Lactonase activity of α‐carbonic anhydrases allows identification of novel inhibitors DOI Creative Commons
Simone Giovannuzzi, Claudiu T. Supuran

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 9, 2024

Abstract Lactones, a diverse and abundant class of molecules found in nature, exhibit wide range bioactivities, including anti‐inflammatory, anticancer, antibacterial effects. Among them, acyl homoserine lactones (AHSLs) play crucial role quorum sensing, influencing bacterial pathogenicity biofilm formation Gram‐negative bacteria. Paraoxonases (PONs), calcium‐containing enzymes known for their lactonase activity, have been shown to hydrolyze AHSLs reduce the several pathogenic In this study, we explored potential activity zinc(II) enzymes, carbonic anhydrases (CAs), aiming uncover new insights into catalytic versatility. Using LC‐MS MS/MS analyses, investigated CAs assessed through stopped‐flow kinetic assay as substrates/inhibitors. Our findings reveal that are novel “prodrug” inhibitors CAs, with DHC 6 showing most promising inhibition constants ( K I s) low micromolar against both human isozymes.

Language: Английский

Evaluation of antioxidant and antibacterial properties of dehydrocostus lactone isolated from Echinops kebericho root DOI Creative Commons
Sisay Awoke Endalew,

Minbale Gashu Taddese,

M. Mumthas Muhammed

et al.

Health Science Reports, Journal Year: 2024, Volume and Issue: 7(3)

Published: March 1, 2024

, an endemic plant to Ethiopia, traditionally used treat infectious as well noninfectious diseases. The primary objective of this study was isolating dehydrocostus lactone (DHCL) from

Language: Английский

Citations

5
Evaluation of Antibacterial Activity of a Sesquiterpenoid Isolated From the Leaves of Laggera tomentosa Endemic to Ethiopia DOI Creative Commons

Tesfamariam Kassa Adal,

Sisay Awoke Endalew,

Amualaw Birara Beshir

et al.

Natural Sciences, Journal Year: 2025, Volume and Issue: unknown

Published: April 23, 2025

ABSTRACT The success in discovering natural therapeutic agents relies on bioassay‐guided fractionation and purification techniques. Active ingredients from herbal medicines are beneficial due to their compatibility with various other active substances. To evaluate the antibacterial activities of sesquiterpenoid compound isolated leaves Laggera tomentosa endemic Ethiopia. crude extract was obtained using maceration technique . Hexane, ethyl acetate, methanol were used fractionate for phytochemical evaluation. screening done test presence or absence alkaloids, phenols, saponins, flavonoids, tannins, steroids, glycosides. Methanol subjected silica gel column chromatography isolate pure compound. Structural elucidation via IR NMR. fractions assess activity potentials this plant material disc diffusion assay against E. coli, S. aureus , L. monocytogen (48 g) 300 g powder separation (65 mg) isolated. indicates tannins steroids Spectral analysis results revealed that identified as 3‐O‐(3′‐acetoxy‐2′‐hydroxy‐2′‐methylbutyryl)‐cuauhtemone. Regarding activities, highest (15.56 ± 1.96 mm) lowest (6.5 0.01 inhibition zone diameters recorded at concentrations 100 10 mg/mL, respectively, by soluble fraction. methanol‐soluble portion exhibited promising warranting further studies.

Language: Английский

Citations

0
Exploring hidden natural resources for bioactive compounds: Focused chemical and biological studies on some Anthemis species. DOI
Dimitrina Zheleva‐Dimitrova, Reneta Gevrenova, Sakina Yagi

et al.

Food and Chemical Toxicology, Journal Year: 2025, Volume and Issue: 202, P. 115467 - 115467

Published: May 2, 2025

Language: Английский

Citations

0
Assessment of antimicrobial, free radical scavenging, and anti-inflammatory activities of Holarrhena pubescens (Buch.-Ham.) Wall. seeds using in vitro methods and evaluation of antiarthritic potential using an in vivo method DOI Creative Commons
Santanu Saha,

EVS Subrahmanyam

Journal of Herbmed Pharmacology, Journal Year: 2024, Volume and Issue: 14(1), P. 82 - 89

Published: Dec. 25, 2024

Introduction: Holarrhena pubescens is used traditionally for treating several infectious and inflammatory disorders with no scientific evidence. The present study was designed to evaluate the antimicrobial free radical scavenging properties of different fractions ethanolic extract H. seeds. Furthermore, potential plant in acute chronic inflammation through vitro vivo experiments also evaluated. Methods: successive seeds, including petroleum ether (HPF), chloroform (HCF), methanol (HMF) were subjected eradicate microorganisms using disc diffusion method scavenge oxidants DPPH method. HCF further an anti-inflammatory activity by inhibition bovine serum albumin denaturation assay effect drug a condition adjuvant-induced arthritis rats’ model. Results: showed most potent among all test drugs. fraction broad-spectrum 80.35 ± 0.46% (IC50 value = 28.41 0.33 µg/mL) antioxidant study. Further, 68.37 1.11% 75.16% (0.38 0.16 mL, P<0.05) rat paw edema Conclusion: exhibited antimicrobial, potentials

Language: Английский

Citations

0
Lactonase activity of α‐carbonic anhydrases allows identification of novel inhibitors DOI Creative Commons
Simone Giovannuzzi, Claudiu T. Supuran

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 9, 2024

Abstract Lactones, a diverse and abundant class of molecules found in nature, exhibit wide range bioactivities, including anti‐inflammatory, anticancer, antibacterial effects. Among them, acyl homoserine lactones (AHSLs) play crucial role quorum sensing, influencing bacterial pathogenicity biofilm formation Gram‐negative bacteria. Paraoxonases (PONs), calcium‐containing enzymes known for their lactonase activity, have been shown to hydrolyze AHSLs reduce the several pathogenic In this study, we explored potential activity zinc(II) enzymes, carbonic anhydrases (CAs), aiming uncover new insights into catalytic versatility. Using LC‐MS MS/MS analyses, investigated CAs assessed through stopped‐flow kinetic assay as substrates/inhibitors. Our findings reveal that are novel “prodrug” inhibitors CAs, with DHC 6 showing most promising inhibition constants ( K I s) low micromolar against both human isozymes.

Language: Английский

Citations

0