Structural modification of natural and synthetic quinones for antiviral screening against human important flaviviruses.

Arboviruses such as dengue and Zika are clinically significant human pathogens lacking effective antiviral treatments. Studies seeking DENV inhibitors, consider lipophilicity as a crucial parameter for optimising drug entry into infected host cells. In this study, Aloesaponarin I (1), Aloe-Emodin (2), obtained from Aloe vera roots, together with Methylnaphthazarin (3) were derivatized to increase lipophilicity, by acylation and alkylation reactions. The derivatives obtained were evaluated for antiviral activity against all four DENV serotypes and ZIKV in vitro using the Focus Reduction Neutralisation Test and Celgosivir and human sera as positive controls. Additionally, cytotoxic studies were performed showed that derivatives from (1) and (2) were non-toxic at 250-1.9 µM, while (3) derivatives from 156-7.8 µM. Derivatives as 10, 19 and 24 had the maximum inhibition percentages ranged from 82 to 99% with IC50 values between 18 to 1 µM, mainly against DENV4 and Zika viruses.

• Publication year

  2026

• Venue

  Natural Product Research

• Publication date

  2026-02-02

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1080/14786419.2026.2621087PMID 41622924
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar

• No claims are published for this paper.

• No concepts are published for this paper.

• Antiviral Compounds from Natural Sources Against Human Arboviruses: An Updated Review Including Illustrative In Silico Analysis

  2025cited by this paper
• The TIRS trial: Enrollment procedures and baseline characterization of a pediatric cohort to quantify the epidemiologic impact of targeted indoor residual spraying on Aedes-borne viruses in Merida, Mexico

  2024cited by this paper
• The Interaction of Anthracycline Based Quinone-Chelators with Model Lipid Membranes: 1H NMR and MD Study

  2023cited by this paper
• Design, synthesis, and biological evaluation of a series of new anthraquinone derivatives as anti-ZIKV agents.

  2023cited by this paper
• Congenital Zika Syndrome: A Nationwide Cohort Study in Brazil, 2015-2018

  2022cited by this paper
• Recent advances in natural products as potential inhibitors of dengue virus with a special emphasis on NS2b/NS3 protease.

  2022cited by this paper
• Promising Role of Emodin as Therapeutics to Against Viral Infections

  2022cited by this paper
• Searching for plant-derived antivirals against dengue virus and Zika virus

  2022cited by this paper
• Recent advances of quinones as a privileged structure in drug discovery.

  2021cited by this paper
• Cheminformatic analysis of natural product-based drugs and chemical probes.

  2021cited by this paper
• Current Trends and Limitations in Dengue Antiviral Research

  2021cited by this paper
• De novo design approaches targeting an envelope protein pocket to identify small molecules against dengue virus.

  2019cited by this paper
• Anti-Herpetic, Anti-Dengue and Antineoplastic Activities of Simple and Heterocycle-Fused Derivatives of Terpenyl-1,4-Naphthoquinone and 1,4-Anthraquinone

  2019cited by this paper
• Effects of lipid composition on membrane distribution and permeability of natural quinones

  2019cited by this paper
• Anthraquinones As Pharmacological Tools and Drugs

  2016cited by this paper
• The dengue virus NS5 protein as a target for drug discovery.

  2015cited by this paper
• Antiviral activities of 15 dengue NS2B-NS3 protease inhibitors using a human cell-based viral quantification assay.

  2015cited by this paper
• Antiviral activity of aloe-emodin against influenza A virus via galectin-3 up-regulation.

  2014cited by this paper
• The global distribution and burden of dengue

  2013cited by this paper
• Targeting Cell Entry of Enveloped Viruses as an Antiviral Strategy

  2010cited by this paper
• Escape from flatland: increasing saturation as an approach to improving clinical success.

  2009cited by this paper

• No citing papers are available for this paper.