Navegando por Palavras-chave "Cytotoxic"
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- ItemAcesso aberto (Open Access)Análise fitoquímica de Ocotea odorifera (Lauraceae), Piper leavicarpu (Piperaceae) e avaliação da atividade biológica dos metabolitos isolados(Universidade Federal de São Paulo, 2014-03-14) Maciel, Dayany da Silva Alves [UNIFESP]; Lago, João Henrique Ghilardi [UNIFESP]; Universidade Federal de São Paulo (UNIFESP)Ocotea odorifera (Lauraceae) is popularly known as “sassafras” or “sassafras-cinnamon” while Piper laevicarpu (Piperaceae) is known as “falsa-pimenteira”. These two species are from the Brazilian Atlantic Forest biome. Previous studies conducted in our laboratory showed that the methanol extract of aerial parts of O. odorifera and dichloromethane extract of the leaves of P. laevicarpu exhibit antitumor and antiparasitic activity, respectively. Thus, in this study, the phytochemical analysis of these extracts biological monitoring aimed to isolate and identify the compounds that are cytotoxic activity for B16F10 Nex2 (murine melanoma) in O. odorifera, and P. laevicarpu antileishmanial and antitrypanosomal activity. For this purpose, the crude extracts were individually subjected to different chromatographic procedures (SiO2 normal phase and Sephadex LH-20). In these processes, five compounds were identified with cytotoxic activity in O. odorifera 1 (eugenol), a mixture of 2 + 3 (4-allyl-2,6-dimethoxyphenol and dioctyl adipate), 4 (isoeugenil acetate) and 5 (sitosterol), 1 and 2 have not yet been previously described in the species under study. In P. laevicarpu was isolated new compound a cyclic amide laevicarpin (6) as natural product, which noted a great potential antiparasitic in vitro. For this substance, the potential for a trypomastigote forms of T. cruzi showed IC50 values determined as 14.75 µM/mL is indicative of excellent activity for T. cruzi with low toxicity compared to positive control benznidazole (42.5 M/mL). These result showed the presence of species in the molecules under study can be used as a prototype for the development of new drugs with anti-tumor and / or anti-parasitic action. .
- ItemAcesso aberto (Open Access)Avaliação da atividade herbicida e citotóxica de produtos naturais de Pluchea sagitallis (asteraceae) e seus derivados sintéticos(Universidade Federal de São Paulo, 2016-07-06) Carvalho, Ana Calheiros de [UNIFESP]; Veiga, Thiago André Moura [UNIFESP]; Universidade Federal de São Paulo (UNIFESP)In this proposal, the herbicide potential of the substances isolated from extracts of the roots of Pluchea sagittalis (Asteraceae) has been studied, a species collected in the area of the copper department of Mina do Sossego, VALE S.A, Canaã dos Carajás - PA. The initial chemical study of that plant drove to the isolation of four compounds: 3,5-dihydroxy-6,7,3', 4'-tetramethoxiflavunol (1), 3,4-dimethoxybenzaldehyde (2), 2,3,4-trihydroxybenzaldeyde (3) 5-hydroxymethylfurfural (4). These metabolites were subjected to in vitro photosynthesis inhibition assays and presented moderate activities. The compound (2) was commercially obtained, as well as its structurally similar derivative, the isovanillin (5), to modify their structures after synthetic procedures. The methods of synthesis allowed to obtain twenty derivatives (6 - 25). The purpose of these transformations is to establish a comparison of the herbicidal activity among natural products and their derivatives, allowing the design of new prototypes for photosynthesis inhibitors. With this same objective, in parallel, the synthetic derivatives, the isolated compound (2) and its structural derivative (5) were evaluated for cytotoxic activity against the following cell lines: B16F10-Nex2 (murine melanoma); HL-60 (human leukemia); MCF-7 (human breast adenocarcinoma); A2058 (human metastatic melanoma); HeLa (human cervical adenocarcinoma); T75 (non-tumorigenic cell). The isolated compounds contributed to the knowledge of some chemical components of the species. The structural changes and biological results can contribute to the design of new herbicides and cytotoxic agents.
- ItemSomente MetadadadosChemical Composition and in vitro Cytotoxic and Antileishmanial Activities of Extract and Essential Oil from Leaves of Piper cernuum(Natural Products Inc, 2015-02-01) Capello, Tabata Molero [UNIFESP]; Martins, Euder Glendes Andrade; Farias, Camyla Fernandez de [UNIFESP]; Figueiredo, Carlos Rogerio [UNIFESP]; Matsuo, Alisson Leonardo [UNIFESP]; Passero, Luiz Felipe Domingues; Oliveira-Silva, Diogo [UNIFESP]; Sartorelli, Patricia [UNIFESP]; Lago, Joao Henrique Ghillardi [UNIFESP]; Universidade Federal de São Paulo (UNIFESP); Universidade de São Paulo (USP)Fractionation of the MeOH extract from leaves of Piper cernuum Veil. (Piperaceae) afforded six phenylpropanoid derivatives: 3',4'-dimethoxydihydrocinnamic acid (1), piplaroxide (2), methyl 4'-hydroxy-3',5'-dimethoxy cinnamate (3), 3',4',5'-trimethoxydihydrocinnamic acid (3), dihydropiplartine (5), and piplartine (6). The structures of isolated metabolites were characterized by NMR and MS spectral data analysis. The chemical composition of essential oil from the leaves was determined using GC/LREIMS followed by the determination of Kovats indexes. This procedure allowed the identification of nineteen terpenoids, with beta-elemene (7), bicyclogermacrene (8), germacrene D (9), and (E)-caryophyllene (10) as the main compounds. Compounds 1 and 3-6 displayed no in vitro cytotoxicity against cancer cell lineages B16F10-Nex2, U87, HeLa, HL-60, HCT, and A2058 while 2 showed moderate activity against B16F10-Nex2 and HL-60 lines. Otherwise, compounds 7-10 displayed high cytotoxic activity. Evaluation against non-tumorigenic HFF cells indicated a reduced selectivity of compounds 7-10 to tumoral cells. No antileishmanial activity on macrophages infected with L. (L.) amazonensis was found for the crude MeOH extract and compounds 1-6. The crude essential oil and compounds 7-10 reduced parasitism and eliminated the majority of infected and non-infected cells at 50 mu g/mL.