摘要
应用多种色谱技术进行分离纯化,从西洋参茎叶中分离得到10个化合物,经理化性质和光谱数据分析鉴定分别为:拟人参皂苷RT4(1)、拟人参皂苷RT5(2)、24(R)-Ocotillol苷元(3)、20(S)-人参皂苷Rh1(4)、20(S)-人参皂苷Rg1(5)、20(S)-人参皂苷Rg2(6)、20(S)-人参皂苷Rh2(7)、20(R)-人参皂苷Rh2(8)、20(S)-人参皂苷Rg3(9)、拟人参皂苷F11(10)。化合物1和3为首次从西洋参茎叶中分离得到。首次建立和认证了20(S)-人参皂苷Rg3肌内注射的生物利用度的测定方法,采用本文方法测定犬肌注20(S)-人参皂苷Rg3的生物利用度为96.7%,为20(S)-人参皂苷Rg3的新药开发提供了临床前药代动力学依据。
Ten compounds were isolated from saponins from the leaves and stems of Panax quinquefolium L. by various column ehromatographic techniques. They were elucidated on the basis of physicochemical property and spectral data ( TLC, 1H and 13 C NMR). They were determined as psuedo-ginsenoside-RT4 ( 1 ), psuedo-ginsenoside-RT5(2), 24 (R)OcotiUol (3),20 (S) -ginsenoside-Rh1(4), 20 (S) -ginsenoside-Rg, ( 5 ), 20 (S) -ginsenoside-Rg2 ( 6 ), 20 (S) -ginsenoside-Rh2 (7) ,20(R) -ginsenoside-Rh2 (8) ,20(S) -ginsenoside-Rg3 (9) and psuedo-ginsenoside-PF1, (10). Compounds 1 and 3 were extracted and separated from the leaves and stems of Panax quinquefolium L. for the first time. The bioavailability of intramuscular 20(S)-ginsenoside-Rg3 in dogs were determined and certificated for the first time. In this way, the bioavailability of intramuscular 20 (S)-ginsenoside-Rg3 in dogs was determined, which was 96.7%. The results provided the preclinical pharmacokinetics basis for the research and development of 20(S)-ginsenoside-Rg3 injection.
出处
《天然产物研究与开发》
CAS
CSCD
北大核心
2012年第10期1393-1397,1423,共6页
Natural Product Research and Development
关键词
西洋参茎叶
化学成分
20(S)-人参皂苷RG3
肌内注射
生物利用度
Panax quinquefolium saponins from leaves and stems
isolation
20 (S) -ginsenoside-Rg3
intramuscular injection
bioavailability