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Made available in DSpace on 2020-12-10T20:11:02Z (GMT). No. of bitstreams: 0 Previous issue date: 2020-09-01 Copaifera langsdorffiiL. is one of the most known medicinal species in Brazil. Its leaves are rich in phenolic compounds with potential biological activities as an antioxidant and chelating agent. This paper reports the isolation of four compounds from the hydroalcoholic extract of the leaves ofC. langsdorffiiand the investigation of their possible cytoprotective effects against heavy metal poisoning. Quercitrin (1), afzelin (2), 3,5-di-O-(3-O-methyl galloyl) quinic acid (3) and 4,5-di-O-(3-O-methyl galloyl) quinic acid (4), were associated with toxic doses of methylmercury and lead and evaluated by Alamar blue cell viability assays in HepG2 and PC12. The compounds displayed significant cytoprotective effect for the HepG2 cell line against both metals. Compounds 1-4 did not protect PC12 cells against methylmercury induced-cytotoxicity, but at lower concentrations, they protected against lead induced-cytotoxicity. The evaluated compounds showed a promising cytoprotection effect against exposure to heavy metals and should be further investigated as protective agents. Univ Sao Paulo, Dept Pharmaceut Sci, Ribeirao Preto, Brazil Sao Paulo State Univ, Dept Biol Sci, Araraquara, SP, Brazil Univ Sao Paulo, Dept Clin Toxicol & Bromatol Anal, Ribeirao Preto, Brazil Univ Franca, Nucleus Res Sci & Technol, Franca, SP, Brazil Sao Paulo State Univ, Dept Biol Sci, Araraquara, SP, Brazil

Propolis is one of the most widely used products in traditional medicine. One of the most prominent types of Brazilian propolis is the red one, whose primary botanical source is Dalbergia ecastaphyllum (L.) Taub. Despite the potential of Brazilian red propolis for developing new products with pharmacological activity, few studies guarantee safety in its use. The objective of this study was the evaluation of the possible toxic effects of Brazilian red propolis and D. ecastaphyllum, as well as the cytotoxicity assessment of the main compounds of red propolis on tumoral cell lines. Hydroalcoholic extracts of the Brazilian red propolis (BRPE) and D. ecastaphyllum stems (DSE) and leaves (DLE) were prepared and chromatographed for isolation of the major compounds. RP-HPLC-DAD was used to quantify the major compounds in the obtained extracts. The XTT assay was used to evaluate the cytotoxic activity of the extracts in the human fibroblast cell line (GM07492A). The results revealed IC50 values of 102.7, 143.4, and 253.1 μg/mL for BRPE, DSE, and DLE, respectively. The extracts were also evaluated for their genotoxic potential in the micronucleus assay in Chinese hamster lung fibroblasts cells (V79), showing the absence of genotoxicity. The BRPE was investigated for its potential in vivo toxicity in the zebrafish model. Concentrations of 0.8-6.3 mg/L were safe for the animals, with a LC50 of 9.37 mg/L. Of the 11 compounds isolated from BRPE, medicarpin showed a selective cytotoxic effect against the HeLa cell line. These are the initial steps to determine the toxicological potential of Brazilian red propolis.

Squarisi IS, De Freitas KS, Lemes DC, Ccana-Ccapatinta GV, Mejia JAA, Bastos JK, Veneziani RCS, Ambrosio SR, Tavares DC. 2018. Evaluation of the antiproliferative activity of red propolis hydroalcoholic extract and its fractions obtained by partition. Biofarmasi J Nat Prod Biochem 18: 66-69. The present study aimed to evaluate the cytotoxicity of red propolis hydroalcoholic extract (RPHE) and its fractions obtained by partition, hexanes (HF), dichloromethane (DF), ethyl acetate (AF) and n-butanol (BF), on tumor and non-tumor cell lines. For this purpose, the XTT colorimetric assay was performed on human lung fibroblasts (GM07492A, non-tumor cell), breast adenocarcinoma (MCF-7), glioblastoma (U343) and cervix adenocarcinoma (HeLa) cells. The results showed that RPHE, HF and DF presented not only cytotoxic potential to all tumor cell lines but also to normal cell line, indicating selectivity absence. HF presented the lowest IC50 (half minimal inhibitory concentration; 33.8-133.3 µg/mL), with significant difference from those observed for RPHE (137.0-262.7 µg/mL). BF and AF revealed an IC50 which was higher than 1250 µg/mL in all cell lines. The results showed that red propolis has substances with antiproliferative activity, indicating that its hexanes fraction may have substances with antitumor potential.