Abstract
Crocetin is an aglycone of crocin naturally occurring in saffron and produced in biological systems by hydrolysis of crocin as a bioactive metabolite. It is known to exist in several medicinal plants, the desiccative ripe fruit of the cape jasmine belonging to the Rubiaceae family, and stigmas of the saffron plant of the Iridaceae family. According to modern pharmacological investigations, crocetin possesses cardioprotective, hepatoprotective, neuroprotective, antidepressant, antiviral, anticancer, atherosclerotic, antidiabetic, and memory-enhancing properties. Although poor bioavailability hinders therapeutic applications, derivatization and formulation preparation technologies have broadened the application prospects for crocetin. To promote the research and development of crocetin, we summarized the distribution, preparation and production, total synthesis and derivatization technology, pharmacological activity, pharmacokinetics, drug safety, drug formulations, and preparation of crocetin.
Highlights
Crocetin is an aglycone of crocin naturally occurring in saffron and is produced in biological systems by hydrolysis of crocin as a bioactive metabolite (Reddy et al, 2020)
Inhibits the proliferation of cancer cells by inducing cell cycle arrest at the G1 phase Attenuates the serum levels of IL-1β, tumor necrosis factor (TNF)-α, polymorphonuclear granulocytes (PMN), and nitrates Upregulates COX-2 expression Increases the activities of glutathione metabolic enzymes and antioxidant enzymes Inhibits polyamine synthesis and glycoprotein changes Inhibits lactate dehydrogenase (LDH) Interferes with topoisomerase II to induce DNA damage and apoptosis, inhibits the migration and invasion of PCa cells Reduces the gene expression and efflux function of multidrug resistance protein 2 (MRP2) transporters Inhibit cells proliferation and differentiation Reduces the expression of prosurvival genes and multidrug resistance proteins and inhibits tyrosyl DNA phosphodiesterase 1 Inhibits the production of myeloperoxidase and hydrogen peroxide Reduces protein levels of tyrosinase and microphthalmia-associated transcription factor
The results demonstrated that crocetin had no significant effect on the expression of HERG potassium channel protein, excluding its inhibitory effect on the expression of HERG potassium channel protein, which may result in QT prolongation
Summary
Crocetin is an aglycone of crocin naturally occurring in saffron and is produced in biological systems by hydrolysis of crocin as a bioactive metabolite (Reddy et al, 2020). Crocetin (C20H24O4; MW: 328.4 g/mol) displays a polyunsaturated conjugated acid structure, 4 side-chain methyl groups, and seven conjugated double bonds, including cis-form and trans-form (Peng et al, 2007). Given the presence of a long chain of conjugated carbon-carbon double bonds, crocetin is sensitive to thermal treatment, light, and pH. It undergoes oxidation and isomerization when exposed to light and heat (Na et al.). This systematic review outlines the distribution, preparation and production, total synthesis and derivatization technology, pharmacological activity, pharmacokinetics, drug safety, drug. Formulation, and preparation of crocetin, which could provide broad research prospects for exploring and utilizing crocetin
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