ABSTRACT

Copaifera langsdorffii Desf. is a plant found in South America, especially in Brazil. Oleoresin and the leaves of this plant is used as a popular medicinal agent. However, few studies on the chemical composition of aerial parts and related biological activities are known. This study aimed to examine the cytotoxic, genotoxic, and antigenotoxic potential of C. langsdorffii aerial parts hydroalcoholic extract (CLE) and two of its major compounds afzelin and quercitrin. The cytotoxic and antigenotoxic potential of CLE was determined as follows: 1) against genotoxicity induced by doxorubicin (DXR) or methyl methanesulfonate (MMS) in V79 cells; 2) by direct and indirect-acting mutagens in Salmonella typhimurium strains; and 3) by MMS in male Swiss mice. The protective effects of afzelin and quercitrin against DXR or MMS were also evaluated in V79 and HepG2 cells. CLE was cytotoxic as evidenced by clonogenic efficiency assay. Further, CLE did not induce a significant change in frequencies of chromosomal aberrations and micronuclei; as well as number of revertants in the Ames test demonstrating absence of genotoxicity. In contrast, CLE was found to be antigenotoxic in mammalian cells. The results also showed that CLE exerted inhibitory effect against indirect-acting mutagens in the Ames test. Afzelin and quercitrin did not reduce genotoxicity induced by DXR or MMS in V79 cells. However, treatments using afzelin and quercitrin decreased MMS-induced genotoxicity in HepG2 cells. The antigenotoxic effect of CLE observed in this study may be partially attributed to the antioxidant activity of the combination of major components afzelin and quercitrin.

摘要

Copaifera langsdorffii Desf。是一种在南美洲发现的植物，尤其是在巴西。油树脂和这种植物的叶子被用作流行的药物。然而，关于地上部分的化学成分和相关生物活动的研究很少。本研究旨在检查C. langsdorffii地上部分水醇提取物 (CLE) 及其两种主要化合物黄柏素和槲皮素的细胞毒性、基因毒性和抗原毒性潜力。CLE 的细胞毒性和抗原毒性潜力测定如下：1) 对 V79 细胞中由阿霉素 (DXR) 或甲磺酸甲酯 (MMS) 诱导的基因毒性；2) 通过鼠伤寒沙门氏菌中的直接和间接诱变剂菌株; 3) 通过 MMS 在雄性瑞士小鼠中。还在 V79 和 HepG2 细胞中评估了 afzelin 和 quercitrin 对 DXR 或 MMS 的保护作用。如克隆形成效率测定所证明的，CLE具有细胞毒性。此外，CLE 没有引起染色体畸变和微核频率的显着变化；以及 Ames 试验中证明不存在遗传毒性的回复突变体的数量。相比之下，发现 CLE 在哺乳动物细胞中具有抗原毒性。结果还表明，CLE 在 Ames 试验中对间接作用诱变剂具有抑制作用。Afzelin 和槲皮素不会降低 DXR 或 MMS 在 V79 细胞中诱导的基因毒性。然而，使用 afzelin 和 quercitrin 的治疗降低了 MMS 诱导的 HepG2 细胞的基因毒性。