15. ORTHOMOLECULAR Flashcards
This module covers:• The dietary sources, bioavailability and interactions of orthomolecular compounds and medicinal mushrooms.• The therapeutic uses and safety considerations.• Appropriate dosage levels and preferred forms for orthomolecular compounds and medicinal mushrooms. (100 cards)
1
Q
What nutrient is reduced by the statin group of pharmaceutical drugs and why does this happen?
A
CoQ10.
Statins are drugs used to reduce cholesterol synthesis through the inhibition of (HMG CoA reductase and) the Mevalonate Pathway. But they also reduce CoQ10 because both compounds are synthesised via this metabolic pathway.
Slide 12-13
2
Q
Why is Alpha Lipoic Acid so effective as an antioxidant?
A
- ALA is referred to as ‘universal antioxidant’ since it functions in a fat-soluble and water-soluble environment. Exogenous forms scavenge free radicals intra- and extra-cellularly.
- Furthermore it can regenerate other antioxidants such as vitamin E, C, glutathione and CoQ10. It also up-regulates the expression of glutathione.
19
3
Q
What are THREE key ways that chondroitin
protects cartilage?
A
Chondroitin protects cartilage from degradation by:
- Reducing degradative enzymes.
- Decreasing inflammation — reduces inflammatory intermediates such as COX-2. This is also seen by reductions in the inflammatory marker ‘CRP’.
- Increasing hyaluronic acid synthesis, thereby enhancing joint lubrication.
4
Q
Outline TWO ways that N-acetyl glucosamine can be of benefit for IBD.
A
- NAG supports the GI epithelial barrier by enhancing mucin functionality, which is dramatically altered in those with IBD. Mucins are a group of proteins found in mucus that form a barrier and prevent microbial overgrowth.
- NAG also reduces biofilm formation associated with IBD.
5
Q
Briefly explain why betaine (TMG) can reduce the risk of cardiovascular disease.
A
TMG serves as a methyl donor, facilitating the conversion of homocysteine to methionine.
(Elevated homocysteine is a risk factor for CVD, so betaine can be used therapeutically to support vascular endothelial health and prevent atherosclerosis.)
6
Q
Outline TWO ways in which phosphatidylserine is beneficial for Alzheimer’s disease.
A
- Phosphatidylserine reduces hippocampal inflammation.
- It also reduces acetylcholinesterase thereby increasing the availability of the neurotransmitter acetylcholine which is vital for memory and information processing.
Other options:
- Increases other neurotransmitters such as noradrenaline, serotonin and dopamine.
- It has been found to preserve glucose metabolism during Alzheimer’s disease.
- Increases cognitive function (including non- Alzheimer’s related cognitive decline) and memory
7
Q
Who coined the term ‘orthomolecular’?
What are orthomolecular compounds?
Give two examples
A
Linus Pauling coined the term ‘orthomolecular’ in the 1960s to mean “the right molecules in the right
amounts” (ortho- in Greek implies ‘correct’).
- Orthomolecular compounds are highly beneficial for health, and although they are naturally synthesised by the body, additional amounts can be sourced from the diet or from supplementation.
- These compounds do not fit into the category of other nutrients such as vitamins or minerals.
- Examples of orthomolecular compounds include: CoQ10, alpha-lipoic acid, glucosamine and chondroitin sulphate.
8
Q
What is accelerated aging caused by?
How might you slow it down or reverse it using orthomolecular therapy?
What else might you consider?
A
The ageing process is typically accelerated as a result of free radical exposure, chronic inflammation and toxic exposure.
- Reversing or slowing it down is one goal of orthomolecular therapy.
This might involve using CoQ10, ALA or antioxidants. - Be sure to address an individual’s overall diet and lifestyle with the guidance of core naturopathic nutrition principles. Supplements alone will not single-handedly support healthy ageing.
9
Q
Where can Coenzyme Q10 be found in the human body?
What role does it play?
What form does it exist in?
What reduces CoQ10?
A
Coenzyme Q10 (CoQ10) is present in each cell’s mitochondria and plays a key role in ATP production.
- CoQ10 is also known as ubiquinone.
- It exists in the body in an oxidised form (ubiquinone) and a reduced form (ubiquinol) and the two forms interconvert.
- It is usually synthesised in the body in sufficient amounts to meet physiological requirements.
- CoQ10 is reduced by: Ageing, drugs (e.g. statins), smoking and certain diseases (e.g. cardiovascular disease).
10
Q
Name 3 plant sources of CoQ10
Name 3 animal sources of CoQ10
How much CoQ10 is lost if food is fried?
A
Dietary intake contributes around 3 to 6 mg per day.
Food sources:
- Plant sources: Nuts (e.g. peanuts, pistachios), sesame seeds, olive oil, fruit and vegetables including oranges, strawberries, avocado, broccoli, cauliflower,
- Animal sources: Meat, poultry, fish (e.g. herring, sardines, mackerel, trout) and eggs
Approx. 14%‒32% of CoQ10 is lost if foods are fried.
11
Q
Why is CoQ10 useful in energy production?
A
- CoQ10 is needed for the electron transport chain (for complex 2 of 4 in this process) — review biochemistry.
This supports mitochondrial function and energy production. - The highest quantities are found in muscle cells (including skeletal and cardiac muscle) due to the high ATP demand for muscle contraction.
- Therapeutic uses: Fatigue, Fibromyalgia. Daily use (300 mg in divided doses; i.e. 3 x 100
12
Q
List 3 ways that CoQ10 is useful as an antioxidant and give one therapeutic use for CoQ10 as an antioxidant.
A
- CoQ10 is a potent fat-soluble antioxidant that inhibits the peroxidation of cell membrane lipids. It neutralises free radicals produced by mitochondria.
- CoQ10 naturally decreases with age; the ageing process involves ROS and impaired mitochondrial function.
- Depletion of CoQ10 can result in mitochondrial dysfunction, which is associated with conditions including fibromyalgia, Type 2 diabetes, CVD, neurodegenerative diseases and cancer.
Therapeutic Uses:
* Healthy ageing: 100–200 mg per day.
* Preventative measures or for directly addressing mitochondrial dysfunction (e.g. fibromyalgia etc.)
13
Q
Name a ways that CoQ10 is useful for periodontal health
Name a therapeutic use for CoQ10 in periodontal health
A
Periodontal health
* Diseased gum tissues have significantly lower levels of CoQ10 in comparison with healthy gum tissue. This is thought to be a result of the lipopolysaccharides from the bacteria Porphyromonas gingivalis, triggering oxidative stress and mitochondrial dysfunction.
Therapeutic Uses:
* Periodontitis. Daily 50–80 mg
* Combine with periodontal care routine.
14
Q
Name 2 ways that CoQ10 is useful for male & female fertility
What would a therapeutic dose of CoQ10 be for male & female fertility?
A
Male fertility
* CoQ10 protects sperm from oxidative stress (to which they are vulnerable).
* 200–300 mg for 6 months increases sperm health.
Female fertility
* Impaired mitochondrial performance (low CoQ10) can drive age-associated oocyte (egg cell) deficits and lead to infertility.
* 100–600 mg for ovarian health.
15
Q
Name 3 ways that CoQ10 is useful for cardiovascular health
What would a therapeutic dose of CoQ10 be for cardiovascular health?
A
Cardiovascular health
* Crucial for cardiac muscle function.
* Protects against endothelial dysfunction and hence atherosclerosis.
* CoQ10 reduces LDL oxidation.
* It inhibits the NF-kB activation that is secondary to ROS.
* Increases superoxide dismutase activity (an anti-oxidant) which is known to preserve the activity of nitric oxide (NO) as a potent vasodilator.
* Hypertension, angina pectoris, congestive heart failure, post myocardial infarction.
- Typical dosage: 60–300 mg / day.
NF-κB = a protein that controls inflammatory cytokine production
16
Q
How do statins and CoQ10 interact?
What are the risks of low CoQ10 levels?
A
Statins and CoQ10:
* Statins are drugs used to reduce cholesterol synthesis but they also reduce CoQ10 because both compounds are synthesised via the same pathway.
* Cholesterol and CoQ10 have vital functions in the body and their loss contributes to the adverse effects caused by statins.
- Low CoQ10 levels increase the risk of various illnesses including cardiovascular disease, myopathy and depression.
- 90–300 mg / day of CoQ10 greatly reduces this risk
17
Q
Describe the Mevalonate Pathway.
A
The Mevalonate Pathway:
* This metabolic pathway is required for the production of cholesterol and CoQ10 — two crucial molecules for health.
* Statins act on this pathway
Acetyl-CoA → HMG-CoA → (HMG-CoA reductase inserts here & is inhibited by statins) → Mevalonic acid → Cholesterol OR → CoQ10
(Check slide 13 for image)
18
Q
There is a debate about which is better, ubiquinol or ubiquinone, describe.
A
It is suggested that ubiquinol is a better supplemental form for CoQ10 status enhancement than ubiquinone. However:
* Results are mixed with very little research supporting this claim.
* Bioavailability is influenced more by the composition of the raw material, which for supplemental purposes is generally synthesised using a yeast-fermentation method.
* This produces a crystalline form which is difficult to digest.
* The crystals needs to be dissociated into individual CoQ10 molecules and remain in the shelf-life of the product.
* Thus solubilised products appear to have the greatest bioavailability.
19
Q
What is the safety profile of supplementing with CoQ10?
What are the adverse effects of supplementing with CoQ10?
Are there any drug interactions with CoQ10?
A
Supplementation:
* Safety: CoQ10 has a remarkable safety profile. There have been no reports of significant adverse side effects of oral CoQ10 supplementation at doses as high as 1200 mg / day for up to 16 months. There have been no safety studies in pregnant and lactating women.
- Mild adverse effects: GIT symptoms such as nausea, diarrhoea, appetite suppression, heartburn, and abdominal discomfort have been reported. These may be minimised if daily doses higher than 100 mg are divided into two or three doses.
- Interactions: CoQ10 may decrease the effects of warfarin.
20
Q
What is Alpha lipoic acid (ALA)?
How is it also known?
Do humans synthesise enough alpha lipoic acid to meet basic needs?
A
Alpha lipoic acid (ALA) is an organosulphur compound that is synthesised by plants and animals, including humans. ALA is a naturally-occurring, short-chain fatty acid.
- ALA is also known as ‘α-lipoic acid’ or ‘lipoic acid’ (LA).
- There are two forms of ALA: R-form (natural) and S-form (synthetic). The R-ALA variant is nearly 10 x more potent.
- It is thought that humans generally synthesise enough to meet basic needs.
- However, additional ALA in the form of supplementation has clear therapeutic benefits in certain health conditions.
21
Q
Name 2 plant sources of Alpha lipoic acid (ALA)
Name 2 animal sources of Alpha lipoic acid (ALA)
A
Food sources:
* Found in a wide variety of foods.
* Plant sources: Brassicas (e.g. broccoli, Brussel sprouts), spinach, potato, carrots, beets, tomatoes, peas, brewer’s yeast.
* Animal sources: Red meat (lamb, beef) and organ meats.
22
Q
Which characteristics of Alpha Lipoic acid (ALA) has earned it the the title of ‘universal antioxidant’?
Give 2 therapeutic uses for ALA as an antioxidant.
A
- ALA is a potent antioxidant that can be produced within the body and functions in both a fat-soluble and water soluble environment. It is anti-inflammatory.
- Exogenous forms (from food and supplements) scavenge free radicals intra- and extra-cellularly.
- It can regenerate other antioxidants such as vitamin E, C, glutathione and CoQ10. It also up-regulates the expression of glutathione.
- Improves the motility of spermatozoa and provides antioxidant protection
Therapeutic uses:
* Infertility (600 mg daily)
* Diabetes, diabetic neuropathy
* Alzheimer’s disease — slows the cognitive decline (600 mg daily for one+ year).
* Multiple sclerosis.
* Healthy ageing.
23
Q
Why would Alpha lipoic acid (ALA) be useful for a client with diabetes?
A
ALA supplementation improves insulin sensitivity, insulin resistance, fasting blood glucose and HbA1c which are all markers of diabetes severity. Diabetes mellitus: 300–1200 mg per day.
24
Q
How is Alpha lipoic acid (ALA) useful for metal chelating
In which pathologies would this be useful?
A
ALA can chelate iron, mercury, copper, lead and zinc.
Therapeutic uses:
* Infertility.
* Alzheimer’s.
* Peripheral neuropathy.
25
How is Alpha lipoic acid (ALA) useful for peripheral neuropathy?
* ALA supplementation reduces oxidation of the myelin sheath.
* ALA improves neuropathic sensory symptoms including pain, burning, numbness, prickling of the feet and legs.
* Dosage: 600 mg per day.
26
How is Alpha lipoic acid (ALA) useful for weight loss?
ALA is thought to promote weight loss via various mechanisms:
* Reducing the oxidative stress that promotes fat storage.
* Suppressing appetite and hence food intake through its influence on the enzyme ‘AMPK’ (AMP-activated protein
kinase) in the hypothalamus (where appetite is regulated).
* Increasing energy expenditure and reducing fat synthesis.
* Dosage: 1800 mg daily.
27
When supplementing with Alpha lipoic acid (ALA) how should supplements be taken?
Are there any adverse effects to be aware of?
What are the drug interactions with ALA?
Supplementation:
* Supplements should be taken on an empty stomach to optimise bioavailability, i.e. one hour before, or two hours after food.
* Rare adverse effects: Allergic reactions affecting the skin (rashes, hives) and GI symptoms (abdominal pain, diarrhoea).
Interactions:
- Biotin and ALA may compete for transport across cell membranes due to similar chemical structures.
Be mindful of biotin deficiency when using high doses of ALA.
- Increased risk of hypoglycaemia in medicated diabetic patients due to additive effect. Monitor blood glucose closely.
28
What is glucosamine?
Where is glucosamine found in high concentrations in the human body?
Glucosamine is an amino sugar naturally present in most body tissues, with high concentrations in joints and cartilage.
* Glucosamine is required for the synthesis of glycoproteins, glycolipids, and glycosaminoglycans (GAGs), also known as mucopolysaccharides.
* These compounds are an important structural component of tendons, ligaments, cartilage, synovial fluid, mucous membranes and structures in the eye, blood vessels and heart valves.
29
Name 2 supplemental forms of glucosamine
Glucosamine can be supplemented in two different forms.
All supplemental forms are highly bioavailable.
* Glucosamine-6-Phosphate (G6P) and N-Acetyl-Glucosamine (NAG) are naturally present within the human body.
- NAG is converted to hyaluronic acid (HLA) as needed. HLA is an important component of synovial fluid.
* Glucosamine sulphate is sourced from marine exoskeletons (so not suitable for vegetarians, vegans and those with seafood allergies). It appears to be absorbed better and hence result in higher tissue concentrations. Sulphate is
found in synovial fluid and is required for GAG synthesis.
* Glucosamine hydrochloride is created synthetically from corn.
30
Name 3 ways that glucosamine is useful for osteoarthritis
* Stimulates metabolism of chondrocytes in the articular cartilage and synovial cells in the synovial tissue. This slows joint degeneration and prevents joint space narrowing.
* Decreases inflammation by inhibiting the formation of cytokines such as interleukin-1.
* Pain reduction is comparable to NSAIDS. NSAIDS provide relief after two weeks compared to four to eight weeks for glucosamine sulphate.
* Less effective for severe, long-standing osteoarthritis.
* More effective combined with chondroitin and MSM.
* Dosage: 1500 mg daily or in three divided doses.
31
How is glucosamine useful in IBD?
NAG supports the GI epithelial barrier by enhancing mucin functionality, which is dramatically altered in those with IBD. Mucins are a group of proteins found in mucus that form a barrier and prevent microbial overgrowth.
* NAG also reduces biofilm formation associated with IBD.
* NAG can be also used in intestinal permeability.
* Dosage: 3–6 g daily for children; 6 g daily for adults in three divided doses. Administered orally or rectally.
32
When supplementing with glucosamine what precautions should be taken?
Are there any adverse effects to be aware of?
What are the drug interactions with glucosamine?
Supplementation:
* Caution: Glucosamine supplements can be synthesised in the laboratory, however most are produced from the shells of crustaceans — so can be problematic for those with a seafood allergy.
* Mild adverse effects: GIT symptoms such as nausea, heartburn, diarrhoea, constipation as well as drowsiness, skin reactions and headaches.
* Interactions: Potential increase in the anticoagulant effect of warfarin, leading to increased risk of bleeding and bruising.
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33
What is chondroitin sulphate?
Where can it be found in the human body?
Chondroitin sulphate is a type of glycosaminoglycan (GAG).
* It is a major component of the extracellular matrix of many
connective tissues. Most notably, this includes cartilage and joint connective tissue.
* Chondroitin provides resistance to compression, partially by thickening synovial fluid.
34
How is chondroitin sulphate useful for osteoarthritis?
Protects cartilage from degradation by:
- Reducing degradative enzymes.
- Decreasing inflammation — reduces inflammatory intermediates such as COX-2. This is also seen by reductions in the inflammatory marker ‘CRP’.
- Increasing hyaluronic acid synthesis — enhancing joint lubrication.
* Dosage: 200–400 mg two to three times a day or 1000–1200 mg daily as a single dose.
35
When supplementing with chondroitin sulphate what precautions should be taken?
Are there any adverse effects to be aware of?
What are the drug interactions with chondroitin sulphate?
Supplementation:
* Supplemental chondroitin is usually well tolerated. Studies show that people absorb only 8–18% of orally-administered chondroitin.
* Safety: There is some concern that chondroitin might exacerbate asthma. Patients with asthma tend to have higher concentrations of chondroitin antibodies in the airway compared to people without asthma.
* Interactions: Potential increase in the anticoagulant effect of warfarin, leading to increased risk of bleeding and bruising
36
What is methyl sulfonylmethane (MSM)?
Name 2 plant sources of MSM
Name an animal source of MSM
Methyl sulfonylmethane (MSM) is a source of sulphur used by plants to create the amino acids, cysteine and methionine. These amino acids are a dietary source of sulphur.
* Plant food sources: Green leafy vegetables, alfalfa sprouts, algae, fruits, vegetables, and grains.
* Animal sources: Milk (cows).
37
How is MSM useful for osteoarthritis?
* Alone or in combination with glucosamine / chondroitin, it can reduce pain and swelling and improve joint function.
* General anti-inflammatory properties by inhibiting the secretion of cytokines (IL-6 and TNF-α) and COX-2.
* Sulphur is a component of cartilage and so exerts a protective effect on cartilage.
* Dosage: 500 mg three times a day.
38
How is MSM useful for cardiovascular health?
* MSM reduces homocysteine levels (by donating methyl groups) and reduces lipid peroxidation.
* This protects the vascular endothelium from damage.
* Dosage: 3 g per day (benefits observed at 28 days).
39
How is MSM useful for tissue repair?
* Decreases oxidative stress and inflammation which helps to repair GI mucosal injury and ↓ chronic GI inflammation.
* Supports tissue healing after an injury (including the skin).
* Can be applied topically to affected skin.
* Dosage: 2 g two to three times daily.
40
How is MSM useful as an immune modulator?
* The immune-regulating and antioxidant properties of MSM make it useful for seasonal allergies and ↓ inflammation.
* Studies show that MSM inhibits NF-κB activity, downregulating inflammatory cytokines.
* Dosage: 2.6 g per day for seasonal allergies
41
When supplementing with MSM what precautions should be taken?
Are there any adverse effects to be aware of?
Are there any drug interactions with MSM?
Supplementation:
* Generally recognised as very safe. Well tolerated up to 4g per day in most patients.
* Mild adverse effects: GIT symptoms such as nausea, diarrhoea and bloating. Other symptoms include headache, difficulty concentrating and insomnia.
* Interactions: None
42
What is betaine (trimethyl glycine (TMG)?
What is betaine's mode of action?
Why is homocysteine important?
The chemical form of betaine is trimethyl glycine (TMG) and it occurs naturally in the body. TMG can be formed from choline (tetramethyl glycine).
* TMG serves as a methyl donor, facilitating the conversion of homocysteine to methionine.
* Elevated homocysteine is a risk factor for cardiovascular disease, so betaine can be used therapeutically to support vascular endothelial health and prevent atherosclerosis.
Homocysteine:
* A biomarker of cardiovascular disease risk, and an indicator of how well an individual is methylating.
* Optimal blood levels are below 9 μmol / L, excess of 14 μmol / L is linked to a high risk of health concerns.
43
Name 2 plant sources of betaine
Name 2 animal sources of betaine
Betaine food sources:
* Plant sources: Beets (1–2 cups per day i.e. 250–500 ml per day), wheat bran, quinoa, spinach, sweet potato.
* Animal sources: Seafood, turkey.
44
How is betaine useful in cardiovascular health?
Name 2 therapeutic uses for betaine
Homocysteine can be remethylated to methionine by betaine-homocysteine methyltransferase (BHMT). This enzyme uses betaine as a methyl donor.
Therapeutic uses:
* Cardiovascular disease (i.e. atherosclerosis).
* Alzheimer’s.
* Dosage: 6 g daily (3 g twice per day).
* For best results pair with 1 mg of folate daily.
45
How is betaine useful for skeletal muscle performance?
* Reduces fat mass and increases muscle mass.
* Improves muscle endurance, body composition, arm size and bench-press work capacity.
* Dosage: 2.5 g daily.
46
How is betaine useful for fatty liver disease?
* Betaine has shown that it can improve liver function in those with non-alcoholic fatty liver disease.
* This has been shown by a reduction in liver enzymes, liver size and abdominal pain.
* Dosage: 3 g twice daily.
47
What is dimethyl glycine (DMG)?
Dimethyl glycine (DMG) is trimethyl glycine (betaine) after it has donated one methyl group during the methylation of homocysteine and only exists for seconds at a time.
48
How is DMG useful for autism?
*In 50% of cases, DMG improves behaviour, eye contact, frustration tolerance and speech. Reduces seizures.
* Preschool age: 65 mg daily with breakfast.
* Older children: 125 mg daily.
* Gradually increase dose to 500 mg for a child and 250–1000 mg for an adult.
* Initial increase in hyperactivity is possible — ↓dose.
* DMG is better tolerated than TMG for autistic patients.
49
What is Phosphatidylserine (PS)?
Where is it most abundant in the human body and what role does it play?
Name 2 food sources of PS
Phosphatidylserine (PS) is the most abundant fat-soluble phospholipid in the human brain.
* It is important in neuronal membrane functions such as maintenance of the cell's internal environment, secretory vesicle release, cell-to-cell communication, and cell growth regulation.
* Although the body is able to synthesise phosphatidylserine, it requires substantial energy expenditure.
* Food sources: White beans, whole grain barley, carrots, mackerel, herring, organ meats
serine = an amino acid
50
How is Phosphatidylserine (PS) useful for Alzheimer’s disease?
* Improves neuronal membrane functioning.
* Increases acetylcholine, norepinephrine, serotonin and dopamine.
* Has been found to preserve glucose metabolism during Alzheimer's disease, and also reduce acetylcholinesterase activity and hippocampal inflammation.
* Increases cognitive function (including non- Alzheimer’s related cognitive decline) and memory.
* More effective in patients with less severe symptoms.
* Dosage: 300 mg daily or 100 mg three times a day
51
How is Phosphatidylserine (PS) useful for depression?
*Improves mood through its effects on cortisol regulation.
* Dosage: 100 mg three times a day.
* More effective when combined with fish oil.
52
How is Phosphatidylserine (PS) useful for ADHD?
* Promotes attention and reduce symptoms of ADHD, and increases short-term memory.
* Dosage: 200 mg daily.
53
How is Phosphatidylserine (PS) useful for stress and insomnia?
* PS dampens the effects of prolonged cortisol secretion on brain function — allowing for better quality sleep and decreased anxiety.
* Dosage: 400 mg before bed for insomnia.
* Dosage: 200 mg daily for stress.
54
What is the safety profile of Phosphatidylserine?
What are the drug interactions of Phosphatidylserine?
Supplementation:
* Safety: Generally recognised as safe. Has been safely used in studies for up to six months.
* Interactions: Possible additive effects when combined with cholinergic drugs which also increase acetylcholine.
* May decrease effectiveness of anticholinergic drugs.
55
What is Phosphatidylcholine (PC) ?
Name 2 plant sources of Phosphatidylcholine (PC)
Name 2 animal sources of Phosphatidylcholine (PC)
Phosphatidylcholine (PC) is a major structural component of cell membranes, maintaining their integrity and fluidity.
* It is synthesised from dietary choline or through the methylation of another phospholipid — phosphatidylethanolamine.
* While the body can synthesise a small amount of choline, dietary intake is essential to meet body demands — about 95% of body tissue stores of choline are found in PC.
PC food sources:
* Plant sources: Nuts, peanuts, wheatgerm, Brussels sprouts, broccoli, spinach, peas.
* Animal sources: Eggs, fish, beef, chicken, pork, liver.
56
How is Phosphatidylcholine (PC) useful for liver health?
*Prevents fat accumulation in the liver and is hepatoprotective reducing chemical and oxidative damage.
* Consider for non-alcoholic fatty liver disease, alcoholic hepatic steatosis, drug-induced liver damage and hepatitis.
* Dosage: Minimum 800 mg daily.
57
How is Phosphatidylcholine (PC) useful for neurological health?
* PC has a neuro-protective role as an essential component of neuronal membranes and supplies choline for the synthesis of the neurotransmitter acetylcholine.
* Acetylcholine is a neurotransmitter involved in memory and is protective against cognitive decline and dementia.
* Dosage: 1–9 grams / day in divided doses
58
How is Phosphatidylcholine (PC) useful for ulcerative colitis?
* PC plays an important role in establishing a protective
mucosal barrier and forms a vital part of intestinal mucus.
* Incorporates into enterocyte membranes to influence
signalling cascades and reduce inflammation.
* Dosage: 1–6 g daily in divided doses.
59
What adverse reactions should you be aware of with Phosphatidylcholine (PC)?
What are the drug interactions of Phosphatidylcholine (PC)?
Supplementation:
* Mild adverse effects: Gastrointestinal symptoms.
* Interactions: Possible additive effect when combined
with cholinergic drugs which increase acetylcholine.
* May decrease effectiveness of anticholinergic medications.
60
What is Myo-inositol?
What is it's role in the human body?
Name 2 plant sources of Myo-inositol
Myo-inositol is the most predominant of nine different stereoisomer forms of inositol, a six-carbon sugar alcohol. It accounts for over 90% of cellular inositol.
* Myo-inositol provides structure to body cells, acts as an intracellular second messenger and regulates a number of hormones including insulin.
* It is synthesised in the body and can also be obtained in the diet.
Food sources:
* Plant sources: Whole grains, beans, fresh fruit (e.g. prunes, melon, oranges) and vegetables (e.g. okra, aubergine)
* Animal sources: Grass-fed meats, eggs.
stereoisomer = two or more compounds that only differ in the configuration of their atoms
61
How is myo-inositol useful for PCOS?
* PCOS is characterised by insulin resistance and ↑ androgens.
* Myo-inositol improves insulin sensitivity as it is a secondary messenger of insulin signalling and promotes mobilisation of GLUT4 vesicles.
* It increases SHBG to reduce bioavailable testosterone.
* Also improves menstrual cycle regularity, oocyte quality
and overall female fertility.
* Dosage: 2–3 g daily. It should be used with folate.
62
How is myo-inositol useful for T2D?
* It improves the ability of cells to respond to insulin and helps regulate blood glucose.
* Dosage: 4 g daily.
63
How is myo-inositol useful for anxiety and depression?
* Inositol is linked to a number of CNS receptor signalling systems in the CNS, including the neurotransmitters serotonin and dopamine.
* Decreases anxiety symptoms and panic attack frequency.
* Decreases depression symptoms including that associated with PMS.
* Dosage: 12–18 g daily.
64
What is the safety profile of myo-inositol?
Supplementation:
* Safety: Generally well tolerated up to 12 g. About 5%
incidence of mild GI symptoms observed at higher doses.
* No adverse effects noted when used in pregnancy (up to 4 g).
65
What is Mycotherapy?
How many species are there and how many are considered medicinal?
The kingdom Fungi is one of the seven kingdoms of living
organisms. About 20,000 of fungal species are mushrooms,
with around 1000 of them considered medicinal.
* Mycotherapy is the use of mushrooms and their compounds as medicines or health-promoting agents.
* Fungi are believed to have survived the meteor hits that extinguished many other species, and helped to renew the planet.
* Fungi create a mycelial (root-like) network that releases enzymes and acids to externally digest dead organisms. They move the nutrients back into the life cycle (i.e. into soil).
* Fungi compensate for their inability to move by growing quickly and branching their filaments and threads in any direction
66
What are Beta-glucans?
What are they useful for?
Medicinal mushroom compounds:
* Medicinal mushrooms produce compounds that can be harnessed therapeutically. The most useful medicinal compounds are:
Beta-glucans:
* Beta-glucans are polysaccharides that sometimes contain protein.
* 1,3 and 1,6 beta-glucans are the most common forms.
* Their most important action on the body is on the immune system, where they can support optimal immune function, promote immunomodulation and exert anti-tumour activity.
* They are captured by various cells in the lymphatic tissue of the intestines and stimulate macrophages, neutrophils, monocytes, natural killer (NK) cells and dendritic cells.
67
What are Triterpenes?
What are they useful for?
Triterpenes:
* Mushrooms such as reishi are composed of over 120 different triterpenes which have various medicinal properties, e.g. hepato-protective, anti-tumour.
68
What are Sterols (with regard to mushrooms)?
What are they useful for?
Sterols:
* Mushrooms contain sterols such as ergosterol (a precursor of vitamin D). Studies have shown that these mushroom-derived sterols can have anti-cancer properties.
69
What are Lectins (with regard to mushrooms)?
What are they useful for?
Lectins:
* Those in certain medicinal mushrooms agglutinate tumour cells, preventing their proliferation. They are also immune-modulatory.
70
What are the drug interactions when using medicinal mushrooms?
Medicinal mushrooms and drug interactions.
* Research has explored the possible interactions of the most common medicinal mushroom strains with drugs that are metabolised by CYP450 enzymes.
* The results have highlighted that the mushrooms demonstrate no appreciable inhibition, and so the possibility of a drug interaction by inhibition of CYP450 is extremely unlikely.
* This means that unless there is an interaction via another mechanism, the medicinal mushrooms covered can be used alongside other drug treatments.
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What is Reishi also known as?
How is considered in TCM?
What are the important constituents of reshi?
Reishi is referred to as “the mushroom of eternal youth” and has been used for over 2000 years in the traditional medical systems of China, Japan, Korea and other Asian countries for its
health-promoting effects.
* It is considered a ‘tonic’ in Chinese medicine, or an ‘adaptogen’ in Western medicine.
* Important constituents include primarily polysaccharides (e.g. beta-glucans) and triterpenes (ganoderic acids), but also lectins, sterols and B vitamins.
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Reshi is immune boosting, describe why
Reshi is antiviral, describe why
Immune boosting
* Increases the number and activity of numerous immune
cells including T-lymphocytes, macrophages and NK cells.
Antiviral
* The triterpenes inhibit the replication of the Epstein-Barr
and hepatitis B viruses.
* They also inhibit reverse transcriptase in HIV.
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Reshi has anti cancer properties, describe why
*It induces apoptosis (programmed cell death) in cancer cells and inhibits angiogenesis.
* Evidence suggests it can inhibit tumour metastases by limiting attachment to endothelial cells.
* The beta glucans strengthen the immune system contributing to its anti-cancer properties.
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Reishi has anti inflammatory properties, describe
Reishi has anticoagulant properties, describe
Anti inflammatory
* Triterpenes provide an anti-inflammatory (reduces the activity of NF-kB) and anti-histamine action. The anti inflammatory and antioxidant properties of reishi are thought to provide it with its healthy ageing properties.
Anticoagulant
* Ganoderic acids inhibit platelet aggregation, thinning the blood. Supportive in cardiovascular disease.
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Reshi is useful for benign prostatic hyperplasia, describe why
Reshi is useful for stress and sleep, describe why
Benign prostatic hyperplasia
* It is a 5α-reductase inhibitor meaning that it blocks the conversion of testosterone to dihydrotestosterone (DHT), preventing abnormal prostate growth.
Stress and sleep
* Triterpenes have a sedative action and calm nervous system activity, supporting sleep and relaxation.
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Reshi is useful for blood sugar regulation, describe why
Blood-sugar regulating
* Ganoderic acids increase insulin secretion and decrease cellular resistance to insulin.
* Useful in cases of insulin resistance such as Type 2 diabetes and PCOS.
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What would be a sensible starting dose of Reishi?
What are the drug interactions with Reishi?
Reishi dosage range: 3–9 g / day (doses of up to 15 g / day are used in some circumstances). Start at the lower of the dosage range and gradually increase with tolerance. Use as a powder in food, tea or capsules for higher dosages. It is a bitter, woody-tasting mushroom that is considered non-edible.
* Reishi interactions: Combining high dose reishi with anticoagulant drugs may increase the risk of bleeding.
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Describe Shiitake mushrooms, what are the important constituents?
Large scale Japanese studies have been conducted and have confirmed significant anti-cancer activity from a licensed pharmaceutical drug, what is it called?
How are shiitake used in TCM?
Shiitake is a common edible mushroom. Its Japanese name comes from the words ‘shii’ (species of chestnut) and ‘take’ (mushroom), since it grows on chestnut wood.
- Important constituents include the beta-glucan Lentinan, choline, zinc, provitamin D, iron, B vitamins and unsaturated fatty acids.
- Large-scale clinical trials have confirmed significant anti-cancer activity from Lentinan.
- Lentinan (injected) is a licensed pharmaceutical in Japan and is the third most widely prescribed anti-cancer ‘drug’ in the world today.
- In Traditional Chinese Medicine (TCM), shiitake is used to replenish Qi and nourish the blood.
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How are shiitake immune modulating?
Immune modulating
* Increases phagocytes, T-lymphocytes and NK cells.
* Increases interferon synthesis (anti-viral proteins).
* These properties are useful for general immune support, immune support in cancer patients and HIV.
* Shiitake is also a good anti-candida agent.
* Has antibacterial activity on bacteria resident in the oral cavity that cause gingivitis and periodontitis.
Also prevents dental plaque formation.
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How are shiitake useful for cardiovascular disease?
Cardiovascular diseases
* Shown to lower LDL by increasing faecal excretion, and increase HDL levels.
* Inhibits platelet aggregation and is anti-thrombotic.
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How are shiitake useful in the treatment of cancer?
How is shiitake useful in the treatment of gout?
How is shiitake useful in the treatment of benign prostatic hyperplasia
Cancer
* Shiitake is anti-proliferative and anti-angiogenic.
* Studies have demonstrated life-prolonging effects of Lentinan in those with gastric, pancreatic, colorectal and liver cancer receiving chemotherapy.
Gout
* Has an alkalising effect and lowers uric acid levels.
Note: The deposition of uric acid crystals in joints such as the big toe is a key feature of gout.
Benign prostatic hyperplasia
* The high zinc levels act to block the conversion of testosterone to dihydrotestosterone (DHT), preventing prostate growth.
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What is the safety profile of shiitake?
What are the drug interactions when using shiitake?
* Shiitake dosage range: 1.5–10 g / day (up to 16 g / day used in some circumstances).
* Safety: Taking a high dose long term can lead to rare side effects such as abdominal discomfort, shiitake dermatitis, photosensitivity and asthma.
* Caution with anticoagulant drugs.
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Describe Lion's mane mushrooms
What important constituents do lion's mane contain?
Lion’s mane is a white-flesh, edible fungus, noted for its lobster-like flavour.
* Important constituents include beta-glucans, erinacines, high protein, selenium and zinc.
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How are lion's mane mushrooms useful in the treatment of GI disorders?
How are lion's mane mushrooms useful in the treatment of GORD?
GI disorders
* Promotes regeneration of the gastric and intestinal mucosa. As a result, it is especially therapeutic in cases of: Increased intestinal permeability, inflammatory bowel disease, peptic ulcers, gastritis and
GORD.
* It also acts as a prebiotic to support the intestinal flora and can be used in cases of dysbiosis.
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How are lion's mane mushrooms useful in the treatment of nervous system disorders?
Nervous system disorders
* The erinacine in Lion’s mane has a stimulatory effect on the production of nerve growth factor (NGF), a protein required in order to regenerate and repair nerve tissue.
* Powerful anti-oxidant effects.
* Use in cases of Alzheimer’s, concussion recovery, multiple sclerosis, Parkinson’s disease, peripheral neuropathies (e.g. diabetic) and general cognitive decline.
* Nerve injuries heal progressively and often slowly over time. Longer-term supplementation (months to years depending on the extent of disease) may be necessary.
* Lion’s mane dosage range: 1–6 g / day.
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Describe Turkey tail mushrooms
Turkey tail is probably the most-studied medicinal mushroom, it's extracts are commonly used in Japan as official cancer treatments, what are the two polysaccharide extracts called?
Turkey tail (Coriolus Versicolor) is a mushroom that is found in most parts of the world and tends to grow on dead logs. The English name of the species is derived from its coloured patterns, which look similar to the tail of a turkey.
* Turkey tail is probably the most-studied medicinal mushroom and its extracts are commonly used in Japan as part of official cancer treatment protocols.
* Two polysaccharide extracts from turkey tail — polysaccharide K (PSK) and polysaccharidepeptide (PSP) were approved as drugs in cancer patients. In 1990, PSK accounted for 25% of drugs in cancer treatment in Japan
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Describe how Turkey tail is useful in the treatment of cancer
Cancer
* Anti-proliferative, anti-metastatic and anti-angiogenic properties. It can induce apoptosis of cancer cells.
* The anti-cancer properties are due to the action of PSK and PSP. Improves survival in some cancer cases when combined with conventional therapies and minimises side effects. It protects against mutations caused by radiotherapy.
* It is especially indicated in hormonally-driven cancers such as breast, prostate and ovarian, although it has also been used in a number of other cancer types such as oesophageal, gastric, lung, hepatic and colorectal.
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Describe how turkey tail is useful as an immune modulator
What are the side effects of turkey tail?
Immune modulatory
* Increases the activity of macrophages, T-lymphocytes and NK cells.
* Has an anti-viral action against viruses such as HIV, EBV, HPV and the hepatitis B virus.
* Normalises an overactive immune system, which is especially useful in autoimmunity.
* Studies have shown that whilst it can upregulate the immune response in immunocompromised individuals, it has no effect in those considered ‘healthy’.
* Turkey tail dosage range: 1–9 g / day.
* Turkey tail side effects: Nausea, loss of appetite, diarrhoea.
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Describe Maitake (Grifola frondosa)
Where does it mostly grow?
What are the important constituents of maitake?
Maitake is often found among chestnut trees. It is crowned by the Japanese as the ‘king of mushrooms’ and is valued for its effect as a tonic and an adaptogen.
* Maitake grows mostly in Japan. The mushroom has a porous structure and is made up of brown and grey clusters of overlapping caps.
* Important constituents include beta-glucans, metalloproteins, lectins, enzymes and ergosterol.
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Describe how maitake is immune regulatory
Describe how maitake helps in the treatment of cancer
Immune regulatory
* The beta-glucans regulate the immune system — causing an increase in Th1 lymphocytes. They stimulate macrophages and NK cells.
* The fatty acids in maitake inhibit the COX-1 and COX-2 pathways, subsequently reducing inflammation.
Cancer
* The immune-boosting effects of beta-glucans provide an anti-cancer benefit.
* Alleviates side effects of chemotherapy including loss of appetite, vomiting, hair loss and leukopenia.
* Anti-metastatic action and inhibits tumour growth.
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Describe how maitake is beneficial for cardiovascular disease
Describe how maitake is beneficial for metabolic diseases
Cardiovascular disease
* Contains a protease which prevents clot formation.
* Reduces LDL cholesterol and regulates the reninangiotensin-
aldosterone system (normalising blood pressure).
Metabolic diseases
* Contains a proteoglycan that improves insulin sensitivity. Useful in cases of insulin resistance — especially Type 2 diabetes. It can also help to induce ovulation in polycystic ovarian syndrome.
* Recommended for fatty liver issues due to its hypolipidemic effects.
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What are the drug interactions to be aware of with maitake?
Maitake dosage range: 3–7 g / day.
Interactions: Potential additive effect when combined with blood glucose lowering medications (such as metformin) or supplements.
Monitor blood glucose to prevent hypoglycaemia.
93
Describe Chaga (Inonotus obliquus)
What are the key constituents of chaga?
Chaga grows mainly on birch trees in cooler climates where it develops a woody growth that has the appearance of burnt charcoal.
* The inside of the hardened clumps reveals an orange-coloured, soft centre.
* Chaga has a long traditional use for certain cancers, heart disease, diabetes mellitus and to increase endurance.
* Key constituents include beta-glucans, triterpenoids and sterols including ergosterol.
* It is rich in antioxidant compounds and reduces inflammation by down-regulating inflammatory mediators
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Describe how chaga can be useful for immunity
Describe how chaga can be useful for cancer treatment
**Immunity**
* Acts as an immunomodulator that can support bone marrow activity and the proliferation of immune cells including T-lymphocytes.
* Anti-viral activity — e.g. against hepatitis C.
* Helps to prevent ‘cytokine storms’, where the immune system over-responds and damages healthy tissue.
* The immune-modulatory and anti-inflammatory actions can be used in diseases such as ulcerative colitis.
**Cancer**
* Antioxidant and induces cancer cell apoptosis.
* Offsets bone marrow-suppressing effects of chemotherapy.
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What is the safety profile of chaga?
Chaga dosage range: 1–4 g / day.
Safety:
* Appears to inhibit platelet aggregation. Caution with antiplatelet medications and use before surgery is advised.
* Safety in pregnancy and lactation has not been established
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Describe how Cordyceps (Cordyceps sinensis) grows (it's gross)
Where did cordyceps originate?
How is cordyceps used in TCM?
Cordyceps is a fungal species that acts as a parasite in insects. It infects the insect, killing and mummifying it, then grows from the insect’s body!
* Cordyceps originated in Tibet — growing at an altitude of over 3500 m, but is now cultivated elsewhere in the world.
* Important constituents include polysaccharides, cordycepin acid, nucleosides, ergosterol and sterols.
* In Traditional Chinese Medicine, it is said to support the energy-stimulating capacity of the kidney, playing an important role in rejuvenation during convalescence.
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How is cordyceps useful in the treatment of kidney diseases?
How is cordyceps useful in the treatment of liver diseases?
Kidney diseases
* Supports renal health — decreases proteinuria, improves creatine clearance and has been shown to promote regeneration of kidney tubular cells.
* Protects kidney from damage due to immunosuppressants.
* Stimulates the formation of erythrocytes, which is often decreased in kidney failure.
* Traditionally used for chronic kidney disease.
Liver diseases
* The cordycepin acid in cordyceps improves hepatocyte function and decreases the formation of fibrotic tissue in liver cirrhosis.
* Improves liver function in hepatitis B and C.
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How is cordyceps useful in the treatment of cardiovascular diseases?
How is cordyceps useful in the treatment of respiratory diseases?
Cardiovascular diseases
* Contains polysaccharides with strong anti inflammatory activity.
* Acts as a cardiotonic — helping in cases of arrythmias. In addition, it increases nitric oxide production and relaxes vascular walls (lowering BP).
* Anti-thrombotic properties.
Respiratory diseases
* Improves respiratory function in asthma, chronic bronchitis and chronic obstructive pulmonary disease.
* Reduces inflammation and airway remodelling.
* Strengthens the immune system and is anti-viral.
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How is cordyceps useful in the treatment of fatigue and concentration?
How is cordyceps useful in the treatment of reproductive diseases?
How is cordyceps useful in the treatment of depression?
Fatigue and concentration
* Adenosine content provides extra energy, reducing fatigue. Also improves learning capacity and memory.
Reproductive diseases
* Enhances fertility and libido in men and women.
* Increases testosterone production in men and can be used in cases of impotency.
* Up-regulates ovarian hormone production in women, helping to regulate the menstrual cycle.
Depression
* MAO inhibitor leading to increased dopamine and serotonin which improves mood.
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What is the safety profile of cordyceps?
Cordyceps dosage range: 2–5 g / day.
Safety:
* Immunostimulatory effects may interfere with immunosuppressant drugs.
* Caution in hormone-dependent cancers due to influence on reproductive hormones.
* Safety in pregnancy and lactation has not been established and caution is advised due to hormonal effects.
