ArticleInternational journal for parasitology. Drugs and drug resistance2019
Antileishmanial activity of terpenylquinones on Leishmania infantum and their effects on Leishmania topoisomerase IB.
Article in International journal for parasitology. Drugs and drug resistance, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 36 citations in OpenAlex.
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- Targeting of Leishmania proteins by β-Lapachone derivatives reveals a promising multitarget candidate.Archives of microbiology · 2026Article
- Antileishmanial and Immunomodulatory Activity of Paclitaxel and Docetaxel Combined with Miltefosine and Paromomycin.International journal of molecular sciences · 2026Article
- Molecular docking: a computational approach for the discovery of novel targets against visceral leishmaniasis.Journal of molecular modeling · 2026Review
- Pharmacomodulation of the Redox-Active Lead Plasmodione: Synthesis of Substituted 2-Benzylnaphthoquinone Derivatives, Antiplasmodial Activities, and Physicochemical Properties.International journal of molecular sciences · 2025Article
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- Evaluation of sugar meal administered anti-Leishmania compounds on the vectorial capacity of the vector, Lutzomyia longipalpis.PloS one · 2025Article
- Molecular docking ofIn silico pharmacology · 2025Article
- Gastroprotective role of a flavonoid-rich subfraction from Fridericia chica (Bonpl.) L. G. Lohmann: a medicinal plant used in the Amazon region.Inflammopharmacology · 2024Article
- Natural-Product-Inspired Microwave-Assisted Synthesis of Novel Spirooxindoles as Antileishmanial Agents: Synthesis, Stereochemical Assignment, Bioevaluation, SAR, and Molecular Docking Studies.Molecules (Basel, Switzerland) · 2023Article
- Antiprotozoal activity of natural products from Nigerien plants used in folk medicine.Frontiers in pharmacology · 2023Article
- In vitro nematocidal activity ofJournal of parasitic diseases : official organ of the Indian Society for Parasitology · 2022Article
- Potential therapeutic targets shared between leishmaniasis and cancer.Parasitology · 2021Review
- New Antineoplastic Naphthohydroquinones Attached to Labdane and Rearranged Diterpene Skeletons.Molecules (Basel, Switzerland) · 2021Article
- A Novel Cytotoxic Conjugate Derived from the Natural Product Podophyllotoxin as a Direct-Target Protein Dual Inhibitor.Molecules (Basel, Switzerland) · 2020Article
- Immunogenicity and Protective Effect of a Virus-Like Particle Containing the SAG1 Antigen ofBiomedicines · 2020Article
- Investigating the Antiparasitic Potential of the Marine Sesquiterpene Avarone, Its Reduced form Avarol, and the Novel Semisynthetic Thiazinoquinone Analogue Thiazoavarone.Marine drugs · 2020Article
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Leishmania is the aethiological agent responsible for the visceral leishmaniasis, a serious parasite-borne disease widely spread all over the World. The emergence of resistant strains makes classical treatments less effective; therefore, new and better drugs are necessary. Naphthoquinones are interesting compounds for which many pharmacological properties have been described, including leishmanicidal activity. This work shows the antileishmanial effect of two series of terpenyl-1,4-naphthoquinones (NQ) and 1,4-anthraquinones (AQ) obtained from natural terpenoids, such as myrcene and myrceocommunic acid. They were evaluated both in vitro and ex vivo against the transgenic iRFP-Leishmania infantum strain and also tested on liver HepG2 cells to determine their selectivity indexes. The results indicated that NQ derivatives showed better antileishmanial activity than AQ analogues, and among them, compounds with a diacetylated hydroquinone moiety provided better results than their corresponding quinones. Regarding the terpenic precursor, compounds obtained from the monoterpenoid myrcene displayed good antiparasitic efficiency and low cytotoxicity for mammalian cells, whereas those derived from the diterpenoid showed better antileishmanial activity without selectivity. In order to explore their mechanism of action, all the compounds have been tested as potential inhibitors of Leishmania type IB DNA topoisomerases, but only some compounds that displayed the quinone ring were able to inhibit the recombinant enzyme in vitro. This fact together with the docking studies performed on LTopIB suggested the existence of another mechanism of action, alternative or complementary to LTopIB inhibition. In silico druglikeness and ADME evaluation of the best leishmanicidal compounds has shown good predictable druggability.
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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 Socratic graph.