Evaluation of Phytocannabinoid Bioavailability Rates Using the Caco-2 Cell Model

Kód výsledku v IS VaVaI

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Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Evaluation of Phytocannabinoid Bioavailability Rates Using the Caco-2 Cell Model

Popis výsledku v původním jazyce

Phytocannabinoids are biologically active secondary metabolites occurring in Cannabis sativa L. plants. Due to their therapeutic potential, attention has focused mainly on delta9-tetrahydrocannabinol (Δ9- THC) and its non-psychotropic isomer cannabidiol (CBD)[1]. In the recent decade, research studies have reported a number of other cannabinoids that also have interesting biological activities, for example antibacterial, analgesic, anticonvulsant, or neuroprotective; the examples are cannabigerol (CBG), cannabinol (CBN), cannabichromene (CBC) or cannabidivarin (CBDV)[2-4]. Cannabinoid acids (precursors of neutral phytocannabinoids) and other biologically active substances found in cannabis may also have these properties, but sufficient scientific information is not available. In addition to the effectiveness of individual substances, a synergistic effect was also observed[5]. In the current project, we have been investigating the anti-inflammatory effect of phytocannabinoids in the context of the potential to treat/prevent atherosclerosis. For this purpose, the in vitro bioavailability including possible biotransformation of phytocannabinoids (CBD, CBC, CBG, CBN, CBDV, and relevant acids) using a model system with Caco-2 cells (human colon adenocarcinoma cells) was investigated. Cells were exposed either to phytocannabinoids or their mixture with some other non-cannabinoid components of cannabis extract obtained by preparative high-performance chromatography. To study the transfer of analytes, a Boyden chamber containing tissue culture medium Ham&apos;s Nutrient Mixture F12 and a monolayer of Caco-2 cells on a semipermeable membrane was used. After 24 hours of incubation, individual layers (apical medium, basolateral medium, and cells) were subjected to Analysis by ultra-performance liquid chromatography coupled with tandem mass spectrometry was used for both parent phytocannabinoids and potential metabolites. Relatively significant differences between simulated bioavailability neutral phytocannabinoids and relevant phytocannabinoid acids were observed indicating that the polarity of respective compounds plays an important role. After 24 hours of incubation, neutral substances were retained to a greater extent in Caco-2 cells, and part of them was transferred to the basolateral medium. In contrast, phytocannabinoid acids were less retained by cells and reached the basolateral part. This trend was observed regardless of whether cannabinoids were applied alone or in combination with cannabis extract. Any metabolites of phytocannabinoids were not detected.

Název v anglickém jazyce

Evaluation of Phytocannabinoid Bioavailability Rates Using the Caco-2 Cell Model

Popis výsledku anglicky

Phytocannabinoids are biologically active secondary metabolites occurring in Cannabis sativa L. plants. Due to their therapeutic potential, attention has focused mainly on delta9-tetrahydrocannabinol (Δ9- THC) and its non-psychotropic isomer cannabidiol (CBD)[1]. In the recent decade, research studies have reported a number of other cannabinoids that also have interesting biological activities, for example antibacterial, analgesic, anticonvulsant, or neuroprotective; the examples are cannabigerol (CBG), cannabinol (CBN), cannabichromene (CBC) or cannabidivarin (CBDV)[2-4]. Cannabinoid acids (precursors of neutral phytocannabinoids) and other biologically active substances found in cannabis may also have these properties, but sufficient scientific information is not available. In addition to the effectiveness of individual substances, a synergistic effect was also observed[5]. In the current project, we have been investigating the anti-inflammatory effect of phytocannabinoids in the context of the potential to treat/prevent atherosclerosis. For this purpose, the in vitro bioavailability including possible biotransformation of phytocannabinoids (CBD, CBC, CBG, CBN, CBDV, and relevant acids) using a model system with Caco-2 cells (human colon adenocarcinoma cells) was investigated. Cells were exposed either to phytocannabinoids or their mixture with some other non-cannabinoid components of cannabis extract obtained by preparative high-performance chromatography. To study the transfer of analytes, a Boyden chamber containing tissue culture medium Ham&apos;s Nutrient Mixture F12 and a monolayer of Caco-2 cells on a semipermeable membrane was used. After 24 hours of incubation, individual layers (apical medium, basolateral medium, and cells) were subjected to Analysis by ultra-performance liquid chromatography coupled with tandem mass spectrometry was used for both parent phytocannabinoids and potential metabolites. Relatively significant differences between simulated bioavailability neutral phytocannabinoids and relevant phytocannabinoid acids were observed indicating that the polarity of respective compounds plays an important role. After 24 hours of incubation, neutral substances were retained to a greater extent in Caco-2 cells, and part of them was transferred to the basolateral medium. In contrast, phytocannabinoid acids were less retained by cells and reached the basolateral part. This trend was observed regardless of whether cannabinoids were applied alone or in combination with cannabis extract. Any metabolites of phytocannabinoids were not detected.

Druh

O - Ostatní výsledky

CEP obor

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OECD FORD obor

10608 - Biochemistry and molecular biology

Projekt

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Návaznosti

S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2023

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů