Cannabinoid WIN‑55,212‑2 mesylate inhibits ADAMTS‑4 activity in human osteoarthritic articular chondrocytes by inhibiting expression of syndecan‑1.

Posted on April 16, 2016 by David

“A central feature of osteoarthritis (OA) is the loss of articular cartilage, which is primarily attributed to cartilage breakdown.

Accumulating evidence also suggests that cannabinoids have chondroprotective effects.

In conclusion, to the best of our knowledge, the present study provides the first in vitro evidence supporting that the synthetic cannabinoid WIN‑55 inhibits ADAMTS‑4 activity in unstimulated and IL‑1β‑stimulated human OA articular chondrocytes by decreasing the mRNA stability/expression of syndecan‑1 via CB2.

This suggests a novel mechanism by which cannabinoids may prevent cartilage breakdown in OA.

In addition, it also provides novel insights into the pharmacological effects of synthetic cannabinoids on OA.” http://www.ncbi.nlm.nih.gov/pubmed/27082728

“Chondroprotective: A specific compound or chemical that delays progressive joint space narrowing characteristic of arthritis and improvesthe biomechanics of articular joints by protecting chondrocytes.” http://medical-dictionary.thefreedictionary.com/chondroprotective

Role of the endocannabinoid system in the emotional manifestations of osteoarthritis pain.

Posted on June 13, 2015 by David

“The levels of the endocannabinoids anandamide (AEA) and 2-arachidonoylglycerol.

In this study, we investigated the role of the endocannabinoid system (ECS) in the emotional and cognitive alterations associated with osteoarthritis pain.

Changes found in these biomarkers of the ECS correlated with pain, affective and cognitive symptoms in these patients.

The ECS plays a crucial role in osteoarthritis and represents an interesting pharmacological target and biomarker of this disease.”

http://www.ncbi.nlm.nih.gov/pubmed/26067584

http://www.thctotalhealthcare.com/category/osteoarthritis/

The type 2 cannabinoid receptor regulates susceptibility to osteoarthritis in mice.

Posted on May 6, 2015 by David

“The aim of this study was to evaluate the role of the type 2 cannabinoid receptor (Cnr2) in regulating susceptibility to osteoarthritis in mice.

These studies demonstrate that the Cnr2 pathway plays a role in the pathophysiology of osteoarthritis in mice and shows that pharmacological activation of CB2 has a protective effect.

Further studies of the role of cannabinoid receptors in the pathogenesis of osteoarthritis in man are warranted.”

http://www.ncbi.nlm.nih.gov/pubmed/25937028

http://www.thctotalhealthcare.com/category/osteoarthritis/

Emerging targets and therapeutic approaches for the treatment of osteoarthritis pain.

Posted on March 3, 2015 by David

“Osteoarthritis is a complex and often painful disease that is inadequately controlled with current analgesics. This review discusses emerging targets and therapeutic approaches that may lead to the development of better analgesics…

Aberrant excitability in peripheral and central pain pathways drives osteoarthritis pain, reversing this via modulation of nerve growth factor, voltage-gated sodium channel, voltage-gated calcium channel and transient receptor potential vanilloid one activity, and increasing inhibitory mechanisms through modulation of cannabinoid and descending modulatory systems hold promise for osteoarthritis pain therapy.”

http://www.ncbi.nlm.nih.gov/pubmed/25730180

http://www.thctotalhealthcare.com/category/osteoarthritis/

Cannabinoid Receptor CB2 Is Involved in Tetrahydrocannabinol-Induced Anti-Inflammation against Lipopolysaccharide in MG-63 Cells.

Posted on February 6, 2015 by David

“Cannabinoid Δ9-tetrahydrocannabinol (THC) is effective in treating osteoarthritis (OA)…

Activation of cannabinoid receptor CB2 reduces inflammation; whether the activation CB2 is involved in THC-induced therapeutic action for OA is still unknown.

We hypothesized that the activation of CB2 is involved in THC-induced anti-inflammation in the MG-63 cells exposed to LPS, and the anti-inflammation is mediated by cofilin-1…

We found that THC suppressed the release of proinflammatory factors, including tumor necrosis factor α (TNF-α), interleukin- (IL-) 1β, IL-6, and IL-8, decreased nuclear factor-κB (NF-κB) expression, and inhibited the upregulation of cofilin-1 protein in the LPS-stimulated MG-63 cells.

These results suggested that CB2 is involved in the THC-induced anti-inflammation in LPS-stimulated MG-63 cells, and the anti-inflammation may be mediated by cofilin-1.”

http://www.ncbi.nlm.nih.gov/pubmed/25653478

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4310496/

http://www.thctotalhealthcare.com/category/osteoarthritis/

Endocannabinoids and acute pain after total knee arthroplasty.

Posted on January 22, 2015 by David

“Osteoarthritis (OA) of the knee is a progressive disease that is associated with inflammation of the joints and lower extremity pain. Total knee arthroplasty (TKA) is a surgical procedure that aims to reduce pain and restore motor function in patients suffering from OA. The immediate postoperative period can be intensely painful leading to extended recovery times including persistent pain.

The endocannabinoid system regulates nociception, and the activation of cannabinoid receptors produces antinociceptive effects in preclinical models of OA…

Taken together, our results are the first to reveal associations between central and peripheral endocannabinoid levels and postoperative pain. This suggests that endocannabinoid metabolism may serve as a target for the development of novel analgesics both for systemic or local delivery into the joint.”

http://www.ncbi.nlm.nih.gov/pubmed/25599456

Involvement of the endocannabinoid system in osteoarthritis pain.

Posted on February 6, 2014 by David

“Increasing evidence from preclinical studies supports the interest of the endocannabinoid system as an emerging therapeutic target for osteoarthritis pain.

Indeed, pharmacological studies have shown the anti-nociceptive effects of cannabinoids in different rodent models of osteoarthritis, and compelling evidence suggests an active participation of the endocannabinoid system in the pathophysiology of this disease.

The ubiquitous distribution of cannabinoid receptors, together with the physiological role of the endocannabinoid system in the regulation of pain, inflammation and even joint function further support the therapeutic interest of cannabinoids for osteoarthritis.

…review summarizes the promising results that have been recently obtained in support of the therapeutic value of cannabinoids for osteoarthritis management.”

http://www.ncbi.nlm.nih.gov/pubmed/24494687

Increase of mesenchymal stem cell migration by Cannabidiol via activation of p42/44 MAPK.

Posted on December 7, 2013 by David

“Migration and differentiation of mesenchymal stem cells (MSCs) are known to be involved in various regenerative processes such as bone healing.

The present study therefore focussed on cannabinoids which have been demonstrated to exhibit tissue healing properties…

Collectively, this study demonstrates CBD to promote the migration of MSCs via activation of the CB2 receptor and inhibition of GPR55 and to induce osteoblastic differentiation. CBD may therefore recruit MSCs to sites of calcifying tissue regeneration and subsequently support bone regeneration via an osteoanabolic action on MSCs.”

http://www.ncbi.nlm.nih.gov/pubmed/24304686

Cannabinoid CB2 Receptors Regulate Central Sensitization and Pain Responses Associated with Osteoarthritis of the Knee Joint.

Posted on November 29, 2013 by David

“Osteoarthritis (OA) of the joint is a prevalent disease accompanied by chronic, debilitating pain. Recent clinical evidence has demonstrated that central sensitization contributes to OA pain. An improved understanding of how OA joint pathology impacts upon the central processing of pain is crucial for the identification of novel analgesic targets/new therapeutic strategies.

Inhibitory cannabinoid 2 (CB2) receptors attenuate peripheral immune cell function and modulate central neuro-immune responses in models of neurodegeneration…

These findings suggest that targeting CB2 receptors may have therapeutic potential for treating OA pain.”

http://www.ncbi.nlm.nih.gov/pubmed/24282543

Therapeutic potential of cannabinoid medicines.

Posted on September 6, 2013 by David

Drug Testing and Analysis

“Cannabis was extensively used as a medicine throughout the developed world in the nineteenth century but went into decline early in the twentieth century ahead of its emergence as the most widely used illicit recreational drug later that century. Recent advances in cannabinoid pharmacology alongside the discovery of the endocannabinoid system (ECS) have re-ignited interest in cannabis-based medicines.

The ECS has emerged as an important physiological system and plausible target for new medicines. Its receptors and endogenous ligands play a vital modulatory role in diverse functions including immune response, food intake, cognition, emotion, perception, behavioural reinforcement, motor co-ordination, body temperature, wake/sleep cycle, bone formation and resorption, and various aspects of hormonal control. In disease it may act as part of the physiological response or as a component of the underlying pathology.

In the forefront of clinical research are the cannabinoids delta-9-tetrahydrocannabinol and cannabidiol, and their contrasting pharmacology will be briefly outlined. The therapeutic potential and possible risks of drugs that inhibit the ECS will also be considered. This paper will then go on to review clinical research exploring the potential of cannabinoid medicines in the following indications: symptomatic relief in multiple sclerosis, chronic neuropathic pain, intractable nausea and vomiting, loss of appetite and weight in the context of cancer or AIDS, psychosis, epilepsy, addiction, and metabolic disorders.”

http://www.ncbi.nlm.nih.gov/pubmed/24006213

http://onlinelibrary.wiley.com/doi/10.1002/dta.1529/abstract