8 results on '"Yu, Lintao"'
Search Results
2. Research on Spectrum Sharing Algorithm Based on Potential Game Theory
- Author
-
Zhou Yuxuan, Luo Shouzhi, and Yu Lintao
- Subjects
Computer Science::Computer Science and Game Theory ,Optimization problem ,Computer science ,Spectrum (functional analysis) ,020206 networking & telecommunications ,020302 automobile design & engineering ,Throughput ,02 engineering and technology ,Interference (wave propagation) ,Frequency allocation ,symbols.namesake ,Cognitive radio ,0203 mechanical engineering ,Nash equilibrium ,0202 electrical engineering, electronic engineering, information engineering ,symbols ,General Earth and Planetary Sciences ,Potential game ,Spectrum sharing ,Throughput (business) ,Algorithm ,General Environmental Science ,Communication channel - Abstract
Aiming at the problem of dynamic spectrum allocation in cognitive radio network, a novel spectrum allocation sharing algorithm based on improved interference coordination(Non-cooperation Spectrum Sharing Algorithm based on Interference Coordination, NCSSA-IC)is proposed. Firstly, the spectrum allocation problem is transformed into joint optimization problem. Then, the potential game algorithm is used to realize the optimal spectrum allocation scheme. In the stage of allocation, the second users choose the communication channel that can minimize the interference and maximize the throughput of the system, thus achieving the optimal spectrum allocation. Finally, the proposed algorithm is compared with other algorithms verified by spectrum allocation simulation. All the experiment results indicate that the proposed algorithm could converge to Nash equilibrium in a short time, and the total interference of the system is reduced to minimal and the throughput of the user could reach the maximum. Meanwhile the fairness of the users is greatly improved, and the efficient utilization of the spectrum realized.
- Published
- 2018
3. Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer’s disease
- Author
-
Ma Qianwen, Zhipei Sang, Wang Huijuan, Wenmin Liu, Wang Keren, Han Xue, Huifang Wang, Yu Lintao, and Ye Mengyao
- Subjects
0301 basic medicine ,Monoamine Oxidase Inhibitors ,Molecular model ,Cell Survival ,Stereochemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Phthalimides ,01 natural sciences ,Biochemistry ,Phthalimide ,Inhibitory Concentration 50 ,Structure-Activity Relationship ,03 medical and health sciences ,chemistry.chemical_compound ,Alzheimer Disease ,Cell Line, Tumor ,Drug Discovery ,Cholinesterases ,Humans ,Amines ,Cytotoxicity ,Monoamine Oxidase ,Molecular Biology ,Cholinesterase ,Binding Sites ,biology ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,Active site ,In vitro ,Protein Structure, Tertiary ,0104 chemical sciences ,Molecular Docking Simulation ,Kinetics ,030104 developmental biology ,Blood-Brain Barrier ,Drug Design ,biology.protein ,Lipinski's rule of five ,Molecular Medicine ,Cholinesterase Inhibitors ,Monoamine oxidase B - Abstract
A series of novel phthalimide-alkylamine derivatives were synthesized and evaluated as multi-functions inhibitors for the treatment of Alzheimer’s disease (AD). The results showed that compound TM - 9 could be regarded as a balanced multi-targets active molecule. It exhibited potent and balanced inhibitory activities against ChE and MAO-B ( hu AChE, hu BuChE, and hu MAO-B with IC 50 values of 1.2 μM, 3.8 μM and 2.6 μM, respectively) with low selectivity. Both kinetic analysis of AChE inhibition and molecular modeling study suggested that TM - 9 binds simultaneously to the catalytic active site and peripheral anionic site of AChE. Interestingly, compound TM - 9 abided by Lipinski’s rule of five. Furthermore, our investigation proved that TM - 9 indicated weak cytotoxicity, and it could cross the blood-brain barrier (BBB) in vitro . The results suggest that compound TM - 9 , an interesting multi-targeted active molecule, offers an attractive starting point for further lead optimization in the drug-discovery process against Alzheimer’s disease.
- Published
- 2017
4. Design, synthesis and biological evaluation of 3,4-dihydro-2(1 H )-quinoline- O -alkylamine derivatives as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer’s disease
- Author
-
Yu Lintao, Wanli Pan, Zhipei Sang, Liu Wenmin, Wang Keren, and Ma Qinge
- Subjects
0301 basic medicine ,Monoamine Oxidase Inhibitors ,Swine ,Monoamine oxidase ,Stereochemistry ,Clinical Biochemistry ,Pharmaceutical Science ,01 natural sciences ,Biochemistry ,03 medical and health sciences ,chemistry.chemical_compound ,Alzheimer Disease ,Drug Discovery ,Animals ,Humans ,Monoamine Oxidase ,Molecular Biology ,Butyrylcholinesterase ,Cholinesterase ,Oxidase test ,biology ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,Quinoline ,Active site ,Acetylcholinesterase ,0104 chemical sciences ,030104 developmental biology ,Blood-Brain Barrier ,Drug Design ,Electrophorus ,Quinolines ,biology.protein ,Lipinski's rule of five ,Molecular Medicine ,Cholinesterase Inhibitors - Abstract
A new family of multitarget molecules able to interact with acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), as well as with monoamino oxidase (MAO) A and B, has been synthesized. Novel 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives have been designed using a conjunctive approach that combines the JMC49 and donepezil. The most promising compound TM-33 showed potent and balance inhibitory activities toward ChE and MAO (eeAChE, eqBuChE, hMAO-A and hMAO-B with IC50 values of 0.56μM, 2.3μM, 0.3μM and 1.4μM, respectively) but low selectivity. Both kinetic analysis of AChE inhibition and molecular modeling study suggested that TM-33 binds simultaneously to the catalytic active site and peripheral anionic site of AChE. Furthermore, our investigation proved that TM-33 could cross the blood-brain barrier (BBB) in vitro, and abided by Lipinski's rule of five. The results suggest that compound TM-33, an interesting multi-targeted active molecule, offers an attractive starting point for further lead optimization in the drug-discovery process against Alzheimer's disease.
- Published
- 2017
5. Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease
- Author
-
Yu Lintao, Jian Shi, Qinge Ma, Wenmin Liu, Zhipei Sang, Cheng Xinfeng, Zhenghuai Tan, Wang Keren, Gaofeng Zhu, Yiyang Zhao, and Rongrui Wei
- Subjects
Antioxidant ,medicine.medical_treatment ,Rivastigmine ,Pharmacology ,Ligands ,01 natural sciences ,Neuroprotection ,03 medical and health sciences ,chemistry.chemical_compound ,Structure-Activity Relationship ,Alzheimer Disease ,Drug Discovery ,medicine ,Potency ,Animals ,Humans ,Apigenin ,Zebrafish ,030304 developmental biology ,0303 health sciences ,Amyloid beta-Peptides ,Dose-Response Relationship, Drug ,Molecular Structure ,010405 organic chemistry ,Organic Chemistry ,General Medicine ,Metabolism ,Acute toxicity ,0104 chemical sciences ,Rats ,Molecular Docking Simulation ,Neuroprotective Agents ,chemistry ,Butyrylcholinesterase ,Microsome ,Acetylcholinesterase ,Microsomes, Liver ,Cholinesterase Inhibitors ,medicine.drug - Abstract
Here we reported novel apigenin-rivastigmine hybrids were rationally designed and synthesized by the multi-target-directed ligands (MTDLs) strategy, their activity in vitro results revealed that compound 3d showed significant antioxidant potency (ORAC = 1.3 eq), and it was a reversible huAChE (IC50 = 6.8 μM) and huBChE (IC50 = 16.1 μM) inhibitor. 3d also served as a selective metal chelator, and it significantly inhibited and disaggregated self-mediated and Cu2+-mediated Aβ1-42 aggregation, and also inhibited hAChE-mediated induced Aβ1-40 aggregation. Compound 3d exhibited remarkable neuroprotective effect and hepatoprotective activity. In addition, compound 3d presented favourable blood-brain barrier penetration in vitro and drug-like property. Further, the in vivo assay displayed that 3d indicated remarkable dyskinesia recovery rate and response efficiency on AD zebrafish, and exhibited surprising protective effect on Aβ1-40-mediated zebrafish vascular injury. More importantly, 3d did not indicate obvious acute toxicity at dose up to 2000 mg/kg, and could improve scopolamine-induced memory impairment. Subsequently, the regulation of multi-targets for 3d were further confirmed through transcriptome sequencing of brain hippocampi, which also offered novel potential targets and opened a new way to treat Alzheimer’s disease. More interestingly, the metabolism of 3d in vitro indicated that 4 metabolites in rat liver microsome metabolism, 2 metabolites in human liver microsome metabolism, and 4 metabolites in intestinal flora metabolism, which offered supports for the preclinical study of 3d. Overall, this study exhibited that compound 3d was a promising advanced compound targeted multiple factors associated with AD.
- Published
- 2019
6. Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease
- Author
-
Huifang Wang, Ma Qianwen, Yu Lintao, Wang Huijuan, Wenmin Liu, Wang Keren, Han Xue, Zhipei Sang, and Ye Mengyao
- Subjects
0301 basic medicine ,Antioxidant ,Molecular model ,medicine.medical_treatment ,Clinical Biochemistry ,Pharmaceutical Science ,01 natural sciences ,Biochemistry ,PC12 Cells ,Antioxidants ,Piperazines ,chemistry.chemical_compound ,Drug Discovery ,ADME ,biology ,Molecular Docking Simulation ,Neuroprotective Agents ,Blood-Brain Barrier ,Lipinski's rule of five ,Acetylcholinesterase ,Molecular Medicine ,Stereochemistry ,Cell Survival ,Permeability ,03 medical and health sciences ,Benzophenones ,Inhibitory Concentration 50 ,Structure-Activity Relationship ,Phenols ,Alzheimer Disease ,medicine ,Phenol ,Animals ,Humans ,Chelation ,Molecular Biology ,Monoamine Oxidase ,Binding Sites ,010405 organic chemistry ,Organic Chemistry ,Active site ,Hydrogen Peroxide ,In vitro ,0104 chemical sciences ,Protein Structure, Tertiary ,Rats ,030104 developmental biology ,chemistry ,Drug Design ,biology.protein ,Cholinesterase Inhibitors - Abstract
A series of 2-acetyl-5-O-(amino-alkyl)phenol derivatives was designed, synthesized and evaluated as multi-function inhibitors for the treatment of Alzheimer’s disease (AD). The results revealed that compound TM-3 indicated selective AChE inhibitory potency (eeAChE, IC50 = 0.69 μM, selective index (SI) = 32.7). Both kinetic analysis of AChE inhibition and molecular modeling study suggested that TM-3 could simultaneously bind to the catalytic active site and peripheral anionic site of AChE. And TM-3 was also a highly selective MAO-B inhibitor (IC50 = 6.8 μM). Moreover, TM-3 could act as antioxidant (ORAC value was 1.5eq) and neuroprotectant, as well as a selective metal chelating agent. More interestingly, compound TM-3 could cross the blood-brain barrier (BBB) in vitro and abided by Lipinski’s rule of five. Therefore, compound TM-3, a promising multi-targeted active molecule, offers an attractive starting point for further lead optimization in the drug-discovery process against AD.
- Published
- 2017
7. Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease
- Author
-
Yan Yang, Qinge Ma, Xiaoqing Li, Qian Xu, Wenmin Liu, Wanli Pan, Yu Lintao, Chaoliang Leng, Zhenghuai Tan, Ping Bai, Zhipei Sang, and Wang Keren
- Subjects
0301 basic medicine ,Antioxidant ,Coumaric Acids ,Aché ,medicine.medical_treatment ,01 natural sciences ,PC12 Cells ,Antioxidants ,Ferulic acid ,03 medical and health sciences ,chemistry.chemical_compound ,Mice ,Alzheimer Disease ,Drug Discovery ,medicine ,Animals ,Humans ,IC50 ,Butyrylcholinesterase ,Pharmacology ,Memory Disorders ,Amyloid beta-Peptides ,Eels ,010405 organic chemistry ,Organic Chemistry ,General Medicine ,Acetylcholinesterase ,Acute toxicity ,language.human_language ,0104 chemical sciences ,Rats ,030104 developmental biology ,chemistry ,Biochemistry ,Blood-Brain Barrier ,Drug Design ,language ,Trolox ,Cholinesterase Inhibitors - Abstract
A series of novel ferulic acid-O-alkylamines derivatives were designed, synthesized, and evaluated as multitarget-directed ligands against Alzheimer's disease. In vitro studies displayed that all the synthesized target compounds showed impressive inhibitory activity against butyrylcholinesterase (BuChE), significant inhibition/disaggregation of self-induced β-amyloid (Aβ) aggregation and acted as potential antioxidants. Particularly, compound 7f, one of the most potent BuChE inhibitor (IC50 value of 0.021 μM for equine serum BuChE, 8.63 μM for ratBuChE and 0.07 μM for human serum BuChE), was found to be a good acetylcholinesterase (AChE) inhibitor (IC50 = 2.13 μM for electric eel AChE, 1.8 μM for ratAChE and 3.82 μM for human erythrocytes AChE), and the result of molecular docking provided an explanation for its selective BuChE inhibitory activity. Compound 7f also had noteworthy inhibitory effects on self-induced Aβ1-42 aggregation (50.8 ± 0.82%) and was found to disaggregate self-induced Aβ1-42 aggregation (38.7 ± 0.65%), which was further elucidated by the transmission electron microscopy. Meanwhile, compound 7f showed the modest antioxidant activity (0.55 eq of Trolox), good protective effect against H2O2-induced PC12 cell injury, with low toxicity. Moreover, compound 7f could cross the blood-brain barrier (BBB) in vitro. Significantly, compound 7f did not exhibit any acute toxicity in mice at doses up to 1000 mg/kg, and the step-down passive avoidance test showed this compound significantly reversed scopolamine-induced memory deficit in mice. Taken together, the results indicated that compound 7f is a very promising multifunctional agent in the treatment of Alzheimer's disease, particularly the advanced stages of AD.
- Published
- 2016
8. Design, synthesis and evaluation of novel ferulic acid-memoquin hybrids as potential multifunctional agents for the treatment of Alzheimer's disease
- Author
-
Ke Hu, Chen Changzhong, Kelin Peng, Xu Zhang, Yu Lintao, Ping Bai, Li Tao, Qin-Ge Ma, Wenmin Liu, Zhipei Sang, and Wanli Pan
- Subjects
0301 basic medicine ,Antioxidant ,Coumaric Acids ,medicine.medical_treatment ,Clinical Biochemistry ,Drug Evaluation, Preclinical ,Pharmaceutical Science ,Chemistry Techniques, Synthetic ,Blood–brain barrier ,01 natural sciences ,Biochemistry ,PC12 Cells ,Antioxidants ,Ferulic acid ,03 medical and health sciences ,chemistry.chemical_compound ,Alzheimer Disease ,Drug Discovery ,Alkanes ,medicine ,Ethylamines ,Animals ,Humans ,Molecular Biology ,IC50 ,Cholinesterase ,Amyloid beta-Peptides ,biology ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,Hydrogen Peroxide ,medicine.disease ,Acetylcholinesterase ,In vitro ,0104 chemical sciences ,Rats ,030104 developmental biology ,medicine.anatomical_structure ,Neuroprotective Agents ,Blood-Brain Barrier ,Drug Design ,biology.protein ,Molecular Medicine ,Cholinesterase Inhibitors ,Alzheimer's disease - Abstract
A novel series of ferulic acid-memoquin hybrids were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease (AD). The in vitro studies showed that most of the compounds exhibited a significant ability to inhibit acetylcholinesterase (AChE) (IC50 of 3.2-34.7μM) and self-induced β-amyloid (Aβ1-42) aggregation (30.8-39.1%, 25μM), to act as potential antioxidants (ORAC-FL value of 0.9-1.3). In particular, compound 17d had the greatest ability to inhibit AChE (IC50=3.2μM), and Aβ1-42 aggregation (30.8%) was also an excellent antioxidant and neuroprotectant. Moreover, it is capable of disaggregating self-induced Aβ aggregation. Furthermore, 17d could cross the blood-brain barrier (BBB) in vitro. The results showed that compound 17d is a potential multifunctional agent for the treatment of AD.
- Published
- 2015
Catalog
Discovery Service for Jio Institute Digital Library
For full access to our library's resources, please sign in.