O latex de Euphorbia conspicua foi fracionado nas frações triterpênica e irritantes I e II. Da fração triterpênica foram isolados 15 compostos já conhecidos e um novo triterpeno denominado 3β-(E)-cinamoileuforbol. A fração irritante II forneceu o 20-O-acetil-3-O-angeloil-ingenol. A atividade moluscicida dos compostos eufol, 3β-acetoxieufa-8,24-dieno, 3β-(E)-cinamoileuforbol e 20-O-acetil-3-O-angeloil-ingenol foi avaliada. O 20-O-acetil-3-O-angeloil-ingenol apresentou uma LC 100 de 1 mg mL -1 , a qual foi equivalente ao moluscicida padrão niclosamida. Os compostos eufol, 3β-acetoxieufa-8,24-dieno e 3β-(E)-cinamoileuforbol apresentaram uma fraca atividade moluscicida. O 3β-(E)-cinamoileuforbol foi submetido a testes de mutagenicidade (teste de Ames com TA 98, 100 e 102) na presença e ausência de ativação metabólica (mistura S9). Foram também realizados os ensaios de citotoxicidade (teste MTT) e genotoxicidade (teste dos micronúcleos, CBMN) com e sem mistura S9, em células V79 de Hamster chinês. O 3β-(E)-cinamoileuforbol revelou-se fracamente citotóxico e sem atividade mutagênica ou genotóxica.Euphorbia conspicua latex was fractionated into triterpenic and irritant fractions I and II. The triterpenic fraction afforded 15 known compounds and a new triterpene, 3β-(E)-cinnamoyleuphorbol. 20-O-Acetyl-3-O-angeloylingenol was isolated from irritant fraction II. The compounds euphol, 3β-acetoxyeupha-8,24-diene, 3β-(E)-cinnamoyleuphorbol and 20-O-Acetyl-3-O-angeloylingenol were evaluated for molluscicidal activity. 20-O-Acetyl-3-O-angeloylingenol presented LC 100 value of 1 mg mL -1 , equivalent to that of the standard molluscicide niclosamide. Compounds euphol, 3β-acetoxyeupha-8,24-diene and 3β-(E)-cinnamoyleuphorbol showed low molluscicidal activity. Mutagenic assays (Ames test with strains TA 98, 100 and 102) were performed with 3β-(E)-cinnamoyleuphorbol in the presence and absence of metabolic activation (S9 mix). In V79 cells, the cytotoxicity of 3β-(E)-cinnamoyleuphorbol was evaluated using the MTT assay and the genotoxicity was assessed using the cytokinesis-block micronucleus assay (CBMN) with or without S9 mix. Mutagenic or genotoxic activity was not detected, and no significant cytotoxicity was observed for 3β-(E)-cinnamoyleuphorbol at lower doses.
Três novos labdanos com anel 8α,15-epoxi [8α,15-epoxilabdan-16β-oato de metila, 8α,15-epoxilabdan-16β-ol e 8α,15-epoxi-16-norlabdan-13β-ol] e cinco compostos conhecidos [8α,15-epoxi-16-norlabdan-13-ona, ácido 8α,15-epoxilabdan- Three new labdanes with 8α,15-epoxy ring [methyl 8α,15-epoxylabdan-16β-oate, 8α,15-epoxylabdan-16β-ol and 8α,15-epoxy-16-norlabdan-13β-ol] and five known compounds [8α,15-epoxy-16-norlabdan-13-one, 8α,15-epoxylabdan-16β-oic acid, 3β-(3'',4''-dihydroxy)-(E)-cinnamoyloxylup-20(29)-ene, 3-(2',3',4',6'-tetra-O-acetyl-β-D-glucopyranosyloxy)-β-sitosterol and 16-acetoxy-8α,15-epoxylabdane] were isolated from toluene and dichloromethane extracts of aerial parts of Eragrostis viscosa. The structures of all the compounds were established based on their spectroscopic data and X-ray diffraction analysis of 8α,15-epoxylabdan-16β-ol. It was also studied the genotoxicity of E. viscosa, particularly compounds 16-acetoxy-8α,15-epoxylabdane, 8α,15-epoxy-16-norlabdan-13-one and 8α,15-epoxilabdan-16β-ol, using a cytokinesis-block micronucleus assay and the Ames test to assess mutagenicity. Both assays were negative. Cytotoxicity was also analyzed using an MTT assay, and 8α,15-epoxy-16β-ol was shown to be the most cytotoxic of the compounds tested. E. viscosa extracts were also tested to determine their antioxidant capacities, peroxide values and total phenolic contents.
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