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Characterization and Biological Activities of Silver Nanoparticles Synthesized using Grewia tiliifolia Vahl Leaf Extract 百合叶提取物合成银纳米颗粒的表征及生物活性研究
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-07-14 DOI: 10.34172/ps.2022.29
Sneha Desai K, T. Taranath
Background: An eco-friendly approach for the synthesis of noble metal nanoparticles employing various plant extracts has become of great interest in the field of nanotechnology. In the present study, the efficacy of Grewia tiliifolia leaf extract in reducing 1mM silver nitrate to silver nanoparticles(AgNPs) has been reported for the first time and also we investigated the anticancer, antituberculosis and antioxidant activity. Methods: Characterization of biosynthesized AgNPs using G. tiliifolia leaf extract was evaluated by Uv-Vis, FTIR, XRD, DLS and TEM with SAED. Efficacy of biosynthesized AgNPs using G. tiliifolia leaf extract was tested for cytotoxicity against A549 Lung cancer cell lines by MTT Assay and also against the infectious agent Mycobacterium tuberculosis using MABA Assay. Further antioxidant activity was evaluated by DPPH radical scavaging assay. Results: The biosynthesis of AgNPs was evident by color change of reaction mixture from dark yellow to reddish-brown. Biofabricated AgNPs was further confirmed by characteristic surface plasmon absorption peak at 409nm by UV-vis analysis. FTIR data reveals the presence of phytochemicals involved in bioreduction and biocapping of AgNPs, XRD analysis depicted crystallographic nature of AgNPs. Further, size, charge, and polydispersity nature were studied using DLS (40.2nm with polydispersity index 0.361) and Zeta potential (-35.8mV). The morphology of AgNPs was determined by TEM analysis with size ranging from 11-34nm. The plant derived AgNPs exhibited a cytotoxic effect on the Lung cancer cell line with IC50 value of 23.45µg/ml and also found to be effective against M. tuberculosis with a MIC of 6.25µg/ml in comparison to the leaf extract (MIC 50µg/ml). Antioxidant activity observed by AgNPs was moderate with IC50 value 49.60 µg/ml. Conclusion: The findings indicate that the AgNPs synthesized from leaf extract of G. tiliifolia are eco-friendly, cost-effective, non-toxic and can be the effective natural anticancer, antituberculosis agents and antioxidant agent.
背景:利用多种植物提取物合成贵金属纳米颗粒的环保方法已成为纳米技术领域的研究热点。本研究首次报道了杜立叶提取物将1mM硝酸银还原成纳米银(AgNPs)的作用,并对其抗癌、抗结核和抗氧化活性进行了研究。方法:采用紫外可见光谱(Uv-Vis)、红外光谱(FTIR)、x射线衍射(XRD)、能谱分析(DLS)、透射电镜(TEM)和红外光谱分析(SAED)等方法对杜立叶提取物生物合成AgNPs进行表征。采用MTT法和MABA法分别对杜立叶提取物生物合成AgNPs对A549肺癌细胞株和结核分枝杆菌的细胞毒性进行了研究。通过DPPH自由基清除实验进一步评价其抗氧化活性。结果:AgNPs的生物合成明显,反应混合物的颜色由深黄色变为红褐色。通过紫外-可见光谱分析,在409nm处的特征表面等离子体吸收峰进一步证实了生物制备的AgNPs。FTIR数据揭示了AgNPs生物还原和生物覆盖过程中植物化学物质的存在,XRD分析描述了AgNPs的晶体性质。利用DLS (40.2nm,多分散性指数0.361)和Zeta电位(-35.8mV)对其粒径、电荷和多分散性进行了研究。通过TEM分析确定了AgNPs的形貌,尺寸在11-34nm之间。植物源AgNPs对肺癌细胞系的IC50值为23.45µg/ml,对结核分枝杆菌的MIC值为6.25µg/ml,与叶提取物的MIC值(50µg/ml)相比,植物源AgNPs对肺癌细胞系的IC50值为23.45µg/ml。AgNPs抗氧化活性中等,IC50值为49.60µg/ml。结论:以白藜芦醇叶提取物为原料合成的AgNPs具有环保、经济、无毒等特点,是一种有效的天然抗癌、抗结核和抗氧化剂。
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引用次数: 2
miR-451a-5p modulates breast cancer cell apoptosis, migration, and chemosensitivity to carboplatin through the PTEN pathway miR-451a-5p通过PTEN途径调节乳腺癌细胞凋亡、迁移和对卡铂的化学敏感性
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-07-10 DOI: 10.34172/ps.2022.28
M. Khordadmehr, Hamed Ezzati, A. Shahbazfar, Farinaz Jigari Asl, B. Baradaran, Elham Baghebani, Saeed Noorolyai
Background: MicroRNAs (miRNAs) can play essential roles in the modulation of cancer cell growth, survival, and resistance to chemotherapy. Thus, we hypothesized that restoration of miR-451a-5p (a tumor suppressor) might affect sensitivity to chemotherapeutics in breast cancer cells. Methods: For this purpose, malignant breast cancer cells (MDA-MB-231) were transfected with miR-451a-5p mimic and exposed with carboplatin. Then, the apoptotic rate was evaluated by flow cytometry and DAPI staining (apoptosis), q-RT-PCR (expression levels of caspase-3, caspase-8, MMP9, ROCK, vimentin, c-Myc genes). Moreover, the proliferation and migration of cancer cells were assessed by MTT (cell viability) and wound healing assay. The western blot assay was used for protein expression of PTEN, AKT, and P-AKT. Results: Our findings demonstrated that a combination of miR-451a-5p restoration with carboplatin administration could additionally induce apoptosis, repress the proliferation and migration, and also increase PTEN protein expression with no significant alteration on the AKT/P-AKT protein expressions in the breast cancer cells. The present data was analyzed using GraphPad Prism 6 software by non-parametric one-way ANOVA and t-test. Conclusion: In conclusion, it seems that overexpression of miR-451a can enhance the chemosensitivity of breast cancer cells to carboplatin therapy. Thus, it may shed new light on miR-451a management of breast cancer chemoresistance and may be a beneficial strategy for future cancer therapy. However, further studies, particularly in other signaling pathways, should be required.
背景:MicroRNAs (miRNAs)在调节癌细胞生长、生存和化疗耐药中发挥重要作用。因此,我们假设miR-451a-5p(一种肿瘤抑制因子)的恢复可能影响乳腺癌细胞对化疗药物的敏感性。方法:为此,用miR-451a-5p模拟物转染恶性乳腺癌细胞(MDA-MB-231),并用卡铂暴露。采用流式细胞术、DAPI染色(凋亡)、q-RT-PCR (caspase-3、caspase-8、MMP9、ROCK、vimentin、c-Myc基因表达水平)检测细胞凋亡率。此外,通过MTT(细胞活力)和伤口愈合试验评估癌细胞的增殖和迁移。western blot法检测PTEN、AKT、P-AKT蛋白表达。结果:我们的研究结果表明,miR-451a-5p修复联合卡铂可诱导乳腺癌细胞凋亡,抑制增殖和迁移,增加PTEN蛋白表达,但对乳腺癌细胞中AKT/P-AKT蛋白表达无明显改变。采用GraphPad Prism 6软件进行非参数单因素方差分析和t检验。结论:总之,miR-451a的过表达似乎可以增强乳腺癌细胞对卡铂治疗的化疗敏感性。因此,它可能为miR-451a对乳腺癌化疗耐药的管理提供新的思路,并可能成为未来癌症治疗的有益策略。然而,需要进一步的研究,特别是在其他信号通路方面的研究。
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引用次数: 0
Phytochemical analysis and antioxidant activity of eight cultivars of tea (Camellia sinensis) and rapid discrimination with FTIR spectroscopy and pattern recognition techniques 8个茶树品种的植物化学分析、抗氧化活性及FTIR光谱和模式识别技术的快速鉴别
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-07-08 DOI: 10.34172/ps.2022.27
Fatemeh Yousefbeyk, Heshmatollah Ebrahimi-Najafabadi, Sara Dabirian, Salar Salimi, Farshid Baniardalani, Saeed Ghasemi
Background: Tea (Camellia sinensis L.O. Kuntze) is one of the most commonly consumed beverages globally, with several beneficial health effects. The composition of leaves is affected by different factors such as climate and tea cultivar. Methods: In this study, the total phenolic, flavonoid, and tannin contents, and antioxidant activities of eight cultivars of tea growing in Iran were determined. The epigallocatechin gallate (EGCG) contents were measured by high-performance liquid chromatography (HPLC) analysis. The Fourier-transform infrared (FT-IR) spectra were used to construct a supervised pattern recognition model using a genetic algorithm-support vector machine (GA-SVM) for the classification of cultivars. Results: The results indicated a wide variation of total phenolic content (178.04 to 316.09 mg gallic acid equivalents (GAE)/g extract). Also, the flavonoid contents ranged from 25.54 to 41.1 mg quercetin equivalents )QE(/g extract. All the samples had close tannin amounts (ranging from 40.32 to 45.90 mg as tannic acid equivalent (TAE)/g extract). There was a significant linear relationship among total phenolic and flavonoid contents and antioxidant properties. The cultivars DN, PK2, and C.Y.9 had the highest content of phenolic and flavonoid content as well as the best antioxidant activity. The EGCG contents were from 2.66 to 4.12%. The highest amount of EGCG was found in cultivars 282, PK2, and C.Y.9. The discriminative region of FT-IR spectra (1350-1650 cm-1) were selected using a GA-SVM. This model showed 100% sensitivity and specificity for training and test sets. Conclusion: The leaves phytochemical compositions and antioxidant effect are deeply dependent on the type of tea cultivars. The cultivars PK2 and C.Y.9 can be considered richer sources of polyphenols, especially EGCG. The eight different cultivars can be classified based on chemical components using the recorded FT-IR spectra.
背景:茶(Camellia sinensis L.O. Kuntze)是全球最常见的饮料之一,具有多种有益健康的功效。茶叶的成分受气候、品种等因素的影响。方法:测定伊朗8个茶叶品种的总酚、类黄酮、单宁含量及抗氧化活性。采用高效液相色谱法测定了没食子儿茶素没食子酸酯(EGCG)的含量。利用傅里叶变换红外(FT-IR)光谱,建立了基于遗传算法-支持向量机(GA-SVM)的有监督模式识别模型,用于品种分类。结果:总酚含量变化较大(178.04 ~ 316.09 mg没食子酸当量/g提取物)。黄酮类化合物含量为25.54 ~ 41.1 mg槲皮素当量(QE) /g。所有样品的单宁含量相近(单宁酸当量(TAE)为40.32 ~ 45.90 mg /g)。总酚和类黄酮含量与抗氧化性能呈显著的线性关系。品种DN、PK2和C.Y.9的酚类和类黄酮含量最高,抗氧化活性最好。EGCG含量为2.66% ~ 4.12%。EGCG含量最高的品种是282、PK2和C.Y.9。利用GA-SVM选择FT-IR光谱的判别区(1350 ~ 1650 cm-1)。该模型对训练集和测试集具有100%的灵敏度和特异性。结论:茶树叶片的化学成分和抗氧化作用与茶树品种密切相关。品种PK2和C.Y.9可以被认为是更丰富的多酚来源,特别是EGCG。利用记录的FT-IR光谱可以根据化学成分对8个不同品种进行分类。
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引用次数: 1
Effect of Delphinium denudatum Wall. (Jadwar) on knee osteoarthritis: A randomized double-blinded placebo-controlled clinical trial 白玉飞燕壁的作用。(Jadwar)对膝关节骨关节炎的治疗:一项随机双盲安慰剂对照临床试验
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-06-11 DOI: 10.34172/ps.2022.26
Roghayeh Baghervand Navid, M. Karimi, M. Ghojazadeh, Alireza Bagherzadeh-karimi, R. Mohammadinasab, S. Dolati, Mehri Basnas, Roya Cheraghi, S. Fazljou
Introduction: Osteoarthritis (OA) is the most common disease of joints. The management of OA is challenging due to the efficacy and safety of treatments. In recent decades, traditional herbal medicines have been introduced for treatment of disease. Delphinium denudatum Wall. (Jadwar) is a medicinal herb with a long-lasting usage in traditional Persian medicine for joint diseases. The present study aimed to investigate the effect of Jadwar on pain and symptoms of knee OA. Methods: In this randomized double-blind placebo-controlled trial, 104 patients with knee OA were randomly assigned into two groups of intervention and control. While the intervention group received one Jadwar capsule (500 mg) twice a day for four weeks, the control group received placebo capsules. The primary outcomes, including pain, stiffness, and physical activity were evaluated using the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) questionnaire and the Visual Analogue Scale (VAS) at baseline two and four weeks after the intervention. Results: Ninety-four participants completed the study. Considering the time of interaction, after four weeks, data analysis revealed a significant decrease in the VAS score (37.23±12.58 vs. 57.87±13.21), total WOMAC score (24.83±9.70 vs. 49.17±12.89), WOMAC pain score (7.19±2.90 vs. 12.40±4.46), stiffness (2.06± 0.845 vs. 4.11±1.14), and physical function (15.57±7.25 vs. 32.66±9.78) in the intervention group compared to the control group (P<0.0001 for all outcomes). Additionally, no serious adverse effects were reported. Conclusions: Jadwar can be suggested as a safe medicinal plant for knee OA because it can relieve the pain and symptoms of OA.
骨关节炎(OA)是最常见的关节疾病。由于治疗的有效性和安全性,OA的管理具有挑战性。近几十年来,传统草药被用于治疗疾病。飞燕草壁。(Jadwar)是一种草药,在传统波斯医学中长期用于治疗关节疾病。本研究旨在探讨Jadwar对膝关节OA疼痛和症状的影响。方法:采用随机双盲安慰剂对照试验,将104例膝关节OA患者随机分为干预组和对照组。干预组服用Jadwar胶囊(500毫克),每天两次,持续四周,对照组服用安慰剂胶囊。主要结果包括疼痛、僵硬和身体活动,在干预后的基线2周和4周使用西安大略省和麦克马斯特大学骨关节炎指数(WOMAC)问卷和视觉模拟量表(VAS)进行评估。结果:94名参与者完成了研究。考虑到相互作用的时间,4周后,数据分析显示,干预组VAS评分(37.23±12.58比57.87±13.21)、WOMAC总分(24.83±9.70比49.17±12.89)、WOMAC疼痛评分(7.19±2.90比12.40±4.46)、僵硬度(2.06±0.845比4.11±1.14)、身体功能(15.57±7.25比32.66±9.78)均较对照组显著降低(各指标P<0.0001)。此外,没有严重的不良反应报告。结论:黄芪可有效缓解膝关节炎的疼痛和症状,可作为治疗膝关节炎的安全药用植物。
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引用次数: 0
The Role of Andrographis paniculata in Modulating the Immune Response in Cancer-Associated Chronic Inflammation, Angiogenesis, and Metastasis 穿心莲在调节癌症相关慢性炎症、血管生成和转移的免疫反应中的作用
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-06-09 DOI: 10.34172/ps.2022.25
Rengganis Ulvia, A. P. Gani, R. Murwanti
The immune system plays an essential role in cancer pathogenesis through providing an inflammatory immune response. Chronic inflammation causes tumor growth, angiogenesis, and metastasis facilitated by interactions between tumor, immune, and stromal cells in the tumor microenvironment (TME). Various inflammatory mediators and growth factors secreted by cells in the TME exert a synergistic effect on cancer promotion. Thus, the development of cancer therapies that lead to inhibition of the activity of immune cells, cytokines, chemokines, and cancer-inducing growth factors is a promising therapeutic strategy. Andrographis paniculata (A. paniculata) is an ethnomedicinal plant with immunomodulatory and anticancer activity. A. paniculata can also inhibit the resistance of chemotherapy agents associated with the TME as adjuvant chemotherapy. This review focuses on the mechanism of A. paniculata in suppressing cancer-associated chronic inflammation, angiogenesis, and metastasis through modulation of the immune response. The results show that A. paniculata exerts anticancer effects directly targeting cancer cells, inhibiting cancer growth by modulating immune responses. A. paniculata exerts anticancer effects by inhibiting the production of cytokines, growth factors, and chemokines via the nuclear factor-kappa B (NF-ĸB), mitogen-activated protein kinase (MAPK), Janus kinase (JAK)/signal transducer and activator of transcription (STAT) signaling pathways. In addition, this review provides a new hypothesis regarding the potential of A. paniculata to serve as an anticancer agent that can inhibit cancer cell proliferation at the angiogenesis and metastatic stages through regulating inflammation due to interactions between cancer cells, immune cells, and stromal cells in the TME.
免疫系统通过提供炎症免疫反应在癌症发病机制中发挥重要作用。在肿瘤微环境(TME)中,肿瘤、免疫细胞和基质细胞之间的相互作用促进了慢性炎症引起肿瘤生长、血管生成和转移。TME细胞分泌的多种炎症介质和生长因子在促癌过程中发挥协同作用。因此,开发抑制免疫细胞、细胞因子、趋化因子和癌症诱导生长因子活性的癌症疗法是一种很有前途的治疗策略。穿心莲(A. paniculata)是一种具有免疫调节和抗癌作用的民族药材。作为辅助化疗,金针叶还能抑制化疗药物对TME的耐药性。本文就金针叶通过调节免疫反应抑制肿瘤相关慢性炎症、血管生成和转移的机制进行综述。结果表明,金针叶直接针对癌细胞发挥抗癌作用,通过调节免疫反应抑制癌细胞生长。金银花通过核因子- κ B (NF- -ĸB)、丝裂原活化蛋白激酶(MAPK)、Janus激酶(JAK)/信号转导和转录激活因子(STAT)信号通路抑制细胞因子、生长因子和趋化因子的产生,发挥抗癌作用。此外,本综述还提出了一种新的假设,即金针叶作为一种抗癌药物,可以通过调节肿瘤细胞、免疫细胞和基质细胞之间的相互作用,抑制肿瘤细胞在血管生成和转移阶段的增殖。
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引用次数: 1
Construction and transfer of PEI-miRNA-126/210 polyplex into Human Umbilical Vein Endothelial Cells with investigation of its effect on islets survival and function PEI-miRNA-126/210复合物在人脐静脉内皮细胞中的构建和转移及其对胰岛存活和功能的影响
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-06-06 DOI: 10.34172/ps.2022.24
F. Sabet Sarvestani, A. Tamaddon, M. Karimi, R. Yaghoobi, B. Geramizadeh, M. Heydari, I. Al-Abdullah, N. Azarpira
Background:Type 1 diabetes is an autoimmune disorder characterized by the loss of pancreatic islets. Islet allotransplantation is a potentially beneficial therapeutic approach for diabetes. Islets suffer a variety of cellular insults including ischemia and partial vascular loss during isolation, resulting in a significant reduction in viability prior to transplantation. The present study aimed to investigate the effect of angiogenic microRNA (miRNA)-126 and -210 on islet function and viability in an indirect way. Methods:Poly Ethylenimine (PEI)-miRNA-126 and -210 polyplexes were constructed at various Nitrogen/Phosphate (N/P) ratios. After confirmation by gel retardation and ethidium bromide dye exclusion assay, its cytotoxicity and transfection efficiency were analyzed by MTT and fluorescent assays, respectively. After that, the selected polyplexes were used to transfect Human Umbilical Vein Endothelial Cells (HUVECs) in vitro and were indirectly co-cultured with islet cells for three days. Real-time polymerase chain reaction and enzyme-linked immunoassay were conducted to verify the regulation of target genes and the functionality of the islets. Results:The findings showed that PEI could condense miRNAs at N/P=5. The viability of the HUVECs was decreased by increasing the amount of PEI. Additionally, ployplex-126 and -210 led to a decrease in the expressions of target genes, phosphoinositol-3 kinase regulatory subunit 2, sprouty-related EVH1 domain-containing protein 1, and ephrin-A3 in the islets. Moreover, the expressions of Bax and Bcl2 and their ratio in the treated groups by polyplex-126 and -210 led to better survival and function of the islets, with a higher expression of insulin and response to glucose stimulations. Furthermore, polyplex-210 could downregulate the anti-angiogenic protein, thrombospondin 1, compared to the other groups. Finally, the secretion of C-peptide was higher in polyplex-210 than in the other groups, adjusted for insulin secretion. Conclusion:The results indicated that angiogenic miRNAs could promote the survival and function of islet cells by interacting with their targets.
背景:1型糖尿病是一种以胰岛丧失为特征的自身免疫性疾病。胰岛异体移植是一种潜在的有益的糖尿病治疗方法。胰岛在分离期间遭受各种细胞损伤,包括缺血和部分血管丧失,导致移植前生存能力显著降低。本研究旨在间接探讨血管生成microRNA (miRNA)-126和-210对胰岛功能和活力的影响。方法:以不同的氮/磷酸盐(N/P)比构建聚乙亚胺(PEI)-miRNA-126和-210多聚物。经凝胶阻滞和溴化乙锭染色排除试验证实后,分别用MTT法和荧光法分析其细胞毒性和转染效率。之后,将选择的复合物体外转染人脐静脉内皮细胞(HUVECs),并与胰岛细胞间接共培养3天。实时聚合酶链反应和酶联免疫分析验证靶基因的调控和胰岛的功能。结果:PEI能在N/P=5时凝聚miRNAs。随着PEI用量的增加,HUVECs的活力降低。此外,ployplex-126和-210导致靶基因、磷酸肌醇-3激酶调控亚基2、发芽相关EVH1结构域含蛋白1和ephrin-A3在胰岛中的表达减少。此外,在polyplex-126和-210处理组中,Bax和Bcl2的表达及其比值导致胰岛的生存和功能改善,胰岛素表达增加,对葡萄糖刺激的反应增加。此外,与其他组相比,polyplex-210可以下调抗血管生成蛋白血栓反应蛋白1。最后,经胰岛素分泌调整后,polyplex-210的c肽分泌高于其他组。结论:血管生成mirna可通过与靶细胞的相互作用促进胰岛细胞的存活和功能。
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引用次数: 0
Modulation of Nrf2 by activation of estrogen receptor β as a therapeutic strategy to prevent cancer development and overcome inflammation-related drug resistance in breast cancer 通过激活雌激素受体β调节Nrf2作为预防癌症发展和克服乳腺癌炎症相关耐药的治疗策略
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-05-11 DOI: 10.34172/ps.2022.23
Emdormi Rymbai, D. Sugumar, J. Selvaraj, Ram Kothandam, Divakar Selvaraj
Despite the tremendous progress in breast cancer diagnosis and treatment, the mortality rate is expected to increase due to the emergence of drug resistance. Pro-inflammatory markers are thought to contribute to drug resistance by activation of its naive receptors and its downstream signaling pathways. Elevation of pro-inflammatory markers leads to an increase in the biosynthesis of estrogen which can promote the proliferation of estrogen receptor (ER)+ breast cancer. Inflammation also results in obesity which is one of the key risk factors. Estrogen receptor-beta (ER-β) is an important target that has been widely studied and accepted to possess anti-cancer activity in a number of cancers including breast cancer. ER-β elicits its action through genomic and non-genomic pathways. The genomic pathway increases the transcription of potent cyclin-dependent kinase inhibitor (p21), and tumor suppressor genes such as melanoma differentiation associated gene 7 and tumor protein (p53). The non-genomic pathway works through protein-protein interaction and phosphorylation. Here, we propose that the activation of ER-β might enhance the activation of nuclear factor-erythroid factor 2-related factor 2 (Nrf2) via estrogen receptor-alpha (ER-α) repression. The activation of Nrf2 increases the transcription of antioxidant genes such as NADH quinone oxidoreductase 1 (NQO1), heme oxygenase-1 (HO-1), etc., and decreases the expression of pro-inflammatory genes such as tumor necrosis factor-α (TNF-α), interleukin-1 (IL-1), etc. This review hypothesizes and suggests that ER-β agonists could play a beneficial role to overcome inflammation-related drug resistance by modulation of the Nrf2/antioxidant response element (Nrf2/ARE) pathway.
尽管在乳腺癌诊断和治疗方面取得了巨大进展,但由于出现耐药性,死亡率预计会增加。促炎标记物被认为通过激活其初始受体及其下游信号通路来促进耐药。促炎标志物的升高导致雌激素的生物合成增加,从而促进雌激素受体(ER)阳性乳腺癌的增殖。炎症也会导致肥胖,这是一个关键的危险因素。雌激素受体β (Estrogen - receptor -β, ER-β)是一个重要的靶点,在包括乳腺癌在内的多种癌症中具有抗癌活性,已被广泛研究和接受。ER-β通过基因组和非基因组途径引发其作用。基因组途径增加了强效周期蛋白依赖性激酶抑制剂(p21)和肿瘤抑制基因(如黑色素瘤分化相关基因7和肿瘤蛋白(p53))的转录。非基因组途径通过蛋白-蛋白相互作用和磷酸化起作用。本研究提出,ER-β的激活可能通过雌激素受体α (ER-α)抑制来增强核因子-红细胞因子2相关因子2 (Nrf2)的激活。Nrf2的激活增加了NADH醌氧化还原酶1 (NQO1)、血红素氧合酶1 (HO-1)等抗氧化基因的转录,降低了肿瘤坏死因子-α (TNF-α)、白细胞介素-1 (IL-1)等促炎基因的表达。这篇综述假设并表明,ER-β激动剂可能通过调节Nrf2/抗氧化反应元件(Nrf2/ARE)途径,在克服炎症相关的耐药中发挥有益作用。
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引用次数: 0
The novel pharmacological approaches to coumestrol: focusing on the psychiatric and neurological benefits and the newly identified receptor interactions 新药理学途径库美司醇:专注于精神病学和神经学的益处和新发现的受体相互作用
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-05-08 DOI: 10.34172/ps.2022.22
K. Fekri, A. Mohajjel Nayebi, J. Mahmoudi, S. Sadigh-Eteghad
For years, the health benefits of coumestrol (CMT) have been investigated by researchers around the world. Anti-oxidative properties of the phytoestrogen which can be extracted from several plant tissues, have already been reported as well as the cancer chemopreventive capabilities. Recently, psychiatric and neurological effects of this natural compound have become of interest to researchers so that strong evidence would support the idea that CMT can exert significant effects on the central nervous system. Pharmacologically, this phytoestrogen would act as a selective estrogen receptor modulator with several-fold more affinity to β sub-types of the receptors (ERβ); although other mechanisms of action may be involved. The aim of this review was to gather the recent reports regarding the most important pharmacological benefits of CMT focusing on the psychiatric and neurological ones. Furthermore, the mechanisms of action underlying the pharmacological effects were tried to be clarified more. For this purpose, some keywords such as "Coumestrol", "Pharmacological Effects", "Neurologic", "Psychiatric" and "Neuropsychiatric" were searched in popular scientific databases such as Google scholar, Scopus and Pubmed. Then the delegated documentations were brought together, categorized and discussed on this basis. Reviewing the gathered information showed that, apart from the effects on reproduction and the related organs which are mainly conducted through estrogen receptors, CMT has reported to improve various disorders all over the body. Particularly, regarding the neurological and psychiatric systems, the advantages in cerebral hypoxia-ischemia, the Alzheimer’s disease, anxiety, depression and cognitive impairments would be the most important ones. Here, other receptors that have shown interactions with CMT (beside estrogen receptors which are the main target), were also reviewed among which insulin receptors, farnesoid X receptors, pregnane X receptors, and constitutive androstane receptors can be mentioned while only the last two seem to be involved in forming the neurological and psychiatric effects.
多年来,世界各地的研究人员一直在研究库美特罗(CMT)的健康益处。植物雌激素可从多种植物组织中提取,其抗氧化特性和癌症化学预防能力已被报道。最近,这种天然化合物对精神和神经系统的影响引起了研究人员的兴趣,因此强有力的证据将支持CMT可以对中枢神经系统产生重大影响的观点。药理学上,该植物雌激素可作为选择性雌激素受体调节剂,对受体β亚型(ERβ)具有数倍的亲和力;尽管可能涉及其他作用机制。本综述的目的是收集最近关于CMT最重要的药理学益处的报道,主要集中在精神病学和神经学方面。此外,还试图进一步阐明其药理作用的作用机制。为此,在Google scholar、Scopus和Pubmed等热门科学数据库中检索了“Coumestrol”、“药理效应”、“神经学”、“精神病学”和“神经精神病学”等关键词。然后在此基础上对委托的文件进行整理、分类和讨论。回顾收集到的资料表明,CMT除了主要通过雌激素受体对生殖和相关器官产生影响外,还报道了对全身各种疾病的改善。特别是在神经和精神系统方面,在脑缺氧缺血、阿尔茨海默病、焦虑、抑郁和认知障碍方面的优势将是最重要的。本文还综述了与CMT相互作用的其他受体(除了雌激素受体是主要靶点),其中包括胰岛素受体、法内甾体X受体、妊娠X受体和构形雄甾受体,但似乎只有后两种受体参与形成神经和精神效应。
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引用次数: 0
Utilizing Nanoparticle Catalyzed TMB/H2O2 System for Determination of Aspirin in Exhaled Breath Condensate 纳米粒子催化TMB/H2O2体系测定呼出液中阿司匹林
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-05-06 DOI: 10.34172/ps.2022.21
Samineh Mohammadzadeh Abachi, Homa Rezaei, M. Khoubnasabjafari, V. Jouyban-Gharamaleki, E. Rahimpour, A. Jouyban
Background: According to the poison center data for most countries, more than thousands of people’s exposure to aspirin or salicylate-containing products. So, this work aimed was to offer a rapid colorimetric method for monitoring aspirin concentration in exhaled breath condensate (EBC). Methods: A method based on a redox reaction catalyzed by nanoparticles was validated for the analysis of aspirin. 3,3 ,5,5 –Tetramethyl benzidine /H2O2 and sodium dodecyl sulfate modified silver nanoparticles were used as the redox reagents and catalyst, respectively. Results: Detection mechanism of aspirin using this system is based on the inhibitory effect of aspirin on the signal intensity of the colorimetric systems. Since the decrement in signal intensity was proportional to aspirin level, a colorimetric method was proposed for its quantification in EBC samples. This method shows a linear relationship with aspirin concentration in the range of 10‒250 mg.L−1 with a relative standard deviation of < 3.5%. Conclusion: This method has great potential for aspirin determination due to some features such as high reliability, and fast response time.
背景:根据大多数国家中毒中心的数据,成千上万的人暴露于阿司匹林或含有水杨酸的产品。因此,本工作旨在提供一种快速比色法监测呼出液(EBC)中阿司匹林浓度。方法:采用纳米颗粒催化氧化还原反应分析阿司匹林。以3,3,5,5 -四甲基联苯胺/H2O2和十二烷基硫酸钠修饰的纳米银分别作为氧化还原试剂和催化剂。结果:该系统检测阿司匹林的机制是基于阿司匹林对比色系统信号强度的抑制作用。由于信号强度的衰减与阿司匹林水平成正比,因此提出了一种比色法定量测定EBC样品中的阿司匹林。该方法与阿司匹林浓度在10 ~ 250 mg范围内呈线性关系。L−1,相对标准偏差< 3.5%。结论:该方法具有可靠度高、反应速度快等特点,具有很大的应用潜力。
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引用次数: 1
Effect of a probiotic preparation on gut microbiota in critically ill septic patients admitted to intensive care unit: A pilot randomized controlled trial 益生菌制剂对重症化脓症患者肠道菌群的影响:一项随机对照试验
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-04-25 DOI: 10.34172/ps.2022.20
A. Mahmoodpoor, Roya Ghaemi, Kamran Shadvar, S. Saghaleini, Sama Rahnemayan, Ali Shamekh, S. Sanaie
Background: Sepsis promotes severe physiologic alterations in patients, and it has been reported to induce profound changes in the gut microbial composition. The decrease of 'health ‑benefiting' microbes and the increase in dysbiosis in critically ill patients are thought to induce or aggravate sepsis. In this study, we aimed to explore the effect of a probiotic preparation, Lactocare®, on gut microbiota in critically ill septic patients admitted to the intensive care unit (ICU). Methods: Forty critically ill patients diagnosed with sepsis were assessed in this pilot randomized controlled trial. Patients were randomized into two groups: Lactocare and control groups. Patients in the Lactocare group received two capsules of Lactocare® for 10 days. Fecal samples were taken from all patients on days 1 and 10 for determining the gut microbial pattern. The primary outcome was gut microbial flora, and secondary outcomes were intensive care unit (ICU) length of stay and mortality. Results: Intragroup changes showed that all microbial flora considerably changed during the study period; the number of microbial flora significantly decreased in the control group and increased in the Lactocare group. Patients in the Lactocare group had a significantly lower incidence of diarrhea and infection with multidrug-resistant organisms. There was no difference in ICU length of stay in the Lactocare group compared to the control group (p= 0.289). The mortality rate was 30% in the control group compared to 20% in the Lactocare group (p: 0.465). Conclusions: This study showed a remarkable effect of the probiotic preparation on the gut microbiota in critically ill septic patients as it decreased the number of opportunistic pathogens. However, additional clinical research is needed to translate research into clinical practice to refine the clinical indication of the specific probiotic strains.
背景:脓毒症促进患者严重的生理改变,据报道,脓毒症会引起肠道微生物组成的深刻变化。在危重病人中,“有益健康”的微生物减少和生态失调增加被认为会诱发或加重败血症。在这项研究中,我们旨在探讨益生菌制剂乳护®对重症监护室(ICU)重症脓毒症患者肠道微生物群的影响。方法:对40例诊断为脓毒症的危重患者进行随机对照试验。患者随机分为两组:乳护组和对照组。乳护理组患者连续10天服用两粒乳护理®胶囊。在第1天和第10天采集所有患者的粪便样本以确定肠道微生物模式。主要结局是肠道微生物菌群,次要结局是重症监护病房(ICU)的住院时间和死亡率。结果:组内变化表明,在研究期间,所有微生物区系都发生了显著变化;对照组微生物菌群数量显著减少,乳糖组微生物菌群数量显著增加。乳护组患者腹泻和多重耐药菌感染的发生率显著降低。与对照组相比,乳护理组的ICU住院时间无差异(p= 0.289)。对照组的死亡率为30%,而乳护理组为20% (p: 0.465)。结论:本研究显示益生菌制剂对脓毒症危重患者肠道菌群有显著影响,可减少条件致病菌的数量。然而,需要更多的临床研究将研究转化为临床实践,以完善特定益生菌菌株的临床适应症。
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引用次数: 0
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Infarma Pharmaceutical Sciences
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