Herbs for Cardiovascular

Disorder

Dr Deny Susanti

Congestive Heart Failure

• Congestive Heart Failure (CHF) or congestive

cardiac failure (CCF) or heart failure …

is a condition that can result from any structural

or functional cardiac disorder that impairs the

ability of the heart to fill with or pump a sufficient amount of blood throughout the body

Schmidt and Dalton Osteopathic Medicine and Primary Care 2007 1:14 doi:10.1186/1750-

4732-1-14

Erythropoietin (EPO): A hormone

produced by the kidney that

promotes the formation of red blood

cells in the bone marrow.

LVH: Left ventricular hypertrophy

CKD: chronic kidney

disease

• New York Heart Association (NYHA) Functional Classification System classify the CHF patients according to their level of disability and useful in determining of the treatment

• This system divides patients into functional class: – FC-I (patients with cardiac disease but without limitations

of physical activity)

– FC-II (patients in whom physical activity results in fatigue, palpitations, dyspnea, or angina)

– FC-III (patients who have marked limitation of physical activity)

– FC-IV (patients unable to carry on physical activity without discomfort).

Sign and symptoms

• General– Weakness

– Fatigue

– Exercise intolerance

– Increased urination at night

– Increase heart rate

– Pale appearance

– Cold, blue finger and toes

The goals of therapy in heart failure are

1. to reduce symptoms and hospitalization

2. to slow the progression of the disease process and prolong survival.

3. reduction of the work load of the failing heart can be accomplished by physical and emotional rest as well as correction of obesity.

4. restriction of dietary sodium, one of the major compensatory responses to heart failure is sodium and water retention

Treatment Option-Conventional

• The most common drug used – Vasodilators

– Nitrates

– Diuretics

– Digitalis

– -blockers

• Other drugs– Angiotensin II antagonists

– Calcium channel bolckers

– Drugs to regulate heart rhythm

Nutritional Supplementation• Coenzyme Q10 (Co-Q10)

is naturally occurring vitamin-like nutrient that helps improve function of the heart muscle

• Magnesium

In general magnesium plays a critical role in regulating the heart muscle.

• L-carnitine-plays a key role in the metabolic function of heart muscle cells

• Taurine-an amino acid that helps to protect heart muscle from a variety of damaging conditions.

• Pottasium-important nutritional mineral that help regulate the electrical activity that keeps the heart beating normally and it reduces the danger of severe disturbance in heart rhythm

• Arginine-amino acid that help to regulate some aspects of cardiovascular function. Arginine is required for the production of nitric oxide, which helps increase circulation by dilating blood vessel.

Herbal Supplementation

Herbs Containing Potent Cardioactive

Glycoside

• Digitalis purpurea L. or D. lanata (the dried

leaves).

– potent cardiac glycosides: digitoxin and digoxin.

These 2 glycosides now account for all of

digitalis prescriptions in US

• Pharmacological action

– strengthen the force of the heartbeat by increasing the amount of calcium in the heart's cells

– increasing the amount of blood being oxygenated, the blood in general circulation, as much as 30% with each beat.

– strengthens the contraction of the heart muscle

– slows the heart rate and helps eliminate fluid from body tissues

– control irregular heart rhythms (arrhythmias) by slowing the signals that start in the sinoatrial (SA) node

• The cardiac glycoside are extremely potent

drugs, the dosage of which must be carefully

adjusted to the needs of the individual patient.

In the case of phytomedicines containing them,

this is possible only with the standardized powdered digitalis.

Side Effects

• Serious side effects:– An irregular heartbeat that causes dizziness, the feeling

that your heart has skipped a beat (palpitations), shortness of breath, sweating, or fainting

– Hallucinations, confusion, and mental changes like depression

– Unusual tiredness or weakness

– Trouble with your eyesight, such as blurry eyesight, double vision, or seeing yellow, green, or white halos around objects

– A loss of appetite or an upset stomach

• Common side effects:– Erectile dysfunction

– Breast enlargement in men

• Less common side effects:– A skin rash or hives

– Headache

– A numbness or tingling sensation over your body

– Eye sensitivity to light

– Diarrhea

– Throwing up

Adonis vernalis L. Apocynum cannabium L. Helleborus niger L.

Convalaria majalis L. Nerium oleander L. Urginea maritima L.

Strophantus kombe Oliv.

Other herbs containing cardiac glycoside:

Other Herbs for Treating CHF

• Hawthorn (consist of the leaves with flowers

and/or fruits of Crataegus laevigata (Poir.) DC

and C. monogyna Jacq.)

Herbal Use:

Use to improve the pumping capacity of the heart and to reduce the patients susceptibility to cardiac angina.

• Pharmacological action

Based on the clinical studies the Hawthorn

extract are active to increase coronary blood

flow, reduce blood pressure, reduce

peripheral blood flow and reduce peripheral

resistance.

• Side-effect and toxicity

Nausea and fatigue, sweating and rash on

the hands. Acute toxicity (LD50) : 50-2600

mg/kg (by i.v. injection) and 6 g/kg (by oral)

• Contra-indication:

It should not be taken during pregnancy

and lactation cause there is a reduction

in tone and motility.

• The vasodilation effect of Hawthorn

extract have been attributed to the

oligomeric procyanidin

(tannins/proanthocyanidins) and

flavonoids constituents

Proanthocyanidins are largely responsible for the cardiovascular action of:

1. Improving blood supply to the heart by dilating coronary vessel

2. Improving metabolic process in the heart, which results in an increase in the force of contraction of the heart muscle with elimination of some types of arrhythmia

3. Inhibiting angiotension converting enzyme (ACE) effective in the treatment of high blood pressure)

Based on the pharmacology study, Hawthorn extract was equivalent to the ACE inhibitor (captopril) in terms of influence on stress tolerance.

German Commission E has approved the use of

hawthorn for cardiac insufficiency corresponding to

NYHA FC-I and FC-II patients with a feeling of

pressure and tightness in the cardiac region, as well

as for the aging heart not yet requiring cardiotonic

glycosides

The minimal daily dosage is established on the

basis of flavone (5 mg) calculated as hyperoside,

total flavonoids determined as total phenols (10 mg),

or oligomeric procyanidins calculated as epicatechin

(5 mg)

Atherosclerosis

• Atherosclerosis is a disease affecting arterial blood vessels. It is a chronic inflammatory

response in the walls of arteries, in large part to

the deposition of lipoproteins (plasma proteins

that carry cholesterol and triglycerides).

• It is commonly referred to as a "hardening" or

"furring" of the arteries. It is caused by the

formation of multiple plaques within the arteries.

Figure A shows a normal artery with normal blood flow. Figure B

shows an artery with plaque buildup.

http://www.medmovie.com/mmdatabase/MediaPlayer.aspx?ClientID=65&TopicID=573

• Atherosclerosis is characterized by discrete

deposits of fatty substance (atheromatous

plaques) in the arteries and by fibrosis and

calcification of their inner layer.

• Atheroma plaque or fatty substance build up

over time, cause being a diet rich animal fats,

refine sugar, cigarette smoking, obesity and

inactivity

The prime targets of atherosclerosis are :

1. Aortawith the major consequences being aorta aneurysm

2. Cerebral arteries produce cerebral infarction (stroke)

Pharmacology action of the herbs that

would be beneficial in the prevention

and treatment of atherosclerosis : 1. Reduce cholesterol level

2. Enhances blood fibrinolytic activity

3. Inhibit platelet aggregation

Herbs for treatment atherosclerosis

1. Garlic (Allium sativum L.)

Constituents:

– Enzymes: Allinase, peroxidase, myrosinase, and others.

– Volatile oils: Sulfur-containing compounds including alicin (diallyl thiosulfunate), allylpropildisulfide, diallyl disulfide, ojoene, citral, geraniol, linalool, and -phellandrene.

– Other constituents: proteins, amino acids, mineral, vitamins, trace elements, lipids, prostaglandins.

• When a clove of garlic is crushed or sliced, the

compound alicin and other sulfur-containing compounds

are formed from alliin by the enzyme allinase. Alicin is

the main sulfur compound responsible for garlic’s health

benefits

Transformations and origins of bioactive

constituents of garlic

Awang, D. V. C.,2009

Herbal use:Garlic is stated to possess expectorant, antispasmodic, antiseptic, bacteriostatic, antiviral, hypotensive and anthelmentic properties and to be a promoter of leukocytosis.

Traditionally, it has been used to treat chronic bronchitis, bronchitic asthma, influenza, recurrent colds.

Modern use of garlic and garlic preparation is focused on their reputed antihypertensive, antithrombotic, antimicrobial, cancer preventive and lipid lowering effects

• The pharmacological properties

of garlic are attributed mainly to

its sulphur-containing

compounds.• cholesterol- and lipid-lowering

effects

The constituents of garlic causing

inhibition of the enzyme that

involve in biosynthesis pathway of

cholesterol. Recently, fresh garlic

extract and the constituents were

shown to inhibit human squalene

monooxygenase (an enzyme

catalysing a step in cholesterol

biosynthesis)

• Anti-artherosclerosis

The constituents of garlic

reduce: • the surface area of the thoracic

aorta covered by fatty streak

(atherosclerosis)

• hepatic triglyceride and cholesterol

concentration

• aortic lipid deposition and

atheromatous lesions

• Antithrombotic and fibrinolytic

activities

Garlic has been shown:• to increase serum fibrinogen

concentration together with a

decrease in blood coagulation time

and fibrinolytic activity.

• to inhibit platelet aggregation caused

by several inducer such as ADP,

collagen, adrenaline

The mechanism of anti-artherosclerosis

include: • inhibition of thromboxane synthesis via

cyclooxygenase and lypoxygenase inhibition.

• inhibition of membrane phospholipase activity

Allicin is a major inhibitor platelet aggregation.

Ajoenes are responsible for much of

antithrombotic properties of garlic.

Side-effect and toxicity

Garlic is generally considered to be

non toxic. Adverse effect that have

been documented in human including a

burning sensation in the mouth and

gastrointestinal tract, nausea, diarrhea

and vomiting

The German Commission E recommends 4 g

(approximately one average-size clove) of fresh garlic

as the daily dose for reducing elevated blood lipid

levels.

Assuming that fresh garlic yields, on the average,

0.37 percent allicin, the 5.4-mg allicin potential

contained in the 900 mg of garlic powder ingested

daily is equivalent to only 1.5 g of fresh garlic—less

than one-half of an average-sized clove

2. Green Tea Extract

The ingestion of green tea extract has

significantly decrease plasma cholesterol

and triglyceride concentration and the

ratio of low density lipoprotein (LDL)

cholesterol concentration to high density

lipoprotein (HDL) cholesterol

concentration

Green tea contains antioxidant polyphenol

including epicatechin, epicatechin gallate,

epigallocatechin gallate and

proanthocyanidin. These antioxidants are

important in preventing the oxidation of

LDL cholesterol, which plays a central role

in the development of atheroclerosis

Capsules containing dried green extract that

has been standardized for antioxidant

polyphenol content are available and should

be taken with food and water.

Those that are standardized to 97 percent

polyphenols are said to be equivalent to four

cups of green tea.

(-)-epigallocatechin gallate (EGCG), (-)-epicatechin gallate (ECG),

(+)-epicatechin (EC),

3. Red YeastRed yeast is the rice fermentation product of a mixture of several species of Monascus purpureus Went.In China, red yeast used in traditional medicine for the treatment of indigestion, diarrhea and improving blood circulation and the health of the spleen and stomach.The major active constituent of red yeast is monacolin K

Monacolin K is representative of a group of functionalized

hexahydronaphthalene β-hydroxy-δ-lactone compounds

formed by certain fungi and collectively termed mevinic

acids.

These compounds are inhibitors of β-hydroxy-β-

methylglutaryl CoA (HMG-CoA) reductase, the rate-limiting

enzyme in endogenous cholesterol biosynthesis

Mechanism of action of red yeast (monacolin K).

The blocking of cholesterol

biosynthesis by red yeast

(monacolin K) stimulates

hepatocytes to form a

greater number of LDL

receptors, which promotes

an increased influx of LDL

cholesterol from the plasma

to serve the precursor need

bile acid synthesis with

resulting decreased in

plasma LDL cholesterol

levels.

Awang, D. V. C.,2009

• In healthy adults who maintained their usual diet,

lovastatin produced mean reductions in serum total

and LDL cholesterol of 23–27 percent and 35–45

percent, respectively, at dosages of 6.25–50 mg

twice daily.

• The adverse effects reported in clinical trial with red

yeast were gastritis, abdominal discomfort and

elevated levels of liver enzymes.

Red yeast is available in capsules.

Red yeast is available in capsules that contain 600 mg

of a yeast–rice mixture standardized to supply 2.4 mg

of HMG-CoA reductase inhibitor. The recommended

dose is two 600-mg capsules taken twice daily with

meals (2,400 mg/day).

Thank you