An Overview on Ethnopharmacological, Phytochemical, and Clinical Significance of Selected Dietary Polyphenols

 

Arjun Singh1*, Rupendra Kumar2

1Department of Medicine, Sidney Kimmel Medical College, Thomas Jefferson University,

Philadelphia, PA 19107, United States.

2Department of Pharmacognosy, School of Pharmaceutical Sciences,

Bhagwant University, Sikar Road, Ajmer, Rajasthan305004, India.

*Corresponding Author E-mail: arjunphar@gmail.com

 

ABSTRACT:

In recent years, there has been a significant increase in interest in plant-derived compounds and their function in sustaining health and avoiding illness. These substances are referred to as phytochemicals or nutraceuticals, which are essentially defined as a food or component of a food that delivers medicinal or health advantages. Natural bioactive phytochemicals, particularly those found in fruits and vegetables, are significant food components because they may provide health advantages associated to the prevention of a variety of diseases, including obesity. Health problems are now a major public health concern all over the world due to the clinical complications it causes, which have a significant impact on life expectancy. Cancer and cardiovascular disease, in particular, are the leading causes of death associated with obesity. However, convincing proof for identification is lacking.

 

KEYWORDS: Plant derived, Herbal medicine, Ethnopharmacological, Phytochemicals, Polyphenols.

 

 


INTRODUCTION:

Polyphenols are a group of naturally occurring secondary metabolites that may be found in a variety of foods, including fruits, vegetables, cereals, and drinks like red wine1,2. These secondary metabolites have been shown to be important in the protection of a variety of disorders, including cancer and cardiovascular disease3,4. Polyphenols also provide protection against UV light and infections, among other things. Bitterness, astringency, colour, taste, and odour are all characteristics of polyphenols in food.

 

Oxidative stability against oxidative stress is a major trait that plays a vital influence in sick states. Due to the multiple health advantages of food polyphenols, substantial study has been undertaken, and it strongly

 

supports that frequent use of polyphenol-rich dietary supplements reduces the risk of cardiovascular illnesses6. Polyphenols have been linked to a variety of different illnesses, including diabetes, osteoporosis, and neurodegenerative diseases like Alzheimer's7. More than 8000 polyphenolic chemicals have been discovered in various plant species, some of which may be found in the fruits of plants like strawberries and berries. Over 8000 polyphenolic chemicals have been isolated from diverse plant species, some of which may be found in plant fruits such as strawberries and berries. The majority of plant phenols are derived from a common intermediary such as phenylalanine or a separate precursor such as shikimic acid8. The most prevalent types are conjugated with structural changes such hydroxylation, methoxylation, and glycosylation. Amines, carboxylic and organic acids, and lipids connected with other phenols are examples of structural relationships9.

 


 

Figure 1: A flow diagram of pharmacological effects of different polyphenols and their chemical structures.

 


Polyphenols are classified into several classes based on the arrangement and quantity of phenol rings present, as well as the addition of functional groups to the phenol rings. Polyphenols are classified as flavonoids, phenolic acids, stilbenes, and lignans10-15.

 

Several environmental and edaphic factors, including as maturity, harvest timing, soil type, sun exposure, the presence of surrounding alleliopathic crops, and rainfall, all contribute to polyphenol concentration16-20. During ripening, the concentration of phenolic acids decreases while the content of anthocyanin increases21-25.

 

Several epidemiological studies have found a substantial link between polyphenol-rich diet and illness prevention. Polyphenol-rich foods have been proven to have therapeutic capabilities in a variety of disorders, including Parkinson's, stroke, several forms of cancer, and coronary heart disease26-30. As a result, we now have a better grasp of polyphenols' biological activity and mechanism. Polyphenols have been found to reduce oxidative stress when combined with other dietary components such as vitamin C, vitamin E, and carotenoids.


 

 

Figure 2: A flow diagram of classification of polyphenols and their study selection of initial and updated literature searches (inclusion and exclusion) for the systematic review based on the scope of polyphenols.

 


 

Figure 3: Some chemicals structures of major Phyto polyphenols

 


METHODS:

Materials:

The available information on various plants based traditionally used polyphenols for pharmacological, ethnomedicinal, phytochemical and treatment of disorders was collected through electronic databases searches using PubMed, Scopus, ScienceDirect, Google Scholar, and Web of Science, as well as a library search for articles published in peer-reviewed journal articles in this review survey.


 

Table 1. The Effect of Dietary Polyphenols on DNA Methylation31-45

Dietary

polyphenol

Origin of compound

Mechanism on DNA methylation

Gene targets

Caffeic acid

Catechol-containing

coffee polyphenols

Inhibition of concentration-dependent manner DNA methylation catalyzed by DNMT1

Inhibition of methylation of the promoter region of RARb

RARb

Chlorogenic acid

Catechol-containing

coffee polyphenols

Inhibition of concentration-dependent manner

DNA methylation catalyzed by DNMT1

Inhibition of methylation of the promoter region of RARb

RARb

Curcumin

Turmeric

Inhibition of DNMT1 analog through blocking of a catalytic group in DNMT1

 

Epigallocatechin-3-

gallate (EGCG)

Green tea

Formation of S-adenosyl-L-homocysteine (SAH)

SAH—potent inhibitor of DNMT

Formation of hydrogen bonds with different

residues in the catalytic pocket of DNMT

Inhibitor of human dihydrofolate reductase

Tumor suppressor genes: p16,

RAR, MGMT, MLH1

Genistein

Phytoestrogens from

soy bean

Dose-dependent inhibition of the DNMT

Competitive inhibition of substrate poly(dI-dC)

Noncompetitive inhibition of SAM

p16, RARb, MGMT

Isothiocyanates

Cruciferous vegetables

Demethylation and reexpression of GSTP1

GSTP1

Lycopene

Carotenoid pigment

from tomatoes

Partial demethylation of promoter of GSTP1 tumor

suppressor gene

GSTP1 tumor suppressor gene

Rosmarinic acid

Lamiaceae herbs

Potent inhibitor of DNMT1

RASSF1A, GSTP1, and HIN-1

 

Table 2. The Pharmacological Effect of Dietary Polyphenols46-51

Ailment

Polyphenol source/compound

Study results

Cardiovascular disease

Grape seed extract (proanthocyanidins)

Decrease of systolic and diastolic blood pressure by approx. 5 mm Hg in hypertensive women

Cocoa powder in skimmed milk

Increased HDL and decreased oxLDL in subjects with high coronary heart disease risk

Dark chocolate (epicatechin and catechin)

Increased HDL and decreased total cholesterol/HDL ratio and LDL/HDL ratio in normal weight obese women

Olive oil

Decreased systolic and diastolic blood pressure by approx. 7 mm Hg and lower oxLDL in pre- and mild hypertensive women

Green tea extract (EGCG)

Reduction of blood pressure, inflammatory biomarkers, and oxidative stress Improvement of insulin resistance in obese hypertensive patients

Cancer

Citrus polyphenols

Cytotoxic to oral and cervical cancer cells

Tea polyphenols

Lower risk of development of colon cancer in humans

Polyphenol-rich extract of Salvia chinensis

Cytotoxic to the human breast cancer cells, human lung cancer cells, human colon cancer cells, and human pancreatic cancer cells

Soy isoflavone daidzein

Induces breast cancer cell apoptosis by generation of ROS

Curcumin

Induces gastric cancer cell apoptosis by generation of ROS

Anthocyanins, quercetin, resveratrol

Anti-skin cancer agents, prevention of carcinogenesis and metastasis through several mechanisms

Diabetes

Anthocyanin-rich bilberry extract

Improvement of hyperglycemia and insulin sensitivity in type II diabetic mice

Chlorogenic and ferulic acid

Enhance glucose uptake and show synergistic effect with antidiabetic drugs

Phenolic extract of Castanea mollissima

Decrease in serum glucose, triglyceride, total cholesterol and LDL in diabetic rats; significant body weight loss

Obesity

Mulberry leaf polyphenol extract (quercetin, caffeic acid, hydroxyflavin, hesperetin)

Inhibition of differentiation preadipocytes

EGCG

Dose-dependent reduction of body weight of New Zealand black mice

Polyphenol-rich peach and plum juice

Protection from obesity-induced metabolic disorders (hyperglycemia, insulin and leptin resistance, dyslipidemia)

Only plum juice prevented body weight gain in Zucker rats

Black tea polyphenol extract

Inhibition of pancreatic lipase activity—inhibition of lipid absorption

Cognitive disorders

Polyphenol-rich blueberry extract

Cognitive enhancement in adult mice (improvement in learning and memory); higher brain antioxidant properties

Blueberry juice

Improvement of memory performance in older adults

Wild blueberry extract

Better episodic memory performance and improvement of cardiovascular function in elderly population

Resveratrol

Enhancement of cognitive and cerebrovascular functions in postmenopausal women

Other

Anthocyanin enriched bilberry extract

Improves visual function by antioxidant activity in retinal pigment epithelium

Green tea polyphenols

Protection of retinal pigment epithelial cells from UV-B damage

Polyphenol-rich extract from tea (Camellia sinensis)

Anti-inflammatory effects on acute and immunological inflammation in mice

Grape seed extract

Antiallergic activity through inhibition of degranulation of inflammatory mediators, reduction of expression of IgE receptors and reduction of calcium influx in mast cells

Concentrated pomegranate juice

Beneficial effects on blood pressure, triglycerides (TG), and HDL levels in polycystic ovary (PCO) women

Curcumin

Partial support for the antidepressant effects in people with major depressive disorder (particularly atypical depression)

 


CONCLUSION AND FUTURE PROSPECTIVE:

Several studies using epidemiological studies, animal studies, and human clinical trials show that polyphenols have therapeutic effects on a variety of pathologies, including cardiovascular disease, atherosclerosis, and inflammation9; they also have anticancer10 and neuroprotective properties. These therapeutic processes are accomplished through their considerable antioxidant qualities22, inhibition of intracellular kinase activity, disruption of cell-to-cell communication through binding to cell surface receptors, and disruption of cell plasma membrane integrity. Several epidemiological and clinical investigations have demonstrated polyphenols' medicinal potential and advantages.

 

However, the precise significance of these molecules has yet to be determined. Beneficial benefits of polyphenol dietary supplementation can be attained at supraphysiological quantities, which have been shown to be hazardous. Understanding the mechanisms, such as inhibitory activity/potency of these molecules of the specific functional group, enables for the development of more powerful and selective analogues. Extensive structure-activity studies have resulted in the development of more structurally selective analogues, such as the polyphenolic metabolite quercetin-3-O-amino acid esters, which were more beneficial for Src tyrosine kinase than EGF receptor kinase. One key technique used to boost the potency of the chemicals is to employ analogues of the original drug.

CONFLICT OF INTEREST:

The author has no conflicts of interest.

 

ACKNOWLEDGMENTS:

The author would like to thank NCBI, PubMed and Web of Science for the free database services for their kind support during this study.

 

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Received on 14.03.2022                    Modified on 17.08.2022

Accepted on 02.12.2022                   ©AJRC All right reserved

Asian J. Research Chem. 2023; 16(1):8-12.

DOI: 10.52711/0974-4150.2023.00002