title: Structural characterization of a homogalacturonan from Capparis spinosa L. fruits and anti-complement activity of its sulfated derivative.
abstract: A water-soluble polysaccharide CSPS-2B-2 with a molecular mass of 8.8 kDa, was obtained from the fruits of Capparis spinosa L. Chemical and NMR spectral analysis verified CSPS-2B-2 was a linear poly-(1-4)-α-D-galactopyranosyluronic acid in which 12.9±0.4% of carboxyl groups existed as methyl ester and 2.6±0.1% of D-GalpA residues were acetylated. A sulfated derivative Sul-2B-2 with a sulfation degree of 0.88±0.02 was prepared via the substitution of C-2 and/or C-3 of GalpA residues in CSPS-2B-2. Bioassay on the complement and coagulation system demonstrated that Sul-2B-2 (CH(50): 3.5±0.2 μg/mL) had a stronger inhibitory effect on the activation of complement system through the classic pathway than that of heparin (CH(50): 8.9±0.3 μg/mL). Interestingly, Sul-2B-2 at low dose even middle dose (for example 52 μg/mL) had no effect on coagulation system, which was totally different from heparin. Thus, our observation indicated that Sul-2B-2 was more efficient than heparin in inhibiting the activation of the complement system through classical pathway and exhibiting a relatively less anti-coagulant activity. These results suggested that the sulfated derivative Sul-2B-2 prepared from the homogalacturonan in the fruits of Capparis spinosa L, might be a promising drug candidate in case of necessary therapeutic complement inhibition.
authors: Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
authors: Huijun
authors: H
authors: Wang
authors: Hongwei
authors: H
authors: Wang
authors: Songshan
authors: S
authors: Shi
authors: Jinyou
authors: J
authors: Duan
authors: Shunchun
authors: S
authors: Wang
mesh_terms: D000818:Animals; D000925:Anticoagulants / Q000737:chemistry; D001777:Blood Coagulation; D031484:Capparis / Q000737:chemistry*; D002845:Chromatography; D051056:Complement Inactivating Agents / Q000737:chemistry* / Q000302:isolation & purification; D003165:Complement System Proteins / Q000737:chemistry* / Q000378:metabolism; D004912:Erythrocytes / Q000737:chemistry; D005638:Fruit / Q000737:chemistry*; D006493:Heparin / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D010368:Pectins / Q000737:chemistry* / Q000302:isolation & purification; D010936:Plant Extracts / Q000737:chemistry; D011817:Rabbits; D012756:Sheep; D013463:Sulfuric Acid Esters / Q000737:chemistry*
chemical_list: D000925:Anticoagulants; D051056:Complement Inactivating Agents; D010936:Plant Extracts; D013463:Sulfuric Acid Esters; D010368:Pectins; D006493:Heparin; D003165:Complement System Proteins; C003181:polygalacturonic acid