numbness) changes during treatment period due to minor toxicity were minimized after the treatment in normal mice. The biochemical parameters, including serum glutamate pyruvate transaminase, glutamate oxaloactate transaminase, alkaline phosphatase, serum glucose, cholesterol, urea, triglyceride and billirubin changed modestly in normal mice receiving ASC. Though the treatment continued, these values gradually decreased to normal level after the treatment. In EAC bearing mice, the toxic effects due to EAC cells in all cases were nullified by treatment with the ASC. Significant abnormalities were not detected in histology of the various organs of the normal mice treated with ASC.</p><p><b>CONCLUSIONS</b>ASC can, therefore, be considered safe in formulating novel anticancer drug, as it exhibits strong protective effect against EAC cell bearing mice.</p>

Avaliação da atividade e toxicidade de derivados de tiossemicarbazonas e semicarbazonas contra Trypanosoma cruzi e Leishmania (L. ) amazonensis in vitro / Evaluation of the activity and toxicity of thiosemicarbazones and semi-carbazones against Trypanosoma cruzi and Leishmania (L. ) amazonensis in vitro

Os tratamentos disponíveis para a Doença de Chagas e as leishmanioses não são eficientes e apresentam alta toxicidade. Efeito sinérgico tem sido demonstrado, quando drogas referência e novos compostos, são associados e utilizados contra estas patologias. Tiossemicarbazonas (TS) e semicarbazonas (SC) são classes de compostos com importante atividade sobre vários patógenos, incluindo o T. cruzi e a Leishmania sp. Na presente tese foram avaliados in vitro, os efeitos de três derivados de tiossemicarbazonas [estiril-tiosemicarbazona, (2-metoxi-estiril)-tiosemicarbazona e (3-metoxi-4-hidroxi-estiril)-tiosemicarbazona] e de duas semicarbazonas [(2-metoxi-estiril)-semicarbazona e (3-metoxi-4-hidroxi-estiril)-semicarbazona] sobre o T. cruzi e a Leishmania (L.) amazonensis. Nossos resultados revelaram a excelente atividade antiparasitária da maioria dos compostos, sendo que as tiossemicarbazonas mostraram-se mais ativas sobre formas tripomastigotas de T. cruzi em relação as formas promastigotas de L. (L.) amazonensis. Também observamos que a (2-metoxi-esteril)-tiossemicarbazona foi mais efetiva sobre formas amastigotas de T. cruzi, presentes em culturas de macrófagos humanos, em comparação aos parasitos intracelulares alojados em macrófagos peritoneais de camundongos, infectados in vitro. Os ensaios de associação dos compostos as drogas de referência Benzonidazol (BZ) para T. cruzi e Pentamidina (PT) para L. (L) amazonensis), revelaram uma importante potencialização da ação tripanocida e leishmanicida das TS e SC, apresentando baixa toxicidade sobre células de mamíferos. Nossos resultados promissores reforçam a importância da continuidade destes estudos, de modo a identificar terapias mais eficientes para o tratamento das doenças de Chagas e leishmanioses.

Microwave-assisted synthesis, anticonvulsant activity and quantum mechanical modelling of N-(4-bromo-3-methylphenyl) semicarbazones / 浙江大学学报（英文版）（B辑：生物医学和生物技术）

<p><b>OBJECTIVE</b>To study the effect of halo substitution on disubstituted aryl semicarbazones on the anticonvulsant potential and model the activity based on quantum mechanics.</p><p><b>METHODS</b>A series of twenty-six compounds of N(4)-(4-bromo-3-methylphenyl) semicarbazones were synthesized and evaluated for the anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure threshold tests. Some potential compounds were also tested in the subcutaneous strychnine (scSTY) and subcutaneous picrotoxin (scPIC) seizure threshold tests. The synthesized compounds were tested for behavioral impairment and CNS (central nervous system) depression in mice. Quantum mechanical modelling was carried out on these compounds to gain understanding on the structural features essential for activity.</p><p><b>RESULTS</b>Some compounds possessed broad spectrum anticonvulsant activity as indicated by their effect in pentylenetetrazole, strychnine, picrotoxin and maximal electroshock seizures models in resemblance to other aryl semicarbazone derivatives reported earlier. The higher the difference in HOMO (highest occupied molecular orbital) and LUMO (lowest unoccupied molecular orbital) energy levels was, the greater was the activity profile.</p><p><b>CONCLUSION</b>The pharmacophoric requirements for compounds to exhibit anticonvulsant activity that includes one aryl unit in proximity to a hydrogen donor-acceptor domain and an electron donor have been justified with the molecular orbital surface analysis of the synthesized compounds.</p>

Synthesis and evaluation of 4-substituted semicarbazones of levulinic acid for anticonvulsant activity / 浙江大学学报（英文版）（B辑：生物医学和生物技术）

<p><b>OBJECTIVE</b>A series of 4-aryl substituted semicarbazones of levulinic acid (4-oxo pentanoic acid) was designed and synthesized to meet the structural requirements essential for anticonvulsant activity.</p><p><b>METHODS</b>All the compounds were evaluated for anticonvulsant activity. Anticonvulsant activity was determined after intraperitoneal (i.p.) administration to mice by maximal electroshock (MES) and subcutaneous metrazol (ScMet) induced seizure methods and minimal motor impairment was determined by rotorod test.</p><p><b>RESULTS</b>A majority of the compounds exhibited significant anticonvulsant activity after intraperitoneal administration. In the present study 4-(4'-fluoro phenyl) levulinic acid semicarbazone emerged as the most active molecule, showing broad spectrum of activity with low neurotoxicity. Unsubstituted levulinic acid semicarbazone was found to be inactive in all the screens.</p><p><b>CONCLUSION</b>The results obtained validate the hypothesis that presence of an aryl group near the semicarbazone moiety is essential for anticonvulsant activity. The results also indicate that the hydrophilic-hydrophobic site can accommodate hydrophilic groups.</p>

Síntese e atividade biológica de novas tiossemicarbazonas / Synthesis and biological activity of new thiosemicarbazones

Este trabalho descreve a síntese e avaliaçäo estrutural de nove tiossemicarbazonas, obtidas pela condensaçäo de ariltioacetaldeídos e artiopropanonas substituídas com cloridrato de tiossemicarbazida. Estes novos compostos foram testados in vitro pelo fitoteste Lepidium sativum. Todos eles apresentaram atividade inibidora do crescimento celular (pI50) superior àquela de 5-fluoruacila, composto anticancerígeno, utilizado como referência.

Synthesis of some new 1, 2, 3-selena and thiadiazole derivatives

Several compounds of 1,2,3-selena and/or thioadizoles with evident biological activity were previously reported by the authors, certainly as antibacterial and antifungal agents [1-6] e.g. 1,2,3-thiadiozolo and/or selenadiazolo-4-yl-pheynyl-hydrazophyrazolones [10] were tested in vitro against a variety of Gram positive strains of bacteria. Certain compounds show strong activity against Bacillus sub., staphylococcus areus and Mycobacterium phlei. Thus, pyridine [7], furan [8] and thiophene [9] containing 1,2,3-selena and thiadiazoles motivated their synthesis and testing as biologically active compounds. In this work, compounds [1-3] were easily condensed with semicarbazide to give the corresponding semicarbazones [4-6] respectively. On the other hand, the purified semicarbazones [4-6] were then oxidized either with selenium dioxide [11] in glacial acetic acid to give 1,2,-3-selenadiazole Derivatives[9,11] or with thionyl chloride[12] to afford, 1,2,3-thiadiazole derivatives[10,12]

New antimicrobial quinazolinone derivatives

A series of quinazolin-4-ones incorporated with pyridones, iminopyridines, thiazole, semicarbazone and thiosemicarbazone moieties were synthesized. Some tested compounds showed considerable biological activity against some microorganisms

Mecanismo da reacao de semicarbazida com aldeidos aromaticos heterociclicos / Mechanism of the reaction of semicarbazide with some heterocyclic aromatic aldehydes

A reacao entre semicarbazina e 2-tiofenocarboxaldeido, 2-pirrolcarboxaldeido e N-metil-2-pirrolcarboxaldeido, dando origem a semicarbazonas, em solucao aquosa, a 25,0 graus centigrados e com forca ionica 0,50, ocorre em duas etapas: formacao de uma carbinolamina intermediaria (etapa lenta em valores de pH inferiores a 5) e desidratacao da carbinolamida (etapa lenta em valores de pH superiores a 5). A formacao da carbinolamina e susceptivel a catalise acida geral, efetuada pelo ion hidronio e pelos carboxilicos, enquanto que a desidratacao da carbinolamina e catalisada somente pelo ion hidronio

Semicarbazonas heterociclicas: 2. Atividade antimicrobiana / Heterocyclic semicarbazones: 2. Antimicrobial activity

O estudo da atividade antimicrobiana de nove semicarbazonas heterociclicas foi efetuado atraves de tres metodos, ineditos para estes compostos nas condicoes em que foram efetuados. No metodo da diluicao seriada em meio liquido utilizaram-se Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans e Aspergillus niger como microorganismos testes, ao passo que no metodo da difusao em meio solido utilizaram-se apenas Staphylococcus aureus, Escherichia coli e Candida albicans. Verificou-se que a atividade dos compostos foi muito baixa quando comparada com a 5-nitro-2-furanocarboxaldeidos semicarbazona, de atividade anteriormente comprovada. Pelo metodo da bioautografia verificou-se que das nove semicarbazonas ensaiadas, seis inibiram o crescimento do Cladosporium sphaerospermum

Semicarbazonas heterociclicas potencialmente antifungicas: 1. Preparacao e caracterizacao / Potentially antifungical heterocyclic semicarbazones: 1. Preparation and characterization

Com o objetivo de elucidar a estrutura de semicarbazonas heterociclicas potencialmente antifungicas, foram preparados quatro compostos desta classe. Eles foram analisados mediante espectrometria de infravermelho, ultravioleta e ressonancia magnetica protonica, que corresponderam as estruturas esperadas

Sobre los compuestos de coordinaciòn como agentes antitumorales: IV: acciòn sobre el radical superóxido / On coordination compounds as antitumorigenic agents: IV: action on superoxide radical

Como modelaciòn de la actividad protectora de la superoxidodismutasa, se estudiò cinéticamente el sistema O2 Cu (II) mediante la determinaciòn de seudoconstantes de velocidad en la reacciòn de 17 compuestos de algunas tio y semicarbazonas de cobre (II) con el radical superóxido. Se correlacionaron estas seudoconstantes de velocidad con la citotoxidad in vitro de los 17 compuestos, así como de cada familia de compuestos por separado. La mejor correlaciòn se logró en el caso de las semicarbazonas. Las tiosemicarbazonas, por su parte, resultaron ser las más citotóxicas. Se interpretan estos resultados a partir de las características del enlace quìmico