Chiang H C, Wang J J, Wu R T
School of Pharmacy, College of Medicine, National Taiwan University, Taipei, ROC.
Anticancer Res. 1992 Sep-Oct;12(5):1475-8.
Formosanin C (PF-3, I), a diosgenin glycoside with four sugars isolated from Paris formosana Hayata as main constituent, significantly showed immunomodulating effects on the proliferative response of mouse lymphocytes to concanavalin A (Con A). The partialy hydrolysis products of formosanin C, dioscin (II) and prosapogenin A of dioscin (III), also increased 3H-thymidine incorporation of Con A-stimulated lymphocytes maximally at 0.01 micrograms/ml, whereas formosanin C did so at 0.0001 micrograms/ml. However, trillin (IV) and diosgenin (V) obtained from the partial hydrolysis of formosanin C had no effects on these immune responses. Evidently, the immunomodulating activities increased in the order of increasing polarity. Probably the solubility in water was a factor. This demonstrated that the sugar moiety in the structure of formosanin C (I) displays a very important pattern for the effect on the proliferative response of mouse lymphocytes to Con A. On the other hand, these hydrolysis products at higher concentrations of 1 and 10 micrograms/ml reduced the cytotoxic effects on spleen cells as compared with formosanin C. The other constituent, beta-ecdysone (VI) isolated from the stems of Paris formosana Hayata also increased 3H-thymidine incorporation of Con A-stimulated splenocytes. At the concentration of 0.001 micrograms/ml, the stimulation index of beta-ecdysone (2) is higher than that of formosanin C (1.65), and at the concentration of 100 micrograms/ml, beta-ecdysone had no cytotoxicity for normal spleen cells whereas formosanin C at the lower concentration of 10 micrograms/ml showed cytotoxicity. Based on this study, beta-ecdysone (VI) is therefore a better immunomodulator than formosanin C.
台湾薯蓣皂苷元C(PF-3,I)是从台湾重楼中分离得到的一种含有四种糖的薯蓣皂苷元苷,作为主要成分,它对小鼠淋巴细胞对刀豆球蛋白A(Con A)的增殖反应具有显著的免疫调节作用。台湾薯蓣皂苷元C的部分水解产物,薯蓣皂苷(II)和薯蓣皂苷元A(III),也能使Con A刺激的淋巴细胞的3H-胸腺嘧啶核苷掺入量在0.01微克/毫升时达到最大值,而台湾薯蓣皂苷元C在0.0001微克/毫升时就能达到此效果。然而,从台湾薯蓣皂苷元C的部分水解产物中得到的重楼皂苷(IV)和薯蓣皂苷元(V)对这些免疫反应没有影响。显然,免疫调节活性随极性增加而增强。水溶性可能是一个因素。这表明台湾薯蓣皂苷元C(I)结构中的糖部分对小鼠淋巴细胞对Con A的增殖反应的影响呈现出非常重要的模式。另一方面,与台湾薯蓣皂苷元C相比,这些水解产物在1和10微克/毫升的较高浓度下对脾细胞的细胞毒性作用降低。从台湾重楼茎中分离得到的另一种成分β-蜕皮激素(VI)也能增加Con A刺激的脾细胞的3H-胸腺嘧啶核苷掺入量。在0.001微克/毫升的浓度下,β-蜕皮激素的刺激指数(2)高于台湾薯蓣皂苷元C(1.65),在100微克/毫升的浓度下,β-蜕皮激素对正常脾细胞没有细胞毒性,而台湾薯蓣皂苷元C在10微克/毫升的较低浓度下就显示出细胞毒性。基于这项研究,β-蜕皮激素(VI)因此是一种比台湾薯蓣皂苷元C更好的免疫调节剂。