RESUMEN
The traditional use of the M. charantia L. plant to treat coughs, fever and expectoration is widely practiced in different cultures, but its effectiveness and safety still require scientific investigation. This study sought to perform a chemical analysis and evaluate the antitussive, expectorant and antipyretic effects of the ethanolic extract of M. charantia leaves (EEMc) in rats and mice. The EEMc was subjected to chemical analysis by HPLC-DAD, revealing the presence of the flavonoids astragalin and isoquercetin. Acute oral toxicity in mice did not result in deaths, although changes in liver weight and stool consistency were observed. EEMc demonstrated an antitussive effect at doses of 100 and 300â mg/kg in mice subjected to cough induction by citric acid nebulization. Furthermore, it showed expectorant activity at a dose of 300â mg/kg, assessed based on the elimination of the phenol red marker in bronchoalveolar lavage. In the evaluation of antipyretic activity in rats, fever induced by Saccharomyces cerevisiae was reduced at all doses tested during the first hour after treatment. This innovative study identified the presence of astragalin and isoquercetin in EEMc and indicated that the extract has antitussive, expectorant and antipyretic properties. Therefore, EEMc presents itself as a promising option in herbal medicine for the treatment of respiratory symptoms and fever.
Asunto(s)
Antipiréticos , Antitusígenos , Etanol , Expectorantes , Momordica charantia , Extractos Vegetales , Hojas de la Planta , Animales , Extractos Vegetales/química , Extractos Vegetales/farmacología , Extractos Vegetales/aislamiento & purificación , Ratones , Antitusígenos/farmacología , Antitusígenos/química , Antitusígenos/aislamiento & purificación , Hojas de la Planta/química , Ratas , Etanol/química , Antipiréticos/farmacología , Antipiréticos/química , Antipiréticos/aislamiento & purificación , Masculino , Momordica charantia/química , Expectorantes/farmacología , Expectorantes/aislamiento & purificación , Expectorantes/química , Tos/tratamiento farmacológico , Ratas Wistar , Relación Dosis-Respuesta a Droga , Saccharomyces cerevisiae/efectos de los fármacos , Fiebre/tratamiento farmacológicoRESUMEN
Althaea officinalis Linn. (AO) is a widely distributed herbaceous plant with a long history of medicinal and food functions in Europe and Western Asia. Althaea officinalis polysaccharide (AOP), as one of the main components and a crucial bioactive substance of AO, has a variety of pharmacological activities, including antitussive, antioxidant, antibacterial, anticancer, wound healing, immunomodulatory, and infertility therapy effects. Many polysaccharides have been successfully obtained in the last five decades from AO. However, there is currently no review available concerning AOP. Considering the importance of AOP for biological study and drug discovery, the present review aims to systematically summarize the recent major studies on extraction and purification methods of polysaccharides from different AO parts (seeds, roots, leaves and flowers), as well as the characterization of their chemical structure, biological activity, structure-activity relationship, and the application of AOP in different fields. Meanwhile, the shortcomings of AOP research are further discussed in detail, and new valuable insights for future AOP research as therapeutic agents and functional foods are proposed.
Asunto(s)
Althaea , Antitusígenos , Althaea/química , Polisacáridos/química , Antioxidantes/química , Extractos Vegetales/farmacología , Antitusígenos/farmacologíaRESUMEN
Cannabis sativa is a millenary medicinal plant. However, contrary to worldwide paradigm-shifting, countries like Brazil still prohibit C. sativa cultivation and its medicinal use, even though many populations use aerial parts and roots of this plant for healthcare. As such, the objective of this work was to identify substances in the samples of the C. sativa roots, tracing a correlation with antitussive and expectorant effects. Therefore, samples of C. sativa roots were donated by the Polícia Federal Brasileira, and its aqueous extract (AECsR) was prepared with subsequent lyophilization, to maintain the material stability. After that, the material was analyzed by LC-MS to observe its chemical profile. Four samples (AECsR-A, B, C, and D) were tested in animal models of citric acid-induced cough (0.4 M) and phenol red expectoration (500 mg/kg). Using LC-MS it was possible to identify 5 molecules in C. sativa roots: p-coumaroyltyramine, tetrahydrocannabinol-C4, feruoiltyramine, anhydrocanabisativine, and cannabisativine. In experimental protocols, male mice (Mus musculus) were treated with samples of AECsR at doses of 12.5, 25, or 50 mg/kg regardless of the pharmacological test. In these tests, all samples showed the potential to treat cough and promote fluid expectoration, differing only in the dose at which these effects were observed. Therefore, the data showed that the C. sativa roots of the Brazilian Northeast showed antitussive and expectorant effects, even with intense secondary metabolites' variation, which alters its potency, but not its effect. This highlights the importance of this medicinal plant for future therapy and corroborates to traditional use.
Asunto(s)
Antitusígenos , Cannabis , Plantas Medicinales , Ratones , Animales , Antitusígenos/farmacología , Antitusígenos/uso terapéutico , Expectorantes/farmacología , Expectorantes/uso terapéutico , Tos/inducido químicamente , Tos/tratamiento farmacológico , Brasil , Fenolsulfonftaleína , Cromatografía Liquida , Dronabinol/uso terapéutico , Espectrometría de Masas en Tándem , Plantas Medicinales/química , Ácido Cítrico/toxicidad , Ácido Cítrico/uso terapéuticoRESUMEN
Candida albicans is involved in periodontal disease, which is influenced by sex hormones. AIM: To study the effects of the estrogen antagonist tamoxifen (TAM) on periodontal disease of oncological patients; clinical oral strains of C. albicans. PATIENTS: With periodontitis and breast cancer and other with AIDS were used. MATERIALS & METHODS: Periodontal disease was evaluated by the academy of periodontology procedures and the growth of clinical C. albicans isolates were evaluated by the Clinical and Laboratory Standards Institute techniques. RESULTS: Women who consumed TAM for more than 2 years decreased periodontitis severity. In vitro, TAM inhibited the growth of both fluconazole-sensitive and resistant C. albicans. CONCLUSION: Administered TAM chronically improves periodontal health and has antifungal activity on oral strains isolated from patients with odontologic and medical pathologies.
Asunto(s)
Antifúngicos/farmacología , Neoplasias de la Mama/complicaciones , Candida albicans/efectos de los fármacos , Enfermedades Periodontales/tratamiento farmacológico , Enfermedades Periodontales/microbiología , Tamoxifeno/farmacología , Antitusígenos/farmacología , Azoles , Neoplasias de la Mama/tratamiento farmacológico , Candida albicans/aislamiento & purificación , Candida albicans/patogenicidad , Estrógenos , Femenino , Fluconazol/farmacología , Humanos , Huésped Inmunocomprometido , Bolsa Periodontal/microbiología , PeriodontitisRESUMEN
ETHNOPHARMACOLOGY RELEVANCE: Blepharocalyx salicifolius (Kunth) O. Berg (Myrtaceae) is a tree native to Argentina and Uruguay that grows and is cultivated along the riverside of the Rio de la Plata. The leaves of this plant species, locally known as "anacahuita" are used in South America to prepare infusions for the empiric treatment of cough and bronchospasm, as well as diarrhoea and other intestinal disorders. Although previous phytochemical studies have been performed with the essential oil extracted from Blepharocalyx salicifolius, pharmacological evidence supporting its traditional use is still lacking. AIM OF THE STUDY: To experimentally evaluate the pharmacological properties of Blepharocalyx salicifolius based on its traditional use. The studies were performed with tincture (T-Bs) and essential oil (EO-Bs) prepared from its leaves, in isolated rat trachea, intestine and heart preparations. METHODS: The ex-vivo effects of T-Bs and EO-Bs were evaluated with the agonists carbachol (CCh) and calcium chloride (Ca2+) in the contractile concentration-response curves (CRC) of the isolated intestine. The muscle relaxant effect of EO-Bs was evaluated in the isolated trachea and compared with the effect achieved with papaverine as a positive control. The T-Bs and EO-Bs cardiac effects were analysed by perfusion of an isolated rat heart before a period of ischemia/reperfusion (stunning model). The antitussive effect of both T-Bs and EO-Bs was evaluated in mice exposed to ammonia using codeine as a positive control. RESULTS: Both T-Bs and EO-Bs induced a non-competitive inhibition of the CCh-CRC in the rat intestine, with IC50 values of 170.3 ± 48.5µg T-Bs/mL (n = 6) and 5.9 ± 1.6µg EO-Bs/mL (n = 6), respectively. EO-Bs also inhibited non-competitively the Ca2+-CRC, with IC50 value of 1.8 ± 0.3µg EO-Bs/mL (n = 8). A similar effect was obtained with the main active component of the EO-Bs 1,8-cineole. In isolated trachea, EO-Bs induced the relaxation of the CCh-contracted tissue (1.7 ± 0.2µg EO-Bs/mL, n = 11) up to a maximal relaxation that was 1.9 times higher than that of papaverine. In the isolated heart, EO-Bs induced a poor negative inotropic response, and did not improve the contractile and energetic recovery after ischemia and reperfusion. In the mouse cough model, EO-Bs (90mg/Kg) was as effective as codeine (30mg/Kg) in reducing cough frequency. CONCLUSIONS: The results indicate that the preparations from Blepharocalyx salicifolius leaves were effective as central antitussive, bronchodilating and antispasmodic agents, suggestive of a mechanism associated with the inhibition of Ca2+ influx into smooth muscle. The EO-Bs displayed only a poor ability to reduce cardiac inotropism, and was devoid of any cardioprotective properties. Thus, the present study validates the traditional use of this South American plant for asthma, cough and bronchospasm, shedding new light into its potency and putative mechanism of action.
Asunto(s)
Medicina Tradicional/métodos , Myrtaceae/química , Aceites Volátiles/farmacología , Extractos Vegetales/farmacología , Animales , Antitusígenos/administración & dosificación , Antitusígenos/aislamiento & purificación , Antitusígenos/farmacología , Broncodilatadores/administración & dosificación , Broncodilatadores/aislamiento & purificación , Broncodilatadores/farmacología , Calcio/metabolismo , Cardiotónicos/administración & dosificación , Cardiotónicos/aislamiento & purificación , Cardiotónicos/farmacología , Tos/tratamiento farmacológico , Modelos Animales de Enfermedad , Femenino , Concentración 50 Inhibidora , Masculino , Ratones , Aceites Volátiles/administración & dosificación , Aceites Volátiles/aislamiento & purificación , Parasimpatolíticos/administración & dosificación , Parasimpatolíticos/aislamiento & purificación , Parasimpatolíticos/farmacología , Extractos Vegetales/administración & dosificación , Hojas de la Planta , Ratas , Ratas Sprague-Dawley , América del SurRESUMEN
Several drugs acting on the nervous system have been implicated in the prolongation of the QT interval. Leaving aside the antidepressant and antipsychotic drugs, some have shown to prolong the QT interval in vivo. These include opioids, particularly methadone, inhalational anesthetics, and some preparations used for treatment of cough. These drugs have a narrow therapeutic interval or possible drug interactions that lead to clinical toxicity manifested by arrhythmias. They share the ability to block potassium channels (HERG), prolong the action potential and QT interval, and generate arrhythmias and Torsades de Pointes like other typicality recognized like antiarrhythmics, antihistamines, prokinetics, psychotropics and anti-infectives agents. Muscle relaxants like alcuronium, pancuronium and atracurium associated with or without atropine prolong significantly the QT interval. Methadone is the opiod most tightly associated with QTc prolongation; with much lesser potency buprenorphine and oxycodone can block HERG channels and depress the IKr current in vitro.Antineoplastic chemotherapy like anthracyclines, alkylating drugs, alkilants and cisplatin are associated with electrocardiographic alterations including prolongation of QT and emesis of different grades. It's very important take in account the synergic effects over the QT prolongation when effective antiemetics like 5-HT3 receptor antagonist (granisetron, ondansetron, and dolasetron) are administered. The Knowledge of their pharmacological properties is of vital importance to avoid exposing particularly vulnerable individuals as those with congenital long QT syndrome, and even the general public to unnecessary risk of potentially fatal arrhythmias.
Asunto(s)
Fármacos del Sistema Nervioso Central/efectos adversos , Síndrome de QT Prolongado/inducido químicamente , Torsades de Pointes/inducido químicamente , Analgésicos Opioides/efectos adversos , Analgésicos Opioides/farmacología , Anestésicos por Inhalación/efectos adversos , Anestésicos por Inhalación/farmacología , Animales , Antitusígenos/efectos adversos , Antitusígenos/farmacología , Fármacos del Sistema Nervioso Central/farmacología , Interacciones Farmacológicas , Canal de Potasio ERG1 , Canales de Potasio Éter-A-Go-Go/antagonistas & inhibidores , Humanos , Síndrome de QT Prolongado/congénito , Factores de RiesgoRESUMEN
AIM OF THE STUDY: Evaluate the potential inhibition of cough in a mouse model induced by sulfur dioxide gas of methanol and chloroform extracts of aerial parts of Chamaedorea tepejilote. MATERIAL AND METHODS: The antitussive effect was examined using the Ogyhara method. The extracts and theobromine were orally administered to mice. Each extract was administered to one group (400mg/Kg) and theobromine (2mg), and negative control received PVP. The frequency of cough was measured at 60, 90min after the administration of chloroform extract. RESULTS: The water extract of C. tepejilote had no effect on the pharmacological model used in this study. The effects of the methanol and chloroform extracts of this plant on sulfur-dioxide-induced cough in experimental animals show activity dose-dependently in the range between 100 to 500mg/Kg. At doses of 400mg/kg, the methanol and chloroform extracts inhibited cough by 41.72% and 49.1%, respectively; these results are comparable to the effect produced by the antitussive agent theobromine (53.4% inhibition). CONCLUSIONS: Both extracts exhibited significant antitussive activity, and the effect of the chloroform extract was dose dependent. The antitussive activity of this extract was comparable to that of theobromine. The effect of chloroform extract on the trachea was also tested; it did not relax pre-contractions in guinea pig trachealis induced KCl, carbachol or histamine.
Asunto(s)
Antitusígenos/farmacología , Arecaceae/química , Tos/tratamiento farmacológico , Extractos Vegetales/farmacología , Administración Oral , Animales , Antitusígenos/administración & dosificación , Antitusígenos/aislamiento & purificación , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Cobayas , Masculino , Ratones , Contracción Muscular/efectos de los fármacos , Componentes Aéreos de las Plantas , Extractos Vegetales/administración & dosificación , Dióxido de Azufre , Teobromina/farmacología , Factores de Tiempo , Tráquea/efectos de los fármacosRESUMEN
El ziprepol es un medicamento antitusígeno, derivado de piperazina, que en dosis elevadas tiene propiedades adictivas y neurotóxicas. En Chile hay un aumento del abuso de este fármaco por parte de jóvenes, con fines alucinógenos, euforizantes y sedantes. Se analizan las propiedades farmacológicas del ziprepol y las características de la adiccón y de la toxicidad por sobredosis