@article {1009, title = {Chemical and Biological Evaluation of the Aqueous Extract of Peumus boldus Molina (Monimiaceae) Leaves}, journal = {Pharmacognosy Research}, volume = {14}, year = {2022}, month = {December 2021}, pages = {45-52}, type = {Original Article}, chapter = {45}, abstract = {

Background: Traditional medicine has inspired the scientific community to discover natural compounds with the ability to inhibit the enzyme acetylcholinesterase (AChE) and with significant antioxidant capacity. These themes are associated with therapeutic processes to decrease the symptoms of Alzheimer{\textquoteright}s disease (AD). Acetylcholine (Ach) is an important neurotransmitter in the central nervous system responsible for transmitting the nervous impulse and increasing intestinal motility and dilation of sphincters in the gastrointestinal tract. As the species Peumus boldus Molina is widely known and used in folk medicine to treat gastrointestinal discomfort, its constituents could have an affinity for AChE and could be used to treat AD. Materials and Methods: This study evaluated the chemical, inhibitory activity of AChE (using the Elmann method and in silico), antioxidant capacity (DPPH, ABTS, FRAP, and oxidation inhibition of the β-carotene/linoleic acid system), and quantification of total leaf phenols from a commercial sample of P. boldus. Results: The mass spectral analysis allowed identification of the alkaloids isoboldine, boldine, clocaurine, laurotetanine, N-methylurotetanine, reticuline, and N-methylcoclaurine. In the in silico prediction test, the alkaloid N-metillaurotetanine was the best acetylcholinesterase enzyme inhibitor, with energy of -10.1 kcal mol-1. Conclusion: These results are of scientific relevance for the discovery of new drugs to treat dementia associated with Alzheimer{\textquoteright}s disease and stimulate the continuity of chemical and biological studies (anticholinesterase and antioxidant action) of prepurified fractions and substances isolated from P. boldus leaves.

}, keywords = {Acetylcholine, Acetylcholinesterase, Alzheimer., Antioxidant activity, Boldo}, doi = {10.5530/pres.14.1.8}, url = {https://phcogres.com/fulltext/v14i1/105530pres1418.html}, author = {Bruna Yuka Koide da Silva and Aniele da Silva Neves Lopes and Paulo Jos{\'e} Sousa Maia and Josiana Moreira Mar and Laiane Souza da Silva and Edgar Aparecido Sanches and Geone Maia Corr{\^e}a and Jaqueline de Ara{\'u}jo Bezerra and Dominique Fernandes de Moura do Carmo} } @article {1015, title = {Pharmacological Evaluation of Green Chilli in Alzheimer{\textquoteright}s Disease}, journal = {Pharmacognosy Research}, volume = {14}, year = {2022}, month = {December 2021}, pages = {61-70}, type = {Research Article}, chapter = {61}, abstract = {

Background: Green chilli pepper (Capsicum annum L. car frutescens) is popular as a spice used in many cuisines across the world. Capsaicin, as the pharmacologically active composition of chilli pepper, has been shown to possess antioxidant, local analgesic, and hypoglycemic effects according to many studies conducted on the red chilli pepper. However, there is no data associated with the role of green chilli peppers in Alzheimer{\textquoteright}s disease (AD) caused by capsaicin, rather than red chilli peppers. Objectives: To evaluate the acetylcholinesterase (AChE) and beta-secretase enzyme inhibition of ethanolic extract of Capsicum frutescens (EECF) or known as green chilli in in-vitro manner. Materials and Methods: Extraction was carried out on the fruits of Capsicum frutescens with ethanol. Its ethanolic extract in different concentrations was applied as the analyte to test its anti-acetylcholinesterase activity and enzymatic inhibitory action on the beta-secretase. Donepezil with various concentrations was also prepared as the control set for comparison of effect with EECF. Both the analytes were tested using the QuantiChromTM and BACE-1 FRET assay kits, for evaluation of inhibition activity against acetylcholinesterase and BACE-1 respectively. Results: There is significant increase in the percentage of inhibition against acetylcholinesterase and BACE-1 when tested with increased concentration of EECF. Compared to inhibitory effects by EECF, donepezil exhibited higher values of IC50 against both the assayed key enzymes, though also demonstrated vital inhibitory actions in both assays. EECF also showed higher potency in controlling AD progression in terms of inhibition against acetylcholinesterase, shown by IC50 value for the acetylcholinesterase, if compared to IC50 value for BACE-1. Conclusion: Green chilli or EECF has potential to have inhibitory action on acetylcholinesterase and beta-secretase enzymes in patients with AD, but limited to optimum concentration or dose.

}, keywords = {Acetylcholinesterase, Alzheimer{\textquoteright}s disease, Betasecretase, Capsaicin., Green chilli}, doi = {10.5530/pres.14.1.10}, url = {https://phcogres.com/fulltext/v14i1/105530pres14110.html}, author = {Pandurangan Perumal and Desmond Yong Hua Chong} } @article {158, title = {Two Lycopodium Alkaloids from the Aerial Parts of Huperzia phlegmaria}, journal = {Pharmacognosy Research}, volume = {11}, year = {2019}, month = {November,2019}, pages = {396-399}, type = {Original Article}, chapter = {396}, abstract = {

Background: Huperzia phlegmaria has been used to enhancing memory and alleviate brain disorders. It contains high amount of alkaloids, which are potent acetylcholinesterase (AChE) inhibitor. Materials and Methods: Lycopodium alkaloids from aerial parts of H. phlegmaria were isolated by chromatographic methods. Their structures were elucidated by spectroscopic methods, including mass spectrometry and nuclear magnetic resonance. AChE inhibitory effect of isolated compounds in vitro was evaluated using Ellman{\textquoteright}s assay. Results: These compounds were identified as fawcettidine and 12-epilycodoline N-oxide. Two compounds showed moderately AChE inhibitory effects with IC50 values of 33.11 {\textmu}g/mL and 64.56 {\textmu}g/mL, respectively. Conclusion: These isolated compounds could be promising drugs for the treatment of Alzheimer{\textquoteright}s disease.

}, keywords = {12-epilycodoline N-oxide, Acetylcholinesterase, Fawcettidine, Huperzia phlegmaria, Lycopodium alkaloids.}, doi = {10.4103/pr.pr_82_19}, author = {Dang Kim Thu and Dao Thi Vui and Bui Thanh Tung} } @article {298, title = {Dual Anti-cholinesterase Activity of Ajoene by In silico and In vitro Studies}, journal = {Pharmacognosy Research}, volume = {10}, year = {2018}, month = {April 2018}, pages = {225-229}, type = {Original Article}, chapter = {225}, abstract = {

The two major forms of cholinesterase enzymes found in the mammalian brain are acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). BuChE usually found mainly in glial cells and neuron in normal physiological condition, whereas AChE found near nerve synapse and axons, both are involved in the breakdown of acetylcholine (ACh) in the brain. The dual inhibition of these enzymes is considered as a promising strategy for the treatment of a neurological disorder such as Alzheimer{\textquoteright}s disease, senile dementia, ataxia, and myasthenia gravis. The objective is to study the dual anticholinesterase activity of ajoene using in silico and in vitro methods. The anticholinesterase activity of ajoene was evaluated using Ellman{\textquoteright}s assay, and molecular docking was performed on Schr{\"o}dinger suite software. The present study demonstrated ajoene ([E, Z]-4, 5, 9-trithiadodeca-1, 6, 11-triene-9-oxide) inhibited both AChE and BuChE in a concentration-dependent manner. The IC50 value of ajoene was 2.34 mM for AChE and 2.09 mM for BuChE. Kinetic studies showed mixed noncompetitive inhibition of AChE and uncompetitive inhibition of BuChE. Molecular docking studies revealed that ajoene interacts hydrophobically with catalytic residues of AChE while in case of BuChE the interaction is through noncatalytic binding site residues. Ajoene exhibits dual inhibitory activity against both AChE and BuChE enzymes.

}, keywords = {Acetylcholinesterase, Ajoene, Alzheimer{\textquoteright}s diseases, Butyrylcholinesterase, Molecular docking}, doi = {10.4103/pr.pr_140_17}, author = {Shivani Kumar and Sayan Chatterjee and Suresh Kumar} } @article {786, title = {Effect of Ethanolic Extract of Acacia Auriculiformis Leaves on Learning and Memory in Rats}, journal = {Pharmacognosy Research}, volume = {6}, year = {2012}, month = {May,2014}, pages = {246-250}, type = {Original Article}, chapter = {246}, abstract = {

Background: The effects and benefits of Acacia auriculiformis on health are not well established. This study was planned to evaluate the effect of ethanolic extract of Acacia auriculiformis leaves on learning and memory in rats. Materials and Methods: Learning and memory were evaluated using passive avoidance paradigm and rewarded alternation test (T-maze) after the oral administration of two doses (200mg/kg and 400mg/kg) of ethanolic extract of Acacia auriculiformis with rivastigmine as positive control. Forty eight rats were divided into 4 groups in each study model. Estimation of brain cholinesterase activity was done to substantiate the results of the above mentioned tests. Data was analyzed using one way Analysis of Variance (ANOVA) followed by Tukey{\textquoteright}s post-hoc test using GraphPad InStat software, version 3.06. Results: The extract produced a dose-dependent improvement in the memory score namely the step through latency in passive avoidance model (P \< 0.001) and the percentage of correct responses in rewarded alternation test (P \< 0.05). Dose-dependent inhibition of brain cholinesterase activity (P \< 0.001) was also noted. Conclusion: The acetylcholinesterase inhibiting property of Acacia auriculiformis contributes to its memory enhancing potential. Further large scale studies are required to elucidate its benefits on cognitive function. This may offer a promising new option for the treatment of dementia and other cognitive deficits.

}, keywords = {Acacia auriculiformis, Acetylcholinesterase, Memory, Passive Avoidance, Rewarded alternation}, doi = {10.4103/0974-8490.132605} }