A microplate assay and a thin-layer chromatography (TLC) "in situ" assay based on the Ellman assay was used to screen for acetylcholinesterase inhibitors from ethyl acetate and methanol extracts of Brazilian medicinal plants of families that, according to the literature, have traditional uses that might be connected with acetylcholinesterase inhibition. Eighteen species belonging to Convolvulac...

Boesenbergia thorelii extract of rhizomes and its compounds were investigated for anti-allergic activities using antigen-induced β-hexosaminidase release in RBL-2H3 cells. From bioassay-guided fractionation, the chloroform fraction was separated to afford four compounds: asaronaldehyde (1), β-sitosterol-D-glucoside (2), protocatechuic acid methyl ester (3) and 2-hydroxy-1-(3, 4-dimethoxyphenyl)...

Chemical investigation of the 90% acetone extract of the branches and leaves of Sabina gaussenii led to the isolation of two new cinnamyl isovalerate derivatives (1-2) and eighteen known compounds (3-20). Their structures were determined mainly by means of MS, 1D- and 2D-NMR data, and this is the first time these compounds have been reported from this plant. The biological activity test results...

Tewtrakul, S., Subhadhirasakul, S., Kummee, S Anti-HIV-1 integrase activity of medicinal plants used as self medication by AIDS patients Songklanakarin J. Sci. Technol., 2006, 28(4) : 785-790 The extracts of selected medicinal plants used as self medication by AIDS patients were investigated for their inhibitory activities against HIV-1 integrase (HIV-1 IN) using the multiplate integration assa...

The effects of pharmacological agents on the T-type Ca2+ current were studied in dissociated spermatogenic cells from the mouse. Ca2+ currents were elicited by depolarization in 10 mM Ca2+ and recorded in the whole-cell configuration of the patch clamp technique. The T-type current was inhibited by the following compounds: PN200-110 (IC50 = 4 x 10(-8) M) > nifedipine (IC50 = 4 x 10(-7) M) > pim...

The cytosolic phospholipase A2α(cPLA2α) is one of the potential targets for anti-inflammatory drugs, since this enzyme plays a key role in the inflammation processes seen in health disorders, like asthma, allergic reactions, arthritis and neuronal diseases. In this study, cPLA2α inhibition by 43 methanol extracts from medicinal plants rich in polyphenols was determined. The eight most active ex...

BACKGROUND Knowledge of the structure-activity relationships of multidrug resistance protein 1 (MRP1, ABCC1) inhibitors may aid in developing potent inhibitors that can be used to circumvent MRP1-mediated multidrug resistance. MATERIALS AND METHODS Six stilbenes were examined for their ability to inhibit MRP1-mediated transport of 2',7'-bis-(carboxypropyl)-5(6)-carboxyfluorescein (BCPCF) from...

A series of thieno[2,3-d]pyrimidine-based hydroxamic acid hybrids was designed and synthesised as multitarget anti-cancer agents, through incorporating the pharmacophore EGFR, VEGFR2 into inhibitory functionality HDAC6. Three compounds (12c, 15b 20b) were promising hits, whereas (12c) exhibited potent inhibition (IC50=185 nM), EGFR (IC50=1.14 µM), mild HDAC6 (23% inhibition). Moreover, compound...

BACKGROUND The derivatives of thieno[2,3-b]thiophene belong to a significant category of heterocyclic compounds, which have shown a wide spectrum of medical and industrial application. RESULTS A new building block with two electrophilic center of thieno[2,3-b]thiophene derivatives 2 has been reported by one-pot reaction of diketone derivative 1 with Br2/AcOH in excellent yield. A variety of h...