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Limonoids from the Fruits of Melia toosendan and Their NF-kB Modulating Activities

机译:Mel子果实中的柠檬苦素及其NF-κB调节活性

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#$%^&*AU2014100777A420140814.pdf#####Limonoids from the Fruits of Melia toosendan and Their NF-xIB Modulating Activities ABSTRACT Meliaceous limonoids are well known bioactive components of natural pesticides and contemporary medicines. In this study, we identified eight new ring C-seco and ring intact limonoids, named meliatoosins A-H (compounds 1-8), along with 25 known limonoids (compounds 9-33) from the fruits of Melia toosendan (Meliaceae). Their structures were elucidated on the basis of extensive spectroscopic methods including HRMS, ID and 2D NMR experiments. 29 components were evaluated for NF-xIB activities by examining their effects on TNFu-stimulated NF-xIB luciferase activity in HepG2-NF-xB-Luc cells. Among them, 8 compounds (4, 6, 25, 26, 28-31) significantly enhanced the TNFu-induced NF-xIB luciferase activity at 10 ptM, while 10 compounds (11-13, 16, 19, 20, 22-24, 27) suppressed NF-xIB activation. These results suggested that limonoids from M. toosendan could biphasically regulate the TNFu-induced NF-xIB activation. DocRef#00126821-CX M006.030.DRF 26 spec final1/5 0j 23 22/0 100 j0_ /0 0 0 18 _ 21 0 119 11 30 1522 - - ::20 - 15 17 23 0 12- 1 2 1 8 14 20 HO 19 1130 13 17 HO 0 2 9 H1 10 9 14 15 29 2 3 5 6 'OH '" "OH R1 R2 29 28 '-d 1 A OAc 2 OH OAc 4 5 3 B OH R O O HOO HO HO 0/ , 0 A0] . OH 0'l 0 0 R2 R1 R2 0 6 OH C 8 7 OAc D A:4 B: O 0 C: O D: 4 2' 2 F 2' 2' Figure 1
机译:#$%^&* AU2014100777A420140814.pdf #####Mel子果实中的柠檬苦素及其NF-xIB的调节活性抽象melaceceous柠檬苦素是众所周知的天然农药的生物活性成分,当代药物。在这项研究中,我们确定了八个新的环C-seco和环完整的柠檬苦素,称为褪黑激素A-H(化合物1-8),以及25种已知苦Mel(Meliaceae)的果实中的柠檬苦素(化合物9-33)。其在广泛的光谱学方法的基础上阐明了结构,包括HRMS,1D和2D NMR实验。评价了29种成分的NF-xIB通过检查它们对TNFu刺激的NF-xIB荧光素酶活性的影响来检测其活性HepG2-NF-xB-Luc细胞。其中,有8种化合物(4、6、25、26、28-31)在10 ptM下可增强TNFu诱导的NF-xIB荧光素酶活性,而10种化合物(11-13、16、19、20、22-24、27)抑制了NF-xIB的激活。这些结果表明太子参中的柠檬苦素可以双相调节TNFu诱导的NF-xIB激活。M006.030.DRF 26规格最终1/50j 2322/0 100 j0_ / 0 0 0 18 _ 21 0 119 11 30 1522--:: 20-15 17 23 0 12-12 1 8 14 20 HO 19 1130 13 17 HO 02 9 H1 10 9 14 1529 2 3 5 6'OH'“” OHR1 R2 29 28'-d1个OAc2 OH OAc 4 53 B OHO哦好HO0 /,0A0]。 OH 0'l 0 0R2 R1 R2 06羟基碳87 OAc DA:4 B:O 0 C:O D:42'2 F 2'2'图1

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