Metabolism and pharmacological activities of the natural health-benefiting compound diosmin

Zheng, Yizhou; Zhang, Rui; Shi, Weimei; Li, Linfu; Liu, Hai; Chen, Zhixi; Wu, Longhuo

doi:10.1039/d0fo01598a

Cited by 73 publications

(44 citation statements)

References 167 publications

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“…The agent for AD treatment through upregulates NEP should be safe and effective. Diosmin is a flavonoid isolated from citrus that is widely used in the clinical management of chronic venous insufficiency and varicose veins 55 . Many studies showed that diosmin has various pharmacological activities, including anti-inflammation, anti-diabetes, anti-cancer and organ protection 55 .…”

Section: Discussionmentioning

confidence: 99%

“…Diosmin is a flavonoid isolated from citrus that is widely used in the clinical management of chronic venous insufficiency and varicose veins 55 . Many studies showed that diosmin has various pharmacological activities, including anti-inflammation, anti-diabetes, anti-cancer and organ protection 55 . I3C is a compound isolated from cruciferous vegetables and is used as a dietary supplement.…”

Section: Discussionmentioning

confidence: 99%

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Activating AhR alleviates cognitive deficits of Alzheimer's disease model mice by upregulating endogenous Aβ catabolic enzyme Neprilysin

Qian

Yang

et al. 2021

Theranostics

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Rationale: Neprilysin (NEP) is a major endogenous catabolic enzyme of amyloid β (Aβ). Previous studies have suggested that increasing NEP expression in animal models of Alzheimer's disease had an ameliorative effect. However, the underlying signaling pathway that regulates NEP expression remains unclear. The aryl hydrocarbon receptor (AhR) is a ligand-activated cytoplasmic receptor and transcription factor. Recent studies have shown that AhR plays essential roles in the central nervous system (CNS), but its physiological and pathological roles in regulating NEP are not entirely known. Methods: Western blotting, immunofluorescence, quantitative RT-PCR and enzyme activity assay were used to verify the effects of AhR agonists on NEP in a cell model (N2a) and a mouse model (APP/PS1). Luciferase reporter assay and chromatin immunoprecipitation (ChIP) assay were conducted to investigate the roles of AhR in regulating NEP transcription. Object recognition test and the Morris water maze task were performed to assess the cognitive capacity of the mice. Results: Activating AhR by the endogenous ligand L-Kynurenine (L-KN) or FICZ, or by the exogenous ligand diosmin or indole-3-carbinol (I3C) significantly increases NEP expression and enzyme activity in N2a cells and APP/PS1 mice. We also found that AhR is a direct transcription factor of NEP. Diosmin treatment effectively ameliorated the cognitive disorder and memory deficit of APP/PS1 transgenic mice. By knocking down AhR or using a small molecular inhibitor targeting AhR or NEP, we found that diosmin enhanced Aβ degradation through activated AhR and increased NEP expression. Conclusions: These results indicate a novel pathway for regulating NEP expression in neurons and that AhR may be a potential therapeutic target for the treatment of Alzheimer's disease.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Activating AhR alleviates cognitive deficits of Alzheimer's disease model mice by upregulating endogenous Aβ catabolic enzyme Neprilysin

Qian

Yang

et al. 2021

Theranostics

View full text Add to dashboard Cite

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“…Hesperidin, one of the principal polyphenols in lemon, have been shown to possess various biological properties, such as anti-oxidant, anti-inflammatory, and anti-cancer effects [19][20][21]. Diosmin, eriocitrin, and narirutin are also reported to contribute to health care [22][23][24]. In addition, the supplemental dietary fibers influence the activity and composition of intestinal microflora, which are closely related to our health.…”

Section: Introductionmentioning

confidence: 99%

Citrus limon Peel Powder Reduces Intestinal Barrier Defects and Inflammation in a Colitic Murine Experimental Model

Tinh

Sitolo

Yamamoto

et al. 2021

Foods

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This study examines the ameliorative effects of lemon (Citrus limon) peel (LP) powder on intestinal inflammation and barrier defects in dextran sulfate sodium (DSS)-induced colitic mice. The whole LP powder was fractionated into methanol (MetOH) extract and its extraction residue (MetOH residue), which were rich in polyphenolic compounds and dietary fibers, respectively. Mice were fed diets containing whole LP powder, MetOH extract, and MetOH residue for 16 d. DSS administration for 9 d induced bodyweight loss, reduced colon length, reduced the colonic expression of tight junction proteins including zonula occludens-1 and -2, and claudin-3 and -7, and upregulated colonic mRNA expression of interleukin 6, chemokine (C-X-C motif) ligand 2, and C-C motif chemokine ligand 2. Feeding LP powder restored these abnormalities, and the MetOH residue, but not MetOH extract, also showed similar restorations. Feeding LP powder and MetOH residue increased fecal concentrations of acetate and n-butyrate. Taken together, LP powder reduced intestinal damage through the protection of tight junction barriers and suppressed an inflammatory reaction in colitic mice. These results suggest that acetate and n-butyrate produced from the microbial metabolism of dietary fibers in LP powder contributed to reducing colitis.

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“…Diosmin is a well-known natural flavonoid used for the treatment of chronic venous insufficiency and varicose veins. Numerous recent studies showed that diosmin exerts various pharmacological activities including anti-inflammatory, antioxidative, antidiabetic, anticancer, antimicrobial, liver-protective, neuroprotective, cardiovascular-protective, kidney-protective, and retina-protective effects ( 132 , 133 ).…”

Section: Epigenetic Effects Of Flavonoids During Cancermentioning

confidence: 99%

Remodeling the Epigenetic Landscape of Cancer—Application Potential of Flavonoids in the Prevention and Treatment of Cancer

et al. 2021

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Epigenetics, including DNA methylation, histone modification, and noncoding RNA regulation, are physiological regulatory changes that affect gene expression without modifying the DNA sequence. Although epigenetic disorders are considered a sign of cell carcinogenesis and malignant events that affect tumor progression and drug resistance, in view of the reversible nature of epigenetic modifications, clinicians believe that associated mechanisms can be a key target for cancer prevention and treatment. In contrast, epidemiological and preclinical studies indicated that the epigenome is constantly reprogrammed by intake of natural organic compounds and the environment, suggesting the possibility of utilizing natural compounds to influence epigenetics in cancer therapy. Flavonoids, although not synthesized in the human body, can be consumed daily and are common in medicinal plants, vegetables, fruits, and tea. Recently, numerous reports provided evidence for the regulation of cancer epigenetics by flavonoids. Considering their origin in natural and food sources, few side effects, and remarkable biological activity, the epigenetic antitumor effects of flavonoids warrant further investigation. In this article, we summarized and analyzed the multi-dimensional epigenetic effects of all 6 subtypes of flavonoids (including flavonols, flavones, isoflavones, flavanones, flavanols, and anthocyanidin) in different cancer types. Additionally, our report also provides new insights and a promising direction for future research and development of flavonoids in tumor prevention and treatment via epigenetic modification, in order to realize their potential as cancer therapeutic agents.

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Metabolism and pharmacological activities of the natural health-benefiting compound diosmin

Abstract: Diosmin is a famous natural flavonoid for treating chronic venous insufficiency and varicose veins. Recently, the extensive study indicates that diosmin possesses diverse pharmacological activities, including anti-inflammation, anti-oxidation, anti-diabetes, anti-cancer,...

Cited by 73 publications

References 167 publications

Activating AhR alleviates cognitive deficits of Alzheimer's disease model mice by upregulating endogenous Aβ catabolic enzyme Neprilysin

Activating AhR alleviates cognitive deficits of Alzheimer's disease model mice by upregulating endogenous Aβ catabolic enzyme Neprilysin

Citrus limon Peel Powder Reduces Intestinal Barrier Defects and Inflammation in a Colitic Murine Experimental Model

Remodeling the Epigenetic Landscape of Cancer—Application Potential of Flavonoids in the Prevention and Treatment of Cancer

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