School of Pharmacy, Sungkyunkwan University, Suwon, 16419, Republic of Korea.
College of Korean Medicine, Gachon University, Seongnam, 461-701, Republic of Korea.
Arch Pharm Res. 2018 Aug;41(8):815-822. doi: 10.1007/s12272-018-1064-9. Epub 2018 Aug 14.
Identification of bioactive natural products with anticancer activity as well as alleviating effects on chemotherapy-induced side effects has significant implications for cancer treatment. Betula platyphylla var. japonica, commonly known as Asian white birch, has been used in Chinese traditional medicine for a variety of purposes. In this study, the medicinal properties of betulin from B. platyphylla var. japonica useful for cancer management were investigated. LC/MS analysis revealed that betulin is a main chemical component of the EtOH extract of B. platyphylla var. japonica bark, and betulin was isolated from EtOH extract using an LC/MS-guided isolation method. Its structure was identified with H and C NMR spectroscopic data and LC/MS analysis and then compared to the previously reported spectroscopic and physical data. We first verified the cytotoxicity of betulin against three human lung adenocarcinoma cell lines, A549, H1264, and Calu-6, with IC values ranging from 18.7 to 39.6 μM. Regarding alleviation of side effects associated with anticancer chemotherapy, betulin ameliorated cisplatin-induced renal cell damage to 80% of the control value from the concentration of 5 μM. In addition, betulin showed anti-gastritis activity against ethanol-induced gastric damage in rats and notably reduced the gastric damage index compared to control in a concentration-dependent manner. These findings provide the first experimental evidence for potential use of B. platyphylla var. japonica as a functional food for cancer treatment that simultaneously alleviates the side effects of chemotherapy.
鉴定具有抗癌活性以及缓解化疗副作用的生物活性天然产物对癌症治疗具有重要意义。白桦，俗称亚洲白桦，在中国传统医学中被用于多种用途。在这项研究中，研究了白桦中的桦木醇对癌症管理的药用特性。LC/MS 分析表明，桦木醇是白桦树皮乙醇提取物的主要化学成分，并且使用 LC/MS 引导的分离方法从乙醇提取物中分离出桦木醇。其结构通过 H 和 C NMR 光谱数据和 LC/MS 分析进行了鉴定，并与以前报道的光谱和物理数据进行了比较。我们首先验证了桦木醇对三种人肺腺癌细胞系 A549、H1264 和 Calu-6 的细胞毒性，IC 值范围为 18.7 至 39.6 μM。关于缓解与抗癌化疗相关的副作用，桦木醇将顺铂诱导的肾细胞损伤从 5 μM 浓度下的对照值的 80%改善至 80%。此外，桦木醇对乙醇诱导的大鼠胃炎具有抗胃炎活性，并且与对照组相比，其胃损伤指数呈浓度依赖性显著降低。这些发现为白桦作为治疗癌症的功能性食品的潜在用途提供了第一个实验证据，同时缓解了化疗的副作用。
