番石榴莖部與大葉千斤拔根部：降血糖成分之探討

Studies on the Hypoglycemic Constituents：Stem of Psidium guajava and Root of Flemingia macrophylla

吳宗儒(Zong-Ru Wu)

指導教授 ： 徐鳳麟

臺北醫學大學/藥學院/生藥學研究所/碩士(2011年)

摘要

糖尿病為常見之疾病，除了影響人們健康之外，亦衍生許多相關之病
症而造成社會問題，因此研發降血糖藥物，為目前非常迫切的需求。番石榴是台灣民間用於控制糖尿病的傳統中草藥，而大葉千斤拔最近也有文獻表示，在治療糖尿病上有顯著的效果，因此本研究選用這兩種植物，探討其中之活性成分。經由各種層析管柱及不同溶媒系統分離純化後，共分離到二十九個化合物，並根據物理數據、核磁共振光譜判定及文獻資料的比對，而確定其化學結構。從番石榴莖部70 ％ acetone/ H2O 之萃取物，於n-BuOH 層分離出八個化合物：gallic acid (1)、protocatechuic acid (2)、ferulic acid (3)；quercetin (4)、myricetin (5)、(+)-catechin (6)、pedunculagin (7)、castalagin (8)。另外，從大葉千斤拔的根部之萃取物於ethyl acetate 層以及n-hexane 層，共分離出二十一個化合物：phloroglucinol (9)、4'-O-methyl-gallocatechin (10)、genistein (11)、prunetin (12)、genistin (13)、6'-O-acetylgenistin (14)、2'-hydroxygenistein (15)、dalbergioidin (16)、naringenine (17)、lespedezaflavanone A (18)、lespedezaflavanone B (19)、flemichin D (20)、khonklonginol H (21)、eriosematin (22)、iso-eriosematin
(23)、aureol (24)、5,7,2',4'-tetrahydroxy-3-arylcoumarin (25)、lupeol (26)、β-sitosterol (27)、β-stigmasterol (28) 及β-sitosterol-O-D-glucoside (29)。其中化合物9、14、16、21 等四個化合物為首次自千斤拔屬植物分離出，而化合物25 為新化合物。降血糖活性試驗中，使用TNF-α 誘導小鼠肝臟FL83B 細胞株產生胰島素阻抗，於化合物濃度10 μM 之下進行體外試驗，經由細胞攝入螢光葡萄糖 (2-NBDG) 染劑量，篩選出活性化合物。結果顯示，化合物1、3、4、5、6、10、11、12、14、15、16、17、25、26 具有較顯著促進胰島素阻抗之FL83B cell 之glucose uptake 的作用。

關鍵字

番石榴莖 ； 大葉千斤拔根 ； 降血糖作用

並列摘要

No matter in Taiwan perhaps overseas, chronic metabolic diseases such diabetes mellitus is gradually injure the health of our people. In order to improve their quality of life, there is an urgent need to discover new drugs
that effectively treat diabetes. Psidium guajava Linn. is often used as folk medicine to improve diabetes in Taiwan. Flemingia macrophylla (Willd.) O. Ktze. is also proved useful at controlling diabetes. This is the reason that we
choose such two plants to rsearch. Twenty nine compounds were isolated via various chromatographic techniques and their structures were further identified according to their physical data, NMR. Eight compounds have been isolated from the n-BuOH layer of 70 ％ acetone/H2O extract of P. guajava including gallic acid (1), protocatechuic acid (2), ferulic acid (3), quercetin (4), myricetin (5), (+)-catechin (6), pedunculagin (7), castalagin (8). In addition twenty-one compounds have been isolated from the ethyl acetate and n-hexane layer of extracts of F. macrophylla including phloroglucinol (9), 4'-O-methyl-gallocatechin (10), genistein (11), prunetin (12), genistin (13), 6'-O-acetylgenistin (14), 2'-hydroxygenistein (15), dalbergioidin (16), naringenine (17), lespedezaflavanone A (18), lespedezaflavanone B (19), flemichin D (20), khonklonginol H (21), eriosematin (22), iso-eriosematin
(23), aureol (24), 5,7,2',4'-tetrahydroxy-3-arylcoumarin (25), lupeol (26), β-sitosterol (27), β-stigmasterol (28), β-sitosterol-O-D-glucoside (29). Among them, compound (25) is a new compound, and compounds 9, 14, 16, 21 were
first found in Flemingia species. Tumor necrosis factor-alpha was used to induce insulin resistance of mouse liver FL83B cells. Compound was evaluated for their acute effects in vitro by measuring 2-NBDG uptake of the insulin-resistant cells at 10 μM dose. The results suggest that these compounds 1, 3, 4, 5, 6, 10, 11, 12, 14, 15, 16, 17, 25, 26 can enhance glucose.
uptake in insulin resistant cell.

並列關鍵字

Psidium guajava ； Flemingia macrophylla ； antiglycemia

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