ArticleFrontiers in pharmacology2017
Structure-Activity Relationships of Pentacyclic Triterpenoids as Potent and Selective Inhibitors against Human Carboxylesterase 1.
Article in Frontiers in pharmacology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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18 citing papers in PubMed, 56 citations in OpenAlex.
- Acetylation of Oleanolic Acid Dimers as a Method of Synthesis of Powerful Cytotoxic Agents.Molecules (Basel, Switzerland) · 2024Article
- Principal Bioactive Properties of Oleanolic Acid, Its Derivatives, and Analogues.Molecules (Basel, Switzerland) · 2024Review
- Article
- Discovery of triterpenoids as potent dual inhibitors of pancreatic lipase and human carboxylesterase 1.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Optical substrates for drug-metabolizing enzymes: Recent advances and future perspectives.Acta pharmaceutica Sinica. B · 2022Review
- Inhibition of catechol-Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Two New Triterpenes from Basidiomata of the Medicinal and Edible Mushroom,Molecules (Basel, Switzerland) · 2021Article
- Tumor-suppressing effect of bartogenic acid in ovarian (SKOV-3) xenograft mouse model.Naunyn-Schmiedeberg's archives of pharmacology · 2021Article
- Human carboxylesterases and fluorescent probes to image their activity in live cells.RSC medicinal chemistry · 2021Review
- Biotransformation of Oleanane and Ursane Triterpenic Acids.Molecules (Basel, Switzerland) · 2020Review
- Therapeutic Potential of Ursonic Acid: Comparison with Ursolic Acid.Biomolecules · 2020Review
- Serjanic Acid Improves Immunometabolic Markers in a Diet-Induced Obesity Mouse Model.Molecules (Basel, Switzerland) · 2020Article
- Development and Evaluation of Oleanolic Acid Dosage Forms and Its Derivatives.BioMed research international · 2020Review
- Article
- Inhibition of human carboxylesterases by ginsenosides: structure-activity relationships and inhibitory mechanism.Chinese medicine · 2019Article
- Effects of Panax Notoginseng Saponins on Esterases Responsible for Aspirin Hydrolysis In Vitro.International journal of molecular sciences · 2018Article
- Human carboxylesterases: a comprehensive review.Acta pharmaceutica Sinica. B · 2018Review
- Inhibitory Influence of Panax notoginseng Saponins on Aspirin Hydrolysis in Human Intestinal Caco-2 Cells.Molecules (Basel, Switzerland) · 2018Article
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Authors and funding
11 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Human carboxylesterase 1 (hCE1), one of the most important serine hydrolases distributed in liver and adipocytes, plays key roles in endobiotic homeostasis and xenobiotic metabolism. This study aimed to find potent and selective inhibitors against hCE1 from phytochemicals and their derivatives. To this end, a series of natural triterpenoids were collected and their inhibitory effects against human carboxylesterases (hCEs) were assayed using D-Luciferin methyl ester (DME) and 6,8-dichloro-9,9-dimethyl-7-oxo-7,9-dihydroacridin-2-yl benzoate (DDAB) as specific optical substrate for hCE1, and hCE2, respectively. Following screening of a series of natural triterpenoids, oleanolic acid (OA), and ursolic acid (UA) were found with strong inhibitory effects on hCE1 and relative high selectivity over hCE2. In order to get the highly selective and potent inhibitors of hCE1, a series of OA and UA derivatives were synthesized from OA and UA by chemical modifications including oxidation, reduction, esterification, and amidation. The inhibitory effects of these derivatives on hCEs were assayed and the structure-activity relationships of tested triterpenoids as hCE1 inhibitors were carefully investigated. The results demonstrated that the carbonyl group at the C-28 site is essential for hCE1 inhibition, the modifications of OA or UA at this site including esters, amides and alcohols are unbeneficial for hCE1 inhibition. In contrast, the structural modifications on OA and UA at other sites, such as converting the C-3 hydroxy group to 3-O-β-carboxypropionyl (compounds
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