臺灣博碩士論文加值系統

本研究在篩選具抑制膽固醇酯轉移蛋白活性的食品或中藥材，並進一步的
分離純化出膽固醇酯轉移蛋白的抑制劑。
在材料篩選時，選擇了17種可能具降血脂活性的食品或中藥材，以其水萃
出物來進行膽固醇酯轉移蛋白活性的測定，篩選的結果以山楂水萃出物最
好，有15 % 的抑制效果。接著進行山楂不同溶劑的萃取，各種溶劑萃出
物的抑制效果分別是水萃出物15 %、乙醇萃出物27 %、丙酮萃出物33 %，
然而甲醇萃出物有12 %的促進效果，故選擇抑制效果最好的山楂丙酮萃出
物進行抑制劑的分離與純化；首先利用液液萃取進行簡單的區分，結果第
一次正己烷區分物有49 % 促進效果、第二次正己烷區分物有12 % 促進效
果、第三次正己烷區分物有15 % 促進效果、甲醇區分物有74 % 抑制效? G，將甲醇區分物進行吸附性的管柱層析 (Amberlite XAD-7)，各區分物
的效果為第一、第二、第三區分物分別有15 %、34 %、14 % 的抑制效果
，第四、第五、第六區分物分別有205 %、91 %、11 % 的促進效果；將第
二區分物進行兼具親和與分子篩特性的管柱層析 (Sephadex LH-20)，第
一、第四、第五區分物有10 %、20 %、50 % 的抑制效果，第二、第三區
分物有5 %、42 % 促進效果；將第五區分物進行高效能液相層析，取第三
、第四區分物進行活性測定，第三區分物有91 % 的抑制程度 (IC50 =
15 μM、第四區分物有93 % 的抑制活性93 % 的抑制程度 (IC50 = 25 μ
M)。第三
、四區分物經質譜的結構鑑定可能為procyanidin trimer，需進一步之光
譜分析來確認其化學結構。

The purpose of this study was to select food and Chinese
medicine which have the ability to inhibit the activity of
cholestery ester transfer protein (CETP), then isolate and
purify CETP inhibitors.
Seventeen materials which might be hypolipidemic were chosen
to screen for the CETP inhibition activity. The aqueous extract
of these materials were used in the CETP activity test. Results
showed that aqueous extract of hawthorn exhibited best
inhibition level (15 %). Hawthorn extracts from different
solvents were then assayed for CETP activity. The inhibition
levels of aqueous, ethanolic and acetonic extracts were 15 %,
27 % and 33 % respectively. However methanolic extract
exhibited 12 % activation level
. Acetonic extract of hawthorn was therefore selected for
isolating and purifying CETP inhibitors.
At first, liquid-liquid partition was employed for simple
separation, it was found that first, second and third hexane-
soluble fractions exhibited 49 %, 12 % and 15 % activation
levels, respectively. The methanol-soluble fraction exhibited
74 % inhibition level. The methanol-soluble fraction was then
separated with absorptive column chromatography (Amberlite
XAD-7). The inhibition levels of the first, second and third
fractions were 15 %, 34 % and 14 %. The fourth, fifth and sixth
fractions showed activation
levels of 205 %, 91 % and 11 %, on the contrary. The second
fraction, which had the highest inhibition level, was further
fractionated with partial absorptive and partial size-exclusion
column chromatograph (Sephadex LH-20). The first, fourth and
fifth fractions exhibited 10 %, 20 % and 50 % inhibition
levels; while the second and third fractions exhibited 5 % and
42 % activation levels. The fifth fraction was then separated
by preparative HPLC with C18 column. The third fraction of HPLC
exhibited 91 % inhibi
tion level with IC50 = 15 μM. The fourth fraction of HPLC
exhibited 93 % inhibition level with IC50 = 25 μM. The
chemical structure of these two fractions were tentatively
identified as isomers of procyanidin trimer by LC-MS. Further
spectroscopic analysis of these two compounds were needed in
order to positively identify the structures.