Aloesin is a potent and selective inhibitor of tyrosinase with IC50 value of 31.5μM [1]. Aloesin has direct inhibitory effects on melanogenesis and showed dose-dependent reductions in tyrosinase activity[2]. Aloesin has been widely used to inhibit excessive pigmentation caused by ultraviolet radiation[3].
In vitro, Aloesin treatment for 48 hours significantly inhibited the proliferation of SKOV3 cells, with an IC50 value of 5μM[4]. Without the presence of Wnt3a ligand, treatment with 20μM Aloesin for 12 hours can increase the protein level of active β-catenin in NIH/3T3 cells, and promote the expression of Wnt cascade genes[5]. Treatment with 20μM Aloesin for 24 hours significantly increased the levels of cyclin E, CDK2 and CDC25A in SK-HEP-1 cells[6].
In vivo, Aloesin treatment via oral administration at a dose of 40mg/kg/day for 7 consecutive days effectively reduced psoriasis area severity index (PASI) scores without any significant changes in the body weight of mice and ameliorated psoriatic lesions [7]. Administer Aloesin (200mg/kg) orally twice a week for 12 weeks significantly reduced obesity-related oxidative stress and hepatic steatosis in rats fed with a high-fat diet (HFD)[8].
References:
[1] Mikayoulou M, Mayr F, Temml V, et al. Anti-tyrosinase activity of South African Aloe species and isolated compounds plicataloside and aloesin[J]. Fitoterapia, 2021, 150: 104828.
[2] Wang Z, Li X, Yang Z, et al. Effects of aloesin on melanogenesis in pigmented skin equivalents[J]. International journal of cosmetic science, 2008, 30(2): 121-130.
[3] Choi S, Park Y I, Lee S K, et al. Aloesin inhibits hyperpigmentation induced by UV radiation[J]. Clinical and experimental dermatology, 2002, 27(6): 513-515.
[4] Zhang L, Lv R, Qu X, et al. Aloesin suppresses cell growth and metastasis in ovarian cancer SKOV3 cells through the inhibition of the MAPK signaling pathway[J]. Analytical Cellular Pathology, 2017, 2017(1): 8158254.
[5] Peng C, Zhang W J, Dai C, et al. Study of the aqueous extract of Aloe vera and its two active components on the Wnt/β-catenin and Notch signaling pathways in colorectal cancer cells[J]. Journal of ethnopharmacology, 2019, 243: 112092.
[6] Lee K Y, Park J H, Chung M H, et al. Aloesin up‐regulates cyclin E/CDK2 kinase activity via inducing the protein levels of cyclin E, CDK2, and CDC25A in SK‐HEP‐1 cells[J]. IUBMB Life, 1997, 41(2): 285-292.
[7] Alsahli T G, Alharbi K S, Alenezi S K, et al. Aloesin alleviates imiquimod-induced psoriasis in dermal layers through inhibition of interleukins and NF-κB signaling pathways[J]. Scientific Reports, 2025.
[8] Alamri S M, Al-Harbi L N, Alshammari G M, et al. Aloesin activates Nrf2 signaling to attenuate obesity-associated oxidative stress and hepatic steatosis in high-fat diet-fed rats[J]. Scientific Reports, 2025, 15(1): 34888.
Aloesin是一种强效、选择性的酪氨酸酶抑制剂，IC50值为31.5μM[1]。Aloesin对黑色素生成具有直接抑制作用，并显示出酪氨酸酶活性的剂量依赖性降低[2]。Aloesin已广泛应用于抑制由紫外线辐射引起的过度色素沉着[3]。
在体外，Aloesin处理48小时显著抑制了SKOV3细胞的增殖，IC50值为5μM[4]。在无Wnt3a配体存在的情况下，用20μM的Aloesin处理12小时可增加NIH/3T3细胞中活性β-catenin的蛋白水平，并促进Wnt级联基因的表达[5]。用20μM的Aloesin处理24小时显著提高了SK-HEP-1细胞中细胞周期蛋白E、CDK2和CDC25A的水平[6]。
在体内，以40mg/kg/天的剂量连续口服Aloesin 7天，有效降低了银屑病面积和严重程度指数（PASI）评分，且未引起小鼠体重的显著变化，并改善了银屑病皮损[7]。每周口服两次Aloesin（200mg/kg），持续12周，显著降低了高脂饮食(HFD)喂养大鼠的肥胖相关氧化应激和肝脏脂肪变性[8]。