Clerodin 

Clerodin (3-deoxycaryoptinol) is a natural diterpenoid compound that can be isolated from traditional Chinese medicinal plants such as Clerodendrum infortunatum. Clerodin exhibits caspase-3 regulation, apoptosis induction, cell cycle arrest, ROS induction and glutathione depletion effects, along with anti-cancer and antifeedant activities. It shows selective cytotoxicity against leukemia cells and breast cancer cells, but has no obvious toxicity to normal human blood cells and lymphocytes. Clerodin significantly upregulates the expression of caspase-3 and promotes its activation, induces cell cycle arrest at the G2/M phase, increases intracellular ROS levels and reduces the content of reduced glutathione. Clerodin also reduces the feeding behavior of Helicoverpa armigera larvae on cabbage leaf discs, but has no significant contact toxicity to these larvae. Clerodin can be used in research related to acute monocytic leukemia and human breast cancer^[1][2][3].

Clerodin (30-150 μM) potently reduces viability of human monocytic leukemia (THP-1) cells with an IC₅₀ of 60 μM^[1].
Clerodin (60 μM) induces apoptosis-related morphological changes including nuclear condensation and apoptotic body formation in human monocytic leukemia (THP-1) cells^[1].
Clerodin (60 μM) induces significant apoptosis in human monocytic leukemia (THP-1) cells, with 86.6% of cells in early or late apoptotic stages^[1].
Clerodin (60 μM) increases intracellular ROS levels by ≥80% in human monocytic leukemia (THP-1) cells^[1].
Clerodin (60 μM; 18 h) significantly upregulates caspase-3 gene expression 6-fold without altering Bcl-2 gene expression in human monocytic leukemia (THP-1) cells^[1].
Clerodin (60 μM) activates caspase-3/7 in human monocytic leukemia (THP-1) cells^[1].
Clerodin (60 μM) increases caspase-3 protein levels 5-fold and decreases Bcl-2 protein levels in human monocytic leukemia (THP-1) cells^[1].
Clerodin (60 μM) induces a dose-dependent increase in cleaved caspase-3 activation (2 to 4-fold) in human monocytic leukemia (THP-1) cells^[1].
Clerodin (60 μM) induces G₂/M phase cell cycle arrest and increases the Sub G₀/G₁ apoptotic cell population in human monocytic leukemia (THP-1) cells^[1].
Clerodin (60 μM) exhibits no significant cytotoxicity to ex vivo healthy human peripheral blood mononuclear cells (PBMNCs)^[1].
Clerodin binds with highest affinity to human farnesyltransferase (PDB ID 1JCQ, ΔG = -8.2 kcal/mol) and second-highest affinity to human phosphoinositide 3-kinase (PDB ID 4FLH, ΔG = -7.9 kcal/mol), with weaker binding to other tested human cancer-related proteins^[2].
Clerodin (0.5-100 μg/mL; 24 h) potently inhibits human breast carcinoma MCF-7 cell viability with an IC₅₀ of 30.88 μg/mL, while showing lower toxicity to normal human lymphocyte cells (HLCs) at concentrations up to 50 μg/mL^[2].
Clerodin (30.88 μg/mL; 24 h) significantly increases intracellular reactive oxygen species (ROS) generation in human breast carcinoma MCF-7 cells^[2].
Clerodin significantly reduces reduced glutathione (GSH) levels and increases oxidized glutathione (GSSG) levels in human breast carcinoma MCF-7 cells, disrupting redox homeostasis^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

434.52

C₂₄H₃₄O₇

464-71-1

CC(OC[C@]12[C@]3(CCC[C@]1([H])[C@]([C@@H](C[C@@H]2OC(C)=O)C)([C@]4([H])C[C@]5([H])[C@](OC=C5)([H])O4)C)CO3)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Nagaraj B, et al. Clerodane diterpene 3-deoxycaryoptinol (Clerodin) selectively induces apoptosis in human monocytic leukemia (THP-1) cells and upregulates apoptotic protein caspase-3. Free radical biology & medicine. 2024 Nov 20;225:925-932.  [Content Brief]

  [2]. Pakrashy S, et al. Bioinformatics and Network Pharmacology of the First Crystal Structured Clerodin: Anticancer and Antioxidant Potential against Human Breast Carcinoma Cell. ACS omega. 2022 Dec 27;7(51):48572-48582.  [Content Brief]

  [3]. Abbaszadeh G, et al. Insecticidal and antifeedant activities of clerodane diterpenoids isolated from the Indian bhant tree, Clerodendron infortunatum, against the cotton bollworm, Helicoverpa armigera. Journal of insect science (Online). 2014 Feb 26;14:29.  [Content Brief]