RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The tea made with the fruits of Luffa operculata (L.) Cogn. (Cucurbitaceae; EBN) is popularly used as abortive. AIM OF THE STUDY: The present work aimed at accessing how the exposition of female Wistar rats to 1.0 mg/kg of EBN (experimental group, EG), or distilled water (control group, CG), by gavage, at gestational days (GD) 17-21 interfered with the reproductive performance, and with dams' behavior after weaning. MATERIALS AND METHODS: At post-natal day 2 (PND2), the number of male and female pups was evaluated, as well as their weight. After weaning (PND21), dams were euthanized, and their liver and kidneys were removed for histological and biochemical analyses, while the blood was used in the evaluation of cytokines IL-1α, IL-1ß, IL-6 and TNF-α, corticosterone, adrenocorticotrophic hormone, melatonin, AST, ALT and creatinine levels. RESULTS AND DISCUSSION: Dams that were treated with EBN showed an anxiety-like behavior, weight loss at the end of gestation and weight gain at weaning, accompanied with a significant decrease in pro-inflammatory cytokines and in the melatonin level. No significant histological or biochemical alterations have occurred in the liver or kidneys. The number of female pups was significantly higher in the EG. The male pups showed weight gain at PND60. CONCLUSION: The presence of cucurbitacins is probably involved in the dysregulations that were found, due to their polycyclic steroid triterpene structure.
Assuntos
Citocinas/sangue , Luffa/química , Melatonina/sangue , Extratos Vegetais/farmacologia , Administração Oral , Hormônio Adrenocorticotrópico/sangue , Animais , Animais Recém-Nascidos , Comportamento Animal/efeitos dos fármacos , Peso Corporal/efeitos dos fármacos , Corticosterona/sangue , Cucurbitacinas/química , Cucurbitacinas/farmacologia , Cucurbitacinas/toxicidade , Feminino , Frutas/química , Hormônios/sangue , Rim/efeitos dos fármacos , Rim/patologia , Fígado/efeitos dos fármacos , Masculino , Exposição Materna , Extratos Vegetais/administração & dosagem , Extratos Vegetais/toxicidade , Gravidez , Efeitos Tardios da Exposição Pré-Natal , Ratos Wistar , Reprodução/efeitos dos fármacos , Caracteres SexuaisRESUMO
Assembly of cucurbitacin inspired estrone analogs has been previously synthesized and screened against melanoma cell lines. Further synthetic optimization was executed via installation of Azide polar functional moiety across 23, 24 α, ß-unsaturated ketone side chain using Michael addition reaction. This was followed by biological screening against melanoma cell lines employing MTT assay, in-cell-based ELISA assay, and Western blot analysis to monitor the potential of the synthesized analogs to inhibit the phosphorylated ERK levels. This resulted in evolution of MH-4 possessing IC50 of 3.59 µm with significant decrease in the p-ERK and targeting MAPK pathway.
Assuntos
Cucurbitacinas/toxicidade , Estrona/toxicidade , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Sítios de Ligação , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Cucurbitacinas/química , Cucurbitacinas/metabolismo , Ensaio de Imunoadsorção Enzimática , Estrona/análogos & derivados , Estrona/metabolismo , Humanos , Proteína Quinase 1 Ativada por Mitógeno/análise , Proteína Quinase 1 Ativada por Mitógeno/metabolismo , Proteína Quinase 3 Ativada por Mitógeno/análise , Proteína Quinase 3 Ativada por Mitógeno/metabolismo , Simulação de Acoplamento Molecular , Fosforilação , Estrutura Terciária de Proteína , Proteínas Proto-Oncogênicas B-raf/química , Proteínas Proto-Oncogênicas B-raf/metabolismoRESUMO
Análise de Investigação sobre a presença de cucurbitacinas em abobrinhas de tronco redondas (cucurbita pepo l.) e sua relação com casos de intoxicação alimentar. (AU)