| Plants of the Rabdosia serra(Maxim.) Hara are perennial herbs, widely grown in central, south and south of China and can be used for the treatment of dysentery, acute jaundice hepatitis, acute cholecystitis, etc.Researchers at home and abroad studied its chemical constituents, including diterpenoids.In order to search for novel lead compounds from Rabdosia serra(Maxim.) Hara,we have conducted an in-depth study on aerial part of Rabdosia serra(Maxim.) Hara,at the same time, we modified the kirenol structure by reacted with a series of organic acids, for getting better bioavailability and pharmacokinetics lead compounds.Fifteen compounds were isolated from 75% methanol extract of the Rabdosia serra (Maxim.) Hara by silica gel column chromatography, ODS column chromatogr-aphy, Sephadex LH-20 and semi-preparative HPLC, etc. Among them, thirteen compounds were elucidated on the basis of physicochemical, sepectroscopic analyses and were characterized as, 1α,7α,14β,20-tetrahydroxy-11(12),16(17)Dinen-ent-kaur-15-one (1),1β,14β,19-trihydroxy-16(17)en-ent-kaur-15-one-20,7-lactone(2), Kamebakaurin (3), RabdoserrinA (4), ExcisaninA (5), Kamebakaurinin (6), Epinodo-sinol (7), RabdoinflexinA (8), daidzain (9),5-hydroxy-4'-methoxyflavone-7-glucose-dase (10), Hyperoside (11), Daucosterol (12),β-sitosterol (13). Among them, 1α,7α, 14β,20-tetrahydroxy-11(12),16(17)dinen-ent-kaur-15-one (1) and 1α,14β,18-trihydr-oxy-16(17)en-ent-kaur-15-one-20,7-lactone (2) were new compounds. (6), (9), (11) were isolated from this plant for the first time from this plant. In addition, compounds Kamebakaurin (3), RabdoserrinA (4), ExcisaninA (5), Kamebakaurinin (6), Rabdoinfle-xinA(8) and daidzain(9) have been screende for in vitro activities. The results displayed that it showed different level in vitro cytotoxic activities against human leukemia HL-60, human gastric cancer BGC-823, hepatoma Bel-7402 and nasopharyngeal carcinoma KB, which supply elementary information for further studying anti-tumor activities. |
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