Gambogic Acid(Guttatic Acid, Guttic Acid, Beta-Guttiferrin)能够激活caspases,其EC50值在0.78至1.64 μM之间。此外,它还能完全抑制Bcl-XL、Bcl-2、Bcl-W、Bcl-B、Bfl-1 和 Mcl-1等Bcl-2家族蛋白的活性,IC50值分别为1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM 和 0.79 μM。
靶点Target | Value |
---|---|
Bcl-w | 0.02 μM |
Bcl-B | 0.66 μM |
Mcl-1 | 0.79 μM |
Bfl-1 | 1.06 μM |
Bcl-2 | 1.21 μM |
Gambogic Acid 是一种笼呫吨酮,来源于藤黄。它通过抑制人类Bcl-2家族蛋白并活化胱天蛋白酶,在多种癌细胞中产生了强烈的凋亡诱导作用。此外,它还能阻断Kir2.1通道(EC50 ≤ 100 nM),并在纳摩尔浓度下显著抑制人脐静脉内皮细胞 (HUVEC) 的增殖、迁移、侵袭、血管形成和微血管生长。
体内研究Gambogic Acid 能够有效抑制肿瘤血管生成,并减缓肿瘤生长,副作用较小,适合用于节律化疗。该物质具有多种功能效应,包括诱导细胞凋亡、抑制增殖、防止癌症转移以及抑制肿瘤血管生成。在动物模型和临床试验中,Gambogic Acid 有效地抑制了肿瘤的生长,并且其副作用较低,对免疫系统和造血系统的毒性较小。它还能产生组织特异性蛋白酶抑制作用及肿瘤特异性毒性。LD50: 小鼠45毫克/千克(腹腔注射)。
化学性质 用途中文名称 | 英文名称 | CAS号 | 化学式 | 分子量 |
---|---|---|---|---|
—— | (2Z)-4-[(1R,3aS,5S,11R,14aS)-3a,4,5,7-tetrahydro-8-hydroxy-13-[(2E)-4-hydroxy-3-methylbut-2-en-1-yl]-3,3,11-trimethyl-11-(4-methylpent-3-en-1-yl)-7,15-dioxo-3H,11H-1,5-methanofuro[3,4-g]pyrano[3,2-b]xanthen-1-yl]-2-methylbut-2-enoic acid | 918153-84-1 | C38H44O9 | 644.762 |
—— | methyl gambogate | —— | C39H46O8 | 642.789 |
—— | methyl 6-O-methylgambogate | 2752-66-1 | C40H48O8 | 656.816 |
—— | methyl (2Z)-4-{(1R,3aS,5S,11R,14aS)-3a,4,5,7-tetrahydro-11-[(3E)-5-hydroxy-4-methylpent-3-en-1-yl]-8-methoxy-3,3,11-trimethyl-13-(3-methylbut-2-en-1-yl)-7,15-dioxo-3H,11H-1,5-methanofuro[3,4-g]pyrano[3,2-b]xanthen-1-yl}-2-methylbut-2-enoate | 1160999-20-1 | C40H48O9 | 672.816 |
—— | (37,38)-epoxy-6-methoxy-gambogic acid methyl ester | 933041-21-5 | C40H48O9 | 672.816 |
—— | 2-morpholin-4-ylethyl (Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoate | 857500-60-8 | C44H55NO9 | 741.922 |
—— | 4-piperidin-1-ylbutyl (Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoate | 1355062-28-0 | C47H61NO8 | 768.003 |
—— | 2-piperidin-1-ylethyl (Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoate | 1355062-20-2 | C45H57NO8 | 739.949 |
—— | 3-piperidin-1-ylpropyl (Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoate | 1355062-24-6 | C46H59NO8 | 753.976 |
—— | 4-morpholin-4-ylbutyl (Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoate | 1355062-27-9 | C46H59NO9 | 769.976 |
—— | 2-piperazin-1-ylethyl (Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoate | 1355062-22-4 | C44H56N2O8 | 740.937 |
—— | 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethyl (Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoate | 1355062-21-3 | C46H60N2O9 | 784.99 |
—— | 3-morpholin-4-ylpropyl (Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoate | 1355062-23-5 | C45H57NO9 | 755.949 |
—— | 3-piperazin-1-ylpropyl (Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoate | 1355062-26-8 | C45H58N2O8 | 754.964 |
—— | 4-[4-(2-hydroxyethyl)piperazin-1-yl]butyl (Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoate | 1355062-29-1 | C48H64N2O9 | 813.044 |
—— | (Z)-4-[(1S,2S,8R,17S,19R)-8-[2-(3,3-dimethyloxiran-2-yl)ethyl]-5-[(3,3-dimethyloxiran-2-yl)methyl]-12-hydroxy-8,21,21-trimethyl-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoic acid | 918153-56-7 | C38H44O10 | 660.761 |
—— | 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl (Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoate | 1355062-25-7 | C47H62N2O9 | 799.017 |
—— | [(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl] (Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoate | 1372627-71-8 | C44H54O13 | 790.905 |
—— | methyl (Z)-4-[(1S,2S,17S,19R)-12-hydroxy-11-[(5R)-5-methoxy-5-methyl-2-propan-2-ylidenecyclohexyl]-8,8,21,21-tetramethyl-14,18-dioxo-3,9,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.05,10]docosa-4(13),5(10),11,15-tetraen-19-yl]-2-methylbut-2-enoate | 1228272-49-8 | C40H50O9 | 674.832 |
—— | 9,10-dihydrogambogic acid | —— | C38H46O8 | 630.778 |
—— | (9,10)-Dihydroxy-gambogic acid | 1160999-17-6 | C38H46O10 | 662.777 |