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Ellagitannin geraniin: a review of the natural sources, biosynthesis, pharmacokinetics and biological effects

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Abstract

The discovery of the ellagitannin geraniin was made exactly 40 years ago. It is a secondary metabolite found in plants and is categorised as a hydrolysable tannin under the huge family of polyphenolic compounds. At present, the occurrence of geraniin has been verified in at least 71 plant species, many of which are used in traditional medicine. Hence, like other polyphenols, geraniin has also received widespread interest as a research focus to unearth its beneficial biological effects and therapeutic values apart from understanding its chemical properties, biosynthesis and interaction with the body system. Indeed, it has been demonstrated that geraniin possesses antioxidant, antimicrobial, anticancer, cytoprotective, immune-modulatory, analgesic properties besides exerting promising therapeutic effects on hypertension, cardiovascular disease and metabolic dysregulation. The objective of this review is to summarise the current knowledge about the basic chemistry, natural sources, isolation techniques, biosynthesis, pharmacokinetics and pharmacodynamics of geraniin. With reference to this information, the clinical significance, obstacles and future perspectives in geraniin research will also be scrutinised.

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Abbreviations

DPPH:

2,2-Diphenyl-1-picrylhydrazyl

IC50 :

50 % inhibition concentration

5-LOX:

5-Lipoxygenase

AGEs:

Advanced glycation end products

ACE:

Angiotensin-converting enzyme

COMT:

Catechol-O-methyl transferase

CSF-1:

Colony-stimulating factor-1

CYP1A1:

Cytochrome P450 1A1

DHHDP:

Dehydrohexahydrodiphenoyl

EV71:

Enterovirus-71

ERK:

Extracellular signal-regulated kinase

FRAP:

Ferric reducing antioxidant power

GSH:

Glutathione

Hsp90:

Heat shock protein 90

HBV:

Hepatitis B virus

HBeAg:

Hepatitis B virus e antigen

HBsAg:

Hepatitis B virus surface antigen

HSV:

Herpes simplex virus

HHDP:

Hexahydroxydiphenoyl

HPLC:

High performance liquid chromatography

HIV:

Human immunodeficiency virus

iNOS:

Inducible nitric oxide synthase

LPS:

Lipopolysaccharide

MIC:

Minimum inhibitory concentration

NF-kB:

Nuclear factor kB

Nrf2:

Nuclear factor-erythroid 2-related factor 2

ORAC:

Oxygen radical absorbance capacity

PGG:

Pentagalloylglucose

PPAR:

Peroxisome proliferator-activated receptor

PAI-1:

Plasminogen activator inhibitor-1

RNS:

Reactive nitrogen species

ROS:

Reactive oxygen species

RANKL:

Receptor activator of nuclear factor kB ligand

SOD:

Superoxide dismutase

tPA:

Tissue plasminogen activator

TGF:

Transforming growth factor

TNF:

Tumour necrosis factor

UDP:

Uridine diphosphate

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Acknowledgments

The work was supported by ScienceFund of Malaysia Ministry of Science, Technology and Innovation (MOSTI Grant No.: 02-02-10-SF0249) as well as internal grant from the School of Science, Monash University Malaysia.

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Cheng, H.S., Ton, S.H. & Abdul Kadir, K. Ellagitannin geraniin: a review of the natural sources, biosynthesis, pharmacokinetics and biological effects. Phytochem Rev 16, 159–193 (2017). https://doi.org/10.1007/s11101-016-9464-2

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