The primary target identified for Aloesin is the mitogen‑activated protein kinase (MAPK) signaling pathway. Treatment with Aloesin resulted in decreased phosphorylation levels of MEK, ERK, JNK, and p38 MAPK, without altering their total protein levels. No IC50, Ki, EC50, or DC50 values for target binding were reported in this study. [1]

Aloesin (0-40 μM, 24, 48, and 72 h) inhibits the growth of ovarian cancer cells in a time- and dose-dependent way[1].
Aloesin (0-10 μM; 48 h) dose-dependently arrests the cell cycle at S-phase in SKOV3 cells[1].
Aloesin (0-10 μM; 48 h) induces cell death in SKOV3 cells[1].
Aloesin (0-10 μM; 48 h) prevents the MAPK signaling pathway from becoming phosphorylated[1].

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Aloesin inhibited cell viability in a dose‑dependent (2.5‑40 µM) and time‑dependent (24‑72 h) manner across five ovarian cancer cell lines (OV‑1063, CoC1, CaoV‑3, OVCAR3, and SKOV3), with an IC50 of approximately 5 µM in SKOV3 cells after 48 h treatment.
It suppressed colony formation in SKOV3 cells in a dose‑dependent manner (2.5‑10 µM), reducing colony number and average clone size.
Aloesin arrested the cell cycle at the S‑phase in SKOV3 cells, with G2/M phase cells decreasing and S‑phase cells increasing with higher doses (2.5‑10 µM). Western blot confirmed downregulation of S‑G2/M‑related proteins cyclin A, CDK2, and cyclin D1.
It induced apoptosis in SKOV3 cells as shown by Hoechst 33342 staining (chromatin condensation and nuclear fragmentation) and Annexin V/PI flow cytometry, with a marked dose‑dependent increase in late apoptosis (2.5‑10 µM). Western blot revealed proteolytic cleavage of caspase‑3, caspase‑9, and PARP1, increased Bax expression, and decreased Bcl‑2 expression.
Aloesin inhibited cell migration and invasion in SKOV3 cells in wound healing and Transwell assays (2.5‑10 µM). Migration was reduced by ~80% and invasion by ~75% at 10 µM. Western blot showed dose‑dependent decreases in MMP‑2 and MMP‑9 expression.
Mechanistically, Aloesin decreased the phosphorylation levels of MEK, ERK, JNK, and p38 MAPK in a dose‑dependent manner (2.5‑10 µM), indicating inhibition of the MAPK signaling pathway. [1]

Aloesin (injection; 20 mg/kg or 40 mg/kg; once daily; 7 w) reduces the growth of tumors in an ovarian cancer xenograft model[1].
In a xenograft model using SKOV3 cells in athymic nude mice, Aloesin at 20 mg/kg and 40 mg/kg (daily for seven weeks) significantly inhibited tumor growth. Tumor volumes in treated groups were smaller than controls from week four onward, and at seven weeks, dissected tumors weighed less in treated groups compared to controls.
Immunohistochemistry of xenograft tumors showed fewer proliferative cells (lower PCNA) and more apoptotic cells (higher cleaved caspase‑3) in Aloesin‑treated groups.
In an experimental pulmonary metastasis model (intravenous SKOV3 injection via tail vein), Aloesin treatment (dose not specified for this model) significantly reduced the number of metastatic colonies in the lungs and lowered the incidence of tumor nodules compared to PBS‑treated controls. [1]

Tyrosinase activity was determined using a modified Pomerantz method. The reaction mixture contained 0.1 U/µL mushroom tyrosinase, 0.1 M potassium phosphate buffer (pH 6.8), 0.02 µCi/µL (6×10⁻⁵ M) L‑[3,5‑³H]‑tyrosine, and indicated concentrations of Aloesin, arbutin, or their combination. The mixture was incubated at 37°C for 20 minutes. Then, 30 µL of activated charcoal (50 mg/mL in 0.2 N HCl) was added, vortexed, and centrifuged at 15,000×g for 15 minutes. Fifty microliters of the supernatant were mixed with 300 µL of activated Dowex 50 resin, briefly centrifuged, and the radioactivity in the supernatant was counted with a liquid scintillation counter.
For kinetic analysis, Lineweaver‑Burk plots were generated using varying substrate concentrations in the absence or presence of Aloesin at 0.4 mM and 0.8 mM. The Ki value for non‑competitive inhibition was calculated from the plots.
The synergistic effect was evaluated according to the Bürgi method: the percentage of control activity was calculated as % activity = (A‑C)/(B‑C) × 100, where A and B are enzyme activities (in DPM) in the presence and absence of inhibitors, respectively, and C is the background (no enzyme). Synergy is defined when m × n > S, where m and n are the % of control activities with individual inhibitors, and S is the % of control activity with both inhibitors. [3]

SKOV3 cells were seeded at 5×10³ cells/well in 96‑well plates, incubated overnight, and treated with Aloesin at 0, 2.5, 5, 10, 20, and 40 µM for 48 h, or with 5 µM for 24, 48, and 72 h. Cell viability was evaluated using the MTT assay.
For colony formation, 500 SKOV3 cells were plated per well in 6‑well plates and allowed to grow for 10 days; colonies were stained with crystal violet, photographed, and manually counted.
For cell cycle analysis, SKOV3 cells treated with 0, 2.5, 5, and 10 µM Aloesin for 48 h were fixed in 80% cold ethanol, incubated with 0.5% Triton X‑100 containing 1 mg/mL RNase A at 37°C for 30 min, and analyzed by flow cytometry with PI staining.
For apoptosis assessment, Hoechst 33342 staining was performed by treating cells with different concentrations for 48 h, washing with PBS, staining with 5 µg/mL Hoechst 33342 at 37°C in the dark for 10 min, and observing under fluorescence microscopy. Annexin V/PI analysis was done using an apoptosis kit per manufacturer's instructions; cells were harvested, washed, resuspended at 1×10⁶ cells/mL in binding buffer with Annexin V‑FITC and PI, incubated at room temperature in the dark for 30 min, and analyzed by flow cytometry.
For wound healing, SKOV3 cells treated with 0, 2.5, 5, and 10 µM Aloesin for 24 h were scratched with a sterile pipette tip, and wound closure was observed and photographed after 24 h.
For Transwell migration and invasion assays, cells treated with Aloesin were trypsinized, washed, and resuspended in serum‑free medium at 2×10⁵ cells/mL, then seeded into upper chambers (100 µL). For migration, lower chambers contained 600 mL DMEM with 10% FBS; cells migrated for 12 h and membranes were stained with crystal violet. For invasion, chambers were pre‑coated with Matrigel (1:30 dilution in serum‑free medium) and the protocol was similar.
Western blot analysis: total protein was extracted and quantified using a BCA kit; 50 ng protein per sample was loaded onto 12% SDS‑PAGE, transferred to PVDF membranes, blocked with 5% skim milk in TBST for 60 min, incubated with primary antibodies overnight at 4°C, washed, incubated with secondary antibody for 1 h at room temperature, and developed with ECL solution. GAPDH was used as loading control. Antibodies detected included MMP‑9, MMP‑2, MEK, ERK, JNK, p38 MAPK, cyclin A, CDK2, cyclin D1, caspase‑3, caspase‑9, PARP1, Bax, and Bcl‑2. [1]

6-week-old athymic nude mice injected with SKOV3 cells
20 mg/kg or 40 mg/kg
Injection; 20 mg/kg or 40 mg/kg; once daily; 7 weeks

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For the xenograft model, 6‑week‑old athymic nude mice were randomly assigned to three groups: control (n=5), Aloesin 20 mg/kg (n=5), and Aloesin 40 mg/kg (n=5). SKOV3 cells (2×10⁶) were injected into the right flank. Mice in experimental groups received daily intraperitoneal injections of Aloesin (20 mg/kg or 40 mg/kg) for three weeks, then monitored for tumor growth. Tumor length (L) and width (W) were measured twice weekly, and tumor volume calculated as TV = L×W²/2. At seven weeks post‑inoculation, mice were sacrificed, tumors dissected, weighed, and photographed.
For the lung metastasis model, nude mice were injected with 1×10⁶ SKOV3 cells via the lateral tail vein. After one month, mice were euthanized, lungs removed, and subjected to HE staining to count metastatic nodules. All animal protocols were approved by the institutional ethics committee. [1]

(1) Cytotoxicity: MTT assay on HaCaT cells showed that Aloesin at concentrations up to 10 μM did not cause significant toxicity after 24 h treatment (viability not reduced). [1]
(2) No other toxicological data (e.g., LD₅₀, organ toxicity, plasma binding) are reported in this study. [1]

[1]. Aloesin Suppresses Cell Growth and Metastasis in Ovarian Cancer SKOV3 Cells through the Inhibition of the MAPK Signaling Pathway. Anal Cell Pathol (Amst). 2017;2017:8158254.

[2]. Aloesin from Aloe vera accelerates skin wound healing by modulating MAPK/Rho and Smad signaling pathways in vitro and in vivo. Phytomedicine. 2017 May 15;28:19-26.

[3]. Aloesin and arbutin inhibit tyrosinase activity in a synergistic manner via a different action mechanism. Arch Pharm Res. 1999 Jun;22(3):232-6.

Aloesin is a type of chromone compound. It has been reported that Aloesin exists in African aloe, Aloe vera, and other organisms with relevant data.

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Aloesin (CAS# 30861‑27‑9) is a bioactive compound from Aloe vera, historically used for anti‑inflammatory, UV protection, and antibacterial applications. This study is the first to demonstrate its anticancer activity in ovarian cancer, showing inhibition of cell growth, metastasis, and tumor progression via MAPK pathway inhibition.
The compound suppressed growth in five ovarian cancer cell lines, with SKOV3 being the most sensitive (IC50 ≈ 5 µM). It induced S‑phase cell cycle arrest and apoptosis through caspase‑dependent and mitochondrial pathways (Bax/Bcl‑2 modulation).
In vivo, Aloesin reduced tumor growth and lung metastasis in mouse models, supporting its therapeutic potential for ovarian cancer.
The study suggests that while previous reports on Aloe vera‑mediated apoptosis in leukemia involved only p38 and JNK, Aloesin in ovarian cancer also implicates ERK inhibition, indicating cancer‑type‑specific mechanisms.
No FDA warnings or clinical trial data are mentioned in this paper. [1]

C19H22O9

394.3726

394.126

C, 57.87; H, 5.62; O, 36.51

30861-27-9

30861-27-9

160190

White to off-white solid powder

1.5±0.1 g/cm3

628.0±55.0 °C at 760 mmHg

224.2±25.0 °C

0.0±1.9 mmHg at 25°C

1.637

0.64

5

9

4

28

647

5

O1[C@]([H])(C([H])([H])O[H])[C@]([H])([C@@]([H])([C@]([H])([C@]1([H])C1=C(C([H])=C(C([H])([H])[H])C2C(C([H])=C(C([H])([H])C(C([H])([H])[H])=O)OC1=2)=O)O[H])O[H])O[H])O[H]

HKIKAXXIWJHWLY-ZIIYPAMZSA-N

InChI=1S/C19H22O9/c1-7-3-10(22)14(19-17(26)16(25)15(24)12(6-20)28-19)18-13(7)11(23)5-9(27-18)4-8(2)21/h3,5,12,15-17,19-20,22,24-26H,4,6H2,1-2H3/t12-,15-,16+,17-,19+/m1/s1

7-hydroxy-5-methyl-2-(2-oxopropyl)-8-[(2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]chromen-4-one

Aloesin; Aloeresin B; Aloe resin B

2934.99.03.00

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: 78~270 mg/mL (197./~684.6 mM)

Solubility in Formulation 1: ≥ 2.25 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.25 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.25 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)