Studies On The Bioactive Constituents Of Two Chinese Medicinal Herbs. Debregeasia Longifolia And Schefflera Venulosa

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, tsFT210. In anticipation of achieving the above objectives, traditional Chinese herbal medicines, Debregeasia longifolia and Schefflera venulosa have been screened by using this model and their ethanol-water extract showed bioactivity of inhibiting the cell cycle progression and cytoclasis of tsF210 cells. Thus, we selected them for further investigation.The ethanol-water extract of Debregeasia longifolia was successively partitioned with CHCls, EtoAc and n-butanol to yield crude extracts. From the bioactive part, n-butanol extract, three compounds 1-3 were isolated by column chromatography on HP-20, MCI, Sephadex LH-20, silica gel and RP18, followed by reverse-phase high performance liquid chromatragraphy and recrystalization. The structures of three compounds 1-3 were elucidated mainly by use of spectroscopic method (UV, IR, MS, 1D-NMR, 2D-NMR) and according to their physicochemical properties: 3,5-diemethoxy benzene carbonic acid-4-O- β -D-Pyranglucose (1), (-)-epicatechin (2), gallic acid (3).The ethanol-water extract of Schefflera venulosa was successively partitioned with CHCh, EtoAc and n-butanol to yield crude extracts. From the bioactive part, CHCls extract, three compounds 4-16 were isolated by repeated column chromatography on silica gel, Sephadex LH-20 and RP18, followed by recrystalization. The structures of 13 compounds 4-16 were elucidated mainly by use of spectroscopic method (UV, IR, MS, 1D-NMR, 2D-NMR) and according to their physicochemical properties: n-hexadecanoic acid (4), n-stearic acid (5), n-hexacosnicacid (6), Chrysophanol (7), 2,6-dimethoxyl P -benzoquinone (8), 2-hydroxy-3-( phenylaninocarbonyl ) naphthalene-1-azobenzene (9), β -sitosterol (10), Stigmasta-4, 22-dien-3-one (11), 3 β -hydroxystigmasta-5,22-dien-7-one (12), 3-Oxo-olean-12-ene-28-oic acid, (Oleanonic acid 13), 12 α ,13-dihydroxyolean -3-oxo-olean-28-oic acid (14 ). The structure of compounds 15% 16 are still in deducing.Bioassay results indicated that compound 4 showed a strong bioactivity in inhibiting the cell progression at the G2/M phase of tsFT210 cells; compound 7 and 13 showed a tender bioactivity in the cell progression at the G2/M phase of tsFT210 cells; compound 8 possessed strong cytoclasis. They are the main anticancer active compounds of this herb.In summary, compounds 1, 2, 3 were isolated for the first time from Debregeasia longifolia the title plant. Compounds 4-9,11-14 were isolated for the first time from Schefflera venulosa the title plant; 7-9, 11,12,14 were isolated for the first time from the Schefflera genus; and 14 is a new compound. The inhibitory activity on cell cycle of compounds 7, 13 and the cytoclasis activity of compound 8 were also discovered for the first time.