As part of our on-going effort to explore the role of dopamine receptors in drug addiction and identify potential novel therapies for this condition, we have a identified a series of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamide D3 ligands. Members of this class are highly sele...

Biguanide (CAS#56-03-01) is a parent compound that is used to synthesize drugs for controlling noninsulin-dependent diabetes mellitus (Type II), or NIDDM. Three clinically important biguanides that were released into the market are buformin, phenformin, and metformin. Phenformin was withdrawn fr...

Conclusion of the opinion: On the basis of the data available, the SCCS concludes that Polyaminopropyl Biguanide (PHMB) is not safe for consumers when used as a preservative in cosmetic spray formulations and in all cosmetic products up to the maximum concentration of 0.3%. The safe use could be...

4-(4′-diamino-di-phenyl)-sulfone supported on hollow magnetic mesoporous (HMMS) Fe3O4@SiO2 NPs has been used as a novel and efficient catalyst in the preparation of ethyl 2-amino-5,10-dihydro-5,10-dioxo-4-phenyl-4H benzo[g]chromene-3-carboxylates by a simple one-pot three-component reaction of ...

The complexity of Alzheimer's disease (AD) calls for search of multifunctional compounds as potential candidates for effective therapy. A series of phthalimide and saccharin derivatives linked by different alicyclic fragments (piperazine, hexahydropyrimidine, 3-aminopyrrolidine or 3-aminopi...

Four optical isomers of SIPI5056 were synthesized and evaluated for their antidepressant activities and acute toxicities as novel multiple reuptake inhibitors of monoamine transmitters. Chiral alanines were used as educts to prepare their respective target compounds in nine steps. Pharmacologica...

2-(3-Methoxyphenyl)-5-methyl-1,8-naphthyridin-4(1H)-one (HKL-1), a 2-phenyl-1,8-naphthyridin-4-one (2-PN) derivative, was synthesized and evaluated as an effective antimitotic agent in our laboratory. However, the molecular mechanisms are uncertain. In this study, HKL-1 was demonstrated to induc...

As a part of studies on biologically active molecule structures with aliphatic linking chain, the structures of 4-[2-diphenylmethylamino)ethyl]-1-(2-methoxyphenyl)piperazine dihydrochloride (1) and 4-[2-diphenylmethoxy)ethyl]-1-(2-methoxyphenyl)piperazine fumarate (2) have been reported. In both...

The synthesis and proteolysis of the spore coat proteins, SpoIVA and YrbA, of Bacillus subtilis were analyzed using antisera. Almost no intact full-length proteins of either type were extracted from wild-type spores, while yabG mutant spores contained intact SpoIVA and YrbA proteins. We purified...

Screening studies aimed at identifying useful biomedical materials that (when combined with implants) can attract bone morphogenetic proteins to their surfaces have been conducted. In this paper, the screening process has involved carrying out protein adsorption studies using cytochrome C, as a ...

The Bacillus subtilis spore coat consists of three morphological layers: a diffuse undercoat, a striated inner coat and a densely staining outer coat. These layers are comprised of at least 15 polypeptides and the absence of one particular, CotE, had extensive pleiotropic effects. Only a partial...

Tobacco has long been considered as a host to produce large quantity of high-valued recombinant proteins. However, dealing with large quantities of biomass is a challenge for downstream processing. Aqueous two-phase extraction (ATPE) has been widely used in purifying proteins from various source...

A variety of fatty acids can become covalently attached to platelet proteins by thioester linkage. These fatty acids include palmitate, myristate, stearate, arachidonate, and eicosapentaenoate. More than 20 platelet proteins can be acylated by fatty acids. Several of the acylated platelet protei...

Conventional farming still consumes considerable amounts of antibiotics such as sulfadiazine (SDZ) or difloxacin (DIF) to protect livestock from infectious diseases. Consequently, slurries from medicated animals are applied to arable soils. Antibiotics, co-applied with pig slurry, are increasing...

Polyamines are ubiquitous positively charged metabolites that play an important role in wide fundamental cellular processes; because of their importance, the homeostasis of these amines is tightly regulated. Spermine synthase catalyzes the formation of polyamine spermine, which is necessary for ...

One of the approaches clinically used for the early diagnosis of cancer is based on the detection and quantification of spermine from the urine. Herein, we have developed platforms of ionic self-assemblies ENS-1 and ENS-2 which elicit highly selective fluorescence quenching with spermine. ENS-1 ...

This study describes the synthesis of fluorescent probes as potential substrates for the polyamine transport system (PTS) of Leishmania donovani. A competitive radioassay was used to determine the most efficient probe. We observed that the conjugate spermine-nitrobenzofurazan (Spm-NBD) was able ...

In this work, a simple, one step and eco-friendly synthetic strategy is developed for the fabrication of gold nanoclusters (Au NCs) using pepsin as a reducing and capping agent. The pepsin-Au NCs (P-Au NCs) displayed the excitation and emission peaks at 416 and 655 nm, and exhibiting red lumines...

Spermine and spermidine are polyamines (PA) naturally present in all organisms, in which they have important physiological functions. However, an excess of PA has been associated with health risks. PA accumulates at quite high concentrations in some foods, but a quantitative assessment of the ri...

We develop a novel and fast colorimetric sensing platform for spermine (Sp) by using macrocyclic host hydroxyl pillar[5]arene (P5) molecule reduced and stabilized Au nanoparticles via the supramolecular host-guest recognition interaction between P5 and Sp. The P5-modified Au nanoparticles (P5-Au...