Sulfation pattern of citrus pectin and its carboxy-reduced derivatives: influence on anticoagulant and antithrombotic effects.
Identifieur interne : 001202 ( Main/Merge ); précédent : 001201; suivant : 001203Sulfation pattern of citrus pectin and its carboxy-reduced derivatives: influence on anticoagulant and antithrombotic effects.
Auteurs : Nadiezda C. Maas [Brésil] ; Ana Helena P. Gracher ; Guilherme L. Sassaki ; Philip A J. Gorin ; Marcello Iacomini ; Thales R. CiprianiSource :
- Carbohydrate polymers [ 1879-1344 ] ; 2012.
English descriptors
- KwdEn :
- Animals, Anticoagulants (chemistry), Anticoagulants (isolation & purification), Anticoagulants (pharmacology), Blood Coagulation (drug effects), Citrus sinensis (chemistry), Female, Fibrinolytic Agents (chemistry), Fibrinolytic Agents (isolation & purification), Fibrinolytic Agents (pharmacology), Male, Pectins (chemistry), Pectins (isolation & purification), Pectins (pharmacology), Polysaccharides (chemistry), Polysaccharides (isolation & purification), Polysaccharides (pharmacology), Rats, Rats, Wistar.
- MESH :
- chemical , chemistry : Anticoagulants, Fibrinolytic Agents, Pectins, Polysaccharides.
- chemical , isolation & purification : Anticoagulants, Fibrinolytic Agents, Pectins, Polysaccharides.
- chemical , pharmacology : Anticoagulants, Fibrinolytic Agents, Pectins, Polysaccharides.
- chemistry : Citrus sinensis.
- drug effects : Blood Coagulation.
- Animals, Female, Male, Rats, Rats, Wistar.
Abstract
Citrus pectin (CP), a polysaccharide composed of [→4)-α-D-GalpA-(1→]n, was submitted to one or four carboxy-reduction cycles, resulting in CP-CR1 and CP-CR4, which had 40% and 2% of GalpA units, respectively. The polysaccharides were chemically sulfated and their anticoagulant and antithrombotic effects determined. Sulfated polysaccharides (CP-S, CP-CR1S and CP-CR4S) had different anticoagulant activities, doubling APTT at concentrations of 28.7, 13.2, and 4.9 μg/ml respectively. CP-CR1S and CP-CR4S also showed antithrombotic activity in vivo with ED50 of 3.01 and 1.70 mg/kg, respectively. Like heparin, they inhibited thrombin by a mechanism dependent on AT and HCII. Their hemorrhagic potential was also similar to that of heparin. According to methylation analysis, 91.1% and 50.2% of 6-O-position in CP-CR4S and CP-CR1S were sulfated, respectively. Therefore, substitution of carboxyl groups by sulfate esters in these polysaccharides increases the anticoagulant and antithrombotic effects.
DOI: 10.1016/j.carbpol.2012.03.070
PubMed: 24750917
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pubmed:24750917Le document en format XML
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<series><title level="j">Carbohydrate polymers</title>
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<term>Blood Coagulation (drug effects)</term>
<term>Citrus sinensis (chemistry)</term>
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<term>Fibrinolytic Agents (chemistry)</term>
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<term>Fibrinolytic Agents (pharmacology)</term>
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<front><div type="abstract" xml:lang="en">Citrus pectin (CP), a polysaccharide composed of [→4)-α-D-GalpA-(1→]n, was submitted to one or four carboxy-reduction cycles, resulting in CP-CR1 and CP-CR4, which had 40% and 2% of GalpA units, respectively. The polysaccharides were chemically sulfated and their anticoagulant and antithrombotic effects determined. Sulfated polysaccharides (CP-S, CP-CR1S and CP-CR4S) had different anticoagulant activities, doubling APTT at concentrations of 28.7, 13.2, and 4.9 μg/ml respectively. CP-CR1S and CP-CR4S also showed antithrombotic activity in vivo with ED50 of 3.01 and 1.70 mg/kg, respectively. Like heparin, they inhibited thrombin by a mechanism dependent on AT and HCII. Their hemorrhagic potential was also similar to that of heparin. According to methylation analysis, 91.1% and 50.2% of 6-O-position in CP-CR4S and CP-CR1S were sulfated, respectively. Therefore, substitution of carboxyl groups by sulfate esters in these polysaccharides increases the anticoagulant and antithrombotic effects.</div>
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