scholarly journals Design, synthesis, in vitro and in vivo evaluation of tacrine–cinnamic acid hybrids as multi-target acetyl- and butyrylcholinesterase inhibitors against Alzheimer's disease

RSC Advances ◽  
2017 ◽  
Vol 7 (54) ◽  
pp. 33851-33867 ◽  
Author(s):  
Yao Chen ◽  
Hongzhi Lin ◽  
Jie Zhu ◽  
Kai Gu ◽  
Qi Li ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cinnamic Acid ◽  
Cholinesterase Inhibitors ◽  
In Vivo Evaluation ◽  
Design Synthesis

A series of tacrine–cinnamic acid hybrids are synthesized as multi-target cholinesterase inhibitors against Alzheimer's disease.

In vivo Evaluation and Alzheimer’s Disease Treatment Outcome of siRNA Loaded Dual Targeting Drug Delivery System

2019 ◽  
Vol 20 (1) ◽  
pp. 56-62 ◽  
Author(s):  
Chi Zhang ◽  
Zhichun Gu ◽  
Long Shen ◽  
Xianyan Liu ◽  
Houwen Lin
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Treatment Outcome ◽  
Neuroprotective Effect ◽  
Sirna Delivery ◽  
Repeated Administration ◽  
Spatial Learning And Memory ◽  
In Vivo Evaluation

Background: To deliver drugs to treat Alzheimer’s Disease (AD), nanoparticles should firstly penetrate through blood brain barrier, and then target neurons. Methods: Recently, we developed an Apo A-I and NL4 dual modified nanoparticle (ANNP) to deliver beta-amyloid converting enzyme 1 (BACE1) siRNA. Although promising in vitro results were obtained, the in vivo performance was not clear. Therefore, in this study, we further evaluated the in vivo neuroprotective effect and toxicity of the ANNP/siRNA. The ANNP/siRNA was 80.6 nm with good stability when incubated with serum. In vivo, the treatment with ANNP/siRNA significantly improves the spatial learning and memory of APP/PS1 double transgenic mice, as determined by mean escape latency, times of crossing the platform area during the 60 s swimming and the percentage of the distance in the target quadrant. Results and Conclusion: After the treatment, BACE1 RNA level of ANNP/siRNA group was greatly reduced, which contributed a good AD treatment outcome. Finally, after repeated administration, the ANNP/siRNA did not lead to significant change as observed by HE staining of main organs, suggesting the good biocompatibility of ANNP/siRNA. These results demonstrated that the ANNP was a good candidate for AD targeting siRNA delivery.

Design, synthesis and in vitro testing of 7-methoxytacrine-amantadine analogues: a novel cholinesterase inhibitors for the treatment of Alzheimer’s disease

2015 ◽  
Vol 24 (6) ◽  
pp. 2645-2655 ◽  
Author(s):  
Katarina Spilovska ◽  
Jan Korabecny ◽  
Anna Horova ◽  
Kamil Musilek ◽  
Eugenie Nepovimova ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cholinesterase Inhibitors ◽  
In Vitro Testing ◽  
Design Synthesis

Design, synthesis, in vitro and in vivo evaluation of novel pyrrolizine-based compounds with potential activity as cholinesterase inhibitors and anti-Alzheimer's agents

2019 ◽  
Vol 93 ◽  
pp. 103312 ◽  
Author(s):  
Nehad Abou-Elmagd El-Sayed ◽  
Awatef El-Said Farag ◽  
Manal Abdel Fattah Ezzat ◽  
Hulya Akincioglu ◽  
İlhami Gülçin ◽  
...  
Keyword(s):  
Cholinesterase Inhibitors ◽  
In Vivo Evaluation ◽  
Design Synthesis ◽  
Potential Activity

In vitro and in vivo evaluation of donepezil-sustained release microparticles for the treatment of Alzheimer's disease

Biomaterials ◽  
2007 ◽  
Vol 28 (10) ◽  
pp. 1882-1888 ◽  
Author(s):  
Pengcheng Zhang ◽  
Lingli Chen ◽  
Wangwen Gu ◽  
Zhenghong Xu ◽  
Yu Gao ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Sustained Release ◽  
In Vivo Evaluation

P4-025: A Novel Formulation of Curcumin for Alzheimer's Disease (AD): in VITRO and in VIVO Evaluation

2016 ◽  
Vol 12 ◽  
pp. P1024-P1024 ◽  
Author(s):  
Ankit Parikh ◽  
Zhengnan Shan ◽  
Yunmei May Song ◽  
Krishna Kathwala ◽  
Chun Chuan Tan ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
In Vivo Evaluation
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