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Creatine lysinate – part I: investigation of the toxicity and the influence on some biochemical parameters in mice 赖氨酸肌酸酯-第一部分:毒性及对小鼠某些生化指标影响的研究
Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-28 DOI: 10.3897/pharmacia.70.e109446
Ivanka Kostadinova, Nikolai Danchev, Boycho Landzhov, Lyubomir Marinov, Ivalina Ivanova, Dobrina Tsvetkova
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.
本实验研究了新合成的溶肌酸酯对小鼠的急性毒性及其对小鼠生化指标的影响。在20°C时,与一水肌酸(1.4%)相比,赖氨酸肌酸在水中的溶解度(3.3%)更好,经腹腔注射(LD50 - 4543 mg/kg)和口服(LD50 >8000毫克/公斤)。口服溶肌酸3 g/kg/天和6 g/kg/天,持续2周,可降低肌酸激酶水平,表明肌肉有保护作用。在补充两种给药剂量的赖氨酸肌酸后,观察到肝酶如丙氨酸转氨酶(ALAT)和天冬氨酸转氨酶(ASAT)水平升高,乳酸水平在研究组和对照组中都是相当的。
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引用次数: 0
In vitro antimitotic activity and in silico study of some 6-fluoro-triazolo-benzothiazole analogues In一些6-氟三唑-苯并噻唑类似物的体外抗有丝分裂活性和硅研究
Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-28 DOI: 10.3897/pharmacia.70.e109898
Naresh Podila, Mithun Rudrapal, Subramanyam Sibbala, Atul R. Bendale, Yanadaiah Palakurthi, Molakpogu Ravindra Babu, Kiran Manda, Renzon Daniel Cosme Pecho, Sreelatha Muddisett
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.
本文制备了9个6-氟三唑-苯并噻唑衍生物,并对其体外抗有丝分裂活性进行了评价。此外,还利用分子对接法对微管蛋白(PDB: 6QQN)进行了硅片上的研究。结果表明,TZ2和TZ9是抗有丝分裂活性最强的化合物,对标准药物阿司匹林具有抗有丝分裂作用。分子对接结果显示了三唑-苯并噻唑对微管蛋白的抑制潜力。有丝分裂研究表明,三唑-苯并噻唑类似物通过促进微管形成或影响微管抑制癌细胞增殖,从而防止微管破裂。
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引用次数: 0
The efficacy of hyaluronic acid in treating premature ejaculation: A systematic review and single-armed meta-analysis The透明质酸治疗早泄的疗效:系统回顾和单臂荟萃分析
Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-28 DOI: 10.3897/pharmacia.70.e111398
Syah Mirsya Warli, Krisna Adhitya Wilantara Yusuf, Dhirajaya Dharma Kadar, Ginanda Putra Siregar, Fauriski Febrian Prapiska
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.
目的:评价透明质酸(HA)注射液治疗早泄(PE)的疗效。方法:对照来自MEDLINE、CENTRAL和CINAHL的介入性研究。结果是阴道内估计潜伏期(雅思)、腺体周长、满意度评分和不良事件发生率。采用Open Meta Analyst、DerSimonian和Laird随机效应模型对数据进行评估。结果:10项介入研究,3项双臂研究,低至中等偏倚风险,显示透明质酸注射后1、3和6个月的基线雅思成绩有显著差异,平均差异为217.035 (95% CI, 89.330-344.739)、161.513 (95% CI, 37.262-285.764)和196.350 (95% CI, 142.314-250.386)秒。6个月后腺体周长增加10.956 mm (95% CI, 3.314-18.598)。结论:透明质酸成功地延长了早泄患者治疗后1个月、3个月和6个月的雅思成绩,没有严重的副作用。它还能提高患者及其伴侣的腺体大小和性满意度。
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引用次数: 0
Molecular docking analysis of ginger (Zingiber officinale) on dopamine compare to bupropion as smoking cessation Molecular生姜(Zingiber officinale)对多巴胺的对接分析与安非他酮戒烟效果的比较
Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-20 DOI: 10.3897/pharmacia.70.e111049
Rika Mayasari Alamsyah, Mieke Hemiawati Satari, Sondang Pintauli, Shelly Iskandar
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.
烟草使用仍然是全世界可预防死亡的主要原因。吸烟很容易上瘾,因为尼古丁会刺激尼古丁乙酰胆碱能(nACh)受体,从而释放多巴胺。戒烟可以通过安非他酮或伐尼克兰等药物治疗来完成,但这与副作用有关。草药是戒烟治疗的一个可能简单的选择。这项研究使用生姜作为天然成分。姜辣素和姜酚是生姜中具有药理作用的活性化合物,已被确定为TRPV1激动剂。在一个硅模型中使用对接分析分析了几种形式的姜辣素和姜辣素与TRPV1的预测结合。采用以多巴胺为比较物进行参数观察和系统文献综述研究的分子对接方法。所有草药化合物样品的分子对接结果表明,没有任何生物活性化合物的结合能值低于天然配体。而姜中所有生物活性化合物的结合能值均在-8,4 ~ -7.2 kkal/mol之间。根据分子对接结果,可以得出结论,生姜中草药化合物具有比对照更好的相互作用电位,尽管不如天然配体好。12-Shogaol, 8-Shogaol, 12-Gingerol, 10-Shogaol和10-Gingerol被认为是潜在的多巴胺受体蛋白靶点。
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引用次数: 0
INNs granted with specific storage requirements in Bulgarian pharmacies. Part 2: Antineoplastic and immunomodulating agents INNs获准在保加利亚药房有特定的储存要求。第2部分:抗肿瘤和免疫调节剂
Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-20 DOI: 10.3897/pharmacia.70.e110353
Evgeni Grigorov, Maya Radeva-Ilieva, Kaloyan D. Georgiev
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.
有些药物需要在保加利亚药店特殊储存,并且在配药过程中要格外小心。这是由于严重的不良反应,甚至可能致命。这些药物包含在第17条第9段的附录中。卫生部发布的2008年12月9日第28/ 9.12.1号法令。对附录中列出的抗癌药物进行的研究表明,这些在保加利亚获得上市许可的药物的主要部分未包括在附录№9中。此外,还有附录中列出的抗肿瘤药物,但迄今为止尚未在保加利亚获得批准。总之,有必要定期更新附录№9中的药物,并制定明确和准确的标准,将药物纳入其中。
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引用次数: 0
Vernonia amygdalina protects against doxorubicin-induced hepatic and renal damage in rats: mechanistic insights Vernonia杏仁核保护大鼠免受阿霉素诱导的肝脏和肾脏损伤:机制见解
Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-19 DOI: 10.3897/pharmacia.70.e112425
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
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 :
化疗药物阿霉素的使用受到限制,因为它有可能引起严重的肝肾损害。摘要本研究旨在探讨具有抗氧化和抗炎作用的药用植物苦杏仁桃对阿霉素所致大鼠肝和肾的潜在保护作用。雄性Wistar大鼠随机分为对照组、阿霉素(DOX)组、阿霉素+苦杏仁糖(DOX+VA)组和单独使用苦杏仁糖(VA)组。DOX组和DOX+VA组均单次腹腔注射阿霉素(15mg /kg体重)。DOX+VA组小鼠在注射阿霉素后灌胃苦杏仁提取物(100、300、500 mg/kg体重)14 d。结果表明,苦杏仁果能显著降低阿霉素引起的肝肾功能生物标志物、谷丙转氨酶(ALT)、天冬氨酸转氨酶(AST)、碱性磷酸酶(ALP)和肌酐水平升高。肝脏和肾脏组织的组织学检查也证实了苦杏仁对阿霉素引起的损伤的保护作用。此外,通过恢复肝脏和肾脏组织中谷胱甘肽(GPx)、过氧化氢酶(过氧化氢酶)、NO和SOD水平以及降低丙二醛(MDA)水平,扁桃苦苷处理可以减轻氧化应激。此外,苦杏仁果显著抑制肾损伤标志物NGAL、胱抑素c、KIM-1和NAG。综上所述,苦杏仁对阿霉素引起的大鼠毒性具有较强的肝保护和肾保护作用。这些保护作用是由其抗氧化和自由基清除特性介导的。还需要进一步的研究来确定扁桃果在保护人类受试者免受阿霉素引起的肝肾损害方面的潜在临床意义。图形摘要:
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引用次数: 0
Prevalence of potentially inappropriate medications among elderly patients with diabetes – study based on STOPP/START criteria Prevalence老年糖尿病患者可能不适当的药物治疗-基于STOPP/START标准的研究
Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-19 DOI: 10.3897/pharmacia.70.e110386
Petya Milushewa, Kristina Kosanova, Petar Nikolov
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.
目的:老年患者中药物相关问题的流行是一个令人关注的问题,可导致发病率、死亡率升高和卫生保健资源的利用。本研究的重点是在人口老龄化的背景下解决糖尿病的重要性,老年人面临着更高的合并症和死亡率风险。本研究的主要目的是评估保加利亚糖尿病患者中潜在的不适当药物(PIMs)和潜在的处方遗漏(PPOs),使用明确的STOPP/START标准,版本2。通过评估药物处方在这一特定患者群体中的适当性,本研究旨在阐明需要优化的领域,以提高患者安全性和治疗效果。材料和方法:在保加利亚对65岁以上的患者进行了一项全国前瞻性问卷调查研究。这项研究是在25家随机选择的药店进行的。根据提供的临床信息,本研究支持使用STOPP/START标准。共有133名T1DM或T2DM患者参与了这项研究。对131例患者进行了潜在不适当药物(PIMs)和潜在处方遗漏(PPOs)的评估。采用卡方检验评估有无pim或PPOs患者的人口统计学和用药数量的统计学差异,p值≤0.05认为有统计学意义。结果:对131例糖尿病患者的药物治疗进行评估,发现57%的患者有多重用药。在研究人群中,确定了90个pim,表明66%的患者处方不当。值得注意的是,与糖尿病相关的不当处方与长效磺脲类药物(n=10)和β受体阻滞剂(n=13)的使用有关。应用START标准,67例患者中有67例PPOs,在研究人群中患病率为50%。然而,在糖尿病药物治疗的背景下,没有发现PPOs。用药次数与pim之间存在显著关系,卡方检验结果p值接近于零,具有统计学意义。结论:该研究揭示了保加利亚老年糖尿病患者中pim的高患病率。内分泌失调占pim的26%。由于保加利亚的老龄化人口面临越来越多的糖尿病挑战,有效的管理策略至关重要。这些发现强调了解决处方实践以加强疾病控制和预防并发症的重要性。
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引用次数: 0
Cost-effectiveness of treatment intervention in prediabetic patients in Bulgaria Cost-effectiveness对保加利亚糖尿病前期患者的治疗干预
Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-19 DOI: 10.3897/pharmacia.70.e110104
Stanislava Yordanova, Konstantin Mitov, Maria Kamusheva
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.
前言:本研究旨在评估早期干预糖尿病前期(二甲双胍)的成本效益(CE),以预防或减缓糖尿病高危人群的发病,与目前“什么都不做”的方法相比。材料与方法:建立基于excel的模型。CE和成本-效用分析的结果分别以ICER(增量成本-效用比)和ICUR(增量成本-效用比)表示。从保加利亚国家健康保险基金的角度对成本或潜在节约进行了马尔科夫模型分析。结果:与“什么都不做”的常规治疗相比,二甲双胍干预前驱糖尿病患者的ICER表明,二甲双胍治疗以更低的成本为公共支付者带来了更多的健康效益(预防糖尿病病例数)。ICER的计算结果是,每预防1例糖尿病患者可减少- 7122.32 BGN,这证实,与“什么都不做”的方法相比,应用二甲双胍可以节省成本。获得的每质量调整生命年(QALYs)的ICUR也显示二甲双胍预防干预是一种主要的、节省成本的替代方案。马尔可夫模型模拟证实,二甲双胍干预在长期内成本较低,并导致更高的QALYs。结论:投资二甲双胍进行预防干预是物超所值的。二甲双胍干预前驱糖尿病患者的ICER与“什么都不做”常规相比表明,二甲双胍预防性干预对保加利亚的公共支付者以较低的成本产生了更多的健康效益。
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引用次数: 0
Antiproliferative activity of ruthenium complex II against human cancer cell in vitro 钌络合物II对人癌细胞的体外抗增殖活性
Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-18 DOI: 10.3897/pharmacia.70.e111410
Mohamed Saadh
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.
尽管癌症治疗取得了重大进展,但仍然需要新的有效的治疗选择。其中一种对抗癌症的潜在武器就是钌络合物II。本文合成、表征并研究了二硫氰酸酯- n -双[8-(二苯基膦)喹啉]钌(II) [Ru(N-P)2(NCS)2]作为正常细胞对MCF-7人腺癌细胞和胎肺成纤维细胞样细胞MRC-5细胞株的活性,以及作用机制和选择性。本研究表明,[Ru(N-P) 2 (NCS) 2]对MCF-7具有细胞毒活性,ic50值为7.56µg/ml,对MRC-5具有细胞毒活性,ic50值为576.6µg/ml。[Ru(N-P) 2 (NCS) 2]对MCF-7癌细胞比MRC-5正常细胞株具有更强的选择性细胞毒活性。本研究通过检测caspase-3的激活,证明了钌络合物II的强效凋亡活性,突出了其作为癌症治疗药物的潜力。[Ru(N-P) 2 (NCS) 2]被认为有希望研究假定的生物活性,特别是抗肿瘤和免疫相关活性。
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引用次数: 0
Anticancer and antiproliferative activity of ruthenium complex (II) bearing 3,3’-dicarboxy-2,2’-bipyridine ligand 含有3,3 ' -二羧基-2,2 ' -联吡啶配体的钌配合物(II)的抗癌和抗增殖活性
Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-18 DOI: 10.3897/pharmacia.70.e111508
Mohamed Saadh
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.
尽管癌症治疗已经取得了重大进展,但仍有改进的余地。实验药物钌复合物II显示出治疗癌症的希望。本文合成了二氯-3,3′-二羧基-2,2′-联吡啶基双(二甲基亚砜)钌(II) [RuCl 2(3,3′-dcbpy)(DMSO) 2],并对其对MDA-MB-231和MRC-5细胞系的抗癌活性、作用机制和选择性进行了研究。研究发现,[RuCl 2(3,3′-dcbpy)(DMSO) 2]对MDA-MB-231细胞毒性高,对MRC-5细胞毒性最低,ic50值分别为5.95和579.6 μg/ml。钌络合物II在破坏癌细胞方面非常有效,同时对健康细胞的危害最小。RuCl 2 (3,3 ' -dcbpy)(DMSO) 2]引起细胞凋亡,通过激活caspase-3证实了这一点。钌络合物作为强效抗癌剂具有很大的前景。它们独特的作用机制、选择性靶向癌细胞的能力以及化学结构的多功能性使它们成为靶向治疗发展的有吸引力的候选者。
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Pharmacia
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