Many plants produce (À)-linalool, a plant-derived monoterpene alcohol, including members of the Lamiaceae (mints) and Lauraceae family (laurels, cinnamon, rosewood). The anti-inflammatory and analgesic effects of (À)-linalool have been widely suggested for various studies. Poor chemical stability and short half-life restrain the clinical applications of some essential oil and monoterpenes, including (À)-linalool. However, b-cyclodextrin (b-CD) has been used to increase solubility and stability of lipophilic compounds and also to improve the pharmacological effects. In this study, the antinociceptive effect of (À)-linalool and (À)-linalool/b-CD was examined using the acetic acid writhing reflex, formalin and hotplate tests in rodents. (À)-Linalool and (À)-linalool/b-CD demonstrated strong antinociceptive activity in all the chemical-and heat-induced mice models (p < 0.01 or p < 0.001). These findings imply the involvement of both peripheral and central antinociceptive mechanisms. In peritonitis induced by carrageenan, isolated monoterpene or b-CD complex also reduced total leucocyte migration and TNF-a levels in peritoneal fluid. The inclusion complexes, (À)-linalool/b-CD, revealed that the antinociceptive effect was significantly (p < 0.01) improved when compared with (À)-linalool alone. Such results were unlikely to be provoked by any motor abnormality. Together, our results suggest that b-CD might represent an important tool for improvement of analgesic and anti-inflammatory profiles of (À)-linalool and other water-insoluble compounds, such as lipophilic monoterpenes or essential oils.
The present study aimed to investigate the gastroprotective activity of carvacrol, a monoterpene present in essential oils from several species of medicinal and aromatic plants, by using different models of acute gastric lesions in rodents and also evaluate possible mechanisms involved in this action. For this study, absolute ethanol-, acidified ethanol-, ischemia and reperfusion-, and nonsteroidal anti-inflammatory drug-induced models of gastric lesions in mice and rats were used. The roles of nonprotein sulfhydryl groups, catalase, nitric oxide (NO), ATP-sensitive potassium channels (K(ATP) channels), and prostaglandins in carvacrol-induced gastroprotective effect were investigated. In addition, the effects of carvacrol on gastric secretion and mucus in pylorus-ligated rats were also determined. The results of the present study demonstrated that carvacrol promoted a marked gastroprotection in all models investigated, possibly mediated by endogenous prostaglandins, increase of mucus production, K(ATP) channels opening, NO synthase activation, and antioxidant properties. These findings markedly substantiate further studies to investigate the therapeutic potential of carvacrol as an effective gastroprotective agent and its safety profile in medicinal use.
This study corroborates the folk medicine use of Cenostigma macrophyllum for treatment of gastric ulcers, as well as reinforces this species as a valuable source of promising natural drugs with gastroprotective activity.
These results provide first-time evidence for the gastroprotective effect of (-)-myrtenol that could be related to GABAA -receptor activation and antioxidant activity.
Obesity remains a global problem. In search of phytochemicals that have antiobesity potential, this study evaluated -amyrin, a triterpenoid mixture from, on high-fat diet-induced obesity in mice. Groups of mice (n = 8) were fed a normal diet or a high-fat diet, and were orally treated or not treated with either -amyrin (10 or 20 mg/kg) or sibutramine (10 mg/kg) for 15 weeks. Variables measured at termination were body weight, visceral fat accumulation, adipocyte surface area, peroxisome proliferator-activated receptor gamma, and lipoprotein lipase expressions in adipose tissue, the levels of plasma glucose and insulin, the satiety hormones ghrelin and leptin, the digestive enzymes amylase and lipase, and the inflammatory mediators TNF-, interleukin-6, and MCP-1. Results showed that -amyrin treatment resulted in lower high-fat diet-induced increases in body weight, visceral fat content, adipocyte surface area, peroxisome proliferator-activated receptor gamma, and lipoprotein lipase expressions, and blood glucose and insulin levels. Additionally, the markedly elevated leptin and decreased ghrelin levels seen in the high-fat diet-fed control mice were significantly modulated by-amyrin treatment. Furthermore, -amyrin decreased serum TNF- and MCP-1. These results suggest that -amyrin could be beneficial in reducing high-fat diet-induced obesity and associated disorders via modulation of enzymatic, hormonal, and inflammatory responses.
(-)-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.
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