The objective of this study was to evaluate the effects of combination therapy with methylene blue (MB) assisted photodynamic therapy (PDT) and salicylic acid (SA) as chemo-therapy anticancer agent. The binding of salicylic acid to methylene blue was studied using spectrophotometric method. The ...

PurposeThe aim of current study was to use methylene blue-curcumin ion pair nanoparticles and single dyes as photosensitizer for comparison of photodynamic therapy (PDT) efficacy on MDA-MB-231 cancer cells, also various light sources effect on activation of photosensitizer (PS) was considered.

Patients with triple negative breast cancer can develop side effects as a result of chemotherapy. Photodynamic therapy may reduce these side effects if the chemotherapy agent could also act as a photosensitizer. Thus, the aim of this work was to evaluate cytotoxicity and reactive oxygen species ...

Resolutions of butanoic esters of 1-phenoxy-2-propanol, 1-phenylmethoxy-2-propanol and 1-(2-phenylethoxy)-2-propanol have been studied with four different lipases as catalysts. Using lipase B from Candida antarctica very high enantiomer ratios were obtained. These substrate-lipase pairs represen...

With the aim of discovering potential and selective inhibitors targeting ROS1 kinase, we rationally designed, synthesized and evaluated two series of novel 2-amino-pyridine derivatives with 1-phenylethoxy at C-3 and C-4 position. The enzymic assays results indicated that six of the new compounds...

15-Keto-13,14-dihydro 6-ketoprostaglandin E1 was positively identified by gas chromatography-mass spectrometry with negative-ion chemical ionisation detection from samples of rat kidney high-speed supernatant incubated with prostaglandin I2 in the presence of NAD+. A decreased formation of this ...

Various resistance mechanisms such as complex formation with DNA, tRNA and MDR1 p-glycoprotein were modified in bacteria and cancer cells in presence of pregnane, pyridoquinoline, and aza-oxafluorene derivatives. Interaction between the compounds, plasmid DNA and tRNA was shown and compared to t...

Quinoline, isoquinoline, quinoxaline, and quinazoline derivatives were synthesized using microwave-assisted synthesis and their CB1/CB2 receptor activities were determined using the [35S]GTPγS binding assay. Most of the prepared quinoline, isoquinoline, and quinoxalinyl phenyl amines showed low...

[RuCl2(p-cymene)]2 efficiently catalyzes the rearrangement of 2-aryl-2-(phenylthio)penta-3,4-dienyl 2,2,2-trichloroacetimidate to afford (Z)-2,2,2-trichloro-N-(4-aryl-1-(phenylthio)penta-2,4-dien-2-yl)acetamide. Ru carbene is assumed as the reactive intermediate in this rearrangement.

The first enantioselective synthesis of (2S,3S,4R)-3,4-dihydroxyglutamic acid was efficiently achieved in six steps from (3R,4R,5R)-1-tert-butoxycarbonyl-3,4-epoxy-5-(1-ethoxy)ethoxymethyl pyrrolidin-2-one 4 derived from (S)-pyroglutaminol.

A peculiar kinetic resolution of E-1-(2-furyl)-2-buten-1-ol (1), which produced two oxidation products, pyranone (2) and epoxyalcohol (3), was developed by using the modified Sharpless reagents. A short synthesis of (+)-Asperlin was achieved starting from the optically active resolution products.

The Paternò–Büchi reaction between 2-furylmethanol derivatives and aliphatic aldehydes and ketones induced by irradiation through Vycor at 8°C shows high regioselectivity but no stereoselectivity. This behaviour can be rationalised by assuming that this type of compound reacts through both s...

Dextrorotatory 1-amino-3′,4′-dichlorobenzylphosphonic acid was found to be a potent inhibitor of the plant enzyme phenylalanine ammonia-lyase both in vitro and in vivo from among the ring-substituted 1-aminobenzylphosphonic acids and other analogues of phenylglycine. A structure activity relat...

The synthesis of enantiomerically pure non-proteinogenic bis and cyclic amino acids 3a,b and achiral amino acid 3c using chiral NiII complex 1 and α,α′-dibromo-o-xylene as a bifunctional agent of alkylation is presented.

α,α-Disubstituted amino acid derivatives are synthesized either by a self-regeneration of stereocenter strategy or using the asymmetric Strecker reaction/alkylation method. Of the four types of substrates tested for intramolecular acylation, those with a 4-alkoxyl group do not react, those wit...

We have postulated that molecules engineered to participate in three chemically distinct and linearly independent intermolecular interactions will self-assemble in a predictable fashion. Six prototypes for molecules capable of manifesting such interactions were synthesized from 2-aminoindan-2-ca...

Incubation of rat hepatocytes with oleate for a period of 1 h gave rise to a decrease in the total (esterified plus unesterified) cholesterol associated with very-low-density lipoprotein (VLDL). This effect was no longer apparent after longer incubation periods. The rate of cholesterol biosynthe...

The 7α-methyl analog (II) of 3β-hydroxy-5α-cholest-8(14)-en-15-one (I) was prepared by chemical synthesis and evaluated with respect to its effects on HMG-CoA reductase activity in CHO-K1 cells and on serum cholesterol levels in rats. The 7α-methyl substitution had no detectable effect on th...

Cholesterol crystals treated with an aqueous solution of sodium oleate give rise to cylindrical lamellar associations which appear under the microscope as rapidly growing tubes. Myelin forms are also obtained with other membrane sterols (desmosterol, cholestanol, 7-dehydrocholesterol) but not wi...

Summary5α-Cholest-8(14)-en-3β-ol-15-one, a potent inhibitor of cholesterol biosynthesis with hypocholesterolemic activity, has been found to serve as an efficient substrate for acyl CoA:cholesterol acyl transferase of rat hepatic and jejunal microsomes and to inhibit the esterification of chol...