Ajugol 

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^[1][2][3][4].

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.

Ajugol (25,50 mg/kg, i.p., once a day, 8 weeks) activates TFEB in vivo and improves the progression of osteoarthritis after DDM (Destabilization of the Medial Meniscus) surgery in an osteoarthritis mouse model^[2].
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.

348.35

C₁₅H₂₄O₉

52949-83-4

Solid

White to off-white

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

Room temperature in continental US; may vary elsewhere.

* 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.

• [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]