Chemical Constituents Of Maesa Indica And Their Antitumor Activity

In the present dissertation, 20 species of Chinese medicinal herbs were retested by emulating their effects on the cell cycle and apoptosis in tsFT210 cells. Among the plant materials reexamined, 8 species showed cell cycle inhibitory and/or apoptosis inducing activities on the tsFT210 cells at the sample concentration of 100μg/ml. In the course of our screening, we found that the aqueous alcohol extract of Maesa indica (Roxb.) A. DC. (the family Mysinaceae) showed the cell cycle inhibitory activity on the tsFT210 cells.This is coinciding with its usage by Chinese people to cure cancers. However, no research report had so far been seen on its antitumor constituents. Thus, an investigation on the title plant was undertaken in the present dissertation to explore its anticancer constituents.The aqueous ethanol extract from the pulverized dry-stems (4.5 kg) of Maesa indica, suspended in water, was extracted with EtOAc and n- BuOH successively to obtain the EtOAc extract (48 g) and n-BuOH (260 g) respectively. The EtOAc and n-BuOH extracts showed mainly the G2/M phase inhibitory activity on the cell cycle of tsFT210 cells. From the EtOAc extract, compound 1-7 (Fig 1) were isolated by repeated column chromatography and preparative TLC. Structures of the compounds obtained were investigated by modern spectroscopy (MS, UV, IR, 1H-NMR, 13C-NMR, DEPT, 1H-1H COSY, HMQC and HMBC), and they were identified as (24R)-stigmast-7,22(E)-dien-3α- ol (1),β-sitosterol (2), n-hexadecanoic acid (3), 1,12-bis (3,3'-dihydroxy-4,4'- dimethyl- 5,5'-dimethoxyphenyl) dodecane (4), chrysophanol (5), 2,3-dihydroxypropyl palmitate (6) and 1' (9Z,12Z)-2,3- dihydroxypropyl octadeca-9,12- dienoate (7), respectively. On the other hand, a total saponin fraction (Maesasaponins) could be obtained from the n-BuOH extract through a fractionation and purification procedure using repeated column chromatography and preparative TLC.The antitumor activity for 1-7 and the total saponin fraction (Maesasaponins) was assayed by SRB method using K562 cells. In the bioassay, compounds 3-7 and the total saponin fraction (Maesasaponins) could inhibit to a different extent the proliferation of K562 cells.In conclusion, compounds 3 and 5-7 were isolated from the genus Maesa for the...