Abstract To date, we still lack disease-modifying thera- pies for Alzheimer＇s disease （AD）. Here, we report that long-term administration of benfotiamine improved the cognitive ability of patients with AD. Five pat...Abstract To date, we still lack disease-modifying thera- pies for Alzheimer＇s disease （AD）. Here, we report that long-term administration of benfotiamine improved the cognitive ability of patients with AD. Five patients with mild to moderate AD received oral benfotiamine （300 mg daily） over 18 months. All patients were examined by positron emission tomography with Pittsburgh compound B （PiB-PET） and exhibited positive imaging with β- amyloid deposition, and three received PiB-PET imaging at follow-up. The five patients exhibited cognitive improve- ment as assayed by the Mini-Mental Status Examination （MMSE） with an average increase of 3.2 points at month 18 of benfotiamine administration. The three patients who received follow-up PiB-PET had a 36.7% increase in the average standardized uptake value ratio in the brain com- pared with that in the first scan. Importantly, the MMSE scores of these three had an average increase of 3 points during the same period. Benfotiamine significantly improved the cognitive abilities of mild to moderate AD patients independently of brain amyloid accumulation. Ourstudy provides new insight to the development of disease- modifying therapy.展开更多
目的:通过GE公司合成器Tracerlab FX C合成β淀粉样蛋白(Aβ)的正电子发射断层扫描(PET)显像剂^(11)C-荧光匹兹堡化合物B(^(11)C-PIB),研究其在小鼠体内分布,并探讨其在人体显像中的应用价值。方法:将经过合成器合成的质量控制显像剂注...目的:通过GE公司合成器Tracerlab FX C合成β淀粉样蛋白(Aβ)的正电子发射断层扫描(PET)显像剂^(11)C-荧光匹兹堡化合物B(^(11)C-PIB),研究其在小鼠体内分布,并探讨其在人体显像中的应用价值。方法:将经过合成器合成的质量控制显像剂注射于12周龄正常小鼠,测出各个时间点的放射性摄取分布。同时将此显像剂分别用于阿尔茨海默病(AD)患者与健康志愿者的检查,对比PET-CT图像特点。结果:产品放射性化学产出率为13.5%(校正后),其纯度>98%。小鼠注射显像剂5 min后放射性摄取分布达到最大,10~15 min后小鼠体内药物分布已经趋近平衡。^(11)C-PIB在人体内图像分布特点是,额前叶(包括眶回)、内侧顶叶(特别在楔前叶)、外侧顶叶、部分外侧颞叶皮层以及纹状体呈高分布区域;岛叶、丘脑及枕叶相关皮层相对低摄取;初级视觉皮层及周围区域、内侧颞叶、初级感觉和(或)运动区域呈更低的区域分布;小脑基本无^(11)C-PIB分布。结论:^(11)C-PIB是较理想的Aβ斑块显像剂,合成快速方便,适于AD患者的诊断与疗效评价。展开更多
基金supported by the Key Fund for Developing New Drugs from the Ministry of Science and Technology of China(2014ZX09101005-005)the National Natural Science Foundation of China(81071019)+2 种基金the National Key Basic Research Program of China(2011CBA00400)the Natural Science Foundation of Shanghai Municipality,China(13JC1401500)the Fund for Medical Emerging Cutting-Edge Technology in Shanghai of China (SHDC12012114)
文摘Abstract To date, we still lack disease-modifying thera- pies for Alzheimer＇s disease （AD）. Here, we report that long-term administration of benfotiamine improved the cognitive ability of patients with AD. Five patients with mild to moderate AD received oral benfotiamine （300 mg daily） over 18 months. All patients were examined by positron emission tomography with Pittsburgh compound B （PiB-PET） and exhibited positive imaging with β- amyloid deposition, and three received PiB-PET imaging at follow-up. The five patients exhibited cognitive improve- ment as assayed by the Mini-Mental Status Examination （MMSE） with an average increase of 3.2 points at month 18 of benfotiamine administration. The three patients who received follow-up PiB-PET had a 36.7% increase in the average standardized uptake value ratio in the brain com- pared with that in the first scan. Importantly, the MMSE scores of these three had an average increase of 3 points during the same period. Benfotiamine significantly improved the cognitive abilities of mild to moderate AD patients independently of brain amyloid accumulation. Ourstudy provides new insight to the development of disease- modifying therapy.
文摘目的:通过GE公司合成器Tracerlab FX C合成β淀粉样蛋白(Aβ)的正电子发射断层扫描(PET)显像剂^(11)C-荧光匹兹堡化合物B(^(11)C-PIB),研究其在小鼠体内分布,并探讨其在人体显像中的应用价值。方法:将经过合成器合成的质量控制显像剂注射于12周龄正常小鼠,测出各个时间点的放射性摄取分布。同时将此显像剂分别用于阿尔茨海默病(AD)患者与健康志愿者的检查,对比PET-CT图像特点。结果:产品放射性化学产出率为13.5%(校正后),其纯度>98%。小鼠注射显像剂5 min后放射性摄取分布达到最大,10~15 min后小鼠体内药物分布已经趋近平衡。^(11)C-PIB在人体内图像分布特点是,额前叶(包括眶回)、内侧顶叶(特别在楔前叶)、外侧顶叶、部分外侧颞叶皮层以及纹状体呈高分布区域;岛叶、丘脑及枕叶相关皮层相对低摄取;初级视觉皮层及周围区域、内侧颞叶、初级感觉和(或)运动区域呈更低的区域分布;小脑基本无^(11)C-PIB分布。结论:^(11)C-PIB是较理想的Aβ斑块显像剂,合成快速方便,适于AD患者的诊断与疗效评价。
