Ethnopharmacological importanceCapsicum and ginger are used widely in human diets and in folklore medicines. Chemically, gingerol is a relative of capsaicin and both classes of compounds are notable for their spiciness and characteristic pungent aroma. Previous studies have demonstrated that the...

Microbial cytochrome P450 enzymes (CYPs) are able to mimic the metabolism of human CYPs. One challenge is to identify the respective drug metabolites and to compare substrate specificities to those of the human enzymes. In this study, a class VIII self-sufficient CYP from Aspergillus fumigatus (...

The use of molecules inspired by natural scaffolds has proven to be a very promising and efficient method of drug discovery. In this work, capsaicin, a natural product from Capsicum peppers with antitumor properties, was used as a prototype to obtain urea and thiourea analogues. Among the most p...

In order to develop a green method for the purification and valorization of lignin, pretreatment of the corncob enzymatic residue with p-toluenesulfonic acid was investigated. The effects of p-toluenesulfonic acid concentration, pretreatment temperature and time on the purity and structure of th...

The uptake of a14C radiolabelled fungicide and its effects on endomembranous lipid biosynthesis was studied in five-day-old etiolated wheat seedlings. An extraction procedure was performed to quantitate the amount of furconazole-cis in the underlying cells. A very fast penetration of the active ...

The consequences of the consumption of cannabinoids with other drugs of abuse are of particular medical relevance. Several studies investigated the ability of cannabinoids to induce a locomotor cross-sensitization to other addictive drugs, but results remain inconsistent. Therefore, we investiga...

(6aR,10aR)-9-(Hydroxymethyl)-6,6-dimethyl-3-(2-methyloctan-2-yl)-6a,7,10,10a-tetrahydrobenzo[c]chromen-1-ol (HU-210) is a synthetic cannabinoid, with a classical cannabinoid structure similar to Δ9-tetrahydrocannabinol (Δ9-THC). In this study, the in vitro metabolism of HU-210 was investigated...

Synthetic cannabinoid abuse and case reports of adverse effects have raised concerns about the pharmacologic mechanisms underlying in vivo effects. Here, a synthetic cannabinoid identified in abused products (HU-210) was compared to the effects of Δ9-THC and two other synthetic cannabinoid agon...

Anxiety disorders are one of the most prevalent classes of mental disorders affecting the general population, but current treatment strategies are restricted by their limited efficacy and side effect profiles. Although the cannabinoid system is speculated to be a key player in the modulation of ...

Calcipotriol (MC903) is a side chain analogue of the biologically active 1,25-dihydroxyvitamin D3 [1,25(OH)2D3]. Due to its anti-inflammatory and anti-proliferative effects on stromal cells, calcipotriol is a promising candidate for the local treatment of arthritis. In this preliminary work, we ...

Diminished expression of the α7 nicotinic acetylcholine receptor occurs in selected brain regions of patients with schizophrenia, which may account for pathophysiological abnormalities and some of the deficits in attention and information processing. In view of this neurotransmitter receptor de...

The anti-inflammatory properties of, particularly the α7, nicotinic acetylcholine receptors (nAChRs) in the peripheral immune system are well documented. There are also reports of anti-inflammatory actions of nicotine in the CNS, but it is unclear, whether this is due to activation or inhibitio...

A series of methyllycaconitine (1a, MLA) analogs was synthesized where the (S)-2-methylsuccinimidobenzoyl group in MLA was replaced with a (R)-2-methyl, 2,2-dimethyl-, 2,3-dimethyl, 2-phenyl-, and 2-cyclohexylsuccinimidobenzoyl (1b–f) group. The analogs 1b–f were evaluated for their inhibition...

To assess the role of the α7 neuronal nicotinic acetylcholine receptor in the discriminative stimulus properties of (−)-nicotine, this study investigated the ability of the α7 receptor antagonist methyllycaconitine to modulate the nicotine cue. In rats trained to discriminate (−)-nicotine from...

α7 nicotinic acetylcholine receptors (α7nAChRs) have been targeted to improve cognition in different neurological and psychiatric disorders. Nevertheless, no α7nAChR activating ligand has been clinically approved. Here, we investigated the effects of antagonizing α7nAChRs using the selective...

Results of studies on the molecular forms of canine motilin suggest that this hormone might be synthesized as a higher molecular weight precursor, as is the case for most other biologically active peptides. Chromatographic analysis of human duodenal mucosa extracts and of human serum, using moti...

Motilin is involved in the regulation of the fasting motility pattern in man and in dog, but may have a different role in other species. Immunoreactive motilin has been demonstrated in several species, but the sequence is mostly unknown. The aim of this study was to isolate and sequence the cDNA...

A new method for the synthesis of 1,3-disubstituted benzimidazole derivatives was developed using aza-Michael addition. The target compounds were synthesized in good yields and purity and tested on isolated hepatocytes for their toxicity and antioxidant activity. The antioxidant properties of th...

Eight new organotin(IV) complexes with 2,4,5-trifluoro-3-methoxybenzoic acid RnSn(O2CC6HF3OCH3)4−n (n = 3: R = Ph (1), PhCH2 (2), Me (3), n-Bu (4); n = 2: R = Ph (5), PhCH2 (6), Me (7), n-Bu (8)) have been synthesized. All complexes were characterized by elemental, IR, 1H and 13C NMR spectra ana...

Hydrothermal reactions of cadmium(II) or silver(I) salt, NaN3, 4-(imidazol-1-ylmethyl)benzonitrile (IBN) yield three coordination complexes, [Cd(L)2(H2O)2]·3H2O (1), [Cd3(L)5(OH)] (2) and [Ag2(L)2] (3) where HL=1-(5-tetrazolyl)-4-(imidazol-1-ylmethyl)benzene. The crystal structure analysis reve...