Acta Poloniae Pharmaceutica - Drug Research最新文献_第5页

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":"27 15","pages":""},"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":"30 3","pages":""},"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":"264 ","pages":""},"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

Polish physicians' views on compounded medicines and factors related to the frequency of their prescription 波兰医生对复方药物的看法及其处方频率的相关因素

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-02-01 DOI: 10.32383/appdr/178181

Piotr Guzy, Andrzej Porębski, Sławomir Łudzik, Natalia Obajtek, Anna Gołda

{"title":"Polish physicians' views on compounded medicines and factors related to the frequency of their prescription","authors":"Piotr Guzy, Andrzej Porębski, Sławomir Łudzik, Natalia Obajtek, Anna Gołda","doi":"10.32383/appdr/178181","DOIUrl":"https://doi.org/10.32383/appdr/178181","url":null,"abstract":"The aim of this study was to verify if there is a relationship between physicians' specialization, place of practice, or views on issues related to compounded medicines and the frequency of prescribing such formulations. Additionally, the study aimed to determine the factors that influence these views. The study also examined the barriers and encouragements, according to physicians, in the use of compounded medicines. The original questionnaire was developed specifically for this study. Included sample consisted of Polish-speaking physicians whose main specialization was gynaecology, gastroenterology, dermatology, family medicine, internal medicine, otorhinolaryngology, paediatric otorhinolaryngology, paediatrics. Answers were gathered using computer-assisted telephone interview. The majority of surveyed physicians believed that every Polish patient receives treatment tailored to their personal needs (68,7%) and agreed that compounded medicines are a way to facilitate individualization of pharmacotherapy (79,3%). Frequency of prescribing of magistral formulations, as well as views on quality of compounded medicines, ease of prescribing, and filling a prescription vary between specializations and places of practice. The problem that negatively affects the practice of the largest group of respondents was complicated and frequently changing legal regulations (63.3%), while the least frequently indicated problems were concerns about the quality of preparation (16.7%). Based on opinion of surveyed physicians, a simplification of the regulations for prescribing and liberalization of reimbursement rules are main changes to consider in order to improve clinical practice in the areas where it relates to the prescription of compounded medicines.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":"99 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139832689","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

Preparation and characterization of a solid dispersion formulation of coenzyme Q10 loaded with protamine: an efficient and novel strategy to enhance bioavailability and stability 添加原胺的辅酶 Q10 固体分散制剂的制备和表征：提高生物利用率和稳定性的高效新策略

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-02-01 DOI: 10.32383/appdr/177294

Yingying Liao, Li Sun, Wenhao Xu, Pei Qiao, Duncong Fan

{"title":"Preparation and characterization of a solid dispersion formulation of coenzyme Q10 loaded with protamine: an efficient and novel strategy to enhance bioavailability and stability","authors":"Yingying Liao, Li Sun, Wenhao Xu, Pei Qiao, Duncong Fan","doi":"10.32383/appdr/177294","DOIUrl":"https://doi.org/10.32383/appdr/177294","url":null,"abstract":"Coenzyme Q10 (CoQ10) is an endogenous, lipophilic quinone compound that functions as an electron carrier in the mitochondrial respiratory chain and plays a pivotal role in cell metabolism. Despite its numerous important physiological functions, the practical application of CoQ10 is limited due to its high molecular weight, poor water solubility, photolability, chemical instability, and low bioavailability. To overcome these challenges, we developed a solid dispersion formulation of protamine loaded CoQ10 (CoQ10/Pr) using an efficient mechanochemical technology without solvents. Protamine was used as carrier and poloxamer 188 as solubilizer, while butylated hydroxytoluene (BHT) and micro powder silica gel were utilized as stabilizers and lubricants. The optimal ball milling condition to prepare CoQ10/Pr was at 100 r/min for 4 hours. The treated CoQ10/Pr has exhibited rapid-release properties, with significantly enhanced water solubility by 392,000 times, and bioavailability by 0.68 times. Furthermore, the treated CoQ10/Pr became resistant to moisture, high temperature and strong light, which makes it suitable for long-term storage. The molecular docking suggested that the solubilization mechanism of CoQ10 was closely associated with the encapsulation and complexation of protamine, as well as the formation of an intermolecular complex through hydrogen bond between CoQ10 and arginine residues on protamine. In summary, the CoQ10 solid dispersion formulation enjoys advantages such as excellent water solubility, stability, bioavailability, and low cost. This formulation also meets the stringent quality requirements of products in the food, cosmetic, and health industries. It offers dual benefits in both theoretical research and industrial development.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":"31 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139881355","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

Simultaneous HPLC method development for azelastine HCl and fluticasone propionate nasal spray formulation 盐酸阿折拉斯汀和丙酸氟替卡松鼻喷雾剂配方的同步高效液相色谱法开发

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-02-01 DOI: 10.32383/appdr/178243

Hani Naseef, Enas Abu Arrah, Ahmad Alian, A. Abukhalil, N. Malkieh

引用次数: 0

Preparation and characterization of a solid dispersion formulation of coenzyme Q10 loaded with protamine: an efficient and novel strategy to enhance bioavailability and stability 添加原胺的辅酶 Q10 固体分散制剂的制备和表征：提高生物利用率和稳定性的高效新策略

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-02-01 DOI: 10.32383/appdr/177294

Yingying Liao, Li Sun, Wenhao Xu, Pei Qiao, Duncong Fan

{"title":"Preparation and characterization of a solid dispersion formulation of coenzyme Q10 loaded with protamine: an efficient and novel strategy to enhance bioavailability and stability","authors":"Yingying Liao, Li Sun, Wenhao Xu, Pei Qiao, Duncong Fan","doi":"10.32383/appdr/177294","DOIUrl":"https://doi.org/10.32383/appdr/177294","url":null,"abstract":"Coenzyme Q10 (CoQ10) is an endogenous, lipophilic quinone compound that functions as an electron carrier in the mitochondrial respiratory chain and plays a pivotal role in cell metabolism. Despite its numerous important physiological functions, the practical application of CoQ10 is limited due to its high molecular weight, poor water solubility, photolability, chemical instability, and low bioavailability. To overcome these challenges, we developed a solid dispersion formulation of protamine loaded CoQ10 (CoQ10/Pr) using an efficient mechanochemical technology without solvents. Protamine was used as carrier and poloxamer 188 as solubilizer, while butylated hydroxytoluene (BHT) and micro powder silica gel were utilized as stabilizers and lubricants. The optimal ball milling condition to prepare CoQ10/Pr was at 100 r/min for 4 hours. The treated CoQ10/Pr has exhibited rapid-release properties, with significantly enhanced water solubility by 392,000 times, and bioavailability by 0.68 times. Furthermore, the treated CoQ10/Pr became resistant to moisture, high temperature and strong light, which makes it suitable for long-term storage. The molecular docking suggested that the solubilization mechanism of CoQ10 was closely associated with the encapsulation and complexation of protamine, as well as the formation of an intermolecular complex through hydrogen bond between CoQ10 and arginine residues on protamine. In summary, the CoQ10 solid dispersion formulation enjoys advantages such as excellent water solubility, stability, bioavailability, and low cost. This formulation also meets the stringent quality requirements of products in the food, cosmetic, and health industries. It offers dual benefits in both theoretical research and industrial development.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":"437 ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139821217","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

Simultaneous HPLC method development for azelastine HCl and fluticasone propionate nasal spray formulation 盐酸阿折拉斯汀和丙酸氟替卡松鼻喷雾剂配方的同步高效液相色谱法开发

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-02-01 DOI: 10.32383/appdr/178243

Hani Naseef, Enas Abu Arrah, Ahmad Alian, A. Abukhalil, N. Malkieh

引用次数: 0

Emollients with natural emulsifier Olivem 1000 as topical formulations for urea or sodium hyaluronate 含有天然乳化剂 Olivem 1000 的润肤剂，可作为尿素或透明质酸钠的外用制剂

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-02-01 DOI: 10.32383/appdr/175847

M. Wróblewska, K. Winnicka

{"title":"Emollients with natural emulsifier Olivem 1000 as topical formulations for urea or sodium hyaluronate","authors":"M. Wróblewska, K. Winnicka","doi":"10.32383/appdr/175847","DOIUrl":"https://doi.org/10.32383/appdr/175847","url":null,"abstract":"Xerosis is one of the common dermatological problems. Preparations recommended for daily care of the dry skin are emollients. Emollient preparations demonstrate a moisturizing effect, they soften and smoothen the skin, keep water in the epidermis, supplement lipids of skin upper layers and protect from external harmful agents. The purpose of this study was to develop and characterize emollients containing natural emulsifier Olivem 1000 as topical delivery systems for urea or sodium hialuronate. Physicochemical and mechanical properties of designed formulations were evaluated. Moreover, ex vivo adhesion study on the hairless mice skin as a model of adhesive layer was carried out and in vivo preliminary assessment of transepidermal water loss (TEWL) was performed. Prepared emollient formulations were characterized by smooth consistency, they were easily spreadable on the skin surface and showed no phase separation. Formulations containing xanthan gum as a thickening agent were characterized by higher viscosity, hardness, cohesiveness and adhesiveness values. Prepared emollients showed thixotropic properties and they were classified as non-Newtonian shear thinning systems. All prepared emollients demonstrated bioadhesive properties. The analysis of TEWL showed that the greatest decrease in the TEWL value was noted in the case of emollient containing sodium hyaluronate which was applied to the person with the skin described as “the skin in a very poor condition”. The results of the conducted research indicate that developed emollients containing natural emulsifier Olivem 1000 seem to be a promising form of care preparations for topical use in case of chronic dryness of the skin.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":"79 3-4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139886317","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

Emollients with natural emulsifier Olivem 1000 as topical formulations for urea or sodium hyaluronate 含有天然乳化剂 Olivem 1000 的润肤剂，可作为尿素或透明质酸钠的外用制剂

Acta Poloniae Pharmaceutica - Drug Research Pub Date : 2024-02-01 DOI: 10.32383/appdr/175847

M. Wróblewska, K. Winnicka

{"title":"Emollients with natural emulsifier Olivem 1000 as topical formulations for urea or sodium hyaluronate","authors":"M. Wróblewska, K. Winnicka","doi":"10.32383/appdr/175847","DOIUrl":"https://doi.org/10.32383/appdr/175847","url":null,"abstract":"Xerosis is one of the common dermatological problems. Preparations recommended for daily care of the dry skin are emollients. Emollient preparations demonstrate a moisturizing effect, they soften and smoothen the skin, keep water in the epidermis, supplement lipids of skin upper layers and protect from external harmful agents. The purpose of this study was to develop and characterize emollients containing natural emulsifier Olivem 1000 as topical delivery systems for urea or sodium hialuronate. Physicochemical and mechanical properties of designed formulations were evaluated. Moreover, ex vivo adhesion study on the hairless mice skin as a model of adhesive layer was carried out and in vivo preliminary assessment of transepidermal water loss (TEWL) was performed. Prepared emollient formulations were characterized by smooth consistency, they were easily spreadable on the skin surface and showed no phase separation. Formulations containing xanthan gum as a thickening agent were characterized by higher viscosity, hardness, cohesiveness and adhesiveness values. Prepared emollients showed thixotropic properties and they were classified as non-Newtonian shear thinning systems. All prepared emollients demonstrated bioadhesive properties. The analysis of TEWL showed that the greatest decrease in the TEWL value was noted in the case of emollient containing sodium hyaluronate which was applied to the person with the skin described as “the skin in a very poor condition”. The results of the conducted research indicate that developed emollients containing natural emulsifier Olivem 1000 seem to be a promising form of care preparations for topical use in case of chronic dryness of the skin.","PeriodicalId":7135,"journal":{"name":"Acta Poloniae Pharmaceutica - Drug Research","volume":"94 ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139826376","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