ABSTRACT
Background: Colombia has a high diversity of medicinal plants, including Tachuelo (Zanthoxylum rhoifolium), a tree belonging to the family Rutaceae, which has been attributed an analgesic use by communities of the Colombian southwest. Nevertheless, this species has been scarce studied in Colombia. The studies have been limited to the isolation of compounds with antifungal and insecticide activity, using the leaves, branches, and bark of the plant in aqueous, and organic extracts. Neither pharmacological tests have been carried out, nor the analgesic and neuromotor activity have been tested from preparations with this plant's fruits. Objectives: To evaluate the analgesic and neuromotor effect of the aqueous and hexane extract of the fruits of Z. rhoifolium.Methods: As there were no preliminary reports of this study, the first observation was made through Irwin's test. The formalin and the rotarod test were performed to determine the analgesic and motor coordination effects, respectively. Results: All the evaluated treatments demonstrated to generate analgesia, anesthesia, passivity, reduction in the alarm reaction, and have antinociceptive activity in the formalin test; while only the high dose of the nonpolar extract generated a deficit in the motor performance of the rodents in the rotarod test. Conclusions: the antinociceptive effect of the aqueous and hexane extracts of this species' fruits was demonstrated. The hexane extract generated a neuromotor effect, which validates the ethnobotanical reports on Z. rhoifolium fruits.
Antecedentes: Colombia tiene una alta diversidad de plantas medicinales, incluyendo al Ta chuelo (Zanthoxylum rhoifolium), un árbol de la familia Rutaceae al que se le ha atribuido un potencial analgésico debido al uso por parte de las comunidades del Suroccidente Colombiano. Sin embargo, esta especie ha sido poco estudiada en Colombia, limitándose al aislamiento de compuestos con actividad antifúngica e insecticida, empleando las hojas, ramas y corteza de la planta en extractos acuosos y orgánicos; sin embargo, no se han realizado ensayos farmacológicos ni se han probado la actividad analgésica y neuromotora a partir de preparaciones con los frutos de esta planta. Objetivos: Evaluar el efecto analgésico y neuromotor del extracto acuoso y en hexano de los frutos de Z. rhoifolium. Métodos: Al no haber reportes preliminares de este estudio, se realizó la primera observación mediante el test de Irwin. Para determinar el efecto analgésico y neuromotor se realizó el test de formalina y el test de rotarod, respectivamente. Resultados: Todos los tratamientos evaluados demostraron generar analgesia, anestesia, pasividad, reducción en la reacción de alarma, tener actividad antinociceptiva en el test de formalina, mientras que solo la dosis alta del extracto apolar generó un déficit en el rendimiento motor de los roedores en el test de rotarod. Conclusiones: Se demostró el efecto antinociceptivo del extracto acuoso y en hexano de los frutos de esta especie y el efecto neuromotor generado por el extracto en hexano, validando los reportes etnobotánicos sobre los frutos de Z. rhoifolium.
Subject(s)
Humans , Plant Extracts , Colombia , Analgesics , MiceABSTRACT
The study evaluated the vasorelaxant effect induced by the ethanolic extract of the leaves of Zanthoxylum rhoifolium Lam (EEtOH-Zr/leaves). Wistar rats were treated with the leaf extract containing a single dose of 2,000 mg / kg, v.o. After 14 days, the animals were anesthetized for blood collection and subsequent analysis of the biochemical parameters; they were then euthanized (sodium pentobarbital-100 mg/kg, i.p.) for the removal and morphological analysis of the heart, lung, liver and kidney. The vasorelaxation activity the and vascular reactivity of EEtOH-Zr/leaves were evaluated on artery mesenteric rings isolated from rats. The extract showed no signs of toxicity and no significant difference in the values of the biochemical parameters between the control group and the group of treated animals. In the evaluation of pharmacological activity in the smooth muscle, the EEtOH-Zr/leaves caused vasorelaxant effect on the tonic contraction induced by phenylephrine in mesenteric artery preparations in the presence (pD2=2.17±0.05 µg/mL; Emax=99.8±5.2%) and absence (pD2=2.14±0.05 µg/mL; Emax=95.3±6.4%) of the vascular endothelium. Oral administration of EEtOH-Zr/leaves reduced the contraction induced by the cumulative addition of PHE. It is concluded that the EEtOH-Zr/leaves promote vasorelaxation and reduce vascular reactivity of adrenergic alpha-1 agonist in the mesenteric artery. The results did not show toxic effects of the extract.
Subject(s)
Animals , Male , Rats , Plant Extracts/adverse effects , /analysis , Zanthoxylum/toxicity , Mesenteric Arteries/drug effects , Blood Vessels/drug effectsABSTRACT
The purpose of this study was to test for antioxidantand allelopathic activities in stem bark of Zanthoxylum rhoifolium Lam., Rutaceae, with the eventual aim of discovering biologically active substances. The plant material was subjected to ethanolic extraction and this extract was partitioned, yielding hexane, chloroform, ethyl acetate and hydroalcoholic fractions. Antioxidant activity was estimated by the reduction of phosphomolybdenum complex, of DPPH. and of thiobarbituric acid-reactive substances (TBARS). To detect allelopathy, the samples were tested, at four concentrations, on the germination and development of the radicle and hypocotyl of L. sativa seeds. The samples showed significant antioxidant activity against the reduction of the phosphomolybdenum complex, as compared to rutin, and reduction of TBARS, ascompared to BHT, as well as allelopathic activity, since they stimulated growth and seed germination. The chloroform and ethyl acetate fractions showed the best antioxidant potentials, with 204.17% and 127.11% compared to rutin, in the reduction of phosphomolybdenum complex, as did the crude ethanolic extract and hexane fraction, with 64.2% and 60.9% compared to BHT, in the TBARS method. In the allelopathic assay, the chloroform fraction stood out as the only sample that stimulated the growth of both the radicle and hypocotyl at most concentrations, ranging from 41 to 144%, while the ethyl acetate fraction achieved the greatest stimulus in this bioassay, increasing the growth of the hypocotyl by 274%. This is the first study that demonstrates the antioxidant and allelopathic activities of the species Z. rhoifolium...
Este trabalho teve como objetivo o estudo das atividades antioxidante e alelopática das cascas do caule de Zanthoxylum rhoifolium Lam., Rutaceae, de modo a conduzir à descoberta de substâncias biologicamente ativas. O material vegetal foi submetido à extração etanólica e este extrato foi fracionado obtendo as frações (hexano, clorofórmio, acetato de etila e hidroalcoólica). Para a avaliação da atividade antioxidante, empregaram-se os métodos de redução do complexo fosfomolibdênio, de redução do radical DPPH e das substâncias reativas ao acido tiobarbitúrico (TBARS). Quanto à alelopatia, as amostras foram testadas em quatro concentrações sobre a germinação e o desenvolvimento de radícula e hipocótilo das sementes de Lactuca sativa. As amostras evidenciaram atividade antioxidante significativa frente ao método de redução do complexo fosfomolibdênio quando comparada à rutina, e do TBARS quando comparado ao BHT, assim como a atividade alelopática, uma vez que estimularam tanto a germinação como o crescimento das sementes. A fração clorofórmica e acetato de etila demonstraram melhor potencial antioxidante com 204,17% e 127,11% em relação à rutina no método de formação do complexo fosfomolibdênio, e o extrato bruto e a fração hexano com 64,2% e 60,9%, em relação ao BHT, no método TBARS. No ensaio alelopático, destaca-se a fração clorofórmica, pois foi a única amostra que estimulou o crescimento do hipocótilo e radícula na maioria das concentrações, variando de 41 a 144%, e a fração acetato de etila que apresentou a maior porcentagem de estímulo nesse bioensaio, demonstrando estímulo de 274% do crescimento do hipocótilo. Este é o primeiro trabalho que demonstra a atividade antioxidante e alelopática de Z. rhoifolium...
Subject(s)
Humans , Antioxidants , Plant Extracts/analysis , ZanthoxylumABSTRACT
Administration of ethanol extract of stem bark from Z. rhoifolium (EEtOH-ZR) induced hypotension associated with a dual effect in heart rate in normotensive rats. This response was highlighted in spontaneously hypertensive rats (SHR). In rat superior mesenteric artery rings, the cumulative addition of EEtOH-ZR (0.1–750 µg/mL) on a phenylephrine-induced pre-contraction (10-5 M) promoted a vasorelaxant effect by a concentration-dependent manner and independent of vascular endothelium. A similar effect was obtained on KCl-induced pre-contractions (80 mM). EEtOH-ZR attenuated contractions induced by cumulative addition of CaCl2 (10-6–3 × 10-2 M) in depolarizing medium without Ca2+ only at 500 or 750 µg/mL. Likewise, on S-(–)-Bay K 8644-induced pre-contractions (10-7 M), the EEtOH-ZR-induced vasorelaxant effect was attenuated. EEtOH-ZR (27, 81, 243 or 500 µg/mL) inhibited contractions induced by cumulative addition of phenylephrine (10-9 - 10-5 M) in endothelium-denuded preparations or by a single concentration (10-5 M) in a Ca2+-free medium. The involvement of K+ channels was evaluated by tetraethylammonium (3 mM); the EEtOH-ZR-induced vasorelaxation was not attenuated. Thus, calcium influx blockade through voltage-operated calcium channels (CaVL) and inhibition of calcium release from intracellular stores are probably underlying EEtOH-ZR-induced cardiovascular effects.
Subject(s)
3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester/pharmacology , Animals , Antihypertensive Agents/pharmacology , Blood Pressure/drug effects , Calcium Channel Agonists/pharmacology , Calcium Channels/drug effects , Calcium Chloride/pharmacology , Endothelium, Vascular/drug effects , Ethanol/chemistry , Male , Phenylephrine/pharmacology , Plant Bark/chemistry , Plant Stems/chemistry , Potassium Channels/drug effects , Potassium Chloride/pharmacology , Rats , Rats, Inbred SHR , Rats, Wistar , Vasoconstrictor Agents/pharmacology , Vasodilation/drug effects , Vasodilator Agents/pharmacology , Zanthoxylum/chemistryABSTRACT
O estudo avaliou a atividade anti-helmíntica do extrato aquoso das folhas de Zanthoxylum rhoifolium em dois experimentos. O teste in vitro utilizou cultivos de fezes de caprinos tratados com diferentes concentrações do extrato: (134,5 a 335,0 mg.mL-1). No teste in vivo, utilizaram-se 20 ovelhas: G1 tratado durante quatro dias (0,63 g.kg-1 PV); G2, mesma dose, por oito dias; G3, ivermectina (200 μg.kg-1); e G4, sem tratamento. In vitro, observou-se redução de larvas de Haemonchus, Trichostrongylus e Oesophagostomum superior a 95% nas concentrações de 193,7 a 335,0 mg.mL-1. In vivo, a redução de ovos por grama de fezes foi de 51, 56 e 90%, respectivamente, para G1, G2 e G3, no oitavo dia de tratamento, enquanto para os estágios imaturos e adultos variou de 0 a 91% no G1 e 26 a 94% no G2. A eficácia da ivermectina alcançou 99% para L4 e L5 de H. contortus e 100% para as demais espécies de nematoides. Parâmetros clínicos e bioquímicos permaneceram na faixa de normalidade, e as análises histopatológicas não revelaram alterações sugestivas de toxicidade. Embora altamente efetivo in vitro, o extrato aquoso de folhas de Z. rhoifolium foi pouco eficaz in vivo na redução de nematoides gastrintestinais.
The study evaluated the anthelmintic activity of aqueous extract of Zanthoxylum rhoifolium leaves in two experiments. In vitro test, cultures of goat fecal samples were treated with different concentrations of extract (134.5 to 335.0 mg.mL-1). In vivo test was composed of 20 sheep: G1: treated with 0.63 g.kg-1, during four days; G2: same dose, for eight days; G3: ivermectin (200 μg.kg-1) and G4 untreated group. In vitro results showed a reduction of Haemonchus spp, Trichostrongylus spp. and Oesophagostomum spp. larvae greater than 95% in the concentrations between 335.0 and 193.7 mg.mL-1. Faecal egg counting reduction was 51, 56 and 90% in G1, G2 and G3, respectively, while immature stages and adults ranged from 0 to 91% in G1 and from 26 to 94% in G2. Ivermectin effectiveness was 99% for L4 and L5 of H. contortus and 100% for other nematodes species. Clinical and biochemical parameters have remained in the normality and histophatologic analyses did not show alteration suggesting absence of toxicity. Although the great effectiveness of Z. rhoifolium leaves extract in vitro test, it displayed poor efficiency in vivo regarding gastrointestinal nematodes reduction.
Subject(s)
Animals , Anthelmintics/pharmacology , Helminths/drug effects , Plant Leaves , Plant Extracts/pharmacology , Zanthoxylum , WaterABSTRACT
The study evaluated the anthelmintic activity of aqueous extract of Zanthoxylum rhoifolium leaves in two experiments. In vitro test, cultures of goat fecal samples were treated with different concentrations of extract (134.5 to 335.0 mg.mL-1). In vivo test was composed of 20 sheep: G1: treated with 0.63 g.kg-1, during four days; G2: same dose, for eight days; G3: ivermectin (200 g.kg-1) and G4 untreated group. In vitro results showed a reduction of Haemonchus spp, Trichostrongylus spp. and Oesophagostomum spp. larvae greater than 95% in the concentrations between 335.0 and 193.7 mg.mL-1. Faecal egg counting reduction was 51, 56 and 90% in G1, G2 and G3, respectively, while immature stages and adults ranged from 0 to 91% in G1 and from 26 to 94% in G2. Ivermectin effectiveness was 99% for L4 and L5 of H. contortus and 100% for other nematodes species. Clinical and biochemical parameters have remained in the normality and histophatologic analyses did not show alteration suggesting absence of toxicity. Although the great effectiveness of Z. rhoifolium leaves extract in vitro test, it displayed poor efficiency in vivo regarding gastrointestinal nematodes reduction.
O estudo avaliou a atividade anti-helmíntica do extrato aquoso das folhas de Zanthoxylum rhoifolium em dois experimentos. O teste in vitro utilizou cultivos de fezes de caprinos tratados com diferentes concentrações do extrato: (134,5 a 335,0 mg.mL-1). No teste in vivo, utilizaram-se 20 ovelhas: G1 tratado durante quatro dias (0,63 g.kg-1 PV); G2, mesma dose, por oito dias; G3, ivermectina (200 g.kg-1); e G4, sem tratamento. In vitro, observou-se redução de larvas de Haemonchus, Trichostrongylus e Oesophagostomum superior a 95% nas concentrações de 193,7 a 335,0 mg.mL-1. In vivo, a redução de ovos por grama de fezes foi de 51, 56 e 90%, respectivamente, para G1, G2 e G3, no oitavo dia de tratamento, enquanto para os estágios imaturos e adultos variou de 0 a 91% no G1 e 26 a 94% no G2. A eficácia da ivermectina alcançou 99% para L4 e L5 de H. contortus e 100% para as demais espécies de nematoides. Parâmetros clínicos e bioquímicos permaneceram na faixa de normalidade, e as análises histopatológicas não revelaram alterações sugestivas de toxicidade. Embora altamente efetivo in vitro, o extrato aquoso de folhas de Z. rhoifolium foi pouco eficaz in vivo na redução de nematoides gastrintestinais.
ABSTRACT
Una nueva cumarina llamada 3 -metoxi-4-(3-me t i l b u t -2-enil)-2H-cromen-2-ona fue aislada de la madera de Z. rhoifolium, junto con los compuestos conocidos, dictamnina y N-metilflindersina. Sus estructuras fueron elucidadas por RMN, incluyendo técnicas bidimensionales y por comparación con datos reportados en la literatura.
A novel coumarin named 3-metoxi-4-(3-me tilbut-2-enil)-2H-cromen-2-one was isolated from the wood of Z. rhoifolium, to get her with the known compounds, dictamnine and N-methylflin dersine. Their structures were elucidated by RMN spectraincluding 2D techniques and comparison with literature data.
Da madeira de Zanthoxylum rhoifolium foi iso la da uma nova cu ma ri na, com o name, 3 metoxi-4- (3-metilbut-2-enil)-2H-cromen 2-ona junto con os compostos, conhecidos: dictamnina y N-methyl- flindersina. Suas estruturas foram elucidadas por RMN, incluindo técnicas bidiomensionais e pela comparação comdados da literatura.