Design of antiseptic formulations containing extract of Plinia cauliflora / Concepção de formulações anti-sépticas que contenham extrato de Plinia cauliflora

The leaves of the Brazilian species Plinia cauliflora were used to obtain active hydroalcoholic extract and fractions enabling the development of efficient antiseptic pharmaceutical formulations. A chemical composition of 70 percent ethanol extract, aqueous and ethyl acetate fractions was analyzed by thin-layer chromatography and for phenol content. Antimicrobial activity was tested against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Lactobacillus acidophilus and Candida albicans by the agar diffusion method and the minimum inhibitory concentration was assayed by broth microdilution. Extract microbiological quality was tested to avoid contamination in the formulations. A mouthwash and a topical cream containing the extract were developed and antiseptic activity was assessed by agar diffusion. Sensory and physicochemical stability of the formulations were assayed. Chromatography indicated the presence of terpenes, flavonoids and tannins in the extract and fractions and total phenol content were found to be high. The plant samples were active against all the microorganisms tested, except for Lactobacillus acidophilus. Both topical formulations showed antiseptic activity and stability. Thus, these may be used as antimicrobials in skin infections, but would be more useful in the treatment of candidiasis.

As folhas da espécie brasileira Plinia cauliflora foram utilizadas a fim de se obter um extrato hidroalcoólico e frações ativas proporcionando o desenvolvimento de eficazes formulações farmacêuticas antissépticas. A composição química do extrato etanólico 70 por cento, fração aquosa e acetato de etila foi analisada por cromatografia em camada delgada e teor de fenóis. A atividade antimicrobiana foi testada frente a Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Lactobacillus acidophilus e Candida albicans por difusão em ágar e a concentração inibitória mínima foi determinada por microdiluição. A qualidade microbiológica do extrato foi avaliada para evitar a contaminação das formulações. Foram desenvolvidos um enxaguatório bucal e um creme tópico contendo o extrato sendo que a atividade antisséptica foi ensaiada por difusão em ágar. A estabilidade sensorial e físico-química foram testadas. A cromatografia indicou a presença de terpenos, flavonóides e taninos no extrato e frações, observando-se alto teor de fenóis totais. As amostras vegetais foram ativas contra todos os micro-organismos testados, exceto Lactobacillus acidophilus. Ambas as formulações apresentaram atividade antisséptica e estabilidade. Desta forma, infere-se que as formulações desenvolvidas podem ser utilizadas como antissépticas em infecções de pele, podendo ser mais eficazes no tratamento de candidíase.

Humoral and cellular immune responses induced in mice by purified iridoid mixture that inhibits penetration of schistosoma mansoni cercariae upon topical treatment of mice tails

When tested for possible blocking effect on the cercarial, serine proteinase, elastase [CE] activity, an iridoid mixture extracted from leaves of Citharexylum quadrangular abolished 31% of the enzyme activity at final concentration l5 micro g. When formulated in jojoba oil and applied to mice tails followed by infection with Schistosoma mansoni cercariae, the iridoid mixture blocked cercarial penetration and caused significant reducetion [94%; P < 0.05] in worm burden in treated mice in comparison to controls. Also, immunomodulatory effects of iridoid mixture, iridoid-treated S. mansoni worm homogenate on mice were studied by measuring IgG and IgM levels against E. coil lysates [ECL], solube S. mansoni worm antigenic preparation [SWAP] and cancer bladder homogenates [CBH] as antigens by ELISA. Cellular immune responses were studied by calculating mean percent of CD4+, CD8 +/- T, B-mesenteric lymph node cells [MLNC] and CD4+, CD8 +/- T thymocytes by direct immuno-fluorescence staining in treated mice as compared to untreated homogenate given mice or untreated mice. Injecting mice with serial dilutions of iridoid mixture resulted in fluctuation, peaks and troughs, in both IgG and IgM responses against the above mentioned antigens. lst and 2nd immunizations with iridoid mixture treated homogenate resulted in significantly elevated [P < 0.05]. 1gM and IgG levels against the 3 used antigens in comparison with sera from control mice. Immunized mice with homogenate treated with iridoid mixture showed a significant increase [P < 0.05] in CD4+T thymocytes, a non significant increase in CD8+T thymocytes, a significant increase [P<0.05] in CD4+T lymphocytes [MLNC] and a non significant increase in CD8+T- and B-lymphocytes [MLNC] compared with mice immunized with untreated homogenate or non-injected normal mice