Min Jeong-Ki, Kim Jung-Ho, Cho Young-Lai, Maeng Yong-Sun, Lee Shin-Jeong, Pyun Bo-Jeong, Kim Young-Myeong, Park Jeong Hill, Kwon Young-Guen
Department of Biochemistry, College of Sciences, Yonsei University, Seoul, Republic of Korea.
Biochem Biophys Res Commun. 2006 Oct 27;349(3):987-94. doi: 10.1016/j.bbrc.2006.08.129. Epub 2006 Aug 30.
Ginseng, refering to the roots of the species of the genus Panax ginseng, has been widely used in traditional oriental medicine for its wide spectrum of medicinal effects, such as anti-inflammatory, anti-tumorigenic, adaptogenic, and anti-aging activities. Many of its medicinal effects are attributed to the triterpene glycosides known as ginsenosides. In this study, we report a novel anti-apoptotic activity of 20(S)-ginsenoside Rg3 ((20S)Rg3) and its underlying molecular mechanism in human endothelial cells (ECs). ECs undergo apoptosis associated with increased LEHDase (caspase-9) and DEVDase (caspase-3) activity and DNA fragmentation after 24h of serum deprivation. These apoptotic markers were suppressed by the addition of (20S)Rg3. (20S)Rg3 increased the expression of Bax and conversely decreased Bcl-2. (20S)Rg3 potently induced a rapid and sustained Akt activation and Bad phosphorylation, resulting in the inhibition of mitochondrial cytochrome c release. These anti-apoptotic activities of (20S)Rg3 were significantly abrogated in cells expressing dominant negative Akt. Taken together, our results suggest that (20S)Rg3 prevents EC apoptosis via Akt-dependent inhibition of the mitochondrial apoptotic signaling pathway. The novel property of (20S)Rg3 may be valuable for developing new pharmaceutical means that will control unwanted endothelial cell death at the site of vascular injury.
人参,指的是五加科人参属植物的根,因其具有广泛的药用功效,如抗炎、抗肿瘤、适应原样作用和抗衰老活性等,在传统东方医学中已被广泛应用。其许多药用功效归因于被称为人参皂苷的三萜糖苷。在本研究中,我们报告了20(S)-人参皂苷Rg3((20S)Rg3)在人内皮细胞(ECs)中的一种新的抗凋亡活性及其潜在分子机制。血清剥夺24小时后,ECs发生凋亡,伴有LEHD酶(半胱天冬酶-9)和DEVD酶(半胱天冬酶-3)活性增加以及DNA片段化。添加(20S)Rg3可抑制这些凋亡标志物。(20S)Rg3增加了Bax的表达,反之降低了Bcl-2的表达。(20S)Rg3强烈诱导Akt快速且持续的激活以及Bad磷酸化,从而抑制线粒体细胞色素c的释放。在表达显性负性Akt的细胞中,(20S)Rg3的这些抗凋亡活性被显著消除。综上所述,我们的结果表明(20S)Rg3通过Akt依赖的方式抑制线粒体凋亡信号通路来预防EC凋亡。(20S)Rg3的这一新特性对于开发新的药物手段以控制血管损伤部位不必要的内皮细胞死亡可能具有重要价值。