Scientia Pharmaceutica最新文献_第8页

Orally Administered Prosochit®-Based Nanoparticles of Insulin Ameliorates Alloxan-Induced Diabetes in Rats 口服基于Prosochit®的胰岛素纳米颗粒改善大鼠四氧嘧啶诱导的糖尿病

IF 2.5

Scientia Pharmaceutica Pub Date : 2022-10-17 DOI: 10.3390/scipharm90040066

E. Olorunsola, K. G. Davies, Enomfon B. Essien, M. Alozie, M. Adedokun, F. Ahsan

{"title":"Orally Administered Prosochit®-Based Nanoparticles of Insulin Ameliorates Alloxan-Induced Diabetes in Rats","authors":"E. Olorunsola, K. G. Davies, Enomfon B. Essien, M. Alozie, M. Adedokun, F. Ahsan","doi":"10.3390/scipharm90040066","DOIUrl":"https://doi.org/10.3390/scipharm90040066","url":null,"abstract":"This work was aimed to assess the antidiabetic effect of orally administered Prosochit®-based nanoparticles of insulin in an animal model. Five batches of insulin-loaded nanoparticles were prepared as dry water-in-oil-in-water emulsions using different emulsifiers (prosopis gum, Prosochit® 201, Prosochit® 101, Prosochit® 102, and chitosan) for the outer emulsion. Unloaded Prosochit® 101-based nanoparticles were also formulated. The morphology and size distribution of the nanoparticles were studied using a scanning electron microscope and Zetasizer. Forty alloxan-induced diabetic Wistar rats were divided into eight groups. The different groups were administered daily with different formulations (unloaded nanoparticles, the 5 loaded nanoparticles equivalent to 50 IU insulin per kg, purified water, and Actrapid) for 14 days. Blood glucose level was monitored and determined over 24 h. Fasting blood sugar was also taken on days 3, 5, 7, and 14. A graph of the percent blood glucose level relative to time 0 h was plotted against time. The particles showed a water-in-oil-in-water constitution. Both the drug-loaded and the unloaded Prosochit®-based nanoparticles were of nano dimension. There was a significant difference (p < 0.0001) in the antidiabetic effects of all insulin-loaded nanoparticles compared with the negative control. There was no significant difference across the insulin-loaded nanoparticles of prosopis gum, Prosochit® 201, Prosochit® 102, and chitosan while the insulin-loaded Prosochit® 101 nanoparticles showed the best activity, which is comparable to subcutaneous insulin, reducing blood glucose levels to 32.20 ± 3.79%. All the oral Prosochit®-based insulin nanoparticles are characterized by appreciable antidiabetic activity with the activity of Prosochit® 101-based nanoformulation being comparable to that of the subcutaneous insulin.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2022-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47833174","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

GC-MS Analysis of the Phytochemical Constituents, Safety Assessment, Wound Healing and Anti-Inflammatory Activities of Cucurbita pepo Leaf Extract in Rats 大鼠南瓜叶提取物的植物化学成分、安全性评价、伤口愈合及抗炎活性的GC-MS分析

IF 2.5

Scientia Pharmaceutica Pub Date : 2022-10-14 DOI: 10.3390/scipharm90040064

E. Akubugwo, O. Emmanuel, C. Ekweogu, Ositadinma Chinyere Ugbogu, Tochukwu Remigius Onuorah, Ozioma Glory Egeduzu, E. Ugbogu

{"title":"GC-MS Analysis of the Phytochemical Constituents, Safety Assessment, Wound Healing and Anti-Inflammatory Activities of Cucurbita pepo Leaf Extract in Rats","authors":"E. Akubugwo, O. Emmanuel, C. Ekweogu, Ositadinma Chinyere Ugbogu, Tochukwu Remigius Onuorah, Ozioma Glory Egeduzu, E. Ugbogu","doi":"10.3390/scipharm90040064","DOIUrl":"https://doi.org/10.3390/scipharm90040064","url":null,"abstract":"In traditional medicine, Cucurbita pepo L. is used for the treatment of rheumatism, diabetes, inflammations, and wound injuries. This study was conducted to evaluate the phytochemical constituents, safety profile, wound healing, and anti-inflammatory activities of Cucurbita pepo leaf extract in rats. The phytochemical analysis of C. pepo extract was carried out using gas chromatography-mass spectrometry (GC-MS). In acute toxicity tests, the rats orally received a single dose of 5 g/kg extract of C. pepo. In a subacute toxicity study, the rats received 200, 400, and 800 mg/kg of the C. pepo extract via daily gavage for 14 days. Bioactive compounds 1-octen-3-ol, nonanal, trans-β-ionone, phytol, trans-farnesol, and squalene were identified. There were no toxic effects detected in any of the evaluated parameters, namely liver, kidney, haematological, lipid, and antioxidant enzymes. In wound healing, C. pepo extract showed greater % wound contraction and tensile strength, as well as reduced wound healing time (12 days) and epithelialization when compared to the control (normal saline) and povidone-iodine treated groups. Rats treated with C. pepo extract elicit anti-inflammatory activity. The findings of this study revealed that the C. pepo extract has wound healing and anti-inflammatory properties with a wide margin of safety.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2022-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47291177","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 4

Synthesis and Anticholinesterase Evaluation of Cassine, Spectaline and Analogues 决明、眼镜碱及其类似物的合成及抗胆碱酯酶活性评价

IF 2.5

Scientia Pharmaceutica Pub Date : 2022-10-13 DOI: 10.3390/scipharm90040063

M. C. R. Silva, A. F. Vilela, C. Cardoso, R. Pilli

引用次数: 1

Production of Bovine Collagen Hydrolysate with Antioxidant Activity; Optimized by Response Surface Methodology 具有抗氧化活性的牛胶原水解产物的制备响应面法优化

IF 2.5

Scientia Pharmaceutica Pub Date : 2022-10-10 DOI: 10.3390/scipharm90040062

B. Pakbin, Samaneh Allahyari, Shaghayegh Pishkhan Dibazar, W. Brück, R. Vahidi, R. Mahmoudi, A. Khanjari

{"title":"Production of Bovine Collagen Hydrolysate with Antioxidant Activity; Optimized by Response Surface Methodology","authors":"B. Pakbin, Samaneh Allahyari, Shaghayegh Pishkhan Dibazar, W. Brück, R. Vahidi, R. Mahmoudi, A. Khanjari","doi":"10.3390/scipharm90040062","DOIUrl":"https://doi.org/10.3390/scipharm90040062","url":null,"abstract":"Antioxidants are widely used in pharmaceutical industries. Gelatin is a byproduct of the meat industry and its hydrolysates showed several functionalities, such as antioxidant activity. The purpose of this study was to describe and optimize the enzymatic hydrolysis conditions including time, temperature, pH, and enzyme/substrate ratio (E/S) to produce protein hydrolysate with antioxidant functionality from bovine gelatin by RSM; the scavenging activity was evaluated using the DPPH method. The model observed was fitted with desirable adequacy and sufficiency. We found that the antioxidant activity increased significantly (p < 0.05) with the increase in pH value, E/S ratio, and time of enzymatic process; however, the temperature had no significant (p < 0.05) effect on the antioxidant activity of the hydrolysate. The optimum hydrolysis conditions were observed at a temperature of 35.3 °C, pH of 8.0, and E/S ratio at 2.5 after 2 h hydrolysis by trypsin enzyme. The results showed that the hydrolysate under these conditions, optimized by RSM, could be more effective on antioxidant activity. Regarding the antioxidant potential, gelatin hydrolysate can be used as an antioxidant supplement in pharmaceutical industries.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2022-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48391546","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

The Effect of Zinc Oxide Nanoparticles on Properties and Burn Wound Healing Activity of Thixotropic Xymedone Gels 氧化锌纳米粒子对触变性Xymedone凝胶性能和烧伤愈合活性的影响

IF 2.5

Scientia Pharmaceutica Pub Date : 2022-10-08 DOI: 10.3390/scipharm90040061

Ilya Sheferov, A. Balakireva, D. Panteleev, I.V. Spitskaya, S. Orekhov, Oleg Kazantsev, A. Solovyeva, D. Novopoltsev, N. Melnikova

{"title":"The Effect of Zinc Oxide Nanoparticles on Properties and Burn Wound Healing Activity of Thixotropic Xymedone Gels","authors":"Ilya Sheferov, A. Balakireva, D. Panteleev, I.V. Spitskaya, S. Orekhov, Oleg Kazantsev, A. Solovyeva, D. Novopoltsev, N. Melnikova","doi":"10.3390/scipharm90040061","DOIUrl":"https://doi.org/10.3390/scipharm90040061","url":null,"abstract":"Zinc oxide nanoparticles (ZnO NPs) modified by oxopyrymidine alcohol, also known as xymedone (Xym), were obtained and studied using FTIR, UV-vis, and fluorescent spectroscopy, and SEM, BET, powder XRD, and DLS analysis. A formulation of thixotropic hydrophilic gels containing Carbopol-based Xym and ZnO NPs was developed. A vertical Franz cell with a cellulose acetate membrane was used as a model to investigate the passive diffusion of the gel components by AAS. The gel components—Xym and ZnO NPs—were shown to penetrate through acetyl cellulose membrane within 5–7 h depending on an initial amount, and its values were in the range of 56–77%. The penetration of modified ZnO NPs by Xym was more effective in contrast to ZnO NPs without modification. The burn wound healing activity of ZnO NPs–Xym gel was demonstrated on a thermal burn wound model on rats. SOD and GR activity was increased by 30–35% during ZnO NPs–Xym gel treatment, the burn area on 10 postburn day decreased by 10% in contrast to a positive control, Methyluracyl®® ointment.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2022-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41360538","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 4

Green Synthesis of Silver Nanoparticles Using Bellevalia Flexuosa Leaves Extract 百合花叶提取物绿色合成纳米银

IF 2.5

Scientia Pharmaceutica Pub Date : 2022-10-06 DOI: 10.3390/scipharm90040060

Nusaiba K. Al-Nemrawi, Fatima Hameedat, T. El-Elimat

{"title":"Green Synthesis of Silver Nanoparticles Using Bellevalia Flexuosa Leaves Extract","authors":"Nusaiba K. Al-Nemrawi, Fatima Hameedat, T. El-Elimat","doi":"10.3390/scipharm90040060","DOIUrl":"https://doi.org/10.3390/scipharm90040060","url":null,"abstract":"Silver nanoparticles (AgNPs) have broad biocidal activities, and are widely employed as an active ingredient in antiseptic, anti-viral, and anti-inflammatory preparations. Green-synthesizing AgNPs would be a rapid, cheap, and environmentally friendly method of synthesis. The methanolic extract of the leaves of Bellevalia flexuosa Boiss. (Asparagaceae) was used for the green synthesis of the AgNPs. The effects of the pH and the concentration of silver nitrate (AgNO3) on the synthesis of the AgNPs were investigated. The AgNPs produced above pH 10, and 1 mM of AgNO3 resulted in lower hydrodynamic diameters. Ultraviolet-visible spectroscopy, Fourier-transform infrared spectroscopy, and X-ray diffraction proved the formation of the AgNPs, with a face-centered, cubed geometry. Scanning electron microscopy images showed colloidal and well-dispersed nanoparticles. In addition, the antibacterial activities of the prepared AgNPs were assessed by optical densities (ODs) against Gram-positive bacteria (Enterococcus faecalis and Staphylococcus epidermidis) and Gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, and Salmonella enterica). The broths of Gram-negative and Gram-positive bacteria that contained AgNPs, showed lower OD values compared to the controls. In conclusion, AgNPs were prepared using B. flexuosa methanolic extract, and showed antibacterial activity against the tested bacterial strains.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":"1 1","pages":""},"PeriodicalIF":2.5,"publicationDate":"2022-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41335777","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Potential and Alternative Bioactive Compounds from Brown Agaricus bisporus Mushroom Extracts for Xerosis Treatment 双孢蘑菇提取物治疗干燥性疾病的潜在和替代生物活性化合物

IF 2.5

Scientia Pharmaceutica Pub Date : 2022-10-05 DOI: 10.3390/scipharm90040059

Nichcha Nitthikan, P. Leelapornpisid, Ornchuma Naksuriya, Nutjeera Intasai, Kanokwan Kiattisin

{"title":"Potential and Alternative Bioactive Compounds from Brown Agaricus bisporus Mushroom Extracts for Xerosis Treatment","authors":"Nichcha Nitthikan, P. Leelapornpisid, Ornchuma Naksuriya, Nutjeera Intasai, Kanokwan Kiattisin","doi":"10.3390/scipharm90040059","DOIUrl":"https://doi.org/10.3390/scipharm90040059","url":null,"abstract":"This study aimed to investigate the ability of brown Agaricus bisporus extracts to enhance xerosis treatment via their biological activities, including their antioxidant, anti-aging, and anti-inflammation. Brown A. bisporus ethanol extract (EE) and brown A. bisporus water extract (WE) contained ergothioneine and gallic acid as their major compounds, as detected by HPLC, respectively. The WE exhibited the highest total polysaccharide content (734.04 ± 0.03 mg glucose/g extract) and total phenolic content (190.90 ± 0.07 mg gallic acid/g extract). The WE exhibited an inhibitory effect of 83.34 ± 18.66% on a collagenase enzyme, whereas the EE inhibited the elastase enzymes by 81.26 ± 4.37%. In addition, the EE also demonstrated strong activities against DPPH, with an IC50 0.30 ± 0.04 mg/mL, ABTS with a TEAC value of 8.06 ± 0.08 µM Trolox/g extract, and a FRAP assay with a FRAP value of 390.50 ± 0.32 mM FeSO4/g. In addition, all extracts were non-cytotoxic and could decrease the secretion of IL-6 and TNF-α in HaCaT cells. Therefore, brown A. bisporus extracts might be a potential natural raw material that can be further used in cosmeceutical products for xerosis treatment due to their good efficacy.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2022-10-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44817733","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 8

Retinoic Acid Potentiates the Therapeutic Efficiency of Bone Marrow-Derived Mesenchymal Stem Cells (BM-MSCs) against Cisplatin-Induced Hepatotoxicity in Rats 维甲酸增强骨髓间充质干细胞(BM-MSCs)对大鼠顺铂诱导的肝毒性的治疗效果

IF 2.5

Scientia Pharmaceutica Pub Date : 2022-09-29 DOI: 10.3390/scipharm90040058

Maha M. Azzam, Abdelaziz M. Hussein, Basma H. Marghani, N. Barakat, M. Khedr, Nabil Abu Heakel

{"title":"Retinoic Acid Potentiates the Therapeutic Efficiency of Bone Marrow-Derived Mesenchymal Stem Cells (BM-MSCs) against Cisplatin-Induced Hepatotoxicity in Rats","authors":"Maha M. Azzam, Abdelaziz M. Hussein, Basma H. Marghani, N. Barakat, M. Khedr, Nabil Abu Heakel","doi":"10.3390/scipharm90040058","DOIUrl":"https://doi.org/10.3390/scipharm90040058","url":null,"abstract":"(1) Background: Hepatotoxicity is a common health problem, and oxidative stress plays a crucial role in its underlying mechanisms. We inspected the possible effect of retinoic acid (RA) in the potentiation of hepatoprotective effect of bone marrow mesenchymal stem cells (BM-MSCs) against Cisplatin (Cis)-induced hepatotoxicity. (2) Methods: 60 male Sprague Dawley rats (SD) were separated randomly and designated to six main equal groups as follows: (1) Control group, (2) Cis group (rats got Cis 7 mg/Kg i.p.), (3) Cis + vehicle group (as group 2, but rats received the (vehicle) culture media of BM-MSCs), (4) Cis as in group 2 + BM-MSCs (1x106), (5) Cis as for group 2 + RA 1 mg/Kg i.p., and (6) Cis and BM-MSCs as for group 3 + RA as for group 4. Liver injury was assessed by measuring liver enzymes (ALT, AST), while liver toxicity was evaluated by histopathological examination. Apoptotic marker caspase-3 protein was detected immunohistochemically. Real time PCR was performed to detect NADPH oxidase and TNF-α at transcription levels. Oxidative stress was investigated by colorimetric measurement of MDA, GSH and catalase. (3) Results: Contrary to the Cis group (p < 0.05), BM-MSCs/RA supplementation resulted in a substantial decrease in serum levels of hepatic impairment indicators such as ALT, AST and oxidative stress markers such as MDA, as well as an increase in hepatic GSH, Catalase, and a decrease in expression of TNF-α and downregulation of NADPH oxidase. The improvement after therapy with BM-MSCs/RA was confirmed by histopathological examination. Moreover, the downregulation of caspase-3 in liver tissue after BM-MSCs/RA treatment was validated by immunohistochemistry investigation. (4) Conclusions: BM-MSCs and RA attenuated Cis induced hepatotoxicity through downregulation of oxidative stress resulted in modulation of anti-inflammatory TNF-α and apoptosis caspase-3 indicating a promising role in hepatotoxicity.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2022-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45753914","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 4

A Narrative Review on the Bioactivity and Health Benefits of Alpha-Phellandrene α-菲仑的生物活性和健康益处综述

IF 2.5

Scientia Pharmaceutica Pub Date : 2022-09-27 DOI: 10.3390/scipharm90040057

Subramanian Thangaleela, B. Sivamaruthi, P. Kesika, Tanawat Tiyajamorn, M. Bharathi, C. Chaiyasut

{"title":"A Narrative Review on the Bioactivity and Health Benefits of Alpha-Phellandrene","authors":"Subramanian Thangaleela, B. Sivamaruthi, P. Kesika, Tanawat Tiyajamorn, M. Bharathi, C. Chaiyasut","doi":"10.3390/scipharm90040057","DOIUrl":"https://doi.org/10.3390/scipharm90040057","url":null,"abstract":"Aromatic essential oils play a significant role in pharmaceuticals, food additives, cosmetics, and perfumery. Essential oils mostly comprise aliphatic hydrocarbons, monoterpenoids, sesquiterpenoids and diterpenes. Plant extracts comprise a complex mixture of terpenes, terpenoids, aliphatic and phenol-derived aromatic components. Terpenes are a significant class of hydrocarbons with numerous health benefits. These biological functions of essential oil components are examined in vitro and in vivo studies. Some studies evaluated the properties and functions of α-phellandrene (α-PHE). Detailed evaluation to determine the functions of α-PHE over a spectrum of health care domains needs to be initiated. Its possible mechanism of action in a biological system could reveal the future opportunities and challenges in using α-PHE as a pharmaceutical candidate. The biological functions of α-PHE are reported, including anti-microbial, insecticidal, anti-inflammatory, anti-cancer, wound healing, analgesic, and neuronal responses. The present narrative review summarizes the synthesis, biotransformation, atmospheric emission, properties, and biological activities of α-PHE. The literature review suggests that extended pre-clinical studies are necessary to develop α-PHE-based adjuvant therapeutic approaches.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2022-09-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45233994","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 8

Evaluation of 5-[(Z)-(4-nitrobenzylidene)]-2-(thiazol-2-ylimino)-4-thiazolidinone (Les-6222) as Potential Anticonvulsant Agent 5-[(Z)-(4-硝基苄基)]-2-(噻唑-2-ylimino)-4-噻唑烷酮(Les-6222)作为潜在抗惊厥剂的评价

IF 2.5

Scientia Pharmaceutica Pub Date : 2022-09-19 DOI: 10.3390/scipharm90030056

M. Mishchenko, S. Shtrygol’, A. Lozynskyi, Mykhailo Hoidyk, Dmytro Khyluk, T. Gorbach, R. Lesyk

{"title":"Evaluation of 5-[(Z)-(4-nitrobenzylidene)]-2-(thiazol-2-ylimino)-4-thiazolidinone (Les-6222) as Potential Anticonvulsant Agent","authors":"M. Mishchenko, S. Shtrygol’, A. Lozynskyi, Mykhailo Hoidyk, Dmytro Khyluk, T. Gorbach, R. Lesyk","doi":"10.3390/scipharm90030056","DOIUrl":"https://doi.org/10.3390/scipharm90030056","url":null,"abstract":"It was determined that the studied 5-[(Z)-(4-nitrobenzylidene)]-2-(thiazol-2-ylimino)-4-thiazolidinone (Les-6222) affects the cyclooxygenase pathway of the arachidonic acid cascade, the markers of damage to neurons on models of PTZ kindling. In the model of chronic epileptogenesis in mice (pentylenetetrazole kindling), a 4-thiazolidinone derivative showed high anticonvulsant activity, which is weaker than the effect of sodium valproate and higher than Celecoxib. The mentioned compound has a pronounced anti-inflammatory effect in the brain on the background of the PTZ kindling, reliably inhibiting COX-1 and COX-2. The predominant inhibition of COX-2 by 44.5% indicates this enzyme’s high selectivity of Les-6222. According to the molecular docking study results, the studied compound revealed the properties of COX-1/COX-2 inhibitor and especially 5-LOX/FLAP. The decreasing content of 8-isoprostane in the brain of mice of the Les-6222 group indicates a beneficial effect on cell membranes in the background of oxidative stress during the long-term administration of PTZ. In addition, Les-6222 significantly decreased the content of neuron-specific enolase, indicating neuroprotective properties in the background of chronic epileptogenesis. The obtained results experimentally substantiate the feasibility of further developing Les-6222 as a promising anticonvulsant agent.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2022-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42582394","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2