Multiomic Analysis Reveals Disruption of Cholesterol Homeostasis by Cannabidiol in Human Cell Lines

Guard, Steven; Chapnick, Douglas A.; Poss, Zachary C.; Ebmeier, Christopher C.; Jacobsen, Jeremy; Nemkov, Travis; Ball, Kerri A.; Webb, Kristofor; Simpson, Helen; Coleman, S. J.; Bunker, Eric; Ramirez, Adrian; Reisz, Julie A.; Sievers, Robert E.; Stowell, Michael H. B.; D’Alessandro, Angelo; Liu, Xuedong; Old, William M.

doi:10.1016/j.mcpro.2022.100262

Cited by 14 publications

(18 citation statements)

References 116 publications

(168 reference statements)

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“…Importantly, CBD is an inhibitor of voltage-dependent sodium (Nav) channels (Ghovanloo et al, 2018;Ghovanloo and Ruben, 2021;Zhang and Bean, 2021), some potassium channels (e.g., Kv2.1) (Ghovanloo et al, 2018;Orvos et al, 2020), calcium channels (Ross et al, 2008) and, in contrast, an activator of Kv7 channels in the nanomolar range (Zhang et al, 2022). Additionally, CBD directly modulates the biophysical properties of the bio-membrane itself Ghovanloo et al, 2022b;Guard et al, 2022), which may facilitate an allosteric modulation of membrane proteins including, but not limited to, those noted above.…”

Section: Introductionmentioning

confidence: 99%

Non-psychotropic phytocannabinoid interactions with voltage-gated sodium channels: An update on cannabidiol and cannabigerol

et al. 2022

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Phytocannabinoids, found in the plant, Cannabis sativa, are an important class of natural compounds with physiological effects. These compounds can be generally divided into two classes: psychoactive and non-psychoactive. Those which do not impart psychoactivity are assumed to predominantly function via endocannabinoid receptor (CB) -independent pathways and molecular targets, including other receptors and ion channels. Among these targets, the voltage-gated sodium (Nav) channels are particularly interesting due to their well-established role in electrical signalling in the nervous system. The interactions between the main non-psychoactive phytocannabinoid, cannabidiol (CBD), and Nav channels were studied in detail. In addition to CBD, cannabigerol (CBG), is another non-psychoactive molecule implicated as a potential therapeutic for several conditions, including pain via interactions with Nav channels. In this mini review, we provide an update on the interactions of Nav channels with CBD and CBG.

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Section: Introductionmentioning

confidence: 99%

Non-psychotropic phytocannabinoid interactions with voltage-gated sodium channels: An update on cannabidiol and cannabigerol

et al. 2022

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“…It is known that CBD decrease the amount of fatty acids (FA), from which during esterification the cholesteryl esters are synthesized, therefore it is possible that for 3 µM CBD the FA are less accessible therefor lower amount of cholesteryl esters is present. 61 Combining CBD with irradiation firstly, the decrease in cholesteryl esters for the 0.1 µM CBD dose is observed, than increase in this molecules to the level present for untreated cells from 0.5 µM till 9µM of CBD concentration. This distinct behavior of cholesteryl esters under the influence of CBD and X-rays suggests different pathways of cholesteryl esters metabolism.…”

Section: Resultsmentioning

confidence: 96%

High resolution optical spectroscopy for the evaluation of cannabidiol efficiency as a radiation therapy support of peripheral nervous system tumors

Chrabąszcz,

Pogoda,

Cieżak

et al. 2023

Preprint

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An increasing number of scientific papers discuss the promising therapeutic potential of cannabidiol (CBD) not only for the treatment of cancer, but also for asthma and neurodegenerative disorders. This happens mainly due to its proven anticancer, anti-inflammatory, and antioxidant properties. In the field of cancer research, the use of CBD has already been investigated on malignant tumors of the central nervous system, like gliomas. So far, CBD has not yet been explored in the therapy of peripheral nervous system (PNS) tumors. Peripheral nerves reside outside the central nervous system, therefore peripheral nerve tumors can occur anywhere in the body. When the tumor develops within large blood vessels, spinal nerves or involves more than one peripheral nerve, radiotherapy is recommended. Due to high doses of ionizing radiation, complications such as dizziness, damage to adjacent nerves, or malignancy of the lesion may occur. Therefore, it is important to develop a treatment scheme that efficiently reduces tumor volume while maintaining the normal functions of the surrounding cells and decrease the side effects. Herein, we proposed to combine hyperspectral imaging using Raman and FTIR spectroscopy and AFM-IR technique as a novel approach to monitor the therapeutic efficacy of CBD. Performed studies reviled the dual effect of CBD, that protects normal cells from ionizing radiation and increases its toxicity in cancer cells.

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“…CBD, AEA, and PEA have all been recognized as activators of AMPK. [34][35][36] The activation of AMPK in the colitis colon induced by DSS may be due to the increased cAMP and Ca 2+ levels. AMPK is activated in response to elevated cellular Ca 2+ levels, which involves phosphorylation at Thr172 by Ca 2+ /calmodulin-dependent protein kinase kinase 𝛽 (CaMKK𝛽) [34,37] .…”

Section: Discussionmentioning

confidence: 99%

“…[34][35][36] The activation of AMPK in the colitis colon induced by DSS may be due to the increased cAMP and Ca 2+ levels. AMPK is activated in response to elevated cellular Ca 2+ levels, which involves phosphorylation at Thr172 by Ca 2+ /calmodulin-dependent protein kinase kinase 𝛽 (CaMKK𝛽) [34,37] . Intracellular cAMP interacts with Epac1, leading to increased intracellular Ca 2+ levels and the activation of the CaMKK𝛽-AMPK pathway.…”

Section: Discussionmentioning

confidence: 99%

Dietary Cannabidiol Activates PKA/AMPK Signaling and Attenuates Chronic Inflammation and Leaky Gut in DSS‐Induced Colitis Mice

Sun,

Bravo Iniguez,

Tian

et al. 2024

Molecular Nutrition Food Res

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ScopeInflammatory bowel disease (IBD) is characterized by chronic inflammation in the gut, accompanied by impaired epithelial integrity, increased macrophage infiltration, and enhanced colon cancer risk.Methods and ResultsCannabidiol (CBD), a phytocannabinoid isolated from cannabis plants, is supplemented into mice diet, and its beneficial effects against dextran sulfate sodium (DSS)‐induced experimental colitis is evaluated. Eight‐week‐old mice were fed a standard diet supplemented with or without CBD (200 mg kg‐1) for 5 weeks. In the 4th week of dietary treatment, mice were subjected to 2.5% DSS induction for 7 days, followed by 7 days of recovery, to induce colitis. CBD supplementation reduced body weight loss, gross bleeding, fecal consistency, and disease activity index. In addition, CBD supplementation protected the colonic structure, promoted tissue recovery, and ameliorated macrophage infiltration in the colonic tissue, which was associated with the activation of cyclic AMP‐protein kinase A, extracellular signal‐regulated kinase ½, and AMP‐activated protein kinase signaling pathways. CBD supplementation also suppressed NLRP3 inflammasome activation and related pro‐inflammatory marker secretion. Consistently, CBD feeding reduced tight junction protein claudin2 and myosin light chain kinase in DSS‐treated mice.ConclusionDietary CBD protects against inflammation and colitis symptoms induced by DSS, providing an alternative approach to IBD management.

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Multiomic Analysis Reveals Disruption of Cholesterol Homeostasis by Cannabidiol in Human Cell Lines

Cited by 14 publications

References 116 publications

Non-psychotropic phytocannabinoid interactions with voltage-gated sodium channels: An update on cannabidiol and cannabigerol

Non-psychotropic phytocannabinoid interactions with voltage-gated sodium channels: An update on cannabidiol and cannabigerol

High resolution optical spectroscopy for the evaluation of cannabidiol efficiency as a radiation therapy support of peripheral nervous system tumors

Dietary Cannabidiol Activates PKA/AMPK Signaling and Attenuates Chronic Inflammation and Leaky Gut in DSS‐Induced Colitis Mice

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