Novel biotin-linked amphiphilic calix[4]arene-based supramolecular micelles as doxorubicin carriers for boosted anticancer activity.

Supramolecular carrier-mediated chemotherapy is a highly attractive strategy for targeted drug delivery. In this study, four novel biotin-linked calix[4]arenes BPCA1-BPCA4 have been rationally designed to construct nano-complex with doxorubicin. The in vitro and in vivo assessments reveal that BPCA4-DOX with excellent stability are capable of affording significantly superior anti-tumor activity and lower side effects.

Phytoecdysteroids from Dianthus superbus L.: Structures and anti-neuroinflammatory evaluation.

Six undescribed C27-phytoecdysteroid derivatives, named superecdysones A-F, and ten known analogs were extracted from the whole plant of Dianthus superbus L. Their structures were identified by extensive spectroscopy, mass spectrometric methods, chemical transformations, chiral HPLC analysis, and the single-crystal X-ray diffraction analysis. Superecdysones A and B possess a tetrahydrofuran ring in the side chain and superecdysones C-E are rare phytoecdysones containing a (R)-lactic acid moiety, whereas superecdysone F is an uncommon B-ring-modified ecdysone. Notably, based on the variable temperature (from 333 K to 253 K) NMR experiments of superecdysone C, the missing carbon signals were visible at 253 K and assigned. The neuroinflammatory bioassay of all compounds were evaluated, and 22-acetyl-2-deoxyecdysone, 2-deoxy-20-hydroxyecdysone, 20-hydroxyecdysone, ecdysterone-22-O-benzoate, 20-hydroxyecdysone-20,22-O-R-ethylidene, and acetonide derivative 20-hydroxyecdysterone-20, 22-acetonide significantly suppressed the LPS-induced nitric oxide generation in microglia cells (BV-2), with IC50 values ranging from 6.9 to 23.0 µM. Structure-activity relationships were also discussed. Molecular docking simulations of the active compounds confirmed the possible mechanism of action against neuroinflammations. Furthermore, none compounds showed cytotoxicity against HepG2 and MCF-7. It is the first report about the occurrence and anti-neuroinflammatory activity of the phytoecdysteroids in the genus Dianthus. Our findings demonstrated that ecdysteroids may be used as potential anti-inflammatory drugs.

Two different one-dimensional Cd(II) halide coordination polymers constructed through bridging carboxylate ligands.

Two cadmium halide complexes, catena-poly[[chloridocadmium(II)]-di-µ-chlorido-[chloridocadmium(II)]-bis[µ2-4-(dimethylamino)pyridin-1-ium-1-acetate]-κ(3)O:O,O';κ(3)O,O':O], [CdCl2(C9H12N2O2)]n, (I), and catena-poly[1-cyanomethyl-1,4-diazoniabicyclo[2.2.2]octane [[dichloridocadmium(II)]-µ-oxalato-κ(4)O(1),O(2):O(1'),O(2')] monohydrate], {(C8H15N3)[CdCl2(C2O4)]·H2O}n, (II), were synthesized in aqueous solution. In (I), the Cd(II) cation is octahedrally coordinated by three O atoms from two carboxylate groups and by one terminal and two bridging chloride ligands. Neighbouring Cd(II) cations are linked together by chloride anions and bridging O atoms to form a one-dimensional zigzag chain. Hydrogen-bond interactions are involved in the formation of the two-dimensional network. In (II), each Cd(II) cation is octahedrally coordinated by four O atoms from two oxalic acid ligands and two terminal Cl(-) ligands. Neighbouring Cd(II) cations are linked together by oxalate groups to form a one-dimensional anionic chain, and the water molecules and organic cations are connected to this one-dimensional zigzag chain through hydrogen-bond interactions.

Isostructural organic-inorganic hybrid compounds: triethylcholine tribromidocadmate and triethylcholine tribromidomercurate.

In order to search for new anionic architectures and develop useful organic-inorganic hybrid materials in halometallate systems, two new crystalline organic-inorganic hybrid compounds have been prepared, i.e. catena-poly[triethyl(2-hydroxyethyl)azanium [[bromidocadmate(II)]-di-µ-bromido]], {(C8H20NO)[CdBr3]}n, (1), and catena-poly[triethyl(2-hydroxyethyl)azanium [[bromidomercurate(II)]-di-µ-bromido]], {(C8H20NO)[HgBr3]}n, (2), and the structures determined by X-ray diffraction analysis. The compounds are isostructural, crystallizing in the space group P21/n. The metal centres are five-coordinated by bromide anions, giving a slightly distorted trigonal-bipyramidal geometry. The crystal structures consist of one-dimensional edge-sharing chains of MBr5 trigonal bipyramids, between which triethylcholine counter-cations are intercalated. O-H···Br hydrogen-bonding interactions are present between the cations and anions.

Toxic effects of copper on antioxidative and metabolic enzymes of the marine gastropod, Onchidium struma.

The goals of this study were to evaluate the acute and sublethal toxicity of copper (Cu(2+)) on the marine gastropod, Onchidium struma, and to examine the utility of enzymatic parameters as indicators of Cu(2+) exposure. In a semistatic renewal test, the 96-hour median lethal concentration of Cu(2+) for O. struma, 74.80 mg/L, was higher than that for other intertidal species. The activities of the antioxidative enzymes, Cu/Zn superoxide dismutase (Cu/Zn-SOD) and catalase (CAT), and those of the metabolic enzymes-acid phosphatase (ACP), alkaline phosphatase (AKP), glutamic-oxaloacetic transaminase (GOT), and glutamic-pyruvic transaminase (GPT) -in both hepatopancreas and muscle were determined after a 1-week exposure to Cu(2+) (range 1.35 to 4.20 mg/L). The activities of both Cu/Zn-SOD and CAT were higher in hepatopancreas than muscle. In addition, there was a negative correlation between Cu(2+) concentration and Cu/Zn-SOD activity in hepatopancreas, whereas a positive correlation was observed for CAT activity. Concentration-dependent changes in ACP and AKP activity showed a similar trend in hepatopancreas, increasing then decreasing and, finally, a slight increase. In contrast, ACP activity was positively correlated with Cu(2+) across the concentration range tested. In both hepatopancreas and muscle, both GOT and GPT were activated by lower concentrations of Cu(2+) and inhibited at higher concentrations.