Park Eun-Ji, Lee Dahae, Baek Seon-Eun, Kim Ki Hyun, Kang Ki Sung, Jang Tae Su, Lee Hye Lim, Song Ji Hoon, Yoo Jeong-Eun
Department of Obstetrics and Gynaecology, College of Korean Medicine, Daejeon University, Daejeon 35235, Republic of Korea.
College of Korean Medicine, Gacheon University, Seongnam 13120, Republic of Korea; School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea.
Bioorg Med Chem Lett. 2017 Sep 15;27(18):4389-4392. doi: 10.1016/j.bmcl.2017.08.019. Epub 2017 Aug 12.
Sanguiin H-6 is a dimer of casuarictin linked by a bond between the gallic acid residue and one of the hexahydroxydiphenic acid units. It is an effective compound extracted from Rubus coreanus. It has an anticancer effect against several human cancer cells; however, its effect on breast cancer cells has not been clearly demonstrated. Thus, we aimed to investigate the anticancer effect and mechanism of action of sanguiin H-6 against two human breast carcinoma cell lines (MCF-7 and MDA-MB-231). We found that sanguiin H-6 significantly reduced cell viability in a concentration-dependent manner. It also increased the rates at which MCF-7 and MDA-MB-231 cells underwent apoptosis. Furthermore, sanguiin H-6 induced the cleavage of caspase-8, caspase-3, and poly(ADP-ribose) polymerase, which resulted in apoptosis. However, cleavage of caspase-9 was only detectable in MCF-7 cells. In addition, sanguiin H-6 increased the ratio of Bax to Bcl-2 in both MCF-7 and MDA-MB-231 cells. These findings suggest that sanguiin H-6 is a potent therapeutic agent against breast cancer cells. In addition, it exerts its anticancer effect in an estrogen-receptor-independent manner.
山奈酚 H-6 是由没食子酸残基与六羟基二苯酸单元之一通过化学键连接而成的卡苏阿林二聚体。它是从朝鲜悬钩子中提取的一种有效化合物。它对多种人类癌细胞具有抗癌作用;然而,其对乳腺癌细胞的作用尚未得到明确证实。因此,我们旨在研究山奈酚 H-6 对两种人乳腺癌细胞系(MCF-7 和 MDA-MB-231)的抗癌作用及其作用机制。我们发现山奈酚 H-6 以浓度依赖性方式显著降低细胞活力。它还提高了 MCF-7 和 MDA-MB-231 细胞发生凋亡的速率。此外,山奈酚 H-6 诱导了半胱天冬酶 -8、半胱天冬酶 -3 和聚(ADP - 核糖)聚合酶的裂解,从而导致细胞凋亡。然而,仅在 MCF-7 细胞中可检测到半胱天冬酶 -9 的裂解。此外,山奈酚 H-6 增加了 MCF-7 和 MDA-MB-231 细胞中 Bax 与 Bcl-2 的比例。这些发现表明山奈酚 H-6 是一种针对乳腺癌细胞的有效治疗剂。此外,它以雌激素受体非依赖性方式发挥其抗癌作用。