Mondia whitei 根部活性成分之探討

1. Mondia whitei根部活性成分之探討 • 本研究目的為探討蘿藦科(Asclepiadaceae )植物Mondia whitei L.根部甲醇萃取物之活性成分。初期結果顯示甲醇萃取物之正己烷層與水層具降血糖活性；而乙酸乙脂層則具抗血管新生活性。經由各種層析管柱及不同溶媒系統層析後，共有三十四個化合物被分離純化。根據物理數據、核磁共振光譜判定及文獻資料比對後，其結構分別確定為：2-Hydroxy-4-methoxybenzaldehyde (1)、L-Phenylalanine (2)、Oleanolic acid acetate (3)、Oleanolic acid (4)、Oleanolic aldehyde acetate (5)、Lantanone (6)、β-Amyrin acetate (7)、α-Amyrin acetate (8)、β-Sitosterone (9)、6β-Hydroxystigmast-4-en-3-one (10) 、6β-Hydroxystigmasta-4,22-dien-3-one (11)、β-Sitosterol (12)與 Stigmasterol (13)之混合物、β-Sitosterol-3-O-β-D-glucoside (14)、Palmitic acid (15)、Stearic acid (17)、Linoleic acid (17)及Linolenic acid (18)之混合物、Methyl palmitate (19)及Methyl linoleate (20)之混合物、Uridine (21)、Adenosine (22)、Myo-inositol (23)、Tyrosol (24)、Methyl caffeate (25)、Methyl chlorogenate (26)、Osthole (27)、Bergenin (28)、(+)-Lariciresinol (29)、(+)-Catechin (30)、Quercetin (31)、Rutin (32)、Isoquecetrin (33)、Hyperoside (34)。根據其骨架的不同，分別歸類為胺基酸類：2，三萜類：3～8，固醇類：9～14，脂肪酸類：15～20，核苷酸類：21~22，六碳糖醇類：23，酚類：1, 24~26，香豆素類：27，異香豆素類︰28，木脂素類：29，黃酮類：30~34。繼而利用鼠肌纖維母細胞 (Mouse myoblast cells；C2C12 cells)葡萄糖攝取，評估經純化後之化合物活性，結果顯示由正己烷層分離出之化合物在濃度1 μM下具有促進葡萄糖攝取之活性有化合物3 (117.66 ± 2.41%)、4 (109.47 ± 2.83%)、6 (124.56 ± 3.31%)、7 (108.71 ± 0.85%)、8 (108.38 ± 2.02%)。以 MTT assay進行抑制人類臍靜脈內皮細胞增生來評估抗血管新生作用，結果顯示乙酸乙脂層分離出之化合物在濃度30 μM下具有抑制細胞增生之活性有化合物25 (32.95 ± 2.51%)、31 (80.67 ± 3.43%)。

2. Studies on the bioactive constituents from the root of Mondia whitei • This study aimed to investigate the active ingredients of the MeOH extract of Mondia whitei L., which belongs to Asclepiadaceae. Preliminary results indicated that its hexane and water layer possess anti-hyperglycemic activity and ethyl acetate layer possess anti-angiogenesis activity. Thirty four compounds were isolated via various chromatographic techniques and their structures were further identified according to their physical data, NMR. They are 2-Hydroxy-4-methoxybenzaldehyde (1), L-Phenylalanine (2), Oleanolic acid acetate (3), Oleanolic acid (4), Oleanolic aldehyde acetate (5), Lantanone (6), β-Amyrin acetate (7), α-Amyrin acetate (8), β-Sitosterone (9), 6β-Hydroxystigmast-4-en-3-one (10), 6β-Hydroxystigmasta-4, 22 -dien-3-one (11), mixture of β-Sitosterol (12) and Stigmasterol (13), β-Sitosterol-3-O-β-D-glucoside (14), Palmitic acid (15), Stearic acid (16), mixture of Linoleic acid (17) and Linolenic acid (18), mixture of Methyl palmitate (19) and Methyl linoleate (20), Uridine (21), Adenosine (22), Myo-inositol (23), Tyrosol (24), Methyl caffeate (25), Methyl chlorogenate (26), Osthole (27), Bergenin (28), (+)-Lariciresinol (29), (+)-Catechin (30), Quercetin (31)、Rutin (32), Isoquecetrin (33), and Hyperoside (34). According to their skeletons, those identified compounds can be classified into Amino acid: 2, Triterpenoids: 3～8, Steroids: 9～14, Fatty acid: 15～20, Nucleosides: 21~22, C6 Sugar alcohol: 23, Phenolics: 1, 24~26, Coumarins: 27, Isocoumarin: 28, Lignans: 29, Flavonoids: 30~34. Among the isolates from the hexane layer , 1 μM of the compounds 3, 4 , 6 , 7 , 8 were demonstrated to enhance glucose uptake to 117.66 ± 2.41%, 109.47 ± 2.83%, 124.56 ± 3.31%, 108.71 ± 0.85%, 108.38 ± 2.02%, respectively, using a mouse myoblast cell (C2C12) culture system. Among the isolates from the ethyl acetate layer, 30 μM of the compounds 25 and 31 inhibited 32.95 ± 2.51%, 80.67± 3.43 % HUVEC cell proliferations.