Department of Thoracic Surgery, Shanghai Chest Hospital Affiliated to Shanghai Jiao Tong University, Shanghai 200030, P.R. China.
Mol Med Rep. 2017 Nov;16(5):6483-6488. doi: 10.3892/mmr.2017.7453. Epub 2017 Sep 11.
Hyperoside (HY) is a major pharmacologically active component from Prunella vulgaris L. and Hypericum perforatum. The present study aimed to determine the anticancer effect of HY and determine the underlying mechanisms involved. Human A549 cells were treated with HY (10, 50 and 100 µM), and cell viability was detected by an MTT assay. Cell apoptosis and mitochondrial membrane potential were determined by flow cytometry. Western blot analysis was used to identify the expression of apoptosis‑associated proteins and phosphorylation of MAPK. The present study demonstrated that HY significantly inhibited the viability of A549 cells in a time‑ and dose‑dependent manner, and enhanced the percentage of apoptotic cells. HY also significantly increased the protein phosphorylation of p38 mitogen‑activated protein kinase (MAPK) and c‑Jun N‑terminal kinase (JNK), disrupted mitochondrial membrane penetrability, and triggered the release of mitochondrial cytochrome c and apoptosis‑inducing factor into the cytosol. Treatment with HY also activated the expression of caspase‑9 and caspase‑3. These results suggested that HY‑induced apoptosis was associated with activation of the p38 MAPK‑ and JNK‑induced mitochondrial death pathway. HY may offer potential for clinical applications in treating human non‑small cell lung cancer and improving cancer chemotherapy.
金丝桃苷（HY）是夏枯草和贯叶连翘中的一种主要的具有药理活性的成分。本研究旨在确定 HY 的抗癌作用，并确定涉及的潜在机制。用人 A549 细胞用 HY（10、50 和 100µM）处理，通过 MTT 法检测细胞活力。通过流式细胞术测定细胞凋亡和线粒体膜电位。Western blot 分析用于鉴定凋亡相关蛋白的表达和 MAPK 的磷酸化。本研究表明，HY 显著地抑制了 A549 细胞的活力，呈时间和剂量依赖性，并且增加了凋亡细胞的百分比。HY 还显著增加了 p38 丝裂原活化蛋白激酶（MAPK）和 c-Jun N-末端激酶（JNK）的蛋白磷酸化，破坏了线粒体膜的通透性，并触发了线粒体细胞色素 c 和凋亡诱导因子向细胞质的释放。HY 处理还激活了 caspase-9 和 caspase-3 的表达。这些结果表明，HY 诱导的细胞凋亡与 p38 MAPK 和 JNK 诱导的线粒体死亡途径的激活有关。HY 可能为治疗人类非小细胞肺癌和改善癌症化疗提供潜在的临床应用。
