Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
In continuation of our drug discovery program on Indian medicinal plants, the gastro protective mechanism of chebulinic acid isolated from Terminalia chebula fruit was investigated. Chebulinic acid was evaluated against cold restraint (CRU), aspirin (AS), alcohol (AL) and pyloric ligation (PL) induced gastric ulcer models in rats. Potential anti-ulcer activity of chebulinic acid was observed against CRU (62.9%), AS (55.3%), AL (80.67%) and PL (66.63%) induced ulcer models.
A pharmacodynamic interactional study with omeprazole was undertaken in rats. Omeprazole (7 mg/kg, orally once daily for 14 days) significantly prolonged pentobarbitone (30 mg/kg, ip) induced hypnosis while it had no effect on haloperidol (1 mg/kg, ip) induced catalepsy or morphine (5 mg/kg, ip) induced analgesia models in rats. The study highlighted the fact that dynamic interaction with omeprazole was selective.
Methods and Findings in Experimental and Clinical Pharmacology
The general pharmacological profiles of a novel proton pump inhibitor, (+/-)-5-methoxy-2-[[(4-methoxy-3,5-dimethylpyrid-2-yl)methyl]sulfi nyl]- 1H-imidazo[4,5-b]pyridine, TU-199) on the central nervous system, cardiorespiratory system, autonomic nervous system, gastrointestinal system and renal functions were investigated. TU-199 had no effects on general signs and behavior in mice. TU-199 (300 mg/kg p.o.) decreased locomotor activity 3 h after administration in mice.
Previous studies have shown that the proton pump inhibitor omeprazole has antimalarial activity in vitro. The interactions of omeprazole with commonly used antimalarial drugs were assessed in vitro. Omeprazole and quinine combinations were synergistic; however, chloroquine and omeprazole combinations were antagonistic. Artemisinin drugs had additive antimalarial activities with omeprazole.
Drug Metabolism and Disposition: The Biological Fate of Chemicals
The female flowers of hops (Humulus lupulus L.) are used in the brewing of beer and are under investigation for use in dietary supplements for the management of menopausal symptoms in women. Hop extracts contain the weakly estrogenic compound isoxanthohumol (IX), proestrogenic xanthohumol, and the potent estrogen 8-prenylnaringenin (8PN). Because IX can be metabolized in the human liver to form 8PN, the specific cytochrome P450 (P450) enzymes responsible for this O-demethylation reaction were identified.
Probe drugs are critical tools for the measurement of drug metabolism and transport activities in human subjects. Often several probe drugs are administered simultaneously in a "cocktail". This cocktail approach requires efficient analytical methods for the simultaneous quantitation of multiple analytes. We have developed and validated a liquid chromatography-tandem mass spectrometry method for the simultaneous determination of three probe drugs and their metabolites in human plasma.
Ephedra pachyclada Boiss. (family Ephedraceae) is a medicinal plant very frequently cited as acting against gastrointestinal disorders in ethno-pharmacological inventories of the Kerman region of Iran. This study was done to evaluate the effect of hydro-alcoholic extract from the stems of E. pachyclada for treatment of gastric ulcers induced by ethanol in Wistar rats. Experimental treatments were the hydro-alcoholic extract of E. pachyclada (250, 500, and 1000 mg/kg, orally), omperazole as standard drug (20 mg/kg, orally), and control group.
The effect of intermittent dosage with omeprazole on basal and pentagastrin stimulated gastric acid secretion and fasting plasma gastrin was assessed in eight duodenal ulcer subjects who were in remission. Omeprazole (20 mg daily) was given for a three day 'weekend' each week for two months. Twenty four hours after the first and eighth weekend, basal and peak acid output were still markedly suppressed (greater than 50%) compared with pretreatment.
A monolithic osmotic pump tablet (MOPT) of Traditional Chinese Medicine Compound Recipe (TCMCR) was successfully prepared and active components of Jingzhiguanxin prescription which has been widely used in China and Japan was selected as model drug. Analysis methods of maker compound in vitro of danshensu, paeoniflorin and safflor yellow A were built, and different methods were compared by f2 factors. The results showed that there were fine correlation among them.
CONTEXT: Functional dyspepsia represents a frequent gastrointestinal disorder in clinical practice. According to the Roma III criteria, functional dyspepsia can be classified into two types as the predominant symptom: epigastric pain and postprandial discomfort. Even though the pathophysiology is still uncertain, the functional dyspepsia seems to be related to multiple mechanisms, among them visceral hypersensitivity, changes in the gastroduodenal motility and gastric accommodation and psychological factors.