gek - dietary and herbal supplements 2015 (pe).ppt

7/23/2019 GEK - Dietary and Herbal Supplements 2015 (PE).Ppt

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VITAMINS, MINERALS AND HERBAL

SUPPLEMENTSGEK2501: Assistant Prof. Pieter Eichhorn (Email: [email protected])


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Objectives of lecture:

1.

to classify the functions of the key vitamins

and minerals, and identify their main

dietary sources

2. to differentiate the pharmacological effects

of four common herbal supplements, and

also appraise the evidence for such effects

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Discovery of Vitamines

In 1906, English biochemist Sir Frederick Gowland Hopkinsdiscovered that certain food factors were important to health.

In 1912, Casimir Funk originally coined the term Vitamine

after "vita" meaning life and "amine" because vitamins were

once thought to contain amino acids.

Together, Hopkins and Funk formulated

the vitamin hypothesis of deficiency disease -

that a lack of vitamins could make you sick.

Casimir Funk 1884-1967 (Isolated Thiamine-Vitamin B1)


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A vitamin is defined as a biologically active organic

compound that is not synthesised within the body, but is

available in the diet in small amounts and is carried at

small concentrations in the circulatory system to act ontarget organs or tissues; it is essential for normal health

and growth; absence of a particular vitamin causes a

deficiency disease or disorder. RJ Kutsky

VITAMINS


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Discovery dates of Vitamins

Vitaminevitamin. The early years of discovery

http://www.clinchem.org/content/43/4/680.long


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VITAMIN GROUPS and NOMENCLATURE

At present there are thirteen distinct vitamins that arerecognized. Vitamin A, B1, B2, B3, B5, B6, B7, B9, B12, C, D, E,

K .

Why are Vitamins named like this? Vitamins used to be

labeled all the way to U, but have been reclassified over time.

For example: -Vitamin PP (Niacin, still sometimes called

this) is now called Vitamin B3.

-Vitamin O (Carnitine; found to be

synthesized in the body)

-Retinol, Retinal, and four carotenoids: the

carotenes alpha-carotene, beta-carotene, gamma- carotene; and the xanthophyll beta-cryptoxanthin,

are all classified as Vitamin A because they share

common functionality and all are convertible to the

active form of the vitamin in the body).


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Vitamins are classified as being

water soluble or fat soluble and sub-

classified by their biological andchemical activity. Not by their

structure.

Vitamins

Water

Soluble

FatSoluble

B

C

A

D

E

K

B1- thiamineB2-riboflavin

B3-niacin

B6-pyridoxine

B9-folic Acid

B12-cobalamin

C-ascorbic acid

D-cholecalciferol

E-tocopherols

K-phylloquinone

A-retinol

VITAMIN GROUPS


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VITAMIN GROUPS

I.Water-soluble vitamins: B and C complexesB complex vitamins include: thiamine (B1)

riboflavin (B2)

niacin (B3)

pyridoxine (B6)

folic acid (B9)

cyanocobalamin (B12)

C complex vitamins include: ascorbic acid (C)

Excess: excreted in the urine; little or no storage in the body, thus

need to be continually supplied in the diet.

Exceptions: folic acid and vitamin B12are stored in the liver. It

may take several years to deplete these stores, before signs and

symptoms of deficiency become manifest.


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VITAMIN DIETARY

SOURCES

FUNCTION RDA DEFICIENCY

DISORDER

B1

THIAMINE

Lean pork,

water melons,

fish, cereals.

Used in the production of

energy from carbohydrates.

Promotes growth and muscle

tone; health of heart, skin

and nerves

1-5

mg

Beriberi (weakness of

leg muscles, nerve

damage, heart

failure), less

concentration, fatigue

B2

RIBOFLAVIN

Bean sprouts,

dairy

products,

whole grains

maintains health of skin,

hair and nails; helps

metabolism of

carbohydrates, fat and

protein

1.5-2

mg

Itching and irritation

of eyes, skin and

mucous membranes

B3

NIACIN

Beef liver,

poultry, corn,

lentils,

mushrooms,

peanuts,

salmon/tuna

Helps release energy from

carbohydrates; maintains

health of digestive system

and nerves

13-18

mg

Pellagra (diarrhoea,

dermatitis,

depression), muscular

weakness/fatigue

B5

PANTOTHENIC

ACID

Meat, brocoli,

avocados.

Require to synthesize

coenzyme-A and help to

metabolize proteins,

carbohydrates and fats.

1-5

mg

Wide range of

symptoms including:

fatigue, apathy, may

in severe cases lead to

hepatic

encephalopathy9


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VITAMIN DIETARY

SOURCES

FUNCTION RDA Deficiency Disorder

B6PYRIDOXINE

Meat, fish,

Cereals, egg

yolk, avocados,

nuts, oatmeal

supports the central nervous

system by promoting the

synthesis of hormones and

neurotransmitters

1.5-

2.6

mg

Nerve damage

(peripheral numbness),

difficulty in

concentrating, short-

term memory loss

B7

BIOTIN

Raw egg yolk,

liver, peanuts,

leafy green

vegetables.

Involved in the synthesis of

fatty acids.

35-70

ug

Alopecia, conjunctivitis,

dermatitis, depression,

hallucination.

B9

FOLIC ACID

Dark green

leafy

vegetables,

cereals,

*legumes,

wheat germ,

yeast

Promotes production and

health of red blood cells;

maintains normal brain

function

400 -

1000

!g

Megaloblastic anaemia,

digestive disorders loss

of appetite; irritability,

headaches

B12

COBALAMIN

Clams/oysters,

dairy products,

egg yolk, organ

meats liver

and kidney

Promotes health of the

nervous system and blood cell

maturation

2-5

ug

Nerve damage

(numbness and tingling

of the extremities),

unsteady gait10


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VITAMIN DIETARY

SOURCES

FUNCTION RDA DEFICIENCY

DISORDER

C

Ascorbic

Acid

Berries, citrus fruits

(oranges,

grapefruit, lemons),

green leafy

vegetables, melons,

peppers, potatoes

Biological

antioxidant;

maintains health

and promotes

repair of body

tissues; keeps

bones and teeth

healthy; facilitates

the absorption of

dietary iron

70 - 150 mg Scurvy (bleeding,

inflamed gums, loose

teeth, poor wound

healing,)

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Please refer to Harvard Health Publications for complete information.

http://www.health.harvard.edu/staying-healthy/listing_of_vitamins


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II. FAT-SOLUBLE VITAMINS

Vitamins A, D, E and K occur in the lipid componentsof both plant and animal foods. Released when these

foods are digested, and are then absorbed in the intestine,

and storedin the liver and adipose tissue.

As fat-soluble vitamins are not excreted in the urine,

excess intake over time, especially of vitamins A and D,

can cause toxicity.

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VITAMIN DIETARY SOURCES FUNCTION RDA Deficiency

Disorder

A

Retinol

Carrots, broccoli, egg

yolk, fish liver oils,

pumpkins, sweet

potatoes, swiss cheese

promotes - good vision,

health of the immune

and reproductive

systems and of skin,

hair, bones and teeth

development

3000-10000

IU

Night Blindness,

dry skin, poor

development of

bones and teeth

D

Calciferol

Egg yolk, high-fat fish

and fish oils, milk or

margarine

facilitates proper

calcium and phosphorus

absorption; promotes

growth and maintains

health of bones

400 IU Rickets,

osteomalacia

E

Tocopherols

Nuts and seeds, peanuts

and peanut butter,

wheat germ, vegetable

oils

biological antioxidant

that protects against

harmful effects of free

radicals; stabilizes cell

membranes

12-18mg Pancreatitis

* Vitamins does

not prevent

wrinkles *

K

Phylloquinone

Green leafy vegetables

Kale,broccoli, brussel

sprouts, cabbage; olive

oil, soybean

needed for the

production of blood

clotting factors in the

liver. (K/C)oagulation

120 ug Nose bleeds,

internal

hemorrhage13


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VITAMIN GROUPS and NOMENCLATURE

Vitamin wheel

Please note vitamin B3 is referred to here as PP

Vitamin K is mostly found in

green leafy veggies, kale,

sprouts.


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Vitamin C(ascorbic acid)

The name Ascorbic acid is derived from the Latin word forscurvy-scorbutus.

Very common among sailors on long sea journeys as food

was perishable. The derogatory word Limeys referring to

people from England was originated as cooks in the Royal

Navy put lime juice in sailors daily ration of watered down

rum. Scurvy caused by vitamin Cdeficiency

Vitamin C plays a critical role in the

maintenance of a normal mature collagen

network in humans by acting as a co-factor for

two enzymes lysyl and prolyl hyroxylase.

These two enzymes are required for the

hydroxylation (-OH) of proline and lysineamino acids in collagen. Effect ive

hydroxylation is required for stability of

collagen during collagen cross-linking.

Defective collagen formation impairs effective

wound healing.

Vitamin C

regulates

hydroxylation

of proline and

lysine

residues inpro-collagen


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Vitamin D(calciferol *** calciferol denotes D2and D3)

Ricketsis the softening and weakening of the bones due to prolonged vitamin D deficiency.

However, lack of calcium in the diet may also lead to rickets.

While both major forms of Vitamin D, Vitamin D2and Vitamin D3can be obtained from

dietary sources or vitamin supplements vitaminD3(cholecalciferol) is synthesizedin the

human skin from 7-dehydrocholesterol upon exposure to ultraviolet-B (UVB) radiation from

sunlight.

Rickets

caused by

vitamin D

deficiency


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Vitamin D

Nevertheless both forms are inactive. Vitamin D is carried to the liver where its converted to the

hormone calcidiol(25 dihydroxyvitamin). Part of the calcidiol is converted by the kidneys tocalcitriol(1,25 dihydroxyvitamin), the biologically active form of vitamin D.

Calcitriol circulates as a hormonein the blood regulating the concentration of calcium and phosphate

in the blood stream promoting growth and remodeling of bone.


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ESSENTIAL MINERALSThese are :

Macrominerals:

calcium potassium

phosphorus magnesium

sodium iron

Microminerals:

zinc copper

selenium fluoride


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MINERALS

These are chemical elements that are required byliving organisms for normal bodily functions. They

may be classified as:

1. macrominerals(required in amounts >100 mg/day)

2. microminerals(trace elements) - required in

amounts < 100 mg/day.

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Macro-

mineral

Sources Functions Result of

deficiency

Result of excess

Calcium Beans,

broccoli,

Cheese,

dark green

veggies (like

spinach andkale),

milk

Key constituent of

bones, teeth;

regulates nerve and

muscle function, and

also blood clotting

In children: rickets

In adults:

osteomalacia.

Osteoporosis may

follow.

Formation of stones

in kidneys, gall

bladder

Phosphorus Dairy

products,

meats, leafy

vegetables,

most fruits

Component of bone

tissue; forms

compounds that are

needed for energy

conversion eg.

adenosine

triphosphate (ATP)

Anaemia, de-

mineralisation of

bones, weakness

Interferes with

absorption of

calcium,

magnesium, zinc,

iron

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Macrominerals


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Macro-mineral Sources Functions/Uses Result of

deficiency

Result of

excess

Sodium

(extracellularfluid)

Processed

foods, table

salt

Regulates plasma

volume, maintains

acid-base balance,

nerve and electrical

potential generated

by activity of Na+/K+

ATPase (

sodium

pump

); thus

maintains muscle and

nerve function

Hyponatraemia -

low blood

pressure, muscle

weakness,

paralysis

Hyper-

natraemia -

dehydration,

hypertension

Potassium

(intracellular fluid)

Fruits, all

vegetables,

milk

Main base ion of

intracellular fluid;

maintains electrical

potential of the

nervous system and

thus maintains

function of nerve andmuscle tissues

Muscular

weakness or

paralysis; mental

confusion

Irregular heart

rate and

rhythm, cardiac

arrest

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Macro-

mineral


deficiency

Result of

excess

Magnesium Green leafy

vegetables,shellfish, nuts

Essential for bone

health; needed forfunctioning of muscle

and nerve tissue and

also of ~90 enzymes

Anxiety, insomnia,

fatigue, depressedmuscle contraction

Unusual

Iron Liver, meat,

green leafy

vegetables,

meat, peas,

whole grain

Anaemia, impaired

immunity

Long-term intake in

excess leads to iron

deposition in body

tissues (liver,

spleen), reduced

absorption of

calcium and

magnesium,

increased

susceptibility to

infection

Essential for

transfer of

oxygen

between tissues

in the body


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Micro-

mineral


deficiency

Result of excess

Zinc Dairy

products,

eggs, liver,

red meat,

whole

grain

Co-factor in > 200 enzyme

systems, including the

antioxidant enzyme,

superoxide dismutase (SOD);

strong immune system

Growth

retardation in

children, poor

immunity

If taken in excess

over a long period,

it leads to

deficiency of

copper absorption

Cooper Legumes,

nuts and

seeds,

whole

grains,

organ

meats,

drinkingwater

Part of many enzymes; needed

for iron metabolism

Very rare.

Results in

hematological

and

neurological

disorders.

Upset stomach,

nausea diarrhea.

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Microminerals


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Micro-

mineral


deficiency

Result of excess

Selenium Meats,

seafood,

grains

Antioxidant Hypothyroidism Hair and nail loss,

skin rashes, fatigue

Fluoride Drinking

water

(either

fluoridated

or

naturally

containing

fluoride),fish, and

most teas

Involved in formation of bones

and teeth; helps prevent tooth

decay

Tooth decay Fluorosis, mottling

of teeth,

calcification of

ligaments.

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Microminerals


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Magnesium

Our body contains at any one time 24 grams of magnesium.

Over 350 enzymes require magnesium for their catalytic function.

Including all enzymes that utilize and/or synthesize ATP.

98% of the ATP that runs our body & cellular functions MUST be

attached to Mg.

Very difficult to overdose on Mg as it is freely filtered through our

kidneys.


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FOUR

TRADITIONAL

HERBAL

SUPPLEMENTS:

GARLIC

GINKGO

BILOBA

GINSENGAND


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1. GARLIC (Allium sativum)

Garlic has been extensively studied scientifically and shown tohave multiple beneficial pharmacological effects on

cardiovascular system by lowering overall cholesterol levels and

reducing blood pressure in hypertensive patients.

*47 hypertensive patients and showed that garlic significantlyreduces mean systolic/diastolic blood pressure by an average of

12/9 mmHg versus.* (Garlic for hypertension: Cochrane database)The authors state that garlic was "free from side effects" and that no serious side effects were reported.

There were 3 cases "where a slight smell of garlic was noted."


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1A.What are the active chemicals in Garlic?

Raw garlic bulbs contain the compound, alliin, which is converted

by the enzyme, allinase, to the active compound, allicin (which givesodour to garlic).

Biological Function:

When the garlic plant comes under attack Allicin is synthesized and

protects the garlic from antifungal and antiviral infections.

Commercially available garlic capsules are enteric-coated to

protect allinase from being inactivated in the acid pH of the

stomach.


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1B. Benefits of consuming Garlic?

. Lowers blood pressure (by 12/9 mmHg)

. Anti-oxidant (inhibits oxidation of LDL-cholesterol)

. Inhibits platelet aggregation

. Enhances fibrinolytic* (clot-dissolving) activity

. Reduces serum cholesterol levels by 5-8%

. Protects the elastic properties of blood vessels

USE:

prevention of atherosclerosis and its effects


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1C. Adverse effects of consuming Garlic?

Daily consumption in excess of 5 cloves (or equivalent) may cause:

-nausea-heartburn

-hypotension

-allergy in the form of contact dermatitis.

1D. Precaution on use of garlic productsUse with caution in patients on oral *anticoagulants.

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2. GINKGO BILOBA

The root and kernels of Ginkgo

bilobahave been used in TCM for

a very long time. In the 1960s, a

concentrated extract of G biloba

leaves was developed. Today, a leafextract with standardised amounts

of the active constituents -

ginkgolides A, B, C and bilobalide -

is in clinical use.

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2A. Some pharmacological effects of ginkgolides

I.Increase blood flow: due to vascular relaxation mediated by nitric

oxide, and also reduced blood viscosity.

II.Scavenge free radicals:In vitrostudies showed that ginkgo has

free radical-scavenging properties.

III. Inhibit platelet activity: Ginkgolide B was found to inhibit the

activity of platelet activating factor (PAF) which promotes

platelet aggregation.


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2B. Evidence of Ginkgo function in Clinical trials

a. In patients with intermittent claudication ( decreased blood

flow during exercise)

At least 1 study showed that ginkgo increased pain-free

walking distance by 40% compared to 20% in placebo-

treated subjects.

b. In patients with cerebral insufficiency and Alzheimers-typedementia.

At least 2 large-scale clinical trials (of 6 months and 1-year

duration) have indicated that ginkgo is useful in mild to

moderately severe dementia.

c. Studies of patients undergoing coronary artery by-pass

surgery showed that ginkgo reduced free radical production

in these patients. 33


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2C. Adverse effects of ginkgo products

Rare: gastrointestinal disturbances,

headache

allergic skin rash.

More serious:drug interaction with aspirin or anti-coagulant agents

increased risk of bleeding


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3. GINSENG

There are different species from different countries:Panax

ginseng(China or Korea),Panax quinquefolium(America).

Siberian ginseng is not true ginseng but belongs to a different

genus,Eleutherococcus senticosus.

The active ingredients in Panax species are the ginsenosidesor

panaxosides (saponin glycosides), which are found mainly in the

roots.

The counterpart ingredient inE senticosusis the eleutherosides

(which have yet to be standardised, unlike the ginsenosides).


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3A. Pharmacological benefits of ginseng

anti-platelet activity anti-stress activity,

energy- and mind-enhancing actions

blood pressure regulation

Of note: Siberian ginseng has been used by Russian cosmonauts

and Olympic athletes as a herbal tonic to promote general health

and well-being, and to reduce physical and mental stress.


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3B. Standardised formulation ofPanax ginsengand suggested

Dossage

(1g crude root = 200mg of extract = 14mg of ginsenosides)

1-2g/day of root extract of Panax ginseng, or 2-3g/day of root extract

of Siberian ginseng

Ginsana G115-each gelatin capsule contains 100 mg root extract;the active ginsenosides make up 7% by weight (=7 mg).


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3C.Clinical trials with ginseng have reported:

1.

improved mental function and physical performance

2. significant enhancement of immune function and quality of life

3. significant reductions in HbA1c* and fasting blood glucose


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3D.Adverse effects of Ginseng

1.Ginseng has weak oestrogenic properties and can cause breast

swelling and pain and also menstrual irregularities, including

excessive bleeding.

2.Insomnia and nervousness (due to excessive brain stimulation)

3.

Hypertension, from high doses (>3g/day)


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4. And. Salicylic Acid.

Used as early as 3000 BC, the

ancient Egyptians used willowbark to reduce pain and fever

In 1897, Felix Hoffmann (a young

chemist working for Bayer)

independently made ASA in a

more chemically pure, stable andmore palatable form.

Two years later, on March 6, 1899,

aspirin was trademarked under

the Imperial Office of Berlin.

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Other infamous Bayer products

The effects of heroin will be covered in detail in the GEK2501 lecture: Drugs of abuse.


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4A Pharmacological effects and uses of Aspirin

Analgesic (minor pain)

Antipyretic (reduces fever)

Anti-inflammatory

Antiplatelet (targets thromboxane and platlet

aggregation)

4B. Mechanism of ActionAspirinis non-steroidal anti-inflammatory drug

(NSAIDs) that irreversible binds and inhibitsthe

enzyme cycloxygenase 1 and 2 (COX1/2). But primarily

COX1. COX enzymes produces hormones called

prostoglandins. Some prostoglandins are involved in the

response mechanism required for signaling pain and

inflammation. 42


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4A Pharmacological effects and uses of Aspirin

Analgesic (minor pain)

Antipyretic (reduces fever)

Anti-inflammatory

Antiplatelet (targets thromboxane and platlet

aggregation)

4B. Mechanism of ActionAspirinis non-steroidal anti-inflammatory drug (NSAIDs) that

irreversible binds and inhibitsthe enzyme cycloxygenase 1 and 2

(COX1/2). But primarily COX1. COX enzymes produces

hormones called prostoglandins. Some prostoglandins are involved

in the response mechanism required for signaling pain andinflammation.


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4C. Evidence of benefit:

In short, too many to count. It truly is a wonder drug.

ex. Cancer, heart attacks, strokes, not to mention the

day to day use in treatment of headaches, pain, and

fever.

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4D. Clinical Evidence

Too many to list:

One example is the use of low dose Aspirin in the prevention of

cancer.

In 2011 a meta-analysis study of eight clinical trials that

compared the risk of cancer death among participants

who took daily aspirin for 4 years or more to those who took no

Aspirin found that, overall, Aspirin use lowered the risk of dyingfrom cancer by approximately 20%.

(NCI.2011)


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4E. Side Effects

The biggest risk is gastrointestinal bleeding.

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The following problems can occur:

1.Allergy to some component of the herbal remedy

2.

Contamination with poisonous chemicals e.g. Residual

herbicide

3. Adulteration with potentially harmful Western drug(s) e.g.

steroid.

4. Misidentification of a plant species, causing a toxic variety to

be used

5.

Interactions between the herbal remedy and a Westerndrug(s), with undesirable outcomes

What dangers to health should consumers

beware of when taking herbal products?


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How does one evaluate the claims of health

supplements?

The gold standard by which Western-trained

scientists and medical practitioners accept a particular

treatment or drug for its therapeutic efficacy is from the

positive outcome of random double blind placebo-

controlled cross-over trials with the drug.

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SHOULD I TAKE A HERBAL REMEDY

FOR A PARTICULAR HEALTH

PROBLEM?

When in doubt, always ask your doctor. He/She has your

medical records, knows your medical history - illnesses,

medications and allergies - and is best able to advise you.

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*** Over 68000 people in the United States alone overdosed

on vitamin and mineral supplements last year resulting in

hospitalization and critical care.***


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END OF LECTURE


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3. Retinol is:

(A) Also known as vitamin B2

(F)

(B) Is a water soluble vitamin

(F)

(C) Is mostly found in Carrots

(T)(D) is required as deficiency may lead to night blindness

(T)

gek - dietary and herbal supplements 2015 (pe).ppt

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