scholarly journals Anticholinesterase Activity of Eight Medicinal Plant Species: In Vitro and In Silico Studies in the Search for Therapeutic Agents against Alzheimer’s Disease

2021 ◽  
Vol 2021 ◽  
pp. 1-14
Author(s):  
Md Josim Uddin ◽  
Daniela Russo ◽  
Md Mahbubur Rahman ◽  
Shaikh Bokhtear Uddin ◽  
Mohammad A. Halim ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Medicinal Plant ◽  
Plant Species ◽  
Inhibitory Effect ◽  
Medicinal Plant Species ◽  
Inhibitory Effects ◽  
In Silico Studies ◽  
Blumea Lacera

Many Bangladeshi medicinal plants have been used to treat Alzheimer’s disease and other neurodegenerative diseases. In the present study, the anticholinesterase effects of eight selected Bangladeshi medicinal plant species were investigated. Species were selected based on the traditional uses against CNS-related diseases. Extracts were prepared using a gentle cold extraction method. In vitro cholinesterase inhibitory effects were measured by Ellman’s method in 96-well microplates. Blumea lacera (Compositae) and Cyclea barbata (Menispermaceae) were found to have the highest acetylcholinesterase inhibitory (IC50, 150 ± 11 and 176 ± 14 µg/mL, respectively) and butyrylcholinesterase inhibitory effect (IC50, 297 ± 13 and 124 ± 2 µg/mL, respectively). Cyclea barbata demonstrated competitive inhibition, where Blumea lacera showed an uncompetitive inhibition mode for acetylcholinesterase. Smilax guianensis (Smilacaceae) and Byttneria pilosa (Malvaceae) were also found to show moderate AChE inhibition (IC50, 205 ± 31 and 221 ± 2 µg/mL, respectively), although no significant BChE inhibitory effect was observed for extracts from these plant species. Among others, Thunbergia Grandiflora (Acanthaceae) and Mikania micrantha (Compositae) were found to display noticeable AChE (IC50, 252 ± 22 µg/mL) and BChE (IC50, 314 ± 15 µg/mL) inhibitory effects, respectively. Molecular docking experiment suggested that compounds 5-hydroxy-3,6,7,3′,4′-pentamethoxyflavone (BL4) and kaempferol-3-O-α-L-rhamnopyranosyl-(1⟶6)-β-D-glucopyranoside (BL5) from Blumea lacera bound stably to the binding groove of the AChE and BChE by hydrogen-bond interactions, respectively. Therefore, these compounds could be candidates for cholinesterase inhibitors. The present findings demonstrated that Blumea lacera and Cyclea barbata are interesting objects for further studies aiming at future therapeutics for Alzheimer’s disease.

scholarly journals Anti-Aggregation Property of Allicin by In Vitro and Molecular Docking Studies

2019 ◽  
Vol 13 ◽  
pp. 117906951986618 ◽  
Author(s):  
Suresh Kumar ◽  
Shivani Kumar ◽  
Heera Ram
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Molecular Docking ◽  
Molecular Interaction ◽  
Fibril Formation ◽  
Amyloid Peptide ◽  
Peptide Aggregation ◽  
Aβ Peptide ◽  
In Silico Studies

Amyloidogenesis is the process in which amyloid beta (Aβ) peptide aggregation results in plaque formation in central nervous system (CNS) are associated with many neurological diseases such as Alzheimer’s disease. The peptide aggregation initiated from peptide monomers results in formation of dimers, tetramers, fibrils, and protofibrils. The ability of allicin, a lipid-soluble volatile organosulfur biological compound, present in freshly crushed garlic ( Allium sativum L.) to inhibit fibril formation by the Aβ peptide in vitro was investigated in the present study. Inhibition of fibrillogenesis was measured by a Thioflavin T (ThT) fluorescence assay and visualized by transmission electron microscopy (TEM). The molecular interaction between allicin and Aβ peptide was also demonstrated by in silico studies. The results show that allicin strongly inhibited Aβ fibrils by 97% at 300 µM, compared with control (Aβ only) ( P < .001). These results were further validated by visual of fibril formation by transmission microscopy and molecular interaction of amyloid peptide with allicin by molecular docking. Aβ forms favourable hydrophobic interaction with Ile32, Met35, Val36, and Val39, and oxygen of allicin forms hydrogen bond with the amino acid residue Lys28. Allicin anti-amyloidogenic property suggests that this naturally occurring compound may have potential to ameliorate and prevent Alzheimer’s disease.

scholarly journals The inhibition of cellular toxicity of amyloid-β by dissociated transthyretin

2020 ◽  
Vol 295 (41) ◽  
pp. 14015-14024 ◽  
Author(s):  
Qin Cao ◽  
Daniel H. Anderson ◽  
Wilson Y. Liang ◽  
Joshua Chou ◽  
Lorena Saelices
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Protective Effect ◽  
Amyloid Β ◽  
Inhibitory Effect ◽  
Aβ Oligomers ◽  
Cellular Toxicity ◽  
Computational Docking

The protective effect of transthyretin (TTR) on cellular toxicity of β-amyloid (Aβ) has been previously reported. TTR is a tetrameric carrier of thyroxine in blood and cerebrospinal fluid, the pathogenic aggregation of which causes systemic amyloidosis. However, studies have documented a protective effect of TTR against cellular toxicity of pathogenic Aβ, a protein associated with Alzheimer's disease. TTR binds Aβ, alters its aggregation, and inhibits its toxicity both in vitro and in vivo. In this study, we investigate whether the amyloidogenic ability of TTR and its antiamyloid inhibitory effect are associated. Using protein aggregation and cytotoxicity assays, we found that the dissociation of the TTR tetramer, required for its amyloid pathogenesis, is also necessary to prevent cellular toxicity from Aβ oligomers. These findings suggest that the Aβ-binding site of TTR may be hidden in its tetrameric form. Aided by computational docking and peptide screening, we identified a TTR segment that is capable of altering Aβ aggregation and toxicity, mimicking TTR cellular protection. EM, immune detection analysis, and assessment of aggregation and cytotoxicity revealed that the TTR segment inhibits Aβ oligomer formation and also promotes the formation of nontoxic, nonamyloid amorphous aggregates, which are more sensitive to protease digestion. Finally, this segment also inhibits seeding of Aβ catalyzed by Aβ fibrils extracted from the brain of an Alzheimer's patient. Together, these findings suggest that mimicking the inhibitory effect of TTR with peptide-based therapeutics represents an additional avenue to explore for the treatment of Alzheimer's disease.

scholarly journals Synthetic Seed Production as a Tool for the Conservation and Domestication of Celastrus paniculatus: A Rare Medicinal Plant

2019 ◽  
pp. 1-8
Author(s):  
D. L. C. K. Fonseka ◽  
W. W. U. I. Wickramaarachchi ◽  
R. P. S. Madushani
Keyword(s):  
Sri Lanka ◽  
Medicinal Plant ◽  
Plant Species ◽  
Synthetic Seeds ◽  
Shoot Tips ◽  
Medicinal Plant Species ◽  
Synthetic Seed ◽  
Black Oil ◽  
Celastrus Paniculatus

The black-oil tree (Celastrus paniculatus Willd) is a highly valued medicinal plant species belong to the Celastraceae family, known as Jyothishmathi in Ayurveda and Duhundu in Sri Lanka and grows as a perennial vine. It is an endangered medicinal plant species recorded in the red list of endangered fauna and flora of Sri Lanka in 1999. The seed oil of Celastrus paniculatus contains sesquiterpene alkaloids namely; celapagine, celapanigine, celapanine and celastrol, used in traditional system of medicine for various disorders and because of its high pharmaceutical value, plants are over exploited in natural habitats. Owing to poor seed germination and lack of successful vegetative propagation methods, domestication and commercial planting of this important medicinal plant species to meet the demand seems impossible. Therefore, it is of high importance to develop a reliable and efficient in vitro propagation to produce black oil plants for commercial use. In this study, it was attempted to produce synthetic seeds of Celestrus paniculatus via in vitro multiple shoot proliferation. Nodal segment explants were collected from freshly emerged age of sprouts, surface sterilized and cultured in Murashige and Skoog medium supplemented with different 6-benzylaminopurine (BAP) and Thidiazuron (TDZ) concentrations for shoot induction. The highest soot proliferation rate; 25 shoot tips/explant were observed with 0.1 mg/L TDZ. Induced shoot tips were used for synthetic seed production after encapsulating with BAP and a-naphthalene acetic (NAA) enriched sodium alginate. Shoot tip encapsulated beads produced with 4% sodium alginate were firm, clear, round and uniform in size and easy to handle. The influence of growth regulators (BAP and NAA) and storage period on the germination of encapsulated shoot tips was studied to evaluate the success of encapsulated shoot tips as a propagule. The beads germinated with 2 mg/L BAP and 0.2 mg/L NAA provided 80% in vitro germination percentage. Shoot tips of synthetic seeds remained green and healthy after storage at 5°C for a period of 8 weeks. Current findings suggest that encapsulated micro shoots (synthetic seeds) could be produced successfully, as the first step in domestication and conservation of Celastrus paniculatus. Further studies required on rooting of micro shoots, acclimatization and transferring of plantlets produced from synthetic seeds to in vivo conditions for domestication and conservation purposes.

Study on the Application of a Novel Nano-Curcumin Drug for Alzheimer’s Disease

2021 ◽  
Vol 11 (3) ◽  
pp. 445-452
Author(s):  
Liu Yang ◽  
Xin Sun ◽  
Jun Huang ◽  
Shimiao Zhu ◽  
Yan Li
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Particle Size ◽  
Polyethylene Glycol ◽  
Inhibitory Effect ◽  
Memory Decline ◽  
Impaired Cognitive Function ◽  
Particle Size Analyzer ◽  
Mental Symptoms

Alzheimer’s disease (AD) is a neurodegenerative disease hallmarked by impaired cognitive function and memory decline; it is accompanied by a variety of mental symptoms and behavioral disorders. This disease has a serious impact on society, families, and the afflicted patients. Curcumin (Cur) nanoparticles were preparation by modifying curcumin with polyethylene glycol-polylactic acid (PEG-PLA) amphiphilic block copolymer. The resulting nanodrug can successfully penetrate the blood brain barrier (BBB) and concentrate in the main pathological areas of AD. As measured with a Zeta particle size analyzer, the particle size of PEG-PLA/Cur was 100 ± 0.53 nm, and it was electrically neutral. In vitro experiments revealed that PEG-PLA/Cur successfully penetrated the membrane of PC12 cells and inhibited proliferation. PEG-PLA/Cur also exhibited an inhibitory effect on the production of amyloid β protein (Aβ fiber) and depolymerization activity on Aβ fiber aggregates. PEG-PLA/Cur represents a novel nanodrug with the potential to treat AD.

scholarly journals Micropropagation, seed propagation and germplasm bank of Mandevilla velutina (Mart.) Woodson

2007 ◽  
Vol 64 (3) ◽  
pp. 263-268 ◽  
Author(s):  
Ronaldo Biondo ◽  
Ana Valéria Souza ◽  
Bianca Waléria Bertoni ◽  
Andreimar Martins Soares ◽  
Suzelei Castro França ◽  
...  
Keyword(s):  
Medicinal Plant ◽  
Plant Species ◽  
In Vitro Propagation ◽  
Nodal Segments ◽  
Medicinal Plant Species ◽  
Soil Conditions ◽  
Ms Medium ◽  
Germplasm Bank ◽  
Seed Propagation

Mandevilla velutina (Mart.) Woodson (Apocynaceae) is a medicinal plant species with antivenom properties, native from Brazilian Savanna regions (Cerrado), which due to overexploitation and habitat deforestation is in danger of extinction. As an initiative for conserving this endangered but economically important plant species, a micropropagation protocol was developed and genotypes were stored in the Germplasm Bank "Cerrado In vitro". For the in vitro propagation of M. velutina, nodal segments were inoculated on Murashige and Skoog (MS) medium supplemented with different concentrations of BA, Zeatin, 2ip, DTT and TDZ. Best multiplication ratio was achieved when to the medium 0.44 µM BA, ranging 1: 6.7, were added. Plantlets cultured on MS/2 medium supplemented with 26.85 µM NAA rooted successfully (50.5%). Although rooted and un-rooted plantlets acclimatized to soil conditions, great losses were observed within un-rooted plantlets, while the rooted presented 100 % survival. It was possible to maintain 43% of the M. velutina germplasm under healthy conditions for six months, with no subcultures, using the MS medium supplemented with 2% sucrose, 13.8 mM spermidine, 2% sorbitol and 2% dextrose.

In vitro Micropropagation of a Medicinal Plant Species Sophora flavescens

2003 ◽  
Vol 46 (1) ◽  
pp. 117-120 ◽  
Author(s):  
D.L. Zhao ◽  
G.Q. Guo ◽  
X.Y. Wang ◽  
G.C. Zheng
Keyword(s):  
Medicinal Plant ◽  
Plant Species ◽  
Medicinal Plant Species ◽  
Sophora Flavescens ◽  
In Vitro Micropropagation

In-silico study of some natural plant phyto-compounds for the identification of novel potent cholinesterase inhibitors against Alzheimer's Disease

2021 ◽  
Vol 12 (3) ◽  
pp. 243-250
Author(s):  
Dhiraj Kumar ◽  
Sanjana Bhagat
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Binding Affinity ◽  
In Silico ◽  
Docking Study ◽  
Inhibitory Effect ◽  
Ache Inhibitor ◽  
Strong Binding ◽  
In Silico Studies ◽  
Autodock 4.0

The main aim of this study is to identify inhibitory binding potent of the available commercially alkaloids, against the crystal structure of acetylcholinesterase (AChE) protein by in silico studies. The inhibitory data of the compounds should be compared with the internal ligand as well as standard AChE inhibitor Aricept (which is used for the treatment of all stages of Alzheimer’s disease). AutoDock 4.0 is used for the docking study, conformational orientation site analysis, and, with the help of docking, we have calculated parameters like binding energy and inhibition constant. Docking's study showed that Glabridin, Isorosmanol, Quercetin, Honokiol, Eckol, Sargaquinoic acid, and Ginsedosides revealed strong binding affinity with the enzyme. Moreover, The ADMET profiling and physicochemical properties of the selected compounds are evaluated using the Molinspiration and Data warrior software. By showing a strong binding affinity value, positive bioactivity score, and good pharmacokinetic properties, the top compound was determined. After evaluation with all parameters, the compound Glabridin and Ginsedosides show the most potent inhibitory effect towards the acetylcholinesterase, so this compound could be used as a novel is required to treat Alzheimer's disease.

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