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Molecular Docking Studies of Glabrene and Human Epidermal Growth Factor Receptor Kinase 光烯与人表皮生长因子受体激酶的分子对接研究
Pub Date : 2022-04-29 DOI: 10.36922/itps.v4i1.56
N. Katari, R. Gundla, P. K. Reddy, Anuradha Vanam, Aruna Talatam, N. Motohashi, Rao Gollapudi
Background: Human epidermal growth factor receptor 2 (Her2) gene located in human chromosome17, encodes Her2 tyrosine kinase protein, and is overexpressed in breast cancer cells. Her2 is activated on phosphorylation of tyrosine by adenosine triphosphate (ATP). Nonetheless, Her2 excessively partakes in the development and prognosis of specific types of aggressive breast cancers. Therefore, Her2 inhibition therapy is primary target for the treatment of aggressive breast cancer. At present, lapatinib is one of the Food and Drug Administration approved Her2 inhibitors used in cancer therapy. In molecular docking process, glabrene with slightly higher binding energy competitively bound to the active receptor site comparable to lapatinib and ATP. Therefore, glabrene could emerge as a potential candidate for restricting Her2 overexpressed breast cancer. Objective: The present study aimed to demonstrate the inhibitory activity of glabrene, an isoflavene and xenoestrogen found in liquorice root, along with known Her2 inhibitor, lapatinib. Methods: ATP, lapatinib, and glabrene were docked on human Her2 protein 3D structure which revealed glabrene as a competitive Her2 inhibitor akin to lapatinib. Results: The docking results suggested the binding site similarities of ATP, lapatinib, and glabrene. The binding energies of docked ATP, lapatinib, and glabrene complexes with Her2 were −9.1 kcal/mol, −10.5 kcal/mol, and −11.3 kcal/mol, respectively. Conclusion: The in silico docking simulation of ATP, lapatinib, and glabrene suggested that glabrene is likewise a competitive Her2 inhibitor.
背景:人表皮生长因子受体2 (Her2)基因位于人17号染色体,编码Her2酪氨酸激酶蛋白,在乳腺癌细胞中过表达。Her2在酪氨酸被三磷酸腺苷(ATP)磷酸化时被激活。然而,Her2过度参与特定类型侵袭性乳腺癌的发展和预后。因此,Her2抑制疗法是治疗侵袭性乳腺癌的主要靶点。目前,拉帕替尼是美国食品和药物管理局批准用于癌症治疗的Her2抑制剂之一。在分子对接过程中,与拉帕替尼和ATP相比,光烯以稍高的结合能竞争性地结合到活性受体位点。因此,光烯可能成为限制Her2过表达乳腺癌的潜在候选物。目的:本研究旨在证明甘草根中发现的glabrene(一种异黄酮和雌激素)与已知的Her2抑制剂拉帕替尼一起抑制活性。方法:将ATP、拉帕替尼和glabrene对接到人Her2蛋白的3D结构上,发现glabrene是与拉帕替尼类似的竞争性Her2抑制剂。结果:对接结果表明ATP、拉帕替尼、光烯的结合位点相似。ATP、拉帕替尼和光烯配合物与Her2的结合能分别为- 9.1 kcal/mol、- 10.5 kcal/mol和- 11.3 kcal/mol。结论:ATP、拉帕替尼和光烯的硅对接模拟表明,光烯同样是一种竞争性Her2抑制剂。
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引用次数: 0
Conjugation of Silver and Gold Nanoparticles for Enhancing Antimicrobial Activity 银和金纳米颗粒的偶联增强抗菌活性
Pub Date : 2022-04-22 DOI: 10.36922/itps.v4i2.70
Muhamad Shakir Yusoff, S. Gopinath, M. Uda, T. LakshmiPriya, Ahmad Radi Wan Yaakub, P. Anbu
Silver and gold nanoparticles are promising agents that can enhance the antibacterial activity of conjugated/capped extract of plant compounds. The aim of our study is to synthesize silver nanoparticles from Gymnema sylvestre plant extract. In this study, the antimicrobial activity of conjugated silver which was green synthesized and gold nanoparticle that was obtained from a commercial source was evaluated using disk-diffusion method against Escherichia coli and Aspergillus niger. Transmission electron microscopy, scanning electron microscopy, ultraviolet-visible spectroscopy, and Fourier transform infrared spectroscopy analyses were also carried out to characterize the conjugated silver and gold nanoparticles. The conjugation of silver and gold nanoparticles was performed chemically using 16-mercaptodecanoic acid. Our results revealed that conjugated silver and gold nanoparticle both showing larger inhibition zones against E. coli and A. niger. The minimum inhibitory concentration (MIC) of the above metallic conjugation was found to be stable with MIC was reported to be 1 mM. When comparing the sample analysis on conjugation of gold and silver nanoparticles against E. coli and A. niger, the antimicrobial activity recorded was 2.0 ± 0.01 and 2.32 ± 0.04 cm, respectively, with no significance difference was found (P = 0.85). In conclusion, the combination of two different nanoparticles is efficient for microbial inhibition and can be useful for studying antimicrobial activities with the combination of different nanomaterials in future.
银纳米粒子和金纳米粒子是提高植物化合物缀合物/盖顶物抑菌活性的有前途的药物。本研究以匙羹藤植物提取物为原料合成纳米银。本研究采用圆盘扩散法研究了绿色合成的共轭银和商业来源的金纳米颗粒对大肠杆菌和黑曲霉的抑菌活性。通过透射电子显微镜、扫描电子显微镜、紫外可见光谱和傅里叶变换红外光谱分析对共轭银和金纳米粒子进行了表征。用16-巯基癸酸进行了银和金纳米粒子的化学偶联。我们的研究结果表明,共轭银和金纳米颗粒对大肠杆菌和黑杆菌都有较大的抑制作用。上述金属偶联物的最小抑菌浓度(MIC)稳定,MIC为1 mM。将金纳米粒子和银纳米粒子偶联物对大肠杆菌和黑孢杆菌的抑菌活性进行对比分析,其抑菌活性分别为2.0±0.01 cm和2.32±0.04 cm,差异无统计学意义(P = 0.85)。综上所述,两种不同纳米材料的组合具有良好的抑菌效果,为今后研究不同纳米材料的组合抑菌活性提供了依据。
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引用次数: 1
Horizontal Gene Transfer: Generating Antibiotic-resistant Bacteria 水平基因转移:产生耐抗生素细菌
Pub Date : 2022-04-15 DOI: 10.36922/itps.v4i1.66
Mohamad Amin Awang, T. Ismail, Thangavel, Lakshmipriya, Subash, C., B., Gopinath, SUMITHA
This study aims to understand the gene mobility and its benefits. In this experiment, we transferred the significant gene horizontally under the appropriate condition and generated an antibiotic-resistant bacterial strain. The process of gene mobility is known as horizontal gene transfer, in which three different modes have been acknowledged that are transduction, transformation, and conjugation. Conjugation is a simple natural occurrence of cell-to-cell contact for transferring gene. The gene sequence that was analyzed in this study is responsible for tetracycline resistance in Proteus mirabilis; the gene was transferred horizontally to Klebsiella pneumoniae. Two methods were used for the conjugation, namely, plate- and broth-mating. The conjugation results were analyzed statistically, where events of probability across the time intervals at the highest spectrophotometric absorbance of 0.43 are tabulated. Broth mating was performed in 25 samples and the probability of an event is successful at P = 0.88. Further, broth mating was accredited to be better than plate-mating as claimed with a 95% confidence interval that yields the value of Z normal test of 4.49. This study suggests a feasible method for generating drug-resistant bacterial strains for use in medical research and industrial applications.
本研究旨在了解基因迁移及其益处。在本实验中,我们在适当的条件下水平转移显著基因,产生了耐药菌株。基因迁移的过程被称为水平基因转移,其中有三种不同的模式被认为是转导、转化和接合。接合是一个简单的自然发生的细胞间接触转移基因。本研究分析的基因序列与变形杆菌对四环素的耐药性有关;该基因水平转移到肺炎克雷伯菌。结合的方法有两种,即板配和焖配。对共轭结果进行统计分析,其中在最高分光光度吸光度为0.43的时间间隔内的概率事件被制表。在25个样本中进行了肉汤交配,事件成功的概率为P = 0.88。此外,肉汤配种被认为比盘子配种更好,95%的置信区间产生Z正态检验值为4.49。本研究提出了一种产生耐药菌株的可行方法,可用于医学研究和工业应用。
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引用次数: 0
Geriatric Oral Health: The Role of Oral Disease Prevention in Vulnerable Patients 老年口腔健康:口腔疾病预防在弱势患者中的作用
Pub Date : 2021-06-04 DOI: 10.36922/ITPS.V4I1.966
M. Goldberg
Prevention of oral diseases plays a crucial role in maintaining the health of vulnerable patients. In this context, vulnerable patients include the adults with no or restricted access to dental treatments, adults above the age of 65 years, and adults residing in Établissement d’hébergement pour personnes âgées dépendantes (EHPADs), which is a type of nursing home for dependent elderly people in France. These vulnerable patients display frailty and/or may need specialized treatment. In addition, oral disease prevention of those living in economically weak countries is equally important. As the global population is increasing at an annual rate of 1.7% while the population of those over 65 years rises at a rate of 2.5%, it is expected that the adults older than 80 years will make up of nearly 20% of the world population in the near future. Therefore, it is without a doubt that early prevention is an important and effective approach to minimize the prevalence of oral disease in the aged population, thereby reducing the related economic repercussions. In general, four levels of prevention have been defined [1,2]. The four levels of prevention are as follows: • Primary prevention aims to prevent the occurrence of a disease or an injury. • Secondary prevention aims to reduce the spread of an already established disease or a progressing disease in a population. It should reduce the impact of a disease or injury that has already occurred or abrogate the progression of a disease and deterioration. • Tertiary prevention aims to reduce the symptoms and complications of a disease and impact of an ongoing illness to improve patient’s functional abilities, quality of life, and life expectancy. Despite that, there is still a risk of recurrence of the disease. Tertiary prevention focuses on the prevention of an already established disease or a progressing disease. • Quaternary prevention aims to identify patients at risk of over-medicalization and suggest interventions that are ethically acceptable, thereby protecting patients from unnecessary medical interventions.
预防口腔疾病对维持弱势病人的健康起着至关重要的作用。在这方面,易受伤害的病人包括无法或受限制获得牙科治疗的成年人、65岁以上的成年人和居住在Établissement d ' hsamberment pour persones 个人 个人获得自由的限期)的成年人,这是法国为受抚养的老年人提供的一种养老院。这些易受伤害的患者表现出虚弱和/或可能需要专门治疗。此外,预防生活在经济薄弱国家的人的口腔疾病也同样重要。由于全球人口以每年1.7%的速度增长,而65岁以上人口以2.5%的速度增长,预计在不久的将来,80岁以上的成年人将占世界人口的近20%。因此,毫无疑问,早期预防是减少老年人口口腔疾病患病率的重要而有效的方法,从而减少相关的经济影响。一般来说,已经定义了四个级别的预防[1,2]。预防的四个级别如下:•初级预防的目的是防止疾病或伤害的发生。•二级预防的目的是减少已经形成的疾病或正在发展的疾病在人群中的传播。它应该减少已经发生的疾病或损伤的影响,或消除疾病的进展和恶化。•三级预防旨在减少疾病的症状和并发症以及持续疾病的影响,以改善患者的功能能力、生活质量和预期寿命。尽管如此,这种疾病仍有复发的危险。三级预防侧重于预防已经形成的疾病或正在发展的疾病。•四级预防旨在确定面临过度用药风险的患者,并提出道德上可接受的干预措施,从而保护患者免受不必要的医疗干预。
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引用次数: 0
Coronavirus Disease 2019: An Overview of the Complications and Management 2019冠状病毒病:并发症及治疗概述
Pub Date : 2021-05-03 DOI: 10.36922/ITPS.V4I1.1037
Huimin Shao, Hany Sadek Ayoub Ghaly, P. Varamini
The severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) is the causative agent of coronavirus disease 2019 (COVID-19). Since the first report of COVID-19 emerging in Wuhan, China, authorities in 216 countries and territories have reported about 47.3 million COVID-19 cases and 1.2 million deaths. The WHO guidelines for the management of COVID-19 are very limited to recommendations for managing symptoms and advice on careful management of pediatric patients, pregnant women, and patients with underlying comorbidities. There is no approved treatment for COVID-19 and guidelines vary between countries. In this review, first, a brief overview is provided on the basic knowledge about the virus, clinical features of the disease, and different diagnostic methods. Then, the relationship between COVID-19, various body systems, and other complications is discussed. Finallly, different management strategies are discussed, including those drawn on computational chemistry analyses, pre-clinical investigations, and clinical trials which involve pharmacological and non-pharmacological interventions. In conclusion, despite the recent approval of different vaccine candidates, more virological characteristics of SARS-CoV-2 are required to be explored, which may result in the discovery of more potential therapeutic targets leading to safer and more effective treatment to COVID-19.
严重急性呼吸综合征冠状病毒-2 (SARS-CoV-2)是2019冠状病毒病(COVID-19)的病原体。自中国武汉首次报告COVID-19以来,216个国家和地区的当局报告了约4730万例COVID-19病例和120万例死亡。世卫组织COVID-19管理指南非常局限于对症状管理的建议以及对儿科患者、孕妇和有潜在合并症的患者进行仔细管理的建议。目前还没有批准的COVID-19治疗方法,各国的指南也各不相同。本文首先对该病毒的基本知识、临床特点及不同的诊断方法作一综述。然后,讨论了COVID-19与各种身体系统以及其他并发症之间的关系。最后,讨论了不同的管理策略,包括计算化学分析、临床前调查和涉及药物和非药物干预的临床试验。总之,尽管最近批准了不同的候选疫苗,但需要探索SARS-CoV-2的更多病毒学特征,这可能导致发现更多潜在的治疗靶点,从而更安全,更有效地治疗COVID-19。
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引用次数: 1
Skin Ultrasound as a Diagnostic Approach for Non-melanocytic Benign Skin Tumors 皮肤超声诊断非黑素细胞良性皮肤肿瘤的研究
Pub Date : 2020-12-30 DOI: 10.36922/itps.v3i2.944
María Elena Del Prado, R. Ruiz-Villaverde, P. Giavedoni, Ana Rodríguez, D. Vidal, G. Roustán, F. Queipo, J. Aneiros-Fernández, Paola Castillo, E. Ruiz, I. Moysset, Lola Suárez, L. Nájera, Fernando Alfajeme
Background. The diagnostic imaging techniques in dermatology, such as skin ultrasound, could improve the diagnosis of non-melanocytic benign tumor lesions, especially those of intradermal and subcutaneous nature. Objective. The general objective of this study was to evaluate the validity and diagnostic safety of high-frequency ultrasound as a diagnostic test for non-melanocytic benign skin tumor detection. The specific objectives were to measure the sensitivity and specificity of ultrasound as a measure of the validity relative to the gold-standard test – diagnostic-therapeutic biopsy. Methods. This study was carried out between January 2017 and June 2019. The patients (n = 641) included in this study comprised of 318 women and 323 men who were between 48 and 74 years. All of them underwent an ultrasound examination of the skin tumor in the dermatology clinic, the removal of the non-melanocytic tumor, and a final histopathological examination. Results. The skin ultrasound has a sensitivity and specificity of 93% and 88%, respectively. Furthermore, the positive and negative predictive values of using skin ultrasound are 84% and 94%, respectively. Conclusion. Skin ultrasound is a diagnostic technique with high sensitivity and specificity in the diagnosis of non-melanocytic skin tumors.
背景。皮肤影像学诊断技术,如皮肤超声,可以提高非黑素细胞性良性肿瘤病变的诊断,特别是皮内和皮下肿瘤的诊断。目标。本研究的总体目的是评价高频超声作为非黑素细胞良性皮肤肿瘤诊断试验的有效性和诊断安全性。具体目的是测量超声的敏感性和特异性,作为相对于金标准测试-诊断-治疗活检的有效性的测量。方法。该研究于2017年1月至2019年6月期间进行。本研究纳入的患者(n = 641)包括318名女性和323名男性,年龄在48至74岁之间。所有患者均在皮肤科门诊接受了皮肤肿瘤的超声检查,非黑素细胞肿瘤切除,最后进行了组织病理学检查。结果。皮肤超声的敏感性和特异性分别为93%和88%。此外,使用皮肤超声的阳性预测值为84%,阴性预测值为94%。结论。皮肤超声诊断是非黑素细胞性皮肤肿瘤具有较高的灵敏度和特异性。
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引用次数: 1
Community Pharmacy Services During the COVID-19 Pandemic: A Systematic Review COVID-19大流行期间的社区药房服务:系统综述
Pub Date : 2020-12-21 DOI: 10.36922/itps.v3i2.971
A. Mendonça, C. Santos, Isabel C. Pinto
Background. As a central part of the healthcare system, the community pharmacies are afflicted by the repercussions of the pandemic. Therefore, they have to adapt their services according to the needs of their communities. Objective. This article presents a systematic review with the aim to identify the additional services that community pharmacies are providing during the COVID-19 pandemic. Methods. The PubMed, Web of Science, and ScienceDirect databases were searched systematically for relevant articles between December 2019 and April 2020, using “Community Pharmacy,” “Services,” “COVID-19,” “Coronavirus,” and “Pandemic” as the keywords. Fifty-nine articles in English, Portuguese, or Spanish were obtained and after applying the filtering criteria, nine of them were selected and included in the study. Results. Community pharmacies should provide pharmaceutical services that are according to the needs of the communities. During the COVID-19 pandemic, changes of these services must be in line with the common goal of preventing the spread of the disease. In addition to the pre-existing services such as medication dispensing and personalized care, community pharmacists must promote other types of services, for example, informing, advising, and educating the community, maintaining a stable supply of pharmaceuticals and health products, and screening of suspected cases. Conclusion. While remaining engaged in the coordinated efforts, community pharmacists should apply innovations in their practices to help prevent the spread of coronavirus.
背景。作为医疗保健系统的核心部分,社区药房受到疫情影响。因此,他们必须根据社区的需要调整他们的服务。目标。本文提出了一项系统综述,旨在确定社区药房在COVID-19大流行期间提供的额外服务。方法。以“社区药房”、“服务”、“COVID-19”、“冠状病毒”和“大流行”为关键词,系统检索了2019年12月至2020年4月期间PubMed、Web of Science和ScienceDirect数据库的相关文章。获得英语、葡萄牙语或西班牙语的59篇文章,在应用筛选标准后,选择其中9篇纳入研究。结果。社区药房应根据社区需求提供药学服务。在2019冠状病毒病大流行期间,这些服务的变化必须符合防止疾病传播的共同目标。除了药物配发和个性化护理等现有服务外,社区药剂师还必须促进其他类型的服务,例如向社区提供信息、咨询和教育,保持药品和保健产品的稳定供应,以及筛查疑似病例。结论。社区药剂师在继续参与协调工作的同时,应在实践中应用创新,帮助防止冠状病毒的传播。
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引用次数: 4
Epidemiological Model for COVID-19 in China 中国COVID-19流行病学模型
Pub Date : 2020-12-11 DOI: 10.36922//itps.v3i2.938
Shanshan Wu, P. Sun, Ruiling Li, Yanli Wang, Lifang Jiang, J. Deng
Background. The epidemic of coronavirus disease 2019 (COVID-19) caused by the SARS-CoV-2 first broke out in Wuhan, Hubei Province in China, and then spread quickly worldwide. Objective. This study aimed to dissect the spread and end of the epidemic in China with a precise mathematical model. Methods. Various data were obtained from the official websites of the Chinese National Health from January 20 to July 8, 2020. The Chinese study participants were divided into three groups, namely, Hubei (including Wuhan), nationwide without Hubei, and Henan. The basic reproduction number (R0), effective reproduction number (Rt), and gender and age ratio of COVID-19 were calculated, and the epidemic’s predicted curves or fitting curves with peak time and end time were plotted with SIR model. These predicted curves were compared with actual scatter plots. Results. The fitting curve of the Hubei group showed a parabola with a peak on February 18, 2020, with 51,673 cases and the gradual decrease of infected patients, which culminates with a downhill after May 2020. During early outbreak, the highest recorded R0 was 6.13, which declined gradually forming a S-type curve, and it approached zero in early May. Similar to Hubei group, the fitting curve of the nationwide without Hubei group also showed a parabola, recording a peak of 9145 cases on February 10, 2020. At first, its R0 was as high as 2.35 but declined to zero in early April. The epidemic in the Henan group also reached its peak on February 10, 2020, and ended in early April as well. Conclusion. The epidemic development of COVID-19 in China followed the shape of parabolic curves. This model provides insights into how to strategize for epidemic control.
背景。由SARS-CoV-2引起的2019冠状病毒病(COVID-19)疫情首先在中国湖北省武汉市爆发,随后在全球迅速蔓延。目标。本研究旨在用精确的数学模型剖析疫情在中国的传播和终结。方法。2020年1月20日至7月8日,从中国国家卫生官网获取各项数据。中国的研究参与者被分为三组,即湖北(含武汉)、全国(不含湖北)和河南。计算COVID-19的基本繁殖数(R0)、有效繁殖数(Rt)、性别和年龄比,用SIR模型绘制疫情的预测曲线或峰值时间和结束时间的拟合曲线。这些预测曲线与实际的散点图进行了比较。结果。湖北组拟合曲线呈抛物线型,在2020年2月18日达到高峰,确诊病例51673例,感染者逐渐减少,5月后呈下降趋势。疫情早期最高记录R0为6.13,呈s型曲线逐渐下降,5月初趋近于零。与湖北组相似,全国无湖北组拟合曲线也呈抛物线型,2月10日达到9145例的峰值。它的R0起初高达2.35,但在4月初降至零。河南组疫情也在2020年2月10日达到高峰,4月初结束。结论。新冠肺炎疫情在中国的发展呈抛物线型。该模型为如何制定流行病控制战略提供了见解。
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引用次数: 1
Importance and Feasibility of Point-of-care Testing in Takayasu’sArteritis 高须性肠炎即时检测的重要性和可行性
Pub Date : 2020-04-30 DOI: 10.36922/itps.v3i1.906
S. Mehta, V. Dhawan
Takayasu’s arteritis (TAK) is known to be a unique, rare, and chronic vasculitis disease that affects large elastic arteries such as aorta and its major branches. TAK is characterized by adventitial thickening, weak pulses and ocular disturbances. The prognosis and diagnosis of TAK are challenging due to the non-specific, silent, or paucisymptomatic presentation of the disease. The effective understanding of TAK lies with the timely recognition of the symptoms and a rapid diagnosis of the disease. Point-of-care testing (POCT) is vital for the quick and reliable detection of parameters near bedside for disease diagnosis, assessment, monitoring, and therapeutics management. Ultrasonography is the most reliable POCT technique. Moreover, erythrocyte sedimentation rate and C-reactive protein assay are the two most valuable non-imaging POCT tests used to determine inflammation and onset of the disease. Other potential biomarkers such as matrix metalloproteinases, soluble receptor for advanced glycation end products, interleukin (IL)-6, and IL-18 have also been advocated for tracking the progression of TAK. Furthermore, vasculitis associated-anti-neutrophil cytoplasmic antibodies have also been reported to reflect the inflammatory phase of the disease. Therefore, the development of POCT based on these blood-based biomarkers may help in quick clinical decision-making for early diagnosis of TAK and targeted therapeutics to improve clinical outcome in patients suffering from this debilitating disease.
Takayasu动脉炎(Takayasu’s arteritis, TAK)是一种罕见的慢性血管炎,主要影响主动脉及其主要分支等大弹性动脉。TAK的特点是角膜外膜增厚、脉搏微弱和眼障碍。由于疾病的非特异性、沉默或无症状表现,TAK的预后和诊断具有挑战性。对TAK的有效认识在于对症状的及时识别和对疾病的快速诊断。即时检测(POCT)对于快速可靠地检测床边附近的疾病诊断、评估、监测和治疗管理参数至关重要。超声检查是最可靠的POCT技术。此外,红细胞沉降率和c反应蛋白测定是用于确定炎症和疾病发病的两种最有价值的非成像POCT检查。其他潜在的生物标志物,如基质金属蛋白酶、晚期糖基化终产物可溶性受体、白细胞介素(IL)-6和IL-18也被提倡用于跟踪TAK的进展。此外,血管炎相关的抗中性粒细胞细胞质抗体也被报道反映了疾病的炎症期。因此,基于这些血液生物标志物的POCT的发展可能有助于快速临床决策,早期诊断TAK和靶向治疗,以改善患有这种使人衰弱的疾病的患者的临床结果。
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引用次数: 1
Long-term Administration of Lovastatin and Rivastigmine: An In Vivo Evaluation on Cognitive Functions and Brain Acetylcholinesterase Activity 长期服用洛伐他汀和利瓦斯汀:对认知功能和脑乙酰胆碱酯酶活性的体内评价
Pub Date : 2020-02-26 DOI: 10.36922/itps.v2i2.904
N. Badruddeen, J. Akhtar, M. Arif, Mohammad Irfan Khan, M. Mujahid, Mohammad Ahmad
Background. There is not much evidence illustrating that statins could be responsible for memory loss or dementia, although increased exposure to statins has been reported to cause cognitive side effects. The present study investigated the effect of lovastatin in combination with rivastigmine on cognitive function as well as brain acetylcholinesterase (AChE) activity in normal mice. Methods. The mice were categorized into four groups, and they were treated with normal saline, lovastatin, rivastigmine, and the combination of lovastatin and rivastigmine, respectively, by oral administration for 60 days. The treatment effect on cognitive functions was assessed by behavioral tests, namely, the passive avoidance test and spontaneous alternation test, as well as the measurement of brain AChE activity by Ellman’s method. Results. In this study, a significant reduction (P < 0.01) of brain AChE activity and positive effects (P < 0.01) on cognitive functions was observed in mice treated with the combination of lovastatin and rivastigmine as compared to rivastigmine alone. However, no significant differences (P < 0.05) were observed on brain AChE activity as well as cognitive functions in mice treated with lovastatin when compared with those treated with normal saline. Conclusion. This study suggested that lovastatin did not contribute to any improvements in cognitive functions and brain AChE activity, but it potentiated the effect of rivastigmine.
背景。没有太多证据表明他汀类药物可能导致记忆丧失或痴呆,尽管有报道称增加他汀类药物的使用会导致认知方面的副作用。本研究探讨了洛伐他汀联合利瓦斯汀对正常小鼠认知功能及脑乙酰胆碱酯酶(AChE)活性的影响。方法。将小鼠分为4组,分别给予生理盐水、洛伐他汀、利伐他汀、洛伐他汀与利伐他汀联合口服,疗程60 d。通过行为测试,即被动回避测试和自发交替测试来评估治疗对认知功能的影响,并采用Ellman法测量脑乙酰胆碱酯酶活性。结果。在本研究中,洛伐他汀和利伐他明联合治疗小鼠脑AChE活性显著降低(P < 0.01),对认知功能有积极影响(P < 0.01)。然而,与生理盐水相比,洛伐他汀治疗小鼠脑AChE活性和认知功能无显著差异(P < 0.05)。结论。本研究提示洛伐他汀对认知功能和脑乙酰胆碱酯酶活性没有任何改善作用,但它增强了雷伐他汀的作用。
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引用次数: 1
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INNOSC Theranostics and Pharmacological Sciences
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