scholarly journals Isolation and Cholinesterase Inhibitory Activity of Narcissus Extracts and Amaryllidaceae Alkaloid

2013 ◽  
Vol 8 (6) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Lucie Cahlíková ◽  
Miroslav Ločárek ◽  
Nina Benešová ◽  
Radim Kučera ◽  
Jakub Chlebek ◽  
...  
Keyword(s):  
Biological Activity ◽  
Inhibitory Activity ◽  
Mass Spectra ◽  
Dependent Manner ◽  
Inhibition Activity ◽  
Narcissus Poeticus ◽  
Cholinesterase Inhibitory Activity ◽  
Alkaloid Extracts ◽  
Dose Dependent ◽  
Retention Indexes

Alkaloid extracts of eleven Narcissus (Amaryllidaceae) species and varieties were studied with respect to their acetylcholinesterase (HuAChE) and butyrylcholinesterase (HuBuChE) inhibitory activity and alkaloid patterns. Forty-two alkaloids were determined by GC/MS, and thirty of them identified from their mass spectra, retention times and retention indexes. Promising HuAChE inhibition activity was demonstrated by nine Narcissus taxa and HuBuChE inhibition by Narcissus poeticus cv. Pink Parasol with an IC50 value of 3.3 ± 0.5 μg/mL. The alkaloid identified as (11C- S)-homolycorine was isolated in pure form from Narcissus Sir W. Churchill using preparative TLC and was tested for its biological activity. Homolycorine inhibited HuAChE and HuBuChE in a dose-dependent manner with IC50 values of 63.7±4.3 μM and 151.0±15.2 μM, respectively.

scholarly journals Chemical Composition of Bioactive Alkaloid Extracts from Some Narcissus Species and Varieties and their Biological Activity

2014 ◽  
Vol 9 (8) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Jana Havlasová ◽  
Marcela Šafratová ◽  
Tomáš Siatka ◽  
Šárka Štěpánková ◽  
Zdeněk Novák ◽  
...  
Keyword(s):  
Biological Activity ◽  
Chemical Composition ◽  
Inhibitory Activity ◽  
Mass Spectra ◽  
Pure Form ◽  
Inhibition Activity ◽  
Prolyl Oligopeptidase ◽  
Alkaloid Extracts ◽  
Retention Indexes

Alkaloid extracts of eight Narcissus (Amaryllidaceae) species and varieties were studied with respect to their acetylcholinesterase (HuAChE) and butyrylcholinesterase (HuBuChE) inhibitory activity and alkaloid patterns. Thirty alkaloids were determined by GC/MS, and twenty-five of them identified from their mass spectra, retention times and retention indexes. Promising HuAChE inhibition activity was demonstrated by six Narcissus taxa and HuBuChE inhibition by N. jonquila cv. Double Campernelle and N. nanus cv. Elka with IC50 values of 24.1 ± 1.9 μg/mL and 25.1 ± 1.8 μg/mL, respectively. Two alkaloids were isolated in pure form using preparative TLC and identified as the galanthamine type alkaloid narwedine and the lycorine type alkaloid incartine. Both compounds were tested for their biological activity. They were considered inactive in HuAChE/HuBuChE assays, but showed promising prolyl oligopeptidase inhibition activities with IC50 values of 0.95 ± 0.12 mM and 0.91 ± 0.09 mM, respectively.

scholarly journals Alkaloids from Some Amaryllidaceae Species and Their Cholinesterase Activity

2012 ◽  
Vol 7 (5) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Lucie Cahlíková ◽  
Nina Benešová ◽  
Kateřina Macáková ◽  
Radim Kučerac ◽  
Václav Hrstka ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Mass Spectra ◽  
Cholinesterase Activity ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Ms Analysis ◽  
Phytochemical Investigation ◽  
Narcissus Poeticus ◽  
Alkaloid Extracts ◽  
Potent Inhibitory Activity

Alkaloid extracts of four Amaryllidaceae species were studied with respect to their acetylcholinesterase and butyrylcholinesterase inhibitory activity and alkaloid patterns. Twenty-one alkaloids were determined by GC/MS, and seventeen of them identified from their mass spectra and retention times. The GC/MS analysis of the alkaloid extract of Nerine filamentosa is the first phytochemical investigation of this species. Promising erythrocytic acetylcholinesterase inhibitory activity was demonstrated by the alkaloid extracts of Narcissus poeticus var recurvus, Nerine filifolia and N. filamentosa (IC50,HuAChE = 6.0 ± 0.1 μg/mL; IC50,HuAChE = 18.5 ± 0.8 μg/mL, IC50,HuAChE = 21.6 ± 1.1 μg/mL). The most potent inhibitory activity against serum butyrylcholinesterase was shown by extracts of Sternbergia lutea and Nerine filamentosa (IC50,HuBuChE = 3.7 ± 0.1 μg/mL; IC50,HuBuChE = 13.0 ± 0.7 μg/mL).

scholarly journals Comparison of Different Methods for Extracting the Astaxanthin from Haematococcus pluvialis: Chemical Composition and Biological Activity

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3569
Author(s):  
Yicheng Tan ◽  
Zhang Ye ◽  
Mansheng Wang ◽  
Muhammad Faisal Manzoor ◽  
Rana Muhammad Aadil ◽  
...  
Keyword(s):  
High Pressure ◽  
Biological Activity ◽  
Chemical Composition ◽  
Haematococcus Pluvialis ◽  
Activity Analysis ◽  
Cell Disruption ◽  
Dependent Manner ◽  
Dpph Activity ◽  
The Impact ◽  
Dose Dependent

In this study, the impact of different cell disruption techniques (high-pressure micro fluidization (HPMF), ionic liquids (ILs), multi-enzyme (ME), and hydrochloric acid (HCl)) on the chemical composition and biological activity of astaxanthin (AST) obtained from Haematococcus pluvialis was investigated. Results indicated that all cell disruption techniques had a significant effect on AST composition, which were confirmed by TLC and UPC2 analysis. AST recovery from HCl (HCl-AST) and ILs (ILs-AST) cell disruption techniques was dominant by free and monoesters AST, while AST recovery from HPMF (HPMF-AST) and ME (ME-AST) cell disruption techniques was composed of monoesters, diesters, and free AST. Further biological activity analysis displayed that HCl-AST showed the highest ABTS and DPPH activity, while ILs-AST showed better results against the ORAC assay. Additionally, ILs-AST exhibits a stronger anti-proliferation of HepG2 cells in a dose-dependent manner, which was ascribed to AST-induced ROS in to inhibit the proliferative of cancer cells.

Human MutT Homolog 1 (MTH1) Inhibitor Reduces the Biological Activity of Ovarian Carcinoma Cells

2022 ◽  
Vol 12 (5) ◽  
pp. 907-913
Author(s):  
Liyan Zhong ◽  
Yi Yi ◽  
Qian Liu ◽  
Yan Peng
Keyword(s):  
Biological Activity ◽  
Ovarian Carcinoma ◽  
Biological Activities ◽  
Carcinoma Cells ◽  
Dependent Manner ◽  
Ovarian Carcinoma Cells ◽  
Proliferative Rate ◽  
Skov3 Cells ◽  
Significant Difference ◽  
Dose Dependent

This study intends to discuss the mechanism of MTH1 inhibitor (TH588) in the biological activity of ovarian carcinoma cells. A2780 and SKOV-3 cells were treated with different concentrations of TH588 and assigned into AT group (control), BT group (8 μmol/L TH588), CT group (16 μmol/L), DT group (32 μmol/L), ET group (64 μmol/L) and FT group (128 μmol/L) followed by measuring level of Bcl-2 and Bax by Western blot and PCR, and cell biological activities by MTT, FCM and Transwell chamber assay. The cell proliferative rate was not affected in AT group, but was lower in other groups in a reverse dose-dependent manner. There was significant difference on apoptotic rate and cell invasion among groups with increased apoptosis and reduce invasion after TH588 treatment. FT group showed lowest expression of Bcl-2 and Bax compared to other groups. In conclusion, the biological activity of A2780/SKOV3 cells could be reduced by MTH1 inhibitor which was probably through regulation of Bax and Bcl-2 expression.

scholarly journals Acetylcholinesterase and Butyrylcholinesterase Inhibitory Compounds from Corydalis Cava (Fumariaceae)

2011 ◽  
Vol 6 (5) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Jakub Chlebek ◽  
Kateřina Macáková ◽  
Lucie Cahlíková ◽  
Milan Kurfürst ◽  
Jiří Kuneš ◽  
...  
Keyword(s):  
Human Blood ◽  
Inhibitory Activity ◽  
Potent Inhibitor ◽  
The Other ◽  
Spectroscopic Techniques ◽  
Dependent Manner ◽  
Isoquinoline Alkaloids ◽  
Chemical Structures ◽  
Inhibitory Compounds ◽  
Dose Dependent

Tubers of Corydalis cava were extracted with ethanol and fractionated using n-hexane, chloroform and ethanol. Repeated column chromatography, preparative TLC and crystallization led to the isolation of fifteen isoquinoline alkaloids. The chemical structures of the isolated compounds were determined on the basis of spectroscopic techniques and by comparison with literature data. All isolated compounds were tested for human blood acetylcholinesterase (HuAChE) and human plasma butyrylcholinesterase (HuBuChE) inhibitory activity. (+)-Canadaline inhibited acetylcholinesterase as well as butyrylcholinesterase in a dose-dependent manner with IC50 values of 20.1 ± 1.1 μM and 85.2 ± 3.2 μM, respectively. (+)-Canadine, with an IC50 value of 12.4 ± 0.9 μM, was the most potent inhibitor of acetylcholinesterase, whilst (±)-corycavidine and (+)-bulbocapnine were effective inhibitors of butyrylcholinesterase with IC50 values of 46.2 ± 2.4 uM and 67.0 ± 2.1 μM, respectively. The other isolated alkaloids were considered inactive (IC50 > 100 μM).

scholarly journals Acetylcholinesterase and Butyrylcholinesterase Inhibitory Compounds from Chelidonium Majus (Papaveraceae)

2010 ◽  
Vol 5 (11) ◽  
pp. 1934578X1000501 ◽  
Author(s):  
Lucie Cahlíková ◽  
Lubomír Opletal ◽  
Milan Kurfürst ◽  
Kateřina Macáková ◽  
Andrea Kulhánková ◽  
...  
Keyword(s):  
Human Plasma ◽  
Human Blood ◽  
Inhibitory Activity ◽  
Dependent Manner ◽  
Isoquinoline Alkaloids ◽  
Chelidonium Majus ◽  
Aerial Parts ◽  
Naturally Occurring ◽  
Inhibitory Compounds ◽  
Dose Dependent

The roots and aerial parts of Chelidonium majus L. were extracted with EtOH and fractionated using CHCl3 and EtOH. Repeated column chromatography, preparative TLC and crystallization led to the isolation of five isoquinoline alkaloids, stylopine (3), chelidonine (4), homochelidonine (5), protopine (6), and allocryptopine (7), along with two isolation artifacts 6-ethoxydihydrosanguinarine (1) and 6-ethoxydihydrochelerythrine (2). All isolated compounds were tested for human blood acetylcholinesterase (HuAChE) and human plasma butyrylcholinesterase (HuBuChE) inhibitory activity. The isolation artifacts exhibited the highest activity against HuAChE and HuBuChE with IC50 values of 0.83 ± 0.04 μM and 4.20 ± 0.19 μM for 6-ethoxydihydrochelerythrine and 3.25 ± 0.24 μM and 4.51 ± 0.31 μM for 6-ethoxydihydrosanguinarine. The most active of the naturally-occurring alkaloids was chelidonine, which inhibited both HuAChE and HuBuChE in a dose-dependent manner with IC50 values of 26.8 ± 1.2 μM and 31.9 ± 1.4 μM, respectively.

scholarly journals Chemical Constituents of Blumea balsamifera of Indonesia and Their Protein Tyrosine Phosphatase 1B Inhibitory Activity

2012 ◽  
Vol 7 (7) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Azis Saifudin ◽  
Ken Tanaka ◽  
Shigetoshi Kadota ◽  
Yasuhiro Tezuka
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Inhibitory Activity ◽  
Methanol Extract ◽  
Chemical Constituents ◽  
Tyrosine Phosphatase ◽  
Spectroscopic Methods ◽  
Protein Tyrosine Phosphatase 1B ◽  
Dependent Manner ◽  
Protein Tyrosine ◽  
Dose Dependent

A methanol extract of the leaves of Blumea balsamifera (L.) DC. (Asteraceae) afforded a new guaian-type sesquiterpene, epiblumeaene K (1), together with four known guaian-type sesquiterpenes (2–5), three known sesquiterpenes (6–8), and nine known flavonoids (9–17) by a combination of chromatography and preparative TLC techniques. Their structures were elucidated by extensive spectroscopic methods and comparison with the literature data. Among the isolated compounds, a known sesquiterpene, β-caryophyllene 8 R,9 R-oxide (6), exhibited a significant PTP1B inhibitory activity in a dose-dependent manner, with an IC50 value of 25.8μM (5.62μg/mL).

In vitro anti-diabetic activity of Tribulus terrestrisL. fruits extracts

2019 ◽  
Vol 50 (4) ◽  
pp. 631-640
Author(s):  
Kholowd AlKhaldi ◽  
Manal Daghestani ◽  
Thanaa Al-Haddad
Keyword(s):  
Acetone Extract ◽  
Hexane Extract ◽  
Tribulus Terrestris ◽  
Dependent Manner ◽  
Inhibition Activity ◽  
Content Type ◽  
Significant Difference ◽  
Ethanol Extracts ◽  
Dose Dependent

Purpose The purpose of this paper is to evaluate the inhibition activity of Tribulus terrestris L. (T. terrestris) fruits extracts with solvents of increasing polarity against α-glucosidase and α-amylase, and to determine the inhibition mode of the most effective extract against both enzymes. Design/methodology/approach Hexane, acetone, ethanol and aqueous extracts of T. terrestris fruits were prepared using ultrasonic sequential extraction and analyzed for their α-amylase and α-glucosidase inhibitory activities by specific assay for each enzyme. The modes of inhibitions were detected using Lineweaver–Burk plots. Findings T. terrestris fruits extracts showed inhibition activity against α-glucosidase and α-amylase which was in the dose-dependent manner. Hexane extract had the highest α-glucosidase inhibition activity (IC50 = 27.28 μg/ml, p = 0.003), followed by acetone and ethanol extracts (IC50 = 60.58 μg/ml and IC50 = 84.21 μg/ml, respectively). The inhibition mode of hexane extract was noncompetitive. While acetone extract showed the highest inhibition activity against α-amylase (IC50 = 6.18 mg/ml, p = 0.002), hexane and ethanol extracts showed no significant difference (IC50 = 13.04 mg/ml and IC50 = 14.20 mg/ml, respectively, p = 0.09). The inhibition mode of acetone extract was competitive. Originality/value T. terrestris fruits extracts had strong inhibition activity against α-glucosidase and α-amylase, and they can be used as a promising anti-diabetic agent.

scholarly journals Tea Polyphenols EGCG and Theaflavin Inhibit the Activity of SARS-CoV-2 3CL-Protease In Vitro

2020 ◽  
Vol 2020 ◽  
pp. 1-7 ◽  
Author(s):  
Minsu Jang ◽  
Yea-In Park ◽  
Yeo-Eun Cha ◽  
Rackhyun Park ◽  
Sim Namkoong ◽  
...  
Keyword(s):  
Effective Treatment ◽  
Green Tea ◽  
Inhibitory Activity ◽  
Inhibitory Concentration ◽  
Black Tea ◽  
Dependent Manner ◽  
Global Pandemic ◽  
3Cl Protease ◽  
Dose Dependent

COVID-19, a global pandemic, has caused over 750,000 deaths worldwide as of August 2020. A vaccine or remedy for SARS-CoV-2, the virus responsible for COVID-19, is necessary to slow down the spread and lethality of COVID-19. However, there is currently no effective treatment available against SARS-CoV-2. In this report, we demonstrated that EGCG and theaflavin, the main active ingredients of green tea and black tea, respectively, are potentially effective to inhibit SARS-CoV-2 activity. Coronaviruses require the 3CL-protease for the cleavage of its polyprotein to make individual proteins functional. EGCG and theaflavin showed inhibitory activity against the SARS-CoV-2 3CL-protease in a dose-dependent manner, and the half inhibitory concentration (IC50) was 7.58 μg/ml for EGCG and 8.44 μg/ml for theaflavin. In addition, we did not observe any cytotoxicity for either EGCG or theaflavin at the concentrations tested up to 40 μg/ml in HEK293T cells. These results suggest that upon further study, EGCG and theaflavin can be potentially useful to treat COVID-19.

Oroxylin A Shows Protective Effects on Biological Activity of Lipopolysaccharide Treated Human Periodontal Ligament Stem Cells

2019 ◽  
Vol 9 (10) ◽  
pp. 1362-1368
Author(s):  
Ting Wang ◽  
Xinqiang Liu ◽  
Chunmiao Jiang ◽  
Dapeng Ren ◽  
Yuli Gao ◽  
...  
Keyword(s):  
Stem Cells ◽  
Cell Proliferation ◽  
Biological Activity ◽  
Periodontal Ligament ◽  
Time Dependent ◽  
Dependent Manner ◽  
Protective Effects ◽  
Oroxylin A ◽  
Periodontal Ligament Stem Cells ◽  
Dose Dependent

The abnormal proliferation and apoptosis of human periodontal ligament stem cells (hPDLSCs) serves a crucial role in the development of periodontitis. Oroxylin A has shown protective effects in a variety of inflammatory diseases. The present study was aimed to investigate the effects of oroxylin A on lipopolysaccharide (LPS) treated hPDLSCs. In the present study, cells were exposed to different concentrations (10, 20, 40 uM) of oroxylin A for 24 h or 48 h, co-treated with LPS. The cell proliferation capacity was assessed using cell counting kit-8 (CCK-8), and the cell apoptosis was evaluated by flow cytometry. The Ki67 expression was measured using immunofluorescence and NO production was detected by enzyme linked immunosorbent assay (ELISA) respectively. Western blot analyses were used to investigate the level of cell proliferation related proteins (PCNA, CDK2 and p21) as well as NF-κB, I-κBα and downstream molecules iNOS, IL-6 and TNF-α. The results demonstrated that oroxylin A increased cell survival of LPS treated hPDLSCs in a dose-dependent and time-dependent manner. In addition, oroxylin A treatment inhibited cell apoptosis in hPDLSCs. Furthermore, the levels of NO, NF-κB, iNOS, IL-6 and TNF-α were significantly reduced. And the expression of Ki67, I-κBα, PCNA and CDK2 were significantly increased. Taken together, these findings indicate that oroxylin A promote proliferation and suppress apoptosis in a dose-dependent and time-dependent manner. Oroxylin A may affects LPS induced biological activity via inhibiting NF-κB activation and proinflammatory cytokines expression in hPDLSCs.

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