| The occurrence and development of cancer are closely related to the regulation of cell cycle and apoptosis. In fact, cancers could be regarded as the undesired and uncontrolled cell proliferation with disregulation in the controlling process of cell cycle or apoptosis. Therefore, novel inhibitors of the cell cycle or inducers of apoptosis would be good candidates for cancer chemotherapy. From this viewpoint, we have undertaken the screening for novel cell cycle inhibitors and apoptosis inducers from the traditional Chinese herbal medicines by use of a mouse cdc2 mutant cell line, tsFT2 10. In anticipation of achieving the above objectives, 137 traditional Chinese herbal medicines have been screened by using this model and the ethanol-water extract of Rubus aleaefolius Poir. showed stronger bioactivity of inhibiting the cell cycle progression of tsFT2 10 cells. Thus, it was selected for further investigation. The initial experimental analysis discovered the extract including two different sorts of active substance. One sort is polyphenolic substance, which inhibited cell cycle progression at the G01G1 phase. The other belongs to triterpenoids, which showed some cytotoxicity and cell cycle inhibiting activity at the 62/M phase. According to their different physicochemical properties, the appropriate methods were used for separating. Then the active fractions were under further isolation. The whole process was monitored by bioactivity. The polyphenolic bioactive fraction was subjected to Sephadex LH-20 filtration and ODS chromatography to afford two new compounds sanguiin H-2 ethyl ester (5) and rubuphenol (6), four known compounds ethyl gallate (1), ellagic acid (2), 1,2,3 ,4,6-penta- O-galloyl-,8-D-glucopyranose (3), 1,2,3 ,6-tetra- O-galloyl-fl-D-glucopyranose (4). Their structures were determined and identified by means of physicochemical methods and spectral analyses (UV IR, MS, ID-NMR, 2D-NMR). Compounds 1-6 were reported for the first time from the title plant and compounds 1, 3-6 were first reported from the genus. The triterpenoids fraction was separated by combinative use of silica gel 5 Abstract chromatography, reverse-phase HPLC chromatography. As a result, thirteen compounds including four new compounds (11, 14, 15, 18) were obtained by bioactivity-guided fractionation. They were detemained and identified by means of physicochemical methods and spectral analyses (IJV, IR, MS. 1D-NMR, 2D-NMR) as 3, 23-O-isopropylidenyl ?c 3cc, 19cc, 23-telrahydroxy-urs-12-en-28-oic acid (11), 3f3-O-cis-ferulyl-2 cc, 19a- dihydroxy-urs-1 2-en-28-oic acid (14), 3J1-O-frans-ferulyl-2a, 19 a-dihydroxy-urs-l 2-en- 28-oic acid (15), 2cc, 3/1, 19,8-trihydroxy-olean-1 1,13(18) -dien-28-oic acid?9, 28-olide (18), and eight known and activity compounds 3,8-hydroyl-urs-12-en-28-oic-acid (ursolic acid 7), l9a-hydroxygen ursolic acid (pomolic acid, 8), 2cc, 3a-dihydroxy-urs-12, 19- dien-28-oic acid (9), 2a, 3a-dihydroxy-urs-12,18(19)- dien-28-oic acid (10), 3, 23-0- isopropylidenyl-3/3, 19cc, 23-trihydroxy-urs- 1 2-en-28-oic acid (rotundic acid isopropylidene, 12), 2, 3-O-isopropylidenyl-2a~ 3 a~ 1 9a-Irihydroxy-urs- I 2-en-28-oic acid (13), 3/1-O-cis-ferulyl-2a-hydroxy-urs-12-en-28-oic acid (16), 3/1-O-trans-femlyl - 2a-hydroxy-urs-1 2-en-28-oic acid (17), and 3/I-hydroxy-olean-12-en-28-oic acid (oleanolic acid) (19). Compounds 7-19 were re...
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