Studies on the Chemical Constituents and Cytotoxic Activities from the Stem and Root of Microtropis fokienensis

• Main Authors: Tsung-Hsien Chou, 周宗賢
• Other Authors: Jih-Jung Chen
• Format: Others
• Language: zh-TW
• Published: 2006
• Online Access: http://ndltd.ncl.edu.tw/handle/37071719091429503889

碩士 === 大仁科技大學 === 製藥科技研究所 === 94 === Abstract Microtropis fokienensis Dunn(Celastraceae) is a small shrub growing in high altitude forests throughout southern China and Taiwan. Sesquiterpene alkaloids, dihydroagarofuranoid sesquiterpenes, triterpenes, and their derivatives are widely distributed in plants of the family Celastraceae. Many of these compounds exhibit immunosuppressive, insecticidal, antiinflammatory, antitumor, and anti-AIDS activities. However, the chemical constituents and biological activities of M. fokienensis have not been studied. Approximately 1000 species of Formosan plants have been screened for cytotoxicity and M. fokienensis was shown to be one of the active species. Investigation on an EtOAc-soluble fraction of the stem of M. fokienensis has led to the isolation of four new dihydro-��-agarofuran sesquiterpene polyesters, fokienagarofuran A (1), fokienagarofuran B (2), fokienagarofuran C (3) and fokienagarofuran D (4), together with nine known compounds, triptogelin (5), mutangin (6), syringic acid (7), vanillic acid (8), 2,6-dimethoxy-p-benzoquinone (9), vanillin (10), p-hydroxybenz- aldehyde (11), ��-sitosterol (12), and ��-sitostenone (13). In addition, investigation on an EtOAc-soluble fraction of the root of M. fokienensis has led to the isolation of four new dihydro-��-agarofuran sesquiterpene polyesters, (1), (2), (3), fokienagarofuran E (14) and a new benzylbenzaldehyde, 2-hydroxy-5-(4-hydroxybenzyl)benzaldehyde (15), together with twelve known compounds, (5), (6), (7), (8), (10), (11), (12), (13), orbiculin G (16), p-hydroxybenzoic acid (17), 1-tetracosanol (18) and 1-hexacosanol(19). The structure of those new compounds were determined through spectral analyses including extensive 2D NMR data. Among the isolates, fokienagarofuran A (1), fokienagarofuran B (2), fokienagarofuran C (3), fokienagarofuran D (4), 2,6-dimethoxy-p- benzoquinone (9), and p-hydroxybenzaldehyde (11) exhibited significant cytotoxicities with IC50 = 0.032, 0.043, 0.051, 0.036, 0.82, and 0.42 �慊/mL, respectively, against P-388 cell line. In addition, fokienagarofuran A (1), fokienagarofuran B (2), fokienagarofuran C (3) and fokienagarofuran D (4) also exhibited significant cytotoxicities with IC50 = 0.054, 0.071, 0.082, and 0.058 �慊/mL, respectively, against HT-29 cell line.