Phytopharmacology of Botanicals

Botanical Metabolism

Metabolism in Plants Gives Rise to Life

Plants are unique from other life forms in that they can convert carbon dioxide into carbohydrates under sunlight through a process called photosynthesis.
All animal life derives its “life energy” through photosynthesis process as their energy source come from plants.
The energy from carbohydrates drives the metabolic pathways to produce secondary metabolites which have therapeutic properties contained within the plant.
When “whole” plant medicines are used every part of the plant has value and contributes to the whole effect of the remedy.

Secondary Metabolites have Healing Properties

Pharmaceutical companies derive many of their drugs from secondary metabolites found in plants.
Secondary metabolites are known as active constituents.
Secondary metabolites come from a “lived plant” and contain life energy.
Secondary metabolites are end-products from basic metabolic pathways.
ex. anti-fungal isoflavonoids produced by plants after injury prevent fungal growth and resinous sap has healing and protective action.

Plant Enzymes: Catalyzing Life Reactions

Plants rely on co-enzymes to catalyze cellular reactions by activating enzymes that support plant function. (Note: The first enzyme isolated was a urease in 1926).
The most important group co-enzymes is the phosphoric acid containing adenosine & uridine mononucleotides which are able to transfer energy from ATP for biochemical reactions.
Another important group of co-enzymes is the dinucleoties, including nicotanamide-adenine dinucleotide (NAD) and nicotinamide-adenine dinucleotide phosphate (NADP) which play a role in oxidation and reduction reactions in plants
used in their “fresh” state enzymes are active, they are deactivated when the herbs are dried.
Plant enzymes have a positive effect on body function as they help to support many of the organs and tissues in the body.

The Importance of Enzymes in Plant Remedies:

It is important to note that “whole plant extracts” have thousands of enzymes from the plant to assist in its biological functioning.
Synthetic drugs utlize only one specific enzyme which has been isolated for it’s activity.
Enzymes are denatured in heat (above 60oC), UV light, X-rays, and any treatment that denatures proteins.
Botanicals which are dried under proper conditions and preserved in water-alcohol solutions will retain their activity.

Botanical Pharmacology:

Botanicals have a wide range of physiological and biochemical effects on the body. The major phytopharmacological constituents are listed below along with their general therapeutic effects on the body. Botanicals contain one or many of these constituents in varying amounts. The naturopathic doctor will select the best botanical / botanical combination for you depending on the nature of your case.

Digestive Enzymes

Plant derived enzymes used to promote digestive functioning in humans and animals
Plant proteases including; bromelain (from pineapple plant) and papain (from fresh latex of papya) can be used as replacements for digestive insufficiency
Botanical actions which are indicated in the case of digestive insufficiency include:
Carminatives
Bitters
Alternatives
Demulcents
Nervines

Fatty Acids

Plants contain fatty acids – solid fat or liquid fat contains 1 molecule of glycerol and 3 fatty acid chains
Plant fatty acids examples include flax seed oil, borage seed oil and evening primrose oil
Super-unsaturated Omega 3 Fatty Acids include: alpha-linolenic acid, steridonic acid, eicosapentaenoic acid and docohexaenoic acid
Polyunsaturated Omega 6 Fatty Acids include: linoleic acid, gamma-linolenic acid, dihomogamma linolenic acid andarachidonic acid
Monounsaturated Omega 9 Fatty Acids include: oleic acid
Monounsaturated Omega 7 Fatty Acids include: palmintoleic acid
Saturated Fatty Acids include: steric acid, palmitic acid, butyric acid, arachidic acid
Saturated Fatty Acids contain carbons joined by single bonds and are solid at room temperature
Unsaturated Fatty Acids: include essential fatty acids. Polyunsaturated fatty acids have more than one hydrogen bond missing from the chain resulting in double bonds occurring between any two carbon atoms in the fatty chain
Benefits of Essentail Fatty Acids are as follows
required for structure of cell membranes
create electrical potentials and move electrical currents from cell to cell
precursors to protstaglandins (hormones)
control ratios of HDL and LDL cholesterol by reducing inflammation
crucial for brain development in infants/children
lower risk of stroke and blood clots by reducing platelet aggregation
lower risk of cardiovascular disease by lowering cholesterol
increase absorption of calcium
decrease osteoporosis
improve insulin function in diabetics
regulate inflammatory response in arthritis and eczema
inhance immune function by increasing T-cells
increase oxygen transport into cells
promote healthy hair and skin

Esters

Plant esters are formed when alcohol and acid combine with the release of water
Esters are common products in plants and is of major constituent in volatile oils, aromatic acids, lipids, resins, balsams, and alkaloids

Carbohydrates

Plant sugars (carbohydrates) are products of photosynthesis
Plant carbohydrates are either aldehyde or ketone bodies and contain carbon, hydrogen, and oxygen atoms (CHO)
Carbohydrates combine with other substances to form other compounds required for plant metabolism
Polysaccharides are more complex than mono or disaccharides containing hundreds or thousands of monosaccharides in a chain
Insulin is a carbohydrate found in the roots of plants and acts as a storage form of carbohydrate. Insulin used in patients with diabetes due to its low glycemic index score

Polysaccharides

Gums and mucilages are a form of polysacharides that have soothing and healing properties when used medicinally
Polysaccharides can also have immune stimulant, anti-fungal, anti-bacterial, and anti-inflammatory effects
Uronic acids are sugars which have been double oxidized at the terminal alcohol group are found n all gums and mucilaginous herbs.
Polysaccharide complexes containing uronic acid:
Hemicelluloses – found in cell walls with cellulose and pectin
Pectins – found in cell walls with cellulose and pectin
Algins – found in lamella cell walls
Agar – found in walls of brown algae
Carrageenan – found in red algae
Gums – gelling agent including acacia sterculia and tragacanth
Mucilages – psyllium seed and marshmallow root

Gums

Gums have protective role in plant chemistry
When a plant becomes injured it secretes gums to allow the plant to heal
Tragacanth Gum composed of sugar and uronic acids and is used as a suspending agent for insoluble powders and fluids. It is often used as a binding agent in pharmaceuticals
Acacia Gum powder used as an emulsifying agent and manufacture of tablets, lozenges. Its demulcent properties make it an ideal addition to cough lozenges and syrups
Guar Gum promotes gastric emptying and increases passage of contents in intestinal tract which can delay the uptake of ingested sugars. Guar gum binds to bile salts and can be used in cases of high cholesterol and atherosclerosis

Mucilages

mucilaginous herbs contain high levels of polysaccharides that contain uronic acids
mucilaginous herbs form a slippery gel when water is added which makes them ideal for soothing inflamed tissue
Acts as a protective barrier from further irritation allowing healing to take place
Protects against abrasion and can be used internally or externally
Protects against stomach acidity and helps with reflux and healing gastric tissue
Protects against infection, neutralizes toxins
Protects against sensitivities of nerve endings
Examples include; slippery elm bark and psyllium

Algal Agents

Algal agents involves sea weeds (brown and red)
Contains properties of being able to form into a gel when combined with water
Yield alginic acid used in industry as a detoxifying agent
Sea weeds have more mucilaginous properties than land plants as they must survive salt water and have to be very resilient

Brown Sea Weeds:

Laminaria and macrocystis soecis are commonly harvested
Alginic acid extracted by treating the brown sea weed with dilute sulfuric acid and extracting it with an alkaline solution
Alginic acids are highly reactive binding to metallic ions and act as a detoxifier agent
Alginic acid is so insoluble that the substance will not be absorbed into tissues and can be used to hold harmful particles in the bowel so they can be excreted – such as heavy metals or other products of detoxification reactions

Agar- Red Algae

Made in Japan for tokoroten food dish
Agar used as a gelling agent in food
In herbal medicine agar is used as a bulking agent

Irish Moss

grows on rocks off the beach and must survive salt water
Moss has a high sulfuric acid content which is used as a clarifying agent in beer and herbal medicine
used as a demulcent, emollient and nutritive properties
used as a soothing expectorant for respiratory ailments due to its affinity for the bronchial and respiratory mucous membranes

Tannins

Tannins contain metabolic byproducts and serve as protective agents after injury and parasitic invasion
Hydrolysable tannins derived from simple phenolic acids which are broken down in the gut to form gallic acid – hydrolisable tannins should not be used internally for long periods
Condensed tannins more resistant to hydrolysis and are poorly absorbed in the gut – when treated with acids they decompose into red pigments called phlobaphens
Found in “galls” on trees after parasitic invasion
Found in un-ripe fruit and act as a source of fruit acids
Used in “protein precipitation” towards epithelial surface leading to its use in tanning of hides and leading to “leather leg” on skin
Tannins have “astringent” actions and toning effects on tissues and are soluble in water, alcohol and glycerol
Topical washes – used to precipitate a layer of cells forming a scab over burns and abrasions
Oral use inhibits secretion of gut – such as diarrhea and help in nutrient absorption
Anti-inflammatory actions – promote healing of inflamed membranes and used in inflammatory bowel disease
Peristalic reflex – decrease sensitivity to nerve endings resulting in inhibition of peristalsis (digestive moltility)

Comarins

comarins are distributed within plants in a glycosidal form – they give an odour of mown fresh hay
anti-coagulant properties – competitive antagonist to vitamin K (natural coagulant)
photosensitvity – used in PUVA therapy which involves the administration of psoralen (comarin) in conjunction with exposure to UV light to treat skin disorders such as eczema and psoriasis
anti-fungal and insecticidal – kills pathogens in the body due to extreme bitterness
vascular tonic – supports vascular tissues

Anthraquinnones

Anthraquinnones occur in glycosidal form in plants.
When ingested in teas, tablets, or tinctures they are inactive until they reach the large intestine where they are acted upon by resident bacteria in the presence of bile
The main functions are to increase volume of fluids in the lower bowel, stimulate peristalsis and increasing tone of tract
eliminatory process used as a bulking agent and laxative, bowel tonic and cleansing tonic but may produce cramps and gas
cause irritation to mucus membrane in gut decrease absorption of water and electrolytes
cause increase in cyclic AMP in colon cells lead to increase chloride levels in lumen and water follows by osmosis
cause leakage of junctional complexes between endotherial cells leading to reabsorption of sodium and water into lumen

Resins and Balsams

Resins & balsams form a large group of plant compounds which are solid and have a gummy consistency and must be extracted with solvents such as alcohol
Used in a wide variety of products due to their gummy consistency
Used medicinally in creams, soaps and other cleansing agents
Oleo resins – volatile oils
Gum Resins – are mixture of volatile oils and gums
Balsamic Resins – are mixed with aromatic compounds such as benzoic and cinnamic acids to have increased water solubility

Isoprene Compounds (Terpenes)

isoprene compounds (terpenes) contain isoprene units which are the building blocks of rubber and give rise to many different compounds such as:
B- carotene: carotenoids
rubber
monoterpenes: limonene and camphor
triterpenes: glycyrrhetinic acid
sesquiterpenes: zingiberene
squalene: steroids

Volatile Oils

Volatile oils can also be known as essential oils are responsible for pleasant aroma of flowers and are known as monoterpene complexes
Come from oil containing organs of plants such as glands, hairs and glandular epidermal scales
Volatile oils are mixtures of hydrocarbons and oxygenated compounds
most abundant of the hydrocarbons are the terpene compounds of isoprine units

lipid solubility – volatile oils are small, making them ideal for passage into the skin and cell membranes of the nose, vagina, rectum and stomach. Since they are lipid soluble volatile oils can be absorbed through the skin and taken up into the systemic circulation
anti-microbial action – combat bacterial infection and inhibit the growth of yeasts and molds – prevent food spoilage by bacteria and mold
counter irritant – stimulate tissues they come into contact with dilates underlying capillaries and facilitates the movement of blood to an area
Carminative – cause slight irritation to the mucous membranes of the gastrointestinal tract and stimulates peristalsis decreases the accumulation of gas
Anthelmintic – combat parasitic infections in humans and animals ex. wormseed oil
insect repellent – seen in smelly oils such as citronella, lemon balm, basil
expectorant – metabolized and partially excreted via the lungs to fumigate lung tissues by stimulating the serous and glandular cells in ciliated epithelium
diuretic – irritating effect on the kidney tissues causing urinary output
anti-inflammatory – triggers the release of anti-inflammatory substances and encourages blood to enter into the area
diaphoretic – stimulate the perfusion of blood in the epidermal layer of skin

Cyanogenic Glycosides

Cyanogenic glycosides upon hydrolysis the oils yielded prussic acid (HCN) in large quantities it is toxic, however, in smaller quantities it is therapeutic
Sedative and antispasmodic – treatment of spasmodic coughs
Cardio-sedative – increases parasympathetic innervation slowing heart rate
Digestive – increasing vagal tone promoting digestion
Cancer – cyano glycoside amygdalin marketed as “laetrile” or vitamin B17” is toxic to cancer cells

Glucosinalates

Glucosinalates are derived from nitrogenous compounds (amino acids) and contain sulfur
Vegetables from the brassica family such as cabbage, cauliflower, cale, broccoli, brussel sprouts have high glucosinalates.
rubfacient actions – applied topically causing irritation effect of glucosinalates which bring nutrient rich blood to the area of application causing the removal of morbid matter from areas of stagnation and congestion
anti-thyroid effects – depresses the thyroid function indicating the use in hyperthyroidism

Saponins

Saponins are diverse group of plants used as detergents
The chemistry of saponins reveals characteristics of hormones such as estrogen, aldosterone, and cortisol and mimic sex hormones
Hemolytic functions – destroy RBC making them highly toxic
Expectorant – cause irritation of gastric mucosa
Steroidal saponins (tetracyclic triterpenoids) – similar to hormones produced in the body such as sex hormones, cortisone, vitamin D and are closely related to cardiac glycosides. Steroidal saponins assist in the regulation of sex hormones and are used to regulate female cycles
Triterpenoid saponins (pentacyclic triterpenoids) are abundant in dicot families and support endocrine system and nervous system

Cardioactive Glycosides

cardioactive glycosides influence the cardiovascular system by interacting with the heart muscle and arterial system
Cardio relaxation – dilates arterioles and causes vasodilatation, helps to tone and strengthen the vessels
Compete with K in the Na/K pump mechanisms – of heart cell membranes resulting in K loss and increase Ca in cells, and supports proper muscle contraction
Inhibit ATPase – responsible for active transport sodium out of the cell causing the accumulation of Na in the cell and increase rate of muscle contraction
Buffering effect – as K competes with cardio-active glycosides in heart tissue

Alkaloids

alkaloids form the largest most complex group of plant constituents
The first alkaloid discovered was morphine
Alkaloids are normally white crystalline compounds which are alkaline and insoluble in water but soluble in alcohol
Alkaloids are derived from amino acid metabolism in plants and are very potent in their effects. For this reason they are prescribed sparingly for a very small subset of conditions

pyrrolidine alkaloids from the solanaceae family affects smooth muscle tissue of perhiperal nervous system causing a reduction in smooth muscle tone and acts as a bronchial dilator, inhibits bodily secretions. They are used to treat acidity and spasms in GI tract and urinary tract as well as motion sickness and Parkinson’s disease
pyridine and piperidine alkaloids found in tobacco, lobelia, hemlock have effects similar to nicotine – acts on chemoreceptors in the carotid artery causing reflex in breathing. Used to treat asthma
pyrrolizidine alkaloids compositae and boraginaceae families are derived from amino acid ornithine. They have carcinogenic, mutagenic and hepatotoxic properties and are never used medicinally
quinolizidine alkaloids are derived from the amino acid lysine found in leguminoseae family. Contains alkaloid sparteine which is a respiratory stimulant, coronary vasodialator, smooth muscle stimulant, vagal nerve stimulant and is also used to increase tone of uterus during labor
indole alkaloids are derived from amino acid tryptophan, have hallucinogenic properties and act as a sedative effects on the nervous system, cause the dilation of coronary blood vessels, reduction of blood pressure, relax smooth muscles accept uterine muscle
quinoline alkaloids derived from amino acid phenyl-alanine or tryptophane, stomatic, antistringent and anti-microbial properties
pure alkaloids derived from pruine nucleotide bases adenine and guanine includes caffeine, theobromine and theophylline found in tea, coffee, and cocoa
isoquinaline alkaloids derived from amino acid tyroside and phenylalanine contains the following subgroups from the poppy family:
Simple isoquinalines are a powerful narcotic and hallucinogenic
Benzyle isoquinalines haveanti-spasmodic effects on smooth muscle reducing muscle tone
morphine, codine, thebaine cause vasodilatation slows breathing and may induce coma
protopines act as analgesic and desensitize nerve endings
protoberberines bitter digestive, anti-microbial and CNS depressan
ipecac alkaloids acts as powerful emetic increases secretion of gastric juices and may induce vomiting – used for acute poisoning

Flavanoids

Flavanoids biased in phenolic ring structure found in higher plants, are water soluble, act as powerful antioxidant and are absorbed best when combined with vitamin C
Flavanoids have a wide range of effects which include:
reduce capillary fragility as they strengthen vascular tissue
prevent fluid retention (edema)
reduce risk of stroke
protect against arthritis
reduce risk of atherosclerosis
decrease menopausal symptoms
protect against oral herpes infection due to the immune stimulatory effects
decrease risk of diabetic cataracts
decrease histamine response to allergen exposure due to mast cell stabilizing effects
reduction in ulcer problems due to the effects on gastric secretion
decrease inflammation after injury due to effects on healing tissue
antioxidant and collagen stabilizing activity
anti-inflammatory inhibit inflammatory mediators
immune modulation inhibit histamine release
allergies prevent allergens from entering into tissues
anti-viral reduces vitamin C oxidation
vasotonic effects treat hypertension
diabetic cataracts inhibits accumulation of sorbitol in retina
glaucoma
cancer treatment cytotoxic effects

Flavones – antispasmodic action steroidal properties and can mimic certain hormones
Anthocyanins – sensitive to pH levels are used to treat night blindness and capillary fragility.
Flavones – easily converted into chalcones found in citrus fruits
Chalcones and Aurones – precursor for other flavinoid pigments

Flavanolignans – milk thistle is an important liver herb with restorative properties by acting on liver cell membranes to strengthen them and to protect against toxic substances