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1.
PLoS One ; 19(4): e0301086, 2024.
Article in English | MEDLINE | ID: mdl-38662719

ABSTRACT

There is still a great global need for efficient treatments for the management of SARS-CoV-2 illness notwithstanding the availability and efficacy of COVID-19 vaccinations. Olive leaf is an herbal remedy with a potential antiviral activity that could improve the recovery of COVID-19 patients. In this work, the olive leaves major metabolites were screened in silico for their activity against SARS-CoV-2 by molecular docking on several viral targets such as methyl transferase, helicase, Plpro, Mpro, and RdRp. The results of in silico docking study showed that olive leaves phytoconstituents exhibited strong potential antiviral activity against SARS-CoV-2 selected targets. Verbacoside demonstrated a strong inhibition against methyl transferase, helicase, Plpro, Mpro, and RdRp (docking scores = -17.2, -20, -18.2, -19.8, and -21.7 kcal/mol.) respectively. Oleuropein inhibited 5rmm, Mpro, and RdRp (docking scores = -15, -16.6 and -18.6 kcal/mol., respectively) respectively. Apigenin-7-O-glucoside exhibited activity against methyl transferase and RdRp (docking score = -16.1 and -19.4 kcal/mol., respectively) while Luteolin-7-O-glucoside inhibited Plpro and RdRp (docking score = -15.2 and -20 kcal/mol., respectively). The in vitro antiviral assay was carried out on standardized olive leaf extract (SOLE) containing 20% oleuropein and IC50 was calculated. The results revealed that 20% SOLE demonstrated a moderate antiviral activity against SARS-CoV-2 with IC50 of 118.3 µg /mL. Accordingly, olive leaf could be a potential herbal therapy against SARS-CoV-2 but more in vivo and clinical investigations are recommended.


Subject(s)
Antiviral Agents , Iridoids , Molecular Docking Simulation , Olea , Plant Extracts , Plant Leaves , Polyphenols , SARS-CoV-2 , Olea/chemistry , Antiviral Agents/pharmacology , Antiviral Agents/chemistry , SARS-CoV-2/drug effects , Plant Leaves/chemistry , Plant Extracts/pharmacology , Plant Extracts/chemistry , Iridoids/pharmacology , Iridoids/chemistry , Humans , Iridoid Glucosides/pharmacology , Iridoid Glucosides/chemistry , Glucosides/pharmacology , Glucosides/chemistry , Methyltransferases/metabolism , Methyltransferases/antagonists & inhibitors , COVID-19/virology , Coronavirus 3C Proteases/antagonists & inhibitors , Coronavirus 3C Proteases/metabolism , Coronavirus 3C Proteases/chemistry , Computer Simulation , COVID-19 Drug Treatment , Luteolin/pharmacology , Luteolin/chemistry , RNA Helicases/metabolism , RNA Helicases/antagonists & inhibitors , Apigenin/pharmacology , Apigenin/chemistry
2.
Int J Nanomedicine ; 19: 3045-3070, 2024.
Article in English | MEDLINE | ID: mdl-38559447

ABSTRACT

Background: Diabetes Mellitus is a multisystem chronic pandemic, wound inflammation, and healing are still major issues for diabetic patients who may suffer from ulcers, gangrene, and other wounds from uncontrolled chronic hyperglycemia. Marshmallows or Althaea officinalis (A.O.) contain bioactive compounds such as flavonoids and phenolics that support wound healing via antioxidant, anti-inflammatory, and antibacterial properties. Our study aimed to develop a combination of eco-friendly formulations of green synthesis of ZnO-NPs by Althaea officinalis extract and further incorporate them into 2% chitosan (CS) gel. Method and Results: First, develop eco-friendly green Zinc Oxide Nanoparticles (ZnO-NPs) and incorporate them into a 2% chitosan (CS) gel. In-vitro study performed by UV-visible spectrum analysis showed a sharp peak at 390 nm, and Energy-dispersive X-ray (EDX) spectrometry showed a peak of zinc and oxygen. Besides, Fourier transforms infrared (FTIR) was used to qualitatively validate biosynthesized ZnO-NPs, and transmission electron microscope (TEM) showed spherical nanoparticles with mean sizes of 76 nm and Zeta potential +30mV. The antibacterial potential of A.O.-ZnO-NPs-Cs was examined by the diffusion agar method against Gram-positive (Staphylococcus aureus and Bacillus subtilis) and Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa). Based on the zone of inhibition and minimal inhibitory indices (MIC). In addition, an in-silico study investigated the binding affinity of A.O. major components to the expected biological targets that may aid wound healing. Althaea Officinalis, A.O-ZnO-NPs group showed reduced downregulation of IL-6, IL-1ß, and TNF-α and increased IL-10 levels compared to the control group signaling pathway expression levels confirming the improved anti-inflammatory effect of the self-assembly method. In-vivo study and histopathological analysis revealed the superiority of the nanoparticles in reducing signs of inflammation and wound incision in rat models. Conclusion: These biocompatible green zinc oxide nanoparticles, by using Althaea Officinalis chitosan gel ensure an excellent new therapeutic approach for quickening diabetic wound healing.


Subject(s)
Althaea , Chitosan , Diabetes Mellitus , Metal Nanoparticles , Zinc Oxide , Humans , Animals , Rats , Zinc Oxide/chemistry , Chitosan/chemistry , Althaea/metabolism , Interleukin-6 , Tumor Necrosis Factor-alpha , Metal Nanoparticles/chemistry , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Wound Healing , Anti-Inflammatory Agents/pharmacology , Inflammation , Flowers , Microbial Sensitivity Tests , Plant Extracts/pharmacology , Plant Extracts/chemistry , Spectroscopy, Fourier Transform Infrared , X-Ray Diffraction
3.
J Enzyme Inhib Med Chem ; 39(1): 2292482, 2024 Dec.
Article in English | MEDLINE | ID: mdl-38086785

ABSTRACT

This study aims to investigate the phytoconstituents of the chloroform fraction of three Cystoseira spp. namely C. myrica, C. trinodis, and C. tamariscifolia using UPLC/ESI/MS technique. The results revealed the identification of 19, 20 and 11 metabolites in C. myrica, C. trinodis, and C. tamariscifolia, respectively mainly terpenoids, flavonoids, phenolic acids and fatty acids. Also, an in vitro antioxidant study using FRAP and DPPH assays was conducted where the chloroform fraction of C. trinodis displayed the highest antioxidant activity in both assays, which would be attributed to its highest total phenolics and total flavonoids. Besides, the investigation of COX-1, α-glucosidase and α-amylase inhibitory activities were performed. Regarding C. trinodis, it showed the strongest inhibitory activity towards COX-1. Moreover, it showed potent inhibitory activity towards α-glucosidase and α-amylase enzymes. According to the molecular docking studies, the major compounds characterised showed efficient binding to the active sites of the target enzymes.


Subject(s)
Chloroform , alpha-Glucosidases , Molecular Docking Simulation , Chromatography, High Pressure Liquid , Plant Extracts/pharmacology , Plant Extracts/chemistry , Antioxidants/pharmacology , Antioxidants/chemistry , Flavonoids/chemistry , alpha-Amylases
4.
Egypt J Immunol ; 30(1): 73-86, 2023 Jan.
Article in English | MEDLINE | ID: mdl-36592120

ABSTRACT

The worldwide medical systems are still being severely impacted by the coronavirus disease-2019 (COVID-19) pandemic, which is responsible for catastrophic mortality and morbidity. It becomes more and more obvious that this unique respiratory virus's impacts go beyond the respiratory system as time goes on and our comprehension of it deepens. The transmembrane serine protease 2 (TMPRSS2) protein is necessary for the severe acute respiratory syndrome coronavirus 2, which is the cause of COVID-19, to gain cellular entry through the angiotensin-converting enzyme 2 (ACE2) receptor. Most endocrine glands exhibit high levels of expression for ACE2 and TMPRSS2. This pays the attention to the effect of COVID-19 on the endocrine system. Besides its capability to pass to the central nervous system especially the hypothalamus inducing a lot of functional disorders in COVID-19 individuals. Although effective vaccines became widely available, and mortality declined but attention is shifting more and more to the lengthy health impacts on COVID-19 survivors. To inform suitable research and effective management, this review provides an overview of the data examining the impacts of COVID-19 on the endocrine glands besides the hypothalamus. In addition, we reported if the endocrinal and thalamic disorders could affect the incidence and progress of COVID-19.


Subject(s)
COVID-19 , SARS-CoV-2 , Humans , SARS-CoV-2/metabolism , Angiotensin-Converting Enzyme 2/metabolism , Peptidyl-Dipeptidase A , Hypothalamus/metabolism
5.
Microsc Res Tech ; 85(8): 2813-2825, 2022 Aug.
Article in English | MEDLINE | ID: mdl-35411989

ABSTRACT

In the present study, we investigated the antioxidant effect of grape seed extract (GSE) against chronic immobilization stress-induced zona fasciculata injury in Wistar male rats. Thirty male rats were divided into three groups: Non-stress group: rats were not subjected to stress protocol and received distilled water orally for 30 days. Stress group: rats received distilled water orally for 15 consecutive days before the induction of chronic immobilization stress experiment (repeated stress for 15 consecutive days), distilled water was continued along with the constant stress experiment. GSE-stress group: rats treated with oral GSE (300 mg/kg), administered orally for 15 consecutive days before the induction of chronic immobilization stress experiment (repeated stress for 15 consecutive days), GSE was continued along with the stress exposure. Chronic stress was induced by placing each animal in a restrainer for 2 h daily for 15 consecutive days in both Stress and GSE-stress groups. The serum corticosterone and adrenal cortex malondialdehyde (MDA) levels were measured as indices of stress. Immunohistochemistry of the inducible nitric oxide synthase (iNOS) as a nitrosative stress marker beside the adrenal cortex's ultrastructure, particularly zona fasciculata, was assessed. Chronic restraint stress significantly elevated the serum corticosterone and adrenal cortex MDA levels, while oral administration of GSE reduced the serum corticosterone level, adrenal cortex MDA levels, and iNOS immunoreactivity in zona fasciculata. Besides, adrenocortical ultrastructure significantly improved. These results suggested that GSE enhanced the antioxidant defense against reactive oxygen species produced under chronic stress conditions, protecting the adrenal cortex. RESEARCH HIGHLIGHTS: This research highlighted the significant protective effects of grape seed extract administration on the histological findings, both in light and electron microscopic studies, as well as the biochemical and functional parameters in cases of stress-induced adrenal cortex injury in rats.


Subject(s)
Grape Seed Extract , Animals , Antioxidants/metabolism , Antioxidants/pharmacology , Corticosterone/pharmacology , Electrons , Grape Seed Extract/pharmacology , Male , Oxidative Stress , Rats , Rats, Wistar , Water , Zona Fasciculata/metabolism
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