Synthesis, Characterization, ADME Study and Anti-proliferative evaluation against MCF-7 breast cancer cell line of new analog of a 4-aminophenyl quinazolinone derivative

New series of 4-aminophenyl quinazolinone attached to an aromatic aldehyde moiety has been designed. Compound (ZA) was synthesized by a reaction of benzene-1,4-diamine with 2-aminobenzoic acid. The reaction between (ZA) intermediate and different substituted aromatic aldehydes (R1- R6) is considered one of the most common chemical reactions for the synthesis of imine compounds (Schiff bases) to produce compound (ZA1-ZA6). FTIR, 1H-NMR, and 13C-NMR have been used to confirm the chemical structures of various substances. MTT assay was used to assess in vitro anti-proliferative action for estrogen receptor alpha. The anti-proliferative study discovered a dose-dependent effect on cell proliferation in breast cancer (MCF-7) with inhibitory concentration In comparison to the reference medication tamoxifen (IC50 of 133.4µg\mL), IC50 of the compounds (ZA1, ZA2, ZA3) was 0.07964, 57.43 & 0.002717 µg\mL, respectively at 72 hours on same cell line mentioned above, that also signifies that compound ZA1 has a significantly greater effect on this cell line typ

Molecular Drug Design, Synthesis and Antibacterial study of Novel 4-Oxothiazolidin-3-yl Derivatives

New compounds containing 4-thiazolidinone pharmacophore 5(a) and (5b) have been synthesized. The chemical structures of the intermediate and final compounds were characterized and confirmed by using FT-IR and 1H-NMR spectroscopy. All final compounds were tested against gram-positive and gram-negative bacteria using a well-diffusion technique for their ability as antimicrobial agents.  The tested compounds 5a and 5b showed variable and modest antibacterial activity against gram-negative bacteria and gram-positive bacteria. Molecular docking simulations were studied to understand the molecular core. The results were achieved by docking, the most active compounds into the active site of protein of the bacteria which completely accorded with in vitro results. 

SULPHATED POLYSACCHARIDES (SPS) FROM THE GREEN ALGA ULVA FASCIATA EXTRACT MODULATES LIVER AND KIDNEY FUNCTION IN HIGH FAT DIET-INDUCED HYPERCHOLESTEROLEMIC RATS

Objective: Hypercholesterolemia (HC) was frequently associated with oxidative stress, and release of inflammatory cytokines is to determine the hypolipidemic effects of sulphated polysaccharides from seaweed Ulva fasciata algal extracts through measuring the activities of some parameters related to liver and kidney functions in the serum of hypercholesterolemic rats as compared to normal one.Methods: Different groups of rats were administered a high cholesterol diet. Liver and kidney functions, inflammatory cytokines (TNF-α, CRP, MPO and IL-10), oxidative stress (GSH, MDA and NO), in addition to cell adhesion molecules (ICAM-1 and VCAM-1) were assessed before and after treatment with the algal polysaccharides. In addition, histological examination of liver and kidney were performed to confirm the biochemical findings.Results: The obtained results showed that oxidative stress and inflammatory markers associated with hypercholesterolemia were significantly increased in HC-rats. The histopathological examination of liver and kidney demonstrated severe degeneration with diffuse vacuolar degeneration, necrosis and the presence of fatty droplets. In addition; nephron-histological examination revealed, mild glomerular injury with mild vascular and inflammatory changes. Treatment with the algal sulphated polysaccharides effectively improved these disorders and diminished the formation of fatty liver, as well as renal dysfunction more than the reference drug; fluvastatin. Conclusion: It could be concluded that the consumption of UFP (Ulva fasciata polysaccharides), may be associated with attenuation of inflammatory markers, amelioration of fatty liver and improvement of renal dysfunction, that in turn lead to counteract hypercholesterolemia and its related disorders; such as obesity, and heart disease.Keywords: Non-alcoholic fatty liver disease, Seaweed, Ulva fasciata, Hypercholesterolemia, Hypolipidemic activity, Sulphated polysaccharides (SPs

MICROPROPAGATION AND START CODON TARGETED CHARACTERIZATION OF FOUR STEVIA CULTIVARS IN EGYPT

calorie crop and commercially used as a non-caloric sweetener for diabetic patients. It is also used as cosmetic ingredient, pickling agent, and dentifrice. Four cultivars (Spantia, Shou2A3, China, and High Sugar) of stevia were included to optimize in vitro micropropagation. Four different combinations of hormonal treatments were investigated [6-benzylamino purine (BAP) + Kinetin (Kin) (0.25 + 0.25 mg/l); Forchloefenuron (Cppu) + Kin (0.25 + 0.25 mg/l); Cppu+ Kin (0.5+0.25 mg/l); and the control medium (hormone-free)]. Out of the different media components, the hormone-free medium produced the best performance of explants. The analysis of variance showed that the control treatment was the most significant for all traits except the number of branches per cutting. Hardening of rooted plants was performed in plastic pots with 70% survival percentage during acclimatization. Molecular characterization, of the four stevia cultivars, was conducted using 11 SCoT primers. The SCoT analysis resulted in 122 amplicons, of which, 62 amplicons (51%) were polymorphic. The range of polymorphism was between 6 % and 91 %. The range of polymorphic amplicons per primer was between one and 12 amplicons. The SCoT-16 produced the highest number of polymorphic bands (12). Meanwhile, the SCoT-24 produced the least polymorphism (6 %). The current study provides a new micropropagation system with low cost, high efficiency, and hormone-free application. Additionally, the study provides the first molecular characterization of stevia using SCoT marker system. Finally, SCoT markers associated with cultivars having high and low contents of stevioside can further be validated by marker-assisted breeding studies

Synthesis, Characterization and Antimicrobial Activityof 3-substituted Benzo[4,5]thiazolo[2,3-c][1,2,4]triazole

New series of tricyclic benzo[d]thiazole derivatives (2-12) incorporated into fused to different five membered nitrogen and sulphur containing heterocyclic were prepared from 2- hydrazinobenzo[d]thiazole (1) when treated with triethylformate, acetic anhydride, ethyl chloro acetate, carbon disulphide in alkali, and urea respectively. Compound(1) converted to Schiff’s bases by the condensation different aromatic aldehydes, the synthesized Schiff’s bases were cyclized by bromine in acetic acid to form triazole ring in the new derivatives (7-11) , which might result in biologically active agents. Similar new tricyclic compounds, triazolobenzothiazol-3-amine [12], was obtained from action of benzo[d]thiazole-2-thiol with thiosemicarbazide. The structures of the new compounds have been characterized by elemental analysis and spectral data. Newly synthesized compounds (2-12) were screened for their antibacterial activity against four bacterial species. They were found to exhibit good antibacterial activity

IMPLEMENTATION OF HAZARD ANALYSIS CRITICAL CONTROL POINTS (HACCP) PRINCIPLES IN PRODUCTION OF FILLING CREAM

For improving the safety of filling cream, the Hazard Analysis Critical Control Points (HACCP) system was applied during different preparation process. Different biological, chemical, and physical hazards that may exist in every preparing step of filling cream were identified and control measures were used for controlling those identified hazards. Dried milk powder was identified as high potential hazard raw materials contaminated with pathogenic bacteria e.g. S. aureus and Salmonella sp. Whipping step in preparing filling cream was identified as critical control point. For improving the safety of preparing filling cream system, different control measures including, thermal processing (pasteurization), addition of natural preservatives (lemongrass oil and herbs of cinnamon, clove and anise) and reduction of pH (fruit pulps of strawberry, apricots and apple) were established. Different applied control measures could be used for improving the safety of prepared filling cream where different investigated microbiological criteria were reduced to acceptable levels especially pathogenic bacteria. In addition, different HACCP principles as the critical control points, critical limits, monitoring, corrective measures, verifications and records were established. Implementing the HACCP system during preparing filling cream can effectively ensure safety of this product and other food products contained filling cram especially bakeries

Multiphase induction motor drives - a technology status review

The area of multiphase variable-speed motor drives in general and multiphase induction motor drives in particular has experienced a substantial growth since the beginning of this century. Research has been conducted worldwide and numerous interesting developments have been reported in the literature. An attempt is made to provide a detailed overview of the current state-of-the-art in this area. The elaborated aspects include advantages of multiphase induction machines, modelling of multiphase induction machines, basic vector control and direct torque control schemes and PWM control of multiphase voltage source inverters. The authors also provide a detailed survey of the control strategies for five-phase and asymmetrical six-phase induction motor drives, as well as an overview of the approaches to the design of fault tolerant strategies for post-fault drive operation, and a discussion of multiphase multi-motor drives with single inverter supply. Experimental results, collected from various multiphase induction motor drive laboratory rigs, are also included to facilitate the understanding of the drive operatio

Mortality and pulmonary complications in patients undergoing surgery with perioperative sars-cov-2 infection: An international cohort study

Background The impact of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) on postoperative recovery needs to be understood to inform clinical decision making during and after the COVID-19 pandemic. This study reports 30-day mortality and pulmonary complication rates in patients with perioperative SARS-CoV-2 infection. Methods This international, multicentre, cohort study at 235 hospitals in 24 countries included all patients undergoing surgery who had SARS-CoV-2 infection confirmed within 7 days before or 30 days after surgery. The primary outcome measure was 30-day postoperative mortality and was assessed in all enrolled patients. The main secondary outcome measure was pulmonary complications, defined as pneumonia, acute respiratory distress syndrome, or unexpected postoperative ventilation. Findings This analysis includes 1128 patients who had surgery between Jan 1 and March 31, 2020, of whom 835 (740%) had emergency surgery and 280 (248%) had elective surgery. SARS-CoV-2 infection was confirmed preoperatively in 294 (261%) patients. 30-day mortality was 238% (268 of 1128). Pulmonary complications occurred in 577 (512%) of 1128 patients; 30-day mortality in these patients was 380% (219 of 577), accounting for 817% (219 of 268) of all deaths. In adjusted analyses, 30-day mortality was associated with male sex (odds ratio 175 [95% CI 128-240], p<00001), age 70 years or older versus younger than 70 years (230 [165-322], p<00001), American Society of Anesthesiologists grades 3-5 versus grades 1-2 (235 [157-353], p<00001), malignant versus benign or obstetric diagnosis (155 [101-239], p=0046), emergency versus elective surgery (167 [106-263], p=0026), and major versus minor surgery (152 [101-231], p=0047). Interpretation Postoperative pulmonary complications occur in half of patients with perioperative SARS-CoV-2 infection and are associated with high mortality. Thresholds for surgery during the COVID-19 pandemic should be higher than during normal practice, particularly in men aged 70 years and older. Consideration should be given for postponing non-urgent procedures and promoting non-operative treatment to delay or avoid the need for surgery. Funding National Institute for Health Research (NIHR), Association of Coloproctology of Great Britain and Ireland, Bowel and Cancer Research, Bowel Disease Research Foundation, Association of Upper Gastrointestinal Surgeons, British Association of Surgical Oncology, British Gynaecological Cancer Society, European Society of Coloproctology, NIHR Academy, Sarcoma UK, Vascular Society for Great Britain and Ireland, and Yorkshire Cancer Research

Mortality and pulmonary complications in patients undergoing surgery with perioperative SARS-CoV-2 infection: an international cohort study

Background: The impact of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) on postoperative recovery needs to be understood to inform clinical decision making during and after the COVID-19 pandemic. This study reports 30-day mortality and pulmonary complication rates in patients with perioperative SARS-CoV-2 infection. Methods: This international, multicentre, cohort study at 235 hospitals in 24 countries included all patients undergoing surgery who had SARS-CoV-2 infection confirmed within 7 days before or 30 days after surgery. The primary outcome measure was 30-day postoperative mortality and was assessed in all enrolled patients. The main secondary outcome measure was pulmonary complications, defined as pneumonia, acute respiratory distress syndrome, or unexpected postoperative ventilation. Findings: This analysis includes 1128 patients who had surgery between Jan 1 and March 31, 2020, of whom 835 (74·0%) had emergency surgery and 280 (24·8%) had elective surgery. SARS-CoV-2 infection was confirmed preoperatively in 294 (26·1%) patients. 30-day mortality was 23·8% (268 of 1128). Pulmonary complications occurred in 577 (51·2%) of 1128 patients; 30-day mortality in these patients was 38·0% (219 of 577), accounting for 81·7% (219 of 268) of all deaths. In adjusted analyses, 30-day mortality was associated with male sex (odds ratio 1·75 [95% CI 1·28–2·40], p\textless0·0001), age 70 years or older versus younger than 70 years (2·30 [1·65–3·22], p\textless0·0001), American Society of Anesthesiologists grades 3–5 versus grades 1–2 (2·35 [1·57–3·53], p\textless0·0001), malignant versus benign or obstetric diagnosis (1·55 [1·01–2·39], p=0·046), emergency versus elective surgery (1·67 [1·06–2·63], p=0·026), and major versus minor surgery (1·52 [1·01–2·31], p=0·047). Interpretation: Postoperative pulmonary complications occur in half of patients with perioperative SARS-CoV-2 infection and are associated with high mortality. Thresholds for surgery during the COVID-19 pandemic should be higher than during normal practice, particularly in men aged 70 years and older. Consideration should be given for postponing non-urgent procedures and promoting non-operative treatment to delay or avoid the need for surgery. Funding: National Institute for Health Research (NIHR), Association of Coloproctology of Great Britain and Ireland, Bowel and Cancer Research, Bowel Disease Research Foundation, Association of Upper Gastrointestinal Surgeons, British Association of Surgical Oncology, British Gynaecological Cancer Society, European Society of Coloproctology, NIHR Academy, Sarcoma UK, Vascular Society for Great Britain and Ireland, and Yorkshire Cancer Research