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1.
Molecules ; 23(10)2018 Sep 27.
Article in English | MEDLINE | ID: mdl-30262744

ABSTRACT

Lippia schaueriana Mart. (Verbenaceae) is an endemic species of Caatinga with a restricted distribution to the states of Bahia and Pernambuco, which presents itself as a potential source of raw material for extraction of essential oil and exploitation by the chemical and pharmaceutical industries. Considering that there are no reports in the literature of research carried out with this species, this paper aimed to establish-for the first time-the chemical composition of its essential oil. The essential oil of the dry leaves at room temperature was obtained by hydrodistillation after 3 h of extraction and the phytochemical analyzes were done by gas chromatography coupled to mass spectrometry (GC/MS). The main compounds found in the oil of leaves were piperitone oxide (51.25%), caryophyllene (17.76%), limonene (8.06%), spathulenol (6.63%), and piperitone (2.90%). The piperitone oxide is a compound described in the literature that shows antinociceptive, cardiovascular, analgesic, and relaxing activities, as well as fungicidal and insecticidal effect, which gives it an interesting potential for the alternative control of agricultural pests.


Subject(s)
Lippia/chemistry , Oils, Volatile/analysis , Plant Leaves/chemistry , Brazil
2.
J Ethnopharmacol ; 221: 65-76, 2018 Jul 15.
Article in English | MEDLINE | ID: mdl-29627297

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Croton conduplicatus Kunth (Euphorbiaceae) is a Brazilian aromatic medicinal plant, widely known as "quebra-faca". In folk medicine, its leaves and stem-barks are used as a natural analgesic for the treatment of headaches. AIM OF THE STUDY: In this study, we describe for the first time the neuropharmacological potential of the essential oil obtained from the leaves of Croton conduplicatus (EO) in experimental models of pain, anxiety and insomnia. The mechanisms of action involved in these activities were also investigated. MATERIAL AND METHODS: Different experimental models were used to evaluate the antinociceptive (acetic acid, formalin-induced nociception and hot plate tests), anxiolytic (elevated plus maze and hole board tests) and sedative (thiopental-induced sleeping time) effects of EO in mice. EO was evaluated in three different doses (25, 50 and 100 mg/kg, i.p.) and compared with positive and negative controls in all experimental protocols. When appropriate, animals were pretreated with pharmacological antagonists (naloxone, atropine and flumazenil) in order to evaluate the mechanisms of action involved. A docking study also was performed to identify possible targets involved. RESULTS: EO (25, 50 and 100 mg/kg, i.p.) demonstrated a significant antinociceptive activity in all experimental models. Pretreatment with naloxone or atropine reversed the antinociceptive response (p < 0.05), suggesting the involvement of opioid and muscarinic receptors, respectively. A docking study was performed with the major components identified in EO (1,8 cineole - 21.42%, spathulenol - 15.47%, p-cymene - 12.41% and caryophyllene oxide - 12.15%), demonstrating favorable interaction profile with different subtypes of muscarinic (M2, M3 and M4) and opioids (delta and mu) receptors. EO also showed anxiolytic (mainly at doses of 25 and 50 mg/kg, i.p.) and sedative (only at the dose of 100 mg/kg, i.p.) effects in mice. These pharmacological responses were reversed by flumazenil (p < 0.05), indicating possible involvement of GABAA receptors. CONCLUSION: Our findings support the traditional use of this plant as a natural analgesic and suggest that EO is a multi-target natural product, presenting not only antinociceptive effect but also anxiolytic and sedative activities depending on the dose used.


Subject(s)
Analgesics , Anti-Anxiety Agents , Croton , Hypnotics and Sedatives , Oils, Volatile , Analgesics/analysis , Analgesics/pharmacology , Analgesics/therapeutic use , Animals , Anti-Anxiety Agents/analysis , Anti-Anxiety Agents/pharmacology , Anti-Anxiety Agents/therapeutic use , Anxiety/drug therapy , Hypnotics and Sedatives/analysis , Hypnotics and Sedatives/pharmacology , Hypnotics and Sedatives/therapeutic use , Male , Mice , Molecular Docking Simulation , Oils, Volatile/analysis , Oils, Volatile/pharmacology , Oils, Volatile/therapeutic use , Pain/drug therapy , Phytochemicals/analysis , Phytochemicals/pharmacology , Phytochemicals/therapeutic use , Phytotherapy , Plant Leaves , Receptors, GABA-A/metabolism , Receptors, Muscarinic/metabolism , Receptors, Opioid/metabolism , Sleep Initiation and Maintenance Disorders/drug therapy
3.
Molecules ; 22(6)2017 May 30.
Article in English | MEDLINE | ID: mdl-28556808

ABSTRACT

Medicinal plants have been widely used in the treatment of chronic pain. In this study, we describe the antinociceptive effect of the essential oil from Croton conduplicatus (the EO 25, 50, and 100 mg/kg, i.p.), a medicinal plant native to Brazil. Antinociceptive activity was investigated by measuring the nociception induced by acetic acid, formalin, hot plate and carrageenan. A docking study was performed with the major constituents of the EO (E-caryophyllene, caryophyllene oxide, and camphor). The EO reduced nociceptive behavior at all doses tested in the acetic acid-induced nociception test (p < 0.05). The same was observed in both phases (neurogenic and inflammatory) of the formalin test. When the hot-plate test was conducted, the EO (50 mg/kg) extended the latency time after 60 min of treatment. The EO also reduced leukocyte migration at all doses, suggesting that its antinociceptive effect involves both central and peripheral mechanisms. Pretreatment with glibenclamide and atropine reversed the antinociceptive effect of the EO on the formalin test, suggesting the involvement of KATP channels and muscarinic receptors. The docking study revealed a satisfactory interaction profile between the major components of the EO and the different muscarinic receptor subtypes (M2, M3, and M4). These results corroborate the medicinal use of C. conduplicatus in folk medicine.


Subject(s)
Analgesics/pharmacology , Croton/chemistry , Oils, Volatile/pharmacology , Plant Extracts/pharmacology , Plants, Medicinal/chemistry , Analgesics/chemistry , Animals , Cell Movement/drug effects , KATP Channels/chemistry , KATP Channels/metabolism , Leukocytes/drug effects , Mice , Models, Molecular , Molecular Conformation , Nociception/drug effects , Oils, Volatile/chemistry , Plant Extracts/chemistry , Protein Binding , Receptors, Muscarinic/chemistry , Receptors, Muscarinic/metabolism , Structure-Activity Relationship
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