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 ◽  
...  
Fitoterapia ◽  
2018 ◽  
Vol 124 ◽  
pp. 73-79 ◽  
Author(s):  
Ji Yang ◽  
Jing Fu ◽  
Xin Liu ◽  
Zhi-Hong Jiang ◽  
Guo-Yuan Zhu

2020 ◽  
Vol 16 ◽  
Author(s):  
Dang Kim Thu ◽  
Dao Thi Vui ◽  
Nguyen Thi Ngoc Huyen ◽  
Nguyen Thi Thanh Binh ◽  
Nguyen Thi Huyen ◽  
...  

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.


2021 ◽  
Vol 43 ◽  
pp. 23-26
Author(s):  
Miao Zhang ◽  
Si-Yu Du ◽  
Jie Liu ◽  
Xue Zhao ◽  
Jia-Ning Liu ◽  
...  

2007 ◽  
Vol 6 (1) ◽  
pp. 183-188 ◽  
Author(s):  
João Xavier de Araújo ◽  
Cyril Antheaume ◽  
Roseane Cristina P. Trindade ◽  
Martine Schmitt ◽  
Jean-Jacques Bourguignon ◽  
...  

2017 ◽  
Vol 15 (1) ◽  
pp. 332-343 ◽  
Author(s):  
Karolina A. Wojtunik-Kulesza ◽  
Katarzyna Targowska-Duda ◽  
Katarzyna Klimek ◽  
Grażyna Ginalska ◽  
Krzysztof Jóźwiak ◽  
...  

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.


ChemInform ◽  
2014 ◽  
Vol 45 (44) ◽  
pp. no-no
Author(s):  
Lei Wang ◽  
Wen-Cai Ye ◽  
Wei Zhang ◽  
Sheng-Yuan Zhang ◽  
Zhi-Qi Yin

2015 ◽  
Vol 5 (4) ◽  
pp. 185-193 ◽  
Author(s):  
Xu-Jie Qin ◽  
Yun-Li Zhao ◽  
Chang-Wei Song ◽  
Bei Wang ◽  
Ying-Ying Chen ◽  
...  

2018 ◽  
Vol 33 (15) ◽  
pp. 2139-2144 ◽  
Author(s):  
Huansha Yuwen ◽  
Yuxi Yuan ◽  
Xiaojiang Hao ◽  
Hongping He ◽  
Yu Zhang

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