Atractylenolide I, a natural compound extracted from largehead atractylodes rhizome, induces apoptosis and brings about cytotoxicity of human promyeloleukemic HL-60 cells. It is also a TLR4-antagonizing agent.
Atractylenolide I/白术内酯 I 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HCT116 cells
30 μM
48 hours
To evaluate the effect of ATT-I on immunoproteasome activity, results showed that ATT-I significantly enhanced the activity of immunoproteasome.
J Clin Invest. 2021 May 17;131(10):e146832.
RAW 264.7 cells
20 μmol/L
24 hours
To evaluate the inhibitory effect of Atractylenolide I on macrophage activation. Results showed that Atractylenolide I significantly inhibited macrophage migration.
Engineering (Beijing). 2023 Jan;20:63-76.
3T3-L1 mature adipocytes
0.625–5 μM
48 hours
The conditioned medium from AI-treated C26 cells significantly attenuated the induction of 3T3-L1 adipocyte lipolysis.
AI directly inhibited EVs biogenesis and IL-6 secretion of cultured C26 cells, significantly attenuating the potency of C26 medium in inducing C2C12 myotube atrophy and 3T3-L1 adipocyte lipolysis.
Inhibited proliferation and migration of LoVo cells
Clin Transl Med. 2020 Aug;10(4):e139.
SKOV3 cells
10, 50, 100 μmol/L
6 hours
AO-1 significantly down-regulated the expression of TLR4/MD-2 complex in SKOV3 cells, inhibited the activation of MyD88/NF-κB signaling pathway, reduced the secretion of immunosuppressive cytokines (IL-6, TGF-β1, VEGF, IL-17A), and decreased the expression and activity of IDO1.
J Transl Med. 2016 Apr 27;14(1):104.
ACHN
285.7 μM
48 hours
Evaluate the effect of ATL-I on ACHN cell proliferation, results showed ATL-I had a mild inhibitory effect on ACHN cells
Autophagy. 2025 Mar;21(3):619-638.
OSRC2
125.0 μM
48 hours
Evaluate the effect of ATL-I on OSRC2 cell proliferation, results showed ATL-I significantly inhibited OSRC2 cell proliferation
Autophagy. 2025 Mar;21(3):619-638.
786O
75.77 μM
48 hours
Evaluate the effect of ATL-I on 786O cell proliferation, results showed ATL-I significantly inhibited 786O cell proliferation
Autophagy. 2025 Mar;21(3):619-638.
HK-2
657.4 μM
48 hours
Evaluate the effect of ATL-I on HK-2 cell proliferation, results showed ATL-I had a mild inhibitory effect on HK-2 cells
Autophagy. 2025 Mar;21(3):619-638.
NCI-H295R cells
0.1-100 μmol/L
24 hours
To evaluate the inhibitory effects of AT-I and its derivatives on ALD production. Results showed that AT-I significantly inhibited Cor and ALD generation, while it had no significant influence on the intermediate products Prog and Cort.
Acta Pharm Sin B. 2022 Jan;12(1):135-148.
Atractylenolide I/白术内酯 I 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Female athymic nude mice
Subcutaneous xenograft tumor model
Intraperitoneal injection
25 mg/kg or 50 mg/kg
Once daily for four weeks
Evaluate the antitumor activity of ATL-I in vivo, results showed 50 mg/kg dosage significantly suppressed tumor growth
Autophagy. 2025 Mar;21(3):619-638.
C57BL/6J mice
Ang II-induced hyperaldosteronism model
Intraperitoneal injection
10, 20, 40 mg/kg/day
Once daily for 7 days
To evaluate the therapeutic effect of AT-I on Ang II-induced hyperaldosteronism. Results showed that AT-I significantly reduced serum ALD levels, improved electrolyte balance and cardiovascular function.
Acta Pharm Sin B. 2022 Jan;12(1):135-148.
C57BL/6 mice
MC38- and CT26-derived tumor models
Intraperitoneal injection
50 mg/kg
Daily until the end of the experiment
To evaluate the effect of ATT-I in combination with PD-1 inhibitor, results showed that the combination therapy significantly inhibited tumor growth and prolonged the survival time of mice.
J Clin Invest. 2021 May 17;131(10):e146832.
Balb/c mice
Orthotopic MSS CRC transplantation model
Tail vein injection
1.25 mg/kg
Once daily for 14 days
Upregulated MHC-I expression in tumor cells and enhanced CTLs' ability to recognize and kill tumor cells
Adv Sci (Weinh). 2024 Oct;11(38):e2405886.
Zebrafish
Zebrafish tail amputation inflammation model
Added to culture medium
20 μmol/L
24 hours pretreatment, 4 hours observation
To evaluate the inhibitory effect of Atractylenolide I on macrophage migration. Results showed that Atractylenolide I significantly inhibited macrophage migration to the wounding site.
Engineering (Beijing). 2023 Jan;20:63-76.
BALB/c mice
C26 tumour-bearing mice model
Intraperitoneal injection
25 mg/kg
Once daily for 18 days
AI ameliorated cancer cachexia symptoms, improved grip strength, and decreased serum EVs and IL-6 levels.
Mouse model of spleen deficiency and cancer cachexia
Intraperitoneal injection
20 mg/kg per day
Once daily for 30 days
Atractylenolide I treatment significantly ameliorated the reduction in body weight and atrophy of muscle, fat, spleen, and thymus in mice with spleen deficiency and cachexia.
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