<i>In Vitro</i> Biological Target Screening and Colloidal Aggregation of Minor Cannabinoids

There is limited information on interactions between cannabinoids and many pharmacologically and toxicologically relevant targets in humans (e.g., receptors, ion channels, enzymes, and transporters). To address this data gap, seven cannabinoids were screened against a panel of 44 safety-related biological targets in competitive ligand binding or enzymatic activity assays. Diverse binding profiles were observed among the cannabinoids; however, colloidal aggregates were detected by dynamic light scattering and a detergent-sensitive enzyme inhibition assay. These aggregates may nonspecifically inhibit targets, yielding false positives. Although screening identified aggregates, additional testing is required to confirm cannabinoid aggregation in individual <i>in vitro</i> assays.

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Publication Details

Journal
Journal of Natural Products
Published
2024-11-20
DOI
https://doi.org/10.1021/acs.jnatprod.4c00608
Citations
2
Primary Topic
Cannabis and Cannabinoid Research
Type
article
Field-Weighted Citation Impact
0.90

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article

In Vitro Biological Target Screening and Colloidal Aggregation of Minor Cannabinoids

Michael F. Santillo, Isabella Glenn, Lu Paris, Robert L. Sprando
2 citations
Journal of Natural Products
Cannabis and Cannabinoid Research
0.90
article

In Vitro Biological Target Screening and Colloidal Aggregation of Minor Cannabinoids

Michael F. Santillo, Isabella Glenn, Lu Paris, Robert L. Sprando
article en
2 citations

Abstract

There is limited information on interactions between cannabinoids and many pharmacologically and toxicologically relevant targets in humans (e.g., receptors, ion channels, enzymes, and transporters). To address this data gap, seven cannabinoids were screened against a panel of 44 safety-related biological targets in competitive ligand binding or enzymatic activity assays. Diverse binding profiles were observed among the cannabinoids; however, colloidal aggregates were detected by dynamic light scattering and a detergent-sensitive enzyme inhibition assay. These aggregates may nonspecifically inhibit targets, yielding false positives. Although screening identified aggregates, additional testing is required to confirm cannabinoid aggregation in individual <i>in vitro</i> assays.

Journal of Natural ProductsVol. 87(12)
Center for Food Safety and Applied Nutrition (US), United States Food and Drug Administration (US), University of California, San Francisco (US)
National Institute of General Medical Sciences
Zero hunger
Openalex Percentile: Top 23%
Cannabis and Cannabinoid Research
0.90
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