- Scutellarein derivative as well as preparation method and application of scutellarein derivative
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The invention belongs to the field of drug synthesis and particularly relates to a scutellarein derivative as well as a preparation method and application of the scutellarein derivative. The scutellarein derivative has a structure shown as the formula 1,
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- 99mTc/Re complexes based on flavone and aurone as SPECT probes for imaging cerebral β-amyloid plaques
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Two 99mTc/Re complexes based on flavone and aurone were tested as potential probes for imaging β-amyloid plaques using single photon emission computed tomography. Both 99mTc-labeled derivatives showed higher affinity for Aβ(1-42) aggregates than did 99mTc-BAT. In sections of brain tissue from an animal model of AD, the Re-flavone derivative 9 and Re-aurone derivative 19 intensely stained β-amyloid plaques. In biodistribution experiments using normal mice, 99mTc-labeled flavone and aurone displayed similar radioactivity pharmacokinetics. With additional modifications to improve their brain uptake, 99mTc complexes based on the flavone or aurone scaffold may serve as probes for imaging cerebral β-amyloid plaques.
- Ono, Masahiro,Ikeoka, Ryoichi,Watanabe, Hiroyuki,Kimura, Hiroyuki,Fuchigami, Takeshi,Haratake, Mamoru,Saji, Hideo,Nakayama, Morio
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supporting information; experimental part
p. 5743 - 5748
(2010/11/18)
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- 18F-labeled flavones for in vivo imaging of β-amyloid plaques in Alzheimer's brains
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In vivo imaging of β-amyloid (Aβ) aggregates in the brain may lead to early detection of Alzheimer's disease (AD) and monitoring of the progression and effectiveness of treatment. The purpose of this study was to develop novel 18F-labeled amyloid-imaging probes based on flavones as a core structure. Fluoropegylated (FPEG) flavone derivatives were designed and synthesized. The affinity of the derivatives for Aβ aggregates varied from 5 to 321 nM. In brain sections of AD model mice, FPEG flavones with the dimethylamino group intensely stained β-amyloid plaques. In biodistrubution experiments using normal mice, they displayed high uptake in the brain ranging from 2.9 to 4.2%ID/g at 2 min postinjection. The radioactivity washed out from the brain rapidly (1.3-2.0%ID/g at 30 min), which is highly desirable for β-amyloid imaging agents. FPEG flavones may be potential PET imaging agents for β-amyloid plaques in Alzheimer's brains.
- Ono, Masahiro,Watanabe, Rumi,Kawashima, Hidekazu,Kawai, Tomoki,Watanabe, Hiroyuki,Haratake, Mamoru,Saji, Hideo,Nakayama, Morio
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experimental part
p. 2069 - 2076
(2009/06/06)
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- COMPOSITION FOR AMYLOID-ASSOCIATED DISEASE DIAGNOSIS
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A composition for diagnosing amyloid-related diseases, which comprises a flavone derivative, a chalcone derivative, a styrylchromone derivative, or a coumarin derivative, is provided. These compounds have high binding specificity to an amyloid β protein,
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Page/Page column 5; 36; 44; 53
(2010/11/28)
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