Inhibition of Prostaglandin and Leukotriene Biosynthesis by Gingerols and Diarylheptanoids.

Kiuchi, Fumiyuki; Iwakami, Satoshi; Shibuya, Masabumi; Hanaoka, Fumio; Sankawa, Ushio

doi:10.1248/cpb.40.387

Cited by 306 publications

(161 citation statements)

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“…A relationship between its structure and the antiinflammatory activity has not been demonstrated as yet. It is assumed that curcumin exerts inhibitory activity on the synthesis of prostaglandines and leukotriens thanks to the presence of hydroxyl groups and phenolic rings [36].…”

Section: Discussionmentioning

confidence: 99%

Age-dependent different action of curcumin in thyroid of rat.

Papież

Kaja²,

Gebarowska³

2008

Folia Histochem Cytobiol.

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Abstract:The aging is associated with alterations in the hypothalamic-pituitary-thyroidal axis which can lead to hypothyreosis. Our previous investigations has shown that polyphenol curcumin can enhance the manifestation of hypothyreosis in rats simultanous treated with propylthiouracil. The aim of the study was to investigate the relationship between age-related changes and curcumin action in the thyroid of old rats. To this end, morphometric and radioimmunological methods were used. The study was conducted on 3-and 18-month-old male Wistar rats. The experimental rats were treated daily for 30 days by gavage with 100 mg/kg b.w. of curcumin. There were observed age-related changes in morphology and endocrine function of the thyroid. It was increase in the percentages of large follicles and significant decrease in FT3 level in 18-month-old rats in comparison to 3-month ones. Curcumin treatment lead to significant increase in FT3 and FT4 levels in 3-month-old experimental rats, but the level of FT3 significantly decreased in 18-month-old rats after curcumin administration. Our results show that curcumin activity depends on the functional condition of the rat thyroid which changes with age. This compound exerts stimulatory influence on the secretory function of the thyroid gland in young rats, but has rather weak antithyroid activity in old animals.

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Section: Discussionmentioning

confidence: 99%

Age-dependent different action of curcumin in thyroid of rat.

Papież

Kaja²,

Gebarowska³

2008

Folia Histochem Cytobiol.

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“…These compounds may be regarded as potent and direct 5-LO inhibitors. Similarly, the well-recognized curcumin 52 from Curcuma longa L. [39], [129] and the structurally related gingerols 53 from Zingiber officnialis Roscoe [115], [116] proved to inhibit 5-LO in cell-based and cell-free assays with IC 50 < 1 mM. Interestingly, compared to the prenylated hyperforin 48, the structurally related polyphenols such as erychristagallin 46 [130], or kuraridin 47 [105] possessing lipophilic prenyl residues (that seemingly enhance the potency of flavonoids) are significantly less effective with IC 50 values > 20 mM.…”

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

149

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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“…The pharmacological properties of gingerols include antioxidant, analgesic and anti-inflammatory [6] , antipyretic [7] , cardiotonic [8] , and hypothermic [9] activities. More recent studies have suggested that gingerols exhibit preventive activity against cancers of the skin [10] , pancreas [11] , gastrointestinal tract [12] , colon [13] , and breast [14] .…”

Section: Introductionmentioning

confidence: 99%

Pungent ginger components modulates human cytochrome P450 enzymes in vitro

Chen

Yue

et al. 2013

Acta Pharmacol Sin

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Aim: Ginger rhizome is used worldwide as a spicy flavor agent. This study was designed to explore the potential effects of pungent ginger components, 6-, 8-, and 10-gingerol, on human cytochrome P450 (CYP450) enzymes that are responsible for the metabolism of many prescription drugs. Methods: The activities of human CYP2C9, CYP2C19, CYP2D6, and CYP3A4 were analyzed using Vivid P450 assay kits. The mRNA expression of CYP3A4 in human hepatocellular carcinoma cell line HepG2 was measured using quantitative real-time PCR assay. Results: All three gingerols potently inhibited CYP2C9 activity, exerted moderate inhibition on CYP2C19 and CYP3A4, and weak inhibion on CYP2D6. 8-Gingerol was the most potent in inhibition of P450 enzymes with IC 50 values of 6.8, 12.5, 8.7, and 42.7 μmol/L for CYP2C9, CYP2C19, CYP3A4, and CYP2D6, respectively. By comparing the effects of gingerols on CYP3A4 with three different fluorescent substrate probes, it was demonstrated that the inhibition of gingerols on CYP3A4 had no substrate-dependence. In HepG2 cells, 8-gingerol and 10-gingerol inhibited, but 6-gingerol induced mRNA expression of CYP3A4. Conclusion: 6-, 8-, and 10-gingerol suppress human cytochrome P450 activity, while 8-and 10-gingerol inhibit CYP3A4 expression. The results may have an implication for the use of ginger or ginger products when combined with therapeutic drugs that are metabolized by cytochrome P450 enzymes.

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Inhibition of Prostaglandin and Leukotriene Biosynthesis by Gingerols and Diarylheptanoids.

Cited by 306 publications

References 0 publications

Age-dependent different action of curcumin in thyroid of rat.

Age-dependent different action of curcumin in thyroid of rat.

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

Pungent ginger components modulates human cytochrome P450 enzymes in vitro

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