Pharmaceuticals (Basel, Switzerland)最新文献_第10页

Identification of a Novel p53 Modulator Endowed with Antitumoural and Antibacterial Activity through a Scaffold Repurposing Approach. 通过支架再利用方法鉴定具有抗肿瘤和抗菌活性的新型p53调节剂。

IF 4.6

Pharmaceuticals (Basel, Switzerland) Pub Date : 2022-10-26 DOI: 10.3390/ph15111318

Elisa Nuti, Valeria La Pietra, Simona Daniele, Doretta Cuffaro, Lidia Ciccone, Chiara Giacomelli, Carolina Cason, Alfonso Carotenuto, Vincenzo Maria D'Amore, Eleonora Da Pozzo, Barbara Costa, Riccardo Di Leo, Manola Comar, Luciana Marinelli, Claudia Martini, Armando Rossello

{"title":"Identification of a Novel p53 Modulator Endowed with Antitumoural and Antibacterial Activity through a Scaffold Repurposing Approach.","authors":"Elisa Nuti, Valeria La Pietra, Simona Daniele, Doretta Cuffaro, Lidia Ciccone, Chiara Giacomelli, Carolina Cason, Alfonso Carotenuto, Vincenzo Maria D'Amore, Eleonora Da Pozzo, Barbara Costa, Riccardo Di Leo, Manola Comar, Luciana Marinelli, Claudia Martini, Armando Rossello","doi":"10.3390/ph15111318","DOIUrl":"https://doi.org/10.3390/ph15111318","url":null,"abstract":"Intracellular pathogens, such as Chlamydia trachomatis, have been recently shown to induce degradation of p53 during infection, thus impairing the protective response of the host cells. Therefore, p53 reactivation by disruption of the p53-MDM2 complex could reduce infection and restore pro-apoptotic effect of p53. Here, we report the identification of a novel MDM2 inhibitor with potential antitumoural and antibacterial activity able to reactivate p53. A virtual screening was performed on an in-house chemical library, previously synthesised for other targets, and led to the identification of a hit compound with a benzo[a]dihydrocarbazole structure, RM37. This compound induced p53 up-regulation in U343MG glioblastoma cells by blocking MDM2-p53 interaction and reduced tumour cell growth. NMR studies confirmed its ability to dissociate the MDM2-p53 complex. Notably, RM37 reduced Chlamydia infection in HeLa cells in a concentration-dependent manner and ameliorated the inflammatory status associated with infection.","PeriodicalId":520747,"journal":{"name":"Pharmaceuticals (Basel, Switzerland)","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2022-10-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9692514/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40455663","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Small-Molecule Fluorescent Probe for Detection of Sulfite. 亚硫酸盐的小分子荧光探针检测。

IF 4.6

Pharmaceuticals (Basel, Switzerland) Pub Date : 2022-10-26 DOI: 10.3390/ph15111326

Ting Li, Xuyang Chen, Kai Wang, Zhigang Hu

{"title":"Small-Molecule Fluorescent Probe for Detection of Sulfite.","authors":"Ting Li, Xuyang Chen, Kai Wang, Zhigang Hu","doi":"10.3390/ph15111326","DOIUrl":"https://doi.org/10.3390/ph15111326","url":null,"abstract":"Sulfite is widely used as an antioxidant additive and preservative in food and beverages. Abnormal levels of sulfite in the body is related to a variety of diseases. There are strict rules for sulfite intake. Therefore, to monitor the sulfite level in physiological and pathological events, there is in urgent need to develop a rapid, accurate, sensitive, and non-invasive approach, which can also be of great significance for the improvement of the corresponding clinical diagnosis. With the development of fluorescent probes, many advantages of fluorescent probes for sulfite detection, such as real time imaging, simple operation, economy, fast response, non-invasive, and so on, have been gradually highlighted. In this review, we enumerated almost all the sulfite fluorescent probes over nearly a decade and summarized their respective characteristics, in order to provide a unified platform for their standardized evaluation. Meanwhile, we tried to systematically review the research progress of sulfite small-molecule fluorescent probes. Logically, we focused on the structures, reaction mechanisms, and applications of sulfite fluorescent probes. We hope that this review will be helpful for the investigators who are interested in sulfite-associated biological procedures.","PeriodicalId":520747,"journal":{"name":"Pharmaceuticals (Basel, Switzerland)","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2022-10-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9699022/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40457672","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 6

Long-Term Fenofibrate Treatment Stimulates the Phenotypic Microevolution of Prostate Cancer Cells In Vitro. 长期非诺贝特治疗刺激体外前列腺癌细胞的表型微进化。

IF 4.6

Pharmaceuticals (Basel, Switzerland) Pub Date : 2022-10-26 DOI: 10.3390/ph15111320

Karolina W Warzecha, Maciej Pudełek, Jessica Catapano, Zbigniew Madeja, Jarosław Czyż

{"title":"Long-Term Fenofibrate Treatment Stimulates the Phenotypic Microevolution of Prostate Cancer Cells In Vitro.","authors":"Karolina W Warzecha, Maciej Pudełek, Jessica Catapano, Zbigniew Madeja, Jarosław Czyż","doi":"10.3390/ph15111320","DOIUrl":"https://doi.org/10.3390/ph15111320","url":null,"abstract":"Fenofibrate is a widely used anti-hyperlipidemic agonist of peroxisome proliferator-activated receptor alpha (PPARα). As a metabolic blocker, fenofibrate interferes with cancer promotion/progression via its misbalancing effects on cellular metabolism. However, the consequences of its long-term application for patients with diagnosed drug-resistant cancers are unknown. We addressed this point by tracing the phenotypic microevolution of naïve and drug-resistant prostate cancer PC3_DCX20 cells that underwent a long-term exposition to 10 μM and 50 μM fenofibrate. Their resistance to fenofibrate, metabolic profile and invasive phenotype were estimated in the control conditions and under fenofibrate-induced stress. Apparently, drug efflux systems are not effective against the cytostatic FF action. However, wtPC3 and PC3_DCX20 cells that survived the long-term 50 μM fenofibrate treatment gave rise to lineages that displayed an increased proliferation rate, lower motility in the control conditions and enhanced fenofibrate resistance. Attenuated fenofibrate bioavailability modified the pattern of PC3 microevolution, as illustrated by phenotypic differences between wtPC3/PC3_DCX20 lineages propagated in the presence of 50 μM and 10 μM fenofibrate. Collectively, our observations indicate that fenofibrate acts as a selective factor that affects prostate cancer microevolution. We also pinpoint potential consequences of long-term exposition of prostate cancer patients to metabolic blockers.","PeriodicalId":520747,"journal":{"name":"Pharmaceuticals (Basel, Switzerland)","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2022-10-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9694160/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40455664","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

The Role of the Adenosine System on Emotional and Cognitive Disturbances Induced by Ethanol Binge Drinking in the Immature Brain and the Beneficial Effects of Caffeine. 腺苷系统在未成熟大脑酒精狂饮引起的情绪和认知障碍中的作用以及咖啡因的有益作用。

IF 4.6

Pharmaceuticals (Basel, Switzerland) Pub Date : 2022-10-26 DOI: 10.3390/ph15111323

Bruno Gonçalves Pinheiro, Diandra Araújo Luz, Sabrina de Carvalho Cartágenes, Luanna de Melo Pereira Fernandes, Sarah Viana Farias, Natália Harumi Correa Kobayashi, Enéas Andrade Fontes-Júnior, Samira G Ferreira, Rodrigo A Cunha, Rui Daniel Prediger, Cristiane do Socorro Ferraz Maia

{"title":"The Role of the Adenosine System on Emotional and Cognitive Disturbances Induced by Ethanol Binge Drinking in the Immature Brain and the Beneficial Effects of Caffeine.","authors":"Bruno Gonçalves Pinheiro, Diandra Araújo Luz, Sabrina de Carvalho Cartágenes, Luanna de Melo Pereira Fernandes, Sarah Viana Farias, Natália Harumi Correa Kobayashi, Enéas Andrade Fontes-Júnior, Samira G Ferreira, Rodrigo A Cunha, Rui Daniel Prediger, Cristiane do Socorro Ferraz Maia","doi":"10.3390/ph15111323","DOIUrl":"https://doi.org/10.3390/ph15111323","url":null,"abstract":"Binge drinking intake is the most common pattern of ethanol consumption by adolescents, which elicits emotional disturbances, mainly anxiety and depressive symptoms, as well as cognitive alterations. Ethanol exposure may act on the adenosine neuromodulation system by increasing adenosine levels, consequently increasing the activation of adenosine receptors in the brain. The adenosine modulation system is involved in the control of mood and memory behavior. However, there is a gap in the knowledge about the exact mechanisms related to ethanol exposure's hazardous effects on the immature brain (i.e., during adolescence) and the role of the adenosine system thereupon. The present review attempts to provide a comprehensive picture of the role of the adenosinergic system on emotional and cognitive disturbances induced by ethanol during adolescence, exploring the potential benefits of caffeine administration in view of its action as a non-selective antagonist of adenosine receptors.","PeriodicalId":520747,"journal":{"name":"Pharmaceuticals (Basel, Switzerland)","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2022-10-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9694775/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40457671","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Discovery of Novel 1,2,3-triazole Derivatives as IDO1 Inhibitors. 新型1,2,3-三唑类IDO1抑制剂的发现。

IF 4.6

Pharmaceuticals (Basel, Switzerland) Pub Date : 2022-10-25 DOI: 10.3390/ph15111316

Xixi Hou, Xiaoqing Gong, Longfei Mao, Jie Zhao, Jianxue Yang

引用次数: 2

Application of AP-MALDI Imaging Mass Microscope for the Rapid Mapping of Imipramine, Chloroquine, and Their Metabolites in the Kidney and Brain of Wild-Type Mice. 应用AP-MALDI成像质粒显微镜快速定位野生型小鼠肾和脑中丙咪嗪、氯喹及其代谢物

IF 4.6

Pharmaceuticals (Basel, Switzerland) Pub Date : 2022-10-25 DOI: 10.3390/ph15111314

Ariful Islam, Takumi Sakamoto, Qing Zhai, Md Muedur Rahman, Md Al Mamun, Yutaka Takahashi, Tomoaki Kahyo, Mitsutoshi Setou

{"title":"Application of AP-MALDI Imaging Mass Microscope for the Rapid Mapping of Imipramine, Chloroquine, and Their Metabolites in the Kidney and Brain of Wild-Type Mice.","authors":"Ariful Islam, Takumi Sakamoto, Qing Zhai, Md Muedur Rahman, Md Al Mamun, Yutaka Takahashi, Tomoaki Kahyo, Mitsutoshi Setou","doi":"10.3390/ph15111314","DOIUrl":"https://doi.org/10.3390/ph15111314","url":null,"abstract":"Mass spectrometry imaging (MSI) is well-known for the non-labeling visualization of analytes, including drugs and their metabolites in biological samples. In this study, we applied three different tools of MSI, desorption electrospray ionization (DESI)-MSI, matrix-assisted laser desorption ionization (MALDI)-MSI, and a newly developed atmospheric pressure (AP)-MALDI-MSI known as iMScopeTM QT for rapid mapping of imipramine, chloroquine, and their metabolites in C57BL/6 male wild-type mice. Among three MSI tools, better detection capability for targeted drugs at higher speed (up to 32 pixels/s) was observed in iMScope QT. It revealed that imipramine and its metabolites were significantly accumulated in the renal cortex of mice, but chloroquine and its metabolites were highly accumulated in the renal pelvis and renal medulla of mice. Additionally, a higher accumulation of imipramine was noted in the thalamus, hypothalamus, septum, and hindbrain of mice brains. However, chloroquine and its metabolites showed notable accumulation in the lateral ventricle, fourth ventricle, and fornix of the mice brains. These findings of our study can be helpful in understanding clinically relevant properties, efficacy, and potential side effects of these drugs. Our study also showed the potentiality of iMScope QT for rapid mapping of small drugs and their metabolites in biological samples.","PeriodicalId":520747,"journal":{"name":"Pharmaceuticals (Basel, Switzerland)","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2022-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9696843/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40455658","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 5

Comparative Studies of Palmatine with Metformin and Glimepiride on the Modulation of Insulin Dependent Signaling Pathway In Vitro, In Vivo & Ex Vivo. 巴马汀与二甲双胍和格列美脲在体外、体内和离体调节胰岛素依赖信号通路的比较研究。

IF 4.6

Pharmaceuticals (Basel, Switzerland) Pub Date : 2022-10-25 DOI: 10.3390/ph15111317

Okechukwu Patrick Nwabueze, Mridula Sharma, Abbirami Balachandran, Anand Gaurav, Anis Najwa Abdul Rani, Jeleń Małgorzata, Morak-Młodawska Beata, Charlie A Lavilla, Merell P Billacura

{"title":"Comparative Studies of Palmatine with Metformin and Glimepiride on the Modulation of Insulin Dependent Signaling Pathway In Vitro, In Vivo & Ex Vivo.","authors":"Okechukwu Patrick Nwabueze, Mridula Sharma, Abbirami Balachandran, Anand Gaurav, Anis Najwa Abdul Rani, Jeleń Małgorzata, Morak-Młodawska Beata, Charlie A Lavilla, Merell P Billacura","doi":"10.3390/ph15111317","DOIUrl":"https://doi.org/10.3390/ph15111317","url":null,"abstract":"(1) Insulin resistance, a symptom of type 2 diabetes mellitus (T2DM), is caused by the inactivation of the insulin signaling pathway, which includes IRS-PI3K-IRS-1-PKC-AKT2 and GLUT4. Metformin (biguanide) and glimepiride (sulfonylurea) are both drugs that are derivatives of urea, and they are widely used as first-line drugs for the treatment of type 2 diabetes mellitus. Palmatine has been previously reported to possess antidiabetic and antioxidant properties. (2) The current study compared palmatine to metformin and glimepiride in a type 2 diabetes model for ADME and insulin resistance via the PI3K/Akt/GLUT4 signaling pathway: in vitro, in vivo, ex vivo, and in silico molecular docking. (3) Methods: Differentiated L6 skeletal muscle cells and soleus muscle tissue were incubated in standard tissue culture media supplemented with high insulin and high glucose as a cellular model of insulin resistance, whilst streptozotocin (STZ)-induced Sprague Dawley rats were used as the diabetic model. The cells/tissue/animals were treated with palmatine, while glimepiride and metformin were used as standard drugs. The differential gene expression of PI3K, IRS-1, PKC-α, AKT2, and GLUT4 was evaluated using qPCR. (4) Results: The results revealed that the genes IRS-PI3K-IRS-1-PKC-AKT2 were significantly down-regulated, whilst PKC-α was upregulated significantly in both insulin-resistant cells and tissue animals. Interestingly, palmatine-treated cells/tissue/animals were able to reverse these effects. (5) Conclusions: Palmatine appears to have rejuvenated the impaired insulin signaling pathway through upregulation of the gene expression of IRS-1, PI3K, AKT2, and GLUT4 and downregulation of PKC-expression, according to in vitro, in vivo, and ex vivo studies.","PeriodicalId":520747,"journal":{"name":"Pharmaceuticals (Basel, Switzerland)","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2022-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9695187/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40455661","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Preclinical Evaluation of the Multiple Tyrosine Kinases Inhibitor Anlotinib in Leukemia Stem Cells. 多种酪氨酸激酶抑制剂安洛替尼在白血病干细胞中的临床前评价。

IF 4.6

Pharmaceuticals (Basel, Switzerland) Pub Date : 2022-10-25 DOI: 10.3390/ph15111313

Yuelong Jiang, Long Liu, Yirong Jiang, Zhifeng Li, Liying Feng, Xinguo Zhuang, Zhijuan Lin, Qiuling Chen, Guoshu Chen, Jixiang He, Guowei Li, Jie Zha, Bing Xu

{"title":"Preclinical Evaluation of the Multiple Tyrosine Kinases Inhibitor Anlotinib in Leukemia Stem Cells.","authors":"Yuelong Jiang, Long Liu, Yirong Jiang, Zhifeng Li, Liying Feng, Xinguo Zhuang, Zhijuan Lin, Qiuling Chen, Guoshu Chen, Jixiang He, Guowei Li, Jie Zha, Bing Xu","doi":"10.3390/ph15111313","DOIUrl":"https://doi.org/10.3390/ph15111313","url":null,"abstract":"Leukemia stem cells (LSCs) constitute the critical barrier to the cure of acute myeloid leukemia (AML) due to their chemoresistance and immune evasion property. Herein, the role of anlotinib, a multiple tyrosine kinase inhibitor, in killing LSCs and regulating chemoresistance and immune evasion was explored. Anlotinib treatment induced apoptosis of LSC-like cells as well as primary AML LSCs, while sparing the normal mononuclear cells in vitro. Moreover, anlotinib could impair the regeneration capacity of LSCs in the patient-derived leukemia xenograft mouse model. Mechanistically, anlotinib inhibited phosphorylation of c-kit, JAK2/STAT3, and STAT5, and downregulated STAT3 and STAT5 expression. In addition, anlotinib downregulated the anti-apoptotic proteins Bcl-2 and Bcl-xL, and upregulated Bax, thereby enhancing the sensitivity of LSCs to idarubicin in vitro. Intriguingly, anlotinib could also partially rescue the interferon-g production of T cells cocultured with LSCs by downregulating PD-L1 expression. In conclusion, anlotinib showed anti-LSC activity and the potential to enhance the sensitivity to idarubicin and inhibit the immunosuppressive feature of LSCs via JAK2/STAT signaling pathway downregulation in the preclinical study. Our results provided a rational basis for combinatory strategies involving anlotinib and chemotherapy or immunotherapy.","PeriodicalId":520747,"journal":{"name":"Pharmaceuticals (Basel, Switzerland)","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2022-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9697152/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40464709","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Safety, Tolerability, and Serum/Tear Pharmacokinetics of Human Recombinant Epidermal Growth Factor Eyedrops in Healthy Subjects. 人重组表皮生长因子滴眼液在健康受试者中的安全性、耐受性和血清/泪液药代动力学

IF 4.6

Pharmaceuticals (Basel, Switzerland) Pub Date : 2022-10-24 DOI: 10.3390/ph15111312

Hyounggyoon Yoo, Seonghae Yoon, In-Jin Jang, Kyung-Sang Yu, Joon Young Hyon, Jungi Hwang, Inyoung Hwang, Jung Sunwoo, Jae-Yong Chung

{"title":"Safety, Tolerability, and Serum/Tear Pharmacokinetics of Human Recombinant Epidermal Growth Factor Eyedrops in Healthy Subjects.","authors":"Hyounggyoon Yoo, Seonghae Yoon, In-Jin Jang, Kyung-Sang Yu, Joon Young Hyon, Jungi Hwang, Inyoung Hwang, Jung Sunwoo, Jae-Yong Chung","doi":"10.3390/ph15111312","DOIUrl":"https://doi.org/10.3390/ph15111312","url":null,"abstract":"The purpose of this study was to evaluate the safety, tolerability, and pharmacokinetics (PKs) of rhEGF eyedrops after the administration of single and multiple doses in healthy subjects. A phase 1, randomized, double-blind, placebo-controlled, and single-ascending dose (SAD) and multiple-ascending dose (MAD) study were conducted in three dose groups (10, 50, and 100 μg/mL). The subjects randomly received rhEGF eyedrops or the placebo in a 3:1 ratio. Serial blood and tear samples for PK analysis were collected up to 36 h and 180 h post-dose in SAD and MAD studies, respectively. In addition, the serum and tear EGF concentrations were measured. Immunogenicity evaluations were conducted using serum anti-EGF antibody levels. A total of 50 subjects were enrolled and 48 subjects completed the study. Adverse drug reactions were mild and transient. There were no serious adverse events in this study. The tear EGF concentrations rapidly increased and returned to baseline after 4 h without any serum EGF level change after the administration of rhEGF eyedrops. rhEGF eyedrops were safe and well-tolerated in healthy subjects in a dose range of 10-100 μg/mL, indicating suitability for further studies in patients with corneal injury.","PeriodicalId":520747,"journal":{"name":"Pharmaceuticals (Basel, Switzerland)","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2022-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9697941/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40464349","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Neuroprotective Effect of Red Sea Marine Sponge Xestospongia testudinaria Extract Using In Vitro and In Vivo Diabetic Peripheral Neuropathy Models. 红海海绵绒绵提取物对糖尿病周围神经病变模型的神经保护作用。

IF 4.6

Pharmaceuticals (Basel, Switzerland) Pub Date : 2022-10-24 DOI: 10.3390/ph15111309

Rania Magadmi, Kariman Borouk, Diaa T A Youssef, Lamiaa A Shaala, Aziza R Alrafiah, Rasheed A Shaik, Sameer E Alharthi

{"title":"Neuroprotective Effect of Red Sea Marine Sponge Xestospongia testudinaria Extract Using In Vitro and In Vivo Diabetic Peripheral Neuropathy Models.","authors":"Rania Magadmi, Kariman Borouk, Diaa T A Youssef, Lamiaa A Shaala, Aziza R Alrafiah, Rasheed A Shaik, Sameer E Alharthi","doi":"10.3390/ph15111309","DOIUrl":"https://doi.org/10.3390/ph15111309","url":null,"abstract":"Diabetic peripheral neuropathy (DPN) is a common complication of diabetes. Oxidative stress plays an important role in the pathophysiology of DPN. Red Sea marine sponge Xestospongia testudinaria extract has a promising neuroprotective effect, presumably owing to its antioxidant and anti-inflammatory properties. Thus, this study aimed to investigate the neuroprotective effect of the sponge X. testudinaria extract on in vitro and in vivo models of DPN. Mice dorsal root ganglia (DRG) were cultured with high glucose (HG) media and used as an in vitro model of DPN. Some of the DRGs were pre-treated with 2 mg/mL of X. testudinaria. The X. testudinaria extract significantly improved the HG-induced decreased neuronal viability and the neurite length. It improved the oxidative stress biomarkers in DRG cultures. The DPN model was induced in vivo by an injection of streptozotocin at a dose of 150 mg/kg in mice. After 35 days, 0.75 mg/kg of the X. testudinaria extract improved the hot hyperalgesia and the DRG histology. Although the sponge extract did not reduce hyperglycemia, it ameliorated the oxidative stress markers and pro-inflammatory markers in the DRG. In conclusion, the current study demonstrates the neuroprotective effect of Red Sea sponge X. testudinaria extract against experimentally induced DPN through its antioxidant and anti-inflammatory mechanisms.","PeriodicalId":520747,"journal":{"name":"Pharmaceuticals (Basel, Switzerland)","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2022-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9693000/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40464347","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 3