Cell lines

RAW264.7 macrophages

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℃. 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.

Reaction Conditions

0、10、20、40 μM Taraxerol for 1h

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 models

Wistar rats (♂, 150 ± 20 g)

Preparation Method

groups were treated with taraxerol at the doses of 5 and 10 mg/kg, i.p., respectively.

Dosage form

5 and 10 mg/kg Taraxerol for 0-4h

Applications

Taraxerol treatment significantly attenuated carrageenan induced paw edema 2 h onward. The anti-inflammatory effect of taraxerol was sustained up to 4 h.

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].

References:
[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]: BertE TE, Dalmagro AP, Zimath PL, GonCalves AE, Meyre-Silva C, BUrger 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.