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In Silico Prediction of Binding Affinities of Hybrid Molecules of Benzothiazole cross-linked with Hydroxamic acid by certain linkers 苯并噻唑与羟肟酸通过某些连接剂交联的杂化分子的结合亲和力的硅学预测
Pub Date : 2024-01-15 DOI: 10.32947/ajps.v24i1.1006
Yazen Alqaysi, Shakir M. Alwan, Ashour H. Dawood
New hybrid molecules of Benzothiazole cross-linked with hydroxamic acid through an amino acid or aminoalkanoic acid are suggested. All the synthesized hybrid molecules (2A-E) were subjected to molecular docking to evaluate their binding affinities with histone deacetylase enzyme (HDAC8, PDB ID: 1T69) and recorded lower ΔG (-8.117, -6.322, -8.16, -7.939, - 9.46, respectively)than Vorinostat (suberoylanilide hydroxamic acid, SAHA), as the reference ligand, which recorded a much less value of -5.375, using the Maestro software (Schrödinger, version 2022-1).  Moreover, compound 2E, which is Benzothiazole-p-amino benzoic acid-hydroxamate has recorded the lowest binding score (-9.460). This may indicate that this compound is the most active hybrid molecule. There were no violations from Lipinski’s rule and all the synthesized hybrid molecules comply with all parameters.  SwissADME server was employed for the in silico molecular docking for prediction of the physicochemical and ADME properties of the investigated compounds.  All hybrid molecules showed low possible passive oral absorption and no penetration into BBB. The hybrid molecules 2B and 2D may be considered as P-gp substrates. SAHA does not inhibit any of the CYP enzymes used in this study, while, the hybrid molecules 2B, 2D and 2E have shown possible inhibitory activities.
提出了苯并噻唑通过氨基酸或氨基烷酸与羟肟酸交联的新杂化分子。对所有合成的杂化分子(2A-E)进行了分子对接,以评估它们与组蛋白去乙酰化酶(HDAC8,PDB ID:1T69)的结合亲和力。用 Maestro 软件(薛定谔,2022-1 版)计算,ΔG(分别为-8.117、-6.322、-8.16、-7.939、-9.46)比作为参考配体的 Vorinostat(亚伯酰苯胺羟肟酸,SAHA)低得多,后者的记录值为-5.375。 此外,苯并噻唑-对氨基苯甲酸-羟肟酸化合物 2E 的结合得分最低(-9.460)。这可能表明该化合物是最活跃的杂化分子。所有合成的杂化分子都符合所有参数的要求。 为了预测所研究化合物的理化和 ADME 特性,我们使用 SwissADME 服务器进行了硅分子对接。 所有杂化分子的被动口服吸收率都很低,而且没有渗透到 BBB。杂交分子 2B 和 2D 可被视为 P-gp 底物。SAHA 不抑制本研究中使用的任何一种 CYP 酶,而杂化分子 2B、2D 和 2E 则显示出可能的抑制活性。
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引用次数: 0
Molecular modelling, Synthesis and Antiproliferative Evaluation of New Phenyldiazenyl)-Pyrazol Schiff Base Derivatives 新型苯二氮基吡唑席夫碱衍生物的分子建模、合成和抗增殖评价
Pub Date : 2024-01-14 DOI: 10.32947/ajps.v24i1.999
Duha E. Taha, Monther F. Mahdi, Ayad M. R. Raauf
Lung cancer is the most prevalent worldwide. In addition, it is also the most common cause of cancer-related deaths worldwide, with around 1.8 million new cases annually. With a 5-year survival rate of fewer than 20%.Cytotoxic medicines are commonly employed in cancer treatment. Although the medicine improves patients' quality of life, several disadvantages diminish its efficacy. This necessitates developing new effective strategies that target tumors with minimal adverse effects. This research aims to overcome these issues by synthesizing a new series of phenyldiazenyl)-pyrazol schiff base derivatives by utilizing the molecular docking (GOLD) suite program and the pharmacokinetic properties determination by utilizing (Swiss) ADME suite; The most appropriate-fitting compounds were subsequently produced and confirmed using spectrum analysis (FTIR, 1HNMR, and 13 CNMR). MTT in vitro assay were performed to assess of antiproliferative activities against A549 lung cancer cell lines. The antiproliferative study showed that compound 3a had an inhibitory concentration (IC50 of 17.37 µM) on lung cancer cells (A549), which was significantly higher inhibitory activity than Erlotinib (IC50 = 25.06 µM). While compound 3b had an inhibitory activity comparable to the reference drug's, The IC50 values for compounds 3c, 3d, and 3e were 47.48, 45.56, and 33.05 µM, respectively
肺癌是全球发病率最高的癌症。此外,它也是全球最常见的癌症相关死亡原因,每年新增病例约 180 万。细胞毒性药物是治疗癌症的常用药物。虽然这种药物能改善患者的生活质量,但它的一些缺点削弱了其疗效。因此,有必要开发新的有效策略,在靶向肿瘤的同时将不良反应降至最低。本研究旨在克服这些问题,利用分子对接(GOLD)套件程序合成了一系列新的苯基二氮杂环唑-席夫碱衍生物,并利用(Swiss)ADME 套件进行了药代动力学特性测定;随后生成了最合适的化合物,并利用光谱分析(傅立叶变换红外光谱、1HNMR 和 13 CNMR)进行了确认。)对 A549 肺癌细胞株进行了 MTT 体外检测,以评估其抗增殖活性。抗增殖研究表明,化合物 3a 对肺癌细胞(A549)的抑制浓度(IC50 为 17.37 µM)明显高于厄洛替尼(IC50 = 25.06 µM)。化合物 3c、3d 和 3e 的 IC50 值分别为 47.48、45.56 和 33.05 µM。
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引用次数: 0
Assessment of Quality of Life in a Sample of Short Stature Iraqi Children with Growth Hormone Deficiency 评估伊拉克生长激素缺乏症矮身材儿童的生活质量
Pub Date : 2024-01-14 DOI: 10.32947/ajps.v24i1.1028
Saba Rabea, Mohammed Mahmood Mohammed, Dawood S. abdoun, Iman Bashet
Background: Short stature (SS) is defined as a height of 2.0 or more standard deviations (SD) below the population-specific mean height for age and gender. 2.5% of children have short stature, and it is one of the most frequent causes for children to see a growth specialist during their childhood.It is challenging to generalize about the effect of short stature on psycho-social adaption given the data currently available.  Health-related quality of life (HrQoL) was generally shown to be lower in clinically identified short stature children than in population-based normal-sized reference groups. Aim: Examine the behavioral pattern and mental health of SS and its psychological influence on QoL of children/adolescence. In addition, compare the behavioral response and QoL between growth hormone deficiency GHD and control groups. Methods: It is a cross sectional study, included 80 participants (60 with GHD and 20 with normal height as control group) between 4 and 18 years old. The parents of the participants were given a parent-reported version of the written Quality of Life in Short Stature Youth QoLISSY questionnaire in Arabic in order to examine the association with the socio-demographic characteristics of the participants. Results: 51.25% female and 48.75% male included in this study, the mean age at assessment was 12.1 ± 2.7, and 11.8 ± 2.6 of the GHD and control group, respectively. There was significant difference in QoLISSY total score between GHD and control groups. The association between socio-demographic characteristics of the participants was significantly different. Conclusion: The QoL of Iraqi children with GHD showed lower scores in all domains of QoLISSY compared to normal children.
背景:身材矮小(SS)是指身高比特定年龄和性别的人口平均身高低 2.0 或更多标准差(SD)。2.5%的儿童有身材矮小的问题,这也是儿童在童年时期最常去看生长发育专科医生的原因之一。 临床上发现,身材矮小儿童的健康相关生活质量(HrQoL)普遍低于以人口为基础的正常身材参照组。目的:研究 SS 的行为模式和心理健康及其对儿童/青少年生活质量的心理影响。此外,比较生长激素缺乏症 GHD 组和对照组的行为反应和 QoL。研究方法这是一项横断面研究,包括 80 名 4 至 18 岁的参与者(60 名生长激素缺乏症患者和 20 名身高正常者作为对照组)。研究人员向参与者的父母提供了一份由父母报告的阿拉伯语书面版矮身材青少年生活质量 QoLISSY 问卷,以研究该问卷与参与者的社会人口特征之间的关联。结果显示GHD组和对照组的平均评估年龄分别为(12.1 ± 2.7)岁和(11.8 ± 2.6)岁。GHD 组和对照组的 QoLISSY 总分有明显差异。参与者的社会人口学特征之间的关联也存在显著差异。结论与正常儿童相比,伊拉克 GHD 儿童在 QoLISSY 各个领域的 QoL 分数都较低。
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引用次数: 0
Impact of Pyridoxine Supplement on Oxidative Stress in Type 2 Diabetic Patients 补充吡哆醇对 2 型糖尿病患者氧化应激的影响
Pub Date : 2024-01-14 DOI: 10.32947/ajps.v24i1.1030
Moatamad Hanoon Dawood, Manal Khalid Abdulridha, Hayder Saadoon Qasim
Background: The physiologically active form of vitamin B6 is pyridoxal 5-phosphate (PLP), which functions as a coenzyme in 150 enzymatic processes such amino acid, carbohydrate, and lipid metabolism and is essential for the production and/or breakdown of neurotransmitters.. It also acts as an antioxidant by quenching Reactive Oxygen Species (ROS) and counteracting the formation of Advanced Glycation End-Product (AGEs). PLP is recycled by mammals from B6 vitamins found in diet and has been linked to a number of clinically significant disorders. This study aim was to evaluate the impact of pyridoxine supplementation on oxidative stress status in type 2 diabetic patients.Method: This prospective controlled randomized open-labeled study of newly diagnosed T2DM patients. The study was conducted from November 2022 to February 2023 at the Mesan Center for Diabetes and Endocrinology under the supervision of a specialist endocrinologist. The total number of participants whose data were collected in this study was one hundred and eight participants, eighty-eight patients newly diagnosed with type 2 diabetes were included in the study, and twenty of the participants were healthy subjects. The patients were allocated into three groups: Group 1: Control group, 20 T2DM patients were treated with non-pharmacological therapy (lifestyle modification) for one month, Group 2: 34 T2DM patients treated with metformin 500 mg/day in addition to non-pharmacological therapy (lifestyle modification) for one month, Group 3: 34 T2DM patients treated with metformin 500 mg/day plus vitamin B6 300 mg/day in addition to non-pharmacological therapy (lifestyle modification) for one month, in addition to Healthy subjects: 20 subjects were taken to compare the study parameters between type 2 diabetic patients and healthy persons at baseline. Measurement of Vitamin B6 (pyridoxine) blood level (PLP), body mass index (BMI) and Serum malondialdehyde level (MDA) was done in this study.Results: The results of the study showed that the use of pyridoxine supplementation plus metformin decreased the level of MDA. There was significant decrease in (MDA) level (P<0.01) pretreatment when compared to after treatment (3.85 μmole/L vs 1.66 μmole/L) respectively.Conclusion: Restoration of vitamin B6 level can leads to a decreased blood level of MDA in diabetic patients.
背景:维生素 B6 的生理活性形式是 5-磷酸吡哆醛(PLP),它在氨基酸、碳水化合物和脂质代谢等 150 个酶过程中发挥辅酶的作用,是神经递质的产生和/或分解所必需的。它还是一种抗氧化剂,能淬灭活性氧(ROS)并抵消高级糖化终产物(AGEs)的形成。PLP是哺乳动物从饮食中的维生素B6中回收的,它与许多临床重大疾病有关。本研究旨在评估补充吡哆醇对 2 型糖尿病患者氧化应激状态的影响:这项前瞻性对照随机开放标签研究的对象是新诊断的 2 型糖尿病患者。研究于 2022 年 11 月至 2023 年 2 月在梅山糖尿病和内分泌中心进行,由内分泌专科医生指导。本研究共收集了 118 名参与者的数据,其中 88 名为新诊断的 2 型糖尿病患者,20 名为健康受试者。患者被分为三组:第一组:对照组,20 名 T2DM 患者接受为期一个月的非药物疗法(生活方式调整)治疗;第二组:34 名 T2DM 患者在接受非药物疗法(生活方式调整)治疗的同时,接受二甲双胍 500 毫克/天治疗,为期一个月;第三组:34 名 T2DM 患者在接受二甲双胍 500 毫克/天治疗的同时,接受二甲双胍 500 毫克/天治疗,为期一个月:第 3 组:34 名 T2DM 患者,除接受非药物疗法(改变生活方式)治疗外,还接受二甲双胍 500 毫克/天加维生素 B6 300 毫克/天的治疗,为期一个月,此外还有健康受试者:20 名受试者,以比较 2 型糖尿病患者和健康人在基线时的研究参数。本研究测量了血液中维生素 B6(吡哆醇)水平(PLP)、体重指数(BMI)和血清丙二醛水平(MDA):研究结果表明,补充吡哆醇和二甲双胍可降低 MDA 水平。与治疗前相比,治疗后的 MDA 水平(3.85 μmole/L vs 1.66 μmole/L)明显下降(P<0.01):结论:恢复维生素 B6 水平可降低糖尿病患者血液中的 MDA 水平。
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引用次数: 0
Association of Dialysis Adequacy, Physical and Emotional Symptoms with Erythropoietin-stimulating agent Responsiveness in Iraqi Patients Undergoing Hemodialysis 接受血液透析的伊拉克患者的透析充分性、身体和情绪症状与促红细胞生成素反应性的关系
Pub Date : 2024-01-14 DOI: 10.32947/ajps.v24i1.1038
Salar Ahmed, Mohammed Mahmood, Arif Sami, Salim Hamadi
Background: Erythropoietin (EPO)-deficient anemia occurs in patients with chronic kidney disease (CKD). Erythropoietin-stimulating agents (ESAs) are the standard treatment for CKD anemia, but patient responses vary.Hemodialysis patients are often anemic due to hypo erythropoiesis and their chronic inflammatory state. Inadequate dialysis is considered one of the factors that are linked to ESA hypo responsiveness. Dialysis patients may experience many symptoms that lower their quality of life.  End stage renal disease (ESRD) symptoms are assessed using Dialysis Symptom Index (DSI). Objective: The current study was designed to measure the association between physical, and emotional symptoms and ESA responsiveness. Also, to determine how dialysis adequacy affects response level.Materials and Methods: The current study included 150 CKD anemic patients  in a multicenter dialysis units. patients were examined for the response to Epoetin alfa (Eprex) after 12 weeks in this cross-sectional study. Clinical, demographic, and laboratory data were collected. The erythropoietin resistance index (ERI) evaluated the effect of erythropoietin dosage on hemoglobin levels. Dialysis adequacy (Kt/V) measured the efficacy of dialysis. The severity of symptoms was evaluated using the 30-question Dialysis Symptom Index (DSI). Results: 150 patients in all were enrolled, with a mean age of 51.6 ± 14.9 for the male patients. There was a significant difference in kt/v among study groups, mainly between hypo response and resistance groups (P-value < 0.01). However, there was no statistically significant difference in the DSI mean (P = 0.4). kt/v was positively correlated with the duration of dialysis and parathyroid hormone (PTH) (R = 0.27, P-value < 0.001), (R = 0.19, P-value = 0.01). additionally, The DSI was strongly connected with the age of the patients (R = 0.18, P-value = 0.02).Conclusion: One of the main causes of Eprex resistance in this study was insufficient dialysis. Patients who received longer hemodialysis sessions exhibited higher hemodialysis sufficiency. However, there was no significant association between DSI and degree of response across research groups, and older hemodialysis patients experienced higher dialysis-related symptoms.
背景:慢性肾脏病(CKD)患者会出现红细胞生成素(EPO)缺乏性贫血。促红细胞生成素刺激剂(ESAs)是治疗 CKD 贫血的标准疗法,但患者的反应各不相同。透析不足被认为是与 ESA 反应性低下有关的因素之一。透析患者可能会出现许多症状,从而降低他们的生活质量。 末期肾病(ESRD)症状可通过透析症状指数(DSI)进行评估。研究目的本研究旨在测量身体和情绪症状与 ESA 反应性之间的关联。同时,确定透析充分性如何影响反应水平:在这项横断面研究中,患者在 12 周后对 Epoetin alfa(Eprex)的反应进行了检查。研究人员收集了临床、人口统计学和实验室数据。红细胞生成素抵抗指数(ERI)评估了红细胞生成素剂量对血红蛋白水平的影响。透析充分性(Kt/V)衡量透析效果。透析症状指数(DSI)包含 30 个问题,用于评估症状的严重程度。结果共招募了 150 名患者,男性患者的平均年龄为 51.6±14.9 岁。研究组之间的 kt/v 有明显差异,主要是低反应组和抵抗组之间(P 值 < 0.01)。kt/v与透析时间和甲状旁腺激素(PTH)呈正相关(R=0.27,P值<0.001)、(R=0.19,P值=0.01),此外,DSI与患者年龄密切相关(R=0.18,P值=0.02):结论:在本研究中,Eprex 耐药性的主要原因之一是透析不足。接受较长时间血液透析的患者血液透析充分性较高。然而,各研究组的 DSI 与反应程度之间并无明显关联,年龄较大的血液透析患者出现的透析相关症状较多。
{"title":"Association of Dialysis Adequacy, Physical and Emotional Symptoms with Erythropoietin-stimulating agent Responsiveness in Iraqi Patients Undergoing Hemodialysis","authors":"Salar Ahmed, Mohammed Mahmood, Arif Sami, Salim Hamadi","doi":"10.32947/ajps.v24i1.1038","DOIUrl":"https://doi.org/10.32947/ajps.v24i1.1038","url":null,"abstract":"Background: Erythropoietin (EPO)-deficient anemia occurs in patients with chronic kidney disease (CKD). Erythropoietin-stimulating agents (ESAs) are the standard treatment for CKD anemia, but patient responses vary.\u0000Hemodialysis patients are often anemic due to hypo erythropoiesis and their chronic inflammatory state. Inadequate dialysis is considered one of the factors that are linked to ESA hypo responsiveness. Dialysis patients may experience many symptoms that lower their quality of life.  End stage renal disease (ESRD) symptoms are assessed using Dialysis Symptom Index (DSI). Objective: The current study was designed to measure the association between physical, and emotional symptoms and ESA responsiveness. Also, to determine how dialysis adequacy affects response level.Materials and Methods: The current study included 150 CKD anemic patients  in a multicenter dialysis units. patients were examined for the response to Epoetin alfa (Eprex) after 12 weeks in this cross-sectional study. Clinical, demographic, and laboratory data were collected. The erythropoietin resistance index (ERI) evaluated the effect of erythropoietin dosage on hemoglobin levels. Dialysis adequacy (Kt/V) measured the efficacy of dialysis. The severity of symptoms was evaluated using the 30-question Dialysis Symptom Index (DSI). Results: 150 patients in all were enrolled, with a mean age of 51.6 ± 14.9 for the male patients. There was a significant difference in kt/v among study groups, mainly between hypo response and resistance groups (P-value < 0.01). However, there was no statistically significant difference in the DSI mean (P = 0.4). kt/v was positively correlated with the duration of dialysis and parathyroid hormone (PTH) (R = 0.27, P-value < 0.001), (R = 0.19, P-value = 0.01). additionally, The DSI was strongly connected with the age of the patients (R = 0.18, P-value = 0.02).\u0000Conclusion: One of the main causes of Eprex resistance in this study was insufficient dialysis. Patients who received longer hemodialysis sessions exhibited higher hemodialysis sufficiency. However, there was no significant association between DSI and degree of response across research groups, and older hemodialysis patients experienced higher dialysis-related symptoms.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140508639","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
Evaluation of Prothrombin Time,International Normalized Ratio, and Activated Partial Thromboplastin Time in Hepatitis B Virus Patients, Sudan2020 -2021 评估苏丹乙型肝炎病毒感染者的凝血酶原时间、国际标准化比率和活化部分凝血活酶时间2020 - 2021年
Pub Date : 2024-01-14 DOI: 10.32947/ajps.v24i1.977
G. Modawe, Esra Awad Mohamed, Ozaz Yagoup Mohamed, AbdelrahmanEldaw Mohammed, Hiba Awadelkareem Osman Fadl, Abdelrahman Hamza Abdelmoneim
Background: Hepatitis B virus is a growing problem worldwide leading to increasing incidences of life-threatening complications of which liver diseases play a major part of it.Materials and Methods: To evaluate these effects in Sudanese patients, a cross-sectional study was carried out in Wad Medani teaching hospital from October 2020 to February 2021 for assessing the effect of the disease on the coagulation profile. Patients were randomly selected according to inclusion and exclusion criteria. 2.5ml of blood samples were collected from each patient in tri-sodium citrate containers, and then semi-automated Coatron M4 was used to estimate Prothrombin Time (PT) and Activated Partial Thromboplastin Time (APTT) after calibrated and controlled setting according to the manufacturer’s instructions. SPSS (version 25) was used to analysed data.Results: A total of 100 hepatitis B virus patients were included in the study, with males representing (79%) and females were (21%), their age were between 18 to 60 years. The study results showed PT prolonged in (98%) of the study population and only (2%) were normal. regarding the APTT (99%) of them had prolonged results (more than the upper normal), and the remaining (1%) was normal. Also, the study results showed there were slight statistically insignificant differences in coagulation profile in hepatitis B virus patients according to gender, age group, family history, and duration of the disease.Conclusion:  hepatitis B infection had a great effect on Coagulation profiles. Therefore, it is recommended on the basis of these results to request PT, INR, and APTT as routine works up for hepatitis B virus patients.
背景:乙型肝炎病毒是一个日益严重的全球性问题,导致危及生命的并发症发病率不断上升,其中肝脏疾病占主要部分:为了评估乙肝对苏丹患者的影响,一项横断面研究于 2020 年 10 月至 2021 年 2 月在 Wad Medani 教学医院进行,以评估乙肝对凝血功能的影响。根据纳入和排除标准随机选取了患者。在枸橼酸三钠容器中收集每位患者 2.5 毫升的血液样本,然后根据制造商的说明,在校准和控制设置后使用半自动 Coatron M4 估算凝血酶原时间(PT)和活化部分凝血活酶时间(APTT)。使用 SPSS(25 版)分析数据:研究共纳入 100 名乙肝病毒携带者,其中男性占 79%,女性占 21%,年龄在 18 至 60 岁之间。研究结果显示,98% 的研究对象 PT 值延长,只有 2% 的研究对象 PT 值正常;99% 的研究对象 APTT 值延长(超过正常值上限),其余 1% 的研究对象 APTT 值正常。此外,研究结果表明,根据性别、年龄组、家族史和病程的不同,乙型肝炎病毒感染者的凝血功能也存在轻微的统计学差异。因此,根据上述结果,建议将 PT、INR 和 APTT 作为乙肝病毒携带者的常规检查项目。
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引用次数: 0
Effect of Aescin in Psoriatic-Induced Animal Model: Immunohistochemical and Pathological Study Aescin 对银屑病诱发动物模型的影响:免疫组织化学和病理学研究
Pub Date : 2024-01-14 DOI: 10.32947/ajps.v24i1.1035
Rafal Wadhah, Basma Talib, Ghaith Ali, Wamidh H Talib
Background: Aescin is a mixture of the triterpene saponins extracted from the seeds of the horse chestnut tree Aesculus hippocastanum. Aescin has a venotonic, anti-inflammatory, antioxidant and anti-edematous characteristics that are mostly connected to the agent molecular mechanism.Objective: The present study aim to investigate the potential effects of Aescin on psoriasis induced by Imiquimod in male rats, ncluding its effect on the level of tumor necrosis factor alpha, Ki-67 and the histopathologic features of the psoriatic skin.Methods: Thirty-six albino male rats were divided into six groups each group containing 6 animals, psoriasis was induced by Imiquimod to five of the groups, while for the last group vasaline was applied and the group served as a control group. The animals were then treated with topical Aescin, topical clobetasol, combination of topical Aescin and clobetasol and oral Aescin, finally all animals were sacrificed and the dorsal back skin was taken to perform histopathological and immunohistochemical analysis.Results: regarding the level of Ki-67, Strong expression of Ki-67 was seen in the group who received Imiquimod only, where the scoring of Ki-67 was notably lowered among the other groups. However, the lowest expression was noticed in the group that were treated with the combination of topical Aescin and clobetasol. While the number of TNF-α positive cells and the intensity of immunostaining were higher in the induction group who received Imiquimod only and the lowest among the group who received the combination of topical Aescin and Clobetasol. Lastly the histopathologic analysis shows that the histopathologic features of psoriasis was markedly affected by the anti-inflammatory effect of Aescin and clobetasol, which was noticed through inhibition of proinflammatory markers, and the decrease in capillary permeability.Conclusion: Topical Aescin alone or in combination with clobetasol reduced Ki-67 expression successfully; furthermore, the combination of topical Aescin and Clobetasol decreased TNF- score and had the strongest anti-inflammatory activity more than the other groups. Lastly Aescin was able to alter the histopathologic features of the psoriatic skin through its anti-inflammatory, venotonic and anti-edematous activity.
背景介绍七叶皂苷(Aescin)是从七叶树(Aesculus hippocastanum)种子中提取的一种三萜皂苷混合物。七叶皂苷具有静脉补液、抗炎、抗氧化和抗风湿等特性,这些特性大多与药剂分子机制有关:本研究旨在探讨 Aescin 对 Imiquimod 诱导的雄性大鼠银屑病的潜在影响,包括对肿瘤坏死因子α、Ki-67 水平和银屑病皮肤组织病理学特征的影响:将 36 只白化雄性大鼠分为 6 组,每组 6 只,其中 5 组使用咪喹莫特诱发银屑病,最后一组使用凡士林,作为对照组。结果:在 Ki-67 水平方面,仅接受咪喹莫特治疗的组中 Ki-67 表达较强,其他组中 Ki-67 的评分明显降低。然而,外用阿司匹林和氯倍他索联合治疗组的 Ki-67 表达最低。仅接受咪喹莫特治疗的诱导组中 TNF-α 阳性细胞的数量和免疫染色的强度较高,而外用艾司馨和氯倍他索联合治疗的组中 TNF-α 阳性细胞的数量和免疫染色的强度最低。最后,组织病理学分析表明,银屑病的组织病理学特征明显受到阿司匹林和氯倍他索抗炎作用的影响,这表现在抑制促炎标志物和降低毛细血管通透性:结论:单独外用安乃近或与氯倍他索联合外用均能成功降低 Ki-67 的表达;此外,与其他组相比,安乃近和氯倍他索联合外用能降低 TNF-评分,并具有最强的抗炎活性。最后,Aescin 通过其抗炎、静脉舒张和抗水肿活性,能够改变银屑病皮肤的组织病理学特征。
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引用次数: 0
Comparative Benefit of Evening Primrose Oil and Soybean Oil on Treatment Satisfaction and Quality of Life among Postmenopausal Women 月见草油和大豆油对绝经后妇女治疗满意度和生活质量的益处比较
Pub Date : 2024-01-14 DOI: 10.32947/ajps.v24i1.993
Raghad Mohammed, Manal Khalid Abdulridha, Bushrah Abd Al-Jbori
Background: Medicinal herbs as alternative therapies, commonly used to treat menopausal symptoms, and some studies have shown that they can be useful in treating menopausal syndrome, which have been linked to worse self-rated health, and decreased work productivity. Aim of the study: This study compared the effectiveness of EPO and Soybean Oil herbal supplement in a sample of Iraqi postmenopausal women on treatment satisfaction and their quality of life. Patients and methods: This prospective study conducted on 20 post-menopausal women who received 500 mg EPO compared to other 20 received 233 mg soybean oil extract, as a capsule twice a day for 8 weeks. The subjective and clinical assessments of Menopause Symptom Treatment Satisfaction, and Menopause-Specific Quality of Life. Data was collected by the researcher via face-to-face interviews with women at baseline and after 2 months of treatment. Results: In this study, Menopause Symptoms Treatment Satisfaction score was not significant within each group post treatment (P>0.05). While after 2 months of treatment, EPO significantly improved the quality of life by decreasing all MEN-QoL domains more than soybean oil, except for the sexual domain (P<0.01). Conclusions: This study revealed that both EPO and soya bean oil supplements had the beneficial effect in improving the postmenopausal quality of life with less treatment satisfaction.
背景:药用草药作为替代疗法,常用于治疗更年期症状,一些研究表明,药用草药可用于治疗更年期综合征,而更年期综合征与自我评价健康状况恶化和工作效率下降有关。研究目的本研究以伊拉克绝经后妇女为样本,比较了 EPO 和大豆油草药补充剂在治疗满意度和生活质量方面的效果。患者和方法:这项前瞻性研究的对象是 20 名绝经后妇女,她们服用了 500 毫克 EPO,而另外 20 名妇女服用了 233 毫克大豆油提取物,每天两次,每次一粒,连续服用 8 周。对更年期症状治疗满意度和更年期生活质量进行了主观和临床评估。研究人员在基线期和治疗 2 个月后通过与妇女面对面访谈收集数据。研究结果在本研究中,更年期症状治疗满意度得分在治疗后各组间差异不显著(P>0.05)。而在治疗 2 个月后,EPO 显著改善了生活质量,除性生活领域(P<0.01)外,MEN-QoL 各领域的下降幅度均高于大豆油(P<0.01)。结论本研究显示,EPO和大豆油补充剂对改善绝经后生活质量均有益处,但治疗满意度较低。
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引用次数: 0
Synthesis, Molecular Docking, Characterization, and Preliminary Evaluation of Some New 1, 3-Diazetidin-2-One Derivatives as Anticancer Agents 作为抗癌剂的一些新的 1,3-二氮杂环丁烷-2-酮衍生物的合成、分子对接、表征和初步评估
Pub Date : 2024-01-14 DOI: 10.32947/ajps.v24i1.1026
Farah Haidar, Monther Faisal Mahdi, Ayad Kareem Khan
A series of novel 1,3-diazetidin-2-one derivatives were designed, synthesized, and evaluated preliminary (In Vitro) for their cytotoxic activity against the lung (A549) cancer cell line. GOLD software (version 2021.2.0) was used to conduct a molecular docking study;the tested derivatives demonstrated significant anticancer activity compared to the reference drug (erlotinib). PLP-fitness values for the final compounds are 79.81, 80.80, and 81.57, respectively, whereas the reference ligand, erlotinib, had a value of 76.20. The synthesized compounds were identified and characterized using physicochemical parameters (melting points and Rf values), FTIR, 1H-NMR, and 13C-NMR spectroscopy. According to the IC50 values for the synthesized derivatives, compounds N4a and N4b exhibit outstanding anti-proliferative activity with IC50 value of (7.51, 7.68) µM against A549 cell line, compared to erlotinib, which has an IC50 value of (11.5) µM. 
研究人员设计、合成了一系列新型 1,3-二氮杂环丁烷-2-酮衍生物,并初步评估了它们对肺癌(A549)细胞系的细胞毒活性(体外)。使用 GOLD 软件(2021.2.0 版)进行了分子对接研究;与参考药物(厄洛替尼)相比,受试衍生物具有显著的抗癌活性。最终化合物的 PLP 适合度值分别为 79.81、80.80 和 81.57,而参考配体厄洛替尼为 76.20。利用理化参数(熔点和 Rf 值)、傅立叶变换红外光谱、1H-NMR 和 13C-NMR 光谱对合成的化合物进行了鉴定和表征。根据合成衍生物的 IC50 值,化合物 N4a 和 N4b 对 A549 细胞株具有出色的抗增殖活性,IC50 值分别为 (7.51, 7.68) µM,而厄洛替尼的 IC50 值为 (11.5) µM。
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引用次数: 0
GC/MS Analysis and Isolation of Stigmasterol from Viola Odorata Cultivated in Iraq 气相色谱/质谱分析和从伊拉克种植的堇菜中分离出豆固醇
Pub Date : 2024-01-14 DOI: 10.32947/ajps.v24i1.1002
Zaineb Ali, Ibrahim Saleh Abbas, Widad MK Alani, Farah Al-Mamoori
Viola odorata is a viola family flowering plant native to Europe and Asia. This is a small, hardy, herbaceous, perennial plant. It is also known as sweet violet and English violet. Numerous pharmacological properties of this flowering plant include anticancer, antibacterial, anti-inflammatory, antioxidant and antipyretic properties.Previous literature review of different parts of Viola odorata resulted in detection of different chemical constituents such as flavonoids (Quercetin, kaempferol), glycosides (Rutin) and terpenoids (stigma sterol). Stigmasterol was detected using TLC and GC-MS in this study. It was isolated from Viola odorata using preparative layer chromatography. HPLC and FTIR analysis confirmed the isolated Stigmasterol
Viola odorata 是一种中提琴科开花植物,原产于欧洲和亚洲。这是一种小型、耐寒、多年生草本植物。它也被称为甜紫罗兰和英国紫罗兰。这种开花植物具有抗癌、抗菌、消炎、抗氧化和解热等多种药理特性。通过对紫罗兰不同部位的文献综述,发现了不同的化学成分,如黄酮类(槲皮素、山柰酚)、苷类(芦丁)和萜类(柱头甾醇)。本研究使用 TLC 和 GC-MS 检测了豆固醇。使用制备层色谱法从 Viola odorata 中分离出了豆固醇。高效液相色谱法和傅立叶变换红外光谱分析证实了分离出的豆固醇
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引用次数: 0
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Al Mustansiriyah Journal of Pharmaceutical Sciences
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