Acta Poloniae Pharmaceutica - Drug Research最新文献_第2页

Validation of Novel High-Performance Liquid Chromatography Method for Meropenem Quantification in Plasma 验证用于血浆中美罗培南定量的新型高效液相色谱法

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-04-09 DOI: 10.32383/appdr/183621

Aleksandar Rančić, M. Folic, Nemanja Petrović, Violeta Ilić Todorović, Milica Stanojević, Miloš N. Milosavljević, Milica Milentijević, Slobodan M Janković

{"title":"Validation of Novel High-Performance Liquid Chromatography Method for Meropenem Quantification in Plasma","authors":"Aleksandar Rančić, M. Folic, Nemanja Petrović, Violeta Ilić Todorović, Milica Stanojević, Miloš N. Milosavljević, Milica Milentijević, Slobodan M Janković","doi":"10.32383/appdr/183621","DOIUrl":"https://doi.org/10.32383/appdr/183621","url":null,"abstract":"Eminent societies of clinicians worldwide advise the implementation of therapeutic monitoring of meropenem. Our aim was to validate the new high-performance liquid chromatography (HPLC) technique for the measurement of meropenem in plasma that we developed. The validation of the method was performed in accordance with the official European Medicines Agency (EMA) guideline for bioanalytical method validation through the assessment of the following validation parameters: linearity and limit of detection/quantification, trueness and precision, recovery, selectivity, matrix-effect assessment, dilution integrity, carry-over assessment, and stability. Our calibration curve was found to be linear over the concentration ranges of 1.25–100 μg/mL, which covers the therapeutic range of meropenem in patients. From the calibration curve, the limits of detection and quantification were calculated to be 0.4 μg/mL and 1.2 μg/mL, respectively. Recovery ranged from 81.7 to 95.9 percent. Intra-day truennes ranged from −1.9 to 2.6% and inter-day trueness ranged from −4.7 to 3.8%. Intra-day precision was less than 4 percent, while inter-day precision was less than 7 percent. Meropenem remained stable in the patient plasma sample for one week at −20°C. Our HPLC technique can be applied in clinical practice for the therapeutic monitoring of meropenem in critically ill and other vulnerable patients since it is simple, rapid, and reliable.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140721424","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

Bioequivalence of Rivaroxaban Hard Capsules vs. Film-Coated Tablets in Healthy White Volunteers 健康白人志愿者服用利伐沙班硬胶囊与薄膜衣片的生物等效性研究

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-04-09 DOI: 10.32383/appdr/185676

Agnieszka Gierczak-Pachulska, M. Kaza, Katarzyna Jarus-Dziedzic, Olga Czerepow-Bielik, A. Segiet-Święcicka, Grzegorz Huszcza, Katarzyna Sidoruk, Daniel Rabczenko, P. Rudzki

{"title":"Bioequivalence of Rivaroxaban Hard Capsules vs. Film-Coated Tablets in Healthy White Volunteers","authors":"Agnieszka Gierczak-Pachulska, M. Kaza, Katarzyna Jarus-Dziedzic, Olga Czerepow-Bielik, A. Segiet-Święcicka, Grzegorz Huszcza, Katarzyna Sidoruk, Daniel Rabczenko, P. Rudzki","doi":"10.32383/appdr/185676","DOIUrl":"https://doi.org/10.32383/appdr/185676","url":null,"abstract":"Rivaroxaban is an oral anticoagulant that is a selective, direct factor Xa inhibitor. It is used to prevent thrombotic events of atherosclerotic etiology and to prevent stroke and peripheral embolism in adult patients with nonvalvular atrial fibrillation. The aim of studies was to assess the bioequivalence of two orally administered products: test (Zarixa hard capsules) vs. reference (Xarelto® film-coated tablets). Two crossover, 2-period, randomized, open-label, laboratory-blinded studies were conducted in healthy White male and female volunteers. A single oral dose (Study 1: 10 mg fasting, Study 2: 20 mg fed) of the test or reference product was followed by a minimum 7-day washout. Blood was collected up to 48 h after administration. Plasma concentrations of rivaroxaban were measured using a validated LC-MS/MS method. The bioequivalence criteria for 90% confidence intervals (CI) of the log-transformed geometric mean ratios (test/reference) for the two primary pharmacokinetic parameters (AUC(0-t) and Cmax) were set at 80.00-125.00%. Vital signs, laboratory parameters, and adverse events were monitored. 34 of 36 volunteers completed Study 1, and geometric mean ratios were 97.96% (90% CI 93.69-102.42%) for AUC(0-t), and 89.35% (90% CI 84.28-94.72%) for Cmax. All 36 volunteers completed Study 2, and geometric mean ratios were 103.57% (90% CI 98.75-108.63%) for AUC(0-t), and 95.17% (90% CI 87.35-103.70%) for Cmax. All of 90% CIs for the primary pharmacokinetic parameter ratios met acceptance criteria. There were no serious adverse events. Results of both studies indicate that the test product (Zarixa) is bioequivalent to the reference product (Xarelto®). Both products were well tolerated.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140724058","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

Phytochemical and Pharmaceutical Characterization of Seseli L. Species From Georgia 格鲁吉亚 Seseli L. 树种的植物化学和药物特性分析

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-04-09 DOI: 10.32383/appdr/185727

Mariam Nersezashvili, K. Skalicka‐Woźniak, Dali Berashvili

{"title":"Phytochemical and Pharmaceutical Characterization of Seseli L. Species From Georgia","authors":"Mariam Nersezashvili, K. Skalicka‐Woźniak, Dali Berashvili","doi":"10.32383/appdr/185727","DOIUrl":"https://doi.org/10.32383/appdr/185727","url":null,"abstract":"The Apiaceae family, formerly known as Umbelliferae, is one of the largest plant families, composed of 466 genera and nearly 3800 species worldwide. According to the Royal Kew Garden, it is also one of 12 plant families with a higher than-normal percentage of medicinal species, ranking 6th with 15% of its plants counted as medicinal. Seseli species, known for their high coumarin content as well as terpenoids, flavonoids, essential oils, and more, have been extensively investigated and found to possess various pharmacological properties such as antimicrobial, antitumor, antioxidant, cytotoxic, anti-nociceptive, anti-inflammatory, etc. Some Seseli species have also been used in treating central nervous system disorders such as anxiety. From 135 species 12 are distributed in Georgia (original name of the country is Sakhartvelo), from which 3 are endemics. Despite numerous studies on the chemical composition and pharmacological properties of various Seseli species, some remain unexplored, especially those found in Georgia, where data is limited and out of date. Therefore, further extensive research is necessary to improve understanding of the pharmacological activities, chemical constituents, and efficacy of plants from the Georgian Seseli species. The presented review draws attention to Seseli species distributed in Georgia, their phytochemistry, botanical characterisation and traditional use. However, as the information on biological activity of Georgian Seseli spp. is limited, we discussed potential pharmacological properties expected based on their chemical composition, also in relation with the same species from other countries or botanical gardens.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140723746","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

Inhibitors of CK2 Kinase for the Treatment of Gliomas and Other Brain Tumors 用于治疗胶质瘤和其他脑肿瘤的 CK2 激酶抑制剂

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-04-09 DOI: 10.32383/appdr/183629

E. Pucko, Robert P. Ostrowski

引用次数: 0

Alleviating effect of Lactobacillus pentosus CQZC01 probiotic strain on antibiotic-induced diarrhea in mice 戊糖乳杆菌 CQZC01 益生菌株对抗生素引起的小鼠腹泻的缓解作用

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-02-01 DOI: 10.32383/appdr/176426

Yanqing Liu, Mengqin Cheng, Bihui Liu, Mengwei Wang, Jing Song, Xin Zhao, Ruokun Yi, X. Long, Huazhi Liu

{"title":"Alleviating effect of Lactobacillus pentosus CQZC01 probiotic strain on antibiotic-induced diarrhea in mice","authors":"Yanqing Liu, Mengqin Cheng, Bihui Liu, Mengwei Wang, Jing Song, Xin Zhao, Ruokun Yi, X. Long, Huazhi Liu","doi":"10.32383/appdr/176426","DOIUrl":"https://doi.org/10.32383/appdr/176426","url":null,"abstract":"This experiment used mice as the experimental subjects to study the alleviating effect of Lactobacillus pentosus CQZC01 (LPCQZC01) on antibiotic-induced diarrhea in mice. After adaptive feeding for seven days, Kunming (KM) mice were randomly divided into the following groups: positive control group, model group, normal group, high concentration group of LPCQZC01 (H-LPCQZC01, 1×109 CFU/mL), and low concentration group of LPCQZC01 (L-LPCQZC01, 1×108 CFU/mL). Except for the normal group, mice were orally administered with lincomycin hydrochloride (120 mg/day) for 7 consecutive days. Changes in body weight, food intake, water consumption, and fecal water content of mice were observed. A histological examination of mouse colon and small intestine sections was done to find out if Lactobacillus pentosus CQZC01 may help mice with antibiotic-induced diarrhea. The findings demonstrated that, in comparison to the model group, mice in the H-LPCQZC01 and L-LPCQZC01 groups had considerably lower blood levels of nterleukin-6 (IL-6), interleukin-17A (IL-17A), 5-hydroxytryptamine (5-HT), and malondialdehyde (MDA), and other variables. In comparison to the model group, the fecal water content in the H-LPCQZC01 and L-LPCQZC01 groups was considerably lower. The H-LPCQZC01 and L-LPCQZC01 groups consumed more food and liquids than the model group did. The H-LPCQZC01 and L-LPCQZC01 groups had more intact colon walls and more compact, regular, and organized intestinal villi. H-LPCQZC01 and L-LPCQZC01 groups had the lower CFTR, EGFR expression and stronger NHE1, NHE2 expression than model group. This study reveals that Lactobacillus pentosus CQZC01 may treat inflammatory lesions in the mouse intestines and successfully treat antibiotic-induced diarrhea in mice.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139826652","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

Alleviating effect of Lactobacillus pentosus CQZC01 probiotic strain on antibiotic-induced diarrhea in mice 戊糖乳杆菌 CQZC01 益生菌株对抗生素引起的小鼠腹泻的缓解作用

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-02-01 DOI: 10.32383/appdr/176426

Yanqing Liu, Mengqin Cheng, Bihui Liu, Mengwei Wang, Jing Song, Xin Zhao, Ruokun Yi, X. Long, Huazhi Liu

{"title":"Alleviating effect of Lactobacillus pentosus CQZC01 probiotic strain on antibiotic-induced diarrhea in mice","authors":"Yanqing Liu, Mengqin Cheng, Bihui Liu, Mengwei Wang, Jing Song, Xin Zhao, Ruokun Yi, X. Long, Huazhi Liu","doi":"10.32383/appdr/176426","DOIUrl":"https://doi.org/10.32383/appdr/176426","url":null,"abstract":"This experiment used mice as the experimental subjects to study the alleviating effect of Lactobacillus pentosus CQZC01 (LPCQZC01) on antibiotic-induced diarrhea in mice. After adaptive feeding for seven days, Kunming (KM) mice were randomly divided into the following groups: positive control group, model group, normal group, high concentration group of LPCQZC01 (H-LPCQZC01, 1×109 CFU/mL), and low concentration group of LPCQZC01 (L-LPCQZC01, 1×108 CFU/mL). Except for the normal group, mice were orally administered with lincomycin hydrochloride (120 mg/day) for 7 consecutive days. Changes in body weight, food intake, water consumption, and fecal water content of mice were observed. A histological examination of mouse colon and small intestine sections was done to find out if Lactobacillus pentosus CQZC01 may help mice with antibiotic-induced diarrhea. The findings demonstrated that, in comparison to the model group, mice in the H-LPCQZC01 and L-LPCQZC01 groups had considerably lower blood levels of nterleukin-6 (IL-6), interleukin-17A (IL-17A), 5-hydroxytryptamine (5-HT), and malondialdehyde (MDA), and other variables. In comparison to the model group, the fecal water content in the H-LPCQZC01 and L-LPCQZC01 groups was considerably lower. The H-LPCQZC01 and L-LPCQZC01 groups consumed more food and liquids than the model group did. The H-LPCQZC01 and L-LPCQZC01 groups had more intact colon walls and more compact, regular, and organized intestinal villi. H-LPCQZC01 and L-LPCQZC01 groups had the lower CFTR, EGFR expression and stronger NHE1, NHE2 expression than model group. This study reveals that Lactobacillus pentosus CQZC01 may treat inflammatory lesions in the mouse intestines and successfully treat antibiotic-induced diarrhea in mice.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139886370","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

Emulsions containing allantoin and D-panthenol as attractive moisturizing agents 含有尿囊素和 D-泛醇的乳液是极具吸引力的保湿剂

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-02-01 DOI: 10.32383/appdr/174461

A. Czajkowska-Kośnik, Zofia Helena Bagińska, K. Winnicka

{"title":"Emulsions containing allantoin and D-panthenol as attractive moisturizing agents","authors":"A. Czajkowska-Kośnik, Zofia Helena Bagińska, K. Winnicka","doi":"10.32383/appdr/174461","DOIUrl":"https://doi.org/10.32383/appdr/174461","url":null,"abstract":"Dry skin is the common problem affecting people which triggers many unpleasant symptoms such as roughness, peeling, burning, itching and greater sensitivity to injury and external conditions. One method to assess the water loss of skin is transepidermal water loss (TEWL) measurement. Various active substances, for instance allantoin and D-panthenol, can be used to overcome the symptoms of the dry skin. In this study, emulsions containing allantoin and D-panthenol as moisturizing agents and various oils (liquid paraffin, Cannabis sativa, Baobab and Coconut oil) were developed. The prepared emulsions were characterized by: visual and microscopic appearance and pH values. Stability analysis was conducted by centrifuge test and sensory test using sensory sensation was evaluated. Rheological experiments were performed using a rheometer, while mechanical and adhesion tests by texture analyzer. TEWL values were measured using a tewameter, after application of the emulsions to the responders skin. TEWL study noticed that regular permanent use of moisturizing emulsions with allantoin and D-panthenol limited the water loss. In conclusion, it can be stated that emulsions containing allantoin and D-panthenol as active agents and Coconut oil as oily ingredient are attractive formulations with moisturizing effect and good application features.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139687456","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

Mechanism of inhibition of growth and metastasis of colon cancer by celecoxib analog OSU-03013 via wnt signaling pathway 塞来昔布类似物 OSU-03013 通过 wnt 信号通路抑制结肠癌生长和转移的机制

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-02-01 DOI: 10.32383/appdr/175914

ChunYong Yang, ZhiQiang Zhou, XueSong Wang, JianZhe Ren, Jing Qi

{"title":"Mechanism of inhibition of growth and metastasis of colon cancer by celecoxib analog OSU-03013 via wnt signaling pathway","authors":"ChunYong Yang, ZhiQiang Zhou, XueSong Wang, JianZhe Ren, Jing Qi","doi":"10.32383/appdr/175914","DOIUrl":"https://doi.org/10.32383/appdr/175914","url":null,"abstract":"OSU-03013 is a structurally modified analog of celecoxib. This study probed the antitumor activity of OSU-03013 on colon cancer (CC) and explored its possible mechanism. CCK-8 method was used to evaluate the activity of OSU-03013 on CC cell SW480 and normal colon epithelial cell FHC, and the anti-proliferation effect of OSU-03013 was detected by CCK-8 and colony formation assay. In addition, flow cytometry and Annexin V-FITC/PI were applied to detect apoptosis of SW480 cells, and Transwell was to detect cell migration and invasion. β-catenin, c-myc, and Wnt1 genes were assessed by RT-qPCR, and E-cadherin, N-cadherin, and β-catenin, c-myc, mTOR, p-mTOR, and Wnt1 proteins were detected by Western Blot. OSU-03013 had dose-dependent and time-dependent antitumor activity on SW480 cells, which can promote tumor cell apoptosis, up-regulate E-cadherin, and down-regulate β-catenin, c-myc, Wnt1, and N-cadherin. OSU-03013 has anti-tumor activity on CC cells. The anti-cancer mechanism of OSU-03013 is achieved by inhibiting the activation of Wnt pathway genes and inhibiting tumor invasion and metastasis. This study provides a scientific basis for the clinical application of OSU-03013 in the treatment of CC.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139881398","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

Content of selected polyphenolic compounds in four Sambucus nigra l. cultivars in relation to their antimicrobial activity 四种黑三叶草栽培品种中某些多酚化合物的含量与其抗菌活性的关系

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-02-01 DOI: 10.32383/appdr/175051

I. Korona-Głowniak, Martyna Kasela, Barbara Pliszka, D. Zalewski, Anna Malm

{"title":"Content of selected polyphenolic compounds in four Sambucus nigra l. cultivars in relation to their antimicrobial activity","authors":"I. Korona-Głowniak, Martyna Kasela, Barbara Pliszka, D. Zalewski, Anna Malm","doi":"10.32383/appdr/175051","DOIUrl":"https://doi.org/10.32383/appdr/175051","url":null,"abstract":"European elderberry (Sambucus nigra L.) fruits constitute a valuable source of biologically active compounds useful in the pharmaceutical industry. We aimed to determine the content of chosen polyphenolic compounds in fruit extracts from four cultivars of elderberry (Alleso, Korsor, Sampo, Samyl) and their relation to antibacterial and antifungal activity. The content of polyphenols was determined with the use of high-performance liquid chromatography (HPLC), while antimicrobial activity, including minimum inhibitory concentration (MIC), minimum bactericidal (MBC) or fungicidal (MFC) concentration, was studied with the use of microbroth dilution method. HPLC analysis revealed the presence of concentrations of cyanidin glycosides, caffeic and quercetin derivatives depending on the plant cultivar. The extracts exhibited the highest antibacterial activity against Staphylococcus spp. (MIC = 0.313 – 0.625 mg/mL) and Helicobacter pylori (MIC = 0.313 – 1.25 mg/mL) and antifungal against Candida albicans and C. parapsilosis (MIC = 0.313 – 2.5 mg/mL). Results showed that the concentration of cyanidin glycosides, caffeic and quercetin derivatives depended on the analyzed S. nigra L. cultivar and pointed towards a correlation between their high content and antimicrobial activity. These results support the idea that elderberry fruits contain bioactive compounds providing them significant antimicrobial potential.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139875807","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

Mechanism of inhibition of growth and metastasis of colon cancer by celecoxib analog OSU-03013 via wnt signaling pathway 塞来昔布类似物 OSU-03013 通过 wnt 信号通路抑制结肠癌生长和转移的机制

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-02-01 DOI: 10.32383/appdr/175914

ChunYong Yang, ZhiQiang Zhou, XueSong Wang, JianZhe Ren, Jing Qi

{"title":"Mechanism of inhibition of growth and metastasis of colon cancer by celecoxib analog OSU-03013 via wnt signaling pathway","authors":"ChunYong Yang, ZhiQiang Zhou, XueSong Wang, JianZhe Ren, Jing Qi","doi":"10.32383/appdr/175914","DOIUrl":"https://doi.org/10.32383/appdr/175914","url":null,"abstract":"OSU-03013 is a structurally modified analog of celecoxib. This study probed the antitumor activity of OSU-03013 on colon cancer (CC) and explored its possible mechanism. CCK-8 method was used to evaluate the activity of OSU-03013 on CC cell SW480 and normal colon epithelial cell FHC, and the anti-proliferation effect of OSU-03013 was detected by CCK-8 and colony formation assay. In addition, flow cytometry and Annexin V-FITC/PI were applied to detect apoptosis of SW480 cells, and Transwell was to detect cell migration and invasion. β-catenin, c-myc, and Wnt1 genes were assessed by RT-qPCR, and E-cadherin, N-cadherin, and β-catenin, c-myc, mTOR, p-mTOR, and Wnt1 proteins were detected by Western Blot. OSU-03013 had dose-dependent and time-dependent antitumor activity on SW480 cells, which can promote tumor cell apoptosis, up-regulate E-cadherin, and down-regulate β-catenin, c-myc, Wnt1, and N-cadherin. OSU-03013 has anti-tumor activity on CC cells. The anti-cancer mechanism of OSU-03013 is achieved by inhibiting the activation of Wnt pathway genes and inhibiting tumor invasion and metastasis. This study provides a scientific basis for the clinical application of OSU-03013 in the treatment of CC.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139821422","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