ArticlePloS one2013
Inhibition of human neutrophil elastase by pentacyclic triterpenes.
Article in PloS one, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
14 citing papers in PubMed, 36 citations in OpenAlex.
- Regenerative therapeutics for chronic obstructive pulmonary disease.Pharmacological reviews · 2026Review
- Sivelestat (Neutrophil Elastase Inhibitor) as an Anti-inflammatory and Anti-viral Agent: An In Silico Study.Cureus · 2024Article
- Plant In Vitro Culture Factories for Pentacyclic Triterpenoid Production.Advances in biochemical engineering/biotechnology · 2024Review
- Anti-Inflammatory and Antioxidant Properties of β-Sitosterol in Copper Sulfate-Induced Inflammation in Zebrafish (Antioxidants (Basel, Switzerland) · 2023Article
- ANTIAGE-DB: A Database and Server for the Prediction of Anti-Aging Compounds Targeting Elastase, Hyaluronidase, and Tyrosinase.Antioxidants (Basel, Switzerland) · 2022Review
- Sequence preference and scaffolding requirement for the inhibition of human neutrophil elastase by ecotin peptide.Protein science : a publication of the Protein Society · 2022Article
- Immunomodulatory properties of triterpenes.Phytochemistry reviews : proceedings of the Phytochemical Society of Europe · 2022Review
- Two triterpenoids from Rubus fraxinifolius leaves and their tyrosinase and elastase inhibitory activities.Scientific reports · 2021Article
- Ursolic Acid and Related Analogues: Triterpenoids with Broad Health Benefits.Antioxidants (Basel, Switzerland) · 2021Review
- Immunomodulatory effects and structure-activity relationship of botanical pentacyclic triterpenes: A review.Chinese herbal medicines · 2020Review
- Novel Sulfonamide Analogs of Sivelestat as Potent Human Neutrophil Elastase Inhibitors.Frontiers in chemistry · 2020Article
- Neutrophil elastase inhibitory effects of pentacyclic triterpenoids from Eriobotrya japonica (loquat leaves).Journal of ethnopharmacology · 2019Article
- Inhibition of Human Kallikrein 5 Protease by Triterpenoids from Natural Sources.Molecules (Basel, Switzerland) · 2017Article
- Pulmonary Complications of Azanucleoside Therapy in Patients with Myelodysplastic Syndrome and Acute Myelogenous Leukemia.Case reports in hematology · 2015Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
scopeInhibiting human neutrophil elastase (HNE) is a promising strategy for treating inflammatory lung diseases, such as H1N1 and SARS virus infections. The use of sivelestat, the only clinically registered synthesized HNE inhibitor, is largely limited by its risk of organ toxicity because it irreversibly inhibits HNE. Therefore, potent reversible HNE inhibitors are promising alternatives to sivelestat. METHODS AND
resultsAn in vitro HNE inhibition assay was employed to screen a series of triterpenes. Six pentacyclic triterpenes, but not tetracyclic triterpenes, significantly inhibited HNE. Of these pentacyclic triterpenes, ursolic acid exhibited the highest inhibitory potency (IC50 = 5.51 µM). The HNE inhibitory activity of ursolic acid was further verified using a mouse model of acute smoke-induced lung inflammation. The results of nuclear magnetic resonance and HNE inhibition kinetic analysis showed that the pentacyclic triterpenes competitively and reversibly inhibited HNE. Molecular docking experiments indicated that the molecular scaffold, 28-COOH, and a double bond at an appropriate location in the pentacyclic triterpenes are important for their inhibitory activity.
conclusionOur results provide insights into the effects of pentacyclic triterpenes on lung inflammatory actions through reversible inhibition of HNE activity.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.