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生地黃降血糖成分之研究 • 在中藥產科方劑生化湯之藥理動物試驗的結果如下：1.生化湯的水抽出隨著生活水平的提高，糖尿病一直高居國人十大死因之第五位，糖尿病的治療藥物在新藥開發上的需求量也相對的增加，故天然物在新藥開發上的地位日趨重要。在傳統中藥上，地黃常被使用在糖尿病的治療，地黃為玄參科植物地黃的乾燥塊根，過去日本學者對其成份之研究甚為廣泛，但除了發現catalpol、rehmannioside D及poly- saccharide (RG-WP) 等成份具有降血糖作用之外，尚未對其降血糖的活性成份做詳細之探討，本論文以活性為導向做降血糖的活性篩檢，確定生地黃的降血糖作用最為顯著，故針對其具有降血糖作用的部份進行研究，探討其所含之主要活性成份。生地黃之60﹪丙酮萃取物，藉由各種管柱層析法，共分離出13個化合物，根據其物理數據，核磁共振光譜判定，其結構分別確定為methyl-β-D-fructofuranoside (1), raffinose [β-D-fructofuranosyl O-α-D-galactopyranosyl-(1→6)-α-D- glucopyranoside] (2), stachyose [β-D-fructofuranosyl-O-α-D-galacto- pyranosyl-(1→6)-O-α-D-galactopyranosyl-(1→6)-O-α-D-gluco- pyranoside] (3), catalpol (4), dihydrocatalpol (5), uridine (6), ajugol (leonuride) (7), jioglutin B (8), adenosine (9), 1-hydroxypinoresinol (10), 6-O-E-feruloyl ajugol (11), martynoside (12), rehmarglutinoside (13)，其中rehmarglutinoside為一新的化合物，而dihydrocatalpol (5) 及1-hydroxypinoresinol (10) 則首次在生地黃中被分離出來，另外stachyose, catalpol及ajugol經初步藥理篩檢確定具有降血糖活性，除了catalpol之降血糖作用已有文獻發表之外，stachyose及ajugol之具有降血糖作用則首次被發現。
Studies on the Hypoglycemic Active Components from Dried Root of Rehmannia glutinosa • In the traditional Chinese medicine, a large number of Rehmannia glutinosa is used to treat for Diabetes Mellitus (DM). The hypoglycemic activity of the dry root is most obvious of the different procession techniques of Rehmannia glutinosa (Scrophulariaceae). Several Japanese investigators reported extensive studies on the constituents of R. glutinosa. But, besides catalpol, rehmannioside D, and a part of polysaccharide, there were fewer compounds focused on the relation between the constituent and hypoglycemic activity. Therefore, a chemical investigation for hypoglycemic active components in R. glutinosa was performed. The dried roots of R. glutinosa were extracted with 60% aqueous acetone, to afford crude extract, which was partitioned between chloroform and water, than butanol and water. Preliminary screen test showed water-soluble and butanol-soluble fractions were hypoglycemic active. These active fractions were subject to various columns chromatography. Thirteen compounds were isolated and purified. The structures of these compounds were determined based on the analysis of NMR and MS spectroscropic data. They are methyl-β-D-fructofuranoside (1), raffinose [β-D-fructofuranosyl O-α-D-galactopyranosyl-(1→6)-α-D- glucopyranoside] (2), stachyose [β-D-fructofuranosyl O-α-D-galacto- pyranosyl-(1→6)-O-α-D-galactopyranosyl-(1→6)-α-D-glucopyranoside] (3), catalpol (4), dihydrocatalpol (5), uridine (6), ajugol (leonuride) (7), jioglutin B (8), adenosine (9), 1-hydroxypinoresinol (10), 6-O-E-feruloyl ajugol (11), martynoside (12), rehmarglutinoside (13). Among them, stachyose, catalpol, and ajugol showed hypoglycemic action on STZ mice. Moreover, it is noteworthy that rehmarglutinoside is a new compound, and dihydrocatalpol, 1-hydroxypinoresinol are first isolated from Rehmannia glutinosa.
