中文摘要 |
本實驗評估人參總皂(crude ginseng saponin )、總皂次萃取物(subfractions, F1 ~F9 )、及皂標準品(Rg1, Rb1, Re )在離體大白兔陰莖海綿組織的舒張活性。結果顯示人參總皂 可以有效舒張phenylephrine (3 ×10-6 M )預收縮的陰莖海綿體,一半有效濃度(EC50 )為3.65 ± 0.27mg/ml ;相反地,皂標準品(Rg1, Rb1, Re )在相當劑量範圍下,則完全不影響海綿體張力,此結果暗示人參總皂中的三個主要皂(Rg1, Rb1, Re )並非是舒張海綿體的主要活性成份。繼續以管柱分離總皂得到9 個部份(F1 ~F9 ),分別呈現不同程度的海綿體舒張活性, 其中以F2 的作用最強(EC50 = 0.49 ± 0.03 mg/ml )、且顯著強於人參總皂。以上結果暗示F2 可能有機會作為治療陽痿的陰莖內注射用藥,但在臨床使用前必須再評估其組成、在活體動物的實驗結果以及是否可作為口服投藥.The corporal relaxant effects of total ginsenosides and nine subfractions (F1~F9) separated from it were evaluated in the rabbit corpus cavernosal strips in vitro . In the tissues precontracted by phenylephrine (PE, 3°—10-6 M), ginsenosides induced a dose-dependent (from 1 to 20 mg/ml) relaxing effect on rabbit corpus cavernosal strips with an EC50 of 3.65± 0.27 mg/ml. Three pure ginsenoside - Rg1 , Rb1 , and Re, at optimal dosages, do not affect the vascular tone at al in PEprecontracted corpus cavernosum. Total ginsenosides was further subfractionated by column chromatography and obtained nine fractions (F1~F9). Among them, F2 (0.1~5 mg/ml) displayed the most potent relaxing activity and turned out to be more effective (EC50 =0.49± 0.03 mg/ml) than total ginsenosides. Additionally, TLC analysis revealed that F2 contained some other components different from Rg1 , Rb1 and Re. These findings suggest none of Rg1 , Rb1 and Re contributes to the beneficial effect of total ginsenosides. In summary, F2 may possibly be used as a drug for intracavernosal injection therapy of impotence. However, further separation and identification the components of F2 and in vivo study are needed before clinical use in an oral form. |