stilbenes and baicalein

Acute pancreatitis (AP) is one of the most common diseases. AP is associated with significant morbidity and mortality, but it lacks specific and effective therapies. Traditional Chinese medicine (TCM) is one of the most popular complementary and alternative medicine modalities worldwide for the treatment of AP. The current evidence from basic research and clinical studies has shown that TCM has good therapeutic effects on AP. This review summarizes the widely used formulas, single herbs and monomers that are used to treat AP and the potential underlying mechanisms of TCM. Because of the abundance, low cost, and safety of TCM as well as its ability to target various aspects of the pathogenesis, TCM provides potential clinical benefits and a new avenue with tremendous potential for the future treatment of AP.

Topics: Acute Disease; Animals; Anti-Inflammatory Agents; Apigenin; Artemisinins; Drugs, Chinese Herbal; Emodin; Flavanones; Glucuronates; Humans; Medicine, Chinese Traditional; Pancreas; Pancreatitis; Patient Safety; Phytotherapy; Plant Extracts; Pyrazines; Resveratrol; Rheum; Salvia miltiorrhiza; Stilbenes; Sulfates

Microbial adhesion to surfaces and the subsequent biofilm formation may result in contamination in food industry and in healthcare-associated infections and may significantly affect postoperative care. Some plants produce substances with antioxidant and antimicrobial properties that are able to inhibit the growth of food-borne pathogens. The aim of our study was to evaluate antimicrobial and anti-biofilm effect of baicalein, resveratrol, and pterostilbene on Candida albicans, Staphylococcus epidermidis, Pseudomonas aeruginosa, and Escherichia coli. We determined the minimum inhibitory concentrations (MIC), the minimum adhesion inhibitory concentration (MAIC), and the minimum biofilm eradication concentration (MBEC) by crystal violet and XTT determination. Resveratrol and pterostilbene have been shown to inhibit the formation of biofilms as well as to disrupt preformed biofilms. Our results suggest that resveratrol and pterostilbene appear potentially very useful to control and inhibit biofilm contaminations by Candida albicans, Staphylococcus epidermidis, and Escherichia coli in the food industry.

Topics: Anti-Infective Agents; Biofilms; Candida albicans; Escherichia coli; Flavanones; Microbial Sensitivity Tests; Plant Extracts; Pseudomonas aeruginosa; Resveratrol; Staphylococcus epidermidis; Stilbenes

Excessive exposure to ultraviolet (UV) B radiation may lead to skin damage, photosensitivity, or even tumorigenesis via induction of oxidative stress. Naturally derived antioxidants could play significant roles in cancer therapy due to their multi-targeted actions and lack of substantial toxicity. Drug combinations target at diverse pathway of cells and make cells export meticulous biological outcomes through the multifaceted signaling network. The UVB protective effects of combinations of naturally derived antioxidants- curcumin, resveratrol, proanthocyanidins, baicalein, and beta-nicotinamide adenine dinucleotide (NADH) were investigated. An oxidative cell damage model was established to study the ultraviolet irradiation system. An orthogonal array composite design (OACD) was employed in the optimization of antioxidants combinations. Combination of resveratrol (0.1μM) and baicalein in medium concentration (0.2μM), with NADH in high concentration (0.8μM) was found to be the most efficacious combination among all the 30 runs performed using OACD. The findings suggested that UVB exposure-inflicted cell apoptosis can be significantly reduced by naturally-derived antioxidant combinations. These results provide an insight into the discovery of synergistic antioxidant combinations in skin cancer, using orthogonal array composite design (OACD). The results also have practical implications in the understanding of drug mechanisms in skin cancer, which can assist clinical practice by recommending better drug combinations.

Topics: Antioxidants; Cell Line; Cell Survival; Curcumin; DNA Fragmentation; Fibroblasts; Flavanones; Humans; Linear Models; Oxidative Stress; Proanthocyanidins; Reactive Oxygen Species; Resveratrol; Skin; Stilbenes; Ultraviolet Rays

Our working hypothesis is that single bioactive phytochemicals with antioxidant properties that are important constituents of Traditional Chinese Medicine (TCM) and their defined mixtures have potential as chemoprotective agents for chronic conditions characterized by oxidative and nitrosative stress, including Alzheimer's. Here we evaluate the ability of baicalein, crocetin, trans-resveratrol or schisanhenol and two defined mixtures of these TCM phytochemicals to attenuate the toxicity resulting from exposure to cell permeant t-butyl hydroperoxide (tBPH) in wild-type and bioengineered (to express choline acetyltransferase) HEK 293 cells.. Endpoints of tBHP-initiated oxidative and nitrosative stress in both types of HEK 293 cells and its attenuation by TCM constituents and mixtures included cytotoxicity (LDH release); depletion of intracellular glutathione (GSH); formation of S-glutathionylated proteins; oxidative changes to the disulfide proteome; and real-time changes in intracellular redox status.. At low µM concentrations, each of the TCM constituents and mixtures effectively attenuated intracellular toxicity due to exposure of HEK 293 cells to 50 or 250 µM tBHP for 30 min to 3 h. Confocal microscopy of HEK 293 cells transfected with mutated green fluorescent protein (roGFP2) showed effective attenuation of tBHP oxidation by baicalein in real time. Three redox-regulated proteins prominent in the disulfide proteome of HEK 293 cells were identified by MALDI-TOF mass spectrometry.. We conclude that single TCM chemicals and their simple mixtures have potential for use in adjunct chemoprotective therapy. Advantages of mixtures compared to single TCM constituents include the ability to combine compounds with varying molecular mechanisms of cytoprotection for enhanced biological activity; and to combine chemicals with complementary pharmacokinetic properties to increase half-life and prolong activity in vivo. This article is open to POST-PUBLICATION REVIEW. Registered readers (see "For Readers") may comment by clicking on ABSTRACT on the issue's contents page.

Topics: Antioxidants; Carotenoids; Cyclooctanes; Dose-Response Relationship, Drug; Drugs, Chinese Herbal; Flavanones; HEK293 Cells; Humans; Medicine, Chinese Traditional; Oxidation-Reduction; Oxidative Stress; Polycyclic Compounds; Resveratrol; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; Stilbenes; tert-Butylhydroperoxide; Vitamin A

Human ATAD5 is a biomarker for identifying genotoxic compounds because ATAD5 protein levels increase posttranscriptionally in response to DNA damage. We screened over 4,000 compounds with a cell-based quantitative high-throughput ATAD5-luciferase assay detecting genotoxic compounds. We identified 22 antioxidants, including resveratrol, genistein, and baicalein, that are currently used or investigated for the treatment of cardiovascular disease, type 2 diabetes, osteopenia, osteoporosis, and chronic hepatitis, as well as for antiaging. Treatment of dividing cells with these compounds induced DNA damage and resulted in cell death. Despite their genotoxic effects, resveratrol, genistein, and baicalein did not cause mutagenesis, which is a major side effect of conventional anticancer drugs. Furthermore, resveratrol and genistein killed multidrug-resistant cancer cells. We therefore propose that resveratrol, genistein, and baicalein are attractive candidates for improved chemotherapeutic agents.

Topics: Antioxidants; Cell Death; Cell Line; DNA Damage; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Flavanones; Genistein; Humans; Mutagenicity Tests; Resveratrol; Stilbenes

The root and stem of Vitis amurensis (Vitaceae) have popularly used as traditional medicine for treatment of cancer and various pains in Korea and Japan. Recent studies, its root and stem possess anti-inflammatory, anti-tumor activities, and protective effects against beta-amyloid-induced oxidative stress.. This study deals with the isolation, structural identification of the potent bioactive compounds from the leaf and stem, and their antioxidant capacity, as well as anti-inflammatory effect via lipoxygenase inhibitory assay.. All isolated compounds yielded after using column chromatography were identified base on the physico-chemical properties and 1D, 2D NMR spectra. The scavenge ability against DPPH and ABTS(+) radicals, and to inhibit lipid peroxidation, as well as lipoxygenase type I inhibitory activity of all isolates were performed using in vitro assays.. Eleven resveratrol derivatives (1-11), including a new oligostilbene cis-amurensin B (9), whose structures were determined on the basis of extensively spectral analyses, were isolated from the leaf and stem of Vitis amurensis. The isolates (1-11) were examined for their antioxidant activities by evaluating scavenge ability against DPPH and ABTS(+) radicals, and to inhibit lipid peroxidation. Stilbenes 1 and 4, and oligostilbenes 5-10 displayed moderate anti-lipid peroxidation activities, but all the isolates exhibited strong ABTS(+) radical scavenging activity in the dose-dependent manner. In addition, the isolates showed stronger inhibitory capacity against soybean lipoxygenase type I than that of baicalein, a positive control. Of the isolates, r-2-viniferin (8) exhibited the strongest scavenging activity against ABTS(+) radical with TEAC value of 5.57, and the most potential inhibitory effect on soybean lipoxygenase with the IC(50) value of 6.39 microM.. This is the first report on the potential antioxidant and LOX-1 inhibitory effects of oligostilbenes isolated from the leaf and stem of Vitis amurensis. In addition, chemical compositions isolated from the leaf and stem are almost similar to those isolated from the root of Vitis amurensis. Therefore, the results may explain, in part, the uses of the leaf and stem, as well as the root of Vitis amurensis in the Korean traditional medicine.

Topics: Antioxidants; Benzofurans; Flavanones; Lipid Peroxidation; Lipoxygenase; Lipoxygenase Inhibitors; Plant Extracts; Plant Leaves; Plant Stems; Resveratrol; Stilbenes; Vitis

Paeoninol and paeonin C, oligostilbene and monoterpene galactoside, have been isolated from the methanolic extract of the fruits of Paeonia emodi. Their structures have been assigned on the basis of spectral analysis including 1D and 2D NMR techniques. In addition, 4-hydroxybenzoic acid 3, gallic acid 4 and methyl gallate 5 have also been reported for the first time from this species. Compounds 1 and 2 have displayed potent inhibitory potential against enzyme lipoxygenase in a concentration-dependent fashion with the IC(50) values 0.77 and 99.5 microM, along with ABTS(.+) radical quenching activity with IC(50) values of 147.5 and 498.2 microM, respectively.

Topics: Antioxidants; Dose-Response Relationship, Drug; Flavanones; Flavonoids; Fruit; Galactosides; Inhibitory Concentration 50; Lipoxygenase Inhibitors; Molecular Structure; Monoterpenes; Nuclear Magnetic Resonance, Biomolecular; Paeonia; Plant Extracts; Stilbenes