CYTOTOXICITY OF BYRSONIMA DUCKEANA W. R. ANDERSON (MALPIGHIACEAE) ON COLON CANCER CELLS

Objective: The objective of this study was the cytotoxicity evaluation of the leaves extract and fractions of Byrsonima duckeana W. R. Anderson. Methods: The toxicity on Artemia salina, haemolytic potential and cytotoxicity activities against two different cell lines a U937 cell line human, and HT29 tumor colon cell line of the leaves extract and fractions of Byrsonima duckeana W. R. Anderson were evaluated. Results: There was no IC50 the Artemia salina assay. The chloroform and ethyl acetate fractions showed haemolytic activity. The results were satisfactory at the most polar fractions, with citotoxicity to the HT29 cell line. Conclusion: The study provides preliminary evidence of cytotoxicity of the most polar fractions at the HT29 cell line, which can indicate a potencial source to offer substances with cytotoxic activity

PHYSICAL AND CHEMICAL CHARACTERISTICS AS PARAMETERS FOR QUALITY CONTROL OF PLANT MATERIAL Rhamnus sphaerosperma var. pubescens

A espécie vegetal Rhamnus sphaerosperma var. pubescens, que é nativa no Brasil, apresenta um grande potencial farmacológico por ser enquadrada no gênero Rhamnus, e possui poucos estudos relatam suas propriedades biológicas, e ainda não foram descritos os parâmetros físico-químicos para o controle de qualidade da matéria-prima vegetal desta espécie. Sendo assim, neste trabalho, os parâmetros físico-químicos, como o teor de umidade, cinzas totais e insolúveis em ácido foram determinados pela primeira vez para esta espécie. Também foi realizada a prospecção fitoquímica, que indentificou a presença marcante de compostos antraquinônicos, que podem ser utilizados como marcadores químicos. Análises microquímicas também foram realizadas, e confirmaram características estruturais presentes em caules e folhas, que já haviam sido descritas na literatura em análises morfonatômicas. Os extratos e frações de caules e folhas deste vegetal também não apresentaram toxicidade em métodos preliminares em Artemia salina e hemólise, sendo, de maneira geral, conisderados atóxicos nestes métodos, o que permite a sequência com estudos farmacológicos e toxicológicos que comprovem a segurança e eficácia destes extratos, para a obtenção de medicamentos fitoterápicos.

Analgesic, Anti-Inflammatory, and Antioxidant Activities of Byrsonima duckeana

Background. Byrsonima is a promising neotropical genus, rich in flavonoids and triterpenes, with several proven pharmacological properties. Nevertheless, Byrsonima duckeana W. R. Anderson is an Amazonian species almost not studied. Objective. To assess the antioxidant, anti-inflammatory, and analgesic activities of Byrsonima duckeana leaves. Materials and Methods. We analyzed an ethanol extract and its fractions for polyphenol content and UHPLC-MS/MS, phosphomolybdenum, DPPH, TBARS antioxidant tests, formalin-induced pain, carrageenan-induced peritonitis, acetic acid-induced abdominal writhings, and hot plate assays. Results. All the samples showed high polyphenol content and antioxidant capacity in the phosphomolybdenum, DPPH, and TBARS tests. We identified ethyl gallate, quinic acid, gallic acid, catechin, epicatechin, quercetrin, and quercetin in the samples. B. duckeana was able to reduce leukocyte migration in the carrageenan-induced peritonitis by 43% and the licking time in the formalin test by 57%. In the acetic acid-induced writhing test, the chloroform (FCL) and ethyl acetate (FEA) fractions were the most active samples. FEA was selected for the hot plate test, where all the dosages tested (5, 50, and 200 mg·kg−1) showed significant analgesic activity. Conclusion. B. duckeana has interesting analgesic and antioxidant activities, due to its high phenolic content, especially phenolic acids

BJcuL, a lectin purified from Bothrops jararacussu venom, induces apoptosis in human gastric carcinoma cells accompanied by inhibition of cell adhesion and actin cytoskeleton disassembly

We show that BJcuL, a lectin purified from Bothrops jararacussu venom, exerts cytotoxic effects to gastric carcinoma cells MKN45 and AGS. This effect was due to the direct interaction with specific glycans on the cells surface and was observed by cell viability decrease, disorganization of actin filaments and apoptosis. In addition, BJcuL was able to reduce tumor cell adhesion to matrigel, what was inhibited by specific carbohydrate or partially inhibited when cells were pre-incubated with matrigel. Our results suggest that BJcuL was able to promote apoptosis in both tumor cells lines and therefore has a prospect for potential use in cancer therapy. (C) 2011 Elsevier Ltd. All rights reserved.CNP

Microbial biotransformation to obtain new antifungals

Antifungal drugs belong to few chemical groups and such low diversity limits the therapeutic choices. The urgent need of innovative options has pushed researchers to search new bioactive molecules. Literature regarding the last 15 years reveals that different research groups have used different approaches to achieve such goal. However, the discovery of molecules with different mechanisms of action still demands considerable time and efforts. This review was conceived to present how Pharmaceutical Biotechnology might contribute to the discovery of molecules with antifungal properties by microbial biotransformation procedures. Authors present some aspects of (1) microbial biotransformation of herbal medicines and food; (2) possibility of major and minor molecular amendments in existing molecules by biocatalysis; (3) methodological improvements in processes involving whole cells and immobilized enzymes; (4) potential of endophytic fungi to produce antimicrobials by bioconversions; and (5) in silico research driving to the improvement of molecules. All these issues belong to a new conception of transformation procedures, so-called green chemistry, which aims the highest possible efficiency with reduced production of waste and the smallest environmental impact

PHYSICAL AND CHEMICAL CHARACTERISTICS AS PARAMETERS FOR QUALITY CONTROL OF PLANT MATERIAL Rhamnus sphaerosperma var. pubescens

A espécie vegetal Rhamnus sphaerosperma var. pubescens, que é nativa no Brasil, apresenta um grande potencial farmacológico por ser enquadrada no gênero Rhamnus, e possui poucos estudos relatam suas propriedades biológicas, e ainda não foram descritos os parâmetros físico-químicos para o controle de qualidade da matéria-prima vegetal desta espécie. Sendo assim, neste trabalho, os parâmetros físico-químicos, como o teor de umidade, cinzas totais e insolúveis em ácido foram determinados pela primeira vez para esta espécie. Também foi realizada a prospecção fitoquímica, que indentificou a presença marcante de compostos antraquinônicos, que podem ser utilizados como marcadores químicos. Análises microquímicas também foram realizadas, e confirmaram características estruturais presentes em caules e folhas, que já haviam sido descritas na literatura em análises morfonatômicas. Os extratos e frações de caules e folhas deste vegetal também não apresentaram toxicidade em métodos preliminares em Artemia salina e hemólise, sendo, de maneira geral, conisderados atóxicos nestes métodos, o que permite a sequência com estudos farmacológicos e toxicológicos que comprovem a segurança e eficácia destes extratos, para a obtenção de medicamentos fitoterápicos.

Lipid peroxidation inhibition by ethanolic extract and fractions from Rhamnus sphaerosperma var. pubescens (Reissek) M.C. Johnst. (Rhamnaceae)

Rhamnus sphaerosperma var. pubescens is a species native to Brazil, found in the southern region, and still there is no data in the literature about biological activities of this plant. Therefore, the aims of this study were to verify the antioxidant activity and determine the ability to inhibit lipid peroxidation of crude ethanolic extract and it fractions hexane, chloroform and ethyl acetate of the stem. The total antioxidant activity was evaluated by phosphomolybdenum complex method. And the ability to inhibit lipid peroxidation was evaluated, in vitro and in vivo experiments, by quantification of thiobarbituric acid reactive species formed from peroxidation induced. The in vitro test about lipoperoxidation, were used lipids obtained from egg yolk. And, for in vivo assay, the peroxidation was determined only for crude extract, using stomachs of female rats injured by administration of absolute ethanol. The samples of Rhamnus sphaerosperma var. pubescens demonstrated an important antioxidant capacity. In the phosphomolybdenum complex method, the chloroform fraction (86.4%) and ethyl acetate fraction (96.2%) showed the best activity than crude extract. For the in vitro induced lipid peroxidation, the chloroform (63.3%) and hexane (59.7%) fractions demonstrated high capacity in prevention of lipid oxidation. The crude extract showed effectiveness in both methods, and was used in the verification of inhibition of lipid peroxidation in vivo. In this test, the lesser dose tested, 20 mg/Kg, showed better effectiveness in inhibiting lipid oxidation, with reduction of 56.9%. Furthermore, was possible identify the stigmasterol and sitosterol as compounds of this plant. Rhamnus sphaerosperma var. pubescens stem possess potential antioxidant activity, reducing lipid peroxidation tested by in vitro and in vivo methods

Lipid peroxidation inhibition by ethanolic extract and fractions from Rhamnus sphaerosperma var. pubescens (Reissek) M.C. Johnst. (Rhamnaceae)

Rhamnus sphaerosperma var. pubescens is a species native to Brazil, found in the southern region, and still there is no data in the literature about biological activities of this plant. Therefore, the aims of this study were to verify the antioxidant activity and determine the ability to inhibit lipid peroxidation of crude ethanolic extract and it fractions hexane, chloroform and ethyl acetate of the stem. The total antioxidant activity was evaluated by phosphomolybdenum complex method. And the ability to inhibit lipid peroxidation was evaluated, in vitro and in vivo experiments, by quantification of thiobarbituric acid reactive species formed from peroxidation induced. The in vitro test about lipoperoxidation, were used lipids obtained from egg yolk. And, for in vivo assay, the peroxidation was determined only for crude extract, using stomachs of female rats injured by administration of absolute ethanol. The samples of Rhamnus sphaerosperma var. pubescens demonstrated an important antioxidant capacity. In the phosphomolybdenum complex method, the chloroform fraction (86.4%) and ethyl acetate fraction (96.2%) showed the best activity than crude extract. For the in vitro induced lipid peroxidation, the chloroform (63.3%) and hexane (59.7%) fractions demonstrated high capacity in prevention of lipid oxidation. The crude extract showed effectiveness in both methods, and was used in the verification of inhibition of lipid peroxidation in vivo. In this test, the lesser dose tested, 20 mg/Kg, showed better effectiveness in inhibiting lipid oxidation, with reduction of 56.9%. Furthermore, was possible identify the stigmasterol and sitosterol as compounds of this plant. Rhamnus sphaerosperma var. pubescens stem possess potential antioxidant activity, reducing lipid peroxidation tested by in vitro and in vivo methods