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Hesperetin effect on MLH1 and MSH2 expression on breast cancer cells BT-549. Hespeerin对乳腺癌症细胞BT-549 MLH1和MSH2表达的影响。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-01 Epub Date: 2023-07-28 DOI: 10.4103/japtr.japtr_277_23
Assim Khattab Hasan, Esmaeil Babaei, Ahmed Salim Kadhim Al-Khafaji

Due to its genetic and phenotypic heterogeneity, breast cancer is very difficult to eliminate. The harmful consequences of conventional therapies like radiation and chemotherapy have prompted the search for organic-based alternatives. Hesperetin (HSP), a flavonoid, has been discovered to possess the ability to hinder the proliferation of cell associated with breast cancer by acting as an epigenetic agent and modifying gene expression. In this investigation, breast cancer cells (BT-549) and normal cells (MCF-10a) were subjected to the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) test and three different doses (200, 400, and 600 μM/mL) of HSP for real-time polymerase chain reaction and flow cytometry to examine its cytotoxic and anti-malignant potential. HSP was shown to be cytotoxic to both normal and breast cancer cells, but had a more pronounced effect on the cancer cell lines. After 48 h of treatment, the half-maximal inhibitory concentration (IC50) for BT-549 was 279.2 μM/mL, whereas the IC50 for MCF-10a was 855.4 μM/mL. At high HSP concentrations, upregulation of the MLH1 and MSH2 genes was observed in both cell lines. The influence of HSP on MLH1 gene expression was concentration dependent. Moreover, HSP had a concentration-dependent effect on MSH2 gene expression in the BT-549 cell line but not in the MCF-10a cell line. Cell death and early apoptosis were shown to be concentration dependent upon the application of HSP, as determined by flow cytometric analysis. HSP's capacity to cause apoptosis and its stronger impact on the malignant cell line when analyzed with the normal cell line imply that it might be useful as an effective therapeutic approach for combating breast cancer.

由于其遗传和表型的异质性,癌症很难消除。放疗和化疗等传统疗法的有害后果促使人们寻找基于有机物的替代品。Hespeerin(HSP)是一种黄酮类化合物,被发现具有作为表观遗传因子和修饰基因表达来抑制癌症相关细胞增殖的能力。在本研究中,对乳腺癌症细胞(BT-549)和正常细胞(MCF-10a)进行3-(4,5-二甲基噻唑-2-基)-2,5-二苯基溴化四唑鎓)试验和三种不同剂量(200、400和600μM/mL)的HSP实时聚合酶链反应和流式细胞术,以检测其细胞毒性和抗恶性潜力。HSP对正常和乳腺癌症细胞均具有细胞毒性,但对癌症细胞系具有更显著的作用。治疗48小时后,BT-549的半数最大抑制浓度(IC50)为279.2μM/mL,而MCF-10a的IC50为855.4μM/mL。在高HSP浓度下,在两种细胞系中都观察到MLH1和MSH2基因的上调。HSP对MLH1基因表达的影响具有浓度依赖性。此外,HSP在BT-549细胞系中对MSH2基因表达具有浓度依赖性影响,但在MCF-10a细胞系中没有。流式细胞术分析表明,细胞死亡和早期凋亡的浓度依赖于HSP的应用。与正常细胞系相比,HSP引起细胞凋亡的能力及其对恶性细胞系的更强影响表明,它可能是对抗癌症的有效治疗方法。
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引用次数: 1
The inflammation process of gout arthritis and its treatment. 痛风性关节炎的炎症过程及其治疗。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-01 Epub Date: 2023-07-28 DOI: 10.4103/japtr.japtr_144_23
Nita Parisa, Muhammad Totong Kamaluddin, Masagus Irsan Saleh, Ernawati Sinaga

Gout arthritis is an inflammatory condition that occurs suddenly in joints affected by high uric acid levels (hyperuricemia). The uric acid levels in this disease fluctuate throughout its various phases, resulting in frequent or recurrent attacks. This study aims to review some aspects of gout arthritis, such as its pathophysiology, treatment goals, and adverse drug reactions. This study employs review literature using articles published between 2017 and 2022 as the research methodology. Furthermore, articles under 2017 are used as references if they are relevant to the study's subject matter. The findings showed the importance of the pathogenesis of inflammation in the treatment of gout arthritis. It is also recommended to use anti-inflammatories such as colchicine and uric acid-lowering medications starting at a specific time to prevent unintended risks. Hence, pharmacotherapy management's adverse effects include nausea, vomiting, myalgia, neuropathy, and stomach pain.

痛风性关节炎是一种突然发生在受高尿酸水平(高尿酸血症)影响的关节中的炎症性疾病。这种疾病的尿酸水平在各个阶段都会波动,导致频繁或反复发作。本研究旨在综述痛风性关节炎的一些方面,如其病理生理学、治疗目标和药物不良反应。本研究采用了2017年至2022年间发表的综述文献作为研究方法。此外,如果2017年以下的文章与研究主题相关,则可作为参考。研究结果显示了炎症发病机制在痛风性关节炎治疗中的重要性。还建议在特定时间开始使用秋水仙碱和降尿酸药物等抗炎药,以防止意外风险。因此,药物治疗的不良反应包括恶心、呕吐、肌痛、神经病变和胃痛。
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引用次数: 0
Utilization of local therapeutic food in preventing and treating nutrition problems in the dry land area of the islands of east nusa tenggara province. 利用当地治疗食品预防和治疗东努沙登加拉省岛屿旱地的营养问题。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-01 Epub Date: 2023-07-28 DOI: 10.4103/japtr.japtr_38_23
Intje Picauly, Marselinus Laga Nur, Marni Marni, Esryk Indriyani Kale

The research aims to produce a local Pemberian makanan tambahan (PMT) biscuit formula that is nutritious, acceptable and has a good shelf life. Experimental research with RAL design used two factors and two treatments, namely the addition of anchovy flour (20% and 30%) and moringa leaf flour (20% and 30%) to 100 g of corn flour. The research was conducted in April-November 2022 with an analysis of nutritional content, and acceptability. Data were processed using SPSS with a statistical test One Way analysis of variance Test. The results of the analysis showed that the P4 product had a higher nutritional content difference, namely: 17.976 g of protein; fat 20.106 g; carbohydrates 60.644 g; minerals 3.632 μg; water content 3.999 aw; and energy 490.9 kcal with acceptance scores: Like-really like for 7 days at room temperature without standard packaging. Each serving portion for children of 2 pieces of biscuits or as much as 25 g/day gets a protein nutritional intake of 2.26 g or 11.3% of the Recommended dietary allowance (RDA); Fat of 2.66 or 5.9% of the RDA; Carbohydrates are 14.3 or 6.7% of the RDA and Energy is 615.23 kcal or 45.6% of the RDA. Product combination of 100 g of corn flour; 20 g of moringa flour; and 20 g of anchovy flour into the local therapeutic food "Iman" biscuit formulation which is very popular.

该研究旨在生产一种营养丰富、可接受且具有良好保质期的当地彭贝里makanan tambahan(PMT)饼干配方。RAL设计的实验研究使用了两个因素和两种处理,即在100g玉米粉中添加凤尾鱼粉(20%和30%)和辣木叶粉(20%或30%)。该研究于2022年4月至11月进行,对营养含量和可接受性进行了分析。数据采用SPSS统计软件进行处理。分析结果表明,P4产品具有较高的营养含量差异,即:蛋白质17.976g;脂肪20.106克;碳水化合物60.644g;矿物3.632μg;含水量3.999 aw;能量490.9千卡,验收分数:在没有标准包装的情况下,在室温下持续7天。儿童每份2块饼干或每天25克饼干的蛋白质营养摄入量为2.26克,相当于推荐膳食摄入量(RDA)的11.3%;脂肪含量为2.66或RDA的5.9%;碳水化合物是RDA的14.3或6.7%,能量是615.23 kcal或RDA的45.6%。100g玉米粉的产品组合;20克辣木粉;将20克凤尾鱼粉加入当地非常受欢迎的治疗食品“伊曼”饼干配方中。
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引用次数: 0
The prevalence of undiagnosed thalassemia minor among primigravida pregnant women before 20 weeks of gestation. 妊娠20周前初产妇中未确诊的轻度地中海贫血的患病率。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-01 Epub Date: 2023-07-28 DOI: 10.4103/JAPTR.JAPTR_280_23
Sahar Jassim Abid, Israa Jameel Najim

Pregnancy-associated anemia is a widespread condition that can have varying impacts on both the mother and the developing fetus, depending on the level of hemoglobin in the mother's blood and the stage of pregnancy at which the anemia occurs. In Iraq, 27% of all registered thalassemia cases are thalassemia minor. Pregnancy may aggravate mild undiagnosed thalassemia early in pregnancy. The objective of the study was to access the prevalence of undetected thalassemia minor in primigravida women who received prenatal care before 20 weeks and to compare the demographic and socioeconomic characteristic features between women with iron-deficiency anemia (IDA) and those without any anemia. A total of 298 primigravida women who attended prenatal care at 20 weeks or less were recruited and their hematocrit level was assessed. Participants were segregated into two groups regarding the presence of anemia. Patients who had packed cell volume lower than 33% underwent iron study and standard Hb electrophoresis. Information about women's demographics, socioeconomic status, and family history of hereditary anemia were recorded. The participants had a mean age of 22.7 years, with an age range spanning from 16 to 43 years. 33.33% of 298 women had pathological anemia. All the participants exhibited microcytic anemia, with 26.85%, had confirmed IDA, whereas 6.71% had β thalassemia minor (BTM) phenotype. Both BTM and IDA patients frequently reported a positive family history of anemia at 80% and 68.7%, respectively, which was significantly greater than the control group at 39.9% (P = 0.001). No significant differences were seen between BTM and IDA in terms of age or socioeconomic status. Anemia due to undetected thalassemia minor was common among primigravida women. Screening for BTM carriers pregnant can help in monitoring their status, assessing the fetus's risk of developing thalassemia, and making a diagnosis in communities with high rates of consanguineous marriages, such as Iraq.

妊娠相关贫血是一种广泛存在的疾病,根据母亲血液中血红蛋白的水平和贫血发生的妊娠阶段,它可能对母亲和发育中的胎儿产生不同的影响。在伊拉克,所有登记的地中海贫血病例中有27%是轻度地中海贫血。妊娠可能会在妊娠早期加重轻度未确诊的地中海贫血。该研究的目的是了解在20周前接受产前护理的初产妇中未被发现的轻度地中海贫血的患病率,并比较患有缺铁性贫血(IDA)和没有任何贫血的妇女的人口统计学和社会经济特征。共招募了298名在20周或更短时间内接受产前护理的初产妇,并对她们的红细胞压积水平进行了评估。参与者根据贫血情况分为两组。细胞堆积体积低于33%的患者接受了铁研究和标准Hb电泳。记录了有关妇女人口统计、社会经济地位和遗传性贫血家族史的信息。参与者的平均年龄为22.7岁,年龄范围从16岁到43岁。298名妇女中33.33%患有病理性贫血。所有参与者都表现出微细胞性贫血,26.85%的参与者已证实IDA,而6.71%的参与者具有轻度β地中海贫血(BTM)表型。BTM和IDA患者的贫血家族史阳性率分别为80%和68.7%,显著高于对照组的39.9%(P=0.001)。BTM和ADA在年龄或社会经济地位方面没有显著差异。未被发现的轻度地中海贫血引起的贫血在初产妇中很常见。对怀孕的BTM携带者进行筛查有助于监测他们的状况,评估胎儿患地中海贫血的风险,并在伊拉克等近亲结婚率高的社区进行诊断。
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引用次数: 0
Transdermal patches based on chitosan/hydroxypropyl methylcellulose and polyvinylpyrrolidone/hydroxypropyl methylcellulose polymer blends for gentamycin administration. 基于壳聚糖/羟丙基甲基纤维素和聚乙烯吡咯烷酮/羟丙基甲纤维素聚合物混合物的用于庆大霉素给药的透皮贴剂。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-01 Epub Date: 2023-07-28 DOI: 10.4103/japtr.japtr_130_23
Saif Aldeen Jaber

Biofilm-forming bacteria have sent alarms to the world about the emerging of bacterial resistance. Gentamycin is an aminoglycoside broad-spectrum antibiotic used against microbial infections. The transdermal drug delivery method is a major system used to reduce drug toxicity and avoid first-pass metabolism. Gentamycin was formulated in a transdermal polymeric formula using hydroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone (PVP), and Chitosan in the presence of palmitic acid as a permeation enhancer. In this research, gentamycin extended drug release behavior was successfully done in different polymeric formulas containing (HPMC/PVP) and (HPMC/Chitosan), with a maximum drug release of <70%. In addition, drug diffusion was found to be dependent on the rate of drug release. The controlled release formulas selected for antimicrobial assay show that HPMC/Chitosan formulas have successfully inhibited microbial and biofilm growth by 90%. In conclusion, gentamycin can be formulated in a transdermal polymeric film to target skin infection, reduce drug side effects and avoid drug first-pass metabolism.

形成生物膜的细菌已经向世界发出了细菌耐药性出现的警报。庆大霉素是一种氨基糖苷类广谱抗生素,用于对抗微生物感染。透皮给药方法是用于降低药物毒性和避免首次通过代谢的主要系统。在棕榈酸作为渗透促进剂的存在下,使用羟丙基甲基纤维素(HPMC)、聚乙烯吡咯烷酮(PVP)和壳聚糖以透皮聚合物配方配制庆大霉素。在本研究中,庆大霉素在含有(HPMC/PVP)和(HPMC/壳聚糖)的不同聚合物配方中成功地进行了缓释行为,最大药物释放量为
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引用次数: 0
Awareness toward breast cancer and practice of breast self-examination among Iraqi female students at faculty of basic education. 基础教育学院伊拉克女学生对癌症的认识和乳腺自查实践。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-01 Epub Date: 2023-07-28 DOI: 10.4103/japtr.japtr_281_23
Nahed Ahmed Hassan

The most prevalent cancer and the one with the highest fatality rate is breast cancer, accounting for 27% of all malignancies in women and ranking one among all cancers in women. It appears that breast cancer affects both developed and developing nations. Hence, raising public awareness of breast malignancy prevention strategies is crucial in lowering the morbidity and mortality associated with the disease. The awareness and practices of female undergraduate students at Tikrit University regarding breast self-examination (BSE) were evaluated in this study. This cross-sectional investigation was performed on 420 Iraqi undergraduate scholars at the Faculty of Basic Education, University of Tikrit. The students were polled online using a self-administrated Google Forms that was disseminated through social media. Microsoft Office Excel and SPSS version 22 were used to analyze the data that had been gathered. The majority of responders (70.2%) claimed to be knowledgeable about breast cancer. Out of the participants, around 31.8% expressed the belief that a positive family history, followed by obesity 18.9% was responsible for its occurrence. BSE as a technique to find breast cancer early was only known by 33.2% of individuals who were aware of breast cancer. The significant relationships between BSE practice and breast cancer were demonstrated (P = 0.01). Timely identification and treatment of breast cancer potentially lead to improved outcomes and complete recovery when individuals promptly report signs and symptoms. By promoting awareness of breast cancer and conducting BSE, it is possible to minimize the financial burden of the treatment plan and mitigate the impact of synonyms.

最常见和死亡率最高的癌症是癌症,占女性所有恶性肿瘤的27%,在女性所有癌症中排名第一。看来癌症影响发达国家和发展中国家。因此,提高公众对乳腺恶性肿瘤预防策略的认识对于降低与该疾病相关的发病率和死亡率至关重要。本研究评估了提克里特大学女本科生对乳房自检(BSE)的认识和实践。这项横断面调查是对提克里特大学基础教育学院的420名伊拉克本科生进行的。学生们使用通过社交媒体传播的自行管理的谷歌表格进行在线调查。使用Microsoft Office Excel和SPSS 22版对收集的数据进行分析。大多数应答者(70.2%)声称了解癌症。在参与者中,约31.8%的人表示相信阳性家族史,其次是肥胖,18.9%的人认为这是其发生的原因。BSE作为一种早期发现癌症的技术,只有33.2%的癌症患者知道。证明了BSE实践与乳腺癌症之间的显著关系(P=0.01)。当个体及时报告体征和症状时,及时识别和治疗癌症乳腺癌可能会改善结果并完全康复。通过提高对癌症的认识和进行BSE,可以最大限度地减少治疗计划的经济负担,减轻同义词的影响。
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引用次数: 0
Effects of oral Mirtogenol on retinal ganglion cell apoptosis index and intraocular pressure in the Wistar glaucoma model. 口服Mirtogenol对Wistar青光眼模型视网膜神经节细胞凋亡指数和眼压的影响。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-01 Epub Date: 2023-07-28 DOI: 10.4103/japtr.japtr_29_23
Yustiadenta Widya Andika, Silka Roudhatul Jannah, Winarto, Arief Wildan, Fifin Luthfia Rahmi, Riski Prihatningtyas, Joko Mulyanto, Maharani

The purpose of this research is to determine how Mirtogenol affects intraocular pressure (IOP) and retinal ganglion cells (RGCs) of apoptosis index in Wistar glaucoma models, as well as the relationship between IOP and RGC apoptosis index. Twelve Wistar glaucoma models were divided into two groups for experimental research with a pretest-posttest and posttest-only. The treatment group got oral administration of Mirtogenol 12.3 mg twice a day for 2 weeks, whereas the control group received a placebo in the same way. Apoptotic index and IOP were evaluated both before and after the intervention. A parametric independent t-test was used to determine the difference between groups, and a parametric paired t-test was used to determine the difference within groups. The results showed that the RGC apoptosis index in treatment groups was considerably less when compared to control groups (P < 0.001). In the treatment group, the IOP is decreased compared to the control group (mean difference: -12.67 ± 3.79 vs. 0.69 ± 4.64, respectively, P = 0.002). A significant and solid correlation was found between IOP and RGC apoptosis index (R = 0.884, P < 0.001). Thus, Mirtogenol supplementation is expected to be used to prevent glaucoma progression.

本研究的目的是确定Mirtogenol如何影响Wistar青光眼模型中眼压(IOP)和视网膜神经节细胞(RGCs)的凋亡指数,以及IOP和RGCs凋亡指数之间的关系。将12个Wistar青光眼模型分为两组进行实验研究,分别进行前测后测和后测。治疗组口服米托烯醇12.3 mg,每天两次,持续2周,而对照组以同样的方式接受安慰剂。在干预前后评估凋亡指数和眼压。使用参数独立t检验来确定组之间的差异,使用参数配对t检验来判断组内的差异。结果显示,与对照组相比,治疗组的RGC凋亡指数显著降低(P<0.001)。治疗组的IOP与对照组比较有所下降(平均差异分别为:-12.67±3.79 vs.0.69±4.64,P=0.002)。IOP与RGC凋亡指数之间存在显著且坚实的相关性(R=0.884,P<0.001,Mirtogenol补充剂有望用于预防青光眼的进展。
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引用次数: 0
Antibacterial activity of hexane and methanol fractions of some selected plants against Klebsiella pneumoniae. 某些植物的己烷和甲醇部分对肺炎克雷伯菌的抗菌活性。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-01 Epub Date: 2023-07-28 DOI: 10.4103/JAPTR.JAPTR_183_23
Yosie Andriani, Wahdini Hanifah, Alifa Husnun Kholieqoh, Fadzilah Adibah Abdul Majid, Hermansyah Hermansyah, Hermansyah Amir, Tengku Sifzizul Tengku Muhammad

Besides adenovirus, pneumonia can also be caused by bacteria. One of the most common bacteria causing the pneumonia is Klebsiella pneumoniae. Currently, treatment by antibiotics has been widely used. Nevertheless, the increasing failure of existing antibiotics because of antibiotic resistance resulted by bacterial pathogens has become a serious problem to human health. Hence, there is a need for a new antibacterial potential agent against K. pneumoniae as an alternative treatment to the pneumonia to prevent the risk of a severe pneumonia for both healthy people and those already infected with the pneumonia. This study, therefore, investigated the antibacterial activity of some selected plants (Pandanus tectorius, Nypa fruticans, Sonneratia alba, Phaleria macrocarpa, Hibiscus tiliaceus, and Pongamia pinnata) against K. pneumoniae. In this study, samples were extracted successively by cold maceration using hexane and methanol. Antibacterial activity was determined by well and disc diffusion methods. Each fraction was prepared by two-fold dilutions from 20 mg/mL to 0.156 mg/mL. All data were analyzed in triplicate replication and presented as mean values ± standard deviation. Results showed that all methanol fractions of selected plants had antibacterial activity against K. pneumoniae, and well-diffusion method showed better antibacterial results compared to the agar well-diffusion method. The strongest activity was obtained by methanol fraction of S. alba leaf, followed by P. pinnata leaf, Nypa fruticans bark, H. tiliaceus leaf, P. macrocarpa leaf, and P. tectorius leaf with the minimum inhibitory concentrations (MICs) value between 0.625 and 5.0 mg/mL. Phytochemical screening revealed that all methanol fractions were rich in flavonoid content, which could have contributed to their antibacterial activity.

除了腺病毒,肺炎也可能由细菌引起。引起肺炎的最常见的细菌之一是肺炎克雷伯菌。目前,抗生素治疗已被广泛使用。然而,由于细菌病原体引起的抗生素耐药性,现有抗生素的失效率越来越高,这已成为人类健康的一个严重问题。因此,需要一种新的针对肺炎克雷伯菌的潜在抗菌剂,作为肺炎的替代治疗方法,以预防健康人和已经感染肺炎的人患严重肺炎的风险。因此,本研究调查了一些选定植物(Pandanus tectorius、Nypa fruticans、Sonneratia alba、Phaleria macrocarpa、Hibiscus tiliaceus和Pongamia羽状)对肺炎克雷伯菌的抗菌活性。在本研究中,样品依次用己烷和甲醇进行冷浸渍提取。采用孔扩散法和圆盘扩散法测定抗菌活性。每个级分通过从20 mg/mL到0.156 mg/mL的两倍稀释制备。所有数据以一式三份的方式进行分析,并以平均值±标准差的形式表示。结果表明,所选植物的甲醇组分均对肺炎克雷伯菌具有抗菌活性,与琼脂扩散法相比,扩散法具有更好的抗菌效果。白叶甲醇组分的活性最强,其次是羽扇叶、紫苏树皮、紫苏叶、大果叶和盖叶,最小抑制浓度(MIC)值在0.625至5.0mg/mL之间。植物化学筛选表明,所有甲醇组分都富含黄酮类化合物,这可能有助于它们的抗菌活性。
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引用次数: 0
COVID-19 in third trimester of pregnancy. 妊娠晚期新冠肺炎。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-01 Epub Date: 2023-07-28 DOI: 10.4103/japtr.japtr_33_23
JosnaVinutha Yadiki, Sultan Abdulkarim Ali Alftaikhah

The COVID-19 pandemic disease, which affects the respiratory system and produces flu-like symptoms, is caused by the SARS-CoV-2 virus. It is transmitted by close contact, oronasal secretions, or droplets. In general, pregnant individuals are at increased risk than nonpregnant individuals for developing serious SARS-CoV-2 virus-related illnesses, particularly during the third trimester. Despite the lack of research on COVID-19-infected pregnant mothers, this review article has discussed the clinical and laboratory characteristics and impact of COVID-19 on delivery, management, and vaccination of pregnant individuals with COVID-19 infection.

新冠肺炎大流行性疾病是由SARS-CoV-2病毒引起的,它影响呼吸系统并产生类似流体的症状。它通过密切接触、口腔分泌物或飞沫传播。一般来说,孕妇患严重严重急性呼吸系统综合征冠状病毒2型相关疾病的风险比非孕妇高,尤其是在妊娠晚期。尽管缺乏对感染新冠肺炎的孕妇的研究,但这篇综述文章讨论了新冠肺炎的临床和实验室特征以及对新冠肺炎感染孕妇的分娩、管理和疫苗接种的影响。
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引用次数: 1
Synthesis, characterization, and antiproliferative evaluation of novel sorafenib analogs for the treatment of hepatocellular carcinoma. 用于治疗肝细胞癌的新型索拉非尼类似物的合成、表征和抗增殖评价。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-01 Epub Date: 2023-07-28 DOI: 10.4103/JAPTR.JAPTR_282_23
Marwan Imad Jihad, Monther Faisal Mahdi

Cancer is a disease triggered by an uncontrolled proliferation of a cluster of cells, typically originating from a single cell. Sorafenib, a widely utilized pharmaceutical, has limitations in clinical use due to pharmacokinetic challenges and the development of resistance mechanisms. This investigation aimed to synthesize new sorafenib analogs and evaluated their activity against HepG2 cell lines, specifically targeting hepatocellular carcinoma (HCC). Seven sorafenib analogs were synthesized and identified by Fourier-transform infrared spectroscopy and 1H-NMR spectra. Cytotoxicity of the analogs was assessed on the human HepG2 cancer cell line by (3-(4, 5-dimethylthazolk-2-yl)-2, 5-diphenyl tetrazolium bromide) colorimetric assay. Results revealed that among the studied compounds, 4b exhibited the most pronounced cytotoxicity against cancer cells, surpassing even the efficacy of sorafenib. This suggested that small substitutions on the NH moiety play a crucial role in the activity against the human HepG2 liver cancer cell line. These findings provide valuable insights for the development of potential anticancer-targeting HCC.

癌症是一种由一群细胞不受控制的增殖引发的疾病,通常起源于单个细胞。索拉非尼是一种广泛使用的药物,由于药代动力学挑战和耐药性机制的发展,其临床应用存在局限性。本研究旨在合成新的索拉非尼类似物,并评估其对HepG2细胞系的活性,特别是靶向肝细胞癌(HCC)。合成了7种索拉非尼类似物,并通过傅立叶变换红外光谱和1H-NMR光谱进行了鉴定。类似物在人HepG2癌症细胞系上的细胞毒性通过(3-(4,5-二甲基恶唑-2-基)-2,5-二苯基四唑溴化物)比色测定来评估。结果显示,在所研究的化合物中,4b对癌症细胞表现出最显著的细胞毒性,甚至超过索拉非尼的疗效。这表明NH部分的小取代在抗人HepG2肝癌癌症细胞系的活性中起着至关重要的作用。这些发现为开发潜在的抗癌靶向HCC提供了有价值的见解。
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Journal of Advanced Pharmaceutical Technology & Research
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