scholarly journals Alkaloids from the Roots and Leaves of Stichoneuron halabalensis and their Acetylcholinesterase Inhibitory Activities

2013 ◽  
Vol 8 (6) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Rosdayati Alino Ramli ◽  
Wilford Lie ◽  
Stephen G. Pyne
Keyword(s):  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Electric Eel ◽  
Inhibitory Activities ◽  
Stemona Alkaloids

A study of the hitherto unreported Stichoneuron halabalensis Inthachub led to the characterization of the known compounds (+)-α-tocopherol and ( R)-(+)-goniothalamin; four known Stemona alkaloids, bisdehydoxystemoninine A (1), stemoninine (2), sessilistemonamine C (3) and sessilistemonamine A (4); and three new alkaloids, stichoneurine C (5), D (6) and E (7). The structures of these compounds were determined on the basis of their spectroscopic data. Alkaloid 7 showed significant inhibitory activity against electric eel acetylcholinesterase (AChE) (IC50 5.90±0.084 μM), while goniothalamin and compounds 1 and 2 showed significant inhibitory activities against human AChE (IC50 7.24±0.52, 5.52±0.13 and 3.74±0.09 μM, respectively).

scholarly journals New Fluorene Derivatives from Dendrobium gibsonii and Their α-Glucosidase Inhibitory Activity

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 4931
Author(s):  
May Thazin Thant ◽  
Nutputsorn Chatsumpun ◽  
Wanwimon Mekboonsonglarp ◽  
Boonchoo Sritularak ◽  
Kittisak Likhitwitayawuid
Keyword(s):  
Kinetic Study ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Enzyme Kinetic ◽  
Whole Plant ◽  
Noncompetitive Inhibitor ◽  
Inhibitory Activities ◽  
New Compounds ◽  
Enzyme Kinetic Study

Two new compounds, dihydrodengibsinin (1) and dendrogibsol (2), were isolated from the whole plant of Dendrobium gibsonii, together with seven known compounds (3–9). The structures of the new compounds were elucidated by their spectroscopic data. All these isolates were evaluated for their α-glucosidase inhibitory activities. Dendrogibsol (2) and lusianthridin (7) showed strong α-glucosidase inhibitory activity when compared with acarbose. An enzyme kinetic study revealed that dendrogibsol (2) is a noncompetitive inhibitor of α-glucosidase.

scholarly journals Characterization of the α-Amylase Inhibitory Activity of Oligomeric Proanthocyanidins from Acacia mearnsii Bark Extract

2016 ◽  
Vol 11 (12) ◽  
pp. 1934578X1601101
Author(s):  
Yosuke Matsuo ◽  
Rie Kusano ◽  
Sosuke Ogawa ◽  
Yoshikazu Yazaki ◽  
Takashi Tanaka
Keyword(s):  
Inhibitory Activity ◽  
Complex Mixture ◽  
Bark Extract ◽  
Type B ◽  
Acacia Mearnsii ◽  
Pyrolysis Products ◽  
Oligomeric Proanthocyanidins ◽  
Inhibitory Activities ◽  
C Nmr

Acacia mearnsii (Fabaceae) contains acacia polyphenols, which are a complex mixture of proanthocyanidins that are mainly composed of 5-deoxycatechin units. In this study, an aqueous extract of A. mearnsii bark was fractionated and the α-amylase inhibitory activity of each fraction was evaluated. The 13C NMR and MS data and the pyrolysis products obtained from the active and inactive fractions were compared. The spectroscopic results clearly indicated that fractions with strong inhibitory activity contained proanthocyanidin oligomers with catechol-type B-rings rather than pyrogallol-type B-rings. HPLC analysis of the pyrolysis products showed peaks for pyrocatechol were only observed in the mixtures obtained from the fractions with high inhibitory activities. In addition, (+)-pinitol was isolated as a major polyol of the extract at a level comparable with that of sucrose.

scholarly journals Bioactive Compounds from an Endophytic Fungi Nigrospora Aurantiaca

2021 ◽  
Author(s):  
Safwan Safwan ◽  
George Hsiao ◽  
Tzong-Huei Lee ◽  
Ching-Kuo Lee
Keyword(s):  
Bioactive Compounds ◽  
Endophytic Fungi ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Biological Activities ◽  
Fungal Strain ◽  
No Production ◽  
Chemical Structures ◽  
Inhibitory Activities ◽  
Melaleuca Leucadendra

Abstract Background: Many groups of fungi live as an endophyte in plants . Endophytic fungi could produce the bioactive compounds which was new or know compounds. Various biological activities of bioactive compounds from endophytic fungi had been reported, including anti-inflammatory and anticancer. Chemical investigation and biological activities of bioactive compounds from endophytic fungi from Melaleuca leucadendra Linn. have not yet been reportedResults: One new compound, namely nigaurdiol (1), together with five known compounds, xyloketal K (2), bostrycin (3), deoxybostrycin (4), xylanthraquinone (5), and ergosterol (6), were isolated from the Melaleuca leucadendra Linn. associated fungal strain Nigrospora aurantiaca #TMU062. Their chemical structures were elucidated by spectroscopic data and compared with literatures. All isolated compounds were evaluated for NO production inhibitory activity in LPS-activated microglial BV-2 cells. Conclusions: Compound 6 exhibited markedly inhibitory activities on NO production with IC50 values of 7.2 ± 1.4 µM and the survival of the cells was 90.8 ± 6.7% at the concentration of 10 µM.

scholarly journals Evaluation of the Antibacterial, Antioxidant and α-Glucosidase Inhibitory Activities of Withanolides from Physalis gracilis

2018 ◽  
Vol 5 (01) ◽  
pp. e1-e4
Author(s):  
Gerardo Padierna ◽  
Ana Pérez-Castorena ◽  
Mahinda Martínez ◽  
Antonio Nieto-Camacho ◽  
Jesús Morales-Jiménez ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Bacillus Subtilis ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
2D Nmr ◽  
Chemical Investigation ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Inhibitory Activities

AbstractA chemical investigation of the leaves, flowers, and stems of Physalis gracilis led to the isolation of three withanolides identified as withanolide D (1), 24,25-dihydrowithanolide D (2), and withaphysacarpin (3). The structures of these compounds were determined by analyses of their spectroscopic data, including 1D and 2D NMR. The antibacterial, antioxidant, and α-glucosidase inhibitory activities of compounds 1 and 3 and derivatives 4 and 5 were evaluated. None of the compounds showed antioxidant or glucosidase inhibitory activity. Also, they were inactive against gram-negative bacteria. However, compound 3 was found active against Bacillus subtilis (MIC=65.5 µM) and compound 5 against Staphylococcus aureus (MIC=27.9 µM).

scholarly journals Assessment of Anticholinesterase Activity ofGelidiella acerosa: Implications for Its Therapeutic Potential against Alzheimer’s Disease

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Arif Nisha Syad ◽  
Karutha Pandian Shunmugiah ◽  
Pandima Devi Kasi
Keyword(s):  
Spectrophotometric Method ◽  
Inhibitory Activity ◽  
Therapeutic Potential ◽  
Phytochemical Analysis ◽  
Phytochemical Screening ◽  
Gelidiella Acerosa ◽  
Cholinesterase Inhibitory Activity ◽  
Inhibitory Activities ◽  
Benzene Extract

The effect of various solvent extracts ofGelidiella acerosaon acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities was investigated. AChE and BuChE inhibitory activities were analyzed by spectrophotometric method. Phytochemical screening of the compounds present in the solvent extracts was done qualitatively. Characterization of the compounds present in the benzene extract ofG. acerosawas done by GC-MS analysis. The results showed that, at 487.80 μg/mL, benzene extract showed significant (P<0.05) inhibitory activity against both AChE and BuChE with the percentage of inhibition54.18±5.65% (IC50 = 434.61±26.53 μg/mL) and78.43±0% (IC50 = 163.01±85.35 μg/mL), respectively. The mode of inhibition exhibited by benzene extract against the AChE and BuChE was found to be competitive and uncompetitive type of inhibition, respectively. Preliminary phytochemical analysis coupled with GC-MS illustrates that the benzene extract possesses high amount of terpenoids, which could be the reason for potential cholinesterase inhibitory activity.

scholarly journals Phenylpropanoids from Liparis nervosa and their in vitro antioxidant and α-glucosidase inhibitory activities

2021 ◽  
Author(s):  
liang liu ◽  
meijia zou ◽  
qimeng yin ◽  
zhenyang zhang ◽  
xianwen zhang
Keyword(s):  
Vitamin C ◽  
Medicinal Plant ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Antioxidant Activities ◽  
Active Constituents ◽  
Inhibitory Activities ◽  
Physicochemical Constants

Abstract Eleven phenylpropanoids were isolated from the whole grass of Liparis nervosa, an orchidaceous medicinal plant. Their structures were elucidated as (+)-Syringaresinol (1), (-)-Syringaresinol-4-O-β-D-glucopyranoside (2), Sinapaldehyde (3), Coniferyl aldehyde (4), Syringin (5), Sinapaldehye glucoside (6), 2,3-dihydroxy-1-(4-hydroxy-3,5-dimethoxyphenyl)-1-propanone (7), C-Veratroylglycol (8), 7S, 7′S, 8R, 8′R-icariol A2 (9), Erigeside 2 (10), and Methylsyringin (11) by comparing the spectroscopic data and physicochemical constants from the isolated compounds with the data reported in the literature. Compounds 1 and 9 were found to have potent in vitro antioxidant activities in the DPPH and ABTS assays, and their IC50 values were lower than those of vitamin C. More importantly, compound 9 had a strong α-glucosidase inhibitory activity with an IC50 value of 43.76 ± 2.03 µM, which was much lower than that of acarbose (IC50 = 273.12 ± 11.84 µM), indicating that compound 9 has the potential for the development of hypoglycemic drugs. In conclusion, the present study suggests that phenylpropanoids may be the additional representative type of active constituents in L. nervosa, which provides a new line of evidence to understand this medicinal plant.

scholarly journals Chemical constituents of aerial parts of Thymus gobicus and their cholinesterase inhibitory activities

2017 ◽  
Vol 17 (43) ◽  
pp. 14-17
Author(s):  
Odonbayar B ◽  
T Murata ◽  
N Matsumoto ◽  
Batkhuu J ◽  
K Sasaki
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
Methyl Ester ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
High Performance ◽  
Chemical Constituents ◽  
Aerial Parts ◽  
Acetone Water ◽  
Inhibitory Activities

From an acetone-water (3:2) extract of aerial parts of Thymus gobicus Czern. (31.1 g), compounds 1-8 were obtained using high-performance liquid chromatography. Based on spectroscopic data, the isolated compounds were identified as rosmarinic acid (1), monardic acid A (2), nepetoidin B (3), aromadendrin (4), apigenin (5), chrysoriol (6), apigenin 7-O-β-D-glucuronopyranoside (7), and apigenin 7-O-β-D-glucuronopyranoside methyl ester (8). Compound 2 was a (7R,8R)-diastereomer of lithospermic acid (2a). Although it was reported that the anti-allergic activity of lithospermic acid was higher than that of 2, the acetylcholine inhibitory activity of 2 was higher than that of lithospermic acid.

Characterization of an Abnormal Antithrombin (Milano 2) with Defective Thrombin Binding

1986 ◽  
Vol 56 (03) ◽  
pp. 349-352 ◽  
Author(s):  
A Tripodi ◽  
A Krachmalnicoff ◽  
P M Mannucci
Keyword(s):  
Venous Thromboembolism ◽  
Active Site ◽  
Inhibitory Activity ◽  
Antithrombin Iii ◽  
Factor Xa ◽  
Molecular Defect ◽  
Affinity Adsorption ◽  
Italian Family ◽  
Crossed Immunoelectrophoresis

SummaryFour members of an Italian family (two with histories of venous thromboembolism) had a qualitative defect of antithrombin III reflected by normal antigen concentrations and halfnormal antithrombin activity with or without heparin. Anti-factor Xa activities were consistently borderline low (about 70% of normal). For the propositus’ plasma and serum the patterns of antithrombin III in crossed-immunoelectrophoresis with or without heparin were indistinguishable from those of normal plasma or serum. A normal affinity of antithrombin III for heparin was documented by heparin-sepharose chromatography. Affinity adsorption of the propositus’ plasma to human α-thrombin immobilized on sepharose beads revealed defective binding of the anti thrombin III to thrombin-sepharose. Hence the molecular defect of this variant appears to be at the active site responsible for binding and neutralizing thrombin, thus accounting for the low thrombin inhibitory activity.

Inhibition of Protein Tyrosine Phosphatase 1B by Lutein Derivatives isolated from Mexican Oregano (Lippia graveolens)

2018 ◽  
Vol 17 (3) ◽  
pp. 134-139
Author(s):  
R.M. Perez-Gutierrez
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Methanol Extract ◽  
Tyrosine Phosphatase ◽  
Positive Control ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Ic50 Value ◽  
Ic50 Values

Methanol extract from Lippia graveolens (Mexican oregano) was studied in order to identify inhibitory bioactives for protein tyrosine phosphatase 1B (PTP1B). Known flavone as lutein (1), and another flavone glycoside such as lutein-7-o-glucoside (2), 6-hydroxy-lutein-7-ohexoside (3) and lutein-7-o-ramnoide (4) were isolated from methanol extract of aerial parts of the Lippia graveolens. All isolates were identified based on extensive spectroscopic data analysis, including UV, IR, NMR, MS and compared with spectroscopic data previously reported. These flavones were evaluated for PTP1B inhibitory activity. Among them, compounds 1 and 3 displayed potential inhibitory activity against PTP1B with IC50 values of 7.01 ± 1.25 μg/ml and 18.4 μg/ml, respectively. In addition, compound 2 and 4 showed moderate inhibitory activity with an IC50 value of 23.8 ± 6.21 and 67.8 ± 5.80 μg/ml respectively. Among the four compounds, luteolin was found to be the most potent PTP1B inhibitor compared to the positive control ursolic acid, with an IC50 value of 8.12 ± 1.06 μg/ml. These results indicate that flavonoids constituents contained in Lippia graveolens can be considered as a natural source for the treatment of type 2 diabetes.

scholarly journals Fine-Tuning the Biological Profile of Multitarget Mitochondriotropic Antioxidants for Neurodegenerative Diseases

Antioxidants ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 329
Author(s):  
Daniel Chavarria ◽  
Ophelie Da Silva ◽  
Sofia Benfeito ◽  
Sandra Barreiro ◽  
Jorge Garrido ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Antioxidant Properties ◽  
Neuroblastoma Cells ◽  
Oxidation Potential ◽  
Fine Tuning ◽  
Mitochondrial Oxidative Stress ◽  
Electric Eel ◽  
Ic50 Values ◽  
System Extension ◽  
Inhibition Potency

Neurotransmitter depletion and mitochondrial dysfunction are among the multiple pathological events that lead to neurodegeneration. Following our previous studies related with the development of multitarget mitochondriotropic antioxidants, this study aims to evaluate whether the π-system extension on the chemical scaffolds of AntiOXCIN2 and AntiOXCIN3 affects their bioactivity and safety profiles. After the synthesis of four triphenylphosphonium (TPP+) conjugates (compounds 2–5), we evaluated their antioxidant properties and their effect on neurotransmitter-metabolizing enzymes. All compounds were potent equine butyrylcholinesterase (eqBChE) and moderate electric eel acetylcholinesterase (eeAChE) inhibitors, with catechols 4 and 5 presenting lower IC50 values than AntiOXCIN2 and AntiOXCIN3, respectively. However, differences in the inhibition potency and selectivity of compounds 2–5 towards non-human and human cholinesterases (ChEs) were observed. Co-crystallization studies with compounds 2–5 in complex with human ChEs (hChEs) showed that these compounds exhibit different binging modes to hAChE and hBChE. Unlike AntiOXCINs, compounds 2–5 displayed moderate human monoamine oxidase (hMAO) inhibitory activity. Moreover, compounds 4 and 5 presented higher ORAC-FL indexes and lower oxidation potential values than the corresponding AntiOXCINs. Catechols 4 and 5 exhibited broader safety windows in differentiated neuroblastoma cells than benzodioxole derivatives 2 and 3. Compound 4 is highlighted as a safe mitochondria-targeted antioxidant with dual ChE/MAO inhibitory activity. Overall, this work is a contribution for the development of dual therapeutic agents addressing both mitochondrial oxidative stress and neurotransmitter depletion.

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