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Pharmaceutical Drugs Based on Cannabis
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Pharmaceutical Drugs Based on Cannabis

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

Deadline for manuscript submissions: closed (15 June 2022) | Viewed by 23719

Special Issue Editors

Prof. Dr. Hinanit Koltai

E-Mail Website
Guest Editor
Institute of Plant Sciences, Agricultural Research Organization (ARO), Volcani Center, Rishon LeZion, Israel
Interests: medicinal plants; medical cannabis; anti-inflammatory activity; anti-cancer activity; neuronal activity
Special Issues, Collections and Topics in MDPI journals
Dr. Dvora Namdar

E-Mail Website
Guest Editor
Institute of Plant Sciences, Agricultural Research Organization (ARO), Volcani Center, Rishon LeZion, Israel
Interests: deep invistigation of chemical compositions of natural biomaterials; structural modification and creation of compounds; cannabis chemical studies and manipulation

Special Issue Information

Dear Colleagues,

Cannabis is being used by millions of patients worldwide, but despite this frequent use, the composition of cannabis-based products is usually not completely known, the active molecules and their optimal combination are insufficiently characterized and, moreover, the mode of action of the combined compositions is unstudied. To substantially improve cannabis medical use, molecular characterization of the content and active compositions should be conducted for each and every medical condition being treated by cannabis.

In this Special Issue of Molecules, we aim to highlight the need to specify cannabis use in terms of indication and active compounds. Studies detailing different aspects of cannabis medical use that are related to the activity of specific molecules and specific medical care are welcome. The collection of these articles may revolutionize the science behind cannabis-based medical care.

Prof. Hinanit Koltai
Dr. Dvora Namdar
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • cannabis
  • medical treatment
  • molecules
  • phytocannabinoids
  • terpenes
  • entourage effect
  • mode of action
  • gene expression
  • metabolomics study
  • statistical study

Published Papers (6 papers)

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Research

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20 pages, 2686 KiB  
Article
Role of Caryophyllane Sesquiterpenes in the Entourage Effect of Felina 32 Hemp Inflorescence Phytocomplex in Triple Negative MDA-MB-468 Breast Cancer Cells
by Silvia Di Giacomo, Alessia Mariano, Marco Gullì, Caterina Fraschetti, Annabella Vitalone, Antonello Filippi, Luisa Mannina, Anna Scotto d’Abusco and Antonella Di Sotto
Molecules 2021, 26(21), 6688; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26216688 - 05 Nov 2021
Cited by 16 | Viewed by 3691
Abstract
Cannabis sativa L. crops have been traditionally exploited as sources of fibers, nutrients, and bioactive phytochemicals of medical interest. In the present study, two terpene-rich organic extracts, namely FOJ and FOS, obtained from Felina 32 hemp inflorescences collected in June and September, respectively, [...] Read more.
Cannabis sativa L. crops have been traditionally exploited as sources of fibers, nutrients, and bioactive phytochemicals of medical interest. In the present study, two terpene-rich organic extracts, namely FOJ and FOS, obtained from Felina 32 hemp inflorescences collected in June and September, respectively, have been studied for their in vitro anticancer properties. Particularly, their cytotoxicity was evaluated in different cancer cell lines, and the possible entourage effect between nonintoxicating phytocannabinoids (cannabidiol and cannabichromene) and caryophyllane sesquiterpenes (β-caryophyllene, β-caryophyllene oxide and α-humulene), as identified at GC/MS analysis, was characterized. Modulation of cannabinoid CB1 and CB2 receptors was studied as a mechanistic hypothesis. Results highlighted marked cytotoxic effects of FOJ, FOS, and pure compounds in triple negative breast cancer MDA-MB-468 cells, likely mediated by a CB2 receptor activation. Cannabidiol was the main cytotoxic constituent, although low levels of caryophyllane sesquiterpenes and cannabichromene induced potentiating effects; the presence in the extracts of unknown antagonistic compounds has been highlighted too. These results suggest an interest in Felina 32 hemp inflorescences as a source of bioactive phytocomplexes with anticancer properties and strengthen the importance of considering the possible involvement of minor terpenes, such as caryophyllane sesquiterpenes, in the entourage effect of hemp-based extracts. Full article
(This article belongs to the Special Issue Pharmaceutical Drugs Based on Cannabis)
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14 pages, 5384 KiB  
Article
Cannabis-Derived Compounds Cannabichromene and Δ9-Tetrahydrocannabinol Interact and Exhibit Cytotoxic Activity against Urothelial Cell Carcinoma Correlated with Inhibition of Cell Migration and Cytoskeleton Organization
by Omer Anis, Ajjampura C. Vinayaka, Nurit Shalev, Dvora Namdar, Stalin Nadarajan, Seegehalli M. Anil, Ofer Cohen, Eduard Belausov, Jacob Ramon, Einav Mayzlish Gati and Hinanit Koltai
Molecules 2021, 26(2), 465; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26020465 - 17 Jan 2021
Cited by 30 | Viewed by 5562
Abstract
Cannabis sativa contains more than 500 constituents, yet the anticancer properties of the vast majority of cannabis compounds remains unknown. We aimed to identify cannabis compounds and their combinations presenting cytotoxicity against bladder urothelial carcinoma (UC), the most common urinary system cancer. An [...] Read more.
Cannabis sativa contains more than 500 constituents, yet the anticancer properties of the vast majority of cannabis compounds remains unknown. We aimed to identify cannabis compounds and their combinations presenting cytotoxicity against bladder urothelial carcinoma (UC), the most common urinary system cancer. An XTT assay was used to determine cytotoxic activity of C. sativa extracts on T24 and HBT-9 cell lines. Extract chemical content was identified by high-performance liquid chromatography (HPLC). Fluorescence-activated cell sorting (FACS) was used to determine apoptosis and cell cycle, using stained F-actin and nuclei. Scratch and transwell assays were used to determine cell migration and invasion, respectively. Gene expression was determined by quantitative Polymerase chain reaction (PCR). The most active decarboxylated extract fraction (F7) of high-cannabidiol (CBD) C. sativa was found to contain cannabichromene (CBC) and Δ9-tetrahydrocannabinol (THC). Synergistic interaction was demonstrated between CBC + THC whereas cannabinoid receptor (CB) type 1 and type 2 inverse agonists reduced cytotoxic activity. Treatments with CBC + THC or CBD led to cell cycle arrest and cell apoptosis. CBC + THC or CBD treatments inhibited cell migration and affected F-actin integrity. Identification of active plant ingredients (API) from cannabis that induce apoptosis and affect cell migration in UC cell lines forms a basis for pre-clinical trials for UC treatment. Full article
(This article belongs to the Special Issue Pharmaceutical Drugs Based on Cannabis)
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16 pages, 3002 KiB  
Article
In Silico and In Vitro Analysis of Major Cannabis-Derived Compounds as Fatty Acid Amide Hydrolase Inhibitors
by Emanuele Criscuolo, Maria Laura De Sciscio, Filomena Fezza and Mauro Maccarrone
Molecules 2021, 26(1), 48; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26010048 - 24 Dec 2020
Cited by 7 | Viewed by 2746
Abstract
Accumulated evidence suggests that enhancing the endocannabinoid (eCB) tone, in particular of anandamide (N-arachidonoylethanolamine, AEA), has therapeutic potential in many human diseases. Fatty acid amide hydrolase (FAAH) is a membrane-bound enzyme principally responsible for the degradation of AEA, and thus it [...] Read more.
Accumulated evidence suggests that enhancing the endocannabinoid (eCB) tone, in particular of anandamide (N-arachidonoylethanolamine, AEA), has therapeutic potential in many human diseases. Fatty acid amide hydrolase (FAAH) is a membrane-bound enzyme principally responsible for the degradation of AEA, and thus it represents a relevant target to increase signaling thereof. In recent years, different synthetic and natural compounds have been developed and tested on rat FAAH, but little is known of their effect on the human enzyme. Here, we sought to investigate six major cannabis-derived compounds to compare their action on rat and human FAAHs. To this aim, we combined an in silico analysis of their binding mode and affinity, with in vitro assays of their effect on enzyme activity. This integrated approach allowed to disclose differences in efficacy towards rat and human FAAHs, and to highlight the role of key residues involved in the inhibition of both enzymes. This study suggests that the therapeutic efficacy of compounds targeted towards FAAH should be always tested in vitro on both rat and human enzymes. Full article
(This article belongs to the Special Issue Pharmaceutical Drugs Based on Cannabis)
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12 pages, 1718 KiB  
Article
Cannabidiol Determination on Peripheral Capillary Blood Using a Microsampling Method and Ultra-High-Performance Liquid Chromatography Tandem Mass Spectrometry with On-Line Sample Preparation
by Federica Pigliasco, Sebastiano Barco, Sara Dubois, Francesca Marchese, Pasquale Striano, Tommaso Lomonaco, Francesca Mattioli, Gino Tripodi and Giuliana Cangemi
Molecules 2020, 25(16), 3608; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules25163608 - 08 Aug 2020
Cited by 12 | Viewed by 3941
Abstract
The aim of this work is to evaluate volumetric absorptive microsampling (VAMS) from capillary blood as an alternative strategy for therapeutic drug monitoring (TDM) in patients treated with the newly available GW-purified form of cannabidiol (Epidiolex®). A fast ultra-high-performance liquid chromatography-tandem [...] Read more.
The aim of this work is to evaluate volumetric absorptive microsampling (VAMS) from capillary blood as an alternative strategy for therapeutic drug monitoring (TDM) in patients treated with the newly available GW-purified form of cannabidiol (Epidiolex®). A fast ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) coupled to an online sample preparation system analysis was carried out on a Thermo Scientific Ultimate 3000 LC system coupled to a TSQ Quantiva triple quadrupole for the quantification of cannabidiol (CBD) and, in addition, delta-9-tetrahydrocannabinol (Δ9-THC). After validation using European Medicine Agency (EMA) guidelines the method was applied to samples obtained by finger prick of five pediatric patients treated with Epidiolex® and the results were compared to those obtained from venous blood and plasma. The method is linear in the range of 1–800 µg/L for both CBD and THC with intra- and inter-day precisions ranging from 5% to 14% and accuracies from −13% to +14% starting from 30 µL of sample. Stability in VAMS is ensured for up to 4 weeks at 25 °C thus allowing simple delivery. There was no difference (p = 0.69) between concentrations of CBD measured from VAMS sampled from capillary or venous blood (range: 52.19–330.14 or 72.15–383.45 µg/L) and those obtained from plasma (range: 64.3–374.09 µg/L) The VAMS-LC-MS/MS method represents a valid alternative strategy for therapeutic drug monitoring of patients treated with Epidiolex®. Full article
(This article belongs to the Special Issue Pharmaceutical Drugs Based on Cannabis)
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17 pages, 2775 KiB  
Article
Mosquitocidal and Anti-Inflammatory Properties of The Essential Oils Obtained from Monoecious, Male, and Female Inflorescences of Hemp (Cannabis sativa L.) and Their Encapsulation in Nanoemulsions
by Paolo Rossi, Alessia Cappelli, Oliviero Marinelli, Matteo Valzano, Lucia Pavoni, Giulia Bonacucina, Riccardo Petrelli, Pierluigi Pompei, Eugenia Mazzara, Irene Ricci, Filippo Maggi and Massimo Nabissi
Molecules 2020, 25(15), 3451; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules25153451 - 29 Jul 2020
Cited by 25 | Viewed by 3561
Abstract
Among the various innovative products obtainable from hemp (Cannabis sativa L.) waste biomass originating from different industrial processes, the essential oil (EO) deserves special attention in order to understand its possible application in different fields, such as cosmetics, pharmaceuticals, and botanical insecticides. [...] Read more.
Among the various innovative products obtainable from hemp (Cannabis sativa L.) waste biomass originating from different industrial processes, the essential oil (EO) deserves special attention in order to understand its possible application in different fields, such as cosmetics, pharmaceuticals, and botanical insecticides. For the purpose, in the present work, we studied the chemical composition of EOs obtained from different hemp varieties, namely Felina 32 and Carmagnola Selezionata (CS) using monoecious, male, and female inflorescences, and we evaluated their mosquitocidal activities on larvae and pupae of two main malaria vectors, Anopheles gambiae and An. stephensi. Then, in order to evaluate the safe use of hemp EOs for operators, the potential pro- or anti-inflammatory effect of hemp EOs together with their toxicological profile were determined on dermal fibroblasts and keratinocytes. Given the promising results obtained by insecticidal and anti-inflammatory studies, a preliminary evaluation of EOs encapsulation into nanoemulsions (NEs) has been performed with the aim to develop a formulation able to improve their poor physicochemical stability. Felina 32 and CS inflorescences provided EOs with an interesting chemical profile, with monoterpene and sesquiterpene hydrocarbons as the major components. This study highlighted the potential application of male inflorescences, which are usually discharged during hemp product processing. These EOs could be exploited as potential sustainable and eco-friendly insecticides, given their capability to be toxic against mosquitoes and the possibility to use them to prepare stable and safe formulations. The LC50 values found in this study (<80 ppm) are lower, on average, than those of many plant EOs, with the advantage of using an industrial waste product. From MTT assay and gene and protein expression analysis, EOs showed no cytotoxicity at the appropriate doses and exerted an anti-inflammatory effect on the human cell lines tested. These findings encourage further applied research on hemp EOs in order support their industrial exploitation. Full article
(This article belongs to the Special Issue Pharmaceutical Drugs Based on Cannabis)
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Review

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13 pages, 637 KiB  
Review
Chronological Review and Rational and Future Prospects of Cannabis-Based Drug Development
by Dvora Namdar, Omer Anis, Patrick Poulin and Hinanit Koltai
Molecules 2020, 25(20), 4821; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules25204821 - 20 Oct 2020
Cited by 17 | Viewed by 3287
Abstract
Despite the surge in cannabis chemistry research and its biological and medical activity, only a few cannabis-based pharmaceutical-grade drugs have been developed and marketed to date. Not many of these drugs are Food and Drug Administration (FDA)-approved, and some are still going through [...] Read more.
Despite the surge in cannabis chemistry research and its biological and medical activity, only a few cannabis-based pharmaceutical-grade drugs have been developed and marketed to date. Not many of these drugs are Food and Drug Administration (FDA)-approved, and some are still going through regulation processes. Active compounds including cannabinergic compounds (i.e., molecules targeted to modulate the endocannabinoid system) or phytocannabinoid analogues (cannabinoids produced by the plant) may be developed into single-molecule drugs. However, since in many cases treatment with whole-plant extract (whether as a solvent extraction, galenic preparation, or crude oil) is preferred over treatment with a single purified molecule, some more recently developed cannabis-derived drugs contain several molecules. Different combinations of active plant ingredients (API) from cannabis with proven synergies may be identified and developed as drugs to treat different medical conditions. However, possible negative effects between cannabis compounds should also be considered, as well as the effect of the cannabis treatment on the endocannabinoid system. FDA registration of single, few, or multiple molecules as drugs is a challenging process, and certain considerations that should be reviewed in this process, including issues of drug–drug interactions, are also discussed here. Full article
(This article belongs to the Special Issue Pharmaceutical Drugs Based on Cannabis)
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