| CAS |
No.2752-65-0 |
| 中文名称 |
藤黄酸(10mM in DMSO,无菌） |
| 英文名称 |
Gambogic Acid(10mM in DMSO，Sterile） |
| 分子式 |
C38H44O8 |
| 分子量 |
628.75 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
Bcl-2 Family |
| 通路 |
Apoptosis |
| 背景说明 |
据报道，可以抑制 Bcl-XL，Bcl-2，Bcl-W，Bcl-B，Bfl-1 和 Mcl-1。 |
| 生物活性 |
Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-XL， Bcl-2， Bcl-W， Bcl-B， Bfl-1 and Mcl-1 with IC50s of 1.47 μM， 1.21 μM， 2.02 μM， 0.66 μM， 1.06 μM and 0.79 μM.[1-2] |
| In Vitro |
Gambogic Acid 已证明对培养的肿瘤细胞系具有细胞毒活性，其浓度可杀死 50% 的细胞 (LD50 约为 1 μM)。使用 FPA 对比了 Gambogic Acid 对 6 种人类抗凋亡 Bcl-2 家族蛋白的活性。Gambogic Acid 在不同程度上取代与所有 6 种蛋白质结合的 FITC-BH3 肽，表观 IC50 对 Bcl-XL 为 1.47 μM，对 Bcl-2 为 1.21 μM，2.02 μM 用于 Bcl-W，0.66 μM 用于 Bcl-B，1.06 μM 用于 Bfl-1，0.79 μM 用于 Mcl-1[1]。暴露 48 小时后，通过 MTT 测定评估 Gambogic Acid 或顺铂 (CDDP) 对 A549、NCI-H460 和 NCI-H1299 细胞的生长抑制作用。Gambogic Acid 和 CDDP 对细胞生长具有浓度依赖性抑制作用，A549 细胞的 IC50 为 3.56±0.36 和 21.88±3.21 μM，NCI 为 4.05±0.51 和 25.76±4.03 μM-H460 细胞，NCI-H1299 细胞为 1.12±0.31 μM 和 25.21±4.38 μM[2]。 |
| In Vivo |
为了进一步研究 Gambogic Acid (Beta-Guttiferrin) 是否协同 CDDP 对抗体内肿瘤生长，将 A549 肿瘤植入 SCID 小鼠体内。CDDP 联合 Gambogic Acid 对小鼠的抑瘤率为 69.3%，而单独用 CDDP 和 Gambogic Acid 对小鼠的抑瘤率分别为57.2%和29.0%[2]。 |
| 细胞实验 |
The in vitro cell viability effects of Gambogic Acid， CDDP alone， or combined treatments are determined by MTT assay. The cells (2×104 cells per mL) are seeded into 96-well culture plates. After overnight incubation， A549 cells are treated with Gambogic Acid (0.44， 0.88， 1.75， 3.5， 7， 10.5 and 14 μM); NCI-H460 cells are treated with Gambogic Acid (0.5， 1， 2， 4， 8， 12 and 16 μM); NCI-H1299 cells are treated with Gambogic Acid (0.125， 0.25， 0.5， 1， 2 and 4 μM). For the combined treatment in NSCLC cells， three sequences are tested: (a) Gambogic Acid followed by CDDP cells are exposed to Gambogic Acid for 48?h， and then after washout of Gambogic Acid， cells are treated with CDDP for an additional 48?h; (b) CDDP followed by Gambogic Acid cells are exposed to CDDP for 48?h， and then after washout of CDDP， cells are treated with Gambogic Acid for an additional 48?h; and (c) concurrent treatment cells are exposed to both Gambogic Acid and ADM for 48?h. The nature of the drug interaction is analysed by using the combination index (CI)[2]. |
| 动物实验 |
Mice[2]To determine the in vivo antitumour activity of Gambogic Acid combined with CDDP， viable A549 cells (5×106/100?μL PBS per mouse) are subcutaneously injected into the right flank of 7- to 8-week-old male SCID mice. When the average tumor volume reach 100?mm3， the mice are randomly divided into four treatment groups， including control (saline only， n=5)， Gambogic Acid (3.0?mg/kg per 2 days， intravenously; n=6)， CDDP (4?mg/kg per week， intravenously; n=6)， and sequential combination (CDDP treatment one day before Gambogic Acid treatment， n=6). CDDP (4?mg/kg， weekly) is generally administered at doses less than the maximum-tolerated dose in an attempt to allow any additive effects of combination treatment with platinum-based agents and Gambogic Acid to be more easily detected. Tumor size is measured once every 2 days with a calipre. Body weight is recorded once every 2 days. After 14 days， the mice are killed and the tumors are excised and stored at -80?°C until further analysis. |
| 数据来源文献 |
[1]. Zhai D， et al. Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins. Mol Cancer Ther. 2008 Jun;7(6):1639-46.
[2]. Wang LH， et al. Gambogic acid synergistically potentiates cisplatin-induced apoptosis in non-small-cell lung cancer through suppressing NF-κB and MAPK/HO-1 signalling. Br J Cancer. 2014 Jan 21;110(2):341-52. |
| 规格 |
1ml |
| 单位 |
瓶 |
中文
英语
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