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1.
J Ethnopharmacol ; 267: 113634, 2021 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-33246113

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The conventional naturopaths of Punjab Province (Pakistan) have trivial usage of Anagallis arvensis Linn.(Primulaceae) for cure of diarrhea, constipation, asthma as well as hypertension. AIM: Present research was focused to discover comprehensive mechanism of spasmogenic, spasmolytic, bronchorelaxant and hypotensive folkloric usage of Anagallis arvensis Linn.. METHODOLOGY: The crude extract of Anagallis arvensis Linn. (Aa.Cr) & its (aqueous & organic) portions tested in-vitro on isolated jejunum, ileum, trachea, aorta, paired atria preparations as well as in-vivo in mice & normotensive anaesthetized rats. The responses have been noted by transducers (isotonic & isometric) coupled to Power Lab. RESULT: Anagallis arvensis Linn. (Aa.Cr; crude aqueous-alcoholic extract) produced contractile action at low concentrations but relaxant action was observed by increasing concentrations on spontaneous contractions of isolated jejunum of rabbit. But, pre-treatment of tissue with atropine prior extract caused suppression of contractile effect indicating presence of cholinergic muscarinic response of Aa.Cr. It also triggered relaxation of high Potassium -stimulated contractions of jejunum with subsequent non-parallel right move in Ca++ CRCs. Moreover, Aa.Cr relaxed carbachol - & high Potassium - stimulated contractions in trachea of rabbit but observed relaxant effect was powerful against CCh (1 µM)- stimulated contractions with rightside parallel move of CCh-curves succeeded by non-parallel move, like Dicyclomine, having dual activities. The Aa.Cr also showed relaxant result on Phenylephrine and High Potassium -prompted contractions in endothelium intact aorta. The fractionation revealed segregations of contractile & relaxant effects in relevant aqueous & organic portions. The Intravenous administration of Aa.Cr to ketamine-diazepam anaesthetized normo-tensive albino rats resulted in decreased MABP, SBP & DBP. The Aa.Cr applied negative (-) inotropic & chronotropic action on paired atria. The Aa.Cr also exhibited anti-diarrheal action in mice against castor oil prompted diarrhea and also mitigated distance covered by charcoal meal in gastrointestinal tract in a manner comparable with loperamide. CONCLUSION: These results revealed presence of CCB and selective muscarinic agonist activity in Aa.Cr, hence validating folkloric practice of Anagallis arvensis Linn. in diarrhea, constipation, asthma & hypertension.


Assuntos
Anagallis , Broncodilatadores/farmacologia , Folclore , Fármacos Gastrointestinais/farmacologia , Medicina Tradicional , Músculo Liso/efeitos dos fármacos , Parassimpatolíticos/farmacologia , Extratos Vegetais/farmacologia , Vasodilatadores/farmacologia , Anagallis/química , Animais , Broncodilatadores/isolamento & purificação , Etnofarmacologia , Feminino , Fármacos Gastrointestinais/isolamento & purificação , Técnicas In Vitro , Masculino , Camundongos Endogâmicos BALB C , Agonistas Muscarínicos/farmacologia , Relaxamento Muscular/efeitos dos fármacos , Músculo Liso Vascular/efeitos dos fármacos , Paquistão , Parassimpatolíticos/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Coelhos , Ratos Sprague-Dawley , Vasodilatação/efeitos dos fármacos , Vasodilatadores/isolamento & purificação
2.
Pharm Biol ; 57(1): 477-484, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31438784

RESUMO

Context: In China, the herb Sophora tonkinensis Gagnep. (Fabaceae, ST) (Committee of National Pharmacopeia. 2015) exhibits anti-inflammatory, antitumor, and antiviral effects. However, to date, there have been few studies on its gastrointestinal effect. Objective: The gastrointestinal effect of the methanol extract of ST rhizome (STR) was evaluated. Materials and methods: Study was conducted from February to December 2018. In vivo, antidiarrheal activity of STR (125, 250 and 500 mg/kg; orally) in castor oil-induced diarrheal mice was studied. In vitro, the effects of STR (0.01-10 mg/mL) on the isolated tissue preparations of rabbit jejunum were also investigated, the rabbit jejunum stripes were pre-contracted with Ach (10-5 M), K+ (60 mM) and tested in the presence of STR, the possible spasmolytic effect was analyzed in the pretreatment of the jejunum preparations with STR or verapamil in Ca2+-free high-K+ (60 mM) solution containing EDTA. Results: STR (125, 250 and 500 mg/kg) exhibited antidiarrheal activity. STR (0.01-10 mg/mL) completely relaxed spontaneously contracting, Ach (10-5 M) and high K+ (60 mM) induced contracted jejunum with an EC50 value of 0.66 (0.49-0.96), 0.39 (0.28-0.44) and 0.17 (0.10-0.21), similar to verapamil. Concentration-response curves of CaCl2 could be significantly moved to the right and down in the presence of STR (0.3, 1 mg/mL). Discussion and conclusions: Results suggest the presence of antidiarrheal activity and spasmolytic effects of STR, possibly mediated through Ca2+ channel blocking activity, providing the pharmacological basis for its traditional uses in gastrointestinal disorders.


Assuntos
Antidiarreicos/uso terapêutico , Asteraceae/química , Diarreia/tratamento farmacológico , Jejuno/efeitos dos fármacos , Contração Muscular/efeitos dos fármacos , Parassimpatolíticos/farmacologia , Extratos Vegetais/uso terapêutico , Animais , Antidiarreicos/isolamento & purificação , Antidiarreicos/toxicidade , Óleo de Rícino , Relação Dose-Resposta a Droga , Motilidade Gastrointestinal/efeitos dos fármacos , Técnicas In Vitro , Dose Letal Mediana , Masculino , Metanol , Camundongos , Músculo Liso/efeitos dos fármacos , Parassimpatolíticos/isolamento & purificação , Parassimpatolíticos/toxicidade , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Coelhos
3.
Nat Prod Res ; 33(17): 2571-2573, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29614872

RESUMO

Lippia thymoides ('alecrim-do-mato' or 'alecrim-do-campo') is used in Brazilian folk medicine to treat various illnesses, including diarrhea. This work aimed to evaluate in vitro spasmolytic and in vivo antidiarrheal activities of the L. thymoides essential oil (OOS) and to correlate with the traditional use of this plant. In isolated guinea-pig ileum, OOS presented a concentration-dependent spasmolytic activity in preparations pre-contracted with KCl 40 mM [EC50 = 16.89 (11.56-24.66) µg/mL], and antagonized phasic contractions induced by 1 µM carbachol [IC50 = 42.71 (37.35-48.83) µg/mL] or histamine [IC50 = 32.38 (27.44-38.20) µg/mL]. In mice, OOS at 400 mg/kg reduced intestinal transit, at 200 and 400 mg/kg reduced total stool mass and at 400 mg/kg reduced intestinal fluid accumulation. It was shown that the antidiarrheal effect of OOS is related to the inhibition of smooth muscle contraction and may be due to the presence of major compound ß-caryophyllene in this essential oil.


Assuntos
Antidiarreicos/isolamento & purificação , Lippia/química , Óleos Voláteis/farmacologia , Parassimpatolíticos/isolamento & purificação , Animais , Antidiarreicos/farmacologia , Brasil , Diarreia/tratamento farmacológico , Cobaias , Íleo/efeitos dos fármacos , Medicina Tradicional , Camundongos , Contração Muscular/efeitos dos fármacos , Parassimpatolíticos/farmacologia , Extratos Vegetais/farmacologia
4.
J Ethnopharmacol ; 220: 16-25, 2018 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-29609011

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Lippia origanoides H.B.K. is an aromatic species used in folk medicine to treat respiratory diseases, including asthma. AIM OF THE STUDY: The aim of this work was to evaluate the relaxing potential and mechanism of action of the L. origanoides (LOO) essential oil in isolated guinea-pig trachea. MATERIALS AND METHODS: Leaves from L. origanoides were collected at experimental fields under organic cultivation, at the Forest Garden of Universidade Estadual de Feira de Santana. Essential oil was extracted by hydrodistillation, analyzed by GC/FID and GC/MS and the volatile constituents were identified. Spasmolytic activity and relaxant mechanism of LOO were assayed in isolated guinea-pig trachea contracted with histamine, carbachol or hyperpolarizing KCl. RESULTS: Chemical analysis revealed the presence of carvacrol (53.89%) as major constituent. LOO relaxed isolated guinea-pig trachea pre-contracted with KCl 60 mM [EC50 = 30.02 µg/mL], histamine 1 µM [EC50 = 9.28 µg/mL] or carbachol 1 µM [EC50 = 51.80 µg/mL]. The pre-incubation of glibenclamide, CsCl, propranolol, indomethacin, hexamethonium, aminophylline or L-NAME in histamine-induced contractions did not alter significantly the relaxant effect of LOO. However, the presence of 4-aminopyridine, tetraethylammonium or methylene blue reduced LOO effect, while the presence of dexamethasone or atropine potentialized the LOO relaxant effect. LOO pre-incubation inhibited carbachol-evoked contractions, with this effect potentialized in the presence of sodium nitroprusside and blocked in the presence of ODQ. CONCLUSIONS: The relaxant mechanism of LOO on the tracheal smooth muscle possibly involves stimulating of soluble guanylyl cyclase with consequent activation of the voltage-gated and Ca2+-activated K+ channels.


Assuntos
Lippia/química , Músculo Liso/efeitos dos fármacos , Óleos Voláteis/farmacologia , Traqueia/efeitos dos fármacos , Animais , Feminino , Cromatografia Gasosa-Espectrometria de Massas , Cobaias , Masculino , Contração Muscular/efeitos dos fármacos , Relaxamento Muscular/efeitos dos fármacos , Músculo Liso/metabolismo , Óleos Voláteis/isolamento & purificação , Parassimpatolíticos/isolamento & purificação , Parassimpatolíticos/farmacologia , Canais de Potássio Cálcio-Ativados/efeitos dos fármacos , Canais de Potássio Cálcio-Ativados/metabolismo , Canais de Potássio de Abertura Dependente da Tensão da Membrana/efeitos dos fármacos , Canais de Potássio de Abertura Dependente da Tensão da Membrana/metabolismo , Guanilil Ciclase Solúvel/metabolismo , Traqueia/metabolismo
5.
J Ethnopharmacol ; 210: 107-117, 2018 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-28811222

RESUMO

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.


Assuntos
Medicina Tradicional/métodos , Myrtaceae/química , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Animais , Antitussígenos/administração & dosagem , Antitussígenos/isolamento & purificação , Antitussígenos/farmacologia , Broncodilatadores/administração & dosagem , Broncodilatadores/isolamento & purificação , Broncodilatadores/farmacologia , Cálcio/metabolismo , Cardiotônicos/administração & dosagem , Cardiotônicos/isolamento & purificação , Cardiotônicos/farmacologia , Tosse/tratamento farmacológico , Modelos Animais de Doenças , Feminino , Concentração Inibidora 50 , Masculino , Camundongos , Óleos Voláteis/administração & dosagem , Óleos Voláteis/isolamento & purificação , Parassimpatolíticos/administração & dosagem , Parassimpatolíticos/isolamento & purificação , Parassimpatolíticos/farmacologia , Extratos Vegetais/administração & dosagem , Folhas de Planta , Ratos , Ratos Sprague-Dawley , América do Sul
6.
J Pharm Pharmacol ; 69(9): 1208-1218, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28543032

RESUMO

OBJECTIVES: As there are no previous studies of the European wild-garlic (Allium ursinum) effects on the gastrointestinal system, despite its traditional applications in gastrointestinal disorders' treatment and regular use in the human diet, we have quantified and compared spasmolytic, antimicrobial and antioxidant activities of its different leaf extracts. METHODS: Wild-garlic extracts were tested for spasmolytic activity on isolated rat ileum, antimicrobial activity on selected Gram-positive and Gram-negative bacteria and fungi by microdilution method and antioxidant capacity by DPPH radical-scavenging assay. KEY FINDINGS: Wild-garlic extracts were found to decrease ileal basal tone. As the relaxation of K+ -induced contractions was similar to one caused by papaverin, the observed spasmolytic effect was most likely mediated through Ca2+ -channel inhibition. Ethanolic extract (with the highest phenolic and high alk(en)yl cysteine sulphoxides' levels) produced the strongest spasmolytic activity. In case of acetylcholine-induced contractions, only hydromethanolic extract showed no statistical difference in comparison with positive control. All samples exhibited certain antioxidant potential and strong antimicrobial activity against tested enteropathogenic strains (Salmonella enteritidis was the most sensitive, followed by Escherichia coli, Proteus mirabilis and Enterococcus faecalis). CONCLUSION: Besides other already established health-promoting effects, wild garlic could be useful in treatment of mild gastrointestinal disturbances.


Assuntos
Allium/química , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Extratos Vegetais/farmacologia , Animais , Antibacterianos/isolamento & purificação , Antifúngicos/isolamento & purificação , Antifúngicos/farmacologia , Antioxidantes/isolamento & purificação , Sequestradores de Radicais Livres/isolamento & purificação , Sequestradores de Radicais Livres/farmacologia , Gastroenteropatias/tratamento farmacológico , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Masculino , Parassimpatolíticos/isolamento & purificação , Parassimpatolíticos/farmacologia , Ratos , Ratos Wistar
7.
J Ethnopharmacol ; 192: 264-272, 2016 Nov 04.
Artigo em Inglês | MEDLINE | ID: mdl-27451258

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Morinda citrifolia L. (Noni) is a medicinal plant used in Polynesia for many properties such as anti-inflammatory, anti-diabetic and antineoplastic effects. Recent studies showed that noni juice have anti-oxidant and acute anti-inflammatory activities likely due to polyphenols, iridoids and vitamin C content. The present study was undertaken to evaluate chronic anti-inflammatory and spasmolytic effects of noni juice. MATERIALS AND METHODS: Therefore, we evaluated the effect of oral or intraperitoneal administrations of noni juice in vivo on the lung inflammation in ovalbumin (OVA) sensitized Brown Norway rat (with prednisolone 10mg/kg intraperitoneously as reference compound) and the ex vivo effect of noni juice on BaCl2 (calcium signal) or methacholine (cholinergic signal) induced spasms in jejunum segments. RESULTS: We found that noni juice (intraperitoneously 2.17mL/kg and orally 4.55mL/kg) reduced the inflammation in OVA-sensitized Brown Norway rat with regard to the decreased number of inflammatory cells in lung (macrophages minus 20-26%, lymphocytes minus 58-34%, eosinophils minus 53-30%, neutrophils minus 70-28% respectively). Noni juice demonstrated a dose-dependent NO scavenging effect up to 8.1nmol of nitrites for 50µL of noni juice. In addition noni juice inhibited (up to 90%) calcium and cholinergic induced spasms on the jejunum segments model with a rightward shift of the concentration response curve. CONCLUSION: We describe for the first time that noni juice demonstrate (1) a chronic anti-inflammatory activity on sensitized lungs along with (2) a spasmolytic effect integrating a calcium channel blocker activity component.


Assuntos
Anti-Inflamatórios/farmacologia , Jejuno/efeitos dos fármacos , Morinda/química , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Parassimpatolíticos/farmacologia , Extratos Vegetais/farmacologia , Pneumonia/prevenção & controle , Administração Oral , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/farmacologia , Bloqueadores dos Canais de Cálcio/farmacologia , Sinalização do Cálcio/efeitos dos fármacos , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Frutas/química , Técnicas In Vitro , Injeções Intraperitoneais , Jejuno/metabolismo , Pulmão/efeitos dos fármacos , Pulmão/metabolismo , Músculo Liso/metabolismo , Óxido Nítrico/metabolismo , Nitritos/metabolismo , Ovalbumina , Parassimpatolíticos/administração & dosagem , Parassimpatolíticos/química , Parassimpatolíticos/isolamento & purificação , Fitoterapia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Pneumonia/induzido quimicamente , Pneumonia/metabolismo , Prednisolona/farmacologia , Ratos Endogâmicos BN
8.
Mini Rev Med Chem ; 14(9): 725-33, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25138085

RESUMO

Highly methoxylated flavones, which have known potential as cancer chemopreventive agents, accumulate on the leaf surfaces of some plant species and their physiological role is to protect the plant against harmful UV radiation. Xanthomicrol is one of the methoxylated flavones currently attracting most attention from researchers worldwide because of its promising pharmacological activities, including anti-spasmodic, anti-platelet and anti-cancer effects, among others. This review covers the chemistry and biological origin, distribution and pharmacological activity of xanthomicrol. Knowledge of the botanical distribution of this compound will not only encourage the use of plant sources for pharmacological purposes, but will also serve as a reference in the search for this valuable flavonoid in another genus or family. New approaches to xanthomicrol production are also described, including biotechnological attempts to develop xanthomicrol-producing plant cell factories.


Assuntos
Fabaceae/química , Flavonas/química , Flavonoides/química , Lamiaceae/química , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/metabolismo , Anti-Infecciosos/farmacologia , Anticarcinógenos/química , Anticarcinógenos/isolamento & purificação , Anticarcinógenos/metabolismo , Anticarcinógenos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Flavonas/biossíntese , Flavonas/isolamento & purificação , Flavonas/farmacologia , Flavonoides/biossíntese , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Humanos , Parassimpatolíticos/química , Parassimpatolíticos/isolamento & purificação , Parassimpatolíticos/metabolismo , Parassimpatolíticos/farmacologia , Extratos Vegetais/química , Inibidores da Agregação Plaquetária/química , Inibidores da Agregação Plaquetária/isolamento & purificação , Inibidores da Agregação Plaquetária/metabolismo , Inibidores da Agregação Plaquetária/farmacologia
9.
BMC Complement Altern Med ; 13: 96, 2013 May 06.
Artigo em Inglês | MEDLINE | ID: mdl-23642022

RESUMO

BACKGROUND: The current work is an attempt to know about additional chemical profile of Artemisia macrocephala. Antioxidant activity is performed as the plant is reported to contain flavonoids, which have antioxidant activity in general. Relaxant activity of fractions of crude methanol extract is performed to know in which fraction(s) the relaxant constituents concentrate as we have already reported that its crude methanol has relaxant activity. Antispasmodic activity of essential oil is also performed as the plant is rich with essential oil. METHODS: Phytochemical profile of the plant is performed. Free radical scavenging activity was performed using 2, 2-diphenyl-1-picrylhydrazyl (DPPH). Relaxation activity tests of fractions and essential oil of Artemisia macrocephala were performed on sections of rabbits' jejunum. Calcium chloride curves were constructed to investigate the mode of action of plant extracts and its essential oil. RESULTS: We detected carbohydrates, flavonoids and saponins in A. macrocephala. At concentration 0.005 mg/ml, free radical scavenging activity of ethyl acetate fraction was 121.5 ± 2.02% of ascorbic acid.n- hexane fraction relaxed spontaneous activity with EC50 0.74 ± 0.04 mg/ml. Essential oil relaxed spontaneous activity with EC50 0.8 ± 0.034 mg/ml. Chloroform and ethylacetate fractions relaxed both spontaneous and KCl-induced contractions suggesting its possible mode through calcium channels. Constructing calcium chloride curves, the test fractions showed a right shift in the EC50. Essential oil at concentration 0.1 mg/ml produced right shift with EC50 (log [Ca++]M) -2.08 ± 0.08 vs. control with EC50 -2.47 ± 0.07. The curve resembled the curves of verapamil, which caused a right shift at 0.1 µM, with EC50 -1.7 ±0.07 vs. control EC50 (log [Ca++]M) -2.45 ± 0.06. CONCLUSIONS: Crude methanol and its fractions (ethyl acetate, chloroform and butanol) are rich sources of antioxidant constituents. The relaxing constituents following calcium channel blocking mechanisms are more concentrated in n-hexane, chloroform and ethyl acetate fractions that warrant isolation.


Assuntos
Antioxidantes/farmacologia , Artemisia/química , Óleos Voláteis/farmacologia , Parassimpatolíticos/farmacologia , Extratos Vegetais/farmacologia , Animais , Antioxidantes/isolamento & purificação , Humanos , Relaxamento Muscular/efeitos dos fármacos , Óleos Voláteis/isolamento & purificação , Parassimpatolíticos/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Coelhos
10.
J Pharm Biomed Anal ; 75: 220-9, 2013 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-23277154

RESUMO

Butterbur (Petasites) is an ancient plant which has been used for medical and edible purposes with its spasmolytic agents. However, toxic alkaloid content of the plant limits its direct usage. The paper covers the pyrrolizidine alkaloids (PAs) and butterbur themes in detail in order to display the outline of alkaloid-free plant extract production for medical and edible purposes. The toxic PAs and medicinal constituents of the plant are described with emphasis on analytics, physiological effects and published patent data on alkaloid free extract production. The analytics is based on several commonly used analytical methods including liquid chromatography-mass spectrometry, gas chromatography-mass spectrometry and enzyme linked immunoassay analysis of PAs and N-oxides based on published literature data of butterbur. The analyses of major medicinal constituents of butterbur are given and the physiological effects of these compounds have been discussed to attract attention to the importance of alkaloid-free extract production. The concentration distributions of the medicinal constituents and toxic PAs in different parts of the plant and the outcomes of the published patent data provide comprehensive information for proper plant raw-material selection and production of alkaloid-free butterbur extracts. The review is intended to guide researchers interested in medical plant extracts by providing comprehensive data on the medical plant butterbur and its chemical constituents.


Assuntos
Carcinógenos/análise , Suplementos Nutricionais , Petasites/química , Extratos Vegetais/química , Alcaloides de Pirrolizidina/análise , Analgésicos não Narcóticos/análise , Analgésicos não Narcóticos/química , Analgésicos não Narcóticos/isolamento & purificação , Analgésicos não Narcóticos/uso terapêutico , Animais , Anti-Inflamatórios não Esteroides/análise , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Anti-Inflamatórios não Esteroides/uso terapêutico , Carcinógenos/metabolismo , Carcinógenos/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Etnofarmacologia , Humanos , Parassimpatolíticos/análise , Parassimpatolíticos/química , Parassimpatolíticos/isolamento & purificação , Parassimpatolíticos/uso terapêutico , Petasites/crescimento & desenvolvimento , Petasites/metabolismo , Fitoterapia , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Folhas de Planta/crescimento & desenvolvimento , Folhas de Planta/metabolismo , Alcaloides de Pirrolizidina/metabolismo , Alcaloides de Pirrolizidina/toxicidade , Rizoma/química , Rizoma/crescimento & desenvolvimento , Rizoma/metabolismo , Sesquiterpenos/análise , Sesquiterpenos/metabolismo , Sesquiterpenos/uso terapêutico , Estereoisomerismo
11.
J Asian Nat Prod Res ; 12(12): 1069-80, 2010 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-21128148

RESUMO

The genus Symplocos has been reviewed for its chemical constituents and biological activities including traditional importance of some common species. The plants of this genus contain terpenoids, flavonoids, lignans, phenols, steroids, alkaloids, and iridoids. Terpenoids are the major constituents within the genus Symplocos and most of them exhibit antiproliferative effects. Some phenolic glycoside derivatives showed inhibitory activity against snake-venom phosphodiesterase I and human nucleotide pyrophosphatase phosphodiesterase I. The members of genus Symplocos are well known for their traditional uses in the treatment of various diseases like leprosy, gynecological disorders, ulcers, leucorrhea, menorrhagia, malaria, and tumefaction. The aim of the present paper is to review the comprehensive knowledge of the plants of this genus including the traditional uses, chemistry, and pharmacology.


Assuntos
Magnoliopsida/química , Plantas Medicinais/química , Alcaloides/química , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Fármacos Anti-HIV/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antidiarreicos/química , Antidiarreicos/isolamento & purificação , Antidiarreicos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Fármacos do Sistema Nervoso Central/química , Fármacos do Sistema Nervoso Central/isolamento & purificação , Fármacos do Sistema Nervoso Central/farmacologia , Quimotripsina/antagonistas & inibidores , Feminino , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Glicosídeos/química , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Hemolíticos/química , Hemolíticos/isolamento & purificação , Hemolíticos/farmacologia , Humanos , Iridoides/química , Iridoides/isolamento & purificação , Iridoides/farmacologia , Lignanas/química , Lignanas/isolamento & purificação , Lignanas/farmacologia , Estrutura Molecular , Parassimpatolíticos/química , Parassimpatolíticos/isolamento & purificação , Parassimpatolíticos/farmacologia , Inibidores de Fosfodiesterase/química , Inibidores de Fosfodiesterase/isolamento & purificação , Inibidores de Fosfodiesterase/farmacologia , Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidores
12.
13.
J Ethnopharmacol ; 113(1): 125-31, 2007 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-17582715

RESUMO

Bioassay guided fractionation of an antimycobacterial extract of Arracacia tolucensis var. multifida (Umbelliferae) led to the isolation of isoimperatorin (1), osthol (2), suberosin (3), 8-methoxypsoralen (8-MOP) (4), herniarin (5), scoparone (6), umbelliferone (7), dihydroxypeucedanin (8), 5-methoxypsoralen (5-MOP) (9), isoscopoletin (10) and scopoletin (11). The isolates were tested against Mycobacterium tuberculosis and only 1-4 showed significant activity with MIC values of 64, 32, 16 and 128 microg/mL, respectively. The essential oil showed moderate in vitro antibacterial activity against representative Gram-positive and Gram-negative bacteria. The volatile oil of Arracacia tolucensis var. multifida was analyzed by GC-MS and found to be composed mainly by 2 and 3. The essential oil (IC(50)=116.4+/-23.2 microg/mL) and the extract (IC(50)=1153.1+/-53.2 microg/mL) of the plant provoked concentration dependent inhibition of the tone and amplitude of the guinea-pig ileum spontaneous contractions; the latter activity was related with the high coumarin content of this species. A suitable (novel and rapid) HPLC method to quantify the major active coumarins of the plant was developed. The method provides also a reproducible fingerprint useful for identity tests of this plant.


Assuntos
Antibacterianos/administração & dosagem , Apiaceae/química , Óleos Voláteis/administração & dosagem , Parassimpatolíticos/administração & dosagem , Extratos Vegetais/administração & dosagem , Animais , Antibacterianos/química , Antibacterianos/isolamento & purificação , Bioensaio , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia Gasosa-Espectrometria de Massas , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Cobaias , Concentração Inibidora 50 , Medicina Tradicional , México , Testes de Sensibilidade Microbiana , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Parassimpatolíticos/química , Parassimpatolíticos/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Controle de Qualidade
14.
J Ethnopharmacol ; 71(1-2): 187-92, 2000 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-10904162

RESUMO

Satureja hortensis L. (Lamiaceae) is an annual herb that is used in the traditional medicine of Iran for treating stomach and intestinal disorders. The antispasmodic activity of S. hortensis essential oil (SHEO) was assessed on contractions of isolated ileum, induced by KCl and acetylcholine, and compared with the effect of atropine and dicyclomine. SHEO inhibited the response to 80 mM KCl in a concentration-dependent manner (pD(2)=1.55+/-0.09 microg/ml; this is negative log concentration of SHEO causing 50% of maximum inhibition) and attenuating the maximum inducible response of acetylcholine concentration-response curve. Effect of SHEO on KCl was similar to that of dicyclomine. Dicyclomine (3.46 and 34.6 ng/ml) also reduced the response to acetylcholine on rat isolated ileum without altering the maximum response and shifted the acetylcholine concentration-response curve to the right by 16-fold at 34.6 ng/ml (100 nM) bath concentration, while atropine only inhibited the response to acetylcholine. This study shows that SHEO is a relaxant of rat isolated ileum. In addition to antispasmodic activity in vitro, essential oil of this plant at a dose of 0.1 ml/100 g inhibited castor oil induced diarrhoea in mice. As the inhibition of contractile overactivity of the ileum is the base of the treatment of some gastrointestinal disorders such as colic, SHEO may have clinical benefits for treatment of these conditions.


Assuntos
Antidiarreicos/farmacologia , Lamiaceae/química , Óleos Voláteis/farmacologia , Parassimpatolíticos/farmacologia , Plantas Medicinais/química , Animais , Antidiarreicos/isolamento & purificação , Óleo de Rícino , Catárticos , Diarreia/induzido quimicamente , Diarreia/prevenção & controle , Feminino , Cromatografia Gasosa-Espectrometria de Massas , Íleo/efeitos dos fármacos , Técnicas In Vitro , Irã (Geográfico) , Medicina Tradicional do Leste Asiático , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Óleos Voláteis/isolamento & purificação , Parassimpatolíticos/isolamento & purificação , Fitoterapia , Ratos , Ratos Wistar
15.
Phytochemistry ; 41(1): 217-23, 1996 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-8588867

RESUMO

The steam volatile components from the hexane extract of dried flower buds of Egletes viscosa were identified by gas chromatography-mass spectrometry as trans-carvyl acetate, cis-carvyl acetate, sabinyl acetate, verbenyl acetate, cyclopentaethylidene, geranyl acetate and 5-methylfuranone, and trans-pinocarvyl acetate (major component). From the non-volatile residue, centipedic acid and a novel clerodane diterpene, 12-acetoxy-hawtriwaic acid lactone, were isolated. From the ethanol extract, ternatin (4',5-dihidroxy-3,3',7,8-tetramethoxyflavone), was isolated. Ternatin showed anti-inflammatory, hepatoprotection and gastroprotection properties, and, according to the NCI protocols, it showed moderate activity against HIV. The diterpenes showed antispasmodic activity. Structure determination of these secondary metabolites was accomplished by spectrometric methods, including 2D NMR, chemical interconversion and X-ray crystallographic analysis.


Assuntos
Antivirais/química , Flavonoides/química , HIV/efeitos dos fármacos , Plantas Medicinais , Terpenos/química , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Anti-Inflamatórios não Esteroides/farmacologia , Antivirais/isolamento & purificação , Antivirais/farmacologia , Brasil , Cristalografia por Raios X , Diterpenos/química , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Humanos , Espectroscopia de Ressonância Magnética , Medicina Tradicional , Modelos Moleculares , Estrutura Molecular , Parassimpatolíticos/química , Parassimpatolíticos/isolamento & purificação , Parassimpatolíticos/farmacologia , Extratos Vegetais , Relação Estrutura-Atividade , Terpenos/isolamento & purificação , Terpenos/farmacologia
16.
Arch Med Res ; 25(1): 17-21, 1994.
Artigo em Inglês | MEDLINE | ID: mdl-8019109

RESUMO

The antidiarrheal properties of water and methanolic extracts of Psidium guajava leaves have been demonstrated with anteriority and their spasmolytic effect was attributed to quercetin, a flavonoid contained in this plant. The present paper reports the intestinal smooth muscle relaxation produced by quercetin on isolated guinea pig ileum previously contracted by a depolarizing KCl solution. Quercetin also inhibited intestinal contraction induced by different concentrations of calcium, shifting the contraction curve to the right showing a clear calcium-antagonistic effect. Quercetin effect on ileal and aortic smooth muscles are compared, the ileum being more sensitive to this flavonoid. The calcium-antagonist property of quercetin is discussed and also its contribution to explain the spasmolytic effect of this popular herbal remedy.


Assuntos
Aorta Torácica/efeitos dos fármacos , Cálcio/antagonistas & inibidores , Íleo/efeitos dos fármacos , Parassimpatolíticos/farmacologia , Plantas Medicinais/química , Quercetina/farmacologia , Animais , ATPase de Ca(2+) e Mg(2+)/antagonistas & inibidores , Cálcio/fisiologia , ATPases Transportadoras de Cálcio/antagonistas & inibidores , Feminino , Cobaias , Masculino , Metanol , Modelos Biológicos , Relaxamento Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Músculo Liso Vascular/efeitos dos fármacos , Parassimpatolíticos/isolamento & purificação , Extratos Vegetais/química , Quercetina/isolamento & purificação , ATPase Trocadora de Sódio-Potássio/antagonistas & inibidores , Água
17.
Planta Med ; 59(3): 203-6, 1993 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-8316587

RESUMO

The sesquiterpene capsidiol, isolated from elicited, cultured cells of Nicotiana silvestris, inhibits contraction induced by the agonists, histamine, acetylcholine, bradykinin, and barium chloride in the isolated guinea-pig ileum. In addition, capsidiol inhibits contraction induced by histamine and carbachol in the isolated guinea-pig trachea in a nonspecific and noncompetitive but concentration-dependent manner. Capsidiol also inhibits prostaglandin synthesis (cyclooxygenase) in vitro in a concentration dependent manner.


Assuntos
Músculo Liso/efeitos dos fármacos , Nicotiana/química , Parassimpatolíticos/farmacologia , Plantas Tóxicas , Sesquiterpenos/farmacologia , Animais , Células Cultivadas , Cobaias , Íleo/efeitos dos fármacos , Relaxamento Muscular/efeitos dos fármacos , Parassimpatolíticos/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Prostaglandinas/biossíntese , Sesquiterpenos/isolamento & purificação , Terpenos , Nicotiana/citologia , Traqueia/efeitos dos fármacos , Fitoalexinas
19.
Regul Pept ; 3(3-4): 207-19, 1982 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-6896240

RESUMO

A novel polypeptide, named Pancreatic Spasmolytic Polypeptide (PSP), was discovered in a side-fraction from the purification of porcine insulin. PSP was prepared by two different purification methods based on combinations of precipitations, anion-exchange and cation-exchange chromatography. The highest yield obtained, 52 mg PSP/kg pancreas, indicates that the content of PSP in porcine pancreas is about half the content of insulin. Both preparations appeared to be very pure as judged by basic disc electrophoresis, isoelectric focusing, analytical gel filtration and radioimmunoassays for various polypeptides known to be present in pancreas. The PSP molecule contains 106 amino acids (MW about 11 700). PSP is an acidic (pI 4.4), non-glycosylated protein without free N-terminal amino groups, and with high contents of proline and cystine. The high content of S-S bridges (7 per molecule), an unexpected low apparent MW determined by gel filtration, and a remarkable resistance towards treatment with trypsin and chymotrypsin, point to a compact structure of the PSP molecule.


Assuntos
Mucinas , Proteínas Musculares , Neuropeptídeos , Pâncreas/análise , Parassimpatolíticos/isolamento & purificação , Peptídeos/isolamento & purificação , Aminoácidos/análise , Animais , Cromatografia por Troca Iônica , Eletroforese Descontínua , Peptídeos e Proteínas de Sinalização Intercelular , Focalização Isoelétrica , Peso Molecular , Parassimpatolíticos/metabolismo , Peptídeos/metabolismo , Suínos , Fator Trefoil-2 , Fator Trefoil-3
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