Synthesis and Three-dimensional Qualitative Structure Selectivity Relationship of 3,5-Disubstituted-2,4- Thiazolidinedione Derivatives As COX2 Inhibitors

Ali, Ahmed M.,Saber, Gamal E.,Mahfouz, Nadia M.,EI-Gendy, Mahmoud A.,Radwan, Awwad A.,Hamid, Mohamed A.-EI. 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.10

In our effort for synthesis of selective COX2 inhibitors, certain new 2,4-thiazolidinedione derivatives were synthesized. It necessitates preparation of potassium salt of 2,4-thiazolidinedione 2, which condensed with intermediate 4a. The resulting 3-[2-(4-methylphenyl)-2-oxo-1-phenylethyl]-2,4-thiazolidinedione 8 was condensed with appropriate aldehyde to afford compounds 10a, 10i-I, 10o and 10p. Compounds (9a-I, 10a-n, 10p, 11 and 12) were obtained through the preparation of 5-arylmethylidene-2,4-thiazolidinediones 6a-p and reaction of its potassium salt 7a-p with compounds 4a, 4b, and 5. Some compounds displayed significant analgesic activity as compared to reference standards. The anti-inflammatory activity of the synthesized compounds revealed that intermediate 8 and compounds 9c, 10c and 10d showed good results. Compound 10c produced no significant mucosal injury. HipHop methodology of Catalyst program was used to build up hypothetical model of selective COX2 inhibitors followed by fitting the synthesized compounds to this model. Compounds 10c and 10d were suspected to be promising selective COX2 inhibitors. Also, compounds (6c, 8, 9a,c,d,k, 10a,c,d,k, 11 and 12) were docked into COX1 and COX2 X-ray structures, using DOCK6 program. Docking results suggested that several of these derivatives are active COX inhibitors with a significant preference for COX2.

Synthesis and Three-dimensional Qualitative Structure Selectivity Relationship of 3,5- Disubstituted-2,4-Thiazolidinedione Derivatives As COX2 Inhibitors

Ahmed M. Ali,Gamal E. Saber,Nadia M. Mahfouz,Mahmoud A. El-Gendy,Awwad A. Radwan,Mohamed A.-El. Hamid 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.10

In our effort for synthesis of selective COX2 inhibitors, certain new 2,4-thiazolidinedione derivatives were synthesized. It necessitates preparation of potassium salt of 2,4-thiazolidinedione 2, which condensed with intermediate 4a. The resulting 3-[2-(4-methylphenyl)-2-oxo-1-phenylethyl]- 2,4-thiazolidinedione 8 was condensed with appropriate aldehyde to afford compounds 10a, 10i-l, 10o and 10p. Compounds (9a-l, 10a-n, 10p, 11 and 12) were obtained through the preparation of 5-arylmethylidene-2,4-thiazolidinediones 6a-p and reaction of its potassium salt 7a-p with compounds 4a, 4b, and 5. Some compounds displayed significant analgesic activity as compared to reference standards. The anti-inflammatory activity of the synthesized compounds revealed that intermediate 8 and compounds 9c, 10c and 10d showed good results. Compound 10c produced no significant mucosal injury. HipHop methodology of Catalyst program was used to build up hypothetical model of selective COX2 inhibitors followed by fitting the synthesized compounds to this model. Compounds 10c and 10d were suspected to be promising selective COX2 inhibitors. Also, compounds (6c, 8, 9a,c,d,k, 10a,c,d,k, 11 and 12) were docked into COX1 and COX2 X-ray structures, using DOCK6 program. Docking results suggested that several of these derivatives are active COX inhibitors with a significant preference for COX2.

Examination of Correlations Between Several Biochemical Components and Powdery Mildew Resistance of Flax Cultivars

Aly, Aly A.,Mansour, Mahmoud T. M.,Mohamed, Heba I.,Abd-Elsalam, Kamel A. The Korean Society of Plant Pathology 2012 Plant Pathology Journal Vol.28 No.2

A field trial was conducted in 2009/2010 and 2010/2011 growing seasons at Giza Agricultural Research Station to examine correlations between some biochemical componets and powdery mildews ($PM_s$) resistance in flax cultivars. Nine flax cultivars could be divided into five distinct groups, i.e., highly susceptible (Cortland and C.I. 2008), moderately susceptible (Giza 7, and Marshall), moderately resistant (Cass), resistant (Koto, Dakota and Wilden), and highly resistant (Ottowa 770B). The cultivars showed considerable variation in PM severity ranged from 8.05 on Ottowa 770B to 97.02% on Cortland. Total soluble proteins, total phenols, antioxidant enzymes (peroxidase and polyphenoloxidase), ascorbic acid, tocopherol, and malondialdehyde (MDA), were determined in uninfected leaves of the tested cultivars. Pearson's correlation coefficient was calculated to measure the degree of association between PM severity and each component. All components showed significant (P < 0.05) or highly significant (P < 0.01) negative correlation with PM severity except MDA, which showed positive correlation (P < 0.01). Linear regression analysis was used to evaluate the causal relationship between the biochemical components (independent variables) and PM severity (dependent variable). Coefficient of determination ($R^2$) values of the generated models ranged from 48.76 to 77.15%. Tocopherol, MDA, and proteins were the most important contributors to the total variation in PM severity as the $R^2$ values of their models were 71.78, 75.28, and 77.15%, respectively. The results of the present study suggest that tocopherol, MDA, and proteins in uninfected leaves can be used as biochemical markers to predict PM resistance in flax.

Examination of Correlations Between Several Biochemical Components and Powdery Mildew Resistance of Flax Cultivars

Aly A. Aly,Kamel A. Abd-Elsalam,Mahmoud T. M. Mansour,Heba I. Mohamed 한국식물병리학회 2012 Plant Pathology Journal Vol.28 No.2

A field trial was conducted in 2009/2010 and 2010/2011growing seasons at Giza Agricultural Research Station to examine correlations between some biochemical componets and powdery mildews (PMs) resistance in flax cultivars. Nine flax cultivars could be divided into five distinct groups, i.e., highly susceptible (Cortland and C.I. 2008), moderately susceptible (Giza 7, and Marshall),moderately resistant (Cass), resistant (Koto, Dakota and Wilden), and highly resistant (Ottowa 770B). The cultivars showed considerable variation in PM severity ranged from 8.05 on Ottowa 770B to 97.02% on Cortland. Total soluble proteins, total phenols, antioxidant enzymes (peroxidase and polyphenoloxidase), ascorbic acid, tocopherol, and malondialdehyde (MDA), were determined in uninfected leaves of the tested cultivars. Pearson’s correlation coefficient was calculated to measure the degree of association between PM severity and each component. All components showed significant (P < 0.05) or highly significant (P < 0.01) negative correlation with PM severity except MDA, which showed positive correlation (P < 0.01). Linear regression analysis was used to evaluate the causal relationship between the biochemical components (independent variables)and PM severity (dependent variable). Coefficient of determination (R2) values of the generated models ranged from 48.76 to 77.15%. Tocopherol, MDA, and proteins were the most important contributors to the total variation in PM severity as the R2 values of their models were 71.78, 75.28, and 77.15%, respectively. The results of the present study suggest that tocopherol,MDA, and proteins in uninfected leaves can be used as biochemical markers to predict PM resistance in flax.

Micro-grid Monitoring and Supervision: Web-based SCADA Approach

Ali Mohamed A.,Barakat Mahmoud M.,Abokhalaf Masoud M.,Fadel Yasmin H.,Kandil Mohamed,Rasmy Mariam W.,Ali Osama N.,Besheer Ahmad H.,Emara Hassan M.,Bahgat Ahmed 대한전기학회 2021 Journal of Electrical Engineering & Technology Vol.16 No.5

Owing to the widespread use of the micro-grid concept to serve many real life applications, the main concern of this paper is to monitor, evaluate and manage the operational performance of an existent, already installed micro-grid that consists of On & Off grid PV systems in addition to the main grid supply. With the aid of customized web based SCADA system fully designed by authors, the performance evaluation of the proposed micro-grid is carried out in terms of energy consumption, power quality indices and energy cost based on Egypt’s energy current tariff . The designed system helps in both micro-grid status monitoring as well as load sharing between the main grid supply and the off grid PV energy system. The data of the on grid PV energy system are accessed and collected online directly from the inverter web server instead of downloading them offl ine from the PV inverter. In this case, data are analyzed with a reasonable refresh rate, which saves time and eff ort. Remote access platform is developed securely through a multi-level security authentication and strong data encryption using the OpenVPN protocol under the Dynamic Domain Name System service. Smart wired and wireless technology—used as integrated sensing devices to the developed SCADA system—enables easy system installation and running cost saving. Finally, to validate the collected data from the newly SCADA designed monitoring system, a performance characterization for the on grid PV system following international standards of yields calculations is carried out for 3 months in 2019.

Host discrimination and interspecific competition of Trissolcus nigripedius and Telenomus gifuensis, sympatric parasitoids of Dolycoris baccarum

Ali M. A. Mahmoud,Un Taek Lim 한국응용곤충학회 2008 한국응용곤충학회 학술대회논문집 Vol.2008 No.05

Trissolcus nigripedius Nakagawa and Telenomus gifuensis Ashmead (Hymenoptera: Scelionidae) are solitary egg parasitoids of Dolycoris baccarum L. (Hemiptera: Pentatomidae), a polyphagous seed-sucking bug of agricultural crops. Field examinations revealed that the two parasitoids are the most common species, but only a single species emerge from a host egg mass. To explain this observation we tested two hypotheses of interspecific host discrimination and asymmetry in competitive interaction between the two parasitoids. When provided with host eggs pre-parasitized by each other, both Tr. nigripedius and Te. gifuensis parasitized 94 and 100% of the host eggs without interspecific host discrimination, respectively. Interestingly, from the multiparasitized eggs irrespective of oviposition sequence, progeny of Te. gifuensis always survive better than Tr. nigripedius. Te. gifuensis is superior in immature competition probably due to shorter egg incubation period, hence progeny of Te. gifuensis become first instar faster than that of Tr. nigripedius. However, adult Tr. nigripedius is always superior competitor in possessing and guarding the host eggs even after oviposition against Te. gifuensis. Therefore, the asymmetry in competitive interaction between Tr. nigripedius and Te. gifuensis may explain the emergence of a single species from a host egg mass in the field in spite of no interspecific host discrimination.

Ecotoxicological effect of fenitrothion on Trissolcus nigripedius (Hymenoptera: Scelionidae) an egg parasitoid of Dolycoris baccarum (Hemiptera: Pentatomidae)

임언택,Ali M.A. Mahmoud 한국응용곤충학회 2008 Journal of Asia-Pacific Entomology Vol.11 No.4

Trissolcus nigripedius Nakagawa (Hymenoptera: Scelionidae) is an egg parasitoid of Dolycoris baccarum L. (Hemiptera: Pentatomidae), a polyphagous insect pest of many crops. Application of chemical insecticides is the most common control method against stink bugs in soybean. As a part of studies to investigate the potential of T. nigripedius as a biocontrol agent of D. baccarum, we assessed ecotoxicological effects of fenitrothion on T. nigripedius. The acute toxicity of fenitrothion was compared with five pesticides by topical application, exposure to residue, and oral ingestion in field recommended rate. Fenitrothion, spinosad, and milbemectin caused 100% mortality within 24 h by topical application or exposure to residue. Fenitrothion was also highly toxic to T. nigripedius when ingested. T. nigripedius was less susceptible to thiamethoxam a neonicotinoid insecticide in topical application or exposure to residue than oral ingestion. Sublethal effects of fenitrothion on T. nigripedius were also assessed. Emergence rate was significantly reduced in the insecticide treatments at 4 and 6 days after the parasitization. The proportion of inviable eggs increased when fenitrothion was applied before the parasitization, but was not affected when it was applied after the parasitization. Since higher proportion of males emerged from the host eggs sprayed with the fenitrothion, the female parasitoid may be more susceptible to the insecticide. Furthermore, T. nigripedius progeny that emerged from host eggs exposed to fenitrothion parasitized fewer host eggs. Therefore, for the conservation of T. nigripedius as a biological control agent of D. baccarum, use of fenitrothion should be minimized. Trissolcus nigripedius Nakagawa (Hymenoptera: Scelionidae) is an egg parasitoid of Dolycoris baccarum L. (Hemiptera: Pentatomidae), a polyphagous insect pest of many crops. Application of chemical insecticides is the most common control method against stink bugs in soybean. As a part of studies to investigate the potential of T. nigripedius as a biocontrol agent of D. baccarum, we assessed ecotoxicological effects of fenitrothion on T. nigripedius. The acute toxicity of fenitrothion was compared with five pesticides by topical application, exposure to residue, and oral ingestion in field recommended rate. Fenitrothion, spinosad, and milbemectin caused 100% mortality within 24 h by topical application or exposure to residue. Fenitrothion was also highly toxic to T. nigripedius when ingested. T. nigripedius was less susceptible to thiamethoxam a neonicotinoid insecticide in topical application or exposure to residue than oral ingestion. Sublethal effects of fenitrothion on T. nigripedius were also assessed. Emergence rate was significantly reduced in the insecticide treatments at 4 and 6 days after the parasitization. The proportion of inviable eggs increased when fenitrothion was applied before the parasitization, but was not affected when it was applied after the parasitization. Since higher proportion of males emerged from the host eggs sprayed with the fenitrothion, the female parasitoid may be more susceptible to the insecticide. Furthermore, T. nigripedius progeny that emerged from host eggs exposed to fenitrothion parasitized fewer host eggs. Therefore, for the conservation of T. nigripedius as a biological control agent of D. baccarum, use of fenitrothion should be minimized.

Anti-cancer Effect of Hyoscyamus muticus Extract via Its Activation of Fas/FasL-ASK1-p38 Pathway

Amer Ali Abd El-Hafeez,Hala Mohamed M. Marzouk,Mohamed A. A. Abdelhamid,Hazim O. Khalifa,Tamer H. A. Hasanin,Ahmed G. K. Habib,Fatma Mahmoud Abdelwahed,Fatma M. Barakat,Eslam M. Bastawy,Eman M. B. Abd 한국생물공학회 2022 Biotechnology and Bioprocess Engineering Vol.27 No.5

Hyoscyamus muticus L. is a traditional medicine used as antispasmodic and sedative. Herein, we aimed to determine the phytochemical constituents and for the first time its anti-cancer activities. The phytochemical constituents of the different extracts were evaluated by calorimetric methods. The anti-cancer activities of the extracts were tested against leukemia, breast, renal, and prostate cancers cell lines. 4, 6-Diamidino-2-phenylindole (DAPI) staining, flow cytometric analysis, knockdown of ASK1, and reactive oxygen species (ROS) production were evaluated to clarify the mechanism of action. Phytochemical screening confirmed the presence of wide range of phytoconstituents. Hyoscyamus muticus methanolic extracts (HMME) showed the highest anti-cancer activities against leukemia, breast, renal, and prostate cancers as compared to ethanol and aqueous extracts. Specifically, HMME exerted cytotoxic effect against the MDA-MB-231 and MDA-MB-468 triple-negative breast cancer (TNBC) cell lines with IC50 values of 8.75 and 7.25 μg/mL, respectively. Mechanistically, DAPI staining and flow cytometric analysis revealed that HMME induces apoptosis via the death receptor, FAS, but not the mitochondrial pathway. Moreover, ASK1 and p38 were rapidly activated in response to HMME, and knockdown of ASK1 by a small interference of RNA specific to Ask1 attenuated p38 and caspase-3 activation and suppressed apoptosis, implying that HMME-induced apoptosis relies on the ASK1-p38-caspase-3 pathway. Furthermore, we confirmed that cellular ROS generation was a critical mediator in HMME-induced apoptosis because the ROSscavenger N-acetyl cysteine significantly decreased the phosphorylation of ASK1 and HMME-induced apoptosis. Our results confirmed HMME cytotoxic effects in TNBCs via ROS-dependent activation of the Fas/FasL-ASK1-p38 axis.

Controllable Biogenic Synthesis of Intracellular Silver/Silver Chloride Nanoparticles by Meyerozyma guilliermondii KX008616

( Saad A. M. Alamri ),( Mohamed Hashem ),( Nivien A. Nafady ),( Mahmoud A. Sayed ),( Ali M. Alshehri ),( Gamal A. El-shaboury ) 한국미생물생명공학회(구 한국산업미생물학회) 2018 Journal of microbiology and biotechnology Vol.28 No.6

Intracellular synthesis of silver/silver chloride nanoparticles (Ag/AgCl-NPs) using Meyerozyma guilliermondii KX008616 is reported under aerobic and anaerobic conditions for the first time. The biogenic synthesis of Ag-NP types has been proposed as an easy and cost-effective alternative for various biomedical applications. The interaction of nanoparticles with ethanol production was mentioned. The purified biogenic Ag/AgCl-nanoparticles were characterized by different spectroscopic and microscopic approaches. The purified nanoparticles exhibited a surface plasmon resonance band at 419 and 415 nm, confirming the formation of Ag/AgCl-NPs under aerobic and anaerobic conditions, respectively. The planes of the cubic crystalline phase of the Ag/AgCl-NPs were confirmed by X-ray diffraction. Fourier-transform infrared spectra showed the interactions between the yeast cell constituents and silver ions to form the biogenic Ag/AgCl-NPs. The intracellular Ag/AgCl-NPs synthesized under aerobic condition were homogenous and spherical in shape, with an approximate particle size of 2.5-30nm as denoted by the transmission electron microscopy (TEM). The reaction mixture was optimized by varying reaction parameters, including temperature and pH. Analysis of ultrathin sections of yeast cells by TEM indicated that the biogenic nanoparticles were formed as clusters, known as nanoaggregates, in the cytoplasm or in the inner and outer regions of the cell wall. The study recommends using the biomass of yeast that is used in industrial or fermentation purposes to produce Ag/AgCl-NPs as associated by-products to maximize benefit and to reduce the production cost.

New Optimization Model for Multi-Period Multi-Product Production Planning System with Uncertainty

Asmaa A. Mahmoud,Mohamed F. Aly,Ahmed M. Mohib,Islam H. Afefy 대한산업공학회 2019 Industrial Engineeering & Management Systems Vol.18 No.4

The focus of this study is to develop a multi-period multi-product (MPMP) production planning system with uncertainty, and products demand (seasonal demand) uncertainty. Mainly, the problem aims reach the production levels ofeach product according to the uncertain demand for various periods, which depend on constraints of capacity, inventory, and resources. An analytical model proposed for this problem that can be categorized into two classes: non-linearand stochastic. The objective is to minimize the summation of variable production costs. As uncertain demand is adynamic stochastic data process in the planning horizon, it is considered as a tree model. Each stage in the demandtree model is related to a cluster of a period time. Hence, depending on the tree model for the fluctuation demand;Two-Stage Stochastic Programming (TSP) model is presented as an alternative for all demand scenarios. In some ofthe reviewed articles validation of the analytical model were missing, while other studies were missing either manufacturing set up costs or assumptions of seasonal demand. Therefore, this study proposes TSP model using SamplingAverage Approximation method (SAA) that is suitable for a production planning system in any manufacturing environment considering seasonal demand using optimization program (Lingo 16) to solve the mathematical model. Further, investigation of seasonal demand is performed using the multiplicative seasonal method, and the model validation was checked using Mathworks Matlab R2015a (64-Bit) considering manufacturing set up costs. Finally, somerecommendations for future research are suggested.