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Correlation between Secreted Aspartyl Protease-5 (SAP5) on Increasing Vaginal Acidity in Vulvovaginal Candidiasis 外阴阴道念珠菌病患者分泌天冬氨酸蛋白酶-5 (SAP5)与阴道酸度升高的关系
IF 0.4 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-08-11 DOI: 10.55561/ajhr.v2i2.116
Ikatan Dokter, Indonesia Wilayah, Jawa Timur, Nur Sophia, Matin, Regina Ayu Fristiyanti, Safrina Dewi, N. Nurdiana, S. Santoso, B. Rahardjo
Introduction: Vulvovaginal candidiasis (VVC) is an infection of the vaginal mucosa that extends to the vulva due to excessive growth of Candida albicans, causing a progressive decrease of Lactobacillus spp., as the main of normal flora. Decrease in the number of Lactobacillus spp. causes a reduction of lactic acid production that it was causing increasing vaginal pH. The increase in pH is due to the progressive growth of C. albicans colonies in the vaginal mucosa. In addition, the mechanism of candidiasis is also influenced by the secretion of virulence factors by C. albicans. Secreted Aspartyl Protease-5 (SAP5) is the dominant virulence factor that plays a role in changing the morphology of yeast cells into hyphae. This study aims to identify the correlation between SAP5 levels and vaginal pH.Material and Methods: This research was conducted in vivo using a sample of Rattus norvegicus with a posttest randomized experimental group design approach. This study has two groups, i.e., Negative Control (NC) and Positive Control group (PC). SAP5 and pH samples were taken from vaginal fluids and then measured using ELISA and a digital pH meter. The statistical analysis used was Pearson Correlation to analyze the correlation between SAP5 and pH levels.Results: There was a strong correlation (R=0.846) that means the increase of SAP5 is related to the increase of vaginal acidity in the PC group.Conclusion: The increase in SAP5 levels is directly followed by an increase in the pH value of vaginal fluids,
简介:外阴阴道念珠菌病(VVC)是由于白色念珠菌过度生长导致阴道粘膜延伸到外阴的感染,导致作为正常菌群主要的乳酸杆菌逐渐减少。乳酸菌数量的减少导致乳酸产量的减少,从而引起阴道pH值的升高。pH值的升高是由于阴道粘膜中白色念珠菌菌落的逐渐增长。此外,念珠菌病的发病机制还受白色念珠菌分泌毒力因子的影响。分泌性天冬氨酸蛋白酶-5 (SAP5)是酵母细胞形态转变为菌丝的主要毒力因子。本研究旨在探讨SAP5水平与阴道ph的相关性。材料与方法:本研究采用褐家鼠体内实验,采用后试验随机分组设计方法。本研究分为阴性对照组(NC)和阳性对照组(PC)两组。从阴道液中提取SAP5和pH样品,然后使用ELISA和数字pH计进行测量。统计学分析采用Pearson Correlation分析SAP5与pH值的相关性。结果:PC组SAP5升高与阴道酸度升高有很强的相关性(R=0.846)。结论:SAP5水平的升高直接伴随着阴道液pH值的升高。
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引用次数: 0
Suspicion of Duchenne Muscular Dystrophy in A 7-Year-Old Madurese Boy: A Rare Case Report 一名7岁男童疑似杜氏肌营养不良:罕见病例报告
IF 0.4 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-08-11 DOI: 10.55561/ajhr.v2i2.88
Suci Rizalah Islamiyah, Garata Dwi, Yulia Nurul Putri, Suci Rizalah
Introduction: Duchenne Muscular Dystrophy (DMD) is an X-linked disorder presenting in early childhood and characterized by proximal muscle weakness and calf hypertrophy in affected boys associated with a functional deficiency of dystrophin. The incidence of these cases reached 1 in 3500-6000 male births. Research at RSUPN Dr Cipto Mangunkusumo (RSCM) showed that DMD is the second most frequent neuromuscular disorder in children regardless there is no prevalence data available yet in Indonesia. It is quite complicated to diagnose DMD due to the limited facilities of genetic testing and its high cost.Case Presentation: A 7-year-old boy came with the main complaint of weakness in both legs progressively two years before admission. He had to hold onto the floor and then both knees when started to stand. There was a history of motor and speech delay but family history was denied. Vital signs and nutritional status were within normal. Laboratory examination revealed significantly elevated levels of CK, ALT, and AST. The EMG result supported the presence of myopathy. Due to a lack of facilities, genetic testing or muscle biopsy could not be done. He received prednisone once a day with a 14 mg dose and was scheduled to attend regular physiotherapy.Conclusion: In a limited facilities area, the clinician should have a suspicion of DMD not only by anamnesis and clinical features, but also by considering the elevated levels of CK and myopathies on EMG.
杜氏肌营养不良症(DMD)是一种儿童早期出现的x连锁疾病,其特征是受影响男孩的近端肌肉无力和小腿肥大,并伴有肌营养不良蛋白的功能缺陷。这些病例的发病率达到每3500至6000名男婴中有1例。RSUPN Cipto Mangunkusumo博士(RSCM)的研究表明,DMD是儿童中第二大最常见的神经肌肉疾病,尽管印度尼西亚尚无患病率数据。由于基因检测设备有限,且费用较高,DMD的诊断相当复杂。病例介绍:一名7岁男孩,入院前两年以两腿逐渐无力为主。当他开始站立时,他不得不抓住地板,然后双膝着地。有运动和语言迟缓史,但否认有家族病史。生命体征及营养状况均在正常范围内。实验室检查显示CK、ALT和AST水平显著升高,肌电图结果支持肌病的存在。由于缺乏设备,无法进行基因检测或肌肉活检。他每天接受一次14毫克剂量的强的松治疗,并定期接受物理治疗。结论:在有限的设施区域,临床医生不仅应通过记忆和临床特征来怀疑DMD,还应考虑肌电图上CK水平升高和肌病。
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引用次数: 0
Shortages of Medical Doctors in Indonesia, Is It True? 印尼医生短缺,是真的吗?
IF 0.4 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-08-11 DOI: 10.55561/ajhr.v2i2.121
Sutrisno, MD, PhD, OG (REI)
All parts of Indonesia need medical doctors, but it is not a simple thing to be solved. The world of medicine in Indonesia faces many internal problems, specifically regarding medical doctor distribution. Where do the medical doctors in Indonesia reside? Recently many areas in Indonesia experienced a ratio between doctors and population of more than 1 : 1000.   Data   From the Indonesia   Medical   Council   (KKI)   and   Indonesia   Medical doctor association (IDI) in the year 2023 total number of medical doctors are  214,878 doctors, dominated by general physician 165,453 doctors, and followed by doctors specialist  49,425. Total dentists are 41,940, and dentist specialists are 5,201. The fundamental problems, according to population ratios, is related to geographical and demographic handicap because Indonesia is an archipelago country with more than 17,000 islands with more than 280 million populations, with many specific problems in access,  communication, transportation system, socio-economic, cultural, and leadership.
印尼各地都需要医生,但这不是一件容易解决的事情。印度尼西亚的医学界面临许多内部问题,特别是在医生分配方面。印度尼西亚的医生住在哪里?最近,印度尼西亚许多地区的医生与人口的比例超过1∶1000。来自印度尼西亚医学委员会(KKI)和印度尼西亚医生协会(IDI)的数据显示,2023年医生总数为214,878名医生,以普通医生165,453名医生为主,其次是专科医生49,425名。牙医共有41,940名,专科牙医有5,201名。根据人口比例,根本问题与地理和人口障碍有关,因为印度尼西亚是一个拥有17,000多个岛屿的群岛国家,人口超过2.8亿,在准入,通信,交通系统,社会经济,文化和领导方面存在许多具体问题。
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引用次数: 0
Implementation of Early Recovery After Caesarean Surgery Protocol in Floating Hospital (Case Series) 漂浮医院剖宫产术后早期康复方案的实施(病例系列)
IF 0.4 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-08-11 DOI: 10.55561/ajhr.v2i2.67
Akhyar Nur Uhud, B. Welantika, Senda Sulvain, T. Y. Aden
Introduction: Enhanced Recovery After Caesarean Surgery (ERACS) is a new concept that combines various evidence-based perioperative care to reduce post-operative complications and accelerate patient recovery after Caesarean Surgery (C-Section). The advantages of the ERACS Protocol, including accelerating patients' recoveries, shortening hospital stays, and reducing post-operative complications, make it suitable to be applied in floating hospitals. The problem is whether this protocol can be applied if it is carried out in a floating hospital with all its limitations. We would like to present our case series with modified ERACS protocol in Floating Hospital Ksatria Airlangga.Case Presentation: We present 4 patients scheduled for elective C-Section. Neuraxial opioids with low-dose morphine, the most frequently used technique in ERACS, were not administered due to its unavailability in Ksatria Airlangga Floating Hospital. We provide pre-emptive analgesia and multimodal analgesia to obtain adequate perioperative analgesia. All patients were admitted to the nearest public health centre for post-operative observation and discharged after 1 to 2 days. Satisfaction was achieved in all patients without any significant postoperative complications.Conclusion: The ERACS protocols’ main goal can be achieved even under limited conditions, but several adjustments are required according to the available resources.
剖宫产术后增强恢复(Enhanced Recovery After Caesarean Surgery, ERACS)是一种结合各种循证围手术期护理的新概念,旨在减少剖宫产术后并发症,加速患者恢复。ERACS方案具有加速患者康复、缩短住院时间、减少术后并发症等优点,适合在浮动医院推广应用。问题是,如果在具有所有局限性的流动医院执行该协议,是否可以适用。我们想介绍我们在Ksatria Airlangga浮动医院采用修改后的ERACS方案的病例系列。病例介绍:我们报告了4例计划择期剖腹产的患者。由于Ksatria Airlangga流动医院无法提供低剂量吗啡,因此没有使用ERACS中最常用的低剂量吗啡的轴向阿片类药物。我们提供了先发制人的镇痛和多模式的镇痛,以获得足够的围手术期镇痛。所有患者均在最近的公共卫生中心接受术后观察,1 ~ 2天后出院。所有患者均满意,无明显术后并发症。结论:在有限的条件下,ERACS协议的主要目标是可以实现的,但需要根据现有资源进行一些调整。
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引用次数: 0
Comparison of the Effects of Dienogest and Leuprolide Acetat on Serum Interferon (IFN-Ɣ) Levels in a Mouse Model of Endometriosis (Mus musculus) 双炔诺孕素和醋酸左炔诺列酯对子宫内膜异位症小鼠血清干扰素-Ɣ水平影响的比较
IF 0.4 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-08-11 DOI: 10.55561/ajhr.v2i2.111
Ikatan Dokter, Indonesia Wilayah, Jawa Timur, María Antonia, Barbara Batu Mali, Siskanita Nur Fitriana, S. Sutrisno, H. Khotimah, Wayan Arsana Wiyasa, W. Indrawan
Introduction: Endometriosis is a medical condition in which there is abnormal growth of tissue resembling the endometrium outside the uterus. It can cause symptoms of pain and/or infertility. The current medical therapy focuses on reducing estradiol levels or stimulating progesterone response. One of the most effective options for medical treatment is the use of GnRH analogs. Dienogest have a direct anti-inflammatory effect on endometriotic stromal cells. However, a comparison of the anti-inflammatory effects of these drugs on IFN-Ɣ has not been previously investigated. Therefore, this study aims to compare the effects of reducing IFN-Ɣ by both Dienogest and Leuprolide Acetat in a mouse model.Material and Methods: This study employed a post-test only control group design and involved 4 groups, namely the negative control group, positive control group, and two treatment groups: one group administered Dienogest at a dosage of 0.0052 milligrams per day for 14 days, and the other administered Leuprolide Acetat at a dosage of 0.00975 milligrams once every 5 days for a period of 14 days. Serum IFN-Ɣ levels were measured using Enzyme-Linked Immunosorbent Assay (ELISA). The data were subsequently analyzed using IBM SPSS 25 with One-Way ANOVA test.Results: This study demonstrated that Leuprolide Acetat significantly decreased serum levels of IFN-Ɣ, whereas Dienogest actually increased the levels .Conclusion: In a mouse model of endometriosis (Mus musculus), Leuprolide Acetat effectively reduced the levels of IFN-Ɣ (pro-inflammatory). Conversely, Dienogest increased the levels of IFN-Ɣ (anti-inflammatory) in the mouse model of endometriosis.
简介:子宫内膜异位症是一种医学状况,在子宫外有类似子宫内膜的组织异常生长。它可以引起疼痛和/或不孕的症状。目前的医学治疗侧重于降低雌二醇水平或刺激黄体酮反应。最有效的医疗选择之一是使用GnRH类似物。孕酮对子宫内膜异位症间质细胞有直接的抗炎作用。然而,这些药物对IFN-Ɣ的抗炎作用的比较以前没有研究过。因此,本研究旨在比较Dienogest和Leuprolide Acetat在小鼠模型中降低IFN-Ɣ的作用。材料与方法:本研究采用单试验后对照组设计,共分为阴性对照组、阳性对照组和2个治疗组,其中一组给药量为0.0052 mg / d,连用14天;另一组给药量为0.00975 mg / d,连用14天。采用酶联免疫吸附试验(ELISA)测定血清IFN-Ɣ水平。随后使用IBM SPSS 25对数据进行单因素方差分析。结果:本研究表明醋酸左连络酯能显著降低血清中IFN-Ɣ的水平,而地诺孕素却能提高血清中IFN的水平。结论:在子宫内膜异位症(小家鼠)小鼠模型中,醋酸左连络酯能有效降低IFN-Ɣ(促炎)水平。相反,Dienogest增加了子宫内膜异位症小鼠模型中IFN-Ɣ(抗炎)的水平。
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引用次数: 0
The Effect of Calcium on Biomarkers of Ovarian Fertility in Premature Ovarian Failure: A Systematic Review 钙对卵巢早衰患者卵巢生育能力生物标志物的影响:系统综述
Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-08-11 DOI: 10.55561/ajhr.v2i2.29
Sutrisno Sutrisno, None Tri Aji Bangun Nuswantoro
Introduction: Premature ovarian failure (POF) is a condition in which ovarian function decreases or follicles are depleted in women aged less than 40 years. Calcium, along with vitamin D, is a mineral with many benefits for the reproduction system. This review is written to observe the effect of calcium on ovarian fertility biomarkers in premature ovarian failure. Methods: The literatures search was conducted utilizing numerous search engines, namely PubMed, Cochrane, Springer, Science Direct, Nature, and Google Scholar. Article publication year was restricted from 2016 to 2022. Article search keywords included “calcium”, “vitamin D”, “premature ovarian failure”, “premature ovarian insufficiency”, “amenorrhoea”, “ovarian reserve biomarkers”, “estradiol”, “follicle stimulating hormone”, and “luteinizing hormone”. Article selection was performed using the preferred reporting items for systematic review and meta-analysis protocols guidelines (PRISMA-P). The first author’s name, publication year, samples number, age range of subjects, duration of data collection, geographical setting, study design, and conclusions of research results were extracted from the selected paper. Results: 8397 articles were obtained from the six search engines. 13 articles met the inclusion criteria. Research conducted by Iran reported a significant correlation between vitamin D levels and AMH levels (p<0.001). In comparison, the research in Bangladesh showed a significant positive correlation between vitamin D levels and AMH levels (r=0.433; p=0.001) and vitamin D levels and AFC values (r=0.419; r=0.001). However, 11 other researchers reported contradictory results. Conclusion: The calcium and vitamin D effect on reproductive health related to POF occurrence is still inconsistent. Therefore, observational and experimental research is needed to analyze this topic.
简介:卵巢早衰(POF)是指年龄小于40岁的女性卵巢功能下降或卵泡衰竭的一种情况。钙和维生素D是一种矿物质,对生殖系统有很多好处。本综述旨在观察钙对卵巢早衰患者卵巢生育能力生物标志物的影响。方法:利用PubMed、Cochrane、Springer、Science Direct、Nature、Google Scholar等多个搜索引擎进行文献检索。文章发表年份限制为2016年至2022年。文章搜索关键词包括“钙”、“维生素D”、“卵巢早衰”、“卵巢早衰不全”、“闭经”、“卵巢储备生物标志物”、“雌二醇”、“促卵泡激素”、“黄体生成素”。采用系统评价和荟萃分析方案指南(PRISMA-P)的首选报告项目进行文章选择。从所选论文中提取第一作者姓名、发表年份、样本数、受试者年龄范围、数据收集时间、地理环境、研究设计、研究结果结论。结果:在6个搜索引擎中共检索到8397篇文章。13篇文章符合纳入标准。伊朗进行的研究报告了维生素D水平与AMH水平之间的显著相关性(p<0.001)。相比之下,孟加拉国的研究显示维生素D水平与AMH水平之间存在显著的正相关(r=0.433;p=0.001)、维生素D水平和AFC值(r=0.419;r = 0.001)。然而,其他11名研究人员报告了相互矛盾的结果。结论:钙和维生素D对生殖健康的影响与POF发生的关系尚不一致。因此,需要通过观察和实验研究来分析这一课题。
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引用次数: 0
Genistein Effect on Estrogen Receptor especially Interleukin-6 and Tumor Necrosis Factor-α in Mice Model of Endometriosis: a Systematic Review and Meta-analysis 染料木素对子宫内膜异位症小鼠雌激素受体特别是白细胞介素-6和肿瘤坏死因子-α的影响:系统回顾和荟萃分析
IF 0.4 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-04-29 DOI: 10.55561/ajhr.v2i1.90
Sutrisno Sutrisno, Lovin Destikatari
Introduction: Endometriosis is the endometrial tissue proliferation outside the uterine space. Anti-angiogenic agents from different groups of substances are currently being discussed as promising therapies for the treatment of endometriosis in the future, one of which is therapy using the phytoestrogen genistein. At the molecular level, genistein's effects on cells include inhibition of proliferation, induction of differentiation, apoptosis, and cell arrest in the cell cycle, which are related to the transforming growth factor. Genistein inhibits cell growth by modulating the signal-transforming growth factor pathway.Methods: We searched PubMed, Scopus, Cochrane Library and Proquest from its inception to December 2022 to collect observational and interventional studies of Genistein consumption in endometriosis mice. Two authors independently screened the literature according to the inclusion and exclusion criteria, extracted data, and assessed the risk of bias. Safety analysis was assessed through TNF-α and IL-6 values of estrogen expression.Results: No significant difference in the values of IL-6 and TNF-α in rats with endometriosis that were given genistein at these three doses. However, if analyzed further, the IL-6 outcome compared to the 0.78mg/day dose most affected the IL-6 value between the two groups, and the TNF-α output compared to the 0.78 mg/day dose most affected the TNF-α value between the two groups. So, a genistein dose of 0.78 mg/day can affect IL-6 and TNF-α in mice with endometriosis.Conclusion: Genistein modulated estrogen expression of TNF-α and IL-6 at all doses, but the best dose for its effect was 0.78 mg/day.
简介:子宫内膜异位症是指子宫内膜组织在子宫间隙外增生。来自不同物质的抗血管生成药物目前正在被讨论作为未来治疗子宫内膜异位症的有希望的治疗方法,其中之一是使用植物雌激素染料木素的治疗。在分子水平上,染料木素对细胞的作用包括在细胞周期中抑制增殖、诱导分化、凋亡和细胞阻滞,这些作用都与转化生长因子有关。染料木素通过调节信号转化生长因子途径抑制细胞生长。方法:检索PubMed、Scopus、Cochrane Library和Proquest自成立至2022年12月,收集子宫内膜异位症小鼠染料木素摄入的观察性和干预性研究。两位作者根据纳入和排除标准独立筛选文献,提取数据,评估偏倚风险。通过雌激素表达TNF-α和IL-6值评估安全性。结果:三种剂量染料木素对子宫内膜异位症大鼠IL-6、TNF-α的影响均无显著性差异。然而,如果进一步分析,与0.78mg/天剂量相比,IL-6结局对两组之间IL-6值的影响最大,与0.78mg/天剂量相比,TNF-α输出对两组之间TNF-α值的影响最大。因此,0.78 mg/天的染料木素剂量可以影响子宫内膜异位症小鼠的IL-6和TNF-α。结论:染料木素在各剂量下均可调节TNF-α和IL-6的雌激素表达,但其效果最佳剂量为0.78 mg/d。
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引用次数: 0
Analysis of Screen Based Activity on Digital Eye Strain in School-Age Children in Peniwen Village, Malang, East Java 东爪哇玛琅Peniwen村学龄儿童数字眼疲劳的屏幕活动分析
IF 0.4 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-04-29 DOI: 10.55561/ajhr.v2i1.98
Minarni Wartiningsih
Introduction: The use of digital devices has increased across all age groups and professional fields, making them inseparable from everyday life. This increase in the duration of screen-based activities causes various symptoms of eye health problems. This study aimed to determine the prediction of the relationship and influence between Screen-Based Activity (SBA) and the incidence of Digital Eye Syndrome (DES) in children aged 9-12 years in Peniwen Village, Malang.Material and Methods: This study used a cross-sectional analytical observational design. There were 62 respondents in the research samples, or the same number as the total population. The analysis technique used in this study is the Partial Leas Square (PLS) modeling technique with testing using software such as SmartPLS (v3.2.9).Results: Based on the results of the analysis, obtained t-count (23.821) is greater than the t-table (1.96), meaning that there is a relationship and influence between SBA variables on DES. The correlation coefficient of SBA to DES is positive 0.818 which means the higher the Screen Based Activity, the higher the risk of Digital Eye Strain. The use of handphone (X2) is an indicator of SBA with the highest correlation strength of 88.1%.Conclusion: There is an association between the duration of Screen Based Activity and the incidence of Digital Eye Strain in children. The higher the Screen Based Activity, the higher the risk of Digital Eye Strain. In addition, the use of handphones has the highest correlation in influencing the occurrence of Digital Eye Strain in school-age children in Peniwen Village.
数字设备的使用在各个年龄段和专业领域都有所增加,使它们与日常生活密不可分。看屏幕时间的增加会导致眼睛健康问题的各种症状。本研究旨在预测玛琅彭尼文村9-12岁儿童屏幕活动(Screen-Based Activity, SBA)与数字眼综合征(Digital Eye Syndrome, DES)发病率的关系及影响。材料和方法:本研究采用横断面分析观察设计。调查样本中有62名受访者,与总人口数量相同。本研究中使用的分析技术是偏最小二乘(PLS)建模技术,并使用SmartPLS (v3.2.9)等软件进行测试。结果:根据分析结果,所得t-count(23.821)大于t-table(1.96),说明SBA各变量对DES存在相关性和影响,SBA与DES的相关系数为正0.818,说明Screen Based Activity越高,数字眼疲劳的风险越高。手机使用(X2)是SBA的一个指标,相关强度最高,为88.1%。结论:基于屏幕的活动时间与儿童数字眼疲劳发生率之间存在关联。屏幕活动越频繁,数字眼疲劳的风险就越高。此外,手机使用对培尼文村学龄儿童数码眼疲劳发生的影响相关性最高。
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引用次数: 0
In vitro‒in vivo correlation of oral biodegradable curcumin nanoparticles for sustained treatment regimen of diabetics 口服可生物降解的姜黄素纳米颗粒在糖尿病患者持续治疗方案中的体内外相关性
IF 0.4 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-04-01 DOI: 10.4103/ajprhc.ajprhc_46_23
K. Shailaja, K. Senthilkumaran, Ubaidulla Uthumansha
Background: Curcumin (CUR) has the potential to treat diabetes, but its low oral bioavailability makes it challenging to use in the treatment of chronic conditions. Objectives: To investigate in vitro–in vivo correlation (IVIVC) of oral biodegradable CUR nanoparticles (NPs) for sustained treatment regimen of diabetics. Materials and Methods: In this study, CUR biodegradable NPs were prepared using Box–Behnken design to optimize the concentration of polymer and process parameters. Results: The optimized formulation was prepared using the values obtained from the Box-Behenken method, 2.5 %w/v of polymer, 3 % w/v of TPP, and 2534 rpm of stirring speed and the actual response was observed 192.31±6.82 nm particle size, 84.26±2.87 % of entrapment efficiency, and 95.22±1.81 % of drug release (Q24 h) with the desirability function of 0.910 which indicated that the model is valid. In vitro release of curcumin from nanoparticles showed prolonged drug release up to 24 h. CUR-NPs administered orally were found to have longer Tmax, higher Cmax, larger AUC, and larger MRT compared to plain CUR. IVIVC model linear regression plots (R2= 0.9949) were obtained by plotting the graph with percent absorbed versus percent dissolved for CUR-NPs. IVIVCs were established for demonstrating the relationship between in vivo absorption and in vitro release. Conclusions: From the results, it can be concluded that this novel CUR-loaded NPs have potential to improve its therapeutic efficacy.
背景:姜黄素(Curcumin, CUR)具有治疗糖尿病的潜力,但其低口服生物利用度使其难以用于慢性疾病的治疗。目的:探讨口服可生物降解CUR纳米颗粒(NPs)在糖尿病患者持续治疗方案中的体内外相关性(IVIVC)。材料与方法:本研究采用Box-Behnken设计,对聚合物的浓度和工艺参数进行优化,制备了CUR可生物降解NPs。结果:采用Box-Behenken法,在聚合物质量分数为2.5% w/v、TPP质量分数为3% w/v、搅拌转速为2534 rpm的条件下,制备出最佳配方,实际反应粒径为192.31±6.82 nm,包封效率为84.26±2.87%,释药量(Q24 h)为95.22±1.81%,期望函数为0.910,表明该模型有效。与普通CUR相比,口服CUR- nps具有更长的Tmax、更高的Cmax、更大的AUC和更大的MRT。通过绘制CUR- nps的吸收百分比与溶解百分比的曲线,得到了IVIVC模型线性回归图(R2= 0.9949)。为了证明体内吸收和体外释放之间的关系,我们建立了ivivc。结论:从结果可以看出,这种新型的cur负载NPs具有提高其治疗效果的潜力。
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引用次数: 0
Mining of small interacting ligands with cytoplasmic polyadenylation element-binding protein 4 与细胞质聚腺苷化元件结合蛋白相互作用的小配体的挖掘
IF 0.4 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-04-01 DOI: 10.4103/ajprhc.ajprhc_29_23
R. Yadav
Cytoplasmic polyadenylation element-binding protein 4 (CPEB 4) is a family member of CPEB proteins that are involved in regulating posttranscriptional expression of mRNAs. These proteins act by binding to cytoplasmic polyadenylation element of genes at their untranslated region with the conservation site of UUUUUAU. CPEB 4 proteins are responsible for modulating gene expression by the process of translational activation or repression by polyadenylation event. Overexpression of CPEB 4 gene has been reported in several classes of cancer such as gastric cancer, neuronal cancer, and pancreatic cancer. CPEB 4 sometimes acts like oncogene and can cause different types of cancer. CPEB 4 protein has been studied in detail in the current research. CPEB 4 protein structure was retrieved from the PDB database with PDB ID: 5DIF and total of 25 ligands were selected through a literature survey, chemical databases, etc., to perform molecular interaction study, docking method was used. Glide docking was done using Schrodinger software, and results were analyzed. Result shows that 2-(2,4-dihydroxyphenyl)-3,5,7-trihydroxy-chromen-4-one (PubChem ID: 5281670) ligand has stable interaction with a Glide score of −8.26 and shows bonds with CPEB 4 protein at positions Lys(A: 924), Gly(B: 791), Asn(A: 879), and Thr(A: 878). These findings can help in modeling suitable ligands against the CPEB 4 protein responsible for several types of cancers.
胞浆多聚腺苷化元件结合蛋白4 (CPEB 4)是CPEB蛋白家族成员,参与调控mrna的转录后表达。这些蛋白通过与基因的胞质多聚腺苷化元件在其未翻译区与UUUUUAU的保护位点结合而起作用。CPEB 4蛋白通过翻译激活或多聚腺苷化事件的抑制过程来调节基因表达。cpeb4基因的过表达已在胃癌、神经细胞癌和胰腺癌等几种癌症中得到报道。CPEB 4有时会像致癌基因一样,导致不同类型的癌症。目前的研究对CPEB - 4蛋白进行了详细的研究。从PDB数据库中检索CPEB 4蛋白结构,PDB ID: 5DIF,通过文献调查、化学数据库等选择共25个配体,进行分子相互作用研究,采用对接方法。利用薛定谔软件进行滑翔对接,并对对接结果进行分析。结果表明,2-(2,4-二羟基苯基)-3,5,7-三羟基铬-4-one (PubChem ID: 5281670)配体与CPEB 4蛋白在Lys(a: 924)、Gly(B: 791)、Asn(a: 879)和Thr(a: 878)位点上具有稳定的相互作用,Glide评分为−8.26。这些发现可以帮助建立合适的配体来对抗导致几种癌症的CPEB 4蛋白。
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Asian Journal of Pharmaceutical Research and Health Care
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