Abstract
The effects of rutin and rutin glycoside with different solubility were compared on antioxidant activity and anti-inflammatory effects in vitro and the effects on platelet aggregation and blood coagulation in vitro and in vivo. Rutin glycoside (consisting of rutin mono-glucoside and rutin di-glucoside) was prepared via enzymatic transglycosylation from rutin. Rutin glycoside showed a higher effect than rutin on radical scavenging activity in antioxidant assays. Rutin showed a higher toxicity than rutin glycoside in murine macrophage RAW264.7 cells. They had similar effects on the levels of nitric oxide (NO), prostaglandin E (PGE) 2 and pro-inflammatory cytokines (such as tumor necrosis factor (TNF)-α, and interleukin (IL)-6) in the cells. Both rutin and rutin glycosides similarly reduced the rate of platelet aggregation compared to controls in vitro. They also similarly delayed prothrombin time (PT) and activated partial thromboplastin time (APTT) in an in vitro blood coagulation test. The effect of repeated administration of rutin and rutin glycoside was evaluated in vivo using SD rats. The platelet aggregation rate of rutin and the rutin glycoside administered group was significantly decreased compared to that of the control group. On the other hand, PT and APTT of rutin and rutin glycoside group were not significantly delayed in vivo blood coagulation test. In conclusion, rutin and rutin glycoside showed differences in antioxidant activities in vitro, while they were similar in the reduction of NO, PGE2, TNF-α and IL-6 in vitro. Rutin and rutin glycoside also showed similar platelet aggregation rates, and blood coagulation both in vitro and in vivo condition. Comparing in vitro and in vivo, rutin and rutin glycoside were effective on platelet aggregation both in vitro and in vivo, but only in vitro on blood coagulation.
Highlights
Introduction published maps and institutional affilRutin (3,30,40,5,7-pentahydroxyflavone-3-rhamnoglucoside) is a flavonol, found abundantly in plants such as the flowers of pagoda tree, buckwheat seeds, tea and berries.Chemically, it is a glycoside composed of flavonol aglycone quercetin along with the disaccharide rhamnosyl glucose
Rutin was dissolved in water to final 10 and 40 mg/mL, Rutin glycoside was dissolved in water to final 13.9 and 55.6 mg/mL and the positive control for platelet aggregation, aspirin was mixed with 1% sodium carboxymethyl cellulose (CMC) to final 5 mg/mL
The platelet aggregation rate of aspirin, a platelet agcontrol group, it was confirmed that prothrombin time (PT) and activated partial thromboplastin time (APTT) of both rutin and rutin glycoside were gregation inhibitor [27,28] used as a positive control, was 0% on average
Summary
Β-amylase (Secura) were products ase (CGTase, and β-amylase were products of of Novozymes (Gladsaxe, Denmark). Dextrin with dextrose equivalent (DE) value 8–15 waswas a product of Sigma-Aldrich. (ABTS) were were purchased purchased from from Sigma-Aldrich ino-bis-(3-ethylbenzothiazoline-6-sulfonic. For a cell based assay, penicillin/streptomycin solution (FBS) and modified eagle’s(DMSO), mediumlipopolysaccharide (DMEM) were pur-(LPS). A nitric oxide (NO) detection was purchased products of. Detection kit from iNtRON Biotechnology (Seongnam, Korea) and an enzyme-linked immunosorbent was assay purchased from iNtRON. Biotechnology (Seongnam, Korea) and an enzyme-linked (ELISA) kit of prostaglandin E (PGE) 2 was purchased from Enzo Biochem. (St. Louis, MO, USA) and heparin (injection grade, 5000 IU/mL) was a product of JW Pharmaceutical corp. MO, USA) and heparin (injection grade, 5000 IU/mL) was a product of JW Pharmaceutical corp. (Seoul, Korea)
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