Ding Pei-Lan, Liao Zhi-Xin, Huang Hai, Zhou Pei, Chen Dao-Feng
Department of Pharmacognosy, School of Pharmacy, Fudan University, 138 Yixueyuan Road, Shanghai 200032, PR China.
Bioorg Med Chem Lett. 2006 Mar 1;16(5):1231-5. doi: 10.1016/j.bmcl.2005.11.073. Epub 2005 Dec 20.
(+)-12alpha-Hydroxysophocarpine (8), a new quinolizidine alkaloid was isolated from the roots of Sophora flavescens, together with 10 known quinolizidine alkaloids, (+)-oxymatrine (1), (+)-matrine (2), (+)-9alpha-hydroxymatrine (3), (+)-allomatrine (4), (+)-oxysophocarpine (5), (-)-sophocarpine (6), (-)-9alpha-hydroxysophocarpine (7), (+)-lehmannine (9), (-)-13,14-dehydrosophoridine (10), and (-)-anagyrine (11). Their structures were elucidated by spectroscopic methods, and the stereochemistry of 8 was confirmed by X-ray analysis. These alkaloids were tested for anti-hepatitis B virus (HBV) activity in vitro, compounds 5, 6, 9, and 10 showed significant anti-HBV activity with inhibitory potency against HBsAg secretion at 48.3-79.3% and that against HBeAg secretion at 24.6-34.6%.
从苦参根中分离得到一种新的喹诺里西啶生物碱(+)-12α-羟基槐果碱(8)，以及10种已知的喹诺里西啶生物碱，即(+)-氧化苦参碱(1)、(+)-苦参碱(2)、(+)-9α-羟基苦参碱(3)、(+)-别苦参碱(4)、(+)-氧化槐果碱(5)、(-)-槐果碱(6)、(-)-9α-羟基槐果碱(7)、(+)-勒曼碱(9)、(-)-13,14-脱氢槐定碱(10)和(-)-臭豆碱(11)。通过光谱方法阐明了它们的结构，并通过X射线分析确定了8的立体化学。对这些生物碱进行了体外抗乙型肝炎病毒(HBV)活性测试，化合物5、6、9和10表现出显著的抗HBV活性，对HBsAg分泌的抑制率为48.3 - 79.3%，对HBeAg分泌的抑制率为24.6 - 34.6%。
