Gastroprotective properties of Lupeol-derived ester: Pre-clinical evidences of Lupeol-stearate as a potent antiulcer agent

Somensi, Líncon Bordignon; Costa, P.; Boeing, Thaise; Mariano, Luísa Nathália Bolda; Longo, Bruna; Magalhães, Cássia Gonçalves; Duarte, Lucenir Pain; Silva, Aline Teixeira Maciel e; Souza, Priscila de; Andrade, Sérgio Faloni de; Silva, Luísa Mota da

doi:10.1016/j.cbi.2020.108964

Cited by 13 publications

(16 citation statements)

References 40 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In agreement with these findings, our research group's previous results using a model of indomethacin-induced ulcers evidenced an increase in PGE2 levels after the treatment of ulcerated rodents with LS [ 18 ]. Given that PGE2 mediates mucin production, it is reasonable to infer that the enhancement in this eicosanoid in the gastric mucosa promoted by LS increases the mucin levels also observed in this study.…”

Section: Discussionsupporting

confidence: 89%

“…In previously experimental investigations about the antiulcer potential of lupeol stearate (LS), our research group showed that this compound promotes a potent gastroprotective effect against gastric lesions induced by ethanol in rodents [ 18 ]. Given those results, the present study evaluated the capacity of LS to promote gastric healing in the acetic acid-induced ulcer model, which highly resembles human gastric ulcers and can relapse [ 29 ].…”

Section: Discussionmentioning

confidence: 99%

“…Apart from mucins, the wound healing capacity of the gastrointestinal tract also depends on the balance in the redox state of the mucosa. Indeed, research with antioxidants has shown that they can interfere with the ulcerative process into the gastric mucosa [ 40 ], and the capability of LS to enhance the antioxidant defenses in the stomach was already evidenced by our research group using acute ulcer models [ 18 ]. Because of this, we evaluated the levels or activity of antioxidative resources at the site of acetic acid-induced ulcers from rats treated or not with LS.…”

Section: Discussionmentioning

confidence: 99%

“…Lupeol was isolated from Maytenus salicifolia Reissek (Celastraceae) hexanic extract as described in detail by Magalhães et al [ 19 ] and esterification with appropriate reagents gave rise to LS was performed as described in detail by Silva et al [ 17 ]. The oral gastroprotective dose of LS of 1 mg/kg was chosen for this study based on findings from Somensi et al [ 18 ].…”

Section: Methodsmentioning

confidence: 99%

“…Moreover, this triterpene has several biological activities, including in vitro [ 11 ] and in vivo [ 12 ] anticancer properties, antidiabetic effects [ 13 ], topical anti-inflammatory actions [ 14 ], and antimalarial potency [ 15 ], besides has been a candidate as a nonhormonal male contraceptive [ 16 ]. Recently, through the esterification of lupeol, it was possible to obtain lupeol stearate (LS) [ 17 ], a derivative with potent gastroprotective activity [ 18 ].…”

Section: Introductionmentioning

confidence: 99%

See 4 more Smart Citations

Lupeol Stearate Accelerates Healing and Prevents Recurrence of Gastric Ulcer in Rodents

Somensi

Costa

Boeing

et al. 2022

Evidence-Based Complementary and Alternative Medicine

Self Cite

View full text Add to dashboard Cite

Objective. The focus of this study was to evaluate the gastric healing effect of lupeol stearate (LS) and its ability to minimize ulcer recurrence in rodents. Methods. To evaluate the gastric healing properties of LS, rats were subjected to 80% acetic acid-induced ulcer model and treated with vehicle, LS (1 mg/kg, p.o.), or omeprazole (20 mg/kg, p.o.), twice daily by seven days. The gastric ulcers were evaluated macroscopically, histologically, and biochemically. To evaluate the effects of LS in gastric ulcer recurrence, mice were ulcerated with 10% acetic acid and treated with vehicle, LS (1 mg/kg, p.o.), or ranitidine (100 mg/kg, p.o.), twice a day for ten days. Then, ulcer recurrence in these animals was induced by IL-1β at five days after the treatment period. Results. The oral treatment with LS accelerated gastric healing by 63% in rats compared to the vehicle group, evidenced by histological improvement and increased gastric mucin levels. Moreover, the gastric healing effects of LS in rats were accompanied by an elevation in glutathione S-transferase activity and a reduction in myeloperoxidase activity. Furthermore, the LS treatment reduced the recurred lesions in mice. Conclusions. The oral treatment of LS accelerates gastric healing in rats by favoring mucus production and reducing neutrophil migration, and it also can reduce ulcer recurrence. These data highlighted this compound as promising for developing new pharmacological strategies for the management of gastric ulcer.

show abstract

Section: Discussionsupporting

confidence: 89%

Section: Discussionmentioning

confidence: 99%