Polar constituents of Ligustrum vulgare L. and their effect on lipoxygenase activity

2011 ◽  
Vol 65 (3) ◽  
Author(s):  
Pavel Mučaji ◽  
Milan Nagy ◽  
Anna Záhradníková ◽  
Ivana Holková ◽  
Lýdia Bezáková ◽  
...  
Keyword(s):  
Kinetic Parameters ◽  
Inhibitory Activity ◽  
Methanolic Extract ◽  
Competitive Inhibition ◽  
Inhibiting Activity ◽  
Rat Lung ◽  
Isolation And Identification ◽  
Cytosol Fraction ◽  
Water Infusion ◽  
Ligustrum Vulgare

AbstractThe present work summarizes results of isolation and identification of polar constituents of the methanolic extract of Ligustrum vulgare L. leaves and of the evaluation of inhibiting activity of selected isolates on rat lung cytosol fraction lipoxygenase. Six different compounds were isolated from the ethylacetate and butanol portions of the methanolic extract (hydroxytyrosol and its glucoside, ligustroflavon, oleuropein, acteoside, echinacoside). The inhibitory activity of oleuropein, echinacoside and the water infusion of Ligustrum vulgare leaves tested on LOX was expressed as IC50. Kinetic parameters (K M, V max) and type of inhibition were determined. As the most effective in competitive inhibition of LOX, oleuropein was proved.

scholarly journals Mammalian Arginase Inhibitory Activity of Methanolic Extracts and Isolated Compounds from Cyperus Species

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1694
Author(s):  
Kamel Arraki ◽  
Perle Totoson ◽  
Alain Decendit ◽  
Andy Zedet ◽  
Justine Maroilley ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Methanolic Extract ◽  
Significant Inhibition ◽  
Isolation And Identification ◽  
Vasorelaxant Effect ◽  
Methanolic Extracts ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
First Time

Polyphenolic enriched extracts from two species of Cyperus, Cyperus glomeratus and Cyperus thunbergii, possess mammalian arginase inhibitory capacities, with the percentage inhibition ranging from 80% to 95% at 100 µg/mL and 40% to 64% at 10 µg/mL. Phytochemical investigation of these species led to the isolation and identification of two new natural stilbene oligomers named thunbergin A-B (1–2), together with three other stilbenes, trans-resveratrol (3), trans-scirpusin A (4), trans-cyperusphenol A (6), and two flavonoids, aureusidin (5) and luteolin (7), which were isolated for the first time from C.thunbergii and C. glomeratus. Structures were established on the basis of the spectroscopic data from MS and NMR experiments. The arginase inhibitory activity of compounds 1–7 was evaluated through an in vitro arginase inhibitory assay using purified liver bovine arginase. As a result, five compounds (1, 4–7) showed significant inhibition of arginase, with IC50 values between 17.6 and 60.6 µM, in the range of those of the natural arginase inhibitor piceatannol (12.6 µM). In addition, methanolic extract from Cyperus thunbergii exhibited an endothelium and NO-dependent vasorelaxant effect on thoracic aortic rings from rats and improved endothelial dysfunction in an adjuvant-induced arthritis rat model.

scholarly journals ALPHA-GLUCOSIDASE INHIBITING ACTIVITY FROM THE MOST ACTIVE FRACTION OF CALOPHYLLUM TOMENTOSUM, WIGHT LEAVES

2017 ◽  
Vol 10 (17) ◽  
pp. 73 ◽  
Author(s):  
Berna Elya ◽  
Nuraini Puspitasari ◽  
Fasya Hadaina Maharani
Keyword(s):  
Enzyme Activity ◽  
Ethyl Acetate ◽  
Inhibitory Activity ◽  
Inhibitory Concentration ◽  
Methanol Extract ◽  
Methanolic Extract ◽  
Inhibiting Activity ◽  
Active Fraction ◽  
Static Phase ◽  
Alpha Glucosidase

Objective: The purpose of this study was to obtain the inhibitory concentration, 50% value from the most active fraction of methanolic extract of leaf Calophyllum tomentosum, Wight, and to identify the group of compounds contained in the most active fraction.Methods: The methanol extract was fractionated using the silica gel static phase, the n-hexane motion phase, ethyl acetate, and methanol enhanced by its polarity. Results: There were nine selected fractions tested in inhibitory activity using an enzyme activity inhibitory assay. Conclusions: The results showed the inhibition by the most active fraction is 51.288 μg/mL; this fraction contains of flavonoid, saponin, and terpenoid.

scholarly journals Four Novel Phenanthrene Derivatives with α-Glucosidase Inhibitory Activity from Gastrochilus bellinus

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 418
Author(s):  
Htoo Tint San ◽  
Nutputsorn Chatsumpun ◽  
Thaweesak Juengwatanatrakul ◽  
Natapol Pornputtapong ◽  
Kittisak Likhitwitayawuid ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Kinetic Study ◽  
Inhibitory Activity ◽  
Methanolic Extract ◽  
Competitive Inhibition ◽  
Spectroscopic Methods ◽  
First Report ◽  
Ic50 Value ◽  
Phytochemical Constituents

Four new phenanthrene derivatives, gastrobellinols A-D (1–4), were isolated from the methanolic extract of Gastrochilus bellinus (Rchb.f.) Kuntze, along with eleven known phenolic compounds including agrostophyllin (5), agrostophyllidin (6), coniferyl aldehyde (7), 4-hydroxybenzaldehyde (8), agrostophyllone (9), gigantol (10), 4-(methoxylmethyl)phenol (11), syringaldehyde (12), 1-(4′-hydroxybenzyl)-imbricartin (13), 6-methoxycoelonin (14), and imbricatin (15). Their structures were determined by spectroscopic methods. Each isolate was evaluated for α-glucosidase inhibitory activity. Compounds 1, 2, 3, 7, 9, 13, and 15 showed higher activity than the drug acarbose. Gastrobellinol C (3) exhibited the strongest α-glucosidase inhibition with an IC50 value of 45.92 μM. A kinetic study of 3 showed competitive inhibition on the α-glucosidase enzyme. This is the first report on the phytochemical constituents and α-glucosidase inhibitory activity of G. bellinus.

Isolation and Identification of a Potent PTP1B Inhibitor, Ursolic Acid, from Carolina Jasmine (Gelsemium sempervirens (L.) J.St.-Hil.)

2020 ◽  
Vol 17 (12) ◽  
pp. 939-943
Author(s):  
Toshiro Noshita ◽  
Yusuke Kakizoe ◽  
Satoshi Tanabe ◽  
Hidekazu Ouchi ◽  
Akihiro Tai
Keyword(s):  
Ursolic Acid ◽  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Active Agent ◽  
Protein Tyrosine Phosphatase 1B ◽  
Inhibiting Activity ◽  
Inhibition Activity ◽  
Isolation And Identification ◽  
Gelsemium Sempervirens

Extracts of Carolina jasmine (Gelsemium sempervirens (L.) J.St.-Hil.) petals were evaluated in vitro for inhibition activity against protein tyrosine phosphatase 1B (PTP1B). The principle active agent was also isolated from the extract and identified as ursolic acid (1). This is the first report of ursolic acid from G. sempervirens and of PTP1B-inhibiting activity in the genus Gelsemium.

Phytoceuticals in aniseeds: a practical approach for isolation and identification

2016 ◽  
Vol 5 (01) ◽  
pp. 4701
Author(s):  
Shobha R. I. ◽  
Andallu B.
Keyword(s):  
Chronic Diseases ◽  
Column Chromatography ◽  
High Performance ◽  
Methanolic Extract ◽  
Analytical Techniques ◽  
Therapeutic Agents ◽  
Systematic Research ◽  
Isolation And Identification ◽  
Traditional System ◽  
Pharmacologically Active

Nature has provided mankind with a broad and structurally diverse array of pharmacologically active chemical compounds, phytoceuticals, which have proved to be indispensable for the cure of chronic diseases or as lead structures for novel therapeutic agents. Almost, 70% of modern medicines in India have been developed from plants used in the traditional system of medicine. With the technological advances and the development of more sophisticated isolation and analytical techniques, there is great scope for further systematic research to screen and isolate many more phytoceuticals which might be more effective/as effective as synthetic drugs and thereby assess their potential in protecting against chronic diseases. The present investigation is aimed at isolation and identification of phytoceuticals in a spice, aniseed (Pimpinella anisum L), therapeutically less-exploited and widely used only for culinary purpose, using analytical techniques viz. column chromatography, high performance thin layer chromatography (HPTLC.) and nuclear magnetic resonance spectrometry. Among all the solvent fractions of methanolic extract tested, methanolic extract and ethyl acetate fraction possessed highest amounts of bioactive compounds viz. phenolics, flavonoids, flavonols which was confirmed by qualitative, quantitative and HPTLC. analyses. Spectral analysis using NMR. of one of the sub-fractions of aniseeds obtained by column chromatography, revealed the presence of a glycosylated flavone, luteolin-6C-glucoside in aniseeds.  The present study revealed aniseeds to be a great source of bioactive phytoceuticals which can be novel candidates for development of new therapeutic agents.

scholarly journals Aldose Reductase Inhibitory Activity of Compounds from  Zea maysL.

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Tae Hyeon Kim ◽  
Jin Kyu Kim ◽  
Young-Hee Kang ◽  
Jae-Yong Lee ◽  
Il Jun Kang ◽  
...  
Keyword(s):  
Zea Mays ◽  
Aldose Reductase ◽  
Inhibitory Activity ◽  
Diabetes Complications ◽  
Therapeutic Agent ◽  
Competitive Inhibition ◽  
Therapeutic Potential ◽  
High Concentration ◽  
Etoh Extract ◽  
Bioassay Guided Fractionation

Aldose reductase (AR) inhibitors have a considerable therapeutic potential against diabetes complications and do not increase the risk of hypoglycemia. Through bioassay-guided fractionation of an EtOH extract of the kernel from purple corn (Zea maysL.), 7 nonanthocyanin phenolic compounds (compound1–7) and 5 anthocyanins (compound8–12) were isolated. These compounds were investigated by rat lens aldose reductase (RLAR) inhibitory assays. Kinetic analyses of recombinant human aldose reductase (rhAR) were performed, and intracellular galactitol levels were measured. Hirsutrin, one of 12 isolated compounds, showed the most potent RLAR inhibitory activity (IC50, 4.78 μM). In the kinetic analyses using Lineweaver-Burk plots of 1/velocity and 1/substrate concentration, hirsutrin showed competitive inhibition against rhAR. Furthermore, hirsutrin inhibited galactitol formation in rat lens and erythrocytes sample incubated with a high concentration of galactose; this finding indicates that hirsutrin may effectively prevent osmotic stress in hyperglycemia. Therefore, hirsutrin derived fromZea maysL. may be a potential therapeutic agent against diabetes complications.

Bioassay-Guided Isolation and Identification of a Acetylcholinesterase Inhibitors from Calophyllum polyanthum

2013 ◽  
Vol 634-638 ◽  
pp. 1225-1228 ◽  
Author(s):  
Fei Zhang ◽  
Hai Wei Ren ◽  
Yong Gang Wang ◽  
Rong Wang ◽  
Jie Sheng
Keyword(s):  
Inhibitory Activity ◽  
Cholinesterase Activity ◽  
Spectral Characteristics ◽  
Ethanolic Extract ◽  
Acetylcholinesterase Inhibitors ◽  
Microplate Assay ◽  
Acetyl Cholinesterase ◽  
Isolation And Identification ◽  
Active Compounds ◽  
Bioautographic Method

A significant acetylcholinesterase inhibitory activity was observed for the Ethanolic extract from the leaves of Calophyllum polyanthum by using TLC bioautographic method. Further bioassay-guided isolation of this extract using TLC bioautographic method resulted in obtaining a pyranochromanone, apetalic acid (1). The structure of 1 was identified by comparison of it’s spectral characteristics with previous reports. The concentration required for 50% inhibition of 1 was 0.95 mM, determined by a microplate assay. The anti-acetylcholinesterase aity of compound 1 was weak, but it was the first pyranochromanone which have anti-acetyl cholinesterase activity. As a new leading compound, it can be modified and transformed to obtain more potently active compounds.

scholarly journals Isolation and identification of compounds with dioxin-induced AhR transformation inhibitory activity from the leaves of Mallotus japonicus (Thunb.) Muell. Arg.

2019 ◽  
Vol 13 (8) ◽  
pp. 167-172
Author(s):  
Hosokawa Keizo ◽  
Hishida Atsuyuki ◽  
Nishiumi Shin ◽  
Fukushi Eri ◽  
Kawabata Jun ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Isolation And Identification ◽  
Mallotus Japonicus

scholarly journals Characterization of platinum(II) complexes exhibiting inhibitory activity against the 20S proteasome

2020 ◽  
Vol 7 (8) ◽  
pp. 200545
Author(s):  
Tatsuto Kiwada ◽  
Hiromu Katakasu ◽  
Serina Okumura ◽  
Akira Odani
Keyword(s):  
Inhibitory Activity ◽  
Chemical Structure ◽  
Competitive Inhibition ◽  
Proteasome Inhibitors ◽  
Platinum Complex ◽  
Platinum Complexes ◽  
Binding Mode ◽  
Structure Activity Relationships ◽  
Structure Activity

Proteasome inhibitors are useful for biochemical research and clinical treatment. In our previous study, we reported that the 4N-coordinated platinum complexes with anthracenyl ring and heterocycle exhibited proteasome-inhibitory activity. In the present study, the structure–activity relationships and characterization of these complexes were determined for the elucidation of the role of aromatic ligands. Lineweaver–Burk analysis revealed that the chemical structure of heterocycles affects the binding mode of platinum complexes. Platinum complexes with anthracenyl ring and pyridine showed competitive inhibition, although platinum complexes with anthracenyl ring and phenanthroline showed non-competitive inhibition. The structure–activity relationships demonstrated that anthracenyl moiety plays a crucial role in proteasome-inhibitory activity. The platinum complexes with naphthyl or phenyl rings exhibited lower inhibitory activities than the platinum complex with anthracenyl ring. The reactivity with N-acetylcysteine varied according to the chemical structure of complexes.

scholarly journals Identification of a Xanthine Oxidase-inhibitory Component from Sophora Flavescens using NMR-based Metabolomics

2013 ◽  
Vol 8 (10) ◽  
pp. 1934578X1300801
Author(s):  
Ryuichiro Suzuki ◽  
Yuka Hasuike ◽  
Moeka Hirabayashi ◽  
Tatsuo Fukuda ◽  
Yoshihito Okada ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Methanolic Extract ◽  
Sophora Flavescens ◽  
Vitro Assay ◽  
H Nmr ◽  
Plot Analysis ◽  
Inhibitory Compounds ◽  
Loading Plot

We demonstrate that NMR-based metabolomics studies can be used to identify xanthine oxidase-inhibitory compounds in the diethyl ether soluble fraction prepared from a methanolic extract of Sophora flavescens. Loading plot analysis, accompanied by direct comparison of 1H NMR spectra exhibiting characteristic signals, identified compounds exhibiting inhibitory activity. NMR analysis indicated that these characteristic signals were attributed to flavanones such as sophoraflavanone G and kurarinone. Sophoraflavanone G showed inhibitory activity towards xanthine oxidase in an in vitro assay.

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