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1.
World J Urol ; 42(1): 221, 2024 Apr 08.
Artículo en Inglés | MEDLINE | ID: mdl-38587648

RESUMEN

PURPOSE: Fosfomycin has been used more frequently in managing uncomplicated urinary tract infections (UTIs) due to decreased compliance and increased multidrug-resistant bacteria. The aim of this network meta-analysis was to assess the efficacy of Fosfomycin compared to Nitrofurantoin, Trimethoprim-Sulfamethoxazole (TMP-SMX), and Ciprofloxacin in terms of clinical and microbiological cure alongside with other measurements. MATERIALS AND METHODS: We searched MEDLINE, Embase, and Cochrane Central Register of Controlled Trials (CENTRAL). We included randomized control trials (RCTs) with uncomplicated UTI patients who received Fosfomycin, Nitrofurantoin, TMP-SMX, or Ciprofloxacin and reported the clinical or microbiological cure. We used Cochrane Risk of Bias Assessment Tool to assess the included studies' quality. R-software was used for all statistical analysis. We ranked all antibiotics using the netrank function which yielded P scores. Frequentist network meta-analysis was used to assess the efficacy of all outcomes. RESULTS: We included 13 RCTs with a total number of 3856 patients that showed Fosfomycin ranked the highest among the other antibiotics with respect to clinical cure (P-score = 0.99) and microbiological cure (P-score = 0.99) while Ciprofloxacin ranked the lowest (P-score = 0.11 and 0.02, respectively). Moreover, Ciprofloxacin yielded the highest relapse rate (P-score = 1), whereas TMP-SMX had the lowest relapse rate (P-score = 0.07). As for the adverse events, Ciprofloxacin demonstrated the highest adverse events as opposed to Fosfomycin (P-score = 0.98 and 0.05, respectively). CONCLUSION: The network meta-analysis demonstrated that Fosfomycin is the most effective antibiotic in treating uncomplicated UTIs with respect to clinical cure, microbiological cure, and adverse events profile.


Asunto(s)
Fosfomicina , Infecciones Urinarias , Humanos , Antibacterianos/uso terapéutico , Fosfomicina/uso terapéutico , Nitrofurantoína , Combinación Trimetoprim y Sulfametoxazol , Metaanálisis en Red , Infecciones Urinarias/tratamiento farmacológico , Ciprofloxacina/uso terapéutico , Recurrencia
2.
Mar Drugs ; 20(10)2022 Oct 01.
Artículo en Inglés | MEDLINE | ID: mdl-36286452

RESUMEN

In this study, the LC-HRMS-assisted chemical profiling of Hyrtios erectus sponge led to the annotation of eleven major compounds (1-11). H. erectus-derived crude extract (HE) was tested in vitro for its antiproliferative activity against three human cancer cell lines, Hep-G2 (human liver cancer cell line), MCF-7 (breast cancer cell line), and Caco-2 (colon cancer cell line), before and after encapsulation within niosomes. Hyrtios erectus extract showed moderate in vitro antiproliferative activities towards the studied cell lines with IC50 values 18.5 ± 0.08, 15.2 ± 0.11, and 13.4 ± 0.12, respectively. The formulated extract-containing niosomes (size 142.3 ± 10.3 nm, PDI 0.279, and zeta potential 22.8 ± 1.6) increased the in vitro antiproliferative activity of the entrapped extract significantly (IC50 8.5 ± 0.04, 4.1 ± 0.07, and 3.4 ± 0.05, respectively). A subsequent computational chemical study was performed to build a sponge-metabolite-targets-cancer diseases network, by focusing on targets that possess anticancer activity toward the three cancer types: breast, colon, and liver. Pubchem, BindingDB, and DisGenet databases were used to build the network. Shinygo and KEGG databases in addition to FunRich software were used for gene ontology and functional analysis. The computational analysis linked the metabolites to 200 genes among which 147 genes related to cancer and only 64 genes are intersected in the three cancer types. The study proved that the co-occurrence of compounds 1, 2, 3, 7, 8, and 10 are the most probable compounds possessing cytotoxic activity due to large number of connections to the intersected cytotoxic genes with edges range from 9-14. The targets possess the anticancer effect through Pathways in cancer, Endocrine resistance and Proteoglycans in cancer as mentioned by KEGG and ShinyGo 7.1 databases. This study introduces niosomes as a promising strategy to promote the cytotoxic potential of H. erectus extract.


Asunto(s)
Antineoplásicos , Liposomas , Humanos , Antineoplásicos/farmacología , Antineoplásicos/química , Células CACO-2 , Mezclas Complejas , Océano Índico , Proteoglicanos , Poríferos
3.
Mar Drugs ; 20(10)2022 Oct 14.
Artículo en Inglés | MEDLINE | ID: mdl-36286462

RESUMEN

The protective and therapeutic anti-inflammatory and antioxidant potency of Malapterurus electricus (F. Malapteruridae) skin fish methanolic extract (FE) (300 mg/kg.b.wt/day for 7 days, orally) was tested in monosodium urate(MSU)-induced arthritic Wistar albino male rats' joints. Serum uric acid, TNF-α, IL-1ß, NF-𝜅B, MDA, GSH, catalase, SOD, and glutathione reductase levels were all measured. According to the findings, FE significantly reduced uric acid levels and ankle swelling in both protective and therapeutic groups. Furthermore, it has anti-inflammatory effects by downregulating inflammatory cytokines, primarily through decreased oxidative stress and increased antioxidant status. All the aforementioned lesions were significantly improved in protected and treated rats with FE, according to histopathological findings. iNOS immunostaining revealed that protected and treated arthritic rats with FE had weak positive immune-reactive cells. Phytochemical analysis revealed that FE was high in fatty and amino acids. The most abundant compounds were vaccenic (24.52%), 9-octadecenoic (11.66%), palmitic (34.66%), stearic acids (14.63%), glycine (0.813 mg/100 mg), and alanine (1.645 mg/100 mg). Extensive molecular modelling and dynamics simulation experiments revealed that compound 4 has the potential to target and inhibit COX isoforms with a higher affinity for COX-2. As a result, we contend that FE could be a promising protective and therapeutic option for arthritis, aiding in the prevention and progression of this chronic inflammatory disease.


Asunto(s)
Antioxidantes , Ácido Úrico , Ratas , Animales , Antioxidantes/metabolismo , Catalasa , Factor de Necrosis Tumoral alfa/metabolismo , Ciclooxigenasa 2 , Metanol , Glutatión Reductasa , Ratas Wistar , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Citocinas/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Extractos Vegetales/química , Fitoquímicos , Superóxido Dismutasa , Ácidos Esteáricos , Alanina , Glicina , Aminoácidos
4.
Molecules ; 27(17)2022 Aug 31.
Artículo en Inglés | MEDLINE | ID: mdl-36080381

RESUMEN

Malaria is one of the most important infectious diseases worldwide. The causative of the most severe forms of malaria, Plasmodium falciparum, has developed resistances against all the available antimalarial drugs. In the present study, the phytochemical investigation of the green seaweed Halimeda macroloba has afforded two new compounds 1-2, along with 4 known ones 3-6. The structures of the compounds had been confirmed using 1& 2D-NMR and HRESIMS analyses. Extensive machine-learning-supported virtual-screening suggested cytochrome-C enzyme as a potential target for compound 2. Docking, absolute-binding-free-energy (ΔGbinding) and molecular-dynamics-simulation (MDS) of compound 2 revealed the strong binding interaction of this compound with cytochrome-C. In vitro testing for crude extract and isolated compounds revealed the potential in vitro inhibitory activity of both extract and compound 2 against P. falciparum. The crude extract was able to inhibit the parasite growth with an IC50 value of 1.8 ± 0.35 µg/mL. Compound 2 also showed good inhibitory activity with an IC50 value of 3.2 ± 0.23 µg/mL. Meanwhile, compound 6 showed moderate inhibitory activity with an IC50 value of 19.3 ± 0.51 µg/mL. Accordingly, the scaffold of compound 2 can be considered as a good lead compound for the future development of new antimalarial agents.


Asunto(s)
Antimaláricos , Malaria Falciparum , Malaria , Algas Marinas , Antimaláricos/química , Citocromos , Humanos , Malaria/tratamiento farmacológico , Malaria Falciparum/tratamiento farmacológico , Extractos Vegetales/química , Plasmodium falciparum
5.
Mar Drugs ; 19(11)2021 Oct 26.
Artículo en Inglés | MEDLINE | ID: mdl-34822477

RESUMEN

Gnathonemuspetersii (F. Mormyridae) commonly known as Peters' elephant-nose fish is a freshwater elephant fish native to West and Central African rivers. The present research aimed at metabolic profiling of its derived crude oil via GC-MS analysis. In addition, wound healing aptitude in adult male New Zealand Dutch strain albino rabbits along with isolated bioactive compounds in comparison with a commercial product (Mebo®). The molecular mechanism was studied through a number of in vitro investigations, i.e., radical scavenging and inhibition of COX enzymes, in addition to in silico molecular docking study. The results revealed a total of 35 identified (71.11%) compounds in the fish oil, belonging to fatty acids (59.57%), sterols (6.11%), and alkanes (5.43%). Phytochemical investigation of the crude oil afforded isolation of six compounds 1-6. Moreover, the crude oil showed significant in vitro hydrogen peroxide and superoxide radical scavenging activities. Furthermore, the crude oil along with one of its major components (compound 4) exhibited selective inhibitory activity towards COX-2 with IC50 values of 15.27 and 2.41 µM, respectively. Topical application of the crude oil on excision wounds showed a significant (p < 0.05) increase in the wound healing rate in comparison to the untreated and Mebo®-treated groups, where fish oil increased the TGF-ß1 expression, down-regulated TNF-α, and IL-1ß. Accordingly, Peters' elephant-nose fish oil may be a potential alternative medication helping wound healing owing to its antioxidant and anti-inflammatory activities.


Asunto(s)
Antioxidantes/farmacología , Aceites de Pescado/farmacología , Peces , Cicatrización de Heridas/efectos de los fármacos , Animales , Antioxidantes/química , Antioxidantes/metabolismo , Organismos Acuáticos , Aceites de Pescado/química , Aceites de Pescado/metabolismo , Cromatografía de Gases y Espectrometría de Masas , Masculino , Modelos Animales , Simulación del Acoplamiento Molecular , Conejos
6.
Saudi Pharm J ; 28(12): 1834-1841, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-33424272

RESUMEN

In recent decades, marine microorganisms have become known for their ability to produce a wide variety of secondary bioactive metabolites. Several compounds have been isolated from marine microorganisms for the development of novel bioactives for the food and pharmaceutical industries. In this study, a number of microalgae were evaluated for their antimicrobial activity against gram-positive and gram-negative bacteria, including food and plant pathogens, using various extraction techniques and antimicrobial assays. Disc diffusion and spot-on-lawn assays were conducted to confirm the antimicrobial activity. To measure the potency of the extracts, minimum inhibition concentrations (MIultCs) were measured. Three microalgae, namely Isochrysis galbana, Scenedesmus sp. NT8c, and Chlorella sp. FN1, showed strong inhibitory activity preferentially against gram-positive bacteria. These microalgal species were then selected for further purification and analysis, leading to compound identification. By using a mixture of different chromatography techniques gas chromatography-mass spectrometry (GC-MS) and high-performance liquid chromatography (HPLC) and ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS), we were able to separate and identify the dominant compounds that are responsible for the inhibitory activity. Additionally, nuclear magnetic resonance (NMR) was used to confirm the presence of these compounds. The dominant compounds that were identified and purified in the extracts are linoleic acid, oleic acid, docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA). These compounds are the potential candidates that inhibit the growth of gram-positive bacteria. This indicates the potential use of microalgae and their antimicrobial compounds as biocontrol agents against food and plant pathogens.

7.
Saudi J Biol Sci ; 31(6): 103998, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38681227

RESUMEN

Alzheimer's disease (AD) continues to be a worldwide health concern, demanding innovative therapeutic approaches. This study investigates the neuroprotective potential of herbal compounds by scrutinizing their interactions with Beta-Secretase-1 (BACE1). Through comprehensive molecular docking analyses, three compounds, Masticadienonic acid (ΔG: -9.6 kcal/mol), Hederagenin (ΔG: -9.3 kcal/mol), and Anthocyanins (ΔG: -8.1 kcal/mol), emerge as promising BACE1 ligands, displaying low binding energies and strong affinities. ADME parameter predictions, drug-likeness assessments, and toxicity analyses reveal favorable pharmacokinetic profiles for these compounds. Notably, Masticadienonic Acid exhibits optimal drug-likeness (-3.3736) and negligible toxicity concerns. Hederagenin (drug-likeness: -5.3272) and Anthocyanins (drug-likeness: -6.2041) also demonstrate promising safety profiles. Furthermore, pharmacophore modeling elucidates the compounds' unique interaction landscapes within BACE1's active site. Masticadienonic acid showcases seven hydrophobic interactions and a hydrogen bond acceptor interaction with Thr232. Hederagenin exhibits a specific hydrogen bond acceptor interaction with Trp76, emphasizing its selective binding. Anthocyanins reveal a multifaceted engagement, combining hydrophobic contacts and hydrogen bond interactions with key residues. In conclusion, Masticadienonic acid, Hederagenin, and Anthocyanins stand out as promising candidates for further experimental validation, presenting a synergistic balance of efficacy and safety in combating AD through BACE1 inhibition.

8.
Int J Surg Case Rep ; 119: 109754, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38749390

RESUMEN

INTRODUCTION: Testicular torsions in elderly individuals are rare occurrences that are often managed surgically. CASE PRESENTATION: We present the first reported case of a successful manual detorsion in a 70-year-old male patient, resulting in clinical and radiological improvement. CLINICAL DISCUSSION: In this case report we discuss the role of manual detorsion alone in elderly without the need for surgery. CONCLUSION: Observation of our patient for 24 h post-detorsion ensured stability before discharge.

9.
Spectrochim Acta A Mol Biomol Spectrosc ; 309: 123842, 2024 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-38181623

RESUMEN

Vitamin D is one of the most essential nutrients for brain development, and deficiencies during pregnancy and early childhood development might be associated with autism. Regular monitoring of serum 25-hydroxyvitamin D3 level could help in early diagnosis and therapy. Analytical measurement of serum 25-hydroxyvitamin D3 level using the traditional matrix-matched calibration technique yields inaccurate results due to absence of serum matrix free from 25-hydroxyvitamin D3. The aim of this work was to develop a validated spectrofluorimetric methodology based on the standard addition approach for quantifying 25-hydroxyvitamin D3 levels in real serum samples of autistic children. The spectrofluorimetric methodology utilizes functionalized graphene quantum dots as a fluorescent probe for selective quantification of 25-hydroxyvitamin D3 level, which is based on measuring the quenching properties of 25-hydroxyvitamin D3 on a fluorescent probe. The standard addition approach exhibits a minimal matrix interference since it identically utilizes the same matrix of each study sample for creating its own calibration curve. The method was validated using the guidelines outlined in ICH M10 draft for endogenous compounds quantification. The method was successfully applied for quantifying the serum 25-hydroxyvitamin D3 levels in autistic and healthy children, and autistic children had significantly lower serum 25-hydroxyvitamin D3 levels (with a mean ± SD of 23.80 ± 17.19) when compared to healthy children (with a mean ± SD of 50.13 ± 18.74, P < 0.001). These results suggested an association between vitamin D deficiency and autism.


Asunto(s)
Trastorno Autístico , Grafito , Puntos Cuánticos , Niño , Humanos , Preescolar , Vitamina D , Calcifediol , Colorantes Fluorescentes , Espectrometría de Fluorescencia , Vitaminas
10.
PLoS One ; 19(2): e0294311, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38319945

RESUMEN

The in-vitro anti-proliferative evaluation of Sinularia levi total extract against three cell lines revealed its potent effect against Caco-2 cell line with IC50 3.3 µg/mL, followed by MCF-7 and HepG-2 with IC50 6.4 µg/mL and 8.5 µg/mL, respectively, in comparison to doxorubicin. Metabolic profiling of S. levi total extract using liquid chromatography coupled with high-resolution electrospray ionization mass spectrometry (LC-HR-ESI-MS) revealed the presence of phytoconstituents clusters consisting mainly of steroids and terpenoids (1-20), together with five metabolites 21-25, which were additionally isolated and identified through the phytochemical investigation of S. levi total extract through various chromatographic and spectroscopic techniques. The isolated metabolites included one sesquiterpene, two steroids and two diterpenes, among which compounds prostantherol (21) and 12-hydroperoxylsarcoph-10-ene (25) were reported for the first time in Sinularia genus. The cytotoxic potential evaluation of the isolated compounds revealed variable cytotoxic effects against the three tested cell lines. Compound 25 was the most potent with IC50 value of 2.13 ± 0.09, 3.54 ± 0.07 and 5.67 ± 0.08 µg/mL against HepG-2, MCF-7 and Caco-2, respectively, followed by gorgosterol (23) and sarcophine (24). Additionally, network analysis showed that cyclin-dependent kinase 1 (CDK1) was encountered in the mechanism of action of the three cancer types. Molecular docking analysis revealed that CDK1 inhibition could possibly be the reason for the cytotoxic potential.


Asunto(s)
Antineoplásicos , Farmacología en Red , Humanos , Células CACO-2 , Simulación del Acoplamiento Molecular , Antineoplásicos/farmacología , Extractos Vegetales/farmacología , Esteroides
11.
RSC Adv ; 14(4): 2340, 2024 Jan 10.
Artículo en Inglés | MEDLINE | ID: mdl-38213982

RESUMEN

Expression of concern for 'The anti-Alzheimer potential of Tamarindus indica: an in vivo investigation supported by in vitro and in silico approaches' by Abeer H. Elmaidomy et al., RSC Adv., 2022, 12, 11769-11785, https://doi.org/10.1039/D2RA01340A.

12.
Urol Case Rep ; 49: 102437, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-37398947

RESUMEN

Nephrolithiasis represents a common cause of non-obstetrical abdominal pain during pregnancy with 1 out of 200 pregnancies being affected. 20%-30% of patients require ureteroscopy. Many studies were done on safety of holmium:yttrium-aluminium-garnet (YAG) during pregnancy but none on Thulium Fiber Laser (TFL). To our knowledge, this is the first reported case of pregnant patient with nephrolithiasis that was treated using ureteroscopy and TFL. We present a 28 years old pregnant woman that presented to our hospital with a left distal ureteric stone. Patient underwent URS and lithotripsy using TFL. The procedure was tolerated with no complications.

13.
Nat Prod Res ; 37(20): 3531-3537, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-35666810

RESUMEN

This work was performed to dig into the phytochemical composition and bioactivities of Nocardiopsis sp. UR67 associated with the marine sponge Callyspongia sp. It was fermented in suspension and immobilised in calcium alginate bead cultures. The ethyl acetate extracts, afforded from the broth in each case named EG-49 and J-48g, respectively, revealed 16 chemical principles mostly belonging to polyketides, macrolides, and peptides. EG-49 and J-48g displayed anti-Candida albicans activity with IC50 values of 8.1 and 8.3 µg/mL, and a substantial cytotoxic effect against lung adenocarcinoma H1650 at IC50 12.6 and 13.7 µg/mL, respectively. However, only EG-49 exhibited a noteworthy anti-trypanosomal activity at 7.5 µg/mL. Molecular docking of the characterised compounds against Trypanosoma brucei trypanothione reductase demonstrated the highest binding models of griseochelin-methyl ester (9) and filipin-II (11), which drew considerable significance of the metabolites derived from Nocardiopsis sp. UR67 developing potential T. brucei trypanothione reductase inhibitors.

14.
Nat Prod Res ; 37(17): 2905-2910, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-36305731

RESUMEN

The main aim of our study is to investigate the anticancer potential of our cultivated entophytic fungal strains from Nigella sativa seeds. The strains were identified by sequencing of the partial 18S rRNA gene and the internal transcribed spacer (ITS) region as Aspergillus sp. (SA4), Penicillium sp. (SA5), and Fusarium sp. (SA6). We carried out metabolic profiling for three fungal strains to investigate their metabolites diversity. Profiling of the different extracts revealed their richness in diverse metabolites and consequently fourteen compounds (1-14) were annotated. In addition, the obtained extracts were examined against three cell lines HepG2, MCF-7 and Caco-2 showed activity with IC50 values in the range of 1.95-39.7 µg/mL. Finally, molecular docking study was performed showing questinol as the lowest glide binding score value (-5.925 kcal/mol) among all identified compounds. Our results showed Nigella sativa-associated endophytes as a promising source for further studies to look for anticancer secondary metabolites.

15.
Metabolites ; 13(6)2023 Jun 07.
Artículo en Inglés | MEDLINE | ID: mdl-37367890

RESUMEN

Tamarindus indica Linn (tamarind, F. Leguminosae) is one of the most widely consumed edible fruits in the world. Phytochemical investigation of tamarind pulp n-butanol fraction yielded one new (+)-pinitol glycoside compound 1 (25% w/w), and 1D, 2D NMR, and HRESIMS investigation were used to confirm the new compound's structure. (+)-Pinitol glycoside showed anti-Alzheimer potential that was confirmed in prophylactic and treatment groups by decreasing time for the T-maze test; decreased TAO, brain and serum AChE, MDA, tau protein levels, and ß amyloid peptide protein levels; and increasing GPX, SOD levels, and in vivo regression of the neurodegenerative features of Alzheimer's dementia in an aluminum-intoxicated rat model. The reported molecular targets for human Alzheimer's disease were then used in a network pharmacology investigation to examine their complex interactions and identify the key targets in the disease pathogenesis. An in silico-based analysis (molecular docking, binding free energy calculation (ΔGBinding), and molecular dynamics simulation) was performed to identify the potential targets for compound 1. The findings of this study may lead to the development of dietary supplements for the treatment of Alzheimer's disease.

16.
Sci Rep ; 13(1): 14192, 2023 08 30.
Artículo en Inglés | MEDLINE | ID: mdl-37648727

RESUMEN

The current study investigated the scabicidal potential of Egyptian mandarin peel oil (Citrus reticulata Blanco, F. Rutaceae) against sarcoptic mange-in-rabbits. Analysis of the oil's GC-MS identified a total of 20 compounds, accounting for 98.91% of all compounds found. Mandarin peel oil topical application improved all signs of infection, causing a scabicidal effect three days later, whereas in vitro application caused complete mite mortality one day later. In comparison to ivermectin, histopathological analysis showed that the epidermis' inflammatory-infiltration/hyperkeratosis-had disappeared. In addition to TIMP-1, the results of the mRNA gene expression analysis showed upregulation of I-CAM-1-and-KGF and downregulation of ILs-1, 6, 10, VEGF, MMP-9, and MCP-1. The scabies network was constructed and subjected to a comprehensive bioinformatic evaluation. TNF-, IL-1B, and IL-6, the top three hub protein-coding genes, have been identified as key therapeutic targets for scabies. From molecular docking data, compounds 15 and 16 acquired sufficient affinity towards the three screened proteins, particularly both possessing higher affinity towards the IL-6 receptor. Interestingly, it achieved a higher binding energy score than the ligand of the docked protein rather than displaying proper binding interactions like those of the ligand. Meanwhile, geraniol (15) showed the highest affinity towards the GST protein, suggesting its contribution to the acaricidal effect of the extract. The subsequent, MD simulations revealed that geraniol can achieve stable binding inside the binding site of both GST and IL-6. Our findings collectively revealed the scabicidal ability of mandarin peel extract for the first time, paving the way for an efficient, economical, and environmentally friendly herbal alternative for treating rabbits with Sarcoptes mange.


Asunto(s)
Lagomorpha , Escabiosis , Animales , Conejos , Escabiosis/tratamiento farmacológico , Regulación hacia Abajo , Egipto , Cromatografía de Gases y Espectrometría de Masas , Interleucina-6 , Ligandos , Simulación del Acoplamiento Molecular , Extractos Vegetales
17.
Food Funct ; 14(15): 7156-7175, 2023 Jul 31.
Artículo en Inglés | MEDLINE | ID: mdl-37462414

RESUMEN

Vitis vinifera Egyptian edible leaf extract loaded on a soybean lecithin, cholesterol, and Carbopol gel preparation (VVL-liposomal gel) was prepared to maximize the in vivo wound healing and anti-MRSA activities for the crude extract, using an excision wound model and focusing on TLR-2, MCP-1, CXCL-1, CXCL-2, IL-6 and IL-1ß, and MRSA (wound infection model, and peritonitis infection model). VVL-liposomal gel was stable with significant drug entrapment efficiency reaching 88% ± 3, zeta potential value ranging from -50 to -63, and a size range of 50-200 µm nm in diameter. The in vivo evaluation proved the ability of VVL-liposomal gel to gradually release the drugs in a sustained manner with greater complete wound healing effect and tissue repair after 7 days of administration, with a significant decrease in bacterial count compared with the crude extract. Phytochemical investigation of the crude extract of the leaves yielded fourteen compounds: two new stilbenes (1, 2), along with twelve known ones (3-14). Furthermore, a computational study was conducted to identify the genes and possible pathways responsible for the anti-MRSA activity of the isolated compounds, and inverse docking was used to identify the most likely molecular targets that could mediate the extract's antibacterial activity. Gyr-B was discovered to be the best target for compounds 1 and 2. Hence, VVL-liposomal gel can be used as a novel anti-dermatophytic agent with potent wound healing and anti-MRSA capacity, paving the way for future clinical research.


Asunto(s)
Vitis , Cicatrización de Heridas , Antibacterianos/química , Liposomas/química , Geles , Fitoquímicos/farmacología , Extractos Vegetales/química
18.
Plants (Basel) ; 12(12)2023 Jun 20.
Artículo en Inglés | MEDLINE | ID: mdl-37376007

RESUMEN

Abelmoschus esculentus Linn. (okra, F. Malvaceae) is a fruit widely consumed all over the world. In our study, the anti-Alzheimer's potential of A. esculentus was evaluated. An in vitro DPPH free radical assay on A. esculentus seed's total extract and AChE inhibition potential screening indicated a significant anti-Alzheimer's activity of the extract, which was confirmed through an in vivo study in an aluminum-intoxicated rat model. Additionally, in vivo results demonstrated significant improvement in Alzheimer's rats, which was confirmed by improving T-maze, beam balance tests, lower serum levels of AChE, norepinephrine, glycated end products, IL-6, and MDA. The levels of dopamine, BDNF, GSH, and TAC returned to normal values during the study. Moreover, histological investigations of brain tissue revealed that the destruction in collagen fiber nearly returns back to the normal pattern. Metabolomic analysis of the ethanolic extract of A. esculentus seeds via LC-HR-ESI-MS dereplicated ten compounds. A network pharmacology study displayed the relation between identified compounds and 136 genes, among which 84 genes related to Alzheimer's disorders, and focused on AChE, APP, BACE1, MAPT and TNF genes with interactions to all Alzheimer's disorders. Consequently, the results revealed in our study grant potential dietary elements for the management of Alzheimer's disorders.

19.
Cureus ; 14(11): e31522, 2022 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-36532936

RESUMEN

BACKGROUND: Uncontrolled diabetes has appeared as one of the major risk factors for morbidity and mortality in diabetic patients with coronavirus disease 2019 (COVID-19). Alterations in dietary habits, physical inactivity, and inability to take advice from the physician are some of the contributing factors. This study aimed to assess the impact of the COVID-19 lockdown in Saudi Arabia on medication accessibility, medication adherence, lifestyle, and quality of life of diabetes patients. METHODS: A cross-sectional observational study was conducted among diabetic patients using a self-reported questionnaire developed on an online platform (SurveyMonkey®). The survey was distributed through social media platforms (WhatsApp, Telegram). For those who were digitally illiterate, responses were collected by family members. The targeted population was type 1, type 2 and gestational diabetes patients. The analysis of the data was done using IBM SPSS Statistics, version 26. RESULTS: Four hundred forty-nine participants completed the survey. Most of the participants had type 2 diabetes (n=359; 79.8%) and were well educated (83.2%) with a high school degree and above. Complications from COVID-19 infection were reported in 12% (n=54) patients. During quarantine, 78.8% (n=354) of participants measured their blood glucose regularly. Results showed that during quarantine, 68.3% (n=311) participants skipped their scheduled follow-up whereas only 5.1% (n=23) of them took their medication inappropriately. CONCLUSION: This study reported good levels of self-monitoring of blood glucose levels, whereas patients' accessibility to seek healthcare services seemed to be interrupted. Further efforts are needed in the post-pandemic era to empower patients' self-care behaviors and utilize telehealth models to facilitate timely access to medical care.

20.
RSC Adv ; 12(19): 11769-11785, 2022 Apr 13.
Artículo en Inglés | MEDLINE | ID: mdl-35481086

RESUMEN

Tamarindus indica Linn. (Tamarind, F. Fabaceae) is one of the most widely consumed fruits in the world. A crude extract and different fractions of T. indica (using n-hexane, dichloromethane, ethyl acetate, and n-butanol) were evaluated in vitro with respect to their DPPH scavenging and AchE inhibition activities. The results showed that the dichloromethane and ethyl acetate fractions showed the highest antioxidant activities, with 84.78 and 86.96% DPPH scavenging at 0.10 µg mL-1. The n-hexane, dichloromethane, and ethyl acetate fractions inhibited AchE activity in a dose-dependent manner, and the n-hexane fraction showed the highest inhibition at 20 µg mL-1. The results were confirmed by using n-hexane, dichloromethane, and ethyl acetate fractions in vivo to regress the neurodegenerative features of Alzheimer's dementia in an aluminum-intoxicated rat model. Phytochemical investigations of those three fractions afforded two new diphenyl ether derivative compounds 1-2, along with five known ones (3-7). The structures of the isolated compounds were confirmed via 1D and 2D NMR and HRESIMS analyses. The isolated compounds were subjected to extensive in silico-based investigations to putatively highlight the most probable compounds responsible for the anti-Alzheimer activity of T. indica. Inverse docking studies followed by molecular dynamics simulation (MDS) and binding free energy (ΔG) investigations suggested that both compounds 1 and 2 could be promising AchE inhibitors. The results presented in this study may provide potential dietary supplements for the management of Alzheimer's disease.

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