Department of Biochemistry, Universidade Federal de Santa Catarina, Florianopolis, Brazil.
Pharm Biol. 2013 Jun;51(6):737-43. doi: 10.3109/13880209.2013.764331. Epub 2013 Apr 9.
Croton celtidifolius Baill (Euphorbiaceae) is a tree found in the Atlantic Forest in Southern Brazil, where it is commonly known as "Sangue-de-Dragão". Its red latex is used traditionally for treating ulcers, diabetes and cancer.
To evaluate antitumor activities of Croton celtififolius latex in vitro and in vivo.
Phytochemical analyses were conducted using HPLC-DAD-MS. Cytotoxic, nuclease and pro-apoptotic properties were determined using the tetrazolium salt assay (MTT), plasmid DNA damage assay and ethidium bromide (EB)/acridine orange methods, respectively, and antitumor activity was determined in the Ehrlich ascites carcinoma (EAC) mouse model.
Phytochemical studies indicated a high phenol content of flavonols (45.67 ± 0.24 and 18.01 ± 0.23 mg/mL of myricetin and quercetin, respectively) and flavan-3-ols (114.12 ± 1.84 and 1527.41 ± 16.42 mg/L of epicatechin and epigallocatechin, respectively) in latex. These compounds reduced MCF-7 and EAC cell viability in the MTT assay (IC50 = 169.0 ± 1.8 and 187.0 ± 2.2 μg/mL, respectively). Latex compounds caused significant DNA fragmentation and increased the number of apoptotic cells (negative control (NC), 12%; latex, 41%) as indicated by differential staining in the EB/acridine orange assay. The in vivo latex treatment at 3.12 mg/kg/day reduced the body weight by 7.57 ± 2.04 g and increased median survival time to 17.5 days when compared to the NC group (13.0 days). In addition, the highest latex concentration inhibited tumor growth by 56%.
These results agree with ethno-pharmacological reports showing cytotoxicity and antitumor activity of C. celtidifolius latex. The mechanism of antitumor action may be related to direct DNA fragmentation that reduces survival and induces apoptosis.
巴伊亚克罗顿 Celtidifolius（大戟科）是一种树在南里奥格兰德州的大西洋森林中发现，在那里它通常被称为“ Sangue-de-Dragão ”。其红色乳液被传统上用于治疗溃疡，糖尿病和癌症。
评价巴伊亚克罗顿 Celtidifolius 乳液的体外和体内抗肿瘤活性。
采用高效液相色谱 - 二极管阵列 - 质谱联用进行植物化学分析。使用噻唑盐比色法（MTT ）测定细胞毒性，核酸酶和促凋亡特性，用溴化乙锭（EB ）/吖啶橙法分别测定质粒 DNA 损伤，并用艾氏腹水癌（EAC ）小鼠模型测定抗肿瘤活性。
植物化学研究表明，乳液中类黄酮（杨梅素和槲皮素分别为 45.67 ± 0.24 和 18.01 ± 0.23mg / mL ）和黄烷 - 3-醇（表儿茶素和表没食子儿茶素分别为 114.12 ± 1.84 和 1527.41 ± 16.42mg / L ）的酚类含量较高。这些化合物在 MTT 测定中降低了 MCF-7 和 EAC 细胞活力（IC50 = 169.0 ± 1.8 和 187.0 ± 2.2μg / mL ）。乳液化合物引起明显的 DNA 片段化，并增加吖啶橙 / EB 染色差异指示的凋亡细胞数（阴性对照（NC ），12 ％;乳液，41 ％）。体内治疗以 3.12mg / kg /天的剂量进行，与 NC 组（13.0 天）相比，体重减轻 7.57 ± 2.04g ，中位生存时间延长至 17.5 天。此外，最高浓度的乳液抑制肿瘤生长 56 ％。
这些结果与民族药理学报告一致，表明巴伊亚克罗顿 Celtidifolius 乳液的细胞毒性和抗肿瘤活性。抗肿瘤作用的机制可能与直接导致 DNA 片段化有关，从而降低生存并诱导凋亡。
