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 Phytochemical screening and In-vitro antioxidant activity of Centella asiatica extracts

2017 ◽  
Vol 9 (4) ◽  
pp. 615
Author(s):  
Mukesh Kumar Yadav ◽  
Santosh Kumar Singh ◽  
JS Tripathi ◽  
YB Tripathi
Keyword(s):  
Hydrogen Peroxide ◽  
Antioxidant Activity ◽  
Free Radical ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Centella Asiatica ◽  
Free Radical Scavenging ◽  
Scavenging Activity ◽  
Phytochemical Screening

<p><em>Centella asiatica</em> also known as <em>mandukparni </em>or Indian pennywort or <em>jalbrahmi</em>, which has been used as a medicine in the Ayurveda from ancient times and mentioned in many classical texts of Ayurveda. <em>Centella asiatica</em> has long been used to improve memory and cognitive function.</p><p>The study aimed to identify the phytochemicals present in different solvent extracts of <em>Centella asiatica </em>(i.e. PECA- Petroleum ether extract of <em>C. asiatica, </em>CCA- Chloroform extract of <em>C. asiatica, </em>EACA- Ethyl acetate extract of <em>C. asiatica,</em> ECA- Ethanolic extract of <em>C. asiatica, </em>HACA- Hydro-alcoholic extract of <em>C. asiatica</em>)<em> </em>and evaluate the respective in-vitro antioxidant potentials. <em></em></p><p>The phytochemical screening of extracts was done with standardized procedures and the antioxidant potential of different solvent extracts of <em>Centella asiatica</em> was assessed by its free radical scavenging activity 2, 2-diphenyl -1- picrylhydrazyl (DPPH) as well as hydrogen peroxide scavenging assay respectively for reducing capability.</p><p>In all different solvent extracts of <em>C. asiatica</em> revealed excellent free radical scavenging activity as revealed by 2-2- diphenyl-1-picryl-hydrazyl (DPPH) assay with  EC<sub>50</sub> values for ECA=128.752±1.85 μg/ml, HACA=274.884±1.21 μg/ml and hydrogen peroxide assay against the standard (Butylated hydroxytoluene) BHT, with the EC<sub>50</sub> values ECA=429.69±0.92 μg/ml HACA=458.08±0.58 μg/ml while rest solvent extracts shown very less antioxidant activity.</p><p> The present study indicates that the <em>Centella asiatica</em> extracts have good antioxidant activity which can be used in stress and anxiety and also a good source to be used as natural drugs.</p>

scholarly journals Design and synthesis of multi-target directed 1,2,3-triazole-dimethylaminoacryloyl-chromenone derivatives with potential use in Alzheimer's disease

BMC Chemistry ◽  
2020 ◽  
Vol 14 (1) ◽  
Author(s):  
Hajar Karimi Askarani ◽  
Aida Iraji ◽  
Arezoo Rastegari ◽  
Syed Nasir Abbas Bukhari ◽  
Omidreza Firuzi ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Biological Activities ◽  
Neuroprotective Effects ◽  
Design And Synthesis ◽  
Catalytic Active Site ◽  
Aβ Aggregation ◽  
Multifunctional Agents ◽  
Potential Use

Abstract To discover multifunctional agents for the treatment of Alzheimer's disease (AD), a new series of 1,2,3-triazole-chromenone derivatives were designed and synthesized based on the multi target-directed ligands approach. The in vitro biological activities included acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition as well as anti-Aβ aggregation, neuroprotective effects, and metal-chelating properties. The results indicated a highly selective BuChE inhibitory activity with an IC50 value of 21.71 μM for compound 10h as the most potent compound. Besides, compound 10h could inhibit self-induced Aβ1–42 aggregation and AChE-induced Aβ aggregation with 32.6% and 29.4% inhibition values, respectively. The Lineweaver–Burk plot and molecular modeling study showed that compound 10h targeted both the catalytic active site (CAS) and peripheral anionic site (PAS) of BuChE. It should be noted that compound 10h was able to chelate biometals. Thus, the designed scaffold could be considered as multifunctional agents in AD drug discovery developments.

scholarly journals Antioxidant & analgesic activities of leaves of Panlata (Derris trifoliate): In vitro investigation

2012 ◽  
Vol 1 (2) ◽  
Author(s):  
Md Raihan Sarkar ◽  
Moynul Hasan ◽  
Md Sariful Islam Howlader ◽  
Mohammad Saydur Rahman ◽  
Shubhra Kanti Dey
Keyword(s):  
Free Radical ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Free Radical Scavenging Activity ◽  
Scavenging Activity ◽  
Immersion Method ◽  
Standard Drug ◽  
In Vitro Investigation

In the present study, the antioxidant and analgesic potential of the ethanolic extract of the leaves of Derris trifoliata was evaluated. The free radical scavenging activity of the crude extract on the stable radical 1, 1-diphenyl-2-picrylhydrazyl (DPPH) was determined by comparing the DPPH inhibitory capacity of the extract. In the quantitative assay, Derris trifoliata extract displayed a free radical scavenging activity in the DPPH assay (IC50 = 19 ?g/ml) which is comparable to that of ascorbic acid (IC50 = 7.80 ?g/ml), a well-known standard antioxidant. The analgesic responses of the given samples of extracts were evaluated using the Tail immersion method. In the analgesic activity test, extract at dose of 200 mg/kg and 400 mg/kg exhibited significant (P<0.05 and P<0.001 respectively) inhibition of pain by 166.82 and 184.95 after 120 and 180 minutes respectively while the standard drug Diclofenac Na inhibition was found to be 217.67 after 180 minutes at a dose of 25 mg/kg body weight DOI: http://dx.doi.org/10.3329/ijpls.v1i2.12951 International Journal of Pharmaceutical and Life Sciences Vol.1(2) 2012

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