He Yu-Min, Zhu Shu, Ge Yue-Wei, Cai Shao-Qing, Komatsu Katsuko
Division of Pharmacognosy, Department of Medicinal Resources, Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama, 930-0194, Japan.
J Nat Med. 2015 Jul;69(3):366-74. doi: 10.1007/s11418-015-0903-y. Epub 2015 Apr 19.
The root of Gentiana crassicaulis has been widely used for the treatment of rheumatism, arthralgia, apoplexy, jaundice and diabetes in traditional medicines, and contains secoiridoid glycosides as the main active ingredients. In the present study, five new secoiridoid glycosides, 6'-O-β-D-xylopyranosylgentiopicroside (1) and gentiananosides A-D (2-5), together with 11 known ones were isolated from the MeOH extract of dried roots of G. crassicaulis. Their structures were elucidated on the basis of extensive spectroscopic evidence. Of them, gentiananosides A (2) and B (3) were concluded to be novel secoiridoid glycosides with an ether linkage between C-2' of the sugar moiety and C-3 of the aglycone. Compounds 1, 4, 5, 7, 8, 12-14 exhibited moderate inhibitory effects against lipopolysaccharide-induced nitric oxide and interleukin-6 (IL-6) production in RAW264 cells, whereas 2 and 15 exhibited moderate inhibitory effects only against IL-6 production.
粗茎秦艽的根在传统医学中已被广泛用于治疗风湿、关节痛、中风、黄疸和糖尿病，其主要活性成分是裂环烯醚萜苷。在本研究中，从粗茎秦艽干燥根的甲醇提取物中分离出5个新的裂环烯醚萜苷，即6'-O-β-D-吡喃木糖基龙胆苦苷（1）和秦艽环苷A-D（2-5），以及11个已知化合物。它们的结构通过广泛的光谱证据得以阐明。其中，秦艽环苷A（2）和B（3）被确定为新型裂环烯醚萜苷，其糖部分的C-2'与苷元的C-3之间存在醚键。化合物1、4、5、7、8、12-14对RAW264细胞中脂多糖诱导的一氧化氮和白细胞介素-6（IL-6）的产生具有中等抑制作用，而化合物2和15仅对IL-6的产生具有中等抑制作用。
