We investigated the effect of hydroxyl substituted chalcone (1a) and some analogues (1b–d) on isolated rat liver mitochondria to gain new insights into cytotoxic mechanism these compounds. observed an inhibitory phosphorylation partial uncoupling compounds 1a 1d. Increased radical generation possible covalent interaction with cellular thiols resulted in glutathione (GSH) depletion modulation mitochondrial activities. Disruption interconnected mechanisms as electron transport chain energetic...

Cyclic C5-curcuminoid derivatives are synthetic analogues of the natural product curcumin possessing diverse pharmacological potential. We described earlier that some cyclic C5-curcuminoids display excellent cytotoxic activity against human neuroblastoma (SH-SY5Y) and grade IV astrocytoma (CCF-STTG1) cell lines in low nanomolar concentrations. Some tested have also proved to be able penetrate blood-brain barrier (BBB) model. discovered at same time certain structure related differences...

Investigation of in vitro hydroxyl radical scavenging (antioxidant) effect 4-methoxychalcone (1a) and its cyclic analogues (2a-4a), as well their substituted counterparts (1b-4b) was performed by means the Fenton-reaction initiated deoxyribose degradation assay short term (10 minute) long (240 experiments. The kinetic method provides possibility to investigate not only antioxidant (hydroxyl scavenger) but possible late prooxidant tested substances well. In studies compounds 2a, 2b 4b showed...

Abstract Cyclic chalcone analogues (2–5) and their ferrocenyl counterparts (6–10) were synthesized logP P388 cyctotoxity investigated. The structures of the newly compounds confirmed by IR 1H 13NMR spectroscopy. Comparison conjugation stereochemistry respective derivatives showed similar characteristics compared to ones with some higher degree in series. determined a validated RP-TLC method have TLC. results demonstrate that differences three dimensional shape, lipophilicity do not strong...

Background/Purpose: Online vendors seize the advantage of high demand on home-use, do-it-yourself dental bleaching products. The study aims to present uncontrolled online market products and provide evidence consumer safety risks associated with utilization peroxide content without dentist's supervision, also identify misleading insufficient information compromised product quality.Materials methodsA complex risk-based methodology was used including website evaluation focusing ingredients,...

The chemical susceptibility of the β-diketone linker between two aromatic rings in structure curcumin to hydrolysis and metabolism has made it crucial investigate structurally modified analogs without such shortcomings. synthesis twenty cyclic C5-curcuminoids is described this study order gain more insight into their anticancer structure-activity relationship (SAR). design included four different cyclanones five substituted aldehydes form four, five-membered subgroups. These model compounds...

Novel series of cyclic C5-curcuminoids 17a-j and 19-22 were prepared as cytotoxic agents evaluated against human neuroblastoma (SH-SY5Y) or grade IV astrocytoma (CCF-STTG1) cell lines in low (∼0.1 nM - 10 nM) concentrations. Among the tested 21 derivatives, 16 displayed potent antiproliferative activity with IC50 values nanomolar to picomolar range (IC50 = 7.483-0.139 nM). Highly active compounds like N-monocarboxylic derivative 19b 0.139 value N-alkyl substituted 11 0.257 proved some degree...

In earlier studies, cytotoxity of chalcones (1) and cyclic chalcone analogues E-2-arylidene-tetralones (2) -benzosuberones (3) towards various murine human tumour cells has been tested. Preliminary biochemical investigations showed the compounds to inhibit protein DNA syntheses. It was also found that affect cellular thiol status treated cells. order gain new insights into cytotoxic mechanism effects some previously investigated 2 3 derivatives on isolated rat liver mitochondria...

Interaction of some cyclic chalcone analogs, (E)-2-(4-X-benzylidene)-1-benzosuberone derivatives with bovine serum albumin (BSA) and human (HSA) has been investigated using UV-Vis spectroscopic methods. Recording the spectra compounds in presence BSA or HSA indicated interaction molecules hydrophobic binding site(s) proteins. Investigated analogs have shown remarkable topo I II inhibitory activity compared to camptothecin etoposide, respectively, at 40 μM concentration. The observed...

Background: Phenolic Mannich bases derived from hydroxychalcones show remarkable cytotoxic potencies towards cancer cell lines. However, the exact mechanism of action is still partially uncleared. Objective: Interaction two and their derivatives with calf thymus DNA (ctDNA) has been investigated. Methods: Thin-layer chromatography UV-Vis spectroscopic method were used for studying interaction. The binding constant determined by spectrophotometric titration. cleavage activity compounds was...

The enantioselective binding of three proton pump inhibitors (PPIs)-omeprazole, rabeprazole, and lansoprazole-to two key plasma proteins, α1-acid glycoprotein (AGP) human serum albumin (HSA), was characterized. interactions between PPI enantiomers proteins were investigated using a multifaceted analytical approach, including high-performance liquid chromatography (HPLC), fluorescence UV spectroscopy, as well in silico molecular docking. HPLC analysis demonstrated that all PPIs exhibited...

Cyclic C5-curcuminoid derivatives are synthetic analogues of the natural product curcumin possessing diverse pharmacological potential. We described earlier that some cyclic C5-curcuminoids display excellent cytotoxic activity against human neuroblastoma (SH-SY5Y) and grade IV astrocytoma (CCF-STTG1) cell lines in low nanomolar concentrations. Some tested have also proved to be able penetrate blood-brain barrier (BBB) model. discovered at same time certain structure related differences...

An isocratic stability-indicating HPLC assay method was developed to quantitate ethacrynic acid in solution formulations. Utilizing the method, main hydrolytic, and one of oxidative degradation products could be separated. The structure separated confirmed by negative ion-mode HPLC-MS. hydrolytic results previously reported sequence formation dimeric Michael adduct. One new metabolite has been identified. validated analytical can used a formulation 0.5-500 µg/ml concentration range.

A Gyógyszerészi Kémiai Intézet 2002. január 1-én alakult, mint a Pécsen 2000-ben indult gyógyszerészképzés egyik szakintézete. Az intézet végleges helyének kialakítása 2003. októberétől kezdődhetett meg. adminisztratív ügyek intézésére és az oktatással kapcsolatos feladatainak ellátására - augusztusától – októberéig PTE Egyetemi Gyógyszertár két helyiségében kapott ideiglenes elhelyezést. munkatársak november elején foglalták el Rókus utcai épület földszinti helyiségeit. Ezt követően...

Cyclic C5-curcuminoid derivatives are synthetic analogues of the natural product curcumin possessing diverse pharmacological potencies. We described earlier that some cyclic C5-curcuminoids display excellent cytotoxic activity against human neuroblastoma (SH-SY5Y) and grade IV astrocytoma (CCF-STTG1) cell lines in low nanomolar concentrations. Some tested have also proved to be able penetrate blood-brain barrier (BBB) model. discovered same time certain structure related differences...