Abstract

Natural bioactive compounds present a better alternative to prevent and treat chronic diseases owing to their lower toxicity and abundant resources. (+)‐Dihydromyricetin (DMY) is a flavanonol, possessing numerous interesting bioactivities with abundant resources. This review provides a comprehensive overview of the recent advances in DMY natural resources, stereoisomerism, physicochemical properties, extraction, biosynthesis, pharmacokinetics, and biotransformation. Stereoisomerism of DMY should be considered for better indication of its efficacy. Biotechnological approach presents a potential tool for the production of DMY using microbial cell factories. DMY high instability is related to its powerful antioxidant capacity due to pyrogallol moiety in ring B, and whether preparation of other analogues could demonstrate improved properties. DMY demonstrates poor bioavailability based on its low solubility and permeability with several attempts to improve its pharmacokinetics and efficacy. DMY possesses various pharmacological effects, which have been proven by many in vitro and in vivo experiments, while clinical trials are rather scarce, with underlying action mechanisms remaining unclear. Consequently, to maximize the usefulness of DMY in nutraceuticals, improvement in bioavailability, and better understanding of its actions mechanisms and drug interactions ought to be examined in the future along with more clinical evidence.

Highlights

  • Rapid urbanization brought on by the modernization process of society has led to the general deterioration of human health manifested by less physical activity, and more high-energy food intake

  • This review provides a comprehensive overview of the recent advances in DMY natural resources, stereoisomerism, physicochemical properties, extraction, biosynthesis, pharmacokinetics, and biotransformation

  • It was found that extraction using 60% ethanol in water for 180 min at 60◦C from A. grossedentata leaves led to maximum DMY recovery rates [39]

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Summary

INTRODUCTION

Rapid urbanization brought on by the modernization process of society has led to the general deterioration of human health manifested by less physical activity, and more high-energy food intake. Flavonoids represent an important class of polyphenolic secondary metabolites, which can be subdivided into different subgroups depending on the structure. These subgroups are: flavones, flavonols, flavanones, flavanonols, flavanols or catechins, anthocyanins and chalcones [5]. Zhang et al / eFood 2021;2(4):164184 mechanisms, underlying DMY health effects, and application in food industries (Figure 1). Such comprehensive review identifies potential uses for DMY in food and functional food industries with emphasis on future needed research to help maximize its value. Homochiral (+) DMY with a (2R, 3R)-configuration is often considered as the default form of DMY in some articles, showing higher anti-inflammatory activity than (±) DMY [14]

NATURAL RESOURCES OF DMY
STEREOISOMERISM OF DMY
PHYSICO-CHEMICAL PROPERTIES AND STABILITY OF DMY
Solubility of DMY
Antioxidant activity of DMY
Stability of DMY
Solvent based extraction
Enzymatic extraction
Commonly used techniques
Chelating extraction
PHARMACOKINETICS AND BIOAVAILABILITY
PK studies of DMY in vitro
Simulated digestive system
Uptake and transport mechanism of DMY across human intestinal Caco-2 cells
PK study of DMY in vivo
Gut microbiota affecting PK of DMY
Self-nanoemulsifying drug delivery systems
Microemulsions
DMY encapsulated zein-caseinate nanoparticles
Enzymatic acylated DMY
Co-crystallization
Gastric floating formulations of DMY
Co- administration of DMY and other compounds
BIOTRANSFORMATION OF DMY IN DIFFERENT BIOLOGICAL SYSTEMS
Metabolites of DMY in fecal matter
Anticancer effects
Cardiovascular protective effects
Hepatoprotection
Protective effect of toxic injuries
Miscellaneous
10. TOXICOLOGY AND SAFETY
11.1.1. Inhibition of spoilage in meat products
11.1.2. Inhibition of lipid peroxidation in edible oils
11.1.3. Anti-browning agent in vegetables and fruit
11.2. Development of green and active packing for food preservation
11.3. Antibacterial agent in food industries
11.4. Antioxidation and hazardous substance reduction in food thermal processing
11.5. Stabilizer in preparation of food-grade Pickering emulsion gels
11.6. Functional supplement for alleviating alcohol intoxication
Findings
12. CONCLUSION AND FUTURE PERSPECTIVES

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