Lyophilization of ImunoparvumR° as an alternative to reduce its side-effects

In Brazil, Imunoparvum R° is used as an immunomodulator. It is commercialized in 2 ml ampoules containing 2 mg of Propionebacterium acnes (formerly known as Corynebacterium parvum)/ml, in a 0.5 % phenol and 0.85% sodium chloride solution. High therapeutic power associated to minimum side effects is a great challenge to the pharmaceuticalindustry. Research results have shown that Imunoparvum R° induces side effects in humans and animals, probably because of its phenol content (SOUSA, 1993; RODRIGUES, 2001). The objective of this study was to determine the phenol content of lyophilized and non-lyophilized Imunoparvum R° and to compare their side effects in mice. It was demonstrated that the lyophilization process reduces the phenol content and the side effects of Imunoparvum R°, when compared to the commercialized Propionebacterium acnes suspension

Antimicrobial, Antiproliferative and Proapoptotic Activities of Extract, Fractions and Isolated Compounds from the Stem of Erythroxylum caatingae Plowman

In the study, we have examined the antitumor and antimicrobial activities of the methanol extract, the fractions, a fraction of total alkaloids and two alkaloids isolated from the stem of Erythroxylum caatingae Plowman. All test fractions, except the hexane fractions, showed antimicrobial activity on gram-positive bacteria and fungi. The acetate: methanol (95:5), acetate, chloroform and hexane fractions show the highest cytotoxicity activity against the NCI-H292, HEp-2 and K562 cell lines using MTT. The absence of hemolysis in the erythrocytes of mice was observed in these fractions and 6β-Benzoyloxy-3α-(3,4,5- trimethoxybenzoyloxy) tropane (catuabine B). Staining with Annexin V-FITC and JC-1 was used to verify the mechanism of action of the compounds of E. caatingae that showed cytotoxicity less than 30 μg/mL in leukemic cells. After 48 h of incubation, we observed that the acetate: methanol (95:5), acetate, and chloroform fractions, as well as the catuabine B, increased in the number of cells in early apoptosis, from 53.0 to 74.8%. An analysis of the potential of the mitochondrial membrane by incorporation of JC-1 showed that most cells during incubation of the acetate: methanol (95:5) and acetate fractions (63.85 and 59.2%) were stained, suggesting the involvement of an intrinsic pathway of apoptosis

In vitro and in vivo antitumor effects of the flavonol glycosides isolated of Herissantia crispa (L.) Brizicky

This paper describes the cytotoxic and antitumoral activities of kaempferol 3-O-(6”-O-E-pcoumaroyl)-β-D-glucopyranoside (tiliroside), kaempferol 3,7-di-O-α-L-rhamnoside (dhiramnoside) and of the mixture of sitosteryl-3-O-β-D-glucopyranoside and stigmasteryl-3-O-β-D-glucopyranoside (GM) isolated of the Herissantia crispa. The compounds did not present cytotoxic activity against NCI-H292, HEp-2 and KB cells. In vivo, dhiramnoside did not present significant inhibitory activity of the growth of sarcoma 180 when compared with the control group; however, tiliroside and GM-treated animals showed a high inhibition rate in the growth of the tumor. Tiliroside inhibits significantly the growth of the carcinoma of Ehrlich. In conclusion, tiliroside exhibited promising antitumor effects without an expressive toxicity.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Atividade antimicrobiana de Lippia alba (Mill.) N. E. Brown (Verbenaceae)

Lippia alba (Mill.) N. E. Brown (Verbenaceae), amplamente distribuída em todo o território brasileiro, é conhecida popularmente como erva cidreira e utilizada na medicina popular como analgésica, febrífuga, antiinflamatória, antigripal e nas afecções hepáticas. Extratos brutos foram preparados a partir de plantas cultivadas, de modo padronizado, em horta medicinal do Laboratório de Fitoterapia da Empresa Pernambucana de Pesquisa Agropecuária (IPA) para a verificação da atividade antimicrobiana, in vitro, pelo método de difusão em disco de papel. A concentração inibitória mínima (CIM) foi determinada para os extratos que exibiram melhores atividades. Os resultados obtidos mostraram que os extratos clorofórmico, acetônico e etanólico da raiz foram ativos frente a Staphylococcus aureus, Micrococcus luteus, Bacillus subtilis, Mycobacterium smegmatis, Candida albicans e Monilia sitophila e os extratos hexânicos, etanólicos e metanólicos das folhas inibiram S. aureus, M. luteus, B. subtilis, M. smegmatis e M. sitophila. A menor concentração inibitória (CIM = 31,2 µg/mL), foi obtida para o extrato clorofórmico da raiz frente a B. subtilis e M. luteus

Synthesis, cytotoxicity activity and acute toxicity evaluation of Primin analogues 3 and 6 alkyl-substituted

Foram obtidos análogos estruturais da primina via alquilação regioseletiva do composto 2-metoxihidroquinona. Compostos 3 e 6-alquil-2-metoxibenzoquinonas foram obtidos e submetidos a testes pré- clínicos com culturas de células. Testes in vivo para verificação da DL50 também foram realizados. Entre os compostos testados, o composto 6-metil-2-metoxi-1,4-benzoquinona apresentou maior atividade frente as células KB, DI50 =0,27 µg/ml. O teste de toxicidade aguda revelou que os novos compostos são menos tó- xicos que o protótipo, a primina, uma vez que a DL50 ficou entre 80-50 mg/Kg.3- and 6-alkyl-2-methoxy-1,4-benzoquinone derivatives primin analogues, were obtained by regioselective alkylation of 2-methoxyhydroquinone compounds. Tests were performed to evaluate the cytotoxicity activity with continuous chain KB cells (epidermoide carcinoma of the floor of the mouth). In this series 6- methyl-2-methoxy-1,4-benzoquinone was the most active that showed the highest inhibition on KB cells (DI50 = 0.27 µg/ml). All tested compounds were less toxic that primin (LD50 = 14 mg/Kg) precursory, in vivo tests of new compounds revealed a LD50 betwen 80-50 mg/Kg.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Synthesis, cytotoxicity activity and acute toxicity evaluation of Primin analogues 3 and 6 alkyl-substituted

Foram obtidos análogos estruturais da primina via alquilação regioseletiva do composto 2-metoxihidroquinona. Compostos 3 e 6-alquil-2-metoxibenzoquinonas foram obtidos e submetidos a testes pré- clínicos com culturas de células. Testes in vivo para verificação da DL50 também foram realizados. Entre os compostos testados, o composto 6-metil-2-metoxi-1,4-benzoquinona apresentou maior atividade frente as células KB, DI50 =0,27 µg/ml. O teste de toxicidade aguda revelou que os novos compostos são menos tó- xicos que o protótipo, a primina, uma vez que a DL50 ficou entre 80-50 mg/Kg.3- and 6-alkyl-2-methoxy-1,4-benzoquinone derivatives primin analogues, were obtained by regioselective alkylation of 2-methoxyhydroquinone compounds. Tests were performed to evaluate the cytotoxicity activity with continuous chain KB cells (epidermoide carcinoma of the floor of the mouth). In this series 6- methyl-2-methoxy-1,4-benzoquinone was the most active that showed the highest inhibition on KB cells (DI50 = 0.27 µg/ml). All tested compounds were less toxic that primin (LD50 = 14 mg/Kg) precursory, in vivo tests of new compounds revealed a LD50 betwen 80-50 mg/Kg.Colegio de Farmacéuticos de la Provincia de Buenos Aire