AKBA (3-acetyl-11-keto-β-Boswellic Acid)
(Synonyms: 11-羰基-Β-乙酰乳香酸,3-O-acetyl-11-keto-β-Boswellic acid,AKBA) 目录号 : GC14282
AKBA (3-acetyl-11-keto-β-Boswellic Acid)是一种五环三萜酸，能够有效地非竞争性地抑制5-脂氧合酶（5-lipoxygenase, 5-LOX），具有抗炎、抗肿瘤、神经保护等多种生物活性。
Cas No.:67416-61-9
Sample solution is provided at 25 µL, 10mM.
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AKBA (3-acetyl-11-keto-β-Boswellic Acid) is a pentacyclic triterpene acid that effectively and non-competitively inhibits 5-lipoxygenase (5-LOX), exhibiting various biological activities including anti-inflammatory, antitumor, and neuroprotective effects[1, 2]. AKBA can inhibit the NF-κB signaling pathway and also acts as an Nrf2/HO-1 activator[3, 4].
In vitro, pretreatment of human lens epithelial cells (HLECs) with AKBA (2, 8μM) for 1h significantly reduced H2O2-induced apoptosis and oxidative damage, significantly decreased intracellular caspase-3 and Bax expression, and increased Bcl-2 expression[5]. Treatment of MCF-7 cells with AKBA (50, 100, 200µg/mL) for 24h dose-dependently inhibited cell viability, reduced cell colony formation ability, and induced apoptosis and cell cycle arrest[6].
In vivo, AKBA (100mg/kg) significantly reduced the volume and weight of subcutaneous xenograft tumors in mice after oral treatment for 14 days with U87-MG glioblastoma cells[7].
References:
[1] Gong Y, Jiang X, Yang S, et al. The biological activity of 3-O-acetyl-11-keto-β-boswellic acid in nervous system diseases[J]. Neuromolecular medicine, 2022, 24(4): 374-384.
[2] Park Y S, Lee J H, Harwalkar J A, et al. Acetyl-11-Keto-ß-Boswellic acid (Akba) is cytotoxic for meningioma cells and inhibits phosphorylation of the extracellular-signal regulated kinase 1 and 2[M]//Eicosanoids and Other Bioactive Lipids in Cancer, Inflammation, and Radiation Injury, 5. Boston, MA: Springer US, 2002: 387-393.
[3] Lv M, Shao S, Zhang Q, et al. Acetyl-11-Keto-β-Boswellic acid exerts the anti-cancer effects via cell cycle arrest, apoptosis induction and autophagy suppression in non-small cell lung cancer cells[J]. OncoTargets and therapy, 2020: 733-744.
[4] Minj E, Upadhayay S, Mehan S. Nrf2/HO-1 signaling activator acetyl-11-keto-beta boswellic acid (AKBA)-mediated neuroprotection in methyl mercury-induced experimental model of ALS[J]. Neurochemical research, 2021, 46(11): 2867-2884.
[5] Yang T, Lin X, Li H, et al. Acetyl-11-keto-beta boswellic acid (AKBA) protects lens epithelial cells against H2O2-induced oxidative injury and attenuates cataract progression by activating Keap1/Nrf2/HO-1 signaling[J]. Frontiers in Pharmacology, 2022, 13: 927871.
[6] Ahmed S A, Al-Shanon A F, Al-Saffar A Z, et al. Antiproliferative and cell cycle arrest potentials of 3-O-acetyl-11-keto-β-boswellic acid against MCF-7 cells in vitro[J]. Journal of Genetic Engineering and Biotechnology, 2023, 21(1): 75.
[7] Li W, Liu J, Fu W, et al. 3-O-acetyl-11-keto-β-boswellic acid exerts anti-tumor effects in glioblastoma by arresting cell cycle at G2/M phase[J]. Journal of Experimental & Clinical Cancer Research, 2018, 37(1): 132.
AKBA (3-acetyl-11-keto-β-Boswellic Acid)是一种五环三萜酸，能够有效地非竞争性地抑制5-脂氧合酶（5-lipoxygenase, 5-LOX），具有抗炎、抗肿瘤、神经保护等多种生物活性[1, 2]。AKBA能够抑制NF-κB信号通路，还能够作为一种Nrf2/HO-1激活剂[3, 4]。
在体外，AKBA（2, 8μM）预处理人晶状体上皮细胞（HLECs）1h，显著减轻了H2O2诱导的细胞凋亡和氧化损伤，显著降低了细胞内caspase-3和Bax的表达，升高了Bcl-2的表达[5]。AKBA（50, 100, 200µg/mL）处理MCF-7细胞24h，以剂量依赖性方式抑制了细胞活力，降低了细胞克隆形成能力，诱导了细胞凋亡和细胞周期阻滞[6]。
在体内，AKBA（100mg/kg）通过口服治疗U87-MG胶质母细胞瘤细胞异种移植小鼠14天，显著降低了小鼠皮下异种移植瘤的体积和重量[7]。
| Cell experiment [1]: | |
Cell lines | Human lens epithelial cells (HLECs) |
Preparation Method | To create the oxidative stress microenvironment, the cells were incubated with 0, 50, 100, 150, 200, and 250μM H2O2 for 24h. AKBA (3-acetyl-11-keto-β-Boswellic Acid) was dissolved in dimethylsulfoxide as a stock solution of 20mM. In the group pretreated with AKBA, the cells were pretreated with AKBA (2μM, 8μM) for 1h before H2O2 treatment. |
Reaction Conditions | 2, 8μM; 1h |
Applications | AKBA (3-acetyl-11-keto-β-Boswellic Acid) treatment attenuates H2O2-induced apoptosis and oxidative injury in HLECs. |
| Animal experiment [2]: | |
Animal models | BALB/c-nu nude mice |
Preparation Method | Human U87-MG glioblastoma cells were subcutaneously injected into the right flanks of the mice. After 20 days, when the tumor volume reached about 100mm3, the mice were randomly divided into 2 groups and treated once daily for 14 days with AKBA (3-acetyl-11-keto-β-Boswellic Acid) (100mg/kg body weight, p.o.) prepared in 0.5% carboxymethylcellulose sodium or vehicle control. The mice were weighed and tumor size was measured every other day. At the end of the experiment, all the mice were euthanized and the tumor weights and organ weights were recorded. |
Dosage form | 100mg/kg; 14 days; p.o. |
Applications | Oral administration of AKBA (3-acetyl-11-keto-β-Boswellic Acid) significantly decreased the volume and weight of subcutaneous U87-MG xenograft tumors in nude mice. |
References: | |
| Cas No. | 67416-61-9 | SDF | |
| 别名 | 11-羰基-Β-乙酰乳香酸,3-O-acetyl-11-keto-β-Boswellic acid,AKBA | ||
| 化学名 | (3α,4β)-3-(acetyloxy)-11-oxo-urs-12-en-23-oic acid | ||
| Canonical SMILES | O=C1C=C2[C@](CC[C@]3(C)[C@@]2([H])[C@@H](C)[C@H](C)CC3)(C)[C@]4(C)CC[C@@]5([H])[C@@](C)(C(O)=O)[C@H](OC(C)=O)CC[C@]5(C)[C@]41[H] | ||
| 分子式 | C32H48O5 | 分子量 | 512.7 |
| 溶解度 | ≤5mg/ml in ethanol;25mg/ml in DMSO;25mg/ml in dimethyl formamide | 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 | 1.9505 mL | 9.7523 mL | 19.5046 mL |
| 5 mM | 390.1 μL | 1.9505 mL | 3.9009 mL |
| 10 mM | 195 μL | 975.2 μL | 1.9505 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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