Cardiovascular diseases are the leading cause of mortality worldwide. In recent years, the relationship between carbonic anhydrase inhibitors and atherosclerosis has attracted attention. In this study, we aimed to determine the effects of 35 frequently used cardiac drugs on human carbonic anhydrase I (hCA I) and II (hCA II). The inhibitory effects of the drugs on hCA I and hCA II were determined with both the hydratase and esterase methods. The most potent inhibitors observed were propafenone (hCA I: 2.8 µM and hCA II: 3.02 µM) and captopril (hCA I: 1.58 µM and hCA II: 6.25 µM). Isosorbide mononitrate, propranolol, furosemide, and atorvastatin were also potent inhibitors. The inhibitor constant, , value from the Lineweaver-Burk plot for propafenone was 2.38 µM for hCA I and 2.97 µM for hCA II. The tested cardiac drugs showed potent inhibition of the hCA I and II isozymes. Especially, in patients with atherosclerotic heart disease, these drugs may be preferred primarily due to the beneficial effects of carbonic anhydrase inhibition on atherosclerosis.
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http://dx.doi.org/10.1080/14756366.2020.1781844 | DOI Listing |
Molecules
December 2024
Marine Natural Products Research and Development Key Laboratory of Qingdao, First Institute of Oceanography, Ministry of Natural Resources, Qingdao 266061, China.
The exploration and exploitation of deep-sea microbial resources is of great scientific value for understanding biological evolution under extreme conditions. Deep-sea microorganisms are critical in the ocean carbon cycle, and marine heterotrophic microorganisms secrete extracellular carbonic anhydrase (CA) to fix inorganic carbon, an important process in climate regulation. Extracellular CA provides a green method for fixing carbon dioxide into stable minerals containing Ca.
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December 2024
Division of Cancer Immunology and Immune Modulation, Boehringer Ingelheim Pharma GmbH & Co. KG, 88397 Biberach, Germany.
Membrane proteins, especially extracellular domains, are key therapeutic targets due to their role in cell communication and associations. Yet, their functions and interactions often remain unclear. This study presents a general method to discover interactions of membrane proteins with immune cells and subsequently to deorphanize their respective receptors.
View Article and Find Full Text PDFAntioxidants (Basel)
December 2024
Department of Chemistry and Biochemistry, Faculty of Agriculture, University of Belgrade, 11080 Belgrade, Serbia.
Bee products are an important source of nutrients and bioactive phytochemicals. This study aimed to determine the chemical composition (proximate composition, general phytochemical composition, sugar, and phenolic profiles) of four different products (honey, bee pollen, bee bread, and propolis), obtained from the same apiary, as well as to assess their biological activity through antioxidant and enzyme inhibition assays (α-amylase, α-glucosidase, lipase, AchE, neuraminidase, angiotensin-converting enzyme, urease, trypsin, tyrosinase, carbonic anhydrase, thioredoxin reductase, adenosine deaminase). Clear differences were observed among the samples in terms of both chemical composition and biological activity.
View Article and Find Full Text PDFMediators Inflamm
January 2025
Biomedical Research Center, Slovak Academy of Sciences, Bratislava, Slovakia.
Spontaneous tumor regression is a recognized phenomenon across various cancer types. Recent research emphasizes the alterations in autoantibodies against carbonic anhydrase I (CA I) (anti-CA I) levels as potential prognostic markers for various malignancies. Particularly, autoantibodies targeting CA I and II appear to induce cellular damage by inhibiting their respective protein's catalytic functions.
View Article and Find Full Text PDFArch Pharm (Weinheim)
January 2025
Section of Pharmaceutical and Nutraceutical Sciences, Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), University of Florence, Sesto Fiorentino, Firenze, Italy.
2,2'-Thio-bis(4,6-dichlorophenol), namely bithionol, is a small molecule endowed with a multifaceted bioactivity. Its peculiar polychlorinated phenolic structure makes it a suitable candidate to explore its potentialities in establishing interaction patterns with enzymes of MedChem interest, such as the human carbonic anhydrase (hCA) metalloenzymes. Herein, bithionol was tested on a panel of specific hCAs through the stopped-flow technique, showing a promising micromolar inhibitory activity for the hCA II isoform.
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