Open Access. Powered by Scholars. Published by Universities.®
Medicinal and Pharmaceutical Chemistry Commons™
Open Access. Powered by Scholars. Published by Universities.®
- Discipline
- Keyword
-
- 15-diene; diterpene; cytotoxicity; doxorubicin; Ehrlich ascites carcinoma (1)
- BCl-2 (1)
- Becium grandiflorum; 18-epoxy-pimara-8(14) (1)
- Cancer (1)
- Celecoxib; repositioning; in-situ provesicular powder; optimization; cytotoxic assay; pharmacokinetic study (1)
-
- Citrus peels waste- anti estrogenic activity-anti-aromatase activity (1)
- Cynara scolymus L.; antioxidant activity; total phenolic; HPLC-DAD; flower; bract; stem; silver nanoparticles; PC-3; A549 (1)
- Cynara scolymus L.; biomedical implementations; cytotoxic; green synthesis; silver nanoparticles (1)
- Graphene nanoplatelets; Green assessment; Pholcodine; Polythiophene; Square wave voltammetry (1)
- Hydrazinoquinazolines (1)
- In vitro assay (1)
- Keywords: repurposing; omarigliptin; docking; A2A adenosine receptor; acetylcholine esterase receptor; GLP-1; rats’ plasma; rats’ brain tissue; 28 days multiple doses; LC-MS/MS (1)
- Molecular docking (1)
- Molecular docking · Quorum sensing inhibitors (QSIs) · Sortase A · Gram-positive bacteria (1)
- Molecular dynamic (1)
- Phosphodiesterase 7 inhibitors (1)
- Synthesis (1)
- Triazoloquinazolines antiinflammatory (1)
Articles 1 - 13 of 13
Full-Text Articles in Medicinal and Pharmaceutical Chemistry
Phytochemical Analysis And In Vivo Anticancer Effect Of Becium Grandiflorum: Isolation And Characterization Of A Promising Cytotoxic Diterpene, Christeen Fahim, Maha R. A. Abdollah, Rola Milad, Nehal Sabry, Noha Swilam
Phytochemical Analysis And In Vivo Anticancer Effect Of Becium Grandiflorum: Isolation And Characterization Of A Promising Cytotoxic Diterpene, Christeen Fahim, Maha R. A. Abdollah, Rola Milad, Nehal Sabry, Noha Swilam
Pharmacy
Background:Becium grandiflorum is a fragrant perennial shrub of the Lamiaceae family. Objectives: The current study aimed to explore the cytotoxic potential of the nhexane fraction from Becium grandiflorum aerial parts and, further, isolate its major diterpene and conduct in vitro and in vivo anticancer activities along with its molecular mechanism and synergy with doxorubicin. Methods: The hydroalcoholic extract of Becium grandiflorum aerial parts was fractionated, and the n-hexane fraction was analyzed via GC-MS. The major isolated diterpene, 18-epoxy-pimara-8(14),15-diene (epoxy-pimaradiene), was quantified using UPLC-PDA. Cytotoxicity assays were conducted on HCT-116, MCF-7, MDA-MB- 231, and HepG2 cell lines. The synergistic effect with …
Voltammetric Analysis Of Pholcodine On Graphene-Modified Gnps/Pts With Green Assessment, Ekram Hany Mohamed, Nahla Abdel Shafy, Hadeer Elkhouly, Nehal Khoudary, Hany Darwish, Aswak Alanzi, Ibrahim Naguib
Voltammetric Analysis Of Pholcodine On Graphene-Modified Gnps/Pts With Green Assessment, Ekram Hany Mohamed, Nahla Abdel Shafy, Hadeer Elkhouly, Nehal Khoudary, Hany Darwish, Aswak Alanzi, Ibrahim Naguib
Pharmacy
Pholcodine, an anti-tussive medication widely used as an over-the-counter, OTC drug, has recently faced restrictions in several countries. This paper presents a sensitive electrochemical approach for pholcodine detection. The electrochemical method involved fabricating a graphene nanoplatelets electrode, incorporating polythiophene nanospheres polymer to promote electron transfer and increase the activated surface area. Characterization of the fabricated electrode was performed using transmission electron microscopy, ATR-Fourier-transform infrared spectroscopy, X-ray crystallography, X-ray photoelectron spectroscopy, and electrochemical impedance spectroscopy. The electrochemical behavior of pholcodine with the fabricated electrode was investigated using cyclic voltammetry, chronoamperometry, square wave voltammetry (SWV), and differential pulse voltammetry (DPV). The developed …
Design, Synthesis, Molecular Docking, And Molecular Dynamic Studies Of Novel Quinazoline Derivatives As Phosphodiesterase 7 Inhibitors, Marwa M. Safar Prof. Dr.
Design, Synthesis, Molecular Docking, And Molecular Dynamic Studies Of Novel Quinazoline Derivatives As Phosphodiesterase 7 Inhibitors, Marwa M. Safar Prof. Dr.
Pharmacy
Introduction: Phosphodiesterase 7 (PDE7) is a high-affinity cyclic AMP (cAMP)- specific PDE that is expressed in immune and proinflammatory cells. In this work, we explore the possibility that selective small molecule inhibitors of this enzyme family could provide a novel approach to alleviate the inflammation that is associated with many inflammatory diseases. Methods: A series of novel substituted 4-hydrazinoquinazoline derivatives and fused triazoloquinazolines were designed, synthesized, and evaluated in vitro for their PDE7A inhibition activities, in comparison with Theophylline, a non-selective PDE inhibitor, and BRL50481, a selective PDE7A inhibitor. This series of novel quinazoline derivatives were synthesized via multi-step reactions. …
In Silico Identifcation Of New Potential Inhibitors Of Quorum Sensing By Gram‑Positive Bacteria Through Specialized Molecular Docking, Amgad Albohy, Najla A. Obaid, Mariam Mojally, Mohammed Abou Rehab, Najd Ahmad Alkhudhir
In Silico Identifcation Of New Potential Inhibitors Of Quorum Sensing By Gram‑Positive Bacteria Through Specialized Molecular Docking, Amgad Albohy, Najla A. Obaid, Mariam Mojally, Mohammed Abou Rehab, Najd Ahmad Alkhudhir
Pharmacy
Quorum sensing is the process by which bacterial cells can communicate by producing substances to regulate viable processes such as gene expression, virulence, and bioflm formation. Gram-positive bacteria such as Staphylococcus aureus and Enterococcus faecalis have specifc enzymes (autoinducers) that control the quorum sensing system. Sortase A is a surface protein that regulates virulence and cell‒cell communication in Gram-positive bacteria. To interfere with this system and reduce virulence and cell‒cell communication, quorum sensing inhibitors are used, which are nonantibiotic substances. In this study, we aimed to use Food and Drug Administration-approved drugs (analgesics and antipsychotics) and investigate their activity using …
Design, Molecular Modelling And Synthesis Of Novel Benzothiazole Derivatives As Bcl-2 Inhibitors, Amira Khalil, Hoda S. Ismail, Dalal A. Abou El Ella, Deena S. Lasheen, Rabah A. Taha
Design, Molecular Modelling And Synthesis Of Novel Benzothiazole Derivatives As Bcl-2 Inhibitors, Amira Khalil, Hoda S. Ismail, Dalal A. Abou El Ella, Deena S. Lasheen, Rabah A. Taha
Pharmacy
Apoptosis plays a crucial role in cancer pathogenesis and drug resistance. BCL-2 family of enzymes is considered as one of the key enzymes which is involved in apoptosis. When there is disruption in the balance between anti-apoptotic and pro-apoptotic members of the BCL-2 family apoptosis is dysregulated in the affected cells. Herein, 33 novel benzothiazole-based molecules 7a-i, 8a-f, 9a-b, 12a-e, 13a-d, 14a,b, and 17a-j were designed, synthesized and tested for their BCL-2 inhibitory activity. Scaffold hopping strategy was applied in designing of the target compounds. Compounds 13c and 13d showed the highest activity with IC50 values equal to 0.471 and …
Isatin-Pyrimidine Hybrid Derivatives As Enoyl Acyl Carrier Protein Reductase (Inha) Inhibitors Against Mycobacterium Tuberculosis, Amira Khalil, Samy Mohamady, Amgad Albohy, Marwa M. Abdel-Aziz, Abdalrahman Khalifa
Isatin-Pyrimidine Hybrid Derivatives As Enoyl Acyl Carrier Protein Reductase (Inha) Inhibitors Against Mycobacterium Tuberculosis, Amira Khalil, Samy Mohamady, Amgad Albohy, Marwa M. Abdel-Aziz, Abdalrahman Khalifa
Pharmacy
Tuberculosis is a worldwide problem that impose a burden on the economy due to continuous development of resistant strains. The development of new antitubercular drugs is a need and can be achieved through inhibition of druggable targets. Mycobacterium tuberculosis enoyl acyl carrier protein (ACP) reductase (InhA) is an important enzyme for Mycobacterium tuberculosis survival. In this study, we report the synthesis of isatin derivatives that could treat TB through inhibition of this enzyme. Compound 4l showed IC50 value (0.6 ± 0.94 µM) similar to isoniazid but is also effective against MDR and XDR Mycobacterium tuberculosis strains (MIC of 0.48 and …
Pyrazole-Sulfonamide Scaffold Featuring Dual-Tail Strategy As Apoptosis Inducers In Colon Cancer, Amira Khalil, Reham M. M. El Hazek, Nashwa H. Zaher, Hagar E. S. Emam, Marwa G. Elgazzar
Pyrazole-Sulfonamide Scaffold Featuring Dual-Tail Strategy As Apoptosis Inducers In Colon Cancer, Amira Khalil, Reham M. M. El Hazek, Nashwa H. Zaher, Hagar E. S. Emam, Marwa G. Elgazzar
Pharmacy
Dual-tail strategy has been successfully utilized in the development of novel carbonic anhydrase IX (CA IX) inhibitors. Herein we adopted this approach in the design and synthesis of a series of novel pyridine sulfonamide-pyrazole hybrid scaffold mimicking dual-tail inhibitors of CA IX. A library of 15 compounds was synthesized and assessed for their potential cytotoxic effects against colorectal cancer cells. Compounds 3, and 11 induced potential cytotoxic effects against the three cancer cell lines (HCT-116, HT-29, and SW-620) with IC50s’ of 45.88, 28.27, and 16.57 uM, 25.01, 8.99, and 3.27 µM, respectively. Both compounds induced cellular apoptosis …
Challenging Breast Cancer Through Novel Sulfonamide–Pyridine Hybrids: Design, Synthesis, Carbonic Anhydrase Ix Inhibition And Induction Of Apoptosis., Amira Khalil, Nashwa H. Zaher, Reham Mm Elhazek, Ahmed E. Gouda, Marwa G. Elgazzar
Challenging Breast Cancer Through Novel Sulfonamide–Pyridine Hybrids: Design, Synthesis, Carbonic Anhydrase Ix Inhibition And Induction Of Apoptosis., Amira Khalil, Nashwa H. Zaher, Reham Mm Elhazek, Ahmed E. Gouda, Marwa G. Elgazzar
Pharmacy
Background: Among the important key modulators of the tumor microenvironment and hypoxia is a family of enzymes named carbonic anhydrases. Herein, 11 novel sulfonamide–pyridine hybrids (2–12) were designed, synthesized and biologically evaluated for their potential use in targeting breast cancer. Methods & results: The para chloro derivative 7 reported the highest cytotoxic activity against the three breast cancer cell lines used. In addition, compound 7 was found to induce cell cycle arrest and autophagy as well as delaying wound healing. The IC50 of compound 7 against carbonic anhydrase IX was 253 ± 12 nM using dorzolamide HCl as control. Conclusion: …
Comparative Estimation Of The Cytotoxic Activity Of Different Parts Of Cynara Scolymus L.: Crude Extracts Versus Green Synthesized Silver Nanoparticles With Apoptotic Investigation, Shady Swidan, Amgad Khedr, Abdelaziz Farrag, Ali Nasr, Mohamed Nafie, Maged Abdel-Kader, Marwa Goda, Jihan Badr, Reda Abdelhameed
Comparative Estimation Of The Cytotoxic Activity Of Different Parts Of Cynara Scolymus L.: Crude Extracts Versus Green Synthesized Silver Nanoparticles With Apoptotic Investigation, Shady Swidan, Amgad Khedr, Abdelaziz Farrag, Ali Nasr, Mohamed Nafie, Maged Abdel-Kader, Marwa Goda, Jihan Badr, Reda Abdelhameed
Pharmacy
Different parts of Cynara scolymus L. and their green synthesized eco-friendly silver nanoparticles (AgNPs) were screened for their cytotoxicity and apoptotic activity. Results showed that flower extract AgNPs exhibited more potent cytotoxicity compared to the normal form against PC-3 and A549 cell lines with IC50 values of 2.47 μg/mL and 1.35 μg/mL, respectively. The results were compared to doxorubicin (IC50 = 5.13 and 6.19 μg/mL, respectively). For apoptosis-induction, AgNPs prepared from the flower extract induced cell death by apoptosis by 41.34-fold change and induced necrotic cell death by 10.2-fold. Additionally, they induced total prostate apoptotic cell death by a 16.18-fold …
Silver Nanoparticles Formulation Of Flower Head’S Polyphenols Of Cynara Scolymus L.: A Promising Candidate Against Prostate (Pc-3) Cancer Cell Line Through Apoptosis Activation, Shady Swidan, Amgad Khedr, Marwa Goda, Abdelaziz Farrag, Ali Nasr, Mohamed Nafie, Maged Abdel-Kader, Jihan Badr, Reda Abdelhameed
Silver Nanoparticles Formulation Of Flower Head’S Polyphenols Of Cynara Scolymus L.: A Promising Candidate Against Prostate (Pc-3) Cancer Cell Line Through Apoptosis Activation, Shady Swidan, Amgad Khedr, Marwa Goda, Abdelaziz Farrag, Ali Nasr, Mohamed Nafie, Maged Abdel-Kader, Jihan Badr, Reda Abdelhameed
Pharmacy
Cynara scolymus L. (Family: Compositae) or artichoke is a nutritious edible plant widely used for its hepatoprotective effect. Crude extracts of flower, bract, and stem were prepared and evaluated for their in vitro antioxidant activity and phenolic content. The flower crude extract exhibited the highest phenolic content (74.29 mg GAE/gm) as well as the best in vitro antioxidant activity using total antioxidant capacity (TAC), ferric reducing antioxidant power (FEAP), and 1,1-diphenyl-2-picrylhyazyl (DPPH) scavenging assays compared with ascorbic acid. Phenolic fractions of the crude extracts of different parts were separated and identified using high-performance liquid chromatography HPLC-DAD analysis. The silver nanoparticles …
Anti‑Estrogenic And Anti‑Aromatase Activities Of Citrus Peels Major Compounds In Breast Cancer, Maha Salama, Dina Mahmoud Elkersh, Shahira M. Ezzat, Yasmeen Attiaa, Engy A. Mahrous, Mohey Elmazar
Anti‑Estrogenic And Anti‑Aromatase Activities Of Citrus Peels Major Compounds In Breast Cancer, Maha Salama, Dina Mahmoud Elkersh, Shahira M. Ezzat, Yasmeen Attiaa, Engy A. Mahrous, Mohey Elmazar
Pharmacy
Estrogen signaling is crucial for breast cancer initiation and progression. Endocrine-based therapies comprising estrogen receptor (ER) modulators and aromatase inhibitors remain the mainstay of treatment. This study aimed at investigating the antitumor potential of the most potent compounds in citrus peels on breast cancer by exploring their anti-estrogenic and anti-aromatase activities. The ethanolic extract of different varieties of citrus peels along with eight isolated flavonoids were screened against estrogen-dependent breast cancer cell lines besides normal cells for evaluating their safety profile. Naringenin, naringin and quercetin demonstrated the lowest IC50s and were therefore selected for further assays. In silico molecular modeling …
Repurposing Of Omarigliptin As A Neuroprotective Agent Based On Docking With A2a Adenosine And Ache Receptors, Brain Glp-1 Response And Its Brain/Plasma Concentration Ratio After 28 Days Multiple Doses In Rats Using Lc-Ms/Ms, Bassam Ayoub, Haidy Michel, Shereen Mowaka, Moataz S. Hendy, Mariam M. Tadros
Repurposing Of Omarigliptin As A Neuroprotective Agent Based On Docking With A2a Adenosine And Ache Receptors, Brain Glp-1 Response And Its Brain/Plasma Concentration Ratio After 28 Days Multiple Doses In Rats Using Lc-Ms/Ms, Bassam Ayoub, Haidy Michel, Shereen Mowaka, Moataz S. Hendy, Mariam M. Tadros
Pharmacy
Abstract: The authors in the current work suggested the potential repurposing of omarigliptin (OMR) for neurodegenerative diseases based on three new findings that support the preliminary finding of crossing BBB after a single dose study in the literature. The first finding is the positive results of the docking study with the crystal structures of A2A adenosine (A2AAR) and acetylcholine esterase (AChE) receptors. A2AAR is a member of non-dopaminergic GPCR superfamily receptor proteins and has essential role in regulation of glutamate and dopamine release in Parkinson’s disease while AChE plays a major role in Alzheimer’s disease as the primary enzyme responsible …
Celecoxib Loaded In-Situ Provesicular Powder And Its In-Vitro Cytotoxic Effect For Cancer Therapy: Fabrication, Characterization, Optimization And Pharmacokinetic Evaluation, Shady Swidan, Ali Nasr, Sameh Elhady, Noha Badawi
Celecoxib Loaded In-Situ Provesicular Powder And Its In-Vitro Cytotoxic Effect For Cancer Therapy: Fabrication, Characterization, Optimization And Pharmacokinetic Evaluation, Shady Swidan, Ali Nasr, Sameh Elhady, Noha Badawi
Pharmacy
Introduction: Several recent studies have shown that the role of cyclooxygenase 2 (COX-2) in carcinogenesis has become more evident. It affects angiogenesis, apoptosis, and invasion, and plays a key role in the production of carcinogens. It has also been reported that COX-2 inhibitors such as celecoxib (CLX) might play an effective role in preventing cancer formation and progression. Formulation of CLX into nanovesicles is a promising technique to improve its bioavailability and anticancer efficacy. Aim: The aim of this study is to optimize and evaluate the anticancer efficacy of CLX-loaded in-situ provesicular powder composed of surfactants and fatty alcohol-based novel …