Hasegawa H, Sung J H, Huh J H
Itto Institute of Life Science Research, Happy World Inc., 3-13-8 Shiraitodai, Fuchu-shi, 183, Tokyo, Japan.
Arch Pharm Res. 1997 Dec;20(6):539-44. doi: 10.1007/BF02975208.
Anti-metastatic activities of IH901, an intestinal bacterial metabolic derivative formed from Ginseng protopanaxadiol saponins, was determinedin vitro andin vivo. Underin vitro conditions, IH901 inhibited the migration of bovine aortic endothelial cells 25 times stronger than suramin and suppressed the invasion of HT1080 human fibrosarcoma cells into reconstituted basement membrane components of Matrigel 1000 times stronger than RGDS peptide. IH901 also showed inhibitory effect on type-IV collagenase secretion from HT1080 cells and platelet aggregation. When the anti-metastatic activity of IH901 was evaluated in comparison with that of 5-FU using a spontaneous lung metastatic model of Lewis lung carcinoma, the administration of IH901 (10 mg/kg p. o.) to tumor-bearing mice led to a significant decrease in lung metastasis (43% of untreated control), which was slightly more effective than that obtained with 5-FU (56% of control). Thus, IH901 seems to exhibit its anti-metastatic activity partly through the inhibition of tumor invasion which results from the blockade of type IV collagenase secretion and also through anti-platelet and anti-angiogenic activities.
人参原人参二醇皂苷形成的肠道细菌代谢衍生物IH901的抗转移活性在体外和体内进行了测定。在体外条件下，IH901抑制牛主动脉内皮细胞迁移的能力比苏拉明强25倍，抑制HT1080人纤维肉瘤细胞侵袭基质胶重构基底膜成分的能力比RGDS肽强1000倍。IH901还对HT1080细胞分泌IV型胶原酶和血小板聚集有抑制作用。当使用Lewis肺癌自发性肺转移模型将IH901与5-氟尿嘧啶的抗转移活性进行比较时，给荷瘤小鼠口服IH901（10mg/kg）导致肺转移显著减少（为未治疗对照组的43%），这比5-氟尿嘧啶（对照组的56%）稍有效。因此，IH901似乎部分通过抑制IV型胶原酶分泌导致的肿瘤侵袭以及抗血小板和抗血管生成活性来发挥其抗转移活性。
