ABSTRACT
The essential oils obtained by hydrodistillation from fresh leaves of Vitex agnus-castus and Ocimum campechianum, and from fresh inflorescences of Ocimum carnosum were analysed by GC-FID and GC-MS. The major components of V. agnus-castus essential oil were identified as 1,8-cineole (47.9%), terpinyl α-acetate (11.6%), sabinene (11.2%) and caryophyllene oxide (9.7%), while in the O. campechianum essential oil were eugenol (72.1%), ß-elemene (6.8%), (E)-caryophyllene (6.4%) and bicyclogermacrene (5.2%). Linalool (79.0%), α-epi-cadinol (5.4%), terpinen-4-ol (3.2%) and 1,8-cineole (2.8%) were the major constituents in the O. carnosum essential oil. The essential oils were subsequently evaluated for their larvicidal and cytotoxic activities. Larval bioassay against Aedes aegypti of V. agnus-castus, O. campechianum and O. carnosum essential oils showed LC50 values of 97.55 ± 0.35, 81.45 ± 0.35 and 109.49 ± 0.35 µg/mL, respectively. The in vitro cytotoxic activities of the essential oils has been evaluated on breast adenocarcinoma (MCF-7), lung carcinoma (NCI-H292), pro-myelocytic leukemia (HL-60), and cervical adenocarcinoma (HEP-2) human cell lines, and pro-myelocytic leukemia cells lines (HL-60) were found to be the most sensitive to all the essential oils tested than the others. This is the first report on larvicidal and cytotoxic activities of these essential oils.
Subject(s)
Aedes/drug effects , Insecticides/pharmacology , Larva/drug effects , Ocimum/chemistry , Oils, Volatile/pharmacology , Plant Oils/pharmacokinetics , Vitex/chemistry , Animals , Biological Assay , Cell Line, Tumor/drug effects , Gas Chromatography-Mass Spectrometry , Humans , Insecticides/isolation & purification , Oils, Volatile/chemistry , Oils, Volatile/isolation & purification , Plant Leaves/chemistry , Plant Oils/chemistry , Toxicity Tests , Vitex/classificationABSTRACT
Plants of the genus Aristolochia have been frequently reported as important medicinal plants. Despite their high bioactive potential, to date, there are no reports of their effects on leaf-cutting ants. Therefore, the present study aimed to evaluate the insecticidal activity of the essential oil of Aristolochia trilobata and its major components on Atta sexdens and Acromyrmex balzani, two species of leaf-cutting ants. The bioassays were performed regarding routes of exposure, acute toxicity, binary mixtures of the major components and behavioral effects. Twenty-five components were identified in the essential oil of A. trilobata using a gas chromatographic system equipped with a mass spectrometer and a flame ionization detector. The components found in higher proportions were sulcatyl acetate, limonene, p-cymene and linalool. The essential oil of A. trilobata and its individual major components were efficient against A. balzani and A. sexdens workers when applied by fumigation. These components showed fast and efficient insecticidal activity on ants. The components acted synergistically and additively on A. balzani and A. sexdens, respectively, and caused a strong repellency/irritability in the ants. Thus, our results demonstrate the great potential of the essential oil of A. trilobata and its major components for the development of new insecticides.
Subject(s)
Ants/drug effects , Aristolochia/chemistry , Insecticides/chemistry , Oils, Volatile/chemistry , Animals , Ants/physiology , Behavior, Animal/drug effects , Chromatography, Gas , Fumigation , Insecticides/pharmacology , Oils, Volatile/pharmacology , Plant Leaves/chemistry , Plant Oils/chemistry , Plant Oils/pharmacologyABSTRACT
Plant-derived natural products can serve as an alternative to synthetic compounds for control of ticks of veterinary and medical importance. Lippia gracilis is an aromatic plant that produces essential oil with high content of carvacrol and thymol monoterpenes. These monoterpenes have high acaricidal activity against Rhipicephalus (Boophilus) microplus. However, there are no studies that show efficacy differences of essential oils between susceptible and organophosphate resistant strains of R. (B.) microplus. The aim of the present study was to compare acaricidal effects of essential oils extracted from two different genotypes of L. gracilis and the main monoterpenes on larvae of both susceptible and organophosphate resistant R. (B.) microplus larvae. The efficacy of the essential oil of two genotypes of L. gracilis (106 and 201) and their monoterpenes carvacrol and thymol was measured using the larval immersion test on coumaphos-resistant and susceptible strains of R. (B.) microplus. Lethal concentrations were calculated using GraphPad Prism 6.0. Chemical analysis was performed by GC-MS and FID. Thymol and carvacrol were observed to be major constituents in 106 and 201L. gracilis genotype essential oils, respectively. Essential oils of both genotypes were more effective against organophosphate-resistant tick strain than susceptible tick strain. Carvacrol was 3.2 times more toxic to organophosphate resistant strain than to susceptible strain. Thymol was equally toxic to resistant and susceptible tick strains. The significantly higher efficacy monoterpene carvacrol against resistant ticks may lead to development of new natural product acaricide formulations for use to control organophosphate resistant R. (B.) microplus populations.
Subject(s)
Acaricides/pharmacology , Lippia/chemistry , Oils, Volatile/pharmacology , Plant Oils/pharmacology , Rhipicephalus/drug effects , Acaricides/chemistry , Animals , Cymenes , Drug Resistance , Female , Gas Chromatography-Mass Spectrometry , Larva , Monoterpenes/chemistry , Monoterpenes/pharmacology , Oils, Volatile/chemistry , Organophosphates/pharmacology , Phytochemicals/chemistry , Phytochemicals/pharmacology , Plant Leaves/chemistry , Plant Oils/chemistry , Thymol/chemistry , Thymol/pharmacologyABSTRACT
This study aimed to evaluate the orofacial antinociceptive effect of the Cymbopogon winterianus essential oil (LEO) complexed in ß-cyclodextrin (LEO-CD) and to assess the possible involvement of the central nervous system (CNS). The LEO was extracted, chromatographed, and complexed in ß-cyclodextrin. The complex was characterized by differential scanning calorimetry (DSC) and thermogravimetry derivative (TG/DTG). Male Swiss mice (2-3 months) were treated with LEO-CD (50-200 mg/kg, p.o.), vehicle (distilled water, p.o.), or standard drug (i.p.) and subjected to the orofacial nociception formalin-, capsaicin-, and glutamate-induced. After the formalin test, the animals were perfused and the brains subjected to immunofluorescence for Fos. The rota-rod test (7 rpm/min) was carried out. Geraniol (37.57%) was the main compound of LEO. DSC and TG/DTG proved the complexation. The orofacial nociceptive behavior was significantly (p < 0.05) reduced. The number of Fos-positive cells was significantly changed in the dorsal raphe nucleus (p < 0.01), locus coeruleus (p < 0.001), trigeminal nucleus (p < 0.05), and trigeminal thalamic tract (p < 0.05). LEO-CD did not cause changes in motor coordination in the rota-rod test. Thus, our results suggested that LEO-CD has an orofacial antinociceptive profile, probably mediated by the activation of the CNS without changing the motor coordination.
ABSTRACT
Ocimum selloi is an herbal species popularly used in Brazil as antispasmodic. Herein, we report the antispasmodic effect of O. selloi essential oil (OS) in segments of guinea-pig ileum. OS did not reduce the tonus of the ileum. In contrast, OS reduced the contraction induced by carbachol (100 µM), BaCl2 (0.03 M) and low- and high-K(+) concentrations (25 and 60 mM, respectively). OS shifted the concentration-response curve for calcium to the right in a parallel manner. GC/MS analysis showed that OS consists mostly of methyl chavicol (97.57%). These results suggest that OS antispasmodic effect is mediated through calcium channel blockade. In addition, OS effect and mode of action could be accounted for methyl chavicol.
Subject(s)
Ileum/drug effects , Ocimum/chemistry , Oils, Volatile/pharmacology , Parasympatholytics/pharmacology , Plant Oils/pharmacology , Allylbenzene Derivatives , Animals , Anisoles/pharmacology , Female , Gas Chromatography-Mass Spectrometry , Guinea Pigs , In Vitro Techniques , Male , Muscle Contraction/drug effects , Muscle, Smooth/drug effects , Plant Leaves/chemistryABSTRACT
The formation of inclusion complexes of Hyptis pectinata essential oil (EOHP), with potent activities such as anti-nociceptive, anti-inflammatory, among others, with ß -cyclodextrin (ß-CD), was obtained by slurry (SC) and paste procedures (PC). The gas chromatography coupled to the mass spectrometry (GC/MS) analysis demonstrated a total of 36.4% monoterpenes and 63.6% sesquiterpenes in the EOHP. The major components of EOHP were identified as (E)- caryophyllene (54.07%). The analysis of samples (PM, PC and SC) by GC/MS involved the surface and the total extracted oils. The GC/MS results suggested important differences between in SC and PC methods indicating the complexation of mono and sesquiterpenoids in different ratios. Furthermore, the thermal analysis techniques suggests the complexation, especially in SC, which show a thermogravimetry/derivative thermogravimetry (TG/DTG) peak at 140-270ºC, probably related to oil loss. Scanning electron microscopy (SEM) images showed reduction size of the samples mainly in the SC product. Additionally, EOHP/ ß-CD improves pharmacological profile of EOHP alone in formalin-induced pain protocol in mice.
Subject(s)
Analgesics/therapeutic use , Hyptis , Oils, Volatile/therapeutic use , Pain/drug therapy , beta-Cyclodextrins/therapeutic use , Analgesics/analysis , Analgesics/chemistry , Animals , Calorimetry, Differential Scanning , Female , Formaldehyde , Gas Chromatography-Mass Spectrometry , Mice , Microscopy, Electron, Scanning , Oils, Volatile/analysis , Oils, Volatile/chemistry , Pain/chemically induced , Phytochemicals/analysis , Phytochemicals/chemistry , Phytochemicals/therapeutic use , Phytotherapy , Plant Leaves , X-Ray Diffraction , beta-Cyclodextrins/chemistryABSTRACT
O. basilicum leaves produce essential oils (LEO) rich in monoterpenes. The short half-life and water insolubility are limitations for LEO medical uses. ß-Cyclodextrin (ß-CD) has been employed to improve the pharmacological properties of LEO. We assessed the antihyperalgesic profile of LEO, isolated or complexed in ß-CD (LEO/ß-CD), on an animal model for fibromyalgia. Behavioral tests: mice were treated every day with either LEO/ß-CD (25, 50 or 100 mg/kg, p.o.), LEO (25 mg/kg, p.o.), tramadol (TRM 4 mg/kg, i.p.) or vehicle (saline), and 60 min after treatment behavioral parameters were assessed. Therefore, mice were evaluated for mechanical hyperalgesia (von Frey), motor coordination (Rota-rod) and muscle strength (Grip Strength Metter) in a mice fibromyalgia model. After 27 days, we evaluated the central nervous system (CNS) pathways involved in the effect induced by experimental drugs through immunofluorescence protocol to Fos protein. The differential scanning analysis (DSC), thermogravimetry/derivate thermogravimetry (TG/DTG) and infrared absorption spectroscopy (FTIR) curves indicated that the products prepared were able to incorporate the LEO efficiently. Oral treatment with LEO or LEO-ßCD, at all doses tested, produced a significant reduction of mechanical hyperalgesia and we were able to significantly increase Fos protein expression. Together, our results provide evidence that LEO, isolated or complexed with ß-CD, produces analgesic effects on chronic non-inflammatory pain as fibromyalgia.
Subject(s)
Analgesics/therapeutic use , Fibromyalgia/drug therapy , Monoterpenes/therapeutic use , Ocimum basilicum/chemistry , Oils, Volatile/therapeutic use , Proto-Oncogene Proteins c-fos/genetics , beta-Cyclodextrins/chemistry , Analgesics/administration & dosage , Analgesics/chemistry , Analgesics/isolation & purification , Animals , Central Nervous System/drug effects , Central Nervous System/metabolism , Central Nervous System/physiopathology , Fibromyalgia/genetics , Fibromyalgia/physiopathology , Hand Strength , Hyperalgesia/drug therapy , Hyperalgesia/genetics , Hyperalgesia/physiopathology , Male , Mice , Monoterpenes/administration & dosage , Monoterpenes/chemistry , Monoterpenes/isolation & purification , Motor Activity/drug effects , Oils, Volatile/administration & dosage , Oils, Volatile/chemistry , Oils, Volatile/isolation & purification , Plant Leaves/chemistry , Up-Regulation/drug effectsABSTRACT
Many species from Croton genus have been used in traditional medicine and its pharmacological activities demonstrated. Croton argyrophyllus Kunth, Euphorbiaceae, is a shrub that grows in the flora of Northeastern Brazilian. The essential oil of C. argyrophyllus leaves was tested in rodents (10-100 mg/kg, p.o.) in classical models of inflammation (carrageenan-induced paw oedema and peritonitis) and its chemical constituents were determined by GC-MS/FID analysis. Nitric oxide radical-scavenging activity and lipidic peroxidation were determined to evaluate the antioxidant capacity of the essential oil (0.001-100 µg/mL). Forty-two components were identified, among them, bicyclogermacrene (14.60%) and spathulenol (8.27%) were the most abundant ones. C. argyrophyllus essential oil reduced significantly the oedema (30 and 100 mg/kg, p<0.05) and, besides, reduced the carrageenan increase in mieloperoxidase activity (10, 30, and 100 mg/kg, p<0.001). The carrageenan-induced peritonitis was significantly reduced (p<0.001) by the essential oil (10, 30, and 100 mg/kg). The essential oil (100 mg/kg) reduces the total peritoneal lavage NOx- concentration (p<0.01). Nitric oxide radical generated from sodium nitroprusside was found to be inhibited by the essential oil (p<0.001). C. argyrophyllus essential oil was able to prevent Fe2+- or Fe2+ plus H2O2-induced lipid peroxidation (p<0.001). This study suggests that the anti-inflammatory effect of the essential oil of C. argyrophyllus observed in the present study can be related, at least in part, its antioxidant capacity.
ABSTRACT
Ants are highly abundant in neotropical regions, with certain species adapted to the urban environment, where they can cause damage to human health. The main method for controlling ants consists of using organosynthetic insecticides, which are potentially toxic to the environment. Essential plant oils are considered a viable alternative to the use of conventional insecticides. In this study, we analyze the bioinsecticidal activity and repellence of patchouli essential oil (Pogostemon cablin) against three species of urban ants: Camponotus melanoticus, Camponotus novograndensis, and Dorymyrmex thoracicus. The chemical composition of the essential oil was analyzed by GC-MS and GC-FID. The major compounds were patchoulol (36.6%) followed by α-bulnesene (13.95%), and α-guaiene (11.96%). Toxicity and repellency bioassays were performed using the essential oil over the ants, and mortality evaluations were performed at 4, 24, and 48 h after performing the bioassays. Mortality percentage of the ants on 7 µg/mg was on average 84%. The essential oil of P. cablin displayed toxicity against all three species of urban ants, with the lowest LD50 being observed for D. thoracicus (2.02 µg oil/mg insect) after 48 h of exposure compared to C. melanoticus (2.34 µg oil/mg insect) and C. novogranadensis (2.95 µg oil/mg insect). The essential oil of P. cablin was strongly repellent to the three species of ants in all concentrations tested (0.01% and 1% v/v). Considering the potential toxicity and repellency of the P. cablin essential oil to the urban ants, future studies could investigate the practical application of this oil to control of this insects.
Subject(s)
Ants/drug effects , Insect Repellents/pharmacology , Insecticides/pharmacology , Lamiaceae/chemistry , Oils, Volatile/pharmacology , Plant Oils/pharmacology , Animals , Biological Assay , Insect Repellents/chemistry , Insecticides/chemistry , Oils, Volatile/chemistry , Plant Oils/chemistry , Time FactorsABSTRACT
The larvicidal activities of essential oils from the leaves of Artemisia vulgaris L., Cymbopogon flexuosus (Nees ex Steud.) Wats. and Piper tuberculatum Jacq. were evaluated using third-instar larvae of Aedes aegypti. The essential oils were obtained by hydrodistillation and analyzed by GC and GC-MS. The essential oil of P. tuberculqatum had the lowest LC50 value (106.3 +/- 2.2 microg/mL), followed by that of A. vulgaris (114.1 +/- 1.7 microg/mL) and C. flexuosus (121.6 +/- 0.8 micro/mL). The results show that these essential oils may be potent sources of natural larvicides.
Subject(s)
Aedes/physiology , Insecticides/toxicity , Oils, Volatile/toxicity , Animals , Artemisia/chemistry , Brazil , Cymbopogon/chemistry , Gas Chromatography-Mass Spectrometry , Larva , Lethal Dose 50 , Oils, Volatile/chemistry , Piper/chemistry , Plant Leaves/chemistry , Sesquiterpenes/chemistry , Sesquiterpenes/isolation & purification , Sesquiterpenes/toxicityABSTRACT
Plants are promising sources of new bioactive compounds. The aim of this study was to investigate the cytotoxic potential of nine plants found in Brazil. The species studied were: Annona pickelii Diels (Annonaceae), Annona salzmannii A. DC. (Annonaceae), Guatteria blepharophylla Mart. (Annonaceae), Guatteria hispida (R.âE. Fr.) Erkens & Maas (Annonaceae), Hancornia speciosa Gomes (Apocynaceae), Jatropha curcas L. (Euphorbiaceae), Kielmeyera rugosa Choisy (Clusiaceae), Lippia gracilis Schauer (Verbenaceae), and Hyptis calida Mart. Ex Benth (Lamiaceae). Different types of extractions from several parts of plants resulted in 43 extracts. Their cytotoxicity was tested against HCT-8 (colon carcinoma), MDA-MB-435 (melanoma), SF-295 (glioblastoma), and HL-60 (promielocitic leukemia) human tumor cell lines, using the thiazolyl blue test (MTT) assay. The active extracts were those obtained from G. blepharophylla, G. hispida, J. curcas, K. rugosa, and L. gracilis. In addition, seven compounds isolated from the active extracts were tested; among them, ß-pinene found in G. hispida and one coumarin isolated from K. rugora showed weak cytotoxic activity. In summary, this manuscript contributes to the understanding of the potentialities of Brazilian plants as sources of new anticancer drugs.
Subject(s)
Bridged Bicyclo Compounds/pharmacology , Coumarins/pharmacology , Magnoliopsida/chemistry , Monoterpenes/pharmacology , Oils, Volatile/pharmacology , Plant Extracts/pharmacology , Annonaceae/chemistry , Antineoplastic Agents, Phytogenic , Apocynaceae/chemistry , Bicyclic Monoterpenes , Brazil , Bridged Bicyclo Compounds/chemistry , Bridged Bicyclo Compounds/isolation & purification , Cell Line, Tumor , Cell Survival , Clusiaceae/chemistry , Coumarins/chemistry , Coumarins/isolation & purification , Humans , Hyptis/chemistry , Jatropha/chemistry , Latex/chemistry , Lippia/chemistry , Monoterpenes/chemistry , Monoterpenes/isolation & purification , Oils, Volatile/chemistry , Oils, Volatile/isolation & purification , Plant Components, Aerial/chemistry , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plants, Medicinal/chemistryABSTRACT
Chrysopogon zizanioides (L.) Roberty, Poaceae, is a plant widely used in northeast Brazil in folk medicine for the treatment of various pathological conditions, including inflammatory pain. The present study evaluated the antinociceptive and anti-inflammatory effects of C. zizanioides essential oil (EO) in rodents. EO was further characterized by GC/MS. The major components of EO were identified as khusimol (19.57%), E-isovalencenol (13.24%), α-vetivone (5.25%), β-vetivone (4.87%) and hydroxy-valencene (4.64%). Following intraperitoneal injection (i.p.), EO at 50 and 100 mg/kg significantly reduced the number of writhes (51.9 and 64.9%, respectively) and the number of paw licks during phase 2 (56.7 and 86.2%, respectively) of a formalin model when compared to control group animals. However, EO-treated mice were ineffective at all doses in hot-plate and rota-rod tests. The EO inhibited the carrageenan-induced leukocyte migration to the peritoneal cavity in a dose-dependent manner (34.7, 35.4, and 62.5% at doses of 25, 50 and 100 mg/kg, respectively). In the paw edema test, the EO (100 mg/kg) inhibited all three phases of the edema equally well, suggesting that the EO has a non-selective inhibitory effect on the release or actions of these mediators. Our results suggest possible antinociceptive and anti-inflammatory effects of the EO.
ABSTRACT
Leishamaniasis is a disease that affects more than 2 million people worldwide, whose causative agent is Leishmania spp. The current therapy for leishmaniasis is far from satisfactory. All available drugs, including pentavalent antimony, require parenteral administration and are potentially toxic. Moreover, an increase in clinical resistance to these drugs has been reported. In this scenario, plant essential oils used traditionally in folk medicine are emerging as alternative sources for chemotherapeutic compounds. In this study, in vitro leishmanicidal effects of a thymol- and a carvacrol-rich essential oil from leaves of Lippia sidoides Cham. were investigated. The essential oils were extracted and their constituents were characterized by gas chromatography coupled to mass spectrometry (GC/MS). Both essential oils showed significant activity against promastigote forms of Leishmania chagasi. However, we found that carvacrol-rich essential oil was more effective, with IC50/72 h of 54.8 µg/mL compared to 74.1 µg/mL for thymol-rich oil. Carvacrol also showed lower IC50 than thymol. Our data suggest that L. sidoides essential oils are indeed promising sources of leishmanicidal compounds.
Subject(s)
Antiprotozoal Agents/pharmacology , Leishmania/drug effects , Lippia/chemistry , Monoterpenes/pharmacology , Oils, Volatile/pharmacology , Plant Oils/pharmacology , Thymol/pharmacology , Cymenes , Gas Chromatography-Mass Spectrometry , Inhibitory Concentration 50 , Monoterpenes/isolation & purification , Plant Leaves/chemistry , Thymol/isolation & purificationABSTRACT
Leishamaniasis is a disease that affects more than 2 million people worldwide, whose causative agent is Leishmania spp. The current therapy for leishmaniasis is far from satisfactory. All available drugs, including pentavalent antimony, require parenteral administration and are potentially toxic. Moreover, an increase in clinical resistance to these drugs has been reported. In this scenario, plant essential oils used traditionally in folk medicine are emerging as alternative sources for chemotherapeutic compounds. In this study, in vitro leishmanicidal effects of a thymol- and a carvacrol-rich essential oil from leaves of Lippia sidoides Cham. were investigated. The essential oils were extracted and their constituents were characterized by gas chromatography coupled to mass spectrometry (GC/MS). Both essential oils showed significant activity against promastigote forms of Leishmania chagasi. However, we found that carvacrol-rich essential oil was more effective, with IC50/72 h of 54.8 μg/mL compared to 74.1 μg/mL for thymol-rich oil. Carvacrol also showed lower IC50 than thymol. Our data suggest that L. sidoides essential oils are indeed promising sources of leishmanicidal compounds.
Subject(s)
Antiprotozoal Agents/pharmacology , Leishmania/drug effects , Lippia/chemistry , Monoterpenes/pharmacology , Oils, Volatile/pharmacology , Plant Oils/pharmacology , Thymol/pharmacology , Gas Chromatography-Mass Spectrometry , Monoterpenes/isolation & purification , Plant Leaves/chemistry , Thymol/isolation & purificationABSTRACT
The composition of three samples of essential oil (EO) extracted from the leaves and flowers of Hyptis fruticosa (Lamiaceae) were investigated by GC/MS and GC-FID. The variability of the constituents and biological activity were evaluated in the oil samples. Acetic acid-induced abdominal constrictions and formalin-induced pain tests in mice were used for screening the antinociceptive activity. The possible antagonism of the essential oils or morphine (MOR) antinociceptive effects by pretreatment with naloxone, showed no influence on the antinociceptive action of the oils in the acetic acid-induced writhing test. All examined oil samples presented antinociceptive activity. The oil sample obtained from the leaves collected during the vegetative growth stage, near São Cristóvão at Sítio Tujubeba exhibited the highest effect. The same oil sample had a main percentage of 1,8-cineole (18.70%). Nevertheless, the oil obtained from flowers collected at the same location, showed a significant difference (p < 0.05) in the response intensity in the first phase of paw licking (100 mg/kg) possibly due to the higher contents of α-pinene (20.51%) and ß-pinene (13.64%). The results provide evidence for the use of H. fruticosa by traditional medicine practitioners in the management of pain.
Subject(s)
Analgesics/pharmacology , Hyptis/chemistry , Nociception/drug effects , Oils, Volatile/pharmacology , Acetic Acid , Animals , Bicyclic Monoterpenes , Bridged Bicyclo Compounds/chemistry , Flowers/chemistry , Formaldehyde , Male , Mice , Monoterpenes/chemistry , Oils, Volatile/analysis , Plant Extracts/pharmacology , Plant Leaves/chemistryABSTRACT
AIM OF THE STUDY: Hyptis pectinata Poit (Lamiaceae) is grown in the northeastern regions of Brazil and is popularly known as "sambacaitá" or "canudinho". It is extensively used in folk medicine to treat inflammatory conditions, bacterial infections, pain, and cancer. MATERIALS AND METHODS: Hyptis pectinata essential oil (EO, 10, 30, and 100mg/kg, p.o.) and the reference drugs morphine (5mg/kg, p.o.) and acetylsalicylic acid (ASA, 200mg/kg, p.o.) were evaluated using models for analgesia (acetic acid-induced contortions and hot plate) or inflammation (formalin-induced licking response and the subcutaneous air-pouch model). To elucidate the EO's mechanism of action, animals were pre-treated with the opioid receptor antagonist naloxone (1mg/kg, i.p.), the cholinergic antagonist atropine (1mg/kg, i.p.), or l-nitro arginine methyl ester (l-NAME, 3mg/kg, i.p.) 30 min prior to the oral administration of the EO. RESULTS: The EO significantly inhibited the number of writhings and the time the animals spent licking their formalin-injected paws (second phase). The EO, at doses of 30 and 100mg/kg, increased baseline measurements and area under the curve measurements in the hot plate model, respectively. The administration of naloxone reversed the antinociceptive effect of the EO in the hot plate model. l-NAME significantly reversed the effects of the EO in the contortions and hot plate models. Atropine completely reversed the antinociceptive activity of the EO in all models. Additionally, the EO inhibited the inflammatory process induced by subcutaneous carrageenan injection by reducing cell migration, exudate volume, protein concentration, and inflammatory mediators (nitric oxide, prostaglandin E2, IL-6, and TNF-α) produced in the pouch. CONCLUSIONS: Our results indicate that the Hyptis pectinata essential oil exhibits antinociceptive effects, likely mediated by opioid and cholinergic receptors, and anti-inflammatory activity through the inhibition of nitric oxide and PGE2 production.
Subject(s)
Analgesics/pharmacology , Anti-Inflammatory Agents/pharmacology , Hyptis/chemistry , Oils, Volatile/pharmacology , Animals , Dinoprostone/metabolism , Dose-Response Relationship, Drug , Interleukin-6/metabolism , Male , Mice , Mice, Inbred BALB C , Nitric Oxide/biosynthesis , Tumor Necrosis Factor-alpha/metabolismABSTRACT
Cymbopogon citratus DC. Stapf, Poaceae, is used in the folk medicine for hypertension treatment. This work investigated the chemical composition and cardiovascular effects in rats of C. citratus essential oil (EOCC). A phytochemical screening demonstrated the presence of eight constituents, being geranial the major compound (43.08 percent). In rats, EOCC (1, 5, 10, and 20 mg/kg, i.v.) induced transient hypotension and bradycardia that were attenuated by atropine and sodium thiopental, but not by L-NAME or indomethacin. In rings of rat superior mesenteric artery pre-contracted with phenylephrine, EOCC (1 to 3000 µg/mL) induced relaxation that was not affected after removal of the endothelium, after TEA or in rings pre-contracted with KCl (80 mM). Furthermore, EOCC (1000 µg/mL) was not able to induce additional effect on maximal relaxation of nifedipine (10 µM). In conclusions, EOCC induces hypotension, possibly by reduction in vascular resistance caused by inhibition of the Ca2+ influx, and bradycardia probably due to an activation of cardiac muscarinic receptors.
C. citratus é utilizada na medicina popular para tratar hipertensão. Este trabalho investigou a composição química e os efeitos cardiovasculares do óleo essencial do C. citratus (OECC). Foram identificados oito constituintes no OECC, sendo geranial o majoritário (43,08 por cento). Em ratos, o OECC (1, 5, 10 e 20 mg/kg, i.v.) induziu hipotensão e bradicardia que foram atenuadas pela atropina e tiopental sódico, mas não por L-NAME ou indometacina. Em anéis de artéria mesentérica de ratos pré-contraídos com fenilefrina, o OECC (1 a 3000 µg/mL) induziu relaxamento que não foi afetado após remoção do endotélio, após TEA ou em anéis pré-contraídos com KCl (80 mM). Além disso, o OECC (1000 µg/mL) não induziu efeito adicional sobre o relaxamento máximo da nifedipina (10 µM). Em conclusão, o OECC induz hipotensão possivelmente devido à redução da resistência vascular que pode ser causada por inibição do influxo de Ca2+, e bradicardia provavelmente devido à ativação de receptores muscarínicos cardíacos.
ABSTRACT
The essential oils of Croton heliotropiifolius Kunth (Euphorbiaceae) and Croton pulegiodorus Baill. were selected for larvicidal evaluation against Aedes aegypti L. (Diptera: Culicidae) and studied qualitatively and quantitatively by GC and GC-MS. Sixty-one compounds representing 92.03% (C. heliotropiifolius) and 85.68% (C. pulegiodorus) of the essential oils, respectively, have been identified. The major components of C. heliotropiifolius essential oil were identified as beta-caryophyllene (35.82%), bicyclogermacrene (19.98%), and germacrene-D (11.85%). The major components in C. pulegiodorus essential oil were identified as beta-caryophyllene (20.96%), bicyclogermacrene (16.89%), germacrene-D (10.55%), tau-cadinol (4.56%), and beta-copaen-4-alpha-ol (4.35%). The essential oil of C. pulegiodorus (LC50 159 ppm) was more effective against Ae. aegypti than that of C. heliotropiifolius (LC50 544 ppm). In order to verify whether the major compound of both essential oils is the active principle responsible for the larvicidal activity, beta-caryophyllene was purchased and its larvicidal potential was further evaluated. However, beta-caryophyllene (LC50 1038 ppm) showed weak larvicidal potency. Results of larvicidal evaluation suggest the existence of a synergistic effect of minor components in the essential oils.
Subject(s)
Aedes , Croton/chemistry , Insecticides/pharmacology , Oils, Volatile/pharmacology , Animals , Brazil , Drug Synergism , Gas Chromatography-Mass Spectrometry , Insecticides/chemistry , Insecticides/isolation & purification , Larva , Lethal Dose 50 , Mosquito Control/methods , Oils, Volatile/chemistry , Oils, Volatile/isolation & purification , Plant Oils/chemistry , Plant Oils/isolation & purification , Plant Oils/pharmacology , Species SpecificityABSTRACT
The chemical compositions of the essential oils from the peel of ripe and unripe fruits of Hymenaea courbaril L., obtained by hydrodistillation, were analyzed by GC and GC-MS. The main constituents of the essential oil from the peel of the ripe fruits were the sesquiterpenes alpha-copaene (11.1%), spathulenol (10.1%) and beta-selinene (8.2%), while germacrene-D (31.9%), beta-caryophyllene (27.1%) and bicyclogermacrene (6.5%) were the major compounds in the oil from unripe fruits. The essential oils were tested against Aedes aegypti larvae and showed LC50 values of 14.8 +/- 0.4 microg/mL and 28.4 +/- 0.3 microg/mL for the ripe and unripe fruit peel oils, respectively. From the peel of the ripe fruits, the diterpenes zanzibaric acid and isoozic acid were isolated, along with the sesquiterpene caryolane-1,9beta-diol. To the best of our knowledge, this is the first report of this sesquiterpene in the genus. The structures of all compounds isolated were identified on the basis of their spectral data (IR, MS, 1D- and 2D-NMR) and by comparison with literature spectral data.
Subject(s)
Hymenaea/chemistry , Insecticides/pharmacology , Oils, Volatile/analysis , Aedes , Animals , Fruit/chemistry , Larva/drug effects , Oils, Volatile/pharmacologyABSTRACT
Ocimum selloi essential oil (2, 20, and 200 mg/kg; p.o.) reduced, in a dose-dependent way, the abdominal contraction induced by acetic acid (0.6%; i.p.) and the diarrhea episodes induced by castor oil in mice. At the higher dose (200 mg/kg; p.o.), the essential oil significantly reduced intestinal transit (P<0.05) in the charcoal meal test. The main component detected in O. selloi essential oil was methyl chavicol (98%; GC and GC/MS).These effects seems to support the use of O. selloi against diarrhea, intestinal spasm and visceral pain.