M.J. Montero

Gastric antisecretory and antiulcer activities of an ethanolic extract of Bidens pilosa L. var. radiata Schult. Bip.

Bidens pilosa var. radiata Schult. Bip. is used in folk medicine to treat stomach disorders including peptic ulcers. The ethanolic extract (0.5-2 g/kg) decreased the gastric juice volume, acid secretion, as well as pepsin secretion in pylorus ligated rats. B. pilosa extract showed antiulcer activity against indomethacin-induced gastric lesions. The extract effectively inhibited gastric haemorrhagic lesions induced by ethanol, and with an effective dose of 2 g/kg being more potent than sucralfate (400 mg/kg). In contrast, ranitidine (50 mg/kg) failed to reduce these lesions. These results indicate that B. pilosa ethanolic extract exerts a cytoprotective effect in addition to its gastric antisecretory activity that could be due, partly at least, to the presence of flavonoids of which quercetin was identified by HPLC.

Analgesic, antipyretic and anti-inflammatory activity of the essential oil of Artemisia caerulescens subsp. gallica

The essential oil of Artemisia caerulescens subsp. gallica was observed to have analgesic, antipyretic and anti-inflammatory actions when administered intraperitoneally to rats and mice at doses one-fourth to one-third that of its LD50 of 1.35 ml/kg. Lysine acetylsalicylate was used as a reference compound.

Antihistaminic activity of pulegone on the guinea-pig ileum

Abstract— Pulegone, a natural monoterpene compound, has an antihistamine effect on guinea‐pig ileum. Its antagonism is of the competitive type (PA2 = 6.35) like that of mepyramine and dexchlorpheniramine, two H1‐antagonists, with PA2 values of 10.15 and 8.74, respectively.

Sedating and antipyretic activity of the essential oil of Calamintha sylvatica subsp. ascendens

The essential oil of Calamintha sylvatica subsp. ascendens exerts significant sedating and antipyretic activities in the rat. The components responsible for these activities appear to be the major monoterpenes present: pulegone, menthone and eucalyptol (1,8-cineol).

Pharmacologic effects of lactones isolated from pulsatilla alpin a subsp. aphfolia

Two lactone compounds, protoanemonin and anemonin, were determined in the flowering aerial parts of P. alpina subsp. apiifolia. Anemonin is the primary compound responsible for the antipyretic activity and both anemonin and protoanemonin participate in the sedating effect.

Antipyretic activity of α- and β-santonin

Abstract The antipyretic activity of two sesquiterpene lactones, β-santonin and arsubin, isolated from the lipid fraction of Artemisia coerulescens subsp. gallica was determined in rats along with the activity of α-santonin. In its α-and β-forms, santonin caused a decrease in the body temperature of rats made febrile by the subcutaneous injection of beer yeast. This decrease, more pronounced in the case of β-santonin, was dose-dependent and antagonized by pretreatment with haloperidol, an agent that also opposes the antipyretic activity of dopamine. These findings seem to show that the α- and β-forms of santonin act on rectal temperature in a way similar to dopamine.

JB‐9322, a new selective histamine H2‐receptor antagonist with potent gastric mucosal protective properties

1 JB‐9322 is a selective histamine H2‐receptor antagonist with gastric antisecretory activity and mucosal protective properties. 2 The affinity of JB‐9322 for the guinea‐pig atria histamine H2‐receptor was approximately 2 times greater than that of ranitidine. 3 In vivo, the ID50 value for the inhibition of gastric acid secretion in pylorus‐ligated rats was 5.28 mg kg−1 intraperitoneally. JB‐9322 also dose‐dependently inhibited gastric juice volume and pepsin secretion. In gastric lumen‐perfused rats, intravenous injection of JB‐9322 dose‐dependently reduced histamine‐, pentagastrin‐ and carbachol‐stimulated gastric acid secretion. 4 JB‐9322 showed antiulcer activity against aspirin and indomethacin‐induced gastric lesions and was more potent than ranitidine. 5 JB‐9322 effectively inhibited macroscopic gastric haemorrhagic lesions induced by ethanol. Intraperitoneal injection was effective in preventing the lesions as well as oral treatment. The oral ID50 value for these lesions was 1.33 mg kg−1. By contrast, ranitidine (50 mg kg−1) failed to reduce these lesions. In addition, the protective effect of JB‐9322 was independent of prostaglandin synthesis. 6 These results indicate that JB‐9322 is a new antiulcer drug that exerts a potent cytoprotective effect in addition to its gastric antisecretory activity.

Pharmacological screening and antimicrobial activity of the essential oil of Artemisia caerulescens subsp. Gallica

Pharmacological screening of Artemisia caerulescens extracts in conscious rats: the hippocratic screening method of Malone and Robichaud is chosen as the preliminary screening protocol. In vitro studies on the antimicrobial activity of the essential oil are conducted according to the agar plate diffusion method

Uterine inhibitory effect of reticuline.

Abstract— Reticuline, the most abundant benzylisoquinoleic alkaloid of Laurobasidium lauri, exerts a uterine inhibitory effect mainly related to a decrease in the concentration of cytosolic calcium available for contraction.

Pharmacology of JB-9315, a new selective histamine H2-receptor antagonist.

1. The histamine H2-receptor antagonistic activity and antisecretory and antiulcer effects of JB-9315 were studied in comparison with the standard H2 blocker ranitidine. 2. In vitro, JB-9315 is a competitive antagonist of histamine H2 receptors in the isolated, spontaneously beating guinea-pig right atrium, with a pA2 value of 7.30 relative to a value of 7.36 for ranitidine. JB-9315 was specific for the histamine H2 receptor because, at high concentration, it did not affect histamine- or acetylcholine-induced contractions in guinea-pig isolated ileum or rat isolated duodenum, respectively. 3. JB-9315 dose dependently inhibited histamine-, pentagastrin- or carbachol-stimulated acid secretion and basal secretion in the perfused stomach preparation of the anesthetized rat. In the pylorus-ligated rat after intraperitoneal administration, total acid output over 4 h was inhibited by JB-9315 with an ID50 of 32.8 mg/kg, confirming its H2-receptor antagonist properties. 4. JB-9315 showed antiulcer activity against cold stress plus indomethacin-induced lesions with an ID50 of 6.8 mg/kg. 5. JB-9315, 50 and 100 mg/kg, inhibited macroscopic gastric hemorrhagic lesions induced by ethanol. In contrast, ranitidine (50 mg/kg) failed to reduce these lesions. 6. These results indicate that JB-9315 is a new antiulcer drug that exerts a cytoprotective effect in addition to its gastric antisecretory activity.