ABSTRACT The fruits of Litchi chinensis Sonn., Sapindaceae, are renowned for their biological activities. However, their leaves are poorly explored, although they represent an important source of vegetable raw material with biological properties as antioxidant, anti-inflammatory and antinociceptive. An HPLC method was developed and validated for the simultaneous quantification of epicatechin and procyanidin A2 in the leaf hydroethanolic extract of L. chinensis. The markers and other unidentified components were separated on a Luna Phenomenex C18 column (250 mm × 4.6 mm, 5 µm) with mobile phase composed of acetonitrile: water pH 3.0 (with sulfuric acid), in a gradient run; at 1.0 ml min-1, 30 ºC and 278 nm for detection. The method was linear over an epicatechin and procyanidin A2 concentration range of 10–100 µg ml-1. The Limit of Quantification for epicatechin and procyanidin A2 were 1.7 and 2 µg ml-1, respectively. The Relative Standard Deviation (%) values for markers (intra- and inter-day precision studies) were <4.0% and the accuracy was 100 ± 5%. The method was applied to ten samples collected in the state of Santa Catarina (Brazil), which showed 14.8–44.5 and 44.8–69.6 mg g-1 of epicatechin and procyanidin A2, respectively. The proposed method could be a valuable tool for quality assessment of L. chinenis leaves as well as their herbal derivatives.

Ipomoea pes-caprae (L.) R. Br., Convolvulaceae, is a medicinal plant that grows abundantly as a pan-tropical stand plant. The 3² (two factors and three levels) factorial design, was applied to determine the best time and drug/solvent proportion to maximize the flavonoid content in the hydroethanolic extract by maceration process. The antinociceptive and anti-inflammatory effects were studied at 5-20 mg/kg, i.p., using the writhing test and carrageenan-induced pleurisy models in mice. The optimized extract was able to inhibit more than 50% of abdominal writhing at 20 mg/kg, with 55.88%±2.4 of maximum inhibition. Indomethacin, used as positive control, inhibited 64.86% at 10 mg/kg. In the pleurisy model, the extract produced dose-dependent inhibition of the first phase of inflammation (4 h) in the pleural cavity induced by injection of carrageenan (1%) in mice. It inhibited 50%±0.82 (p<0.01) of exudation induced by carrageenan, and 60.88%±0.14 (p<0.01) of leukocyte migration to the pleural cavity. In conclusion, the results validate the technological conditions of the maceration process to produce an optimized bioactive herb extract for the development of analgesic and anti-inflammatory phytopharmaceuticals using 70 ºGL ethanol, a plant to solvent ratio of 12.5% (w/v), and ten days of maceration.

Tea from Phyllanthus niruri L., Phyllanthaceae, aerial parts is commonly used by Brazilian folk medicine for its benefits on the treatment of genitourinary disorders, for what the polyphenolic compounds are mainly responsible. The yield of such compounds may be influenced by several variables related with the plant growth. The effects of planting periods and harvesting conditions are investigated in this work, including four different seasons. The cultivation was characterized by dry mass yield of aerial parts, and the effect of pruning was analyzed. Leaves, stems and their mixtures were analyzed after drying and milling. Loss on drying and water soluble extractives were used as physical parameters for quality control. Flavonoid content and gallic acid were chosen as chemical markers for this work. The spectrophotometric trial based on the aluminum chloride complexes was applied to evaluate the total flavonoids content. Gallic acid contents were measured from the water extractive solutions by high-performance liquid chromatography. The pruning caused a positive influence on the amount of leaves and stems. The highest flavonoids and gallic acid contents were found in the leaves, which were developed over the summer and the winter, respectively, both from the second harvesting (after pruning). Chomatographic profile by HPLC was characterizes by the presence of gallic acid and two other major peaks (not identified substances), which relation was peculiar to each aerial part. In conclusion, these results suggest that even under less favorable climatic conditions, in winter, the pruning seems to cause a strong influence over the P. niruri polyphenolics production. Indeed, the total flavonoids content, as well as the HPLC profile, can be used as indicative parameters of the ratio of leaves and stem in the vegetal raw material.

The anti-inflammatory and antiallodynic effects of spray dried powders starting from leaves, stems, roots, the mixture of leaves and stems, as well as the whole plant aqueous solutions of Phyllanthus niruri L., Phyllanthaceae, were assessed. Gallic acid, used as chemical marker, was quantified by HPLC in the spray dried powders. Carrageenan-induced inflammatory and allodynic responses in the mouse paw were used as pharmacological models. Quantitative and qualitative differences among chemical composition of different herb parts were observed. The oral administration of leaves or leaves plus stems spray dried powders (100 mg/kg) significantly inhibited the carrageenan-induced allodynic effect (42±5 and 54±3%, respectively). Additionally, the spray dried powders of leaves significantly reduced carrageenan-induced paw oedema (35±6%). The spray dried powders of roots, stems, or the mixture of leaves, stems and roots (100 mg/kg, p.o.) did not exhibit antiallodynic or antioedematogenic effect in the same model. In conclusion, differences in the chemical composition of spray dried powders from P. niruri are reflected in their in vivo pharmacological actions. Despite of a direct relationship of anti-inflammatory and antiallodynic effects with the gallic acid content had been observed, especially in the spray dried powders of leaves, the use of spray dried powders of leaves plus stems showed to be more effective, suggesting a synergic effect between their constituents.

Ipomoea pes-caprae (L.) R. Br., (Convolvulaceae), planta que ocorre abundantemente nas dunas do litoral é popularmente conhecida como "salsa-da-praia", e usada na medicina popular devido às suas propriedades analgésica, antiinflamatória e cicatrizante. A partir das partes aéreas frescas foram desenvolvidos protocolos para o seu tratamento prévio e controle de qualidade, com o propósito de caracterizar a planta como matéria-prima farmacêutica. A perda por secagem mostrou que as folhas apresentam menor rendimento de matéria seca em relação aos caules, devido ao seu maior teor de água. A secagem e moagem teve por objetivo a manutenção da perda por dessecação abaixo do valor máximo permitido para drogas vegetais. As folhas e caules secos e moídos foram classificados como pós grossos através da análise granulométrica por tamisação, e caracterizados segundo testes farmacopeicos para drogas vegetais. A determinação de cinzas indicou a presença de material inorgânico, possivelmente areia, associado ao habitat da espécie. O teor de extrativos solúveis em água foi maior nas folhas, seguido dos caules e proporcional na planta inteira, correlacionando-se ao teor de flavonoides totais. A cromatografia em camada delgada das soluções extrativas hidroetanólicas mostrou diferenças apenas com relação à intensidade das manchas, e indicação da presença de isoquercitrina, sendo mais evidente nas folhas.

Ipomoea pes caprae (L.) R. Br., (Convolvulaceae), a pantropical stand plant, popularly known as "salsa-da-praia", is used in folk medicine because of its analgesic, antinflammatory and healing properties. Protocols were developed from the fresh aerial plants to establish their previous treatment and quality control in order to get it characterized as a pharmaceutical raw material. The loss of water on drying in an air oven, showed that leaves represent a lesser dried mass yield than branches, as a result of its higher water content. Drying and milling were aimed at keeping the loss on drying below the limit value accepted for herbs. Dried and milled leaves and branches were classified as thick powder through the sieving method, before they were characterized according to pharmacopoeial tests for herbs. The determination of ashes indicated the presence of inorganic materials, most probably due to sand content which came from the herb habitat. The soluble water extractives were greater from the leaves, followed by the branches and proportional for the entire plant. These results showed to be correlated to the total flavonoid content. The thin layer chromatography for the hydroethanolic solutions only demonstrated differences related to the spots color intensity, and indicated the presence of isoquercitrin, being more evident from the leaves.