In Vitro and Clinical Evaluation of Cannabigerol (CBG) Produced via Yeast Biosynthesis: A Cannabinoid with a Broad Range of Anti-Inflammatory and Skin Health-Boosting Properties.

Eduardo Perez,Corey Fitzgerald,Jose R Fernandez,Christopher Savile,Masanori Tamura,Karl Rouzard

doi:10.3390/molecules27020491

Eduardo Perez, Corey Fitzgerald + Show 4 more

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https://doi.org/10.3390/molecules27020491

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Abstract

Cannabigerol (CBG) is a minor non-psychoactive cannabinoid present in Cannabis sativa L. (C. sativa) at low levels (<1% per dry weight) that serves as the direct precursor to both cannabidiol (CBD) and tetrahydrocannabinol (THC). Consequently, efforts to extract and purify CBG from C. sativa is both challenging and expensive. However, utilizing a novel yeast fermentation technology platform, minor cannabinoids such as CBG can be produced in a more sustainable, cost-effective, and timely process as compared to plant-based production. While CBD has been studied extensively, demonstrating several beneficial skin properties, there are a paucity of studies characterizing the activity of CBG in human skin. Therefore, our aim was to characterize and compare the in vitro activity profile of non-psychoactive CBG and CBD in skin and be the first group to test CBG clinically on human skin. Gene microarray analysis conducted using 3D human skin equivalents demonstrates that CBG regulates more genes than CBD, including several key skin targets. Human dermal fibroblasts (HDFs) and normal human epidermal keratinocytes (NHEKs) were exposed in culture to pro-inflammatory inducers to trigger cytokine production and oxidative stress. Results demonstrate that CBG and CBD reduce reactive oxygen species levels in HDFs better than vitamin C. Moreover, CBG inhibits pro-inflammatory cytokine (Interleukin-1β, -6, -8, tumor necrosis factor α) release from several inflammatory inducers, such as ultraviolet A (UVA), ultraviolet B (UVB), chemical, C. acnes, and in several instances does so more potently than CBD. A 20-subject vehicle-controlled clinical study was performed with 0.1% CBG serum and placebo applied topically for 2 weeks after sodium lauryl sulfate (SLS)-induced irritation. CBG serum showed statistically significant improvement above placebo for transepidermal water loss (TEWL) and reduction in the appearance of redness. Altogether, CBG’s broad range of in vitro and clinical skin health-promoting activities demonstrates its strong potential as a safe, effective ingredient for topical use and suggests there are areas where it may be more effective than CBD.

Highlights

Licensee MDPI, Basel, Switzerland.The use of Cannabis sativa L. (C. sativa) for medicinal purposes such as ameliorating inflammation, pain, sleep, and neurological disorders dates back several thousands of years to its use in ancient China [1]
Results showed CBG was non-irritating in both models up to 3%, which was the highest dose tested (Figure S2)
We demonstrate for the first time that minor cannabinoid CBG, when applied topically, clinically promotes skin health by reducing the appearance of redness and improving barrier function better than a placebo

Summary

Introduction

Licensee MDPI, Basel, Switzerland.The use of Cannabis sativa L. (C. sativa) for medicinal purposes such as ameliorating inflammation, pain, sleep, and neurological disorders dates back several thousands of years to its use in ancient China [1]. The most well-known and studied of the cannabinoids is cannabidiol (CBD), which has been reported to possess antioxidant, anti-bacterial, antiacne, and anti-aging properties when studied in vitro and topically in vivo [3]. This in part has led to a recent surge of CBD use in cosmetics, where it has been marketed as an analgesic, anti-wrinkle, skin brightener, and moisturizer with claims to alleviate pruritus, psoriasis, acne, and eczema [4]. The second study was a single-arm phase I safety study in 20 healthy volunteers, where a patented 5%

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