Antifungal repurposing of clinical chelator DMSA against Cryptococcus neoformans via laccase and histidine biosynthesis inhibition.

Bibliographic Details
Title: Antifungal repurposing of clinical chelator DMSA against Cryptococcus neoformans via laccase and histidine biosynthesis inhibition.
Authors: Zhang C; Department of Dermatology, Jinling Hospital, Affiliated Hospital of Medical School, Nanjing University, Nanjing, China., Peng M; Department of Dermatology, Jinling Hospital, Affiliated Hospital of Medical School, Nanjing University, Nanjing, China., Hu Q; MOE Key Laboratory of Bioinorganic and Synthetic Chemistry, School of Chemistry, Sun Yat-Sen University, Guangzhou, 510275, China., Huang S; State Key Laboratory of Coordination Chemistry, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing, 210023, China., Zhang Q; Jinling Clinical Medical College, Nanjing Medical University, China., Zhu J; State Key Laboratory of Coordination Chemistry, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing, 210023, China., Sang H; Department of Dermatology, Jinling Hospital, Affiliated Hospital of Medical School, Nanjing University, Nanjing, China. Electronic address: sanghong@nju.edu.cn., Kong Q; Department of Dermatology, Jinling Hospital, Affiliated Hospital of Medical School, Nanjing University, Nanjing, China. Electronic address: kongqingtao2008@163.com.
Source: Microbial pathogenesis [Microb Pathog] 2026 May; Vol. 214, pp. 108375. Date of Electronic Publication: 2026 Feb 10.
Publication Type: Journal Article
Language: English
Journal Info: Publisher: Academic Press Country of Publication: England NLM ID: 8606191 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1096-1208 (Electronic) Linking ISSN: 08824010 NLM ISO Abbreviation: Microb Pathog Subsets: MEDLINE
Imprint Name(s): Original Publication: London ; Orlando : Academic Press, c1986-
MeSH Terms: Cryptococcus neoformans*/drug effects , Cryptococcus neoformans*/enzymology , Cryptococcus neoformans*/pathogenicity , Laccase*/antagonists & inhibitors , Laccase*/metabolism , Laccase*/drug effects , Antifungal Agents*/pharmacology , Chelating Agents*/pharmacology , Histidine*/biosynthesis , Histidine*/antagonists & inhibitors , Succimer*/pharmacology , Drug Repositioning*, Biofilms/drug effects ; Biofilms/growth & development ; Cryptococcosis/microbiology ; Cryptococcosis/drug therapy ; Moths/microbiology ; Urease/metabolism ; Fungal Capsules/drug effects ; Animals ; Microbial Sensitivity Tests ; Virulence Factors ; Humans ; Disease Models, Animal
Abstract: As a globally distributed opportunistic fungus, Cryptococcus neoformans poses a significant threat to human health by causing fatal meningitis, which is associated with high mortality and morbidity rates. Current antifungals-polyenes, flucytosine, and azoles-are limited by toxicity and resistance, underscoring the need for new agents. This study evaluated dimercaptosuccinic acid (DMSA), a chelating agent used in the treatment of heavy metal poisoning, beginning with its effect on the virulence factor laccase. DMSA showed broad-spectrum activity against standard (H99, B3501) and clinical isolate strains, with MIC values of 32-64 μg/mL. It inhibited laccase (IC50 = 43.98 μM; Km = 0.547 mM with levodopa) and impaired multiple virulence factors, including capsule formation (43.2% reduction in H99), urease activity (68.6% inhibition in H99 and 53.4% in B3501), as well as biofilm formation and its metabolic activity. In a Galleria mellonella infection model, although survival was not significantly improved, DMSA reduced fungal burden by 30% (P < 0.05), supported by histology and Colony-Forming Units (CFU) counts. Further transcriptomic and nutrient supplementation assays indicated that the antifungal action of DMSA is mediated through interference with histidine biosynthesis, suggesting a mechanism beyond laccase inhibition.
(Copyright © 2026. Published by Elsevier Ltd.)
Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
Contributed Indexing: Keywords: Cryptococcus neoformans; Dimercaptosuccinic acid; Drug repurposing; Histidine biosynthesis; Laccase
Substance Nomenclature: EC 1.10.3.2 (Laccase)
0 (Antifungal Agents)
0 (Chelating Agents)
4QD397987E (Histidine)
DX1U2629QE (Succimer)
0 (Virulence Factors)
EC 3.5.1.5 (Urease)
Entry Date(s): Date Created: 20260212 Date Completed: 20260707 Latest Revision: 20260707
Update Code: 20260708
DOI: 10.1016/j.micpath.2026.108375
PMID: 41679612
Database: MEDLINE
Description
ISSN:1096-1208
DOI:10.1016/j.micpath.2026.108375