Abstract Background Various studies are ongoing related to the radioprotective agents. Herbal preparations are currently becoming popular because of their beneficial effects with fewer side effects compared to the synthetic/semi-synthetic medicines, and Nigella sativa oil (NSO) is only one of them. Objective To investigate NSO for its antioxidant effects on the heart tissue of rats exposed to ionizing radiation (IR). Methods Thirty six male albino Wistar rats, divided into four groups, were designated to group I (IR plus NSO group) that received both 5 Gray of gamma IR to total cranium and NSO; group II (IR alone group) that received IR plus saline, group III (control group of NSO) that received saline and did not receive NSO or IR; group IV (control group) that received only sham IR. Alterations in Total antioxidant status (TAS) and Total oxidant status (TOS), Oxidative stres index (OSI), Sulhydryl group (SH), Lipid hydroperoxide (LOOH), Paraoxonase (PON) levels, Arylesterase (ARE) and Ceruloplasmin (CER) activities in homogenized heart tissue of rats were measured by biochemical methods. Results In heart tissue of the rats in the IR alone group (group II) LOOH, TOS and OSI levels were found to be higher, ARE activity and TAS level were found to be lower than all of the other groups (p < 0.01). These results also support that IR increases oxidative stress and NSO's protective effect. Conclusion NSO would reduce the oxidative damage in the irradiated heart tissue in the experimental rat model.

Abstract Obesity is one of the main health problems associated with a range of diseases. Genetic disposition is related to the risk for obesity but external conditions such lifestyle also increase the incidence. Current COVID-19 pandemic conditions around the globe have been reported to increase the cases of Type-2 diabetes mellitus (T2DM) due to prolonged sedentary life. Among the various treatment modalities, applications of α-amylase inhibitors are commonly used worldwide. Commercially available anti-diabetic drugs are potent inhibitors of α-amylase that reduce postprandial hyperglycemia. In this study, α-amylase inhibition efficiencies of some 1,2,4-triazole derivatives were evaluated. Furthermore, it has been attempted to determine the possible inhibition mechanism of the strongest inhibitor compound among the 8 candidate molecules for α-amylase. Compound VII showed the strongest inhibition on α-amylase activity with low IC50 value (150 µM). An inhibitory kinetic analysis on α-amylase activity by Compound VII was found to be reversible and uncompetitive. Furthermore, molecular docking studies with this molecule showed that it could bind to the catalytic site of the enzyme by performing weak interactions with Ser56, Tyr59, Tyr62, Asp176, Asp274 and Leu142 residues. Cytotoxic potential of Compound VII on amylase overexpressing AR42J pancreatic cancer cells was also performed using trypan blue staining and the compound at the highest dose 10 µM was found to be cytotoxic, but effective for alpha amylase inhibition at non-cytotoxic doses. The results showed in vitro effect of Compound VII on alpha-amylase inhibition in cells. Here, we suggest an alternative and non-cytotoxic α-amylase inhibitor for T2DM.

ABSTRACT Introduction: Head and neck cancer patients treated with radiotherapy suffer severe side-effects during and following their treatment. Efforts to decrease toxicity of irradiation to normal tissue, organs and cells have led to a search for cytoprotective agent. Investigations for effective and non-toxic compounds with radioprotective capability led to increasing interest in antioxidant such as thymoquinone (TQ). Objective: The aim of this study was to evaluate the radioprotective effects of TQ on oxidant/antioxidant systems in the tongue-tissue of rats exposed to total cranial irradiation. Materials and Methods: Thirty-two rats were divided into four groups to test the radioprotective effectiveness of TQ administered by either orogastric tube or intraperitoneal injection. Appropriate control groups were also studied. Results: Tongue glutathione peroxidase (GSH-Px), glutathione-S-transferase (GST), total superoxide scavenger activity (TSSA), non-enzymatic superoxide scavenger activity (NSSA), and superoxide dismutase (SOD) activities in the control and sham control groups were significantly increased when compared to the irradiation (IR) group and IR plus TQ groups. Nitric oxide (NO•), peroxynitrite (ONOO–) and malondialdehyde (MDA) levels, xantine oxidase (XO) and nitric oxide synthase (NOS) activities significantly increased in the IR group when compared to the control and sham control groups. Conclusion: Results show that TQ has the radioprotective, antioxidant effects and free radical scavenging activity. Therapy with antioxidants may lead to the increase in the antioxidant defense system and thus, may decrease the clinical symptoms in radiation therapy.

RESUMEN Introducción: Los pacientes con cáncer de cuello y cabeza tratados con radioterapia sufren efectos secundarios severos durante y después de su tratamiento. Los esfuerzos por disminuir la toxicidad de la irradiación al tejido normal, los órganos y las células han llevado a la búsqueda de un agente citoprotector. Las investigaciones en busca de compuestos eficaces y no tóxicos con capacidad radioprotectora llevó a un creciente interés en antioxidantes tales como la timoquinona (TQ). Objetivo: El objetivo de este estudio fue evaluar los efectos radioprotectores de la TQ en sistemas oxidantes/antioxidantes en el tejido de la lengua de las ratas expuestas a radiación craneal total. Materiales y métodos: Treinta y dos ratas fueron divididas en cuatro grupos para probar la efectividad radioprotectora de TQ administrada por inyección intraperitoneal o tubo orogástrico. También se estudiaron los grupos de control apropiados. Resultados: La actividad en lengua del glutatión peroxidasa (GSH-Px), glutatión-S-transferasa (GST), la actividad total de barrido de superóxido (ATBS), la actividad no enzimática de barrido de superóxido (ANBS), y las actividades del superóxido dismutasa (SOD) en los grupos de control y control simulado fueron significativamente mayores en comparación con el grupo de irradiación (IR) y los grupos de IR más TQ. Los niveles del óxido nítrico (NO), el peroxinitrito (ONOO-) y el malondialdehído (MDA), las actividades de la xantina oxidasa (XO) y el la sintasa de óxido nítrico (NOS) aumentaron signifi-cativamente en el grupo de IR en comparación con los grupos de control y control simulado. Conclusión: Los resultados muestran que TQ tiene efectos radioprotectores y antioxidantes y posee una actividad de barrido de radicales libres. La terapia con antioxidantes puede conducir al aumento en el sistema de defensa antioxidante, y así disminuir los síntomas clínicos en la radioterapia.