Anticonvulsant activity of Tetrahydrolinalool: behavioral, electrophysiological, and molecular docking approaches.

Tetrahydrolinalool (THL) is an acyclic monoterpene alcohol, produced during linalol metabolism and also a constituent of essential oils. As described in the literature, many monoterpenes present anticonvulsant properties, and thus we became interested in evaluating the anticonvulsant activity of Tetrahydrolinalool using in mice model as well as in silico approaches. Our results demonstrated that THL increased latency to seizure onset and also reduced the mortality, in picrotoxin induced seizure tests. The results may be related to GABAergic regulation, which was also suggested in seizure testing induced by 3-mercapto-propionic acid. In the strychnine-induced seizure testing, none of the groups pretreated with THL modulated the parameters indicative of anticonvulsant effect. The electrophysiological results revealed that THL treatment reduces seizures induced by pentylenetetrazole. The in silico molecular docking studies showed that the interaction between THL and a GABAA receptor model formed a stable complex, in comparison to the crystaligraphic structure of diazepam, a structurally related ligand. In conclusion, all the evidences showed that THL presents effective anticonvulsant activity related to the GABAergic pathway, being a candidate for treatment of epileptic syndromes.

Pharmacological Effects of Carvacrol in In vitro Studies: A Review.

Carvacrol has a high therapeutic potential, with in vitro studies showing promising results in different cellular models using a variety of methodological designs. Therefore, the objective of this study was to conduct a systematic review to analyze the pharmacological effects of carvacrol in in vitro studies. A comprehensive search of the literature was made using four databases: Science Direct, Scopus, MEDLINE-PubMed, and Web of Science using different combinations of the following keywords: carvacrol, drug therapy, therapeutic uses, in vitro study. The search of the databases was for studies conducted in the period up to and including September 2016. A total of 3,269 studies were initially identified, with only 31 meeting the inclusion criteria. The included studies contained a variety of in vitro models able to determine the properties of Carvacrol. The following properties of Carvacrol were identified: antimicrobial (7 studies), bactericidal (4), bactericidal and antifungal (1), antiinflammatory (4), anticancer (4), mutagenic (4), antioxidant (3), antifungal (3), antidepressant (1), as a modulator of nerve impulses (1) and an immunological modulator (1). The In vitro studies with Carvacrol included in this review showed a diversity of models and confirmed the therapeutic potential of this product in relation to several diseases.

Synthesis and pharmacological evaluation of carvacrol propionate.

This study aimed at synthesizing the carvacrol propionate (CP) and evaluating its pharmacological profile. CP was obtained from carvacrol and propionyl chloride through an esterification reaction. Male Swiss mice were treated with CP (25, 50, or 100 mg/kg). We evaluated the analgesic effect, mechanical hyperalgesia, and anti-inflammatory effect. Pre-treatment with CP inhibited (p<0.01 and 0.001) the formalin-induced nociception in both phases. CP inhibited (p<0.05, 0.01, and 0.001) the development of mechanical hyperalgesia. CP was able to decrease the leukocyte recruitment (p<0.001) and the amount of TNF-α (p<0.001), IL-1ß (p<0.05), and protein leakage (p<0.01) into the pleural cavity. In addition, the paw edema was inhibited by CP (p<0.05, 0.01, and 0.001). The CP attenuates nociception, mechanical hyperalgesia, and inflammation, through an inhibition of cytokines.

Enzymatic production of linalool esters in organic and solvent-free system.

This work investigated the influence of temperature, enzyme concentration, substrates molar ratio, in the absence and presence of organic solvent, at two molar ratios of the substrates on the enzymatic production of linalil esters using the immobilized lipase Novozym 435 as catalyst, different acids and linalool and Ho-Sho essential oil as substrates. The best reaction conversion was obtained at the highest temperature (70 degrees C), for both solvent free (3.81%) and with solvent addition (2.25%), for a solvent to substrates molar ratio of 2:1, enzyme concentration of 5 wt% and acid to alcohol molar ratio of 1:1. The reaction kinetics revealed that Ho-Sho essential oil afforded the greatest conversions when compared with pure linalool. Higher linalil esters production were achieved after 10 h reaction (5.58%) in 2:1 solvent to substrates molar ratio, with enzyme concentration of 5 wt%, at 70 degrees C and anhydride to alcohol molar ratio of 1:1 using Ho-Sho essential oil as substrate.