title: Beta-cyclodextrin enhanced gastroprotective effect of (-)-linalool, a monoterpene present in rosewood essential oil, in gastric lesion models.
abstract: (-)-Linalool is a monoterpene constituent of many essential oils. This particular monoterpene has both anti-inflammatory and antimicrobial activity. Moreover, this compound has been shown to be antinociceptive. However, the poor chemical stability and short half-life prevents the clinical application of (-)-linalool and many other essential oils. Important to the topic of this study, β-cyclodextrin (β-CD) has been used to increase the solubility, stability, and pharmacological effects of numerous lipophilic compounds in vivo. In this study, the gastroprotective activities of (-)-linalool (LIN) and linalool incorporated into inclusion complex containing β-cyclodextrin (LIN-βCD) were evaluated using models of acute and chronic gastric ulcers in rodents. LIN and LIN-βCD showed strong gastroprotective activity (p < 0.001). The LIN-βCD complex revealed that the gastroprotective effect was significantly improved compared with LIN uncomplexed, suggesting that this improvement is related to increased solubility and stability. Taking together the potentiation of the antioxidant profile of this monoterpene, our results suggest that β-CD may represent an important tool for improved gastroprotective activity of (-)-linalool and other water-insoluble compounds.
authors.affiliation: Postgraduate Program in Biotechnology - RENORBIO, Focal Point - Federal University of Piauí, Teresina, Piauí, Brazil.
authors.forename: Francilene Vieira
authors.initials: FV
authors.lastname: da Silva
authors.affiliation: Postgraduate Program in Biotechnology - RENORBIO, Focal Point - Federal University of Piauí, Teresina, Piauí, Brazil.
authors.forename: Hélio
authors.initials: H
authors.lastname: de Barros Fernandes
authors.affiliation: Postgraduate Program in Biotechnology - RENORBIO, Focal Point - Federal University of Piauí, Teresina, Piauí, Brazil.
authors.forename: Irisdalva Sousa
authors.initials: IS
authors.lastname: Oliveira
authors.affiliation: Postgraduate Program in Pharmacology, Department of Physiology and Pharmacology, Faculty of Medicine, Federal University of Ceará, Fortaleza, Ceará, Brazil.
authors.forename: Ana Flávia Seraine Custódio
authors.initials: AF
authors.lastname: Viana
authors.affiliation: Postgraduate Program in Biotechnology - RENORBIO, Focal Point - Federal University of Piauí, Teresina, Piauí, Brazil.
authors.forename: Douglas Soares
authors.initials: DS
authors.lastname: da Costa
authors.affiliation: Laboratory of Tumoral Cell, Federal University of Minas Gerais, Belo Horizonte, Minas Gerais, Brazil.
authors.forename: Miriam Teresa Paz
authors.initials: MT
authors.lastname: Lopes
authors.affiliation: Medicinal Plants Research Center, Health Sciences Center, Federal University of Piauí, Av. Nossa Senhora de Fátima s/n, Teresina, Piauí, 64049-550, Brazil.
authors.forename: Kamila Lopes
authors.initials: KL
authors.lastname: de Lira
authors.affiliation: Department of Physiology, Federal University of Sergipe, Aracaju, Sergipe, Brazil.
authors.forename: Lucindo José
authors.initials: LJ
authors.lastname: Quintans-Júnior
authors.affiliation: Department of Pharmacia, Federal University of Sergipe, Aracaju, Sergipe, Brazil.
authors.forename: Adriano Antunes
authors.initials: AA
authors.lastname: de Sousa
authors.affiliation: Postgraduate Program in Biotechnology - RENORBIO, Focal Point - Federal University of Piauí, Teresina, Piauí, Brazil. menesesoliveira@gmail.com.|Medicinal Plants Research Center, Health Sciences Center, Federal University of Piauí, Av. Nossa Senhora de Fátima s/n, Teresina, Piauí, 64049-550, Brazil. menesesoliveira@gmail.com.
authors.forename: Rita
authors.initials: R
authors.lastname: de Cássia Meneses Oliveira
mesh_terms: D019342:Acetic Acid; D000080462:Acyclic Monoterpenes; D000818:Animals; D000897:Anti-Ulcer Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000975:Antioxidants / Q000302:isolation & purification / Q000494:pharmacology; D019610:Cytoprotection; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D004355:Drug Stability; D004359:Drug Therapy, Combination; D000431:Ethanol; D005260:Female; D005753:Gastric Mucosa / Q000378:metabolism; D015227:Lipid Peroxidation / Q000187:drug effects; D019684:Magnoliopsida / Q000737:chemistry; D008297:Male; D051379:Mice; D039821:Monoterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D009822:Oils, Volatile / Q000302:isolation & purification / Q000494:pharmacology*; D009195:Peroxidase / Q000378:metabolism; D008517:Phytotherapy; D010938:Plant Oils / Q000302:isolation & purification / Q000494:pharmacology*; D010946:Plants, Medicinal; D017208:Rats, Wistar; D012995:Solubility; D013270:Stomach / Q000187:drug effects* / Q000473:pathology; D013276:Stomach Ulcer / Q000139:chemically induced / Q000378:metabolism / Q000473:pathology / Q000517:prevention & control*; D013438:Sulfhydryl Compounds / Q000378:metabolism; D047392:beta-Cyclodextrins / Q000494:pharmacology*
chemical_list: D000080462:Acyclic Monoterpenes; D000897:Anti-Ulcer Agents; D000975:Antioxidants; D039821:Monoterpenes; D009822:Oils, Volatile; D010938:Plant Oils; D013438:Sulfhydryl Compounds; D047392:beta-Cyclodextrins; D000431:Ethanol; C018584:linalool; D009195:Peroxidase; D019342:Acetic Acid
keywords: Acetic acid; Ethanol; Gastric damage; Linalool; β-cyclodextrin