Dillapiole, Isolated from Peperomia pellucida, Shows Gastroprotector Activity against Ethanol-Induced Gastric Lesions in Wistar Rats

Abstract

Peperomia pellucida is a plant used in traditional medicine to treat gastric ulcers. Although this gastroprotective activity was reported, the active compounds have not been identified. Therefore, the aim herein was to identify the most active compound in the gastroprotective activity of P. pellucida using an ethanol-induced gastric ulcer experimental rat model. A gastroprotective effect was observed when the hexane and dichloromethane extracts were tested, with the higher effect being obtained with the dichloromethane extract (82.3 ± 5.6%) at 100 mg/kg. Dillapiole was identified as the most active compound in this extract. Although there have been previous reports on dillapiole, this is the first on its gastroprotective activity. Rats treated with this compound at 3, 10, 30 and 100 mg/kg showed 23.1, 56.1, 73.2 and 85.5% gastroprotection, respectively. The effect elicited by dillapiole at 100 mg/kg was not attenuated by pretreatment with indomethacin (10 mg/kg, s.c.), a prostaglandin synthesis blocker, N G -nitro-L-arginine OPEN ACCESSMolecules 2013, 18 11328 methyl ester (70 mg/kg, i.p.), a nitric oxide (NO) synthase inhibitor, or N-ethylmaleimide (10 mg/kg, s.c.), a blocker of sulfhydryl groups. This suggests that the gastroprotective mechanism of action of dillapiole does not involve prostaglandins, NO or sulfhydryl groups.

Gastroprotective effect of calealactone B: Lack of involvement of prostaglandins, nitric oxide and sulfhydryls

“…Pretreatment with the COX inhibitor, indomethacin (10 mg kg −1) did not modify the gastroprotective effect of calealactone B (Figure a), indicating that PGs are not involved in its mechanism of action. PGs were however found to be involved in the mechanism of action of carbenoxolone (Figure a) in agreement with literature reports (Rojas‐Martínez et al, ). The involvement of NO was also assessed.…”

“…The involvement of NO was also assessed. NO is important in maintaining the integrity of the gastric mucosa via regulation of blood flow, angiogenesis and mucus secretion (Rojas‐Martínez et al, ). Pretreatment with L‐NAME, a nonspecific NOS inhibitor (70 mg kg −1 ) had no effect on the gastroprotective activity of calealactone B (Figure b).…”

Metabolite Profiling Analysis of Conventional and Non-Conventional Extraction Methods on Secondary Metabolite from Peperomia pellucida (L.) Kunth Using UPLC-QToF-MS/MS System

“…1 Some of them have been isolated (particularly polyphenolic groups) including pellucidin A, 2 peperomins, secolignan, 3 xanthone patuloside A, 4 dillapiole, 5 chromene, 6 and quercetin. 7 Also, the herbs have also been reported to have potential pharmacological properties.…”

Isolation and Characterization Compounds From Hexane and Ethyl Acetate Fractions of Peperomia pellucida L.

“…Rojas-Martinez. et al, 2013 [12] reported that dillapiole was identified as the most active compound in the dichloromethane extract and also reported the gastro protector activity of dillapiole. Ethanolic extract of P. pellucida accelerates fracture repairment in rats via stimulatory effects on osteoblast differentiation and mineralisation [13].…”