Triciribine is an adenosine analog that targets protein kinase B (Akt) with an IC50 value of 130nM and has antitumor activity[1, 2]. Triciribine is a DNA synthesis inhibitor of HIV-1 with an IC50 value of 20nM[3].
In vitro, treatment of prostate cancer PC-3 cells with Triciribine (10μM) for 24h enhanced apoptosis induced by TNF-related apoptosis-inducing ligand (TRAIL) and anti-CD95[4]. Treatment of bovine cumulus-oocyte complex (COC) with Triciribine (1μM) for 22h resulted in an increase in the rate of blastocyst formation and increased the in vitro yield of bovine embryos[5].
In vivo, treatment of C57BL/6 J mice with Triciribine (1, 2mg/kg/day) by intraperitoneal injection for 2 weeks significantly increased the level of low-density lipoprotein receptor (LDLR) in the liver of mice[6]. Triciribine (1mg/kg/day) was intraperitoneally injected into mice inoculated with GFP+ Huh7 cells for 14 days, which significantly inhibited the growth of tumors in mice and exerted a synergistic effect when combined with rosiglitazone[7].
References:
[1] Barrichon M, Hadi T, Wendremaire M, et al. EXPRESSION OF CONCERN: Dose‐dependent biphasic leptin‐induced proliferation is caused by non‐specific IL‐6/NF‐κB pathway activation in human myometrial cells[J]. British Journal of Pharmacology, 2015, 172(12): 2974-2990.
[2] Garrett C R, Coppola D, Wenham R M, et al. Phase I pharmacokinetic and pharmacodynamic study of triciribine phosphate monohydrate, a small-molecule inhibitor of AKT phosphorylation, in adult subjects with solid tumors containing activated AKT[J]. Investigational new drugs, 2011, 29: 1381-1389.
[3] KUCERA L S, IYER N P, PUCKETT S H, et al. Activity of triciribine and triciribine-5′-monophosphate against human immunodeficiency virus types 1 and 2[J]. AIDS research and human retroviruses, 1993, 9(4): 307-314.
[4] Dieterle A, Orth R, Daubrawa M, et al. The Akt inhibitor triciribine sensitizes prostate carcinoma cells to TRAIL‐induced apoptosis[J]. International journal of cancer, 2009, 125(4): 932-941.
[5] Curcio A G, Ribeiro T I S, Gomes H F, et al. Increased in vitro production of bovine embryos resulting from oocyte maturation in the presence of triciribine, a specific inhibitor of AKT[J]. Theriogenology, 2025, 231: 222-227.
[6] Bjune K, Wierød L, Naderi S. Triciribine increases LDLR expression and LDL uptake through stabilization of LDLR mRNA[J]. Scientific Reports, 2018, 8(1): 16174.
[7] Liu L, Yang Z, Xu Y, et al. Inhibition of oxidative stress-elicited AKT activation facilitates PPARγ agonist-mediated inhibition of stem cell character and tumor growth of liver cancer cells[J]. PloS one, 2013, 8(8): e73038.
Triciribine是一种腺苷类似物，靶向抑制蛋白激酶B（Akt），IC50值为130nM，具有抗肿瘤活性[1, 2]。Triciribine是HIV-1的DNA合成抑制剂，IC50值为20nM[3]。
在体外，Triciribine（10μM）处理前列腺癌PC-3细胞24h，增强了TNF相关凋亡诱导配体（TRAIL）和抗CD95诱导的细胞凋亡[4]。Triciribine（1μM）处理牛卵丘-卵母细胞复合物（COC）22h，导致囊胚生成速率增加，增加了牛胚胎的体外产量[5]。
在体内，Triciribine（1, 2mg/kg/day）通过腹腔注射处理C57BL/6 J小鼠2周，显著增加了小鼠体内肝脏内低密度脂蛋白受体（LDLR）的水平[6]。Triciribine（1mg/kg/day）通过腹腔注射治疗接种GFP+ Huh7细胞的小鼠14天，显著抑制了小鼠体内肿瘤的生长，与罗格列酮联合治疗发挥协同效应[7]。