Drug Research最新文献_第10页

Protein kinases: Role of their dysregulation in carcinogenesis, identification and inhibition. 蛋白激酶:其失调在癌变、鉴定和抑制中的作用。

IF 2.2

Drug Research Pub Date : 2023-04-01 DOI: 10.1055/a-1989-1856

Niloy Sarkar, Amit Singh, Pankaj Kumar, Mahima Kaushik

{"title":"Protein kinases: Role of their dysregulation in carcinogenesis, identification and inhibition.","authors":"Niloy Sarkar, Amit Singh, Pankaj Kumar, Mahima Kaushik","doi":"10.1055/a-1989-1856","DOIUrl":"https://doi.org/10.1055/a-1989-1856","url":null,"abstract":"Protein kinases belong to the phosphor-transferases superfamily of enzymes, which \"activate\" enzymes via phosphorylation. The kinome of an organism is the total set of genes in the genome, which encode for all the protein kinases. Certain mutations in the kinome have been linked to dysregulation of protein kinases, which in turn can lead to several diseases and disorders including cancer. In this review, we have briefly discussed the role of protein kinases in various biochemical processes by categorizing cancer associated phenotypes and giving their protein kinase examples. Various techniques have also been discussed, which are being used to analyze the structure of protein kinases, and associate their roles in the oncogenesis. We have also discussed protein kinase inhibitors and United States Federal Drug Administration (USFDA) approved drugs, which target protein kinases and can serve as a counter to protein kinase dysregulation and mitigate the effects of oncogenesis. Overall, this review briefs about the importance of protein kinases, their roles in oncogenesis on dysregulation and how their inhibition via various drugs can be used to mitigate their effects.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 4","pages":"189-199"},"PeriodicalIF":2.2,"publicationDate":"2023-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9300658","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

Preparation, Characterization and Evaluation of a Novel Drug Carrier for the Controlled Release of Curcumin. 一种新型姜黄素控释药物载体的制备、表征及评价。

IF 2.2

Drug Research Pub Date : 2023-04-01 DOI: 10.1055/a-1995-5303

Faseela Kasim, Archana Somasekharan Nair, Aswathy Lalitha Balachandran, Moorikoval Parambil Sooraj, Anoop Somasekharan Nair

{"title":"Preparation, Characterization and Evaluation of a Novel Drug Carrier for the Controlled Release of Curcumin.","authors":"Faseela Kasim, Archana Somasekharan Nair, Aswathy Lalitha Balachandran, Moorikoval Parambil Sooraj, Anoop Somasekharan Nair","doi":"10.1055/a-1995-5303","DOIUrl":"https://doi.org/10.1055/a-1995-5303","url":null,"abstract":"The upsurge of cancer demands intense, rapid and effective intervention from the scientific society. Even though nanoparticles helped achieving this, maintaining its size without using toxic capping agents is challenging. Phytochemicals having reducing properties is a proper substitute and the efficiency of such nanoparticles could be further improved by grafting with suitable monomers. It could be further protected from rapid biodegradation by coating with suitable materials. This approach was utilized wherein, the green synthesized silver nanoparticles (AgNps) were initially functionalized with -COOH to couple with -NH2 groups of ethylene diamine. It was then coated with polyethylene glycol (PEG) and hydrogen bonded with curcumin. The formed amide bonds could effectively uptake drug molecules and sensed environmental pH. Swelling studies and release profiles confirmed selective drug release. All these results along with those obtained from MTT assay, suggested the potential applicability of the prepared material in pH sensitive drug delivery of curcumin.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 4","pages":"224-231"},"PeriodicalIF":2.2,"publicationDate":"2023-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9245760","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

Molecular Docking Studies of Rifampicin - rpoB complex: Repurposing Drug Design Implications for against Plasmodium falciparum Malaria through a Computational Approach. 利福平- rpoB复合物的分子对接研究:通过计算方法重新利用药物设计对恶性疟原虫疟疾的影响。

IF 2.2

Drug Research Pub Date : 2023-03-01 DOI: 10.1055/a-1974-9028

Upasana Yadav, Jaya Pandey

{"title":"Molecular Docking Studies of Rifampicin - rpoB complex: Repurposing Drug Design Implications for against Plasmodium falciparum Malaria through a Computational Approach.","authors":"Upasana Yadav, Jaya Pandey","doi":"10.1055/a-1974-9028","DOIUrl":"https://doi.org/10.1055/a-1974-9028","url":null,"abstract":"Malaria is one of the world's most devastating diseases, infecting well over 300 million people annually and killing between 2 and 3 million worldwide. Increasing parasite resistance to many existing drugs is exacerbating disease. Resistance to commonly used malarial drugs is increasing the need to develop new drugs urgently. Due to the slow pace and substantial costs of new drug development, repurposing of old drugs which is recently increasingly becoming an attractive proposition of highly efficient and effective way of drug discovery led us to study the drug rifampicin for this purpose. The present paper aims to investigate the route of Plasmodium falciparum apicoplast-targeted proteins that putatively encode β subunits of RNA polymerase with an objective to develop an effective antimalarial drug. Homology searching for conserved binding site to the rifampicin drug and the functional analysis of rpoB gene were done. Multiple Sequence alignment analysis of rpoB was compared with that in E.coli - rpoB and M. tuberculosis - rpoB. Docking studies of Rifampicin - rpoB complex was also done for finding binding affinity. The results of computational studies showed that rifampicin is a potential drug for malaria.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 3","pages":"164-169"},"PeriodicalIF":2.2,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10856857","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

Biological Activity of a 4-Hydroxy-Furanyl-Benzamide Derivative on Heart Failure. 4-羟基呋喃苯酰胺衍生物对心力衰竭的生物活性。

IF 2.2

Drug Research Pub Date : 2023-03-01 DOI: 10.1055/a-1855-1412

Figueroa-Valverde Lauro, Rosas-Nexticapa Marcela, López-Ramos Maria, Alvarez-Ramirez Magdalena, Mateu-Armad Maria Virginia, Díaz-Cedillo Francisco, Cervantes-Ortega Catalina, Melgarejo-Guutierrez Montserrat

{"title":"Biological Activity of a 4-Hydroxy-Furanyl-Benzamide Derivative on Heart Failure.","authors":"Figueroa-Valverde Lauro, Rosas-Nexticapa Marcela, López-Ramos Maria, Alvarez-Ramirez Magdalena, Mateu-Armad Maria Virginia, Díaz-Cedillo Francisco, Cervantes-Ortega Catalina, Melgarejo-Guutierrez Montserrat","doi":"10.1055/a-1855-1412","DOIUrl":"https://doi.org/10.1055/a-1855-1412","url":null,"abstract":"Abstract Background There are studies that suggest that some benzamide derivatives may exert effects on heart failure; however, their molecular mechanism is not very clear. Objective The aim of this research was to evaluate the biological activity of a 4-hydroxy-furanyl-benzamide derivative against heart failure translated as area infarct. Methods Biological activity produced by 4-hydroxy-furanyl-benzamide derivative against heart failure was determinate using an ischemia-reperfusion injury model. In addition, the effects exerted by the 4-hydroxy-furanyl-benzamide derivative on left ventricular pressure (LVP) was evaluated in the absence or presence of some drugs such as yohimbine, butaxamine, methoctramine and L-NAME using a model of rat heart isolated. Results The results showed that 4-hydroxy-furanyl-benzamide derivative decrease both infarct area and LVP. However, the effect produced by 4-hydroxy-furanyl-benzamide derivative on LVP was inhibited in the presence of both methoctramine and L-NAME. Conclusions All these data suggest that biological activity produced by 4-hydroxy-furanyl-benzamide derivative on left ventricular pressure is through of both M 2 -muscarinic receptor and nitric oxide synthase enzyme activation. It is important to mention that this phenomenon results as a decrease of both infarct area and heart failure.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 3","pages":"175-183"},"PeriodicalIF":2.2,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10861863","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

MicroRNA-32 Suppression: its Effects on Prostate Cancer Cells' Capability to Proliferate and Migrate. 抑制MicroRNA-32对前列腺癌细胞增殖和迁移能力的影响

IF 2.2

Drug Research Pub Date : 2023-03-01 DOI: 10.1055/a-1977-8848

Farah A Al-Marzook, Duha Maithem Hassan, Maha Waleed Alghazal, Rana Abd Alameer Kadheem, Abduladheem Turki Jalil, Marwan Mahmood Saleh

{"title":"MicroRNA-32 Suppression: its Effects on Prostate Cancer Cells' Capability to Proliferate and Migrate.","authors":"Farah A Al-Marzook, Duha Maithem Hassan, Maha Waleed Alghazal, Rana Abd Alameer Kadheem, Abduladheem Turki Jalil, Marwan Mahmood Saleh","doi":"10.1055/a-1977-8848","DOIUrl":"https://doi.org/10.1055/a-1977-8848","url":null,"abstract":"Introduction: This paper sought to scrutinize the role of microRNA-32 (miR-32) on the growth and migration as well as on the expression of metastatic genes in PC3 cells of prostate cancer in vitro.Methods: Subsequent transfection of cells with miR-32 mimics, miR-32 inhibitor, negative control (NC), cell proliferation using MTT, and apoptosis by ELISA were performed. Furthermore, qRT-PCR was directed to measure the expression levels of matrix metalloproteinase 2 (MMP2) and vascular endothelial growth factors (VEGF) as metastatic and angiogenesis genes in the progression of PC3.Results: miR-32 was overexpressed in PC3 cells compared to normal cells (P<0.001). Down-regulation of miR-32 obstructs in vitro proliferation and migration while intensifying the apoptosis rate in PC3 cells. Also, we found that miR-32 negatively modulates the expression of VEGF and MMP2 in PC3 cells.Conclusion: These results indicate that the suppression of miR-32 might offer an auxiliary treatment procedure for addressing the invasion, progression, and metastasis in PCa patients by improving cell apoptosis.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 3","pages":"170-174"},"PeriodicalIF":2.2,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10853607","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

The efficacy of 2-formyl benzoic acid in reactivating diazinon inhibited murine cholinesterase. 2-甲酰基苯甲酸对二嗪醌活化抑制小鼠胆碱酯酶的作用。

IF 2.2

Drug Research Pub Date : 2023-03-01 DOI: 10.1055/a-1934-1806

Humayun Farhat, Ebrahim Zabihi, Fatemeh Alibabaei-Omran, Maryam Mohammadi-Khanaposhti

{"title":"The efficacy of 2-formyl benzoic acid in reactivating diazinon inhibited murine cholinesterase.","authors":"Humayun Farhat, Ebrahim Zabihi, Fatemeh Alibabaei-Omran, Maryam Mohammadi-Khanaposhti","doi":"10.1055/a-1934-1806","DOIUrl":"https://doi.org/10.1055/a-1934-1806","url":null,"abstract":"Oximes, as classical acetylcholinesterase (AChE) reactivators, have some pharmacokinetics/pharmacodynamics disadvantages. During the synthesis of non-oxime compounds, we encountered the compound 2-formylbenzoic acid (2-FBA) with promising in vitro and in vivo cholinesterase (ChE) reactivating properties in the acute exposure to diazinon (DZN). For in vitro experiments, the healthy mice serum and brain homogenate were freshly prepared and exposed to DZN (160 µg/mL). After 10 minutes, 2-FBA was added to the poisoned samples, and ChE activity was measured afterward. For the in vivo assay, the mice were poisoned with DZN subcutaneous (SC) injection (50 mg/kg), and after 1 hour, either 2-FBA or Pralidoxime (2-PAM) was injected intravenously (IV). After 3 h, ChE activity was measured in the serum and brain homogenate samples. The LD50 (IV) for 2-FBA in mice was measured as well. 2-FBA effectively reactivated the inhibited ChE in serum and brain homogenate samples in vitro. In the in vivo experiments, while 2-FBA could significantly reactivate the brain ChE even better than 2-PAM, they failed to reactivate the serum ChE by single IV injection. LD50 of 2-FBA was calculated to be 963 mg/kg. There were no general toxicity signs in any treatment groups. The in silico results support the potential ability of 2-FBA efficacy via possibly Witting reaction mechanism. Our findings indicate that 2-FBA seems to be a suitable non-oxime candidate for AChE reactivation with minimal side effects. Further toxicokinetic studies on this compound are strongly recommended to be performed before conducting the clinical trial in humans.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 3","pages":"156-163"},"PeriodicalIF":2.2,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10853609","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

A Study to Explore the Role of IDH1 (R132) Mutation on Imatinib Toxicity and Effect of ABCG2/OCT1 Expression on N-Desmethyl Imatinib Plasma Level in Egyptian Chronic Myeloid Leukemia Patients. IDH1 (R132)突变对伊马替尼毒性的影响及ABCG2/OCT1表达对埃及慢性髓系白血病患者n -去甲基伊马替尼血浆水平的影响

IF 2.2

Drug Research Pub Date : 2023-03-01 DOI: 10.1055/a-1924-7746

Alaa Sabri, Mervat M Omran, S Abdel Azim, Raafat Abdelfattah, Rasha Mahmoud Allam, Samia A Shouman

{"title":"A Study to Explore the Role of IDH1 (R132) Mutation on Imatinib Toxicity and Effect of ABCG2/OCT1 Expression on N-Desmethyl Imatinib Plasma Level in Egyptian Chronic Myeloid Leukemia Patients.","authors":"Alaa Sabri, Mervat M Omran, S Abdel Azim, Raafat Abdelfattah, Rasha Mahmoud Allam, Samia A Shouman","doi":"10.1055/a-1924-7746","DOIUrl":"https://doi.org/10.1055/a-1924-7746","url":null,"abstract":"Imatinib mesylate (IM) is the gold standard for treatment of Chronic Myeloid Leukemia (CML). This study aimed to gain more knowledge of the altered PK, pharmacogenetic factors, and gene expression leading to variable IM levels. Fifty patients with chronic phase-CML were enrolled in this study and divided as 25 responders and 25 non-responders (patients are directly recruited after response assessment). HPLC/MS/MS was used to determine trough and peak concentration of imatinib and N-desmethyl imatinib in the blood. PCR-RFLP technique was used to detect IDH1 gene mutation (R132). The median value of IM trough level was significantly higher, the P/T ratio was significantly lower and the α-1-acid glycoprotein (AGP) was significantly higher among responders compared to non-responders (P=0.007, 0.009 and 0.048, respectively). Higher N-desmethyl imatinib peak plasma concentration was observed with low mRNA expression of ABCG2 and OCT1 (P=0.01 and 0.037, respectively). IDH1 R132 gene mutation was associated with a significant increase in toxicities (P=0.028). In conclusion, IM trough level, P/T ratio and AGP was significantly higher in responders. In addition, ABCG2 and OCT1 gene expression may affect the interindividual PK variation. Although a prospective study with a larger patient population is necessary to validate these findings. IDH1 mutation is a predictor of increased toxicity with IM treatment.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 3","pages":"146-155"},"PeriodicalIF":2.2,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10846006","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

Curcumin-Loaded Chitosan Nanoparticle Preparation and Its Protective Effect on Celecoxib-induced Toxicity in Rat isolated Cardiomyocytes and Mitochondria. 姜黄素壳聚糖纳米粒制备及其对塞来昔布致大鼠心肌细胞和线粒体毒性的保护作用。

IF 2.2

Drug Research Pub Date : 2023-03-01 DOI: 10.1055/a-1960-3092

Hossein Ali Ebrahimi, Samira Esmaeli, Saleh Khezri, Ahmad Salimi

{"title":"Curcumin-Loaded Chitosan Nanoparticle Preparation and Its Protective Effect on Celecoxib-induced Toxicity in Rat isolated Cardiomyocytes and Mitochondria.","authors":"Hossein Ali Ebrahimi, Samira Esmaeli, Saleh Khezri, Ahmad Salimi","doi":"10.1055/a-1960-3092","DOIUrl":"https://doi.org/10.1055/a-1960-3092","url":null,"abstract":"Curcumin has a wide range of pharmacological activities, including antioxidant, anti-inflammatory and tissue protective. In here we hypothesized that curcumin-loaded chitosan-coated solid lipid nanoparticles (CuCsSLN) are able to increase its overall bioavailability and hence its antioxidant and mitochondria;/lysosomal protective properties of curcumin. CuCsSLN were prepared using solvent diffusion technique for formation of solid lipid nanoparticles (SLNs) and electrostatic coating of positive-charged chitosan to negative surface of SLNs. CuCsSLN showed the encapsulation efficiency of 91.4±2.7%, the mean particle size of 208±9 nm, the polydispersity index of 0.34±0.07, and the zeta potential of+53.5±3.7 mV. The scanning electron microscope (SEM) images of nanoparticles verified their nanometric size and also spherical shape. Curcumin was released from CuCsSLN in a sustain release pattern up to 24 hours. Then isolated cardiomyocytes and mitochondria were simultaneously treated with (1) control (0.05% ethanol), (2) celecoxib (20 µg/ml) treatment, (3) celecoxib (20 µg/ml)+++CuCsSLN (1 µg/ml) treatment, (4) CuCsSLN (1 µg/ml) treatment, (5) celecoxib (20 µg/ml)+++curcumin (10 µM) treatment and (6) curcumin (10 µM) treatment for 4 h at 37°C. The results showed that celecoxib (20 µg/ml) induced a significant increase in cytotoxicity, reactive oxygen species (ROS) formation, mitochondria membrane potential (ΔΨm) collapse, lipid peroxidation, oxidative stress and mitochondrial swelling while CuCsSLN and curcumin reverted the above toxic effect of celecoxib. Our data indicated that the effect of CuCsSLN in a number of experiments, is significantly better than that of curcumin which shows the role of chitosan nanoparticles in increasing effect of curcumin.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 3","pages":"125-136"},"PeriodicalIF":2.2,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10842939","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

Cysteamine Attenuate Intestinal Reperfusion Injury Induced by Occlusion of Mesenteric Artery by Enhancing Intracellular Thiol Activities. 半胱胺通过增强细胞内硫醇活性减轻肠系膜动脉闭塞引起的肠再灌注损伤。

IF 2.2

Drug Research Pub Date : 2023-03-01 DOI: 10.1055/a-1974-9132

Babatunde Alabi, Olugbenga Iwalewa, Temidayo Omobowale, Adeolu Adedapo, Opeyemi Hammed, Richard Ajike, Oladele Afolabi

{"title":"Cysteamine Attenuate Intestinal Reperfusion Injury Induced by Occlusion of Mesenteric Artery by Enhancing Intracellular Thiol Activities.","authors":"Babatunde Alabi, Olugbenga Iwalewa, Temidayo Omobowale, Adeolu Adedapo, Opeyemi Hammed, Richard Ajike, Oladele Afolabi","doi":"10.1055/a-1974-9132","DOIUrl":"https://doi.org/10.1055/a-1974-9132","url":null,"abstract":"Background: Ischemia/reperfusion has been reported to further damage the intestine reperfusion injury (IRI) and cause multiple distal organ dysfunction through oxidative stress, inflammation, and apoptosis. Cysteamine is known to inhibit oxidative stress, inflammatory cytokines and apoptosis. This experiment was designed to evaluate the role of cysteamine against IRI in rats METHODS: Thirty-two Wistar rat strains were assigned to four groups: sham, Intestinal-reperfusion injury (IRI), 50 mg/kg and 100 mg/kg cysteamine treatment IRI. A 5 cm segment of terminal ileum was twisted 360° clockwise along the mesentery for 45 minutes to induce ischemia before detorsion. Tissues were preserved for biochemical evaluation and histology 4 hours after detorsion. Activities of GPx, GSH, protein and non-protein thiol, H2O2, MDA were evaluated. Serum concentration of nitrite, MPO, ALT, AST TNF-alpha and IL-6 were measured. Caspase 3 and bax were evaluated by immunohistochemistry. Statistical significance was set as p<0.05 RESULTS: Significant (p<0.05) increase in H2O2, MDA and nitrite but reduction in GPx, GSH, protein thiol and non-protein thiol in the IRI rats was reversed by 50 and 100 mg/kg cysteamine. Serum MPO, TNF-α, IL6, AST and ALT was significantly elevated in IRI while the rats treated with cysteamine showed a significant decrease (p<0.05) in the activities of these inflammatory and hepatic injury markers.Conclusion: Cysteamine mitigate IRI by enhancing intracellular antioxidant defense system, inhibiting inflammatory mediators and intestinal tissue expression of pro-apoptotic protein.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 3","pages":"137-145"},"PeriodicalIF":2.2,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10856565","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

Aloe Vera-Containing Matrix in Transdermal Fentanyl Therapy Improves Adhesion, Skin Tolerance and Quality of Life: Results of a German Multicenter Study with a New Fentanyl Patch. 含芦荟提取物的芬太尼透皮治疗基质改善粘连、皮肤耐受性和生活质量:德国一项使用新型芬太尼贴片的多中心研究结果

IF 2.2

Drug Research Pub Date : 2023-02-01 DOI: 10.1055/a-1960-2879

Christoph G Dietrich, Tanja Kottmann, Hans Werner Voß, Roxane Lorenz

{"title":"Aloe Vera-Containing Matrix in Transdermal Fentanyl Therapy Improves Adhesion, Skin Tolerance and Quality of Life: Results of a German Multicenter Study with a New Fentanyl Patch.","authors":"Christoph G Dietrich, Tanja Kottmann, Hans Werner Voß, Roxane Lorenz","doi":"10.1055/a-1960-2879","DOIUrl":"https://doi.org/10.1055/a-1960-2879","url":null,"abstract":"Background: Chronic pain represents a significant and costly healthcare problem especially in the older patient. Transdermal opioid therapy is easy to apply and ensures constant supply of active ingredients. However, skin irritation, poor adhesion and systemic side effects complicate transdermal pain therapy.Methods: In the Relief study, comprising 54 centers, all in Germany, 252 patients were recruited and data about the general care situation as well as the characteristics, effects and side effects of the Aloe vera fentanyl patch were collected. 92 patients had a prior treatment with fentanyl patch without Aloe vera, allowing a comparative analysis.Results: Compared to patches without Aloe vera, the new fentanyl patch showed better adhesion. Systemic and local tolerance and pain reduction were also significantly better. Patients also reported improvements in side effects and central parameters of quality of life. The data regarding the care situation in Germany showed remarkably low use of coanalgetics and laxatives in pain patients.Discussion: Aloe vera in transdermal pain treatment improves adhesion and local tolerance of the patch. Pain control and quality of life were also improved. Regional care data concerning cotreatment in pain therapy from this study indicate a lack of penetration of existing guidelines in general practitioners' pain therapy.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 2","pages":"70-74"},"PeriodicalIF":2.2,"publicationDate":"2023-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10664246","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