Pharmacia最新文献

{"title":"Creatine lysinate – part I: investigation of the toxicity and the influence on some biochemical parameters in mice","authors":"Ivanka Kostadinova, Nikolai Danchev, Boycho Landzhov, Lyubomir Marinov, Ivalina Ivanova, Dobrina Tsvetkova","doi":"10.3897/pharmacia.70.e109446","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e109446","url":null,"abstract":"In our study we investigated the acute toxicity of а newly synthesized creatine lysinate as well as its effect on the biochemical parameters in mice. Creatine lysinate exerts better solubility in water (3.3%) in comparison to creatine monohydrate (1.4%) at 20 °C and it is determined as a non-toxic after intraperitoneal (LD50 – 4543 mg/kg) and oral administration (LD50 > 8000 mg/kg). Oral administration of creatine lysinate at doses of 3 g/kg/day and 6 g/kg/day for 2 weeks reduced the creatine kinase levels, which indicates muscle protection. An increased levels of liver enzymes like alanine aminotransferase (ALAT) and aspartate aminotransferase (ASAT) was observed after the supplementation with creatine lysinate at both administered doses and the level of lactate was comparable both in the studied and the control group.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"27 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135388798","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":"In vitro antimitotic activity and in silico study of some 6-fluoro-triazolo-benzothiazole analogues","authors":"Naresh Podila, Mithun Rudrapal, Subramanyam Sibbala, Atul R. Bendale, Yanadaiah Palakurthi, Molakpogu Ravindra Babu, Kiran Manda, Renzon Daniel Cosme Pecho, Sreelatha Muddisett","doi":"10.3897/pharmacia.70.e109898","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e109898","url":null,"abstract":"In this work, nine 6-fluoro-triazolo-benzothiazole derivatives were prepared and evaluated for in vitro antimitotic activity. In addition, in silico study was also done using tubulin protein (PDB: 6QQN) by molecular docking method. Results revealed that TZ2 and TZ9 were the most active compounds with antimitotic action opposing the standard drug, aspirin. Results of molecular docking exhibited the inhibitory potential of triazolo-benzothiazole against tubulin protein. The mitotic study indicates the efficacy of triazolo-benzothiazole analogues in inhibiting the proliferation of cancer cells either by promoting microtubule formation or affecting microtubules, thereby preventing microtubule breakdown.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"6 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135388791","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 efficacy of hyaluronic acid in treating premature ejaculation: A systematic review and single-armed meta-analysis","authors":"Syah Mirsya Warli, Krisna Adhitya Wilantara Yusuf, Dhirajaya Dharma Kadar, Ginanda Putra Siregar, Fauriski Febrian Prapiska","doi":"10.3897/pharmacia.70.e111398","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111398","url":null,"abstract":"Aim : To evaluate the efficacy of hyaluronic acid (HA) injection in treating patients with premature ejaculation (PE). Methods : Matching interventional studies from MEDLINE, CENTRAL, and CINAHL. Outcomes were intravaginal estimated latency time (IELT), glandular circumference, satisfaction score, and adverse event rate. Data were assessed with Open Meta Analyst, DerSimonian and Laird random-effects model. Results : Ten interventional studies, three double-armed, with low to moderate bias risk, revealed significant differences in baseline IELT and 1, 3, and 6-month post-hyaluronic acid injection, with mean differences of 217.035 (95% CI, 89.330–344.739), 161.513 (95% CI, 37.262–285.764), and 196.350 (95% CI, 142.314–250.386) seconds. Glandular circumference increased by 10.956 mm (95% CI, 3.314–18.598) after six months. Conclusion : Hyaluronic acid successfully extended IELT in premature ejaculation patients at one, three, and six months post-treatment with no severe side effects. It also enhanced glandular size and sexual satisfaction for patients and their partners.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"28 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135425285","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":"Molecular docking analysis of ginger (Zingiber officinale) on dopamine compare to bupropion as smoking cessation","authors":"Rika Mayasari Alamsyah, Mieke Hemiawati Satari, Sondang Pintauli, Shelly Iskandar","doi":"10.3897/pharmacia.70.e111049","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111049","url":null,"abstract":"Tobacco use continues to be the leading cause of preventable death worldwide. Smoking is highly addictive because nicotine can stimulate nicotinic acetylcholinergic (nACh) receptors which release dopamine. Smoking cessation can be done with pharmacotherapy such as bupropion or varenicline, but it is associated with side effects. Herbal medicine is a possible easy option for smoking cessation treatment. This study uses ginger as a natural ingredient. Gingerol and shogaol were found to be the active compounds of ginger which are responsible for their pharmacological action and have been identified as TRPV1 agonists. The predictive binding of several forms of gingerol and shogaol to TRPV1 was analyzed using docking analysis in an in silico model. The method used is molecular docking with parameter observations and systematic literature review studies with dopamine as a comparator compound. The results of molecular docking of all herbal compound samples showed that no bioactive compounds had a lower binding energy value than the native ligands. However, all bioactive compounds from ginger show a binding energy value around -8,4 until -7.2 kkal/mol. Based on the molecular docking results, it can be concluded that the ginger herbal compounds have a better interaction potential than the control, although not as good as the native ligands. 12-Shogaol, 8-Shogaol, 12-Gingerol, 10-Shogaol, and 10-Gingerol are thought to target dopamine receptor proteins potentially.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"22 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136309139","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":"INNs granted with specific storage requirements in Bulgarian pharmacies. Part 2: Antineoplastic and immunomodulating agents","authors":"Evgeni Grigorov, Maya Radeva-Ilieva, Kaloyan D. Georgiev","doi":"10.3897/pharmacia.70.e110353","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e110353","url":null,"abstract":"There are drugs that require special storage in Bulgarian pharmacies as well as extra caution during the dispensing process. This is due to serious adverse reactions that may be even fatal. These medicines are included in Appendix № 9 to Art. 17, para. 1 of Ordinance № 28/9.12.2008, issued by the Minister of Health. The performed study of the anticancer drugs listed in the Appendix showed that a major part of these medicines that have a marketing authorization for use in Bulgaria are not included in the Appendix № 9. In addition, there are antitumor drugs that are listed in the appendix but are not authorized in Bulgaria to date. In conclusion, it is necessary to periodically update the drugs in Appendix № 9 as well as to develop clear and precise criteria for the inclusion of medicines in it.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"26 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136308133","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":"Vernonia amygdalina protects against doxorubicin-induced hepatic and renal damage in rats: mechanistic insights","authors":"Arya Tjipta Prananda, Aminah Dalimunthe, Urip Harahap, Rony Abdi Syahputra, Sony Eka Nugraha, Putri Cahaya Situmorang, Yee Teck Fah, Adrian Joshua Velaro, Besa Bilakaya, Muhammad Andika Yudha Harahap","doi":"10.3897/pharmacia.70.e112425","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e112425","url":null,"abstract":"The use of the chemotherapeutic agent doxorubicin is limited due to its potential to cause signifi-cant hepatorenal damage. The present study aimed to investigate the potential hepatoprotective and nephroprotective effects of Vernonia amygdalina , a medicinal plant with known antioxidant and anti-inflammatory properties, against doxorubicin-induced toxicity in rats. Male Wistar rats were randomly divided into four groups: Control, Doxorubicin (DOX), DOX + Vernonia Amyg-dalina (DOX+VA), and Vernonia amygdalina (VA) alone. DOX and DOX+VA groups were treated with a single intraperitoneal injection of doxorubicin (15 mg/kg body weight). The DOX+VA group received Vernonia amygdalina extract (100, 300, 500 mg/kg body weight) by oral gavage for 14 days following doxorubicin injection. The results demonstrated that Vernonia amygdalina significantly reduced the elevated levels of liver and kidney function biomarkers, alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), and creatinine, induced by doxorubicin. The histological examination of the liver and kidney tis-sues also confirmed the protective effects of Vernonia amygdalina against doxorubicin-induced damage. Furthermore, Vernonia amygdalina treatment was found to mitigate oxidative stress by restoring the levels of glutathione (GPx), Catalase, NO and SOD and decreasing the level of malondialdehyde (MDA) in liver and kidney tissues. Additionally, Vernonia amygdalina sig-nificantly suppressed the renal injury markers, NGAL, cystatin-c, KIM-1, and NAG. In conclu-sion, the results of this study suggest that Vernonia amygdalina has potent hepatoprotective and nephroprotective effects against doxorubicin-induced toxicity in rats. These protective effects are mediated by its antioxidant, and free radical scavenging properties. Further investigation is needed to determine the potential clinical relevance of Vernonia amygdalina in protecting against the hepatorenal damage induced by doxorubicin in human subjects. Graphical abstract :","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"98 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135014519","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":"Prevalence of potentially inappropriate medications among elderly patients with diabetes – study based on STOPP/START criteria","authors":"Petya Milushewa, Kristina Kosanova, Petar Nikolov","doi":"10.3897/pharmacia.70.e110386","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e110386","url":null,"abstract":"Objective : The prevalence of drug-related problems in elderly patients is a concerning issue that can lead to elevated morbidity, mortality, and health care resource utilisation. This study focuses on the significance of addressing diabetes in the context of an ageing population, where elderly individuals face higher risks of comorbidities and mortality. The main objective of this study was to assess potentially inappropriate medications (PIMs) and potential prescribing omissions (PPOs) among patients with diabetes in Bulgaria, using the explicit STOPP/START criteria, version 2. By evaluating the appropriateness of drug prescriptions in this specific patient population, this study aims to shed light on areas that require optimisation to enhance patient safety and treatment outcomes. Materials and methods : A national prospective questionnaire study was conducted in Bulgaria among patients aged over 65 years. The research was conducted in 25 randomly selected pharmacies. The study supports the use of the STOPP/START criteria based on the clinical information provided. A total of 133 patients with T1DM or T2DM participated in the study. The evaluation of potentially inappropriate medications (PIMs) and potential prescribing omissions (PPOs) was performed in 131 patients. sStatistical differences in demographics and medication numbers between patients with and without PIMs or PPOs were assessed using a Chi-square test, with a p-value of ≤ 0.05 considered statistically significant. Results : The pharmacotherapy of 131 patients with diabetes was assessed, and it was found that 57% of them had polypharmacy. Among the study population, 90 PIMs were identified, indicating that 66% of the patients had inappropriate prescribing. Notably, inappropriate prescribing concerning diabetes was associated with the use of long-acting sulfonylureas (n=10) and beta-blockers (n=13). Applying the START criteria revealed 67 PPOs among 67 patients, representing a prevalence of 50% in the study population. However, no PPOs were detected in the context of diabetes pharmacotherapy. Furthermore, a significant relationship was observed between the number of medications and PIMs, as evidenced by the chi-square test result with a p-value close to zero, indicating statistical significance. Conclusion : The study revealed a high prevalence of PIMs in elderly patients with diabetes in Bulgaria. Endocrine disorders contribute to 26% of PIMs. As Bulgaria’s ageing population faces increasing diabetes challenges, effective management strategies are crucial. These findings underscore the significance of addressing prescribing practises to enhance disease control and prevent complications.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"20 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135014288","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":"Cost-effectiveness of treatment intervention in prediabetic patients in Bulgaria","authors":"Stanislava Yordanova, Konstantin Mitov, Maria Kamusheva","doi":"10.3897/pharmacia.70.e110104","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e110104","url":null,"abstract":"Introduction : The study aims to evaluate the cost-effectiveness (CE) of an early intervention in prediabetes (metformin) in order to prevent or slow down the onset of diabetes in those at high risk compared with the current “do nothing” approach. Materials and methods : An Excel-based model was developed. The results of the CE and cost-utility analyses are presented as an ICER (incremental cost-effectiveness ratio) and ICUR (incremental cost-utility ratio), respectively. Markov model of the cost or potential savings from the perspective of the National Health Insurance Fund in Bulgaria was performed. Results : The ICER of the metformin intervention in prediabetes patients compared with “do nothing” routine shows that metformin treatment produced more health benefits (number of prevented diabetes cases) on a lower cost for the public payer. The ICER calculated is -7,122.32 BGN per number of prevented diabetes cases and it confirms cost-savings are possible when metformin is applied compared with the “do nothing” approach. The ICUR per quality-adjusted life years (QALYs) gained also shows the metformin preventive intervention as a dominant and cost-saving alternative. The Markov model simulation confirms the intervention with metformin is less costly in a long-term and leads to higher QALYs. Conclusion : The investment in a preventive intervention with metformin offers an excellent value for money. The ICER of the metformin intervention in prediabetes patients compared with “do nothing” routine shows that metformin preventive intervention produced more health benefits on a lower cost for the public payer in Bulgaria.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"30 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135014546","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":"Antiproliferative activity of ruthenium complex II against human cancer cell in vitro","authors":"Mohamed Saadh","doi":"10.3897/pharmacia.70.e111410","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111410","url":null,"abstract":"Despite significant advancements in cancer treatment, there is a constant need for new and effective therapeutic options. One such potential weapon in the fight against cancer is ruthenium complex II. In this article, we synthesized, characterized, and studied the activity of dithiocyanato-N-bis[8-(diphenylphosphino)quinoline]ruthenium (II) [Ru(N-P)2(NCS)2] against MCF-7 human adenocarcinoma cells and the MRC-5 cell lines from fetal lung fibroblast-like cells as normal cells, as well as the mechanisms of action and selectivity. This study demonstrated that [Ru(N-P) 2 (NCS) 2 ] has cytotoxic activity against MCF-7 with IC 50 values of 7.56 µg/ml and cytotoxic activity against MRC-5 cell lines with IC 50 values of 576.6 µg/ml. [Ru(N-P) 2 (NCS) 2 ] showed more selective cytotoxic activity against MCF-7 cancer cell lines than MRC-5 normal cell lines. . This study demonstrated the potent apoptotic activity of ruthenium complex II by determining the activation of caspase-3, highlighting its potential as a therapeutic agent in cancer treatment. The [Ru(N-P) 2 (NCS) 2 ] is considered promising for researchers investigating putative biological activities, particularly antitumor and immune-related activity.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"9 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135154103","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":"Anticancer and antiproliferative activity of ruthenium complex (II) bearing 3,3’-dicarboxy-2,2’-bipyridine ligand","authors":"Mohamed Saadh","doi":"10.3897/pharmacia.70.e111508","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111508","url":null,"abstract":"Even though significant progress has been made in cancer treatment, there is always room for improvement. The experimental drug Ruthenium Complex II shows promise as a cancer treatment. In this article, the dichloro-3,3’-dicarboxy-2,2’-bipyridyl bis(dimethylsulphoxide)ruthenium(II) [RuCl 2 (3,3’-dcbpy)(DMSO) 2 ], have been synthesized, characterized, and studied for its anticancer activity against MDA-MB-231 and MRC-5 cell lines, as well as its mechanisms of action and selectivity. According to research, [RuCl 2 (3,3’-dcbpy)(DMSO) 2 ], is highly cytotoxic to the MDA-MB-231 and minimum cytotoxic to MRC-5 cell lines, with IC 50 values of 5.95 and 579.6 μg/ml, respectively. Ruthenium Complex II is exceptionally effective at destroying cancer cells while causing minimal harm to healthy cells. RuCl 2 (3,3’-dcbpy)(DMSO) 2 ] caused apoptosis, which was confirmed by the activation of caspase-3. Ruthenium complexes hold great promise as powerful anticancer agents. Their unique mechanisms of action, ability to selectively target cancer cells, and versatility in chemical structure make them attractive candidates for the development of targeted therapies.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"29 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135153943","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}