Asiatic acid is a pentacyclic triterpenoid that inhibits EGFR activity, with IC50 values of 0.035nM and 0.348nM for wild-type EGFR and T790M/L858R EGFR, respectively [1]. Asiatic acid induces endoplasmic reticulum stress (by increasing GRP78 and calpain, and decreasing calnexin and IRE1α expression), enhances free intracellular calcium, and damages cellular organization[2]. Asiatic acid has been widely used to attenuate inflammation, tumor cell proliferation, and induce mitochondrial pathway of apoptosis [3].
In vitro, Asiatic acid treatment for 24 hours significantly inhibited the viability of SH-SY5Y cells, with an IC50 value of 34.99±0.12µM[4]. Treatment with 80µM Asiatic acid for 12 hours led to mitochondrial dysfunction in A549 cells, accompanied by an increase in ROS levels[5]. Treatment with Asiatic acid (40µg/ml) for 48 hours can cause the cell cycle of SKOV3 cells to be arrested at the G0/G1 phase, and significantly reduce the protein levels of CDK2, CDK4, CDK6, cyclin D1 and cyclin E[6].
In vivo, Asiatic acid treatment via oral administration at a dose of 20mg/kg daily for 45 days significantly improved the blood glucose and insulin levels of diabetic rats and inhibited oxidative stress[7]. Asiatic acid treatment (20mg/kg/day; p.o.) for 2 weeks improved metabolic, hemodynamic abnormalities in metabolic syndrome (MS) rats[8].
References:
[1] Monmai C, Sabuakham S, Pabuprapap W, et al. Asiatic Acid from Centella asiatica as a Potent EGFR Tyrosine Kinase Inhibitor with Anticancer Activity in NSCLC Cells Harboring Wild-Type and T790M-Mutated EGFR[J]. Biomolecules, 2025, 15(10): 1410.
[2] Lv J, Sharma A, Zhang T, et al. Pharmacological review on asiatic acid and its derivatives: a potential compound[J]. SLAS TECHNOLOGY: Translating Life Sciences Innovation, 2018, 23(2): 111-127.
[3] Nagoor Meeran M F, Goyal S N, Suchal K, et al. Pharmacological properties, molecular mechanisms, and pharmaceutical development of asiatic acid: a pentacyclic triterpenoid of therapeutic promise[J]. Frontiers in pharmacology, 2018, 9: 892.
[4] Tangrodchanapong T, Jiso A, Changkaew P, et al. Radioprotective effects of asiaticoside and asiatic acid in neural stem cells derived from human stem cells from apical papilla through increasing dose-reduction factor and their lowering effects on SH-SY5Y cell viability[J]. PLoS One, 2025, 20(6): e0325480.
[5] Wu T, Geng J, Guo W, et al. Asiatic acid inhibits lung cancer cell growth in vitro and in vivo by destroying mitochondria[J]. Acta Pharmaceutica Sinica B, 2017, 7(1): 65-72.
[6] Ren L, Cao Q X, Zhai F R, et al. Asiatic acid exerts anticancer potential in human ovarian cancer cells via suppression of PI3K/Akt/mTOR signalling[J]. Pharmaceutical biology, 2016, 54(11): 2377-2382.
[7] Ramachandran V, Saravanan R. Asiatic acid prevents lipid peroxidation and improves antioxidant status in rats with streptozotocin-induced diabetes[J]. Journal of Functional Foods, 2013, 5(3): 1077-1087.
[8] Pakdeechote P, Bunbupha S, Kukongviriyapan U, et al. Asiatic acid alleviates hemodynamic and metabolic alterations via restoring eNOS/iNOS expression, oxidative stress, and inflammation in diet-induced metabolic syndrome rats[J]. Nutrients, 2014, 6(1): 355-370.
Asiatic acid是一种五环三萜类化合物，可抑制EGFR活性，对野生型EGFR和T790M/L858R EGFR的IC50值分别为0.035nM和0.348nM[1]。Asiatic acid可诱导内质网应激（通过增加GRP78和钙蛋白酶表达，降低钙联接蛋白和IRE1α表达）、增强细胞内游离钙离子浓度并破坏细胞结构[2]。Asiatic acid已广泛应用于减轻炎症、抑制肿瘤细胞增殖，并诱导线粒体途径的细胞凋亡[3]。
在体外，Asiatic acid处理24小时显著抑制了SH-SY5Y细胞的活力，IC50值为34.99±0.12µM[4]。用80µM的Asiatic acid处理12小时导致A549细胞线粒体功能障碍，并伴随ROS水平升高[5]。用Asiatic acid（40µg/ml）处理48小时可使SKOV3细胞的细胞周期停滞在G0/G1期，并显著降低CDK2、CDK4、CDK6、细胞周期蛋白D1和细胞周期蛋白E的蛋白水平[6]。
在体内，每日口服20mg/kg剂量的Asiatic acid连续45天显著改善了糖尿病大鼠的血糖和胰岛素水平并抑制了氧化应激[7]。Asiatic acid治疗（20mg/kg/day；口服）2周改善了代谢综合征（MS）大鼠的代谢及血流动力学异常[8]。