|(3R,4R,4aR,6aR,6bS,8aR,11R,12S,12aR,14aR,14bS)-3-乙酰氧基-4,6a,6b,8a,11,12,14b-七甲基-14-氧代-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,14,14a,14b-二十氢苉-4-羧酸|CsnPharm

CAS No.: 67416-61-9

AKBA Catalog No. CSN19355

Synonyms: Acetyl-11-keto-β-boswellic acid;3-acetyl-11-keto-β-Boswellic Acid;3-O-acetyl-11-keto-β-Boswellic acid

AKBA is a novel Nrf2 activator which can increase basal and UVA-induced levels of Nrf2.

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生物活性

实验方案

技术信息

生物活性

描述Acetyl-11-keto-β-boswellic acid (AKBA), a naturally occurring pentacyclic triterpene isolated from the gum resin exudate from the stem of the tree Boswellia serrata (frankincense), is a Nrf2 activator against a large number of inflammatory diseases, including cancer, arthritis, chronic colitis, ulcerative colitis, Crohn's disease, and bronchial asthma^[3]. AKBA is as a novel, orally active, non-redox and non-competitive 5-lipoxygenase inhibitor that also inhibits topisomerase I and II in vitro^[4]. AKBA enhances apoptosis induced by cytokines and chemotherapeutic agents, inhibits invasion, and suppresses osteoclastogenesis through inhibition of NF-κB-regulated gene expression^[3]. In tumor cells, AKBA suppressed both inducible and constitutive NF-κB activation examined by DNA binding. AKBA inhibited the TNF-induced activation of IκBα kinase (IKK), IκBα phosphorylation, IκBα ubiquitination, IκBα degradation, p65 phosphorylation, and p65 nuclear translocation^[3]. AKBA inhibited the NF-κB-dependent reporter gene expression activated by TNFR type 1, TNFR-associated death domain protein, TNFR-associated factor 2, NF-κB-inducing kinase, and IKK^[3]. Induction of apoptosis in HL-60 and CCRF-CEM by AKBA may be due to inhibition of topoisomerase I in these cells^[5]. AKBA suppressed tumor growth in the human prostate tumor xenograft mice treated daily (10 mg/kg AKBA), whose inhibitory effect on tumor growth was well correlated with suppression of angiogenesis induced by VEGFR2 signaling pathways^[6]. In mice, AKBA significantly inhibited blood vessel formation in the Matrigel plug assay and effectively suppressed vascular endothelial growth factor (VEGF)–induced microvessel sprouting in rat aortic ring assay ex vivo^[6]. In vitro, AKBA suppressed VEGF-induced phosphorylation of VEGF receptor 2 (VEGFR2) kinase (KDR/Flk-1) with IC50 of 1.68 μmol/L^[6]. At low micromolar concentrations, AKBA rapidly and potently inhibited the phosphorylation of Erk-1/2 and impaired the motility of meningioma cells^[7]. AKBA inhibits the motility of meningioma cells showing a potent cytotoxic activity with half-maximal inhibitory concentrations in the range of 2 - 8 μM^[7].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03612986	Knee Osteoarthritis	Not Applicable	Not yet recruiting	February 15, 2019	Romania ... more >> Opera Contract Research Organization S.r.l. Not yet recruiting Timişoara, Timis, Romania, 300209 Contact: Serban Rosu, MD +40722313224 rosu@operacro.com Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9504 mL
- 9.7519 mL
- 19.5038 mL
- 5 mM
- 0.3901 mL
- 1.9504 mL
- 3.9008 mL
- 10 mM
- 0.1950 mL
- 0.9752 mL
- 1.9504 mL

技术信息

CAS号

67416-61-9

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C32H48O5

运输

蓝冰

分子量

512.72

别名

Acetyl-11-keto-β-boswellic acid;3-acetyl-11-keto-β-Boswellic Acid;3-O-acetyl-11-keto-β-Boswellic acid;Acetylketo-β-boswellic acid;11-羰基-Β-乙酰乳香酸

溶解度

DMSO	100.0 mg/mL (195.0 mM)

动物实验配方

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