Bioactivity of the cannabigerol cannabinoid and its analogues – the role of 3-dimensional conformation DOI Creative Commons
Mohammed S. Salha, Henry Adenusi, John H. Dupuis

et al.

Organic & Biomolecular Chemistry, Journal Year: 2023, Volume and Issue: 21(22), P. 4683 - 4693

Published: Jan. 1, 2023

Computational docking reveals the influence of conformation on inhibition cytochrome P450 3A4. Such structure–activity relationships are dependent intra-molecular interactions in cannabinoids, forming stabilised coiled structures.

Language: Английский

Phytocannabinoids: Exploring Pharmacological Profiles and Their Impact on Therapeutical Use DOI Open Access
Nicoleta Mirela Blebea, Andreea Pricopie, Robert-Alexandru Vlad

et al.

International Journal of Molecular Sciences, Journal Year: 2024, Volume and Issue: 25(8), P. 4204 - 4204

Published: April 10, 2024

Phytocannabinoids, a diverse group of naturally occurring compounds extracted from the Cannabis plant, have attracted interest due to their potential pharmacological effects and medicinal uses. This comprehensive review presents intricate profiles phytocannabinoids while exploring impacts these substances on biological systems. From more than one hundred cannabinoids which were identified in plant so far, cannabidiol (CBD) tetrahydrocannabinol (THC) are two most extensively studied phytocannabinoids. CBD is non-psychoactive compound, exhibits anti-inflammatory, neuroprotective, anxiolytic properties, making it promising candidate for wide array medical conditions. THC, known its psychoactive effects, possesses analgesic antiemetic contributing therapeutic potential. In addition THC CBD, range additional shown intriguing including cannabichromene (CBC), cannabigerol (CBG), cannabinol (CBN). The endocannabinoid system, made up enzymes involved production breakdown endocannabinoids, cannabinoid receptors (CB1 CB2), endogenous ligands (endocannabinoids), essential preserving homeostasis several physiological processes. Beyond ability modify ion channels, neurotransmitter receptors, anti-oxidative pathways. complex interaction between systems offers hope novel treatment approaches lays groundwork further developments field cannabinoid-based medicine. summarizes state field, points out information gaps, emphasizes need studies fully realize

Language: Английский

Citations

17

Phytocannabinoids in the Pharmacotherapy of Psoriasis DOI Creative Commons
Adam Wroński, Iwona Jarocka-Karpowicz, Anna Stasiewicz

et al.

Molecules, Journal Year: 2023, Volume and Issue: 28(3), P. 1192 - 1192

Published: Jan. 25, 2023

Phytocannabinoids are naturally occurring compounds, the main source of which is Cannabis sativa L. Through direct action or interaction with G protein-coupled receptors, they affect ROS and pro-inflammatory cytokines levels modify effectiveness transcription factor responsible for biosynthesis antioxidants lead to oxidative stress its consequences. Due modification redox balance inflammation, phytocannabinoids used in treatment various diseases, including autoimmune dermatoses, such as atopic dermatitis psoriasis. Psoriasis one most common unknown etiology. A disturbed a shift towards oxidation leads stress, resulting modifications, mainly lipids proteins, prolonged activation immune cells increased generation cytokines, chronic inflammation. Given biological activity phytocannabinoids, have become focus research components pharmacotherapy Beneficial effects were shown by representatives but effect cannabidiol (CBD) on skin (in vitro ex vivo) blood from patients psoriasis vulgaris psoriatic arthritis has been often evaluated recent years.

Language: Английский

Citations

19

Effect of Genotype, Year, and Their Interaction on the Accumulation of Bioactive Compounds and the Antioxidant Activity in Industrial Hemp (Cannabis sativa L.) Inflorescences DOI Open Access
Romina Beleggia, Valeria Menga, Flavia Fulvio

et al.

International Journal of Molecular Sciences, Journal Year: 2023, Volume and Issue: 24(10), P. 8969 - 8969

Published: May 18, 2023

The phytochemical content and the antioxidant activity in inflorescences of six industrial hemp (Cannabis sativa L.) genotypes, four monoecious (Codimono, Carmaleonte, Futura 75, Santhica 27), two dioecious (Fibrante Carmagnola Selezionata), were assessed for three consecutive years from 2018 to 2020. total phenolic content, flavonoid determined by spectrophotometric measurements, whereas HPLC GC/MS used identify quantify compounds, terpenes, cannabinoids, tocopherols, phytosterols. All measured traits significantly affected genotype (G), cropping year (Y), their interaction (G × Y), although Y effect prevailed as a source variation, ranging 50.1% 88.5% all metabolites except which equally G, Y, G (33.9%, 36.5%, 21.4%, respectively). genotypes presented more constant performance over compared with highest most stable observed Fibrante, was characterized levels cannabidiol, α-humulene β-caryophyllene, may confer on this great economic value due important pharmacological properties these metabolites. Conversely, 27 lowest accumulation phytochemicals years, notable exception cannabigerol, cannabinoid that exhibits wide range biological activities, found at its level genotype. Overall, findings can be breeders future programs aimed selection new improved inflorescences, provide better health benefits.

Language: Английский

Citations

18

Determining Antioxidant Activity of Cannabis Leaves Extracts from Different Varieties—Unveiling Nature’s Treasure Trove DOI Creative Commons
Anna Stasiłowicz-Krzemień, Szymon Sip, Piotr Szulc

et al.

Antioxidants, Journal Year: 2023, Volume and Issue: 12(7), P. 1390 - 1390

Published: July 6, 2023

Cannabis leaves contain a diverse range of antioxidants, including cannabinoids, flavonoids, and phenolic compounds, which offer significant health benefits. Utilising cannabis as source antioxidants presents cost-effective approach because they are typically discarded during the cultivation plants for their seeds or fibres. Therefore, this presented study aimed to assess antioxidant activity selected hemp cultivars, such Białobrzeska, Tygra, Henola, based on results obtained with 2,2'-Azino-bis(3-ethylbenzthiazoline-6-sulfonic acid, ferric reducing power, cupric capacity, 2,2-Diphenyl-1-picrylhydrazyl assays. The cannabinoid profile was analysed contents cannabidiol (CBD), cannabigerol (CBG), Δ9-tetrahydrocannabinol (Δ9-THC), cannabichromene (CBC), determined chromatographic following variables were tested: impact various extractants (methanol, ethanol, isopropanol), mixtures (50:50, v/v, well extraction methods (maceration ultra-sound-assisted extraction) in obtaining extracts characterised by different profiles. revealed that selection extractant conditions significantly influenced active compounds' efficiency activity. Among tested conditions, ultrasound-assisted using methanol yielded highest profile: CBD = 184.51 ± 5.61; CBG 6.10 0.21; Δ9-THC 0.51 0.01; CBC 0.71 0.01 μg/g potential Białobrzeska leaf extracts.

Language: Английский

Citations

18

Cannabigerol and Cannabicyclol Block SARS-CoV-2 Cell Fusion DOI
Nica Classen, Thanet Pitakbut, Michael Schöfbänker

et al.

Planta Medica, Journal Year: 2024, Volume and Issue: 90(09), P. 717 - 725

Published: June 17, 2024

Abstract The search for new active substances against SARS-CoV-2 is still a central challenge after the COVID-19 pandemic. Antiviral agents to complement vaccination are an important pillar in clinical situation. Selected cannabinoids such as cannabigerol, cannabicyclol, cannabichromene, and cannabicitran from Cannabis sativa synthetic homologues of cannabigerol cannabicyclol were evaluated effects on cell viability Vero cells (CC50 40 resp. 38 µM) reduced virus entry vesicular stomatitis pseudotyped viruses with surface-expressed spike protein at 20 µM. In addition reduction entry, titer assay preincubation Wuhan significantly confirmed antiviral activity. Investigations molecular targets addressed by indicated that both compounds inhibitors protein-mediated membrane fusion, could be shown virus-free reporter fusion inhibition (EC50 5.5 µM 10.8 monitoring syncytia formation cells. Selectivity indices calculated 7.4 3.5 cannabicyclol. Systematic semisynthetic alterations side chains do not contribute observed anti-membrane

Language: Английский

Citations

6

Chromene meroterpenoids from Rhododendron dauricum L. and their anti-inflammatory effects DOI
Na Zhang, Yang Xu,

Dejuan Sun

et al.

Phytochemistry, Journal Year: 2024, Volume and Issue: 225, P. 114200 - 114200

Published: June 25, 2024

Language: Английский

Citations

5

Safety assessment and redox status in rats after chronic exposure to cannabidiol and cannabigerol DOI
Hana Polanská,

Kateřina Petrláková,

Barbora Papoušková

et al.

Toxicology, Journal Year: 2023, Volume and Issue: 488, P. 153460 - 153460

Published: Feb. 14, 2023

Language: Английский

Citations

12

Antitumor Effects of Cannabis sativa Bioactive Compounds on Colorectal Carcinogenesis DOI Creative Commons
Rita Silva‐Reis, Artur M. S. Silva, Paula A. Oliveira

et al.

Biomolecules, Journal Year: 2023, Volume and Issue: 13(5), P. 764 - 764

Published: April 28, 2023

is a multipurpose plant that has been used in medicine for centuries. Recently, considerable research focused on the bioactive compounds of this plant, particularly cannabinoids and terpenes. Among other properties, these exhibit antitumor effects several cancer types, including colorectal (CRC). Cannabinoids show positive treatment CRC by inducing apoptosis, proliferation, metastasis, inflammation, angiogenesis, oxidative stress, autophagy. Terpenes, such as β-caryophyllene, limonene, myrcene, have also reported to potential through induction inhibition cell angiogenesis. In addition, synergy between terpenes are believed be important factors CRC. This review focuses current knowledge about terpenoids from

Language: Английский

Citations

12

Anti-Inflammatory Effects of Cannabigerol in Rheumatoid Arthritis Synovial Fibroblasts and Peripheral Blood Mononuclear Cell Cultures Are Partly Mediated by TRPA1 DOI Open Access
Torsten Lowin,

Marianne Sofia Tigges-Perez,

Eva Constant

et al.

International Journal of Molecular Sciences, Journal Year: 2023, Volume and Issue: 24(1), P. 855 - 855

Published: Jan. 3, 2023

Since its medical legalization, cannabis preparations containing the major phytocannabinoids (cannabidiol (CBD) and δ9-tetrahydrocannabinol (THC)) have been used by patients with rheumatoid arthritis (RA) to alleviate pain inflammation. However, minor cannabinoids such as cannabigerol (CBG) also demonstrated anti-inflammatory properties, but due lack of studies, they are not widely used. CBG binds several cellular target proteins cannabinoid α2-adrenergic receptors, it ligates members transient potential receptor (TRP) family TRPA1 being main target. is only involved in nnociception, protects cells from apoptosis under oxidative stress conditions. Therefore, modulation signaling might be modulate disease activity RA this autoimmune accompanied subsequent activation pro-inflammatory pathways. Rheumatoid synovial fibroblasts (RASF) were stimulated or tumor necrosis factor (TNF) for 72 h induce protein. increased intracellular calcium levels TNF-stimulated RASF unstimulated a TRPA1-dependent manner. In addition, PoPo3 uptake, surrogate marker drug was enhanced CBG. cell viability, IL-6 IL-8 production decreased peripheral blood mononuclear cultures (PBMC) alone together RASF, CBG-modulated interleukin (IL)-6, IL-10, TNF immunoglobulin M G which dependent on stimulus (T cell-dependent independent). effects PBMCs partially mediated antagonist A967079 did inhibit some all cytokine production. contrast, antagonism even inhibitory showed broad isolated PBMC PBMC/RASF co-cultures. As non-psychotropic, add-on therapy reduce autoantibody levels.

Language: Английский

Citations

11

Phytocannabinoids CBD, CBG, and their Derivatives CBD-HQ and CBG-A Induced In Vitro Cytotoxicity in 2D and 3D Colon Cancer Cell Models DOI Creative Commons
Dorota Bęben,

Oliwia Siwiela,

Anna Szyjka

et al.

Current Issues in Molecular Biology, Journal Year: 2024, Volume and Issue: 46(4), P. 3626 - 3639

Published: April 19, 2024

Phytocannabinoids, compounds found in Cannabis sativa L., are used oncology and palliative care to reduce the adverse reactions of standard therapies. Cancer patients use formulations L. manage anxiety, pain, nausea associated with cancer treatment, there is growing evidence that some them may exhibit anticancer properties. In this study, we tested potential selected cannabinoids CBD (cannabidiol) its quinone derivative CBD-HQ (cannabidiol hydroquinone), CBG (cannabigerol) acid CBG-A (cannabigerolic acid), as well a combination CBD+CBG on colon cell line SW-620. The MTT assay was determine cannabinoids’ ability induce death. All were cytotoxic at lowest concentration (3 μg/mL). half maximal inhibitory (IC50) ranged from 3.90 8.24 μg/mL, depending substance. Cytotoxicity confirmed 3D spheroidal culture calcein propidium iodide staining. amount intracellular reactive oxygen species (ROS) examined using DCF-DA assay. showed antioxidant activity all tested. level ROS decreased only by 0.7–18%. However, induced strongest reduction 31–39%. Our results suggest represent an interesting research direction great implementation potential. These preliminary beginning into these substances for treatment underscore further research.

Language: Английский

Citations

4