Nitidine is a benzophenanthridine alkaloid, which has been shown to have anti-tumor properties. Here, we demonstrated that Nitidine Chloride (NC) could inhibit breast cancer cells migration and invasion both in vitro and in vivo. Meanwhile, the protrusion formation and partial proteolytic activi...
Nitidine Chloride (NC) has been shown to have anti-cancer effects on various tumors. However, whether NC could exert anti-metastasis activity in renal cancer cells and the underlying mechanisms have not been elucidated. In this work, our data demonstrated the anti-metastasis effects of NC on ren...
ObjectiveTo study the pharmacokinetics of nitidine chloride (NC) in rat plasma after intragastrical (i.g.) administration.
The treatment of bovine and equine piroplasmosis is limited to diminazene aceturate (DA) and imidocarb dipropionate. To address this challenge, we need to explore novel drug compounds and targets. Topoisomerases are potential drug targets because they play a vital role in solving topological err...
Nitidine chloride (NC) has demonstrated promising anticancer activity. However, NC has also shown non-specific toxicity in various healthy organs such as the liver. In this study, we aimed to develop a supramolecular formulation of NC and investigate the associated benefits of such a supramolecu...
In the effort to identify natural products that regulate immunity and inflammation, we found that nitidine chloride (NC), an alkaloid from herb Zanthoxylum nitidum, enhanced IL-10 production in lipopolysaccharide (LPS)-stimulated myeloid cells. While NC was shown to be capable of inhibiting topo...
BackgroundNitidine chloride (NC) is known to exert anticancer and anti-metastatic effects on a variety of tumors. Recently, NC has also been shown to inhibit PIK3/AKT/mTOR axis in U87 human glioma cells.
Nitidine chloride (NC) has been demonstrated to exert a tumor-suppressive function in various types of human cancers. However, the detailed mechanism of NC-mediated anti-tumor effects remains elusive. It has been reported that SIN1, a component of mTORC2 (mammalian target of rapamycin complex C2...
The effects on the inhibition potencies of monoamine oxidase isoforms A (MAO-A) and B (MAO-B) depending upon changes in the physicochemical properties (size, shape, H-bonding, lipophilicity, etc.) of substituents at the C4 position of 2H-chromen-2-one derivatives were extensively investigated, a...
Novel 2-chloro-4-anilino-quinazolines designed as EGFR and VEGFR-2 dual inhibitors were synthesized and evaluated for inhibitory effects. EGFR and VEGFR-2 are validated targets in cancer therapy and combined inhibition might be synergistic for both antitumor activity and resistance prevention. T...
The purpose of this study is to try to identify the etiology and formulation implications of the significant pKa drop in aqueous solution that occurs when boronic acids are reversibly esterified by reaction with alcohols, especially 1,2-diols. Experimental studies have shown that conversion of a...
In response to the widespread use of β-lactam antibiotics bacteria have evolved drug resistance mechanisms that include the production of resistant Penicillin Binding Proteins (PBPs). Boronic acids are potent β-lactamase inhibitors and have been shown to display some specificity for soluble tr...
This work presents an analytical procedure based on gas chromatography–mass spectrometry which allows the determination of aldoses (glucose, mannose, galactose, arabinose, xylose, fucose, rhamnose) and chetoses (fructose) in plant material.One peak for each target carbohydrate was obtained by u...
A capillary gas chromatographic method has been developed to quantitate the methylboronic acid in a lyophilized formulation. The formulation is first dissolved in 1 M hydrochloric acid. Next a tetrahydrofuran solution of the internal standard, 1-butaneboronic acid, and a methylene chloride solut...
We developed a complete method to measure low [13C] enrichments in glycogen. Fourteen rats were fed a control diet. Six of them also ingested either [U-13C] glucose (n = 2) or a mixture of 20 [U-13C] amino acids (n = 4). Hepatic glycogen was extracted, digested to glucose and purified on anion–...
Methylboronic acid–methylboronate interchange has been studied kinetically by the band shape analysis of 11B NMR signals. The system was analyzed as two-site exchange CH3B(OH)2⇌CH3B(OH)3 − for a self-buffered aqueous solution in pH 9.5–11.4 at 24–55°C. The exchange rate was expressed as: rat...
A stereoselective method for the preparation of dibenzoxapine containing tetrasubstituted exocyclic E-alkenes has been developed. The key reaction involves an intramolecular cyclocarbopalladation of alkynes to form a vinylpalladium species and subsequently coupling the vinylpalladium with methyl...
A simple procedure for the separation of cis–trans-stereoisomeric 1,2-diols by the selective esterification of cis-isomer with methylboronic acid is described.
The solid phase FTIR and FT-Raman spectra of methylboronic acid (MBA) have been recorded in the regions 400–4000 and 50–4000 cm−1, respectively. The spectra were interpreted interms of fundamentals modes, combination and overtone bands. The structure of the molecule was optimized and the struc...
Dipeptidyl peptidase III (DPP III), also known as enkephalinase B, is a zinc-hydrolase with an indicated role in the mammalian pain modulatory system. In order to find a potent antagonist of this enzyme, we synthesized and screened the effect of a small set of benzimidazole derivatives on its ac...
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