Analgesic and anti-inflammatory activities of the 2,8-dihydroxy-1,6-dimethoxyxanthone from Haploclathra paniculata (Mart) Benth (Guttiferae).

In the present study, the pharmacological effects of 2,8-dihydroxy-1,6-dimethoxyxanthone from the bark of Haploclathra paniculata were investigated in mice using in vivo inflammation and nociception models. Acetic acid-induced writhing, paw licking induced by formalin, hot plate, and carrageenan-induced paw edema tests were used to investigate the anti-inflammatory and antinociceptive activities of the xanthone compound. Xanthone, at both doses, inhibited abdominal writhing and the formalin test. At a dose of 20 mg/kg, the time of reaction to the hot plate increased, and significant effects were observed after 30, 60 and 90 min of treatment. At doses of 10 and 20 mg/kg p.o., the 2,8-dihydroxy-1,6-dimethoxyxanthone significantly reduced paw edema at 3 h after the stimulus. The tests also showed no acute toxicity of the xanthone compound in mice. 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging ability was also studied and confirmed the antioxidant activity of the xanthone. To propose the mechanism of action of anti-inflammatory activity of the xanthone, a molecular docking was performed using the isoenzymes cyclooxygenase 1 and 2 and the results indicate that the molecule is capable of inhibiting both the enzymes. Therefore, it can be concluded that 2,8-dihydroxy-1,6-dimethoxyxanthone from H. paniculata demonstrates analgesic, anti-inflammatory, and antioxidant activities.

Atividade antifúngica das folhas de Cissus verticillata (L.) Nicolson & C. E. Jarvis subsp. verticillata frente a Candida albicans, Candida krusei, Candida parapsilosis e Candida tropicalis / Antifungal activity of the leaves of Cissus verticillata (L.) Nicolson & C. E. Jarvis subsp. verticillata against Candida albicans, Candida krusei, Candida parapsilosis and Candida tropicalis

A espécie vegetal Cissus verticillata (L.) Nicolson & C. E. Jarvis subsp. verticillata é conhecida como "Insulina vegetal" eutilizada na medicina popular no tratamento da diabetes mellitus. O paciente diabético tem maior risco de infecções urinárias e Candida spp. é o principal gênero envolvido. Avaliou-se a atividade antifúngica do extrato hidroalcoólico e de suas frações frente aCandida albicans ATCC 18804, Candida krusei ATCC 6258, Candida parapsilosis ATCC 22019 e Candida tropicalis ATCC 750. Os resultados obtidos indicaram que folhas de C. verticillata verticillata têm potencial antifúngico promissor nas frações diclorometano e clorofórmio, com concentração inibitória mínima de 125 μg/mL em C. krusei e em C. tropicalis respectivamente. São necessários novos testes com constituintes químicos isolados dessas frações, buscando atividade superior na inibição do crescimento de Candida spp.

The specie Cissus verticillata (L.) Nicolson & C. E. Jarvis subsp. verticillata is known as "Vegetable insulin" and is used in popular medicine for the treatment of diabetes mellitus. The diabetic patient has a greater risk of urinary infections, and Candida spp. is the main gender involved. Was evaluated, the antifungal activity of the hydroalcoholic extract and its fractions against Candida albicans ATCC 18804, Candida krusei ATCC 6258, Candida parapsilosis ATCC 22019 and Candida tropicalis ATCC 750. The results indicated that leaves of C. verticillata verticillata has promising potential antifungal in fractions diclormetano andchloroform, with minimum inhibitory concentration of 125 μg/mL in C. krusei and C. tropicalis respectively. We need new tests with chemical constituents of these fractions isolated, seeking higher activity in inhibiting the growth of Candida spp.

Antiproliferative effect of benzophenones and their influence on cathepsin activity.

The antiproliferative activity of two prenylated benzophenones isolated from Rheedia brasiliensis, the triprenylated garciniaphenone and the tetraprenylated benzophenone 7-epiclusianone, was investigated against human cancer cell lines. The antiproliferative activity on melanoma (UACC-62), breast (MCF-7), drug-resistant breast (NCI-ADR), lung/non-small cells (NCI460), ovarian (OVCAR 03), prostate (PC03), kidney (786-0), lung (NCI-460) and tongue (CRL-1624 and CRL-1623) cancer cells was determined using spectrophotometric quantification of the cellular protein content. The effect of these benzophenones on the activity of cathepsins B and G was also investigated. Garciniaphenone displayed cytostatic activity in all cell lines, whereas 7-epiclusianone showed a dose-dependent cytotoxic effect. The IC(50) values for cell proliferation revealed that 7-epiclusianone is more active than garciniaphenone against most of the cell lines. Furthermore, the antiproliferative effects demonstrated by garciniaphenone and 7-epiclusianone were related to their cathepsin inhibiting properties. In conclusion, 7-epiclusianone is a promising naturally occurring agent which displays multiple inhibitory effects which may be working in concert to inhibit cancer cell proliferation in vitro. The putative pathway by which 7-epiclusianone affects cancer cell development may involve cathepsin inhibition.

Influência de tinturas de fruto cereja e verde de café no tratamento do Diabetes / Influences of teinturerie of fruits cherry and green the coffee trait the Diabetes

O consumo de café tem sido associado a menor risco de diabetes. Entretanto, os compostos específicos e os mecanismos responsáveis por este efeito ainda não estão claros. Realizou-se um experimento para avaliar o efeito das tinturas de casca de cereja, fruto verde e fruto cereja da planta café (Coffea arabica L.) da variedade Catuai Vermelho em ratos com Diabetes induzido por aloxano. Após 30 dias de tratamento, foram coletados amostras de sangue dos animais para dosagens séricas de glicose, colesterol e triglicerídeos. As tinturas de casca cereja (1,0 mL), fruto verde (0,5 mL e 2,0 mL) e fruto cereja (1,0 mL e 2,0 mL) promoveram aumento significativo nos níveis de colesterol quando comparado ao grupo doente não tratado. Com relação aos níveis de glicose e triglicérideos, observou-se que todas as tinturas reduziram significativamente os valores séricos destes parâmetros. As percentagens de redução das concentrações de glicose e triglicérides variaram entre -28% a -49% e -27% a -47%, respectivamente. A diminuição dos níveis de glicose e triglicerídeos se sobrepõe ao aumento observado do colesterol, indicando que estas tinturas podem ser promissoras como adjuvantes no tratamento da diabetes.

Flavonóides e seu potencial terapêutico: [revisão] / Flavonoids and potential therapeutic: [review]

Entre os fitoterápicos atualmente estudados, os flavonóides têm merecido destaque em virtude de sua ampla gama de ações terapêuticas já demonstradas tanto experimentalmente quanto em humanos. Seu uso para tratamento de sintomas da menopausa tem levado ao consumo indiscriminado, por mulheres nessa faixa de idade e, além disso foram demonstrados efeitos antimicrobiano, antiviral, antiulcerogênico, antineoplásico, antioxidante, antihepatotóxico, antihipertensivo, hipolipidêmico, antiinflamatório, antiplaquetário. Dessa forma, pareceu im-portante apresentar informações sobre os flavonóides, abordando sua ocorrência na natureza, estrutura química, atividade biológica e mecanismo de ação.

Efeito de rutina sobre os níveis de cloreto, cálcio e fósforo em soro de coelhos / Effects of differents rutin dosages on chloride, calcium and phosphorum levels in serum of rabbits

The objective of this research was to evaluate in rabbits the effect of different dosages rutin in seric levels of chloride, calcium and phosphoro. Rabbits of New Zealand strain aged 55 days of age were used. The animals were divides in males and females, being constituted 4 groups by sex, containing each one 5 animals, that received rutin in the dosages of 20, 40 and 60 mg. The controls groups received only the ration. Samples of blood were collected by retro-orbital vein plexo puncture being then centrifuged at 3500 x g for 15 minutes and serum measurement determined in a multiparametric doage of biochemistry (Alizé). For chloride results it was observed that rutin in the tested doses were significant for males although the variations were not considered toxic. It was also observed that the males presented significant values in dosis of 20 mg of rutin when compared with the females. Being analyzed the medium sanguine values of match and being compared males and female, significant differences were verified with the group that received 20 mg of rutin. Whith relatonship at the levels of calcium, this didn´t present significant alterations when we compared male and females. The females submitted to 20 mg rutin presented altered calcium levels, however those alterations did not present omportant physiologic significance once the other doses didn´t act in significant variations in the levels of calcium. It is concluded that the presented variations were not considered toxic for the parameters chloride, calcium and match in the blood of rabbits.

Atividade antimicrobiana em xantonas / Antimycrobial activity in xanthones

Cerca de treze xantonas isoladas de duas espécies do gênero Haploclathra foram submetidos à açäo de microorganismos-teste. Foram eleitos um fungo (Thielaviopsis paradoxa), uma bactéria Gram-positiva (Corynebacterium michiganense pv michiganense) e uma bactéria Gram-negativa (Pseudomonas syringae pv pisi). Nenhuma das xantonas testadas apresentou resultados positivos na inibiçäo do crescimento dos microorganismos em questäo.