CBD’s Mechanisms in the Body: How This Amazing Cannabinoid Keeps You Healthy

Chapter 2:

Cannabidiol (CBD) from hemp oil has taken center stage recently as a way to address many areas of health including supporting a healthy pain response in the joints and other areas of the body, dealing with occasional sleep problems and everyday stress, and supporting a healthy attention span, focus, and concentration, to name just a few of its benefits. (I summarized its health benefits in Table 1 of Chapter 1, and I’ll be talking more about those benefits as this book unfolds.) In June 2018, CBD ended up even more in the spotlight when the US Food and Drug Administration (FDA) approved the first CBD-based drug, Epidiolex®, for treatment of rare, severe epilepsy.

 

Is CBD the Answer to the Opioid Addiction Crisis?

Overuse of opioid drugs, which are highly addictive and lead to fatal overdoses, has hit epidemic proportions. Every day, 128 people in the United States die from an opioid overdose.¹

It’s estimated that 21% to 29% of people using opioids for chronic pain misuse these drugs.²

Not only are opioids potentially dangerous, but taking opioids can actually backfire. Sometimes a patient taking opioids for the treatment of pain could instead make the pain worse since they react even more to certain painful stimuli.³

This crisis has its origins in 1937, when German scientists at the IG Farben company first synthesized the opioid medication methadone to use for surgery-related pain. They claimed it was less addictive than morphine or heroin. However, this claim was clearly false. Methadone is longer-acting than morphine or heroin.⁴ It’s more addictive than these substances and causes withdrawal symptoms that last longer.⁴

Pharmaceutical companies began releasing new opioid painkillers including Vicodin^® (a combination of Hydrocodone Bitartrate and acetaminophen) in 1984, OxyContin^® in 1995, and Percocet^® (Oxycodone plus acetaminophen) in 1999.⁵ This led to an onslaught of opioid over-prescribing. After all, the pharmaceutical industry assured physicians that these medications were not addictive.¹

In 2007 came a turnaround point. Purdue Frederick Company Inc., an affiliate of Purdue Pharma, along with three of the company’s executives admitted to misbranding OxyContin^®. The company had made false statements about the drug, claiming it was less addictive than other opioids and that people taking it were less likely to abuse it. Purdue Frederick pleaded guilty to criminal charges and paid $634 million in fines.⁶

Clearly, we need another alternative to support a healthy pain response. And that alternative may very well be CBD, which does not produce a high and isn’t addictive. Later in this book, I’ll discuss CBD’s ability to support comfortable knee and hip joints, as well as promote a healthy pain response in the neck, back, and more. For now, let’s take a look at the way in which CBD can benefit so many areas of health.

 

How CBD Works

CBD has shown a lot of promise both in doctor’s offices and in studies.  But how does this hemp-derived cannabinoid work?

As a reminder, in Chapter 1, I covered CBD’s effects on CB1 and CB2 receptors and how CBD acts like a key that fits into those receptor locks. These receptors are part of what’s known as the endocannabinoid system, which plays a role in keeping us healthy, both physically and mentally. I also discussed the other receptors that CBD acts upon and explained that two main endocannabinoids produced in the body—anandamide (AEA) and 2-arachidonoylglycerol (2-AG)—activate these same receptors. A lot of what we know about CBD comes from what researchers have observed about the effects of AEA and 2-AG on the body.

In Chapter 1, I also delved briefly into the effects of an enzyme known as FAAH. This enzyme breaks down the endocannabinoid AEA. In doing so, it generally weakens AEA’s beneficial effects. AEA is sometimes called the “bliss molecule” since it plays an important part in maintaining a happy mood and staying optimistic. CBD can increase levels of AEA by blocking FAAH.⁷ Blocking FAAH may help support pain management and neurodegenerative health, maintain healthy levels of beta-amyloid proteins, and relieve occasional stress and frustration.^8-12 When people take opioids, they start to become tolerant to the drugs’ effects, so they have to take higher and higher doses for these medications to remain effective. Based on results of animal research, blocking FAAH may also stop this tolerance to opioids.¹³  

 

Meet MAGL

In this chapter, I am going to introduce another enzyme involved in the endocannabinoid system. It’s called monoacylglycerol lipase—MAGL for short. While FAAH breaks down the endocannabinoid AEA, MAGL breaks down AEA’s endocannabinoid sibling 2-AG.¹⁴ In animal studies, blocking MAGL maintains gastric health when taking non-steroidal anti-inflammatory drugs (NSAIDs).¹⁴ These type of drugs—such as aspirin and ibuprofen—are extremely damaging to gastric health and can cause ulcers. Patients with ulcerative colitis also have elevated MAGL levels, suggesting that in these people the endocannabinoid 2-AG is being broken down faster.¹⁵

Blocking MAGL also can strengthen the intestinal wall, possibly reducing leaky gut.¹⁴ This is a condition where weakened intestinal walls leads to the escape of food particles and inflammatory substances into the circulation. This can cause problems throughout the body. Leaky gut is linked to food intolerances, brain health, and much more. In fact, in my patients, I have noticed that resolving leaky gut leads to dramatic improvements in overall health.

CBD reduces MAGL’s ability to break down the endocannabinoid 2-AG.¹⁶  CBD’s ability to block MAGL’s actions may be part of the reason it can produce feelings of calm during occasional stress, promote a healthy gastrointestinal tract, and reduce cravings in people with addictions.^14,16,17 By blocking the enzymes FAAH and MAGL, CBD may protect the GI tract from the negative effects of NSAIDs since the GI damage caused by these medications is linked to FAAH and MAGL activity.^18,19

 

Beyond CBD’s Healthful Properties

CBD is the most talked about cannabinoid in hemp because it’s found in high levels. But hemp also contains other phytocannabinoids that are beneficial to health. These are found at much lower levels than CBD, but work together with CBD to provide synergistic benefits. And these other phytocannabinoids even have healthful properties on their own. One of these phytocannabinoids is cannabigerol (CBG). CBG is antibacterial and supports a healthy inflammatory response.^20,21 What’s more, it can promote well-being and happiness, thanks to its ability to increase the “bliss molecule” anandamide.²² 

CBG also promotes a healthy pain response, supports healthy cells in the colon and other areas of the body, and is neuroprotective.^22-25 In fact, CBG and CBD each have different neuroprotective effects, indicating they can work together to support brain and nervous system health in people with neurodegenerative concerns.²⁵ In addition, Cannabis with high levels of CBD and CBG inhibits the activity of the enzyme aldose reductase in human cell culture studies.²⁶ Blocking aldose reductase is involved in diabetic health.

Cannabinol (CBN) is another phytocannabinoid in hemp. In animal research, CBN teamed up with CBD to support comfortable muscles and temporomandibular health.²⁷

 

The “Hemptourage Effect”

Two decades ago, Doctors Mechoulam and Ben-Shabat proposed a concept known as the entourage effect.^28,29 Originally, it referred to the ability of certain endocannabinoid system components to boost the beneficial effects of the two most important actors in this system: anandamide and 2-arachidonylglycerol.²⁸

Today, the entourage effect is commonly used to refer to an interesting phenomenon: the ability of CBD to work together with its other minor components to produce even greater health benefits. The term “hemptourage effect” is now used to describe the potential synergistic interactions that take place between the CBD in hemp oil and hemp’s other constituents.

 

Terrific Terpenes

Substances in hemp that work together with CBD are called terpenes, which contain beneficial compounds known as terpenoids, the largest group of plant chemicals. Some of these terpenes are also found in cannabis and are responsible for its aroma. The table below shows some of the ways these terpenes can promote health.

 

Some Terpenes Found in Hemp and How They Benefit Health22,29
D-Limonene	• Also found in citrus fruits, d-limonene is relaxing. In rodent studies, it has increased brain levels of two hormones related to mood and happiness: serotonin and dopamine (DA). • Inhaling citrus fragrance improved mood in depressed human subjects. Nine of the 12 subjects were able to stop taking antidepressant medications. • D-limonene also supported healthy immunity.
Myrcene	• Supports a healthy inflammatory response and a healthy liver after exposure to toxins. • In rodent studies, acts like an analgesic and relaxes muscles. • Promotes relaxation and sleep.
D-Linalool	• Also found in lavender, linalool is calming.   • Acted as an anti-convulsant in rodents and inhibited seizures.   • Compared with a placebo, inhaling lavender decreased the use of morphine opioids in morbidly obese people who underwent gastric banding surgery.
α-Pinene	• α-Pinene is the most common terpenoid in nature. In addition to hemp, it’s found in conifer trees and other plant essential oils, where it acts like a natural insect repellant. • It supports a healthy inflammatory response. • A human study found it supported lung health by clearing the airways. • It supports cognitive function. This could mean it acts synergistically with CBD in counteracting the short-term memory problems caused by THC intoxication after marijuana use. • In a mouse study, essential oils that included pinene and limonene enhanced absorption of estrogen through the skin.
Nerolidol	• Also found at low levels in citrus fruit peels, nerolidol is calming. • A rodent study found it supports colon health. • It may also be able to stop fungal growth. • May weaken protozoan parasites such as malaria and leishmania.
Caryophyllene (Humulene)	• Also found in lemon balm (Melissa officinalis) and eucalyptus. • Serves as a natural insecticide and antifungal in plants. • May block fungal growth.  An 8% concentration eradicated a fungal infection in 15 days. • In cell culture research, it stopped blood platelets from sticking together. • Reduced paw swelling in rodents given an inflammatory substance.
Phytol	• Present in hemp extracts through the breakdown of chlorophyll and tocopherol. • Leads to relaxation thanks to its ability to raise levels of the calming neurotransmitter GABA. It blocks an enzyme responsible for breaking down GABA.
beta-Amyrin	• Supports a healthy inflammatory response and the body’s response to unwanted microorganisms and fungus.

 

Teaming Up with Terpenes

Many terpenes found in hemp may work together with CBD and other phytocannabinoids in hemp. In fact, many terpenes have complimentary actions to CBD. Take a look at the table below to get an idea how these terpenes work together with other components of hemp oil. Since this is such a large topic, I’ll devote a chapter to terpenes later on in the book.

 

How Terpenes Work Together with Other Hemp Components22
Limonene + Linalool + Pinene + CBD	• CBD reduces the increased sebum production linked to acne.   • Limonene was more effective at suppressing Propionibacterium acnes, an acne-related pathogen, compared with triclosan. Linalool and limonene are known to reduce markers of P. acnes-related inflammation.   • Pinene suppresses  P. acnes and Staph spp. • CBD supports cognitive function in people exposed to THC from cannabis, which is known to affect memory.  In cell culture, CBD also reduces formation of beta-amyloid proteins. Low levels of beta-amyloid is linked to a healthy memory during aging.  Limonene, pinene, and linalool likely work with CBD to support cognitive health through their ability to improve mood. • Pinene also improves mental focus, thus acting synergistically to CBD’s ability to support a sharp memory.
Pinene + CBD + CBG	• Pure CBD and CBG blocked methicillin-resistant Staphylococcus aureus (MRSA) in a structure-activity study. This type of study looks at the link between a substance’s chemical structure and its actual biological activity against a microorganism.   • High-pinene essential oils were also effective against MRSA and other antibiotic-resistant bacteria.
Limonene + linalool + CBD	• CBD is calming and reduces everyday stress.  Researchers have proposed that using limonene and linalool with CBD could add to CBD’s relaxing effects since both of these terpenes are also very calming.

 

Hemp’s Powerful Health Benefits

Now that I’ve discussed the mechanisms involved in the beneficial effects of CBD and other components of hemp, in the chapters that follow I’ll go into detail about the specific ways CBD from hemp oil can make you feel happier and healthier.

 

References:

 

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