Ajugol
Based on 3 publication(s) in Google Scholar
Ajugol is an orally active iridoid glycoside found in the traditional Chinese medicine Leonurus japonicus. Ajugol is an autophagy activator. Ajugol activates TFEB-mediated autophagy and lysosomal biogenesis. Ajugol also has anti-inflammatory effects. Ajugol has great potential in the research of asthma, non-alcoholic fatty liver disease (NAFLD), and osteoarthritis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.61%
- CAS 番号: 52949-83-4
- 分子式: C15H24O9
- 分子量:348.35
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 Ajugol
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生物活性
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Trypanosoma |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
>10 μM
Compound: 11
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Cytotoxicity against human A2780 cells by MTT assay
Cytotoxicity against human A2780 cells by MTT assay
|
[PMID: 26859776] |
| A549 | IC50 |
>10 μM
Compound: 11
|
Cytotoxicity against human A549 cells by MTT assay
Cytotoxicity against human A549 cells by MTT assay
|
[PMID: 26859776] |
| Bel-7402 | IC50 |
>10 μM
Compound: 11
|
Cytotoxicity against human Bel7402 cells by MTT assay
Cytotoxicity against human Bel7402 cells by MTT assay
|
[PMID: 26859776] |
| BGC-823 | IC50 |
>10 μM
Compound: 11
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Cytotoxicity against human BGC823 cells by MTT assay
Cytotoxicity against human BGC823 cells by MTT assay
|
[PMID: 26859776] |
| HT-29 | IC50 |
>10 μM
Compound: 11
|
Cytotoxicity against human HT-29 cells by MTT assay
Cytotoxicity against human HT-29 cells by MTT assay
|
[PMID: 26859776] |
Ajugol has antiprotozoal activity against Trypanosoma b. rhodesiense (IC50: 31.8 μg/ml) and Trypanosoma b. rhodesiense (IC50: 7.2 μg/ml)[1].
Ajugol (0-100 μM, 0-72 h) in tert-butyl hydroperoxide (TBHP)-induced mouse primary chondrocytes restores TBHP-induced proliferation restriction and reduces chondrocyte apoptosis, ECM degradation and ROS accumulation without cytotoxicity (≤50 μM)[2].
Ajugol (50 μM) in Palmitate (HY-N0830)-induced mouse hepatocytes significantly reduces cellular triglyceride (TG) and total cholesterol (TC) content and plays a protective role in Palmitate-induced lipid accumulation without cytotoxicity[3].
Ajugol (25,50 μM) activates TFEB-mediated autophagy and promotes TFEB nuclear translocation by regulating mTOR dephosphorylation, enhancing lysosomal biogenesis, alleviating endoplasmic reticulum (ER) stress and lipid degradation in TBHP-induced mouse primary chondrocytes and Alpha Mouse Liver-12 (AML12) cells[2][3].
Ajugol attenuates its protective effects against lipid accumulation and ER stress and ECM after autophagy is blocked by Chloroquine (HY-17589A), indicating that it is dependent on the autophagy pathway to exert its effects[2][3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary mouse hepatocytes, AML12 cells
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Concentration:50 μM
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Incubation Time:24 h
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Result:Increased LC3-II (an autophagosome marker) and decreased p62 (an autophagy substrate), indicating enhanced autophagic activity.
Increased nuclear TFEB and upregulated expression of lysosome-related proteins (LAMP2, ATP6V1A).
Reduced p-mTOR, p-S6K, and p-4EBP1 levels, indicated that it inhibited mTORC1 activity.
| Species | Dose | Route | AUC | MRT | T1/2 | Clearance (CL) |
|---|---|---|---|---|---|---|
| Rat[4] | 2 mg/kg | i.v. | 5743.547 mg·h/L | 0.804 h | 0.746 h | 0.354 L/h/kg |
Ajugol (50 mg/kg, p.o., 12 weeks) improves HFD-induced hepatic steatosis and lipid metabolism disorders by promoting autophagic flux in a high-fat diet (HFD)-fed mouse model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (male aged 10 weeks) the osteoarthritis (OA) model was established using the DMM technique[2]
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Dosage:25, 50 mg/kg
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Administration:i.p., once a day, 8 weeks
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Result:Had a protective effect on the cartilage of knee joint tissue, reduced the expression of TFEB and type II collagen, while increasing the expression of CHOP and ATF4.
Showed good efficacy in delaying OA progression in the DMM mice model.
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Animal Model:C57BL/6 mice (male, aged 6 weeks, 20-23 g) fed HFD[3]
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Dosage:50 mg/kg
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Administration:p.o. 12 weeks
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Result:Lowered blood glucose and improved insulin resistance in HFD-fed obese mice and also prevented HFD-induced liver injury, with significant decreases in serum AST and ALT levels.
Reduced serum TG, LDL-C, TC, FFA and liver FFA levels as well as LDL-C/HDL-C.
Increased LC3-II levels and decreased p62 levels, demonstrated protection against hepatic steatosis by improving autophagic flux.
化学情報
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CAS 番号 52949-83-4
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性状 Solid
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分子量 348.35
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分子式 C15H24O9
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Color White to off-white
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SMILES
O[C@H]1[C@](O[C@H](CO)[C@@H](O)[C@@H]1O)([H])O[C@H](OC=C2)[C@@]3([H])[C@]2([H])[C@H](O)C[C@@]3(O)C
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Structure Classification
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Chin Med
Ajugol's upregulation of TFEB-mediated autophagy alleviates endoplasmic reticulum stress in chondrocytes and retards osteoarthritis progression in a mouse model. [Abstract]2023 Sep 7;18(1):113. PMID: 37679844 -
J Ethnopharmacol
Radix Rehmanniae Praeparata promoted zebrafish fin regeneration through aryl hydrocarbon receptor-dependent autophagy. [Abstract]2024 Sep 15:331:118272. PMID: 38710459 -
Neuropharmacology
Ajugol ameliorates mitochondrial dysfunction and cognitive decline in Alzheimer's Disease via BNIP3-dependent mitophagy. [Abstract]2026 Jun 15:291:110923. PMID: 41819485
溶剤 & 溶解度
DMSO : ≥ 3.7 mg/mL (10.62 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Deniz Tasdemir, et al. Anti-protozoal and plasmodial FabI enzyme inhibiting metabolites of Scrophularia lepidota roots. Phytochemistry. 2005 Feb;66(3):355-62. [Content Brief]
[2]. Wu J, et al. Ajugol's upregulation of TFEB-mediated autophagy alleviates endoplasmic reticulum stress in chondrocytes and retards osteoarthritis progression in a mouse model. Chin Med. 2023 Sep 7;18(1):113. [Content Brief]
[3]. Zhang H, et al. Ajugol enhances TFEB-mediated lysosome biogenesis and lipophagy to alleviate non-alcoholic fatty liver disease. Pharmacol Res. 2021 Dec;174:105964. [Content Brief]
[4]. Yi L, et al.A novel iridoid glycoside leonuride (ajugol) attenuates airway inflammation and remodeling through inhibiting type-2 high cytokine/chemokine activity in OVA-induced asthmatic mice. Phytomedicine. 2022 Oct;105:154345. [Content Brief]
[5]. Xue B, et al. Pharmacokinetics and tissue distribution of Aucubin, Ajugol and Catalpol in rats using a validated simultaneous LC-ESI-MS/MS assay. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Oct 1;1002:245-53. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8707 mL | 14.3534 mL | 28.7068 mL | 71.7669 mL |
| 5 mM | 0.5741 mL | 2.8707 mL | 5.7414 mL | 14.3534 mL | |
| 10 mM | 0.2871 mL | 1.4353 mL | 2.8707 mL | 7.1767 mL |