dinoprost and Gastrointestinal-Hemorrhage

Aloysia triphylla is traditionally utilized for the treatment of menstrual colic (primary dysmenorrhea) in Mexico. Citral is the main chemical component found in Aloysia triphylla leaves extract. Primary dysmenorrhea is a very frequent gynecological disorder in menstruating women, affecting 30-60% of them. It is usually treated with non-steroidal anti-inflammatory drugs (NSAIDs); although their effect is rapid, they possess many side effects. Due to these shortcomings, Mexican folk therapy is considered as a feasible alternative. The effects of the hexane extract of Aloysia triphylla and citral on uterine contractions were evaluated in vitro as well as their anti-inflammatory properties and gastric wound capabilities were assessed in vivo. The inhibitory effects on the contractions were analyzed using isolated uterus strips from estrogen primed rats. Contractions were induced by KCl 60 mM, oxytocin 10 mIU/mL, charbacol 10 µM and PGF(2α) 5 µM. The anti-inflammatory effect was assessed on carrageenan-induced rat hind paw edema model. The inhibitory concentration-50 (IC(50)) of the hexane extract of Aloysia triphylla upon each contractile response was for KCl 44.73 ± 2.48 µg/mL, oxytocin 42.16 ± 3.81 µg/mL, charbacol 41.87 ± 1.73 µg/mL and PGF(2α) 28.70 ± 2.40 µg/mL in a concentration-dependent way. The extract of Aloysia triphylla produced a significant inhibitory effect on PGF(2α)-induced contraction compared to its inhibitory actions on the others. Citral exhibited the same inhibitory effect on the contraction induced by PGF(2α). The oral administration of the extract (100-800 mg/kg) and citral (100-800 mg/kg) showed anti-inflammatory activity; furthermore, the maximal dose utilized did not produce gastric injury. These results were compared with anti-inflammatory effects and gastric damage produced by 30 mg/kg of indomethacin p.o. The spasmolytic and anti-inflammatory effects support the traditional use of Aloysia triphylla leaves in the treatment of the primary dysmenorrhea in Mexican communities.

Topics: Acyclic Monoterpenes; Animals; Anti-Inflammatory Agents; Dinoprost; Female; Gastrointestinal Hemorrhage; In Vitro Techniques; Incidence; Indomethacin; Models, Animal; Monoterpenes; Oxytocin; Parasympatholytics; Plant Extracts; Plant Leaves; Potassium Chloride; Rats; Rats, Wistar; Uterine Contraction; Uterus; Verbenaceae

In humans eicosapentaenoic acid can be converted to 3-series prostaglandins (PGF3 alpha, PGI3, and PGE3). Whether 3-series prostaglandins can protect the gastric mucosa from injury as effectively as their 2-series analogs is unknown. Therefore, we compared the protective effects of PGF3 alpha and PGF2 alpha against gross and microscopic gastric mucosal injury in rats. Animals received a subcutaneous injection of either PGF3 alpha or PGF2 alpha in doses ranging from 0 (vehicle) to 16.8 mumol/kg and 30 min later they received intragastric administration of 1 ml of absolute ethanol. Whether mucosal injury was assessed 60 min or 5 min after ethanol, PGF3 alpha was significantly less protective against ethanol-induced damage than PGF2 alpha. These findings indicate that the presence of a third double bond in the prostaglandin F molecule between carbons 17 and 18 markedly reduces the protective effects of this prostaglandin on the gastric mucosa.

Topics: Alprostadil; Animals; Dinoprost; Dose-Response Relationship, Drug; Ethanol; Female; Gastric Mucosa; Gastrointestinal Hemorrhage; Prostaglandins E; Rats; Rats, Inbred Strains; Stomach Diseases

The hypothesis that vascular injury contributes to the development of hemorrhagic erosions after intragastric administration of ethanol has been examined in the rat using vascular tracers. Extravasation of intravenously injected Evans blue into the gastric wall and into gastric contents was used as an indicator of vascular permeability. India ink and monastral blue, which label damaged blood vessels, were used to demonstrate vascular injury morphologically. Intragastric instillation of 75% and 100% ethanol induced increased vascular permeability within 1-3 min and resulted in monastral blue labeling of vessels in 13% and 17%, respectively, of the glandular mucosa within 1 min. After 1 h of 100% ethanol exposure, the areal density of monastral blue-stained blood vessels did not increase compared with that seen at 1 min, but the areal density of grossly visible hemorrhagic lesions increased strikingly and approximated that of vessel staining. The hemorrhagic erosions consistently occurred in regions of glandular mucosa where vessels were stained with monastral blue. Pretreatment with prostaglandin F2 beta or cysteamine reduced ethanol-induced Evans blue extravasation and monastral blue staining of mucosal blood vessels but did not reduce histologic evidence of gastric surface cell damage in the glandular mucosa. As increased vascular permeability and morphologically detectable vascular lesions consistently preceded the development of grossly visible hemorrhagic erosions in the glandular mucosa, we suggest that vascular injury is an early pathogenetic factor in the development of ethanol-induced gastric hemorrhagic erosions. The data also indicate that the degree of vascular damage, unlike the injury to surface epithelial cells, is reduced by pretreatment with prostaglandin F2 beta or the sulfhydryl cysteamine.

Topics: Animals; Capillary Permeability; Carbon; Coloring Agents; Cysteamine; Dinoprost; Ethanol; Evans Blue; Female; Gastric Mucosa; Gastrointestinal Hemorrhage; Indoles; Organometallic Compounds; Prostaglandins F; Rats; Rats, Inbred Strains

Topics: Adult; Colitis; Dinoprost; Female; Gastrointestinal Hemorrhage; Humans; Male; Mesenteric Arteries; Middle Aged; Prostaglandins F; Radiography; Vasoconstrictor Agents

In a study of 54 patients with a variety of lesions, prostaglandin F2 alpha pharmacoangiography produced vasoconstrictive effects in both neoplastic and inflammatory lesions of the colon. These effects occurred only at the affected sites and their immediate vicinity. Vasoconstriction seemed to correlate directly with the vascularity of the lesion, rather than with pathogenesis. Less marked vasoconstriction was seen in renal lesions. No vasoconstrictive effects were recognized in liver, soft tissue, or bone tumors. Thus prostaglandin F2 alpha acts as a vasodilator in normal human colonic vessels, while it acts as a vasoconstrictor in colonic lesions. The potential use of prostaglandin F2 alpha in the control of bleeding colonic lesions is also discussed.

Topics: Adult; Aged; Angiography; Colon; Colonic Diseases; Colonic Neoplasms; Dinoprost; Gastrointestinal Hemorrhage; Humans; Male; Middle Aged; Prostaglandins F; Regional Blood Flow; Vasoconstriction