Stale Remedy Finds Fresh Uses

A Review of Traditional and Prospective Medicinal

Applications of Garlic

BPS4123
 1. Introduction

The integration of the use of plants in human culture has been a common theme that
dates back to the beginning of civilization. Some of the most involved uses of plants in human
life however is rooted in their medicinal properties. The medicinal properties of plants come
from the various chemical compounds found in them each of which has its own function that
serves a role in maintenances of the organism’s well-being (Sofowora et al., 1993). The usage of
plants for this purpose always has been and currently remains a source of primary health care
in most rural, cultural areas. However, the extent of a plant’s medicinal abilities is not limited to
these groups as they are currently used in the developed world today as sources of raw
material for usage in manufacture of modern medicine as well as a source of alternative health
care in themselves. Much of these modern medicines today that incorporate medicinal plants
came about through traditional knowledge. By pairing this traditional knowledge with scientific
research, new areas of use can be appointed to these traditional medicines where their usage
had not seen before.
Allium sativum, otherwise known as garlic, is a bulbous plant that belongs to the same
genus as other plants such as leeks and onions. Garlic is a widely cultivated plant that is used in
many cultures all over the world. The use of garlic for its therapeutic properties has been a
common theme throughout history first dating back to Ancient Egypt almost 5000 years ago.
Traditionally, garlic has been seen as an antimicrobial agent through treatment of various
diseases throughout history such as cholera, influenza, typhus and various infections. However,
applications of garlic for this purpose have recently been overshadowed by the creation of
antibiotics and vaccines. Nonetheless, recent discoveries regarding the potential applications of
garlic for other diseases is being explored and indications of a promising role in the treatment
of these areas are present. By using scientific investigation rather than simply traditional
medical knowledge, we can validate the historical uses of garlic’s as a medicine as well as
appoint new therapeutic applications to this otherwise ancient remedy. First, we must
understand what active ingredients are present in garlic as well as the potential role they serve
in the body.

2. Phytochemistry

The various bioactive chemicals that can be found in plants are the root of any potential
therapeutic properties it may possess. Allium sativum, otherwise known as garlic, is a bulbous
plant with long stalks rooting up to 30 cm from the ground. However, all of the plants active
materials can be found in the garlic bulb. It has been determined that the key active ingredient
in garlic is allicin (Tattleman, E., 2005). Allicin is an organic sulfate compound which is a
member of the thiosulfinate family that is present in garlic. Allicin is formed when the
compound alliin is subjected to the enzyme allinase. These compounds only interact when
garlic is either chopped or crushed. The conversion of alliin to allicin creates the signature smell
garlic is known for. The creation of allicin can then direct the rise of other sulfur compounds
such as allyl sufides and ajoene (Bayan et al., 2014). However, other compounds are also
present in garlic which can also lend to its therapeutic effects. In order to assay what other
potential active ingredients are present in the bulbs, an extract can be prepared from fresh
garlic and a qualitative assay on the extract can be completed. Extraction methods done as per
Huzaifa et al. (2014) resulted in positive hits for tannins, saponins and cardiac glycosides in
relatively larger amounts and alkaloids and flavonoids in trace amounts with quantitative
results as seen in Table 1. Each of these established active compounds will possess a different
role in the human body.

Table 1. Quantitative phytochemical screening of aqueous extract of Allium sativum bulb

Tannins have been known to be a form of double-edged sword when it comes to

promotion of health. On one hand, beneficial applications of tannins have been observed. In a
population study involving 20 different countries, a negative relationship was seen between tea
drinkers, in which tannins are present in large amounts, and incidence of cancer. Additionally,
cancer death was lower in the tea production areas when compared to the non-production
areas. (Stocks, P., 1970). However, it has also been also observed that tannins can have
detrimental effects when in large doses as well. These effects range from reduction of protein
quality, damage to digestive tract and carcinogenic affect (Huzaifa et al., 2014). Because of
these potential detrimental effects, it is not wise to consume large amounts of foods which
contain high amounts of tannins. However, in moderation tannins may serve a beneficial role in
maintenance of human health.
Furthermore, saponins have been studied in clinical trials exploring their benefits to
human health. These studies concluded that saponins serve roles in promotion of the immune
system, lowering cholesterol levels through prevention of reabsorption and lower cancer risk
through interaction of cholesterol membranes of cancer cells (Shi et al., 2004)
Cardiac glycosides have the ability to inhibit the sodium potassium pump in cardiac cells
which gives rise to the potential to treat heart failure and irregular heartbeats (Langer et al.,
1984). This is accomplished through the buildup of calcium levels in the cardiac cells caused
from this inhibition which increases positive inotropy ultimately leading to stronger
contractions.
Although these discussed secondary metabolites are not the key active ingredients
found in garlic, they certainly may still possess significant roles in the various application of
garlic as a medicinal agent. The areas in which these compounds have shown success are the
same areas in which garlic itself has shown promising results as will be discussed later on. This
correlation provides some evidence that these compounds have potential key roles garlic’s fight
against human disease.
3. Traditional Applications of Garlic for Medicinal Use

3.1 Traditional Use

Usage of garlic for medicinal purposes can be traced back thousands of years
throughout various cultures and is among the earliest of documented plants used as a medicine
for maintenance of health. The first documented usage of garlic as a medicine was seen in
ancient Egypt almost 5000 years ago (Petrovska et al., 2009). Garlic was part of regular diet for
both the wealthy and poor. However, garlic was prescribed as a medical treatment for malaise
as well as insect and parasite infestations as per the “Codex Ebers”, the official medical text of
the era. Likewise, an Indian medical text established in 300 AD called the “Charaka-Samhita”,
states that garlic is recommended for the treatments of infections as well as parasites and
worms. However, traditional Indian medicine does not limit garlic’s uses to anti-microbial
function as it is also recommended for digestion issues as well as weakness and fatigue (Rivlin
et al., 2001). In traditional Chinese medicine, garlic is seen as warm in nature and a strong
stimulant (Petrovska et al., 2009) This understanding of garlic’s nature was then applied to
several different conditions. Consumption of garlic would result in an increase in body
temperature, making the conditions inside the body undesired for any foreign organisms.
Additionally, the increased temperature would aid in digestion of foods and fluids in the
stomach removing blockages and remedying indigestion to settle stomachs. In traditional
Chinese medicine, the lungs were seen as the key component of the immune system and that
sickness was something that could be inhaled. When garlic was consumed, the pungent
smelling oils would vaporize and be absorbed into our lungs. This absorption would mediate the
garlic’s natural warmth to quicken and strengthen our lungs and allow us to fight off and exhale
harmful pathogens more efficiently.
Similar uses of garlic in the Greek and Roman empires led to the transferal of this
ancient knowledge into early middle ages culture through to the end of the Renaissance.
Following the fall of these powers, the sole source of medical knowledge in the beginning of
this era were from Greek and Roman texts. Like the “Codex Ebers” of Egypt and “Charaka-
Samhita” of India, one of the major medical texts of the middle ages was the Hortulus text
established around 800 AD. This text illustrated plants that were thought to have medicinal
properties and of these, garlic’s medicinal uses were a common incidence. Many of these uses
paralleled the ones seen in other previous ancient texts including use to ward off infections and
parasites as well as the same correlation of garlic as a “warm” food as seen in traditional
Chinese medicine. The anti-microbial function of garlic played a massive role in treating
infections during the various plagues that occurred in western Europe (Vanjkevic et al., 2002).
The similarities in medicinal uses of garlic can be seen throughout these various cultures
yet all doing so without ever coming into contact with each other. The uniform conclusions that
these cultures were able to independently establish indicates the effectiveness of garlic as a
legitimate resource of remediation of human sickness, especially its antimicrobial activity.

3.2 Experimental Evidence

As previously mentioned, garlic has seen historical usage as an antibacterial and antiviral
agent during times of infection and disease. However, the first experimental application of
garlic as an antimicrobial agent was seen by Louis Pasteur when he demonstrated its
antibacterial action in laboratory using garlic juice (Sivam, GP. 2001). The antimicrobial actions
of garlic comprise of antibacterial, antiviral and antiparisitic applications. The antibacterial
function of garlic has been seen in studies ranging from gram-positive and gram-negative
bacteria including full garlic extract to just the key active ingredient, allicin. Mozaffari et al.
(2014) showed that Staphylococcus aureus, a gram-positive strain of bacteria food pathogen
responsible for food poisoning, had its growth inhibited when subject to a fresh garlic extract.
Counts of S. areus on 2-week old sample of beef subject to 2mL garlic extract possessed a 16-
fold decrease in colonies when compared to the control sample. Whereas Canizeres et al.
(2004), showed that in vitro growth of Helicobacter pylori, a gram-negative bacterium responsible
for gastric diseases and ulcers, was inhibited when subject to garlic’s active compound, Allicin.
In terms of antiviral activity, an experiment involving mice exposed to influenza virus done by
Mehrbod et al. (2009) demonstrated antiviral activity when subject to garlic extract. A similar
experiment done with 146 healthy human subjects demonstrated that an allicin supplement
was successful in preventing infection of the common cold virus. Finally, the antiparisitic
properties of garlic have been observed is a study showing the complete inhibition of growth of
human intestinal parasite cultures of Entamoeba histolytica when subject to small
concentrations of allicin. (Mirelman et al., 1987).
These basic interpretations of experimental results that have been presented include
different types of microbes using various preparations of garlic to validate the uses of garlic as
an antimicrobial agent in various traditional medicines. The remained effectiveness of this
function when reduced down to just allicin suggests that garlic’s antimicrobial function is
rooted in allicin. The ability of garlic to serve as an antibacterial agent against both gram-
negative and gram-positive bacteria as well as an antiviral agent both in vitro and in vivo lend to
the legitimacy of garlic’s historical use as a combatant against plagues, pathogens, parasites
and general malaise. It is a fact that most human deaths throughout history were due to these
diseases caused by various microorganisms. Plants with the ability, such as garlic, to prevent
and treat these ailments became known for this function due to the extreme demand for a
cure. However, since these needs have now been replaced by the creation of antibiotics and
vaccines, the demand for these plants for this purpose has in turn declined. In today’s society,
the demand of treatments for human ailments are those that arise from human ageing as
vaccines and antibiotics have eradicated death from infections. Is it possible that a plant such as
garlic that was so successful at combating these ancient diseases could fill the same role in
these new diseases? Current research regarding this question provides promising answers.

4. New Applications of Garlic for Medicinal Uses

Today, ailments that have the largest effect on human health are more related to issues
that arise with age rather that infections and disease as seen through past history. Many of the
treatments developed from modern science to combat these new ailments require invasive,
unfamiliar practices using man made compounds that many may find unappealing. However,
new scientific methods paired with traditional herbal medicinal knowledge may lead to new
applications of ancient remedies which will be seen as a more natural option when compared
to previous practices. Today in modern medicine, we see this potential application of garlic as a
medicinal plant in other fields of study through promising clinical trials. Clinical trials are one of
the best indicators of efficacy and safety of a product that has potential to be a promising
candidate in combating certain ailments. Various clinical trials have been completed using garlic
as an agent for cardiovascular health including hypotensive action and serum lipid lowering
action as well as usage for anticancer activity.

4.1 Cardiovascular
One of the first uses of garlic as a hypotensive agent was in 1941 when a study done
involving 26 patients with hypertension were subject to garlic supplementation. After
treatment, 85% of patients observed a lower blood pressure with average drop of 12.3 mmHg
and 6.5 mmHg in systolic and diastolic blood pressure respectively. (Damru et al., 1941) A more
recent meta-analysis of the hypotensive effect involving 7 separate trails using the same
preparation method along with placebo, 3 of the 7 experienced a drop in systolic blood
pressure where 4 of the 7 showed a drop in diastolic blood pressure. (Silagy et al., 1994). It was
noted that these clinical trials all lacked consistency when it came to how the trials were ran
including un-uniform sources of garlic as well as duration and stringency of the trials. Along
with hypotensive properties, it has been established that garlic is also a good source of
cholesterol lowering agents. A study involving 3 groups of people each subject to vegetarian
diets with varying amounts of garlic showed that the group whose diet contained the highest
amount of garlic consumption resulted in the lowest presence of serum lipids in the blood.
(Sainani et al., 1979). Furthermore, a meta-analysis completed in 1994 incorporating 16
separate trails found an average 12% reduction in total cholesterol when comparing diets rich
in garlic to that of placebo or diets excluding it. (Silagy et al., 1994)

4.2 Anticancer Application

In addition to cardiovascular health, garlic usage has seen promising results as an anti-
cancer agent. Even though the extent to which garlic can serve a role in the battle against
cancer has been much less investigated, the few studied that have been done show promising
results and a potential future in this field. The National Cancer Institute recognizes several
population studies show a positive relationship between increased garlic consumption and
decreased risk of cancers such as stomach, skin, esophageal, breast and colon. However, only a
few clinical trials have been completed showing this correlation. Three separate clinical trials
have been completed showing the relationship between garlic consumption and gastric cancer
incidence one of which completed in 2004 involving 5000 men and women showed this positive
correlation. Over a span of 5 years, participants were administered either a daily dose of garlic
extract or a placebo. At the end of the trial, it was observed that the participants subject to the
garlic extract saw a 33% decrease in total tumors and 52% decrease in stomach cancer when
compared to the placebo group (Li et al., 2004). In addition to gastric cancers, a positive
correlation has also been observed with skin cancers. A 21-person study involving participants
with basal cell carcinoma were subject to application of a garlic extract to the affected area.
After one month of usage, an average size reduction of 47% was seen in the cancerous area
(Tilli et al., 2003).
Although limited, the clinical trials presented regarding the potential therapeutic
application of garlic to combat these new disorders shows indications that the possibility is
there. However, in order to progress this possibility into a reality, more research must be
completed with more organized trials with stringent controls and better documented results.

5. Mechanisms

The current evidence presented supports garlic’s traditional and newer applications for
various ailments. However, the mechanism to which they operate must be better understood in
order to legitimize their past usage as well as to help advance their usage in these new areas of
interest. Some theories of the mechanism are presented below.

5.1 Antimicrobial Mechanism

It is understood that the antibacterial effect of garlic comes from its key active
ingredient, allicin. Allicin is a type of organosulfer compound that is able to react with cysteine
residue thiol groups on proteins. Wallock-Richards et al. (2014) showed that through the
covalent modification of cysteine residues by various garlic extracts, peroxiredoxin, a key
enzyme in the bacterial defense mechanism (Hall et al., 2009), was inhibited through the
addition of allyl thiol groups on key catalytic cysteine residues Cys44 and Cys98. The mass of
the enzyme not subjected to the extracts was determined to be 18992 Da (Fig. 2A). However,
after subject to allicin and garlic extract, mass spectrometry readings gave two new species of
mass 19064 and 19136 Da (Fig. 2B/C). These results were consistent with the increased mass
expected from allyl thiol groups being added to one (72 Da) or both (144 Da) key cysteine
groups. Mass spectrometry results can be found in Figure 1. This understanding of the
mechanisms to which garlic affects bacterium can be applied to other organisms with this
similar enzyme.

Figure 1. Mass spectrometry of enzyme BCP after incubation with various garlic extracts.

5.2 Cardiovascular Mechanism

The mechanism to which garlic affects cardiovascular disease is not well understood.
However, Ried et al. (2006) hypothesized that the blood pressure lowering effect of garlic also
comes from the organosulfides that are present in garlic. These compounds stimulate the
production of the vascular gasotransmitter, hydrogen sulfide, as well as increase the regulation
of endothelial nitric oxide which induces smooth muscle cell relaxation and vasodilation which
ultimately lowers blood pressure. Likewise, the mechanism to which garlic lowers serum lipid
levels in the blood is also not fully understood. Yeh et al. (2004) provided data which supports
the idea that garlic is able to inhibit hepatic cholesterol. This inhibition comes from the
organosulfur compounds present in the garlic that are potent inhibitors of cholesterol
synthesis. Finally, the secondary metabolite diallyl disulfide that is created from allicin is
believed to have a role in prevention of coronary heart disease and atherosclerosis from an
antioxidant effect. This oxidative effect is seen in its ability to increase production of the
detoxification enzyme GST (Wu et al., 2002). Both coronary heart disease and atherosclerosis
are initiated from the oxidation of LDL leading to the formation of plaque in the vascular
endothelial cells. (Omar et al., 2007)

5.3 Anticancer Mechanism

So far, not much is understood on how garlic is able to combat against some cases of
cancer. The observed success at combating gastric cancers compared to others from garlic may
be attributed back to its antimicrobial attributes. As previously stated, the active compound
allicin of garlic was able to inhibit the growth of Helicobacter pylori in in vitro studies.
Helicobacter pylori is known to cause gastric diseases such as cancer to those who are infected
by it (Uemura et al., 2001). Because of the previously mentioned antibacterial activity of garlic,
it can be suggested that the same antibacterial effect indirectly leads to the anticancer effect in
gastric cancers from the inhibitory effect it has on these harmful gastric bacteria.

It is apparent that most of the bioactivity of garlic is rooted in the organosulfer

compounds it possesses. However, since much of this activity is yet to be fully understood, it is
not wrong to assume that the other previously mentioned secondary metabolites found in
garlic also possess a role in this activity. More investigation into the activity of garlic and its
constituents must be done in order to gain a better comprehension of these mechanisms. This
better understanding will allow for more educated applications of the therapeutic uses of garlic
in combating additional disorders.

6. Conclusion

The role garlic has had in serving the medical needs of humans has been a common theme
throughout history. The plethora of active compounds that garlic possesses makes for a plant
that has incredibly large potential to treat several various diseases. Regardless of the fact that
garlic’s antimicrobial usage is not a new concept, evidence supports that its effectiveness is
adequate and can be seen as a more natural alternative choice to the current man-made
options. Additionally, it has been observed that through clinical trials, garlic has proven itself as
a very promising candidate as a combatant against other diseases such as cardiovascular and
cancer. However, in order to progress from a candidate to a treatment, more attention must be
given to garlic with additional completion of clinical trials regarding its use as a combatant for
these diseases. Furthermore, a better understand of how garlic combats these and the
mechanisms to which they work will lead to larger and more effective applications to garlic’s
therapeutic potential.
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