Faculty Of Pharmacy Research Paper

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Clinical uses of cannabis and Catha edulis products
(Elsevier, 2024-01-01) Shahira M. Ezzat; Passent M. Abdel Baki; Rana M. Ibrahim; Doaa Abu Elezz; Mahmoud Abdelaziz; Mohamed A. Salem
The medicinal use of cannabis (Cannabis sativa) and khat (Catha edulis) as well as their products has been increased in the last decade. Medical cannabis and khat have been legalized in several countries. Additionally, the major cannabinoids, particularly cannabidiol and tetrahydrocannabinol, have been utilized for the development of FDA-approved pharmaceuticals. The clinical applications of cannabis and C. edulis products are complicated by legislation and regulations that are varied among countries. In this chapter, the pharmacological and the side effect profiles for the clinical uses of cannabis and C. edulis products are highlighted. Although, the clinical data for their use are continuing to evolve, the legal status needs to be authorized to keep the balance between clinical applications and limitations.
Extraction and isolation of cannabinoids
(Elsevier, 2024-01-01) Mohamed A. Salem; Rana M. Ibrahim; Passent M. Abdel Baki; Sohila M. Osman; Shahira M. Ezzat
Cannabis sativa L. is one of the most important medicinal plants that belongs to the family Cannabaceae. C. sativa is a herbaceous flowering plant that is indigenous to eastern Asia, but it is now cultivated worldwide due to the importance of its active constituents known as cannabinoids. Due to the growing interest in these compounds, various methods for their extraction and isolation were proposed. In this chapter, we will have an overview about the conventional and nonconventional methods for extraction of cannabinoids both from plant material and from biological samples for forensic purposes. Also we will review the methods for isolation of such compounds from different types of extracts as well as the modern methods for metabolomics and chemometric tools for analysis of cannabinoids.
Enhancing oral cancer treatment via photodynamic therapy: Gold nanoparticle-based delivery system for 5-aminolevulinic acid (5-ALA)
(Elsevier Ltd, 2024-09-10) Romesa Soomro; Mohamed Abdelmonem; Bachren Azra Saputra; Che Azurahanim Che Abdullah
Oral squamous cell carcinoma (OSCC) is a significant global health concern, responsible for approximately 300,000 new cases and 145,000 deaths annually, making it the sixth most common malignancy worldwide. Traditional treatments, including surgery, radiation, and chemotherapy, often lead to severe side effects such as physical disfigurement, functional loss, and systemic toxicity. These limitations have spurred the search for alternative therapies, with photodynamic therapy (PDT) gaining recognition for its reduced invasiveness, improved targeting, and better cosmetic outcomes. However, PDT faces challenges, including inadequate photosensitizer (PS) delivery, poor specificity, and degradation in physiological environments. Nanotechnology has emerged as a promising solution to enhance PDT by improving the stability, selectivity, and therapeutic efficacy of PSs. Gold nanoparticles (AuNPs) have shown the potential to enhance PDT outcomes, particularly in OSCC, by inhibiting tumor proliferation and improving diagnostic accuracy without systemic toxicity. Despite these advancements, the conventional chemical synthesis of AuNPs poses environmental concerns, high costs, and potential biocompatibility issues. This study introduces a novel biogenic synthesis approach for AuNPs, utilizing green chemistry principles to create more biocompatible and environmentally sustainable nanoparticles. The novelty of this research lies in the application of green-synthesized AuNPs to enhance PS delivery in PDT, offering a more effective and less toxic treatment option for oral cancer. This innovative approach addresses the limitations of current PDT and nanoparticle synthesis methods, contributing to the development of more sustainable and biocompatible cancer therapies. The study's findings are contextualized within the increasing scholarly and patent activity surrounding AuNPs and 5-aminolevulinic acid (5-ALA) in cancer therapies, underscoring the growing importance of this field in advancing OSCC management.
Metabolic Profiling of Millingtonia hortensis L.f. Leaves Using UHPLCMS/MS and Evaluation of its Antioxidant, Cytotoxic, Anticholinesterase Activities and Molecular Docking
(National Information and Documentation Centre (NIDOC), 2024-11-02) Sohila M. Elnaggar; Soumaya S. Zaghloul; Hanaa A. Kassem; Amira K. El Motayam
Background: Millingtonia hortensis L.f. known as Tree Jasmine or Indian Cork tree, stands as the only species within the genus Millingtonia and it is originated from South-East Asia, it belongs to family Bignoniaceae. The genus name, Millingtonia, is in honor of Sir Thomas Millington, the English botanist, while hortensis means “grown in gardens”. The phytochemical screening of M. hortensis L.f. showed the presence of different chemical classes as carbohydrates, tannins, saponins, flavonoids, cyclohexylethanoid glycosides, and volatile oil. Different pharmacological actions were reported such as antiproliferative, antimutagenic, antibacterial, antifungal, and antioxidant activities. Aim: This study aims to investigate the phytochemical constituents of M. hortensis L.f. and evaluate its biological activities. Material and Methods: The total ethanolic extract M. hortensis L.f. was assessed by LC-MS/MS profiling followed by spectrophotometric determination of total phenolics and flavonoids. For biological evaluation, the antioxidant activity was assessed using (DPPH, ABTS, FRAP, and ORAC) assays. In-vitro cytotoxic study was performed using colorectal cancer (LS-513) and hepatocellular carcinoma (HepG2) cell lines and also anticholinesterase activity was determined. Furthermore, some of the identified compounds were analyzed by molecular docking studies to determine the binding affinity between the ligands and the enzyme (acetylcholinesterase). Results: The LC-MS/MS analysis of the total ethanolic extract resulted in identification of twenty eight compounds. The level of total phenolic contents was (34.137 ± 0.509 µg Gallic acid Eq/mg) in the total ethanolic extract while the level of total flavonoid content in total ethanolic extract was (10.256 ± 0.579 µg Rutin Eq/mg). The results of ABTs, ORAC and DPPH antioxidant assays demonstrated that dichloromethane fraction of M. hortensis L.f. leaves has the highest effect for free radical scavenging, while the n-hexane extract showed the highest effect for free radical scavenging in the FRAP assay, in-vitro cytotoxic activity showed that the total ethanolic extract has the least IC50 which indicates its highest activity compared to the other fractions, anticholinesterase activity obtained by Ellman’s method indicates that dichloromethane fraction showed a significant activity against AChE causing 80.6 ± 0.007 % inhibition while ethyl acetate fraction showed least activity against AChE causing 31.8 ± 0.02 % inhibition at 0.1 mg/mL concentration. The molecular docking study revealed that apigenin was found to be more potent than hispidulin due to the strong interactions with amino acid residue SerA:200, HisA:440 and those of the peripheral region are crucial for strong inhibitory activities against AChE. Conclusions: The results of this study revealed that the plant’s identified phenolics and flavonoids, as detected in the LC-MS/MS analysis, may be correlated with the plant’s notable antioxidant, cytotoxic, and anticholinesterase activities.
Eco-friendly tea waste magnetite nanoparticles for enhanced adsorptive removal of norfloxacin and paroxetine from water
(Elsevier Inc., 2024-11-01) Lamis M. Fahmy; Dalia Mohamed; Marianne Nebsen; Ahmed H. Nadim
Traces of pharmaceuticals have been detected in water cycle raising concerns regarding the potential risks to human health and aquatic environment. Accordingly, removal of such compounds from water samples is a major concern. Herein, a facile and green NaOH modified tea waste magnetite nanoparticles have been fabricated for the adsorptive removal of a commonly used antibiotic (norfloxacin) and antidepressant (paroxetine) from water samples. The synthesized nanoparticles were characterized using TEM, FT-IR, DLS and VSM. Factors affecting the adsorption efficiency have been investigated with respect to pH (5, 7 and 9), adsorbent amount (0.125, 0.25 and 0.5 g), initial drug concentration (25, 50 and 100 µg/mL) and contact time (0.5, 1 and 2 h). The adsorption isotherms have been calculated. A percentage removal of 98 % and 99 % were obtained for simultaneous removal of 50 µg/mL norfloxacin and paroxetine, respectively in 2 h. Monitoring norfloxacin and paroxetine concentrations was performed through a validated HPLC-DAD method. The reusability of the nanoparticles has been studied for 3 adsorption–desorption cycles. No significant loss in adsorption efficiency was observed offering a sustainable water treatment. This study would offer a facile, green and economic protocol for the removal of complex organic compounds from water resources.
The efcacy of tixagevimab/cilgavimab (Evusheld) in prophylaxis and treatment of COVID-19 in immunocompromised patients: a systematic review and meta-analysis
(BioMed Central Ltd, 2024-12-01) Shaymaa Glhoom; Aya Fergany; Dina El‑Araby; Asmaa A. Abdelkhalek; Asmaa Gomaa; Eman O. Zayed; Mohamed Abd‑ElGwad
Background During the COVID-19 pandemic, some populations, including immunocompromised patients, could not tolerate COVID-19 vaccination or had low responses. Evusheld is a combined neutralizing monoclonal antibody containing tixagevimab and cilgavimab. The World Health Organization (WHO) has approved this combination as preexposure prophylaxis (PrEP) and treatment for immunocompromised patients. With the new variant, the (WHO) recommended an increase in dose from 300 to 600 mg with a booster dose after 6 months. The target of this review was to compare the efcacy of the two doses, 300 mg and 600 mg of tixagevimab/cilgavimab (Evusheld) as prophy‑ laxis for higher-risk individuals to reveal if there is a signifcant diference in efcacy between those two doses of the drug.
A cutting edge potentiometric determination of baricitinib in synthetic wastewater and in tablet dosage form using modified carbon paste ion-selective membrane
(Elsevier Inc., 2024-09-21) Heba T. Elbalkiny; Mona S. Elshahed; Dalia Mohamed; Azza A. Ashour; Rasha Th. El-Eryan
After the recent hit of COVID-19, many drugs were successively administered to save patients’ lives and those drugs reached aquatic sources, one of those drugs was Baricitinib. Driven by the current situation, a potentiometric technique using an ion-selective membrane (ISM) recipe drop cast on a modified carbon paste electrode was optimized for the superior determination of Baricitinib (BAR). The molecular docking was customized to optimize the proper ionophores incorporated in the ISM, revealing that beta-cyclodextrin (β-CD) is the most compatible ionophore with the studied drug. A multivariate optimization experimental design was employed to optimize the best experimental condition for the analytical method. To this end; dual nanoparticles (multi-walled carbon nanotubes and copper oxide nanoparticles) were incorporated in the carbon paste electrode, and the ISM recipe was enriched with β-CD and cation-exchanger (phosphotungstic acid) in a polyvinylchloride matrix plasticized with dibutyl phthalate. A Nernstian slope equal to 19.97 mV/decade with a linearity range of 7.99 × 10−7–1.00 × 10−3 M was obtained. The validated sensor exhibited good recovery when used to determine the studied drug in synthetic wastewater and tablet dosage form. The greenness of the method was evaluated using the Complementary Green Analytical Procedure Index and Blue Applicability Grade Index.
Optimizing nutraceutical-loaded trehalosomes in-situ gel for diabetic cataract management: Comprehensive in vitro and in vivo evaluations
(Editions de Sante, 2024-11-03) Aya Hussein; Maha El-Kayal; Rehab Nabil Shamma; Heba H. Awad; Nihal Farid Younes
This study aimed to develop Baicalin-loaded trehalosomes in situ gel (BA-THs-ISG) for the treatment of cataract, a degenerative eye condition that requires innovative approaches to enhance visual acuity and quality of life. A 33 D-optimal design was implemented for the preparation and statistical optimization of BA-THs. Various in-vitro studies were conducted to evaluate the features of the optimized formula, which was subsequently loaded into an optimum ISG to sustain the release pattern. To assess the therapeutic efficacy of BA-THs-ISG, an in-vivo study was conducted using a streptozotocin (STZ) induced diabetic cataract model. The results demonstrated that the optimized formula of desirability function of 0.878 had a particle size (PS) of 237.9 ± 2.87 nm, a polydispersity index (PDI) of 0.27 ± 0.03, a zeta potential (ZP) of −27.31 ± 1.27 mV, an entrapment efficiency (EE%) of 74.32 ± 1.08 % and sustained drug release over 6 h. After being loaded into ISG, BA-THs-ISG exhibited a gelation temperature of 35.00 ± 0.30 °C and a gelation time of 49 ± 2.63 s, meeting the intended criteria. Moreover, it effectively maintained drug release for a duration of 12 h. Compared to the BA solution in the in-vivo studies, BA-THs-ISG significantly reduced malondialdehyde content and enhanced superoxide dismutase and glutathione peroxidase activities without any irritation potential. Therefore, BA-THs-ISG is inferred to be a highly effective option for improving cataract symptoms.
Design, synthesis, and cytotoxicity screening of novel pyrazolopyrimidines over renal cell carcinoma (UO-31 cells) as p38α inhibitors, and apoptotic cells inducing activities
(Elsevier Masson s.r.l., 2025-01-05) Sara Y. Ewieda; Amr Sonousi; Aliaa M. Kamal; Mohamed K. Abdelhamid
A series of novel molecules with pyrazolopyrimidine-4-amine core were designed and synthesized as potential cytotoxic agents over Renal Cell Carcinoma cells (UO-31). Results of cytotoxic activity against UO-31 cells showed that pyrazolopyrimidines 19 and 31 were found to be more cytotoxic than sorafenib (SOR). The cytotoxic activity of these compounds appeared to correlate with their ability to inhibit p38α MAPK which are 2.53- and 2.27- folds more potent than SOR. Moreover, results of the cell cycle analysis as well as the results of annexin-V on the (UO-31) cells showed that pyrazolopyrimidines 19 and 31 had a pro-apoptotic activity higher than SOR by 1.42- and 1.20- folds, respectively. Furthermore, compounds 19 and 31 were found to be effective in arresting the cell cycle throughout the accumulation of the cells at G2/M phase. Finally, the tested compounds decreased the TNF concentration as well as increased the expression of tumor suppressor gene p53, Bax/BCL-2 ratio and caspase 3/7.
Relieving postherpetic neuralgia pain via gabapentin‑loaded bigels as an auspicious topical drug delivery system
(BioMed Central Ltd, 2024-10-08) Wessam H. Abd‑Elsalam; Abdulaziz Mohsen Al‑Mahallawi; Amal Makhlouf
Background Over the past decades, a substantial portion of the population worldwide has been infected with varicella zoster and most cases developed shingles. Unfortunately, shingles is usually accompanied by postherpetic neuralgia, which may persist for months to years after the resolution of the viral infection. Objectives Gabapentin is an orally gamma-aminobutyric acid analogue approved by the Food and Drug Administration to manage shingles postherpetic neuralgia. However, gabapentin shows nonlinear pharmacokinetics, with variable absorption and bioavailability along with its short half-life and long side efects that may include dizziness and somnolence, which calls for an appropriate topical dosage form. Bigels are unique semisolid dosage forms with boosted penetrability and satisfactory hydrophilic texture. Methods The current work pointed to formulating gabapentin-loaded bigels for the treatment of postherpetic neuralgia, where the analysis and optimization of design were performed via Design-Expert®. Results and conclusions The selected bigel (F5), incorporating 400 mg Span 60, 1000 mg Tween 80, and 1000 mg Transcutol, displayed spherical nanosized particles with acceptable viscosity and spreadability. Subsequent topical application of the selected bigel on the skin of Wistar rats, F5, demonstrated a boosted accumulation of gabapentin in the skin similar to PLO gel but superior to the drug solution. Furthermore, a histopathological study demonstrated the biosafety of the selected bigel when applied topically. Accordingly, gabapentin-loaded bigel would be considered a potentially topical dosage form for the delivery of gabapentin for the management of postherpetic neuralgia.
In silico analysis and comprehensive review of circular-RNA regulatory roles in breast diseases; a step-toward non-coding RNA precision
(Elsevier GmbH, 2024-10-19) Nadia M. Hamdy; Mona G. El-Sisi; Sherine M. Ibrahim; Heba ElNokoudy; Ahmad A. Hady; Gamal Eldein Fathy Abd-ellatef; Al-Aliaa M. Sallam; Bassant Mohamed Barakat
In the current comprehensive review, we first highlighted circRNAs, which are key ncRNAs. Next, we discussed the relationships among circRNAs and breast cancer subtypes via in silico databases analysis and extensive literature search. CircRNAs, that sponge miRNA axes or act as silencers of oncogenic mRNAs, have been extensively addressed in the context of this review. During BC pathogenesis, the circRNA/microRNA/messenger RNA (mRNA) axis plays a major role in disease growth, progression, and survival/resistance and could be targeted for improved treatment options. This review also aimed to address oncogenic and tumor suppressor mRNAs, which are regulated by various circRNAs in BC. Moreover, we mentioned the relation of different circRNAs with cancer hallmarks, patient survival together with drug resistance. Additionally, we discussed circRNAs as vaccines and biomarkers in BC. Finally, we studied exosomal circRNAs as a hot interesting area in the research.
A sustainable and green HPLC-PDA technique for the simultaneous estimation of Post-COVID-19 syndrome co-administered drugs with greenness and whiteness assessment
(Nature Publishing Group, 2024-10-01) Passant M. Medhat; Manal Mohamed Fouad; Hany H. Monir; Nermine S.Ghoniem
COVID-19 has been a growing global concern in the past four years. Several syndromes associated with this multi-organ viral infection have been observed since the outbreak. According to estimates, 10–15% of people with SARS-CoV- infection may have post-COVID-19 syndrome. Even months after infection, common residual signs and symptoms include myalgia, exhaustion, shortness of breath, rapid heartbeat, stroke, and memory and cognitive impairment which can negatively affect survivors’ quality of life and may consequently lead to their death. Therefore, it is necessary to think about potential therapy options for dealing with both short and long-term impacts. Paracetamol (a common analgesic and antipyretic) and Dexketoprofen Trometamol (a non-steroidal anti-inflammatory drug) are used together to relieve post-COVID symptoms like myalgia (muscle pain) and headache. Additionally, to prevent thrombotic events, Rivaroxaban is recommended for 35 days following discharge. Thus an eco-friendly HPLC-DAD technique was developed for simultaneous quantification of Paracetamol, Dexketoprofen Trometamol, and Rivaroxaban which are co-administered for treatment of post-COVID-19 syndrome. The suggested method was found to be linear in the concentration ranges of 3.00–45.00 µg/mL, 0.5–50.00 µg/mL, and 0.15–20.00 µg/mL, and a limit of detection down to 0.531 µg/mL, 0.095 µg/mL and 0.047 µg/mL for Paracetamol, Dexketoprofen Trometamol and Rivaroxaban, respectively. This method was effectively used to quantify the studied drugs in their bulk powder and spiked human plasma with high percentage recoveries (96.55–99.46%). The suggested approach was validated per International Conference on Harmonization (ICH) requirements and found to be within the acceptable ranges. The method was developed using Green Analytical Chemistry (GAC) principles, with the solvents used and run time having a significant effect on the method’s greenness. “Non-toxic” ethanol served as the organic modifier in the mobile phase, moreover, the total run time was 12 min making it suitable for the routine analysis of the mentioned drugs in plasma samples. To get a full image of the method’s greenness profile; two most recent greenness assessment tools, the Green Analytical Procedure Index (GAPI), and the Analytical GREEnness metric (AGREE), were employed, with White Analytical Chemistry (WAC) principles proving its environmental safety.
Synthesis of S-alkylated oxadiazole bearing imidazo[2,1-b]thiazole derivatives targeting breast cancer: In vitro cytotoxic evaluation and in vivo radioactive tracing studies
(Academic Press Inc, 2024-11-02) Eman R. Mohammed; Manal Abdel Fattah Ezzat; Emad M. Seif; Basma M. Essa; Hatem A. Abdel-Aziz; Tamer M. Sakr; Hany S. Ibrahim
Breast cancer is the most common invasive cancer diagnosed in women, accounting for most cancer-related fatalities globally. Numerous investigations have revealed that breast cancer is characterized by abnormal expression and maintenance of EGFR levels. In terms of structural study and optimization of several EGFR inhibitors, two series of oxadiazole bearing imidazo[2,1-b]thiazole derivatives were designed and synthesized as potential EGFR inhibitors and assessed for their antitumor activity at NCI-USA. Four derivatives 3b, 3c, 3d and 3e elicited remarkable GI% against MDA-MB-468, T-47D and MCF-7 breast cancer cell lines. Thereafter, MTT assay was performed to reveal that compounds 3b (IC50 = 2.27 µM) and 3d (IC50 = 1.46 µM) showed promising cytotoxic activity against MCF-7 and MDA-MB-468 cell lines, respectively, compared to their reference drugs. Compounds 3b, 3d and 3e revealed good selectivity toward tumor cells with reasonable safety profile when tested against the normal cell line MCF-10a. In vitro EGFR inhibitory assay demonstrated that compounds 3b (IC50 = 0.099 µM) and 3d (IC50 = 0.086 µM) exhibited comparable inhibitory activity to the standard drug erlotinib (IC50 = 0.046 µM). A flow cytometric analysis demonstrated that derivatives 3b and 3d arrested the cell cycle at the S phase in MCF-7 and MDB-MB-468, respectively. Furthermore, the most active derivative 3d was subjected to in vivo radioactive studies. In-vivo biodistribution of 99mTc-3d complex showed a notable elevated accumulation in the targeted sarcoma muscle, indicating the targeting capacity of compound 3d in the tumor of sarcoma mice model. The binding mode of compounds 3b and 3d with EGFR was studied by molecular docking and was further inspected by molecular dynamic simulations. Both compounds were shown to be stable during the course of simulation and demonstrated a plausible interaction pattern with the EGFR binding pocket.
Cilostazol Combats Lipopolysaccharide-Induced Hippocampal Injury in Rats: Role of AKT/GSK3β/CREB Curbing Neuroinflammation
(Wiley Online Library , 2024-09-26) Doaa Abou El-ezz; Waleed Aldahmash; Tuba Esatbeyoglu; Sherif M. Afifi; Marawan Abd Elbaset
Neuroinflammation is important in the pathophysiology of several degenerative brain disorders. This study looked at the potential neuroprotective benefits of cilostazol, a phosphodiesterase inhibitor, against LPS-induced hippocampus damage in rodents and the principal molecular involvement of AKT/GSK3β/CREB signaling pathways. Behavioral tests revealed that cilostazol successfully corrected LPS-induced neurobehavioral impairments. Furthermore, cilostazol therapy lowered hippocampal levels of amyloid beta 1–42 (Aβ1-42) and p-tau protein, both of which are critical pathological indicators of neurodegenerative disorders. Furthermore, cilostazol administration suppressed LPS-induced rises in hippocampus caspase-3 and NF-κB levels while elevating rat B-cell/lymphoma 2 (BCL2) and brain-derived neurotrophic factor (BDNF) levels, which are implicated in neuronal survival and synaptic plasticity. Cilostazol treatment also restored the decreased phosphorylation of protein kinase B (p-AKT) and reduced the elevated levels of phosphorylated glycogen synthase kinase-3 beta (p-GSK3β) and cAMP response element-binding protein (CREB) in the hippocampus of LPS-treated rats. Histopathological examination revealed that cilostazol ameliorated LPS-induced brain damage with reduced neuronal loss and gliosis. Immunohistochemistry analysis showed a decrease in Iba-1 expression, indicating a reduction in microglial activation in the cilostazol-treated group compared to the LPS group. The findings advocate that cilostazol exerts neuroprotective effects against LPS-induced hippocampal injury by modulating the AKT/GSK3β/CREB pathway and curbing neuroinflammation. Cilostazol may hold promise as a therapeutic agent for neuroinflammatory conditions associated with neurodegenerative diseases.
Aspirin-based Organoiron Dendrimers as Promising Anti-inflammatory, Anticancer, and Antimicrobial Drugs.
(Multidisciplinary Digital Publishing Institute (MDPI), 2021-10-22) Maysun Ramadan; Amani Anwar Abdelghani; Laila H. Abdelrahman; Rabin Bissessur
Designing nanocarriers with actions directed at a specific organ or tissue is a very promising strategy since it can significantly reduce the toxicity of a bioactive drug. In this study, an organometallic dendrimer was used to synthesize a biocompatible drug delivery system by attaching aspirin to the periphery of the dendrimer. Our goal is to enhance the bioavailability and anticancer activity of aspirin and reduce its toxicity through successive generations of organoiron dendrimers. The biological activity of aspirin-based dendrimer complexes was evaluated. The result of antimicrobial activity of the synthesized dendrimers also demonstrated an increase in their antimicrobial activity with increased generation of the dendrimers for most types of microorganisms. This study reveals for the first time that organoiron dendrimers linked with aspirin exhibit an excellent Gram-negative activity comparable to the reference drug Gentamicin. All synthesized dendrimers were tested for their anticancer activity against breast cancer cell lines (MCF-7), hepatocellular cell lines (Hep-G2), and a non-cancer cell line, Human Embryonic Kidney (HEK293), using the MTT cell viability assay and compared against a standard anticancer drug, Doxorubicin. Compounds G3-D9-Asp and G4-D12-Asp exhibited noticeable activity against both cell lines, both of which were more effective than aspirin itself. In addition, the in vivo anti-inflammatory activity and histopathology of swollen paws showed that the designed aspirin-based dendrimers displayed significant anti-inflammatory activity; however, G2-D6-Asp showed the best anti-inflammatory activity, which was more potent than the reference drug aspirin during the same period. Moreover, the coupling of aspirin to the periphery of organoiron dendrimers showed a significant reduction in the toxicity of aspirin on the stomach.
A comparative UPLC‑orbitrap‑MS‑based metabolite profiling of three Pelargonium species cultivated in Egypt
(Springer Nature, 2024-10-01) Rana M. Merghany; Mohamed A. Salem; Shahira M. Ezzat; Sherifa F. A. Moustafa; Salma A. El‑Sawi; Meselhy R. Meselhy
Several Pelargonium species are cultivated mainly to produce essential oils used in perfume industry and for ornamental purposes. Although the chemical composition and biological activities of their essential oils were extensively investigated, there is limited information about the chemical composition of their non-volatile constituents. In this study, we report an Ultra-Performance Liquid Chromatography-Mass Spectrometry (UPLC-MS)-based metabolomics approach for the annotation and analysis of various metabolites in three species; P. graveolens, P. denticulatum, and P. fragrans utilizing The Global Natural Product Social Molecular Networking (GNPS) and multivariate data analyses for clustering of the metabolites. A total of 154 metabolites belonging to different classes were annotated. The three species are good sources of coumarins, benzoic acid derivatives, organic acids, fatty acids, and phospholipids. However, the highest level of flavonols (mono- and di-O-glycosides) and cinnamic acid derivatives was found in P. graveolens and P. denticulatum, whereas tannins and flavone C-glycosides were abundant in P. fragrans. The metabolic profiles clarified here provide comprehensive information on the non-volatile constituents of the three Pelargonium species and can be employed for their authentication and possible therapeutic applications.
Formulation and characterization of tea tree and jojoba oils nano-emulgel for in-vivo wound healing assessment
(Elsevier B.V, 2025-01-01) Nehal Kh. Mohamed; Asmaa A. Metwally; Sally M.Y. Fared; A. Farid; Mohamed Taha
Cutaneous wounds are the most common surgical affections among living organisms worldwide, and their healing may be interrupted by several factors. This study aimed to formulate and evaluate the antioxidant, anti-inflammatory, and antimicrobial activity of tea tree and jojoba oils nano-emulsions, additionally, investigating the cytotoxicity of the optimized formula was investigated on normal human lung fibroblast cells (WI-38) by MTT colorimetric assay, additionally its in-vivo wound healing. Nano-emulsions (NEs) were prepared using a high-energy method and characterized by Transmission electron microscopy (TEM), Zeta potential, droplet size, and poly dispersive index (PDI). Nano-emulgel (NEG) was formulated by mixing the standard NE with carbopol® 940. For in-vivo wound healing, thirty adult female albino rats were assigned into control, moist exposed burn ointment (Mebo), and NEG-treated groups. The healing was assessed by analysis of superoxide dismutase (SOD), malondialdehyde (MDA), tumor necrosis factor-alpha (TNF-α), interleukin-1β (IL-1β), and histopathology in healed wound tissues. All formulations demonstrated antioxidant, anti-inflammatory, and antimicrobial activity against Bacillus Subtilis, Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Salmonella typhi, Enterococcus faecalis, and Candida albicans. The CC50 of the optimized formula was 453.82± 3.87 µg/mL, with a mean droplet size of 105.4 nm and a zeta potential of −39.2 ± 2.1 mV. NEG enhanced wound closure compared to Mebo-treated and control groups. Also, MDA significantly decreased and SOD significantly increased in NEG and Mebo-treated groups compared to the control (p ˂ 0.05). TNF-α, and IL-1β significantly decreased in NEG and Mebo-treated compared to the control (p < 0.05). Histopathology revealed reduced inflammatory cell infiltration, rapid epithelization, and increased collagen deposition in NEG-treated wound tissues compared to the control and Mebo-treated wounds. In conclusion, the NEG containing tea tree and jojoba oils demonstrated significant antioxidant, anti-inflammatory, antimicrobial, and wound healing activities.
Molecular insight of miRNA-217 role in the pathogenesis of myocardial infarction: Promising diagnostic biomarker and therapeutic target
(KeAi Communications Co., 2025-02-01) Mai A. Zaafan; Amr M. Abdelhamid
Background: Globally, myocardial infarction (MI) is one of the main causes of death. This study aims to investigate the role of miR-217 in the pathogenesis through targeting MAPK and PI3K/AKT signaling pathways in experimental model of myocardial infarction and studying the possible cardioprotective role of dihydromyricetin (DHM) through modulation of this pathway. Methods: Dihydromyricetin was injected (100 mg/kg; p.o.) in isoprenaline induced myocardial infarction rat model for 14 days. Rats were anaesthetized and blood samples were taken for serum separation, estimation of creatine kinase-MB (CK-MB), and troponin-I levels after 24 h had passed since the last isoprenaline injection. In addition, the hearts were also used for the other biochemical studies and the histological evaluation. Results: DHM resulted in a significant suppression of the elevated levels miR-217 and MAPK compared to the MI control group and restored the normal level of serum CK-MB. Furthermore, DHM successfully restored the oxidative balance and halted the pro-inflammatory mediators in the cardiac tissue. Conclusion: Accordingly, our experiment emphasizes the anti-ischemic property that has been demonstrated through modulation of expression level of miR-217 and consequent deactivation of MAPK and PI3K/AKT signaling pathways, and this was assured by halting downstream pro-inflammatory markers.
Computational metal-flavonoids complexes presentation of greenly synthesized silver nanoparticles combined flavonoids from Lens culinaris L. as anticancer agents using BcL-2 and IspC proteins
(Taylor and Francis Ltd, 2024-10-01) Heba W. Alhamdi; Fatma Alzahraa Mokhtar; Fouad Lamghari Ridouane; Ali A. Shati; Serag Eldin I. Elbehairi; Lamiaa I. Fahmy; Mohammad Y. Alfaifi; Nada K. Sedky; Heba A. Fahmy
Lens culinaris L., has been widely recognized for its medical applications. LC-ESI-TOF-MS identified 22 secondary metabolites including phenolics, flavonoids, and anthocyanidin glycosides among its total extract (LCTE). The study aimed to apply LCTE as a biogenic material for reducing and capping the silver nanoparticles (LC-AgNPs). The ynthesized LC-AgNPs were characterized using different techniques. The UV absorption was observed at λmax 379 nm. LC-AgNPs were spherical, with 19.22 nm average size. The face cubic centre nature was demonstrated by HR-TEM and XRD. The LC-AgNPs were then evaluated for their anticancer and antimicrobial potentials. LC-AgNPs showed an extremely potent cytotoxic activity against MCF-7, HCT-116 and HepG2 cell lines (IC50= 0.37, 0.35 and 0.1 µg/mL, respectively). LC-AgNPs induced significant apoptotic effects in the three examined cancer cell lines. LC-AgNPs resulted in sequestration of cells in G1 phase of the cell cycle in both MCF-7 and HCT-116 cells, meanwhile it trapped cells at the G2 phase in HepG2 cells. Moreover, the antimicrobial activity of LC-AgNPs was highly confirmed against Klebsiella pneumoniae and Acinetobacter baumannii. Molecular docking study designated Kaempferol-3-O-robinoside-7-O-rhamnoside and Quercetin-3-D-xyloside as the topmost LCTE active constituents that caused inhibition of both Bcl-2 and IspC cancer targets in combination with the produced silver nanoparticles.
Enhancing oral cancer treatment via photodynamic therapy: Gold nanoparticle-based delivery system for 5-aminolevulinic acid (5-ALA)
(Published by Elsevier Ltd, 2024-09-10) Romesa Soomro; Mohamed Abdelmonem; Bachren Azra Saputra; Che Azurahanim Che Abdullah
Oral squamous cell carcinoma (OSCC) is a significant global health concern, responsible for approximately 300,000 new cases and 145,000 deaths annually, making it the sixth most common malignancy worldwide. Traditional treatments, including surgery, radiation, and chemotherapy, often lead to severe side effects such as physical disfigurement, functional loss, and systemic toxicity. These limitations have spurred the search for alternative therapies, with photodynamic therapy (PDT) gaining recognition for its reduced invasiveness, improved targeting, and better cosmetic outcomes. However, PDT faces challenges, including inadequate photosensitizer (PS) delivery, poor specificity, and degradation in physiological environments. Nanotechnology has emerged as a promising solution to enhance PDT by improving the stability, selectivity, and therapeutic efficacy of PSs. Gold nanoparticles (AuNPs) have shown the potential to enhance PDT outcomes, particularly in OSCC, by inhibiting tumor proliferation and improving diagnostic accuracy without systemic toxicity. Despite these advancements, the conventional chemical synthesis of AuNPs poses environmental concerns, high costs, and potential biocompatibility issues. This study introduces a novel biogenic synthesis approach for AuNPs, utilizing green chemistry principles to create more biocompatible and environmentally sustainable nanoparticles. The novelty of this research lies in the application of green-synthesized AuNPs to enhance PS delivery in PDT, offering a more effective and less toxic treatment option for oral cancer. This innovative approach addresses the limitations of current PDT and nanoparticle synthesis methods, contributing to the development of more sustainable and biocompatible cancer therapies. The study's findings are contextualized within the increasing scholarly and patent activity surrounding AuNPs and 5-aminolevulinic acid (5-ALA) in cancer therapies, underscoring the growing importance of this field in advancing OSCC

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