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Dengue is a mosquito-borne flavivirus that causes 21,000 deaths annually. Depsides and depsidones of lichens have previously been reported to be antimicrobials. In this study, our objective was to identify lichen-derived depsides and depsidones as dengue virus inhibitors. The 18 depsides and depsidones of , , , and were tested against dengue virus serotype 2. Two depsides and one depsidone inhibited dengue virus serotype 2 without any apparent cytotoxicity. Diffractaic acid, barbatic acid, and Parmosidone C were three active compounds further characterized for their efficacies (EC), cytotoxicities (CC), and selectivity index (SI; CC/EC). Their EC (SI) values were 2.43 ± 0.19 (20.59), 0.91 ± 0.15 (13.33), and 17.42 ± 3.21 (8.95) μM, respectively. Diffractaic acid showed the highest selectivity index, and similar efficacies were also found in dengue serotypes 1-4, Zika, and chikungunya viruses. Cell-based studies revealed that the target was mainly in the late stage with replication and the formation of infectious particles. This report highlights that a lichen-derived diffractaic acid could become a mosquito-borne antiviral lead as its selectivity indices ranged from 8.07 to 20.59 with a proposed target at viral replication.
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http://dx.doi.org/10.3390/molecules28030974 | DOI Listing |
3 Biotech
July 2025
Center for Sickle Cell Disease, College of Medicine, Howard University, Washington, DC USA.
Unlabelled: Prostate cancer (PCa) is the second most frequent and the fifth greatest cause of death in men. Although there are already therapies for early-stage PCa, their effectiveness in advanced PCa is limited, primarily because of medication resistance or poor efficacy. To find new therapeutic indications or repurpose current medications, this project intends to use computational approaches to investigate possible anti-PCa compounds based on simulated screening of FDA-approved drug bank databases.
View Article and Find Full Text PDFSci Rep
February 2025
College of Pharmacy, Sunchon National University, 255 Jungang-ro, Sunchon, Jeonnam, 57922, Republic of Korea.
In recent years, evidence for the anti-cancer activity of lichen secondary metabolites has been rapidly increasing. In this study, we synthesised analogues of diffractaic acid, a lichen secondary metabolite, and evaluated their ability to suppress colorectal cancer stem potential. Among the 10 compounds after H/CH₃/benzylation of the diffractaic acid structure or modifications in an aromatic hydrophobic domain, TU3 has a more inhibition effect on the stem potential of colorectal cancer compared to other compounds.
View Article and Find Full Text PDFNat Prod Res
February 2025
Núcleo de Pesquisas em Ciências Exatas e Tecnológicas, Universidade de Franca, Franca, Brazil.
More than 2.5 billion people live in endemic areas for neglected tropical diseases caused by the protozoan . Which establishes chronic infections and increases public health spending.
View Article and Find Full Text PDFIn Silico Pharmacol
February 2025
Faculty of Industrial Sciences and Technology, Universiti Malaysia Pahang Al-Sultan Abdullah, Lebuhraya Persiaran Tun Khalil Yaakob, 26300 Gambang, Kuantan, Pahang Malaysia.
Unlabelled: Diabetes mellitus (DM) is one of the most common long-term metabolic illnesses with detrimental implications on health and 90-95% of DM cases worldwide are caused by type 2 diabetes (T2DM). The side effects of the existing medicines include vomiting, diarrhea, and serious damage to the kidneys, blood vessels, and nerves. Therefore, finding anti-diabetic medications without side effects is crucial.
View Article and Find Full Text PDFRSC Adv
October 2024
Department of Chemistry, Ho Chi Minh City University of Education 280 An Duong Vuong Street, District 5 Ho Chi Minh City 748342 Vietnam
Using a bio-guided isolation on the Vietnamese lichen based on alpha-glucosidase inhibition, eleven compounds were isolated and structurally elucidated, namely, protocetraric acid (1), 8'-methylstictic acid (2), stictic acid (3), 4,6-diformyl-8-hydroxy-3-methoxy-1,9-dimethyl-11-oxo-11-dibenzo[,][1,4]dioxepine-7-carboxylic acid (4), vicanicin (5), norstictic acid (6), diffractaic acid (7), barbatic acid (8), atranol (9), 5-chlorohaematommic acid (10), and eumitrin A1 (11). Their chemical structures were identified by extensive 1D and 2D NMR analysis and high-resolution mass spectroscopy and compared with those reported in literature. Protocetraric acid (1) and norstictic acid (6) were selected for further modification to derive new compounds, namely, 1a-1e and 6a.
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