Pharmacia最新文献

{"title":"Influence of experimental heart failure therapy with different generations of β-adrenergic blockers on Cardiac Electrical Activity (ECG) and Autonomic Regulation of Heart Rhythm (ARHR)","authors":"Olexiy Goncharov, Igor Belenichev, Andrii Abramov, Olena Popazova, Liudmyla Kucherenko, Nina Bukhtiyarova, Ivan Pavliuk","doi":"10.3897/pharmacia.70.e110924","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e110924","url":null,"abstract":"Abstract : In the complex treatment of chronic heart failure (CHF) β-adrenoblockers (carvedilol, nebivolol, bisoprolol, metoprolol) are used, which due to their pharmacological properties increase the survival rate of patients, improve cardio- and haemodynamic parameters, metabolism. However, modern realities in medicine require creation of new more effective and safe β-adrenoblockers. In this regard, the potential drug Hypertirl is of interest. The aim was to evaluate the cardioprotective effect of 1-(b-phenylethyl)-4-amino-1,2,4-triazolium bromide (Hypertril) on cardiac electrical activity and autonomic regulation of heart rhythm in a model of CHF in comparison with β-adrenoblockers of different generations (Nebivolol, Carvedilol, Bisoprolol, Metoprolol). Materials and methods : Chronic heart failure was induced by 14-day administration of doxorubicin in a cumulative dose of 15 mg/kg to white mongrel rats weighing 190–220g (total 85). The investigated drugs were administered after doxorubicin course for 30 days: Hypertril at an experimentally substantiated dose of 3.5 mg/kg, Metoprolol succinate 15 mg/kg, Nebivolol 10 mg/kg, Carvedilol 50 mg/kg, Bisoprolol 10 mg/kg. At the end of drug administration under thiopental anaesthesia (40 mg/kg), electrocardiogram (ECG) and autonomic regulation of heart rhythm (ARHR) were analysed using a computer analyser CardioCom-2000plus (KAI-Medica, Ukraine). The results of the study were calculated using a standard statistical package “STATISTICA for Windows 6.0” (StatSoftInc., №AXXR712D833214FAN5), “SPSS 16.0” and “Microsoft Office Excell 2003”. Results and discussion : Hypertril administration resulted in a negative chronotropic effect, normalisation of atrial (P) and ventricular (R) spike amplitude, ST segment inversion below isoline, increased amplitude of ventricular myocardial repolarisation T. Myocardial repolarisation spike were observed, as well as normalised the duration of atrial (P) and ventricular depolarisation phase (QRS complex) to the intact value and restored the duration of electrical diastole (TR interval). Hypertril reduced systolic and diastolic myocardial dysfunction in animals with CHF. Hypertril restored autonomic mechanisms of heart rhythm regulation and balanced activity of sympathetic and parasympathetic parts of autonomic nervous system in the control of cardiac function. Conclusion : The obtained results demonstrated the undoubted advantage of the new original molecule (Hypertril) over basic β-adrenoblockers (Metoprolol, Nebivolol, Carvedilol and Bisoprolol) and experimentally justify further in-depth study to create on its basis a drug for the treatment of CHF.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"124 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135779196","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}

{"title":" De novo design of pimarane diterpenoid compounds as potential alternatives to sarecycline for acne vulgaris treatment","authors":"Adeola Tawakalitu Kola-Mustapha","doi":"10.3897/pharmacia.70.e113065","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e113065","url":null,"abstract":"Acne vulgaris is a prevalent skin disorder that affects both adolescents and adults and has a major psychological impact. Antibiotic resistance is one issue that current therapies, including antibiotics, must address. A viable approach is to target Cutibacterium acnes , a crucial bacterium in the development of acne. An antibiotic of the tetracycline class called sarecycline shows efficacy despite resistance and adverse effect issues. The purpose of this study is to develop, assess, and compare the efficacy of Sandracopimar (Pimarane diterpenoids) compounds and Sarecycline in the treatment of acne by targeting the 30S ribosomal subunit of Cutibacterium acnes . Sarecycline’s binding affinity and PheSA score were assessed at the 30S ribosomal subunit binding site of Cutibacterium acnes . There were distinct interactions between Sarecycline and the ribosomal subunit, including hydrophobic and hydrogen bonding. Sarecycline demonstrated a strong binding affinity (-8.2 kcal/mol) and a PheSA score of 0.53184 within the Cutibacterium acnes 30S ribosomal subunit binding site. Sandaracopimar-15-ene-6.beta.,8.beta.-diol exhibited a binding affinity of -7.3 kcal/mol and PheSA score of 0.37252. Compound 1, a novel compound derived from Sandaracopimar-15-ene-6.beta.,8.beta.-diol, showed a slightly higher binding affinity (-8.3 kcal/mol) than Sarecycline. The molecular dynamics simulation results reveal that Compound 1 exhibited stability during a specific phase, indicating favorable binding potential with the Cutibacterium acnes 30S ribosomal subunit drug target. The compound demonstrated structural flexibility, advantageous for molecular interactions. The study indicates that Sandracopimar-derived compounds, including Compound 1, show comparable parameters to Sarecycline, suggesting similar activity in targeting the Cutibacterium acnes 30S ribosomal subunit. These compounds may serve as a potential source of novel anti-acne compounds.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"42 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135778850","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}

{"title":"Co-occurrence of lung adenocarcinoma and pulmonary fibrosis in a patient: A comprehensive case study and review of existing literature on the successful utilization of nintedanib","authors":"Tanya Zlatanova, Jeliazko Arabadjiev","doi":"10.3897/pharmacia.70.e111820","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111820","url":null,"abstract":"Both lung carcinoma and idiopathic pulmonary fibrosis (IPF) have an adverse prognosis, and the co-existence of both diseases is not uncommon. We introduce a clinical case involving a patient diagnosed with concurrent occurrences of lung adenocarcinoma and IPF. The patient underwent a therapeutic regimen comprising the administration of docetaxel in conjunction with nintedanib. This treatment approach was followed by the sustained utilization of maintenance nintedanib over an extended duration, leading to substantial enhancements in the patient’s quality of life. Furthermore, we discuss the few therapeutic options concerning this clinical challenge and possible future therapeutic options.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"38 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135918836","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}

{"title":"A current insight and future perspective of edible bird nest as caviar of the east","authors":"Muhammad Andika Haraharap, Osfar Sjofjan, Lilik Eka Radiati, Muhammad Halim Natsir, Rony Abdi Syahputra, Fahrul Nurkolis","doi":"10.3897/pharmacia.70.e112494","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e112494","url":null,"abstract":"Edible bird’s nest (EBN) is a highly valuable food product obtained from swiftlet nests, primarily those of the Aerodramus genus. Due to its purported health benefits and exceptional taste, EBN is often referred to as the “caviar of the East.” This abstract presents a comprehensive review of the current state of EBN research, focusing on its chemical composition, nutritional value, pharmacological effects, and safety considerations. The chemical composition of EBN is intricate and influenced by various factors, including bird species, geographic origin, nest collection time, and processing methods. It is primarily composed of proteins, polysaccharides, minerals, lipids, and a wide range of bioactive compounds such as sialic acid, amino acids, and antioxidants. Additionally, EBN has demonstrated antioxidant, anti-inflammatory, anti-tumor, and anti-aging properties attributed to these bioactive constituents. While EBN is generally considered safe for human consumption, it is essential to address concerns related to potential contaminants like heavy metals, microbial pathogens, and allergens. This review offers a comprehensive overview of previous research conducted on residual impurities that may be present in edible bird’s nests (EBNs). The review encompasses various aspects, including, the regulatory framework and associated concerns regarding EBNs, the levels of nitrite and nitrate detected in EBNs, the presence of bacteria, fungi, and mites in EBNs, the identification of allergenic substances in EBNs, and the presence of heavy metals and excessive mineral content at different stages of EBN processing, including raw uncleaned (RUC) EBNs, raw cleaned (RC) EBNs, and EBNs after undergoing treatment. Graphical abstract :","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"46 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135918529","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}

{"title":"Synthesis and antitumor activity of 1,3,4-oxadiazole substituted 2-(5-ylidene-2,4-dioxothiazolidin-3-yl)-acetamides","authors":"Maryan Lelyukh, Myroslava Kalytovska, Marta Zastryzhna, Arkadii Savchenko, Ihor Chaban, Stefan Harkov","doi":"10.3897/pharmacia.70.e102449","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e102449","url":null,"abstract":"A series of novel 1,3,4-oxadiazole substituted 2-(5-aryl/heterylidene-2,4-dioxothiazolidine-3-ylidene)-acetamides and their 5-unsubstituted analogues have been synthesized following N -alkylation reaction of 2-chloro- N -(5-aryl-[1,3,4]oxadiazol-2-yl)-acetamides with thiazolidinedione and potassium salts of its arylidene derivatives. The structures of target compounds were confirmed by using 1H NMR spectroscopy and elemental analysis. Evaluation of anticancer activity in vitro for the synthesized compounds was performed in accordance with the National Cancer Institute protocol. A selective influence of some tested compounds against leukaemia MOLT-4 ( 3e , GP = 76.85%) and K-562 ( 3e , GP = 79.84%), colon cancer HCT-15 ( 3d , GP = 76.86%), renal cancer A498 ( 4a , GP = 74.37%), CAKI-1 ( 3d , GP = 68.49%) and UO-31 ( 3b-e, 4a-b , GP = 66.67 ÷ 86.30%) cell lines was established. Grafical abstract :","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"16 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135963287","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}

{"title":"Chronic toxicity assessment of nano-formulated Bischofia javanica leaves: Implications for pharmacological use","authors":"Cheryl Grace Pratiwi Rumahorbo, Syafruddin Ilyas, Salomo Hutahaean, Cut Fatimah Zuhra, Putri Cahaya Situmorang","doi":"10.3897/pharmacia.70.e110640","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e110640","url":null,"abstract":"This study explores the chronic toxicity of nano-formulated Bischofia javanica leaves, a plant with pharmacological significance in Indonesia, following OECD guidelines 452. Graded doses (2, 4, 6, and 8 g/kg BW) of nano-formulated Bischofia javanica were administered to the treatment groups for 60 days, while the control group (K-) received only water. On the 61 st day, the mice were euthanized, and samples for biochemical, hematological, and histopathological analysis were collected. Statistical analysis involved one-way ANOVA and Tukey’s post hoc tests. Graded doses of nano-formulated Bischofia javanica leaves caused significant alterations in liver function. Doses between 2 and 4 g/kg BW improved liver histology and physiological markers. Higher doses (6 to 8 g/kg BW) led to liver dysfunction and histological degeneration, characterized by substantial fatty alterations, intracellular fat accumulation in hepatocytes, and compromised central blood vessels and sinusoids. The lungs showed signs of alveolar inflammation, epithelial exfoliation, debris, and the accumulation of inflammatory cells in alveolar spaces. Lower doses showed uniformly distributed cardiac blood vessels, while higher doses resulted in heart hemorrhages and amorphous exudates. Except for high doses, which significantly elevated specific liver damage indicators, no other levels of Bischofia javanica caused treatment-related mortality or significant alterations in hematological and biochemical parameters. Blood sugar levels remained stable across the dose range. In conclusion, moderate doses of nano-formulated Bischofia javanica leaf extracts can enhance physiological functions positively. However, caution is necessary when contemplating high doses, as they can cause dysfunction or damage vital organ systems.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"37 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135969951","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}

{"title":"Monitoring the change in the quality of life of patients with post-COVID syndrome by influence on their functional status","authors":"Maria Stamova Vakrilova Becheva, Angelina Georgieva Kirkova-Bogdanova, Petar Jordanov Atanasov, Mariya Sevdelinova Chaneva, Daniela Ivova Taneva, Stefka Achkova Ivanova","doi":"10.3897/pharmacia.70.e113061","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e113061","url":null,"abstract":"Coronavirus disease 2019 (COVID-19) is still a major medical concern. Patients who have recovered from the infection from COVID-19 face the ordeal of post-covid syndrome. In these patients, there is a decrease in physical abilities, in particular musculoskeletal complications and post-traumatic stress, depression and chronic fatigue, which impair their quality of life. This necessitates long-term rehabilitation, which supports recovery after hospitalization. Treatment through movement is part of the rehabilitation measures contributing to the functional recovery of patients with post-covid syndrome. To study how the functional capabilities of these patients improve and how their quality of life is affected, we created a set of physical exercises to be performed at home for 6 months. At baseline and at the end of the study, patients completed the SF-36 quality of life questionnaire. The aim of the study was to track the changes in the quality of life of patients with post-covid syndrome by influencing their functional state. Our study found a decline in the quality of life of the examined patients. After the application of the kinesitherapy program, the functional status of the patients improved, their functional independence was optimized, which contributed to the improvement of the quality of life of the post-covid patients syndrome.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"48 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136013188","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}

{"title":"Weight management strategies and food supplement intake among Bulgarian adults: results of a national survey","authors":"Radiana Staynova, Vesselina Yanachkova","doi":"10.3897/pharmacia.70.e109835","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e109835","url":null,"abstract":"The number of overweight and obese people has dramatically risen in the last two decades and has become one of the most serious health concerns. This study aimed to assess the use of food supplements as aids in reducing body weight and different approaches for weight management practised by Bulgarian adults. A cross-sectional, questionnaire-based online survey was conducted between December 2019 and February 2020. A total of 508 adults completed the survey. According to study participants, the Internet was the most used source of weight reduction information (66.9%). One hundred and seventy-two adults (33.9%) have sought weight-loss advice from a personal trainer/fitness instructor, and only 12.6% (n = 64) have consulted with a physician. More than half of the respondents (n = 288, 56.7%) reported food supplement use to maintain weight. The majority of the consumers were female (76.4%, p < 0.001) and adults with higher education (89.9%, p < 0.001). The main reasons for food supplement intake were individual research on the Internet (43%), advice from a personal trainer/fitness instructor (23.6%), and a recommendation from a healthcare provider (22.2%). With the increasing rates of overweight and obesity, food supplements are becoming a popular weight-loss approach, which is confirmed by our findings.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"14 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136013355","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}

{"title":"The most promising Southeastern European Tanacetum species: a review of chemical composition and biological studies","authors":"Reneta Gevrenova, Vessela Balabanova, Dimitrina Zheleva-Dimitrova, Georgi Momekov","doi":"10.3897/pharmacia.70.e110748","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e110748","url":null,"abstract":"Several species of the genus Tanacetum L. (Asteraceae) spread in the Southestern Europe are traditionally used as medicinal and aromatic plants, including T. vulgare , T. parthenium , T. macrophyllum , T. balsamita , T. poteriifolium . The review is focused on the phytochemical and pharmacological studies of these taxa. Major chemical constituents are acylquinic acids, sesquiterpenes, sesquiterpene lactones, methoxylated flavonoids. An in-depth depiction of more than 100 secondary metabolites was achieved in Tanacetum species by liquid chromatography-high resolution mass spectrometry. The ethnopharmacological studies indicate that species possess antioxidant, enzyme inhibitory and cytotoxic activity along with antimicrobial and antiviral effects. Reports revealed anti-inflamatory and neuromodulatory activity involved in the pharmacological approach in counteracting migraine attacks. Multivariate data analysis allowed the identification of the most discriminant metabolites and bioactivities in the herbal drugs. This review emphasizes T. vulgare , T. macrophyllum , T. balsamita and T. parthenium as potential raw material for health-promoting application in pharmaceutical area.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"43 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136098165","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}

{"title":"The era of digital pharmacy. 3D printing - realities and perspectives","authors":"Milen Dimitrov, Dilyana Georgieva, Sofiya Ilieva, Valentina Petkova","doi":"10.3897/pharmacia.70.e111731","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111731","url":null,"abstract":"3D printing is an innovative technology for building three-dimensional objects by laying down successive layers of material under the control of a computer software. It is entering pharmacy mainly because of its revolutionary potential to provide individualized dosage forms that meet the needs of each patient, due to the possibility to produce objects of many different sizes and shapes. An important aspect of personalized 3D tablets is the possibility to include several active substances in one dosage form, which would reduce the daily number of medications and the frequency of their administration and improve patient compliance. Another advantage of 3D printing is the possibility of producing small batches or even individual drugs for each patient. Despite the many advantages, 3D printing has several technological challenges to overcome before it becomes widely applicable in pharmacy. Five basic technologies are currently applied in pharmaceutical practice: powder-based printing, selective laser sintering, stereolithography, extrusion moulding printing, and electrohydrodynamic 3D printing. This article reviewed development, research focus, and prospects of each technology respectively.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"25 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136062447","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}