@article {1228, title = {In silico and Biological Screening of Phytochemicals against NMDA Receptor for Alzheimer{\textquoteright}s Disease Therapeutics}, journal = {Pharmacognosy Research}, volume = {16}, year = {2024}, month = {April 2024}, pages = {244-253}, type = {Original Article}, chapter = {244}, abstract = {

Background: Alzheimer{\textquoteright}s Disease (AD), characterized by irreversible neurodegeneration and cognitive decline, lacks a definitive cure, and current medications merely alleviate symptoms. Cognitive manifestations in AD are linked to disrupted glutamatergic neurotransmission, where β-Amyloid (A) accumulation at specific synapses interacts with glutamine synthetase, causing enzyme inactivation and subsequent NMDA signalling impairment. Dysregulation of glutamine synthetase leads to NMDA receptor hyper activation, resulting in neuronal damage and cell death. Aim: The focus of this investigation is on N-Methyl D-Aspartate (NMDA) receptors, which belong to the ionotropic glutamate receptor family and play vital roles in various physiological and pathological processes such as neuron development, synaptic plasticity, and central nervous system learning and memory. This study seeks to analyze target data to differentiate between effective and ineffective options for virtual screening. Utilizing this information, the study aims to generate a novel or enhanced reaction product. Materials and Methods: Computational embedding was employed to explore interactions between NMDA receptors and phytoconstituents of selected plants, including Amla, Shankhapushpi, Giloy, Ashwagandha, and Turmeric. ADMET descriptions for well-known botanical compounds were also scrutinized. Results: Structural analysis of 75 compounds derived from selected phytochemicals was conducted based on molecular properties. Key compounds were identified, and additional ADMET properties were evaluated. Quercetin emerged as the top-ranking compound based on shear score, shear strength, and molecular interactions with NMDA receptors. Conclusion: This computational study identifies specific plants as potential NMDA receptor antagonists, offering promise for mitigating Alzheimer{\textquoteright}s disease symptoms in the future.

}, keywords = {ADMET descriptions, Alzheimer{\textquoteright}s disease, Computational embedding, Dock ligands, Molecular docking, N-methyl-D-aspartate-receptor, Quercetin.}, doi = {10.5530/pres.16.2.31}, author = {Bhushan Arun Baviskar and Sharada Laxman Deore and Bhavana Ashok Shende and Somshekhar Khadabadi and Anjali Ashokrao Kide} } @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 {175, title = {Cholinergic-Enhancing and Antioxidant Effect of Vigna subterranea (L.) Verdc. (Fabaceae) Landrace Aqueous Extract on Scopolamine-Induced Amnesia in Male Swiss Mice}, journal = {Pharmacognosy Research}, volume = {12}, year = {2020}, month = {August 2020}, pages = {303-312}, type = {Original Article}, chapter = {303}, abstract = {

Background: Currently, no drug effectively curbs down the progression of Alzheimer{\textquoteright}s disease (AD), and thus early prevention is important. Objectives: The present study was conducted to investigate the protective effects of the aqueous extract of Vigna subterranea seed landrace on amnesia induced by scopolamine in mice. Materials and Methods: V. subterranea aqueous extract (100, 200, and 400 mg/kg BW) was administered by gavage for 9 consecutive days and memory impairment was induced by repeated intraperitoneal injection of scopolamine (1.5 mg/kg). The Y-maze (YM), Morris water maze (MWM), novel object recognition paradigm (NOR), and the T maze{\texttrademark} were used to assess learning, memory, and retention. Superoxide dismutase (SOD), catalase (CAT), malondialdehyde (MDA) levels, and acetyclcholine esterase activity were also evaluated in the mouse hippocampi homogenates. Results: V. subterranea aqueous extract (400 mg/kg) significantly increased the percentage of spontaneous alternation in the YM task and decreased escape latency in the MWM. Moreover, this dose brought about a significant improvement in the time spent in the preferred TM arm and discrimination index in the NOR tasks despite repeated scopolamine injection. Additionally, low acetylcholine esterase levels, reduced lipid peroxidation (MDA), but increased antioxidant enzyme (CAT and SOD) activity were observed in hippocampi homogenate of mice pretreated with the extract. A protective action against hippocampal cell damage was also evident. Conclusion: This finding suggests that the aqueous extract of V. subterranea seed landrace may improve learning and memory.

}, keywords = {Acetylcholine esterase, Alzheimer{\textquoteright}s disease, Antioxidant, Memory impairment, Scopolamine, Vigna subterranean}, doi = {10.4103/pr.pr_62_19}, author = {Herv{\'e} Herv{\'e} Ngatanko Abaissou and Harquin Simplice Foyet and Eglantine Keugong Wado and Balbine Kamleu Nkwingwa and Jorelle Linda Damo Kamda and Lea Blondelle Kenko Djomessie and Alin Ciobica and Elisabeth Ngo Bum} }