Gastroprotective effect and cytotoxicity of terpenes from the Paraguayan crude drug “yagua rova” ( Jatropha isabelli)

• Published in: Journal of ethnopharmacology 2007-05, Vol.111 (3), p.553-559
• Main Authors: Pertino, Mariano, Schmeda-Hirschmann, Guillermo, Rodríguez, Jaime A., Theoduloz, Cristina
• Format: Article
• Language: English
• Subjects: 2-Pyridinylmethylsulfinylbenzimidazoles - pharmacology; Administration, Oral; Animals; Anti-Ulcer Agents - administration & dosage; Anti-Ulcer Agents - isolation & purification; Anti-Ulcer Agents - pharmacology; bioassays; Biological and medical sciences; Cell Line - drug effects; Cell Survival - drug effects; chemical constituents of plants; cyperenoic acid; Cytotoxicity; digestive system diseases; Dose-Response Relationship, Drug; ethnobotany; Euphorbiaceae; Gastric Mucosa - drug effects; Gastroprotective effect; General pharmacology; herbal medicines; Inhibitory Concentration 50; Jatropha; Jatropha - chemistry; Jatropha isabelli; Jatropholones; jatrophone; Jatrophone derivatives; Lansoprazole; Medical sciences; medicinal plants; medicinal properties; Medicine, Traditional; Mice; monoterpenoids; Paraguay; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; plant extracts; Protective Agents - administration & dosage; Protective Agents - isolation & purification; Protective Agents - pharmacology; protective effect; rats; Rhizome; rhizomes; Spectrum Analysis; Stomach Diseases - drug therapy; Terpenes - administration & dosage; Terpenes - isolation & purification; Terpenes - pharmacology; traditional medicine
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2007.01.003

A new jatrophone derivative ( 6), jatrophone ( 3), jatropholone A ( 4) and jatropholone B ( 5), acetyl aleuritolic acid ( 1), cyperenoic acid ( 2) and a monoterpene were isolated from the rhizomes of the Paraguayan crude drug Jatropha isabelli. The compounds were characterized by spectroscopic means. The gastroprotective effect of jatrophone, jatropholone A and B as well as 9β,13α-dihydroxyisabellione 6 and the triterpene 1 was assessed in the HCl/EtOH-induced gastric lesions model in mice. Jatrophone elicited a strong gastroprotective effect with no significant differences between 25, 50 or 100 mg/kg and reducing lesions from 88 to 93%. The jatropholones A and B showed remarkable differences in the gastroprotective assay. Jatropholone A presented a dose-related response, with maximum effect (54% lesion reduction) at the highest dose (100 mg/kg), jatropholone B showed a strong action at all the doses, reducing lesions by 83–91%. The cytotoxicity of the compounds was assessed towards fibroblasts and AGS cells. Jatrophone was toxic against both cell lines (IC 50 values: 2.8 and 2.5 μM, respectively). Jatropholone B ( 5) was not cytotoxic while jatropholone A ( 4) displayed a selective effect against AGS cells (IC 50: 49 μM). The relevance of stereochemistry in the biological effects is clear comparing the effect of jatropholone A and B against AGS cells, with IC 50 values of 49 and >1000 μM for the β and α C-16 isomers, respectively. The results provide scientific support for the use of “yagua rova” as a gastroprotective crude drug in Paraguayan traditional medicine.