scholarly journals Scopoletin: Antiamyloidogenic, Anticholinesterase, and Neuroprotective Potential of a Natural Compound Present in Argyreia speciosa Roots by In Vitro and In Silico Study

2020 ◽  
Vol 15 ◽  
pp. 263310552093769 ◽  
Author(s):  
Priya Kashyap ◽  
Heera Ram ◽  
Sunil Dutt Shukla ◽  
Suresh Kumar

Alzheimer’s disease (AD) is characterized by depositions of amyloid β (Aβ) peptides aggregates resulting in plaques formation in the central nervous system (CNS). This study evaluates the disease-modifying potential of scopoletin against multiple factors associated with AD such as cholinesterase enzymes, Aβ peptides, and neuroprotective properties against Aβ- and H2O2-induced cytotoxicity under in vitro conditions. Scopoletin was identified and quantified using UPLC-QTOF (ultra-high performance liquid chromatography-quadrupole time-of-flight) and high-performance liquid chromatography (HPLC), respectively. The antiamyloidogenic potential was evaluated by thioflavin T and congo red binding assay. Inhibition of key enzymes, that is, acetylcholinesterase and butyrylcholinesterase, was investigated by Ellman’s assay. UPLC-QTOF analysis showed that most abundant phytoconstituent present in Argyreia speciosa hydroalcoholic root extract was scopoletin followed by festuclavine and ergometrine. Scopoletin was further quantified using novel reverse phase (RP)-HPLC method developed in this study. The neuroprotective potential of scopoletin was found to be 69% against Aβ42-induced neurotoxicity and 73% against H2O2-induced cytotoxicity in PC12 cell culture at 40 μM final concentration. At the same concentration, scopoletin inhibited Aβ42 fibril formation up to 57%. The IC50 concentration for AChE and BuChE enzyme inhibition by scopoletin was 5.34 and 9.11 μM, respectively. The antiaggregation and enzyme inhibition results were complemented with strong molecular interactions of scopoletin with target proteins validated by in silico molecular docking analysis. Based on this study, it can be concluded that scopoletin can be used as a lead for amelioration of symptoms and disease-modifying effects in AD.

Plants ◽  
2020 ◽  
Vol 9 (3) ◽  
pp. 388
Author(s):  
Hammad Saleem ◽  
Thet Thet Htar ◽  
Rakesh Naidu ◽  
Sirajudheen Anwar ◽  
Gokhan Zengin ◽  
...  

The plants of the Bougainvillea genus are widely explored regarding nutritive and medicinal purposes. In this study, dichloromethane (DCM) and methanol (MeOH) extracts of Bougainvillea glabra (Choisy.) aerial and flower parts were analyzed for high-performance liquid chromatography with photodiode array detection (HPLC–PDA), ultra-high-performance liquid chromatography–mass spectrometry (UHPLC–MS) phytochemical composition, and enzyme inhibition potential against key enzymes involved in diabetes (α-amylase), skin problems (tyrosinase), and inflammatory disorders (lipoxygenase (LOX)). HPLC–PDA quantification revealed the identification of nine different polyphenolics, amongst which both flower extracts were richest. The flower MeOH extract contained the highest amount of catechin (6.31 μg/g), gallic acid (2.39 μg/g), and rutin (1.26 μg/g). However, none of the quantified compounds were detected in the aerial DCM extract. UHPLC–MS analysis of DCM extracts revealed the tentative identification of 27 secondary metabolites, where the most common belonged to terpenoid, alkaloid, and phenolic derivatives. Similarly, for enzyme inhibition, all the extracts presented moderate activity against tyrosinase and α-amylases, whereas, for LOX, both methanolic extracts showed higher percentage inhibition compared with DCM extracts. Based on our findings, B. glabra could be regarded as a perspective starting material for designing novel pharmaceuticals.


Author(s):  
Mariola Dreger ◽  
Katarzyna Seidler-Łożykowska ◽  
Milena Szalata ◽  
Artur Adamczak ◽  
Karolina Wielgus

AbstractThe purpose of the study was to evaluate Chamerion angustifolium (L.) Holub genotypes for preliminary selection and further breeding programs aimed at obtaining a suitable industrial form for the pharmaceutical applications. Clonally propagated plants representing 10 genotypes of Ch. angustifolium were regenerated under in vitro conditions, hardened and planted in the field. Studies included an evaluation of shoot proliferation, phytochemical assessment of in vitro and ex vitro plants as well as investigations of intraspecies variability regarding four phenological stages: vegetative, beginning of blooming, full blooming, and green fruit phases. Quantitative and qualitative analyses of bioactive compounds were performed using high-performance liquid chromatography coupled with diode array detector and tandem mass spectrometer (HPLC–DAD–MS/MS) and high-performance liquid chromatography (HPLC) methods. The efficiency of shoot multiplication varied between genotypes from 8.12 to 21.48 shoots per explant. A high reproduction rate (> 20 shoots per explant) was recorded for four lines (PL_45, PL_44, PL_58, DE_2). Plants grown in vitro synthesized oenothein B (11.2–22.3 mg g−1 DW) and caffeic acid derivatives. Plants harvested from field contained the full spectrum of polyphenols characteristic for this species, and oenothein B and quercetin 3-O-glucuronide were the most abundant. The maximal content of oenothein B was determined in the vegetative phase of fireweed, while some flavonoids were found in the highest amount in full blooming phase. The results of analysis of variance indicated significant differences among genotypes in oenothein B, 3-O-caffeoylquinic acid and flavonoids accumulation in four phenological phases. PL_44 plants were characterized by high content of oenothein B and quercetin 3-O-glucuronide as well as a relatively high level of other flavonoids. Based on our phytochemical and micropropagation studies, PL_44 genotype was the best candidate for early selection and further breeding programs.


2008 ◽  
Vol 54 (6) ◽  
pp. 501-508 ◽  
Author(s):  
Karina Cogo ◽  
Michelle Franz Montan ◽  
Cristiane de Cássia Bergamaschi ◽  
Eduardo D. Andrade ◽  
Pedro Luiz Rosalen ◽  
...  

The aim of this in vitro study was to evaluate the effects of nicotine, cotinine, and caffeine on the viability of some oral bacterial species. It also evaluated the ability of these bacteria to metabolize those substances. Single-species biofilms of Streptococcus gordonii , Porphyromonas gingivalis , or Fusobacterium nucleatum and dual-species biofilms of S. gordonii – F. nucleatum and F. nucleatum – P. gingivalis were grown on hydroxyapatite discs. Seven species were studied as planktonic cells, including Streptococcus oralis , Streptococcus mitis , Propionibacterium acnes , Actinomyces naeslundii , and the species mentioned above. The viability of planktonic cells and biofilms was analyzed by susceptibility tests and time-kill assays, respectively, against different concentrations of nicotine, cotinine, and caffeine. High-performance liquid chromatography was performed to quantify nicotine, cotinine, and caffeine concentrations in the culture media after the assays. Susceptibility tests and viability assays showed that nicotine, cotinine, and caffeine cannot reduce or stimulate bacterial growth. High-performance liquid chromatography results showed that nicotine, cotinine, and caffeine concentrations were not altered after bacteria exposure. These findings indicate that nicotine, cotinine, and caffeine, in the concentrations used, cannot affect significantly the growth of these oral bacterial strains. Moreover, these species do not seem to metabolize these substances.


2008 ◽  
Vol 74 (6) ◽  
pp. 524-529
Author(s):  
Peter E. Fischer ◽  
Timothy C. Fabian ◽  
Waldemar G. Derijk ◽  
Norma M. Edwards ◽  
Michael Decuypere ◽  
...  

Vascular reconstruction using prosthetic materials in contaminated fields can lead to infection, graft loss, and subsequent amputation. We hypothesized that minocycline and rifampin bound to an ePTFE graft using a unique methacrylate technology would provide for resistance from infection and controlled antibiotic elution. Kirby Bauer susceptibility testing was performed on plates overlaid with Staph aureus (SA) and Staph epidermidis (SE) using 6 mm diameter discs of uncoated graft or antibiotic coated graft (ABX). Zones of inhibition (ZIH) were determined after 24 hours. ABX grafts were then placed in a continuous water bath and a recirculating, pulsatile flow device. Susceptibility testing and high performance liquid chromatography with mass spectroscopy was performed to determine graft performance and antibiotic elution rate. ABX grafts had an average ZIH of 35 mm for SA and 44 mm for SE (each P < 0.0001). After the 1 week water bath, the ZIH of the ABX grafts was 23 mm on both the SA and SE plates. The high performance liquid chromatography with mass spectroscopy revealed that after 24 hours, 50 per cent of the antibiotics remained on the graft, and there was a sustained elution for 7 days. Minocycline and rifampin can be bound to ePTFE vascular grafts using a unique methacrylate method. In vitro, the grafts provide a slow elution of antibiotics that provide resistance from infection by SA and SE for up to 2 weeks after graft insertion.


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