The Hypocholesterolemic Effects of F. Delaroche Are Mediated by the Involvement of the Intestinal Transporters ABCG5 and ABCG8.

Hypercholesterolemia is a metabolic disorder characterized by a high concentration of cholesterol in the blood. is a medicinal plant used to treat lipid diseases. The goal of this work was to evaluate, in a model of hypercholesterolemia in mice, the hypocholesterolemic effect of a hydroalcoholic extract of and its main metabolite, D-mannitol.

Future therapeutic targets for the treatment and prevention of cholesterol gallstones.

The formation of cholesterol gallstones involves very complex imbalances, such as alterations in the secretion of biliary lipids (which involves the ABCG5, ABCG8, ABCB4 and ABCB11 transporters), biochemical and immunological reactions in the gallbladder that produce biliary sludge (mucins), physicochemical changes in the structure of cholesterol (crystallization), alterations in gallbladder motility, changes in the intestinal absorption of cholesterol (ABCG5/8 transporters and Niemann-Pick C1L1 protein) and alterations in small intestine motility. Some of these proteins have been studied at the clinical and experimental levels, but more research is required. In this review, we discuss the results of studies on some molecules involved in the pathophysiology of gallstones that may be future therapeutic targets to prevent the development of this disease, and possible sites for treatment based mainly on the absorption of intestinal cholesterol (Niemann-Pick C1L1 and ABCG5/8 proteins).

Raphanus sativus L. var niger as a source of phytochemicals for the prevention of cholesterol gallstones.

Raphanus sativus L. var niger (black radish) is a plant of the cruciferous family with important ethnobotanical uses for the treatment of gallstones in Mexican traditional medicine. It has been established that the juice of black radish decreases cholesterol levels in plasma and dissolves gallstones in mice.

Antilithiasic and hypolipidaemic effects of Raphanus sativus L. var. niger on mice fed with a lithogenic diet.

In Mexico, Raphanus sativus L. var. niger (black radish) has uses for the treatment of gallstones and for decreasing lipids serum levels.

Behavioural actions of two new 1-N substituted analogues of melatonin.

Melatonin has been mainly used for alleviating some disorders related with insomnia and circadian rhythmicity. The use of this hormone has been limited, among others, due to its short half-life and instability. This study reports some behavioural actions of two new melatonin analogues that incorporate a phenyl or a benzoyl group at the nitrogen atom of the melatonin molecule.

The biological activity of derivatives of 2-[(o-; and p-substituted)aminophenyl]-3H-5-[(o-; and p-substituted)phenyl]-7-chloro-1,4-benzodiazepines and 1-alkyl-3H-5-[(o-; and p- substituted) phenyl]-7-chloro-1,4-benzodiazepin-2-one.

Eight of a series of twelve new 2-[(o-; and p-substituted)aminophenyl]-3H-5-[(o-; and p-substituted)phenyl]-7-chloro-1,4-benzodiazepinines (VI, 1-12; Fig. 1) and two of eleven new 1-alkyl-3H-5-[(o-; and p-substituted)phenyl]-7-chloro-1,4-benzodiazepin-2-one (IV, 1-12; Fig. 2) were tested for their pharmacological and/or biological activity as anxiolytics.

Cross-talking between 5-HT3 and GABAA receptors in cultured myenteric neurons.

We recorded whole-cell ion currents induced by gamma-aminobutyric acid (I(GABA)) and serotonin (I(5-HT)) to investigate and characterize putative interactions between GABA(A) and 5-HT(3) receptors in myenteric neurons from the guinea pig small intestine. I(GABA) and I(5-HT) were inhibited by bicuculline and ondansetron, respectively. Currents induced by the simultaneous application of both, GABA and 5-HT (I(GABA+5-HT)) were significantly lower than the sum of I(GABA) and I(5-HT), indicating the existence of a current occlusion.

New 5alpha-reductase inhibitors: in vitro and in vivo effects.

The enzyme 5alpha-reductase is responsible for the conversion of testosterone (T) to its more potent androgen dihydrotestosterone (DHT). This steroid had been implicated in androgen-dependent diseases such as: benign prostatic hyperplasia, prostate cancer, acne and androgenic alopecia. The inhibition of 5alpha-reductase enzyme offers a potentially useful treatment for these diseases.

Receptor-binding studies of 1-N-substituted melatonin analogues.

In order to analyse the relevance of the indole electronic region in the binding of melatonin to its receptors, we prepared several analogues with p-H, p-NO(2), p-MeO, p-F and p-Me of benzyl, benzoyl and phenyl substituents at position 1 of the melatonin skeleton. The electronic properties of the analogues, as calculated with the semiempirical method AM1, were correlated with their affinity for the melatonin receptor from chicken brain membranes. Different trends were observed for each compound series.

Anxiolytic-like actions of melatonin, 5-metoxytryptophol, 5-hydroxytryptophol and benzodiazepines on a conflict procedure.

Male Wistar rats (120-230 g) were used in these experiments. Some rats were deprived of water for 48 h before testing in a conflict procedure. Then, after 20 licks from a water bottle with a metal drinking tube, the animal received an electric shock (0.

Apamin blocks the direct relaxant effect of melatonin on rat ileal smooth muscle.

The present study investigated the mechanisms of melatonin-induced inhibition of the ileal smooth muscle contraction. Rat isolated ileal smooth muscle strips were stimulated in an organ bath using carbachol (CAR) or potassium chloride (KCl) depolarization. Under these conditions, melatonin produced a concentration-dependent inhibition of muscle contraction (mean inhibitory concentration, IC50: 17.

Melatonin modifies the spontaneous multiunit activity recorded in several brain nuclei of freely behaving rats.

Melatonin, a pineal hormone, released photoperiodically, was administered systemically in rats, previously implanted with semimicroelectrodes into six different brain structures. The multiunit electrical activity of these structures was recorded for 10 min before and 60 min after melatonin administration in unanesthetized, freely moving rats. Different melatonin doses (100, 200, 500, and 1000 micrograms/kg) produced changes in the electrical activity of all tested structures.