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作 者:王亚丹[1] 张贵杰[1] 屈晶[1] 李玉环[2] 蒋建东[1,2] 庾石山[1]
机构地区:[1]中国医学科学院&北京协和医学院药物研究所、天然药物活性物质与功能国家重点实验室,北京100050 [2]中国医学科学院&北京协和医学院医药生物技术研究所,北京100050
出 处:《国际药学研究杂志》2013年第6期772-777,共6页Journal of International Pharmaceutical Research
摘 要:目的研究大八角根(RadixIlliciiMaji)中二萜类化学成分及其抗B3型柯萨奇病毒的活性。方法采用硅胶、C18反相硅胶、SephadexLH-20柱色谱以及制备HPLC等方法对二萜类化合物进行分离纯化,通过波谱学方法以及Mo(OAc)。诱导的圆二色谱法鉴定其结构,并采用细胞病变效应(cytopathiceffect,CPE)法对分离得到的化合物进行抗柯萨奇病毒B3的活性评价。结果分离鉴定了12个二萜类化合物,分别为4-表-脱氢松香酸(4-epi—dehydroabieticacid,1)、8,11,13,15-四烯松香烷-19-烷酸(8,11,13,15-abietatraen-19-oicacid,2)、jiadifenoicacidsB(3)、C(4)、G(5)和I(6)、majusanicacidsB(7)和D(8)、lamberticacid(9)、angustanoicacidsF(10)和G(11),及13-hydroxy-8,11,13-podocarpatrien-19-oicacid(12),经活性筛选发现,这些化合物具有较好的抗柯萨奇病毒B3的活性,IC50值为3.3—66.7μmol/ml。结论大八角根中的二萜类化合物抗B3型柯萨奇病毒的活性及毒性与其分子中的含氧取代密切相关,化合物3—6和9为首次从该植物中分离得到的化合物。Objective To investigate the diterpenoids from the roots of lllicium majus (Radix lllcii Maji) and their antiviral activity against the Coxsackie B virus. Methods The compounds were isolated by column chromatography over silica gel, octadecylsi- lane chemically bonded silica gel(ODS) , and Sephadex HL-20 coupled with preparative HPLC. Their stuctures were elucidated by spectroscopic analysis and the in situ dimolybdenum circular dichroism (CD) method, and their antiviral activities against the Coxsackie B3 virus were evaluated by cytopathic effect(CPE) method. Results Twelve diterpenoids were isolated from the roots of Illicium rea- l'us, which were identified as 4-epi-dehydroabietic acid ( 1 ), 8,11,13,15-abietatraen-19-oic acid ( 2 ), jiadifenoic acids B ( 3 ), C ( 4 ), G(5) and I(6), majusanic acids B(7) and D(8), lambertic acid(9), angustanoic acids F(10) and G(ll), and 13-hydroxy-8,11, 13-podocarpatrien-19-oic acid(12). These diterpenoids displayed antiviral activity against the Coxsackie B3 virus, with IC50 values of 3.3-66.7 μmol/ml. Conclusion The antiviral activity and cytotoxicity of the diterpenoids relate to the substituent species and posi- tion. Compounds 3-6 and 9 were obtained from this plant for the first time.
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