Grapefruit juice potentiates the anti-inflammatory effects of diclofenac on the carrageenan-induced rat’s paw oedema

Mahgoub, Afaf A.

doi:10.1006/phrs.2001.0856

Cited by 36 publications

(28 citation statements)

References 26 publications

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“…It reduces inflammation, swelling, and arthritic pain by inhibiting prostaglandin synthesis and/or production (Skoutakis et al, 1988;Todd & Sorkin, 1988;Small, 1989). The drug also affects polymorphonuclear leukocyte function in vitro, thereby reducing chemotaxis, superoxide toxic radical formation, oxygen-derived free radical generation, and neutral protease production (Freeman et al, 1986;Mahgoub, 2002). Diclofenac has also been reported to suppress inflammation induced by various phlogistic agents in experimental animal models (Menasse et al, 1978;Freeman et al, 1986;Al-Tuwaijri & Mustafa, 1992).…”

Section: Resultsmentioning

confidence: 99%

Antinociceptive and anti-inflammatory properties ofRuellia tuberosa

Alam¹,

Subhan²,

Awal³

et al. 2009

Pharmaceutical Biology

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Section: Resultsmentioning

confidence: 99%

Antinociceptive and anti-inflammatory properties ofRuellia tuberosa

Alam¹,

Subhan²,

Awal³

et al. 2009

Pharmaceutical Biology

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“…Diclofenac reduces inflammation, swelling and arthritic pain by inhibiting prostaglandins synthesis and/or production (Todd and Sorkin, 1988;Skoutakis et al, 1988;Mahgoub, 2002). The drug also affects polymorphonuclear leukocytes function in vitro, thereby reducing chemotaxis, superoxide toxic radical formation, oxygen-derived free radical generation, and neutral protease production (Freeman et al, 1986; Mahgoub, 2002). Diclofenac has also been reported to suppress inflammation induced by various phlogistic agents in experimental animal models (Menasse et al, 1978;Al-Tuwaijri and Mustafa, 1992;Mahgoub, 2002).…”

Section: Discussionmentioning

confidence: 95%

“…Diclofenac, a non-steroidal antiinflammatory drug (NSAID), is commonly employed in the treatment and/or management of rheumatoid arthritis, osteo-arthritis and ankylosing spondylitis (Siraux, 1977;Brooks et al, 1980;Sigmeth and Sieberer, 1980) for its anti-inflammatory and analgesic effects (Small, 1989). Diclofenac reduces inflammation, swelling and arthritic pain by inhibiting prostaglandins synthesis and/or production (Todd and Sorkin, 1988;Skoutakis et al, 1988;Mahgoub, 2002). The drug also affects polymorphonuclear leukocytes function in vitro, thereby reducing chemotaxis, superoxide toxic radical formation, oxygen-derived free radical generation, and neutral protease production (Freeman et al, 1986; Mahgoub, 2002).…”

Section: Discussionmentioning

confidence: 98%

Evaluation of the analgesic, anti‐inﬂammatory and anti‐diabetic properties of Sclerocarya birrea (A. Rich.) Hochst. stem‐bark aqueous extract in mice and rats

Ojewole

2004

Phytotherapy Research

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In order to appraise some of the ethnomedical uses of Sclerocarya birrea (A. Rich.) Hochst., subspecies caffra (Sond.) Kokwaro [family: Anacardiaceae], the present study was undertaken to investigate the analgesic, anti-inflammatory and anti-diabetic properties of the plant's stem-bark aqueous extract in experimental models of pain, inflammation and diabetes mellitus. The analgesic effect of Sclerocarya birrea stem-bark aqueous extract was evaluated in mice, while its anti-inflammatory and anti-diabetic effects were investigated in rats. Diclofenac (DIC, 100 mg/kg p. o.) and chlorpropamide (250 mg/kg p. o.) were used respectively as reference analgesic, anti-inflammatory and anti-diabetic agents for comparison. Like diclofenac (DIC, 100 mg/kg p. o.), Sclerocarya birrea stem-bark aqueous extract (SBE, 100-800 mg/kg p. o.) produced dose-dependent, significant protection (p < 0.05-0.001) against electrical heat-induced pain. The plant extract (SBE, 25-800 mg/kg p. o.) also produced dose- and time-related, sustained and significant reductions (p < 0.05-0.001) in the fresh egg albumin-induced acute inflammation of the rat hind paw oedema. However, the analgesic and anti-inflammatory effects of the plant's extract were found to be approximately 10-15 times less than that of diclofenac. In one set of experiments involving hypoglycaemic/antidiabetic evaluation of the plant's extract, graded doses of Sclerocarya birrea stem-bark aqueous extract (SBE, 25-800 mg/kg p. o.) were separately administered to groups of fasted normal and fasted diabetic rats. In another set of experiments, a single dose of the plant's aqueous extract (SBE, 800 mg/kg p. o.) was used. The hypoglycaemic effect of this single dose of Sclerocarya birrea stem-bark aqueous extract (SBE, 800 mg/kg p. o.) was compared with that of chlorpropamide (250 mg/kg p. o.) in both fasted normal and fasted streptozotocin (STZ)-treated diabetic rats. Following acute treatment, relatively moderate to high doses of Sclerocarya birrea stem-bark aqueous extract (SBE, 25-800 mg/kg p. o.) produced dose-dependent, significant reductions (p < 0.05-0.001) in the blood glucose concentrations of both fasted normal and fasted diabetic rats. Chlorpropamide (250 mg/kg p. o.) also produced significant reductions (p < 0.05-0.001) in the blood glucose concentrations of the fasted normal and fasted diabetic rats. Administration of the single dose of Sclerocarya birrea stem-bark aqueous extract (SBE, 800 mg/kg p. o.) significantly reduced (p < 0.01-0.001) the blood glucose levels of both fasted normal (normoglycaemic) and fasted STZ-treated, diabetic rats. The results of this experimental animal study indicate that Sclerocarya birrea stem-bark aqueous extract possesses analgesic, anti-inflammatory and hypoglycaemic properties. These experimental findings lend pharmacological support to the suggested folkloric uses of the plant's stem-bark in the management and/or control of pain, inflammatory conditions, and adult-onset, type-2 diabetes mellitus in some communities of South Africa.

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“…Therefore, oral consumption of GFJ would not affect the systemic therapeutic efficacy of DCF, while reducing DCF's side effects in the gut. Indeed, GFJ has been found to potentiate the anti-inflammatory effects of DCF on carrageenan-induced paw edema in rats (Mahgoub, 2002); that result was proposed by the authors to be caused by the inhibition of P450-mediated DCF clearance by GFJ, although the effect of GFJ on DCF pharmacokinetics was not studied.…”

Section: Discussionmentioning

confidence: 99%

Role of Intestinal Cytochrome P450 Enzymes in Diclofenac-Induced Toxicity in the Small Intestine

Zhu¹

2012

J Pharmacol Exp Ther

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The aim of this study was to determine the role of small intestinal (SI) cytochrome P450 (P450) enzymes in the metabolic activation of diclofenac (DCF), a widely used nonsteroidal antiinflammatory drug, and DCF-induced intestinal toxicity. DCF induces intestinal ulcers in humans and mice, but the underlying mechanisms, including the necessity for drug bioactivation in the target tissues and the sources and identities of reactive intermediates, are not fully understood. We found that the number of DCF-induced (at 50 mg/kg p.o.) intestinal ulcers was significantly smaller in an intestinal epithelium (IE)-specific P450 reductase (CPR) knockout (IE-Cpr-null) mouse model, which has little P450 activity in the IE, than in wild-type (WT) mice, determined at 14 h after DCF administration. The involvement of intestinal P450 enzymes was confirmed by large reductions (Ͼ80 -90%) in the rates of in vitro formation, in SI microsomal reactions, of hydroxylated DCF metabolites and reactive intermediates, trapped as DCFglutathione (GSH) conjugates, in the IE-Cpr-null, compared with WT mice. The SI levels of DCF-GSH conjugates (at 4 h after dosing) and DCF-protein adducts (at 14 h after dosing) were significantly lower in IE-Cpr-null than in WT mice. In additional experiments, we found that pretreatment of mice with grapefruit juice, which is known to inhibit SI P450 activity, ameliorated DCF-induced intestinal toxicity in WT mice. Our results not only strongly support the notion that SI P450 enzymes play an important role in DCF-induced intestinal toxicity, but also illustrate the possibility of preventing DCF-induced intestinal toxicity through dietary intervention.

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Grapefruit juice potentiates the anti-inflammatory effects of diclofenac on the carrageenan-induced rat’s paw oedema

Cited by 36 publications

References 26 publications

Antinociceptive and anti-inflammatory properties ofRuellia tuberosa

Antinociceptive and anti-inflammatory properties ofRuellia tuberosa

Evaluation of the analgesic, anti‐inﬂammatory and anti‐diabetic properties of Sclerocarya birrea (A. Rich.) Hochst. stem‐bark aqueous extract in mice and rats

Role of Intestinal Cytochrome P450 Enzymes in Diclofenac-Induced Toxicity in the Small Intestine

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