Design and Synthesis of Thiourea-Conjugating Organic Arsenic D-Glucose with Anticancer Activities.

Organic arsenic compounds such as -aminophenylarsine oxide (-APAO) are easier for structural optimization to improve drug-like properties such as pharmacokinetic properties, therapeutic efficacy, and target selectivity. In order to strengthen the selectivity of 4-(1,3,2-dithiarsinan-2-yl) aniline 7 to tumor cell, a thiourea moiety was used to strengthen the anticancer activity. To avoid forming a mixture of α/β anomers, the strategy of 2-acetyl's neighboring group participation was used to lock the configuration of 2,3,4,6-tetra--acetyl-β-d-glucopyranosyl isothiocyanate from 2,3,4,6-tetra--acetyl-α-d-glucopyranosyl bromide.

Method for the extraction of circulating nucleic acids based on MOF reveals cell-free RNA signatures in liver cancer.

Cell-free RNA (cfRNA) allows assessment of health, status, and phenotype of a variety of human organs and is a potential biomarker to non-invasively diagnose numerous diseases. Nevertheless, there is a lack of highly efficient and bias-free cfRNA isolation technologies due to the low abundance and instability of cfRNA. Here, we developed a reproducible and high-efficiency isolation technology for different types of cell-free nucleic acids (containing cfRNA and viral RNA) in serum/plasma based on the inclusion of nucleic acids by metal-organic framework (MOF) materials, which greatly improved the isolation efficiency and was able to preserve RNA integrity compared with the most widely used research kit method.

A Novel Imidazolinone Derivative with 5-Arylidene and 2-Substituted Mercapto Group as Potent Anti-Hepatitis C Virus Compound.

Here six novel imidazolinone derivatives have been synthesized and the compound 4b containing 5-para-methoxy-phenylidene and 2-thioalkylation terminal substitution with 3'-cyano-2',6'-dimethylphenyl showed the best anti-HCV activity and the lowest cytotoxicity. Selectivity index (SI=CC /IC ) for the 4b was determined as 36, indicating that compound 4b was highly selective towards HCV.

Synthesis and pharmacological characterization of glucopyranosyl-conjugated benzyl derivatives as novel selective cytotoxic agents against colon cancer.

Glucopyranosyl-conjugated benzyl derivatives containing a [1,2,3]-triazole linker were synthesized. Benzyl served as an important pharmacophore in anti-cancer compounds. Compound inhibited the proliferation of colorectal cancer cells with the potency comparable to 5-fluorouracil (5-FU) with improved selectivity towards cancer cells.

Chitosan quaternary ammonium salt induced mitochondrial membrane permeability transition pore opening study in a spectroscopic perspective.

Chitosan is non-toxic, biodegradable and biocompatible. However, it is insoluble in water, which limits its applications in biomedical areas. Hydroxypropyltrimethyl ammonium chloride chitosan (HACC), a chitosan derivative, can be dissolved in physiological condition and has been widely used in the field of biomedicine and bioengineering.

Microcalorimetric and microscopic studies of the effect of chitosan quaternary ammonium salt on mitochondria.

Chitosan quaternary ammonium salt (HACC) has been regarded as an effective biomedical carrier with good application because of its good water-solubility, high cationic potential and strong cell adhesion. Mitochondria are important organelle involved in ATP production and are the center of energy metabolism. In this work, we firstly investigated the effect of HACC on the thermogenic curve of isolated mitochondrial metabolism by microcalorimetry.

Exploring 6-Azaindole and 7-Azaindole Rings for Developing Cannabinoid Receptor 1 Allosteric Modulators.

Org27569 is a prototypical allosteric modulator of the cannabinoid receptor 1 (CB). It belongs to the indole-2-carboxamide scaffold and has been intensively investigated in pharmacology and in structure-activity relationship (SAR) studies. Although azaindoles are rare in natural products and differ only by the presence of an extra ring nitrogen, they were demonstrated as valuable bioisosteres in many pharmacologically important molecules.

Carbohydrate-conjugated 4-(1,3,2-dithiarsolan-2-yl)aniline as a cytotoxic agent against colorectal cancer.

Arsenic trioxide (AsO) has been approved for the treatment of acute promyelocytic leukemia (APL); however, its use in the treatment of solid tumors is limited due to its pharmacokinetic properties. Organic arsenic compounds provide better options for pharmaceutical optimization. -Aminophenyl arsenoxide (-APAO), an organic arsenic compound, was found to interact with the promyelocytic leukemia-retinoic acid receptor alpha (PML-RARα) fusion protein in a similar manner to arsenic trioxide.

Chitosan combined with swimming promotes health in rats.

Purpose: Chitosan is an easily accessible and biocompatible natural molecule which facilitate the immune system. In recent studies, chitosan is being applied to the drug nanosphere to deliver drugs. However, whether chitosan could promote health under exercising condition remains yet to be elucidated.

Physical, antibacterial and antioxidant properties of chitosan films containing hardleaf oatchestnut starch and Litsea cubeba oil.

More and more attention was attached to food safety, it is necessary to endow food packaging films with good antibacterial and antioxidant properties Edible films based on chitosan (CH), hardleaf oatchestnut starch (HOS) and Litsea cubeba oil (LEO) were prepared by solution casting. The properties and structures of the blend film with different proportion (xCH/yHOS) were evaluated. The CH-HOS films were firstly prepared by blending CH solution with HOS paste.

Pyrimidinyl Biphenylureas: Identification of New Lead Compounds as Allosteric Modulators of the Cannabinoid Receptor CB.

The allosteric modulator 1-(4-chlorophenyl)-3-(3-(6-(pyrrolidin-1-yl)pyridin-2-yl)phenyl)urea (PSNCBAM-1, 2) bound the cannabinoid receptor 1 (CB) and antagonized G protein coupling. This compound demonstrated potent anorectic effects similar to the CB antagonist rimonabant that once was marketed for the treatment of obesity, suggesting a new chemical entity for the discovery of antiobesity drugs. To increase structural diversity of this class of CB ligands, we designed and synthesized two classes of novel analogues, in which the pyridine ring of 2 was replaced by a pyrimidine ring.

Operationally simple hydrotrifluoromethylation of alkenes with sodium triflinate enabled by Ir photoredox catalysis.

We report herein a single component Ir photoredox catalyst which is capable of catalyzing the hydrotrifluoromethylation of terminal alkenes and Michael acceptors with sodium triflinate (Langlois reagent) in methanol under irradiation at room temperature. Various synthetically useful functional groups, including ester, amide, ether, aldehyde, sulfone, ketone and aryl boronate, are well tolerated in this reaction.

Nd(III)-induced rice mitochondrial dysfunction investigated by spectroscopic and microscopic methods.

The production capacity and yield of neodymium (Nd) in China have ranked the first in the world. Because of its unique biophysical and biochemical properties, Nd compounds have entered into the agricultural environment greatly to promote plant growth. Mitochondria play a crucial role in respiration and metabolism during the growth of plants.

A twisted intramolecular charge transfer probe for rapid and specific detection of trace biological SO2 derivatives and bio-imaging applications.

We reported a reactive probe for HSO3(-), which showed a colorimetric and ratiometric fluorescence response to HSO3(-) with fast response (t1/2 = 20 s), good specificity and low detection limit (3.0 nM). The probe was cell membrane permeable and successfully used for visualizing trace SO2 derivatives in living cells.

Effect of orally administered hydroxypropyl chitosan on the levels of iron, copper, zinc and calcium in mice.

Two hydroxypropyl chitosan HPCS samples (HPCS1 Mw 1.6 × 10(5), HPCS2 Mw 3.5 × 10(4)) were prepared by the reaction of chitosan with propylene oxide under alkali conditions.

A novel and photostable pH probe for selectively staining nuclei in living cells.

A novel pH probe based on hemi-cyanine was synthesized, which displays extremely large Stokes shift (122 nm) and good photostability. The probe responds to basic pH (pKa 8.32) with a colorimetric and fluorescence turn-on signal.

Total synthesis of landomycin A, a potent antitumor angucycline antibiotic.

The first total synthesis of landomycin A, the longest and most potent antitumor angucycline antibiotic, has been achieved in 63 steps and 0.34% overall yield starting from 2,5-dihydroxybenzoic acid, 3,5-dimethylphenol, triacetyl d-glucal, and d-xylose, with a convergent linear sequence of 21 steps.

Cationic porphyrins and analogues as new DNA topoisomerase I and II inhibitors.

A series of cationic porphyrins, and analogues such as cationic corroles and phthalocyanines were found to have biological activities towards topoisomerases I and II in vitro. Cationic porphyrins and phthalocyanines do not induce Topo I-DNA covalent complexes but inhibit topoisomerase I by direct binding to DNA, which limits topoisomerase I access to the DNA substrate. The lowest concentration where an inhibition effect is clearly visible of some derivatives is between 0.

Cationic metal-corrole complexes: design, synthesis, and properties of guanine-quadruplex stabilizers.

A series of pyridinium and quaternary ammonium copper corroles has been designed and synthesized. All new compounds have been fully characterized by NMR spectroscopy, high-resolution mass spectrometry, UV/Vis spectrscopy, and elemental analysis. Biochemical studies have indicated that all of these corrole derivatives can stabilize G-quadruplex structures, with corrole 4 being the most effective according to the results of circular dichroism (CD) melting experiments, polymerase chain reaction (PCR) stop assays, and surface plasmon resonance (SPR) experiments.

Cationic corrole derivatives: a new family of G-quadruplex inducing and stabilizing ligands.

Water-soluble cationic corrole derivatives were designed and synthesized, and the first observation of their interactions with the telomeric G-quadruplex was made.