ChemInform Abstract: Synthesis and Evaluation of AChE Inhibitory Activity of 5-Substituted- 1H-Indole-2,3-dione-3-((6H)bromo-3,4-dihydro-3-(4-Substituted-phenyl)- 4-oxo-2-quinazolinyl)hydrazones.

ChemInform ◽  
1988 ◽  
Vol 19 (15) ◽  
Author(s):  
A. K. SENGUPTA ◽  
S. ANAND ◽  
A. K. PANDEY
Keyword(s):  
Inhibitory Activity ◽  
Ache Inhibitory Activity

Effect of alkaloid extracted from Huperzia phlegmaria on cognitive deficits scopolamine-induced in mice

2020 ◽  
Vol 16 ◽  
Author(s):  
Dang Kim Thu ◽  
Dao Thi Vui ◽  
Nguyen Thi Ngoc Huyen ◽  
Nguyen Thi Thanh Binh ◽  
Nguyen Thi Huyen ◽  
...  
Keyword(s):  
Cognitive Impairment ◽  
Mouse Brain ◽  
Cognitive Deficits ◽  
Inhibitory Activity ◽  
Water Maze ◽  
Ache Activity ◽  
Y Maze ◽  
Ache Inhibitory Activity ◽  
Kinetic Inhibition ◽  
Brain Tissues

Background: Huperzia phlegmaria has been used for the treatment of neurological disorder. Alkaloids are main bioactive compounds found in Huperzia phlegmaria. We aimed to investigate the acetylcholinesterase (AChE) inhibitory activity in vitro of Huperzia phlegmaria alkaloid extract (HpAE) and protective effects on mice which were induced cognitive deficits by scopolamine. Methods: AChE inhibitory activity and kinetic inhibition mechanism was investigated by Ellman's assay. Mice were administrated orally HpAE (30 mg/kg and 60 mg/kg) for fourteen days, and injected scopolamine at a dose of 1 mg/kg intraperitoneally for four days to induce cognitive impairment. The Y-maze and the Morris water maze were used for evaluating the memory behaviors. Acetylcholine (ACh) levels and AChE activity were measured in brain tissue. Glutathione peroxidase (GPx), superoxide dismutase (SOD) activities, and malondialdehyde (MDA) groups were also evaluated in the mouse brain tissues. Results: Our data showed that HpAE had the strong AChE inhibitory activity with an IC50 value of 5.12 ± 0.48 μg/mL in a concentration-dependent manner. Kinetic inhibition analysis demonstrated that HpPAE inhibited AChE followed the mixed inhibition type with Ki (representing the affinity of the enzyme and inhibitor) was 4.37 ± 0.35 µg/mL. Scopolamine induced the cognitive impairment in Morris Water Maze and Y-maze test along with reduced brain levels of ACh and antioxidant enzyme and increased AChE activity in mouse brain tissues. Treatment with HpAE at both dose (30 mg/kg and 60 mg/kg) decreased the SCP-induced cognitive impairment in both behavioral tests along with decreased acetylcholinesterase activity and MDA level, and increased ACh level and antioxidant enzyme in mouse brain tissues. Conclusion: Our results suggested that the HpAE at both dose (30 mg/kg and 60 mg/kg) may be used for prevent and treatment of Alzheimer’s disease.

scholarly journals Volatile terpenoids as potential drug leads in Alzheimer’s disease

2017 ◽  
Vol 15 (1) ◽  
pp. 332-343 ◽  
Author(s):  
Karolina A. Wojtunik-Kulesza ◽  
Katarzyna Targowska-Duda ◽  
Katarzyna Klimek ◽  
Grażyna Ginalska ◽  
Krzysztof Jóźwiak ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Mtt Assay ◽  
Inhibitory Activity ◽  
Biological Activities ◽  
Plant Metabolites ◽  
Secondary Plant Metabolites ◽  
Docking Simulations ◽  
Ache Inhibitory Activity ◽  
Volatile Terpenoids

AbstractAlzheimer’s disease (AD) is by far the most prevalent of all known forms of dementia. Despite wide-spread research, the main causes of emergence and development of AD have not been fully recognized. Natural, low-molecular, lipophilic terpenoids constitute an interesting group of secondary plant metabolites, that exert biological activities of possible use in the prevention and treatment of AD. In order to identify secondary metabolites possessing both antioxidant activity and the potential to increase the level of acetylcholine, selected terpenoids have been screened for possible acetylcholinesterase inhibitory activity by use of two methods, namely Marston (chromatographic assay) and Ellman (spectrophotometric assay). In order to describe the interaction between terpenes and AChE active gorge, molecular docking simulations were performed. Additionally, all analyzed terpenes were also evaluated for their cytotoxic properties against two normal cell lines using MTT assay. The obtained results show that: carvone (6), pulegone (8) and γ-terpinene (7) possess desirable AChE inhibitory activity. MTT assay revealed low or lack of cytotoxicity of these metabolites. Thus, among the investigated terpenes, carvone (6), pulegone (8) and y-terpinene (7) can be recognized as compounds with most promising activities in the development of multi-target directed ligands.

Sesquiterpenes and a monoterpenoid with acetylcholinesterase (AchE) inhibitory activity from Valeriana officinalis var. latiofolia in vitro and in vivo

Fitoterapia ◽  
2016 ◽  
Vol 110 ◽  
pp. 142-149 ◽  
Author(s):  
Heng-Wen Chen ◽  
Xuan-Hui He ◽  
Rong Yuan ◽  
Ben-Jun Wei ◽  
Zhong Chen ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Valeriana Officinalis ◽  
Ache Inhibitory Activity

Voacafrines A-N, aspidosperma-type monoterpenoid indole alkaloids from Voacanga africana with AChE inhibitory activity

2021 ◽  
Vol 181 ◽  
pp. 112566 ◽  
Author(s):  
Qian Zhao ◽  
Wen-Tao Zhu ◽  
Xiao Ding ◽  
Zong-Qing Huo ◽  
Paul O. Donkor ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Indole Alkaloids ◽  
Monoterpenoid Indole Alkaloids ◽  
Ache Inhibitory Activity

Glutathione S-Transferase, Acetylcholinesterase Inhibitory and Antibacterial Activities of Chemical Constituents of Barleria prionitis

2007 ◽  
Vol 62 (4) ◽  
pp. 580-586 ◽  
Author(s):  
Kalhari S. Kosmulalage ◽  
Shamsulhaq Zahid ◽  
Chibuike C. Udenigwe ◽  
Sarfraz Akhtar ◽  
Athar Ata ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Chemical Constituents ◽  
Ethanolic Extract ◽  
Antibacterial Activities ◽  
Spectroscopic Studies ◽  
Sri Lankan ◽  
Glutathione S Transferase ◽  
Ache Inhibitory Activity ◽  
Phytochemical Studies ◽  
Derivatives Of

Phytochemical studies on the ethanolic extract of Barleria prionitis of Sri Lankan origin have resulted in the isolation of a new compound, balarenone (1), along with three known compounds, pipataline (2), lupeol (3) and 13,14-seco-stigmasta-5,14-diene-3-α-ol (4). The structures of 1 - 4 were elucidated with the aid of extensive NMR spectroscopic studies. Compounds 1 - 4 showed moderate inhibitory activity against glutathione S-transferase (GST) and acetylcholinesterase (AChE). Compounds 1, 2 and 4 also exhibited antibacterial activity against Bacillus cereus and Pseudomonas aeruginosa (25 μg/disk). Three different derivatives of compound (2), 7,8-epoxypipataline (5), 8- amino-7-hydroxypipataline (6) and 7,8-dibromopipataline (7) were synthesized to evaluate them for GST and AChE inhibitory activities. Household microwave radiations were used to synthesize compound (6). Among all tested compounds, 8-amino-7-hydroxypipataline (6) exhibited a significant AChE inhibitory activity with an IC50 value of 36.8 μM.

Synthesis of Novel Benzimidazole and Benzothiazole Derivatives Bearing a 1,2,3-triazole Ring System and their Acetylcholinesterase Inhibitory Activity

2017 ◽  
Vol 41 (1) ◽  
pp. 30-35 ◽  
Author(s):  
Laleh Faraji ◽  
Shiva Shahkarami ◽  
Hamid Nadri ◽  
Alireza Moradi ◽  
Mina Saeedi ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Docking Simulation ◽  
Triazole Ring ◽  
Copper Catalysts ◽  
Inhibitory Effect ◽  
Ring System ◽  
Benzothiazole Derivatives ◽  
Ache Inhibitory Activity ◽  
Group A

A series of 20 novel benzimidazole and benzothiazole derivatives linked to a 1,2,3-triazole ring system was synthesised, characterised and evaluated for in vitro acetylcholinesterase (AChE) inhibitory activity. Several copper catalysts and solvents were screened to establish the optimal conditions for the preparation of the target compounds. Three different linkers were used to optimise the enzyme inhibitory effect. Out of the 20 compounds, 13 showed some AChE inhibition. The most potent compound, which showed 84% inhibition at 100 μM, contained a 1-(2-fluorobenzyl)-1,2,3-triazole linked to a benzimidazole group. A docking simulation study showed that the most active compound bound preferentially to the catalytic anionic subsite of the AChE enzyme.

Synthesis and Biological Evaluation of Acetylcholinesterase Inhibitor Macakurzin C and Its Derivatives

Synlett ◽  
2015 ◽  
Vol 26 (08) ◽  
pp. 1131-1134 ◽  
Author(s):  
Hyoungsu Kim ◽  
Seung-Hoon Baek ◽  
Hongjun Jang
Keyword(s):  
Inhibitory Activity ◽  
Acetylcholinesterase Inhibitor ◽  
Biological Evaluation ◽  
Hydroxyl Groups ◽  
Structural Requirements ◽  
Ache Inhibitory Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

The derivatives of macakurzin C containing a modified D ring and protected C(3)/C(5)-hydroxyl groups were synthesized and their in vitro AChE inhibitory activity and neurotoxicity were evaluated to identify the structural requirements for the activities. The results indicated that C(3)-benzyl-protected derivative has a more potent AChE inhibitory activity (IC50, 2.6 μM) and a less neurotoxicity (GI50, >100 μM) than synthetic macakurzin C (IC50, 9.1 μM; GI50, 16.6 μM).

Delineating the pharmacophoric elements of huperzine A: importance of the unsaturated three-carbon bridge to its AChE inhibitory activity

1991 ◽  
Vol 34 (12) ◽  
pp. 3399-3402 ◽  
Author(s):  
Alan P. Kozikowski ◽  
Chris P. Miller ◽  
Fumio Yamada ◽  
Yuan Ping Pang ◽  
Jacqueline H. Miller ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Huperzine A ◽  
Ache Inhibitory Activity
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