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Abstract

Gastric Cytoprotective Activity of Ilicic Aldehyde in Rats and Mice

1
Química Orgánica-INTEQUI-CONICET, Argentina
2
Cátedra de Farmacología. Fac. de Qca., Bioqca. y Fcia. U.N. San Luis - Chacabuco y Pedernera - 5700 - San Luis, Argentina
*
Authors to whom correspondence should be addressed.
Molecules 2000, 5(3), 462-464; https://doi.org/10.3390/50300462
Published: 22 March 2000

Abstract

:
Ilicic alcohol, a natural sesquiterpene, was converted into an aldehyde by using Jones’ oxidation. The gastroprotective activity of ilicic aldehyde was evaluated in mice and rats.

Introduction

Molecules 05 00462 i001
It is well known that gastric cytoprotective activity is closely related to the presence of α,β-unsaturated carbonyl groups [1]. Taking into account this fact, we have studied the activity of ilicic aldehyde. This compound was obtained by oxidation of the corresponding natural alcohol. This work reports the gastroprotective ability against different necrotizing agents (absolute ethanol, NaOH 0.2 N, HCl 0.6 N, NaCl 25%, in rats and absolute ethanol in mice).

Material and Methods

Oxidation

Ilicic alcohol [1], an eudesmane sesquiterpene, isolated from Fluorensia oolepis [2] was oxidised with Jones' reagent, by the usual method proposed for allylic alcohols [3]. Through this reaction it was possible to obtain ilicic aldehyde [2].

Pharmacological assays

Wistar rats, were grouped in six lots: 1, 2 y 3: received as necrotizing agent NaOH 0.2 N (p.o.) (n=6), HCl 0.6 N (p.o.) (n=5) and NaCl 25% (p.o.) (n=5), respectively. Lots 4, 5 y 6: were administered with ilicic aldehyde (2), 40 mg/kg, 1 ml (p.o., n=5) 60 min before the administration of necrotizing agents, NaOH 0.2 N, HCl 0.6 N and NaCl 25%, respectively. The degree of erosion in the glandular part of the stomach was assessed from a scoring system designed by Marazzi, Uberti and Turba [4]. In another experiment, gastric mucosal damage in Wistar rats was induced by absolute ethanol (EA, 1 ml/rat, p. o.) according to Robert et al. (1979) [5]. Four experimental groups received 2 (1 ml, 25, 50, 75 and 100 mM). The effective dose, ED50, were obtained with software ALLFIT (De Lean et al., 1988) [6]. In another experiment with Rockland mice, EA was employed as the necrotizing agent (0,1 ml/10 g, p.o.), according to the method of Robert et al. (1979) [5]. The results were expressed as Ulcer Index (UI) and as the percentage cytoprotection, method by Yamasaki et al. (1989) [7]. The statistical significance of difference among means was assessed by analysis of variance (ANOVA) with the multiple comparison method by Tukey, and by Students´s t-test.

Results and discussion

The results were expressed as follows (Ulcer Index) :
  • In the first experiment: L. 1: 4,80 ± 0,27; L. 2: 4,37 ± 0,25; L. 3: 4,33 ± 0,57; L. 4: 1,50 ± 0,50*; L. 5: 0,83 ± 0,28*; L. 6: 0,75 ± 0,28** (*p<0,00001; **p<0,0001 vs. controls. Each value represents the mean ± SEM).
  • In the experiment performed to study whether 2 protects the gastric mucosa in rats at different doses: 25 mM: 1,5 ± 0,11; 50 mM: 1,08 ± 0,12; 75 mM: 0,6 ± 0,11; 100 mM: 0,20 ± 0,10. ED50 = 21,57 ± 4,22 mM.
  • In the evaluation of gastroprotective activity in mice: L. control: 4,75 ± 0,15; L. 0,43 ± 0,11* (91% of cytoprotection) ( *p<0,00001 vs. control).
These results indicate that 2 prevents the formation of gastric mucosal lesions induced by absolute ethanol and by other necrotizing agents in rats and mice.

Acknowledgements 

To Dr. Eduardo Guerreiro, in memoriam. This work is part of Lic O.J. Donadel DT and was supported by UNSL and CONICET.

References and Notes

  1. Rodriguez, A. M.; Enriz, R.D.; Santágata, L.N.; Jauregui, E.A.; Pestchanker, M.J.; Santágata, O.S. J. Med. Chem. 1997, 40(12), 1827. [PubMed]
  2. Guerreiro, E.; Kavka, J.; Giordano, O.S.; Gros, E. Phytochemistry 1979, 18, 1235–37.
  3. Donadel, O.; Tonn, C.; Guerreiro, E. «IV Simposio Internacional de Química de Productos Naturales y sus Aplicaciones»; Talca, Chile, 1-4 /12/98.
  4. Marazzi-Uberti, E.; Turba, C. Med.Exp. 1961, 4, 284.
  5. Robert, A.; Nezamis, J.E.; Lancaster, C. Gastroenterology 1979, 77, 433. [PubMed]
  6. De Lean, A.; Munson, P.J.; Guardabasso, V.; Rodbard, D. Lab. of Theoretical and Physical Biology, U.S.A. Program version 2.7 (1988).
  7. Yamasaki, K.; Ishiyama, H.; Imaizum, T.; Kanbe, T.; Yabuuchi, Y. Japan J. Pharmacol. 1989, 49, 441.

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MDPI and ACS Style

Donadel, O.J.; María, A.; Wendel, G.; Guerreiro, E.; Giordano, O. Gastric Cytoprotective Activity of Ilicic Aldehyde in Rats and Mice. Molecules 2000, 5, 462-464. https://doi.org/10.3390/50300462

AMA Style

Donadel OJ, María A, Wendel G, Guerreiro E, Giordano O. Gastric Cytoprotective Activity of Ilicic Aldehyde in Rats and Mice. Molecules. 2000; 5(3):462-464. https://doi.org/10.3390/50300462

Chicago/Turabian Style

Donadel, O. J., A. María, G. Wendel, E. Guerreiro, and O. Giordano. 2000. "Gastric Cytoprotective Activity of Ilicic Aldehyde in Rats and Mice" Molecules 5, no. 3: 462-464. https://doi.org/10.3390/50300462

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