Synthesis and preliminary assessment of the anticancer and Wnt/β-catenin inhibitory activity of small amide libraries of fenamates and profens

As part of an ongoing program to study the anticancer activity of non-steroidal anti-inflammatory drugs (NSAIDs) through generating diversity libraries of multiple NSAID scaffolds, we synthesized a series of NSAID amide derivatives and screened these sets against three cancer cell lines (prostate, colon and breast) and Wnt/β-catenin signaling. The evaluated amide analog libraries show significant anticancer activity/cell proliferation inhibition, and specific members of the sets show inhibition of Wnt/β-catenin signaling.</p

A Sub-Acute Dosing Study of Saxitoxin and Tetrodotoxin Mixtures in Mice Suggests That the Current Paralytic Shellfish Toxin Regulatory Limit Is Fit for Purpose.

Paralytic shellfish poisoning is a worldwide problem induced by shellfish contaminated with paralytic shellfish toxins. To protect human health, a regulatory limit for these toxins in shellfish flesh has been adopted by many countries. In a recent study, mice were dosed with saxitoxin and tetrodotoxin mixtures daily for 28 days showing toxicity at low concentrations, which appeared to be at odds with other work. To further investigate this reported toxicity, we dosed groups of mice with saxitoxin and tetrodotoxin mixtures daily for 21 days. In contrast to the previous study, no effects on mouse bodyweight, food consumption, heart rate, blood pressure, grip strength, blood chemistry or hematology were observed. Furthermore, no histological findings were associated with dosing in this trial. The dose rates in this study were 2.6, 3.8 and 4.9 times greater, respectively, than the highest dose of the previous study. As rapid mortality in three out of five mice was observed in the previous study, the deaths are likely to be due to the methodology used rather than the shellfish toxins. To convert animal data to that used in a human risk assessment, a 100-fold safety factor is required. After applying this safety factor, the dose rates used in the current study were 3.5, 5.0 and 6.5 times greater, respectively, than the acute reference dose for each toxin type set by the European Union. Furthermore, it has previously been proposed that tetrodotoxin be included in the paralytic shellfish poisoning suite of toxins. If this were done, the highest dose rate used in this study would be 13 times the acute reference dose. This study suggests that the previous 28-day trial was flawed and that the current paralytic shellfish toxin regulatory limit is fit for purpose. An additional study, feeding mice a diet laced with the test compounds at higher concentrations than those of the current experiment, would be required to comment on whether the current paralytic shellfish toxin regulatory limit should be modified.fals

Extrato etanólico de Senna alata no controle de Fusarium oxysporum, causador da murcha-de-fusarium do meloeiro

A murcha-de-fusarium, causada pelo fungo Fusarium oxysporum, vem-se tornando uma doença importante no meloeiro devido às grandes perdas em áreas de produção no Brasil e no mundo, razão pela qual o objetivo do presente trabalho foi avaliar a eficácia de extratos etanólicos de partes de Senna alata no controle do crescimento micelial de F. oxysporum isolado de plantas de meloeiro. O delineamento experimental foi inteiramente casualizado, distribuído em esquema fatorial 4 x 6 + 1, sendo o primeiro fator partes da planta (caule, folha, raiz e vagem) e, como segundo, seis concentrações (0,25; 0,50; 50; 75; 250; 500 µg mL-1) mais a testemunha, com quatro repetições por tratamento. As variáveis avaliadas foram: taxa de crescimento micelial inibição do crescimento micelial e área abaixo da curva do crescimento micelial. Extratos etanólicos de todas as partes de Senna alata foram eficazes no controle de F. oxysporum. Extratos de raiz e vagem foram os mais eficientes em inibir o crescimento micelial de F. oxysporum, na concentração 500 µg mL-1.Fusarium wilt, caused by Fusarium oxysporum fungi has become an important melon disease, due to great losses in the production areas in Brazil and in the world. Therefore, the objective of the present work was to evaluate efficacy of ethanolic extracts of Senna alata parts in the control of F. oxysporum micelial growth, isolated of melon plants. The experimental design was entirely randomized distributed in factorial scheme 4 x 6 + 1, being the first factor parts of the plant (stalk, leaf, root, and green bean), and as second, six concentrations (0.25; 0.50, 50, 75, 250, 500 µg mL-1), plus the control, with four repetitions per treatment. The variables evaluated were: rate of mycelial growth, inhibition of the mycelial growth (IGM) and area under the curve of the mycelia growth. Ethanolic extracts of all Senna alata parts were efficient in control of F. oxysporum. Extracts of root and string bean were most efficient in inhibiting the mycelial growth of F. oxysporum, in 500 µg mL-1 concentration

Dietary supplementation of Zingiber officinale and Zingiber zerumbet to heat-stressed broiler chickens and its effect on heat shock protein 70 expression, blood parameters and body temperature

The present study was conducted to assess the effects of dietary supplementation of Zingiber officinale and Zingiber zerumbet and to heat-stressed broiler chickens on heat shock protein (HSP) 70 density, plasma corticosterone concentration (CORT), heterophil to lymphocyte ratio (HLR) and body temperature. Beginning from day 28, chicks were divided into five dietary groups: (i) basal diet (control), (ii) basal diet +1%Z. zerumbet powder (ZZ1%), (iii) basal diet +2%Z. zerumbet powder (ZZ2%), (iv) basal diet +1%Z. officinale powder (ZO1%) and (v) basal diet +2%Z. officinale powder (ZO2%). From day 35-42, heat stress was induced by exposing birds to 38±1°C and 80% RH for 2 h/day. Irrespective of diet, heat challenge elevated HSP70 expression, CORT and HLR on day 42. On day 42, following heat challenge, the ZZ1% birds showed lower body temperatures than those of control, ZO1% and ZO2%. Neither CORT nor HLR was significantly affected by diet. The ZO2% and ZZ2% diets enhanced HSP70 expression when compared to the control groups. We concluded that dietary supplementation of Z. officinale and Z. zerumbet powder may induce HSP70 reaction in broiler chickens exposed to heat stress

A Biosecurity Tool: High-Intensity, Pulsed Polychromatic Light and UV-C Treatments of Oil Palm Pollen and Spores of Fusarium oxysporum f. sp. elaeidis

The movement of oil palm (Elaeis guineensis) pollen as a germplasm material between oil palm-growing countries for the purposes of plant-breeding programs is common in West Africa, Southeast Asia, and South America. Reports of pollen contamination with Fusarium oxysporum f. sp. elaeidis (Foe), the causal agent of Fusarium wilt disease for oil palm, heightened the need for an operational decontamination technique for oil palm pollen prior to export. In this study, high-intensity, pulsed polychromatic light (HIPPL) and conventional UV (UV-C) were used as decontamination tools to treat Foe spores and oil palm pollen. We combined qualitative studies for HIPPL- and UV-C-treated Foe spores and quantitative studies for treated pollen. The study showed that despite UV-C and HIPPL successfully controlling Foe, oil palm pollen had reduced viability or was inviable upon exposure to various doses of UV-C and HIPPL sources. The effects of UV-C at doses of 2.5, 5, and 10 kJ/m2 and HIPPL at 10, 20, and 40 pulses were determined for oil palm pollen and Foe germination. UV-C doses of 10 kJ/m2 and 40 pulses of HIPPL showed significant reduction in germination of oil palm pollen but had no adverse effect on Foe viability. At 60 kJ/m2 of UV-C and 240 pulses of HIPPL, Foe was inviable, and pollen could not germinate. [Graphic: see text] Copyright © 2022 The Author(s). This is an open access article distributed under the CC BY 4.0 International license