HCO₃^- is involved in pH homoeostasis and plays a multifaceted role in human health. HCO₃^- has been recognized for its antimicrobial properties and is pivotal in bacterial antibiotic susceptibility. Notably, the interconversion between CO₂ and HCO₃^-, facilitated by the enzyme carbonic anhydrase (CA), is crucial in tissues infected by pathogens. Studies have highlighted the antimicrobial potency of CA inhibitors, emphasizing the importance of this enzyme in this area. The potential of HCO₃^- as an antibiotic adjuvant is evident; its ability to increase virulence in pathogens such as Enterococcus faecalis and Mycobacterium tuberculosis requires meticulous scrutiny. HCO₃^- modulates bacterial behaviours in diverse manners: it promotes Escherichia coli O157:H7 colonization in the human gut by altering specific gene expression and, with Pseudomonas aeruginosa, amplifies the effect of tobramycin on planktonic cells while promoting biofilm formation. These multifaceted effects necessitate profound mechanistic exploration before HCO₃^- can be considered a promising clinical adjuvant.

01 May 2025·Bioactive Materials

Self-healable and pH-responsive spermidine/ferrous ion complexed hydrogel Co-loaded with CA inhibitor and glucose oxidase for combined cancer immunotherapy through triple ferroptosis mechanism

Article

Author: Wu, Jun ; Cai, Yishui ; Zhang, Ruhe ; Fang, Yifei ; Jiao, Yuenong ; Wang, Xiaobo ; Nie, Tianqi

Tumor microenvironment governs various therapeutic tolerability of cancer such as ferroptosis and immunotherapy through rewiring tumor metabolic reprogramming like Warburg metabolism. Highly expressed carbonic anhydrases (CA) in tumor that maintaining the delicate metabolic homeostasis is thus the most potential target to be modulated to resolve the therapeutic tolerability. Hence, in this article, a self-healable and pH-responsive spermidine/ferrous ion hydrogel loaded with CA inhibitor (acetazolamide, ACZ) and glucose oxidase (ACZ/GOx@SPM-HA Gel) was fabricated through the Schiff-base reaction between spermidine-dextran and oxidized hyaluronic acid, along with ferrous coordination. Investigation on cancer cell lines (MOC-1) demonstrated ACZ/GOx@SPM-HA Gel may induce cellular oxidative stress and mitochondrial dysfunction through disrupting the cellular homeostasis. Moreover, with the facilitation of autophagy induced by spermidine, ACZ/GOx@SPM-HA Gel may trigger a positive feedback loop to maximally amplify cellular ferroptosis and promote DAMPs release. The anti-tumor evaluation on xenograft mice models furtherly proved the local injection of such hydrogel formulation could efficiently inhibit the tumor growth and distinctively promote the immunogenicity of tumor bed to provide a more favorable environment for immunotherapy. Overall, ACZ/GOx@SPM-HA Gel, with such feasible physiochemical properties and great biocompatibility, holds great potential in treating solid tumors with acidosis-mediated immunotherapy tolerance.

01 Apr 2025·International Journal of Biological Macromolecules

Identification of new 1,2,3-Triazole analogues of sulfanilamide as inhibitors of the carbonic anhydrase II enzyme: Comprehensive in-vitro and in-vivo analyses

Article

Author: Malik, Aqsa ; Tahir, Syeda Sarah ; Huda, Noor Ul ; Arif, Rida ; Rasheed, Saima ; Warsi, Zoha ; Khan, Maria Aqeel

Carbonic anhydrases (CAs) play a vital role in various physiological processes by catalyzing the reversible hydration of CO₂ into HCO₃^-, hence maintaining the fluid and pH balance. Overexpression of carbonic anhydrases II (CA II) is associated with diseases, such as glaucoma, and epilepsy; therefore, it is considered as an important clinical target. Therapeutically used CA inhibitors exhibit several undesirable effects; therefore, there is an urgent need to identify new, safe, and effective inhibitors of the CAs. Keeping in view the importance of CA II inhibition, a library of new 1,3-disubstituted-1,2,3-triazole analogues of sulfanilamide is synthesized via Click chemistry, starting from sulfanilamide azide and different substituted propargyl ethers, incorporating benzyl and heteroarylmethyl moieties. The new derivatives showed significant CA II inhibitory activity (IC₅₀ ranging between 0.19 and 0.66 μM) when compared with the standard inhibitor, acetazolamide (0.13 ± 0.01 μM). Among all, compounds 16 and 17 showed the most potent activity (IC₅₀ = 0.19 μM) followed by compounds 23, and 18 (IC₅₀ = 0.24 ± 0.014 and 0.26 ± 0.04 μM, respectively). Kinetics studies showed that all compounds are competitive inhibitors of bCA II enzyme (K_i ranging between 0.14 and 0.68 μM). Additionally, molecular docking studies revealed that all compounds formed network of interactions with the active site residues of the bCA II enzyme. All compounds were found to be non-toxic against BJ Human fibroblast cells. From in-vivo studies, we found that CA activity was significantly inhibited by the intraperitoneal administration of compounds 16 and 17 for up to 5 h. In conclusion, new 1,2,3-triazole analogues of sulfanilamide were identified as good CA II inhibitors.

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