ABSTRACT
BACKGROUND: Triterpenes are ubiquitous secondary metabolites present in plants. They can be found in both forms, as genins or conjugated as glycosides. Although distinct analytical methods to quantify these compounds in vegetal tissues are available in the literature, limitations like high cost, complexity on sample preparation, and selectivity are often challenging issues. This study aimed to develop and to validate a simple and rapid spectrophotometric method to detect and quantify total triterpenes in plant matrices. METHODS: The assay was conducted directly into glass tubes using vanillin, acetic acid, and sulphuric acid as reagents, and ß-sitosterol as reference standard. The samples were analyzed at 548 nm assessing the quality parameters of selectivity, linearity, precision, accuracy, limit of detection (LOD), limit of quantification (LOQ), and robustness. RESULTS: The method was selective, with precision and accuracy varying from 0.56% to 4.98% and 96.63% to 113.87%, respectively. The values of the limit of detection and quantification were 0.042 µg.mL-1 and 0.14 µg.mL-1, correspondingly. The correlation coefficient (r) at the concentration range of 3.08 µg.mL-1to 24.61 µg.mL-1 was 0.9998. The total of triterpenes found in of B. holophylla and M. ilicifolia leaves were 132.36 ± 20.36 mg EßS.g-1 of dry extract and 53.91 ± 2.6 mg EßS.g-1 of dry extract, respectively. CONCLUSION: The method was reliable to quantify total triterpenes extracted from Maytenus ilicifolia and Bauhinia holophylla. Graphical abstract.
Subject(s)
Bauhinia , Celastraceae , Plant Leaves/chemistry , Spectrophotometry/methods , Triterpenes/analysis , Acetic Acid/chemistry , Benzaldehydes/chemistry , Limit of Detection , Reproducibility of Results , Sulfuric Acids/chemistryABSTRACT
Maytenus ilicifolia is a plant widely used in South American folk medicine as an effective anti-dyspeptic agent, and the aim of this study was to evaluate their clinical and toxicological effects in healthy volunteers in order to establish its maximum safe dose. We selected 24 volunteers (12 women and 12 men) between 20 and 40 years of age and put them through clinical/laboratory screening and testing to ascertain their psychomotor functions (simple visual reaction, speed and accuracy, finger tapping tests). M. ilicifolia tablets were administered in increasing weekly dosages, from an initial dose of 100 mg to a final dose of 2000 mg. The volunteers' clinical and biochemical profiles and psychomotor functions were evaluated weekly, and they also completed a questionnaire about any adverse reactions. All subjects completed the study without significant changes in the evaluated parameters. The most cited adverse reactions were xerostomia (dry mouth syndrome) (16.7%) and polyuria (20.8%), with reversal of these symptoms without any intervention during the study. The clinical Phase I study showed that the administration of up to 2000 mg of the extract was well tolerated, with few changes in biochemical, hematological or psychomotor function parameters, and no significant adverse reactions. Copyright © 2017 John Wiley & Sons, Ltd.
Subject(s)
Maytenus/chemistry , Plant Extracts/pharmacology , Plant Leaves/chemistry , Adult , Female , Humans , Male , Plant Extracts/adverse effects , Plants, Medicinal/chemistry , Psychomotor Performance/drug effects , Tablets , Young AdultABSTRACT
One of the Brazilians medicinal plants most cited in ethnopharmacological surveys for the treatment of ulcers and gastric diseases was evaluated for its efficacy and toxicity. Maytenus ilicifolia leaf extract (MIE) was acutely and chronically (180 days) administered to rats, mice, and dogs. Acute tests were antiulcer effect and toxicological trials (observational pharmacological screening, LD50, motor coordination, sleeping time and motor activity). Chronic tests were the following: weight gain/loss and behavioral parameters in rats and mice; estrus cycle, effects on fertility, and teratogenic studies in rats and mutagenic features in mice, in addition to the Ames and micronucleus test. The following parameters were assessed in dogs: weight gain/loss, general physical conditions, water/food consumption, and anatomopathological examination of the organs subsequent to the 180-day treatment. The results showed a clear antiulcer activity for MIE from 70 mg/kg and an absence of toxicological effects in the three animal species, even if given in high doses or over a long period. The present results confirm the antiulcer property and absence of toxicological effects in three animal species of MIE, which is in line with its current popular medicinal use. Copyright © 2017 John Wiley & Sons, Ltd.
Subject(s)
Maytenus/chemistry , Plant Extracts/pharmacology , Plant Leaves/chemistry , Stomach Ulcer/drug therapy , Animals , Brazil , Dogs , Drug Evaluation, Preclinical , Female , Fertility/drug effects , Male , Mice , Plant Extracts/toxicity , Plants, Medicinal/chemistry , Rats , Rats, Wistar , Toxicity Tests, Acute , Toxicity Tests, ChronicABSTRACT
Large elongated glands occur on Cercideae leaf surfaces. Leaves of Bauhinia (55 taxa, 53 species), Cercis (1 species), Phanera (1 species), Piliostigma (2 species), Schnella (19 species) and Tylosema (1 species) were observed to determine location and relative number of glands. They were only observed on the abaxial leaf surface of 42 Bauhinia taxa. The glands were analyzed by light stereomicroscope and scanning electron microscopy. They are large (up to 270 µm long and 115 µm wide) and multicellular, containing lipophilic substances, probably volatile oils. Presence or absence and density of the glands in species of Bauhinia may be useful to determine species delimitation or distinction among infraspecific taxa. Higher density of glands is more common in species from "cerrado" (a savanna ecosystem) and "caatinga" (a semiarid ecosystem from northeast Brazil) areas. Bauhinia species devoid of foliar glands are frequently from humid forests.
Subject(s)
Bauhinia/ultrastructure , Plant Leaves/ultrastructure , Bauhinia/classification , Bauhinia/cytology , Microscopy, Electron, Scanning , Plant Leaves/cytology , Species SpecificityABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: HETEROPTERYS TOMENTOSA: A. Juss (Malpighiaceae), commonly mistaken as Heteropterys aphrodisiaca, is chronically used by the Brazilian population to improve general health due to its claimed protective effects against a wide range of medical conditions. AIM OF THE STUDY: This study in rodents aimed to verify the adaptogenic potential of the hydroalcoholic extracts of the roots (the most commonly used portion), branches and leaves of the plant. MATERIALS AND METHODS: The phytochemical constitution of the extracts was analyzed through thin-layer chromatography and high-performance liquid chromatography. Restriction- and cold-induced stress in rats treated for 14 days with 100 or 300 mg/kg of the extracts were used to evaluate parameters such as ulceration, adrenals, thymus and spleen weights, as well as ACTH and corticosterone plasmatic levels. The stress response also was evaluated in mice by self-analgesia induced by restraint stress, after 7 days of treatment at doses of 100 and 300 mg/kg. The learning and memory of aged rats treated with extracts of root or branches at the dose of 50 mg/kg for 80 days were evaluated in the elevated T-maze test. RESULTS: The chemical constituents of the three parts of the plant were relatively similar in the presence of saponins, hydrolysable tannins, flavonoids, polyphenols and triterpenes. None of the three extracts were capable of protecting the stomach from ulcerations in rats submitted to cold restraint stress or protecting from alterations in adrenal or spleen weight (p>0.05). Furthermore, the extracts did not inhibit increases in plasma levels of corticosterone and adrenocorticotropic hormone. Moreover, the extracts did not inhibit self-analgesia induced by restraint stress in mice and did not improve the performance of aged rats in the T-maze test (p>0.05). CONCLUSION: The tests employed in this study did not show evidence of adaptogenic activity in the three extracts of Heteropterys tomentosa.
Subject(s)
Malpighiaceae , Plant Extracts/therapeutic use , Plant Leaves , Plant Roots , Plant Stems , Adrenocorticotropic Hormone/blood , Analgesia , Animals , Cold Temperature , Corticosterone/blood , Flavonoids/analysis , Male , Maze Learning/drug effects , Mice , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Leaves/chemistry , Plant Roots/chemistry , Plant Stems/chemistry , Rats , Rats, Wistar , Restraint, Physical , Saponins/analysis , Stomach Ulcer/blood , Stomach Ulcer/drug therapy , Stress, Physiological/drug effects , Tannins/analysis , Triterpenes/analysisABSTRACT
Medicinal plants (MP) have been used world-wide for the treatment or prevention of health conditions and due to their natural origin; they have been historically considered harmless. Semi-structured interviews were carried out with an intentional sample of twenty plant vendors in the city of Diadema to explore their knowledge and beliefs on the safety and efficacy of MP. Different levels of perceptions about the safety of MP were found, varying from "completely safe" to "completely harmful". The majority of the interviewees declared that "if herbs have an effect, they are also likely to have a side effect", depending on many factors such as dosage, concomitant use of other drugs, characteristics of the plant material and consumer related factors, specially those related to pregnant women, children and elderly people. Thirty-nine unexpected events related to 21 species of MP were reported. One case of serious gastrointestinal disease related to the consumption of a contaminated "slim mixture" was also described. Adverse events and other problems that result from MP are relatively uncommon, but they are almost certainly underreported and occur more often than acknowledged. This study strengthens the call for further research and educational efforts into this complex area.
ABSTRACT
Croton macrobothrys Baill, Euphorbiaceae, is a tree from the Atlantic Forest in Southern Brazil, used in traditional medicine and popularly known as "dragon's blood" and "pau-sangue". Leaf n-hexane, dichloromethane and methanol extracts were analyzed by GC/MS and evaluated for their in vitro antiproliferative activity on cell lines 786-0 (kidney), HT-29 (colon), K562 (leukemia), NCI-ADR/RES (drug resistant ovary), NCI-H460 (lung), MCF-7 (mammary), PC-3 (prostate), OVCAR-3 (ovary), U251 (glioma) and UACC-62 (melanoma). The dicloromethane extract exhibited activity against all cell lines at the concentration 25 µg/mL, in particular on cell lines NCI-H460 (GI50 0.33 μg/mL) and K5662 (GI50 0.91 μg/mL). Relevant constituents in dichloromethane extract are the alkaloids corydine and salutaridine, as well as the diterpenes geranylgeraniol and crotonin-derived clerodanes.
ABSTRACT
Muitos estudos de plantas medicinais baseiam-se em informações etnofarmacológicas, na intenção de encurtar o tempo e diminuir os recursos financeiros no desenvolvimento de novas drogas. O presente trabalho teve como objetivo realizar estudos de farmacologia pré-clínica e fitoquímica com três extratos vegetais, obtidos de duas das 42 plantas com potenciais efeitos analgésico e/ou antiinflamatório, indicadas pelos moradores do Parque Nacional do Jaú, AM. Os extratos hidroalcoólicos foram submetidos à caracterização fitoquímica por meio de cromatografia em camada delgada (CCD). Os testes de farmacologia pré-clínica empregados foram: screening inicial, rota rod, atividade motora, placa quente, tail flick e contorções abdominais, nas doses de 300 e 500 mg/kg. Os três extratos foram obtidos a partir das cascas da cumandá: Campsiandra comosa Benth., Fabaceae (EHCC) e das folhas (EHSF) e cascas (EHSC) da sucuuba: Himatanthus sucuuba (Spruce ex Müll. Arg.) Woodson, Apocynaceae. As análises fitoquímicas revelaram a presença de flavonóides, taninos, iridóides e triterpenos nos diferentes extratos; enquanto os alcalóides e cumarinas não foram detectados. A investigação farmacológica demonstrou atividade analgésica discreta apenas no teste de contorções abdominais para os extratos EHSF e EHCC; nenhuma alteração foi observada no aparelho de rota rod e de modo geral, observou-se diminuição da atividade motora em todos os extratos nas diferentes doses testadas. Diferentes extratos destas plantas estão sendo testados em outros modelos, pelo mesmo grupo de trabalho, a fim de aprofundar os conhecimentos acerca do perfil farmacológico destas espécies.
This work aimed to study the pre-clinical pharmacology and phytochemistry of three plant extracts, obtained from two of the 42 plants with potential analgesic and / or anti-inflammatory, indicated by the residents of the National Park of Jaú, AM. The hydroalcoholic extracts were subjected to phytochemical characterization by thin-layer chromatography (TLC). Tests for pre-clinical pharmacology employed were: initial screening, rota rod, motor activity, hot plate, tail flick and abdominal contortions at doses of 300 and 500 mg / kg. The three extracts were obtained from the bark of cumandá: Campsiandra comosa Benth., Fabaceae (EHCC) and leaves (EHSF) and bark (EHSC) of sucuuba: Himatanthus sucuuba (Spruce ex Müll. Arg.) Woodson, Apocynaceae. The phytochemical analysis revealed the presence of flavonoids, tannins, triterpenes and iridoids in different extracts, while the alkaloids and coumarins were not detected. Research has shown pharmacological activity for EHSF and EHCC extracts, only in the mild analgesic test for abdominal contortions, while no change was observed in the rota rod; and in general, there was decrease in motor activity in all extracts at different doses tested. Different extracts of these plants are being tested in other models by the same working group, in order to deepen the knowledge about the pharmacological profile of these species.
ABSTRACT
Schinus terebinthifolius Raddi and the Myracrodruon urundeuva Allemão were evaluated in rats and mice for antiulcer effects, as these two plants are widely used in Brazil for gastric ulcer treatment. Extracts of the plants showed a marked protective effect against gastric ulcerations induced by immobilization stress at low temperature in rats. They also showed an increase in the pH and volume of the gastric contents, and reduction in gastric hemorrhage in rats, and decrease in intestinal transit in mice, even at the low doses of 3.4 mg/kg (1/4 of the dose used by humans).
Foram avaliados, em ratos e camundongos, os efeitos antiúlcera de duas plantas usadas popularmente no Brasil para o tratamento de "males gástricos": a Schinus terebinthifolius Raddi (aroeira-da-praia) e a Myracrodruon urundeuva Allemão (aroeira-do-sertão). Os decoctos de ambas as plantas apresentaram um marcante efeito protetor da mucosa gástrica contra as ulcerações induzidas por estresse de imobilização em baixa temperatura em ratos. Ambas as plantas apresentaram, ainda: elevação do pH, do volume do conteúdo gástrico, redução das hemorragias gástricas e do trânsito intestinal em camundongos, mesmo em doses tão reduzidas quanto 3,4 mg/kg (1/4 da dose utilizada pelo homem).
ABSTRACT
A crença de que medicamentos à base de plantas são isentos de riscos à saúde faz parte da bagagem cultural da população afeita ao seu uso: "o que vêm da terra não faz mal". No entanto, o potencial tóxico, as características específicas do usuário, a possibilidade de contaminação e a falta de regulamentação constituem fatores de risco para a ocorrência de reações adversas, intoxicações e outras complicações decorrentes de seu uso. Foram realizadas entrevistas semi-estruturadas junto a 20 raizeiros (vendedores de ervas "in natura") na cidade de Diadema/SP. Foram relatados 40 casos de problemas relacionados ao uso de 22 espécies de plantas medicinais. As espécies mais citadas foram Luffa operculata - buchinha (7 casos), Senna alexandrina - sene (4 casos) e Paullinia cupana - guaraná (3 casos). Dentre os sinais e sintomas relatados, os mais freqüentes foram relacionados ao sistema nervoso central, problemas gastrointestinais e cardiovasculares. Os entrevistados também relataram um caso de aborto relacionado ao uso de S. alexandrina e três casos de óbito após a ingestão do chá do fruto de L. operculata. O caráter "natural" das plantas medicinais não é sinônimo de ausência de riscos para a população usuária. É necessária a implantação de políticas de fitofarmacovigilância eficientes, a fim de tornar o consumo mais racional e, deste modo, minimizar os riscos à população usuária.
Traditionally, medicinal herbs have been considered gentle and harmless because of their natural origin: "natural and therefore free of risks". However, toxic potential, various consumer-related factors (such as age, disease factors, pregnancy, etc), contamination, and lack of regulation concerning quality control are some of the risk factors deemed to be associated with herbal adverse reactions, poisonings and other complications. Over a 7-month period, semi-structured interviews were carried out with 20 "raizeiros" (traditional healers) in Diadema/SP. We found 40 unexpected events related to 22 species of medicinal herbs. The most frequent species reported were Luffa operculata - "buchinha" (7 reports), Senna alexandrina - "sene" (4 reports) and Paullinia cupana - "guaraná" (3 reports). Among the adverse events, the most frequent signs and symptoms reported involved the central nervous, gastrointestinal and cardiovascular systems. They also reported one case of abortion (related with S. alexandrina) and three deaths related with L. operculata. Adverse events that result from "natural" medicines are relatively uncommon, but they certainly occur more often than acknowledged. Medicinal plants are traditionally considered as innocuous, but as commercially available medicinal products they require sanitary surveillance in order to identify their risks, to give them a legal status, to evaluate their efficacy and to ascertain their safety.
ABSTRACT
The hydroalcohol extracts of Achillea millefolium L. (AM) and Artemisia vulgaris L. (AV), both belonging to the Asteraceae family, were evaluated by the hot plate, writhing, formalin and intestinal transit tests in an attempt to confirm their folk use as analgesic, antiinflammatory and antispasmodic agents. AM 500 and 1000 mg/kg significantly inhibited abdominal contortions by 65% and 23%, respectively, whereas AV 500 and 1000 mg/kg inhibited them by 48% and 59%, respectively. None of the extracts produced differences in the intestinal transit in mice, nor in the response time in the hot plate or in the immediate or late responses in the formalin test. In HPLC/DAD analyses 'fingerprint', monitored at 360 and 270 nm, both hydroalcohol extracts showed the same flavonoid glycoside as a principal constituent, which was identified as rutin. A high content of caffeic acid derivatives were also found in both extracts. The main differences were observed at 240 nm: AM had a higher content of rutin, while in AV the hydroxybenzoic acid derivative was the major component.
