Aloesin
(Synonyms: 芦荟苦素; Aloeresin) 目录号 : GC38398
Aloesin是一种强效、选择性的酪氨酸酶抑制剂，IC50值为31.5μM。
Cas No.:30861-27-9
Sample solution is provided at 25 µL, 10mM.
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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]。
| Cell experiment [1]: | |
Cell lines | SKOV3 cells |
Preparation Method | SKOV3 cells were cultured in a medium supplemented with 10% fetal bovine serum (FBS) and 100U/ml penicillin/streptomycin. The cells were incubated in a humidified environment at 37°C with 5% CO2. SKOV3 cells were seeded at a density of 5×103 cells per well in a 96-well plate and cultured overnight. Then, the cells were treated with different concentrations (0, 2.5, 5, 10, 20, and 40μM) of Aloesin for 48 hours, and the cell viability after aloin treatment was analyzed. |
Reaction Conditions | 0, 2.5, 5, 10, 20, and 40μM; 48h |
Applications | Aloesin treatment inhibited the growth of SKOV3 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Wistar albino rats |
Preparation Method | Wistar albino rats (120±15g) were placed in standard laboratory cages lined with suitable wood chips and maintained in a controlled environment with a temperature of (20-22°C) and humidity of (40-60%). A 12-hour light/12-hour dark daily cycle was maintained throughout the entire study period. The rats had free access to food and water. After one week of adapting to the environment, 24 adult rats were randomly divided into 3 groups (n=8 in each group): (1) Control group (standard diet+solvent); (2) Control group+Aloesin (200mg/kg); (3) HFD+Aloesin (200mg/kg), with the Aloesin administered orally twice a week for 12 weeks. Liver tissues of the rats were collected for analysis. |
Dosage form | 200mg/kg; twice a week for 12 weeks; p.o. |
Applications | Aloesin reduced liver damage and mitigated the increase in liver enzymes in HFD-fed rats. |
References: | |
| Cas No. | 30861-27-9 | SDF | |
| 别名 | 芦荟苦素; Aloeresin | ||
| Canonical SMILES | OC1=CC(C)=C(C(C=C(CC(C)=O)O2)=O)C2=C1[C@@H]3O[C@@H]([C@@H](O)[C@H](O)[C@H]3O)CO | ||
| 分子式 | C19H22O9 | 分子量 | 394.37 |
| 溶解度 | DMSO: 270 mg/mL (684.64 mM) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5357 mL | 12.6784 mL | 25.3569 mL |
| 5 mM | 507.1 μL | 2.5357 mL | 5.0714 mL |
| 10 mM | 253.6 μL | 1.2678 mL | 2.5357 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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