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(jiàn)問(wèn)題列表
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(duì) 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.