Oleuropein is the major phenolic compound in the olive tree, with potent antioxidant and anti-inflammatory properties [1]. Oleuropein can cross the brain blood barrier and reduce neurotoxicity by promoting autophagy in neurons via regulation of the Ca2+-CaMKKβ-AMPK axis [2]. Oleuropein has been widely used in cell and animal models to inhibit tumor progression and inflammation[3].
In vitro, Oleuropein treatment for 72 hours significantly inhibited the proliferation of FM3 cells, HCT-116 cells and HeLa cells, with IC50 values of 274.53μM, 185.12μM and 265.28μM, respectively[4]. Treatment with 200μM Oleuropein for 72 hours significantly inhibited the viability of MCF 7 cells, reduced the expression of Bcl-2 and Bax genes, promoted the expression of p53 and induced cell apoptosis[5]. Treatment with 400μM Oleuropein for 11 days inhibited the differentiation of 3T3-L1 adipocytes, reduced the total lipid content, and suppressed the expression of PPARγ, FAS, C/EBPα and SREBP-1c genes[6].
In vivo, Oleuropein treatment via daily intraperitoneal injection at a dose of 200mg/kg for three consecutive days significantly alleviated liver necrosis and inflammatory responses induced by carbon tetrachloride, and improved the histological and plasma markers of liver damage in mice[7]. Continuous intradermal injection of 50mg/kg dose of Oleuropein for 7 consecutive days can accelerate the skin wound healing in aged male Balb/c mice[8].
References:
[1] Nediani C, Ruzzolini J, Romani A, et al. Oleuropein, a bioactive compound from Olea europaea L., as a potential preventive and therapeutic agent in non-communicable diseases[J]. Antioxidants, 2019, 8(12): 578.
[2] Gu Y, Han J. Autophagy and polyphenol intervention strategy in aging[J]. Trends in Food Science & Technology, 2023, 132: 1-10.
[3] Gorzynik-Debicka M, Przychodzen P, Cappello F, et al. Potential health benefits of olive oil and plant polyphenols[J]. International journal of molecular sciences, 2018, 19(3): 686.
[4] Samara P, Christoforidou N, Lemus C, et al. New semi-synthetic analogs of oleuropein show improved anticancer activity in vitro and in vivo[J]. European Journal of Medicinal Chemistry, 2017, 137: 11-29.
[5] Hassan Z K, Elamin M H, Omer S A, et al. Oleuropein induces apoptosis via the p53 pathway in breast cancer cells[J]. Asian Pacific Journal of Cancer Prevention, 2013, 14(11): 6739-6742.
[6] Svobodova M, Andreadou I, Skaltsounis A L, et al. Oleuropein as an inhibitor of peroxisome proliferator-activated receptor gamma[J]. Genes & nutrition, 2014, 9(1): 376.
[7] Domitrović R, Jakovac H, Marchesi V V, et al. Preventive and therapeutic effects of oleuropein against carbon tetrachloride-induced liver damage in mice[J]. Pharmacological research, 2012, 65(4): 451-464.
[8] Mehraein F, Sarbishegi M, Aslani A. Evaluation of effect of oleuropein on skin wound healing in aged male BALB/c mice[J]. Cell Journal (Yakhteh), 2014, 16(1): 25.
Oleuropein是橄榄树中的主要酚类化合物，具有强效的抗氧化和抗炎特性[1]。Oleuropein能够穿过血脑屏障，并通过调节Ca2+-CaMKKβ-AMPK轴促进神经元自噬，从而降低神经毒性[2]。Oleuropein已被广泛用于细胞和动物模型中以抑制肿瘤进展和炎症[3]。
在体外，Oleuropein处理72小时显著抑制了FM3细胞、HCT-116细胞和HeLa细胞的增殖，IC50值分别为274.53µM、185.12µM和265.28µM[4]。使用200µM的Oleuropein处理72小时，显著抑制了MCF 7细胞的活力，降低了Bcl-2和Bax基因的表达，促进了p53的表达，并诱导了细胞凋亡[5]。使用400µM的Oleuropein处理11天，抑制了3T3-L1脂肪细胞的分化，减少了总脂质含量，并降低了PPARγ、FAS、C/EBPα和SREBP-1c基因的表达[6]。
在体内，每日腹腔注射200mg/kg剂量的Oleuropein，连续三天，显著减轻了四氯化碳诱导的小鼠肝坏死和炎症反应，并改善了肝损伤的组织学及血浆标志物[7]。连续7天每日皮内注射50mg/kg剂量的Oleuropein，可加速老年雄性Balb/c小鼠的皮肤伤口愈合[8]。