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A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (31 May 2020) | Viewed by 41952

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Prof. Dr. Raffaele Capasso

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Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy
Interests: pharmacology; natural products; neurotransmission; behavioral pharmacology; experimental pharmacology; preclinical pharmacology; CB1 receptor; PPARs; cannabinoids; endocannabinoids; CB2 receptor
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Special Issue Information

Dear Colleagues,

Interest in the use of cannabinoids in medicine has increased in recent years, as the many advances in basic science and clinical achievements using cannabis or cannabinoids have shown excellent results. Cannabinoids are the general term used to indicate: (i) Compounds derived from cannabis (i.e., fitocannabinoids); (ii) endocannabinoids, endogenous neurotransmitters, which act on the cannabinoid receptors and/or other actors of the endocannabinoid system; (iii) synthetic cannabinoids, structurally analogous to phytocannabinoids and/or endocannabinoids.

The activation of cannabinoid receptors determines many pharmacological actions with numerous beneficial therapeutic effects.

The purpose of this Special Issue is to publish original research papers and/or relevant updates of literature data, on the beneficial effects of cannabinoids and cannabinoid receptors in many pathologic conditions, sustaining the use of cannabinoids for medical purposes.

Prof. Dr. Raffaele Capasso
Guest Editor

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Keywords

Cannabinoids receptors
Cannabinoids
Cannabis sativa
Phytocannabinoids
Endocannabinoids
Medical cannabis

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Published Papers (6 papers)

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Research

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14 pages, 7857 KiB

Open AccessArticle

Capsaicin Causes Vasorelaxation of Rat Aorta through Blocking of L-type Ca²⁺ Channels and Activation of CB₁ Receptors

by Felipa Andrade, Cinthia Rangel-Sandoval, Alejandrina Rodríguez-Hernández, Evelyn López-Dyck, Alejandro Elizalde, Adolfo Virgen-Ortiz, Edgar Bonales-Alatorre, Georgina Valencia-Cruz and Enrique Sánchez-Pastor

Molecules 2020, 25(17), 3957; https://doi.org/10.3390/molecules25173957 - 30 Aug 2020

Cited by 12 | Viewed by 3367

Abstract

The aim of this work was to determine whether Capsaicin may exert a vascular regulation through the activation of CB₁ and/or CB₂ receptors causing vasorelaxation in the rat aorta. Our results show the location of TRPV1 mainly in the endothelial and smooth muscle cells membrane. Nevertheless, Capsaicin caused vasorelaxation of this artery through a mechanism independent of TRPV1, since the specific antagonists Capsazepine and SB-366791 did not block the effect of Capsaicin. Because the significant expression of CB₁ and CB₂ receptors has been previously reported in the rat aorta, we used antagonists for these two receptors prior to the addition of Capsaicin. In these experiments, we found that the inhibition of CB₁ using AM281, decreases the vasorelaxant effect caused by Capsaicin. On the other hand, the vasorelaxant effect is not altered in the presence of the CB₂ receptor antagonist AM630. Furthermore, a partial decrease of the effect of Capsaicin was also seen when L-type calcium channels are blocked. A complete block of Capsaicin-induced vasorelaxation was achieved using a combination of Verapamil and AM281. In accordance to our results, Capsaicin-induced vasorelaxation of the rat aorta is neither dependent of TRPV1 or CB₂ receptors, but rather it is strongly suggested that a tandem mechanism between inactivation of L-type calcium channels and the direct activation of CB₁ receptors is involved. These findings are supported by CB₁ docking simulation which predicted a binding site on CB₁ receptors for Capsaicin. Full article

(This article belongs to the Special Issue Research on the Cannabinoid Receptors Pharmacology)

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16 pages, 2243 KiB

Open AccessFeature PaperArticle

Exacerbated LPS/GalN-Induced Liver Injury in the Stress-Sensitive Wistar Kyoto Rat Is Associated with Changes in the Endocannabinoid System

by Marykate Killilea, Daniel M. Kerr, Beth M. Mallard, Michelle Roche and Antony M. Wheatley

Molecules 2020, 25(17), 3834; https://doi.org/10.3390/molecules25173834 - 23 Aug 2020

Cited by 3 | Viewed by 3161

Abstract

Acute liver injury (ALI) is a highly destructive and potentially life-threatening condition, exacerbated by physical and psychological stress. The endocannabinoid system plays a key role in modulating stress and hepatic function. The aim of this study was to examine the development of acute liver injury in the genetically susceptible stress-sensitive Wistar-Kyoto (WKY) rat compared with normo-stress-sensitive Sprague Dawley (SD) rats, and associated changes in the endocannabinoid system. Administration of the hepatotoxin lipopolysaccharide/D-Galactosamine (LPS/GalN) resulted in marked liver injury in WKY, but not SD rats, with increased alanine aminotransferase (ALT), aspartate aminotransferase (AST) and glutamate dehydrogenase (GLDH) plasma levels, significant histopathological changes, increased hepatic pro-inflammatory cytokine expression and caspase-3 activity and expression and reduced Glutathione (GSH) activity. Furthermore, compared to SD controls, WKY rats display increased anandamide and 2-Arachidonoylglycerol levels concurrent with decreased expression of their metabolic enzymes and a decrease in cannabinoid (CB)₁ receptor expression following LPS/GalN. CB₁ antagonism with AM6545 or CB₂ agonism with JWH133 did not alter LPS/GalN-induced liver injury in SD or WKY rats. These findings demonstrate exacerbation of acute liver injury induced by LPS/GalN in a stress-sensitive rat strain, with effects associated with alterations in the hepatic endocannabinoid system. Further studies are required to determine if the endocannabinoid system mediates or modulates the exacerbation of liver injury in this stress-sensitive rat strain. Full article

(This article belongs to the Special Issue Research on the Cannabinoid Receptors Pharmacology)

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20 pages, 478 KiB

Open AccessArticle

A Novel Alternative in the Treatment of Detrusor Overactivity? In Vivo Activity of O-1602, the Newly Synthesized Agonist of GPR55 and GPR18 Cannabinoid Receptors

by Andrzej Wróbel, Aleksandra Szopa, Anna Serefko and Ewa Poleszak

Molecules 2020, 25(6), 1384; https://doi.org/10.3390/molecules25061384 - 18 Mar 2020

Cited by 15 | Viewed by 3753

Abstract

The aim of the research was to assess the impact of O-1602—novel GPR55 and GPR18 agonist—in the rat model of detrusor overactivity (DO). Additionally, its effect on the level of specific biomarkers was examined. To stimulate DO, 0.75% retinyl acetate (RA) was administered to female rats’ bladders. O-1602, at a single dose of 0.25 mg/kg, was injected intra-arterially during conscious cystometry. Furthermore, heart rate, blood pressure, and urine production were monitored for 24 h, and the impact of O-1602 on the levels of specific biomarkers was evaluated. An exposure of the urothelium to RA changed cystometric parameters and enhanced the biomarker levels. O-1602 did not affect any of the examined cystometric parameters or levels of biomarkers in control rats. However, the O-1602 injection into animals with RA-induced DO ameliorated the symptoms of DO and caused a reversal in the described changes in the concentration of CGRP, OCT₃, BDNF, and NGF to the levels observed in the control, while the values of ERK1/2 and VAChT were significantly lowered compared with the RA-induced DO group, but were still statistically higher than in the control. O-1602 can improve DO, and may serve as a promising novel substance for the pharmacotherapy of bladder diseases. Full article

(This article belongs to the Special Issue Research on the Cannabinoid Receptors Pharmacology)

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24 pages, 3438 KiB

Open AccessArticle

CB1 Receptor-Dependent and Independent Induction of Lipolysis in Primary Rat Adipocytes by the Inverse Agonist Rimonabant (SR141716A)

by Günter A. Müller, Andreas W. Herling, Susanne Wied and Timo D. Müller

Molecules 2020, 25(4), 896; https://doi.org/10.3390/molecules25040896 - 18 Feb 2020

Cited by 7 | Viewed by 3511

Abstract

(1) Background: Acute administration of the cannabinoid receptor 1 (CB1R) inverse agonist Rimonabant (SR141716A) to fed Wistar rats was shown to elicit a rapid and short-lasting elevation of serum free fatty acids. (2) Methods: The effect of Rimonabant on lipolysis in isolated primary rat adipocytes was studied to raise the possibility for direct mechanisms not involving the (hypothalamic) CB1R. (3) Results: Incubation of these cells with Rimonabant-stimulated lipolysis to up to 25% of the maximal isoproterenol effect, which was based on both CB1R-dependent and independent mechanisms. The CB1R-dependent one was already effective at Rimonabant concentrations of less than 1 µM and after short-term incubation, partially additive to β-adrenergic agonists and blocked by insulin and, in part, by adenosine deaminase, but not by propranolol. It was accompanied by protein kinase A (PKA)-mediated association of hormone-sensitive lipase (HSL) with lipid droplets (LD) and dissociation of perilipin-1 from LD. The CB1R-independent stimulation of lipolysis was observed only at Rimonabant concentrations above 1 µM and after long-term incubation and was not affected by insulin. It was recapitulated by a cell-free system reconstituted with rat adipocyte LD and HSL. Rimonabant-induced cell-free lipolysis was not affected by PKA-mediated phosphorylation of LD and HSL, but abrogated by phospholipase digestion or emulsification of the LD. Furthermore, LD isolated from adipocytes and then treated with Rimonabant (>1 µM) were more efficient substrates for exogenously added HSL compared to control LD. The CB1R-independent lipolysis was also demonstrated in primary adipocytes from fed rats which had been treated with a single dose of Rimonabant (30 mg/kg). (4) Conclusions: These data argue for interaction of Rimonabant (at high concentrations) with both the LD surface and the CB1R of primary rat adipocytes, each leading to increased access of HSL to LD in phosphorylation-independent and dependent fashion, respectively. Both mechanisms may lead to direct and acute stimulation of lipolysis at peripheral tissues upon Rimonabant administration and represent targets for future obesity therapy which do not encompass the hypothalamic CB1R. Full article

(This article belongs to the Special Issue Research on the Cannabinoid Receptors Pharmacology)

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Review

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47 pages, 1625 KiB

Open AccessReview

Terpenoids, Cannabimimetic Ligands, beyond the Cannabis Plant

by Elaine C. D. Gonçalves, Gabriela M. Baldasso, Maíra A. Bicca, Rodrigo S. Paes, Raffaele Capasso and Rafael C. Dutra

Molecules 2020, 25(7), 1567; https://doi.org/10.3390/molecules25071567 - 29 Mar 2020

Cited by 74 | Viewed by 21143

Abstract

Medicinal use of Cannabis sativa L. has an extensive history and it was essential in the discovery of phytocannabinoids, including the Cannabis major psychoactive compound—Δ9-tetrahydrocannabinol (Δ9-THC)—as well as the G-protein-coupled cannabinoid receptors (CBR), named cannabinoid receptor type-1 (CB1R) and cannabinoid receptor type-2 (CB2R), both part of the now known endocannabinoid system (ECS). Cannabinoids is a vast term that defines several compounds that have been characterized in three categories: (i) endogenous, (ii) synthetic, and (iii) phytocannabinoids, and are able to modulate the CBR and ECS. Particularly, phytocannabinoids are natural terpenoids or phenolic compounds derived from Cannabis sativa. However, these terpenoids and phenolic compounds can also be derived from other plants (non-cannabinoids) and still induce cannabinoid-like properties. Cannabimimetic ligands, beyond the Cannabis plant, can act as CBR agonists or antagonists, or ECS enzyme inhibitors, besides being able of playing a role in immune-mediated inflammatory and infectious diseases, neuroinflammatory, neurological, and neurodegenerative diseases, as well as in cancer, and autoimmunity by itself. In this review, we summarize and critically highlight past, present, and future progress on the understanding of the role of cannabinoid-like molecules, mainly terpenes, as prospective therapeutics for different pathological conditions. Full article

(This article belongs to the Special Issue Research on the Cannabinoid Receptors Pharmacology)

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16 pages, 820 KiB

Open AccessReview

Endocannabinoid System in the Airways

by Turgut Emrah Bozkurt

Molecules 2019, 24(24), 4626; https://doi.org/10.3390/molecules24244626 - 17 Dec 2019

Cited by 28 | Viewed by 5599

Abstract

Cannabinoids and the mammalian endocannabinoid system is an important research area of interest and attracted many researchers because of their widespread biological effects. The significant immune-modulatory role of cannabinoids has suggested their therapeutic use in several inflammatory conditions. Airways are prone to environmental irritants and stimulants, and increased inflammation is an important process in most of the respiratory diseases. Therefore, the main strategies for treating airway diseases are suppression of inflammation and producing bronchodilation. The ability of cannabinoids to induce bronchodilation and modify inflammation indicates their importance for airway physiology and pathologies. In this review, the contribution of cannabinoids and the endocannabinoid system in the airways are discussed, and the existing data for their therapeutic use in airway diseases are presented. Full article

(This article belongs to the Special Issue Research on the Cannabinoid Receptors Pharmacology)

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