Pharmacokinetic studies of diosmin and diosmetin in perfused rat liver

Perego, Rita; Beccaglia, Patrizia; Angelini, M; Villa, Pia; Cova, D.

doi:10.3109/00498259309059444

Cited by 13 publications

(5 citation statements)

References 18 publications

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“…Diosmin and diosmetin have been shown in other studies to be rapidly metabolized in perfused rat liver, and excreted in the bile as glucuronide and sulfate conjugates [135]. Boutin et al [136] found no free diosmetin in the blood or urine following 100 mg Kg -1 diosmin administration to rat.…”

Section: Metabolismmentioning

confidence: 97%

Biological Properties of Citrus Flavonoids Pertaining to Cancer and Inflammation

Manthey¹,

Guthrie²,

Grohmann³

2001

CMC

494

312

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Citrus flavonoids encompass a diverse set of structures, including numerous flavanone and flavone O- and C-glycosides and methoxylated flavones. Each of these groups of compounds exhibits a number of in vitro and in vivo anti-inflammatory and anticancer actions. These biological properties are consistent with their effects on the microvascular endothelial tissue. Evidence suggests that the biological actions of the citrus flavonoids are possibly linked to their interactions with key regulatory enzymes involved in cell activation and receptor binding. The citrus flavonoids show little effect on normal, healthy cells, and thus typically exhibit remarkably low toxicity in animals. The citrus flavonoids extend their influence in vivo through their induction of hepatic phase I and II enzymes, and through the biological actions of their metabolites. Evidence clearly indicates to the potential health promoting properties of these dietary compounds.

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Section: Metabolismmentioning

confidence: 97%

Biological Properties of Citrus Flavonoids Pertaining to Cancer and Inflammation

Manthey¹,

Guthrie²,

Grohmann³

2001

CMC

494

312

View full text Add to dashboard Cite

show abstract

“…In Europe, it is prescribed for treatment of venous insufficiency while in the US, it is marketed as a food supplement [60,61]. A study in rat liver perfusate showed that diosmin was mainly excreted in the bile as a glucuronide conjugate [62]. Glucuronides of diosmetin (diosmin aglycone) were detected on the apical side of Caco-2 cell culture [61].…”

Section: Diosminmentioning

confidence: 99%

Effects of Herbal Supplements on Drug Glucuronidation. Review of Clinical, Animal, andIn VitroStudies

Mohamed

Frye

2010

Planta Med

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“…Most flavonoid glycosides are deglycosylated by β-glucosidases in the small intestine; subsequently, the polyphenols are found in the blood as conjugates, glucuronate or sulfate, with or without methylation of the B-ring catechol functional group . According to several authors, the diosmin is metabolized by bacterial flora to form an aglycone, diosmetin, which is then metabolized to form glucuronides and sulfate, the major metabolite , . As in the case of diosmin, the first metabolite formed with rutin is the aglycone quercetin.…”

Section: Anticarcinogenic Propertiesmentioning

confidence: 99%

Update on Uses and Properties of Citrus Flavonoids: New Findings in Anticancer, Cardiovascular, and Anti-inflammatory Activity

Benavente-García

Castillo

2008

J. Agric. Food Chem.

989

575

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Significantly, much of the activity of Citrus flavonoids appears to impact blood and microvascular endothelial cells, and it is not surprising that the two main areas of research on the biological actions of Citrus flavonoids have been inflammation and cancer. Epidemiological and animal studies point to a possible protective effect of flavonoids against cardiovascular diseases and some types of cancer. Although flavonoids have been studied for about 50 years, the cellular mechanisms involved in their biological action are still not completely known. Many of the pharmacological properties of Citrus flavonoids can be linked to the abilities of these compounds to inhibit enzymes involved in cell activation. Attempts to control cancer involve a variety of means, including the use of suppressing, blocking, and transforming agents. Suppressing agents prevent the formation of new cancers from procarcinogens, and blocking agents prevent carcinogenic compounds from reaching critical initiation sites, while transformation agents act to facilitate the metabolism of carcinogenic components into less toxic materials or prevent their biological actions. Flavonoids can act as all three types of agent. Many epidemiological studies have shown that regular flavonoid intake is associated with a reduced risk of cardiovascular diseases. In coronary heart disease, the protective effects of flavonoids include mainly antithrombotic, anti-ischemic, anti-oxidant, and vasorelaxant. It is suggested that flavonoids decrease the risk of coronary heart disease by three major actions: improving coronary vasodilatation, decreasing the ability of platelets in the blood to clot, and preventing low-density lipoproteins (LDLs) from oxidizing. The anti-inflammatory properties of the Citrus flavonoids have also been studied. Several key studies have shown that the anti-inflammatory properties of Citrus flavonoids are due to its inhibition of the synthesis and biological activities of different pro-inflammatory mediators, mainly the arachidonic acid derivatives, prostaglandins E 2, F 2, and thromboxane A 2. The anti-oxidant and anti-inflammatory properties of Citrus flavonoids can play a key role in their activity against several degenerative diseases and particularly brain diseases. The most abundant Citrus flavonoids are flavanones, such as hesperidin, naringin, or neohesperidin. However, generally, the flavones, such as diosmin, apigenin, or luteolin, exhibit higher biological activity, even though they occur in much lower concentrations. Diosmin and rutin have a demonstrated activity as a venotonic agent and are present in several pharmaceutical products. Apigenin and their glucosides have been shown a good anti-inflammatory activity without the side effects of other anti-inflammatory products. In this paper, we discuss the relation between each structural factor of Citrus flavonoids and the anticancer, anti-inflammatory, and cardiovascular protection activity of Citrus flavonoids and their role in degenerative diseases.

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Pharmacokinetic studies of diosmin and diosmetin in perfused rat liver

Cited by 13 publications

References 18 publications

Biological Properties of Citrus Flavonoids Pertaining to Cancer and Inflammation

Biological Properties of Citrus Flavonoids Pertaining to Cancer and Inflammation

Effects of Herbal Supplements on Drug Glucuronidation. Review of Clinical, Animal, andIn VitroStudies

Update on Uses and Properties of Citrus Flavonoids: New Findings in Anticancer, Cardiovascular, and Anti-inflammatory Activity

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