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Oral acute toxicity study of ethanol extract of Mobe leaves (Artocarpus lacucha Buch-Ham) in Wistar rats 莫比叶(Artocarpus lacucha Buch-Ham)乙醇提取物对 Wistar 大鼠的口服急性毒性研究
Pub Date : 2024-03-25 DOI: 10.3897/pharmacia.71.e117500
Denny Satria, P. Sitorus, A. Dalimunthe, S. B. Waruwu, Vivi Asfianti
Many medicinal plants are now being chosen because the treatment is safer and cheaper. Artocarpus lacucha Buch-Ham is a plant with many pharmacological activities and is efficacious; its safety has not been studied. Acute oral toxicity evaluation followed Organization for Economic Co-operation and Development guidelines using the fixed dose method. The evaluation began with a preliminary test, then a primary test with three groups: a 2000 mg/Kg BW dose test group, a 5000 mg/Kg BW dose test group, and a control group. The results of visual observations, haematological and clinical examinations, and histological examination of organs (liver, spleen, kidneys, lungs and heart) showed no toxicity in the animals, and they did not die during testing. The findings of this study support the safety of Artocarpus lacucha Buch-Ham leaf ethanol extract, which did not produce harmful results in acute toxicity tests.
由于治疗更安全、更便宜,许多药用植物现在都被选用。Artocarpus lacucha Buch-Ham 是一种具有多种药理活性的植物,疗效显著,但其安全性尚未得到研究。急性口服毒性评估遵循经济合作与发展组织的指导方针,采用固定剂量法。评估首先进行初步试验,然后进行三组主要试验:2000 毫克/千克体重剂量试验组、5000 毫克/千克体重剂量试验组和对照组。肉眼观察、血液学和临床检查以及器官(肝脏、脾脏、肾脏、肺脏和心脏)组织学检查的结果表明,动物没有毒性,在试验过程中也没有死亡。这项研究结果证明,Artocarpus lacucha Buch-Ham 叶乙醇提取物是安全的,在急性毒性试验中没有产生有害结果。
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引用次数: 0
Pharmacists’ burnout and motivation for pharmaceutical care in chronically ill patients – a pilot study for the north-eastern region of Bulgaria 药剂师的职业倦怠与慢性病患者药物治疗的动力--保加利亚东北部地区的试点研究
Pub Date : 2024-03-25 DOI: 10.3897/pharmacia.71.e120566
Anna Todorova, Mariya Ivanova, V. Petkova
Medical professionals are the most susceptible to professional burnout. An anonymous survey of master pharmacists was conducted to assess burnout with the MBI-HSS-MP tool and analyse the challenges of working in community pharmacies. Burnout affected 53% of the 127 pharmacists surveyed. Factors influencing the scales forming burnout emotional exhaustion (EE) depersonalisation (DP), and personal accomplishment (PA) were: administrative difficulties in servicing the prescriptions of chronically ill patients: affected 57% of respondents and influenced EE (p = 0.036); lack of precise instructions at work (38% of respondents, influenced DP, p = 0.007) and (EE, p = 0.000); lack of prior information about innovations 38% (EE p = 0.002). Lack of time to carry out pharmaceutical care (PhC) influenced EE (p = 0.019) and DP (p = 0.006) and DP was associated with lower empathy for patients, Lack of perceived professional satisfaction (PA; p = 0.042) was increased. The increased administrative duties shifted the focus away from PhC and decreased pharmacists’ motivation.
医务人员最容易产生职业倦怠。我们对药剂师进行了匿名调查,利用 MBI-HSS-MP 工具评估职业倦怠,并分析了在社区药房工作所面临的挑战。在接受调查的 127 名药剂师中,53% 的人受到职业倦怠的影响。影响职业倦怠情绪衰竭(EE)、人格解体(DP)和个人成就感(PA)量表的因素有:为慢性病患者开处方时遇到的行政困难:影响了 57% 的受访者,并对 EE 产生了影响(p = 0.036);工作中缺乏准确的指示(38% 的受访者,对 DP 产生了影响,p = 0.007)和(EE,p = 0.000);事先缺乏有关创新的信息(38% 的受访者,对 EE 产生了影响,p = 0.002)。缺乏开展药物护理(PhC)的时间影响了 EE(p = 0.019)和 DP(p = 0.006),DP 与对病人的同情心降低有关,缺乏感知到的专业满意度(PA;p = 0.042)增加。行政职责的增加转移了药剂师对 PhC 的关注,降低了药剂师的积极性。
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引用次数: 0
Antihypertensive activity of spray-dried nanoemulsion containing Asiatic acid-Palm oil in high salt diet-fed rats 含亚西亚酸-棕榈油的喷雾干燥纳米乳液对高盐饮食大鼠的抗高血压活性
Pub Date : 2024-03-05 DOI: 10.3897/pharmacia.71.e115091
A. Pradana, G. Ritthidej, Vudhiporn Limprasutr, Ausana Wongtayan, V. Lipipun, Iksen
Asiatic acid (AA) is a compound isolated from Centella asiatica, which possesses significant antihypertensive activity. Several studies have shown that its hypertensive activity can be attributed to various mechanisms, such as Angiotensin-Converting-Enzyme (ACE) inhibition in the renin-angiotensin-aldosterone system (RAAS) pathway. Meanwhile, palm oil (PO) is an antioxidant, which has proven to have synergistic effects with the compound by preventing arterial thrombosis and atherosclerosis. Despite these synergistic effects, AA dosage in antihypertensive therapy has been reported to be relatively high compared to the common synthetic drug captopril. Therefore, this study aimed to produce spray-dried powder of nanoemulsion to enhance the solubility of AA, decrease the possibility of oxidation, and increase its activity. Redispersed AA nanoparticles were also successfully obtained during the synthesis process. Several evaluations were carried out, including particle size, particle distribution, zeta potential, cell viability, and antihypertensive activity in rats to ensure the improvement of physicochemical characteristics and activity as antihypertensive agent. The results showed that AA succeeded in forming nanoemulsion with excipients. In addition, it was encapsulated in a maltodextrin carrier, exhibiting good physicochemical characteristics and safety to the Caco-2 cells. The redispersion of the spray-dried powder yielded nanoparticles with a size of 217.4 ± 10.196 nm. The spray-dried nanoemulsion of AA also had faster effect than non-formulated AA (raw powder) in lowering the blood pressure of hypertensive Sprague-Dawley (SD) rats. Graphical abstract:
积雪草酸(AA)是从积雪草中分离出来的一种化合物,具有显著的降压活性。多项研究表明,其高血压活性可归因于多种机制,如抑制肾素-血管紧张素-醛固酮系统(RAAS)途径中的血管紧张素转换酶(ACE)。同时,棕榈油(PO)是一种抗氧化剂,已被证明与该化合物具有协同作用,可防止动脉血栓形成和动脉粥样硬化。尽管有这些协同作用,但据报道,与常见的合成药物卡托普利相比,AA 在降压治疗中的用量相对较高。因此,本研究旨在生产纳米乳液喷雾干燥粉末,以提高 AA 的溶解度,降低氧化的可能性,并增加其活性。在合成过程中,还成功获得了再分散 AA 纳米粒子。研究人员进行了多项评估,包括粒度、粒度分布、ZETA电位、细胞存活率和大鼠降压活性,以确保改善 AA 的理化特性并提高其作为降压药的活性。结果表明,AA 成功地与辅料形成了纳米乳液。此外,它还被包裹在麦芽糊精载体中,显示出良好的理化特性和对 Caco-2 细胞的安全性。喷雾干燥粉末再分散后得到的纳米颗粒大小为 217.4 ± 10.196 nm。喷雾干燥的AA纳米乳液在降低高血压Sprague-Dawley(SD)大鼠血压方面的效果也比非制剂AA(原粉)更快。图表摘要:
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引用次数: 0
Qualitative chemical compounds analysis and in vitro estimation of antiproliferative, antidiabetic and anti-Alzheimer’s disease effects of Ononis natrix (L.) family Fabaceae 豆科植物 Ononis natrix (L.) 的化合物定性分析及抗增殖、抗糖尿病和抗老年痴呆症作用的体外评估
Pub Date : 2024-03-01 DOI: 10.3897/pharmacia.71.e119755
Ahmed M M Youssef, D. A. M. Maaty, Yousef M Al-Saraireh
The O. natrix belongs to the family Fabaceae and is distributed in Jordan. Different species of the family Fabaceae contain chemical compounds that may have potential antiproliferative, antidiabetic, and anti-Alzheimer’s disease. High-performance liquid chromatography (HPLC) was applied to analyse the phenolic compounds found in O. natrix methanolic extract. Using the MTT assay, the antiproliferative action was studied. The enzymes α-glucosidase and butyrylcholinesterase inhibition assays were used to study the antidiabetic and anti-Alzheimer’s disease actions, respectively, of methanolic extract of O. natrix. Eleven phenolics and seven flavonoids were identified in the methanolic extract of O. natrix by HPLC. The highest phenolics and flavonoids were gallic acid (1.25 mg/100 g dry weight) and rutin (1.44 mg/100 g dry weight), respectively. The most cancer cell lines influenced by the extract of O. natrix were PC-3 (IC50 = 55 ± 2 µg/mL) and HepG-2 (IC50 = 68 ± 2 µg/mL) compared to positive control cisplatin. However, the cancer cell lines CaCo-2, MCF-7, and HeLa showed IC50 values of 109 ± 2 µg/mL, 123 ± 2 µg/mL, and 79 ± 1 µg/mL, respectively, related to cisplatin. The O. natrix extract inhibited the α-glucosidase enzyme and butyrylcholinesterase enzyme by 84% and 86%, respectively compared to positive controls acarbose and rivastigmine. The O. natrix may possess antiproliferative effects against prostate cancer and hepatocellular carcinoma. It also may have antidiabetic and anti-Alzheimer’s disease effects.
O. natrix属于豆科植物,分布在约旦。豆科植物的不同种类都含有可能具有抗增殖、抗糖尿病和抗老年痴呆症作用的化合物。高效液相色谱法(HPLC)用于分析 O. natrix 甲醇提取物中的酚类化合物。使用 MTT 法研究了抗增殖作用。α-葡萄糖苷酶和丁酰胆碱酯酶抑制试验分别用于研究 O. natrix 甲醇提取物的抗糖尿病和抗老年痴呆症作用。通过高效液相色谱法,鉴定出 O. natrix 的甲醇提取物中含有 11 种酚类物质和 7 种黄酮类物质。酚类和类黄酮含量最高的分别是没食子酸(1.25 毫克/100 克干重)和芦丁(1.44 毫克/100 克干重)。与阳性对照顺铂相比,受 O. natrix 提取物影响最大的癌细胞系是 PC-3(IC50 = 55 ± 2 µg/mL)和 HepG-2(IC50 = 68 ± 2 µg/mL)。然而,癌细胞系 CaCo-2、MCF-7 和 HeLa 与顺铂相比的 IC50 值分别为 109 ± 2 µg/mL、123 ± 2 µg/mL 和 79 ± 1 µg/mL。与阳性对照阿卡波糖和利伐斯的明相比,O. natrix 提取物对α-葡萄糖苷酶和丁酰胆碱酯酶的抑制率分别为 84% 和 86%。O. natrix 可能具有抗前列腺癌和肝细胞癌的增殖作用。它还可能具有抗糖尿病和抗老年痴呆症的作用。
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引用次数: 0
Chrysin’s dose-dependent effects on steroidogenesis in female BALB/c mice: In vivo study of adrenal, ovarian, and uterine hormone regulation 蛹虫草素对雌性 BALB/c 小鼠类固醇生成的剂量依赖性影响:肾上腺、卵巢和子宫激素调节的体内研究
Pub Date : 2024-02-29 DOI: 10.3897/pharmacia.71.e114547
Khalid M. Alqaisi, M. Abbas, Rand Alshawawreh
Background: Chrysin is known for its pharmacological effects and structural resemblance to estrogen. The study explores the impact of chrysin on steroidogenesis focusing on adrenal and ovarian steroidogenic enzymes. Materials and methods: Thirty female BALB/c mice were divided into three groups: a control group and two chrysin-treated groups (50 mg and 100 mg). Gene expression of key steroidogenic enzymes was assessed in adrenal glands and ovaries using RT-qPCR. Uterine expression of estrogen receptor alpha (ERα) was also examined. Histological analysis of adrenal glands and ovaries was performed. Results: High-dose chrysin downregulated CYP17A1 expression in adrenal glands compared to control and low-dose groups. In contrast, 3β-HSD was significantly downregulated in the high-dose group. In ovaries, high dose chrysin reduced aromatase expression. Conclusion: Our findings revealed that chrysin’s impact on steroidogenesis is dose-dependent. By downregulating CYP17A1 in adrenal glands, potentially affecting androgen and estrogen synthesis, and enhancing aromatase expression in ovaries at lower doses.
背景:菊黄素因其药理作用和与雌激素相似的结构而闻名。本研究探讨了菊黄素对类固醇生成的影响,重点是肾上腺和卵巢类固醇生成酶。材料和方法:将 30 只雌性 BALB/c 小鼠分为三组:对照组和两组菊粉处理组(50 毫克和 100 毫克)。使用 RT-qPCR 评估肾上腺和卵巢中关键类固醇生成酶的基因表达。还检测了子宫雌激素受体α(ERα)的表达。对肾上腺和卵巢进行了组织学分析。结果与对照组和低剂量组相比,高剂量菊粉会降低肾上腺中 CYP17A1 的表达。相反,高剂量组中 3β-HSD 的表达明显下调。在卵巢中,高剂量菊粉降低了芳香化酶的表达。结论我们的研究结果表明,菊粉对类固醇生成的影响与剂量有关。通过下调肾上腺中的 CYP17A1,可能会影响雄激素和雌激素的合成,而低剂量则会增强卵巢中芳香化酶的表达。
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引用次数: 0
The effects of meloxicam, lornoxicam, ketoprofen, and dexketoprofen on human cervical, colorectal, and mammary carcinoma cell lines 美洛昔康、洛诺昔康、酮洛芬和右酮洛芬对人类宫颈癌、结直肠癌和乳腺癌细胞系的影响
Pub Date : 2024-02-29 DOI: 10.3897/pharmacia.71.e113677
Lyubomir Marinov, A. Georgieva, R. Toshkova, Ivanka Kostadinova, I. Mangarov, Tanya Toshkova-Yotova, Irina Nikolova
Targeting the inflammation-related molecules with nonsteroidal anti-inflammatory drugs (NSAIDs) represents a promising approach for cancer prevention/therapy. We evaluated the in vitro anticancer effects of meloxicam, lornoxicam, ketoprofen, and dexketoprofen on the proliferation, migration, and apoptosis of human cervical, colorectal, and mammary carcinoma cells. The antiproliferative activity and cytotoxicity of tested NSAIDs on HeLa, HT-29, and MCF-7 cell lines were assessed by the MTT test. The apoptosis-inducing potential was analyzed by fluorescent staining with acridine orange/ethidium bromide and DAPI. Migration activity was assessed by a wound-healing scratch assay. The tested NSAIDs reduced the viability of the used tumor cell lines. The cytomorphological analysis revealed reduced cell density and mitotic activity and the presence of cells with morphological features of early and late apoptosis. Significant inhibition of the migration capacity was established as well. In conclusion, NSAIDs could be candidates for the development of new pharmacological strategies for the treatment and prevention of cancer.
用非甾体抗炎药(NSAIDs)靶向炎症相关分子是一种很有前景的癌症预防/治疗方法。我们评估了美洛昔康、洛诺昔康、酮洛芬和右酮洛芬对人宫颈癌、结直肠癌和乳腺癌细胞的增殖、迁移和凋亡的体外抗癌作用。通过 MTT 试验评估了受试非甾体抗炎药对 HeLa、HT-29 和 MCF-7 细胞系的抗增殖活性和细胞毒性。用吖啶橙/溴化乙锭和 DAPI 进行荧光染色,分析诱导细胞凋亡的潜力。迁移活性通过伤口愈合划痕试验进行评估。测试的非甾体抗炎药降低了所用肿瘤细胞系的活力。细胞形态学分析表明,细胞密度和有丝分裂活性降低,出现了具有早期和晚期凋亡形态特征的细胞。迁移能力也受到明显抑制。总之,非甾体抗炎药可作为开发治疗和预防癌症新药理策略的候选药物。
{"title":"The effects of meloxicam, lornoxicam, ketoprofen, and dexketoprofen on human cervical, colorectal, and mammary carcinoma cell lines","authors":"Lyubomir Marinov, A. Georgieva, R. Toshkova, Ivanka Kostadinova, I. Mangarov, Tanya Toshkova-Yotova, Irina Nikolova","doi":"10.3897/pharmacia.71.e113677","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e113677","url":null,"abstract":"Targeting the inflammation-related molecules with nonsteroidal anti-inflammatory drugs (NSAIDs) represents a promising approach for cancer prevention/therapy. We evaluated the in vitro anticancer effects of meloxicam, lornoxicam, ketoprofen, and dexketoprofen on the proliferation, migration, and apoptosis of human cervical, colorectal, and mammary carcinoma cells. The antiproliferative activity and cytotoxicity of tested NSAIDs on HeLa, HT-29, and MCF-7 cell lines were assessed by the MTT test. The apoptosis-inducing potential was analyzed by fluorescent staining with acridine orange/ethidium bromide and DAPI. Migration activity was assessed by a wound-healing scratch assay. The tested NSAIDs reduced the viability of the used tumor cell lines. The cytomorphological analysis revealed reduced cell density and mitotic activity and the presence of cells with morphological features of early and late apoptosis. Significant inhibition of the migration capacity was established as well. In conclusion, NSAIDs could be candidates for the development of new pharmacological strategies for the treatment and prevention of cancer.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140417108","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Malaria’s molecular dance: Mechanism, therapies, and emerging insights 疟疾的分子舞蹈:机制、疗法和新见解
Pub Date : 2024-02-28 DOI: 10.3897/pharmacia.71.e117145
Nabila Ananda, Athaya Sabina, Ulfa Rahmadani, Ali Syahrizal, Nabillah Deskya, Sinta Maria, Muhammad Riza, Lusi Rahmadia, Anni Holila, Dwi Putri, Kevin Gabriel, Ratna Sari Zai, Mega Carensia, Princella Halim, Naomi Regina, Dinda Rizka, Aulia Syahfitri, Tessa Rotua, Maria Belen, Fahmy Nanda, Rizzanda Pramuditya, Khairunnisa Khairunnisa, Emil Salim, F. Nurkolis, Chindy Umaya, Rony Abdi Syahputra
Malaria, caused by Plasmodium parasites and transmitted through Anopheles mosquitoes, remains a formidable global health challenge. This abstract provides an overview of the intricate molecular mechanisms underlying malaria pathogenesis, explores current therapeutic approaches, and highlights emerging insights that may shape future strategies for malaria control. The intricate dance between Plasmodium parasites and their human hosts begins with the mosquito’s bite, leading to the invasion of erythrocytes by Plasmodium species. We delve into the molecular mechanisms governing parasite entry and subsequent replication within host cells, shedding light on key factors such as erythrocyte surface receptors and parasite-encoded proteins critical to invasion and survival. While malaria treatment has relied heavily on antimalarial drugs, the emergence of drug resistance necessitates ongoing exploration of novel therapeutic strategies. This abstract reviews current antimalarial drug classes, their mechanisms of action, and the challenges posed by drug resistance. We also highlight promising drug candidates and innovative approaches in the pipeline, including the use of advanced molecular techniques and immunotherapies. Emerging insights from genomics, proteomics, and transcriptomics have deepened our understanding of Plasmodium biology and host-parasite interactions. We discuss the potential of these omics approaches in identifying new drug targets, understanding drug resistance mechanisms, and developing vaccines. Additionally, we examine the role of human genetics in influencing susceptibility to malaria and response to treatment. Vector control remains a critical component of malaria prevention. We touch upon emerging strategies, such as genetically modified mosquitoes and novel insecticides, in the context of integrated vector management programs. Finally, we emphasize the importance of a multifaceted approach to malaria control, combining advances in molecular biology, drug development, vector control, and public health interventions.
疟疾由疟原虫引起,通过按蚊传播,仍然是全球健康面临的严峻挑战。本摘要概述了疟疾发病机制背后错综复杂的分子机制,探讨了当前的治疗方法,并重点介绍了可能影响未来疟疾控制策略的新见解。疟原虫与人类宿主之间错综复杂的关系始于蚊子叮咬,导致疟原虫入侵红细胞。我们深入研究了寄生虫进入宿主细胞以及随后在宿主细胞内复制的分子机制,揭示了红细胞表面受体和寄生虫编码蛋白等对入侵和存活至关重要的关键因素。虽然疟疾的治疗主要依靠抗疟药物,但抗药性的出现要求我们不断探索新的治疗策略。本摘要回顾了目前的抗疟药物类别、作用机制以及抗药性带来的挑战。我们还重点介绍了前景看好的候选药物和正在研发中的创新方法,包括先进分子技术和免疫疗法的应用。基因组学、蛋白质组学和转录组学的新见解加深了我们对疟原虫生物学和宿主-寄生虫相互作用的了解。我们讨论了这些 omics 方法在确定新的药物靶点、了解耐药机制和开发疫苗方面的潜力。此外,我们还探讨了人类遗传学在影响疟疾易感性和治疗反应方面的作用。病媒控制仍然是疟疾预防的重要组成部分。我们将结合病媒综合管理计划,探讨转基因蚊子和新型杀虫剂等新兴战略。最后,我们强调采取多方面方法控制疟疾的重要性,将分子生物学、药物开发、病媒控制和公共卫生干预方面的进展结合起来。
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引用次数: 0
Association of the rs1801133 and rs1801131 polymorphisms in the MTHFR gene and the adverse drug reaction of methotrexate treatment in a sample of Iraqi rheumatoid arthritis patients 伊拉克类风湿性关节炎患者样本中 MTHFR 基因 rs1801133 和 rs1801131 多态性与甲氨蝶呤治疗药物不良反应的关系
Pub Date : 2024-02-27 DOI: 10.3897/pharmacia.71.e113597
Qassim Mahdi Mutlak, Ali Abdulhussain Kasim
Background: Methotrexate is one of the mainstays for treating rheumatoid arthritis (RA) with a wide range of adverse drug reactions, however, it’s the relationship between adverse drug reactions and genetic polymorphism remains to be highlighted, and there is a lack of studies concerning Arabic Iraqi population regarding this aspect. Objective: Evaluate the association between genetic mutations in the MTHFR gene in SNPs (rs1801133G>A and rs1801131T>G) on the adverse drug reaction for RA Iraqi patients. Methods: An observational study, that involved 95 Iraqi RA patients with established RA. Patients were divided according to the occurrence of adverse drug reactions. A polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) was being utilized for MTHFR variants (rs1801133 and rs1801131). The Macrogen Company (Korea) provided the forward and reverse primers in lyophilized form. All PCR procedures are carried out using a PCR thermal cycler (Germany). Results: The study included 95 patients with RA, with a mean age of 43.1 ± 10.6 years, most of the patients were female (85.3%), about 35.8% were smokers, most of the patients had disease low activity (45.2%), followed by moderate (41.1%), high (9.5%), and remission (4.2%). No significant association between individual genetic polymorphism with adverse drug reactions. AG haplotype for rs1801133 rs1801131 polymorphism is associated with reducing the risk of overall adverse drug reactions, meanwhile, GT haplotype for rs1801133, and rs1801131 polymorphism were marginally associated with increased risk of adverse drug reactions. Conclusion: In conclusion, we have successfully found a panel of pharmacogenetic indicators that have the potential to be valuable in predicting the response to methotrexate treatment in patients with rheumatoid arthritis. Haplotypes for rs1801133 rs1801131 polymorphism are associated with reducing or increasing the risk of MTX adverse drug reactions. It is very important to evaluate patients’ haplotypes before starting the therapy program so that we can expect the treatment outcome with the most suitable dose and most tolerable one at the same time.
背景:甲氨蝶呤是治疗类风湿性关节炎(RA)的主要药物之一,具有广泛的药物不良反应,然而,药物不良反应与基因多态性之间的关系仍有待进一步研究,而且缺乏针对阿拉伯裔伊拉克人在这方面的研究。研究目的评估伊拉克 RA 患者 MTHFR 基因中 SNPs(rs1801133G>A 和 rs1801131T>G)基因突变与药物不良反应之间的关系。研究方法一项观察性研究,涉及 95 名已确诊的伊拉克 RA 患者。根据药物不良反应的发生情况对患者进行分类。采用聚合酶链式反应-限制性片段长度多态性(PCR-RFLP)检测 MTHFR 变体(rs1801133 和 rs1801131)。韩国 Macrogen 公司提供了冻干形式的正向和反向引物。所有 PCR 过程均使用 PCR 热循环仪(德国)进行。研究结果研究共纳入 95 例 RA 患者,平均年龄(43.1±10.6)岁,大多数患者为女性(85.3%),约 35.8%为吸烟者,大多数患者的疾病活动度较低(45.2%),其次为中度(41.1%)、高度(9.5%)和缓解(4.2%)。个别基因多态性与药物不良反应无明显关联。rs1801133的AG单倍型和rs1801131多态性与总体药物不良反应风险的降低有关,而rs1801133的GT单倍型和rs1801131多态性与药物不良反应风险的增加略有关联。结论总之,我们成功地找到了一组药物遗传学指标,它们在预测类风湿关节炎患者对甲氨蝶呤治疗的反应方面具有潜在价值。rs1801133 rs1801131 多态性的单倍型与降低或增加 MTX 药物不良反应的风险有关。因此,在开始治疗前对患者的单倍型进行评估非常重要,这样我们就能以最合适的剂量和最可耐受的剂量获得预期的治疗效果。
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引用次数: 0
Kidney protective effect of sitagliptin in 5-fluorouracil-challenged rats 西他列汀对5-氟尿嘧啶挑战大鼠肾脏的保护作用
Pub Date : 2024-02-27 DOI: 10.3897/pharmacia.71.e114441
Ahmed Hassan Al-Ghamdi, Mervat Z. Mohamed, Rabei M. Elbadry, A. Fouad
The possible protective effect of sitagliptin (SIT) against nephrotoxicity induced by a single dose 5-fluorouracil (5-FU) (150 mg/kg, i.p.) was investigated in rats. SIT treatment (5 and 10 mg/kg/day, p.o.) was given for 7 days, starting 5 days before 5-FU administration. Both SIT doses caused significant reductions of serum creatinine and neutrophil gelatinase-associated lipocalin levels in rats received 5-FU. Both doses of SIT also significantly decreased malondialdehyde, tumor necrosis factor-α, interleukin-1β, nuclear factor-κB p65 (NF-κB p65), Bax/Bcl-2 ratio, and cleaved caspase-3 in kidneys of 5-FU-challenged rats. Additionally, SIT, at both doses, significantly increased renal total antioxidant capacity and nuclear factor erythroid 2related factor 2 (Nrf2) in rats received 5-FU. Besides, SIT markedly attenuated the 5-FU-induced histopathological kidney tissue injury in rats. It was concluded that SIT, at both doses, provided a significant nephroprotective effect in 5-FU-challenged rats, through its antioxidant, antiinflammatory, and antiapoptotic activities, and by modulating Nrf2 and NF-κB pathways.
研究人员以大鼠为研究对象,探讨了西他列汀(SIT)对单剂量 5-氟尿嘧啶(5-FU)(150 毫克/千克,静脉注射)诱导的肾毒性可能具有的保护作用。SIT 治疗(5 和 10 毫克/千克/天,口服)为期 7 天,在服用 5-FU 前 5 天开始。两种剂量的 SIT 均可显著降低接受 5-FU 治疗的大鼠的血清肌酐和中性粒细胞明胶酶相关脂褐质水平。两种剂量的 SIT 还能显著降低 5-FU 挑战大鼠肾脏中的丙二醛、肿瘤坏死因子-α、白细胞介素-1β、核因子-κB p65(NF-κB p65)、Bax/Bcl-2 比率和裂解的 Caspase-3。此外,两种剂量的 SIT 都能显著提高 5-FU 大鼠肾脏的总抗氧化能力和核因子红细胞 2 相关因子 2(Nrf2)。此外,SIT 还能明显减轻 5-FU 引起的大鼠肾组织损伤。结论是,两种剂量的 SIT 都能通过其抗氧化、抗炎和抗细胞凋亡活性,以及通过调节 Nrf2 和 NF-κB 通路,对接受 5-FU 治疗的大鼠产生显著的肾保护作用。
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引用次数: 0
Curcumin is comparable to metformin for the treatment of PCOS in rats: a preclinical study 姜黄素治疗大鼠多囊卵巢综合征的效果与二甲双胍相当:一项临床前研究
Pub Date : 2024-02-27 DOI: 10.3897/pharmacia.71.e119708
Salam Shannag, K. Nuseir, Linda Tahaineh, Wael Hananeh
Background: Ploy cystic ovary syndrome (PCOS) is a common gynecological disorder affecting between 4–20% of females worldwide. Curcumin, the active ingredient in turmeric (Curcuma longaZingiberaceae) is a yellow polyphenol with a wide range of pharmacological activities such as antioxidant, anti-inflammatory, anti-tumor, neuroprotective and cardioprotective properties. Methods: Letrozole was used to induce PCOS in female Wistar rats. Curcumin, metformin, or a combination of both was given to assess their therapeutic effects. Body weight, estrogen, progesterone, testosterone, and glucose levels were measured after disease induction and at the conclusion of treatment. Additionally ovarian histomorphology was examined after sacrificing the animals and removal of the ovaries. Results and conclusion: Weight was significantly reduced in the curcumin, metformin and curcumin and metformin combination groups. Testosterone was decreased, progesterone was increased, and normal ovarian morphology was restored in the three groups. Conclusions: curcumin is therapeutically effective for PCOS and is comparable to metformin.
背景:多囊卵巢综合征(PCOS多囊卵巢综合征(PCOS)是一种常见的妇科疾病,影响着全球4-20%的女性。姜黄素(Curcuma longaZingiberaceae)的活性成分姜黄素是一种黄色多酚,具有抗氧化、抗炎、抗肿瘤、神经保护和心脏保护等多种药理活性。研究方法用来曲唑诱导雌性 Wistar 大鼠患多囊卵巢综合征。给予姜黄素、二甲双胍或二者的组合以评估其治疗效果。在疾病诱导后和治疗结束时测量体重、雌激素、孕酮、睾酮和血糖水平。此外,在牺牲动物并切除卵巢后,还对卵巢组织形态学进行了检查。结果和结论姜黄素组、二甲双胍组以及姜黄素和二甲双胍联合组的体重明显降低。三组动物的睾酮降低,孕酮升高,卵巢形态恢复正常。结论:姜黄素对多囊卵巢综合症有疗效,且疗效与二甲双胍相当。
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