The influence of rhein on the biosynthesis of prostaglandin-like substances in-vitro

Franchi‐Micheli, S.; Lavacchi, Laura; Friedmann, Christina; Zilletti, Lucilla

doi:10.1111/j.2042-7158.1983.tb02929.x

Cited by 42 publications

(10 citation statements)

References 12 publications

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“…On the other hand, diacerein did not affect the content of PGE 2 in both normal rats and indometha-cin-treated rats. It was reported that rhein does not reduce PGE 2 synthesis [21] and may even have the opposite effect of increasing it [22]. These data indicate that the inhibitory effect of diacerein on indomethacin-induced gastric ulceration is not mediated by an augmentation of gastric mucosal PGE 2 production.…”

Section: Discussionsupporting

confidence: 58%

Effects of Diacerein on Indomethacin-Induced Gastric Ulceration

2001

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We investigated the effect of diacerein, an antiosteoarthritic agent, and its metabolite, rhein, on the production of reactive oxygen species (ROS) from neutrophils as well as the protective effect of diacerein on indomethacin-induced gastric ulceration and its protection mechanism. Rhein inhibited the ROS production from N-formyl-methionyl-leucyl-phenylalanine or phorbol-12-myristate-13-acetate-activated human peripheral neutrophils. Indomethacin-induced gastric ulceration was significantly inhibited by oxygen radical scavengers and 16,16-dimethyl-prostaglandin E₂ (dmPGE₂) but not by allopurinol. Diacerein inhibited indomethacin-induced gastric ulceration in a dose-dependent manner. Diacerein did not affect the gastric mucosal PGE₂ content. In addition, diacerein inhibited HCl + ethanol-induced gastric ulceration. These data indicate that the inhibitory effect of diacerein on indomethacin-induced gastric ulceration could be mediated not by the augmentation of gastric mucosal PGE₂ production but by the suppression of ROS production based on its inhibition of neutrophil activation.

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Section: Discussionsupporting

confidence: 58%

Effects of Diacerein on Indomethacin-Induced Gastric Ulceration

2001

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“…DAR has no inhibitory effect on phospholipase A2, cyclooxygenase, or 5-lipooxygenase in vitro. However, it is able to stimulate prostaglandin E2 synthesis in human chondrocyte cultures [8,9] and to inhibit the effects of IL-1 on chondrocytes [10,11]. Drug absorption from a dosage form after oral administration depends on the release of the drug from the pharmaceutical formulation, the dissolution and/or its solubilisation under physiological conditions, and the permeability across the gastrointestinal tract.…”

Section: Introductionmentioning

confidence: 99%

Development and Validation of a Dissolution Method with Spectrophotometric Analysis for Diacerhein Capsules

Borgmann¹,

Parcianello²,

Arend³

et al. 2008

Sci Pharm

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The aim of this work was to develop and validate a dissolution test for diacerhein in capsules using spectrophotometric method. The dissolution established conditions were: 900 mL of sodium phosphate buffer pH 7.0 with 0.75 % of sodium lauryl sulphate as dissolution medium, using a basket apparatus at a stirring rate of 50 rpm. The drug release was evaluated by UV spectrophotometric method at 258 nm. The method was validated to meet requirements for a global regulatory filing. The validation included specificity, linearity, precision and accuracy. In addition, filter suitability and drug stability in medium were demonstrated. The comparison of the obtained dissolution profiles of capsules, obtained from three different brands (denominate product A, B and C) of 50 mg diacerhein, was performed and the results showed no significative difference among the products.

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“…Diacetylrhein, in in-vivo experiments, and rhein, in in-vitro experiments, did not inhibit prostaglandin synthesis in inflammatory exudates and in guinea-pig lung homogenates that had been incubated with arachidonic acid and challenged with rhein in the concentration range 3.2 x 10-6-3.2 x 1 0 -4~ (Pomarelli et a1 1980;Franchi-Micheli et al 1983).…”

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confidence: 96%

Rhein: an anthraquinone that modulates superoxide anion production from human neutrophils

Mian

Brunelleschi

Tarli

et al. 1987

Journal of Pharmacy and Pharmacology

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Rhein (4,5-dihydroxyanthraquinone-2-carboxylic acid), the active metabolite of diacetylrhein, which has been reported as an effective antirheumatic drug in man, inhibited superoxide anion production from human neutrophils challenged with N-formylmethionyl-leucyl-phenylalanine (FMLP: IC50, 2 x 10(-5) M) and A23186 (IC50, 10(-5) M), but not with phorbol myristate acetate. In the same concentration range (10(-6)-10(-3) M), the drug did not affect oxy-radical production by a cell-free hypoxanthine-xanthine oxidase system and exerted weak inhibitory effects on FMLP-evoked lysosomal enzyme release. Rhein inhibitory effects on neutrophil functioning may contribute to the overall therapeutic activity of the parent drug, diacetylrhein.

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The influence of rhein on the biosynthesis of prostaglandin-like substances in-vitro

Cited by 42 publications

References 12 publications

Effects of Diacerein on Indomethacin-Induced Gastric Ulceration

Effects of Diacerein on Indomethacin-Induced Gastric Ulceration

Development and Validation of a Dissolution Method with Spectrophotometric Analysis for Diacerhein Capsules

Rhein: an anthraquinone that modulates superoxide anion production from human neutrophils

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