Activation of PPARγ by a Natural Flavonoid Modulator, Apigenin Ameliorates Obesity-Related Inflammation Via Regulation of Macrophage Polarization.

PPARγ has emerged as a master regulator of macrophage polarization and is the molecular target of the thiazolidinedione drugs. Here we show that apigenin binds and activates PPARγ by acting as a modulator. Activation of PPARγ by apigenin blocks p65 translocation into nuclei through inhibition of p65/PPARγ complex translocation into nuclei, thereby decreasing NF-κB activation and favoringM2 macrophage polarization.

Ursolic acid derivatives as bone anabolic agents targeted to tryptophan hydroxylase 1 (Tph-1).

Tryptophan hydroxylase 1 (Tph-1) initiates the biosynthesis of peripheral serotonin. As peripheral serotonin suppresses bone formation, inhibitor of Tph-1 provides a useful tool to discover anabolic agents for osteoporosis. In the present study, series of ursolic acid (UA) derivatives were synthesized, and their inhibitory activity on serotonin biosynthesis and cytotoxicity were evaluated.

A new synthetic ursolic acid derivative IUA with anti-tumor efficacy against osteosarcoma cells via inhibition of JNK signaling pathway.

Background: Osteosarcoma is the most common primary malignant bone tumor in children and adolescents and is characterized by frequent metastasis and resistance to chemotherapy. Because osteosarcoma cells are not highly susceptible to current chemotherapy drugs, new alternative strategies for the treatment of osteosarcoma are needed. This study was undertaken to investigate the inhibitory effects of a new synthetic ursolic acid derivative IUA on osteosarcoma cells and to explore its molecular mechanism.

Tryptophan hydroxylase 1 (Tph-1)-targeted bone anabolic agents for osteoporosis.

Tryptophan hydroxylase 1 (Tph-1), the principal enzyme for peripheral serotonin biosynthesis, provides a novel target to design anabolic agents for osteoporosis. Here, we present a design, synthesis of a novel series of ursolic acid derivatives under the guidance of docking technique, and bioevaluation of the derivatives using RBL2H3 cells and ovariectomized (OVX) rats. Of the compounds, 9a showed a potent inhibitory activity on serotonin biosynthesis.

Cu(II)-catalyzed C-H (SP3) oxidation and C-N cleavage: base-switched methylenation and formylation using tetramethylethylenediamine as a carbon source.

Base-switched methylenation and formylation using tetramethylethylenediamine (TMEDA) as a carbon source have been achieved under mild conditions, catalyzed by CuCl(2), with atmospheric oxygen as oxidant. Bisindolylmethanes, diphenylmethanes and 3-formylindoles were synthesized with excellent regioselectivity and good yield.

The formation of a luminescent Mn(III,IV) intermediate of bis(2-pyridylmethyl)amine and acetone assistant its intramolecular C-H oxidation.

The dinuclear Mn(II) complexes of bis(2-pyridylmethyl)amine (dpa) reacted with H(2)O(2) producing a fluorescent dioxodimanganese(III,IV) intermediate [(dpa)Mn(2)Cl(2)(μ-O(2))(OHdpa)](3+), which was characterized by IR, UV, ESR, ES-MS and fluorescence spectra. ES-MS data show that this intermediate could bind an acetone molecule forming dioxodimanganese(III,IV)-acetone adduct [(dpa)Mn(2)Cl(2)(μ-O)(CH(3)COCH(3))(OHdpa)](3+). The emission of dioxodimanganese(III,IV)-acetone at 378 nm was stronger than that of dioxodimanganese(III,IV) complex.

Anticancer activity, attenuation on the absorption of calcium in mitochondria, and catalase activity for manganese complexes of N-substituted di(picolyl)amine.

In order to find multifunction anticancer complexes, three Mn(II) complexes of N-substituted di(2-pyridylmethyl)amine were characterized and used as agents to interfere with the functions of mitochondria and the metabolite of O(2) in cancer cells. It was found that carboxylate-bridged dimanganese(II) systems are good models of catalase and exhibit good inhibition of the proliferation of U251 and HeLa cells. The inhibiting activity of these manganese(II) complexes on the tumor cells in vitro was related to their disproportionating H(2)O(2) activity.

Interaction with DNA and different effect on the nucleus of cancer cells for copper(II) complexes of N-benzyl di(pyridylmethyl)amine.

Three new copper(II) complexes of N-benzyl di(pyridylmethyl)amine (phdpa) were synthesized and characterized by spectroscopic methods. The interaction between CT-DNA and the complexes was studied by UV and fluorescence titration methods. It was found that the complex [(phdpa)Cu(H(2)O)Ac)](Ac), with the non-planar aromatic heterocyclic ring ligand (phdpa), showed good anticancer properties and could cause the fragmentation of the nucleus, although its interaction with CT-DNA was weaker than that of 1,10-phenanthroline (phen)-based copper(II) complexes.

Synthesis, characterization, bioactivities of copper complexes with N-allyl di(picolyl)amine.

Four copper(II) complexes with N-allyl di(picolyl)amine were synthesized and characterized by physico-chemical and spectroscopic methods. The spectrophotometric and fluorescence titration data indicate that the [(Aldpa)Cu(L)](ClO(4))(2) (L=dppz, dione, phen) with conjugated aromatic rings as coordinated ligands can be inserted into the base stacks of DNA more deeply than the [(Aldpa)CuCl(2)]. The copper(II) complexes [(Aldpa)Cu(L)](ClO(4))(2) (L=dppz, dione, phen) can inhibit the proliferation of the four cancer cells (Mcf-7, Eca-109, A549 and HeLa) with IC(50) 0.