硒对氟致雄性大鼠生殖损害的拮抗作用

目的 :探讨硒对高氟所致雄性大鼠生殖损害的拮抗作用。方法 :1 0 0只雄性Wistar大鼠随机分成对照组、氟 (NaF 1 5 0mg/L)组、氟加低硒 (0 .5mg/L亚硒酸钠 )组、氟 (NaF 1 5 0mg/L)加中硒 (2 .0mg/L亚硒酸钠 )组、氟(NaF 1 5 0mg/L)加高硒 (4 .0mg/L亚硒酸钠 )组 5组 ,通过饮水加氟、加硒的方法染毒 1 0周。观察氟、硒对大鼠体重、睾丸和附睾质量及其脏器系数 ,精子计数、活动率及畸形率 ,睾丸、附睾生化标志酶 ,血清性激素 ,睾丸组织病理切片以及初级精母细胞染色体畸形率的影响。结果 :①右侧睾丸质量对照组为 (1 .80± 0 .2 2 )g ,氟加高硒组为 (1 .6 1±0 .1 1 )g ,2者相比差异有统计学意义 (P <0 .0 5 )。②精子计数 :氟组 (9.2 3× 1 0 7ml-1 )、氟加中硒组 (37.6 7× 1 0 7ml-1 )与对照组 (2 8.6 0× 1 0 7ml-1 )比较 ,差异有统计学意义 (P <0 .0 0 1 ) ;精子畸形率 :氟组 (36 .33% )氟加中硒组 (1 2 .70 % )与对照组 (1 4 .83% )比较 ,差异有统计学意义 (P <0 .0 0 1 ) ;精子活动率 :氟组 (6 2 .0 7%± 6 .5 0 % )氟加中硒组 (6 8.2 1 %± 4 .99% )与对照组 (73.6 7%± 6 .5 1 % )比较 ,差异有统计学意义 (P <0 .0 0 1 )。③LDH :氟组 ((5 79.4 7± 97.1 6 )u/g)、氟加中硒组 ((72 6 .1 3± 1 1     

缺碘和氟中毒对大鼠甲状腺的协同作用

实验用Wistar大鼠212只,按饮食中碘和氟含量不同随机分为五组,实验期为7个月。结果显示:摄碘正常的大鼠长期饮用30ppm氟水后引起甲状腺功能和形态的严重损害,而饮用10ppm氟水的大鼠仅见甲状腺滤泡上皮超微结构的轻度异常变化;单纯性缺碘大鼠甲状腺肿大并伴有代偿性功能变化,缺碘并饮用10ppm氟水的大鼠在其甲状腺肿大的同时伴有明显的形态结构损伤及甲状腺代偿功能抑制,甚至功能低下。     

A report of the automated radiosynthesis of the tau positron emission tomography radiopharmaceutical, [18F]‐THK‐5351

The radiotracer, [¹⁸F]‐THK‐5351, is a highly selective and high‐binding affinity PET imaging agent for aggregates of hyper‐phosphorylated tau protein. Our report is a simplified 1‐pot, 2‐step radiosynthesis of [¹⁸F]‐THK‐5351. This report is broadly applicable for routine clinical production and multi‐center trials on account of favorable half‐life of flourine‐18 and the use of a commercially available radiosynthesis module, the GE TRACERlab™ FX_FN. First, the O‐THP protected tosyl precursor underwent nucleophilic fluorinating reaction with potassium cryptand fluoride ([¹⁸F] fluoride (K[¹⁸F]/K₂₂₂)) in Dimethyl sulfoxide at 110°C for 10 minutes followed by O‐THP removal by using diluted hydrochloric acid (HCl) at same temperature. [¹⁸F]‐THK‐5351 was purified via semi‐preparative high‐performance liquid chromatography and formulated by using 10% EtOH, United States Pharmacopeia (USP) in 0.9% sodium chloride for injection, USP and an uncorrected radiochemical yield of 21 ± 3.5%, with a specific activity of 153.11 ± 25.9 GBq/μmol (4138 ± 700 mCi/μmol) at the end of synthesis (63 minutes; n  = 3).     

An improved radiosynthesis of O‐(2‐[18F]fluoroethyl)‐O‐(p‐nitrophenyl)methylphosphonate: A first‐in‐class cholinesterase PET tracer

O‐(2‐Fluoroethyl)‐O‐(p‐nitrophenyl) methylphosphonate 1 is an organophosphate cholinesterase inhibitor that creates a phosphonyl‐serine covalent adduct at the enzyme active site blocking cholinesterase activity in vivo . The corresponding radiolabeled O‐(2‐[¹⁸F]fluoroethyl)‐O‐(p‐nitrophenyl) methylphosphonate, [ ¹⁸ F]1 , has been previously prepared and found to be an excellent positron emission tomography imaging tracer for assessment of cholinesterases in live brain, peripheral tissues, and blood. However, the previously reported [ ¹⁸ F]1 tracer synthesis was slow even with microwave acceleration, required high‐performance liquid chromatography separation of the tracer from impurities, and gave less optimal radiochemical yields. In this paper, we report a new synthetic approach to circumvent these shortcomings that is reliant on the facile reactivity of bis‐(O,O‐p‐nitrophenyl) methylphosphonate, 2 , with 2‐fluoroethanol in the presence of DBU. The cold synthesis was successfully translated to provide a more robust radiosynthesis. Using this new strategy, the desired tracer, [ ¹⁸ F]1 , was obtained in a non‐decay–corrected radiochemical yield of 8 ± 2% (n = 7) in >99% radiochemical and >95% chemical purity with a specific activity of 3174 ± 345 Ci/mmol (EOS). This new facile radiosynthesis routinely affords highly pure quantities of [ ¹⁸ F]1 , which will further enable tracer development of OP cholinesterase inhibitors and their evaluation in vivo .     

18氟-脱氧葡萄糖PET显像对鼻咽癌放射治疗后咽旁间隙复发的诊断价值

目的探讨18氟-脱氧葡萄糖正电子发射断层扫描仪(18FDG-PET)对鼻咽癌放射治疗后咽旁间隙复发或纤维化的临床诊断价值。方法32例行CT、MRI检查后不能确定鼻咽癌放射治疗后咽旁间隙是否复发或纤维化的患者,采用18FDG-PET显像,同时行CT、MRI检查。所有患者于CT、MRI及18FDG-PET检查后,在CT引导下穿刺活检,观察不同检查方法的灵敏度、特异度和诊断符合率。结果CT检查的灵敏度79.16%、特异度75.00%、诊断符合率78.13%;MRI检查的灵敏度83.33%、特异度87.50%、诊断符合率84.38%;18FDG-PET检查的灵敏度95.83%、特异度87.50%、诊断符合率93.75%。结论怀疑鼻咽癌放射治疗后咽旁间隙复发的患者可以考虑行18FDG PET检查,免除病理穿刺活检的风险;也可通过CT和/或MRI检查,采取CT引导下咽旁间隙穿刺活检达到确诊的目的。     

离体培养条件下氟与硒对毛囊影响的初步研究

目的:观察氟与硒对离体培养条件下的人头皮毛囊生长的影响。方法:在离体人头皮毛囊培养模型中,加入不同浓度的氟化钠和亚硒酸钠,目镜测微器测量毛囊长度的变化;连续观察毛囊形态学改变并做电镜切片检查。结果:1mmol/L和10mmol/L的氟化钠能不同程度的抑制离体毛囊的生长(P<0.05)。0.01mmol/L的亚硒酸钠对1mmol/L氟化钠毒性有拮抗作用(P<0.05)。0.1mmol/L氟化钠单独作用对毛囊生长无影响(P>0.05),0.1mmol/L氟化钠及0.01mmol/L亚硒酸钠共同作用对毛囊生长无影响(P>0.05)。电镜观察发现10mmol/L氟化钠作用的毛囊在培养5天时即可见较为严重的凋亡前改变及凋亡现象,10mmol/L氟化钠加0.01mmol/L亚硒酸钠组毛囊也可见到类似的改变,培养9天时还可见到细胞内有空泡,连接紊乱,桥粒连接破坏等现象。结论:不同浓度的氟化钠对游离的人头皮毛囊的生长有不同作用,一定浓度的亚硒酸钠能拮抗氟化钠对毛囊的毒性作用。     

氟对干热地区居民血清Fe、Zn、Ca和Mg含量的影响

本文对吐鲁大地区２个水氟含量不同〔其含量分别为０．９１ｍｇ／Ｌ（Ａ村）和０．５８ｍｇ／Ｌ（Ｂ村）〕的居民村维吾尔族居民饮水量、摄氟量、尿氟和血清Ｆｅ、ｚｎ、Ｃａ和Ｍｇ含量以及氟斑牙患病率进行了分析。结果显示，居民夏季饮水量明显升高（５～８Ｌ／ｄ），饮水摄氟量增多。尿氟含量增加，并出现氟中毒患者。氟斑牙患病率Ａ村为６５．５７％；Ｂ村为４８．９３％。通过对两村居民血清Ｆｅ、Ｚｎ、Ｃａ和Ｍｇ含量分析，发现血清Ｚｎ和Ｍｇ含量，两村居民无明显差异（Ｐ＞０．０５），说明短期（夏季）过量摄氟对Ｚｎ和Ｍｇ代谢的影响不大，但血清Ｆｅ和Ｃａ差别显著，Ａ村居民血清Ｆｅ含量明显升高，血清Ｃａ含量明显降低。表明氟对血清Ｆｅ和Ｃａ的代谢有明显影响。由此可见，氟对机体的损伤不仅表现为直接损伤，还可通过影响体内无机元素的代谢造成损伤。     

氟对小鼠子代生长发育的影响

观察结果显示，染氟各组仔鼠机体组织氟含量增高，大脑皮质神经细胞超微结构异常。０．４５ｍｇ／ｋｇ剂量组仔鼠已表现为体格和早期神经行为发育迟缓；而０．４５ｍｇ／ｋｇ剂量组３０日龄仔鼠血清溶血素水平显著增高。表明氟可经母体对仔鼠各系统的发育产生不同影响。