Chen Xiao-Xin, Lam Kar Ho, Chen Qing-Xi, Leung George Pak-Heng, Tang Sydney Chi Wai, Sze Stephen Cho-Wing, Xiao Jian-Bo, Feng Feng, Wang Ying, Zhang Kalin Yan-Bo, Zhang Zhang-Jin
School of Chinese Medicine, LKS Faculty of Medicine, University of Hong Kong, 10 Sassoon Road, Pokfulam, Hong Kong.
Key Lab of the Ministry of Education for Coastal and Wetland Ecosystems, School of Life Sciences, Xiamen University, Xiamen, China.
Food Chem Toxicol. 2017 Dec;110:49-61. doi: 10.1016/j.fct.2017.10.017. Epub 2017 Oct 10.
5-Fluorouracil (5-FU) is a commonly used chemotherapeutic agent for breast cancer. However, its use often leads to drug resistance and mucositis. This study aimed to investigate whether proanthocyanidins from Ficus virens possessed anti-breast cancer and anti-mucositis activities. The results showed that the cytotoxic effects of the proanthocyanidins against MDA-MB-231 and MCF-7 breast cancer cells were in the order of stem barks proanthocyanidins (SPAs) > leaves proanthocyanidins > fruits proanthocyanidins. Moreover, SPAs induced apoptosis in both cell lines which were accompanied with an increase in loss of mitochondrial membrane potential, production of reactive oxygen species, Bax to Bcl-2 protein expression ratio, and activated caspase 3. Furthermore, intraperitoneal injection of 5-FU (150 mg/kg body weight) resulted in body weight loss and jejunal injury in the rats while administration of SPAs (100 mg/kg body weight) counteracted these changes. Collectively, our study demonstrated that SPAs induced apoptosis cell death in breast cancer cells while ameliorating the symptoms of intestinal mucositis in rats.Therefore, SPAs merits further exploration as a potential therapeutic agent for breast cancer and chemotherapy-induced mucositis.
5-氟尿嘧啶（5-FU）是一种常用于治疗乳腺癌的化疗药物。然而，其使用常常导致耐药性和粘膜炎。本研究旨在调查垂叶榕原花青素是否具有抗乳腺癌和抗粘膜炎活性。结果表明，原花青素对MDA-MB-231和MCF-7乳腺癌细胞的细胞毒性作用顺序为：茎皮原花青素（SPAs）＞叶原花青素＞果实原花青素。此外，SPAs诱导两种细胞系凋亡，同时伴随着线粒体膜电位丧失、活性氧生成、Bax与Bcl-2蛋白表达比值增加以及caspase 3激活。此外，腹腔注射5-FU（150 mg/kg体重）导致大鼠体重减轻和空肠损伤，而给予SPAs（100 mg/kg体重）可抵消这些变化。总体而言，我们的研究表明，SPAs诱导乳腺癌细胞凋亡，同时改善大鼠肠道粘膜炎症状。因此，SPAs作为一种潜在的乳腺癌和化疗诱导粘膜炎治疗药物值得进一步探索。
