Effects of Zuccagnia punctata on the gastrointestinal tract in rats and mice.

A pharmacological evaluation of Zuccagnia punctata Cav. (Fabaceae) on the gastrointestinal tract was made in rats and mice. 2',4'-dihydroxychalcone and 2',4'-dihydroxy-3'-methoxychalcone were isolated from Zuccagnia punctata. The data reported in the present work indicate that the acetone extract and infusion of Zuccagnia punctata reduced intestinal transit in rats and mice and offered protection against ethanol-induced ulceration in rats. The Z. punctata effect could be due, in part, to the presence of 2',4'-dihydroxychalcone and 2',4'-dihydroxy-3'-methoxychalcone in this plant.

Sesquiterpene lactone dehydroleucodine selectively induces transient arrest in G2 in Allium cepa root meristematic cells.

Dehydroleucodine is a sesquiterpene lactone recently isolated from aerial parts of a medicinal herb, Artemisia douglasiana Besser. We have previously shown that 25 and 100 microM dehydroleucodine slowed down onion root growth by 30 and 70%, respectively, affecting neither cell viability nor cell elongation. In the present study we analyze the effect of dehydroleucodine on cell cycle phases in onion (Allium cepa L.) root meristematic cells synchronized with caffeine or caffeine and hydroxyurea. Synchronized root cells treated with 100 and 200 microM dehydroleucodine present an interphase lengthening of 5.2 h and 8.2 h, respectively. The S-phase length, estimated by [3H]thymidine incorporation assay, was 6 h for both control roots and roots that had been immersed in dehydroleucodine. The peak of [3H]leucine incorporation was observed 6 h after release from synchronization in controls and in dehydroleucodine-treated roots, indicating that protein synthesis in G2 was not affected. Thus, these results show that dose-dependently dehydroleucodine selectively induces a transient arrest of meristematic cell in G2 and that dehydroleucodine can be used experimentally as a cell cycle suppressor.

The sesquiterpene lactone dehydroleucodine reversibly inhibits Allium cepa L. root growth.

Here, we prove that dehydroleucodine, a sesquiterpene lactone, at low concentrations (25-100 microM) slowed down the Allium cepa L root growth by 22-70% respectively neither affecting cell viability nor cell size. Removal of the drug after 24 h incubation restored the normal growth rate of the roots. Higher concentrations (200 microM) of dehydroleucodine were deleterious for the roots. As cell size did not change, it is most likely that dehydroleucodine affected some event of cell division cycle making it longer. Thus, dehydroleucodine could be a useful tool to slow down cell proliferation.

Two new labdane diterpene glycosides from flowers of Baccharis medullosa DC.

From the flowers of Baccharis medullosa DC (Asteraceae) two new ent-labdane-type diterpene glycosides were isolated. Structures were established by application of various spectroscopic techniques. The sugar residues were identified after acid hydrolysis of the isolated products.

Icetexane and abietane diterpenoids from Salvia gilliessi.

One icetexane and two abietane diterpenes were isolated from the aerial parts of Salvia gilliesii, and characterized as 5-epi-icetexone; 12-hydroxy-11,14-diketo-6,8,12-abietatrien-19,20-olide and 6 alpha,12,19-trihydroxy-11,14-diketo-8,12-abietadien-20,7 beta-olide, respectively. The structures were established by analysis of their 1H and 13C NMR spectra with the aid of 2D experiments. The triterpene oleanolic acid was isolated from the same source.

The sesquiterpene lactone dehydroleucodine (DhL) affects the growth of cultured epimastigotes of Trypanosoma cruzi.

Here, we report an inhibitory effect of a sesquiterpene lactone dehydroleucodine (DhL) on the growth of Trypanosoma cruzi in culture. At concentrations of the drug between 5 and 10 microg/ml in the medium,the parasites remained alive for at least 4 days. Higher concentrations of DhL were lethal for the parasites within a few hours. The effect of DhL is irreversible. Morphological changes induced by DhL were also observed in the parasites. The effect of DhL was blocked by the presence of reducing substrates such as glutathione or dithiothreitol, but these agents were not able to reverse the effect of DhL if added 2 days after the start of drug exposure.

Effect of dehydroleucodine in experimental colitis in rats and mice.

Dehydroleucodine (DhL), a sesquiterpene lactone (SQL) of the guaianolide type isolated from Artemisia douglasiana Besser, shows a pharmacological cytoprotective effect and significantly prevents the formation of gastric and duodenal lesions induced by various necrotising agents in rodents. The effects of DhL, on two models of experimental colitis were examined. Colitis was produced in male Wistar rats by rectal instillation of 5 and 10% acetic acid, following the methods of Eliakim et al. and Le Duc et al., respectively. In mice colitis was produced by rectal instillation of 0.1 ml of 2,4,6-trinitrobenzene sulphonic acid (5 mg in 50% ethanol) (TNB) as previously described by Chin et al. In this study, the administration of DhL 40 mg kg(-1)(1 h before the induction of colitis) significantly decreased mucosal damage. This effect was consistent in both models. The protection provided by DhL was accompanied by significant decreases in diarrhoea and colon weight; and histologically normal mucosa without ulceration and mucus production were observed. This study shows that both TNB and acetic acid colitis can be pharmacologically controlled by DhL. Our results suggest that the protective activity of DhL in experimental colitis is mediated, at least in part, through the increase of glycoprotein synthesis, anti-inflammatory effect and inhibition of COX-2 induction, and by inhibiting the degranulation of cells containing monoamines.

Mucus synthesis and sulfhydryl groups in cytoprotection mediated by dehydroleucodine, a sesquiterpene lactone.

The aerial parts of Artemisia douglasiana have been used in folk medicine as a cytoprotective agent against the development of peptic ulcer. Dehydroleucodine [1], its active principle, significantly prevents the formation of gastric lesions induced by the exposure of the rats to absolute ErOH. It was found in this study that (a) pretreatment of rats with 1 (40 mg/kg, po) caused a significant increase in glycoprotein synthetic activity, approximately sevenfold as large as that of the control; and (b) pretreatment of the rats with the thiol reagent N-methylmaleimide (NEM) significantly diminished the cytoprotection provided by 1. However, the protective effect of 1 was not totally abolished by pretreatment with a combination of indomethacin and NEM, indicating additional mechanisms are involved in the cytoprotective action of 1.

Dehydroleucodine prevents ethanol-induced necrosis in the rat gastric mucosa. A histological study.

The aerial part of Artemisia douglasiana Besser (6) has been used in folk medicine as a cytoprotective agent against the development of peptic ulcer. The dehydroleucodine (DhL), its active principle, significantly prevents the formation of gastric lesions induced by the exposure of the rats to absolute ethanol orally administered. The stomachs of control and experimental rats (after ethanol and pretreated with DhL) were removed, opened along the greater curvature and studied under stereo microscope and with light and scanning electron microscope. Absolute ethanol produced focal visible hemorrhagic lesions, extensive hyperemia, vascular stasis, cell disruption, and necrosis of the mucosa. Abundant mass of mucus was observed with scanning. The stomachs of rats pretreated with DhL showed a reduction of lesions. No hemorrhage and hyperemia were observed. The epithelia of the mucosa had a cobblestone appearance, similar to control rats and was covered by a fine layer of mucus. The mechanism of the protective action of DhL is unknown although it seems to be related to endogenous prostaglandins (PG).

Dehydroleucodine prevents ethanol-induced necrosis in the rat gastric mucosa. A histological study

The aerial part of Artemisia douglasiana Besser (6) has been used in folk medicine as a cytoprotective agent against the development of peptic ulcer. The dehydroleucodine (DhL), its active principle, significantly prevents the formation of gastric lesions induced by the exposure of the rats to absolute ethanol orally administered. The stomachs of control and experimental rats (after ethanol and pretreated with DhL) were removed, opened along the greater curvature and studied under stereo microscope and with light and scanning electron microscope. Absolute ethanol produced focal visible hemorrhagic lesions, extensive hyperemia, vascular stasis, cell disruption, and necrosis of the mucosa. Abundant mass of mucus was observed with scanning. The stomachs of rats pretreated with DhL showed a reduction of lesions. No hemorrhage and hyperemia were observed. The epithelia of the mucosa had a cobblestone appearance, similar to control rats and was covered by a fine layer of mucus. The mechanism of the protective action of DhL is unknown although it seems to be related to endogenous prostaglandins (PG).

Dehydroleucodine prevents ethanol-induced necrosis in the rat gastric mucosa. A histological study

The aerial part of Artemisia douglasiana Besser (6) has been used in folk medicine as a cytoprotective agent against the development of peptic ulcer. The dehydroleucodine (DhL), its active principle, significantly prevents the formation of gastric lesions induced by the exposure of the rats to absolute ethanol orally administered. The stomachs of control and experimental rats (after ethanol and pretreated with DhL) were removed, opened along the greater curvature and studied under stereo microscope and with light and scanning electron microscope. Absolute ethanol produced focal visible hemorrhagic lesions, extensive hyperemia, vascular stasis, cell disruption, and necrosis of the mucosa. Abundant mass of mucus was observed with scanning. The stomachs of rats pretreated with DhL showed a reduction of lesions. No hemorrhage and hyperemia were observed. The epithelia of the mucosa had a cobblestone appearance, similar to control rats and was covered by a fine layer of mucus. The mechanism of the protective action of DhL is unknown although it seems to be related to endogenous prostaglandins (PG).

Dehydroleucodine prevents ethanol-induced necrosis in the rat gastric mucosa. A histological study.

The aerial part of Artemisia douglasiana Besser (6) has been used in folk medicine as a cytoprotective agent against the development of peptic ulcer. The dehydroleucodine (DhL), its active principle, significantly prevents the formation of gastric lesions induced by the exposure of the rats to absolute ethanol orally administered. The stomachs of control and experimental rats (after ethanol and pretreated with DhL) were removed, opened along the greater curvature and studied under stereo microscope and with light and scanning electron microscope. Absolute ethanol produced focal visible hemorrhagic lesions, extensive hyperemia, vascular stasis, cell disruption, and necrosis of the mucosa. Abundant mass of mucus was observed with scanning. The stomachs of rats pretreated with DhL showed a reduction of lesions. No hemorrhage and hyperemia were observed. The epithelia of the mucosa had a cobblestone appearance, similar to control rats and was covered by a fine layer of mucus. The mechanism of the protective action of DhL is unknown although it seems to be related to endogenous prostaglandins (PG).

Dehydroleucodine prevents ethanol-induced necrosis in the rat gastric mucosa. A histological study.

The aerial part of Artemisia douglasiana Besser (6) has been used in folk medicine as a cytoprotective agent against the development of peptic ulcer. The dehydroleucodine (DhL), its active principle, significantly prevents the formation of gastric lesions induced by the exposure of the rats to absolute ethanol orally administered. The stomachs of control and experimental rats (after ethanol and pretreated with DhL) were removed, opened along the greater curvature and studied under stereo microscope and with light and scanning electron microscope. Absolute ethanol produced focal visible hemorrhagic lesions, extensive hyperemia, vascular stasis, cell disruption, and necrosis of the mucosa. Abundant mass of mucus was observed with scanning. The stomachs of rats pretreated with DhL showed a reduction of lesions. No hemorrhage and hyperemia were observed. The epithelia of the mucosa had a cobblestone appearance, similar to control rats and was covered by a fine layer of mucus. The mechanism of the protective action of DhL is unknown although it seems to be related to endogenous prostaglandins (PG).

The gastric cytoprotective effect of several sesquiterpene lactones.

The aerial part of Artemisia douglasiana, used in folk medicine as a cytoprotective agent against the development of peptic ulcer, was studied, its active principle dehydroleucodine [1] isolated, and its pharmacological properties analyzed. In order to establish whether or not the reported activity is particular to sesquiterpene lactones, the study of the cytoprotective activity of several related guaianolides and pseudoguaianolides from plants was undertaken. Ludartin [3], 8-angeloyloxy-3-hydroxyguaia-3(15),10(14),11(13)-trien-6,12- olide [4], hymenin [5], mexicanin I [6], helenanin [7], and 9-O-desacetylsparthulin-2-O-angelate [8] were found to exhibit protection. Desacetoxymatricarin [2] did not show cytoprotective activity. The results obtained from the different sesquiterpene lactones studied suggest that the presence of the alpha-methylene-gamma-lactone moiety is, in principle, a requirement for the observed antiulcerogenic activity.

Furanoeremophilanes in Senecio filaginoides and S. pinnatus.

Aerial parts of Senecio filaginoides yielded two new furanoeremophilane type sesquiterpenoids: 6alpha-acetyloxy-10betaH-furanoeremophil-1-one, 1 and 6alpha-tiglinoyloxy-10betaH-furanoerernophil-1-one, 2. Their structures have been elucidated by spectroscopic data. From roots and aerial parts of S. pinnatus 1alpha-hydroxy-6betaangeloyloxy-10alphaH-furanoeremophil-9-one, 3 has been isolated.