• Food Science and Biotechnology
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• v.18 no.5
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• pp.1237-1242
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• 2009

Polymethoxylated flavones (PMFs) extracted from Citrus sinensis 'Jincheng' peel were characterized by chromatographic and spectroscopic techniques. Seven individual PMF were identified. 3, 3', 4', 5, 6, 7-hexamethoxyflavone (HEX), nobiletin (NOB), heptamethoxyflavone (HEP), 5-demethylnobiletin (DN), and tangeretin (TAN) were characterized through electrospray ionization mass spectrometry (ESI-MS) in positive mode of protonated molecular ions $[M+H]^+$, the diagnostic fragment ions, together with the UV-Vis spectra and high performance liquid chromatography (HPLC) elution order from literature data. Sinensetin (SIN) and tetramethyl-O-scutellarein (SCU) were isolated and identified through their MS, $^1H$ nuclear magnetic resonance (NMR) and UV-Vis spectral studies. The levels of PMFs in peels from different cultivars of citrus fruits grown in China were determined for the first time. The results showed that C. aurantium 'Bitter orange' peel was the most promising variety for HEP. C. sinensis peel was a good source for SIN and SCU.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.2
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• pp.427-436
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• 2012

Targeted therapy has been a very promising strategy of drug development research. Many molecular mechanims of diseases have been known to be regulated by abundance of proteins, such as receptors and hormones. Chemoprevention for treatment and prevention of diseases are continuously developed. Pre-clinical and clinical studies in chemoprevention field yielded many valuable data in preventing the onset of disease and suppressing the progress of their growth, making chemoprevention a challenging and a very rational strategy in future researches. Natural products being rich of flavonoids are those fruits belong to the genus citrus. Ethanolic extract of Citrus reticulata and Citrus aurantiifolia peels showed anticarcinogenic, antiproliferative, co-chemotherapeutic and estrogenic effects. Several examples of citrus flavonoids that are potential as chemotherapeutic agents are tangeretin, nobiletin, hesperetin, hesperidin, naringenin, and naringin. Those flavonoids have been shown to possess inhibition activity on certain cancer cells' growth through various mechanisms. Moreover, citrus flavonoids also perform promising effect in combination with several chemotherapeutic agents against the growth of cancer cells. Some mechanisms involved in those activities are through cell cycle modulation, antiangiogenic effect, and apoptosis induction.Previous studies showed that tangeretin suppressed the growth of T47D breast cancer cells by inhibiting ERK phosphorylation. While in combination with tamoxifen, doxorubicin, and 5-FU, respectively, it was proven to be synergist on several cancer cells. Hesperidin and naringenin increased cytotoxicitity of doxorubicin on MCF-7 cells and HeLa cells. Besides, citrus flavonoids also performed estrogenic effect in vivo. One example is hesperidin having the ability to decrease the concentration of serum and hepatic lipid and reduce osteoporosis of ovariectomized rats. Those studies showed the great potential of citrus fruits as natural product to be developed as not only the source of co-chemotherapeutic agents, but also phyto-estrogens. Therefore, further study needs to be conducted to explore the potential of citrus fruits in overcoming cancer.

• Korean Journal of Pharmacognosy
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• v.47 no.4
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• pp.381-388
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• 2016

Hyangso-san is a traditional herbal medicine that consists of the seven herbal medicines, Cyperi Rhizoma, Perillae Folium, Atractylodis Rhizoma, Citri Unshius Pericarpium, Glycyrrhizae Radix et Rhizoma, Zingiberis Rhizoma Crudus, and Allii Fistulosi Bulbus. Hyangso-san has long been clinically used to treat the influenza, including headache, ferver, chills, and pantalgia. In this study, we were performed the simultaneous analysis of the 15 marker compounds (liquiritin apioside, liquiritin, ferulic acid, naringin, hesperidin, rosmarinic acid, liquiritigenin, kaempferol, glycyrrhizin, nobiletin, 6-gingerol, elemicin, atractylenolide III, nootkatone, and atractylenolide I) in Hyangso-san using liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS/MS). Column for the separation of the 15 ingredients was used a Waters Acquity UPLC BEH $C_{18}$ analytical column ($2.1{\times}100mm$, $1.7{\mu}m$) at $45^{\circ}C$ by using a mobile phase of 0.1% (v/v) formic acid in water and acetonitrile with gradient condition. Identifications of all analytes were performed using a Waters ACQUITY TQD LC-MS/MS system. The flow rate and injection volume were 0.3 mL/min and $2.0{\mu}L$, respectively. Correlation coefficient of the calibration curve was ${\geq}0.9958$. The values of limits of detection and quantification of the 15 components were 0.002-4.29 and 0.01-12.88 ng/mL, respectively. The result of an analysis using the established LC-MS/MS method, kaempferol and atractylenolide I were not detected, while other 13 compounds were 0.08-56.87 mg/g in lyophilized Hyangso-san sample.

• Advances in Traditional Medicine
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• v.8 no.3
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• pp.222-227
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• 2008

Citrus aurantium var. amara L., commonly known as 'bitter orange' or 'sour orange', of the family Rutaceae, has traditionally been used in the treatment of various ailments, and it possesses different types of pharmacological properties. As a part of our on-going studies on the plantsfrom the Iranian flora, the extract of C. aurantium var. amara has been studied for its weight lossproperties using the mice model. While the Sep-Pak fraction, 20% methanol (MeOH) in water, of the hydro-methanolic extract of the peels of C. aurantium var. amara fruits, when injectedintraperitoneal (i.p.) at a dose of 10 mg/kg, significantly decreased the level of weight gain of the mice in comparison with control the group (P < 0.01), the Sep-Pak fraction 80% MeOH in water decreased the initial weight of mice by 0.44% in six weeks. The administration of the total extract(10 and 20 mg/kg, i.p.), and the Sep-Pak fractions, 40% and 60% MeOH in water (10 mg/kg, i.p.)did not show any significant change of weight of the test mice. Of the two active fractions, the80% MeOH in water fraction did not show any noticeable adverse effects on mice, and was therefore analysed by reversed-phase preparative high performance liquid chromatography resulting in the isolation and identification of four major components, two coumarins, meranzin hydrate (1) and bergamottin (2), and two flavonoids, xanthomicrol 5,4'-di-methyl ether (tangeritin, 3) and hymenoxin 5,7-di-methyl ether (nobiletin, 4).

• Journal of Korean Clinical Health Science
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• v.2 no.1
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• pp.73-78
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• 2014

Purpose. Citrus aurantium L.(familyRutaceae), alsoknownasbitter orange, have been used as traditional herbal medicine in many Asian countries since ancient times. Hence, the purpose of the study was to briefly discuss the new findings about anti-inflammatory and anti-cancer activities of Citrus aurantium L in-vitro. Methods. The articles for this study were collected from pubmed and scopus electronic resources. Results. Citrus aurantium L contains an abundant Flavonoids, including hesperidin, naringin and nobiletin. These Flavonoids has reported to have various medicinal benefits that include antioxidant, antimicrobial, anti-inflammatory, anticancer, anti-diabetic activities, and also used to treat cardiovascular diseases. Conclusion. Based on the above evidence, we propose that Flavonoids from Korea Citrus aurantium L would be a therapeutic potential for cancer treatment and pharmacological benefit for inhibiting the inflammatory effect.

• Food Science and Preservation
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• v.14 no.4
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• pp.351-355
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• 2007

Solvent-extracted volatile components from dry powder prepared from Citrus unshiu products such as immature Citrus unshiu (PCU), mature Citrus unshiu (MCU), Citrus unshiu peel (CUP), and citrus juice processing wastes (CJPW), were examined. Also, solvent-extracted volatile components from mushroom mycelia of Pycnoporus coccineus (PC), Lentinus edodes (LE), Pleurotus eryngii (PE), Hericium coralloides (HC), Panellus serotinus (PS), and Ganoderma lucidum(GL), all cultivated using citrus pulp solid media, were assayed. Twenty-nine volatile components were identified in dry powder prepared Citrus unshiu and 18 volatile components were characterized from mushroom mycelia. Of these, ${\beta}-elemene$, germacrene-D, and ${\delta}-cadinene$, were derived from CJPW, but caryophyllene, hexadecanoic acid, decanoic acid, and tetradecanoic acid were synthesized by mushroom mycelia.

• Journal of Life Science
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• v.23 no.12
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• pp.1553-1556
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• 2013

Flavonoids are one of the major components found in the peels of citrus fruits. Present evidence has suggested that polymethoxyflavonoids, including nobiletin and tangeretin isolated from Citrus sunki, have many biological properties, such as anti-inflammatory, anti-oxidant, and anti-obesity capabilities. Here, we investigated the effect of Citrus sunki peel extract and its possible mechanisms on oxidative stress-induced MMP-1 expression, a major marker of skin photoaging. $H_2O_2$ induced MMP-1 expression in a dose- and time-dependent manner. Extract of Citrus sunki peel (1-25 ${\mu}g/ml$) dose-dependently decreased MMP-1 mRNA levels. When $H_2O_2$ was combined with Citrus sunki peel extract, the phosphorylation of ERK was further decreased compared to a single treatment with $H_2O_2$ alone. Moreover, U0216, an MEK inhibitor, markedly prevented the production of MMP-1. These data suggest that Citrus sunki peel extract has demonstrated protective activity against oxidative damage on MMP-1 expression, and ERK MAP kinase may be involved.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.36 no.1
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• pp.50-63
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• 2023

Objectives : This study used a network pharmacology approach to explore the active compounds and therapeutic mechanisms of Yijin-tang on Meniere's disease. Methods : The active compounds of Yijin-tang were screened via the TCMSP database and their target proteins were screened via the STITCH database. The GeneCard was used to establish the Meniere's disease-related genes. The intersection targets were obtained through Venny 2.1.0. The related protein interaction network was constructed with the STRING database, and topology analysis was performed through CytoNCA. GO biological function analysis and KEGG enrichment analysis for core targets were performed through the ClueGO. Results : Network analysis identified 126 compounds in five herbal medicines of Yijin-tang. Among them, 15 compounds(naringenin, beta-sitosterol, stigmasterol, baicalein, baicalin, calycosin, dihydrocapsaicin, formononetin, glabridin, isorhamnetin, kaempferol, mairin, quercetin, sitosterol, nobiletin) were the key chemicals. The target proteins were 119, and 7 proteins(TNF, CASP9, PARP1, CCL2, CFTR, NOS2, NOS1) were linked to Meniere's disease-related genes. Core genes in this network were TNF, CASP9, and NOS2. GO/KEGG pathway analysis results indicate that these targets are primarily involved in regulating biological processes, such as excitotoxicity, oxidative stress, and apoptosis. Conclusion : Pharmacological network analysis can help to explain the applicability of Yijin-tang on Meniere's disease.

• Journal of Veterinary Science
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• v.23 no.1
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• pp.4.1-4.15
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• 2022

Background: Flavonoids are natural polyphenols found widely in citrus fruit and peel that possess anti-adipogenic effects. On the other hand, the detailed mechanisms for the antiadipogenic effects of flavonoids are unclear. Objectives: The present study observed the anti-adipogenic effects of five major citrus flavonoids, including hesperidin (HES), narirutin (NAR), nobiletin (NOB), sinensetin (SIN), and tangeretin (TAN), on AMP-activated protein kinase (AMPK) activation in palmitate (PA)-treated HepG2 cells. Methods: The intracellular lipid accumulation and triglyceride (TG) contents were quantified by Oil-red O staining and TG assay, respectively. The glucose uptake was assessed using 2-[N-(7-Nitrobenz-2-oxa-1,3-diazol-4-yl)amino]-2-deoxy-d-glucose (2-NBDG) assay. The levels of AMPK, acetyl-CoA carboxylase (ACC), and glycogen synthase kinase 3 beta (GSK3β) phosphorylation, and levels of sterol regulatory element-binding protein 2 (SREBP-2) and 3-hydroxy-3-methylglutaryl-CoA reductase (HMGCR) expression were analyzed by Western blot analysis. The potential interaction between the flavonoids and the γ-subunit of AMPK was investigated by molecular docking analysis. Results: The flavonoid treatment reduced both intracellular lipid accumulation and TG content in PA-treated HepG2 cells significantly. In addition, the flavonoids showed increased 2-NBDG uptake in an insulin-independent manner in PA-treated HepG2 cells. The flavonoids increased the AMPK, ACC, and GSK3β phosphorylation levels and decreased the SREBP-2 and HMGCR expression levels in PA-treated HepG2 cells. Molecular docking analysis showed that the flavonoids bind to the CBS domains in the regulatory γ-subunit of AMPK with high binding affinities and could serve as potential AMPK activators. Conclusion: The overall results suggest that the anti-adipogenic effect of flavonoids on PA-treated HepG2 cells results from the activation of AMPK by flavonoids.

• Korean Journal of Food Science and Technology
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• v.52 no.2
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• pp.130-137
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• 2020

The present study was undertaken to compare the effects exerted by different extraction solvents on the extraction of active components, such as polyphenols and flavonoids, from the dried leaves of Artemisia annua L. Different extracts were prepared using a heating mantle. The extraction solvents used were distilled water, and 20, 40, 60, 80, and 99.5% ethanol solution. It was observed that the 40% ethanol solution yielded the most significant results in the extraction of various phytochemicals with phenol concentration of 154.8±0.28 mg of gallic acid equivalent/g and flavonoid content of 25.28±0.01 mg quercetin equivalent/g. However, based on the extraction solvent used, varying trends were observed in the antioxidant, enzyme inhibition, and bacterial inhibition analyses. It was concluded that the extraction solvent should be selected based on the purpose of use of the dried leaves of A. annua L.