Gambogic Acid
(Synonyms: 藤黄酸; Beta-Guttiferrin) 目录号 : GC12139
Gambogic Acid 是一种细胞渗透性 caspase 激活剂和细胞凋亡诱导剂，常用于乳腺癌、肺癌和肝癌等的研究。
Cas No.:2752-65-0
Sample solution is provided at 25 µL, 10mM.
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Gambogic Acid A cell-permeable caspase activator and apoptosis inducer commonly used in studies of breast, lung, and liver cancers[1].
Gambogic Acid (1.2-4.8μM; 24-72h) reduced the viability of Jurkat and Molt-4 cells in a dose-dependent manner, The IC50 values of Gambogic Acid for Jurkat and Molt-4 were 2.23 and 3.03µM, respectively[2]. Gambogic Acid (2.4, 4.8µM; 72h) at concentrations of 2.4 and 4.8µM led to a remarkable increase in G2/M phase, with a corresponding decrease in the S phase compared with exposure of cells to 1.2µM Gambogic Acid[3]. Gambogic Acid (1μM; 24h) treatment increased the levels of poly-ubiquitinated proteins, proteasome-substrate proteins (e.g. Nrf1, Mcl-1, and Noxa) and ER stress marker proteins (e.g. phospho-eIF2α, ATF4, and CHOP) [4].
Gambogic Acid (4, 8mg/kg; ip; twice) dose-dependently reduced the tumor size without inducing any loss of body weight[4]. In murine CT26 tumor-bearing mouse models, the treatment with Gambogic Acid (2, 8mg/kg; bid; 12d) reduced the volumes and weights of CRC solid tumors,The average of tumor weight decreased from 1.139g (control group) to 0.445g (low-dose group), or 0.214g (high-dose group) [5].
References:
[1]Vichitsakul K, Laowichuwakonnukul K, Soontornworajit B, et al. Anti-proliferation and induction of mitochondria-mediated apoptosis by Garcinia hanburyi resin in colorectal cancer cells[J]. Heliyon, 2023, 9(6).
[2].Zhai D, Jin C, Shiau CW, Kitada S, Satterthwait AC, Reed JC. Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins. Mol Cancer Ther. 2008 Jun;7(6):1639-46.
[3].Gambogic acid inhibits proliferation and induces apoptosis of human acute T‑cell leukemia cells by inducing autophagy and downregulating β‑catenin signaling pathway: Mechanisms underlying the effect of Gambogic acid on T‑ALL cells. Oncol Rep. 2020 Oct;44(4):1747-1757.
[4]. Seo MJ, Lee DM, Kim IY, Lee D, Choi MK, Lee JY, Park SS, Jeong SY, Choi EK, Choi KS. Gambogic acid triggers vacuolization-associated cell death in cancer cells via disruption of thiol proteostasis. Cell Death Dis. 2019 Feb 22;10(3):187.
[5]. Xu H, Zhang D, Wei R, Zhou Y, Dai G, Li J, Sun Y, Li F, Xi L. Gambogic Acid Induces Pyroptosis of Colorectal Cancer Cells through the GSDME-Dependent Pathway and Elicits an Antitumor Immune Response. Cancers (Basel). 2022 Nov 9;14(22):5505.
Gambogic Acid 是一种细胞渗透性 caspase 激活剂和细胞凋亡诱导剂，常用于乳腺癌、肺癌和肝癌等的研究[1]。
Gambogic Acid（1.2-4.8μM；24-72h）以剂量依赖性方式降低 Jurkat 和 Molt-4 细胞的活力，Gambogic Acid对 Jurkat 和 Molt-4 的 IC50 值分别为 2.23 和 3.03µM[2]。浓度为 2.4 和 4.8µM 的Gambogic Acid（2.4，4.8µM；72h）导致 G2/M 期显著增加，而与暴露于 1.2µM Gambogic Acid的细胞相比，S 期相应减少[3]。Gambogic Acid（1μM；24 h）治疗可增加多泛素化蛋白、蛋白酶体底物蛋白 (例如 Nrf1、Mcl-1 和 Noxa) 和 ER 应激标记蛋白 (例如磷酸化 eIF2α、ATF4 和 CHOP) 的水平 [4]。
Gambogic Acid（4，8mg/kg；ip；twice）剂量依赖性地缩小了肿瘤大小，而不会引起体重减轻[4]。在小鼠CT26肿瘤模型中，Gambogic Acid（2.8mg/kg；bid；12d）治疗可减小CRC实体瘤的体积和重量，平均肿瘤重量从1.139g(对照组)降低到0.445g(低剂量组)或0.214g(高剂量组)[5]。
| Cell experiment [1]: | |
Cell lines | MDA-MB 435S cell |
Preparation Method | To test the detoxification of Gambogic Acid, aliquots of serum-free DMEM containing 1μM Gambogic Acid and different concentrations of NAC were pre-incubated at room temperature for the indicated time points, and then incubated with MDA-MB 435S cell cultures for 24h. |
Reaction Conditions | Gambogic Acid: 1μM; 24h |
Applications | Gambogic Acid treatment progressively increased the levels of poly-ubiquitinated proteins, proteasome-substrate proteins (e.g.Nrf1, Mcl-1, and Noxa) and ER stress marker proteins (e.g. phospho-eIF2α, ATF4, and CHOP). |
| Animal experiment [1]: | |
Animal models | Xenograft tumor model |
Preparation Method | Mice were randomized into 3 groups, including vehicle (PBS containing 0.25% DMSO), 4mg/kg Gambogic Acid and 8mg/kg Gambogic Acid, and mice were received twice intraperitoneal (ip) injections of Gambogic Acid at the indicated concentrations (day 0 and day 2). On the 14th day, mice were sacrificed and the tumors were isolated. |
Dosage form | Gambogic Acid: 4, 8mg/kg; ip; twice |
Applications | Gambogic Acid (4, 8mg/kg; ip; twice) dose-dependently reduced the tumor size without inducing any significant loss of body weight. |
References: | |
| Cas No. | 2752-65-0 | SDF | |
| 别名 | 藤黄酸; Beta-Guttiferrin | ||
| 化学名 | (Z)-4-((1S,3aR,5S,11R,14aS)-8-hydroxy-2,2,11-trimethyl-13-(3-methylbut-2-en-1-yl)-11-(4-methylpent-3-en-1-yl)-4,7-dioxo-2,3a,4,5,7,11-hexahydro-1H-1,5-methanofuro[3,2-g]pyrano[3,2-b]xanthen-3a-yl)-2-methylbut-2-enoic acid | ||
| Canonical SMILES | C/C(C)=C\CC[C@]1(C)C=CC(C(O)=C(C(C([C@]2([C@@H](C3)C(C)(C)O[C@]24C/C=C(C(O)=O)/C)O5)=C[C@H]3C4=O)=O)C5=C6C/C=C(C)\C)=C6O1 | ||
| 分子式 | C38H44O8 | 分子量 | 628.75 |
| 溶解度 | ≥ 22.45 mg/mL in DMSO, ≥ 48.2 mg/mL in EtOH | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5905 mL | 7.9523 mL | 15.9046 mL |
| 5 mM | 0.3181 mL | 1.5905 mL | 3.1809 mL |
| 10 mM | 0.159 mL | 0.7952 mL | 1.5905 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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