Related Experiment Video
Updated: Oct 15, 2026

Human Neuroendocrine Tumor Cell Lines as a Three-Dimensional Model for the Study of Human Neuroendocrine Tumor Therapy
Published on: August 14, 2012
Ergostane-type steroids from Euphorbia thymifolia with acetylcholinesterase inhibitory effects
Chun-Gu Wang1, Fan-Fan Wang2, Yuan-Ling Shao1
1Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Southeast University, Nanjing, China.
Abstract:
Thymifolisteroid A (1), a previously undescribed ergostane-type steroid, and five known related compounds (2-6), were obtained from Euphorbia thymifolia. The known compounds were identified as 3β-hydroxy-4α,14α-dimethyl-5α-ergosta-8,24(28)-dien-7-one (2), β-sitosterol (3), β-sitosteryl-3-O-glucopyranoside (4), 5α-stigmastane-3,6-dione (5) and (6β)-6-hydroxyergost-4-en-3-one (6). Their chemical structures and absolute configuration were determined through comprehensive spectroscopic and mass spectrometric (MS) analyses. Biological evaluation revealed that compound 3 possessed moderate acetylcholinesterase (AChE) inhibitory activity, with an IC50 value of 14.43 ± 0.68 μM, compared with 4.19 ± 0.25 μM for the positive control drug donepezil. Furthermore, molecular docking and molecular dynamics simulations jointly suggested that compound 3 can stably bind to the active site of AChE.
Related Concept Videos
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
The direct-acting...
Indirect-Acting Cholinergic Agonists: Pharmacological Actions
At the neuromuscular junction, these agents work by inhibiting the breakdown of acetylcholine, allowing it to remain bound to the receptor and bind to nearby receptors. This process leads to repetitive firing of the endplate, causing muscle...
Indirect-Acting Cholinergic Agonists: Mechanism of Action
Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex, leading to...
Direct-Acting Cholinergic Agonists: Therapeutic Uses
Direct-Acting Cholinergic Agonists: Pharmacokinetics