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A pharmacodynamic research on chromone glucosides of Fang-feng

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Abstract

To investigate the pharmacological activity of prim-O-glucosylcimifugin and 4'-O-beta-D-glucosyl-5-O-methylvisamminol con tained in Fangfeng. Analgesic, antipyretic and antiinflammatory effects were assessed using the models of yeast-induced rat fever, acetic acidinduced peritoneal pain thermalpain, and dimethylbenzol-induced mouse ear edema. Prim-O-glucosylcimifugin and 4'-O-beta-D-glucosyl-5-O-methylvisamminol could reduce the body temperature of rats in a model of yeast-induced fever. Both components could decrease the spasm action induced by peritoneal injection of acetic acid, increase the pain-threshold in a thermal-pain model, relieve the mouse ear edema caused by dimethybenzol and significantly inhibit ADP-induced platelet aggregation. Prim-O-glucosylcimifugin and 4'-O-beta-D-glucosyl-5-O-methylvisamminol have significant analgesic, antipyretic, anti-inflammatory and anti-platelet aggregation actions.

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... (1,21,22) At present, a total of 35 coumarins, primarily furanocoumarins and pyranocoumarins, have been identified from S. divaricata (Appendixes 4 and 5). Among them, the 17 furanocoumarins isolated include bergapten (18), byakangelicin (19), deltoin (20), imperatorin (21), isoimperatorin (22), isobergapten (23), marmesin (24), methoxy-8-(3-hydroxymethylbut-2-enyloxy)-psoralen (25), nodakenetin (26), oxypeucedanin hydrate (27), phellopterin (28), psoralen (29), sapodivarin (30), xanthotoxin (31), 5-hydroxy-8-methoxypsoralen (32), nodakenin (33), and xanthoarnol (34). (23) Five simple coumarins isolated from the herb, including fraxidin (35), isofraxidin (36), scopoletin (37), umbelliferone (38) and 5-methoxy-7-(3, 3-dimethylallyloxy)-coumarin (39), have simple structures but show a variety of biological activities such as dispelling phlegm and antitumor activity. ...
... Previous studies have demonstrated that S. divaricate exhibits a broad range of pharmacological activities, including anti-inflammatory, analgesic, a n t i o x i d a n t , a n t i p r o l i f e r a t i v e , a n t i t u m o r , i m m u n o r e g u l a t o r y , a n t i a l l e r g i c , a n t i p y r e t i c , a n t i c o a g u l a n t , b l o o d c i r c u l a t i o n -p r o m o t i n g , anticonvulsive, antileukemia, anti-atherosclerosis, and hepatoprotective effects (Appendix 10). (18,(33)(34)(35)(36)(37)(38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49) ...
... Many reports have demonstrated that the extract of S. divaricata (SDE) and several of its constituents, including sec -O -glucosylhamaudol, cimifugin, prim -O -glucosylcimifugin, 4'-O -β -D-glucosyl-5-O -methylvisamminol, 5-O -methylvisamminol and anomalin, exhibit significant anti-inflammatory and analgesic activities. (33)(34)(35)(36)(37)(38)(39) Chun, et al (42) reported that SDE extracted with 70% ethanol demonstrated an anti-inflammatory and anti-osteoarthritis activities through in vitro and in vivo studies. They examined the levels of 4 proinfl ammatory cytokines in LPS-stimulated RAW 264.7 cells to evaluate the anti-infl ammatory activity of SDE in vitro, and found that it significantly inhibited the production of NO, prostaglandin E 2 (PGE 2 ), tumor necrosis factor (TNF), and interleukin-6 (IL-6) at a concentration of 200 or 400 μg/mL. ...
Article
Saposhnikovia divaricata (Turcz.) Schischk., a perennial herb belonging to the family Umbelliferae, is widely distributed in Northeast Asia. Its dried root (Radix Saposhnikoviae) is used as a Chinese herbal medicine for the treatment of immune system, nervous system, and respiratory diseases. Phytochemical and pharmacological studies have shown that the main constituents of S. divaricata are chromones, coumarins, acid esters, and polyacetylenes, and these compounds exhibited significant anti-inflammatory, analgesic, antioxidant, antiproliferative, antitumor, and immunoregulatory activities. The purpose of this review is to provide comprehensive information on the botanical characterization and distribution, traditional use and ethnopharmacology, phytochemistry, and pharmacology of S. divaricata for further study concerning its mechanism of action and development of better therapeutic agents and health products from S. divaricata.
... Pharmacological studies suggest that Schischk extracts have anti-inflammatory, analgesic, anti-convulsion and anti-tumor effects (Wang et al., 1999;Deng et al., 2005;Jiang et al., 2006) but anti-nociception of primo-glucosylcimifugin (POG) is unclear. POG, a chromone extracted from Schischk root ( Fig. 1) comprises 0.24% (g/g) of the entire root (Xue et al., 2000;Dai et al., 2008) and is the active ingredient standardized in the Chinese Pharmacopoeia (Dai et al., 2008;He et al., 2009). Therefore, we measured the anti-nociception effects of POG in a formalin or arthritisinduced nociception rat model and measured prostaglandin E2 (PGE2) which mediates pro-inflammatory cytokine production and cyclooxygenase 2 (COX-2). ...
... Schischk is said to be widely used in traditional Chinese medicine for thousands of years and may have pharmacological properties (Xue et al., 2000) and its extract is said to have anti-bacterial, antipyretic, anti-inflammatory and analgesic properties (Xue et al., 2000;Deng et al., 2005). We assessed analgesic effects of POG which we hypothesized had specific anti-nociceptive effects on inflammatory pain as tested in rat tonic and chronic pain models. ...
... Schischk is said to be widely used in traditional Chinese medicine for thousands of years and may have pharmacological properties (Xue et al., 2000) and its extract is said to have anti-bacterial, antipyretic, anti-inflammatory and analgesic properties (Xue et al., 2000;Deng et al., 2005). We assessed analgesic effects of POG which we hypothesized had specific anti-nociceptive effects on inflammatory pain as tested in rat tonic and chronic pain models. ...
Article
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We measured anti-nociceptive activity of prim-o-glucosylcimifugin (POG), a molecule from Saposhnikovia divaricate (Turcz) Schischk. Anti-nociceptive or anti-inflammatory effects of POG on a formalin-induced tonic nociceptive response and a complete Freund's adjuvant (CFA) inoculation-induced rat arthritis pain model were studied. Single subcutaneous injections of POG produced potent anti-nociception in both models that was comparable to indomethacin analgesia. Anti-nociceptive activity of POG was dose-dependent, maximally reducing pain 56.6% with an ED50 of 1.6 mg. Rats given POG over time did not develop tolerance. POG also time-dependently reduced serum TNFα, IL-1β and IL-6 in arthritic rats and both POG and indomethacin reduced spinal prostaglandin E2 (PGE2). Like indomethacin which inhibits cyclooxygenase-2 (COX-2) activity, POG dose-dependently decreased spinal COX-2 content in arthritic rats. Additionally, POG, and its metabolite cimifugin, downregulated COX-2 expression in vitro. Thus, POG produced potent anti-nociception by downregulating spinal COX-2 expression.
... AMR is bitter, sweet and warm in nature, and which is beneficial for anti-inflammation, anti-hepatotoxic, anti-ulcer, anti-obesity, anti-cancer and so on [8][9][10][11]. SR is used to expel ''wind'', to relieve exterior syndrome, to eliminate dampness, to relieve convulsion and diarrhea [12][13][14]. Having these herbs, YPFS is being used to replenish ''Qi'' and to consolidate the superficies and arrest perspiration, i.e. clinical symptoms having spontaneous sweating, frequent colds, aversion to wind, fatigue and a pale and shiny complexion. ...
... In order to standardize YPFS chemically, a typical HPLC (13), ononin (4), calycosin (1), astragaloside III (6), astragaloside IV (7), astragaloside II (5), formononetin (3), aesculetin (IS1), Rg1 (IS2) and chrysin (IS3) was made by a MS detector in the negative mode. Representative chromatograms are shown, n = 3; (B): The identification of prim-O-glucosylcimifugin (11), 5-O-methylvisammioside (12), psoralen (14), isopsoralen (15), atractylenolide III (10), atractylenolide II (9), atractylenolide I (8), esculin (IS4), crytotanshinone (IS5) was made by a MS detector in the positive mode. The chemical markers were numbered according to Fig. S1. ...
Article
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Yu Ping Feng San (YPFS), a Chinese herbal decoction, is composed of Astragali Radix (AR; Huangqi), Atractylodis Macrocephalae Rhizoma (AMR; Baizhu) and Saposhnikoviae Radix (SR; Fangfeng) in a weight ratio of 1∶2∶1. Clinically, YPFS has been widely used to regulate immune functions; however, the action mechanism of it is not known. Here, we addressed this issue by providing detail analyses of chemical and biological properties of YPFS. By using rapid resolution liquid chromatography coupled with mass spectrometry, fifteen chemicals deriving from different herbs of YPFS were determined, and which served as a control for the standardization of the herbal extract of YPFS. In general, the amounts of chosen chemical markers were higher in a preparation of YPFS as compared to that of single herb or two-herb compositions. In order to reveal the immune functions of YPFS, the standardized extract was applied onto cultured murine macrophages. The treatment of YPFS stimulated the mRNA and protein expressions of pro-inflammatory cytokines via activation of NF-κB by enhancing IκBα degradation. In contrast, the application of YPFS suppressed the expressions of pro-inflammatory cytokines significantly in the lipopolysaccharide (LPS)-induced chronic inflammation model. In addition, YPFS could up regulate the phagocytic activity in cultured macrophages. These results therefore supported the bi-directional immune-modulatory roles of YPFS in regulating the releases of cytokines from macrophages.
... Among 9 phytochemistry papers with in vitro studies [8][9][10][11][12][13][14][15][16] , 5 [11,[13][14][15][16] were selected based on their relevance, but the phytochemistry component did not adhere to the selection criteria. A total of 10 in vitro studies only were included in this review [17][18][19][20][21][22][23][24][25][26] . Fig. 1 illustrates the study selection process. ...
... These analgesic effects were also detected in a pain threshold tail writhing test with intramuscular injection of GC and GV in murine models at doses of 25, 50 and 100 mg·kg −1 . Pain deterrent at higher doses were prolonged with a considerable reduction of spasmodic pain were observed in the models [26] . Anomalin is particularly effective against hyperalgesia and allodynia, exerting strong anti-nociceptive effects after 4 hour at 50 mg·kg −1 , inhibiting carrageenan-induced hyperalgesia [19] . ...
Article
Saposhnikoviae divaricata (Turcz.) Schischk (SD) is a traditional Chinese herb commonly used to treat clinical conditions such as rheumatism and allergic rhinitis. This review article evaluates a collection of works on in vitro and biochemical studies of SD. The discourse on the diverse class of chromones and coumarins in SD offers an insight to the pharmacological effects of these bioactive constituents as anti-inflammatory, analgesic, immunoregulatory, antioxidative, and anti-proliferative agents. It is highlighted that there is a structural relationship between the constituents and bioactive activities, which in effect provides a valid reasoning and reaffirm the use of SD in the treatment of the pathologies in Chinese medicine.
... In Radix Astragali, astragalosides have been identified as potential bioactive compounds via intestinal absorption and cell extraction studies (Xu et al., 2006;Zhang et al., 2008). Furthermore, numerous pharmacological studies have shown anti-inflammatory, antiviral, and antioxidant activities for the constituents astragalosides, astragaloside IV, calycosin-7-O-b-D-glucoside, prim-O-glucosylcimifugin and 4 0 -O-b-glucopyranosyl-5-O-methylvisamminol (Wang et al., 2008;Xue et al., 2000;Yin et al., 2010;Yu et al., 2005;Zhang et al., 2003Zhang et al., , 2006. These glycosides ( Fig. 1) may explain the effectiveness of YPFS. ...
... However, its aglycone cycloastragenol can be absorbed through intestinal epithelium efficiently . This is similar to prim-O-glucosylcimifugin, 4 0 -O-b-glucopyranosyl-5-O-methylvisamminol, and their aglycone cimifugin Xue et al., 2000;Zhao et al., 2011). It has been reported that changes in telomere lengths are relevant to immune function (Weng, 2012), and cycloastragenol upregulates telomerase activity (Fauce et al., 2008;Ríos, 2010;Yung et al., 2012). ...
Article
Ethnopharmacological relevance: Yu Ping Feng San (YPFS, in Chinese: Jade Windscreen Powder), a well-known traditional Chinese medicine, is commonly used to cure the diseases of respiratory systems and immune systems. Aim of the study: A selective and sensitive high-performance liquid chromatography coupled with mass spectrometry method (HPLC-MS) was developed and validated for simultaneous quantification of cycloastragenol, formononetin, calycosin, 4'-O-β-glucopyranosyl-5-O-methylvisamminol (GMV) and cimifugin in rat plasma after oral administration of Yu Ping Feng San decoction. Materials and methods: Plasma samples were extracted via solid-phase extraction (SPE), separated on a Zorbax SB-C18 column, detected by single quadruple mass spectrometry with an electrospray ionization interface, and quantified using selected ion monitoring mode. The current SPE-HPLC-MS assay was validated for linearity, intra-day and inter-day precisions, accuracy, extraction recovery and stability. The method was applied to a comparative pharmacokinetic study after administration of Yu Ping Feng San to rats at different doses (10, 20 and 40g/kg). Results: The calibration curves were linear over the ranges 0.50-50ng/mL and 17.36-1736ng/mL. Intra- and inter-day precisions (relative standard deviations) were from 0.45% to 10.95%, and accuracy (relative recovery) from 95% to 115%. The extraction recoveries were greater than 88.42% for all analytes. Dose-dependence was shown for some constituents in the drug concentration-time profiles. Among all the active ingredients detected, cimifugin had the highest blood concentration (881-1510ng/mL), and cycloastragenol had the longest retention time in the rat body (15.06-20.44h). Conclusion: This analytical method is a selective, sensitive, precise, accurate, and reliable assay for simultaneous determination of cycloastragenol, calycosin, formononetin, GMV, and cimifugin in rat plasma.
... SR contains chromones, coumarins, organic acids, polysaccharides, polyacetylenes, and sterols components in which chromones are the main active constituents [3][4][5][6]. According to research, prim-o-glucosylcimifugin (POG) and 5-o-methylvisamminoside (5OM) can not only decrease the temperature of febrile rats but also has obvious antipyretic, analgesic, anti-inflammatory, and antiplatelet aggregation effects [7]. Moreover, the content of cimicifugin (CIM) is found to be the highest in plasma. ...
Article
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In this paper, ultrasonic-assisted deep eutectic solvent (DES) extraction was applied to the acquisition of chromones (cimicifugin, prim-o-glucosylcimifugin, and 5-o-methylvisamminoside) from Saposhnikoviae radix (SR). The extraction effects of 11 prepared DESs were screened taking contents of chromones as indexes. Furthermore, the optimum extraction conditions were confirmed using a single-factor test and response surface optimization test. Scavenging activities of DPPH anion and ABTS cation radicals of different SR extracts (DES, methanol, and ethanol) were studied. The analysis results of best extraction conditions optimized by Design-Expert software were as follows: extraction time (40 min), extraction temperature (60°C), and the solid/liquid ratio (32 mL/g). Scavenging rates of the DES extract for DPPH anion radical and ABTS cation radical were found to be 75.31% and 65.71%, which were higher than those of methanol and ethanol extracts. In conclusion, the developed extraction method can be regarded as a safe, green, and more effective approach for the extraction of chromones in SR.
... Some members of the chromone alkaloids (Houghton 2000) display strong HIV and Herpes Simplex Virus inhibitory activity, while some chromone glycosides, including prim-O-glucosylcimifugin and 4 0 -O-b-D-glucosyl-5-O-methylvisamminol (Xue et al. 2000) expressed analgesic, antipyretic, anti-inflammatory and anti-platelet aggregation activities in different in vivo models. Chromone glycosides, takanechromones A-C (22-24), isolated from Hypericum sikokumontanum, inhibited the growth of Helicobacter pylori and displayed cytotoxic activity towards a variety of human cancer cells (Tanaka et al. 2009). ...
Article
Full-text available
Chromones are naturally occurring phenolic compounds that are universally present in a healthy human diet. To date, thousands of chromone derivatives, including chromone glycosides have been discovered, both from natural and synthetic origin. Many plant genera, including Aloe, Aquilaria, Cassia, Hypericum and Polygonum, are rich sources of chromones. Several genera of fungi, such as Aspergillus, Mycoleptodiscus, Orbiocrella, and Penicillium produce bioactive chromones. This class of compounds is mainly associated with anti-oxidant, antimicrobial, anticancer and anti-inflammatory activities. Various in vitro, in vivo and clinical studies have established the role of chromones in alleviating allergies, reducing oxidative damage, inhibiting cancer, infections and inflammation, and for treating neurological and psychiatric disorders. This review focuses mainly on natural chromones, and elaborates on their nutritional benefits, pharmacological activities, and mechanisms of action. Various scientific databases, including PubMed, Scopus and Google Scholar, were used to find relevant literature on chromones covering all available literature up to, and including the year 2019. This critical analysis of completed research regarding the nutraceutical properties of various chromone derivatives may provide new insight to scientists working in related fields.
... Prim-O-glucosylcimifugin and 4′-O-β-d-glucosyl-5-O-methylvisamminol are the main bioactive secondary metabolites in its roots. It was reported that these two components have obvious antipyretic, analgesic, anti-inflammatory and antiplatelet aggregation effects (Xue et al. 2000). Volatile components are another class of secondary metabolites in Saposhnikovia divaricata. ...
Article
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Saposhnikovia divaricata (Turcz.) Schischk is a traditional herb of East Asia. Bioactive chromones and volatile components in its roots are known to exhibit pharmacological functions. However, limited information is available on the drought resistance of this herb. In this study, potted Saposhnikovia divaricata seedlings were subjected to a progressive drought stress of 20 days by withholding water followed by twice rehydration, which resulted in some physiological, biochemical and secondary metabolite responses as well as drought acclimatization. A decline in leaf water content but increase in electrolyte leakage, malondialdehyde (MDA), hydrogen peroxide (H2O2), glutathione (GSH), proline, soluble sugar, prim-O-glucosylcimifugin and 4′-O-β-d-glucosyl-5-O-methylvisamminol content was observed. After rehydration, some of the indices recovered except proline, soluble sugar, prim-O-glucosylcimifugin and 4′-O-β-d-glucosyl-5-O-methylvisamminol content. Moreover, mild (day 8), moderate (days 12–16) and severe (day 20) drought phases were identified. A total of 18 volatile components were identified by GC–MS under different drought phases, of which aromatic alcohols (42.02%) and sesquiterpenes (37.35%) were the major components. The characteristic component named falcarinol was decreased by severe drought stress. This study demonstrated that Saposhnikovia divaricata had strong drought acclimatization, and resisted drought by activating the antioxidant system and accumulating osmolytes. In addition, moderate and severe drought stress promoted bioactive secondary metabolites prim-O-glucosylcimifugin and 4′-O-β-d-glucosyl-5-O-methylvisamminol accumulation. Severe drought stress reduced falcarinol relative content, which provided an insight for improving the quantity of Saposhnikovia divaricata bioactive components.
... The data shown in Table 2, indicate that anti-inflammatory properties of 1, 1a and 2 could be explained in terms of the inhibition of NF-kB transcriptional activity and inhibition of iNOS. The results are also in agreement with the previously reported anti-inflammatory effects of acalyphin (Nirmal et al., 2008), chromone glucosides (Xue et al., 2000 ), and apigenin (Funakoshi-Tago et al., 2011). However, the chloroform and methanol extracts of the Saudi A. fruticosa species did not show anti-inflammatory activity, probably implying the antagonistic action of various constituents present in them. ...
Article
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Acalypha is an important genus of the Euphorbiaceae family. The genus is represented by five species in Saudi Arabia. Acalypha fruticosa Forssk. Fl. Aeg is traditionally used as a cure for stomachache, dyspepsia, rheumatism, dermatitis, and swellings of the body. The present study endeavors to provide a phytochemical and biological evaluation of the plant, with the aim of relating activity to constituting secondary metabolites in the plant. Column chromatographic separation of the methanol extract led to the isolation of four compounds namely; 2-methyl-5,7-dihydroxychromone 5-O-β-D-glucopyranoside 1, acalyphin 2, apigenin 3 and kaempferol 3-O-rutinoside 4. The plant extracts and the isolated compounds were subjected to biological assays to screen peroxisome proliferator-activated receptor alpha (PPARα) and PPARγ agonistic, anti-inflammatory and cytotoxic activities. Results proved for the first time, the PPARγ activator effect of acalyphin, as well as its promising anti-inflammatory activity, in addition to the dual PPAR activator effect of the chromone glucoside. The plant extracts and isolated compounds were non-cytotoxic to the tested cell lines. Thus A. fruticosa could be a valuable source of important therapeutics that may hold clinical prospect.
Article
Ethnopharmacological relevance: Saposhnikovia divaricata (SD), called "Fangfeng" in China, is commonly used in clinical compound prescription for treatment of rheumatoid arthritis (RA), but its actions on RA have not been clarified. The present study aims to determine the anti-inflammatory activity of SD chromone extract (SCE), the major bioactive component of SD, on collagen-induced arthritis (CIA) rats, and elucidate its underlying mechanisms with regards to its molecular basis of action on human fibroblast-like synoviocytes derived from RA patients (HFLS-RA). Materials and methods: CIA model on rats was constructed by injection of bovine type II collagen. Rats were pre-treated with different dosages of SCE from 3 days before till 35 days after model building. The progression of CIA was evaluated by macroscopic scoring, X-ray observation and hematoxylin and eosin (HE) staining of paws. HFLS-RA were pre-treated with different concentrations of SCE prior to stimulation with 10 ng/ml of tumor necrosis factor (TNF) α. By radioimmunoassay (RIA) and enzyme-linked immunosorbent assay (ELISA), levels of interleukin (IL)-1β, IL-6, TNFα and prostaglandin E2 (PGE2) were quantified respectively. Nuclear factor (NF-κB) p65 expression and DNA-binding activity were tested by immunohistochemisty and electrophoretic mobility shift assay (EMSA) respectively. Phosphorylation of extracellular signal-regulated kinase (ERK), Jun N-terminal kinase (JNK) and p38 MAPKs were examined by immunohistochemisty staining and western blot analysis. Results: Histological examination and radiological observation demonstrated that SCE significantly reduced the inflammatory responses in the joints of CIA rats. SCE inhibited the production of TNFα, IL-1β, and IL-6 in the joint tissues and sera. The level of PGE2 in sera was also decreased by SCE. Moreover, SCE treatment in vivo was able to reduce protein level of NF-κB, the transcriptional factor closely related to the inflammatory process, in articular synovium and cartilage of CIA rats. In addition, SCE inhibited p-ERK, p-JNK and p-p38 expression, which were considered to be involved in the phosphorylation of transcription factor NF-κB and the transcription of pro-inflammatory factors. Further, SCE inhibited NF-κB DNA binding activity and attenuated the phosphorylation of ERK, JNK and p38 MAPKs, in a concentration-dependent manner in cultured HFLS-RA. Conclusion: These results highlight the anti-arthritic potential of SCE, and provide further evidence of the involvement of the NF-κB and MARKs inhibition in the effects of SCE.
Article
A sensitive and reliable liquid chromatography-mass spectrometry method has been developed and validated for simultaneous determination of cimifugin and prim-O-glucosylcimifugin in rat plasma after oral administration of Radix Saposhnikoviae (RS) extract, prim-O-glucosylcimifugin monomer solution and cimifugin monomer solution. Plasma samples were pretreated by protein precipitation with acetonitrile containing the internal standards puerarin and daidzein. LC separation was achieved on a Zorbax SB-C(18) column (150 × 4.6 mm i.d., 5 µm) with 0.1% formic acid in water and methanol by isocratic elution. The detection was carried out in select-ion-monitoring mode with a positive electrospray ionization interface. The fully validated method was successfully applied to the pharmacokinetic study of the analytes in rats. A bimodal phenomenon appeared in the concentration-time curve of prim-O-glucosylcimifugin and cimifugin after oral administration of RS extract. Prim-O-glucosylcimifugin mainly transformed to cimifugin when it was absorbed into blood. Both absorption and elimination of cimifugin after oral administration of RS were longer than after administration of single cimifugin. The pharmacokinetic parameters (AUC(0-t) , AUC(0-∞) and t(1/2) ) of prim-O-glucosylcimifugin and cimifugin by giving cimifugin monomer solution, prim-O-glucosylcimifugin monomer solution and RS extract had significant differences (P < 0.05).
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Migraine is a common clinical disabling disease that seriously affects the patient's health, and there are many adverse reactions associated with the drugs that treat it. Chuanxiong Chatiao granules (CXCT) have the effect of dispersing wind and relieving pain, and are often used to treat migraine. At present, the potential compounds and mechanism of CXCT in the treatment of migraine are unclear. In this study, a total of 119 components of CXCT were identified, based on UHPLC-QE-Orbitrap-MS, which preliminarily characterized the potential compounds of CXCT, and Schrodinger software was used to carry out molecular docking between these 119 components and migraine targets. The first 30 components with low binding energy were selected and entered on the Swisstarget website to predict targets, resulting in 318 treating targets being obtained by intersection of the components with the disease targets. Cytoscape software was used to construct the "compounds-targets-disease" network, and 124 related pathways were obtained from the Kyoto Encyclopedia of Genes and Genomes (KEGG) database. It was predicted that CXCT could play a role in the treatment of migraine by regulating neurotransmitter transmission, inflammation, angiogenesis, vasomotor, immunity and other pathways.
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Methods using high performance liquid chromatography with diode array detection (HPLC-DAD) and tandem mass spectrometry (HPLC-MS/MS) were developed and validated for the simultaneous determination of 5 chromones and 6 coumarins: prim-O-glucosylcimifugin (1), cimifugin (2), nodakenin (3), 4'-O-β-d-glucosyl-5-O-methylvisamminol (4), sec-O-glucosylhamaudol (5), psoralen (6), bergapten (7), imperatorin (8), phellopterin (9), 3'-O-angeloylhamaudol (10) and anomalin (11), in Radix Saposhnikoviae. The separation conditions for HPLC-DAD were optimized using an Ascentis Express C18 (4.6 mm×100 mm, 2.7 μm particle size) fused-core column. The mobile phase was composed of 10% aqueous acetonitrile (A) and 90% acetonitrile (B) and the elution was performed under a gradient mode at a flow rate of 1.0 mL/min. The detection wavelength was set at 300 nm. The HPLC-DAD method yielded a base line separation of the 11 components in 50% methanol extract of Radix Saposhnikoviae with no interfering peaks detected. The HPLC-DAD method was validated in terms of linearity, accuracy and precision (intra- and inter-day), limit of quantification (LOQ), recovery, and robustness. Specific determination of the 11 components was also accomplished by a triple quadrupole tandem mass spectrometer equipped with an electrospray ionization (ESI) source. This HPLC-MS/MS method was also validated by determining the linearity, limit of quantification, accuracy, and precision. Quantification of the 11 components in 51 commercial Radix Saposhnikoviae samples was successfully performed using the developed HPLC-DAD method. The identity, batch-to-batch consistency, and authenticity of Radix Saposhnikoviae were successfully monitored by the proposed HPLC-DAD and HPLC-MS/MS methods.
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Radix Saposhnikoviae is one of the most famous Chinese herbal medicines with many pharmacological activities towards inflammatory symptoms and antioxidation. Chromones are considered as one of the effective components. It is important to find a reasonable method to extract the chromones in S. divaricata. To develop an ultrasonic-assisted extraction (UAE) to extract chromones in Radix Saposhnikoviae and to optimise extraction conditions. Four chromones (prim-O-glucosylcimifugin, cimifugin, 5-O-methylvisammioside and sec-O-glucosylhamaudol) were extracted by the UAE method combined with response surface methodology (RSM). Box-Behnken design (BBD) was applied to evaluate the effects of three independent variables (ethanol concentration, extraction time and extraction temperature) on the chromones yield of Radix Saposhnikoviae. Correlation analysis of the mathematical-regression model indicated that a quadratic polynomial model could be employed to optimise the extraction of chromones by UAE method. The optimal conditions to obtain the highest chromones yield of Radix Saposhnikoviae were a solvent of 75% ethanol, an extraction time of 48 min and an extraction temperature of 67°C. Under these optimal conditions, the experimental values agreed closely with the predicted values. The analysis of variance indicated a high goodness of model fit and the success of RSM method for optimising chromones extraction in Radix Saposhnikoviae.
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A high‐speed counter‐current chromatography (HSCCC) method for separation and purification of prim‐O‐glucosyl‐cinmifugin and 4′‐O‐β‐D‐glucosyl‐5‐O‐methylvisamminol from the extract of Radix saposhnikoviae was developed by using chloroform‐methanol‐water (10∶8∶4, v/v) as the two‐phase solvent system. Prim‐O‐glucosyl‐cinmifugin (21.7 mg) and 44.7 mg of 4′‐O‐β‐D‐glucosyl‐5‐O‐methylvisamminol were produced from 100 mg of the crude sample, both at over 99.0% purity, determined by HPLC. The structures of the isolated compounds were identified by H‐NMR and C‐NMR.
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An efficient pressurized liquid extraction (PLE) technique was employed in extracting chromones from the roots of Saposhnikovia divaricata (Radix Saposhnikoviae). Chromones were quantified and analyzed by LC-ESI/MS. The PLE procedure was optimized, validated and compared with the other conventional extraction techniques. PLE gained the best result due to the highest extraction efficiency within the shortest extraction time. The optimal conditions of PLE were employing 50% ethanol as the extraction solvent at a temperature of 140°C and an extraction pressure of 1500 psi, using one extraction cycle with a static extraction time of 8 min. A good LC separation was achieved using a Hypersil ODS2 column and methanol/water as the mobile phase at a flow rate of 0.8 mL/min. MS coupling with an ESI interface in the positive ion mode was used as the detection technique. This is the first report on combining PLE with LC-ESI/MS for the extraction and quantification of chromones in Radix Saposhnikoviae. The elaborated PLE method also provided a good alternative for the chromone extraction from other plant substances.
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The traditional Chinese herbal formula Cang Er Zi San has been used for the treatment of rhinitis, paranasal sinusitis, and allergic rhinitis for several centuries. However, its therapeutic mechanisms remain largely unclear. To study the effects of Shi-Bi-Lin (SBL), a modified Cang Er Zi San formula, on cytokine release from and expressions in the human mast cell line (HMC-1). The HMC-1 was preincubated with different concentrations of SBL extract solution 1 hour before being stimulated with 25 ng/mL of phorbol myristate acetate plus 2.5 x 10(-7)M calcium ionophore A23187 and then further incubated for 6, 12, and 24 hours, respectively. The cell culture supernatants were harvested, and the cytokines of interleukin 4 (IL-4), IL-6, IL-8, and tumor necrosis factor alpha (TNF-alpha) in the supernatants were measured by enzyme-linked immunosorbent assay. Furthermore, the total RNA of the cells was extracted, and the cytokines' messenger RNA expressions were examined using semiquantitative reverse transcriptase-polymerase chain reaction. After different incubation periods at different concentrations, SBL could potently inhibit the cytokines of IL-4 and TNF-alpha and modestly affect IL-6 but not obviously affect IL-8 release from the HMC-1. However, no inhibitory effects were detected on the messenger RNA expressions of these cytokines. These results demonstrate that SBL could modulate the mast cell-mediated hypersensitivity reaction in allergy. Inhibition of mast cell-derived IL-4 and TNF-alpha might explain the efficacy of SBL in treating allergic disease.
Article
A preparative high-speed counter-current chromatography (HSCCC) method for the isolation and purification of 1''-O-glucosylcimifugin (1), 4'-O-beta-d-glucosyl-5-O-methylvisamminol (2), cimifugin (3) and 3'-O-glucosylhamaudol (4) from the Chinese medicinal herb radix saposhnikoviae has been successfully developed. A sample of 300 mg of crude extract was separated using ethyl acetate:n-butanol:1% aqueous acetic acid (1:4:5, v/v) as the two-phase solvent system and yielded 102.4 mg of 1 and 81.6 mg of 2. During this separation 3 and 4 remained in the stationary phase, which was collected, evaporated to dryness and separated with another two-phase solvent system involving ethyl acetate:n-butanol:1% aqueous acetic acid (5:0.5:5, v/v) to yield 31.4 mg of 3 and 12.7 mg of 4. The purities of compounds 1-4 were 98.4, 98.7, 99.3 and 98.2%, respectively, as determined by HPLC. The chemical structures of these components were established by (1)H-NMR and (13)C-NMR.
Article
Four chromones, prim-O-glucosylcimifugin, 4'-O-β-D-glucosyl-5-O-methylvisamminol, cimifugin and sec-O-glucosylhamaudol, were isolated and purified from Saposhnikovia divaricata for the first time by high-performance counter-current chromatography (HPCCC) using a system consisting of ethyl acetate/n-butanol/ethanol/water (1:1:0.1:2, v/v/v/v). The separation parameters were first performed on the analytical HPCCC and the optimized conditions were then scaled up to preparative HPCCC. A total of 72.1 mg of prim-O-glucosylcimifugin, 27 mg of 4'-O-β-D-glucosyl-5-O-methylvisamminol, 14.1 mg of cimifugin and 1.1 mg of sec-O-glucosylhamaudol were purified from 960 mg of the n-butanol extract of S. divaricata, each at over 90% purity as determined by high-performance liquid chromatography (HPLC). The structures of four compounds were identified by their retention time, the liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS) in the positive ion mode, and confirmed by NMR. The characteristic LC-ESI-MS fragmentation patterns of the four compounds were discussed, and found to be a very specific and useful tool for the structural identification of chromones from S. divaricata.
Article
Background: Radix Saposhnikovia (RS), called "Fangfeng" in China, is commonly used in Chinese medicinal formulae to treat allergic and inflammatory diseases. However, the underlying mechanisms of RS in ameliorating allergy remain unknown. Purpose: To study the effects of RS extract on allergic contact dermatitis (ACD) in a mouse model and to investigate the underlying mechanisms in vivo and ex vivo. Methods: ACD was induced by sensitizing the mice and treating an ear auricle with 1-chloro-2,4-dinitrobenzene (DNCB). RS extract was administered during the sensitization and/or elicitation phase. Ear swelling was noted and lymphocytic infiltration was investigated with hematoxylin and eosin staining. The cytokines in the sera and the supernatants of lymphocyte cultures were determined with enzyme-linked immunosorbent assays. Lymphocyte proliferation was assessed with a 3-(4,5)-dimethylthiazol-2-y1)-2,5-diphenyltetrazolium bromide (MTT) assay. The maturation of dendritic cells (DCs) and the differentiation of T cells were examined with flow cytometry. The mRNA expression of T-bet, GATA-3, and forkhead box p3 (Foxp3) was evaluated with real-time PCR. Results: RS extract (1.3 or 2.6 g/kg) markedly reduced the ear swelling and the intense cellular infiltration of inflammatory cells in the ear tissue. The ratio of interferon γ (IFN-γ)/interleukin 4 (IL-4) was reduced in the sera of the DNCB-sensitized mice and the lymphocyte culture supernatants after treatment with the extract. Further study of the initial stage of ACD revealed that RS extract prevented the differentiation of naïve T cells into Th1 cells, reduced the proportion of CD3(+)CD4(+) (Th) cells, and suppressed the secretion of IFN-γ and the expression of T-bet mRNA in lymphocytes. The RS extract also reduced the proportion of DCs in the sensitized mouse lymphocytes and the expression of CD40(+)CD86(+) cells in the DCs. Conclusion: RS extract is effective in treating ACD because it regulates the development of DCs and DC-activated Th1 differentiation.
Article
Five known chromones were isolated and purified from Saposhnikovia divaricata for the first time by combination of reverse-phase medium-pressure liquid chromatography (RP-MPLC) and high performance counter-current chromatography (HPCCC). The n-butanol extracts of S. divaricata were preliminarily chromatographed by RP-MPLC, and further isolated by preparative HPCCC. A total of 582.8 mg of prim-O-glucosylcimifugin, 228.9 mg of 4′-O-β-D-glucosyl-5-O- methylvisamminol, 113 mg of cimifugin, 14.5 mg of sec-O-glucosylhamaudol, and 4.68 mg of 5-O-methylvisamminol were purified from 7.48 g of the n-butanol extract of S. divaricata, each at over 95% purity as determined by high performance liquid chromatography (HPLC). The identification of the five purified compounds was achieved by congruent retention times, the data of the liquid chromatography- electrospray ionization mass spectrometry (LC-ESI-MS) and nuclear magnetic resonance spectroscopy (NMR) with those of the authentic standards and literature reports.
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Xiao-xu-ming decoction (XXMD) is a traditional Chinese medicine that has been widely used to treat theoplegia and its sequelae. This paper reports the development of three separate assays based on reversed phase high-performance liquid chromatography–mass spectrometry (HPLC–MS) and HPLC–MS/MS for the determination of seven active constituents of XXMD viz oroxylin A-7-O-glucuronide, wogonoside, liquiritigenin, cimifugin, 5-O-methylvisammiol, glycyrrhizic acid and glycyrrhetinic acid in rat plasma. All calibration curves were linear (r >0.99) with lower limits of quantitation (LLOQs)<12.4 ng/mL. Intra- and inter-day precisions (as relative standard deviation) were all <10.7% with recoveries in the range of 88.7–113%. In addition, the seven analytes were shown to be stable in rat plasma samples under relevant storage conditions. The validated methods were successfully applied to a pharmacokinetic study in rat after oral administration of XXMD.
Article
Aims The current study aims to investigate the effect of Yupingfeng (YPF) powder on immunosuppression, and explore the possible mechanisms. Main methods Firstly, the monomer components of YPF powder were analyzed by UPLC-QTOF-MS combined with UNIFI automatic analysis platform, then the mechanism of YPF on immunosuppressive treatment was investigated using network pharmacological method, and finally the prediction was verified in a Candida albicans (Can)-induced immunosuppressive BALB/c mouse model. Key findings 98 monomer compounds in YPF were obtained. Through virtual analysis and screening on the oral utilization and drug likeness properties of the components, 47 effective components were got. 9 core targets obtained were enriched in IL-17 signaling pathway. In the mouse model, YPF could reduce the number of Can and alleviate Can-induced inflammation in the kidney effectively, upregulate Can-induced low proportion of CD4⁺/CD8⁺ of splenic lymphocytes, and increase Can-induced low activity of IL-17 pathway. Significance These results demonstrate that YPF could improve the immunity of Can-induced immunosuppression in BALB/c mice through upregulating the activity of IL-17 pathway.
Article
Ethnopharmacological relevance: An efficacious antidepressant without unwanted side effects is need urgently at present. This study aimed to investigate whether treatment with four Chinese herbal medicines (CHMs), namely Radix Astragali, Saposhnikovia divaricate (SD), Eucommia ulmoides Oliv. bark (EU), and Corydalis yanhusuo W. T. Wang (C. yanhusuo), could reverse the effects of chronic mild stress (CMS) in a depression-like mouse model and the potential mechanism(s) of their action. Materials and methods: In vitro study, the proliferation of NSCs was assessed using the MTS assay. In vivo study, chronic mild stress (CMS) was used in mice for 14 days to establish a depression-like mouse model. Plasma corticosterone levels were assessed by UPLC coupled to a triple-quadrupole mass spectrometer. The forced swim test (FST) was used to assess the effects of the four CHMs on depression. BrdU incorporation and TUNEL staining were used to assay hippocampal precursor cell proliferation rate and apoptosis. Results: The CHMs included Radix Astragali, EU, C. yanhusuo, and SD were shown to promote neuroproliferation in vitro. In vivo study, oral administration of these four CHMs for 14 days reversed the elevated plasma corticosterone levels, body weight loss, decrease in proliferation of hippocampal precursor cells; they also inhibited hippocampal cell apoptosis, and exhibited an antidepressant-like effect in a depression-like mouse model induced by CMS. Conclusions: Our study indicates that each of these CHMs has the potential to ameliorate depression. The possible mechanisms of action include modulation of the HPA axis, reduction in stress hormone levels, inhibition of apoptosis, and promotion of hippocampal neuronal plasticity and neurogenesis.
Article
Introduction 4’-O-β-D-glucosyl-5-O-methylvisamminol (GML) is a conventional marker compound for quality control of Radix Saposhnikoviae. Despite that, neither pharmacodynamic or pharmacokinetic information is available with regard to GML. As such, the aim of thisstudy was to assess the conventional evaluation indices for the quality of Radix Saposhnikoviae. Materials and methods Pyretic animal model, hot plate test, and ear edema model were established to evaluate and compare the antipyretic, analgesic, and anti-inflammatory effect of the chromone derivativescimifugin, prime-O-glucosylcimifugin (PGCN), and GML in Radix Saposhnikoviae. High performance liquid chromatography separation and analysis was used to obtain pharmacokinetic parameters. Simulated gastric fluid and simulated intestinal fluid was used to investigate the metabolite profiles of PGCN and GML in gastrointestinal tract. Results Cimifugin exerted a marked dose-dependent antipyretic, analgesic, and anti-inflammatory effect, whereas the effects of PGCN were relatively lower. GML had feeble pharmacodynamic effects. Pharmacokinetic study showed that only cimifugin was detected in the plasma sample of cimifugin and PGCN-treated animals, with drug concentration in the former much higher than the latter. No components were traced in the plasma samples from GML-treated rats. Stability study showed that PGCN and GML was predominantly biotransformed into cimifugin and 5-O-methyvisammiol, respectively. The latter was proven to be extremely unstable in liver tissue homogenate and plasma. Conclusions A feeble antipyretic, analgesic, and anti-inflammatory activities was observed when GML was orally delivered. Given that Radix Saposhnikoviae extract is generally administered orally, we speculate that this compound might be a nonpharmacolagically active agent in real usage. Thus, it might be unscientific to evaluate the quality of Radix Saposhnikoviae based on the content of GML. SUMMARY GML-derived cimifugin, which represents the potential pharma codynamic component of Radix Saposhnikoviae chromones, in plasma was almost nil in contrast to cimifugin and PGCN. And thus, feeble antipyretic, analgesic, and anti-inflammatory activities were found with GML. Abbreviations used: AUC:area under concentration-time curve, DNP:2,4-Dinitrophenol, HPLC:high performance liquid chromatography, HPLC-MS:high performance liquid chromatography- mass spectrography, GML:4’-O-β-D-glucosyl-5-O-methylvisamminol, MVL:5-O-methyvisammiol, PGCN:prime-O-glucosylcimifugin, SGF:alkaline phosphatase. SIF:simulated intestinal fluid
Article
Prim-O-glucosylcimifugin is a major constituent in Radix Saposhnikovia that has been long used for the treatment of pyrexia, rheumatism, and cancer in traditional Chinese medicine. However, the molecular and cellular mechanisms remain unknown regarding the therapeutic effect of prim-O-lucosylcimifugin. Here, we investigated the effects of prim-O-glucosylcimifugin on cell cycle progression and apoptosis in human acute lymphoblastic leukemia cells. Prim-O-glucosylcimifugin treatment resulted in marked increases in cell apoptosis and cell cycle arrest at the G2/M phase. Mechanistically, prim-O-glucosylcimifugin induced the degradation of β-tubulin and downregulated phosphorylated CDK1 levels, a molecular indicator in the G2/M cell cycle arrest. Furthermore, activation of caspase-3, caspase-8, and caspase-9 was involved in the prim-O-glucosylcimifugin-induced apoptosis. Our study reveals the anticancer activity of prim-O-glucosylcimifugin and the potential underlying mechanisms.
Article
Background Radix Saposhnikoviae (RS) exerts anti-inflammatory, analgesic, antipyretic, antioxidation effects and has been used in traditional Chinese medicine to treat common colds, headache, and rheumatoid arthritis. Prim-O-glucosylcimifugin (POG) is the highest content chromone and one of the major active constituents in RS. Objective The study was aimed to explore the anti-inflammation effects of POG in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Materials and Methods Cell viability was detected by Cell Counting Kit-8 assay. Production of nitric oxide (NO), tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and IL-6 was assessed by enzyme-linked immunosorbent assay. Real-time polymerase chain reaction and Western blot were performed to analyze mRNA and protein levels, respectively. Results During the whole experiment, 15, 50, and 100 μg/mL of POG had no cytotoxicity on RAW 264.7 cells. POG dose-dependently inhibited the production of NO, TNF-α, IL-1β, and IL-6 that were induced by LPS. POG treatment downregulated the mRNA and protein expression inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2) in LPS-activated RAW 264.7 macrophages in a concentration-dependent manner. Furthermore, LPS-induced JAK2/STAT3 activation was prevented in RAW 264.7 macrophages by POG treatment. STAT3 overexpression significantly reversed the effects of POG on LPS-activated RAW 264.7 macrophages. Conclusion These results demonstrate that POG exerts anti-inflammatory effects through the inhibition of iNOS and COX-2 expression by inhibiting the phosphorylation of JAK2/STAT3. SUMMARY POG exerts anti-inflammatory effects in RAW 264.7 macrophages through the inhibition of iNOS and COX-2 expression by inhibiting JAK2/STAT3 signaling. Abbreviations used: LPS: Lipopolyssacharide; NO: Nitric oxide; TNF-α: Tumor necrosis factor-α; IL: Interleukin; RS: Radix Saposhnikoviae; POG: Prim-O-glucosylcimifugin; iNOS: Inducible NO synthase; COX2: Cyclooxygenase; FBS: Fetal bovine serum; DMSO: Dimethylsulfoxide; CCK-8: Cell Counting Kit; RIPA: Radio immunoprecipitation assay buffer; ECL: Enhanced chemiluminescence; SD: Standard deviation; ELISA: Enzyme-Linked immunosorbent assay.
Article
Ultra-performance convergence chromatography is an environmentally friendly analytical technique that employs dramatically reduced amounts of organic solvents compared to conventional chromatographic methods. In this study, a rapid, sensitive, and environmentally friendly method based on ultra-performance convergence chromatography was developed for the quantification of four major chromones present in the roots of Saposhnikovia divaricata (Turcz.) Schischk. Using this method, the analysis time was significantly shortened compared to conventional high-performance liquid chromatography techniques. In addition, the influence of co-solvent type, co-solvent ratio, column temperature, system pressure, and flow rate on the peak resolution was investigated. The proposed method was validated in terms of its limits of detection, limits of quantitation, linearity, precision, and accuracy. More specifically, the limits of detection of the four chromones ranged from 0.006 to 0.033 μg/mL, while the limits of quantitation ranged from 0.019 to 0.101 μg/mL. Our method also exhibited a good regression (r² > 0.999), excellent precision (RSD < 0.60%), and acceptable recoveries (99.48–102.89%). Finally, the quantities of these four chromones present in 20 commercial samples from Korea and China were successfully evaluated using the developed method, indicating that the proposed method is suitable for the rapid and accurate quality control of S. divaricata.
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Colorectal cancer ranks 3rd in terms of cancer incidence. Growth and development of colon cancer cells may be affected by juice and extracts from Saposhnikovia divaricata root. The objective of the research was to analyze the effect of S. divaricata juice and extracts on the viability, membrane integrity and types of cell death of Caco-2 cells. Juice and extracts were analyzed using Ultra-High Performance Liquid Chromatography-Mass Spectrometry (UHPLC-MS) and in respect of the presence of antioxidants, total carbohydrates, protein, fat and polyphenols. The contents of cimifugin β-D-glucopyranoside, cimifugin, 4-O-glucopyranosyl-5-O-methylvisamminol, imperatorin and protein were the highest in juice. 50% Hydroethanolic extract had the greatest antioxidant potential, concentration of polyphenols and fat. Water extract was characterized by the highest content of glutathione. Juice and 75% hydroethanolic extract contained the most carbohydrates. After the application of juice, 50% extract and the juice fraction containing the molecules with molecular weights >50 kDa, a decrease of the cell viability was noted. Juice and this extract exhibited the protective properties in relation to the cell membranes and they induced apoptosis. The knowledge of further mechanisms of anticancer activity of the examined products will allow to consider their use as part of combination therapy.
Article
Qu‐feng‐sheng‐shi Grannules (QFSSG), a common prescription for the treatment of chronic inflammation and allergic rhinitis (AR), is widely used in the clinic as a traditional Chinese medicine. Chemical analysis and quality control studies of this formulation are relatively limited compared to pharmacological studies. In this study, a high‐performance liquid chromatography coupled with electrospray ionization quadrupole time‐of‐flight tandem mass spectrometry (HPLC‐ESI‐Q/TOF‐MSn) was used to identify the components in this prescription. Next, to quantify six major compounds, a HPLC‐UV method was developed and validated. The results showed that 53 compounds were identified based on the MSn data, retention time and previous reports, including 17 coumarins, 14 lignans, 10 chromones, 9 phenylethanoid glycosides, and 3 other compounds, were identified or tentatively assigned. Contents of six major bioactive compounds (4'‐O‐beta‐Glucopyranosyl‐5‐O‐Methylvisamminol, Prim‐O‐glucosylcimifugin, Forsythin, Magnolin, Imperatorin, Isoimperatorin) could be determined by HPLC simultaneously. In addition, the potential anti‐inflammatory activity of six major compounds was determined, too, and we found that four compounds (4'‐O‐beta‐Glucopyranosyl‐5‐O‐Methylvisamminol, Prim‐O‐glucosylcimifugin, Forsythin, Imperatorin) have a potent nitric oxide inhibitory effect. In conclusion, this work provided comprehensive information on the quality control of QFSSG and evaluated the potential biological activity of the main components in QFSSG, which can be contributed to understanding and using it more scientifically.
Article
A sensitive and efficient liquid chromatography-mass spectrometry method was developed and validated for the simultaneous determination of two active chromones (prim-O-glucosylcimifugin and 4'-O-D-glucosyl-5-O-methylvisamminol) from Saposhnikovia root in rat plasma and urine. The plasma or urine samples were prepared by protein precipitation. Chromatographic separation of the two active chromones from matrix interferences was achieved on an Angilent TC-C(18) column with a mobile phase consisted of methanol, water and 0.1% formic acid. Puerarin was added as the internal standard. The method was validated with the concentration range 1.0-100 ng/mL in rat plasma and 10-1000 ng/mL in urine for prim-O-glucosylcimifugin, 1.5-150 ng/mL in plasma and 15-1500 ng/mL in urine for 4'-O-D-glucosyl-5-O-methylvisamminol. The lower limit of quantitation (LLOQ) of prim-O-glucosylcimifugin and 4'-O-D-glucosyl-5-O-methylvisamminol was 1.0 and 1.5 ng/mL in plasma, 10 and 15 ng/mL in urine, respectively. The intra- and inter-day precision across three validation days over the entire concentration range was lower than 9.0% as terms of relative standard deviation (R.S.D.). Accuracy determined at three quality control concentrations (2.0, 25 and 75 ng/mL for prim-O-glucosylcimifugin; 3.0, 37.5 and 112.5 ng/mL for 4'-O-D-glucosyl-5-O-methylvisamminol) ranged from -1.9 to 3.9% as terms of relative error (R.E.). The LC-ESI-MS method was further applied to assess pharmacokinetics and urine excretion of the two chromones after oral administration of Fangfeng extract to rats. Practical utility of this new LC-MS method was confirmed in pilot pharmacokinetic studies in rats following oral administration.
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