Taraxerol has anti-inflammatory and anticancer effects. Taraxerol attenuates acute inflammation by inhibiting NF-κB signaling[5,6].
Taraxerol downregulates the expression of proinflammatory mediators in macrophages by interfering with the activation of TAK1 and Akt, thus preventing NF-κB activation[3].
Taraxerol enhanced ROS levels and attenuated the MMP (Δψm) in HeLa cells. Taraxerol induced apoptosis mainly via the mitochondrial pathway including the release of cytochrome c to the cytosol and activation of caspases 9 and 3, and anti-poly (ADPribose) polymerase (PARP). Taraxerol could induce the down-regulation of the anti-apoptotic protein Bcl-2 and up-regulation of pro-apoptotic protein Bax. It suppressed the PI3K/ Akt signaling pathway [1].
Taraxerol treatment significantly attenuated carrageenan induced paw edema 2 h onward. The anti-inflammatory effect of taraxerol was sustained up to 4 h[2]. Taraxerol (20mg/kg, p.o.) treatment stimulated glucose metabolism in skeletal muscle, regulated blood glycaemic status and lipid profile in the sera, reduced the secretion of pro-inflammatory cytokines, and restored the renal physiology in T2D rats[4]. AChE activity inhibition in animals and indicate that Taraxerol has anti-amnesic activity that may hold significant therapeutic value in alleviating certain memory impairments observed in AD[7].
参考文献:
[1]: Yaoi X, Lu B, et,al. Taraxerol Induces Cell Apoptosis through A Mitochondria-Mediated Pathway in HeLa Cells. Cell J. 2017 Oct;19(3):512-519. doi: 10.22074/cellj.2017.4543. Epub 2017 Aug 19. PMID: 28836414; PMCID: PMC5572297.
[2]: Khanra R, Dewanjee S, et,al. Taraxerol, a pentacyclic triterpene from Abroma augusta leaf, attenuates acute inflammation via inhibition of NF-κB signaling. Biomed Pharmacother. 2017 Apr;88:918-923. doi: 10.1016/j.biopha.2017.01.132. Epub 2017 Feb 6. PMID: 28178622.
[3]: Yao X, Li G, et,al. Taraxerol inhibits LPS-induced inflammatory responses through suppression of TAK1 and Akt activation. Int Immunopharmacol. 2013 Feb;15(2):316-24. doi: 10.1016/j.intimp.2012.12.032. Epub 2013 Jan 15. PMID: 23333629.
[4]: Khanra R, Bhattacharjee N, et,al. Taraxerol, a pentacyclic triterpenoid, from Abroma augusta leaf attenuates diabetic nephropathy in type 2 diabetic rats. Biomed Pharmacother. 2017 Oct;94:726-741. doi: 10.1016/j.biopha.2017.07.112. Epub 2017 Aug 9. PMID: 28802226.
[5]: Khanra R, Dewanjee S, et,al. (Malvaceae) leaf extract attenuates diabetes induced nephropathy and cardiomyopathy via inhibition of oxidative stress and inflammatory response. J Transl Med. 2015 Jan 16;13:6. doi: 10.1186/s12967-014-0364-1. PMID: 25591455; PMCID: PMC4301895.
[6]: Tsao CC, Shen YC, et,al. New diterpenoids and the bioactivity of Erythrophleum fordii. Bioorg Med Chem. 2008 Nov 15;16(22):9867-70. doi: 10.1016/j.bmc.2008.09.021. Epub 2008 Sep 12. PMID: 18926710.
[7]: Berté TE, Dalmagro AP, Zimath PL, Gon?alves AE, Meyre-Silva C, Bürger C, Weber CJ, Dos Santos DA, Cechinel-Filho V, de Souza MM. Taraxerol as a possible therapeutic agent on memory impairments and Alzheimer's disease: Effects against scopolamine and streptozotocin-induced cognitive dysfunctions. Steroids. 2018 Apr;132:5-11. doi: 10.1016/j.steroids.2018.01.002. PMID: 29355563.
Taraxerol 具有抗炎和抗癌作用。蒲公英甾醇通过抑制 NF-κB 信号通路减轻急性炎症[5,6]。
紫杉醇通过干扰 TAK1 和 Akt 的激活来下调巨噬细胞中促炎介质的表达，从而阻止 NF-κB 激活[3]。
紫杉醇增强了 HeLa 细胞中的 ROS 水平并减弱了 MMP (δψm)。 Taraxerol 主要通过线粒体途径诱导细胞凋亡，包括将细胞色素 c 释放到胞质溶胶和半胱天冬酶 9 和 3 的激活，以及抗多聚 (ADPribose) 聚合酶 (PARP)。 Taraxerol 可诱导抗凋亡蛋白 Bcl-2 的下调和促凋亡蛋白 Bax 的上调。抑制PI3K/Akt信号通路[1]。
2 小时后，紫杉醇处理可显着减轻角叉菜胶诱导的爪水肿。蒲公英甾醇的抗炎作用可持续长达4 h[2]。蒲公英甾醇（20 毫克/千克，口服）治疗可刺激骨骼肌中的葡萄糖代谢，调节血糖状态和血清中的脂质分布，减少促炎细胞因子的分泌，并恢复 T2D 大鼠的肾脏生理机能[4] 。动物 AChE 活性抑制表明 Taraxerol 具有抗遗忘活性，在减轻 AD[7] 中观察到的某些记忆障碍方面可能具有重要的治疗价值。
| Cell experiment [1]: | |
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Cell lines |
RAW264.7 macrophages |
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Preparation Method |
The cells were treated with various concentrations of taraxerol or LPS plus taraxerol for 24 h. Then cells were incubated with 5 mg/ml of MTT working solution for 4 h at 37°C. After being treated with 100 μl of DMSO to dissolve the crystals, the cells were detected under an ELx800 Universal Microplate Reader to measure the absorbance at 570 nm. |
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Reaction Conditions |
0、10、20、40 μM Taraxerol for 1h |
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Applications |
Taraxerol downregulates the expression of proinflammatory mediators in macrophages by interfering with the activation of TAK1 and Akt, thus preventing NF-κB activation. |
| Animal experiment [2]: | |
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Animal models |
Wistar rats (♂, 150 ± 20 g) |
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Preparation Method |
groups were treated with taraxerol at the doses of 5 and 10 mg/kg, i.p., respectively. |
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Dosage form |
5 and 10 mg/kg Taraxerol for 0-4h |
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Applications |
Taraxerol treatment significantly attenuated carrageenan induced paw edema 2 h onward. The anti-inflammatory effect of taraxerol was sustained up to 4 h. |
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参考文献: [1]. Yao X, Li G, et,al. Taraxerol inhibits LPS-induced inflammatory responses through suppression of TAK1 and Akt activation. Int Immunopharmacol. 2013 Feb;15(2):316-24. doi: 10.1016/j.intimp.2012.12.032. Epub 2013 Jan 15. PMID: 23333629. |
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