poncirin and isosakuranetin

Poncirin (PC) and its aglycone, isosakuranetin (IR), occur naturally in citrus fruits. This study aimed to explore the pathways behind the different health benefits of PC and IR by evaluating the effect of these two bioactive flavonoids on the gut microbial diversity and metabolomics of mice. The 16S rRNA gene sequencing was used to analyze the alteration of gut microbiota in mice after PC and IR intervention. The metabolic impact of PC and IR in mice were studied using a metabolomics approach based on LC-MS analysis. Results showed that, after 7 days intervention, PC and IR multiplied the abundance of

Topics: Animals; Citrus; Flavonoids; Gastrointestinal Microbiome; Metabolomics; Mice; RNA, Ribosomal, 16S

Poncirin (PO) and isosakuranetin (or ponciretin [PT]) are compounds found in fruits of the genus Citrus. They are frequently used in traditional Chinese medicine for the treatment of inflammation and asthma. Therefore, we examined their anti-gastritis effects in vitro and in vivo.. The anti-inflammatory effects of PO and PT were examined using ethanol- or LPS-stimulated KATO III cells. Gastritis was induced in ICR mice via intragastric injection of absolute ethanol. Levels of inflammatory markers were measured by enzyme-linked immunosorbent assay, immunoblotting, and quantitative polymerase chain reaction.. Treatment with PT or PO inhibited the secretion of interleukin (IL)-8 and tumor necrosis factor (TNF) in ethanol- or LPS-stimulated KATO III cells. They also reduced the activation of nuclear factor kappa B (NF-κB). Pre-treatment with PT or PO significantly protected against ethanol-induced hemorrhagic gastritis, characterized by edema, tissue erosions, and mucosal friability in mice. Treatment with PT or PO suppressed ethanol-induced NF-κB activation and the release of TNF, IL-8, and IFN-γ. The protective effect of PT was greater than that of PO and comparable to ranitidine, a positive control.. PT may attenuate ethanol-induced gastritis by inhibiting the infiltration of immune cells, including neutrophils, via the regulation of CXCL4 (or IL-8) secretion and the activation NF-κB.

Topics: Animals; Anti-Inflammatory Agents; Cell Line; Cell Movement; Citrus; Ethanol; Flavonoids; Gastric Mucosa; Gastritis; Interleukin-8; Male; Medicine, Chinese Traditional; Mice; Mice, Inbred ICR; Neutrophils; NF-kappa B; Tumor Necrosis Factor-alpha

The total phenolic and flavonoid content of extracts from peel of kumquat were higher than those from pulp, and those extracted from immature kumquat were higher than those from mature kumquat. The highest levels of phenolic and flavonoid content were obtained in hot water extracts. The flavonoids of kumquat extracted from hot water were mainly soluble conjugated compounds, including C-glycosides, such as 3',5'-di-C-β-glucopyranosylphloretin (DGPP), acacetin 8-C-neohesperidoside (margaritene), acacetin 6-C-neohesperidoside (isomargaritene), apigenin 8-C-neohesperidoside, and O-glycosides, such as acacetin 7-O-neohesperidoside (fortunellin), isosakuranetin 7-O-neohesperidoside (poncirin) and apigenin 7-O-neohesperidoside (rhoifolin). A positive relationship existed between total phenolic content and DPPH scavenging potency (p<0.001). Total flavonoid content showed a similar correlation (p<0.001) to DPPH scavenging potency. The effective flavonoids contributing to antioxidant activity were DGPP and apigenin 8-C-neohesperidoside, which could be extracted in high amounts, by hot water at 90°C, from immature kumquat peel.

Topics: Antioxidants; Apigenin; Biphenyl Compounds; Disaccharides; Flavonoids; Fruit; Glycosides; Oxidation-Reduction; Phenols; Picrates; Plant Extracts; Rutaceae; Solvents

Naringenin and its derivatives have been assessed in bone health for their oestrogen-'like' effects but low bioavailability impedes clinical potential. This study was aimed at finding a potent form of naringenin with osteogenic action.. Osteoblast cultures were harvested from mouse calvaria to study differentiation by naringenin, isosakuranetin, poncirin, phloretin and naringenin-6-C-glucoside (NCG). Balb/cByJ ovariectomized (OVx) mice without or with osteopenia were given naringenin, NCG, 17β-oestradiol (E2) or parathyroid hormone (PTH). Efficacy was evaluated by bone microarchitecture using microcomputed tomography and determination of new bone formation by fluorescent labelling of bone. Plasma levels of NCG and naringenin were determined by HPLC.. NCG stimulated osteoblast differentiation more potently than naringenin, while isosakuranetin, poncirin or phloretin had no effect. NCG had better oral bioavailability than naringenin. NCG increased the mRNA levels of oestrogen receptors (ERs) and bone morphogenetic protein (an ER responsive gene) in vivo, more than naringenin. In OVx mice, NCG treatment in a preventive protocol increased bone formation rate (BFR) and improved trabecular microarchitecture more than naringenin or E2. In osteopenic mice, NCG but not naringenin, in a therapeutic protocol, increased BFR and improved trabecular microarchitecture, comparable with effects of PTH treatment. Stimulatory effects of NCG on osteoblasts were abolished by an ER antagonist. NCG transactivated ERβ but not ERα. NCG exhibited no uterine oestrogenicity unlike naringenin.. NCG is a potent derivative of naringenin that has bone anabolic action through the activation of osteoblast ERs and exhibited substantial oral bioavailability.

Topics: Anabolic Agents; Animals; Biological Availability; Body Weight; Bone Diseases, Metabolic; Bone Morphogenetic Proteins; Cell Differentiation; Estrogens; Female; Flavanones; Flavonoids; Glucosides; Male; Mice; Mice, Inbred BALB C; Osteoblasts; Osteogenesis; Ovariectomy; Parathyroid Hormone; Phloretin; Rats; Rats, Wistar; Receptors, Estrogen; Skull