Hesperetin’s health potential: moving from preclinical to clinical evidence and bioavailability issues, to upcoming strategies to overcome current limitations

Salehi, Bahare; Cruz‐Martins, Natália; Butnariu, Monica; Sărac, Ioan; Bagiu, Iulia Cristina; Ezzat, Shahira M.; Wang, Jinfan; Koay, Aaron; Sheridan, Helen; Adetunji, Charles Oluwaseun; Semwal, Prabhakar; Schoebitz, Mauricio; Martorell, Miquel; Sharifi‐Rad, Javad

doi:10.1080/10408398.2021.1875979

Cited by 31 publications

(22 citation statements)

References 142 publications

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“…Medicinal plants have shown immense pharmacological activities like fungicidal, bactericidal, virucidal, analgesic, anticancer, anti-inflammatory, neuroprotective, sedative, and antioxidant, due to the presence of significant phytochemicals or active compounds including flavonoids, phenols, terpenoids alkaloids, tannins, saponins, and glycosides [ 140 – 143 ].…”

Section: The Challenge Of Standardizing Extract Toxicity and Bioavailability Of The Extractmentioning

confidence: 99%

“…14 Oxidative Medicine and Cellular Longevity and antioxidant, due to the presence of significant phytochemicals or active compounds including flavonoids, phenols, terpenoids alkaloids, tannins, saponins, and glycosides [140][141][142][143]. Presently, excessive use of synthetic drugs and antibiotics has developed serious side effects, toxicity, and resistance against pathogenic microorganisms, which has limited their use in many countries; therefore, researchers are now paying more attention to traditional herbal medicines and their active compounds to fight against diseases and disorders [144][145][146].…”

Section: Thementioning

confidence: 99%

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Nutraceutical Profiling, Bioactive Composition, and Biological Applications of Lepidium sativum L.

Painuli

Quispe

Herrera‐Bravo

et al. 2022

Oxidative Medicine and Cellular Longevity

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The roots, leaves, and seeds of Lepidium sativum L., popularly known as Garden cress in different regions, have high economic importance; although, the crop is particularly cultivated for the seeds. In traditional medicine, this plant has been reported to possess various biological activities. This review is aimed at providing updated and critical scientific information about the traditional, nutritional, phytochemical, and biological activities of L. sativum. In addition, the geographic distribution is also reviewed. The comprehensive literature search was carried out with the help of different search engines PubMed, Web of Science, and Science Direct. This review highlighted the importance of L. sativum as an edible herb that possesses a wide range of therapeutic properties along with high nutritional values. Preclinical studies (in vitro and in vivo) displayed anticancer, hepatoprotective, antidiabetic, hypoglycemic, antioxidant, antimicrobial, gastrointestinal, and fracture/bone healing activities of L. sativum and support the clinical importance of plant-derived bioactive compounds for the treatment of different diseases. Screening of literature revealed that L. sativum species and their bioactive compounds may be a significant source for new drug compounds and also could be used against malnutrition. Further clinical trials are needed to effectively assess the actual potential of the species and its bioactive compounds.

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Section: The Challenge Of Standardizing Extract Toxicity and Bioavailability Of The Extractmentioning

confidence: 99%

Section: Thementioning

confidence: 99%

Nutraceutical Profiling, Bioactive Composition, and Biological Applications of Lepidium sativum L.

Painuli

Quispe

Herrera‐Bravo

et al. 2022

Oxidative Medicine and Cellular Longevity

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“…Hesperidin has been reported to be resistant to degradation in the stomach and small intestine, in vitro and in vivo, but deconjugated on reaching the proximal colon [19][20][21]. Hesperetin is produced upon release of the rutinose moiety by the gut microbial rhamnosidases and further phase-II conjugations to yield circulating metabolites with anti-inflammatory and cardioprotective effects in preclinical studies [21][22][23][24]. However, the low hesperidin solubility hampers its bioavailability and microbial metabolism, yielding a high inter-individual variability in the production of hesperetin derivatives [18], which could prevent consistent health-related evidence [25,26].…”

Section: Introductionmentioning

confidence: 99%

New Insights into the Metabolism of the Flavanones Eriocitrin and Hesperidin: A Comparative Human Pharmacokinetic Study

et al. 2021

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The intake of hesperidin-rich sources, mostly found in orange juice, can decrease cardiometabolic risk, potentially linked to the gut microbial phase-II hesperetin derivatives. However, the low hesperidin solubility hampers its bioavailability and microbial metabolism, yielding a high inter-individual variability (high vs. low-producers) that prevents consistent health-related evidence. Contrarily, the human metabolism of (lemon) eriocitrin is hardly known. We hypothesize that the higher solubility of (lemon) eriocitrin vs. (orange) hesperidin might yield more bioavailable metabolites than hesperidin. A randomized-crossover human pharmacokinetic study (n = 16) compared the bioavailability and metabolism of flavanones from lemon and orange extracts and postprandial changes in oxidative, inflammatory, and metabolic markers after a high-fat-high-sugars meal. A total of 17 phase-II flavanone-derived metabolites were identified. No significant biomarker changes were observed. Plasma and urinary concentrations of all metabolites, including hesperetin metabolites, were higher after lemon extract intake. Total plasma metabolites showed significantly mean lower Tmax (6.0 ± 0.4 vs. 8.0 ± 0.5 h) and higher Cmax and AUC values after lemon extract intake. We provide new insights on hesperetin-eriodictyol interconversion and naringenin formation from hesperidin in humans. Our results suggest that regular consumption of a soluble and eco-friendly eriocitrin-rich lemon extract could provide a circulating concentration metabolites threshold to exert health benefits, even in the so-called low-producers.

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“…In addition to this antioxidant effect, it exerts positive effects on synaptic plasticity in cortical and hippocampal neurons ( Vauzour et al 2007 ). Only very few clinical trials have established the cognitive effects of hesperetin, which enhances cerebral blood flow and cognition ( Salehi et al 2021 ).…”

Section: Discussionmentioning

confidence: 99%

Dietary Intake of Polyphenols Enhances Executive/Attentional Functioning and Memory with an Improvement of the Milk Lipid Profile of Postpartum Women from Argentina

et al. 2022

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Puerperium may lead to memory and executive/attentional complaints that interfere with women’s daily life. This might be prevented by dietary compounds, such as neuroprotective polyphenols. Their bioactivity depends on their effects on lipid metabolism in different tissues, such as the brain, fat, and breast. Thus, a polyphenol-related cognitive improvement may be associated with changes of lipids in human milk, which are key for infant neurodevelopment. A cross-sectional study was conducted on 75 postpartum women from Córdoba (Argentina), involving several neuropsychological tests. Diet was registered to identify polyphenol intake and food pattern adherence, with sociodemographic and other psychological variables (insomnia, stress, subjective cognitive complaints) being also studied. Triacylglycerols, cholesterol, and their oxidative forms were analyzed as milk biomarkers. Multivariate statistical methods were applied. Results confirmed that women who consumed polyphenols presented better executive/attentional performance (i.e., higher correct responses, conceptual level responses, complete categories, verbal fluency; lower attentional interferences, and perseverative errors) and word retention with lower interference. Polyphenols were positively associated with milk lipids, which were higher in women with better cognition. Furthermore, they had lower oxidized triacylglycerols. In conclusion, polyphenolic intake during postpartum may improve executive/attentional functioning, memory, and milk lipid profile.

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Hesperetin’s health potential: moving from preclinical to clinical evidence and bioavailability issues, to upcoming strategies to overcome current limitations

Cited by 31 publications

References 142 publications

Nutraceutical Profiling, Bioactive Composition, and Biological Applications of Lepidium sativum L.

Nutraceutical Profiling, Bioactive Composition, and Biological Applications of Lepidium sativum L.

New Insights into the Metabolism of the Flavanones Eriocitrin and Hesperidin: A Comparative Human Pharmacokinetic Study

Dietary Intake of Polyphenols Enhances Executive/Attentional Functioning and Memory with an Improvement of the Milk Lipid Profile of Postpartum Women from Argentina

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