Sinteza 1-acil-2-alkiltio-1,2,4-triazolobenzimidazola s antimikotskim, protuupalnim i analgetskim učinkom

Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo[2,3-a]benzimidazole-2-thione intermediate reacted with one equivalent of the appropriate respective alkyl halide to give the corresponding 2-alkylthio derivative 3a-g. The latters were acylated to afford the 1-acyl-2-alkylthio-1,2,4-triazolo[2,3-a]-benzimidazole derivatives 4-10 in good yields. Structures of the new compounds were verified on the basis of spectral and elemental methods of analyses. Fourteen of the prepared compounds were tested for their possible antifungal activities. Most of the tested compounds showed activity against Candida albicans and Fusarium oxysporum comparable to that of fluconazole as a reference drug. Compounds 8a, 9a, and 10d are the most active ones against most of the used fungi. Compounds 3e, 4d, 5d, 6d, 7d, 8c, 8d, 9d, and 10d were tested for their anti-inflammatory and analgesic effects; most of these compounds showed potent and significant results compared to indomethacin. Moreover, ulcerogenicity and the median lethal dose (LD50) of the most active compound 8d were determined in mice; LD50 was found to be 275 mg kg-1 (i.p.).Sintetizirani su novi derivati 1,2,4-triazolo[2,3-a]benzimidazola reakcijom 1,2-diaminobenzimidazola s ugljičnim disulfidom. Nastali 1,2,4-triazolo[2,3-a]benzimidazol-2-tioni reagiraju s jednim ekvivalentom odgovarajućeg alkil halida pri čemu nastaju 2-alkiltio derivati 3a-g. Acilacijom produkata 3 dobiveni su derivati 1-acil-2-alkiltio-1,2,4-triazolo[2,3-a]-benzimidazola 4-10 u dobrim iskorištenjima. Strukture novih spojeva potvrđene su spektroskopskim metodama i elementarnom analizom. Ispitivano je antimikotsko djelovanje 14 priređenih spojeva, uz flukonazol kao poredbenu tvar. Većina testiranih spojeva djeluje na Candida albicans i Fusarium oxysporum slično kao flukonazol. Najaktivniji su bili spojevi 8a, 9a i 10d. Produkti 3e, 4c, 5c, 6c, 7c, 8b, 8c, 9c i 10c ispitani su na protuupalno i analgetsko djelovanje, uz indometacin kao poredbenu tvar. Većina spojeva ima značajno djelovanje. Najaktivniji spoj testiran je na ulcerogenost. Srednja letalna doza (LD50) određena je na miševima i iznosi 275 mg kg-1 (i.p.)

Cancer in Children at El Obeid Hospital, Western Sudan.

Background: Cancers form one of the major causes of death in children. They differ markedly from adult cancers in their nature, distribution and prognosis. Objectives: To determine the pattern of childhood cancer at El Obeid Hospital, Western Sudan. Patients and Methods: The records of all patients admitted with cancer aged 15 years and below tothe wards of El Obeid Hospital, Western Sudan over two years were studied. The cancers were classified according to the organs affected and then ranked in their order of relative frequency. The mean age, age range, gender and the relative frequency rates were calculated. Results: There were 40 newly diagnosed childhood cancer patients during the study period. Males were 29 patients (72.5%). The age ranged three months to 14 years. Leukaemias were the most common malignancy in both sexes, followed by bone tumours and then nephroblastoma.Conclusions: Cancers in children were seen at Western Sudan, and cases admitted to hospital only reflect the tip of the iceberg as many cases were directly referred to Oncology Hospitals. Establishment of a local radiation and isotopes centre is needed in this part of the country to provide oncology services and to integrate preventive programs.Key words: Acute lymphocytic leukaemia, osteosarcoma, nephroblastoma, Western Sudan

Prediction of preterm birth by evaluating the fetal adrenal gland volume and blood flow: a pilot study

Background: The aim of the current study was to estimate the risk of preterm birth (delivery < 37 weeks of gestation) by evaluating the fetal adrenal gland volume and blood flow at Women’s Health Hospital, Assiut University, Egypt.Methods: A pilot prospective cohort study included pregnant women presented to our hospital with threatened preterm labor between December 2016 and May 2018. All women were recruited consecutively at the emergency unit of Women’s Health Hospital at Assiut University. The fetal adrenal gland volume was assessed using 3-dimensional images of the fetal adrenal with the aid of Virtual Organ Computer-Aided Analysis (VOCAL) software. Doppler evaluation of the fetal adrenal blood vessels was carried out. The RI, PI and S/D ratio was calculated for every case. The neonatal outcomes at delivery were assessed and compared with respect to the duration of actual delivery from the time of evaluation. The obtained data were analyzed by SPSS software (version 22.0) and p<0.05 was taken as the significant level.Results: The study included 30 pregnant women at the final analysis. Women were classified according to the time of actual delivery into two groups. Group (I, n=13) those who delivered within 7 days and group (II, n=17) those who delivered 7 days or more. No difference between both groups regarding the baseline characteristics. No difference regarding the mode of delivery (p=0.708). All Doppler indices were statistically in-different between both groups. The fetal adrenal gland volume was significantly lower in group II than group I (p=0.001). On ROC analysis, the area under the curve (AUC) for prediction of preterm birth based on the fetal adrenal gland volume was (AUC= 0.873). The ROC curve shows that the best cut off value using the volume was ≥0.461 with 76.92% sensitivity and 88.24% specificity for prediction of preterm birth with an overall accuracy of 83.3%.Conclusions: Fetal adrenal gland volume was identified as a significant predictor of delivery in pregnant women who had spontaneous preterm births with intact membranes

First-trimester rupture of a scarred uterus after use of sublingual misoprostol: a case report

Uterine rupture is a disastrous obstetric complication, occurring mostly in the second and third trimesters. The risk of uterine rupture markedly increases with previous uterine surgeries. Termination of early pregnancy failure using misoprostol is common. However, its use in women with a scarred uterus is speculative and usually puts the obstetricians in a stressful situation. Here we present a case of rupture of a scarred uterus in the first trimester after sublingual misoprostol. A 35 years old multiparous woman presented with uterine rupture after administration of small doses of sublingual misoprostol for termination of early pregnancy failure. Immediate laparotomy was done and the defect was repaired. Termination of early pregnancy failure, in women with a scarred uterus, using sublingual misoprostol can lead to uterine rupture. Sublingual misoprostol should be used cautiously under close supervision or other routes (vaginal or oral) should be used instead

Copper(II)-Complexes of an Isatinic Quinolyl Hydrazone-Anion effect

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Establishment of Gypsophila paniculata root culture for biomass, saponin, and flavonoid production

Baby’s breath (Gypsophila paniculata L.) roots are valuable as pharmaceuticals due to the content of triterpenoid saponins and other bioactive phytochemicals. However, the long root harvest period and fluctuation of these constituent’s content are among the constraints to traditional agricultural production. The present study shows an efficient and reliable liquid root culture of G. paniculata cv. ‘Perfecta’ established in a shake flask system using different auxins, media, and sugars. Hairy root (HR) induction in G. paniculata through Rhizobium rhizogenes-mediated transformation was also investigated. α-Naphthaleneacetic acid (NAA) was optimized for adventitious roots (AR) biomass, saponin, and flavonoid production at 1 or 2 mg/L compared to IBA. Full strength Gamborg’s medium (B5) recorded higher saponin content; however, the highest yield of total saponin and total flavonoids was achieved by full strength Murashige and Skoog's (MS) medium. Sucrose was more essential for root growth and accumulated total saponins and flavonoids rather than fructose and glucose. Polymerase chain reaction (PCR) analysis showed that G. paniculata HR carried rolC gene of R. rhizogenes A4 strain in its genome but not virD2 gene. Compared to non-transformed root, saponin content of leaf and stem-derived HR was 2.7 and 2.3-fold, while total flavonoid content was 2.1 and 2.0-fold, respectively. The DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging activity was also higher in HR extracts than in non-transgenic roots. This study established an efficient protocol for G. paniculata root cultures for sustainable production of important natural saponins and flavonoids

Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical:improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats

Diabetes mellitus is a life-threatening metabolic disease. At the moment, there is no effective treatment available to combat it. In this study, we aimed to develop berberine-loaded bilosomes (BER-BLS) to boost the oral bioavailability and therapeutic efficacy of berberine, a natural antidiabetic medication. The BER-BLS was fabricated using a thin-film hydration strategy and optimized using a central composite design (face-centered). The average vesicle size, entrapment efficiency, and surface charge of the optimized BER-BLS preparation were 196.5 nm, 89.7%, (−) 36.4 mV, respectively. In addition, it exhibited higher stability and better-sustained release of berberine than the berberine solution (BER-SOL). BER-BLS and BER-SOL were administered to streptozocin-induced diabetic rats. The optimized BER-BLS formulation had a significant hypoglycemic impact, with a maximum blood glucose decrease of 41%, whereas BER-SOL only reduced blood glucose by 19%. Furthermore, the pharmacological effect of oral BER-BLS and BER-SOL corresponded to 99.3% and 31.7%, respectively, when compared to subcutaneous insulin (1 IU). A pharmacokinetic analysis found a 6.4-fold rise in the relative bioavailability of berberine in BER-BLS when compared to BER-SOL at a dosage of 100 mg/kg body weight. Histopathological investigation revealed that BER-BLS is suitable for oral administration. Our data demonstrate that BLS is a potential nanocarrier for berberine administration, enhancing its oral bioavailability and antidiabetic activity

HSO: A hybrid swarm optimization algorithm for reducing energy consumption in the cloudlets

Mobile Cloud Computing (MCC) is an emerging technology for the improvement of mobile service quality. MCC resources are dynamically allocated to the users who pay for the resources based on their needs. The drawback of this process is that it is prone to failure and demands a high energy input. Resource providers mainly focus on resource performance and utilization with more consideration on the constraints of service level agreement (SLA). Resource performance can be achieved through virtualization techniques which facilitates the sharing of resource providers’ information between different virtual machines. To address these issues, this study sets forth a novel algorithm (HSO) that optimized energy efficiency resource management in the cloud; the process of the proposed method involves the use of the developed cost and runtime-effective model to create a minimum energy configuration of the cloud compute nodes while guaranteeing the maintenance of all minimum performances. The cost functions will cover energy, performance and reliability concerns. With the proposed model, the performance of the Hybrid swarm algorithm was significantly increased, as observed by optimizing the number of tasks through simulation, (power consumption was reduced by 42%). The simulation studies also showed a reduction in the number of required calculations by about 20% by the inclusion of the presented algorithms compared to the traditional static approach. There was also a decrease in the node loss which allowed the optimization algorithm to achieve a minimal overhead on cloud compute resources while still saving energy significantly. Conclusively, an energy-aware optimization model which describes the required system constraints was presented in this study, and a further proposal for techniques to determine the best overall solution was also made

Seroprevalence of Toxoplasma Gondii among Cancer patient in Qena Governate

Background: Toxoplasmosis is one of the most important cosmopolitan life-threatening diseases in immune-compromised patients. It is caused by an intracellular protozoon: Toxoplasma gondii (T. gondii), this parasite can cause pneumonia, encephalitis or disseminated disease in immune-deficient patients. Objectives: This study aimed to evaluate the prevalence of toxoplasmosis in Egyptian cancer patients and to correlate the prevalence with type of malignancy and the different cancer treatment modalities. Patients and Methods: This study conducted on 100 cancer patients (21 male and 79 female) who attended the Oncology Outpatient Clinic of Qena University Hospital and diagnosed by cancer , receiving chemotherapy or both chemotherapy and radiotherapy, and their ages ranging from 20 year to 76 years from January 2019 until December2020. Results: The high incidence of Toxoplasmosis was among cancer breast patient. The mean of Ig M titre is 0.849 with minimum level is 0.15 and maximum level is 10.43. There were 70 cancer patients undergoing chemotherapy, 6 of them were positive for toxoplasma Ig M (8.7%) , but 30 of whom received chemotherapy and radiotherapy, 11 of whom were infected (36.7%) according to the IgM level. Conclusion: Patients with a positive result are at risk of reactivation of the infection, while patients with a negative result should be informed to prevent primary infection