Cannabis, Cannabinoids and Its Derivatives

Topic Information

Dear Colleagues,

Following the legalization of Cannabis sativa for medicinal use in many countries, modulation of the endocannabinoid system has been the subject of intense research interest. Despite being used since ancient times in traditional Asian medicine, its use in modern pharmacology has only become more commonplace in the last few years. Research into cannabis, cannabinoids, and their derivatives first began in 1964, when Gaoni and Mechoulam identified delta9-tetrahydocannabinol, the main psychoactive ingredient in cannabis. In the 1990s, the cannabinoid type 1 (CB1) receptor was cloned in both rats and humans, followed shortly after by a second cannabinoid receptor (CB2). Endogenous cannabinoid receptor agonists (i.e., anandamide and 2-arachidonoyl glycerol) along with receptors and enzymes for the biosynthesis and degradation of endocannabinoids were then identified, and the endogenous cannabinoid signaling system was termed the “endocannabinoid system”. Since the discovery of endocannabinoids, many synthetic agonists and antagonists, as well as naturally occurring “phytocannabinoids” that target the endocannabinoid system, have been investigated and found to exhibit therapeutic potential in preclinical and clinical studies. This Topic will review and present novel scientific and clinical results regarding the potential therapeutic use of cannabis, cannabinoids, and their derivatives.

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Participating Journals

Journal Name	Impact Factor	CiteScore	Launched Year	First Decision (median)	APC
Biomedicines biomedicines	4.7	3.7	2013	15.4 Days	CHF 2600	Submit
Journal of Clinical Medicine jcm	3.9	5.4	2012	17.9 Days	CHF 2600	Submit
Molecules molecules	4.6	6.7	1996	14.6 Days	CHF 2700	Submit
Pharmaceutics pharmaceutics	5.4	6.9	2009	14.2 Days	CHF 2900	Submit
Scientia Pharmaceutica scipharm	2.5	6.4	1930	22.7 Days	CHF 1000	Submit
International Journal of Molecular Sciences ijms	5.6	7.8	2000	16.3 Days	CHF 2900	Submit

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Published Papers (6 papers)

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All Biomedicines JCM Molecules Pharmaceutics Sci. Pharm. IJMS

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23 pages, 2590 KiB  

Open AccessReview

Possible Role of Cannabis in the Management of Neuroinflammation in Patients with Post-COVID Condition

by Noemi Cárdenas-Rodríguez, Iván Ignacio-Mejía, Jose Correa-Basurto, Humberto Carrasco-Vargas, Marco Antonio Vargas-Hernández, Exal Manuel Albores-Méndez, Rodolfo David Mayen-Quinto, Reynita De La Paz-Valente and Cindy Bandala

Int. J. Mol. Sci. 2024, 25(7), 3805; https://doi.org/10.3390/ijms25073805 - 29 Mar 2024

Viewed by 2446

Abstract

The post-COVID condition (PCC) is a pathology stemming from COVID-19, and studying its pathophysiology, diagnosis, and treatment is crucial. Neuroinflammation causes the most common manifestations of this disease including headaches, fatigue, insomnia, depression, anxiety, among others. Currently, there are no specific management proposals; [...] Read more.

The post-COVID condition (PCC) is a pathology stemming from COVID-19, and studying its pathophysiology, diagnosis, and treatment is crucial. Neuroinflammation causes the most common manifestations of this disease including headaches, fatigue, insomnia, depression, anxiety, among others. Currently, there are no specific management proposals; however, given that the inflammatory component involves cytokines and free radicals, these conditions must be treated to reduce the current symptoms and provide neuroprotection to reduce the risk of a long-term neurodegenerative disease. It has been shown that cannabis has compounds with immunomodulatory and antioxidant functions in other pathologies. Therefore, exploring this approach could provide a viable therapeutic option for PCC, which is the purpose of this review. This review involved an exhaustive search in specialized databases including PubMed, PubChem, ProQuest, EBSCO, Scopus, Science Direct, Web of Science, and Clinical Trials. Phytocannabinoids, including cannabidiol (CBD), cannabigerol (CBG), and Delta-9-tetrahydrocannabinol (THC), exhibit significant antioxidative and anti-inflammatory properties and have been shown to be an effective treatment for neuroinflammatory conditions. These compounds could be promising adjuvants for PCC alone or in combination with other antioxidants or therapies. PCC presents significant challenges to neurological health, and neuroinflammation and oxidative stress play central roles in its pathogenesis. Antioxidant therapy and cannabinoid-based approaches represent promising areas of research and treatment for mitigating adverse effects, but further studies are needed. Full article

(This article belongs to the Topic Cannabis, Cannabinoids and Its Derivatives)

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18 pages, 1210 KiB  

Open AccessReview

Cannabinoids and the Endocannabinoid System in Early SARS-CoV-2 Infection and Long COVID-19—A Scoping Review

by Cassidy Scott, Stefan Hall, Juan Zhou and Christian Lehmann

J. Clin. Med. 2024, 13(1), 227; https://doi.org/10.3390/jcm13010227 - 30 Dec 2023

Viewed by 12783

Abstract

Coronavirus disease-19 (COVID-19) is a highly contagious illness caused by the SARS-CoV-2 virus. The clinical presentation of COVID-19 is variable, often including symptoms such as fever, cough, headache, fatigue, and an altered sense of smell and taste. Recently, post-acute “long” COVID-19 has emerged [...] Read more.

Coronavirus disease-19 (COVID-19) is a highly contagious illness caused by the SARS-CoV-2 virus. The clinical presentation of COVID-19 is variable, often including symptoms such as fever, cough, headache, fatigue, and an altered sense of smell and taste. Recently, post-acute “long” COVID-19 has emerged as a concern, with symptoms persisting beyond the acute infection. Vaccinations remain one of the most effective preventative methods against severe COVID-19 outcomes and the development of long-term COVID-19. However, individuals with underlying health conditions may not mount an adequate protective response to COVID-19 vaccines, increasing the likelihood of severe symptoms, hospitalization, and the development of long-term COVID-19 in high-risk populations. This review explores the potential therapeutic role of cannabinoids in limiting the susceptibility and severity of infection, both pre- and post-SARS-CoV-19 infection. Early in the SARS-CoV-19 infection, cannabinoids have been shown to prevent viral entry, mitigate oxidative stress, and alleviate the associated cytokine storm. Post-SARS-CoV-2 infection, cannabinoids have shown promise in treating symptoms associated with post-acute long COVID-19, including depression, anxiety, post-traumatic stress injury, insomnia, pain, and decreased appetite. While current research primarily focuses on potential treatments for the acute phase of COVID-19, there is a gap in research addressing therapeutics for the early and post-infectious phases. This review highlights the potential for future research to bridge this gap by investigating cannabinoids and the endocannabinoid system as a potential treatment strategy for both early and post-SARS-CoV-19 infection. Full article

(This article belongs to the Topic Cannabis, Cannabinoids and Its Derivatives)

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14 pages, 2183 KiB  

Open AccessArticle

A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery

by Gemma Navarro, Eddy Sotelo, Iu Raïch, María Isabel Loza, Jose Brea and Maria Majellaro

Molecules 2023, 28(24), 8107; https://doi.org/10.3390/molecules28248107 - 15 Dec 2023

Viewed by 835

Abstract

The identification of new modulators for Cannabinoid Receptors (CBRs) has garnered significant attention in drug discovery over recent years, owing to their manifold pathophysiological implications. In the context of hit identification, the availability of robust and sensitive high-throughput screening assays is essential to [...] Read more.

The identification of new modulators for Cannabinoid Receptors (CBRs) has garnered significant attention in drug discovery over recent years, owing to their manifold pathophysiological implications. In the context of hit identification, the availability of robust and sensitive high-throughput screening assays is essential to enhance the likelihood of success. In this study, we present the development and validation of a Tag-lite^® binding assay designed for screening hCB₁/hCB₂ binding, employing a dual fluorescent ligand, CELT-335. Representative ligands for CBRs, exhibiting diverse affinity and functional profiles, were utilized as reference compounds to validate the robustness and efficiency of the newly developed Tag-lite^® binding assay protocol. The homogeneous format, coupled with the sensitivity and optimal performance of the fluorescent ligand CELT-335, establishes this assay as a viable and reliable method for screening in hit and lead identification campaigns. Full article

(This article belongs to the Topic Cannabis, Cannabinoids and Its Derivatives)

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19 pages, 957 KiB  

Open AccessReview

The Use of Cannabidiol in Metabolic Syndrome—An Opportunity to Improve the Patient’s Health or Much Ado about Nothing?

by Michał Wiciński, Anna Fajkiel-Madajczyk, Zuzanna Kurant, Karol Gryczka, Dominik Kurant, Monika Szambelan, Bartosz Malinowski, Michal Falkowski, Jan Zabrzyński and Maciej Słupski

J. Clin. Med. 2023, 12(14), 4620; https://doi.org/10.3390/jcm12144620 - 11 Jul 2023

Cited by 1 | Viewed by 1615

Abstract

Cannabis-derived therapies are gaining popularity in the medical world. More and more perfect forms of cannabinoids are sought, which could be used in the treatment of many common diseases, including metabolic syndrome, whose occurrence is also increasing. The purpose of this review was [...] Read more.

Cannabis-derived therapies are gaining popularity in the medical world. More and more perfect forms of cannabinoids are sought, which could be used in the treatment of many common diseases, including metabolic syndrome, whose occurrence is also increasing. The purpose of this review was to investigate the usefulness of cannabinoids, mainly cannabidiol (CBD), in individuals with obesity, impaired glucose and lipid metabolism, high blood pressure, and non-alcoholic fatty liver disease (NAFLD). We summarised the most recent research on the broad topic of cannabis-derived influence on metabolic syndrome components. Since there is a lot of work on the effects of Δ9-THC (Δ9-tetrahydrocannabinol) on metabolism and far less on cannabidiol, we felt it needed to be sorted out and summarised in this review. The research results on the use of cannabidiol in obesity are contraindicatory. When it comes to glucose homeostasis, it appears that CBD maintains it, sensitises adipose tissue to insulin, and reduces fasting glucose levels, so it seems to be a potential target in this kind of metabolic disorder, but some research results are inconclusive. CBD shows some promising results in the treatment of various lipid disorders. Some studies have proven its positive effect by decreasing LDL and increasing HDL as well. Despite their probable efficacy, CBD and its derivatives will likely remain an adjunctive treatment rather than a mainstay of therapy. Studies have also shown that CBD in patients with hypertension has positive effects, even though the hypotensive properties of cannabidiol are small. However, CBD can be used to prevent blood pressure surges, stabilise them, and have a protective effect on blood vessels. Results from preclinical studies have shown that the effect of cannabidiol on NAFLD may be potentially beneficial in the treatment of the metabolic syndrome and its components. Nevertheless, there is limited data on CBD and NAFLD in human studies. Because of the numerous confounding factors, the conclusions are unclear, and more research in this field is required. Full article

(This article belongs to the Topic Cannabis, Cannabinoids and Its Derivatives)

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20 pages, 14945 KiB  

Open AccessArticle

The Antibacterial Effect of Cannabigerol toward Streptococcus mutans Is Influenced by the Autoinducers 21-CSP and AI-2

by Muna Aqawi, Ronit Vogt Sionov, Michael Friedman and Doron Steinberg

Biomedicines 2023, 11(3), 668; https://doi.org/10.3390/biomedicines11030668 - 22 Feb 2023

Cited by 5 | Viewed by 1624

Abstract

Bacteria can communicate through an intercellular signaling system referred to as quorum sensing (QS). The QS system involves the production of autoinducers that interact with their respective receptors, leading to the induction of specific signal transduction pathways. The QS systems of the oral [...] Read more.

Bacteria can communicate through an intercellular signaling system referred to as quorum sensing (QS). The QS system involves the production of autoinducers that interact with their respective receptors, leading to the induction of specific signal transduction pathways. The QS systems of the oral cariogenic Streptococcus mutans regulate the maturation of biofilms and affect its virulent properties. We have previously shown that the non-psychoactive compound cannabigerol (CBG) of the Cannabis sativa L. plant has anti-bacterial and anti-biofilm activities towards S. mutans. Here we were interested in investigating the effect of the two QS systems ComCDE and LuxS on the susceptibility of S. mutans to CBG and the anti-QS activities of CBG. This was assessed by using various comCDE and luxS mutant strains and complementation with the respective autoinducers, competence stimulating peptide (CSP) and (S)-4,5-dihydroxy-2,3-pentandione (DPD, pre-AI-2). We found that S. mutans comCDE knockout strains were more sensitive to the anti-bacterial actions of CBG compared to the WT strain. Exogenously added 21-CSP prevented the anti-bacterial actions caused by CBG on the ΔcomC, ΔcomE and ΔluxS mutants, while having no effect on the susceptibility of the WT and ΔcomCDE strains to CBG. Exogenously added DPD increased the susceptibility of WT and ΔluxS to CBG. Vice versa, CBG significantly reduced the 21-CSP-induced expression of comCDE genes and ComE-regulated genes and suppressed the expression of luxS with concomitant reduction in AI-2 production. DPD induced the expression of comCDE genes and ComE-regulated genes, and this induction was repressed by CBG. 21-CSP alone had no significant effect on luxS gene expression, while ΔcomCDE strains showed reduced AI-2 production. In conclusion, our study shows that the susceptibility of S. mutans to CBG is affected by the ComCDE and LuxS QS pathways, and CBG is a potential anti-QS compound for S. mutans. Additionally, we provide evidence for crosstalk between the ComCDE and LuxS QS systems. Full article

(This article belongs to the Topic Cannabis, Cannabinoids and Its Derivatives)

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28 pages, 1797 KiB  

Open AccessReview

Clinical Research Evidence Supporting Administration and Dosing Recommendations of Medicinal Cannabis as Analgesic in Cancer Patients

by Catalina Christensen, Morten Allesø, Martin Rose and Claus Cornett

J. Clin. Med. 2023, 12(1), 307; https://doi.org/10.3390/jcm12010307 - 30 Dec 2022

Cited by 3 | Viewed by 3938

Abstract

The analgesic potential of Cannabis sativa L.—based medicinal cannabis products for treatment of cancer associated chronic pains has gained increased interest in recent years. To ensure a controlled distribution of these products and investigate their therapeutic potential, several countries have established so-called pilot [...] Read more.

The analgesic potential of Cannabis sativa L.—based medicinal cannabis products for treatment of cancer associated chronic pains has gained increased interest in recent years. To ensure a controlled distribution of these products and investigate their therapeutic potential, several countries have established so-called pilot trials. Many doctors, however, are hesitant to prescribe medicinal cannabis primarily due to lack of research evidence regarding the products’ efficacy, safety and thus questionable dosing guidelines. This review aims to elucidate clinical research supporting administration of medicinal cannabis in cancer patients for analgesic purposes. The cannabinoids’ effects on the endocannabinoid system (ECS) and its implication in pain regulation is included to illustrate the complexity related to this research field. Published clinical studies on medicinal cannabis primarily consist of observational studies and only one pilot randomized controlled trial (RCT), where more RCTs exist on the cannabis-based product, Sativex^® (GW Pharma Ltd., Cambridge, UK). The studies indicate analgesic potential, however non-significantly, for most patients and with acceptable safety profile. Summarizing, high-quality RCTs are scarce in this research field, and the limitations of the observational studies complicates interpretation of clinical outcomes. Despite discrepancy among the studies, they do show indications for administration and dosing regimens providing analgesic effects for some cancer patients. Full article

(This article belongs to the Topic Cannabis, Cannabinoids and Its Derivatives)

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