Quantitative Chemical Composition, Anti-Oxidant Activity, and Inhibition of TNF Release by THP-1 Cells Induced by Extracts of Echinodorus macrophyllus and Echinodorus grandiflorus.

This study investigated the similarities between Echinodorus macrophyllus and Echinodorus grandiflorus, plant species that are traditionally used in Brazil to treat rheumatism and arthritis, whose anti-inflammatory effects are supported by scientific evidence. The contents of cis- and trans-aconitic acid, homoorientin, chicoric acid, swertisin, caffeoyl-feruloyl-tartaric acid, and di-feruloyl-tartaric acid were quantified by UPLC-DAD in various hydroethanolic extracts from the leaves, whereas their anti-oxidant activity and their effect on TNF release by LPS-stimulated THP-1 cells were assessed to evaluate potential anti-inflammatory effects. The 50% and 70% ethanol extracts showed higher concentrations of the analyzed markers in two commercial samples and a cultivated specimen of E. macrophyllus, as well as in a commercial lot of E. grandiflorus. However, distinguishing between the species based on marker concentrations was not feasible. The 50% and 70% ethanol extracts also exhibited higher biological activity, yet they did not allow differentiation between the species, indicating similar chemical composition and biological effects. Principal component analysis highlighted comparable chemical composition and biological activity among the commercial samples of E. macrophyllus, while successfully distinguishing the cultivated specimen from the commercial lots. In summary, no differences were observed between the two species in terms of the evaluated chemical markers and biological activities.

Echinodorus grandiflorus: Ethnobotanical, phytochemical and pharmacological overview of a medicinal plant used in Brazil.

Echinodorus grandiflorus (Cham. & Schltdl.) Micheli is a native Brazilian species used in traditional practices for the treatment of several conditions such as inflammatory diseases, arthritis and hypertension. Through a systematic review of the accumulated knowledge about the species E. grandiflorus, the botanical, phytochemistry, ethnobotanical and pharmacological properties of this medicinal plant demonstrates its potential to naturally provide anti-inflammatory and anti-oxidant with a special emphasis on anti-hypertensive and cardioprotective effects. The body of literature reports that the chemical composition of crude E. grandiflorus extracts are notably composed of diterpenoids and flavonoids metabolites. Pharmacological studies have shown that oral treatments using the hydroalcoholic extracts of leaves from this plant has a significant anti-inflammatory, anti-hypertensive, diuretic and cardioprotective effects in rats with no toxicity. The holistic activities of complex extracts are corroborated by the individuals mechanisms of action, as well as, synergistic benefits attributed to the isolated chemical major constituents in this species. In light of the serious health concerns ascribed, it is important to investigate medicinal plant species with histories of traditional use for circulatory problems to meet the growing demands by scientifically validating their use and safety.

Involvement of bradykinin B2 and muscarinic receptors in the prolonged diuretic and antihypertensive properties of Echinodorus grandiflorus (Cham. & Schltdl.) Micheli.

BACKGROUND: Although Echinodorus grandiflorus (Cham. & Schltr.) Michel are used in Brazilian folk medicine as a diuretic drug, to date, no study has evaluated the mechanisms involved in this activity after prolonged administration in rats. AIM OF THE STUDY: Evaluate the possible mechanisms involved in the prolonged diuretic activity of ethanol soluble fraction obtained from Echinodorus grandiflorus (ES-EG) and to assess its relationship with hypotensive and antihypertensive activity using normotensive rats and those with renovascular hypertension (2K1C). METHODS: The diuretic effects of ES-EG (30-300 mg/kg; p.o.) were compared with hydrochlorothiazide in a repeated-dose treatment for 7 days. The urinary volume and sodium, potassium, chloride, bicarbonate contents, conductivity, pH and density were estimated in sample collected in 24 h for 7 days. Plasma sodium, potassium, total protein, urea, creatinine, aldosterone, vasopressin, nitrite, acetylcholinesterase concentration and angiotensin converting enzyme (ACE) activity were measured in samples collected at the end of the experimental period (seventh day). Using pharmacological antagonists or inhibitors, the involvement of bradykinin, prostaglandin, acetylcholine and nitric oxide (NO) in ES-EG-induced diuresis was determined. In addition, activities of erythrocytary carbonic anhydrase and renal Na+/K+/ATPase were evaluated in vitro. RESULTS: ES-EG increased diuresis similarly to hydrochlorothiazide and also presented HCO3-sparing effects and increased serum nitrite levels. Moreover, the intraduodenal administration of ES-EG induces significant hypotensive and antihypertensive effects in 2K1C rats. Previous treatment with HOE-140, indometacin and atropine fully avoided the diuretic effect of ES-EG, and including L-NAME pre-administration, it prevented the hypotensive and hypertensive activity induced by ES-EG. In addition, the association between HOE-140 and atropine or indometacin and L-NAME fully inhibited the hypotensive and antihypertensive effects of ES-EG. The 7-day treatment with ES-EG resulted in increased plasma nitrite levels. All other parameters were not affected by treatment with ES-EG. CONCLUSIONS: Our results suggest that the mechanisms through which Echinodorus grandiflorus extracts induce prolonged diuresis and reduce blood pressure in normotensive and 2K1C rats are mainly related to activation of muscarinic and bradykinin receptors with direct effects on prostaglandins and nitric oxide pathways.

Ethnopharmacological investigation of the diuretic and hemodynamic properties of native species of the Brazilian biodiversity.

ETHNOPHARMACOLOGICAL RELEVANCE: Although Echinodorus grandiflorus, Cuphea carthagenensis, and Phyllanthus tenellus infusions are used in Brazilian folk medicine due to their possible diuretic effect, none of these species was critically investigated as a diuretic drug. So, the aim of this study was to evaluate the possible acute diuretic activity of ethanol soluble fractions (ES) obtained from these species and assess the relationship between renal cortical blood flow and their antioxidant and hypotensive activity using normotensive Wistar rats. MATERIAL AND METHODS: The preparation obtained from E. grandiflorus (ES-EG), C. carthagenensis (ES-CC), and P. tenellus (ES-PT) infusions was orally administered in a single dose to rats. Urine excretion rate, pH, density, conductivity and Na(+), K(+), Cl(-) and HCO3(-) contents were measured in the urine of saline-loaded animals. Concentration of electrolytes, total protein, urea, creatinine, and angiotensin converting enzyme (ACE) activity were evaluated in collected serum. The involvement of the renal cortical blood flow and antioxidative activity in the hypotensive and diuretic effects was also determined. RESULTS: Water and Na(+), Cl(-) and Na(+) excretion rates were significantly increased by ES-EG, while urinary bicarbonate excretion was reduced. Moreover, ES obtained from E. grandiflorus was able to significantly increase renal blood flow and reduce mean arterial pressure and oxidative stress in "in vitro" and "in vivo" models. All other parameters evaluated were not affected by any treatment. CONCLUSION: The results presented here shown that the ES-EG obtained from E. grandiflorus leaves shown a significant diuretic and hypotensive activity and suggest that these effects could be related with an important renal and systemic vasodilator effect. In addition, it was shown for the first time that the pharmacological effects of ES obtained from P. tenellus and C. carthagenensis do not support its popular use as a diuretic agent.

Qualidade e autenticidade de folhas de chapéu-de-couro (Echinodorus grandiflorus) oriundas de fornecedores de São Paulo / Quality and authenticity of leaves of "chapéu-de-couro" (Echinodorus grandiflorus) from suppliers in São Paulo

Echinodorus grandiflorus e Echinodorus macrophyllus, conhecidas como chapéu-de-couro, são empregadas de forma indistinta como anti-inflamatório. O objetivo deste trabalho foi realizar análises físico-químicas de três amostras (A, B e C) de folhas de chapéu-de-couro (E. grandiflorus) provenientes de fornecedores de São Paulo buscando avaliar a qualidade e autenticidade destas amostras considerando a Farmacopéia Brasileira, 5ª edição, como referência. Verificou-se que as amostras estavam de acordo com as especificações farmacopeicas em relação às características organolépticas, material estranho, umidade, cinzas totais, cinzas sulfatadas (exceto amostras A e B) e teores de derivados de ácido o-hidroxicinâmico (exceto amostra A). Na descrição macro e microscópica foram identificadas estruturas características de E. grandiflorus. Após análise dos perfis cromatográficos por cromatografia em camada delgada de sílica (CCDS) constatou-se a presença de ácido caféico, isoorientina e swertiajaponina, conforme a monografia da espécie. A amostra C foi a única droga vegetal aprovada segundo os critérios da Farmacopeia Brasileira, evidenciando-se a necessidade da realização do controle de qualidade de matérias-primas vegetais para garantir a obtenção de fitoterápicos seguros e eficazes.

Echinodorus grandiflorus and Echinodorus macrophyllus, known as "chapéu-de-couro", have been differently used as anti-inflammatory agents. The aim of the present study was to carry out physicochemical analyses of three leaf samples (A, B and C) from "chapéu-de-couro" (E. grandiflorus) obtained from suppliers in São Paulo to assess the quality and the authenticity of these samples according to the Brazilian Pharmacopoeia (BP) 5th edition. All samples were in agreement with the specifications of the Pharmacopoeia considering their organoleptic characteristics, foreign material, humidity, total ash and sulfated ash (except for samples A and B), as well as the levels of o-hydroxycinnamic acid derivatives (except for sample A). Macroscopic and microscopic analysis of the samples revealed structures typical of E. grandiflorus. Analysis of chromatographic profiles by thin-layer chromatography (TLC) on silica gel indicated the presence caffeic acid, isoorientin and swertiajaponin, which are in accordance with the monography for this species. Sample C was the only plant drug approved according to the criteria of the Brazilian Pharmacopoeia, evidencing the need of quality control of raw plant material to ensure the production of safe and effective phytomedicines.

Validação de metodologia analítica para a determinação de derivados do ácido o-hidroxicinâmico de Echinodorus grandiflorus / Validation of analytical methodology for the determination of derivatives of o-hydroxycinnamic acid from Echinodorus grandiflorus

Este artigo descreve o desenvolvimento e a validação de método espectrofotométrico UV-Visível para quantificação de derivados do ácido o-hidroxicinâmico em folhas de Echinodorus grandiflorus. O método demonstrou ser linear (r² = 0,9974), preciso (DPR < 15%) na análise de matriz complexa e exata (recuperação = 107,56%).

This paper describes the development and the validation of an UV-Vis spectrophotometric method for the quantification of derivatives of o-hydroxycinnamic acid in leaves of Echinodorus grandiflorus. The method showed to be linear (r² = 0.9974), precise (RSD < 15%) in the analysis of complex matrix and accurate (recovery = 107.56%).