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N‐Heterocyclic Carbene (NHC) Silver Complexes as Versatile Chemotherapeutic Agents Targeting Human Topoisomerases and Actin

Research Abstract

In recent years, the number of people suffering from cancer has risen rapidly and the World Health Organization and U.S. and European governments have identified this pathology as a priority issue. It is known that most bioactive anticancer molecules do not target a single protein but exert pleiotropic effects, simultaneously affecting multiple pathways. In our study, we designed and synthesized a new series of silver N‐heterocyclic carbene (NHC) complexes [(NHC)2Ag]+[AgX2]− (X=iodide or acetate). The new complexes were active against two human breast cancer cell lines, MCF‐7 and MDA‐MB‐231. These compounds showed multiple target actions as anticancer, by inhibiting in vitro the activity of the human topoisomerases I and II and interfering with the cytoskeleton dynamic, as also confirmed by in silico studies. Moreover, the antimicrobial activity of these silver complexes was studied against Gram …

Research Authors
hussein el kashef
Research Date
Research Department
Research Year
2022

Metal complexes with Schiff bases: Data collection and recent studies on biological activities

Research Abstract

Metal complexes play a crucial role in pharmaceutical sciences owing to their wide and significant activities. Schiff bases (SBs) are multifaceted pharmacophores capable of forming chelating complexes with various metals in different oxidation states. Complexes with SBs are extensively studied for their numerous advantages, including low cost and simple synthetic strategies. They have been reported to possess a variety of biological activities, including antimicrobial, anticancer, antioxidant, antimalarial, analgesic, antiviral, antipyretic, and antidiabetic ones. This review summarizes the most recent studies on the antimicrobial and antiproliferative activities of SBs-metal complexes. Moreover, recent studies regarding mononuclear and binuclear complexes with SBs are described, including antioxidant, antidiabetic, antimalarial, antileishmanial, anti-Alzheimer, and catecholase activities.

Research Authors
hussein el kashef
Research Date
Research Department
Research Year
2022

An Update of Carbazole Treatment Strategies for COVID-19 Infection

Research Abstract

The Coronavirus disease 2019 (COVID-19) outbreak was declared by the World Health Organization (WHO) in March 2020 to be a pandemic and many drugs used at the beginning proved useless in fighting the infection. Lately, there has been approval of some new generation drugs for the clinical treatment of severe or critical COVID-19 infections. Nevertheless, more drugs are required to reduce the pandemic’s impact. Several treatment approaches for COVID-19 were employed since the beginning of the pandemic, such as immunomodulatory, antiviral, anti-inflammatory, antimicrobial agents, and again corticosteroids, angiotensin II receptor blockers, and bradykinin B2 receptor antagonists, but many of them were proven ineffective in targeting the virus. So, the identification of drugs to be used effectively for treatment of COVID-19 is strongly needed. It is aimed in this review to collect the information so far known about the COVID-19 studies and treatments. Moreover, the observations reported in this review about carbazoles as a treatment can signify a potentially useful clinical application; various drugs that can be introduced into the therapeutic equipment to fight COVID-19 or their molecules can be used as the basis for designing new antivirals.

Research Authors
hussein el kashef
Research Date
Research Department
Research Year
2023

Carbazoles: Role and Functions in Fighting Diabetes

Research Abstract

Carbazole derivatives have gained a lot of attention in medicinal chemistry over the last few decades due to their wide range of biological and pharmacological properties, including antibacterial, antitumor, antioxidant, and anti-inflammatory activities. The therapeutic potential of natural, semi-synthetic or synthetic carbazole-containing molecules has expanded considerably owing to their role in the pathogenesis and development of diabetes. Several studies have demonstrated the ability of carbazole derivatives to reduce oxidative stress, block adrenergic hyperactivation, prevent damage to pancreatic cells and modulate carbohydrate metabolism. In this survey, we summarize the latest advances in the synthetic and natural carbazole-containing compounds involved in diabetes pathways.

Research Authors
Fedora Grande, Giuseppina Ioele, Anna Caruso, Maria Occhiuzzi, Hussein El-Kashef, Carmela Saturnino, and Maria Stefania Sinicropi
Research Date
Research Department
Research Journal
Applied Sciences
Research Year
2023

Annona cherimola Mill. Leaf Extracts Affect Melanoma Cells Growth and Progression

Research Abstract

Cancer represents one of the major causes of mortality worldwide; indeed, 19.3 million new cases and almost 10.0 million deaths were estimated last year. Among the different type of cancers, malignant melanoma represents the most aggressive and deadly skin cancer. Unfortunately, the long-term efficacy of melanoma treatments is limited by the lack of clinical efficacy, onset of side effects and resistance. The latter is a major obstacle for the success of the melanoma therapy; thus, the exploration of new potent and safer anticancer agents is of great importance. Recently, numerous plant species, used for therapeutic purposes and containing various non-toxic nutraceuticals have been widely studied. Herein, we investigated the antioxidant and anticancer properties on melanoma cells of the ethanolic, methanolic and aqueous Annona cherimola leaf extracts (ACE, ACM and ACW, respectively). The ethanolic extract showed higher anticancer activity, mostly against the malignant A2058 melanoma cell line (IC50 = 5.6 ± 0.8 ng/mL), together with a very low activity on the normal cells. It blocks the melanoma cells migration process, and induces a clear disorganization of cytoskeleton, triggering cell apoptosis. Finally, some bioactive compounds were identified in the studied extracts

Research Authors
hussein el kashef
Research Date
Research Department
Research Year
2022

Sustainable Biodiesel Production from a New Oleaginous Fungus, Aspergillus carneus Strain OQ275240: Biomass and Lipid Production Optimization Using Box–Behnken Design

Research Abstract

Due to their low cost and ability to synthesize lipids for sustainable biodiesel production, oleaginous fungus has recently gained more prominence than other microorganisms. The new oleaginous fungus Aspergillus carneus OQ275240’s dry biomass, lipid content, and lipid yield were all optimized in this work, using the response surface methodology-based Box–Behnken design. Analysis of variance (ANOVA) was also used to examine the experimental data, and multiple regression analysis was used to fit the data to a second-order polynomial equation. Three independent variables, such as the concentration of yeast, glucose, and phosphorus, were examined for their mutual impacts. Maximum dry biomass (0.024 g/50 mL), lipid content (36.20%), and lipid yield (8.70 mg/50 mL) were achieved at optimal concentrations of 2.68 g/L of yeast, 20.82 g/L of glucose, and 0.10 g/L of phosphorus, respectively, showing that the actual data and predictions of the models were in good agreement. A. carneus OQ275240 has a favorable fatty acid profile that can be used to successfully create biodiesel, as shown by the presence of palmitic acid (C16:0), stearic acid (C18:0), and oleic acid (C18:1) in its fatty acid methyl esters (FAMEs) profile. Furthermore, the qualities of the biodiesel were investigated, and it was found that they fell within the parameters established by the international specifications EN 14214 (Europe) and ASTM D6751-08 (United States). These findings point to the newly evaluated filamentous fungal strain as a potential feedstock for the production of high-quality biodiesel.

Research Authors
Amany G Ibrahim, Alaa Baazeem, Mayasar I Al-Zaban, Mustafa A Fawzy, Sedky HA Hassan, Mostafa Koutb
Research Date
Research Journal
Sustainability
Research Pages
6836
Research Publisher
MDPI
Research Year
2023

SUSCEPTIBILITY OF THE DIFFERENT STAGES OF THE MEDFLY CERATITIS CAPITATA WIEDEMANN (DIPTERA: TEPHRITIDAE) TO THE EXTRACTS OF VIOLA ODORATA AND EUCALYPTUS CAMALDEULENSIS

Research Abstract

The medfly (Ceratitis capitata) is a polyphagous serious fruit pests spreaded in Africa and worldwide. The medfly infests several plant species and causes economic losses in many crops.The problems of using undesirable chemical insecticides against medfly have forced the scientists to look for more safe pesticides. Therefore, two plant extracts, Viola odorata and Eucalyptus camaldeulensis, were tested against the adult and immature stages of C. capitata. Each extract composition was analyzed using GC-MS. Terpenoids were identified as the major constituents in V. odorata extract, while E. camaldeulensis extract contains heterocyclic organic compounds together with terpenoids. The toxicity of both extracts on C. capitata was addressed using the contact and spray application methods. The contact treatment method showed higher toxicity than the spray method. In the meantime, the pupae were more susceptible to V. odorata extract than the full grown larvae; while E. camaldeulensis extract showed higher toxicity on larvae. Both extracts affected adult flies with higher toxicity in V. odorata-treated flies. The pupal deformations were recorded in the plant extracts-treated C. capitata. The malformations of pupae included emergence of only head and thorax of the flies and keeping the rest of the body inside the puparia, decoloration of the puparium, and no emergence of the flies at all. Furthermore, the V. odorata extract induced adult antennal and wings abnormalities. Both extracts degraded within a short period of time in the soil. In conclusion, the V. odorata and E. camaldeulensis extracts might act as powerful insecticides against C. capitata.

Research Authors
Ahmed Ibrahim, Nehad A Soliman, Sherihan M Alamin, Amira E Mesbah, Ali Mahmoud
Research Date
Research Department
Research Journal
Egyptian Journal of Zoology
Research Publisher
The Zoological Society of AR Egypt
Research Year
2023
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