| 摘要: | 益智仁是薑科山薑屬植物益智的乾燥果實。據中國藥典之描述，本品具有溫脾、暖腎、固氣、攝精等作用。李棪云：「服之令人智慧，故名」。益智作為補益藥，在益智健腦方面臨床應用很多，但其藥理作用機制仍尚未明確。
二十公斤之益智仁藥材，以50%乙醇萃取，再透過大孔吸附樹脂進行層析分離，經25%、50%、75%及95%等四種不同濃度乙醇進行沖提，可分別獲得四種區分物AO-A（113.73 g）、 AO -B（81.59 g）、 AO-C（79.39 g）及AO-D（94.58 g）。另取5公斤之益智仁藥材，以水蒸餾提取法，共獲得11g之精油（AO-E）。
AO-C、AO-D及益智仁甲醇萃取物經進一步之純化分離，共獲得三種倍半?衛?化合物及一種庚烷類衍生物，分別為Nootkatone (AO-1)、α-cyperone (AO-2)、epi-α-cyperone (AO-3)及Yakuchinone A (AO-4)。其中AO-1及AO-4為益智仁之代表性成分，可作為益智仁藥材之指標成分。取市售藥材四批進行含量分析，AO-1及AO-4之含量分別為7.27 ± 0.74 mg/g及0.60 ± 0.19 mg/g。
益智仁粗萃物AO-A及AO-B中，幾乎不含有AO-1及AO-4此二成分，AO-C中此二成分之含量分別為39.14 ± 2.6 9 mg/g及4.92 ± 0.34 mg/g，AO-D為248.14 ± 35.83 mg/g及24.46 ± 3.64 mg/g，AO-E則為179.88 ± 6.04 mg/g及7.42 ± 0.52 mg/g。
五種粗萃物AO-A、AO-B、AO-C、AO-D及AO-E中，均能於β-amyloid損傷PC12細胞之評估模式中，觀察到明顯的保護作用。並能調節因β-amyloid引起的胞內鈣離子濃度上升以及抑制ROS升高之能力。益智仁代表性成分AO-1及AO-4亦具有抑制β-Amyloid毒性之作用。
Yizhiren is the dry fruit of Alpinia oxyphylla Miq. as a kind of crude drug in traditional chinese medicine. According to the description of Chinese pharmacopoeia, the kind of fruit has some healthy functions correspond to spleen and kidney. Lee-Tan was an ancient doctor in China descripted the benefit of this fruit as making people become wiser. There are many clinical applications to enhance brain functions and human memory by using Yizhiren, but its pharmacological mechanisms are still not yet clear.
Extracting 20 kg Yizhiren by 50% EtOH and then separating by diaion HP-20 with 25%, 50%, 75% and 95% EtOH could collect four fractions, AO-A (113.73 g), AO-B (81.59 g), AO-C (79.39 g) and AO-D (94.58 g). Extracting 5 kg Yizhiren by steam distillation method could collect 11.0 g essential oil marked as AO-E.
Four pure compounds, Nootkatone (AO-1), α-cyperone (AO-2), epi-α-cyperone (AO-3) and Yakuchinone A (AO-4) were from further purifications of AO-C, AO-D and Yizhiren methanol extract. AO-1 and AO-4 are marker constituent representative sesquiterpene and heptane derivative in Yizhiren, respectively. The contents of AO-1 and AO-4 were 7.27 ± 0.74 mg/g and 0.60 ± 0.19 mg/g in Yizhiren by analyzing four batches crude drug from local market.
Compounds AO-1 and AO-4 were almost absent in fraction AO-A and AO-B but rich in fraction AO-C, AO-D and AO-E. In AO-C, AO-1 and AO-4 were 39.14 ± 2.69 mg/g and 4.92 ± 0.34 mg/g, respectively. There were 248.14 ± 35.83 mg/g and 24.46 ± 3.64 mg/g in AO-D, respectively. And there were 179.88 ± 6.04 mg/g and 7.42 ± 0.52 mg/g in AO-E.
The protective effects were obviously on β-amyloid injury in PC-12 cell by using these fractions AO-A, AO-B, AO-C, AO-D and AO-E and pure compounds AO-1 and AO-4. All the fractions could also decrease the intracellular calcium and ROS. |
