scholarly journals Tacrine, Trolox and Tryptoline as Lead Compounds for the Design and Synthesis of Multi-target Agents for Alzheimer’s Disease Therapy

2017 ◽  
Vol 11 (1) ◽  
pp. 24-37 ◽  
Author(s):  
Gerard A. K. Teponnou ◽  
Jacques Joubert ◽  
Sarel F. Malan
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Free Radical ◽  
Inhibitory Activity ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Linker Chain ◽  
Chain Lengths ◽  
Free Radical Scavenging Activities

The versatile biological activities of tacrine, trolox and β-carboline derivatives make them promising lead structures for the development of multifunctional Alzheimer’s disease (AD) agents. Based on the topology of the active site of cholinesterases and other target proteins involved in the pathogenesis of AD, we have designed and synthesized tacrine-trolox and tacrine-tryptoline hybrids with various linker chain lengths. The hybrids containing the trolox moiety (8a-8d) showed moderate to high TcAChE inhibition (IC50: 17.37 - 2200 nM), eqBuChE inhibition (IC50: 3.16 – 128.82 nM) and free radical scavenging activities (IC50: 11.48 – 49.23 µM). The hybrids with longer linker chain lengths in general showed better ChE inhibitory activity. As expected, free radical scavenging activities were not significantly affected by varying linker chain lengths. The hybrid compound containing the tryptoline moiety linked with a 7 carbon spacer to tacrine (14) displayed the best AChE and BuChE inhibitory activity (IC50 = 17.37 and 3.16 nM). Docking experiments exhibited that compounds 8d and 14 were able to bind to both the CAS and PAS of TcAChE and eqBuChE, suggesting that they will be able to inhibit ChE induced Aβ aggregation. Novel multi-target agents that exhibit good ChE inhibition (8d and 14) and anti-oxidant (8d) activity were identified as suitable candidates for further investigation.

scholarly journals Evaluation of Primary Metabolites and Antioxidant Potential Activity of Cayratia trifolia (Leaf and Stems)

2019 ◽  
Vol 9 (4-A) ◽  
pp. 367-372
Author(s):  
, Anita ◽  
Nakuleshwer Dut Jasuja ◽  
Manas Mahur T
Keyword(s):  
Free Radical ◽  
Secondary Metabolites ◽  
Maximum Concentration ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Ethanolic Extract ◽  
Free Radical Scavenging ◽  
Minimum Concentration ◽  
Cayratia Trifolia ◽  
Free Radical Scavenging Activities

Cayratia trifolia Linn. Domin Syn. Vitis trifolia (Family: Vitaceae) is commonly known as Fox grape in English; Amlabel, Ramchana in Hindi and Amlavetash in Sanskrit. It is native to Asia and Australia. This plant is used for chronic fever, rheumatic, anti-inflammatory etc. In the present study, quantitative analysis and free radical scavenging activities of stem ethanolic extract of Cayratia trifolia was investigated. The extract was found to possess more secondary metabolites and it exhibit radical scavenging activities, Based on the results it can be concluded that, the stem ethanolic extract of Cayratia trifolia which contains high amount of secondary metabolites and exhibits free radical scavenging activities, phytochemistry from leaves and stems using spectral techniques. This research paper provides information mainly on various biological activities like antimitotic, antidiabetic and anti-implantation and several medicinal uses. Biological activities of few of them have been studied maximum concentration of Proteins (58.4mg/gdw) and minimum concentration in total soluble sugar (0.7mg/gdw) and maximum concentration of Lipid peroxidase (5.01mg/gdw) and minimum concentration in FRAP (0.197mg/gdw). Keywords: Cayratia trifolia; Vitaceae; Phytochemistry; Antioxidant.

scholarly journals Screening for some biological activities of cultured cordyceps neovolkiana

2017 ◽  
Vol 20 (K3) ◽  
pp. 106-112
Author(s):  
Chi-Dung Nguyen ◽  
Thu Huynh ◽  
Minh-Hiep Dinh
Keyword(s):  
Free Radical ◽  
Inhibitory Activity ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Proliferation Inhibition ◽  
Etoh Extract ◽  
Toxicity Effect ◽  
Biological Compounds ◽  
Ic50 Values

Cordyceps has been demonstrated to possess a myriad of biological compounds and effects. There are various strains of Cordyceps. In this study, we evaluated some biological activities of cultured Cordyceps neovolkiana extracts. The result exhibited that all C. neovolkiana extracts almost showed no toxicity effect on HepG2 cells at the concentration of 100 μg/ml. Besides, all C. neovolkiana extracts also were not α-glucosidase inhibitory activity at the concentration from 1000 to 8000 μg/ml. However, some extracts had ABTS• free radical scavenging potential with IC50 values between 4129.92 ± 25.12 and 4926.25 ± 41.01 μg/ml. In addition, at 200 μg/ml, the EtOH extract exhibited 64.57 ± 6.30 % (p<0.001) of PBMC proliferation inhibition. In conclusion, these data revealed biological activities of cultured C. neovolkiana, suggesting that further studies would be necessary.

Antioxidant and Free Radical Scavenging Activities of Chitosan Materials

2014 ◽  
Vol 1002 ◽  
pp. 81-90 ◽  
Author(s):  
Qing Xu ◽  
Tian Zhong ◽  
Hui Li Li
Keyword(s):  
Free Radical ◽  
Functional Properties ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Natural Antioxidant ◽  
Biomedical Science ◽  
Antioxidant Ability ◽  
Potential Applications ◽  
Free Radical Scavenging Activities

Chitosan and its derivatives, which are known to possess multiple functional properties, have captured considerable interest due to their biological activities and potential applications in food, pharmaceutical, agricultural and environmental industries. This paper focuses on the antioxidant and free radical scavenging activities of various chitosan materials based on our and others’ latest research results, including scaffold, film, tablet, nanoparticle, and so on. The free radical scavenging mechanisms are summarized. This work may provide more insights into the antioxidant ability of chitosan and its derivatives and potentially enable them to use as natural antioxidant materials for application in food, agriculture, cosmetic and biomedical science.

scholarly journals Claulansine F–Donepezil Hybrids as Anti-Alzheimer’s Disease Agents with Cholinergic, Free-Radical Scavenging, and Neuroprotective Activities

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1303
Author(s):  
Yingda Zang ◽  
Ke Liu ◽  
Weiping Wang ◽  
Chuangjun Li ◽  
Jie Ma ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Free Radical ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Glucose Deprivation ◽  
Free Radical Scavenging ◽  
Neuroprotective Effects ◽  
Catalytic Active Site

The multifactorial nature of Alzheimer’s disease (AD) calls for the development of multitarget agents addressing key pathogenic processes. A total of 26 Claulansine F–donepezil hybrids were designed and synthesized as multitarget drugs. Among these compounds, six compounds exhibited excellent acetylcholinesterase (AChE) inhibitory activity (half maximal inhibitory concentration (IC50) 1.63–4.62 μM). Moreover, (E)-3-(8-(tert-Butyl)-3,3-dimethyl-3,11-dihydropyrano[3,2-a]carbazol-5-yl)-N-((1-(2-chlorobenzyl)piperidin-4-yl)methyl)acrylamide (6bd) exhibited better neuroprotective effects against OGD/R (oxygen–glucose deprivation/reoxygenation) than lead compound Claulansine F. Furthermore, 6bd could cross the blood–brain barrier in vitro. More importantly, compared to edaravone, 6bd had stronger free-radical scavenging activity. Molecular docking studies revealed that 6bd could interact with the catalytic active site of AChE. All of these outstanding in vitro results indicate 6bd as a leading structure worthy of further investigation.

Acetylcholinesterase Inhibitory Potential and Antioxidant Activities of Five Cultivars of Rosa Damascena Mill. From Isparta, Turkey

2020 ◽  
Vol 18 (4) ◽  
pp. 354-359
Author(s):  
Shirin Tarbiat ◽  
Azize Simay Türütoğlu ◽  
Merve Ekingen
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Free Radical ◽  
Neurodegenerative Disorder ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Acetylcholinesterase Activity ◽  
Rosa Damascena ◽  
Free Radical Damage

Alzheimer's disease is a neurodegenerative disorder characterized by memory loss and impairment of language. Alzheimer's disease is strongly associated with oxidative stress and impairment in the cholinergic pathway, which results in decreased levels of acetylcholine in certain areas of the brain. Hence, inhibition of acetylcholinesterase activity has been recognized as an acceptable treatment against Alzheimer's disease. Nature provides an array of bioactive compounds, which may protect against free radical damage and inhibit acetylcholinesterase activity. This study compares the in vitro antioxidant and anticholinesterase activities of hydroalcoholic extracts of five cultivars of Rosa Damascena Mill. petals (R. damascena 'Bulgarica', R. damascena 'Faik', R. damascena 'Iranica', R. damascena 'Complex-635' and R. damascena 'Complex-637') from Isparta, Turkey. The antioxidant activities of the hydroalcoholic extracts were tested for ferric ion reduction and DPPH radical scavenging activities. The anti-acetylcholinesterase activity was also evaluated. All rose cultivars showed a high potency for scavenging free radical and inhibiting acetylcholinesterase activity. There was a significant correlation between antioxidant and acetylcholinesterase inhibitory activity. Among cultivars, Complex-635 showed the highest inhibitory effect with an IC50 value of 3.92 µg/mL. Our results suggest that all these extracts may have the potential to treat Alzheimer's disease with Complex-635 showing more promise.

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.

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