Acetohydroxy acid synthase (EC 4.1.3.18; AHAS) isozymes I and III are expressed in Escherichia coli strain K-12 and, when inhibited by L-valine, cannot support cell growth. AHAS IV, expressed from mutation at ilvJ662, exhibits valine-sensitivity similar to that of AHAS III, yet AHAS IV does supp...

Over the course of many decades, life sciences have gained an insight into the structure–activity relationship of biologically active molecules, thereby allowing for a deeper understanding of how such molecules can be modified to produce the desired effect within a living organism. The introduc...

In nephrotic syndrome, significant amounts of plasma proteins, mostly of hepatic origin, are lost in urine. Total hepatic protein synthesis increases, suggesting that other protein pools must be conserved to maintain steady state. This can be accomplished either by decreased amino acid oxidation...

Twenty-four new dipeptide analogs (1–24) of aurantiamide acetate were designed, synthesized, and assayed for effects on superoxide anion generation and elastase release by human neutrophils in response to fMLP/CB. Among them, seven N-(fluorenyl-9-methoxycarbonyl) (Fmoc)-dipeptides (6, 9, 12, 14...

We report a validated method for the determination of extra- and intracellular [1-13C]-α-ketoisovalerate ([1-13C]-KIV) enrichments by gas chromatography–mass spectrometry. Standardization curves were prepared by enzymatic oxidation of [1-13C]-valine enriched standards of known composition. Slo...

A gas chromatographic–combustion isotope ratio mass spectrometric (GC–C-IRMS) method for the determination of [1-13C]valine enrichments in protein hydrolysates is described. Using a quick derivatization method, δ13C values of the N-methoxycarbonyl methyl ester of valine can be determined from...

Tyrosine kinase inhibitors (TKIs) have achieved substantial clinical effects for cancer treatment while causing a number of adverse effects. Since hypoxia is an intrinsic difference between solid tumor and healthy tissues, one strategy to overcome the adverse effects of TKIs is to enhance the sp...

ABSTRACTCombretastatin A-4 (CA-4) is a highly cytotoxic natural product and several derivatives have been prepared which underwent clinical trial. These investigations revealed that the cis-stilbene moiety of the natural product is prone to undergo cis/trans isomerization under physiological con...

A number of pyrimidine bridged combretastatin derivatives were designed, synthesized and evaluated for anticancer activities against breast cancer (MCF-7) and lung cancer (A549) cell lines using MTT assays. Most of the synthesized compounds displayed good anticancer activity with IC50 values in ...

To explore a new set of cytotoxic agents, β-carboline-combretastatin carboxamide conjugates were designed, synthesized and evaluated for their in vitro cytotoxicity potential, DNA binding affinity and Topoisomerase-II (topo-II) inhibition activity. Among the designed hybrids, 10v and 10af have ...

For the first time combretastatins were isolated from African willow tree Combretum Caffrum. Subsequent studies have shown the impact of combretastatin A4 phosphate, a water-soluble prodrug, on endothelial cells in tumor vascular system. The same effect was not observed in the vascular system. T...

Effective systemic therapy is highly desired for the treatment of hepatocellular carcinoma (HCC). In this study, a combination of nanoparticles of poly(L-glutamic acid)-graft-methoxy poly(ethylene glycol)/combretastatin A4 sodium salt (CA4-NPs) plus sorafenib is developed for the cooperative sys...

The combretastatins are isolated from South African tree combretum caffrum kuntze. The lead compound combretastatin A-4 has displayed remarkable cytotoxic effect in a wide variety of preclinical tumor models and inhibits tubulin polymerization by interacting at colchicine binding site of microtu...

To explore the application of photoremovable protecting groups (PPGs) in the field of combination chemotherapy, we designed and synthesized a photoresponsive hybrid prodrug 4 that bearing both doxorubicin (DOX) and combretastatin A4 (CA4). Light triggered drug release investigation found that DO...

Publisher SummarySterols, minor compounds present in dietary fat, comprise a major portion of the unsaponifiable matter of most vegetable oils. They are mainly present as free sterols and esters of fatty acids, in addition to sterol glucosides and acetylated. Vegetable oil sterols are collective...

We have investigated a new optically active photochromic homopolymer poly[(R)-3-methacryloyloxy-1-(4′-cyano-4-azobenzene)pyrrolidine] containing in the side-chain a chiral group of one prevailing configuration linked to a trans-azoaromatic system. As expected it exhibits in solution homogeneous...

SummaryThe supply of recreational drugs has changed in the early 2000s and users increasingly buy cathinones over the Internet. There is a potential for significant toxicity associated with their use. Cathinone named “NRG-3” seems to be the most popular in Parisian CEIP data: the adverse event...

The aep-PNA is a chiral and cyclic PNA analogue, which has a stronger and base dependent binding affinity with complementary DNA. To understand the base dependent properties at monomer level, the structural studies of aep-PNA-(T/C/A) monomers have been carried out focussing on the conformational...

Toxicity of the neonicotinoid pesticide thiacloprid to embryos and larvae of common carp Cyprinus carpio was assessed under laboratory conditions. Carp embryos and larvae were exposed to thiacloprid at four concentrations: 4.5 (environmental concentration), 45, 225, and 450 μg/L for 35 days and...

In this paper, a test strip-based sensor was developed for thiacloprid quantitative detection based on PDA molecularly imprinted polymer (MIP) and nitrogen-doped graphene quantum dots (N-GQDs). Thiacloprid is a new type of nicotine insecticide, which can block the normal neurotransmitter deliver...