Alantolactone is a sesquiterpene lactone extracted from Inula Helenium L with anti-inflammatory, antibacterial and anticancer activities. The half maximal inhibitory effect of alantolactone on cell proliferation concentration (IC50) was 35.45 μΜ at 24 h and 24.29 μΜ at 48 h. In addition, alantolactone at 10, 20 and 30 μΜ significantly downregulated the expression levels of MMP-2, MMP-7 and MMP-9 (matrix metalloproteinase ) protein[3]. Moreover, alantolactone induced apoptosis in HepG2 cells in a dose-dependent manner. The IC50 value of alantolactone was 33 μM after 12 h treatment[5].
Alantolactone/土木香内酯 细胞实验
Cell Line
Concentration
Treated Time
Description
References
K562/A02
2.73 μM
72 h
Inhibited K562/A02 cell proliferation
J Hematol Oncol. 2016 Sep 22;9(1):93.
HL60/ADR
3.28 μM
72 h
Inhibited HL60/ADR cell proliferation
J Hematol Oncol. 2016 Sep 22;9(1):93.
K562
2.75 μM
72 h
Inhibited K562 cell proliferation
J Hematol Oncol. 2016 Sep 22;9(1):93.
HL60
3.26 μM
72 h
Inhibited HL60 cell proliferation
J Hematol Oncol. 2016 Sep 22;9(1):93.
Normal hematopoietic cells
26.37 μM
72 h
Low toxicity to normal hematopoietic cells
J Hematol Oncol. 2016 Sep 22;9(1):93.
KG1a
2.75 μM
72 h
Inhibited KG1a cell proliferation
J Hematol Oncol. 2016 Sep 22;9(1):93.
HEB human brain glial cells
289.8 μM (IC50)
Relatively lower cytotoxicity
Genes Dis. 2020 Aug 8;9(2):466-478.
HS5 human bone marrow stromal cells
44.07 μM (IC50)
Relatively lower cytotoxicity
Genes Dis. 2020 Aug 8;9(2):466-478.
LO2 human hepatocytes
128.6 μM (IC50)
Relatively lower cytotoxicity
Genes Dis. 2020 Aug 8;9(2):466-478.
THP-1
2.17 μM
72 h
Inhibited THP-1 cell proliferation
J Hematol Oncol. 2016 Sep 22;9(1):93.
SaoS2 osteosarcoma cells
0 μM, 4 μM, 6 μM, 8 μM, 10 μM
24h, 48h, 72h
Inhibited cell proliferation, reduced PCNA protein level
Genes Dis. 2020 Aug 8;9(2):466-478.
U2OS osteosarcoma cells
5.531 μM (IC50)
24h, 48h, 72h
Inhibited cell proliferation, reduced PCNA protein level
Genes Dis. 2020 Aug 8;9(2):466-478.
MG63 osteosarcoma cells
6.963 μM (IC50)
24h, 48h, 72h
Inhibited cell proliferation, reduced PCNA protein level
Genes Dis. 2020 Aug 8;9(2):466-478.
143B osteosarcoma cells
4.251 μM (IC50)
24h, 48h, 72h
Inhibited cell proliferation, reduced PCNA protein level
Genes Dis. 2020 Aug 8;9(2):466-478.
SH-SY5Y cells
0, 1, 10, 25, 50 μM
48 h
Evaluate the effect of ATL on cell viability, IC50 value was 24.06 ± 2.38 μM.
J Exp Clin Cancer Res. 2017 Jul 12;36(1):93.
U118 cells
0, 1, 10, 25, 50 μM
48 h
Evaluate the effect of ATL on cell viability, IC50 value was 29.16 ± 2.84 μM.
J Exp Clin Cancer Res. 2017 Jul 12;36(1):93.
U251 cells
0, 10, 20 μM
24 h
Evaluate the effect of ATL on cell cycle and apoptosis, results showed ATL significantly increased the proportion of cells in G0/G1 phase and induced apoptosis.
J Exp Clin Cancer Res. 2017 Jul 12;36(1):93.
U87 cells
0, 10, 20 μM
24 h
Evaluate the effect of ATL on cell cycle and apoptosis, results showed ATL significantly increased the proportion of cells in G0/G1 phase and induced apoptosis.
J Exp Clin Cancer Res. 2017 Jul 12;36(1):93.
NRK-52E cells
10 μM
24 h
The combined treatment had little effect on normal NRK-52E cells.
Int J Biol Sci. 2019 Jun 4;15(8):1676-1684.
HL-7702 cells
10 μM
24 h
The combined treatment had little effect on normal HL-7702 cells.
Int J Biol Sci. 2019 Jun 4;15(8):1676-1684.
RKO cells
10 μM
24 h
Enhanced oxaliplatin-induced growth inhibition and apoptosis in RKO cells through significant accumulation of intracellular reactive oxygen species (ROS) and activation of JNK and p38 MAPK signaling pathways.
Int J Biol Sci. 2019 Jun 4;15(8):1676-1684.
HCT116 cells
10 μM
24 h
Enhanced oxaliplatin-induced growth inhibition and apoptosis in HCT116 cells through significant accumulation of intracellular reactive oxygen species (ROS) and activation of JNK and p38 MAPK signaling pathways.
Int J Biol Sci. 2019 Jun 4;15(8):1676-1684.
HUVEC cells
0.01-20 μM
48 h
Assess the toxicity of A@HAP NPs on normal cells, showing no significant toxicity to HUVEC cells at equivalent concentrations.
Asian J Pharm Sci. 2025 Feb;20(1):100993.
CT26 cells
0.01-20 μM
48 h
Evaluate the in vitro anti-tumor efficacy of A@HAP NPs, showing dose-dependent cytotoxicity against CT26 cells, with stronger effects than HA-PTX or PTX alone.
Asian J Pharm Sci. 2025 Feb;20(1):100993.
MCF-7 human breast cancer cells
10, 20, 30 µM
15 days
To evaluate the effect of Alantolactone on colony formation in MCF-7 cells. The results showed that Alantolactone significantly inhibited colony formation in a concentration-dependent manner.
Int J Mol Med. 2018 Oct;42(4):1847-1856.
MCF-7 human breast cancer cells
10, 20, 30 µM
24 h
To evaluate the effect of Alantolactone on the migration of MCF-7 cells. The results showed that Alantolactone significantly inhibited cell migration in a dose- and time-dependent manner.
Int J Mol Med. 2018 Oct;42(4):1847-1856.
MCF-7 human breast cancer cells
10, 20, 30 µM
24 h
To evaluate the effect of Alantolactone on apoptosis in MCF-7 cells. The results showed that Alantolactone significantly increased the percentage of apoptotic cells in a concentration-dependent manner.
Int J Mol Med. 2018 Oct;42(4):1847-1856.
MCF-7 human breast cancer cells
5, 10, 20, 30, 40, 80 µM
24 and 48 h
To evaluate the inhibitory effect of Alantolactone on the proliferation of MCF-7 cells. The results showed that Alantolactone significantly reduced cell viability, with IC50 values of 35.45 µM at 24 h and 24.29 µM at 48 h.
Int J Mol Med. 2018 Oct;42(4):1847-1856.
HK-2 cells
1, 2, 4 µM
24 h
To evaluate the effect of Alantolactone on TGF-β-stimulated expression of fibrotic factors in HK-2 cells. Results showed that Alantolactone inhibited TGF-β-stimulated expression of collagen type I and PAI-1 mRNA and protein.
Diabetes Metab J. 2024 Jan;48(1):72-82.
NRK-49F cells
1, 2, 4 µM
24 h
To evaluate the effect of Alantolactone on TGF-β-stimulated expression of fibrotic factors in NRK-49F cells. Results showed that Alantolactone dose-dependently inhibited TGF-β-stimulated expression of collagen type I, fibronectin, PAI-1, and α-SMA mRNAs.
Diabetes Metab J. 2024 Jan;48(1):72-82.
SCC9 cells
8 µM
Evaluate the effect of ALT on SCC9 cell ROS production, results showed ALT significantly increased ROS levels
J Transl Med. 2023 May 18;21(1):328.
CAL27 cells
12 µM
Evaluate the effect of ALT on CAL27 cell ROS production, results showed ALT significantly increased ROS levels
J Transl Med. 2023 May 18;21(1):328.
SCC9 cells
4 µM
24 h
Evaluate the effect of ALT on SCC9 cell viability, results showed ALT significantly reduced cell viability
J Transl Med. 2023 May 18;21(1):328.
CAL27 cells
10 µM
24 h
Evaluate the effect of ALT on CAL27 cell viability, results showed ALT significantly reduced cell viability
J Transl Med. 2023 May 18;21(1):328.
Alantolactone/土木香内酯 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nude mice
KG1a xenograft model
Oral
100 mg/kg
Every 3 days for 30 days
Suppressed tumor growth
J Hematol Oncol. 2016 Sep 22;9(1):93.
Female athymic mice
143B osteosarcoma xenograft model
Intra-gastric administration
5 mg/kg, 15 mg/kg, 25 mg/kg
Once every 2 days, for 21 days
Inhibited tumor growth and metastasis, reduced PCNA, Bcl-2, Vimentin, β-catenin and p-p38 protein levels
Genes Dis. 2020 Aug 8;9(2):466-478.
BALB/c mice
IMQ-induced psoriasis model
Topical application
20 μM and 30 μM
Once daily for one week
To evaluate the therapeutic effect of CHALT on psoriasis symptoms. Results showed that CHALT significantly ameliorated IMQ-induced psoriasis symptoms, including reduced skin thickening, erythema, and scaling, and inhibited the activation of STAT3 signaling pathway.
Asian J Pharm Sci. 2022 Mar;17(2):268-283
Nude mice (BALB/c nu/nu)
U87 xenograft model
Intraperitoneal injection
10, 20 mg/kg
Once daily for 15 days
Evaluate the inhibitory effect of ATL on tumor growth, results showed ATL significantly reduced tumor volume and weight.
J Exp Clin Cancer Res. 2017 Jul 12;36(1):93.
BALB/c nude mice
HCT116 xenograft model
Intraperitoneal injection
10 mg/kg
Once daily for 13 days
The combined treatment significantly inhibited the growth of HCT116 xenograft tumors by increasing the phosphorylation levels of JNK and p38 and decreasing Ki-67 expression.
Int J Biol Sci. 2019 Jun 4;15(8):1676-1684.
BALB/c mice
CT26 tumor model
Intravenous injection
2 mg/kg
Every 2 days for 14 days
Evaluate the in vivo anti-tumor efficacy of A@HAP NPs, showing significant tumor growth inhibition and enhanced immune cell infiltration and antigen presentation.
Asian J Pharm Sci. 2025 Feb;20(1):100993.
C57BL/6 mice
Unilateral ureteral obstruction (UUO) model
Oral gavage
5 mg/kg
Once daily for 15 days (including 5 days of pretreatment)
To evaluate the effect of Alantolactone on UUO-induced renal fibrosis. Results showed that Alantolactone significantly alleviated UUO-induced renal tubulointerstitial damage and fibrosis and decreased collagen type I, fibronectin, and α-SMA expression.
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