| 摘要: | 三葉崖爬藤 (Tetrastigma formosanum (Hemsl.) Gagnep. (葡萄科))是一種廣布在台灣各地低海拔地區的爬藤植物。它在台灣傳統藥用主要為治療肺炎、哮喘、肝炎、風濕和喉嚨痛等。研究顯示三葉崖爬藤莖部的甲醇萃取物具有口腔癌細胞 HSC-3 和肺鱗狀細胞 CH27選擇性的毒殺活性。經過分液層析以及管柱層析甲醇萃取物以後，得知在正己烷層活性分劃以及乙酸已酯層活性分劃具有顯著的抗癌活性。
由正己烷層活性分劃得到10個化合物：β-sitosterol (1)、stigmasterol (2)、24-ethylcholest-4-en-3-one (3)、24-ethylcholest-4,22-dien-3-one (4)、(－)-6β-hydroxystigmasta-4-en-3-one (7)、(－)-6β-hydroxystigmast-4,22-dien-3-one (8)、3β-hydroxystigmast-5-en-7-one (9)、3β-hydroxystigmast-5,22-dien-7-one (10)、(－)-lupeol (12)及α-tocospiro B (15)。
由乙酸乙酯層活性分劃，得到5個化合物：stigmast-5-en-3??-ol acetate (5) 、stigmast-5,22-dien-3β-ol acetate (6) 、(3β,5α,8α,22E,24R)-5,8-epidi-oxyergosta-6,22-dien-3-ol (11) 、protocatechuic acid (13) 及 5-carboxymellein (15)。
其中具有負旋光之化合物7, 8 及 12為首次分離。且由文獻得知化合物6, 7, 8, 11及15具有抑制不同癌症細胞株的能力。
Tetrastigma formosanum (Hemsl.) Gagnep. (Vitaceae), a plant distributed at low altitudes of whole Taiwan, is a climbing shrub. It is used as treatments for pneumonia, asthma, hepatitis, rheumatoid, and sore throat for folk uses in Taiwan. The study showed the methanolic extract of the stem of T. formosanun owning the selective cytotoxic activities against human oral squamous carcinoma HSC-3 cells and human lung squamous carcinoma CH27 cells. After partition and column chromatography, the sub-fractions of n-hexane layer and EtOAc layer showed significantly anti-cancer activities.
Ten compounds including β-sitosterol (1), stigmasterol (2), 24-ethylcholest-4-en-3-one (3), 24-ethylcholest-4,22-dien-3-one (4), (－)-6β-hydroxystigmasta-4-en-3-one (7), (－)-6β-hydroxystigmast-4,22-dien-3-one (8), 3??-hydroxystigmast-5-en-7-one (9), 3β-hydroxystigmast-5,22-dien-7-one (10), (－)-lupeol (12), and α-tocospiro B (15) were isolated from n-hexane layer .
Five compounds including stigmast-5-en-3β-ol acetate (5), stigmast-5,22-dien-3??-ol acetate (6), (3β,5α,8α,22E,24R)-5,8-epidioxyergosta-6,22-dien-3-ol (11), protocatechuic acid (13), and 5-carboxymellein (15) were isolated from EtOAc layer.
Among them, compounds 7, 8 and 12 owning negtive optical rotatory were first isolated. The literature showed that compounds 6, 7, 8, 11 and 15 owned the cytotoxic activities against different cancer cell lines. |
