Cho J Y, Yoo E S, Baik K U, Park M H, Han B H
Department of Immunopharmacology, R & D Center, Daewoong Pharmaceutical Co, Sungnam, Korea.
Planta Med. 2001 Apr;67(3):213-8. doi: 10.1055/s-2001-12005.
Ginsenosides are the major principles of Panax ginseng C. A. Meyer (Araliaceae) used as a mild oriental folk medicine. In this report, we have examined the inhibitory potency of protopanaxadiol ginsenosides (PPDGs) such as Rb1, Rb2 and Rc, and their co-treatment effect with known tumor necrosis factor (TNF)-alpha antagonists on TNF-alpha production in either murine (RAW264.7) or human (U937) macrophages stimulated with lipopolysaccharide (LPS). Rb1, and Rb2 strongly suppressed TNF-alpha production in RAW264.7 cells with an IC50 of 56.5 and 27.5 microM, respectively, and in differentiated U937 cells with an IC50 of 51.3, and 26.8 microM, respectively. The inhibitory activity of Rb1 and Rb2 was significantly increased by pharmacological agents against protein kinase C, protein tyrosine kinase, and protein kinase A, and anti-rheumatoid arthritis drugs, such as chloroquine and steroid drugs. In contrast, only cyclic AMP phosphodiesterase (cAMP PDE) inhibitors among cAMP-elevating agents did not change the inhibitory potency of PPDGs. These data suggest that PPDGs may possess potential therapeutic efficacy against TNF-alpha mediated disease and the therapeutic potency of PPDGs may be enhanced when co-treated with various kinds of known TNF-alpha antagonists but not with cAMP PDE inhibitors.
人参皂苷是五加科植物人参（Panax ginseng C. A. Meyer）中的主要成分，人参作为一种温和的东方民间药物使用。在本报告中，我们检测了原人参二醇型人参皂苷（PPDGs）如Rb1、Rb2和Rc的抑制效力，以及它们与已知肿瘤坏死因子（TNF）-α拮抗剂联合处理对脂多糖（LPS）刺激的小鼠（RAW264.7）或人（U937）巨噬细胞中TNF-α产生的影响。Rb1和Rb2分别以56.5和27.5微摩尔的半数抑制浓度（IC50）强烈抑制RAW264.7细胞中的TNF-α产生，在分化的U937细胞中，IC50分别为51.3和26.8微摩尔。蛋白激酶C、蛋白酪氨酸激酶和蛋白激酶A的药理学试剂以及抗类风湿性关节炎药物如氯喹和类固醇药物可显著增强Rb1和Rb2的抑制活性。相比之下，在升高环磷酸腺苷（cAMP）的试剂中，只有环磷酸腺苷磷酸二酯酶（cAMP PDE）抑制剂不会改变PPDGs的抑制效力。这些数据表明，PPDGs可能对TNF-α介导的疾病具有潜在的治疗效果，并且当与各种已知的TNF-α拮抗剂联合治疗时，PPDGs的治疗效力可能会增强，但与cAMP PDE抑制剂联合治疗时则不会。
