Abstract Formulations containing chitosan incorporated with methanolic fraction of Euphorbia umbellata (Pax) Bruyns, Euphorbiaceae, were studied aiming future applications of this new material as medicine. In order to investigate potential interactions between chitosan and the methanolic fraction (10, 50 and 100% in relation to the amount of chitosan) physicochemical characterization was performed by scanning electron microscopy, density, differential scanning calorimetry, thermogravimetry, X-ray diffraction, Fourier-transform infrared spectroscopy and colorimetry techniques. The phenolic compounds released from the chitosan membranes were evaluated using the Folin-Ciocalteau quantification method; antioxidant and antimicrobial activity were also studied. Increasing amounts of the methanolic fraction added to polymeric matrix produced different numbers of pores on the surface of the membranes, changes in the calorimetric, spectroscopic and crystalline properties as well as color changes, when compared to the inert membrane. These changes can be attributed to chemical interactions that occurred between the structure of the chitosan and the phenolic compounds present in the studied fraction. The matrix samples incorporated with 50 and 100% of the methanolic fraction presented different release profiles of phenolic compounds from the membranes (controlled manner) and promoted antioxidant and antimicrobial activity.

ABSTRACT Euphorbia umbellata (Pax) Bruyns, Euphorbiaceae, is commonly used in folk medicine of southern Brazil to treat several kinds of cancer. The latex (part of the plant used for this purpose) is mixed with water and taken as treatment; but this matrix contains toxic potential related to the presence of some phorbol type diterpenes. So the aim of this study was to evaluate the cytotoxicity of the crude extract of the bark of E. umbellata and its fractions (Hex, CHCl3, EtOAc and MeOH) using in vitro assay (applying Jurkat cells line). A preliminary cytotoxic study (MTT reduction, trypan blue exclusion and DNA quantification assays) was executed to identify the most active material. The CHCl3 fraction displayed the highest activity and was selected for further investigation of any cytotoxic mechanism and evaluation of chemical composition; flow cytometry, Acridine orange and Hoechst 33342 staining experiments and Gas chromatography–mass spectrometry analysis were applied to achieve these results. This fraction demonstrated the best cytotoxic results against Jurkat cells line with IC50 of 29.00 ± 1.49, 10.06 ± 1.48 and 4.83 ± 2.25 µg/ml for 24, 48 and 72 h of experiment, respectively (trypan blue exclusion). The mechanism responsible for this action can be associated with the promotion of cell cycle arrest and apoptosis. The two main classes of compounds present in the CHCl3 fraction are steroids and triterpenes. Further, phytochemical studies with this fraction need to be evaluated, to try isolating these substances and establishing a more detailed cytotoxic study against Jurkat cells.

Abstract Zingiber zerumbet (L.) Roscoe ex Sm., Zingiberaceae, is a perennial, aromatic and tuberose plant that grows in humid locations. Also known as bitter ginger, Z. zerumbet is traditionally found throughout Asia, where it is widely used in foods, beverages and for ornamental purposes. The viscous juice present in the inflorescence of the plant is rich in surfactants and is also known as "ginger shampoo". The rhizome can be macerated in ethanol and used as a tonic and a stimulant. In Brazil Z. zerumbet is found in the Amazon region, in Taruma-mirim and Puraquequara (rural areas of Manaus, Amazon, Brazil). The main chemical compounds found in Z. zerumbet are terpenes and polyphenols. Zerumbone, a sesquiterpene, is the principal bioactive compound of Z. zerumbet and it is widely studied for its medicinal properties. The extracts and isolated metabolites of Z. zerumbet have exhibited the following properties: anti-inflammatory, antioxidant, antidiabetic, anticancer, antimicrobial, analgesic and antiviral. The National Institute of Amazon Research in Brazil is currently conducting studies using extracts from this plant to obtain compounds active in tumor models. The aim of this review is to provide a overview about the main aspects related with pharmacognosy and pharmacology of Z. zerumbet published in the literature over the last decade.

Ilex paraguariensis (yerba-mate) is used as a beverage, and its extract requires adequate quality control methods in order to guarantee quality and safe use. Strategies to develop and optimize a chromatographic method to quantify theobromine, caffeine, and chlorogenic acid in I. paraguariensis extracts were evaluated by applying a quality by design (QbD) model and ultra high-performance liquid chromatography (UHPLC). The presence of these three phytochemical markers in the extracts was evaluated using UHPLC-MS and was confirmed by the chromatographic bands in the total ion current traces (m/z of 181.1 [M+H]+, 195.0 [M+H]+, and 353.0 [M−H]−, respectively). The developed method was then transferred to a high-performance liquid chromatography (HPLC) platform, and the three phytochemical markers were used as external standards in the validation of a method for analyses of these compounds in extracts using a diode array detector (DAD). The validated method was applied to quantify the chlorogenic acid, caffeine, and theobromine in the samples. HPLC-DAD chromatographic fingerprinting was also used in a multivariate approach to process the entire data and to separate the I. paraguariensis extracts into two groups. The developed method is very useful for qualifying and quantifying I. paraguariensis extracts.

AbstractIn southern Brazil, the bottled latex of Synadenium grantii Hook f., Euphorbiaceae, is popularly used as a treatment of all types of cancer. Similarly, Synadenium umbellatum Pax. is used in the central western region of Brazil for the same purpose and in the same manner of use. Both plants are popularly known as janaúba or leitosinha. The objectives of this study were to use pharmacobotanical analysis to verify whether these two species, which are considered to be distinct, are actually the same to determine anatomical markers; to assist in the identification and differentiation of other Euphorbia; and to evaluate the cytotoxic activity of the latex in relation to HeLa and HRT-18 cells. Leaves and stems of the species were collected in Goiânia and Ponta Grossa and were investigated using scanning electron microscopy and optical microscopy techniques. The latex was also collected and analyzed in relation to its cytotoxic effect by employing MTT and NR techniques. The pharmacobotanical study of the specimens in both localities showed that they were the same species, namely Euphorbia umbellata (Pax) Bruyns, which is the scientific nomenclature accepted and confirmed by an expert taxonomist who specializes in Euphorbia. The pharmacobotanical characteristics highlighted in this study can assist in the identification of the taxon and contribute to the control of the quality of this plant drug. The evaluation of the latex in relation to HRT-18 cells demonstrated action after 48 h of experiment. In contrast, in relation to HeLa cells its induced cytotoxicity in all times and a dose-dependent manner. The IC50 values (72 h) observed were 252.58 ± 18.51 µg/ml and 263.42 ± 15.92 µg/ml to MTT experiment and 250.18 ± 19.48 µg/ml and 430.56 ± 19.71 µg/ml to NR experiment for the HeLa and HRT-18 cells, respectively.

Synadenium grantii Hook f., Euphorbiaceae, is popularly known as leitosinha or janaúba. The diluted latex (18 drops/L of water) is commonly used in the south of Brazil to treat gastric disturbances. This study evaluated phytochemical screening and toxicity using Artemia salina Leach of crude bark extract and also latex. The toxicity and the anti-ulcer activity of S. grantii latex were also tested in rats. Phytochemical results showed presence of tannins, terpenes, unsaponificable substances, coumarins and anthraquinones in the crude bark extract and terpenes in the latex. Gas chromatography-mass spectrometry (GC-MS) analysis demonstrated the presence of diterpene tigliane esters in the latex, identified as 12-deoxyphorbol-13-(2-metilpropionate) and phorbol 12,13,20-triacetate. The toxicity results using A. salina presented CL50 26.58μg/mL and CL50 778.66μg/mL, for the latex and the crude bark extract respectively. The toxicological hepatic parameters of the diluted latex were not different to the control group (p<0.05). The eosinophils cells showed an increase in both the diluted and pure latex groups. The pure latex showed gastric protection of 90% (p<0.05) and the diluted latex showed 6% compared to the negative control. Therefore, our data indicate that S. grantii latex, under research conditions presented gastric protection. Pure latex showed more toxicity than the diluted latex.