Anti-Inflammatory Activity of Diosmin and Hesperidin in Rat Colitis Induced by TNBS

Crespo, M. E.; Gálvez, Júlio; Cruz, T.; Ocete, M. A.; Zarzuelo, Antonio

doi:10.1055/s-2006-960838

Cited by 148 publications

(81 citation statements)

References 9 publications

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“…Several poliphenolic compounds, particularly flavonoids, also shown non dose-dependent response in TNBS model of rat colitis, probably due to produce in lower doses antioxidant effects and higher doses pro-oxidant effects. 13,37,[40][41][42] In addition, several phenols have a dual effect on prostaglandin H synthase, with low concentrations stimulating and high concentrations inhibiting this enzyme. 43) Phenols stimulate prostaglandin H synthase by acting as reducing substrates for the oxidized intermediates of prostaglandin biosynthesis, thereby accelerating the peroxidase cycle and by functioning as electron-donating cosubstrates for the peroxidase component of prostaglandin synthase.…”

Section: Discussionmentioning

confidence: 99%

Intestinal Anti-inflammatory Activity of Coumarin and 4-Hydroxycoumarin in the Trinitrobenzenesulphonic Acid Model of Rat Colitis

Luchini

Rodrigues-Orsi

Cestari

et al. 2008

Biological & Pharmaceutical Bulletin

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Coumarins represent an important class of phenolic compounds with multiple biological activities, including inhibition of lipidic peroxidation and neutrophil-dependent anion superoxide generation, anti-inflammatory and immunosuppressor actions. All of these proprieties are essential for that a drug may be used in the treatment of inflammatory bowel disease. The present study examined intestinal anti-inflammatory activity of coumarin and its derivative, the 4-hydroxycoumarin on experimental ulcerative colitis in rats. This was performed in two different experimental settings, i.e. when the colonic mucosa is intact or when the mucosa is in process of recovery after an initial insult. The results obtained revealed that the coumarin and 4-hydroxycoumarin, at doses of 5 and 25 mg/kg, significantly attenuated the colonic damage induced by trinitrobenzenesulphonic acid (TNBS) in both situations, as evidenced macroscopically, microscopically and biochemically. This effect was related to an improvement in the colonic oxidative status, since coumarin and 4-hydroxycoumarin prevented the glutathione depletion that occurred as a consequence of the colonic inflammation.

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Section: Discussionmentioning

confidence: 99%

Intestinal Anti-inflammatory Activity of Coumarin and 4-Hydroxycoumarin in the Trinitrobenzenesulphonic Acid Model of Rat Colitis

Luchini

Rodrigues-Orsi

Cestari

et al. 2008

Biological & Pharmaceutical Bulletin

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“…Hesperidin and naringin are the main flavanone glycosides naturally occurring in citrus fruits (Rouseff et al, 1987;Kanaze et al, 2003). They exert antioxidant (RiceEvans et al, 1996;Miyake et al, 1998;Franke et al, 2005), anti-inflammatory (Crespo et al, 1999), blood lipid and cholesterol-lowering (Montforte et al, 1995;Bok et al, 1999;Lee et al, 1999;Santos et al, 1999) and anticarcinogenic activities Yang et al, 1997;Berkarda et al, 1998). Epidemiological studies indicate an association between the intake of citrus fruits and juices and the risk of ischemic stroke (Joshipura et al, 1999).…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of the citrus flavanone aglycones hesperetin and naringenin after single oral administration in human subjects

et al. 2006

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Background and objective: Hesperetin and naringenin, the aglycones of the flavanone glycosides hesperidin and naringin, occur naturally in citrus fruits. They exert interesting pharmacological properties such as antioxidant, anti-inflammatory, blood lipid and cholesterol lowering and are considered to contribute to health benefits in humans. However, no information is available on the pharmacokinetics of the citrus flavanones hesperetin and naringenin after their oral administration to humans as pure aglycones. Therefore, the objective of the present investigation was the evaluation of the pharmacokinetic parameters of hesperetin and naringenin in plasma and urine, after their single oral administration in humans in the form of solid dispersion capsules, and also to improve the absorption rate of flavanones by using aglycones rather than the naturally occurring glycosides. Design: Six healthy volunteers received orally 135 mg of each compound, hesperetin and naringenin, under fasting conditions. Blood samples were collected at 14 different time points over a 12 h period. Urine was collected over 24 h, in five sequential timed intervals. Plasma and urine hesperetin and naringenin concentrations, after enzymatic hydrolysis of their conjugated forms, were measured using validated high-pressure liquid chromatography methods. Pharmacokinetic parameters for hesperetin and naringenin, such as C max , T max , AUC 0Àt , AUC 0ÀN , CL/F, V/F, t 1/2 , MRT, A e , A e ( 0-24 ), and R max were calculated from their plasma or urine concentrations. Results: Pharmacokinetic analysis showed that both hesperetin and naringenin were rapidly absorbed and their concentrations in plasma observed 20 min after dosing and reached a peak in 4.0 and 3.5 h, respectively. The mean peak plasma concentration (C max ) for hesperetin and naringenin were 825.787410.63 ng/ml (2731.871358.4 nmol/l) and 2009.517770.82 ng/ml (7386.672833.4 nmol/l), respectively and the mean AUC 0ÀN values were 4846.2071675.99 ng h/ml and 9424.527 2960.52 ng h/ml for hesperetin and naringenin, respectively. The elimination half-life for hesperetin was found to be 3.0570.91 h and for naringenin 2.3170.40 h, respectively. The mean values of the relative cumulative urinary excretion, as percentage of the administered dose, for hesperetin and naringenin, were found to be 3.2670.44 and 5.8170.81%, respectively. Conclusions: Oral administration of the flavanone aglycones, hesperetin and naringenin, lead to their rapid absorption as their conjugated forms. The cumulative urinary recovery data indicated low bioavailability for both flavanone aglycones, owing to extensive first-pass metabolism partly by cleavage of the C-ring by the enzymes of intestinal bacteria leading to degradation products such as phenolic acids.

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“…it is a flavonoid glycoside which is isolated from citrus plant [1]. Hesperidin has been proven to have anti-inflammation, antimicrobial, antioxidant, anti-hemorrhoid, and anticancer activity so it could be used in therapy of some colon related diseases such as hemorrhoid, chronic vein insufficiency, colon cancer, and ulcerative colitis [1][2][3][4][5][6], however, hesperidin has low solubility on digestive tract (<100 mg/l) as well as low bioavailability (<25%) [1,7]. Therefore, the correct delivery system is required to increase the bioavailability and therapy effectiveness from hesperidin, one of them is by formulating it into a hydrogel.…”

Section: Introductionmentioning

confidence: 99%

Hesperidin Hydrogel Formulation Using Pectin-Chitosan Polymer Combination

Fahrurroji

Thendriani

Riza

2017

Int J Pharm Pharm Sci

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Objective: Hesperidin, a flavonoid glycosides that have been proven to have therapeutic activity to some disease, one of them is colon disease; in addition of its efficacy,low solubility(<100 mg/l) makes hesperidin slightly absorbed,hence it needs a delivery system which could deliver hesperidin to its therapeutic target. This research aims to obtain an optimum formula for pectin polymer combination which can regulate in vitro hesperidin release. Methods:Determination of optimum hydrogel formula uses Design Expert 7.0.0 with factorial method design, resulting in pectin-chitosan concentration formula plan-comparison, which are (P3%: C1%), (P3%: C2%), (P5%: C1%), (P5%: C2%) respectively. Hydrogel was obtained from a variety of formulas,then evaluation of the entrapment efficiency test, swelling index, in vitro drug release test, mucoadhesive strength were conducted.Results: Optimum formula with: pectin: chitosan concentration comparison (5: %: 1%) have an entrapment efficiency of 96.658%; k (/hour) swelling index at pH 5.0, 6.8, and 7.4, was 34.917, 15.766, and 8.146 respectively; drug release at pH 5.0, 6.8, and a medium contained 2% rat caecum was 0.461, 20.116, and the mucoadhesive strength was 0.184 N/cm 2 Conclusion: Combination of pectin-chitosan polymer in hydrogel mucoadhesive regulates hesperidin shesperidin in vitro release, with highest drug release in medium containing 2% rats caecum which releases 56% of active substance. Hesperidin hydrogel release mechanism follows Higuchi kinetics. The optimum hesperidin hydrogel formula is the formula with 5% of pectin and 1% of chitosan. Based on experimental data value which uses simplex lattice design, optimum hesperidin hydrogel formula has insignificant difference between observed and predicted value (p value>0.05).. Based on the test result using independent t-test sample, actual and prediction value from every test parameter produced by the optimum formula was not significantly different with p-value>0,05.

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Anti-Inflammatory Activity of Diosmin and Hesperidin in Rat Colitis Induced by TNBS

Cited by 148 publications

References 9 publications

Intestinal Anti-inflammatory Activity of Coumarin and 4-Hydroxycoumarin in the Trinitrobenzenesulphonic Acid Model of Rat Colitis

Intestinal Anti-inflammatory Activity of Coumarin and 4-Hydroxycoumarin in the Trinitrobenzenesulphonic Acid Model of Rat Colitis

Pharmacokinetics of the citrus flavanone aglycones hesperetin and naringenin after single oral administration in human subjects

Hesperidin Hydrogel Formulation Using Pectin-Chitosan Polymer Combination

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