Pub Date : 2024-07-12DOI: 10.3897/pharmacia.71.e130302
Atanas Toshev, Elina S Petkova-Gueorguieva, A. Mihaylova, V. Kirkov, V. Madzharov, H. Lebanova, Svetoslav Stoev, S. Gueorguiev
The digitization of health systems is a topic of immense significance for the modern world. It holds the potential to transform the delivery of healthcare services, enhancing their quality, efficiency, and accessibility. Electronic prescriptions are a key element of this process, but it is crucial to ensure their implementation protects patients’ personal data and privacy. This article examines the digitization of health systems in Bulgaria, with a focus on electronic prescriptions. It highlights aspects of data protection, the potential risks associated with data misuse, and the advantages of electronic prescriptions.
{"title":"Digitalization of health care and aspects of implementing electronic prescriptions in Bulgaria","authors":"Atanas Toshev, Elina S Petkova-Gueorguieva, A. Mihaylova, V. Kirkov, V. Madzharov, H. Lebanova, Svetoslav Stoev, S. Gueorguiev","doi":"10.3897/pharmacia.71.e130302","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e130302","url":null,"abstract":"The digitization of health systems is a topic of immense significance for the modern world. It holds the potential to transform the delivery of healthcare services, enhancing their quality, efficiency, and accessibility. Electronic prescriptions are a key element of this process, but it is crucial to ensure their implementation protects patients’ personal data and privacy. This article examines the digitization of health systems in Bulgaria, with a focus on electronic prescriptions. It highlights aspects of data protection, the potential risks associated with data misuse, and the advantages of electronic prescriptions.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141653028","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}
Pub Date : 2024-07-10DOI: 10.3897/pharmacia.71.e126108
C. T. Yupanqui, Anunya Suksanga, Sutasinee Ardhanwanich, S. Ungphaiboon
This study aimed to enhance the delivery of turmeric by encapsulating its extract within microparticles using chitosan and mannitol through the spray drying technique and to assess their acute oral toxicity. The resulting microparticles were spherical, with an average diameter of 4 microns, and comprised 17% curcuminoids and 4% ar-turmerone. In vitro studies demonstrated that these microparticles had a higher release rate of curcuminoids compared to raw turmeric extract and preserved antioxidant activity. In the acute toxicity study, conducted in Wistar rats with a single dose of 2,000 mg/kg, no acute toxic symptoms were observed. According to the Globally Harmonized System of Classification and Labeling of Chemicals, the microparticles were categorized as having relatively low acute toxicity (category 5). These findings support the potential utility of the microparticles in dietary supplements and pharmaceutical applications due to their effective delivery properties and safety profile.
{"title":"Spray-dried microparticles of turmeric extract for improved delivery and low toxicity","authors":"C. T. Yupanqui, Anunya Suksanga, Sutasinee Ardhanwanich, S. Ungphaiboon","doi":"10.3897/pharmacia.71.e126108","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e126108","url":null,"abstract":"This study aimed to enhance the delivery of turmeric by encapsulating its extract within microparticles using chitosan and mannitol through the spray drying technique and to assess their acute oral toxicity. The resulting microparticles were spherical, with an average diameter of 4 microns, and comprised 17% curcuminoids and 4% ar-turmerone. In vitro studies demonstrated that these microparticles had a higher release rate of curcuminoids compared to raw turmeric extract and preserved antioxidant activity. In the acute toxicity study, conducted in Wistar rats with a single dose of 2,000 mg/kg, no acute toxic symptoms were observed. According to the Globally Harmonized System of Classification and Labeling of Chemicals, the microparticles were categorized as having relatively low acute toxicity (category 5). These findings support the potential utility of the microparticles in dietary supplements and pharmaceutical applications due to their effective delivery properties and safety profile.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141661999","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}
Pub Date : 2024-07-10DOI: 10.3897/pharmacia.71.e127784
Yaseen S. Hamdoon, Mohammed K. Hadi
Bacterial infections pose an ongoing challenge due to resistance developed by infectious bacteria. So much research targeting designing new antibacterials is published annually. Our goal is to synthesize compounds that have given antibacterial activity according to molecular docking against the chosen target protein and that have acceptable ADMET properties that can be synthesized and used in the future. New 2-(5-methoxy-1-(4-chlorobenzene)-2-methyl-1H-indol-3-yl)acetohydrazide derivatives’ antibacterial efficacy against two common strains of Gram-negative and Gram-positive microorganisms has been developed, produced, and investigated. Sophisticated, modern analytical methods, including ATR-FTIR and 1H NMR spectroscopy, were used to determine their spectral and physicochemical features. Compound YA3N is more effective than ciprofloxacin against K. pneumonia (MIC = 125 µg/mL) and shows good suppression of isolated tests of E. coli (MIC = 125 µg/mL). While compound YA4C demonstrated comparable suppression of S. pyogenes strains (MIC = 250 µg/mL), compounds YA3S and YA4B exhibit lesser activity towards the tested strain of bacteria.
{"title":"Molecular docking, ADMET, synthesis and evaluation of new indomethacin hydrazide derivatives as antibacterial agents","authors":"Yaseen S. Hamdoon, Mohammed K. Hadi","doi":"10.3897/pharmacia.71.e127784","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e127784","url":null,"abstract":"Bacterial infections pose an ongoing challenge due to resistance developed by infectious bacteria. So much research targeting designing new antibacterials is published annually. Our goal is to synthesize compounds that have given antibacterial activity according to molecular docking against the chosen target protein and that have acceptable ADMET properties that can be synthesized and used in the future. New 2-(5-methoxy-1-(4-chlorobenzene)-2-methyl-1H-indol-3-yl)acetohydrazide derivatives’ antibacterial efficacy against two common strains of Gram-negative and Gram-positive microorganisms has been developed, produced, and investigated. Sophisticated, modern analytical methods, including ATR-FTIR and 1H NMR spectroscopy, were used to determine their spectral and physicochemical features. Compound YA3N is more effective than ciprofloxacin against K. pneumonia (MIC = 125 µg/mL) and shows good suppression of isolated tests of E. coli (MIC = 125 µg/mL). While compound YA4C demonstrated comparable suppression of S. pyogenes strains (MIC = 250 µg/mL), compounds YA3S and YA4B exhibit lesser activity towards the tested strain of bacteria.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141661342","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}
Pub Date : 2024-07-10DOI: 10.3897/pharmacia.71.e127565
Leo Simanjuntak, Cheryl Grace Pratiwi Rumahorbo
Preeclampsia, a complex pregnancy disorder characterized by hypertension and proteinuria, poses significant risks to maternal and perinatal health. Despite extensive research, its etiology remains elusive. This study investigates the therapeutic potential of nano-herbal Phaleria macrocarpa, a medicinal plant known for its anti-inflammatory and antioxidant properties, in a rat model of preeclampsia. The study elucidates the formulation’s effects through a multifaceted evaluation of physiological parameters, including blood pressure, organ weight, and complete blood counts. Pregnant rats were divided into five treatment groups (C-, C+, C1, T1, T2, and T3) and intraperitoneally injected with prednisone and 6% NaCl for 14 days to induce preeclampsia. Preeclamptic rats exhibited a blood pressure of 140/90 mmHg. C- served as the negative control and C+ as the positive control; C1 received nifedipine, while T1, T2, and T3 received varying doses of the herbal formulation. Blood pressure was measured on days 5, 13, and 20 of pregnancy, with a complete blood count and organ weight analyses conducted on the final treatment day. The results indicated significant differences among the three administered doses. The T3 group (720 mg/kg BW) exhibited noteworthy similarities to nifedipine. Implementing the T3 dosage demonstrated superior efficacy in preserving blood pressure, a complete blood profile, and organ health in preeclampsia rat models. Substantial reductions in diastolic blood pressure, changes in organ weights, and enhancements in hematological parameters supported these findings, underscoring the potential of Phaleria macrocarpa as both an antihypertensive and organ-protective agent.
{"title":"Effectiveness of nano-herbal Phaleria macrocarpa on physiological evaluation in Rattus norvegicus","authors":"Leo Simanjuntak, Cheryl Grace Pratiwi Rumahorbo","doi":"10.3897/pharmacia.71.e127565","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e127565","url":null,"abstract":"Preeclampsia, a complex pregnancy disorder characterized by hypertension and proteinuria, poses significant risks to maternal and perinatal health. Despite extensive research, its etiology remains elusive. This study investigates the therapeutic potential of nano-herbal Phaleria macrocarpa, a medicinal plant known for its anti-inflammatory and antioxidant properties, in a rat model of preeclampsia. The study elucidates the formulation’s effects through a multifaceted evaluation of physiological parameters, including blood pressure, organ weight, and complete blood counts. Pregnant rats were divided into five treatment groups (C-, C+, C1, T1, T2, and T3) and intraperitoneally injected with prednisone and 6% NaCl for 14 days to induce preeclampsia. Preeclamptic rats exhibited a blood pressure of 140/90 mmHg. C- served as the negative control and C+ as the positive control; C1 received nifedipine, while T1, T2, and T3 received varying doses of the herbal formulation. Blood pressure was measured on days 5, 13, and 20 of pregnancy, with a complete blood count and organ weight analyses conducted on the final treatment day. The results indicated significant differences among the three administered doses. The T3 group (720 mg/kg BW) exhibited noteworthy similarities to nifedipine. Implementing the T3 dosage demonstrated superior efficacy in preserving blood pressure, a complete blood profile, and organ health in preeclampsia rat models. Substantial reductions in diastolic blood pressure, changes in organ weights, and enhancements in hematological parameters supported these findings, underscoring the potential of Phaleria macrocarpa as both an antihypertensive and organ-protective agent.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141662879","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}
Pub Date : 2024-07-09DOI: 10.3897/pharmacia.71.e127981
Lauren Emily Fajardo, Mark Andrian B Macalalad, N. M. Odchimar, John Christian de Guzman, Fredmoore L. Orosco
The majority of hepatocellular carcinoma cases are caused by infection with hepatitis B (HBV) or C (HCV) viruses. CTNNB1 is the most mutated oncogene in HBV- and HCV-associated tumors. CTNNB1 mutations can lead to β-catenin accumulation, resulting in tumor progression. Small interfering RNAs (siRNAs) can be used to silence CTNNB1 mRNA. After prediction and evaluation, four siRNAs were found to have the highest silencing potential. All four siRNAs had an acceptable GC content, no palindromic sequences, no off-targets, were thermostable, and had accessible target sites. Molecular docking of the siRNAs to Argonaute 2 demonstrated favorable docking scores within the binding pocket for three siRNAs. Molecular dynamics simulations and binding energy calculations demonstrated that the siRNAs steadily remained in the binding pocket. In this study, three siRNAs were successfully designed to silence oncogenic CTNNB1 mRNA as a therapeutic strategy against hepatocellular carcinoma and warrant further in vitro and in vivo validation.
{"title":"Computational design and validation of siRNA molecules to silence oncogenic CTNNB1 mRNA as a potential therapeutic strategy against hepatitis B/C virus-associated hepatocellular carcinoma","authors":"Lauren Emily Fajardo, Mark Andrian B Macalalad, N. M. Odchimar, John Christian de Guzman, Fredmoore L. Orosco","doi":"10.3897/pharmacia.71.e127981","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e127981","url":null,"abstract":"The majority of hepatocellular carcinoma cases are caused by infection with hepatitis B (HBV) or C (HCV) viruses. CTNNB1 is the most mutated oncogene in HBV- and HCV-associated tumors. CTNNB1 mutations can lead to β-catenin accumulation, resulting in tumor progression. Small interfering RNAs (siRNAs) can be used to silence CTNNB1 mRNA. After prediction and evaluation, four siRNAs were found to have the highest silencing potential. All four siRNAs had an acceptable GC content, no palindromic sequences, no off-targets, were thermostable, and had accessible target sites. Molecular docking of the siRNAs to Argonaute 2 demonstrated favorable docking scores within the binding pocket for three siRNAs. Molecular dynamics simulations and binding energy calculations demonstrated that the siRNAs steadily remained in the binding pocket. In this study, three siRNAs were successfully designed to silence oncogenic CTNNB1 mRNA as a therapeutic strategy against hepatocellular carcinoma and warrant further in vitro and in vivo validation.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141664368","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}
Pub Date : 2024-07-05DOI: 10.3897/pharmacia.71.e128428
Ika Citra Dewi Tanjung, Dina Keumala Sari, O. R. Ramayani, M. Amin, B. Medise, M. Rusda, Masitha Dewi Sari, Nuraiza Meutia
Background: Nephrotic syndrome (NS) is a pediatric kidney disease with a high recurrence rate, impacting patient quality of life (QoL). This study aimed to assess the QoL of NS children in North Sumatera using a parent-and-child proxy report. Methods: This was a cross-sectional study (February–December 2023) in the nephrology and growth and developmental outpatient ward, Pediatrics Department, Adam Malik Hospital, and Prof. Dr. Chairuddin P. Lubis Universitas Sumatera Utara Hospital, Medan, Indonesia. The inclusion criteria for cases were children aged 5–18 who met the diagnostic criteria of NS. Cases were age-matched with healthy children as controls. The PedsQL 4.0 generic core scale instrument was used for the QoL assessment. Normally distributed continuous data were expressed as the mean and standard deviation; categorical data were expressed as proportions. Differences between the groups were analyzed using an independent t-test, and the correlation of illness duration and daily steroid dose with QoL was determined using the Pearson correlation test. Results: A total of 44 NS pediatric patients were age-matched with 44 healthy children. A significant difference in QoL existed between the school scores of the NS and healthy groups in the parent proxy report (p = 0.001) and between the school score and total score of the child proxy report (p = 0.003 and p = 0.040, respectively). A significant difference in QoL existed in emotional scores between the remission and relapse groups in the parent-and-child proxy reports (p = 0.019 and 0.030, respectively). A significant negative correlation existed between the daily steroid dose and QoL in school and the total score of the parent proxy report (p = 0.025; r = –0.338). Conclusion: The parent and child reports revealed a significant difference in QoL between the school scores of NS pediatric patients and healthy children. A significant difference in the emotional scores of NS pediatric patients in remission and relapse was also observed. The daily steroid dose was negatively correlated with the school score in the parent proxy report.
背景：肾病综合征（NS）是一种小儿肾病，复发率高，影响患者的生活质量（QoL）。本研究旨在使用家长和儿童代理报告评估北苏门答腊省肾病综合征儿童的生活质量。研究方法这是一项横断面研究（2023 年 2 月至 12 月），研究地点位于印度尼西亚棉兰市亚当-马利克医院儿科肾脏病和生长发育门诊病房，以及苏门答腊大学医院 Chairuddin P. Lubis 教授。纳入病例的标准是符合 NS 诊断标准的 5-18 岁儿童。病例与健康儿童作为对照进行年龄匹配。QoL 评估采用 PedsQL 4.0 通用核心量表。正态分布的连续数据以均值和标准差表示；分类数据以比例表示。组间差异采用独立 t 检验，病程和每日类固醇剂量与 QoL 的相关性采用皮尔逊相关检验。结果44名NS儿童患者与44名健康儿童进行了年龄配对。在家长代理报告中，NS组和健康组的学校得分（p = 0.001）以及儿童代理报告中的学校得分和总分（分别为p = 0.003和p = 0.040）之间存在明显的QoL差异。在家长和儿童代理报告中，缓解组和复发组的情绪得分在 QoL 方面存在明显差异（分别为 p = 0.019 和 0.030）。每日类固醇剂量与学习生活质量以及家长代理报告总分之间存在明显的负相关（p = 0.025；r = -0.338）。结论家长和儿童的报告显示，NS儿科患者和健康儿童的学校生活质量得分存在显著差异。此外，还观察到缓解期和复发期NS儿科患者的情绪评分存在明显差异。在家长代理报告中，每日类固醇剂量与学校评分呈负相关。
{"title":"Quality of life assessment in pediatric nephrotic syndrome in North Sumatera Province: Parent-and-child proxy report","authors":"Ika Citra Dewi Tanjung, Dina Keumala Sari, O. R. Ramayani, M. Amin, B. Medise, M. Rusda, Masitha Dewi Sari, Nuraiza Meutia","doi":"10.3897/pharmacia.71.e128428","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e128428","url":null,"abstract":"Background: Nephrotic syndrome (NS) is a pediatric kidney disease with a high recurrence rate, impacting patient quality of life (QoL). This study aimed to assess the QoL of NS children in North Sumatera using a parent-and-child proxy report.\u0000 Methods: This was a cross-sectional study (February–December 2023) in the nephrology and growth and developmental outpatient ward, Pediatrics Department, Adam Malik Hospital, and Prof. Dr. Chairuddin P. Lubis Universitas Sumatera Utara Hospital, Medan, Indonesia. The inclusion criteria for cases were children aged 5–18 who met the diagnostic criteria of NS. Cases were age-matched with healthy children as controls. The PedsQL 4.0 generic core scale instrument was used for the QoL assessment. Normally distributed continuous data were expressed as the mean and standard deviation; categorical data were expressed as proportions. Differences between the groups were analyzed using an independent t-test, and the correlation of illness duration and daily steroid dose with QoL was determined using the Pearson correlation test.\u0000 Results: A total of 44 NS pediatric patients were age-matched with 44 healthy children. A significant difference in QoL existed between the school scores of the NS and healthy groups in the parent proxy report (p = 0.001) and between the school score and total score of the child proxy report (p = 0.003 and p = 0.040, respectively). A significant difference in QoL existed in emotional scores between the remission and relapse groups in the parent-and-child proxy reports (p = 0.019 and 0.030, respectively). A significant negative correlation existed between the daily steroid dose and QoL in school and the total score of the parent proxy report (p = 0.025; r = –0.338).\u0000 Conclusion: The parent and child reports revealed a significant difference in QoL between the school scores of NS pediatric patients and healthy children. A significant difference in the emotional scores of NS pediatric patients in remission and relapse was also observed. The daily steroid dose was negatively correlated with the school score in the parent proxy report.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141675874","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}
Pub Date : 2024-07-03DOI: 10.3897/pharmacia.71.e126246
Ana Marković, M. Atanasova, R. Buyukliev, A. Bakalova, A. Šmelcerović, E. Cherneva
Deoxyribonuclease I (DNase I) is one of the main nucleases involved in deoxyribonucleic acid (DNA) degradation during apoptosis. It catalyzes the hydrolytic cleavage of DNA, producing 5‘-oligonucleotides. The inhibition of DNase I may serve as an important mechanism for protecting DNA against premature degradation during cell damage. Fourteen hydantoin-containing compounds, including two newly synthesized and seven previously synthesized metal complexes, along with five previously synthesized hydantoin ligands, were evaluated in vitro for their inhibitory properties against bovine pancreatic DNase I. As a result, the 3’-methyl-4-thio-1H-tetrahydropyranspiro-5’-hydantoin platinum complex (8) inhibited the enzyme with an IC50 value of 110.20 ± 24.20 µM, a potency 3-fold greater than that of the reference crystal violet (IC50 = 378.27 ± 47.75 µM). To understand the binding mode and mechanism of inhibition of compound 8 with DNase I, molecular docking calculations were performed. The analysis revealed that compound 8 interacts with the most important catalytic residues of DNase I. To the best of our knowledge, this is the first report of a platinum complex inhibiting DNase I.
脱氧核糖核酸酶 I（DNase I）是参与细胞凋亡过程中脱氧核糖核酸（DNA）降解的主要核酸酶之一。它催化 DNA 的水解裂解，产生 5'-oligonucleotides 。抑制 DNase I 可能是保护 DNA 免受细胞损伤时过早降解的重要机制。研究人员在体外评估了 14 种含海因的化合物（包括两种新合成的金属复合物、七种以前合成的金属复合物以及五种以前合成的海因配体）对牛胰腺 DNase I 的抑制特性。结果发现，3'-甲基-4-硫代-1H-四氢吡喃螺-5'-海因铂络合物（8）对该酶的抑制作用 IC50 值为 110.20 ± 24.20 µM，比参照物结晶紫（IC50 = 378.27 ± 47.75 µM）高出 3 倍。为了了解化合物 8 与 DNase I 的结合模式和抑制机制，研究人员进行了分子对接计算。据我们所知，这是首次报道铂复合物对 DNase I 的抑制作用。
{"title":"3’-Methyl-4-thio-1H-tetrahydropyranspiro-5’-hydantoin platinum complex as a novel deoxyribonuclease I inhibitor","authors":"Ana Marković, M. Atanasova, R. Buyukliev, A. Bakalova, A. Šmelcerović, E. Cherneva","doi":"10.3897/pharmacia.71.e126246","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e126246","url":null,"abstract":"Deoxyribonuclease I (DNase I) is one of the main nucleases involved in deoxyribonucleic acid (DNA) degradation during apoptosis. It catalyzes the hydrolytic cleavage of DNA, producing 5‘-oligonucleotides. The inhibition of DNase I may serve as an important mechanism for protecting DNA against premature degradation during cell damage. Fourteen hydantoin-containing compounds, including two newly synthesized and seven previously synthesized metal complexes, along with five previously synthesized hydantoin ligands, were evaluated in vitro for their inhibitory properties against bovine pancreatic DNase I. As a result, the 3’-methyl-4-thio-1H-tetrahydropyranspiro-5’-hydantoin platinum complex (8) inhibited the enzyme with an IC50 value of 110.20 ± 24.20 µM, a potency 3-fold greater than that of the reference crystal violet (IC50 = 378.27 ± 47.75 µM). To understand the binding mode and mechanism of inhibition of compound 8 with DNase I, molecular docking calculations were performed. The analysis revealed that compound 8 interacts with the most important catalytic residues of DNase I. To the best of our knowledge, this is the first report of a platinum complex inhibiting DNase I.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141683195","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}
Pub Date : 2024-07-02DOI: 10.3897/pharmacia.71.e129379
Maria Dimitrova, Nezabravka Tsvetanova, Daniel Penchev, G. Petrova
Head and neck cancers (HNC) are one of the most severe types of cancer in Europe, accounting for almost 4.5% of all cancer types, according to GLOBOCAN. The incidence is geographically variable, with higher rates observed in Eastern and Southern Europe than in Northern and Western Europe. Proton and photon therapies are both available treatment approaches for head and neck cancer, as each has its own unique advantages, characteristics, and considerations. Proton therapy is the newest one and is considered safer among both. The current study aims to analyse the available data for patients with head and neck cancer treated with proton therapy in Bulgaria based on real-world data generated through AI-based patient registries and the current availability of strategic policy documents ensuring the affordability of proton therapy on a national level. We wanted to explore the feasibility of building a national proton therapy centre based on available patients’ information and strategic policy documents. We conducted a 3-year (2020–2022) combined non-interventional retrospective database study on head and neck cancer using secondary use of real-world data from dynamic patient registries and desktop analysis of strategic policy documents for capacity and financial affordability for proton therapy in Bulgaria. The results show that Bulgaria has a strategic policy document that focuses on the need and funding possibilities for establishing this treatment within the country. However, the country lacks the political will to ensure appropriate funding for it. Building a national proton centre is a feasible investment but needs additional detailed budget impact analysis.
{"title":"Proton therapy for head and neck cancer therapy: A real-world data case study from Bulgaria","authors":"Maria Dimitrova, Nezabravka Tsvetanova, Daniel Penchev, G. Petrova","doi":"10.3897/pharmacia.71.e129379","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e129379","url":null,"abstract":"Head and neck cancers (HNC) are one of the most severe types of cancer in Europe, accounting for almost 4.5% of all cancer types, according to GLOBOCAN. The incidence is geographically variable, with higher rates observed in Eastern and Southern Europe than in Northern and Western Europe. Proton and photon therapies are both available treatment approaches for head and neck cancer, as each has its own unique advantages, characteristics, and considerations. Proton therapy is the newest one and is considered safer among both. The current study aims to analyse the available data for patients with head and neck cancer treated with proton therapy in Bulgaria based on real-world data generated through AI-based patient registries and the current availability of strategic policy documents ensuring the affordability of proton therapy on a national level. We wanted to explore the feasibility of building a national proton therapy centre based on available patients’ information and strategic policy documents. We conducted a 3-year (2020–2022) combined non-interventional retrospective database study on head and neck cancer using secondary use of real-world data from dynamic patient registries and desktop analysis of strategic policy documents for capacity and financial affordability for proton therapy in Bulgaria. The results show that Bulgaria has a strategic policy document that focuses on the need and funding possibilities for establishing this treatment within the country. However, the country lacks the political will to ensure appropriate funding for it. Building a national proton centre is a feasible investment but needs additional detailed budget impact analysis.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141685750","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}
Pub Date : 2024-07-02DOI: 10.3897/pharmacia.71.e124050
Tho Do Chau Minh Vinh, Sil Nguyen Thanh, Ngan Nguyen Thanh, Tham Le Kim, Thi Huynh Huynh Anh, Giang Le Thi Truc, Mai Nguyen Thi Hong
Turmeric, extensively cultivated across Southeast Asia, especially in Vietnam, harbors active polyphenols, primarily curcumin (2–5%), renowned for its diverse health benefits. Pharmacopoeias recognize turmeric, yet it lacks standardized quality assessments and encounters challenges in extraction and identification due to natural variations and adulteration. This analytical method is vital for verifying the authenticity, purity, and quality of turmeric products in both the pharmaceutical and nutraceutical industries. This study successfully developed an efficient extraction process for curcumin (CUR), demethoxycurcumin (DMC), and bisdemethoxycurcumin (BDMC) from Curcuma longa L. rhizomes. The herbal powder was extracted with methanol (1:30, w/v) by the ultrasound-assisted method for 10 minutes, and this process was repeated three times. A high-performance liquid chromatography-diode array detector (HPLC-DAD) method was validated for the simultaneous quantification of three analytes, following the AOAC guideline and achieving a correlation coefficient (R2) value greater than 0.9950. Utilizing the HPLC-DAD method, the study developed a chemical fingerprint analysis for three analytes to identify the characteristic chemical components distinguishing turmeric from each region. Nineteen samples collected from various provinces across Vietnam were subjected to analysis. In all analyzed samples, the concentrations of CUR, DMC, and BDMC ranged from 0.77–10.30%, 0.33–6.92%, and 0.03–3.23%, respectively. CUR was determined to be the dominant compound in most samples, while BDMC consistently exhibited the lowest levels of content. Utilizing the findings derived from the analysis of RRT and RPA metrics, the research assessed variances across sample batches. It is suggested that this newly established approach can be applied to construct and develop raw material areas to serve the needs of each field.
{"title":"Chemical fingerprint analysis for quality assessment and control of Curcuma longa L. rhizomes from Vietnam using a high-performance liquid chromatography-diode array detector (HPLC-DAD)","authors":"Tho Do Chau Minh Vinh, Sil Nguyen Thanh, Ngan Nguyen Thanh, Tham Le Kim, Thi Huynh Huynh Anh, Giang Le Thi Truc, Mai Nguyen Thi Hong","doi":"10.3897/pharmacia.71.e124050","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e124050","url":null,"abstract":"Turmeric, extensively cultivated across Southeast Asia, especially in Vietnam, harbors active polyphenols, primarily curcumin (2–5%), renowned for its diverse health benefits. Pharmacopoeias recognize turmeric, yet it lacks standardized quality assessments and encounters challenges in extraction and identification due to natural variations and adulteration. This analytical method is vital for verifying the authenticity, purity, and quality of turmeric products in both the pharmaceutical and nutraceutical industries. This study successfully developed an efficient extraction process for curcumin (CUR), demethoxycurcumin (DMC), and bisdemethoxycurcumin (BDMC) from Curcuma longa L. rhizomes. The herbal powder was extracted with methanol (1:30, w/v) by the ultrasound-assisted method for 10 minutes, and this process was repeated three times. A high-performance liquid chromatography-diode array detector (HPLC-DAD) method was validated for the simultaneous quantification of three analytes, following the AOAC guideline and achieving a correlation coefficient (R2) value greater than 0.9950. Utilizing the HPLC-DAD method, the study developed a chemical fingerprint analysis for three analytes to identify the characteristic chemical components distinguishing turmeric from each region. Nineteen samples collected from various provinces across Vietnam were subjected to analysis. In all analyzed samples, the concentrations of CUR, DMC, and BDMC ranged from 0.77–10.30%, 0.33–6.92%, and 0.03–3.23%, respectively. CUR was determined to be the dominant compound in most samples, while BDMC consistently exhibited the lowest levels of content. Utilizing the findings derived from the analysis of RRT and RPA metrics, the research assessed variances across sample batches. It is suggested that this newly established approach can be applied to construct and develop raw material areas to serve the needs of each field.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141686426","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}
Pub Date : 2024-07-01DOI: 10.3897/pharmacia.71.e125879
Malak AlBathish, A. Gazy, Marwa Al Jamal, A. Bejjani
Levothyroxine sodium is a narrow therapeutic index drug used for the treatment of hypothyroidism. The medication is marketed in tablet form with very low doses ranging from 25 to 150 µg, which requires the development of a sensitive quantitative analytical method to ensure a safe and effective pharmacological response. In the present work, a Fourier transform infrared method has been developed and validated for levothyroxine sodium determination in various pharmaceutical formulations. The proposed method involves selectively extracting levothyroxine sodium from the studied tablets using chloroform as solvent, then depositing it on a KBr pellet, followed by infrared measurements and spectra analysis. The peak band area corresponding to the C=C centered at 1409 cm-1 has been chosen for the quantification. The method has been validated according to ICH guidelines and was found to be simple, precise, accurate, and specific. The linearity, detection, and quantitation limits are 25–800, 8.121, and 24.545 µg/pellet, respectively. These values confer the method’s sensitivity and applicability for the determination of different pharmaceutical tablets with various dosages. A statistical comparison with a reference HPLC method showed no significant difference. Accordingly, the developed method can be employed for quality control testing of levothyroxine sodium due to its simplicity and the absence of sophisticated instrumentation and procedures. Graphical abstract:
{"title":"Utilization of the FTIR spectroscopic method for the quantitative determination of the narrow therapeutic index levothyroxine sodium in pharmaceutical tablets","authors":"Malak AlBathish, A. Gazy, Marwa Al Jamal, A. Bejjani","doi":"10.3897/pharmacia.71.e125879","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e125879","url":null,"abstract":"Levothyroxine sodium is a narrow therapeutic index drug used for the treatment of hypothyroidism. The medication is marketed in tablet form with very low doses ranging from 25 to 150 µg, which requires the development of a sensitive quantitative analytical method to ensure a safe and effective pharmacological response. In the present work, a Fourier transform infrared method has been developed and validated for levothyroxine sodium determination in various pharmaceutical formulations. The proposed method involves selectively extracting levothyroxine sodium from the studied tablets using chloroform as solvent, then depositing it on a KBr pellet, followed by infrared measurements and spectra analysis. The peak band area corresponding to the C=C centered at 1409 cm-1 has been chosen for the quantification. The method has been validated according to ICH guidelines and was found to be simple, precise, accurate, and specific. The linearity, detection, and quantitation limits are 25–800, 8.121, and 24.545 µg/pellet, respectively. These values confer the method’s sensitivity and applicability for the determination of different pharmaceutical tablets with various dosages. A statistical comparison with a reference HPLC method showed no significant difference. Accordingly, the developed method can be employed for quality control testing of levothyroxine sodium due to its simplicity and the absence of sophisticated instrumentation and procedures.\u0000 Graphical abstract:\u0000 \u0000 \u0000","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141700578","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}
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