Studies On The Chemical Constituents And Biological Activities Of Lycoris Aurea And Bidens Pilosa

In order to find the unknown chemical constituents and physiologically active substances, two plants (Lycoris aurea and Bidens pilosa) have been subjected to phytochemical investigations. As a result, forty-four compounds were identified on the basis of the spectroscopic methods, and the comparison to authentic sample on the TLC and literatures data. The compounds include flavonoids, diterpenoids, aromatic compounds, alkaloids and steroids. Among them, three compounds (including two alkaloids and one diterpene) were proved to be new ones. Twelve alkaloids were tested for antitumour activity against Ramos and BEL-7402 cells. Compound 5 and 8 with haemanthamine skeletons exhibited the strongest activity.1. Chemical constituents and bioactivities of Lycoris aureaAs an important member of Amatyllidaceae, Lycoris aurea, is widely distributed in southwest, southeast and northwest of China. Plants of the Amaryllidaceae are known to produce structurally unique alkaloids with a wide range of interesting physiological effects. In order to search active substances from this plant, we phytochemically investigated the whole plants of Lycoris aurea collected in Kunming of Yunnan province, which has not been studied previously. 1.1 Investigation on alkaloids and its activities from Lycoris aureaPlants of the Amaryllidaceae are known to produce structurally unique alkaloids with a wide range of interesting physiological effects, including antitumour, antiviral,acetylcholinesterase inhibitory, immunostimulatory and antimalarial activities. Galanthamine, an alkaloid isolated from Amaryllidaceae species, as a potent inhibitor of the acetylcholinesterase, has been approved in several countries for treating the symptoms of Alzheimer's type senile dementia.Extensive column chromatography led to the isolation of 19 compounds, including fifteen alkaloids, two diterpene, one aromatic compound. Compound 1, 2 were new indole alkaloids, and 18 was new rosane diterpene lactone. Other compounds were determined by spectral analysis, named galanthamine (3), hippeastrine (4), haemanthidine (5), JV-demethylgalanthamine (6), Odemethylgalanthamine (7), haemanthamine (8), homolycorine (9), 0-demethyllycoramine (10), lycorine (11), O-methyllycorenine (12), 9-demethylhomolycorine (13), lycoramine (14), pluviine (15), echinulin (16), 2',4',6'-trimethoxyacetophenone (17), rosololactone (19).Twelve alkaloids belonged to five skeletons were tested their anticancer activity against Ramos and Bel-7402 cells. Compound 5 and 8 with haemanthamine skeleton exhibited the strongest activity. This type compounds are worth to be further investigated.1.2 Study on non-alkaloids of Lycoris aureaOnly few literatures can be use in the non-alkaloids constituents of Lycoris genus, our investigation led to the isolation of 15 compounds from Lycoris aurea. Except for 8, 15, all compounds were isolated firstly from Lycoris aurea. All structure were determined on the base of spectral data as follow: (25)-4'-hydroxy-7-methoxyflavan (1),(2S>3',7-dihydroxy-4'-methoxyflavan (2), (2S)-4',7-dihydroxyflavan (3), (25)-4'.7-dihydroxy-8-methyfiavan (4), (25)-4',7-dihydroxy-3'-methoxy-8-methyl-falvan (5), (2S)-4',5,7-trihydroxy-8-methylflavanone (6), 2,4'-dihydroxy-4-methoxydihydro-chalcone (7), (2S)-4'-hydroxy-7-methoxylflavanone (8), a-tocopherol (9), (25)-3'-hydroxy-4',7-dimethoxylfalvan (10), coniferaldehyde (11), 2,4-dihydroxy-6-methoxy-3-methyacetophenone (12), 2',6'-dimethoxy-4'-hydroxyacetophenone (13), (2-hydroxy-4-methoxyphenyl) ethanol (14), p-sitosterol (15).These results showed that non-alkaloids portion of Lycoris aurea, as the same as other genus of Amaryllidaceae, contains mainly flavans. Other compounds as for aromatic compounds maybe the biosynthesis materials of flavonoid in this plant. It is interesting that compound 9, a vitamin, was isolated from this plant, which exited ubiquitously in vegetables and fruits. The flavans existed widely in this plant were different from generic flavonoids, and only few literatures concerned activities about them, so we could use this plant of Lycoris aurea as a source of falvans to study its activities. 2. Study on chemical constituents of Bidens pilosaIn Chinese fork medicine, Bidens pilosa has been used for various diseases. Recently, its hypotensive activities attracted the attention of scientists. In the course of screening hypotensive fractions, it was found that the extracts of water of Bidens pilosa exhibited stronger hypotensive effect than total extracts. In order to isolate and identify the bioactive constituents, we investigated the extracts of water.Investigation on the chemical constituents of the plant collected in kunming, led to...