Physio-Pharmacological Potentials of Taurine:

A Review in Animal and Human Studies

Oyovwi Mega Obukohwo
Department of Physiology, Adeleke University, Ede, Osun State, Nigeria

ABSTRACT
Taurine, a sulfur-containing non-protein amino acid is one of the most prevalent amino acids in all
mammalian plasma and tissues. The objective is to identify the therapeutic role of taurine in animal
models and human systemic physiology. Various electronic databases, including author, year of
publication, country, purpose, data collection, significant findings and research focus/domain were used
in search of published material referencing assessment of the physio-pharmacological potentials of
taurine. Taurine protects against a wide range of pathophysiological conditions, including neurological
abnormalities, mitochondrial malfunction, metabolic disease, reproductive failure and poor fetal
development. Taurine was also reviewed to possess antioxidant, reno-protective, hemo-protective,
hepato-protective and anti-inflammatory potentials as well as cardio-protective and anti-aging effects.
Taurine, found in excitable tissues, protects systemic physiology against maladaptive responses.
Further research is needed to determine if taurine insufficiency can monitor maladaptive responses.
Although, clinical trials are also needed to determine optimal therapeutic doses.

KEYWORDS
Taurine, health, systemic physiology, maladaptive responses, antioxidant, fetal development,
repro-protective potential

Copyright © 2023 Obukohwo. This is an open-access article distributed under the Creative Commons
Attribution License, which permits unrestricted use, distribution and reproduction in any medium, provided
the original work is properly cited.

INTRODUCTION
Taurine, a 2-aminomethane sulfonic acid, is mostly found in almost all cells, especially excitable ones1.
Its cytoprotective activities have a substantial impact on the health and nutritional state of numerous
species, regulating essential cellular events and balancing life and death2. Taurine’s physiological functions
have piqued the interest of researchers because of its cytoprotective properties3-6.

Taurine has received interest in infant formula, dietary supplements and energy drinks due to its possible
medicinal applications7. Clinical investigations demonstrate that taurine is a necessary ingredient in several
species, such as cats and foxes8. Taurine is categorized as a conditionally necessary or useful nutrient in
humans, with higher tissue retention than in cats or foxes8. Humans, unlike cats, do not show obvious
indications of taurine insufficiency, albeit parenteral feeding has been linked to taurine deficiency9.
Human studies have demonstrated taurine’s nutritional significance, with increased dietary consumption
lowering the incidence of hypertension and hypercholesterolemia10. In obese women, taurine
supplementation decreases body mass index and inflammatory markers11-13. Taurine’s cytoprotective

ISSN: 1996-3351 (Print) Received: 30 Apr. 2023

https://doi.org/10.3923/ajbs.2023.452.463 Accepted: 16 Sep. 2023
Published: 31 Dec. 2023
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actions contribute to better clinical and nutritional health. The current study examines the
physio-pharmacological pathway behind taurine’s cytoprotective effect, the impact of taurine on a variety
of disorders and the nutritional value of taurine supplementation.

COMMON AND SCIENTIFIC NAMES

Taurine, commonly known as 2-aminoethanesulfonic acid, has a molecular formula of H2NCH2CH2SO3H
(Formula: C2H7NO3S) (Fig. 1) and a recognized abbreviation of Tau14-16.

Biochemistry and functions: Taurine is a crystalline substance that is tasteless, colorless and has a
pH of 1.73417. It has a melting point between 325 and 328EC. Its zwitter ionic nature necessitates active
transport in order to maintain high-concentration gradients in tissues like the retina and neurons.
Neither inorganic sulfate nor organic sulfur can be found in taurine. Significant additional roles for taurine
have been demonstrated in lipid metabolism, calcium homeostasis, heart failure, prevention of ischemic
cardiac damage, cardiomyopathy, reduction of hypertension, osmoregulation, glucose metabolism
regulation, immunity and inflammation regulation, antioxidant/free radical scavenger and membrane
stabilization2,17-19. The metabolic actions of taurine and its possible medical benefits are further examined.

Taurine homeostasis in the body: Absorption, distribution, excretion and synthesis of taurine are all part
of an organism’s homeostasis process, with intestinal uptake and liver production providing for dietary
requirements20-22.

Taurine absorption: TauT and PAT1 transporters control how much taurine is transported in the small
intestine. Type 2 diabetes and inflammation may both increase transport while decreasing absorption20.

Taurine distribution: Taurine is absorbed in the gut and then released non-saturable into the
bloodstream, where it reaches a plasma concentration of 10-100 µM23. TauT or PAT1 transporters then
absorb taurine, with TauT serving as the primary absorption mechanism. The range of tissue taurine
concentrations is 5-50 mM, with metabolically active tissues containing the highest levels24. The biggest
source of taurine is found in skeletal muscle, which makes up more than 70% of the body’s total taurine
content.

Taurine excretion: Due to a lack of enzymes, mammals cannot digest taurine. It eventually ends up in
feces after being expelled by the kidney or converted to bile acids. The amount of taurine in the body is
controlled and cats given high doses of taurine have increased urine excretion25. Increased faecal bile acid
excretion and urinary taurine levels may be indicators of dietary seafood consumption.

Biosynthesis of taurine: Cysteine dioxygenase (CDO) and cysteine-sulfinate decarboxylase (CSAD)

convert cysteine to taurine, generating cysteine-sulfinate and hypotaurine26. It undergoes an ambiguous
oxidation process to get taurine. Coenzyme A breakdown is a minor synthesis route that results in
cysteamine, which can then be oxidized to hypotaurine. Although, other tissues, such as the brain, lungs,
skeletal muscle, adipose tissue and mammary glands, also produce taurine, the liver is in charge of
maintaining taurine levels26.

S
HO NH₂
O

Fig.1: Showing molecular structure of taurine

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Taurine concentrations in food can range from 1 mmol per 100 g of wet weight to 20 mmol per 100 mL27.
The average daily consumption in omnivores is 1000-1500 mmol (125-188 mg)28. However, it is
challenging to determine the general population’s intake of taurine due to the absence of updated food
tables. There has been a surge in energy drinks with a high taurine concentration and compared to
omnivores, vegans may have significantly lower plasma taurine levels and urinary excretion. Unknown is
the magnitude of this drop in tissue taurine content and plasma taurine.

Transporters of taurine: The high-affinity, low-capacity, Na+-dependent TauT transporter and the
high-capacity, proton-coupled, but Na+-independent b-amino acid transporter PAT1 allow TauT/PAT1 cells
to accumulate taurine29. With binding taking place in the first N-terminal extracellular loop and gating and
ionic binding to TauT, taurine transport is Na+ and Cl- dependent. Taurine binding and the start of the
transport cycle both require Na+ ions. Because Na+ is recycled to the extracellular compartment by the
Na+/K+-ATPase, TauT-mediated taurine absorption in EATC is electro-neutral. The second Na+ is more
easily bound to TauT with the help of Cl- ions29.

Due to acidification, osmotic swelling, exposure to reactive oxygen species and activation of
serine/threonine kinase protein kinase C (PKC)29, tauT activity is downregulated in a variety of cell types.
TauT’s structural changes brought on by PKC-mediated phosphorylation prohibit taurine from binding
to Arg-324. Taurine uptake that is Na+-dependent is stimulated by PKA, but this effect is eliminated by
PKC activation. Through Thr-28 phosphorylation, casein kinase 2 inhibits TauT activity by raising TauT0's
affinity for Na+ and decreasing the Na+/taurine stoichiometry for taurine transport. Gene transcription has
a role in the long-term control of TauT function, with downregulation occurring after p53 activation,
exposure to high extracellular taurine levels and hypotonicity29. After being exposed to a hypertonic
solution, the tonicity-responsive enhancer binding protein (TonEBP/NFAT5) is upregulated. TauT mRNA
abundance, translation and activity are decreased in primary human trophoblasts, NIH3T3 and ELA murine
fibroblasts when rapamycin mTOR is inhibited. Following hypertonic exposure, enhanced TauT activity may
be due to increased mTOR-dependent TonEBP activity29. Through the activation of mTOR, the low-affinity,
high-capacity transporter PAT1 is linked to cellular amino acid sensing and cell proliferation29.

PHYSIO-PHARMACOLOGICAL POTENTIALS OF TAURINE

Membrane stabilizer: Taurine causes a variety of membrane-related activities in tissues29. It was first
proposed as a membrane stabilizer in 1973. Its functions are explained by protein phosphorylation,
taurine-phospholipid binding, antioxidant hypothesis and phospholipid N-methylation hypothesis.
According to the protein phosphorylation hypothesis, taurine modulates calcium binding and transport,
while the antioxidant hypothesis contends that taurine lessens the inflammatory response caused by
cytotoxic oxidants. According to the phospholipid N-methylation theory, taurine’s actions result from
inhibition, which changes the structure and content of membranes.

Taurine and cell volume regulation: In order to control intracellular osmolality, morphology and
processes including cell migration, metabolism and death, it is essential to control cell volume.
Water-permeable mammals have systems for volume restoration in response to osmotic disturbance. The
renal medulla, gut and airways are exposed to an isotonic extracellular medium while the kidneys control
osmolality. In the EATC, the taurine release is responsible for 30% of the osmolyte loss and loading cells
with radioactively labelled taurine can cause taurine tracers to be depleted29-30.

Body organs development: Insufficient synthesis of taurine in the human fetus results in
problems with birth weight since taurine is an important amino acid throughout development. Mice that
lack TauT are often smaller and have abnormalities in the growth of the heart and skeletal muscles29-31.

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Taurine supplementation has an impact on learning ability and low plasma taurine content can harm
mental development32. These problems may be better studied using different animal models, such as CDO
(cysteine dioxygenase) or CSAD (cysteine sulphinic acid dioxygenase).

Lung function improvement: Taurine affects mucus production and lung relaxation by acting as a weak
agonist for GABAAR and GlyR receptors. In pathological conditions like asthma where immune cells
secrete CysLTs, boosting mucus output and reversing taurine’s relaxing actions on smooth muscle cells,
it may have a role in lung regulation29. By decreasing inflammation and oxidative stress, taurine shields
cells against lung damage33.

Modulation of mitochondrial function: Protein translation and the production of ATP synthase depend
on taurine for proper mitochondrial function. Reduced respiration in the liver mitochondria is a result of
depletion, which might alter mitochondrial function. TauT knockout mice may be exercise-intolerant29-30
and taurine supplementation may enhance mitochondrial function. Taurine might have a direct impact
on the control of mitochondrial metabolism, possibly blocking PDH and possibly influencing sulfur and
carbohydrate metabolism34.

Antioxidative defence: Reactive oxygen species (ROS) are the main culprits in endogenous
oxidant-induced cell damage and antioxidants like taurine can reduce ROS production, scavenge ROS, or
block their actions35. Taurine guards against calcium excess scavenges hypochlorous acid and guards
against mitochondrial damage36. In addition, it has cytoprotective effects on rat liver, decreasing lung
tissue oxidative damage and lipid peroxidation37. By modulating Ca2+ homeostasis and boosting cardiac
and skeletal muscle contraction under exhausting conditions, taurine supplementation may enhance
exercise performance38.

Modulation of muscle contraction: Guanidine-ethane-sulfonate reduces the taurine content of the

extensor digitorum longus by 60%, which has an effect on the contractile performance of cardiac and
skeletal muscle in taurine shortage. The effects of administration on exercise performance, rodent
contractile function, exhaustion time, weariness and muscle protection are all improved39. Taurine reduces
inflammation and oxidative stress, which reduces vascular stiffness40.

Implicated in counteracting sarcopenia: Aging is the root cause of sarcopenia, a major health concern
that affects the aged and is brought on by abnormalities in protein biosynthesis and breakdown.
Taurine insufficiency may enhance taurine’s potential in other applications by reducing the consequences
of sarcopenia41.

Treatment of duchenne muscular dystrophy: Duchenne muscular dystrophy, a deadly illness

characterized by muscle loss and inflammation, is successfully treated in mice by taurine therapy42.
The severity of the illness may be lessened with leupeptin and nNOS. When taurine levels are restored,
inflammation is reduced and forelimb strength is improved42. Enhancing muscle strength with creatine is
almost as effective.

Attenuating myotonic dystrophy: A condition known as myotonia results in delayed muscle relaxation
after contraction. Treatment with taurine lessens the intensity of discharges and may be useful in treating
congenital paramyotonia and sodium channel myotonia2,29.

Prevention of cardiovascular disease: Further Randomized Controlled Trials (RCTs) are required before
taurine is included in micronutrient supplements43. Taurine may help prevent and treat heart failure,
hypertension, ischemic heart disease, atherosclerosis and diabetic cardiomyopathy.

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Hypercholesterolemia: By enhancing cholesterol catabolism and bile acid excretion, taurine reduces
hypercholesterolemia in animal models44. In people who are overweight or obese, it enhances lipid
metabolism and may avoid cardiovascular disease. According to a study, pretreatment with 1.5 g dayG1
of taurines restored any vasoconstriction that was already present45. Its effects on hyperlipidemia and the
prevention of cardiovascular disease (CVD) require further study.

Hypertension: By lowering blood pressure through decreased Ca2+, oxidative stress, sympathetic activity,
inflammatory activity and renal function, taurine supplementation has been demonstrated to prevent the
development of hypertension in animal models44,45. Recent clinical investigations have demonstrated an
improvement in blood pressure and a 1.5-fold rise in plasma taurine concentration45.

Congestive heart failure: Myocyte calcium overload increased oxidative stress and decreased myocardial
energy generation is common in heart failure patients. Norepinephrine and angiotensin II activities are
decreased by taurine, a Japanese-approved treatment2. Although, it increases exercise capacity, there is
untapped potential for it to lessen mortality rates and the risk of overt heart failure. In Korean women with
significant cardiovascular risk factors, taurine supplementation decreased plasma taurine levels, which may
have beneficial effects on calcium homeostasis, atherosclerosis and coronary heart disease risk46.

Diminishes atherosclerosis: The intricate process of atherosclerosis includes the intake of

cholesterol-enriched lipoproteins, the recruitment of monocytes, the adherence of endothelial cells, the
development of macrophages and the production of foam cells. By accelerating cholesterol regression,
lowering cholesterol biosynthesis and safeguarding endothelial cells, taurine therapy lowers
atherogenesis2,47. Additionally, it inhibits the proliferation of vascular smooth muscle cells and the
reduction of oxidative stress2,47.

Alteration of ischemia-reperfusion injury: Taurine is crucial in ischemia-reperfusion insults, which alter

the course of damage treatment and injury outcomes48. It can be used in heart transplantation and bypass
surgery to reduce oxidative stress and cellular necrosis, but it is not appropriate for acute cardioprotective
agents such myocardial infarctions20.

Reduction of myocardial arrhythmias: Digoxin and adrenaline are two examples of pro-arrhythmic
substances that taurine inhibits2. Under the right circumstances, taurine plus L-arginine treatment
effectively decreased cardiac arrhythmias in three patients, making it a potent antiarrhythmic agent49.

Treatment of metabolic diseases:

C Mitochondrial disease, MELAS: Myopathy, encephalopathy, lactic acidosis and stroke-like events are
some of the signs of taurine deficiency50. Mutations in tRNALeu that influence the amount of
mitochondrial taurine and UUG-dependent proteins are the cause of MELAS (Fig. 2). The MELAS
patients may benefit from taurine therapy50
C Diabetes mellitus: An autoimmune condition called diabetes mellitus causes high blood sugar and
insulin resistance. The T-cell death causes type 1 diabetes, but type 2 diabetes is progressive and
inhibits insulin activity. In mice, taurine therapy decreases the pathophysiology associated with
diabetes, obesity and metabolic syndrome51. It lessens type II diabetic consequences by enhancing
respiratory function, boosting ATP synthesis and reducing mitochondrial ROS generation. To ascertain
if there is impaired renal re-absorption or decreased intestinal absorption, more research is required
C Modulation of inflammatory diseases: Joint stiffness, discomfort, inflammation and tissue
destruction are all symptoms of arthritis, especially rheumatoid and osteoarthritis. Inflammation of
the synovium, bone erosion and cartilage thinning are all symptoms of rheumatoid arthritis. Leukocyte
recruitment occurs during the acute inflammatory phase, resulting in tissue damage. Taurine, which
has a high neutrophil concentration, inhibits TNF- and protects against spinal cord injury52 while, also
acting as an anti-inflammatory and antioxidant

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3243 (793%) Leucine

Mitochondria UA S271 UA
A

UA
tRNA
Leu
S A (10%)
EL A

A
[MELAS] M Mutated AS
Leu (UUR)
tRNA Taurine
Leucine
N D1 Taurine

ND
N
deficiency

D6

5
Human
mtDNA
ND2

UAA UAA UAA

ND
LS N D6 tRNALeu (UUR) AS

4
ND UUG UUG
3 mt mRNA Multiple UUG-containing
HS
mt mRNA (eg., ND6)

mt IS

mt IM

mt matrix
ND6 is one of
O2 H20
44 subunits
of complex I ADP ATP

Fig. 2: Comparison of MELAS and taurine deficiency in mitochondria50

Taurine and central nervous system:

C Stroke: Glutamate toxicity, which overstimulates receptors and causes hyperexcitability and
toxicity, is what causes stroke. In Fig. 3, taurine, a neuroprotective compound reduces
Ca2+, raises the Bcl-2/Bad ratio and inhibits ER stress to counteract glutamate damage53. It might
lessen the severity of strokes, lessen ROS produced by NADPH oxidase and downregulate
Nox2/Nox454
C Neurodegenerative diseases, such as Alzheimer’s, Huntington’s and Parkinson’s disease:
Cell death, mitochondrial membrane collapse, calcium overload and increased ROS generation are
all symptoms of neurodegenerative illnesses like stroke. Degenerative illnesses cause
abnormalities in the respiratory chain; taurine therapy may lessen the severity of Parkinson’s
disease55,56
C Fragile X Syndrome and Succinic Semialdehyde Dehydrogenase (SSADH) deficiency: Fragile mice
with the genetic ailment fragile X syndrome, which causes behavioral issues and intellectual deficits,
have better memory retention. In SSADH-deficient individuals, taurine therapy has been demonstrated
to enhance social behavior, coordination and activity2
C Epilepsy: Unbalances between excitatory and inhibitory neurotransmitters are the cause of seizures.
Seizures brought on by stimulants are reduced by taurine57
C Retinal degeneration: The loss of photoreceptors and retinal degeneration are connected to taurine,
a crucial vitamin for cats58. Taurine insufficiency has been linked to nuclear ganglion cell loss and
degeneration, according to studies Gaucher et al.59. Vigabatrin, an anti-epileptic drug, can cause
retinal degeneration60. In two individuals with succinic semialdehyde dehydrogenase insufficiency,
taurine therapy partially mitigates the retinal damage brought on by vigabatrin treatment2,61

Repro-protective effects: Taurine promotes spermatogenesis, maturation and the activity of the
testicular dehydrogenases (3-HSD, 17-HSD, G6PDH and LDH-X) and electrogenic pumps (Na+/K+, Ca2+,
Mg2+ and H+-ATPase), as well as sexual ability in male animals62-65. It might lessen pathological harm to
the male reproductive system, such as oxidative harm35, reperfusion harm66-68 and difficulties brought on
by diabetes69. Through processes such as decreased oxidative stress, higher antioxidant capacity,
inflammation, apoptosis and improved sperm mitochondrial energy metabolism, taurine also functions
as a preventive agent against toxic damage from exogenous substances35,70-72. Taurine has also been linked
to sperm preservation in hypothermia62,64.

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Stroke
Neurodegenerative diseases
(e.g., Alzheimer, Huntington Heart failure
and Parkinson) Hypertension
FXS and SSDD Atherosclerosis
Epilepsy Ischemia-reperfusion injury
Retinal degeneration Myocardial arrhythmias

MELAS
Muscle contraction
MELAS
Sarcopenia
Diabetes mellitus
Duchenne muscular dystrophy
Arthritis
Myotonic dystrophy
Oxidative stress

Fig. 3: Taurine-mediated protection against pathology and disease53

Hemato-protective effects: Taurine is required by blood cells, particularly neutrophils, lymphocytes and
platelets73. Taurine is an essential component of energy drinks and healthy foods74. In fish, taurine
suppresses hemolysis and perinatal taurine supplementation affects hematological parameters75. Taurine
therapy inhibits hematotoxicity caused by marijuana bromate76.

Retino-protective effects: Retinal cells are involved in the neurodegenerative process of OS, which calls
for balanced redox signalling and antioxidant activity. Rodents have an abundance of taurine, an amino
acid that may be used to cure and prevent retinopathies such as retinitis pigmentosa41,61,77.

Anti-aging effects: A study shows that taurine supplementation may slow down the aging process, thus
benefiting older individuals8.

Reno-protective effects: Taurine is a known dietary supplement necessary for the prevention of kidney
diseases such as acute kidney injury, glomerulonephritis, renal failure and diabetic nephropathy78-80.
It controls the actions of renal cells, has anti-inflammatory and antioxidant characteristics and guards
against hypertension and diabetic nephropathy. However, its therapeutic potential is constrained,
necessitating more study.

Taurine is required for cellular homeostasis and other activities in organisms. Adverse reactions to
regularly given drugs influence its potential application in human health protection. This article introduces
taurine and discusses its pharmacological applications. However, more research on taurine’s toxicity is

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required before it can be made into a medicine. More study is needed to identify potential taurine
signaling targets in diverse human disorders and to validate previous studies.

CONCLUSION
For therapeutic purposes, natural bioactive substances like taurine are being studied, enabling more
complete and targeted clinical trials. Taurine is a substance that is found in excitable tissues and is crucial
for protecting systemic physiology from adverse effects. It is necessary to conduct more studies to
determine whether taurine deficiency may be utilized as a monitoring metric for maladaptive responses
and whether taurine during and after treatment can inhibit or reverse maladaptive responses. Clinical
studies are required to define the appropriate therapeutic dosages.

SIGNIFICANCE STATEMENT
Taurine has the ability to protect against a wide range of pathophysiological conditions, including
neurological abnormalities, mitochondrial malfunction, metabolic disease, reproductive failure and poor
fetal development. Despite different treatments, effective management continues to be a global concern.
Taurine formation design could lead to prospective medications for health maintenance and the treatment
of systemic illnesses. This review covers taurine’s physio-pharmacological capabilities and underlying
mechanisms, demonstrating its promise as a physiotherapeutic option.

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