Preparation, Characterization and Anti-Complementary Activity of Three Novel Polysaccharides from Cordyceps militaris.

This investigation focuses on the three novel polysaccharides from Cordyceps militaris and then discusses their characterization and anti-complementary activity. The three polysaccharides from C. militaris (CMP-1, CMP-2 and CMP-3) were prepared using a DEAE-52 cellulose column. The HPLC, HPGPC, FT-IR and Congo red analyses were used to characterize their monosaccharides, molecular weight and stereo conformation, which demonstrated that the three polysaccharides were homogenous polysaccharides with different molecular weights and were composed of at least ten monosaccharides with different molar ratios, and all had a triple-helix conformation. The evaluation of anti-complementary activity demonstrated that the three polysaccharides significantly inhibited complement activation through the classical pathway and alternative pathway. Preliminary mechanism studies indicated that CMP-1, CMP-2 and CMP-3 acted with C2, C5, C9, factor B, factor B, and P components in the overactivation cascade of the complement system. The analysis of the Pearson correlation and network confirmed that the ribose, glucuronic acid and galacturonic acid composition were negatively correlated with the anti-complementary activity of polysaccharides. These results suggested that the three novel polysaccharides are potential candidates for anti-complementary drugs.

Acetylation Modification, Characterization, and Anticomplementary Activity of Polysaccharides from Rhododendron dauricum Leaves.

This study focuses on the acetylation modification of polysaccharides from Rhododendron dauricum leaves (RDPs) with a high degree of substitution (DS) and then discusses their characterization and biological activity. The optimum acetylation conditions of RDPs were optimized by response surface methodology, which were reaction time 3 h, reaction temperature 50 °C, and the liquid-solid ratio 16 mL/g. Under the optima schemes, two eco-friendly acetylated polysaccharides from R. dauricum leaves (AcRDP-1 with DS of 0.439 ± 0.025 and AcRDP-2 with DS of 0.445 ± 0.022) were prepared. The results of structural characterization showed that the AcRDP-1 (9.3525 × 103 kDa) and AcRDP-2 (4.7016 × 103 kDa) were composed of mannose, glucose, galactose, and arabinose with molar ratios of 1.00:5.01:1.17:0.15 and 1.00:4.47:2.39:0.88, respectively. Compared with unmodified polysaccharides, the arabinose content and molecular weight of the two acetylated polysaccharides decreased, and their triple helix conformation disappeared, and further improved their anticomplementary activity. The two acetylated polysaccharides showed stronger a complement inhibition effect than the positive drug by blocking C2, C3, C4, C5, C9, and factor B targets in the classical and alternative pathways. This research indicated that acetylation modification could effectively enhance the anticomplementary activity of RDPs, which is beneficial for the development and utilization of R. dauricum leaves.

Isolation, Characterization and Anticomplementary Activity of Polysaccharides from the Rhizomes of Belamcanda chinensis (L.) DC.

The polysaccharides from the rhizomes of Belamcanda chinensis (L.) DC. (BCPs) were obtained by optimal water extraction (extraction temperature 84 °C, liquid to solid ratio 42 mL/g and extraction time 100 min), the extraction yield of BCPs was 23.01±0.27 % (n=3). Furthermore, two novel polysaccharides (BCP-A1 and BCP-B1) were purified by column chromatography. The BCP-A1 (6.0820×104  kDa) was composed of ß-D-Manp-(1→, ß-D-Glcp-(1→, →4)-α-D-Galp-(1→ and →3,4)-ß-D-Galp-(1→, and BCP-B1 (2.2744×104  kDa) was composed of →5)-α-L-Araf-(1→, ß-D-Manp-(1→, ß-D-Glcp-(1→, →4)-α-D-Glcp, →4)-α-D-Galp-(1→, →4)-α-D-GalpA-(1→ and →3,4)-ß-D-Galp-(1→. In anticomplementary experiments, BCP-A1 (CH50 : 0.009±0.003 mg/mL; AP50 : 0.015±0.003 mg/mL) and BCP-B1 (CH50 : 0.004±0.001 mg/mL; AP50 : 0.028±0.005 mg/mL) exhibited potent anticomplementary activity, and acted on C2-, C4- and Factor B components. Our study provides a foundation for BCP-A1 and BCP-B1 as potential complement inhibitors to treat diseases involving with excessive activation of the complement system.

Two new stilbene glucosides and a new benzoic acid derivative from Tournefortia sibirica.

Two new stilbene glucosides, trans-3,5-dihydroxy-4-methoxystilbene 3-O-ß-D-glucopyranoside (1), cis-3,5-dihydroxy-4-methoxystilbene 3-O-ß-D-glucopyranoside (2), one new benzoic acid derivative, cis-4-hydroxy-3-hydroxymethyl-2-butenyl benzoate 4-O-ß-D-glucopyranoside (3), and four known compounds (4 - 7) were isolated from Tournefortia sibirica L. The structures of these compounds were elucidated on the basis of spectral data. Anti-inflammatory effects of compounds (1 - 7) were evaluated in terms of inhibition on production of NO, TNF-α and IL-6 in LPS-induced RAW 264.7 cells. Compounds 1, 2 and 5 - 7 could inhibit the levels of NO, TNF-α and IL-6 in LPS-induced RAW264.7 cells with IC50 values ranging from 40.96 to 88.76 µM.

Two new phenolic glycosides from the fruits of Illicium verum.

Two new phenolic glycosides (1-2) and eleven known compounds (3-13) were isolated from the fruits of Illicium verum Hook.f. using silica-gel column and preparative middle pressure liquid chromatography (MPLC). The structures of the compounds were elucidated by NMR spectroscopic data. Among them, compounds 3, 5, and 10 were isolated from the family Magnoliaceae for the first time. Additionally, all the compounds were evaluated for their anti-complementary activities against the classical pathway (CP) and the alternative pathway (AP).