Effects of molecular size and chemical structure on renal and hepatic removal of exogenously administered chondroitin sulfate in rats

Pecly, Inah Maria Drummond; Melo-Filho, Nelson M.; Mourāo, Paulo A.S.

doi:10.1016/j.bbagen.2005.11.009

Cited by 17 publications

(6 citation statements)

References 38 publications

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“…49) Absorbed CHS reaching the plasma compartment can be taken up rapidly by the liver cells, where polysaccharides are recovered in rats. 50) In the present study, we proved that CHS isolated from sea cucumber, with a structure different from CHS from other species, decreased blood glucose levels through promotion of hepatic glycogen synthesis, which have to do with the micromolecular metabolite of CHS after digestion of relevant enzymes in the intestine. Hence we intend to investigate the bioavailability of CHS with a specific structure after administration.…”

Section: Discussionmentioning

confidence: 83%

Fucosylated Chondroitin Sulfate from Sea Cucumber in Combination with Rosiglitazone Improved Glucose Metabolism in the Liver of the Insulin-Resistant Mice

Chang

Wang

et al. 2013

Bioscience, Biotechnology, and Biochemistry

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Section: Discussionmentioning

confidence: 83%

Fucosylated Chondroitin Sulfate from Sea Cucumber in Combination with Rosiglitazone Improved Glucose Metabolism in the Liver of the Insulin-Resistant Mice

Chang

Wang

et al. 2013

Bioscience, Biotechnology, and Biochemistry

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“…Considering that CS is eliminated by hepatic metabolism and urinary excretion generally with a half-life of several dozen min-a few h in human and animals, [21][22][23] CS-GP was considered to be concentrated well in the systemic circulation. Thus, it could be proposed that the high distribution of CS-GP in the systemic circulation should promote the localization of PD at the inflamed tissue due to the enhanced permeability and retention (EPR) effect.…”

Section: Pharmacokinetics After IV Injection In Rats With Adjuvant-mentioning

confidence: 99%

Chondroitin Sulfate–Glycyl-Prednisolone Conjugate as Arthritis Targeting System: Localization and Drug Release in Inflammatory Joints

Onishi

Yoshida

Matsuyama

2014

Biological & Pharmaceutical Bulletin

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Chondroitin sulfate-glycyl-prednisolone conjugate (CS-GP) was previously demonstrated to exhibit superior anti-arthritic effects compared to prednisolone (PD) alone. In this study, CS-GP was examined for its pharmacokinetic features and tropism for inflammatory joints using rats with adjuvant-induced arthritis in order to identify the mechanism of the potential enhancement. After intravenous injection (2.5 mg PD eq./ kg), CS-GP yielded an area under the curve (AUC) of the total (free conjugated) drug much higher than that of PD alone. After intravenous administration at the same dose, the drug distribution to the hind paw inflammatory joints was investigated. For PD alone, the PD concentration was 1.2-1.7 µg/g at 1 h and fell to 0.12-0.14 µg/g at 24 h. In contrast, CS-GP maintained the total concentration in the range of 0.55-0.97 µg/g for 1-24 h, and maintained the free PD concentration at 0.06-0.16 µg/g for 1-24 h. Furthermore, at 24 h after intravenous administration (2.5 mg PD eq./kg), CS-GP exhibited a higher total drug concentration in arthritic rats than in healthy rats. These findings suggested that CS-GP may have the ability to target inflammatory joints. As the apparent molecular weight of CS-GP became greater in plasma, it might interact with blood components and cause high plasma retention and good tropism to the inflammatory sites. Enhancement of the anti-inflammatory potential of CS-GP was found to be due to good maintenance of drug levels in the inflamed area.

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“…43 And absorbed CHS reaching the plasma compartment may be rapidly taken up in experimental rats. 44 In our study, we proved that CHS isolated from sea cucumber, with a specic structure distinguished from other species, could decrease blood glucose level. It might be concerned with the micromolecular metabolite of CHS aer digestion of relevant enzymes in the intestine.…”

Section: Discussionmentioning

confidence: 51%

Fucosylated chondroitin sulfate from Acaudina molpadioides improves hyperglycemia via activation of PKB/GLUT4 signaling in skeletal muscle of insulin resistant mice

Chang

Wang

et al. 2013

Food Funct.

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In this study, we investigated the improvement of fucosylated chondroitin sulfate (CHS) from the cucumber Acaudina molpadioides on hyperglycemia in skeletal muscle of insulin resistant mice. CHS, rosiglitazone (RSG), and their combinations were supplemented to high-fat high-sucrose diet (HFSD)-fed C57BL/6J mice for 19 weeks. The results showed that CHS treatment remarkably decreased blood glucose level and insulin resistance. The glucose metabolism-related genes expressions at the transcriptional level were apparently increased in skeletal muscle. Although the total protein expressions of IR-β, IRS-1, PI3K, PKB and GLUT4 in skeletal muscle were not affected, insulin-stimulated GLUT4 translocation and phosphorylation of Tyr-IR-β, Tyr612-IRS-1, p85-PI3K, Ser473-PKB, and Thr308-PKB were significantly increased by CHS supplement. Additionally, combination of CHS and RSG produced synergistic effects on anti-hyperglycemia. These results indicate that CHS can alleviate hyperglycemia via activation of the PKB/GLUT4 signaling pathway in skeletal muscle of insulin resistant mice.

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Effects of molecular size and chemical structure on renal and hepatic removal of exogenously administered chondroitin sulfate in rats

Cited by 17 publications

References 38 publications

Fucosylated Chondroitin Sulfate from Sea Cucumber in Combination with Rosiglitazone Improved Glucose Metabolism in the Liver of the Insulin-Resistant Mice

Fucosylated Chondroitin Sulfate from Sea Cucumber in Combination with Rosiglitazone Improved Glucose Metabolism in the Liver of the Insulin-Resistant Mice

Chondroitin Sulfate–Glycyl-Prednisolone Conjugate as Arthritis Targeting System: Localization and Drug Release in Inflammatory Joints

Fucosylated chondroitin sulfate from Acaudina molpadioides improves hyperglycemia via activation of PKB/GLUT4 signaling in skeletal muscle of insulin resistant mice

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