Metabolite Profiling and Dipeptidyl Peptidase IV Inhibitory Activity of Coreopsis Cultivars in Different Mutations.

Coreopsis species have been developed to produce cultivars of various floral colors and sizes and are also used in traditional medicine. To identify and evaluate mutant cultivars of C. rosea and C. verticillata, their phytochemical profiles were systematically characterized using ultra-performance liquid chromatography time-of-flight mass spectrometry, and their anti-diabetic effects were evaluated using the dipeptidyl peptidase (DPP)-IV inhibitor screening assay. Forty compounds were tentatively identified. This study is the first to provide comprehensive chemical information on the anti-diabetic effect of C. rosea and C. verticillata. All 32 methanol extracts of Coreopsis cultivars inhibited DPP-IV activity in a concentration-dependent manner (IC50 values: 34.01-158.83 µg/mL). Thirteen compounds presented as potential markers for distinction among the 32 Coreopsis cultivars via principal component analysis and orthogonal partial least squares discriminant analysis. Therefore, these bio-chemometric models can be useful in distinguishing cultivars as potential dietary supplements for functional plants.

Composition and Antioxidant Activities of Volatile Organic Compounds in Radiation-Bred Coreopsis Cultivars.

Coreopsis is a flowering plant belonging to the Asteraceae family. It is an ornamental plant native to the Americas, Asia and Oceania and its flower is used as a raw material for tea and food manufacture in China. In this study, new cultivars of C. rosea ("golden ring") were developed via radiation-induced mutation of the original cultivar, "pumpkin pie". The chemical composition and antioxidant activities of flowers belonging to three different Coreopsis cultivars were evaluated: "golden ring", "pumpkin pie" and "snow chrysanthemum" (coreopsis tea; C. tinctoria). The volatile compounds were characterized via gas chromatography-mass spectrometry (GC-MS) and 50-59 oils representing 95.3-96.8% of the total volatile compounds in these flower materials were identified. "Golden ring" contained a high amount of fatty acids (38.13%), while "pumpkin pie" and "snow chrysanthemum" teas were rich in aliphatic amides (43.01%) and esters (67.22%), respectively. The antioxidant activities of the volatile oils of these cultivars were evaluated using 1,1-diphenyl-2-picrylhydraxyl (DPPH) and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging assays. The volatile extract of "golden ring" showed higher antioxidant activities compared with the extracts of the other cultivars. Therefore, "golden ring" can be used for further development as a raw material for tea manufacture or as a dietary supplement.

Human colorectal cancer antigen GA733-2-Fc fused to endoplasmic reticulum retention motif KDEL enhances its immunotherapeutic effects.

OBJECTIVE: The aim of this is to compare the immunotherapeutic effects of human colorectal cancer antigen GA733-2 fused to the Fc fragment of antibody (GA733-2-Fc) and to Fc and endoplasmic reticulum (ER) retention motif KDEL (GA733-2-Fc-KDEL). MATERIALS AND METHODS: Recombinant GA733-2-Fc and GA733-2-Fc-KDEL were produced from infiltrated Nicotiana benthamiana leaves and purified by affinity chromatography. Glycan structures were determined by matrix-assisted laser desorption/ionization-time-of-flight mass spectrometry. The allergic and immunogenic responses of recombinant GA733-2-Fc and GA733-2-Fc-KDEL were estimated in an intraperitoneally immunized mouse. The tumor regression effect of recombinant GA733-2-Fc and GA733-2-Fc-KDEL was examined using a colorectal carcinoma CT-26 animal model. RESULTS: Recombinant GA733-2-Fc contained plant-specific glycan structures including ß(1,2)-xylose and α(1,3)-fucose whereas recombinant GA733-2-Fc-KDEL contained oligomannose type glycan structures. Mice immunized intraperitoneally with recombinant GA733-2-Fc and GA733-2-Fc-KDEL elicited strong GA733-2-Fc-specific immunoglobulin G (IgG) and IgA serum antibody responses. Recombinant GA733-2-Fc-KDEL reduced the production of GA733-2-Fc-specific IgE. Recombinant GA733-2-Fc-KDEL increased the production of interferon-γ. Intraperitoneal preimmunization with recombinant GA733-2-Fc and GA733-2-Fc-KDEL regressed tumor growth in a colorectal carcinoma CT-26 animal model. The tumor regression effect induced by recombinant GA733-2-Fc-KDEL was greater than that induced by recombinant GA733-2-Fc. The human and mouse colorectal carcinoma cell binding activities of recombinant GA733-2-Fc-KDEL-immunized sera were higher than those of recombinant GA733-2-Fc. CONCLUSIONS: Our results suggest that GA733-2-Fc conjugated to ER-retention motif KDEL is a more efficient antigen to prevent tumor growth induced by colorectal carcinoma and minimize an allergic response.