20831-76-9
20831-76-9 結(jié)構(gòu)式
基本信息
龍膽苦苷
GENTIOPICRIN
GENTIOPICROSIDE
(5R-trans)-6-(beta-D-glucopyranosyloxy)-5,6-dihydro-5-vinyl-1H,3H-pyrano[3,4-c]pyran-1-one
Gentiop icroin
1H,3H-Pyrano[3,4-c]pyran-1-one,5-ethenyl-6-(β-D-
glucopyranosyloxy)-5,6-dihydro-,(5R-trans)-
(5R,6S)-5-ethenyl-6-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-5,6-dihydro-3H-pyrano[5,4-c]pyran-1-one
1H,3H-Pyrano[3,4-c]pyran-1-one, 5-ethenyl-6-(b-D-glucopyranosyloxy)-5,6-dihydro-, (5R,6S)-
1H,3H-Pyrano[3,4-c]pyran-1-one, 5-ethenyl-6-(b-D-glucopyranosyloxy)-5,6-dihydro-, (5R-trans)-
(5R)-5β-Ethenyl-6α-(β-D-glucopyranosyloxy)-5,6-dihydro-1H,3H-pyrano[3,4-c]pyran-1-one
(5R)-5β-Vinyl-6α-(β-D-glucopyranosyloxy)-5,6-dihydro-1H,3H-pyrano[3,4-c]pyran-1-one
6α-(β-D-Glucopyranosyloxy)-5,6-dihydro-5β-vinyl-1H,3H-pyrano[3,4-c]pyran-1-one
物理化學(xué)性質(zhì)
常見問題列表
龍膽苦苷（Gentiopicroside, GPS）是龍膽科植物（如秦艽、龍膽草）中的主要活性成分，為環(huán)烯醚萜苷類，分子式為C16H20O9，具有保護肝臟、抗氧化、抗炎、鎮(zhèn)痛、改善糖尿病并發(fā)癥以及調(diào)節(jié)糖代謝等作用。GPS被中華人民共和國藥典收錄作為龍膽藥材的活性物質(zhì)測試指標(biāo)。
龍膽苦苷是一種天然的環(huán)烯醚萜苷，能夠抑制 P450 的活性，對 CYP2A6 的 IC50 和 Ki 值分別為 61 μM 和 22.8 μM；Gentiopicroside 具有抗炎和抗氧化活性。
| Target | Value |
|
CYP2A6
(in human liver microsomes) | |
|
CYP2E1
(in human liver microsomes) |
Gentiopicroside inhibits P450 activity, with an IC 50 and a K i of 61 μM and 8.12 μM for CYP2A6, also slightly inhibits CYP2E1 activity with an IC 50 of 1.6 mM, but shows no inhibition on CYP1A2 and CYP3A4. Gentiopicroside (12.5, 25 and 50?μM) inhibits RANKL-induced osteoclast formation from mouse bone marrow macrophages (BMMs) in a dose-dependent manner, blocks the expression of osteoclast-related proteins, prevents receptor activator of nuclear factor-κB ligand (RANKL)-triggered JNK and NF-κB activation. Gentiopicroside (50?μM) also inhibits RANKL-induced bone resorption.
Gentiopicroside (20, 40, and 80 mg/kg, p.o.) significantly reduces gastric ulcerindex in mice. Gentiopicroside (20, 40, and 80 mg/kg) also ovbiously decreases the levels of HSP-70, TNF-α, IL-6, MDA and increases ncreased GSH level and SOD activity. In addition, Gentiopicroside normalizes EGF and VEGF level in mice.