雷公藤茎中的二萜类成分及生物活性研究  

Diterpenoids from the Tripterygium wilfordii stems and their biological activities

作　　者：周晓琼 饶凯瑞 陈宣钦[1] ZHOU Xiao-qiong;RAO Kai-rui;CHEN Xuan-qin(School of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, China)

机构地区：[1]昆明理工大学生命科学与技术学院,昆明650500

出　　处：《天然产物研究与开发》2021年第7期1137-1146,共10页Natural Product Research and Development

基　　金：国家自然科学基金(31660102);云南省自然科学基金(2018FB034)。

摘　　要：综合运用正相硅胶柱色谱、中压液相色谱(MPLC)、羟丙基葡聚糖凝胶(Sephadex LH-20)及高效液相色谱等多种方法,从雷公藤Tripterygium wilfordii Hook.f.茎乙醇提取物的乙酸乙酯相中分离鉴定了1个新的松香烷型二萜wiltriptobenzene(1)和19个已知的二萜,包括雷藤二萜醌H(2)、triptoquinone B(3)、hinokione(4)、雷酚萜(5)、triptonediol(6)、triptobenzene A(7)、wilforol F(8)、triptobenzene B(9)、abietatrien-3β-ol(10)、triptobenzene S(11)、hypoglicin B(12)、triregelin H(13)、雷酚内酯(14)、雷酚新内酯(15)、16α-hydroxy-19,20-epoxy-19R*-methoxy-kaurane(16)、16α-hydroxy-19,20-epoxy-20R*-ethoxy-kaurane(17)、16α-hydroxy-19,20-epoxy-19R*-ethoxy-kaurane(18)、fischericin D(19)和ent-pimara-8(14),15-diene-19-ol(20)。化合物的结构通过与文献对比核磁共振波谱数据确定。化合物10、19和20首次报道从雷公藤中分离得到。在脂多糖(LPS)诱导小鼠单核巨噬细胞(RAW 264.7)的模型中,评价了化合物1~20的体外抗炎活性;采用MTT法评价了化合物1~20的体外抗人体宫颈癌(Hela)细胞株活性。化合物2、3和20具有显著的抗炎活性,其半数抑制NO生成的IC50值分别为2.01、1.70和1.77μmol/L。化合物11具有微弱的体外抗肿瘤活性,IC50值为18.41μmol/L。A new diterpene quinone wiltriptobenzene(1)and nineteen known ones,including triptoquinone H(2),triptoquinone B(3),hinokione(4),triptonoterpene(5),triptonediol(6),triptobenzene A(7),wilforol F(8),triptobenzene B(9),abietatrien-3β-ol(10),triptobenzene S(11),hypoglicin B(12),triregelin H(13),triptophenolide(14),neotriptophenolide(15),16α-hydroxy-19,20-epoxy-19R*-methoxy-kaurane(16),16α-hydroxy-19,20-epoxy-20R*-ethoxy-kaurane(17),16α-hydroxy-19,20-epoxy-19R*-ethoxy-kaurane(18),fischericin D(19),and ent-pimara-8(14),15-diene-19-ol(20)were isolated from the ethyl acetate extract of Tripterygium wilfordii by silica gel,medium pressure liquid chromatography(MPLC),Sephadex LH-20,and HPLC chromatograph.The structures of them were established by extensive spectroscopic methods and comparing the data with those in the literature.Compounds 10,19,and 20 were isolated from T.wilfordii for the first time.The anti-inflammatory of activity of 1~20 was evaluated in LPS-induced RAW 264.7 cells.Anti-tumor activity of 1-20 in vitro against HeLa cell line was examined by MTT method.Compounds 2,3,and 20 exhibited significant activity to inhibit NO production with IC50 values of 2.01,1.70 and 1.77μmol/L.Compound 11 exhibited weak anti-tumor activity(IC50=18.41μmol/L).

关 键 词：雷公藤 二萜 抗炎活性 抗肿瘤活性 

分 类 号：R284.1[医药卫生—中药学]