rottlerin and 1-1-diphenyl-2-picrylhydrazyl

Mallotus philippinensis is an important source of molecules with strong antioxidant activity widely used medicinal plant. Previous studies have highlighted their anticestodal, antibacterial, wound healing activities, and so forth. So, present investigation was designed to evaluate the total antioxidant activity and radical scavenging effect of 50% ethanol fruit glandular hair extract (MPE) and its role on Human Erythrocytes. MPE was tested for phytochemical test followed by its HPLC analysis. Standard antioxidant assays like DPPH, ABTS, hydroxyl, superoxide radical, nitric oxide, and lipid peroxidation assay were determined along with total phenolic and flavonoids content. Results showed that MPE contains the presence of various phytochemicals, with high total phenolic and flavonoid content. HPLC analysis showed the presence of rottlerin, a polyphenolic compound in a very rich quantity. MPE exhibits significant strong scavenging activity on DPPH and ABTS assay. Reducing power showed dose dependent increase in concentration absorption compared to standard, Quercetin. Superoxide, hydroxyl radical, lipid peroxidation, nitric oxide assay showed a comparable scavenging activity compared to its standard. Our finding further provides evidence that Mallotus fruit extract is a potential natural source of antioxidants which have a protective role on human Erythrocytes exhibiting minimum hemolytic activity and this justified its uses in folklore medicines.

Topics: Acetophenones; Antioxidants; Benzopyrans; Benzothiazoles; Biphenyl Compounds; Chromatography, High Pressure Liquid; Chromatography, Thin Layer; Erythrocytes; Free Radical Scavengers; Fruit; Hemolysis; Humans; Hydroxyl Radical; Lipid Peroxidation; Mallotus Plant; Nitric Oxide; Oxidation-Reduction; Phytochemicals; Picrates; Plant Extracts; Polyphenols; Reference Standards; Sulfonic Acids

Rottlerin, a polyphenol isolated from Mallotus Philippinensis, has been recently used as a selective inhibitor of PKC delta, although it can inhibit many kinases and has several biological effects. Among them, we recently found that Rottlerin inhibits the Nuclear Factor kappaB (NFkappaB), activated by either phorbol esters or H(2)O(2). Because of the redox sensitivity of NFkappaB and on the basis of Rottlerin antioxidant property, we hypothesized that Rottlerin could prevent NFkappaB activation acting as a free radicals scavenger, as other natural polyphenols. The current study confirms the antioxidant property of Rottlerin against the 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) in vitro and against oxidative stress induced by H(2)O(2) and by menadione in culture cells. We also demonstrate that Rottlerin prevents TNFalpha-dependent NFkappaB activation in MCF-7 cells and in HT-29 cells transfected with the NFkappaB-driven plasmid pBIIX-LUC, suggesting that Rottlerin can inhibit NFkappaB via several pathways and in several cell types.

Topics: Acetophenones; Benzopyrans; Biphenyl Compounds; Cell Nucleus; DNA; Electron Spin Resonance Spectroscopy; Free Radical Scavengers; HT29 Cells; Humans; Hydrogen Peroxide; Intracellular Space; NF-kappa B; Picrates; Protein Binding; Protein Transport; Reactive Oxygen Species; Spectrophotometry, Ultraviolet; Transcription, Genetic; Transfection; Tumor Necrosis Factor-alpha

The bile salt, deoxycholate (DOC), can harm cells and cause disease. Hence, there is interest in identifying compounds capable of protecting cells against DOC. In HCT-116 colon epithelial cells, DOC increased generation of reactive oxygen species and caused DNA damage and apoptosis. These effects of DOC were inhibited by rottlerin, which is a phenolic compound of plant origin. In elucidating its mechansim, rottlerin prevented the release of cytochrome c from mitochondria into cytosol, and also prevented the cleavage of caspase-3. Yet, rottlerin by itself markedly decreased mitochondrial membrane potential and increased mitochondrial superoxide production, but this did not result in cytochrome c release or in caspase-3 cleavage. At a higher test concentration, two other phenolic phytochemicals, namely, quercetin and resveratrol, were each able to largely prevent the occurrence of apoptosis in cells exposed to DOC. In contrast, epigallocatechin gallate, curcumin, and genistein were ineffective.

Topics: Acetophenones; Apoptosis; Benzopyrans; Biphenyl Compounds; Caspase 3; Colon; Cytochromes c; Cytoprotection; Deoxycholic Acid; DNA Damage; DNA, Neoplasm; Epithelial Cells; HCT116 Cells; Humans; Hydrazines; Mitochondria; Phenols; Picrates; Quercetin; Resveratrol; Stilbenes; Superoxides