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Shawqi H Alawdi,1,2 Housam Eidi,3 Marwa M Safar,4,5 Mosaad A Abdel-Wahhab6 1Department of Pharmacology, Faculty of Medicine and Health Sciences, Thamar University, Dhamar, Yemen; 2Department of Pharmacy Practice, Faculty of Pharmacy, University of Science and Technology, Sana’a, Yemen; 3Department of Ophthalmology and Visual Sciences, University of British Columbia, Vancouver, Canada; 4Pharmacology and Toxicology Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 5Pharmacology and Biochemistry Department, Faculty of Pharmacy, The British University in Egypt, El Shorouk, Egypt; 6Department of Food Toxicology and Contaminants, National Research Center, Cairo, EgyptCorrespondence: Shawqi H AlawdiDepartment of Pharmacology, Faculty of Medicine, Thamar University, Sana’a Street, Dhamar, YemenTel +967-777498977Email shawqialawdi@yahoo.comBackground: Diamond nanoparticles (Nanodiamond) are biocompatible drug delivery platforms with outstanding surface properties. Their passage into the brain has been confirmed previously. Thus, nanodiamond could provide a drug delivery system to shuttle several drugs through the blood-brain barrier (BBB) which represents a real challenge for the effective delivery of several drugs into the brain. Amlodipine is a calcium channel blocker that cannot pass through BBB and may elicit neuroprotective effects to reverse calcium-induced excitotoxicity and mitochondrial dysfunction that underlie several neurologic disorders including Alzheimer’s disease and stroke.Aim: The study aimed to investigate the loading of amlodipine on nanodiamond particles.Methods: Nanodiamond particles were oxidized in a strong oxidizing acidic mixture of sulfuric and nitric acids. Adsorption of amlodipine on nanodiamond particles was achieved in alkaline pH using various concentrations of sodium hydroxide. The loaded amlodipine was determined by high-performance liquid chromatography and confirmed by Fourier transform infrared (FTIR) spectroscopy and transmission electron microscopy.Results: The highest percentage (41%) of loaded amlodipine onto nanodiamond particles was achieved in alkaline medium using 2 mM NaOH at a corresponding pH of 8.5. Also, characteristic FTIR bands of amlodipine and nanodiamond were shown obviously in the nanodiamond–amlodipine conjugates. Moreover, the successful loading of amlodipine on diamond nanoparticles was confirmed by transmission electron microscopy.Conclusion: The present study demonstrates the successful loading of amlodipine onto nanodiamond particles. These findings offer a potential for applying diamond nanoparticles as a drug delivery system to shuttle amlodipine into the brain and open the door to deliver other similar drugs into the brain.Keywords: diamond nanoparticles, nanodiamond, amlodipine, calcium channel antagonists, drug delivery system, blood-brain barrier, excitotoxicity

The aim of this study was to prepare Eudragit Retard L (Eudragit RL) nanoparticles (ENPs) and to determine their properties, their uptake by the human THP-1 cell line in vitro and their effect on the hematological parameters and erythrocyte damage in rats. ENPs showed an average size of 329.0 ± 18.5 nm, a positive zeta potential value of +57.5 ± 5.47 mV and nearly spherical shape with a smooth surface. THP-1 cell lines could phagocyte ENPs after 2 h of incubation. In the in vivo study, male Sprague-Dawley rats were exposed orally or intraperitoneally (IP) with a single dose of ENP (50 mg/kg body weight). Blood samples were collected after 4 h, 48 h, one week and three weeks for hematological and erythrocytes analysis. ENPs induced significant hematological disturbances in platelets, red blood cell (RBC) total and differential counts of white blood cells (WBCs) after 4 h, 48 h and one week. ENP increased met-Hb and Co-Hb derivatives and decreased met-Hb reductase activity. These parameters were comparable to the control after three weeks when administrated orally. It could be concluded that the route of administration has a major effect on the induction of hematological disturbances and should be considered when ENPs are applied for drug delivery systems.

Food commodities such as cereals are subjected to spoilage and bio-deterioration during storage by mycotoxigenic fungi such as Aspergillus flavus. Efforts are done to biologically control toxigenic A. flavus and subsequently prevent or at least minimize its aflatoxin production ability, without the need of using synthetic fungicides. Antifungal activity of corn and rice seed-borne mycoflora was tested against aflatoxigenic A. flavus in vitro, using bioassays such as dual culture technique; ability to produce volatile and non-volatile metabolites; ability to inhibit germination and reduce germ tube length of A. flavus conidia; in vivo reduction of aflatoxins level in corn seeds co-inoculated with the pathogen and antagonists. Penicillum crustosum, Aspergillus giganteus, Fusarium verticillioides and Aspergillus fumigatus isolates showed promising antifungal activities and varying efficiencies of reducing aflatoxins level; however, only A. fumigatus isolate was non-aflatoxigenic. It could be concluded that A. fumigatus could be used effectively as a biopreservative to increase shelf life of cereals during storage, but after testing its tendency to produce other mycotoxins or causing human Aspergillosis.

International audience; The aim of this study was to prepare Eudragit Retard L (Eudragit RL) nanoparticles (ENPs) and to determine their properties, their uptake by the human THP-1 cell line in vitro and their effect on the hematological parameters and erythrocyte damage in rats. ENPs showed an average size of 329.0 +/- 18.5 nm, a positive zeta potential value of +57.5 +/- 5.47 mV and nearly spherical shape with a smooth surface. THP-1 cell lines could phagocyte ENPs after 2 h of incubation. In the in vivo study, male Sprague-Dawley rats were exposed orally or intraperitoneally (IP) with a single dose of ENP (50 mg/kg body weight). Blood samples were collected after 4 h, 48 h, one week and three weeks for hematological and erythrocytes analysis. ENPs induced significant hematological disturbances in platelets, red blood cell (RBC) total and differential counts of white blood cells (WBCs) after 4 h, 48 h and one week. ENP increased met-Hb and Co-Hb derivatives and decreased met-Hb reductase activity. These parameters were comparable to the control after three weeks when administrated orally. It could be concluded that the route of administration has a major effect on the induction of hematological disturbances and should be considered when ENPs are applied for drug delivery systems.

International audience; Aim: The aim of this study was to evaluate the effects of Panax ginseng extract standardized with ginsenoside Rg3 (PGRg3) on the mating behavior of sexually active or inactive male rats treated with dopamine antagonists. Methodology: Animals were treated with PGRg3 (50,150 and 450mg/kgb.w) with or without dopamine antagonists. The penile erection, motor activity and stretching-yawning episode were evaluated in animals treated with PGRg3 alone or in combination with lisurode or SND 919. Testosterone and sperm counts were also evaluated in different treatment groups. Results: The results showed that (-) Eticlopride counteracted PGRg3-induced penile erection but not motor hyperactivity. PGRg3 treatment enhanced lisuride-induced behavioral effects. Moreover, PGRg3 plus SND 919 showed a marked stretching-yawning behavior compared to the animals received SND 919 alone. PGRg3 also succeeded to increase testosterone level and sperm count in a dose dependent fashion. Conclusion: It could be concluded that DAD2 receptors are involved in PGRg3-induced mating behavior and testicular function improvement. PGRg3 could be used to improve sexual function and mating behavior in people suffering from erectile dysfunction.

International audience; In traditional medicine, Panax ginseng has been used to treat various behavioral effects. However, a little is known about the effect of ginsenoside Rg3, the most ingredients in panax ginseng, on male copulatory and sexual behavior. The aim of the current study was to investigate the effect of panax ginseng extract standardized with ginsenoside Rg3 (PGRg3) on general mating behaviour, libido, potency and the adverse effects in normal male Sprague-Dawley rats. Four tests were carried out to evaluate different sexual parameters. Male rats were divided into different groups in each test and treated with different doses of PGRg3 (50, 250 and 500 mg/kg b.w.) and Sildenafil citrate (5 mg/kg b.w). Female rats with oestrus phase were used to analyze the mating behavior.The results indicated that PGRg3 significantly increased mounting frequency, intromission frequency, ejaculatory latency in the first and second series, erection, quick flips, long flips and aggregate of penile reflexes. Whereas, it significantly decreases mounting latency, intromission latency and post ejaculatory intervals in dose dependent manner. Moreover, PGRg3 was found to be devoid of any conspicuous gastric ulceration and any other adverse effects. PGRg3 extract at the higher dose (500 mg/kg b.w.) was comparable to the standards drug Sildenafil citrate with regards to all the tested parameters. It could be concluded that PGRg3 extract produced a significant and sustained increase in the sexual activity of normal male rats without any conspicuous gastric ulceration and adverse effects. The most important conclusion is that the resultant aphrodisiac effectively of PGRg3 extract lends support to the claims for its traditional usage in sexual disorders.

This study aimed to determine the total phenols and DPPH scavenging properties of aqueous (AE) and ethanolic (EE) extracts of papaya fruits in vitro and to evaluate their hepatoprotective effects against aflatoxicosis in vivo. Sixty female Sprague-Dawley rats were divided into six groups and treated for 4 weeks including the control group, the group fed aflatoxins-contaminated diet (2 mg/ kg diet); the group treated orally with EE (250 mg/kg b.w); the group treated orally with AE (250 mg/ kg b.w); the groups fed AFs-contaminated diet and treated with EE or AE. At the end of the treatment period, blood and liver samples were collected for biochemical, histological and histochemical study. The results revealed that AE has higher total phenol content and DPPH scavenging activity if compared to EE. The in vivo results indicated that animals fed AFs-contaminated diet showed significant biochemical, histological and histochemical changes typical to those reported in the literature. Animals treated with the extracts and AFs showed a significant improvement in all biochemical parameters, histological and histochemical picture of the liver. This improvement was more pronounced in the group treated with AE. It could be concluded that papaya fruits can be used as a functional dietary ingredient to reduce hepatotoxicity., This study aimed to determine the total phenols and DPPH scavenging properties of aqueous (AE) and ethanolic (EE) extracts of papaya fruits in vitro and to evaluate their hepatoprotective effects against aflatoxicosis in vivo. Sixty female Sprague-Dawley rats were divided into six groups and treated for 4 weeks including the control group, the group fed aflatoxins-contaminated diet (2 mg/ kg diet); the group treated orally with EE (250 mg/kg b.w); the group treated orally with AE (250 mg/ kg b.w); the groups fed AFs-contaminated diet and treated with EE or AE. At the end of the treatment period, blood and liver samples were collected for biochemical, histological and histochemical study. The results revealed that AE has higher total phenol content and DPPH scavenging activity if compared to EE. The in vivo results indicated that animals fed AFs-contaminated diet showed significant biochemical, histological and histochemical changes typical to those reported in the literature. Animals treated with the extracts and AFs showed a significant improvement in all biochemical parameters, histological and histochemical picture of the liver. This improvement was more pronounced in the group treated with AE. It could be concluded that papaya fruits can be used as a functional dietary ingredient to reduce hepatotoxicity. Avaliação das propriedades radicais de limpeza e o papel protetor deextratos de frutos de mamão contra o estresse oxidativo em ratosalimentados com dieta contaminada com aflatoxinas.ResumoEste estudo teve como objetivo determinar o teor de fenóis e propriedades de remoção deDPPH em extratos aquosos (AE) e etanólicos (EE) de frutos de mamão in vitro e avaliar seus efeitoshepatoprotetores contra aflatoxicose in vivo. Sessenta fêmeas Sprague-Dawley foram divididas emseis grupos e foram tratadas durante 4 semanas, sendo o grupo de controle, o grupo alimentadocom a dieta contaminada com aflatoxinas-(2 mg / kg de dieta), o grupo tratado oralmente comEE (250 mg / kg de peso corporal); o grupo tratado por via oral com AE (250 mg / kg de pesocorporal), os grupos alimentados com dieta AFS contaminado e tratado com EE ou AE. No finaldo período de tratamento, as amostras de sangue e do fígado foram colhidas para estudosbioquímicos, histológicos e histoquímicos. Os resultados revelaram que AE tem maior teor defenóis totais e atividade DPPH se comparado a EE. Os resultados in vivo indicaram que os animaisalimentados com a dieta AFs contaminado mostraram significativas alterações bioquímicas,histológicas e histoquímicas, típicas dos relatos na literatura. Os animais tratados com os extratose AFS apresentaram uma melhora significativa em todos os parâmetros bioquímicos, quadrohistológico e histoquímico do fígado. Esta melhoria foi mais pronunciada no grupo tratado com AE.Pode-se concluir que os frutos de mamoeiro podem ser usados como um ingrediente funcional nadieta para reduzir a hepatoxicidade.

The current study was conducted to evaluate the protective effects of Panax ginseng extract (PGE)against the toxicity and oxidative stress in rats fed aflatoxin (AFs) and/or fumonisin (FB)-contaminateddiet. Eighty female Sprague-Dawley rats were divided into eight experimental groups included thecontrol group, the group treated orally with PGE (0.5 mg/kg b.w.) and the groups fed AFs (1.4 mg/kg diet) and/or FB (20 mg/kg b.w.) contaminated diet alone or plus PGE for 11 weeks. Blood, liverand kidney tissue samples were collected at the end of treatment period for biochemical andhistological studies. The results indicated that PGE increased super oxide dismutase (SOD) levelin liver; however, the other parameters were comparable to controls. Animals fed AFs and/or FBcontaminateddiet showed a significant increase in serum biochemical parameters and oxidativestress markers accompanied with a significant decrease in antioxidant parameters levels and asevere histological changes in the liver tissue. These changes were more pronounced in the groupfed AFs plus FB. PGE succeeded to induce a significant improvement in all biochemical parametersand the histological picture towards the control although it did not normalize them. It could beconcluded that PGE is a promise candidate against the exposure to multi-mycotoxins in food., O presente estudo foi conduzido para avaliar os efeitos protetores do extrato de Panax ginseng(PGE) contra a toxicidade e estresse oxidativo em ratos alimentados com aflatoxinas (AFs) e/oudieta contaminada por fumonisina (FB). Oitenta fêmeas de ratos Sprague-Dawley foram divididasem oito grupos experimentais, incluindo o grupo controle, o grupo tratado com PGE oralmente (0,5mg/kg de peso corporal) e os grupos alimentados com as dietas contaminadas de AFs (1,4 dieta mg/kg) e/ou FB (20 mg/kg de peso corporal) isoladas ou com mais PGE durante 11 semanas. Amostrasde sangue, do fígado e do tecido do rim foram recolhidas no final do período de tratamentopara estudos bioquímicos e histológicos. Os resultados indicaram que a PGE aumenta o nível desuperóxido dismutase (SOD) no fígado, no entanto, os outros parâmetros foram comparáveis aosdo grupo controle. Animais alimentados com dieta contaminada por AF e/ou FB mostraram umaumento significativo nos parâmetros bioquímicos séricos e marcadores de estresse oxidativo,acompanhados de uma diminuição significativa nos níveis de antioxidantes e nos parâmetros dealterações histológicas graves no tecido do fígado. Essas alterações foram mais pronunciadas nogrupo alimentado com AFs mais FB. PGE obteve sucesso quanto à introdução de uma melhoriasignificativa em todos os parâmetros bioquímicos e histológicos com relação ao grupo controle,embora não os tenha normalizado. Pode-se concluir que a PGE é uma promissora candidatacontra a exposição às multimicotoxinas em alimentos.