The pharmacological potential of hesperidin (original) (raw)
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The Journal of nutrition, 2006
Hesperidin is the predominant polyphenol consumed from citrus fruits and juices. However, hesperidin is proposed to have limited bioavailability due to the rutinoside moiety attached to the flavonoid. The aim of this study was to demonstrate in human subjects that the removal of the rhamnose group to yield the corresponding flavonoid glucoside (i.e., hesperetin-7-glucoside) will improve the bioavailability of the aglycone hesperetin. Healthy volunteers (n=16) completed the double-blind, randomized, crossover study. Subjects randomly consumed hesperetin equivalents supplied as orange juice with natural hesperidin ("low dose"), orange juice treated with hesperidinase enzyme to yield hesperetin-7-glucoside, and orange juice fortified to obtain 3 times more hesperidin than naturally present ("high dose"). The area under the curve (AUC) for total plasma hesperetin of subjects consuming hesperetin-7-glucoside juice was 2-fold higher than that of subjects consuming the ...
Molecules
Cancer represents one of the most frequent causes of death in the world. The current therapeutic options, including radiation therapy and chemotherapy, have various adverse effects on patients’ health. In this vista, the bioactive ingredient of natural products plays a vital role in disease management via the inhibition and activation of biological processes such as oxidative stress, inflammation, and cell signaling molecules. Although natural products are not a substitute for medicine, they can be effective adjuvants or a type of supporting therapy. Hesperidin, a flavonoid commonly found in citrus fruits, with its potential antioxidant, anti-inflammatory, and hepatoprotective properties, and cardio-preventive factor for disease prevention, is well-known. Furthermore, its anticancer potential has been suggested to be a promising alternative in cancer treatment or management through the modulation of signal transduction pathways, which includes apoptosis, cell cycle, angiogenesis, ER...
Benefits of hesperidin in central nervous system disorders: a review
Anatomy & Cell Biology, 2019
Citrus species contain significant amounts of flavonoids that possess antioxidant activities; furthermore, dietary citrus is not associated with adverse effects or cytotoxicity in healthy individuals. Hesperidin, which is an abundant flavanone glycoside in the peel of citrus fruits, possesses a variety of biological capabilities that include antioxidant and anti-inflammatory actions. Over the last few decades, many studies have been investigated the biological actions of hesperidin and its aglycone, hesperetin, as well as their underlying mechanisms. Due to the antioxidant effects of hesperidin and its derivatives, the cardioprotective and anti-cancer effects of these compounds have been widely reviewed. Although the biological activities of hesperidin in neurodegenerative diseases have been evaluated, its potential involvement in a variety of central nervous system (CNS) disorders, including autoimmune demyelinating disease, requires further investigation in terms of the underlying mechanisms. Thus, the present review will focus on the potential role of hesperidin in diverse models of CNS neuroinflammation, including experimental autoimmune encephalomyelitis, with special consideration given to its antioxidant and anti-inflammatory effects in neurodegenerative disease models. Additionally, current evidence provides information regarding the nutraceutical use of hesperidin to prevent various CNS disorders.
Revista Brasileira de Farmacognosia, 2014
Free radicals play an important role in stomach ulcer formation. The present investigation validates the anti ulcer activity of hesperidin, isolated from Citrus sinensis (L.) Osbeck, Rutaceae, through the assessment of its antioxidant potential over stomach mucosal tissue by histological examination. Hesperidin was isolated from the dried peel of C. sinensis, and authenticated by TLC, IR and HPLC. The anti-ulcerogenic potential of this fruit was assessed using indomethacin and hypothermic restrain stress-induced ulceration models on rats at 150, 300 and 450 mg/kg dose orally. The parameters measured were gastric pH, volume, free and total acidity, ulcer index, and mucin, glutathione, super oxide dismutase, catalase and protein content. Hesperidin at 300 and 450 mg/kg dose showed significant (p < 0.01-0.001) increase in pH, decrease in acidity and ulcer index against indomethacin and hypothermic restrain stress, along with histological evidence of cytoprotection. Glutathione, super oxide dismutase, catalase and mucin levels increased significantly at 450 mg/kg (p < 0.05-0.001) after indomethacin ulceration, whereas hypothermic restrain stress only increased glutathione and mucin levels. Hesperidin prevents oxidative cell injury by significant rise of super oxide dismutase, glutathione and catalase levels in gastric mucosa. Hesperidin allowed the regeneration of ulcerated tissue, and prevented hemorrhagic injury of gastric mucosa. The potential anti-ulcer effect of hesperidin may be due to antioxidant, mucoprotective and cytoprotective activities.
Phytotherapy Research, 2019
Previous studies have led to conflicting results regarding the effect of hesperidin supplementation on cardiometabolic markers. This study aimed to evaluate the efficacy of hesperidin supplementation on lipid profile and blood pressure through a systematic review and meta-analysis of randomized controlled trials (RCTs). PubMed, Web of Science, Scopus, and Google Scholar, as well as the reference lists of the identified relevant RCTs, were searched up to May 2018. Effect sizes were pooled by using the random effects model. Ten RCTs (577 participants) were eligible to be included in the systematic review. The meta-analysis revealed that hesperidin supplementation had no effect on serum total cholesterol (weighted mean difference [WMD] = −1.04 mg/dl; 95% confidence interval [CI]: −5.65, 3.57), low-density lipoprotein cholesterol (WMD = −1.96 mg/dl; 95% CI [−7.56, 3.64]), high-density lipoprotein cholesterol (WMD = 0.16 mg/dl; 95% CI [−1.94, 2.28]), and triglyceride (WMD = 0.69 mg/dl; 95% CI [−5.91, 7.30]), with no significant between-study heterogeneity. Hesperidin supplement also had no effect on systolic (WMD = −0.85 mmHg; 95% CI [−3.07, 1.36]) and diastolic blood pressure (WMD = −0.48 mmHg; 95% CI [−2.39, 1.42]). Hesperidin supplementation might not improve lipid profile and blood pressure. Future well-designed trials are still needed to confirm these results.
Nutrients
Neurodegenerative disorders affect more than fifty million Americans each year and represent serious health threats as the population ages. Neuroinflammation and oxidative stress are critical in the onset, progression, and pathogenesis of neurodegenerative diseases such as Alzheimer’s (AD), Parkinson’s (PD), and amyotrophic lateral sclerosis (ALS). A wide range of natural compounds has been investigated because of their antioxidant, anti-inflammatory, and neuroprotective properties. The citrus flavonoid hesperetin (HPT), an aglycone of hesperidin found in oranges, mandarins, and lemons, has been extensively reported to exert neuroprotective effects in experimental models of neurogenerative diseases. This review has compiled multiple studies on HPT in both in vivo and in vitro models to study neurodegeneration. We focused on the modulatory effects of hesperetin on the release of cellular anti-inflammatory and antioxidative stress mediators. Additionally, this review discusses the hes...
Journal of Agricultural and Food Chemistry, 2008
Significantly, much of the activity of Citrus flavonoids appears to impact blood and microvascular endothelial cells, and it is not surprising that the two main areas of research on the biological actions of Citrus flavonoids have been inflammation and cancer. Epidemiological and animal studies point to a possible protective effect of flavonoids against cardiovascular diseases and some types of cancer. Although flavonoids have been studied for about 50 years, the cellular mechanisms involved in their biological action are still not completely known. Many of the pharmacological properties of Citrus flavonoids can be linked to the abilities of these compounds to inhibit enzymes involved in cell activation. Attempts to control cancer involve a variety of means, including the use of suppressing, blocking, and transforming agents. Suppressing agents prevent the formation of new cancers from procarcinogens, and blocking agents prevent carcinogenic compounds from reaching critical initiation sites, while transformation agents act to facilitate the metabolism of carcinogenic components into less toxic materials or prevent their biological actions. Flavonoids can act as all three types of agent. Many epidemiological studies have shown that regular flavonoid intake is associated with a reduced risk of cardiovascular diseases. In coronary heart disease, the protective effects of flavonoids include mainly antithrombotic, anti-ischemic, anti-oxidant, and vasorelaxant. It is suggested that flavonoids decrease the risk of coronary heart disease by three major actions: improving coronary vasodilatation, decreasing the ability of platelets in the blood to clot, and preventing low-density lipoproteins (LDLs) from oxidizing. The anti-inflammatory properties of the Citrus flavonoids have also been studied. Several key studies have shown that the anti-inflammatory properties of Citrus flavonoids are due to its inhibition of the synthesis and biological activities of different pro-inflammatory mediators, mainly the arachidonic acid derivatives, prostaglandins E 2 , F 2 , and thromboxane A 2. The anti-oxidant and anti-inflammatory properties of Citrus flavonoids can play a key role in their activity against several degenerative diseases and particularly brain diseases. The most abundant Citrus flavonoids are flavanones, such as hesperidin, naringin, or neohesperidin. However, generally, the flavones, such as diosmin, apigenin, or luteolin, exhibit higher biological activity, even though they occur in much lower concentrations. Diosmin and rutin have a demonstrated activity as a venotonic agent and are present in several pharmaceutical products. Apigenin and their glucosides have been shown a good anti-inflammatory activity without the side effects of other anti-inflammatory products. In this paper, we discuss the relation between each structural factor of Citrus flavonoids and the anticancer, antiinflammatory, and cardiovascular protection activity of Citrus flavonoids and their role in degenerative diseases.