Category Archives: Uncategorized

Pharmaceutical potentialities of β-caryophyllene for drug delivery systems: a prospection.

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“The β-caryophyllene (BCP), a phytocannabinoid presents in various essential oils, demonstrated selective action on the CB2 endocannabinoid receptor and attracted considerable attention because of its several pharmacological activities. Despite this recognized potential, this hydrophobic compound is a volatile and acid-sensitive sesquiterpene that readily oxidizes when exposed to air, and has low bioavailability in oral formulations. Thus, the development of formulations that guarantee its stability and increase its bioavailability is a challenge for its use in the pharmaceutical field.

RESULTS:

The systems presented here may represent an interesting approach to overcome the limitations already mentioned for this terpene. These systems proved to be promising for improving solubility, stability and controlled release of this pharmacological relevant sesquiterpene. In the industrial field, some companies have filed patent applications for the commercial use of the BCP, however, the use of pharmaceutical formulations still appeared moderate.

CONCLUSION:

This prospective study evidenced the new perspectives related to BCP vectorization systems in the pharmaceutical and industrial marketing field and may serve as a basis for further research and pharmaceutical use of this powerful cannabinoid.”

https://www.ncbi.nlm.nih.gov/pubmed/30207226

http://www.eurekaselect.com/165376/article

“β-caryophyllene (BCP) is a common constitute of the essential oils of numerous spice, food plants and major component in Cannabis.”   http://www.ncbi.nlm.nih.gov/pubmed/23138934

Computational systems pharmacology analysis of cannabidiol: a combination of chemogenomics-knowledgebase network analysis and integrated in silico modeling and simulation.

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“With treatment benefits in both the central nervous system and the peripheral system, the medical use of cannabidiol (CBD) has gained increasing popularity.

Given that the therapeutic mechanisms of CBD are still vague, the systematic identification of its potential targets, signaling pathways, and their associations with corresponding diseases is of great interest for researchers.

In the present work, chemogenomics-knowledgebase systems pharmacology analysis was applied for systematic network studies to generate CBD-target, target-pathway, and target-disease networks by combining both the results from the in silico analysis and the reported experimental validations.

Based on the network analysis, three human neuro-related rhodopsin-like GPCRs, i.e., 5-hydroxytryptamine receptor 1 A (5HT1A), delta-type opioid receptor (OPRD) and G protein-coupled receptor 55 (GPR55), were selected for close evaluation. Integrated computational methodologies, including homology modeling, molecular docking, and molecular dynamics simulation, were used to evaluate the protein-CBD binding modes. A CBD-preferred pocket consisting of a hydrophobic cavity and backbone hinges was proposed and tested for CBD-class A GPCR binding.

Finally, the neurophysiological effects of CBD were illustrated at the molecular level, and dopamine receptor 3 (DRD3) was further predicted to be an active target for CBD.”

https://www.ncbi.nlm.nih.gov/pubmed/30202014

https://www.nature.com/articles/s41401-018-0071-1

The Endocannabinoid/Cannabinoid Receptor 2 System Protects Against Cisplatin-Induced Hearing Loss.

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“Previous studies have demonstrated the presence of cannabinoid 2 receptor (CB2R) in the rat cochlea which was induced by cisplatin. In an organ of Corti-derived cell culture model, it was also shown that an agonist of the CB2R protected these cells against cisplatin-induced apoptosis.

In the current study, we determined the distribution of CB2R in the mouse and rat cochleae and examined whether these receptors provide protection against cisplatin-induced hearing loss.

These data unmask a protective role of the cochlear endocannabinoid/CB2R system which appears tonically active under normal conditions to preserve normal hearing. However, an exogenous agonist is needed to boost the activity of endocannabinoid/CB2R system for protection against a more traumatic cochlear insult, as observed with cisplatin administration.”

https://www.ncbi.nlm.nih.gov/pubmed/30186120

https://www.frontiersin.org/articles/10.3389/fncel.2018.00271/full

Attenuation of Listeria monocytogenes Virulence by Cannabis sativa L. Essential Oil.

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“Anti-virulence strategies are being explored as a novel approach to combat pathogens. Such strategies include inhibition of surface adhesion, tissue invasion, toxin production, and/or interference with the gene regulation of other virulence traits.

Listeria monocytogenes, the causative agent of listeriosis, is a facultative intracellular food pathogen characterized by a wide distribution in the environment. Its ability to persist within biofilms and to develop resistance to sanitizers is the cause of significant problems in food processing plants and of steep costs for the food industry.

In humans, the treatment of listeriosis is hampered by the intracellular location of listeriae and the poor intracellular penetration of some antibiotics. Eleven L. monocytogenes isolates from patients who were diagnosed with invasive listeriosis in Italy in 2014-2016 were studied.

This in vitro and in vivo study explored the antibacterial and anti-virulence properties of a steam-distilled essential oil of Cannabis sativa L., which is being intensively investigated for its high content in powerful bioactive phytochemicals.

Susceptibility experiments demonstrated a moderate bactericidal activity of the essential oil (Minimum Bactericidal Concentration > 2048 μg/mL).

Food contamination with L. monocytogenes is a major concern for the food industry, particularly for plants making ready-to-eat and processed food.

The present work provides a baseline in the study of the anti-virulence properties of the C. sativa essential oil against L. monocytogenes. Further studies are needed to understand if it could be used as an alternative agent for the control of L. monocytogenes in food processing plants.”

 https://www.ncbi.nlm.nih.gov/pubmed/30186775
https://www.frontiersin.org/articles/10.3389/fcimb.2018.00293/full

Cannabis in palliative care: current challenges and practical recommendations.

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 “Pain and symptom control challenges are common in palliative care, and the search for other therapeutic strategies is ongoing.

Unfortunately, patients and their caregivers are receiving little information or support from healthcare providers regarding the increasingly popular cannabinoid-based medicines (CBM).

Clinicians, meanwhile, feel understandably perplexed by the discrepancy between the available evidence and the rapid interest in which patients and their families have demonstrated for CBM.

There is an urgent need to address the many challenges that are delaying the appropriate integration of CBM into clinical practice, notwithstanding the obvious need for a solid general knowledge of pharmacology, mechanism of action and available clinical evidence supporting its use.

The authors will address these challenges and provide practical recommendations regarding patient assessment for the use of CBM. The authors will also make suggestions regarding patient expectations in order to define clear objectives, review the necessary precautions prior to initiating treatment, aid in selecting the appropriate strain and route of administration as well as establishing proper titration and monitoring protocols. The authors will also discuss the lesser known but potentially therapeutic psychoactive effects of cannabis.

As this class of therapeutic agents are likely to play a major role in palliative medicine in the near future, clinicians would benefit from familiarizing themselves with CBM and we can expect that patients and their caregivers will appreciate receiving support in their search for safe and effective therapeutic alternatives.”

https://www.ncbi.nlm.nih.gov/pubmed/30180728

http://apm.amegroups.com/article/view/20097

Fast extraction of cannabinoids in marijuana samples by using hard-cap espresso machines.

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Talanta

“A simple, quick and low cost procedure was developed for the extraction of Δ9-tetrahydrocannabinol, cannabidiol, and cannabinol from marijuana samples, based on the use of a hard-cap espresso extraction with 2-propanol. After extraction, cannabinoids were directly determined after appropriate dilution by gas-chromatography-mass spectrometry, reaching a limit of detection from 0.03 to 0.05 mg g-1. Extraction efficiency was evaluated by the comparison of results obtained for seized samples by the proposed method and a reference methodology based on ultrasound-assisted extraction. Moreover, ion mobility was proposed for the rapid and sensitive determination of Δ9-tetrahydrocannabinol and cannabidiol providing a quick response for the analysis of seized marijuana samples in 1 min, including extraction, dilution and determination.”

https://www.ncbi.nlm.nih.gov/pubmed/30172516

https://www.sciencedirect.com/science/article/pii/S0039914018308178?via%3Dihub

“Turns Out You Can Use Espresso Machines to Make Marijuana Extracts”  https://www.civilized.life/articles/espresso-machine-marijuana-extracts/

Δ9-tetrahydrocannabivarin impairs epithelial calcium transport through inhibition of TRPV5 and TRPV6.

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 Pharmacological Research

“Compounds extracted from the cannabis plant, including the psychoactive Δ9-tetrahydrocannabinol (THC) and related phytocannabinoids, evoke multiple diverse biological actions as ligands of the G protein-coupled cannabinoid receptors CB1 and CB2. In addition, there is increasing evidence that phytocannabinoids also have non-CB targets, including several ion channels of the transient receptor potential superfamily.

We investigated the effects of six non-THC phytocannabinoids on the epithelial calcium channels TRPV5 and TRPV6, and found that one of them, Δ9-tetrahydrocannabivarin (THCV), exerted a strong and concentration-dependent inhibitory effect on mammalian TRPV5 and TRPV6 and on the single zebrafish orthologue drTRPV5/6. Moreover, THCV attenuated the drTRPV5/6-dependent ossification in zebrafish embryos in vivo. Oppositely, 11-hydroxy-THCV (THCV-OH), a product of THCV metabolism in mammals, stimulated drTRPV5/6-mediated Ca2+ uptake and ossification.

These results identify the epithelial calcium channels TRPV5 and TRPV6 as novel targets of phytocannabinoids, and suggest that THCV-containing products may modulate TRPV5- and TRPV6-dependent epithelial calcium transport.”

https://www.ncbi.nlm.nih.gov/pubmed/30170189

https://linkinghub.elsevier.com/retrieve/pii/S1043661818311095

The Association Between Tetrahydrocannabinol and Lower Urinary Tract Symptoms Utilizing the National Health and Nutrition Examination Survey.

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Urology Home

“To further define the relationship between tetrahydrocannabinol (THC) and lower urinary tract symptoms (LUTS), specifically how THC use associates with the frequency of LUTS in young community-dwelling men in the United States.

MATERIALS AND METHODS:

The National Health and Nutrition Examination Survey (NHANES) database was queried (2005-2008). Men ages 20-59 who completed the urinary and substance abuse questionnaires were included. The presence of LUTS was defined as having ≥2 of the following: nocturia (≥2), hesitancy, incomplete emptying, or incontinence. THC use was self-reported, and participants were considered regular smokers if they endorsed smoking at least once per month. Multivariable logistic regression was performed to analyze the relationship between THC and LUTS.

RESULTS:

Among 3,037 men who met inclusion criteria, 14.4% (n=477) of subjects reported THC use. In multivariable analyses, adjusting for clinical variables, regular THC users remained significantly less likely to report LUTS (odds ratio of 0.55; CI 95% 0.408-0.751, p<0.01) compared to non-users.

CONCLUSION:

Obesity, diabetes, and multiple co-morbidities are well-established risk factors for LUTS within the NHANES. Regular THC use, however, appears to be protective from LUTS in young community-dwelling men.”

https://www.ncbi.nlm.nih.gov/pubmed/30142408

https://www.goldjournal.net/article/S0090-4295(18)30881-1/fulltext

Cannabis and the Health and Performance of the Elite Athlete.

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“Cannabis (marijuana) is undergoing extensive regulatory review in many global jurisdictions for medical and nonmedical access. Cannabis has potential impact on the health of athletes as well as on performance in both training and in competition. The aim of this general review is to identify and highlight the challenges in interpreting information with respect to elite athletic performance, and to point to important research areas that need to be addressed.

MAIN RESULTS:

Cannabis may be primarily inhaled or ingested orally for a range of medical and nonmedical reasons; evidence for efficacy is limited but promising for chronic pain management. Although evidence for serious harms from cannabis use on health of athletes is limited, one should be cognizant of the potential for abuse and mental health issues. Although the prevalence of cannabis use among elite athletes is not well-known, use is associated with certain high-risk sports. There is no evidence for cannabis use as a performance-enhancing drug.

CONCLUSIONS:

Medical and nonmedical cannabis use among athletes reflects changing societal and cultural norms and experiences. Although cannabis use is more prevalent in some athletes engaged in high-risk sports, there is no direct evidence of performance-enhancing effects in athletes. The potential beneficial effects of cannabis as part of a pain management protocol, including reducing concussion-related symptoms, deserve further attention.”

https://www.ncbi.nlm.nih.gov/pubmed/30153174

https://insights.ovid.com/crossref?an=00042752-201809000-00009

Orthopaedic surgery patients who use recreational marijuana have less pre-operative pain.

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“To determine the baseline clinical characteristics of recreational marijuana users undergoing outpatient orthopaedic surgery.

We hypothesized that patients who report marijuana use would have worse pain, function, and general health status.

The results do not support our hypothesis, as marijuana use was associated with less pain and better lower extremity activity rating scale scores when compared to non-users.”

https://www.ncbi.nlm.nih.gov/pubmed/30135987

https://link.springer.com/article/10.1007%2Fs00264-018-4101-x