Flavonoids: Potent inhibitors of arachidonate 5-lipoxygenase

Yoshimoto, Tanihiro; Furukawa, Masayuki; Yamamoto, Shozo; Hòrie, Tokunaru; Watanabe-Kohno, Shigekatsu

doi:10.1016/0006-291x(83)90568-5

Cited by 198 publications

(75 citation statements)

References 22 publications

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“…Note that these different ª5-LO activeº compounds mentioned (and many more, see below) have a cathechol partial structure in common, and it is assumed that the combined ironchelating and antioxidant feature of this moiety is eventually responsible for uncoupling of the 5-LO catalytic cycle. Since the plant kingdom is a rich source for various polyphenols, flavonoids and coumarins, subsequent investigations addressed various representatives with phenolic or coumarin structure from different plants [91], [92], [93]. A second class of plant-derived 5-LO inhibitors constitutes compounds lacking reducing properties that may mimic fatty (arachidonic) acid structures including polyacetylenes, and triterpenes and thus, inhibit 5-LO activity by binding and/or competing at the substrate-binding site or at a hypothetical fatty acid-binding cleft of 5-LO.…”

Section: Inhibitors Of 5-lo Product Synthesis From Plant Originmentioning

confidence: 99%

Inhibition of 5-Lipoxygenase Product Synthesis by Natural Compounds of Plant Origin

Werz¹

2007

Planta Med

155

135

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The biosynthesis of leukotrienes (LTs) is initiated by the transformation of free arachidonic acid to LTA 4 by 5-lipoxygenase (5-LO). Subsequent enzymatic conversion of LTA 4 yields LTB 4 and the cysteinyl-LTs C 4 , D 4 and E 4 . LTs have prominent functions in pathophysiology and are connected to numerous disorders including bronchial asthma, allergic rhinitis, inflammatory bowel and skin diseases, rheumatoid arthritis, cancer, osteoporosis and cardiovascular diseases. Pharmacological and genetic interruption of the 5-LO pathway or blockade of LT receptors, serving as means for intervention with LTs, may be of therapeutic value for certain related disorders. Natural or plant-derived substances were among the first 5-LO inhibitors identified in the early 1980 s. To date, a huge number of diverse plant-derived compounds have been reported to interfere with 5-LO product synthesis. However, many investigations have addressed the efficacy of a given compound solely in cellular test systems and analysis of direct interference with 5-LO has been neglected. In the first part of this review, the biology and molecular pharmacology of the 5-LO pathway is summarized in order to understand its overall regulation and complexity as well as to comprehend the possible points of attack of compounds that eventually lead to inhibition of 5-LO product formation in intact cells. In the second part, natural compounds that interfere with 5-LO product formation are compiled and grouped into structural classes, and the underlying molecular mechanisms and structureactivity relationships are discussed.

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Section: Inhibitors Of 5-lo Product Synthesis From Plant Originmentioning

confidence: 99%

Inhibition of 5-Lipoxygenase Product Synthesis by Natural Compounds of Plant Origin

Werz¹

2007

Planta Med

155

135

View full text Add to dashboard Cite

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“…They potentiate antiaggregatory PGI2 activity, inhibit thromboxane synthesis by inhibiting both lipoxygenase and cyclooxygenase activity, and also block platelet thromboxane receptors (41,43,44,53).…”

Section: Mechanisms Involved In the Antiaggregatory Effect Of Wine Phmentioning

confidence: 99%

Alcohol, Wine and Platelet Function

Ruf¹

2004

Biol. Res.

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Epidemiological studies have demonstrated an inverse correlation between moderate wine and alcohol consumption and morbidity and mortality from coronary heart disease. The protective effect has been associated with an increase in the plasma level of HDL cholesterol, as it is well recognized that plasma HDL is inversely correlated with CHD. In addition, it has become evident that blood platelets contribute to the rate of development of atherosclerosis and CHD through several mechanisms. In recent studies it has been shown that the level of HDL cholesterol can explain only 50 % of the protective effect of alcoholic beverages; the other 50 % may be partly related to a decrease in platelet activity. This anti-platelet activity of wine is explained by ethanol but also by the polyphenolic components with which red wines are richly endowed. Several studies carried out on humans and animals have shown that wine phenolics could exert their effects by reducing prostanoid synthesis from arachidonate. In addition, it has been suggested that wine phenolics could reduce platelet activity mediated by nitric oxide. Moreover, wine phenolics increase vitamin E levels while decreasing the oxidation of platelets submitted to oxidative stress. However, a rebound phenomenon of hyperaggregability is observed after an acute alcohol consumption which is not observed with wine consumption. This protection afforded by wine has been duplicated in animals with grape phenolics added to alcohol. The rebound phenomenon may explain ischemic strokes or sudden deaths known to occur after episodes of drunkenness. It appears that wine, and wine phenolics in particular, could have a more significant inhibitory effect on platelet aggregation and could explain, in part, the hypothesis that red wine is more protective against atherosclerosis and coronary heart disease.

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“…Penghambatan ini akan menyebabkan penurunan kandungan asam arakidonat pada jaringan membran fosfolipid sel 40 yang lebih lanjut akan mengakibatkan terhambatnya pelepasan sejumlah mediator inflamasi seperti prostaglandin, leukotrin dan tromboksan. 41,42 Oleh karena ekstrak etanol propolis yang digunakan pada penelitian ini mempunyai konsistensi yang kental, maka diduga bahwa 1 minggu setelah aplikasi, konsentrasi ekstrak ini relatif masih tinggi. Konsentrasi yang masih tinggi ini erat hubungannya dengan kemampuan antibakteri dari ekstrak flavonoid maupun ekstrak non flavonoid.…”

Section: Pembahasanunclassified

Respons inflamasi pada pulpa gigi tikus setelah aplikasi ekstrak etanol propolis (EEP) (The inflammatory response on rat dental pulp following ethanolic extract of propolis (EEP) application)

Sabir

2005

Dent. J. (Majalah Kedokteran Gigi)

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Propolis is a resinous hive product collected by bees from tree buds and mixed with secreted bee wax in order to avoid bacterial contamination in the hive, and also to seal it. Propolis is employed for the treatment of various infectious diseases because it is wellknown that is has antibacterial and anti-inflammatory properties. The therapeutic use of propolis in dentistry has PENDAHULUANKata propolis berasal dari bahasa Yunani, yaitu pro berarti pertahanan dan polis berarti kota, sehingga propolis bermakna pertahanan kota (atau sarang lebah). 1,2 Propolis atau lem lebah adalah nama generik yang diberikan untuk bahan resin yang dikumpulkan oleh lebah madu dari berbagai macam jenis tumbuhan, terutama dari bagian kuncup dan daun tumbuhan tersebut. 1,3 Lebah kemudian mencampur bahan resin ini dengan enzim yang disekresikan dari kelenjar mandibula lebah, 4 meskipun demikian komponen yang terdapat di dalam propolis tidak mengalami perubahan. 1 Lebah menggunakan propolis sebagai: 1) memperkuat sarang lebah; 1 2) bahan pelapis untuk melindungi sarangnya dari faktor pengganggu dari luar, misalnya serangga, kumbang, atau tikus; 3,5 3) meratakan dinding sarang lebah; 4 4) bahan pengisi lubang atau celah dan perekat keretakan yang terdapat pada sarang lebah, 5,6 5) melindungi sel sarang tempat ratu lebah menetaskan telurnya sehingga larva lebah terlindungi dari penyakit 6 dan 6) antibakteri. 7 Komposisi propolis sangat bervariasi dan erat hubungannya dengan jenis dan umur tumbuhan di mana propolis tersebut berasal. 4,5 Umumnya propolis terdiri dari: 4 campuran resin dan getah 39-53%, polifenol 1,2-17%, polisakarida 2-3%, lilin (wax) 19-35%, dan bahan lain 8-12%. Menurut Kaal, 6 komposisi propolis meliputi: resin dan balsem ± 50%, lilin (wax) ± 30%, minyak esensial ± 10%, pollen ± 5%, dan senyawa organik dan mineral ± 5%. Penelitian terhadap propolis yang berasal dari 15 daerah yang berbeda di Rusia menunjukkan hasil yang hampir sama, yaitu: 5 resin 50-55%, lilin (wax) maksimal 30%, minyak esensial ± 8-10%, dan bahan padat ± 5%.Jenis senyawa kimia yang terdapat pada propolis sangat kompleks. Berdasarkan analisis dengan menggunakan metode Gas Chromatography-Mass Spectrometry (GC-MS) yang dilakukan oleh Greenaway et al. 3 terhadap propolis yang dihimpun oleh lebah yang berasal dari tumbuhan poplar menunjukkan bahwa propolis mengandung berbagai macam senyawa, yaitu: asam amino, asam alifatik dan esternya, asam aromatik dan esternya, alkohol, aldehida, khalkon, dihidrokhalkon,

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Flavonoids: Potent inhibitors of arachidonate 5-lipoxygenase

Cited by 198 publications

References 22 publications

Inhibition of 5-Lipoxygenase Product Synthesis by Natural Compounds of Plant Origin

Inhibition of 5-Lipoxygenase Product Synthesis by Natural Compounds of Plant Origin

Alcohol, Wine and Platelet Function

Respons inflamasi pada pulpa gigi tikus setelah aplikasi ekstrak etanol propolis (EEP) (The inflammatory response on rat dental pulp following ethanolic extract of propolis (EEP) application)

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