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Eight function of CBD

發表時間:2019-04-26 20:23

Cannabidiol (CBD) has pharmacological activitiessuch as anti-spasm, anti-rheumatoid arthritis and anxiolysis.

In the early 1990s,Matsuda and Munro discovered two cannabinoid receptors, one of which is composedof 473 amino acids called the central cannabinoid receptor and named CB1.TheCB1 receptor is mainly located in the brain, spinal cord and peripheral nervoussystem including lung, heart, urogenital, gastrointestinal tract and eyes.Human CB1 is very similar to rats but only one amino acid less. The otherconsists of 360 amino acids, called the peripheral cannabis receptor, namedCB2. CB2 receptors are mainly distributed in the periphery, such as the spleenborder area, immune cell surface and tonsils, etc. The differences in tissuedistribution between CB1 and CB2 are not absolute, but they differ in theirexpression scale. Certified by high-sensitivity PCR techniques, high expressionof CB1 in brain tissue was also found in the adrenal gland, heart, lung,prostate, uterus, ovary, testis, bone marrow, thymus, spleen, and tonsils. BothCB1 and CB2 are diphtheria toxin-sensitive inhibitory G-protein receptors,which inhibit the activity of adenylate cyclase through inhibitory G protein(Gi) and reduce intracellular cAMP levels. Wiley and Fride speculated there isa new cannabinoid receptor through pharmacological experiments, which Estercalled the CB3 receptor, but there is not enough evidence to confirm theexistence of the receptor.


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Many experiments haveshown that there is a high correlation between the affinity of a large numberof cannabinoid analogues for receptor binding and their intensities in variouspharmacological evaluations, including analgesia, cooling, and psychotropicactivity in mice and humans. In addition, the function of the receptor locatedarea is related to the physiological and pharmacological effects caused bydrug. The highest density of cannabinoid receptors in the nerve tissues is themolecular layer of the basal ganglia and cerebellum, which could explain whycannabinol binds to these areas and causes changes of motor function. Extensivepharmacological studies have shown that THC regulates central and peripheralneurotransmission by acting on CB1 receptors and modulates the cytokinesreleased by immune cells through acting on CB2 receptors, and produce a varietyof biological activities. Currently there is no relevant report on themechanism action of CBD. However, there is no doubt that a neuroactive CBD haspharmacological activity and its pharmacological effects are not the same asTHC.



The pharmacological studyof CBD did not occur until the early 1970s.In the following years,pharmacological aspects of CBD was reported one after another; especially afterthe anti-convulsive effects of CBD were reported; CBD anti-emetic effects werereported as well as anti-oxidants and anti-rheumatic arthritis drugs inbiological systems. Related pharmacological studies have shown that CBDregulates THC levels in the brain; moreover, CBD exerts analgesic andanti-inflammatory effects through dual inhibition of cyclooxygenase andlipoxygenase which is stronger than aspirin; it mainly through inhibitoryaction on lipoxygenase after oral administration. CBD, same as THC, stimulatesthe release of prostaglandins from synovial cells. In recent years, people havemodified the structure of CBD and synthesized a series of CBD analogues, whichalso have different pharmacological activities.


1:relievepain and anti-inflammatory effects


The pathogenesis ofinflammation is complex and inflammation is caused and maintained by variousintercellular mediators. Among them, tumor necrosis factor (TNF) is alsoinvolved in the process of inflammation and plays a particularly importantrole. The antibacterial and antitumor activity of the antioxidant media (ROI)plays a key role in protecting the body. Nitric oxide (NO) is an endogenousregulator with a variety of biological functions and also exhibitsantibacterial and antitumor activity and affects all aspects of the inflamedstack. Inflammation will be caused once the levels of TNF, ROI, and NO in thebody are going high, and the cells and tissues of the body will be damaged andcause hematosepsis. Therefore, main target for the treatment of inflammation isto take medicine which will act on the immune system to inhibit TNF, ROI, andNO. According to report, CBD could produce TNF regulatory products throughperipheral blood mononuclear cells in the human body. Due to the potentialanti-inflammatory, low toxicity and non-neurotoxicity effect of CBD, it hasbeen used as a therapeutic agent for collagenous arthritis and it also has acertain effect on the treatment of rheumatoid arthritis.

In vitro experiments haveshown that CBD can significantly reduce TNF and NO produced by peritonealmacrophages. Fride et al. found that (+)- 7-OH-cannabidiol-DMH has a centralactivity and (+)- Cannabidionl-DMH inhibits ear peripheral pain and arachidonicacid-induced inflammation in mice through the research of (+)-CBD and itsanalogues which acted on the central and peripheral anti-inflammatory andanti-peripheral pain in the intestinal tract of mice.


2:Anti-schizophrenic

GW Pharmaceuticalsannounced positive key results for a phase 2a placebo-controlled exploratoryclinical trial of cannabidiol (CBD) for 88 patients with schizophrenia who havenot responded adequately to first-line antipsychotic drugs. During the trial,patients still used their antipsychotics and they were randomized to receivetreatment with cannabidiol or placebo as adjuvant treatment.

On a series of endpoints,cannabidiol was consistently superior to placebo, with the most significantdifferences being the PANSS positive scale, the severity clinical overallimpression scale, and the degree of clinical improvement overall impressionscale. The proportion of patients who responded to cannabidiol (improving thePANSS overall score greater than 20%) was higher than that of placebo-treatedpatients, with an odds ratio of 2.65.

In terms of cognition,cannabidiol is superior to placebo, and significant differences can be observedin subdomains that are particularly relevant to the prospect of improvement inschizophrenia patients. For negative symptoms, the Negative Symptom AssessmentScale showed a trend to support cannabidiol, and this trend reached asignificant difference in patients taking cannabidiol plus a major first-lineantipsychotic. Most of the other endpoints in the study supported cannabidiol,which was close to statistical significance in most cases.



3: anxiety

Musty's experiments withmice revealed that CBD can relieve stress and reduce pressure-induced ulcers. ABrazilian research team found that CBD can prevent anxiety caused by THC andeven have an impedance effect on other central nervous system effects caused byTHC. Of course, not all THC effects can be blocked by CBD.The team alsoconducted a double-blind trial of diazepam and CBD, confirming that dose of CBDis higher, but has same sedative effect as diazepam. Later, the team found thatthe dimethyl heptyl analogues of CBD were better than the sedative effects ofdiazepam and CBD.



      4:Anti-cancereffect

Brain tumors are not onlydifficult to treat but also have poor prognosis. Recently, scientists researchhas shown that certain components of cannabis combined with radiation therapyfor the treatment of brain cancer can completely inhibit the growth of tumors.The main acting compounds are THC and CBD.

Cannabinoids componentsis the active chemical substance in cannabis, there are 85 known cannabinoidscomponents in cannabis plants, and the main active ingredient in cannabis iscalled tetrahydrocannabinol (THC). This study focused on mouse brain tumors andthe results are the first time to prove that the growth of brain tumors sloweddown significantly when THC/CBD was combined with radiation therapy.

Researcher Dr. Wai Liusaid: The results are very exciting. In the experiment, three methods were usedfor cancer treatment: cannabis alone treatment, radiation alone treatment, andradiation and cannabinoid combined treatment. As a result, the combination ofradiation and cannabinoid treatment reached the most favorable results, and thetumor size was greatly reduced. Even in some cases, animal brain tumors couldbe completely disappeared. The research team is discussing the possibility ofcombining cannabinoids with radiation in clinical trials in humans. Theresearch results have been published in the Molecular Cancer TherapeuticsMagazine.



     5:Relieve nausea and vomiting

Cancer patients often usechemotherapy, which prolongs the life of the patient, but it producessignificant side effects, causing great suffering to the patient. Thederivative of THC, dronabinol, has been used clinically as antiemetic drug.However, due to its hallucinogenic effect and its addiction, the application islimited. Parker et al. evaluated the anti-vomiting effects of CBD and itsanalog CBD-DMH in a conditional rejection model. The results showed that CBDand CBD-DMH have anti-vomiting effects in mice. Due to the low toxicity of CBD;it has a good applicable prospect for relieving nausea and vomiting afterchemotherapy


   

     6: Epilepsia and other neurological diseases treatment

As early as the 1970s,some research groups discovered that CBD has the ability to reduce or preventthe paralysis of experimental animals. Later, it was found that CBD can enhancethe anti-spasm effects of phenytoin and sedative hypnotics.

Karler et al. comparedthe anti-convulsive activity of THC and CBD through the maximal electric shocktest in mice. The results showed that the ED50 of the CBD (half effective dose)118mg/kg was very close to the ED50 of the THC (half effective dose) of 101 mg/kg.Both enantiomers of CBD have anti-spastic activity.

GW Pharmaceuticalspublished the result in the "New England Journal of Medicine" for itscannabidiol (CBD) liquid formulation called Epidiolex in the treatment of veryrare clinical stage III epilepsy called Dravet syndrome. After observation for4 weeks, the patient used CBD or placebo for 14 weeks. As a result, the numberof monthly seizure in the CBD group dropped from 12.4 to 5.9, while the placebogroup dropped from 14.9 to 14.1. 43% of CBD patients reduced half number ofseizure, and only 17% of placebo patients had same results. In addition, 5% ofCBD patients group had epilepsy syndrome disappeared after taking CBD, and theplacebo epilepsy patients group did not have completely controlled cases.GW hasanother phase III clinical trial of very rare epilepsy called Lennox-Gastaut(LGS) that is about to end.

GW announced that theywill apply for these two indications to be listed in the United States based onthese results.


     7:. Reducethe incidence of diabetes

In a study published inThe Journal of Pain Magazine in July2015, a small trial found that cannabis can reduce peripheral nerve pain indiabetic patients in a dose-dependent manner, confirmed that industrialcannabis CBD could help to reduce the incidence of diabetes

     8:Improve cardiovascular health

CBD also has ananti-oxidant effect against glutamate neurotoxin (stronger than ascorbate orvitamin E), and it is a potential antioxidant. In addition, CBD also hasanti-diazepam effect and anti-gram-positive bacteria; it is effective incontrolling dystonia and Meige's disease. The CBD analog called Δ6-CBD hasTHC-like activity.




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