The anti-inflammatory secoiridoid glycosides from Gentianae Scabrae Radix: the root and rhizome of Gentiana scabra
The anti-inflammatory secoiridoid glycosides from Gentianae Scabrae Radix: the root and rhizome of Gentiana scabra
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DOI：
10.1007/s11418-015-0894-8
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发表时间：
2015-07-01
影响因子：
3.3
通讯作者：
Komatsu, Katsuko
中科院分区：
文献类型：
--
作者：
He, Yu-Min;Zhu, Shu;Komatsu, Katsuko
龙胆是一种著名的传统药物，用于治疗肝炎、胆囊炎和炎症性疾病。它主要由开环环烯醚萜苷组成，代表为龙胆苦苷、当药苷和当药苦苷。本研究对龙胆（Gentiana scabra Bunge）的CHCl 3提取物进行了化学研究，得到了7个新的（1-7）和10个已知的（8- 1 - 7）开环环烯醚萜苷。通过大量的光谱分析和与文献数据的比较，确定了它们的结构。评价了所有17个化合物对脂多糖（LPS）诱导的RAW 264细胞中NO、IL-6和TNF-α产生的抑制作用。其中，8-表姜苷衍生物1-3，姜苷衍生物4、5和10，和一种SWERO SIDE衍生物6显示出对IL-6产生的抑制活性，其IC 50值为51.70-61.10 μ M，而当药苷衍生物12和15-17以及当药苦苷衍生物13显示出对NO和IL-2的抑制作用，IC_（50）分别为64.74-94.95和48.91-75.45 μ M。在TNF-α生物测定中，所有化合物均表现出弱的抑制活性（IC 50> 100 μ M）。最后，这些开环环烯醚萜苷的一级构效关系进行了讨论。
Gentianae Scabrae Radix is a well-known traditional medicine that is used for the treatment of hepatitis, cholecystitis and inflammatory diseases. It consists mainly of secoiridoid glycosides, with representatives of gentiopicroside, sweroside and swertiamarin. In the present study, a chemical investigation of the CHCl3 extract of Gentianae Scabrae Radix derived from Gentiana scabra Bunge yielded seven new (1-7) and ten known (8-17) secoiridoid glycosides. Their structures were elucidated by extensive spectroscopic analyses and comparison with literature data. All 17 compounds were evaluated for their inhibitory effects against NO, IL-6 and TNF-alpha productions induced by lipopolysaccharide (LPS) in RAW264 cells. Among them, 8-epi-kingiside derivatives 1-3; kingiside derivatives 4, 5 and 10; and a sweroside derivative 6 showed inhibition activity against IL-6 production with IC50 values of 51.70-61.10 mu M, whereas sweroside derivatives 12 and 15-17 and a swertiamarin derivative 13 showed inhibition effects on both NO and IL-6 productions with IC50 values of 64.74-94.95 and 48.91-75.45 mu M, respectively. All the compounds exhibited weak inhibitory activity (IC50 > 100 mu M) in a TNF-alpha bioassay. Finally, a primary structure-activity relationship of these secoiridoid glycosides is discussed.