Studies On The Anti-hepatoma Constituents Of Nigella Glandulifera

The genus Nigella (Ranunculaceae) contains about20species, distributed mainly in theMediterranean region and west Asia. Nigella glandulifera Freyn et Sint is one of the speciegrowing in China, Xinjiang and Xishuangbanna.The whole herb has been used as a folkremedy for treatment of colds, cough and insomnia, its seeds are commonly eaten in manyfood preparations by Uigur. The seeds are believed to have diuretic, analgesic, spasmolytic,galactagogue and bronchodilator properties, and can cure edema, urinary calculus andbronchial asthma.The seeds of Nigella glandulifera as the raw material were extracted with butyl alcoholand ethyl ethanoate, then isolated with the silica gel columnchromatography, ODS columnchromatography. At last, nine compounds were obtained. On the grounds of chemical andspectroscopic methods, their structures were identified as Salfredione B11(1), NigellamineA1(2), Nigellamine A2(3), Nigellamine B1(4), Sieboldianoside A (5), Nigephenol A (6),Nigephenol B (7), Nigephenol C (8) and nigeglamine (9). As a result, the compound (6),(7),(9) is a new compound, and the compound (8) is a new natural compound. By biologicalactivity tests, we found that nine compounds have certain anti-hepatoma activity, which ofcompound (3) has the strongest activity.We use natural products--hederagenin as a lead compounds, methods of organicsynthesis and NMR technology as a tool, combined with biological activity tests, carried outresearch work to optimize its strueture. By hederagenin at C-12and C-13structuralmodification and transformation, exploration and research synthesis route, the final sixhederagenin derivatives was synthesized, in which4compounds has never been reported inthe literature. By biological activity tests, we found that to be compared with hederagenin,after structural modification of compounds have better anti-hepatoma activity.