genipin and geniposide

Herein a series of Geniposide derivatives were designed, synthesized and evaluated as protein tyrosine phosphatase 1B (PTPlB) inhibitors. Most of these compounds exhibited potent in vitro PTP1B inhibitory activities, the representative 7a and 17f were found to be the most potent inhibitors against the enzyme with IC

Topics: Biological Transport; Cell Line; Chemistry Techniques, Synthetic; Enzyme Inhibitors; Glucose; Inhibitory Concentration 50; Insulin; Iridoids; Molecular Docking Simulation; Protein Tyrosine Phosphatase, Non-Receptor Type 1; Structure-Activity Relationship; Sulfonic Acids

Fructus gardeniae has long been used by traditional Chinese medical practitioners for its anti-inflammatory, anti-oxidant, anti-tumor and anti-hyperlipidemic characteristics. Here we describe our finding that F. gardeniae greatly reduces anti-enterovirus 71 (EV71) activity, resulting in significant decreases in EV71 virus yields, EV71 infections, and internal ribosome entry site activity. We also found that geniposide, a primary F. gardeniae component, inhibited both EV71 replication and viral IRES activity. Our data suggest the presence of a mechanism that blocks viral protein translation. According to our findings, F. gardeniae and geniposide deserve a closer look as potential chemopreventive agents against EV71 infections.

Topics: Antiviral Agents; Cell Line, Tumor; Drugs, Chinese Herbal; Enterovirus A, Human; Enterovirus Infections; Gardenia; Humans; Iridoids; Medicine, Chinese Traditional; Microbial Sensitivity Tests; Molecular Sequence Data; Protein Biosynthesis; Ribosomes; RNA, Viral; Virus Replication

Phytochemical study of the aqueous extract of the flowering tops of Lamium album led to identification of the antiviral iridoid isomers lamiridosins A and B (1, 2). These compounds were found to significantly inhibit hepatitis C virus entry (IC(50) 2.31 muM) in vitro. Studies of 14 iridoid analogues showed that, while the parent iridoid glucosides demonstrated no anti-HCV entry activity, the aglycones of shanzhiside methyl ester (4), loganin (5), loganic acid (6), geniposide (10), verbenalin (12), eurostoside (15), and picroside II (17) exhibited significant anti-HCV entry and anti-infectivity activities.

Topics: Antiviral Agents; Hepacivirus; Iridoids; Lamiaceae; Molecular Structure; Plants, Medicinal; Stereoisomerism