Kalopanaxsaponin A is a basic saponin structure for the anti-tumor activity of hederagenin monodesmosides
Kalopanaxsaponin A is a basic saponin structure for the anti-tumor activity of hederagenin monodesmosides
复制标题
DOI：
10.1055/s-2001-11516
复制
发表时间：
2001-03-01
期刊：
影响因子：
2.7
通讯作者：
Lee, KT
中科院分区：
文献类型：
--
作者：
Park, HJ;Kwon, SH;Lee, KT
常春藤素、δ-常春藤素{常春藤素α-(L)-阿拉伯糖苷}、kalopanax-皂苷A{常春藤素3-O-α-(L)-鼠李糖基(1 -->2)-α-(L)-阿拉伯糖苷}、kalopanaxsaponin l [常春藤素3-O-β-(D)-木糖基(1)从茎皮中分离出 -->3)-α-(L)-鼠李糖基(1 -->2)-α-(L)-阿拉伯糖苷]和无患子皂苷 C [常春藤素 3-O-β-(D)-葡萄糖酰(1 -->4)-β-(D)-木糖基 (1 -->3)-α (L)-鼠李糖基(1 -->2)-α-(L)-阿拉伯糖苷] Kolopanax pictus Nakai（五加科）。常春藤皂苷元中，二糖（kalopanaxsaponin A，俗称α-常春藤素）、三糖（kalopanaxsaponin 1）、四糖（无患子皂苷C）对多种肿瘤细胞均表现出显着的细胞毒性，而常春藤素本身仅表现出较弱的细胞毒性，其单糖（δ-常春藤素）无细胞毒性。从这些结果来看，表明C-3处的阿拉伯糖基部分阻断了常春藤配基的活性，并且糖苷连接的第二个糖的位置对于细胞毒性也很重要。在体内实验中，苦参皂苷 A（15 mg/kg，腹腔注射）以及顺铂（3 mg/kg，腹腔注射）明显延长了患有结肠 26 和 3LL Lewis 肺癌的小鼠的寿命。这些结果表明kalopanaxsaponin A具有潜在的抗肿瘤应用。
Hederagenin, delta -hederin {hederagenin alpha-(L)-arabinoside}, kalopanax-saponin A {hederagenin 3-O-alpha-(L)-rhamnosyl (1 -->2)-alpha-(L)-arabinoside}, kalopanaxsaponin l [hederagenin 3-O-beta-(D)-xylosyl (1 -->3)-alpha-(L)-rhamnosyl(1 -->2)-alpha-(L)-arabinoside], and sapindoside C [hederagenin 3-O-beta-(D)-glucoyl(1 -->4)-beta-(D)-xylosyl (1 -->3)-alpha (L)-rhamnosyl(1 -->2)-alpha-(L)-arabinoside] were isolated from stem bark of Kolopanax pictus Nakai (Araliaceae). Among glycosides of hederagenin, disaccharide (kalopanaxsaponin A, commonly also called alpha -hederin), trisaccharide (kalopanaxsaponin 1), and tetrasaccharide (sapindoside C) showed significant cytotoxicity on several types of tumor cells, while hederagenin itself exhibited only weak cytotoxicity and its monosaccharide (delta -hederin) was non-cytotoxic. From these results, it suggests that the arabinosyl moiety at C-3 blocks the activity of hederagenin and the position of the second sugar for glycoside linkage is also important for cytotoxicity. In the in vivo experiments, kalopanaxsaponin A (15 mg/kg, i.p.) apparently increased the life span of mice bearing Colon 26 and 3LL Lewis lung carcinoma, as well as cisplatin (3 mg/kg, i.p.). These results indicated that kalopanaxsaponin A has potential anti-tumor applications.