Evaluation of the antiulcerogenic and antidiarrheal activities of essential oils from Croton jacobinensis Baill. (Euphorbiaceae) and its major compound α-pinene.

ETHNOPHARMACOLOGICAL RELEVANCE: In traditional Brazilian medicine, Croton jacobinensis Baill. (syn. Croton sonderianus) is widely used in the treatment of gastrointestinal disorders, such as gastric discomfort, diarrhea, heartburn, abdominal pain, and indigestion. However, these traditional uses still lack scientific validation.

AIM OF THE STUDY: The present study aimed to investigate the antiulcerogenic and antidiarrheal activities of the essential oils from the leaves (EOL) and bark (EOB) of C. jacobinensis, as well as its main constituent, α-pinene.

MATERIALS AND

METHODS

The quantification of α-pinene in EOL and EOB was performed by gas chromatography with flame ionization detection (GC-FID). Acute oral toxicity was evaluated in female Swiss mice after administration of a single dose of 2000 mg/kg, with monitoring of the animals for 14 days. The antiulcerogenic activity of EOL, EOB, and α-pinene was investigated using the absolute ethanol-induced gastric ulcer model in male Swiss mice, followed by quantification of the levels of the pro-inflammatory cytokines IL-1β and TNF-α. The antidiarrheal activity was evaluated using a castor oil-induced diarrhea model in male Swiss mice.

RESULTS

Analyses using GC-FID revealed α-pinene as the major compound of EOB (69.13%) and an abundant constituent of EOL (10.10%). In the acute oral toxicity test, EOL and EOB did not induce clinical signs of toxicity during the 14-day observation period. Hematological and biochemical parameters remained within physiological limits when compared to the vehicle group (DMSO 2%). Samples of EOL, EOB, and α-pinene showed significant antiulcerogenic activity. At the highest dose evaluated (300 mg/kg), EOL and EOB reduced the gastric lesion area (GLA) to 5.50 and 3.39%, respectively. α-Pinene (100 mg/kg) also demonstrated a protective effect against ethanol-induced gastric lesions (GLA = 9.98%). Furthermore, treatments with essential oils of C. jacobinensis and α-pinene significantly reduced IL-1β and TNF-α levels. Although EOL and EOB showed potential antidiarrheal activity, isolated α-pinene (100 mg/kg) did not exhibit antidiarrheal activity in the experimental model evaluated (evacuation index = 25.66 ± 10.63).

CONCLUSIONS

The essential oils of C. jacobinensis and α-pinene showed promising antiulcerogenic activity, associated with a reduction in IL-1β and TNF-α levels, indicating modulation of the inflammatory response in the gastric mucosa. Evaluated in isolation, α-pinene did not demonstrate an antidiarrheal effect, suggesting that the chemical diversity present in EOL and EOB may act synergistically in controlling castor oil-induced diarrhea. Taken together, the results corroborate the traditional use of C. jacobinensis in the treatment of gastrointestinal disorders and demonstrate its biological safety.