The Experts below are selected from a list of 20364 Experts worldwide ranked by ideXlab platform
Wen Luo - One of the best experts on this subject based on the ideXlab platform.
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Synthesis, in vitro and in vivo biological evaluation of novel graveolinine derivatives as potential Anti-Alzheimer agents.
Bioorganic & medicinal chemistry, 2019Co-Authors: Wen Luo, Chao-jie Wang, Ting Wang, Hui-yan Guo, Zhi-yang Zhang, Zhi-yi Song, Yi-ping ChenAbstract:Abstract A novel series of graveolinine derivatives were synthesized and evaluated as potential Anti-Alzheimer agents. Compound 5f exhibited the best inhibitory activity for acetylcholinesterase (AChE) and had surprisingly potent inhibitory activity for butyrylcholinesterase (BuChE), with IC50 values of 0.72 μM and 0.16 μM, respectively. The results from Lineweaver–Burk plot and molecular modeling study indicated non-competitive inhibition of AChE by compound 5f. In addition, these derivatives showed potent self-induced β-amyloid (Aβ) aggregation inhibition. Moreover, 5f didn’t show obvious toxicity against PC12 and HepG2 cells at 50 μM. Finally, in vivo studies confirmed that 5f significantly ameliorates the cognitive performances of scopolamine-treated ICR mice. Therefore, these graveolinine derivatives should be thoroughly and systematically studied for the treatment of Alzheimer’s disease.
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Synthesis and biological evaluation of genistein-O-alkylamine derivatives as potential multifunctional Anti-Alzheimer agents.
Chemical biology & drug design, 2018Co-Authors: Chen Hong, Xin Zhang, Hui-yan Guo, Shuai Chen, Ya-cheng Yang, Kang Huang, Yi-juan Zhang, Zhiyong Tian, Wen LuoAbstract:A series of genistein derivatives were synthesized and evaluated as multifunctional Anti-Alzheimer agents. The results showed that these derivatives had significant acetylcholinesterase (AChE) inhibitory activity; compound 5a exhibited the strongest inhibition to AChE with an IC50 value (0.034 μM) much lower than that of rivastigmine (6.53 μM). A Lineweaver-Burk plot and molecular modeling study showed that compound 5a targeted both the catalytic active site and the peripheral anionic site of AChE. These compounds also showed potent peroxy scavenging activity and metal-chelating ability. The compounds did not show obvious effect on HepG2 and PC12 cell viability at the concentration of 100 μM. Therefore, these genistein derivatives can be utilized as multifunctional agents for the treatment of AD.
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Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional Anti-Alzheimer agents
European Journal of Medicinal Chemistry, 2016Co-Authors: Wen Luo, Ya Chen Yang, Juan Cen, Song Qiang Xie, Chen Hong, Ting Wang, Ying Chen, Chao-jie WangAbstract:A new series of 4-dimethylamine flavonoid derivatives were designed and synthesized as potential multifunctional Anti-Alzheimer agents. The inhibition of cholinesterase activity, self-induced β-amyloid (Aβ) aggregation, and Antioxidant activity by these derivatives was investigated. Most of the compounds exhibited potent acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity. A Lineweaver-Burk plot and molecular modeling study showed that these compounds targeted both the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE. The derivatives showed potent self-induced Aβ aggregation inhibition and peroxyl radical absorbance activity. Moreover, compound 6d significantly protected PC12 neurons against H2O2-induced cell death at low concentrations. Thus, these compounds could become multifunctional agents for further development for the treatment of AD.
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Design, synthesis and evaluation of genistein-polyamine conjugates as multi-functional Anti-Alzheimer agents
Acta Pharmaceutica Sinica B, 2015Co-Authors: Xin Zhang, Jiang Wang, Wen Luo, Chen Hong, Chao-jie WangAbstract:A series of genistein-polyamine conjugates (4a-4h) were designed, synthesized and evaluated as multi-functional Anti-Alzheimer agents. The results showed that these compounds had significant cholinesterases (ChEs) inhibitory activity. Compound 4b exhibited the strongest inhibition to acetylcholinesterase (AChE) with an IC50value of 2.75μmol/L, which was better than that of rivastigmine (5.60μmol/L). Lineweaver-Burk plot and molecular modeling study showed that compound 4b targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, compound 4b showed potent metal-chelating ability. In addition, it was found that 4a-4h did not affect HepG-2 cell viability at the concentration of 10μmol/L.
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design synthesis and evaluation of novel 4 dimethylamine flavonoid derivatives as potential multi functional Anti Alzheimer agents
Bioorganic & Medicinal Chemistry, 2013Co-Authors: Wen Luo, Chen Hong, Runguo Tian, Yueqiao Wang, Junjie Yue, Chao-jie WangAbstract:A series of 4-dimethylamine flavonoid derivatives 5a-5r were designed, synthesized and evaluated as potential multi-functional Anti-Alzheimer agents. The results showed that most of the synthesized compounds exhibited high acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity at the micromolar range (IC50, 1.83-33.20 μM for AChE and 0.82-11.45 μM for BChE). A Lineweaver-Burk plot indicated a mixed-type inhibition for compound 5j with AChE, and molecular modeling study showed that 5j targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, the derivatives showed potent self-induced Aβ aggregation inhibitory activity at 20 μM with percentage from 25% to 48%. In addition, some compounds (5j-5q) showed potent oxygen radical absorbance capacity (ORAC) ranging from 1.5- to 2.6-fold of the Trolox value. These compounds should be further investigated as multi-potent agents for the treatment of Alzheimer's disease.
Chao-jie Wang - One of the best experts on this subject based on the ideXlab platform.
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Synthesis, in vitro and in vivo biological evaluation of novel graveolinine derivatives as potential Anti-Alzheimer agents.
Bioorganic & medicinal chemistry, 2019Co-Authors: Wen Luo, Chao-jie Wang, Ting Wang, Hui-yan Guo, Zhi-yang Zhang, Zhi-yi Song, Yi-ping ChenAbstract:Abstract A novel series of graveolinine derivatives were synthesized and evaluated as potential Anti-Alzheimer agents. Compound 5f exhibited the best inhibitory activity for acetylcholinesterase (AChE) and had surprisingly potent inhibitory activity for butyrylcholinesterase (BuChE), with IC50 values of 0.72 μM and 0.16 μM, respectively. The results from Lineweaver–Burk plot and molecular modeling study indicated non-competitive inhibition of AChE by compound 5f. In addition, these derivatives showed potent self-induced β-amyloid (Aβ) aggregation inhibition. Moreover, 5f didn’t show obvious toxicity against PC12 and HepG2 cells at 50 μM. Finally, in vivo studies confirmed that 5f significantly ameliorates the cognitive performances of scopolamine-treated ICR mice. Therefore, these graveolinine derivatives should be thoroughly and systematically studied for the treatment of Alzheimer’s disease.
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Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional Anti-Alzheimer agents
European Journal of Medicinal Chemistry, 2016Co-Authors: Wen Luo, Ya Chen Yang, Juan Cen, Song Qiang Xie, Chen Hong, Ting Wang, Ying Chen, Chao-jie WangAbstract:A new series of 4-dimethylamine flavonoid derivatives were designed and synthesized as potential multifunctional Anti-Alzheimer agents. The inhibition of cholinesterase activity, self-induced β-amyloid (Aβ) aggregation, and Antioxidant activity by these derivatives was investigated. Most of the compounds exhibited potent acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity. A Lineweaver-Burk plot and molecular modeling study showed that these compounds targeted both the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE. The derivatives showed potent self-induced Aβ aggregation inhibition and peroxyl radical absorbance activity. Moreover, compound 6d significantly protected PC12 neurons against H2O2-induced cell death at low concentrations. Thus, these compounds could become multifunctional agents for further development for the treatment of AD.
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Design, synthesis and evaluation of genistein-polyamine conjugates as multi-functional Anti-Alzheimer agents
Acta Pharmaceutica Sinica B, 2015Co-Authors: Xin Zhang, Jiang Wang, Wen Luo, Chen Hong, Chao-jie WangAbstract:A series of genistein-polyamine conjugates (4a-4h) were designed, synthesized and evaluated as multi-functional Anti-Alzheimer agents. The results showed that these compounds had significant cholinesterases (ChEs) inhibitory activity. Compound 4b exhibited the strongest inhibition to acetylcholinesterase (AChE) with an IC50value of 2.75μmol/L, which was better than that of rivastigmine (5.60μmol/L). Lineweaver-Burk plot and molecular modeling study showed that compound 4b targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, compound 4b showed potent metal-chelating ability. In addition, it was found that 4a-4h did not affect HepG-2 cell viability at the concentration of 10μmol/L.
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design synthesis and evaluation of novel 4 dimethylamine flavonoid derivatives as potential multi functional Anti Alzheimer agents
Bioorganic & Medicinal Chemistry, 2013Co-Authors: Wen Luo, Chen Hong, Runguo Tian, Yueqiao Wang, Junjie Yue, Chao-jie WangAbstract:A series of 4-dimethylamine flavonoid derivatives 5a-5r were designed, synthesized and evaluated as potential multi-functional Anti-Alzheimer agents. The results showed that most of the synthesized compounds exhibited high acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity at the micromolar range (IC50, 1.83-33.20 μM for AChE and 0.82-11.45 μM for BChE). A Lineweaver-Burk plot indicated a mixed-type inhibition for compound 5j with AChE, and molecular modeling study showed that 5j targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, the derivatives showed potent self-induced Aβ aggregation inhibitory activity at 20 μM with percentage from 25% to 48%. In addition, some compounds (5j-5q) showed potent oxygen radical absorbance capacity (ORAC) ranging from 1.5- to 2.6-fold of the Trolox value. These compounds should be further investigated as multi-potent agents for the treatment of Alzheimer's disease.
Davide Franceschini - One of the best experts on this subject based on the ideXlab platform.
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Promising in Vitro Anti-Alzheimer Properties for a Ruthenium(III) Complex.
ACS Medicinal Chemistry Letters, 2013Co-Authors: Luigi Messori, Michela Camarri, Teresa Ferraro, Chiara Gabbiani, Davide FranceschiniAbstract:Metal complexes represent today an attractive class of experimental Anti-Alzheimer agents with the potential of blocking β-amyloid 1–42 aggregation and scavenging its toxicity. Three representative ruthenium(III) complexes, namely NAMI A, KP1019, and PMRU20, were specifically evaluated to this end in an established in vitro model of AD relying on primary cortical neurons. Notably, PMRU20 turned out to be highly effective in protecting cortical neurons against Aβ 1–42 toxicity, while the other tested ruthenium compounds were poorly active or even inactive; we also found that PMRU20 is virtually devoid of any significant toxicity in vitro at the applied concentrations. Interestingly, PMRU20 was neuroprotective even against the toxicity induced by Aβ 25–35. The direct reaction of PMRU20 with Aβ 1–42 was explored through ESI MS analysis and some adduct formation evidenced. In addition, thioflavin T assays revealed that PMRU20 greatly reduces Aβ 1–42 aggregation. The implications of these findings are discusse...
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Promising in Vitro Anti-Alzheimer Properties for a Ruthenium(III) Complex.
ACS medicinal chemistry letters, 2013Co-Authors: Luigi Messori, Michela Camarri, Teresa Ferraro, Chiara Gabbiani, Davide FranceschiniAbstract:Metal complexes represent today an attractive class of experimental Anti-Alzheimer agents with the potential of blocking β-amyloid 1–42 aggregation and scavenging its toxicity. Three representative...
Chen Hong - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and biological evaluation of genistein-O-alkylamine derivatives as potential multifunctional Anti-Alzheimer agents.
Chemical biology & drug design, 2018Co-Authors: Chen Hong, Xin Zhang, Hui-yan Guo, Shuai Chen, Ya-cheng Yang, Kang Huang, Yi-juan Zhang, Zhiyong Tian, Wen LuoAbstract:A series of genistein derivatives were synthesized and evaluated as multifunctional Anti-Alzheimer agents. The results showed that these derivatives had significant acetylcholinesterase (AChE) inhibitory activity; compound 5a exhibited the strongest inhibition to AChE with an IC50 value (0.034 μM) much lower than that of rivastigmine (6.53 μM). A Lineweaver-Burk plot and molecular modeling study showed that compound 5a targeted both the catalytic active site and the peripheral anionic site of AChE. These compounds also showed potent peroxy scavenging activity and metal-chelating ability. The compounds did not show obvious effect on HepG2 and PC12 cell viability at the concentration of 100 μM. Therefore, these genistein derivatives can be utilized as multifunctional agents for the treatment of AD.
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Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional Anti-Alzheimer agents
European Journal of Medicinal Chemistry, 2016Co-Authors: Wen Luo, Ya Chen Yang, Juan Cen, Song Qiang Xie, Chen Hong, Ting Wang, Ying Chen, Chao-jie WangAbstract:A new series of 4-dimethylamine flavonoid derivatives were designed and synthesized as potential multifunctional Anti-Alzheimer agents. The inhibition of cholinesterase activity, self-induced β-amyloid (Aβ) aggregation, and Antioxidant activity by these derivatives was investigated. Most of the compounds exhibited potent acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity. A Lineweaver-Burk plot and molecular modeling study showed that these compounds targeted both the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE. The derivatives showed potent self-induced Aβ aggregation inhibition and peroxyl radical absorbance activity. Moreover, compound 6d significantly protected PC12 neurons against H2O2-induced cell death at low concentrations. Thus, these compounds could become multifunctional agents for further development for the treatment of AD.
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Design, synthesis and evaluation of genistein-polyamine conjugates as multi-functional Anti-Alzheimer agents
Acta Pharmaceutica Sinica B, 2015Co-Authors: Xin Zhang, Jiang Wang, Wen Luo, Chen Hong, Chao-jie WangAbstract:A series of genistein-polyamine conjugates (4a-4h) were designed, synthesized and evaluated as multi-functional Anti-Alzheimer agents. The results showed that these compounds had significant cholinesterases (ChEs) inhibitory activity. Compound 4b exhibited the strongest inhibition to acetylcholinesterase (AChE) with an IC50value of 2.75μmol/L, which was better than that of rivastigmine (5.60μmol/L). Lineweaver-Burk plot and molecular modeling study showed that compound 4b targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, compound 4b showed potent metal-chelating ability. In addition, it was found that 4a-4h did not affect HepG-2 cell viability at the concentration of 10μmol/L.
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design synthesis and evaluation of novel 4 dimethylamine flavonoid derivatives as potential multi functional Anti Alzheimer agents
Bioorganic & Medicinal Chemistry, 2013Co-Authors: Wen Luo, Chen Hong, Runguo Tian, Yueqiao Wang, Junjie Yue, Chao-jie WangAbstract:A series of 4-dimethylamine flavonoid derivatives 5a-5r were designed, synthesized and evaluated as potential multi-functional Anti-Alzheimer agents. The results showed that most of the synthesized compounds exhibited high acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity at the micromolar range (IC50, 1.83-33.20 μM for AChE and 0.82-11.45 μM for BChE). A Lineweaver-Burk plot indicated a mixed-type inhibition for compound 5j with AChE, and molecular modeling study showed that 5j targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, the derivatives showed potent self-induced Aβ aggregation inhibitory activity at 20 μM with percentage from 25% to 48%. In addition, some compounds (5j-5q) showed potent oxygen radical absorbance capacity (ORAC) ranging from 1.5- to 2.6-fold of the Trolox value. These compounds should be further investigated as multi-potent agents for the treatment of Alzheimer's disease.
Luigi Messori - One of the best experts on this subject based on the ideXlab platform.
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Promising in Vitro Anti-Alzheimer Properties for a Ruthenium(III) Complex.
ACS Medicinal Chemistry Letters, 2013Co-Authors: Luigi Messori, Michela Camarri, Teresa Ferraro, Chiara Gabbiani, Davide FranceschiniAbstract:Metal complexes represent today an attractive class of experimental Anti-Alzheimer agents with the potential of blocking β-amyloid 1–42 aggregation and scavenging its toxicity. Three representative ruthenium(III) complexes, namely NAMI A, KP1019, and PMRU20, were specifically evaluated to this end in an established in vitro model of AD relying on primary cortical neurons. Notably, PMRU20 turned out to be highly effective in protecting cortical neurons against Aβ 1–42 toxicity, while the other tested ruthenium compounds were poorly active or even inactive; we also found that PMRU20 is virtually devoid of any significant toxicity in vitro at the applied concentrations. Interestingly, PMRU20 was neuroprotective even against the toxicity induced by Aβ 25–35. The direct reaction of PMRU20 with Aβ 1–42 was explored through ESI MS analysis and some adduct formation evidenced. In addition, thioflavin T assays revealed that PMRU20 greatly reduces Aβ 1–42 aggregation. The implications of these findings are discusse...
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Promising in Vitro Anti-Alzheimer Properties for a Ruthenium(III) Complex.
ACS medicinal chemistry letters, 2013Co-Authors: Luigi Messori, Michela Camarri, Teresa Ferraro, Chiara Gabbiani, Davide FranceschiniAbstract:Metal complexes represent today an attractive class of experimental Anti-Alzheimer agents with the potential of blocking β-amyloid 1–42 aggregation and scavenging its toxicity. Three representative...