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1.
Eksp Klin Farmakol ; 76(10): 20-4, 2013.
Article in Russian | MEDLINE | ID: mdl-24400384

ABSTRACT

Polyanions (in an amount within 1.5 - 6.0 mg), including cellulose sulfates (excreted from Gossipium hirsutum L., molecular weight 22.0 kDa, degree of sulfation within 0.8 - 1.8), inulin sulfates (excreted from Helianthus tuberosus, molecular weight 8.0 kDa, degree of sulfation within 0.6 - 1.6), pectin sulfates (excreted from Abies sibirica L., molecular weight 24.0 kDa, degree of sulfation within 0.8 - 1.1), give rise to peaks of precipitation with polycations of protamine sulfate. Only cellulose sulfates (in amount within 0.38 - 6.00 mg) give the peaks of precipitation with chitosan polycations (molecular weight 10 kDa, degree of deacetylation 85%) during horizontal biospecific electrophoresis. The height of the peak of precipitation with protamin sulfate was found to grow with increasing antithrombin activity of cellulose sulfates and pectin sulfate (for polyanions in an amount within 1.5 - 6 mg). The size of the area of precipitation with chitosan was found to decrease with increasing antithrombin activity of cellulose sulfates.


Subject(s)
Anticoagulants/chemistry , Cellulose/analogs & derivatives , Chondroitin Sulfates/chemistry , Inulin/chemistry , Pectins/chemistry , Polyamines/chemistry , Protamines/chemistry , Anticoagulants/isolation & purification , Blood Coagulation , Cellulose/chemistry , Cellulose/isolation & purification , Chondroitin Sulfates/isolation & purification , Electrophoresis, Agar Gel/methods , Gossypium/chemistry , Humans , Inulin/analogs & derivatives , Inulin/isolation & purification , Molecular Weight , Pectins/isolation & purification , Pinus/chemistry , Polyamines/isolation & purification , Polyelectrolytes , Thrombin/chemistry
2.
Eksp Klin Farmakol ; 75(6): 31-5, 2012.
Article in Russian | MEDLINE | ID: mdl-22891439

ABSTRACT

We have studied a relationship between the degree of sulfonation and anticoagulant activity of starch from Solanum tuberosum (molecular weight, 25000-30000 Da; sulfonation degree, 0.4-2.5) and inulin from Helianthus tuberosus (molecular weight, 7000-8000 Da; sulfonation degree, 0.6-1.6). Starch and inulin sulfates (i) increased the time of appearance of fibrin clots in plasma in coagulometric tests and (ii) reduced (via antithrombin) the rate of thrombin-induced hydrolysis of a chromogen substrate. The antithrombin (aIIa) activity of starch sulfates reached 16.8-70.0 IU/mg and the activity against factor Xa (aXa activity) was 2.3-16.6 IU/mg. The antithrombin activity of inulin sulfates was within 5.5-11.4 IU/mg and the activity against factor Xa (aXa activity) was within 0-1.4 IU/mg. An increase in the degree of sulfonation led to a growth in the anticoagulant activity of starch sulfates. The anticoagulant activity of starch sulfates and inulin sulfate with sulfonation degree 1.0 is mediated by antithrombin, which is the plasma inhibitor of serine proteases.


Subject(s)
Anticoagulants/pharmacology , Blood Coagulation/drug effects , Fibrin/antagonists & inhibitors , Inulin/pharmacology , Starch/pharmacology , Sulfur Compounds/pharmacology , Antithrombin III/antagonists & inhibitors , Factor Xa Inhibitors , Fibrin/biosynthesis , Helianthus/chemistry , Humans , Inulin/analogs & derivatives , Molecular Weight , Solanum tuberosum/chemistry , Starch/analogs & derivatives , Structure-Activity Relationship , Thrombin/antagonists & inhibitors
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