Department of Gynecology, The Affiliated Hospital of Qingdao University, Qingdao, China.
Eur Rev Med Pharmacol Sci. 2018 Apr;22(8):2356-2363. doi: 10.26355/eurrev_201804_14827.
To investigate the anti-tumor effect of acridone against breast cancer in vivo and provide a therapeutic agent for treatment of breast cancer.
The nude mice xenografted tumor model was established by MCF-7 cells. The mice were randomly divided into four groups. The mice in each group (n=6) were intraperitoneally injected with 0.1 mg/kg saline (low-dose), 0.5 mg/kg (middle-dose) and 1.0 mg/kg (high-dose) of acridone for 21 days, respectively. At the end of the animal experiment, the weight of tumors was recorded to calculate the tumor inhibition rate. The serum hormone levels in peripheral blood were determined using ELISA. Hematoxylin and eosin (HE) staining was used to analyze the histopathological changes. The expression of ABCG2 protein and mRNA were determined by Western blot and RT-PCR, respectively.
The inhibition rates of tumor growth in the high-dose, middle-dose, and low-dose groups were 29.18%, 17.21%, and 4.27%, respectively. Compared with control and low-dose group, the tumors growth rate in high-dose and middle-dose groups were decreased significantly. Histologically, the tumors were inhibited in the growth rate, the tissue structure was broken. Estrogen in all groups with acridone treatment decreased, the progesterone in high-dose and middle-dose groups increased remarkably. The expression of ABCG2 protein and ABCG2 mRNA decreased after treatment with acridone.
We showed that acridone could induce cell apoptosis, inhibited ABCG2 (ATP-binding cassette sub-family G member 2) protein and adjusted hormone level. The results suggested that acridone could serve as a chemotherapeutic agent for treatment of breast cancer in vivo.
研究吖啶酮体内抗乳腺癌作用，为乳腺癌的治疗提供治疗剂。
采用 MCF-7 细胞建立裸鼠异种移植肿瘤模型。将小鼠随机分为 4 组，每组 6 只。每组小鼠分别腹腔注射 0.1mg/kg 生理盐水（低剂量组）、0.5mg/kg（中剂量组）和 1.0mg/kg（高剂量组）的吖啶酮，连续给药 21 天。动物实验结束时，记录肿瘤重量，计算肿瘤抑制率。采用 ELISA 法检测外周血中激素水平。采用苏木精-伊红（HE）染色分析组织病理学变化。采用 Western blot 和 RT-PCR 分别检测 ABCG2 蛋白和 mRNA 的表达。
高剂量组、中剂量组和低剂量组的肿瘤生长抑制率分别为 29.18%、17.21%和 4.27%。与对照组和低剂量组相比，高剂量组和中剂量组的肿瘤生长速度明显降低。组织学上，肿瘤生长速度受到抑制，组织结构被破坏。各组用吖啶酮处理后，雌激素降低，高剂量组和中剂量组孕激素显著增加。吖啶酮处理后 ABCG2 蛋白和 ABCG2mRNA 的表达降低。
我们表明吖啶酮可诱导细胞凋亡，抑制 ABCG2（ATP 结合盒亚家族 G 成员 2）蛋白并调节激素水平。结果表明，吖啶酮可作为体内治疗乳腺癌的化疗药物。
