Pharmacological effects of selected flavonoids on rat isolated ileum: Structure-activity relationship

Hammad, Hana; Abdalla, Shtaywy

doi:10.1016/s0306-3623(96)00299-6

Cited by 55 publications

(39 citation statements)

References 23 publications

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“…It is widely accepted that flavonoids and tannins show gastroprotective effects against several necrotizing agents [3][4][5]. Another important activity of flavonoids is their ability to reduce small and large intestinal transit in mice [6,7], to cause intestinal smooth muscle relaxation [8] and to prevent castor oil-induced diarrhea [9]. These properties are consistent with the use of flavonoids as antidiarrheal drugs in traditional medicine.…”

Section: Introductionsupporting

confidence: 55%

Inhibition of Guinea Pig Intestinal Peristalsis by the Flavonoids Quercetin, Naringenin, Apigenin and Genistein

Gharzouli

Holzer

2003

Pharmacology

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Flavonoids are known to relax precontracted intestinal smooth muscle and to delay intestinal transit. We therefore investigated the effects of quercetin, naringenin, apigenin and genistein on intestinal peristalsis in vitro. Peristalsis in fluid-perfused segments of the guinea pig small intestine was recorded through the intraluminal pressure changes associated with the peristaltic waves. Alterations of distension sensitivity were reflected by changes in the peristaltic pressure threshold and alterations of peristaltic performance by changes in the maximal acceleration, amplitude and residual baseline pressure of the peristaltic waves. Quercetin, naringenin, apigenin and genistein (10–300 µmol/l) depressed intestinal peristalsis in a structure- and concentration-dependent manner. The flavonoid-evoked changes in peristalsis parameters made it possible to distinguish between two patterns of peristaltic motor inhibition: a decrease in distension sensitivity and peristaltic performance (apigenin and genistein) and a decrease in distension sensitivity without a major change in peristaltic performance (quercetin and naringenin). The antiperistaltic effect of quercetin was partially prevented by apamin (0.5 µmol/l), N-nitro-L-arginine methylester (100 µmol/l) and naloxone (0.5 µmol/l), whereas the effect of genistein was hardly affected by these drugs. Peristaltic motor activity suppressed by quercetin (300 µmol/l), but not genistein (100 µmol/l), was partially restored by apamin. In contrast, neostigmine (0.3 µmol/l) caused a significant recovery of peristalsis from blockade by genistein but failed to reverse peristaltic motor blockade due to quercetin. These observations suggest that naringenin and quercetin inhibit peristalsis by facilitating inhibitory enteric pathways, whereas apigenin and genistein interfere with muscle excitation or excitation-contraction coupling.

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Section: Introductionsupporting

confidence: 55%

Inhibition of Guinea Pig Intestinal Peristalsis by the Flavonoids Quercetin, Naringenin, Apigenin and Genistein

Gharzouli

Holzer

2003

Pharmacology

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“…8,31) Structure-activity relationships of flavonoids have been proposed for the antioxidant and the antispasmodic effects. 31) Due to the presence of different substituents on the carbon atoms of the basic skeleton, flavonoids may have different activities and potencies.…”

Section: Fig 1 Effects Of Flavonoids On Liver Uric Acid Levelsmentioning

confidence: 99%

“…Allopurinol, an XOD inhibitor which is structurally related to xanthine, binds tightly to the active site of XOD thus causes inhibition on XOD. Allopurinol is used to treat gout for more than 40 years and remains a cornerstone in the therapy of primary and secondary hyperuricemia.2-7) However, the most common adverse effects of allopurinol are gastrointestinal distress, hypersensitivity reactions, 8) and renal toxicity. …”

mentioning

confidence: 99%

Hypouricemic Action of Selected Flavonoids in Mice: Structure-Activity Relationships

Zhou

et al. 2007

Biological & Pharmaceutical Bulletin

154

104

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Gout occurs in individuals who have high serum uric acid levels, in response to precipitation of monosodium urate monohydrate crystals in various tissues, followed by an inflammatory response. 1) The essence of the prevention and treatment of gout is antihyperuricemic therapy, either by uricosuric drugs or by xanthine oxidase (XOD) inhibitors. Allopurinol, an XOD inhibitor which is structurally related to xanthine, binds tightly to the active site of XOD thus causes inhibition on XOD. Allopurinol is used to treat gout for more than 40 years and remains a cornerstone in the therapy of primary and secondary hyperuricemia. 2-7) However, the most common adverse effects of allopurinol are gastrointestinal distress, hypersensitivity reactions, 8) and renal toxicity. 9) Thus, new alternatives with an increased therapeutic activity and less side effects are desired.Dietary flavonoids have been attracted attention because of their potential beneficial effects on human health. The structural components common to these molecules include two benzene rings on either side of a 3-carbon ring (Table 1). 10) Multiple combinations of hydroxyl groups, sugars, oxygens, and methyl groups attached to these structures create the various classes of flavonoids: flavanols, flavanones, flavones, flavanonol, flavan-3-ols (catechins), anthocyanins, and isoflavones. 11) Flavonoids are well known to possess antiviral, antiallergic, antiplatelet, antiinflammatory, antitumor and antioxidant activities. 12-15) Catechin and its derivatives, oligomeric proanthocyanidins, quercetin and quercetin chalcone, Ginkgo flavone glycosides, silymarin, and others can be utilized in preventative and treatment protocols for cardiovascular disease, cancer, inflammatory conditions, asthma, periodontal disease, liver disease, cataracts and macular degeneration. 16,17) Hyperuricemia is a risk factor for the disorder metabolic syndrome and increased cardiovascular disease, and the mechanisms involve inflammation and generation of oxidative stress in the vasculature. 18) Thus, the antiinflammatory and antioxidant activities of flavonoids might bring benefit for hyperuricemia and its complications. In addition, the flavonoids have increasingly aroused interest recently for their hypouricemic action in hyperuricemic animal models. [19][20][21] In the present study, we have explored hypouricemic actions from 15 flavonoids including quercetin, morin, myricetin, kaempferol, icariin, apigenin, luteolin, baicalin, silibinin, naringenin, formonoetin, genistein, puerarin, daidzin and naringin dihydrochalcone in a hyperuricemic animal model induced by potassium oxonate. We have also studied the effects of six most active compounds on serum and liver uric acid levels in normal mice. The effects on liver XOD activities were further examined in animals. MATERIALS AND METHODSMaterials Quercetin, morin, myricetin, kaempferol, icariin, apigenin, luteolin, baicalin, silibinin, naringenin, formonoetin, genistein, puerarin, daidzin and naringin dihydrochalcone were obtained commerci...

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“…In the present study, the hypothesis tested was that one antioxidant (the flavonoid galangin) would have the capacity to avoid tissue damage induced by oxidative stress in the detrusor cells of guinea pigs. Galangin was chosen from among other flavonoids because it has been demonstrated to be one of the flavonoids with greatest relaxant power of smooth musculature (14). Furthermore, galangin is the most lipophilic of the flavonoids, which makes it appropriate for intravesical use due to the facility with which it penetrates the barrier formed by bladder mucosa (15).…”

Section: Discussionmentioning

confidence: 99%

Influence of oxidative stress on inducing micturition dysfunction following chronic infravesical obstruction and the protective role of an antioxidant diet - association of in vivo and in vitro studies in rats

Bisogni¹,

Ferreira

Neto

et al. 2012

Int. braz j urol.

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ARTIcLE INFO _________________________________________________________ ___________________Objective: This study was developed to determine whether the generation of free radicals, induced by ischemia followed by reperfusion in a model of chronic intravesical obstruction in rats, would lead to damage in the detrusor. It also investigates the possible protective action of the flavonoid galangin on the tissue lesion induced by lipid peroxidation. Materials and Methods: Twenty-one male rats were divided into three groups of seven animals each. Group A was subjected to a sham procedure; group B to partial obstruction of the bladder neck; and group C to partial obstruction of the bladder neck, but also received a diet rich in the flavonoid galangin. All the animals were subjected to urodynamic evaluation and then sacrificed. The bladders were sent for enzymatic tests. Results:The urodynamic showed that group B developed significantly greater numbers of involuntary contractions of the detrusor, greater post-micturition residue and lower compliance. The group A presented TEAC levels greater than to the group B. Comparative analysis of group A, B and C demonstrated significantly greater malondialdehyde levels in group B in relation to groups A and C. The group B presented smaller contraction amplitudes than did groups A and C, in electrically stimulated contractions. Conclusions: That oxidative stress is implicated in the damage to the detrusor musculature following a period of chronic intravesical obstruction. We show, for the first time, that administration of an antioxidant prior to and following the start of chronic obstruction makes it possible to avoid the cellular lesions that cause detrusor dysfunction.

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Pharmacological effects of selected flavonoids on rat isolated ileum: Structure-activity relationship

Cited by 55 publications

References 23 publications

Inhibition of Guinea Pig Intestinal Peristalsis by the Flavonoids Quercetin, Naringenin, Apigenin and Genistein

Inhibition of Guinea Pig Intestinal Peristalsis by the Flavonoids Quercetin, Naringenin, Apigenin and Genistein

Hypouricemic Action of Selected Flavonoids in Mice: Structure-Activity Relationships

Influence of oxidative stress on inducing micturition dysfunction following chronic infravesical obstruction and the protective role of an antioxidant diet - association of in vivo and in vitro studies in rats

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