title: Effects of Glycosylation on Biodistribution and Imaging Quality of Necrotic Myocardium of Iodine-131-Labeled Sennidins.
abstract: Sennidins are necrosis-avid agents for noninvasive assessment of myocardial viability which is important for patients with myocardial infarction (MI). However, high accumulation of radioactivity in the liver interferes with the assessment of myocardial viability. In this study, we compared sennidins with sennosides to investigate the effects of glycosylation on biodistribution and imaging quality of sennidins.
  
  
  
  Sennidin A (SA), sennidin B (SB), sennoside A (SSA), and sennoside B (SSB) were labeled with I-131. In vitro binding to necrotic cells and hepatic cells and in vivo biodistribution in rats with muscular necrosis were evaluated by gamma counting, autoradiography, and histopathology. Single photon emission computed tomography/computed tomography (SPECT/CT) images were acquired in rats with acute MI.
  
  
  
  The uptake of [131I]SA, [131I]SSA, [131I]SB, and [131I]SSB in necrotic cells was significantly higher than that in viable cells (p < 0.05). Hepatic cells uptake of [131I]SSA and [131I]SSB were 7-fold and 10-fold lower than that of corresponding [131I]SA and [131I]SB, respectively. The biodistribution data showed that the radioactivities in the liver and feces were significantly lower with [131I]sennosides than those with [131I]sennidins (p < 0.01). Autoradiography showed preferential accumulation of these four radiotracers in necrotic areas of muscle, confirmed by histopathology. SPECT/CT imaging studies showed better image quality with [131I]SSB than with [131I]SB due to less liver interference.
  
  
  
  Glycosylation significantly decreased the liver uptake and improved the quality of cardiac imaging. [131I]SSB may serve as a promising necrosis-avid agent for noninvasive assessment of myocardial viability.
authors.affiliation: Department of Natural Medicinal Chemistry & Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, No.24, Tongjiaxiang, Gulou District, Nanjing, 210009, Jiangsu Province, People's Republic of China.|Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, 210028, Jiangsu Province, People's Republic of China.|Laboratories of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, No.100, Shizi Street, Hongshan Road, Nanjing, 210028, Jiangsu Province, People's Republic of China.
authors.forename: Ling
authors.initials: L
authors.lastname: Li
authors.affiliation: Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, 210028, Jiangsu Province, People's Republic of China.|Laboratories of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, No.100, Shizi Street, Hongshan Road, Nanjing, 210028, Jiangsu Province, People's Republic of China.
authors.forename: Dongjian
authors.initials: D
authors.lastname: Zhang
authors.affiliation: Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, 210028, Jiangsu Province, People's Republic of China.|Laboratories of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, No.100, Shizi Street, Hongshan Road, Nanjing, 210028, Jiangsu Province, People's Republic of China.
authors.forename: Shengwei
authors.initials: S
authors.lastname: Yang
authors.affiliation: Department of Nuclear Medicine, Renji Hospital, Shanghai Jiaotong University, School of Medicine, Shanghai, 200127, People's Republic of China.
authors.forename: Shaoli
authors.initials: S
authors.lastname: Song
authors.affiliation: Department of Natural Medicinal Chemistry & Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, No.24, Tongjiaxiang, Gulou District, Nanjing, 210009, Jiangsu Province, People's Republic of China.|Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, 210028, Jiangsu Province, People's Republic of China.|Laboratories of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, No.100, Shizi Street, Hongshan Road, Nanjing, 210028, Jiangsu Province, People's Republic of China.
authors.forename: Jindian
authors.initials: J
authors.lastname: Li
authors.affiliation: Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, 210028, Jiangsu Province, People's Republic of China.|Laboratories of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, No.100, Shizi Street, Hongshan Road, Nanjing, 210028, Jiangsu Province, People's Republic of China.
authors.forename: Qin
authors.initials: Q
authors.lastname: Wang
authors.affiliation: Department of Natural Medicinal Chemistry & Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, No.24, Tongjiaxiang, Gulou District, Nanjing, 210009, Jiangsu Province, People's Republic of China.|Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, 210028, Jiangsu Province, People's Republic of China.|Laboratories of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, No.100, Shizi Street, Hongshan Road, Nanjing, 210028, Jiangsu Province, People's Republic of China.
authors.forename: Cong
authors.initials: C
authors.lastname: Wang
authors.affiliation: Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, 210028, Jiangsu Province, People's Republic of China.|Laboratories of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, No.100, Shizi Street, Hongshan Road, Nanjing, 210028, Jiangsu Province, People's Republic of China.|Theragnostic Laboratory, Campus Gasthuisberg, KU Leuven, 3000, Leuven, Belgium.
authors.forename: Yuanbo
authors.initials: Y
authors.lastname: Feng
authors.affiliation: Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, 210028, Jiangsu Province, People's Republic of China.|Laboratories of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, No.100, Shizi Street, Hongshan Road, Nanjing, 210028, Jiangsu Province, People's Republic of China.|Theragnostic Laboratory, Campus Gasthuisberg, KU Leuven, 3000, Leuven, Belgium.
authors.forename: Yicheng
authors.initials: Y
authors.lastname: Ni
authors.affiliation: Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, 210028, Jiangsu Province, People's Republic of China. zhangjian@jsatcm.com.|Laboratories of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, No.100, Shizi Street, Hongshan Road, Nanjing, 210028, Jiangsu Province, People's Republic of China. zhangjian@jsatcm.com.
authors.forename: Jian
authors.initials: J
authors.lastname: Zhang
authors.affiliation: Department of Nuclear Medicine, The First Affiliated Hospital of Nanjing Medical University, No.300, Guangzhou Road, Nanjing, 210029, Jiangsu Province, People's Republic of China. nuclearmedicine@163.com.
authors.forename: Wei
authors.initials: W
authors.lastname: Liu
authors.affiliation: Department of Natural Medicinal Chemistry & Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, No.24, Tongjiaxiang, Gulou District, Nanjing, 210009, Jiangsu Province, People's Republic of China. cpu-yzq@cpu.edu.cn.
authors.forename: Zhiqi
authors.initials: Z
authors.lastname: Yin
mesh_terms: D000818:Animals; D000873:Anthracenes / Q000737:chemistry* / Q000493:pharmacokinetics; D001345:Autoradiography; D002470:Cell Survival; D006031:Glycosylation; D006801:Humans; D007457:Iodine Radioisotopes / Q000737:chemistry*; D008297:Male; D009206:Myocardium / Q000473:pathology*; D009336:Necrosis; D000442:Octanols / Q000737:chemistry; D017207:Rats, Sprague-Dawley; D012676:Senna Extract / Q000737:chemistry* / Q000493:pharmacokinetics; D013194:Staining and Labeling; D013997:Time Factors; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon; D014057:Tomography, X-Ray Computed; D014867:Water / Q000737:chemistry
chemical_list: D000873:Anthracenes; D007457:Iodine Radioisotopes; D000442:Octanols; D014867:Water; D012676:Senna Extract
keywords: Glycosylation; Lipophilicity; Liver uptake; Myocardial viability; Necrosis targetability