Baicalein is a potent in vitro inhibitor against both reticulocyte 15-human and platelet 12-human lipoxygenases

Deschamps, Joshua D.; Kenyon, Victor; Holman, Theodore R.

doi:10.1016/j.bmc.2006.01.057

Cited by 144 publications

(139 citation statements)

References 58 publications

Supporting

Mentioning

125

Contrasting

Unclassified

Order By: Relevance

“…The decrease in the amount of ROS/RNS in the presence of 3 μM NDGA can be partially explained by its antioxidant properties, which should have the same effect in the aortas of the two experimental groups of rats. Baicalein, as an inhibitor of 12-and 15-lipogenases (Deschamps et al 2006), reduces essentially the amount of ROS/RNS in the aortas of control rats (line 2), whereas the effect of caffeic acid, a specific inhibitor of 5-lipoxygenase (Koshihara et al 1984), is insignificant (line 4). In the aortas of rats treated with L-NAME, the effect of these inhibitors is the opposite: NDGA and baicalein have a lesser effect than in the aortas of control rats, and caffeic acid has a far greater effect.…”

Section: The Effect Of Taxifolin On the Formation Of Ros/rnsmentioning

confidence: 98%

Effects of taxifolin on the activity of angiotensin-converting enzyme and reactive oxygen and nitrogen species in the aorta of aging rats and rats treated with the nitric oxide synthase inhibitor and dexamethasone

Arutyunyan

Korystova

Kublik

et al. 2012

AGE

View full text Add to dashboard Cite

The action of taxifolin on the angiotensinconverting enzyme (ACE) and the formation of reactive oxygen and nitrogen species (ROS/RNS) in the aorta of aging rats and rats treated with nitric oxide synthase inhibitor (N ω -nitro-L-arginine methyl ester (L-NAME)) or dexamethasone have been studied. The ACE activity in aorta sections was determined by measuring the hydrolysis of hippuryl-L-histidyl-L-leucine, and the ROS/ RNS production was measured by oxidation of dichlorodihydrofluorescein. It was shown that taxifolin at a dose of 30-100 μg/kg/day decreases the ACE activity in the aorta of aging rats and of rats treated with L-NAME or dexamethasone to the level of the ACE activity in young control rats. Taxifolin (100 μg/kg/day) was found to also reduce the amount of ROS/RNS in the aorta that increased as a result of L-NAME intake. L-NAME treatment increases the contribution of 5-lipoxygenase and NADPH oxidase to ROS/RNS production in the aorta, while taxifolin (100 μg/kg/day) decreases the contribution of these enzymes to the normal level.

show abstract

Section: The Effect Of Taxifolin On the Formation Of Ros/rnsmentioning

confidence: 98%

Effects of taxifolin on the activity of angiotensin-converting enzyme and reactive oxygen and nitrogen species in the aorta of aging rats and rats treated with the nitric oxide synthase inhibitor and dexamethasone

Arutyunyan

Korystova

Kublik

et al. 2012

AGE

View full text Add to dashboard Cite

show abstract

“…Baicalein, a trihydroxylated flavonoid derivative, was found to be a potent and selective human lipoxygenase (LO) inhibitor [84], through direct binding of its catecholic moiety to the iron centre at the enzyme´s active site. This chromone derivative may therefore become a promising chemopreventive/chemotherapeutic agent, since lipoxygenase is implicated in pathologies such as asthma, immune disorders and several types of cancer.…”

Section: Chromones As Bioactive Agentsmentioning

confidence: 99%

Bioactive Chromone Derivatives – Structural Diversity

Machado¹,

Marques

2010

CBC

View full text Add to dashboard Cite

Chromones (1-benzopyran-4-ones) and chromone derivatives are naturally occurring compounds ubiquitously found in the plant kingdom, and therefore present in representative amounts in a normal human diet. These phytochemicals possess a wide spectrum of biological activities -such as anti-inflammatory, antifungal, antimicrobial, antiviral, antitumour and anticancer -mainly due to their well-recognised antioxidant properties, which stem from their ability to neutralise active forms of oxygen and to cut off free radical processes.Since oxidative stress is known to be the basis for numerous severe pathologies, from cardiovascular and neurodegenerative disorders to cancer, the development of effective antioxidant agents from natural origin (namely dietary constituents) has been the object of vigorous research in the last decade, in view of establishing novel chemopreventive strategies against such diseases which are nowadays the main cause of death worldwide. In fact, the chromone moiety is an important element of pharmacophores of many biologically active molecules displaying diverse medicinal applications.These potential health benefits arising from the antioxidant activity of chromone derivatives are ruled by strict structureactivity/structure-property relationships, which, apart from determining their biological action, modulate their systemic distribution and bioavailability in sites of oxidation within the cell.The present work aims at reviewing the main reported studies on the cytoprotective and anticancer activities of chromone derivatives, with particular emphasis on the effect of their structural features and conformational behaviour on activity, which is the basis of a tailored design of novel chromone-based antioxidants for chemopreventive and chemotherapeutic use.

show abstract

“…In conclusion, our data demonstrate that baicalein is a direct free radical scavenger, however, IC 50 for antioxidative activity is over 100 times higher than IC 50 for catalytic activity (Tab. 1) [16]. Also, nordihydroguaiaretic acid, which is used in traditional medicine, is a natural compound (from Larrea tridentate) with a broad spectrum of biological properties [35].…”

Section: +mentioning

confidence: 99%

“…g effect on synthesis of LTB 4 tested in human whole blood [5]; h effect on activity of 15-LOX-1 tested in human reticulocytes [16];…”

Section: +mentioning

confidence: 99%

“…i effect on activity of 12-LOX in human platelets [16]; j effect on activity of 15-LOX tested in rabbit reticulocytes [27,40]; k effect on activity of 12-LOX tested in human platelets [27,40]; l effect on synthesis of CysLT tested in rat peritoneal cells [27] treatment of asthma in adults and children, but it does cause some serious side effects, including hepatotoxicity and neuropsychiatric events [44,51]. AA-861, a redox-active 5-LOX inhibitor, demonstrated weak antioxidative properties against lipid peroxidation.…”

Section: +mentioning

confidence: 99%

See 1 more Smart Citation

5-lipoxygenase inhibitors

SpringerReference

View full text Add to dashboard Cite

Abstract:Background: Oxidative stress is a component of many pathological conditions including neurodegenerative diseases and inflammation. An important source of reactive oxygen species (ROS) are lipoxygenases (LOX) -enzymes responsible for the metabolism of arachidonic acid and other polyunsaturated fatty acids. LOX inhibitors have a protective effect in inflammatory diseases and in neurodegenerative disorders because of their anti-inflammatory activity. However, the molecular mechanism of the protective action of LOX inhibitors has not yet been fully elucidated. Methods: The aim of this study was to compare the antioxidative potential of widely used LOX inhibitors: BWB70C, AA-861, zileuton, baicalein and NDGA. The antioxidative properties were evaluated in cell-free systems. We measured the effect of the tested compounds on iron/ascorbate-induced lipid peroxidation and on carbonyl group formation in the rat brain homogenate. Direct free radical scavenging was analyzed by using DPPH assay. Results: Our data showed that the inhibitor of all LOXs, i.e., NDGA, 5-LOX inhibitor BWB70C and the inhibitor of 12/15-LOX, baicalein, significantly decreased the level of lipid and protein oxidation. The free radical scavenging activity of these inhibitors was comparable to known ROS scavengers, i.e., resveratrol and trolox. Zileuton (the inhibitor of 5-LOX) slightly prevented lipid and protein oxidation, it also scavenged the DPPH radical. AA-861 (the inhibitor of 5 and 12/15-LOX) slightly protected lipids against Fe/asc-evoked lipid peroxidation at high concentrations, but had no effect on carbonyl group formation and DPPH scavenging. Conclusions: Our results indicate that some LOX inhibitors demonstrate potent anti-oxidative, free radical scavenging properties. AA-861, whose antioxidative potential is very weak, may be a specific tool to be used in experimental and perhaps even clinical applications.

show abstract

Baicalein is a potent in vitro inhibitor against both reticulocyte 15-human and platelet 12-human lipoxygenases

Cited by 144 publications

References 58 publications

Effects of taxifolin on the activity of angiotensin-converting enzyme and reactive oxygen and nitrogen species in the aorta of aging rats and rats treated with the nitric oxide synthase inhibitor and dexamethasone

Effects of taxifolin on the activity of angiotensin-converting enzyme and reactive oxygen and nitrogen species in the aorta of aging rats and rats treated with the nitric oxide synthase inhibitor and dexamethasone

Bioactive Chromone Derivatives – Structural Diversity

5-lipoxygenase inhibitors

Contact Info

Product

Resources

About