Psychotria leiocarpa Extract and Vincosamide Reduce Chemically-Induced Inflammation in Mice and Inhibit the Acetylcholinesterase Activity

Formagio, Anelise Samara Nazari; Volobuff, Carla Roberta Ferreira; Kassuya, Cândida Aparecida Leite; Cardoso, Cláudia Andréa Lima; Vieira, Maria do Carmo; Pereira, Zefa Valdevina; Bagatin, Mariane Cristovão; Gauze, Gisele F.

doi:10.1007/s10753-019-01018-w

Cited by 15 publications

(11 citation statements)

References 49 publications

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“…The theoretical chemistry bases on two strong physicochemical phenomena; these are quantum mechanics (QM) and molecular dynamics (MD). The subatomic particle (protons, electrons, and neutrons) interactions form the drawback of quantum chemistry that also describes the molecular properties depending on subatomic interactions (13,12). The molecular dynamic theory is based on the spatial conformation of molecule interaction from their active sites by intermolecular interactions like weak Van der Waals interactions or hydrogen bonding.…”

Section: Methodsmentioning

confidence: 99%

Identification of Potent COVID-19 Main Protease (Mpro) Inhibitors from Natural Polyphenols: An in Silico Strategy Unveils a Hope against CORONA

Adem¹,

Eyupoglu²,

Sarfraz³

et al. 2020

Preprint

175

169

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COVID-19, a rapidly spreading new strain of coronavirus, has affected more than 150 countries and received worldwide attention. The lack of efficacious drugs or vaccines against SARS-CoV-2 has further worsened the situation. Thus, there is an urgent need to boost up research for the development of effective therapeutics and affordable diagnostic against COVID-19. The crystallized form of SARS-CoV-2 main protease (Mpro) was demonstrated by a Chinese researcher Liu et al. (2020) which is a novel therapeutic drug target. This study was conducted to evaluate the efficacy of medicinal plant-based bioactive compounds against COVID-19 Mpro by molecular docking study. Molecular docking investigations were performed by using Molegro Virtual Docker 7 to analyze the inhibition probability of these compounds against COVID-19. COVID-19 Mpro was docked with 80 flavonoid compounds and the binding energies were obtained from the docking of (PDB ID: 6LU7: Resolution 2.16 Å) with the native ligand. According to obtained results, hesperidin, rutin, diosmin, apiin, diacetylcurcumin, (E)-1-(2-Hydroxy-4-methoxyphenyl)-3-[3-[(E)-3-(2-hydroxy-4- methoxyphenyl)-3-oxoprop-1-enyl]phenyl]prop-2-en-1-one, and beta,beta'-(4-Methoxy-1,3- phenylene)bis(2'-hydroxy-4',6'-dimethoxyacrylophenone have been found as more effective on COVID-19 than nelfinavir. So, this study will pave a way for doing advanced experimental research to evaluate the real medicinal potential of these compounds to cure COVID-19.

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Section: Methodsmentioning

confidence: 99%

Identification of Potent COVID-19 Main Protease (Mpro) Inhibitors from Natural Polyphenols: An in Silico Strategy Unveils a Hope against CORONA

Adem¹,

Eyupoglu²,

Sarfraz³

et al. 2020

Preprint

175

169

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“…Out of the rejected compounds, 3-dihydrocadambine (546.6 g/mol) and vincosamide (498.5 g/mol) were rejected because their predicted numbers of rigid bonds and max ring size exceeded the threshold. They were included in the library based on their reported bioactivities from the literature search or previous studies [4,36,37]. Therefore, a total of 85 Uncaria alkaloids were used in the following target prediction.…”

Section: The In-house Library Of Uncaria Alkaloids and Drug-likeness mentioning

confidence: 99%

A Network-Based Approach to Explore the Mechanisms of Uncaria Alkaloids in Treating Hypertension and Alleviating Alzheimer’s Disease

Zhang

et al. 2020

IJMS

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Uncaria alkaloids are the major bioactive chemicals found in the Uncaria genus, which have a long history of clinical application in treating cardiovascular and mental diseases in traditional Chinese medicine (TCM). However, there are gaps in understanding the multiple targets, pathways, and biological activities of Uncaria alkaloids. By constructing the interactions among drug-targets-diseases, network pharmacology provides a systemic methodology and a novel perspective to present the intricate connections among drugs, potential targets, and related pathways. It is a valuable tool for studying TCM drugs with multiple indications, and how these multi-indication drugs are affected by complex interactions in the biological system. To better understand the mechanisms and targets of Uncaria alkaloids, we built an integrated analytical platform based on network pharmacology, including target prediction, protein–protein interaction (PPI) network, topology analysis, gene enrichment analysis, and molecular docking. Using this platform, we revealed the underlying mechanisms of Uncaria alkaloids’ anti-hypertensive effects and explored the possible application of Uncaria alkaloids in preventing Alzheimer’s disease. These results were further evaluated and refined using biological experiments. Our study provides a novel strategy for understanding the holistic pharmacology of TCM, as well as for exploring the multi-indication properties of TCM beyond its traditional applications.

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“…Many plant extracts demonstrate acetylcholinesterase activity, for example, extract from Crinum jagus containing Amaryllidaceae and isoquinolinone alkaloids [6], Cryptocarya species containing isoquinoline alkaloids [10], Narcissus pseudonarcissus L. containing Amarylidaceae alkaloids [7], Catharanthus roseus containing indole alkaloids [9], secophenanthroindolizidine and proaporphine alkaloids from Cryptocarya densiflora Blume [10], Ocotea percoriacea containing benzylisoquinoline, bisbenzylisoquinoline, aporphine, proaporphine, phenanthrene, and morphinane alkaloids [9], Rauvolfia vomitoria containing monoterpene indole alkaloids [11], Crinum jagus containing Amarylidaceae and isoquinoline alkaloids [6], Lycoris longituba containing Amaryllidaceae alkaloid [12], Psychotria leiocarpa containing alkaloid vincosamide [13], Huperzia serrata containing macrocyclic Lycopodium alkaloids [14], Psychotria nemorosa containing azepine-indole alkaloids [15], Uncaria rhynchophylla containing indole alkaloids [16], Berberis vulgaris containing isoquinoline alkaloids [17], Lycopodium platyrhizoma containing Lycopodium alkaloids [18], Huperzia cunninghamioides containing Lycopodium alkaloids [19], Corydalis mucronifera containing isoquinoline alkaloids [20], Palicourea sessilis containing indole alkaloids [21], and Zephyranthes candida containing galanthamine, plicamine, and secoplicamine [22]. There have also been published articles summarizing the application of plant materials containing alkaloids for inhibition of acetylcholinesterase activity [23,24].…”

Section: Introductionmentioning

confidence: 99%

Application of HPLC-DAD for In Vitro Investigation of Acetylcholinesterase Inhibition Activity of Selected Isoquinoline Alkaloids from Sanguinaria canadensis Extracts

Tuzimski

Petruczynik

2021

Molecules

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Isoquinoline alkaloids may have a wide range of pharmacological activities. Some of them have acetylcholinesterase activity inhibition. Nowadays, neurodegenerative disorders such as Alzheimer’s disease have become a serious public health problem. Searching for new effective compounds with inhibited acetylcholinesterase activity is one of the most significant challenges of modern scientific research. The aim of this study was the in vitro investigation of acetylcholinesterase activity inhibition of extracts obtained from Sanguinaria canadensis collected before, during and after flowering. The acetylcholinesterase activity inhibition of these extracts has not been previously tested. The aim was also to quantify selected alkaloids in the investigated extracts by high performance liquid chromatography (HPLC). The analyses of alkaloid content were performed using HPLC in reversed phase (RP) mode using Polar RP column and mobile phase containing acetonitrile, water and ionic liquid (IL). The acetylcholinesterase activity inhibition of the tested plant extracts and respective alkaloid standards were examined using high performance liquid chromatography with diode-array detector (HPLC-DAD) for the quantification of 5-thio-2-nitro-benzoic acid, which is the product of the reaction between the thiocholine (product of the hydrolysis of acetylthiocholine reaction) with Ellman reagent. The application of the HPLC method allowed for elimination of absorption of interfering components, for example, alkaloids such as sanguinarine and berberine. It is revealed that the HPLC method can be successfully used for the evaluation of the acetylcholinesterase inhibitory activity in samples such as plant extracts, especially those containing colored components adsorbing at wavelength in the range 405–412 nm. The acetylcholinesterase inhibition activity synergy of pairs of alkaloid standards and mixture of all investigated alkaloids was also determined. Most investigated alkaloids and all Sanguinaria canadensis extracts exhibited very high acetylcholinesterase activity inhibition. IC50 values obtained for alkaloid standards were from 0.36 for berberine to 23.13 µg/mL for protopine and from 61.24 to 89.14 µg/mL for Sanguinaria canadensis extracts. Our investigations demonstrated that these plant extracts can be recommended for further in vivo experiments to confirm their acetylcholinesterase activity inhibition.

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Psychotria leiocarpa Extract and Vincosamide Reduce Chemically-Induced Inflammation in Mice and Inhibit the Acetylcholinesterase Activity

Cited by 15 publications

References 49 publications

Identification of Potent COVID-19 Main Protease (Mpro) Inhibitors from Natural Polyphenols: An in Silico Strategy Unveils a Hope against CORONA

Identification of Potent COVID-19 Main Protease (Mpro) Inhibitors from Natural Polyphenols: An in Silico Strategy Unveils a Hope against CORONA

A Network-Based Approach to Explore the Mechanisms of Uncaria Alkaloids in Treating Hypertension and Alleviating Alzheimer’s Disease

Application of HPLC-DAD for In Vitro Investigation of Acetylcholinesterase Inhibition Activity of Selected Isoquinoline Alkaloids from Sanguinaria canadensis Extracts

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