Bioactive Chemical Composition of Cannabis Extracts and Cannabinoid Receptors

Abstract

Cannabis is widely used as a therapeutic drug, especially by patients suffering from psychiatric and neurodegenerative diseases. However, the complex interplay between phytocannabinoids and their targets in the human receptome remains largely a mystery, and there have been few investigations into the relationship between the chemical composition of medical cannabis and the corresponding biological activity. In this study, we investigated 59 cannabis samples used by patients for medical reasons. The samples were subjected to extraction (microwave and supercritical carbon dioxide) and chemical analyses, and the resulting extracts were assayed in vitro using the CB1 and CB2 receptors. Using a partial least squares regression analysis, the chemical compositions of the extracts were then correlated to their corresponding cannabinoid receptor activities, thus generating predictive models that describe the receptor potency as a function of major phytocannabinoid content. Using the current dataset, meaningful models for CB1 and CB2 receptor agonism were obtained, and these reveal the insignificant relationships between the major phytocannabinoid content and receptor affinity for CB1 but good correlations between the two at CB2 receptors. These results also explain the anomalies between the receptor activities of pure phytocannabinoids and cannabis extracts. Furthermore, the models for CB1 and CB2 agonism in cannabis extracts predict the cannabinoid receptor activities of individual phytocannabinoids with reasonable accuracy. Here for the first time, we disclose a method to predict the relationship between the chemical composition, including phytocannabinoids, of cannabis extracts and cannabinoid receptor responses.

Anti-Microbial Activity of Phytocannabinoids and Endocannabinoids in the Light of Their Physiological and Pathophysiological Roles

“…The Cannabis sativa L. plants produce more than 560 chemicals, including at least 144 cannabinoids and 200 terpenoids, as well as flavonoids and polyunsaturated fatty acids [15,33,34,42,63,67,72,73,[90][91][92][93][94][95][96][97][98][99][100][101][102][103][104][105][106][107]. The most common phytocannabinoids are ∆ 9 -tetrahy drocannabinol (∆ 9 -THC) and cannabidiol (CBD), which are the neutral homologs of tetrahydrocannabinolic acid (THCA) and cannabidiol acid (CBDA), respectively [108].…”

In silico genome-wide analysis of homeodomain-leucine zipper transcription factors in Cannabis sativa L

“…Medicinal cannabis contains a variety of natural plant products, and cannabinoids are the most important class of known compounds [ 33 ]. The process of cannabinoid metabolism and synthesis has been clarified, but the molecular regulation mechanism is unknown.…”

Produtos alimentícios à base de extrato de Cannabis: do “Brisadeiro” à busca por efeito terapêutico

“…A Cânabis, ou Cannabis, popularmente conhecida como maconha, é uma espécie de planta do gênero Cannabis, que produz mais de 568 compostos únicos, dos quais mais de 100 pertencem à classe dos fitocanabinóides (Figura 2). Estes são moléculas orgânicas com estrutura polifenólica, que exibem uma ampla gama de ações farmacodinâmicas nos receptores canabinoides humanos (Elsohly et al, 2017;Yang et al, 2020). Fonte: Elaborada pelos autores (Software ACD/ChemSketch) (2022).…”