Vasorelaxant and tracheorelaxant effects of Bocconia arborea and their isolated benzophenanthridine alkaloids.

Bocconia arborea S. Watson (Papaveraceae) is an abundant medicinal plant in the North of Morelos State, Mexico, which is used for the treatment of several diseases. The aim of current investigation was to isolate the compounds responsible of the relaxant effect shown by the active extracts. Thus, phytochemical bio-guided fractionation allowed the isolation of angoline (1), dihydrosanguinarine (2), bocconarborine A (3), oxisanguinarine (4), and oxychelerithrine (5) from dichloromethanic and methanolic extracts from the bark of Bocconia arborea (Papaveraceae). The relaxant study on aortic and tracheal rat rings of all benzophenanthridines indicates that 1 was the most active compound of the entire series investigated. Angoline (1) induces its relaxant effect by a concentration-dependent manner through the calcium channel blockade in both tissues.

Ex Vivo and In Silico Approaches of Tracheal Relaxation through Calcium Channel Blockade of 6-Aminoflavone and Its Toxicological Studies in Murine Models.

Asthma is a condition in which a person's airways become inflamed, narrowed, and produce greater amounts of mucus than normal. It can cause shortness of breath, chest pain, coughing, or wheezing. In some cases, symptoms may be exacerbated. Thus, the current study was designed to determine the mechanism of action of 6-aminoflavone (6-NH2F) in ex vivo experiments, as well as to determine its toxicity in acute and sub-chronic murine models. Tissues were pre-incubated with 6-NH2F, and concentration-response curves to carbachol-induced contraction were constructed. Therefore, tracheal rings pre-treated with glibenclamide, 2-aminopyridine, or isoproterenol were contracted with carbachol (1 µM), then 6-NH2F relaxation curves were obtained. In other sets of experiments, to explore the calcium channel role in the 6-NH2F relaxant action, tissues were contracted with KCl (80 mM), and 6-NH2F was cumulatively added to induce relaxation. On the other hand, tissues were pre-incubated with the test sample, and after that, CaCl2 concentration-response curves were developed. In this context, 6-NH2F induced significant relaxation in ex vivo assays, and the effect showed a non-competitive antagonism pattern. In addition, 6-NH2F significantly relaxed the contraction induced by KCl and CaCl2, suggesting a potential calcium channel blockade, which was corroborated by in silico molecular docking that was used to approximate the mode of interaction with the L-type Ca2+ channel, where 6-NH2F showed lower affinity energy when compared with nifedipine. Finally, toxicological studies revealed that 6-NH2F possesses pharmacological safety, since it did not produce any toxic effect in both acute and sub-acute murine models. In conclusion, 6-aminoflavone exerted significant relaxation through calcium channel blockade, and the compound seems to be safe.

Revisión de la fisiología anorrectal y posibles compuestos bioactivos para la erocosmética / Anorectal physiology and possible bioactive compounds for erocosmetics: A review / Fisiologia anorretal e possíveis compostos bioativos para erocosméticos: uma revisão

RESUMEN Objetivo: realizar una revisión bibliográfica sobre la fisiología ano-rectal, el proceso de relajación y contracción del músculo liso del tracto digestivo y posibles materias primas y formulaciones que podrían incorporarse a formulaciones erocosméticas de uso tópico en la región ano-rectal. Métodos: la revisión bibliográfica se realizó utilizando diferentes descriptores y mediante la consulta en las bases de datos ScienceDirect, PubMed, Clinical Key, Google Scholar y Google Patents. Resultados: inicialmente la revisión de la literatura permite comprender la anatomía y fisiología ano-rectal y los mecanismos que modulan la continencia anal, el tono basal del esfínter anal interno y el reflejo inhibitorio rectoanal (RAIR). Posteriormente, se obtuvo información sobre ejemplos de afrodisíacos naturales y se analizaron formulaciones cosméticas utilizadas como lubricantes anales con el fin de estudiar a profundidad los ingredientes de origen natural e identificar su utilidad, mecanismos de acción tópicos y su función dentro de la formulación. Conclusiones: el entendimiento de la fisiología ano-rectal permite el estudio y desarrollo de formulaciones cosméticas con propiedades analgésicas, anestésicas y relajantes, como los lubricantes anales. Productos naturales como la manzanilla, árnica, Aloe vera y mentol han sido estudiados para su uso cosmético y tópico como analgésicos, anestésicos o relajantes, por lo que su utilidad comprobada los hace útiles en el desarrollo de productos erocosméticos destinados para ser utilizados en la región anogenital.

SUMMARY Aim: To review the anorectal physiology, the process of relaxation and contraction of the smooth muscle of the digestive tract, and possible raw materials and formulations that could be incorporated into erocosmetic formulations for topical use in the anorectal region. Methods: The bibliographic review was carried out using different descriptors and by consulting the databases ScienceDirect, PubMed, Clinical Key, Google Scholar and, Google Patents. Results: Initially, a literature review was carried out to understand anorectal anatomy and physiology and the mechanisms that modulate anal continence, the internal anal sphincter basal tone, and the recto-anal inhibitory reflex (RAIR). Subsequently, information related to natural aphrodisiacs examples was obtained, and cosmetic formulations used as anal lubricants were analyzed to study the natural ingredients and identify their usefulness, mechanisms of action, and function in the formulation. Conclusion: Understanding anorectal physiology allows the study and development of cosmetic formulations with analgesic, anesthetic, and relaxing properties, such as anal lubricants. Natural products such as chamomile, arnica, Aloe vera, and menthol have been studied for cosmetic and topical use as analgesics, anesthetics, and relaxants, so the evidence makes them helpful in developing erocosmetic products intended to be used in the anogenital region.

RESUMO Objetivo: revisar a fisiologia anorretal, o processo de relaxamento e contração da musculatura lisa do trato digestivo e possíveis matérias-primas e formulações que possam ser incorporadas em formulações erocosméticas de uso tópico na região anorretal. Métodos: a revisão bibliográfica foi realizada utilizando diferentes descritores e consultando as bases de dados ScienceDirect, PubMed, Clinical Key, Google Scholar e, Google Patents. Resultados: inicialmente, foi realizada uma revisão da literatura para entender a anatomia e fisiologia anorretal e os mecanismos que modulam a continência anal, o tônus basal do esfíncter anal interno e o reflexo inibitório retoanal (RAIR). Posteriormente, foram obtidas informações relacionadas aos exemplos de afrodisíacos naturais e analisadas formulações cosméticas usadas como lubrificantes anais para estudar os ingredientes naturais e identificar sua utilidade, mecanismos de ação e função na formulação. Conclusão: a compreensão da fisiologia anorretal permite o estudo e o desenvolvimento de formulações cosméticas com propriedades analgésicas, anestésicas e relaxantes, como os lubrificantes anais. Produtos naturais como camomila, arnica, Aloe vera e mentol foram estudados para uso cosmético e tópico como analgésicos, anestésicos e relaxantes, de modo que as evidências os tornam úteis no desenvolvimento de produtos erocosméticos destinados ao uso na região anogenital.

Sambucus nigra: A traditional medicine effective in reducing inflammation in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Sambucus nigra L. is a plant of European origin and popularly known as elder, elderberry, black elder, European elder, European elderberry, and European black elderberry, being described in pharmacopoeia of several countries. Its flowers and berries have been used in folk medicine to treat feverish conditions, coughing, nasal congestion, and influenza besides its popular use as anti-inflammatory, analgesic, and diuretic agent. AIM OF THE STUDY: The aim of this investigation was to elucidate the anti-inflammatory and the relaxant effect of the lyophilized aqueous extract obtained from S. nigra's flowers on in vivo and in vitro inflammation assays and on the isolated rat vascular and airway smooth muscle tissue. MATERIAL AND METHODS: The anti-inflammatory activity of the extract was investigated using carrageenan-induced inflammation model in the subcutaneous tissue of male Swiss mice orally treated with S. nigra extract (30, 100, 300 or 600 mg/kg). Leukocyte influx and the secretion of chemical mediators were quantified in the inflamed exudate. Additionally, histological analysis of the pouches was performed. N-Formyl-methionine-leucine-phenylalanine-induced chemotaxis, lipopolysaccharide-induced TNF, IL-6, IL-1ß, IL-10 and NO production, and adhesion molecule expression (CD62L, CD49d and CD18, flow cytometry) were analyzed in vitro using oyster glycogen-recruited peritoneal neutrophils or macrophages (RAW 264.7) stimulated with LPS and treated with the extract (1, 10 or 100 µg/mL). The resolution of inflammation was accessed by efferocytosis assay, and the antinociceptive activity was investigated using carrageenan-induced mechanical hypersensitivity. Finally, the effect of the extract was evaluated in isolated rat aorta and trachea rings. RESULTS: The oral treatment with S. nigra promoted reduction in the neutrophil migration as well as the decrease of TNF, IL-1ß and IL-6 levels in the inflamed exudate. In vitro treatment with S. nigra decreased NO2-, TNF, IL-1ß and IL-6 and promoted increase of IL-10 in LPS-stimulated neutrophils. Similarly, the extract reduced the NO2-, TNF and IL-6 in LPS-stimulated macrophages. Rutin, the major constituent of S. nigra extract reduced NO2-, TNF, IL-1ß, and IL-6 and promoted the increase of IL-10 in LPS-stimulated neutrophils supernatant. The extract also shed CD62L and CD18 expressions. The extract was able to increase the efferocytosis of apoptotic neutrophils by increasing the IL-10 and decreasing the TNF levels. Additionally, the extract reduced the hypersensitivity induced by carrageenan and promoted a relaxant effect in isolated vascular and non-vascular rat tissue. CONCLUSIONS: S. nigra flowers extract presents anti-inflammatory effect by modulating macrophage and neutrophil functions including the production of inflammatory mediators and cell migration, by promoting efferocytosis and consequently the resolution of acute inflammation, besides exerting antinociceptive effects, scientifically proving its popular use as medicinal plant. Allied to the relaxant effect in both vascular and non-vascular smooth muscle tissue, S. nigra extract represents an important tool for the management of acute inflammation.

In vitro and in silico studies of 8(17),12E,14-labdatrien-18-oic acid in airways smooth muscle relaxation: new molecular insights about its mechanism of action.

In the field of experimental pharmacology, researchers continuously investigate new relaxant agents of the airway smooth muscle cells (ASMCs), since the pathophysiology of respiratory illnesses, such as asthma, involves hyperresponsiveness and changes in ASMC homeostasis. In this scenario, labdane-type diterpenes, like forskolin (FSK), are a class of compounds known for their relaxing action on smooth muscle cells (SMCs), being this phenomenon related to the direct activation of AC-cAMP-PKA pathway. Considering the continuous effort of our group to study the mechanism of action and prospecting for compounds isolated from natural sources, in this paper, we presented how the diterpene 8(17),12E,14-labdatrien-18-oic acid (LBD) promotes relaxant effect on ASMC, performing in vitro experiments using isolated guinea pig trachea and in silico molecular docking/dynamics simulations. In vitro experiments showed that in the presence of aminophylline, FSK and LBD had their relaxant effect potentiated (EC50 from 1.4 ± 0.2 × 10-5 M to 1.5 ± 0.3 × 10-6 M for LBD and from 2.0 ± 0.2 × 10-7 M to 6.4 ± 0.4 × 10-8 M for FSK) while in the presence of Rp-cAMPS this effect was attenuated (EC50 from 1.4 ± 0.2 × 10-5 M to 3 × 10-4 M for LBD and from 2.0 ± 0.2 × 10-7 to 3.1 ± 1.0 × 10-6 M for FSK). Additionally, in silico simulations evidenced that the lipophilic character of LBD is probably responsible for its stability on AC binding site. LBD presented two preferential orientations, where the double bonds of the isoprene moiety as well as the unique polar group (carboxylic acid) in this compound form important anchoring points. In this sense, we consider that the LBD can interact stabilizing the catalytic dimmer of AC as the FSK, although less efficiently.

Pharmacological screening of the phenolic compound caffeic acid using rat aorta, uterus and ileum smooth muscle.

Caffeic acid is a phenolic compound widely found in commonly consumed foods such as pears, apples and coffee, and is pharmacologically known for its antioxidant, anti-inflammatory and anti-asthmatic properties. However, its relaxant activity in the aorta, uterus and ileum smooth muscle has not been investigated. This study aimed to comparatively evaluate the effect of caffeic acid on smooth muscle from different organs (aorta, uterus and ileum), and the contractions of this different organ were induced by different agonists. The organ bath technique was used, where the organs were placed in different cuvettes with 10 mL of Tyrode solution for 1 h to stabilize, then, myometrial, intestinal strip and aortic ring contractions were evoked using different contractile agonists (KCl 60 mM, PHE 0.1 µM, OT 10-2 IU/mL, CCh 10-6 M and BaCl2 0.1-30 mM); increasing concentrations of caffeic acid (0.03-7 mM) were administered in the experimental preparations. In the presence of KCl (60 mM), caffeic acid caused relaxations with the following EC50 values: 2.7 ± 0.26 mM/mL (aorta), 5.7 ± 0.71 mM/mL (uterus) and 2.1 ± 0.39 mM/mL (ileum). When in the presence of different agonists, PHE (0.1 µM) for the aorta, OT (10-2 IU/mL) for the uterus and CCh (10-6 M) for the ileum, caffeic acid caused relaxations with EC50 values of: 2.7 ± 0.31 mM/mL; 2.2 ± 0.34 mM/mL and 2.0 ± 0.28 mM/mL, respectively. The inhibitory effect of caffeic acid on serotonergic (aorta and uterus) and muscarinic receptors (uterus and ileum), as well as its possible involvement with L-type Ca2+ channels, was also observed. This study reports the pharmacological characterization of caffeic acid on smooth muscle from different organs, for which caffeic acid was more potent in the ileum. A diverse understanding of its performance as a possible therapeutic product is attributed to its relaxant effect.

Chemistry and Biology of Selected Mexican Medicinal Plants.

Herbal medicines are an integral element of alternative medical care in Mexico, and the best testimony to their efficacy and cultural value is their persistence in contemporary Mexican marketplaces where the highest percentages of medicinal and aromatic plants are sold. This chapter summarizes current trends in research on medicinal plants in Mexico, with emphasis on work carried out at the authors' laboratories. The most relevant phytochemical and pharmacological profiles of a selected group of plants used widely for treating major national health problems are described.From this contribution, it is evident that in the last five decades a significant amount of research on medicinal plants has been performed by Mexican scientists. Such efforts have led to the publication of many research papers in noted peer-reviewed journals and technical books. The isolation and structural characterization of hundreds of bioactive secondary metabolites have been accomplished, and most importantly, these studies have tended to support the ethnomedical uses of many different species. A multidisciplinary approach for investigating these plants has led to an increased emphasis on areas such as phytopharmacology, phytotoxicology, quality control, regulation, and conservation issues for these valuable resources. The medicinal plants analyzed so far have shown a very broad chemical diversity of their constituents, which have a high potential for exhibiting novel mechanistic effects biologically. The chapter shows also that there is need to conduct additional clinical studies on herbal drugs, in particular because the longstanding traditional evidence for their safety is not always sufficient to assure their rational use. There is also need to move to "omics" approaches for investigating the holistic effect and the influence of groups of phytochemicals on the whole organism. Mexican scientists may be expected to have bright prospects in this regard, which will imbue medicinal plant research with a new dynamism in the future.

New insights on relaxant effects of (-)-borneol monoterpene in rat aortic rings.

The monoterpene alcohol (-)-borneol has many biological effects such as sedative, anti-inflammatory, analgesic, anti-nociceptive, antithrombotic and vasorelaxant effects. Our objective in this study was to investigate the mechanism of action of (-)-borneol and determine its vasorelaxant effect. (-)-Borneol was tested on isolated aortic rings contracted with PE (10-6  m). This study was performed in the absence or in the presence of endothelium, L-NAME (100 µm), indomethacin (10 µm), TEA (1 and 10 mm), 4-AP (1 mm) or glibenclamide (1 mm) to assess the participation of EDRF, nitric oxide, prostanoids and potassium channels on the relaxing effect of (-)-borneol. In this work, (-)-borneol induced a relaxant effect in aortic rings, with and without endothelium, in a concentration-dependent manner. The pharmacological characterization obtained using L-NAME, indomethacin, TEA, 4-AP and glibenclamide demonstrates that the effect of (-)-borneol was modified in the presence of L-NAME, indomethacin and glibenclamide showing that these signal transduction pathways are involved in the relaxing effect of the monoterpene. (-)-Borneol has a vasorelaxant effect that depends on the presence of vascular endothelium, with the participation of nitric oxide and prostanoids. Also, (-)-borneol displayed a direct action on the vascular smooth muscle, greatly dependent on KATP channels.

Relaxant effects of Peperomia hispidula (Sw.) A. Dietr. on isolated rat tracheal rings / Efecto relajante de Peperomia hispidula (Sw.) A. Dietr. sobre anillos aislados de tráquea de rata

Peperomia hispidula (Sw.) A. Dietr. is used in Mexican traditional medicine for treating respiratory illnesses such as asthma. The latter disorder results from an excessive and inappropriate constriction of airway smooth muscle. The aim of the present study was to evaluate the relaxant activity of P. hispidula on isolated rat tracheal rings contracted with carbachol. The methyleugenol was identified as the main active constituent in the dichloromethane extract. To explore the possible mechanism of action, concentration-response curves were constructed in the presence and absence of propranolol (3 µM), indomethacin (10 µM), glibenclamide (1 µM), and L-NAME (300 µM), finding that neither reduced methyleugenol-induced smooth muscle relaxation. In conclusion, P. hispidula herein displayed relaxant activity on rat tracheal rings. The effect of methyleugenol, was probably not related to the activation of ß2-adrenoceptors, prostaglandins, K+ATP channels or nitric oxide.

Peperomia hispidula (Sw.) A. Dietr. es utilizada en la medicina tradicional mexicana para tratar enfermedades respiratorias como el asma. Este último trastorno es el resultado de una contracción excesiva e inapropiada del músculo liso de las vías respiratorias. El objetivo del presente estudio fue evaluar la actividad relajante de P. hispidula sobre anillos aislados de tráquea de rata contraídos con carbacol. El metileugenol fue identificado como el principal constituyente activo en el extracto de diclorometano. Para explorar el posible mecanismo de acción, se construyeron curvas concentración-respuesta en presencia y ausencia de propranolol (3 µM), indometacina (10 µM), glibenclamida (1 µM), y L-NAME (300 µM), encontrando que ninguno redujo la relajación del músculo liso inducida por metileugenol. En conclusión, P. hispidula muestra actividad relajante en anillos de tráquea de rata. El efecto de metileugenol, al parecer no está implicado con la activación de los receptores ß2-adrenérgicos, prostaglandinas, canales de K+ATP u óxido nítrico.

Assessment of Candida SPP. proliferation in occlusal and palatal splints / Avaliação da proliferação Candida SPP. em placas oclusais e palatais

Candida species inhabit the oral cavity of all individuals who wear complete denture and whose material is the same as that used in splints. Assess the growth of C. albicans in occlusal and palatal splints used for treatment of TMD so that the potential risks of oral microbiota can be assessed. The growth of Candida spp. was assessed in the saliva of 27 individuals wearing splints for treatment of TMD. They were divided into two groups: G1 (n = 14), individuals wearing occlusal splint; and G2 (n = 13), individuals wearing palatal splint. Saliva samples were collected during placement of the splints (T1) and after 4 months (T2), being stored in PBS (10 mL) after 60-second rinses. It was observed that patients wearing occlusal splints (G1) had an increase of 0.648 CFU/mL (Log 10), with statistically significant differences (P = 0.043) for C. albicans (42.33%), C. glabrata (5.52%), C. krusei (41.72%) and C. tropicalis (10.43%). In the group of patients wearing palatal splints (G2), there was a decrease of 0.101 CFU/mL (Log 10), was observed with (P = 0.964) only the presence of C. albicans. The results suggest that growth of Candida species was greater in patients wearing occlusal splints compared to those wearing palatal ones as the presence of different yeast species was found in the former.

Espécies de Candida habitam a cavidade oral de 60-100% de indivíduos usuários de prótese total, cujo material é o mesmo utilizado em placas miorrelaxante. Avaliar o crescimento de C. albicans. em placas relaxantes musculares oclusais e palatais, usadas para o tratamento de DTM, na intenção de verificar riscos em potencial à microbiota bucal. Avaliou-se o crescimento de Candida spp. na saliva de 27 indivíduos, usuários de placa miorrelaxante, em tratamento para DTM no ICT-UNESP. Os indivíduos foram divididos em dois grupos: G1(n=14) ­ placa com recobrimento oclusal; e G2 (n=13) ­ sem recobrimento. As coletas foram com PBS (10mL), em bochechos por 60seg, na instalação das placas (T1) e após 4 meses (T2). Observou-se que pacientes usuários da placa miorrelaxante com recobrimento oclusal (grupo G1) apresentaram aumento de 0,648 UFC/mL (Log10) com diferença estatisticamente significante (p=0,043) analisando-se 42,33% C. albicans, 5,52% C. glabrata, 41,72% C. krusei e 10,43% C. tropicalis. No grupo de pacientes que utilizaram a placa sem recobrimento (grupo G2), observou-se diminuição de 0,101 UFC/mL (Log10) com (p=0,954) apresentando apenas C. albicans. Os resultados sugerem que os pacientes que fizeram uso de placa miorrelaxante com recobrimento oclusal apresentaram maior crescimento de Candida spp. em relação aos usuários de placa sem recobrimento, verificando-se a presença de diferentes espécies da levedura.

Clove oil induces anaesthesia and blunts muscle contraction power in three Amazon fish species.

Clove oil is used as an anaesthetic for many species of fish worldwide; however, relatively few studies have assessed its effectiveness on Amazon fish species and no compelling evidence has ever been reported on the relaxant properties of this oil for skeletal muscle of fish. Thus, the objective of this study was to evaluate the latencies to deep anaesthesia and recovery, along with the myorelaxant effect of clove oil on three Amazon fish species: cardinal tetra, Paracheirodon axelrodi, banded cichlid, Heros severus and angelfish, Pterophyllum scalare, submitted to short-term anaesthetic baths. Fish were assayed in three groups of 60 fish each and individually anaesthetized in a completely randomized design with six clove oil concentrations using 10 fish/species/concentration. Electromyographic recordings from dorsal muscle were performed during stages of induction and recovery in which nine fish/species/stage were used. Deep anaesthesia was attained for all concentrations tested, and no mortalities were observed throughout the experiments and after a 48-h observation period. Concentration of 90 µL L-1 and above promoted fast deep anaesthesia (< 3 min) and calm recovery in angelfish and cardinal tetra, whereas the concentration of 60 µL L-1 sufficed to quickly anaesthetize banded cichlid. Times to full recovery were not significantly contrasting among species and occurred within appropriate time threshold (< 5 min). Clove oil exerted a conspicuous depression of muscle contraction power, and therefore can be effectively used as a muscle relaxant agent for P. scalare, P. axelrodi, H. severus and potentially, for other fish species.

Sedative and muscle relaxant activities of diterpenoids from Phlomidoschema parviflorum

Abstract Phlomidoschema parviflorum (Benth.) Vved. (Basionym: Stachys parviflora Benth.) Lamiaceae, have significance medicinal importance as it is used in number of health disorders including diarrhea, fever, sore mouth and throat, internal bleeding, weaknesses of the liver and heart genital tumors, sclerosis of the spleen, inflammatory tumors and cancerous ulcers. The present contribution deals with the sedative and muscle relaxant like effects of diterpenoids trivially named stachysrosane and stachysrosane, isolated from the ethyl acetate soluble fraction of P. parviflorum. Both compounds (at 5, 10 and 15 mg/kg, i.p) were assessed for their in vivo sedative and muscle relaxant activity in open field and inclined plane test, respectively. The geometries of both compounds were optimized with density functional theory. The molecular docking of both compounds were performed with receptor gamma aminobutyric acid. Both compounds showed marked activity in a dose dependent manner. The docking studies showed that both compounds interact strongly with important residues in receptor gamma aminobutyric acid. The reported data demonstrate that both compounds exhibited significant sedative and muscle relaxant-like effects in animal models, which opens a door for novel therapeutic applications.

A Systematic Review of the Anxiolytic-Like Effects of Essential Oils in Animal Models.

The clinical efficacy of standardized essential oils (such as Lavender officinalis), in treating anxiety disorders strongly suggests that these natural products are an important candidate source for new anxiolytic drugs. A systematic review of essential oils, their bioactive constituents, and anxiolytic-like activity is conducted. The essential oil with the best profile is Lavendula angustifolia, which has already been tested in controlled clinical trials with positive results. Citrus aurantium using different routes of administration also showed significant effects in several animal models, and was corroborated by different research groups. Other promising essential oils are Citrus sinensis and bergamot oil, which showed certain clinical anxiolytic actions; along with Achillea wilhemsii, Alpinia zerumbet, Citrus aurantium, and Spiranthera odoratissima, which, like Lavendula angustifolia, appear to exert anxiolytic-like effects without GABA/benzodiazepine activity, thus differing in their mechanisms of action from the benzodiazepines. The anxiolytic activity of 25 compounds commonly found in essential oils is also discussed.

Relaxant effects of a hydroalcoholic extract of Ruta graveolens on isolated rat tracheal rings

BACKGROUND: Ruta graveolens L. (R. graveolens) is a medicinal plant employed in non-traditional medicines that has various therapeutic properties, including anthelmintic, and vasodilatory actions, among others. We evaluated the trachea-relaxant effects of hydroalcoholic extract of R. graveolens against potassium chloride (KCl)- and carbachol-induced contraction of rat tracheal rings in an isolated organ bath. RESULTS: The results showed that the airway smooth muscle contraction induced by the depolarizing agent (KCl) and cholinergic agonist (carbachol) was markedly reduced by R. graveolens in a concentration-dependent manner, with maximum values of 109 ± 7.9 % and 118 ± 2.6 %, respectively (changes in tension expressed as positive percentages of change in proportion to maximum contraction), at the concentration of 45 µg/mL (half-maximal inhibitory concentration IC50: 35.5 µg/mL and 27.8 µg/mL for KCl- and carbachol-induced contraction, respectively). Additionally, the presence of R. graveolens produced rightward parallel displacement of carbachol dose-response curves and reduced over 35 % of the maximum smooth muscle contraction. CONCLUSIONS: The hydroalcoholic extract of R. graveolens exhibited relaxant activity on rat tracheal rings. The results suggest that the trachea-relaxant effect is mediated by a non-competitive antagonistic mechanism. More detailed studies are needed to identify the target of the inhibition, and to determine more precisely the pharmacological mechanisms involved in the observed biological effects.

Anesthesia for cesarean section in pregnant woman with Guillain Barré syndrome: a case report / Anestesia para cesariana em gestante com síndrome de Guillain Barré: relato de caso / Anestesia para cesárea en gestante con síndrome de Guillain Barré: relato de caso

Background and objectives: Guillain Barré syndrome (GBS) is an autoimmune neurological disease characterized by an acute or subacute demyelinating polyradiculoneuritis. It is an unusual event during pregnancy and a challenge for the anesthesiologist, due to the possibility of impairment of neuromuscular function and occurrence of respiratory complications in the post-operative period. The objective of this paper is to discuss the anesthetic management of a pregnant patient affected by the disease. Case report: Female patient, 30 years old, 38 weeks' pregnant, diagnosed with fetal death that occurred about a day, and with SGB. Cesarean section was performed under general anesthesia, progressing without complications perioperatively. Conclusions: Although it is uncommon, GBS can affect pregnant women and the anesthesiologist may encounter such patients in his (her) daily practice. It is important to understand the peculiarities of GBS to adequately address the patient in the perioperative period, contributing to its better evolution. .

Justificativa e objetivos: A síndrome de Guillain Barré (SGB) é uma doença neurológica autoimune que se caracteriza por uma polirradiculoneurite desmielinizante aguda ou subaguda. É um evento incomum durante a gravidez e um desafio para o anestesiologista pela possibilidade de comprometimento da função neuromuscular e de complicações respiratórias no pós-operatório. O objetivo deste trabalho é discutir o manejo anestésico da paciente gestante afetada pela doença. Relato de caso: Paciente do sexo feminino com 30 anos, gestante de 38 semanas, com diagnóstico de óbito fetal havia um dia e SGB. Foi submetida à cesariana sob anestesia geral, evoluindo sem intercorrências no perioperatório. Conclusões: Apesar de ser incomum, a SGB pode acometer gestantes e o anestesiologista pode se deparar com esse tipo de paciente na sua prática diária. É importante compreender as peculiaridades da SGB para se abordar adequadamente a paciente no perioperatório, contribuindo para a sua melhor evolução. .

Justificación y objetivos: El síndrome de Guillain Barré (SGB) es una enfermedad neurológica autoinmune que se caracteriza por una polirradiculoneuritis desmielinizante aguda o subaguda. Es un evento poco común durante el embarazo y se le considera un reto para el anestesista por la posibilidad de compromiso de la función neuromuscular y de complicaciones respiratorias en el postoperatorio. El objetivo de este trabajo es discutir el manejo anestésico de la paciente gestante afectada por la enfermedad. Caso clínico: Paciente del sexo femenino con 30 años, gestante de 38 semanas, con diagnóstico de óbito fetal hacía un día y SGB. Fue sometida a cesárea bajo anestesia general, evolucionando sin intercurrencias en el perioperatorio. Conclusiones: A pesar de ser poco común, el SGB puede perjudicar a las gestantes y el anestesista puede tener que enfrentarse con ese tipo de paciente en su práctica diaria. Es importante comprender las peculiaridades del SGB para abordar adecuadamente a la paciente en el perioperatorio, contribuyendo así a su mejor evolución. .

[Anesthesia for cesarean section in pregnant woman with Guillain Barré syndrome: a case report]. / Anestesia para cesariana em gestante com síndrome de Guillain Barré: relato de caso.

BACKGROUND AND OBJECTIVES: Guillain Barré syndrome (GBS) is an autoimmune neurological disease characterized by an acute or subacute demyelinating polyradiculoneuritis. It is an unusual event during pregnancy and a challenge for the anesthesiologist, due to the possibility of impairment of neuromuscular function and occurrence of respiratory complications in the postoperative period. The objective of this paper is to discuss the anesthetic management of a pregnant patient affected by the disease. CASE REPORT: Female patient, 30 years old, 38 weeks' pregnant, diagnosed with fetal death that occurred about a day, and with SGB. Cesarean section was performed under general anesthesia, progressing without complications perioperatively. CONCLUSIONS: Although it is uncommon, GBS can affect pregnant women and the anesthesiologist may encounter such patients in his (her) daily practice. It is important to understand the peculiarities of GBS to adequately address the patient in the perioperative period, contributing to its better evolution.

Tracheal relaxation of five medicinal plants used in Mexico for the treatment of several diseases.

OBJECTIVE: To assess the relaxant effect of several organic extracts obtained from Agastache mexicana (A. mexicana), Cochlospermum vitifolium (C. vitifolium), Cordia morelosana (C. morelosana), Lepechinia caulescens (L. caulescens) and Talauma mexicana (T. mexicana) used in Mexican traditional medicine for the treatment of several diseases. METHODS: Extracts were obtained by maceration at room temperature using hexane, dichloromethane and methanol for each plant material. The organic extracts were evaluated ex vivo to determine their relaxant activity on the contractions induced by carbachol (cholinergic receptor agonist, 1 µ mol/L) in isolated rat tracheal rings. RESULTS: A total of 15 extracts were evaluated (three for each species). All test samples showed significant relaxant effect, in a concentration-dependent manner, on the contractions induced by 1 µ mol/L carbachol, with exception of extracts from C. morelosana. Active extracts were less potent than theophylline [phosphodiesterase inhibitor, EC50: (28.79±0.82) µg/mL] that was used as positive control. Concentration-response curves revealed that the extracts with more significant effects were dichloromethanic extracts of T. mexicana [Emax: (103.03±3.32)% and EC50: (159.39±3.72) µg/mL) and C. vitifolium [Emax: (106.58±2.42)% and EC50: (219.54±7.61) µg/mL]. Finally, hexanic and dichloromethanic extracts from A. mexicana were fully effective but less potent than T. mexicana and C. vitifolium. CONCLUSIONS: Less polar extracts obtained from A. mexicana, T. mexicana and C. vitifolium exhibited greater relaxant effect on tracheal rat rings, which allows us to suggest them as sources for the isolation of bioactive molecules with potential therapeutic value in the treatment of asthma.

Influence of laser therapy and muscle relaxant on the masseter muscle under occlusal wear: an ultrastructural study / Influencia de la terapia laser y relajante muscular en el músculo masetero bajo oclusión: un estudio ultraestructural

The aim of this study was to analyze the influence of low-intensity laser therapy and muscle relaxant in the characteristic ultra structural masseter muscle occlusal wear. Animals and Methods: 40 male Wistar rats were randomly divided into four groups: the control group (GI), occlusal wear (G-II), laser occlusal wear (G-III), and the muscle relaxant occlusal wear (G-IV). Under general anesthesia given intraperitoneally, animals in groups II, III and IV had unilateral amputation of upper and lower molar cusps to simulate an occlusal wear situation. The masseter muscle G-III received laser therapy (830nm, 4J/cm2, 40mW, f ~ 2mm) and the procedure was subsequently repeated every other day for 14/30 days. G-IV animals were treated with daily injection of dantrolene ® (2.5 mg / kg in 0.5 ml of H2O). From 24 hours after the elimination peak. The animals were euthanized with an overdose of anesthesia on days 14 and 30 after the removal of the cusps and the ipsilateral masseter muscle was excised and divided in two, one half was routinely processed for light microscopy and other for electron microscopy. There was no statistical difference between each experimental group and the control and between periods in each experimental group. However, the muscle fibers in the G-II showed the most pronounced changes. There is no causal relationship between muscles fibers injuries and occlusion and, despite signs of muscular tissue injury were more evident in the occlusal wear group. Results indicates a moderate action of laser therapy and muscle relaxants in skeletal muscle...

El objetivo del estudio fue analizar la influencia de la terapia láser de baja intensidad y del relajante muscular sobre las características ultraestructurales del músculo masetero en el desgaste oclusal. 40 ratas macho Wistar, se dividieron al azar en cuatro grupos: grupo de control (GI), desgaste oclusal (G-II), laserterapia desgaste oclusal (G-III), y relajante muscular desgaste oclusal (G-IV). Bajo anestesia general por vía intraperitoneal, los animales de los grupos II, III y IV sufrieron amputación unilateral de las cúspides de los molares superiores e inferiores para simular una situación de desgaste oclusal. El músculo masetero del G-III recibió la terapia con laser (830nm, 4J/cm2, 40mW, f ~ 2mm) después del procedimiento el cual se repitió durante 14/30 días. Los animales del G-IV fueron tratados con una inyección diaria de Dantroleno® (2,5 mg/Kg en 0,5 ml de H2O). Los animales fueron sacrificados con una sobredosis de anestesia general en los días 14 y 30. Después de la remoción de las cúspides el músculo masetero ipsilateral se extirpó y se dividió en dos, una mitad fue procesada para microscopía de luz y la otra para microscopía electrónica. No hubo diferencias estadísticamente significativas entre cada grupo experimental y el control, así como, entre los períodos en cada grupo experimental. Sin embargo, las fibras musculares en el G-II mostraron los cambios más pronunciados. En conclusión no existe relación causal entre las lesiones de las fibras musculares y la oclusión, a pesar que los signos de lesión de los tejidos musculares fue más evidente en el grupo con desgaste oclusal. Los resultados indican una acción moderada ejercida por la terapia láser y de los relajantes musculares sobre el músculo esquelético...

Comparison of the variability of the onset and recovery from neuromuscular blockade with cisatracurium versus rocuronium in elderly patients under total intravenous anesthesia

This study was designed to compare the variability of the onset and offset of the effect of two neuromuscular blocking drugs with different elimination pathways in adult and elderly patients during total intravenous anesthesia (TIVA). After Ethics Committee approval and patients’ informed consent, the drugs were compared in 40 adult and 40 elderly patients scheduled for elective surgery under TIVA with tracheal intubation who were randomized to receive a single bolus dose of 0.15 mg/kg cisatracurium or 0.9 mg/kg rocuronium. The time of onset of maximum depression, duration of action, and recovery index time were measured and recorded for each patient and variability is reported as means ± standard deviation. Time of onset was significantly shorter for rocuronium than cisatracurium for the adult and elderly groups (P = 0.000), but the variability of cisatracurium was significantly greater compared with rocuronium for the same age groups (93.25 vs 37.01 s in the adult group and 64.56 vs 33.75 s in the elderly group; P = 0.000). The duration of the effect in the elderly group receiving rocuronium was significantly longer than in the elderly group receiving cisatracurium, and the variability of the duration was significantly greater in the rocuronium group than in the cisatracurium group. Mean time of recovery was significantly longer for the elderly group receiving rocuronium than for the elderly group receiving cisatracurium (P = 0.022), and variability was also greater (P = 0.002). Both drugs favored good intubating conditions. In conclusion, cisatracurium showed less variability in these parameters than rocuronium, especially in the elderly, a fact that may be of particular clinical interest.

Relaxant effect of the essential oil of Croton nepetifolius on ovine cervix

We investigated the in vitro effect of the essential oil of Croton nepetifolius Baill., Euphorbiaceae (EOCN), on spontaneous or induced contractions of circular and longitudinal muscles from the ovine cervix during the luteal phase of the estrous cycle. The relaxant effect of EOCN was expressed as a percentage of the contraction recorded before the addition of the oil and calculated relative to the preparations exposed only to the vehicle. The IC50 (concentration of oil required to produce a 50% maximal reduction in muscle contraction) for relaxation of spontaneous contractions in circular and longitudinal muscles was significantly lower than the IC50 for blockade of K+-induced contraction (27.19 µg mL-1 versus 262.72 µg mL-1 and 40.92 µg mL-1 versus 222.47 µg mL-1, respectively). Interestingly, there was a high degree of selectivity in the action of EOCN on cervix layers concerning the inhibition of acetylcholine-induced contraction in circular (IC50 277.10 µg mL-1) and longitudinal (IC50 52.56 µg mL-1) muscles. In conclusion, EOCN is able to relax ovine cervix during the luteal phase. This work opens the perspective of applying EOCN in ovine embryo transfer.