Flavone Glycosides Research Articles

Total flavone of Abelmoschus manihot ameliorates Crohn's disease by regulating the NF‑κB and MAPK signaling pathways.

Crohn's disease (CD) is a chronic relapsing form of inflammatory bowel disease, and its pathogenesis remains unknown. Total flavone of Abelmoschus manihot L. Medic (TFA), has been used as anti‑inflammatory and myocardial ischemia protective drug. The present study aimed to explore the effects of TFA on CD and its underlying mechanism. We reported that TFA comprises eight flavone glycosides, including quercetin‑3‑O‑robinobioside, gossypetin‑3‑O‑glucoside, quercetin‑3'‑O‑glucoside, isoquercetin, hyperoside, myricetin, gossypetin and quercetin. In vivo, TFA promoted the survival of 2,4,6‑trinitrobenzene sulfonic acid (TNBS)‑induced colitis in mice, decreased weight loss and increased colon length in a dose‑dependent manner. Additionally, TFA notably ameliorated the inflammatory response in mice with TNBS‑induced colitis as determined by histopathological analysis. In addition, the administration of TFA in mice with TNBS‑induced colitis led to a significant decrease in the levels of cytokines in the sera and colon tissues; a significant decrease myeloperoxidase activity in the colon tissues was also observed. These findings may be associated with the suppression of the nuclear factor‑κB (NF‑κB) and mitogen‑activated protein kinase (MAPK) signaling pathways. In vitro, TFA significantly downregulated the expression of cytokines in lipopolysaccharide (LPS)‑induced RAW264.7 cells. In addition, TFA suppressed LPS‑induced activation of the NF‑κB and MAPK signaling pathways in RAW264.7 cells. Our findings indicated that TFA could suppress the inflammatory response in mice with TNBS‑induced colitis via inhibition of the NF‑κB and MAPK signaling pathways. The results of the present study may improve understanding of the function of TFA and provide a novel theoretical basis for the treatment of CD.

Effect of Post-Harvest LED and UV Light Irradiation on the Accumulation of Flavonoids and Limonoids in the Segments of Newhall Navel Oranges (Citrus sinensis Osbeck).

To investigate the effect of post-harvest light irradiation on the accumulation of flavonoids and limonoids, harvested Newhall navel oranges were continuously exposed to light-emitting diode (LED) and ultraviolet (UV) light irradiation for 6 days, and the composition and content of flavonoids and limonoids in the segments were determined using UPLC-qTOF-MS at 0, 6, and 15 days after harvest. In total, six polymethoxylated flavonoids (PMFs), five flavone-O/C-glycosides, seven flavanone-O-glycosides, and three limonoids were identified in the segments. The accumulation of these components was altered by light irradiation. Red and blue light resulted in higher levels of PMFs during exposure periods. The accumulation of PMFs was also significantly induced after white light, UVB and UVC irradiation were removed. Red and UVC irradiation induced the accumulation of flavone and flavanone glycosides throughout the entire experimental period. Single light induced limonoid accumulation during exposure periods, but limonoid levels decreased significantly when irradiation was removed. Principal component analysis showed a clear correlation between PMFs and white light, between flavonoid glycosides and red light and UVC, and between limonoids and UVC. These results suggest that the accumulation of flavonoids and limonoids in citrus is regulated by light irradiation. White light, red light and UVC irradiation might be a good potential method for improving the nutrition and flavor quality of post-harvest citrus.

Chemical Constituents From Phalaenopsis Hybrids and Their Bioactivities

One new flavone glycoside and 11 known compounds were characterized from the methanolic extracts of Dtps. Tinny Ribbon × Dtps. Plum Rose ( Phalaenopsis hybrids) by nuclear magnetic resonance and mass spectrometric analyses. In addition, the major pigment constituents 1 to 3 were examined for their antioxidant and antityrosinase activities. The experimental results indicated that the Phalaenopsis flower extracts were potential for developing new cosmetic products.

Justicialosides A and B, two new flavone glycosides from the leaves of Ruspolia hypocrateriformis (Vahl) Milne-Redh. (Acanthaceae)

Two new flavone glycosides, luteolin 7-O-α-l-rhamnopyranosyl-(1→2)-β-d-xylopyranoside (1) and chrysoeriol 7-O-α-l-rhamnopyranosyl-(1→2)-β-d-xylopyranoside (2), along with five known compounds, luteolin 7-O-β-d-apiofuranosyl-(1→2)-β-d-xylopyranoside (3), grandulosides A and B (4 and 5), luteolin 7-O-[β-d-glucopyranosyl-(1→2)-α-l-rhamnosyl-(1→6)]-β-D-glucopyranoside (6) and 10H-quindoline (7) were isolated from the leaves of Ruspolia hypocrateriformis (Acanthaceae). Their structures were elucidated by spectroscopic means, including 1D and 2D NMR, HRESIMS and by comparison with published data.

Breeding of blue chrysanthemums by genetic engineering

Breeding of blue flowers in commercially important ornamental plants, such as chrysanthemum and rose, is relatively difficult by conventional breeding techniques because there are no closely-related species with blue flowers. Therefore, the creation of novel blue flowers has been attempted in various ornamental plants by using biotechnology. As a result, bluish colored carnations and roses have been produced and successfully commercialized. Our research group has also succeeded in developing technology based on genetic engineering to confer the pure blue flower color trait to chrysanthemum (Chrysanthemum morifolium). The blue coloration of the chrysanthemum was accomplished by constructing functional genes producing flavonoid 3’,5’-hydroxylase and anthocyanin 3’,5’-O-glucosyltransferase. Accumulation of 3’,5’-O-glucosylated delphinidin-based anthocyanins synthesized by the transgenes led to the development of blue color via intermolecular copigmentation with flavone glycosides present in chrysanthemum petal. Subsequently, by introducing the two genes necessary for blue petal coloration, we succeeded in conferring the blue flower color trait to various chrysanthemums with different floral shapes and color shades. Successful commercialization of blue chrysanthemums should facilitate an expansion of flower color variation, increase potential flower value, and raise new possibilities and applications for chrysanthemums. Furthermore, in vitro experiments suggested that, in addition to flavone glycosides, flavonol glycosides might have an effect on 3’,5’-O-glucosylated delphinidin-based anthocyanins as blue-coloring copigments in planta. These results indicate that the method established in chrysanthemums for the blue color development of petals by hydroxylation and glucosylation of the B-ring of anthocyanins is likely to be applicable to other ornamental plants.

Thrombin Inhibition: Preliminary Assessment of the Anticoagulant Potential of Turnera subulata (Passifloraceae).

Cardiovascular and thromboembolic disturbances are the main causes of disease-related deaths worldwide. Regardless of the etiological factors involved in thrombus formation, coagulation is mainly activated by thrombin, one of the most important blood clotting molecules. Thus, this study evaluated the Turnera subulata leaf crude extract, its ethyl acetate fraction effect on the coagulation cascade, and its possible side effects. Their phytocomposition indicated polyphenols, mainly flavonol-3-O-glycosylate and a flavone glycoside, without in vitro and in vivo toxicity. Regarding their potential anticoagulants, results displayed partial thromboplastin and prothrombin time activation, and Xa and IIa, and thrombin inhibition by heparin II cofactor, indicating significant anticoagulant activity, suggesting direct and indirect thrombin inhibition as the main mechanism of action. Therefore, T. subulata leaf active compounds exhibit therapeutic potential required to develop phytotherapeutic formulations to assist conventional anticoagulants in clinical treatments.

Profiling Metabolites and Biological Activities of Sugarcane (Saccharum officinarum Linn.) Juice and its Product Molasses via a Multiplex Metabolomics Approach.

Sugarcane (Saccharum officinarum L.) is an important perennial grass in the Poaceae family cultivated worldwide due to its economical and medicinal value. In this study, a combined approach using mass spectrometry (MS) and nuclear magnetic resonance (NMR) spectroscopy was employed for the large-scale metabolite profiling of sugarcane juice and its by-product molasses. The polyphenols were analysed via UPLC-UV-ESI-MS, whereas the primary metabolites such as sugars and organic and amino acids were profiled using NMR spectroscopy and gas chromatography/mass spectrometry (GC/MS). UPLC/MS was more effective than NMR spectroscopy or GC/MS for determining differences among the metabolite compositions of the products. Under the optimized conditions, UPLC/MS led to the identification of 42 metabolites, including nine flavonoids, nine fatty acids, and two sterols. C/O Flavone glycosides were the main subclass detected, with tricin-7-O-deoxyhexosyl glucuronide being detected in sugarcane and molasses for the first time. Based on GC/MS analysis, disaccharides were the predominant species in the sugarcane juice and molasses, with sucrose accounting for 66% and 59%, respectively, by mass of all identified metabolites. The phenolic profiles of sugarcane and molasses were further investigated in relation to their in vitro antioxidant activities using free radical scavenging assays such as 2,2-Diphenyl-1-picrylhydrazyl free radical-scavenging ability (DPPH), Trolox equivalent antioxidant capacity (TEAC) and ferric reducing antioxidant power (FRAP). In view of its higher total phenolic content (TPC) (196 ± 2.1 mg GAE/100 g extract) compared to that of sugarcane juice (93 ± 2.9 mg GAE/100 g extract), molasses exhibited a substantially higher antioxidant effect. Interestingly, both extracts were also found to inhibit α-glucosidase and α-amylase enzymes, suggesting a possible antihyperglycaemic effect. These findings suggest molasses may be a new source of natural antioxidants for functional foods.

Metabolomics driven analysis of 11 Portulaca leaf taxa as analysed via UPLC-ESI-MS/MS and chemometrics

Portulaca oleracea, commonly known as purslane, is a popular plant of considerable value for its nutritive composition as well as traditional medicinal uses. P. oleracea is reported to possess neuroprotective, antimicrobial, antidiabetic, antioxidant, anti-inflammatory, antiulcerogenic, and anticancer activities. Three taxa of P. oleracea L. (P. oleracea, P. rausii and P. granulatostellulata) are grown as mixed populations in several locations in Egypt. The close morphological similarities among these taxa warrants development of methods for their correct identification or classification. We aimed in this study to assess metabolome differences among three P. oleracea taxa via ultra-performance liquid chromatography-mass spectrometry (UPLC–MS) in the context of their genetic diversity and/or geographical origin. A total of 85 metabolites were identified including 6 amino acids, 22 phenolic compounds, 16 alkaloids, and 11 fatty acids characterized based on their MSn and UV spectra. Methoxylated flavone glycosides, O-flavonoids, C-flavonoids and four previously undescribed cyclodopa alkaloids are reported in P. oleracea for the first time. Multivariate data analyses were used for samples classification and revealing that cyclodopa alkaloids (oleracein A, C, K and N) contributed the most for accessions classification. To the best of our knowledge, this study presents the first metabolite profile of Portulaca and its compositional differences that provide chemical based evidence for its nutritive and/or health benefits.

Valeriana jatamansi: An herbaceous plant with multiple medicinal uses.

Valeriana jatamansi Jones (Family: Caprifoliaceae), a high value medicinal plant, was distributed in many countries of Asia. The species possesses important valepotriates and is a good source of flavones or flavone glycosides, lignans, sesquiterpenoids or sesquiterpenoid glycoside, bakkenolide type sesquiterpenoids, phenolic compounds, terpinoids, etc. The use of the species in traditional and modern medicines is well known. For instance, V.jatamansi is very important for its insect repelling and antihelmethic properties. Similarly, sedative, neurotoxic, cytotoxic, antidepressant, antioxidant, and antimicrobial activities of the species in various ailments in the indigenous system of medicine, particularly in Asia, are reported. This review focuses on the detailed phytochemical composition, medicinal uses, and pharmacological properties of V.jatamansi along with analysis of botanical errors in published literature and reproducibility of the biomedical researches on this multipurpose herbaceous species.

New cytotoxic flavonoids from aerial parts of Platycladus orientalis L.

Investigation of Platycladus orientalis yielded five flavonoids, including aglycone flavone 1 (apigenin), flavone glycoside 2 (apigenin 7-O-β-D-glucopyranoside), new gernaylated flavone glycoside 3 (apigenin 8-gernayl-4′-O-α-gluco pyranoside) and two new pernylated flavonoid glycosides 4 & 5 (apigenin 8-pernyl-4′-glucopyranosyl-7-O-α-glucopyranoside and apigenin 5-pernyl-7-glucopyranosyl-4′-O-β-D-glucopyranoside). Their structures were elucidated on the basis of spectroscopic evidence. The cytotoxicity of compounds 1–5 were tested against Lung adenocarcinoma (A549), human hepatocellular liver carcinoma (HepG2), human breast carcinoma (MCF-7) cell lines and mouse fibroblast cell line NIH/3T3 as normal cells. This assay gave spot on structure activity relationship which, showed that cytotoxicity of compounds (1) and (2) against three cell lines was weak as IC50 > 15. Compounds (4) and (5) had moderate cytotoxic and no toxic effect on normal cell. Compound (3) showed high cytotoxic activity against tested three cell lines with no toxic effect of normal cells.

Verification of Authenticity of Ginkgo biloba L. Leaf Extract and Its Products Present on the Croatian Market by Analysis of Quantity and Ratio of Ginkgo Flavone Glycosides (Quercetin, Kaempferol and Isorhamnetin) to Terpene Trilactones to the Effect of Unmasking Counterfeit Drugs Endangering Patient Health

SUMMARYGinkgo biloba L. is the eldest plant growing on the Earth; preparations made of its leaves and seeds represent an integral part of the Chinese medicine for over a millennium. The plant species was first discovered by Linnaeus in 1771, its name thereby originating from the Latin words bis (two) and lobus (lobe), which duly illustrate the specific shape of its leaf. Contemporary Ginkgo biloba L. plant based pharmaceuticals mostly comprise extracts recovered from leaves harvested during fall, when the concentration of active components reaches its peak. Recent investigations have managed to establish the chemical composition of the plant leaf, together with the mechanisms underlying its beneficial effects on rheological profile of the blood and acceleration of its flow. High price of these preparations and their vast popularity have soon become an incentive for counterfeiting Ginkgo biloba L. extracts and the release of bogus drugs comprising cheaper extracts coming from other plants. Namely, modern Ginkgo biloba L.-based medicinal products and food supplements comprise extracts recovered from the plant leaf that get to be standardized according to its key pharmacological active components, most often flavone glycosides (represented in the share of 22%-27%) and terpene trilactones (represented in the share of 6%-7%). The flavonoids that predominate such preparations and are most relevant from the pharmacological standpoint are quercetin, kaempferol and isorhamnetin, their total amount and mutual ratios, thereby being an unquestionable indicator of the extract authenticity. Therefore, most of the analyses aiming at verifying the authenticity of a given Ginkgo biloba L.-based product boil down to the analysis of these parameters. Counterfeiting involves partial or full replacement of the Ginkgo biloba L. extract (GBE) with a cheaper plant extract of a similar composition, the latter occasionally being enriched with an additional amount of flavonoids, most often quercetin, not originating from the Ginkgo biloba L. plant. The aim of this study was to verify the authenticity and quality of Ginkgo biloba L.-based products circulating on the Croatian market. To that effect, 10 samples of products produced by various manufacturers were analyzed in a certified laboratory. The parameters based on which the authenticity of the preparations was assessed were the shares of aglycones of typical ginkgo flavone glycosides, that is to say, quercetin, kaempferol and isorhamnetin, and mutual ratios of the established quantities of quercetin to kaempferol as the key clues to unmasking Ginkgo extracts counterfeiting. The amount of ginkgo flavone glycosides was established using high performance liquid chromatography. The analysis proved 80% of the samples analyzed to be conformant to the label statements as regards the total amount of flavone glycosides and their mutual ratios. In 20% of the samples, the ratio of quercetin to kaempferol deviated from normal values; on top of that, the presence of the phytoestrogen genistein, one of the components typically comprised by the Sophora japonica L. plant, was also proven, documenting counterfeiting of the GBE and its replacement by the Sophora japonica L. extracts in the samples under consideration. Due to the untrue label statements descriptive of these products, the information on the presence of pharmacologically active genistein was neglected to be mentioned despite its unfavorable health impact that can be expected in some consumer groups. The results of this study indicated the frequency of counterfeiting the Ginkgo biloba L.-based products found on the Croatian market to be deemed substantial. Therefore, a more rigorous and more thorough control of these products and sanctioning of irresponsible manufacturers and distributers is proposed, so as to contribute to a higher market representation of high-quality products, as well as to avoid health risks and downsize the rate of their counterfeiting.

A Rare Threono-1,4-Lactone Containing Flavone Glycoside from Cassia nomame

One new flavone glycoside, nomaminoside (3), containing a threono-1,4-lactone moiety, together with three known compounds, isoorientin 2′′-O-rhamnoside (1), coatline B (2), and myrcetin (4), were isolated from the n-butanol fraction of Cassia nomame methanolic extract. The chemical structure of the new compound was elucidated by spectroscopic analysis including HR-ESI-MS, 1D and 2D NMR techniques.

Role of scutellarin in human cancer—A review

Clerodendrum serratum: A clinical approachMukesh Kr. Singh, Gaurav Khare, Shiv Kr. Iyer, Gotmi Sharwan, D. K. Tripathi

Diosmin induces caspase-dependent apoptosis in human glioblastoma cells.

Diosmin is a flavone glycoside clinically used as the main component of Daflon for the treatment of venous diseases. Several studies demonstrated that this natural compound can induce apoptosis in different tumors. However, isolated diosmin has not been studied regarding its effects on glioblastoma so far. Since glioblastoma is a highly lethal and fast-growing brain tumor, new therapeutic strategies are urgently needed. Herein, we evaluated the role of this flavonoid against glioblastoma cells using in vitro assays. Diosmin significantly reduced the viability of GBM95, GBM02, and U87MG glioblastoma cells, but not of healthy human astrocytes, as verified by MTT assay. Vimentin immunostaining showed that diosmin induced morphological changes in GBM95 and GBM02 cells, making them smaller and more polygonal. Diosmin did not inhibit GBM95 and GBM02 cell proliferation, but it caused DNA fragmentation, as verified by the TUNEL assay, and increased cleaved caspase-3 expression in these cells. In summary, diosmin is able to induce caspase-dependent apoptosis specifically in tumor cells and, therefore, could be considered a promising therapeutic compound against glioblastoma.

Protective Effects of Baicalin on Diabetes Mellitus-Induced Renal Fibrosis in Mice

Baicalin is a flavone glycoside that possess numerous pharmacological properties including anti-inflammatory, anti-cancer and anti-pruritic effects. Based on these properties, we investigated whether baicalin could be used to alleviate kidney fibrosis induced by diabetes mellitus. Using a streptozotocin (STZ)-induced diabetic mouse model, we found that baicalin treatment could suppress diabetes-enhanced water consumption, urine volume production, blood urea nitrogen (BUN), serum creatinine and urinary albumin/urinary creatinine (UACR). Correspondingly, baicalin treatment could significantly maintain the morphology of the glomerulus and renal tubules in diabetes-induced kidney lesions by repressing WT1 and Nephrin expressions in the glomeruli, as well as LTL, caspases-9 and Fas expressions in the renal tubules. We also determined that baicalin could suppress inflammation responses and reduced MDA activities that were enhnaced by diabetes while increasing SOD, CAT, GPX and Nrf2 expressions that were inversely lowered. We demonstrated the presence of interstitial fibrosis in the diabetic kidney but this could be alleviated by baicalin which downregulated ɑ-SMA and TGF-β1 expressiond (key pro-fibrotic markers). We investigated Klotho a transmembrane protein that is expressed by renal tubule epithelial cells. Secreted form of Klotho could bind to TGF-β1 receptors and block the TGFβ1 signaling pathway. We determined that hypermethylation of the Klotho promoter plays an important role in baicalin's ability to rescue renal fibrosis induced by diabetes mellitus. In sum, our results showed that baicalin could alleviate renal fibrosis-induced by diabetes through partly modulating Klotho promoter methylation. Funding Statement: This study was supported by NSFC grant (31771331, 81741016), Science and Technology Planning Project of Guangdong Province (2017A050506029, 2017A020214015, 2016B030229002), Science and Technology Program of Guangzhou (201710010054), Guangdong Natural Science Foundation (2016A030311044), Project of National University Students Challenge Cup (18112003). Declaration of Interests: The authors declare that there are no competing financial interests. Ethics Approval Statement: This study was carried out in strict accordance with the recommendations of the Guide for the Care and Use of Laboratory Animals of the National Institutes of Health. The protocol was approved by the Animal Ethic Committee at Jinan University.

Nobiletin inhibits breast cancer via p38 mitogen-activated protein kinase, nuclear transcription factor-κB, and nuclear factor erythroid 2-related factor 2 pathways in MCF-7 cells.

IntroductionBreast cancer is one of the most commonly diagnosed cancers in women, with a high mortality rate.ObjectiveIn the present study, we evaluated the anticancer effect of nobiletin, a flavone glycoside, on the breast cancer cell line MCF-7.ResultCell viability and proliferation decreased and cell morphology changed from diamond to round after being treated with nobiletin. Nobiletin induced apoptosis of breast cancer MCF-7 cells via regulating the protein expression of Bax, Bcl-2, cleaved caspase-3, and p53. The expression of Bcl-2 decreased, while the expression of Bax and p53 increased in MCF-7 cells treated with nobiletin. Meanwhile, nobiletin inhibited cell migration by downregulating the protein expression of matrix metalloproteinase-2 (MMP-2) and matrix metalloproteinase-9 (MMP-9). Moreover, phosphorylation of p38 was increased, and the translocation of p65 and nuclear factor erythroid 2-related factor 2 (Nrf2) to the nucleus was decreased, which suggested that the anticancer effects of nobiletin might at least partially rely on mediating the p38 mitogen-activated protein kinase, nuclear transcription factor-κB, and Nrf2 pathways in MCF-7 breast cancer cells.Conclusion and recommendationOur data showed that nobiletin was a potential antitumor drug, and it provided some experimental basis for the clinical application of tumor therapy.

Chrysoeriol derivatives and other constituents from Glandularia selloi

Glandularia selloi (Verbenaceae) presents phenylethanoids, iridoids and flavone glycosides as the main constituents. Two novel chrysoeriol derivatives, selloiside A (1) and selloiside B (2) were isolated from the methanolic extract of the aerial parts. Both flavones are acylated disaccharides. Two known compounds, verbascoside (3) and 6β-hydroxy-ipolamiide (4), were isolated from the methanolic extract of the roots. The structures were elucidated using 1D, 2D NMR and MS. Acylflavones have taxonomic significance since they occur mainly is species from the order Lamiales, specifically from the family Lamiaceae, closely related to Verbenaceae. The compounds 1 – 4 and the methanolic extract were investigated for antichemotactic activity.

Enteral Baicalin, a Flavone Glycoside, Reduces Indicators of Cardiac Surgery-Associated Acute Kidney Injury in Rats

Background/Aims: Cardiac surgery-associated acute kidney injury (CSA-AKI) is one of the most common postoperative complications in intensive care medicine. Baicalin has been shown to have anti-inflammatory and antioxidant roles in various disorders. We aimed to test the protective effects of baicalin on CSA-AKI using a rat model. Methods: Sprague-Dawley rats underwent 75 min of cardiopulmonary bypass (CPB) with 45 min of cardioplegic arrest (CA) to establish the AKI model. Baicalin was administered at different doses intragastrically 1 h before CPB. The control and treated rats were subjected to the evaluation of different kidney injury index and inflammation biomarkers. Results: Baicalin significantly attenuated CPB/CA-induced AKI in rats, as evidenced by the lower levels of serum creatinine, serum NGAL, and Kim1. Baicalin remarkably inhibited oxidative stress, reflected in the decreased malondialdehyde and myeloperoxidase activity, and enhanced superoxide dismutase activity and glutathione in renal tissue. Baicalin suppressed the expression of IL-18 and iNOS, and activated the Nrf2/HO-1 pathway. Conclusion: Our data indicated that baicalin mediated CPB/CA-induced AKI by decreasing the oxidative stress and inflammation in the renal tissues, and that baicalin possesses the potential to be developed as a therapeutic tool in clinical use for CSA-AKI.

Desmiflavanoside, a New Bioactive Flavonoid Glycoside Isolated from Desmidorchis flava

A new flavonoid glycoside, named desmiflavanoside (1), was isolated from the MeOH extract of Desmidorchis flava (N.E.Br.) Meve & Liede, and its structure was elucidated based on 1D and 2D NMR spectroscopic techniques as well as mass spectrometry. Preliminary studies demonstrated that although compound 1 is moderately cytotoxic at lower concentrations, its activity plateaus at higher concentrations. Notably, compound 1 demonstrated a significant dose-dependent response to lipid peroxidation and that its antilipid peroxidation was similar (89.6 ± 0.81%) to the known standard (BHT; 91.3 ± 0.49%; p < 0.051). On the other hand, the flavone glycoside 1 did not show inhibitory effects against urease and acetylcholinesterase enzymes.

Metabolic and excretory process of Citri Reticulatae Pericarpium Viride and Citri Reticulatae Pericarpium in rats' urine and feces analyzed by RRLC-QqQ-MSn

This present study was to investigate the metabolism and excretion of characteristic polyphenols such as flavonoids and coumarins in urine and feces of rats after intragastric administration of ethanol extracts of Citri Reticulatae Pericarpium Viride and Citri Reticulatae Pericarpium. The urine and feces of rats were collected after intragastric administration of 70% ethanol extracts of Citri Reticulatae Pericarpium Viride and Citri Reticulatae Pericarpium. Rapid resolution liquid chromatography coupled with quadrupole tandem mass spectrometry (RRLC-QqQ-MSn) was applied to compare the contents of polyphenols in ethanol extract, urine and feces. By comparing with reference substance, 30 polyphenols were identified from the ethanol extracts of Citri Reticulatae Pericarpium Viride and Citri Reticulatae Pericarpium, including flavone glycosides, flavones, flavonone glycosides, flavonones, flavonol glycosides, polymethoxyflavones, coumarins, and limonoids and so on. The detection of various types of compounds showed differences in contents between the intestinal metabolism and excretion in the feces after systemic circulatory metabolism and renal excretion. The results showed that the polymethoxyflavones and flavonones were primarily excreted through urine, and the flavonone glycosides and limonoids were primarily excreted through feces. However, coumarins were hardly detected in feces and urine, indicating that coumarins may be metabolized in the body.