Oral Absorption and Clearance of Partially Depolymerized Fucosyl Chondroitin Sulfate from Sea Cucumber

Imanari, Toshio; Washio, Yukio; Huang, Yong; Toyoda, Hidenao; Suzuki, Atsushi; Toida, Toshihiko

doi:10.1016/s0049-3848(98)00171-6

Cited by 38 publications

(28 citation statements)

References 19 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…heparin, the absorption is negligible. The pharmacokinetics of intravenously administered (1 mg/kg) highly sulfated CS, DS and oversulfated DS has been studied in rats (Huang et al, 1996;Imanari et al, 1999). The analytical procedure used includes a simple preparation step (treatment with proteinases and ethanol precipitation) from blood plasma, HPLC for the separation using an Asahipak NH 2 P-50 column and fluorimetric detection after reaction of the polysaccharides with guanidine in strong alkaline medium.…”

Section: Metabolism Of Administered Chondroitin Sulfate In Experimentmentioning

confidence: 99%

“…The half-lives (t 1/2 ) of DS [80-85% di-mono4S I and 5-10% di-di(2,4)S I ] and oversulfated DS [60-65% di-di(4,6)S I , 20-25% di-tri (2,4,6)S I and 10-15% di-tri(3,4,6)S I ] in blood plasma were calculated as 7.8 ± 0.3 and 20.1 ± 1.1 min, respectively (Huang et al, 1996). Intravenous administration of a highly sulfated (sulfate to carboxyl ratio of about 4:1) partially depolymerized (12 kDa) holothurian fucose-branched CS also resulted in rapid decrease of blood plasma concentrations, but similarly administered intact holothurian CS (40 kDa) was undetectable in the plasma at all time points (Imanari et al, 1999). Oral administration of this highly sulfated CS (50 mg/kg) resulted in peak concentration (about 90 µg/mL) after 5 h. Furthermore, only 0.1% of the orally administered CS was recovered in urine collected for 24 h, while more than 5% of the intravenously administered (1 mg/kg) was excreted into urine in 24 h, suggesting that at least 2% of the orally administered partially depolymerized holothurian fucose-branched CS is being absorbed in the gastrointestinal tract (Imanari et al, 1999).…”

Section: Metabolism Of Administered Chondroitin Sulfate In Experimentmentioning

confidence: 99%

See 1 more Smart Citation

Metabolism and biochemical/physiological roles of chondroitin sulfates: analysis of endogenous and supplemental chondroitin sulfates in blood circulation

Lamari

Theocharis

Asimakopoulou

et al. 2006

Biomedical Chromatography

View full text Add to dashboard Cite

Chondroitin sulfate (CS) is a linear heteropolysaccharide consisting of repeating disaccharide units of glucuronic acid and galactosamine, which is commonly sulfated at C-4 and/or C-6 of galactosamine. The administration of CS as a supplement or a drug for the treatment of osteoarthrosis, the prevention of subsequent coronary events, treatment of psoriasis and ophthalmic diseases has been suggested. Much debate on the metabolism of CS and therefore the effectiveness of these treatments, especially after oral administration, has arisen due to the macromolecular nature of CS. Difficulties in analysing CS in blood due to the low endogenous concentrations and the covalent and anionic complexes with proteins have hampered the resolution of these issues. In this review, the information on the pharmacokinetics of CS obtained from studies in experimental animals and in humans is presented. Emphasis has been given to the analytical methods used for the determination of glycosaminoglycans, intact CS and CS-derived disaccharides in blood serum and plasma.

show abstract

Section: Metabolism Of Administered Chondroitin Sulfate In Experimentmentioning

confidence: 99%

Section: Metabolism Of Administered Chondroitin Sulfate In Experimentmentioning

confidence: 99%

Metabolism and biochemical/physiological roles of chondroitin sulfates: analysis of endogenous and supplemental chondroitin sulfates in blood circulation

Lamari

Theocharis

Asimakopoulou

et al. 2006

Biomedical Chromatography

View full text Add to dashboard Cite

show abstract

“…[7][8][9][10] Furthermore, glycosaminoglycans with a low molecular mass and charge density are preferentially absorbed. 8,11) In case of CS, some reports have been issued concerning its oral administration, metabolisms and chondroprotective function in arthritis.…”

mentioning

confidence: 99%

Effects of Low Molecular Weight Chondroitin Sulfate on Type II Collagen-Induced Arthritis in DBA/1J Mice

Cho

Sim

Jeong

et al. 2004

Biological & Pharmaceutical Bulletin

Self Cite

View full text Add to dashboard Cite

Chondroitin sulfate (CS) is a glycosaminoglycan, which is composed of an alternating sequence of sulfated and/or unsulfated residue of D-glucuronic acid (GlcA) and D-N-acetylgalactosamine (GalNAc) linked by b(1→3) and b(1→4) bonds.1) CS is a major class of glycosaminoglycans required for the formation of proteoglycans found in the joint cartilage. It has been well established that basic damage to the arthritic cartilage involves the alteration of proteoglycans and collagen fibers.

show abstract

“…A partially depolymerized fucosyl-CS polysaccharide [64] isolated from sea cucumber, was administered by the intravenous and oral routes to experimental animals. After oral administration (50 mg/kg), 0.1% of the dose was found in urine collected for 24 hours, and anion-exchange chromatographic behavior of fucosyl-CS polysaccharide excreted into urine after oral administration showed that partial desulfation might occur through intestinal absorption.…”

Section: Pharmacology and Pharmacokineticsmentioning

confidence: 99%

Chondroitin Sulphate for the Treatment of Osteoarthritis

Volpi

2005

CMCAIAA

View full text Add to dashboard Cite

The aim of this review is to illustrate the structural biology and functions of chondroitin sulphate (CS) in the light of recent glycobiological studies suggesting its new fundamental biological functions, and to evaluate the literature on CS concerning the pathobiology of osteoarthritis (OA), to ascertain whether this agent should be classified as a symptomatic slow-acting drug (SYSADOA), a compound that has a slow onset of action in alleviating OA symptoms. A previous review [Volpi, N. The pathobiology of osteoarthritis and the rationale for the use of chondroitin sulfate for its treatment. Curr. Drug Targets Immune Endocr. Metabol. Disord., 2004, 4, 119] has been published on this topic and this article intends to extend and update CS data and its use in the treatment of OA.CS exhibits a wide range of biological activities and from a pharmacological point of view, it produces a slow but gradual reduction of the clinical symptoms of OA, and these benefits last for a long period after the end of treatment. Furthermore, many animal studies and clinical trials have proved the efficacy of CS as a structure-modifying OA drug agent able to reverse, retard, or stabilize the pathology of OA, thereby providing symptomatic relief in the long-term treatment. In addition, there are fewer side effects when compared with other drugs used to treat the symptoms of OA, as well as a lack of toxicity associated with long-term use of these agents. These properties are also related to the oral absorption of this molecule as high-molecular mass compounds having clusters of sulphate groups and high charge density, capable of exerting their chondroprotective activity in vivo.

show abstract

Oral Absorption and Clearance of Partially Depolymerized Fucosyl Chondroitin Sulfate from Sea Cucumber

Cited by 38 publications

References 19 publications

Metabolism and biochemical/physiological roles of chondroitin sulfates: analysis of endogenous and supplemental chondroitin sulfates in blood circulation

Metabolism and biochemical/physiological roles of chondroitin sulfates: analysis of endogenous and supplemental chondroitin sulfates in blood circulation

Effects of Low Molecular Weight Chondroitin Sulfate on Type II Collagen-Induced Arthritis in DBA/1J Mice

Chondroitin Sulphate for the Treatment of Osteoarthritis

Contact Info

Product

Resources

About