iridoids and epigallocatechin-gallate

The goal of this study was to improve the chemical stability of menhaden oil and control the lipolysis in emulsions with whey protein during in vitro digestion through EGCG conjugation and genipin-mediated interfacial cross-linking (CL). WPI-EGCG conjugate was successfully synthesized, confirmed by SDS-PAGE, ESI-MS, and phenolic group quantifications (125.3 mg/g), and characterized with far UV CD and ATR-FTIR. Emulsion particle diameter with WPI-EGCG is lower than with WPI. Compared to the native emulsion, WPI CL increased particle diameter and physical stability. Higher oxidative stability was observed for emulsions stabilized with WPI-EGCG conjugate than that with interfacial cross-linking due to the great antioxidant activity. Whereas, WPI CL is more effective than WPI-EGCG conjugate in hindering the rate and extent of lipolysis. The combination of EGCG conjugation and interfacial CL showed both the highest protection of menhaden oil against degradation and highest inhibition on the rate and extent of lipolysis of menhaden oil.

Topics: Antioxidants; Catechin; Circular Dichroism; Digestion; Electrophoresis, Polyacrylamide Gel; Emulsions; Fish Oils; Iridoids; Lipolysis; Oxidation-Reduction; Spectrometry, Mass, Electrospray Ionization; Spectroscopy, Fourier Transform Infrared; Whey Proteins

In this study, antitumor activity of epigallocatechin gallate (EGCG; major component of green tea polyphenol), eugenol (active component of clove), and amarogentin (active component of chirata plant) either alone or in combination were evaluated in Hela cell line. It was evident that EGCG with eugenol-amrogentin could highly inhibit the cellular proliferation and colony formation than individual treatments. Induction of apoptosis was also higher after treatment with EGCG in combination with eugenol-amrogentin than individual compound treatments. The antiproliferative effect of these compounds was due to downregulation of cyclinD1 and upregulation of cell cycle inhibitors LIMD1, RBSP3, and p16 at G1/S phase of cell cycle. Treatment of these compounds could induce promoter hypomethylation of LimD1 and P16 genes as a result of reduced expression of DNA methyltransferase 1 (DNMT1). Thus, our study indicated the better chemotherapeutic effect of EGCG in combination with eugenol-amarogentin in Hela cell line. The chemotherapeutic effect might be due to the epigenetic modification particularly DNA hypomethylation through downregulation of DNMT1.

Topics: Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Catechin; Cell Proliferation; DNA (Cytosine-5-)-Methyltransferase 1; Drug Synergism; Eugenol; Female; Gene Expression Regulation, Neoplastic; HeLa Cells; Humans; Intracellular Signaling Peptides and Proteins; Iridoids; LIM Domain Proteins; Tea; Tumor Suppressor Proteins; Uterine Cervical Neoplasms

Osteochondral xenografts are potentially inexpensive, widely available alternatives to fresh allografts. However, antigen removal from xenogenic cartilage may damage the extracellular matrix and reduce compressive stiffness. Non-crosslinked xenogenic cartilage may also undergo rapid enzymatic degradation in vivo. We hypothesized that natural crosslinking agents could be used in place of glutaraldehyde to improve the mechanical properties and enzymatic resistance of decellularized cartilage. This study compared the effects of genipin (GNP), proanthocyanidin (PA), and epigallocatechin gallate (EGCG), on the physical and mechanical properties of decellularized porcine cartilage. Glutaraldehyde (GA) served as a positive control. Porcine articular cartilage discs were decellularized in 2% sodium dodecyl sulfate and DNase I followed by fixation in 0.25% GNP, 0.25% PA, 0.25% EGCG, or 2.5% GA. Decellularization decreased DNA by 15% and GAG by 35%. For natural crosslinkers, the average degree of crosslinking ranged from approximately 50% (EGCG) to 78% (GNP), as compared to 83% for the GA control. Among the natural crosslinkers, only GNP significantly affected the disc diameter, and shrinkage was under 2%. GA fixation had no significant effect on disc diameter. Decellularization decreased aggregate modulus; GA and GNP, but not EGCG and PA, were able to restore it to its original level. GNP, PA, and GA conferred a similar, almost complete resistance to collagenase degradation. EGCG also conferred substantial resistance but to a lesser degree. Overall, the data support our hypothesis and suggest that natural crosslinkers may be suitable alternatives to glutaraldehyde for stabilization of decellularized cartilage. © 2015 Orthopaedic Research Society. Published by Wiley Periodicals, Inc. J Orthop Res 34:1037-1046, 2016.

Topics: Animals; Cartilage; Cartilage, Articular; Catechin; Collagenases; Cross-Linking Reagents; Drug Evaluation, Preclinical; Grape Seed Extract; Heterografts; Iridoids; Proanthocyanidins; Swine

Genipin-cross-linked caseinophosphopeptide (CPP)-chitosan (CS) nanoparticles (smaller than 300 nm) showed significantly improved stability and adjustable release profile in the gastrointestinal (GI) tract. Optimal purification of the nanoparticles was established by centrifugation to terminate the cross-linking reaction, which was further confirmed and characterized by FT-IR. Results from transmission electron microscopy (TEM), dynamic light scattering (DLS), and electrophoretic mobility (ζ-potential) measurements revealed that genipin cross-linking significantly prevented the bursting of the CPP-CS nanoparticles in simulated stomach acid and their precipitation under neutral intestinal environment. Pepsin showed little impact on the nanoparticle colloid stability; however, trypsin induced their aggregations. Genipin cross-linking slowed the burst release of (-)-epigallocatechin-3-gallate (EGCG) from the nanoparticles. The EGCG-loaded nanoparticles showed strong cytotoxicity against cancer cells; meanwhile, the net nanoparticles demonstrated high biocompatibility. The findings in the present work provide fundamental information for the rational design of biopolymer nanoparticles as an effective delivery systems for polyphenols.

Topics: Caseins; Catechin; Cell Line, Tumor; Cell Survival; Chitosan; Drug Carriers; Drug Delivery Systems; Gastrointestinal Tract; Humans; Iridoids; Nanoparticles; Peptide Fragments; Polyphenols; Proteoglycans