ArticleMolecules (Basel, Switzerland)2014
Structure-activity relationship study of sesquiterpene lactones and their semi-synthetic amino derivatives as potential antitrypanosomal products.
Article in Molecules (Basel, Switzerland), 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers, 1 of them a synthesis that pooled it.
What it found
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
15 citing papers in PubMed, 1 synthesis or guideline pooled it, 45 citations in OpenAlex.
- The Effects of Sesquiterpene Lactones on the Differentiation of Human or Animal Cells CulturedFrontiers in pharmacology · 2022Pooled it
- Plant-Derived Terpenes as Emerging Therapeutics Against Schistosomiasis.International journal of molecular sciences · 2026Review
- 8-Epixanthatin Suppresses RANKL-Induced Osteoclast Differentiation via Inhibition of NF-κB and MAPK Signaling.International journal of molecular sciences · 2026Article
- Bioassay-guided isolation of dehydrocostus lactone fromHeliyon · 2024Article
- Arnicolide D: a multi-targeted anticancer sesquiterpene lactone-preclinical efficacy and mechanistic insights.Naunyn-Schmiedeberg's archives of pharmacology · 2024Review
- A novel approach for assessment of antitrypanosomal activity of sesquiterpene lactones through additive and non-additive molecular structure parameters.Molecular diversity · 2023Article
- Article
- Sesquiterpene lactones ofChinese herbal medicines · 2021Review
- Sesquiterpene Lactones fromMolecules (Basel, Switzerland) · 2020Article
- Cynaropicrin Shows Antitumor Progression Potential in Colorectal Cancer Through Mediation of the LIFR/STATs Axis.Frontiers in cell and developmental biology · 2020Article
- Derivatisation of parthenolide to address chemoresistant chronic lymphocytic leukaemia.MedChemComm · 2019Article
- Antiparasitic activity of chicory (Cichorium intybus) and its natural bioactive compounds in livestock: a review.Parasites & vectors · 2018Review
- Acid-Induced Rearrangement of Epoxygermacranolides: Synthesis of Furanoheliangolides and Cadinanes from Nobilin.Molecules (Basel, Switzerland) · 2017Article
- Pan-genotypic Hepatitis C Virus Inhibition by Natural Products Derived from the Wild Egyptian Artichoke.Journal of virology · 2016Article
- Cynaropicrin: A Comprehensive Research Review and Therapeutic Potential As an Anti-Hepatitis C Virus Agent.Frontiers in pharmacology · 2016Review
Corrections and comments
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Authors and funding
11 authors at 5 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Sesquiterpene lactones (STLs) are natural products that have potent antitrypanosomal activity in vitro and, in the case of cynaropicrin, also reduce parasitemia in the murine model of trypanosomiasis. To explore their structure-antitrypanosomal activity relationships, a set of 34 natural and semi-synthetic STLs and amino-STLs was tested in vitro against T. b. rhodesiense (which causes East African sleeping sickness) and mammalian cancer cells (rat bone myoblast L6 cells). It was found that the α-methylene-γ-lactone moiety is necessary for both antitrypanosomal effects and cytotoxicity. Antitrypanosomal selectivity is facilitated by 2-(hydroxymethyl)acrylate or 3,4-dihydroxy-2-methylenebutylate side chains, and by the presence of cyclopentenone rings. Semi-synthetic STL amines with morpholino and dimethylamino groups showed improved in vitro activity over the native STLs. The dimethylamino derivative of cynaropicrin was prepared and tested orally in the T. b. rhodesiense acute mouse model, where it showed reduced toxicity over cynaropicrin, but also lost antitrypanosomal 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.