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Fully Automated Methods for [18F]FDG and [18F]-NaF Productions Using Explora FDG4: Validation and Reliability of Multi-Subsequent Preparations for Clinical Applications. 使用Explora FDG4生产[18F]FDG和[18F]-NaF的全自动方法:临床应用多后续制剂的验证和可靠性。
IF 2.3 4区 医学 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-05-18 DOI: 10.2174/1874471015666220518115244
E. Awad, H. Ali, James Lamb, E. Al‐Momani
BACKGROUND The worldwide usage of [18F]-sodium fluoride in clinical applications increase the interest of the facility of its production. The development of a new automated method for multi-preparations of [18F]-NaF and [18F]FDG on an Explora FDG4 module is described. Explora FDG4 is one of the most widely used synthesizers for FDG production in daily routine use and specifically designed to run up to four different productions with single module. Therefore, slight modifications were carried out in order to increase the potential of the synthesizer to perform more radiopharmaceuticals. METHODS A fully automated method for multi-preparations of [18F]-NaF and [18F]FDG using Explora FDG4 was performed. Slight modifications of the Explora's hardware and software configuration were applied. A new elution vial for NaF preparation was installed and connected to the free position to MVP1. Quality control was carried-out using the standard analytical methods that applied for GMP production. RESULTS This modification successfully provides preparation of [18F]-NaF without affecting the daily FDG production using one set preparation. [18F]-NaF was obtained in a high radiochemical yield (>90%, n=100) in 10 min total preparation time. The quality control results for both obtained products FDG (RCP >95%) and NaF (RCP >98%)showed that the radiopharmaceuticals were in compliance with USP and Ph.Eur. specifications and compatible with clinical applications. CONCLUSION A rapid and simple method for multi preparations of [18F]-NaF and [18F]FDG using single Explora module was designed. Yet, the chemistry module has the potential to generate more radiopharmaceuticals to decrease the cost of preparation of [18F]-NaF comparing with the cassette-based synthesizers, reducing radiation exposure resulted by manual preparations and increase the reproducibility of [18F]-NaF preparation.
[18F]-氟化钠在世界范围内的临床应用增加了对其生产设施的兴趣。本文介绍了在Explora FDG4模块上开发的一种新的自动化方法,用于多种制备[18F]-NaF和[18F]FDG。explorora FDG4是在日常使用中最广泛使用的FDG生产合成器之一,专门设计用于运行多达四个不同的生产与单个模块。因此,进行了轻微的修改,以增加合成器的潜力,以执行更多的放射性药物。方法采用Explora FDG4全自动制备[18F]-NaF和[18F]FDG。对探索者的硬件和软件配置进行了轻微的修改。安装了一个新的NaF制备洗脱瓶,并连接到MVP1的自由位置。质量控制采用GMP生产标准的分析方法进行。结果该修饰成功地制备了[18F]-NaF,而不影响每天的FDG产量。[18F]-NaF在10 min的总制备时间内获得了很高的放射化学产率(>90%,n=100)。所得产品FDG (RCP >95%)和NaF (RCP >98%)的质量控制结果表明,两种放射性药物均符合USP和Ph.Eur标准。规格和兼容临床应用。结论设计了一种快速简便的用单个explore模块制备[18F]-NaF和[18F]FDG的方法。然而,与盒式合成器相比,化学模块有潜力产生更多的放射性药物,以降低[18F]-NaF的制备成本,减少手工制备造成的辐射暴露,提高[18F]-NaF制备的可重复性。
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引用次数: 0
Assessment of knowledge and level of radiation safety awareness among Radiographers working in Nuclear Medicine. 评估从事核医学工作的放射技师的辐射安全知识及意识水平。
IF 2.3 4区 医学 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-04-25 DOI: 10.2174/1874471015666220425121713
Mpumelelo Nyathi
BACKGROUNDRadiopharmaceuticals are used for diagnosis, treatment, staging and follow up of various diseases. However, there is concern that the ionizing radiation (gamma rays, α and ß particles) may result in the exposure of radiographers with limited knowledge of the principles of radiation protection and safety, raising the risk of cancer induction.OBJECTIVETo investigate the knowledge and level of radiation safety awareness among radiographers at a tertiary hospital.METHODSIt is an analytical cross-sectional study. A validated two-part questionnaire was implemented to consenting radiographers in a Nuclear Medicine Department. Part 1 gathered demographic information (age, gender, work experience, attendance to/or passing ionizing radiation protection courses). Part 2 covered questions related to knowledge and level of awareness of radiation protection principles.RESULTSFive radiographers voluntary participated (2/5 were males while 3/5 were females). Three age groups were distinguishable, 21-30, 41-50 and 51-60 years. In the age group of 21-30 years, there was one male with just over 4 years of experience while in the age group 41-50, there were three females with less than three years of experience and in the age group 51-60, there was one male radiographer with over 20 years of experience. All the radiographers showed a high level of awareness and knowledge of radiation safety principles.CONCLUSIONEducation coupled with training in radiation protection is an essential tool for instilling radiation awareness among radiographers. However, education alone is not enough, further skills in preparation and administration of radiopharmaceuticals will reduce exposures.
背景放射性药物用于各种疾病的诊断、治疗、分期和随访。然而,有人担心电离辐射(伽马射线、α和ß粒子)可能会导致放射技师在辐射防护和安全原则知识有限的情况下暴露,从而增加癌症诱发的风险。目的了解某三级医院放射技师辐射安全知识及意识水平。方法这是一项分析性的横断面研究。一份经验证的由两部分组成的问卷被应用于核医学部门的同意放射技师。第1部分收集了人口统计信息(年龄、性别、工作经验、参加/或通过电离辐射防护课程)。第2部分涉及与辐射防护原则的知识和意识水平有关的问题。结果放射技师自愿参加(2/5为男性,3/5为女性)。三个年龄组是可区分的,21-30岁,41-50岁和51-60岁。在21-30岁的年龄组中,有一名男性有4年以上的工作经验,而在41-50岁的年龄段中,有三名女性的工作经验不足3年,在51-60岁的年龄段里,有一位男性放射技师的工作经验超过20年。所有放射技师对辐射安全原则的认识和知识都很高。结论辐射防护教育与培训是在放射技师中灌输辐射意识的重要工具。然而,光靠教育是不够的,进一步掌握放射性药物的制备和管理技能将减少暴露。
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引用次数: 0
Assessment of radiation exposure dose for nuclear medicine workers from 18F-FDG, 99mTc MDP and 99mTc. 核医学工作人员18F-FDG、99mTc - MDP和99mTc辐射暴露剂量评估。
IF 2.3 4区 医学 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-04-13 DOI: 10.2174/1874471015666220413114927
Abdulrahman M Al-Esaei, Emran Eisa Saleh, R. M. E. Shazly, S. Elmaghraby, M. Khalil, A. Kany
BACKGROUNDNuclear medicine or diagnostic radiology personnel are always exposed to low-level radiation from radionuclides used in medical diagnostics, which lead to potential biological hazards or effects.OBJECTIVEExternal exposure for workers in two nuclear medicine centers was measured by recruiting 120 patients.METHODSThree nuclear medicine examinations were performed using F18-FDG PET/CT, 99mTc-MDP bones scan, and 99mTc thyroid scan by a digital radiation dosimeter.RESULTSThe average received accumulative radiation dose for workers was found to be 0.838±0.17, 0.527±0.11 and 0.270±0.05 μSv for F18-FDG PET/CT, 99mTc-MDP bones scan, and 99mTc thyroid scan, respectively. The annual effective dose for workers was estimated to be 2.09±0.42, 1.34±0.27 and 0.68±0.14 mSv, respectively. Moreover, the average patient-to-staff dose coefficients were found to be 0.024±0.005, 0.003±0.001, and 0.007±0.002 μSv m2/MBq h for F18-FDG PET/CT, 99mTc-MDP bones scan, and 99mTc thyroid scan, respectively.CONCLUSIONIt is clear from the results that the radiation doses received by workers during the nuclear medicine imaging examinations were less than the doses recommended by the International Commission on Radiological Protection (ICRP) for such examinations.
背景核医学或放射诊断人员总是暴露在医疗诊断中使用的放射性核素的低水平辐射下,这会导致潜在的生物危害或影响。目的通过招募120名患者,测量两个核医学中心工作人员的外照射。方法应用F18-FDG PET/CT、99mTc-MDP骨显像和99mTc-甲状腺数字放射剂量仪进行三项核医学检查。结果F18-FDG PET/CT、99mTc-MDP骨骼扫描和99mTc-甲状腺扫描的工人平均累积辐射剂量分别为0.838±0.17、0.527±0.11和0.270±0.05μSv。工人的年有效剂量估计分别为2.09±0.42、1.34±0.27和0.68±0.14 mSv。此外,F18-FDG PET/CT、99mTc-MDP骨骼扫描和99mTc甲状腺扫描的患者与工作人员的平均剂量系数分别为0.024±0.005、0.003±0.001和0.007±0.002μSv m2/MBq h。结论从结果中可以清楚地看出,工作人员在核医学成像检查中接受的辐射剂量低于国际辐射防护委员会(ICRP)为此类检查建议的剂量。
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引用次数: 3
Methodological aspects and prognostic value of metabolic tumor volume assessed with 18F-FDG PET/CT in lymphomas. 18F-FDG PET/CT评估淋巴瘤代谢肿瘤体积的方法学方面和预后价值。
IF 2.3 4区 医学 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-03-29 DOI: 10.2174/1874471015666220329120631
F. Tutino, E. Giovannini, S. Pastorino, O. Ferrando, G. Giovacchini, A. Ciarmiello
Metabolic tumor volume (MTV) assessed by pretreatment 18F-FDG PET/CT has shown significant prognostic value across many lymphoma types, although not yet used in clinical practice for technical concerns and need for standardization. Numerous studies on the prognostic value of MTV in lymphomas have been published in recent years, but there is still no full agreement on the best methodology for MTV calculation. In this paper, we reviewed the methodological aspects of MTV assessment and reported recent works about its impact on outcome in lymphomas, with a focus on Hodgkin lymphoma (HL) and diffuse large B cell lymphoma (DLBCL).
通过预处理18F-FDG PET/CT评估的代谢肿瘤体积(MTV)在许多淋巴瘤类型中显示出显著的预后价值,尽管由于技术问题和标准化需求,尚未在临床实践中使用。近年来,关于MTV在淋巴瘤中的预后价值的许多研究已经发表,但对于MTV计算的最佳方法仍然没有完全一致。在本文中,我们回顾了MTV评估的方法学方面,并报道了其对淋巴瘤预后影响的最新工作,重点是霍奇金淋巴瘤(HL)和弥漫性大B细胞淋巴瘤(DLBCL)。
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引用次数: 0
Imperatorin attenuates proliferation of MCF-7 Cells in combination with Radiotherapy or Hyperthermia. Imperatorin与放射治疗或热疗相结合可减弱MCF-7细胞的增殖。
IF 2.3 4区 医学 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-03-18 DOI: 10.2174/1874471015666220318122202
P. Amini, Saeedeh Jafari Nodooshan, M. Ashrafizadeh, A. Aliasgharzadeh, Z. Vakili, S. Tavakoli, T. Aryafar, A. Musa, M. Najafi, S. Taeb, Bagher Farhood
AIMThe aim of this study was to evaluate possible sensitization effect of imperatorin (IMP) for radiotherapy and hyperthermia (HT).BACKGROUNDBreast cancer is one of the most common types of malignancies in the world. Cancer resistance is an unavoidable consequence of therapy with radiation or other modalities. Numerous researches aimed at improving cancer response to therapy are ongoing.OBJECTIVEThus, in this study, we investigated the potential sensitizing effect of IMP in combination with external radiotherapy (ERT) or HT.METHODAfter treatment of MCF-7 breast cancer cells with IMP, cells were exposed to 4 Gy X-rays or HT (42 °C for 1 hour). The viability of MCF-7 cells was measured using MTT assay. Furthermore, the expression of pro-apoptotic genes including Bax, Bcl-2, Caspase-3, Caspase-8 and Caspase-9 were investigated using real-time PCR. The sensitizing effect of IMP in combination with ERT or HT was calculated and compared to ERT or HT alone.RESULTSResults showed an increase in the expression of pro-apoptotic genes and downregulation of anti-apoptotic Bcl-2 following ERT and HT. Furthermore, cell viability reduced following these treatments. IMP was able to augment these effects of ERT and HT.CONCLUSIONIMP could increase the efficiency of HT and ERT. This effect of IMP may suggest it as an adjuvant for increasing the therapeutic efficiency of ERT.
目的评价欧前胡素(IMP)对放疗和热疗(HT)可能的致敏作用。背景:乳腺癌是世界上最常见的恶性肿瘤之一。癌症耐药性是放疗或其他治疗方式不可避免的结果。许多旨在改善癌症治疗反应的研究正在进行中。因此,本研究探讨了IMP联合外部放疗(ERT)或HT的潜在致敏效应。方法用IMP处理MCF-7乳腺癌细胞后,将细胞暴露于4 Gy x射线或高温(42°C)下1小时。MTT法测定MCF-7细胞活力。采用实时荧光定量PCR检测促凋亡基因Bax、Bcl-2、Caspase-3、Caspase-8、Caspase-9的表达。计算IMP联合ERT或HT的致敏效果,并与单独ERT或HT进行比较。结果ERT和HT后,促凋亡基因Bcl-2表达升高,抗凋亡基因Bcl-2表达下调。此外,这些处理后细胞活力降低。IMP能够增强ERT和HT的这些作用。结论imp能提高HT和ERT的治疗效率。IMP的这种作用可能表明它是一种提高ERT治疗效率的辅助剂。
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引用次数: 3
Does Heparin Affect 99mTc-MAA In Vitro Stability? 肝素是否影响99mTc-MAA的体外稳定性?
IF 2.3 4区 医学 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-01-01 DOI: 10.2174/1874471015666220204142608
Teresa Scotognella, Valerio Lanni, Fabiana Moresi, Alessio Rizzo, Andrea Guarneri, Venanzio Valenza

Introduction: Pulmonary embolism (PE) can be diagnosed by perfusion lung scintigraphy using human albumin macroaggregates labelled 99mTc (99mTc-MAA). When PE is suspected, subcutaneous Low Molecular Weight Heparin (LMWH) should be administered even before the results of the PE diagnostic flowchart. In our study, we aimed to evaluate a possible interaction (in vitro interference) between 99mTc-MAA and LMWH.

Methods: The reconstitution of MAA kit was performed according to the manufacturer's instruction. After labelling, we carried out the following preparations: a standard dose of 99mTc-MAA alone, as control; 99mTc-MAA and enoxaparin at different ratios. According to the manufacturer's instruction, the radiochemical purity was performed and evaluated immediately (T0), after 15 and 30 minutes after incubation (T15 and T30).

Results: We compared the radiochemical purity of 99mTc-MAA with: (i) radiochemical purity of 99mTc-MAA and enoxaparin (11 ratio), (ii) radiochemical purity of 99mTc-MAA and enoxaparin (0.5 ratio), and (iii) radiochemical purity of 99mTc-MAA and enoxaparin (ratio 2). No significant differences were found between all the measured parameters at each time point for each ratio. We also tested the stability of 99mTc-MAA in physiological conditions (at 37°C in PBS): the initial radiochemical purity of 99mTc-MAA was 99.78%. The values of 99mTc-MAA radiochemical purity were high in all conditions of possible interaction with LMWH, with values ranging from 98.00% at T0 to 95% at T30.

Conclusion: We found no statistically significant change in the in vitro stability of 99mTc-MAA in the presence of enoxaparin, excluding a possible direct interference. Future studies will be needed to check the 99mTc-MAA stability under physiological conditions.

肺栓塞(PE)可以通过使用人白蛋白大聚集体标记99mTc (99mTc- maa)进行肺灌注显像诊断。当怀疑PE时,应在PE诊断流程图结果出来之前就皮下注射低分子量肝素(LMWH)。在我们的研究中,我们旨在评估99mTc-MAA与低分子肝素之间可能的相互作用(体外干扰)。方法:按照生产厂家说明书对MAA试剂盒进行重组。标记后,我们进行了以下准备:标准剂量99mTc-MAA单独作为对照;99mTc-MAA与依诺肝素的不同比例。根据制造商的说明,在孵育15分钟和30分钟后(T15和T30)立即进行放射化学纯度检测和评估(T0)。结果:我们将99mTc-MAA的放射化学纯度与:(i) 99mTc-MAA与依诺肝素的放射化学纯度(11比),(ii) 99mTc-MAA与依诺肝素的放射化学纯度(0.5比),(iii) 99mTc-MAA与依诺肝素的放射化学纯度(2比)进行了比较。在每个比值的每个时间点,所有测量参数之间均无显著差异。我们还测试了99mTc-MAA在生理条件下(37℃PBS)的稳定性:99mTc-MAA的初始放射化学纯度为99.78%。99mTc-MAA放射化学纯度在所有可能与低分子肝素相互作用的条件下都很高,T0时为98.00%,T30时为95%。结论:我们发现在依诺肝素存在的情况下,99mTc-MAA的体外稳定性无统计学意义的变化,排除了可能的直接干扰。99mTc-MAA在生理条件下的稳定性有待进一步研究。
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引用次数: 0
Clinical Application of a High Sensitivity BGO PET/CT Scanner: Effects of Acquisition Protocols and Reconstruction Parameters on Lesions Quantification. 高灵敏度BGO PET/CT扫描仪的临床应用:采集方案和重建参数对病灶量化的影响。
IF 2.3 4区 医学 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-01-01 DOI: 10.2174/1874471015666220107100200
Elena De Ponti, Cinzia Crivellaro, Sabrina Morzenti, Lavinia Monaco, Sergio Todde, Claudio Landoni, Federica Elisei, Monica Musarra, Luca Guerra

Aims: The aim of this retrospective study was to investigate SUVs variability with respect to lesion size, administered dose, and reconstruction algorithm.

Background: SUVmax and SUVpeak are influenced by technical factors as count statistics and reconstruction algorithms.

Objective: To fulfill the aim, we evaluated the SUVs variability with respect to lesion size, administered dose, and reconstruction algorithm (ordered - subset expectation maximization plus point spread function option - OSEM+PSF, regularized Bayesian Penalized Likelihood - BPL) in a 5 - rings BGO PET/CT scanner.

Methods: Discovery IQ scanner (GE Healthcare, Milwaukee, Wisconsin, US) was used for list mode acquisition of 25 FDG patients, 12 injected with 3.7 MBq/kg (Standard Dose protocol - SD) and 13 injected with 1.8 MBq/kg (Low Dose protocol - LD). Each acquisition was reconstructed at different time/FOV with both OSEM+PSF algorithm and BPL using seven different beta factors. SUVs were calculated in 70 lesions and analysed in function of time/FOV and Beta. Image quality was evaluated as a coefficient of variation of the liver (CV - liver).

Results: SUVs were not considerably affected by time/FOV. However, SUVs were influenced by beta: differences were higher in small lesions (37% for SUVmax, 15% for SUVpeak) compared to larger ones (14% and 6%). CV - liver ranged from 6% with Beta-500 (LD and SD) to 13% with Beta- 200 (LD). CV - liver of BPL with Beta-350 (optimized for clinical practice in our institution) in LD was lower than CV - liver of OSEM+PSF in SD.

Conclusion: When a high sensitivity 5 - rings BGO PET/CT scanner is used with the same reconstruction algorithm, quantification by means of SUVmax and SUVpeak is a robust standard compared to the activity and scan duration. However, both SUVs and image quality are influenced by reconstruction algorithms and the related parameters should be considered to obtain the best compromise between detectability, quantification, and noise.

目的:本回顾性研究的目的是研究suv在病变大小、给药剂量和重建算法方面的可变性。背景:SUVmax和SUVpeak受计数统计和重构算法等技术因素的影响。目的:为了实现目的,我们在5环BGO PET/CT扫描仪上评估了SUVs在病变大小、给药剂量和重建算法(有序子集期望最大化+点扩散函数选项- OSEM+PSF,正则化贝叶斯惩罚似似性- BPL)方面的变异性。方法:采用Discovery IQ扫描仪(GE Healthcare, Milwaukee, Wisconsin, US)对25例FDG患者进行清单模式采集,其中12例注射3.7 MBq/kg(标准剂量方案- SD), 13例注射1.8 MBq/kg(低剂量方案- LD)。采用OSEM+PSF算法和BPL方法,利用7种不同的beta因子,在不同的时间/视场对每个采集进行重构。计算70个病变的suv,并分析时间/FOV和Beta的函数。图像质量用肝脏变异系数(CV - liver)来评价。结果:suv受时间/视场的影响不明显。然而,suv受到β的影响:与较大的病变(14%和6%)相比,小病变(SUVmax为37%,SUVpeak为15%)的差异更高。CV -肝脏从β -500 (LD和SD)的6%到β - 200 (LD)的13%不等。BPL + β -350(针对我院临床实践优化)在LD中的CV -肝脏低于SD中OSEM+PSF的CV -肝脏。结论:采用相同重建算法的高灵敏度5环BGO PET/CT扫描仪,相对于活度和扫描时间,SUVmax和SUVpeak是一个可靠的定量标准。然而,suv和图像质量都受到重建算法的影响,需要考虑相关参数,以在可检测性、量化和噪声之间获得最佳折衷。
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引用次数: 1
Critical Review of the Simple Theoretical Models in Dynamic Imaging: Up-Slope Method and Graphical Analysis. 动态成像简单理论模型的评述:上斜率法和图解分析。
IF 2.3 4区 医学 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-01-01 DOI: 10.2174/1874471015666220107101305
Habib E Ashoor

Clinical imaging equipment technological advancements offer insight into the evolution of mathematical techniques used to estimate parameters necessary to characterize the microvasculature and, thus, differentiate normal tissues from abnormal ones. These parameters are blood flow (F), capillary endothelial permeability surface area product (PS), vascular fraction (ve), and extravascular extracellular space size (EES,ve). There are a number of well-established approaches that exist in the literature; however, their analysis is restricted by complexity and is heavily influenced by noise. On the other hand, these characteristics can also be calculated using simpler and straightforward approaches such as Up-Slope Method (USM) and Graphical Analysis (GA). The review looks into the theoretical background and clinical uses of these methodologies, as well as the applicability of these techniques in various sections of the human body.

临床成像设备技术的进步提供了深入了解数学技术的演变,用于估计表征微血管所需的参数,从而区分正常组织和异常组织。这些参数是血流量(F)、毛细血管内皮通透性表面积积(PS)、血管分数(ve)和血管外细胞外空间大小(EES,ve)。在文献中有许多行之有效的方法;然而,它们的分析受到复杂性的限制,并且受到噪声的严重影响。另一方面,这些特征也可以用更简单和直接的方法来计算,如上斜率法(USM)和图形分析(GA)。回顾了这些方法的理论背景和临床应用,以及这些技术在人体各个部分的适用性。
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引用次数: 0
The Radiosensitizing Effect of Olanzapine as an Antipsychotic Medication on Glioblastoma Cell. 奥氮平抗精神病药物对胶质母细胞瘤细胞的放射增敏作用。
IF 2.3 4区 医学 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-01-01 DOI: 10.2174/1874471014666210120100448
Seyedeh Zahra Allahgholipour, Soghra Farzipour, Arash Ghasemi, Hossein Asgarian-Omran, Seyed Jalal Hosseinimehr

Background: Radiotherapy is used as one of the most effective regimens for cancer treatment, while radioresistance is a major drawback in cancer treatment.

Objectives: This study aimed to evaluate the sensitizing effect of olanzapine (OLA) with X-ray on glioblastoma (U-87 MG) cells death.

Methods: The synergistic killing effect of OLA with ionizing radiation (IR) on glioma was evaluated by colony formation assay. The generations of reactive oxygen species (ROS) and protein carbonyl (PC) as oxidized proteins were determined in OLA-treated and irradiated cells.

Results: Results of this study showed that OLA reduced the number of colonies in irradiated glioma cells.OLA elevated ROS and PC levels in irradiated cells. The synergistic killing effect of OLA with IR in U-87 MG cells was observed at concentrations of 1 μM and 20 μM of OLA. The maximum radiosensitizing effect of OLA was observed at a concentration of 20 μM.

Conclusion: The present study demonstrates that OLA has a radiosensitizing effect on cell death induced by IR in glioma cells.

背景:放射治疗是最有效的癌症治疗方案之一,而放射耐药是癌症治疗的主要缺点。目的:本研究旨在评价奥氮平(OLA) x射线对胶质母细胞瘤(u - 87mg)细胞死亡的增敏作用。方法:采用集落形成法评价OLA与电离辐射(IR)对胶质瘤的协同杀伤作用。测定了氧化后活性氧(ROS)和蛋白羰基(PC)的代数。结果:本研究结果表明,OLA减少了辐照胶质瘤细胞的菌落数量。OLA提高了辐照细胞的ROS和PC水平。在OLA浓度为1 μM和20 μM时,观察了OLA与IR对U-87 MG细胞的协同杀伤作用。在浓度为20 μM时,OLA的辐射增敏效果最大。结论:本研究表明,OLA对IR诱导的胶质瘤细胞死亡具有放射增敏作用。
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引用次数: 2
Detailed Chemistry Studies of 225Actinium Labeled Radiopharmaceuticals. 225锕标记放射性药物的详细化学研究。
IF 2.3 4区 医学 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-01-01 DOI: 10.2174/1874471014666210528123936
Kurtulus Eryilmaz, Benan Kilbas

Background: The synthesis of 225Actinium derivatives was afforded by using PSMA- 617, DOTATATE peptides, and EDTMP ligand. Detailed experiments, quality control (QC), and stability studies were also well described. The radiolabelling reactions were performed in mild conditions with desirable radiochemical yields and high radiochemical purities.

Methods: PSMA-617, DOTATATE were radiolabelled with 225Actinium in 0.1 M HCl in the presence of ascorbate buffer solution and passed through the C-18 light cartridge for purification and the product was eluted by ethanol-water solution. EDTMP was also radiolabelled with 225Actinium without using any stabilizer and purification step. All products were well analyzed by R-TLC and R-HPLC. The stability of those compounds was also studied within the validity period of time.

Results: 225Ac-DOTATATE and 225Ac-PSMA-617 were obtained at the same condition. The radiochemical yield of 225Ac-DOTATATE was less than225Ac-PSMA 617. The stability experiments indicating decay daughters of 225Actinium appeared after T0 +1 h due to the recoil effect radiolysis. On the other hand, 225Ac-EDTMP was more stable than DOTA-peptide radiolabelled compounds. 225Ac-EDTMP was produced with more than 95% radiochemical yield and 99% radiochemical purity.

Conclusion: A detailed chemistry study was presented for the synthesis of 225Actinium derivatives in mild conditions with absolute radiochemical purities and high yields. The experimental results showed that 225Ac-EDTMP could be a suitable radiopharmaceutical alternative for bone metastases arising from primer tumors as a cocktail therapy.

背景:采用PSMA- 617、DOTATATE多肽和EDTMP配体合成了225Actinium衍生物。详细的实验,质量控制(QC)和稳定性研究也很好地描述。放射性标记反应在温和的条件下进行,具有理想的放射化学产率和高放射化学纯度。方法:PSMA-617、DOTATATE在抗坏血酸缓冲液存在下,用225Actinium在0.1 M HCl中放射性标记,通过C-18光盒纯化,用乙醇-水溶液洗脱。EDTMP也用225Actinium进行放射性标记,不使用任何稳定剂和纯化步骤。所有产品均经R-TLC和R-HPLC分析。并在有效期内对这些化合物的稳定性进行了研究。结果:在相同条件下获得225Ac-DOTATATE和225Ac-PSMA-617。225Ac-DOTATATE的放射化学产率小于225ac - psma 617。稳定性实验表明,225Actinium在T0 +1 h后由于反冲效应而出现衰变子。另一方面,225Ac-EDTMP比dota肽放射性标记的化合物更稳定。225Ac-EDTMP的放射化学产率大于95%,放射化学纯度大于99%。结论:在温和的条件下合成了具有绝对放射化学纯度和高收率的225Actinium衍生物。实验结果表明,225Ac-EDTMP作为鸡尾酒疗法可作为引物肿瘤骨转移的一种合适的放射性药物替代方案。
{"title":"Detailed Chemistry Studies of <sup>225</sup>Actinium Labeled Radiopharmaceuticals.","authors":"Kurtulus Eryilmaz,&nbsp;Benan Kilbas","doi":"10.2174/1874471014666210528123936","DOIUrl":"https://doi.org/10.2174/1874471014666210528123936","url":null,"abstract":"<p><strong>Background: </strong>The synthesis of <sup>225</sup>Actinium derivatives was afforded by using PSMA- 617, DOTATATE peptides, and EDTMP ligand. Detailed experiments, quality control (QC), and stability studies were also well described. The radiolabelling reactions were performed in mild conditions with desirable radiochemical yields and high radiochemical purities.</p><p><strong>Methods: </strong>PSMA-617, DOTATATE were radiolabelled with <sup>225</sup>Actinium in 0.1 M HCl in the presence of ascorbate buffer solution and passed through the C-18 light cartridge for purification and the product was eluted by ethanol-water solution. EDTMP was also radiolabelled with <sup>225</sup>Actinium without using any stabilizer and purification step. All products were well analyzed by R-TLC and R-HPLC. The stability of those compounds was also studied within the validity period of time.</p><p><strong>Results: </strong><sup>225</sup>Ac-DOTATATE and 225Ac-PSMA-617 were obtained at the same condition. The radiochemical yield of 225Ac-DOTATATE was less than<sup>225</sup>Ac-PSMA 617. The stability experiments indicating decay daughters of <sup>225</sup>Actinium appeared after T0 +1 h due to the recoil effect radiolysis. On the other hand, <sup>225</sup>Ac-EDTMP was more stable than DOTA-peptide radiolabelled compounds. <sup>225</sup>Ac-EDTMP was produced with more than 95% radiochemical yield and 99% radiochemical purity.</p><p><strong>Conclusion: </strong>A detailed chemistry study was presented for the synthesis of <sup>225</sup>Actinium derivatives in mild conditions with absolute radiochemical purities and high yields. The experimental results showed that <sup>225</sup>Ac-EDTMP could be a suitable radiopharmaceutical alternative for bone metastases arising from primer tumors as a cocktail therapy.</p>","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":"15 1","pages":"76-83"},"PeriodicalIF":2.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39031353","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
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Current radiopharmaceuticals
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