- 简介
人参皂苷CK是原人参二醇型皂苷在人肠道内的主要代谢产物。研究表明,人参皂苷的药理活性主要是通过其代谢组分CK介导的,并且CK具有多种药理活性,如抗炎、抗肿瘤、抗过敏、抗糖尿病、保肝、神经保护、心血管保护等。
- 据报道人参皂苷C-K具有抗皱作用。此外，它还增强了HCT116结肠癌中肿瘤坏死因子(TNF)相关的凋亡诱导配体(TRAIL)诱导的凋亡。
- 生物活性
Ginsenoside C-K 是一种 Ginsenoside Rb1 的细菌代谢物。Ginsenoside C-K 通过抑制诱生型一氧化氮合酶 (iNOS) 和 COX-2 来发挥抗炎作用。在人肝微粒体中，Ginsenoside C-K 抑制 CYP2C9 和 CYP2A6 活性，IC50 分别为 32.0±3.6 μM和 63.6±4.2 μM。
- 靶点
COX-2
iNOS
CYP2C9
32 μM (IC
50
)
CYP2A6
63.6 μM (IC
50
)
- 体外研究
Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects mainly by reducing inducible nitric oxide synthase (iNOS), cyclooxygenase (COX)-2, and proinflammatory cytokines. Ginsenoside C-K suppresses the expression of proinflammatory cytokines by downregulating the activities of IRAK-1, MAPKs, IKK-α, and NF-κB in LPS-treated murine peritoneal macrophages. Ginsenoside C-K also suppresses the expression of iNOS and COX-2 by inhibiting NF-κB signaling in LPS-stimulated RAW264.7 cells. In zymosan-treated bone-marrow-derived macrophages (BMDMs) and RAW264.7 cells, Ginsenoside C-K inhibits inflammatory responses by negatively regulating the secretion of proinflammatory cytokines, the activation of MAPKs, and the generation of ROS. In addition, anti-inflammatory activity of Ginsenoside C-K has been observed in LPS-stimulated microglial cells. Ginsenoside C-K hinders inflammatory responses by controlling both the generation of ROS and the activities of MAPKs, NF-κB, and AP-1. Ginsenoside C-K, a major metabolite of ginsenosides in the gastrointestinal tract, inhibits NF-κB signaling in a PXR-dependent manner. Ginsenoside C-K is shown to promote recovery of dextran sulfate sodium (DSS) -induced colitis by suppressing NF-κB activation. Ginsenoside C-K significantly reduces TNF-α-induced upregulation of IL-1β and iNOS mRNA levels, and restores the mRNA levels of PXR and CYP3A4 in LS174T cells. Ginsenoside C-K, one of the intestinal metabolites of 20(S)-protopanaxadiol derivatives, exhibits an inhibition against the activity of CYP2C9 in human liver microsomes with an IC
50
value of 32.0±3.6 μM, a weak inhibition against the activity of CYP2A6 in human liver microsomes with an IC
50
value of 63.6±4.2 μM, and an even weaker inhibition against the activity of CYP2D6 in human liver microsomes with an IC
50
value of more than 100 μM.
- 体内研究
The weight of the collagen-induced arthritis (CIA) mice increases slowly and is significantly less than that of the normal DBA/1 mice beginning on d 3 after injection of the emulsion. Ginsenoside C-K (28, 56, and 112 mg/kg) mice recover their weight by d 32 after the emulsion injection. Ginsenoside C-K (56 and 112 mg/kg) and Methotrexate (MTX)-treated (2 mg/kg) mice show significantly increased body weight on d 50 as compared with CIA mice. Hind paw-swelling began on d 24 post-immunization. CIA mice are treated from d 28 to d 50. Arthritis scores are measured every 4 d beginning on d 24. Ginsenoside C-K (56 and 112 mg/kg) significantly reduces the arthritis scores of the mice on d 51.
- 化学性质
白色结晶粉末，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于人参根茎，绞股蓝。
- 用于含量测定/鉴定/药理实验等。
药理药效:抗肿瘤、抗炎、保肝和抗过敏。调节神经系统及免疫系统。
- 人参皂苷CK是人参皂苷Rb1的肠道微生物代谢产物，具有抗癌细胞增殖及抗炎等作用。
人参皂苷CK在多种肿瘤细胞系中表现出显著的抗肿瘤活性。它可以抑制多种癌症细胞的生长和增殖，诱导细胞凋亡，如在儿童急性髓系白血病（AML）细胞系中，CK可抑制细胞生长并诱导细胞凋亡，其机制与抑制DNA合成和DNA双链断裂有关。此外，CK还能与化疗药物协同作用，增强治疗效果，如与阿糖胞苷联合使用可显著提高AML治疗效果。
