State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, People's Republic of China.
J Agric Food Chem. 2010 Feb 10;58(3):1572-7. doi: 10.1021/jf903434h.
Two new quassinoids, javanicolide E (1) and javanicolide F (2), along with fifteen known C-20 quassinoids were isolated from the seeds of Brucea javanica (L.) Merr. The antitobacco mosaic virus (TMV) activity of these quassinoids was screened by the conventional half-leaf and leaf-disk method along with Western blot analysis. All of the seventeen quassinoids showed potent anti-TMV activity. Among them, eight compounds, brusatol (3), bruceine B (4), bruceoside B (5), yadanzioside I (6), yadanzioside L (7), bruceine D (8), yadanziolide A (9), and aglycone of yadanziolide D (17), showed strong antiviral activities, with IC(50) values in the range of 3.42-5.66 microM, and were much more effective than the positive control, ningnanmycin (IC(50) = 117.3 microM). The antiviral structure-activity relationships of quassinoids against TMV were also discussed.
从苦木科鸦胆子属植物鸦胆子(Brucea javanica(L.)Merr.)种子中分离得到两个新的苦木苦味素,即 javanicolide E(1)和 javanicolide F(2),以及 15 个已知的 C-20 苦木苦味素。采用传统半叶法和叶圆片法及 Western blot 分析对这些苦木苦味素进行抗烟草花叶病毒(TMV)活性筛选。17 个苦木苦味素均表现出较强的抗 TMV 活性。其中,8 个化合物,即鸦胆子醇(3)、鸦胆子内酯 B(4)、鸦胆子苷 B(5)、鸦胆子苷 I(6)、鸦胆子苷 L(7)、鸦胆子内酯 D(8)、鸦胆子内酯 A(9)和鸦胆子内酯 D 的苷元(17)表现出较强的抗病毒活性,IC50 值在 3.42-5.66 μM 范围内,比阳性对照宁南霉素(IC50 = 117.3 μM)的效果要好得多。还讨论了苦木苦味素类化合物抗 TMV 的构效关系。