Feng Qiu

Shenyang Pharmaceutical University, Feng-t’ien, Liaoning, China

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Publications (116)246.1 Total impact

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    ABSTRACT: Biotransformations of curcumenol (1) were performed by four fungal strains, Mucor spinosus AS 3.2450, Penicillium urticae IFFI 04015, Cunninghamella echinulata AS 3.3400, Aspergillus carbonarius IFFI 02087. Five metabolites were prepared in the biotransformation process of 1, and their structures were elucidated as 15-hydroxycurcumenol (2), 1α-hydroxycurcumenol (3), 14-hydroxycurcumenol (4), 3β-hydroxycurcumenol (5) and 12-hydroxycurcumenol (6) by spectroscopic data analysis. Among them, metabolites 2-5 are novel. All of these four fungal strains showed the ability of highly stereo- and regiospecific hydroxylation for the substrate (1), which could be used as tools for preparing the hydroxylated derivatives and in vivo metabolites of curcumenol. In addition, the inhibitory effects of substrate and obtained products on nitric oxide production in lipopolysaccaride-activated macrophages were evaluated. The substrate (1) and metabolites 2, 5, and 6 showed significant inhibitory effects.
    Journal of Molecular Catalysis B Enzymatic 01/2015; DOI:10.1016/j.molcatb.2015.01.005 · 2.75 Impact Factor
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    ABSTRACT: Three new lanostane-type triterpenes, inonotusanes A-C (1-3), and a new naturally occurring one, 3β-hydroxy-25,26,27-trinorlanosta-8,22E-dien-24-oic acid (4), together with sixteen known triterpenoids (5-20), including 13 lanostane derivatives, 2 lupanes and 1 oleanane-type triterpene were isolated from the sclerotia of Inonotus obliquus. Their structures were elucidated by 1D and 2D NMR spectroscopy and HRMS. Compounds 6, 8, 18 and 20 exhibited strong cytotoxicity against A549 tumor cell lines, with IC50 values of 2.34, 1.63, 8.39 and 5.39μM, respectively. Seven compounds (3, 9, 10, 12, 18-20) exhibited moderate cytotoxicity against A549, HT29, Hela or L1210 tumor cell lines. Copyright © 2014. Published by Elsevier B.V.
    Fitoterapia 12/2014; DOI:10.1016/j.fitote.2014.12.005 · 2.23 Impact Factor
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    ABSTRACT: The aim of the present study was to investigate and compare the anti‑inflammatory activities of curcumin and its three metabolites, tetrahydrocurcumin, hexahydrocurcumin and octahydrocurcumin in lipopolysaccharide (LPS)‑stimulated RAW 264.7 macrophage cells. The results demonstrated that overproduction of nitric oxide (NO) was potently inhibited following treatment with curcumin and its three metabolites. In addition, curcumin and tetrahydrocurcumin significantly inhibited the release of prominent cytokines, including tumor necrosis factor‑α (TNF‑α) and interleukin‑6 (IL‑6); however, hexahydrocurcumin and octahydrocurcumin did not significantly alter cytokine release. Furthermore, the present study investigated the effect of curcumin and its metabolites on the expression of inducible NO synthase (iNOS), cyclooxygenase‑2 (COX‑2) and activated‑nuclear factor kappa B (NF‑κB); the results showed that curcumin and its three metabolites significantly inhibited LPS‑mediated upregulation of iNOS and COX‑2 as well as NF‑κB activation. However, curcumin exerted a more potent effect on LPS‑stimulated RAW 264.7 cells compared to that of its three metabolites, of which tetrahydrocurcuim was found to be the most pharmacologically active. In conclusion, the results of the present study demonstrated that curcumin and its major metabolites inhibited the LPS‑induced inflammatory response via the mechanism of inhibiting NF‑κB translocation to the nucleus.
    Molecular Medicine Reports 12/2014; DOI:10.3892/mmr.2014.3079 · 1.48 Impact Factor
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    ABSTRACT: The aim of the present study was to investigate the expression and effect of progranulin (PGRN) in patients with primary Sjögren's syndrome (pSS). In total, 26 newly diagnosed pSS patients and 26 healthy subjects were enrolled in this study. The serum levels of PGRN and the inflammatory factor, interleukin-6 (IL-6), were detected using ELISA. In addition, the mRNA expression levels of these molecules were detected by quantitative polymerase chain reaction. The serum levels of PGRN and IL-6 in the pSS patients increased significantly compared with the healthy controls (P<0.05). During the remission stages, the levels of PGRN and IL-6 were comparable to those of the healthy controls. The serum level of PGRN in the pSS patients was shown to correlate with that of IL-6 in the pre-treatment and post-treatment stages. PGRN was upregulated in the pSS patients, indicating a possible role of PGRN in the pathogenesis and development of pSS.
    Experimental and therapeutic medicine 11/2014; 8(5):1643-1647. DOI:10.3892/etm.2014.1981 · 0.94 Impact Factor
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    ABSTRACT: Reinvestigation of the n-BuOH extract of the roots of Clematis argentilucida led to the isolation of a new ursane-type triterpenoid saponin 1 and a new taraxerane-type saporiin 2, four known saponins 3-6 first isolated from the species, together with seven saponins 7-13 reported in the previous papers. The structures of saponins 1-6 were elucidated by extensive spectroscopic analysis and chemical evidences. The ursane-type and taraxerane-type triterpenoid saponins were obtained from genus Clematis for the first time, and the aglycone of saponin 1, 3 beta,28-dihydroxy-18 alpha H-ursan-20-en was first encountered. The cytotoxicity of all the saponins was evaluated against human glioblastoma U251MG cell lines. The monodesmosidic saponins 1, 2 and 4-8 exhibited cytotoxic activity against the cells with IC50 values ranging from 6.95 to 38.51 mu M. (c) 2014 Elsevier B.V. All rights reserved.
    Biochemical Systematics and Ecology 09/2014; 40:49–52. DOI:10.1016/j.bse.2011.09.010 · 1.17 Impact Factor
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    ABSTRACT: A selective and sensitive LC–MS/MS method was developed and validated for simultaneous determination of three glucuronide conjugates of scutellarein in rat plasma. Plasma samples were pretreated by protein precipitation with acetonitrile. The analytes (scutellarin, scutellarein-6,7-di-O-β-D-glucuronide and scutellarein-6-O-β-D- glucuronide), together with internal standard (IS, baicalin) were separated on a Diamonsil C18 column (150 mm × 4.6 mm, 5 μm) with an isocratic mobile phase consisting of methanol–water − formic acid (55:45:0.2, v/v/v). Mass spectrometric detection was performed by selected reaction monitoring (SRM) mode via electrospray ionization source operating in negative ionization mode. The method was linear for all the analytes over the investigated concentration ranges with correlation coefficients greater than 0.9954. The intra- and inter-day precisions were less than 9.1% and the accuracy was between–1.7% and 4.2%. The extraction recoveries of the analytes and IS from rat plasma were over 63.7%. The validated method has been successfully applied to a pharmacokinetic study of breviscapine in rats after intragastric administration at a dose of 20 mg/kg. The pharmacokinetic results would be helpful to better understand the pharmacological action mechanism of breviscapine
    Journal of Chromatography B 08/2014; 965. DOI:10.1016/j.jchromb.2014.06.013 · 2.69 Impact Factor
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    ABSTRACT: Eight eudesmane-type sesquiterpenes – phaeusmanes A–H (1–8) – isolated for the first time in this work, and four others (9–12) isolated for the first time from plants in this work, together with fourteen known eudesmane derivatives, were isolated from the rhizomes of Curcuma phaeocaulis. Their structures were elucidated by 1D and 2D NMR and CD spectroscopy and HRMS. Compound 8 is the first example of a nitrogen-containing eudesmane-type sesquiterpene isolated from the genus Curcuma. Furthermore, inhibitory effects of the isolated compounds on NO production in lipopolysaccharide-activated macrophages were evaluated. Compounds 1, 6, 10, 19, 22, and 24 showed strong inhibitory activities on NO production with IC50 values of 3.2, 4.8, 1.2, 0.8, 3.8, and 0.8 μM, respectively. Preliminary structure–activity relationships for these compounds are proposed. A possible biogenetic pathway for nitrogen-containing eudesmane-type sesquiterpene 8 is postulated.
    European Journal of Organic Chemistry 07/2014; 2014(25). DOI:10.1002/ejoc.201402465 · 3.15 Impact Factor
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    ABSTRACT: The reinvestigation of the n-BuOH extract of the roots of Clematis argentilucida led to the isolation of four new oleanane-type triterpenoid saponins, 1-4, four known saponins, 5-8, first isolated from the species, together with ten saponins, 9-18, reported in the preceding papers. The structures of saponins 1-8 were elucidated by extensive spectroscopic analysis and chemical evidences. The cytotoxicity of all the saponins were evaluated against human tumor HL-60, HepG-2, and SGC-7901 cell lines. The monodesmosidic saponins 4, 7, 8, and 14-18 exhibited cytotoxic activity against the three cell lines with IC50 values in the range of 0.87-19.48 µM.
    Planta Medica 07/2014; 80(11). DOI:10.1055/s-0034-1382838 · 2.34 Impact Factor
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    ABSTRACT: Physalin A is an active withanolide isolated from Physalis alkekengi var. franchetii, a traditional Chinese herbal medicine named Jindenglong, which has been used for the treatment of sore throat, hepatitis, eczema and tumors in China. Our previous study demonstrated that physalin A induced apoptosis and cyto-protective autophagy in A375-S2 human melanoma cells. Induction of reactive oxygen species (ROS) with physalin A triggered apoptosis. In this study, NO generated by physalin A induced apoptosis and autophagy in A375-S2 cells, since physalin A induced the expression of inducible nitric oxide synthase (iNOS) in the cells. Generation of NO partially promoted both apoptosis and autophagy in A375-S2 cells. NO suppressed mTOR expression, which led to autophagy induction. An autophagic inhibitor, 3-methyladenine (3MA) promoted NO production, while acceleration of autophagy with an autophagic agonist rapamycin repressed NO production, suggesting that autophagy and NO production form a negative feedback loop that eventually protects the cells from apoptosis. The results together with the previous study indicate apoptosis and autophagy induced by physalin A in A375-S2 cells; the autophagy, repressing production of reactive nitrogen species (RNS) and ROS, protects the cells from apoptosis.
    Food and Chemical Toxicology 06/2014; 71. DOI:10.1016/j.fct.2014.06.007 · 2.61 Impact Factor
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    ABSTRACT: One new monoterpenoid glycoside (1), together with seven known compounds, including two alkaloids (2–3), three phenylpropanoids (4–6), and two nucleosides (7–8) were isolated from the calyces of Physalis alkekengi var. franchetii. Their structures were elucidated by a combination of detailed spectroscopic analyses, chemical methods, and comparison with reported data. These eight compounds were isolated for the first time from the genus Physalis. The chemotaxonomic significance of these compounds was summarized.
    Biochemical Systematics and Ecology 06/2014; 54:31–35. DOI:10.1016/j.bse.2013.12.030 · 1.17 Impact Factor
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    ABSTRACT: Three rare indole-2-S-glycosides, indole-3-acetonitrile-2-S-β-D-glucopyranoside (1), indole-3-acetonitrile-4-methoxy-2-S-β-D-glucopyranoside (2) and N-methoxy-indole-3-acetonitrile-2-S-β-D-glucopyranoside (3), together with 11 known indole alkaloids were isolated from the roots of Isatis indigotica Fort. (Cruciferae). The structures of 1-3 were elucidated on the basis of mass spectrometry and extensive 1D and 2D NMR spectroscopy. All of the isolated compounds were tested for inhibitory activity against LPS-induced nitric oxide production in RAW 264.7 macrophages. A plausible biosynthesis pathway of 1-3 is also proposed.
    Fitoterapia 06/2014; 95. DOI:10.1016/j.fitote.2014.03.019 · 2.23 Impact Factor
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    ABSTRACT: The present phytochemical investigations of Isatis indigotica Fort. resulted in the isolation of seven lignans (1-7), three aromatic glycosides (8-10), three nucleosides (11-13) and two bis-indole alkaloids (14-15). Among them, compounds 5, 6 and 9 were obtained from this genus for the first time. The chemotaxonomic importance of these compounds was also summarized.
    Biochemical Systematics and Ecology 06/2014; 54:313-315. DOI:10.1016/j.bse.2014.03.004 · 1.17 Impact Factor
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    ABSTRACT: Curcumin (CUR) is a major naturally-occurring polyphenol of Curcuma species, which is commonly used as a yellow coloring and flavoring agent in foods. In recent years, it has been reported that CUR exhibits significant anti-tumor activity in vivo. However, the pharmacokinetic features of CUR have indicated poor oral bioavailability, which may be related to its extensive metabolism. The CUR metabolites might be responsible for the antitumor pharmacological effects in vivo. Tetrahydrocurcumin (THC) is one of the major metabolites of CUR. In the present study, we examined the efficacy and associated mechanism of action of THC in human breast cancer MCF-7 cells for the first time. Here, THC exhibited significant cell growth inhibition by inducing MCF-7 cells to undergo mitochondrial apoptosis and G2/M arrest. Moreover, co-treatment of MCF-7 cells with THC and p38 MAPK inhibitor, SB203580, effectively reversed the dissipation in mitochondrial membrane potential (Δψm), and blocked THC-mediated Bax up-regulation, Bcl-2 down-regulation, caspase-3 activation as well as p21 up-regulation, suggesting p38 MAPK might mediate THC-induced apoptosis and G2/M arrest. Taken together, these results indicate THC might be an active antitumor form of CUR in vivo, and it might be selected as a potentially effective agent for treatment of human breast cancer.
    Food and chemical toxicology: an international journal published for the British Industrial Biological Research Association 03/2014; DOI:10.1016/j.fct.2014.02.024 · 2.99 Impact Factor
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    ABSTRACT: Herba Agrimoniae is a traditional Chinese medicine. To date, there is no quantitative control method for Agrimonia pilosa (A. pilosa) with main active constituent contents listed in the Chinese Pharmacopeia. A high performance liquid chromatography coupled with diode-array detection and electrospray ionization tandem mass spectrometry (HPLC-DAD-ESI-MS/MS) method is established for the characterization and simultaneous quantification of nine major constituents in A. pilosa. Furthermore, the contents of these constituents of A. pilosa from 21 different regions of China were analyzed and compared. All calibration curves show good linearity (r ≥ 0.999). The HPLC-DAD method shows good precision, repeatability and stability for the quantification of the nine constituents in A. pilosa with the standard deviations below 3.29%. The recoveries for the quantified constituents are within the range of 95.44-102.55%. The qualitative and quantitative method was proved to be sensitive, accurate and reliable to determine the constituents in A. pilosa. The method is successfully applied to differentiate the A. pilosa of different regions.
    Analytical methods 01/2014; 6(12):4373. DOI:10.1039/c4ay00042k · 1.94 Impact Factor
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    ABSTRACT: Berberine (BBR) is an isoquinoline alkaloid isolated from several Chinese herbal medicines, such as Coptis chinensis, Berberis aristata, and Coptis japonica. It exhibits a lipid-lowering effect by up-regulating hepatic low density lipoprotein receptor (LDLR) expression. However, the plasma concentration of BBR is very low after oral administration for the reason that BBR is poorly absorbed and rapidly metabolized. Therefore, it is hard to explain the pharmacological effects of BBR in vivo. Here, RT-PCR, Western blotting and Oil Red O staining were used to investigate the effects of four BBR metabolites on LDLR expression and lipid accumulation in human hepatoma Hep G2 cells. Our results suggested that BBR increased LDLR mRNA and protein levels in a time- and dose-dependent manner. Four metabolites of BBR, Jatrorrhizin, Columbamine, Berberubine and Demethyleneberberine, were found to be able to up-regulate LDLR mRNA and protein expression. Moreover, almost all the metabolites had potent effects on inhibiting cellular lipid accumulation. These results suggest that both BBR and its metabolites exhibit lipid-lowering effects by up-regulating LDLR expression, and BBR and its metabolites might be the in vivo active forms of BBR produced after oral administration. This study provides information to help us understand the mechanisms underlying the hypolipidemic effects of BBR in vivo.
    Fitoterapia 12/2013; 92. DOI:10.1016/j.fitote.2013.11.010 · 2.23 Impact Factor
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    ABSTRACT: A new flavonoid, 7,8-dimethoxy-2'-hydroxy-5-O-β-d-glucopyranosyloxyflavone (1), along with 15 known flavonoids (2-16), was isolated from the aerial parts of Andrographis paniculata Nees. Their structures were elucidated on the basis of chemical and spectroscopic analyses. Most of them have uncommon O-substitution patterns involving 5-, 7-, 8-, 2'-, 3'-, 4'- and 5'-O-substituents. The antiproliferative effects of these flavonoids against human leukaemia HL-60 cells were investigated. Among them, 13 was the most active, displaying potent antiproliferative activity with IC50 of 3.50 μM. The structure-activity relationships of these isolated compounds were discussed.
    Natural product research 11/2013; 28(3). DOI:10.1080/14786419.2013.856907 · 1.23 Impact Factor
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    ABSTRACT: The aim of this study is to investigate the expression of apolipoprotein E (apoE) and the relationship between apoE and disease activity of SLE, and the possible effects of glucocorticoid on apoE and other cytokines activities in SLE patients METHODS: Forty treatment-naive SLE patients and forty matched healthy controls were studied. All the SLE patients received prednisone 1 mg/kg/day for 28 consecutive days. The sera levels of apoE and related cytokines were evaluated by ELISA. The expression of apoE mRNA in peripheral blood mononuclear cells (PBMCs) were determined by real-time PCR. Compared with healthy controls, the relative expression levels of ApoE proteins and sera levels were significantly up-regulated in active SLE patients. ApoE sera concentrations positively correlated with SLEDAI, anti-dsDNA antibody and the related cytokines including IL-6, IFN-gamma and IL-10, and uncorrelated with the concentration of total cholesterol (TC) and triglyceride (TG) in SLE patients. After 4 weeks prednisone treatment, the relative mRNA expression of apoE and the serum levels of apoE and related cytokines decreased. ApoE correlated with disease activity and related cytokines in SLE patients. Glucocorticoid can down-regulate the expressions of apoE and related cytokines.Virtual slide: virtual slide(s) for this article can be found here:http://www.diagnosticpathology.diagnomx.eu/vs/1646714011077325.
    Diagnostic Pathology 10/2013; 8(1):175. DOI:10.1186/1746-1596-8-175 · 2.41 Impact Factor
  • Biochemical Systematics and Ecology 10/2013; 50:435-437. DOI:10.1016/j.bse.2013.06.012 · 1.17 Impact Factor
  • Kun Wang, Feng Qiu
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    ABSTRACT: Curcuminoids are safe natural yellow pigments used as food coloring agents and traditional drugs with a variety of biological functions such as antitumor, anti-inflammatory and antioxidant activities. Poor oral bioavailability and the low plasma concentration of curcuminoids limited their clinical use, and one of the major reasons is their rapid metabolism in vivo. The predominant metabolic pathways are reduction and conjugation, and some drug metabolizing enzymes such as alcohol dehydrogenase, UDP glucuronosyltransferases (UGTs) or sulfotransferases (SULTs) involved in the metabolic reactions. Besides the major metabolic pathways, dehydroxylation, cyclization and methylation can also occur in vivo. In addition, more than thirty metabolites of curcuminoids have been identified in biological matrices including the plasma, urine and bile from rats or humans by LC-MS/MS analysis and other methods. Some metabolites such as tetrahydro-curcuminoids have been reported to be active, which may explain how and why curcuminoids with poor oral bioavailability display their effectiveness in vivo. The present review mainly summarizes curcuminoid metabolism and its contribution to the pharmacological effects.
    Current Drug Metabolism 08/2013; DOI:10.2174/13892002113149990102 · 3.49 Impact Factor
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    ABSTRACT: Rhizoma Coptidis (Huanglian in Chinese) is commonly used in Chinese folk medicine to treat diarrhea, diabetes, hypertension, hyperlipidemia and tumours. This herb has increasingly gained attention because of its use as a hypolipidemic herb. Berberine (BBR) is the most important constituent of Rhizoma Coptidis that contribute to the pharmacological efficacy of the herb. Pharmacokinetic studies have indicated that BBR has poor oral bioavailability. Interestingly, several reports show that absorbed BBR is extensively metabolized in rats and humans. We speculate that the BBR metabolites might be responsible for the pharmacological effects. The aim of this study is to examine BBR metabolites for their triglyceride (TG)-lowering activities and the molecular mechanism to clarify BBR genuine effective forms in vivo. Four BBR metabolites were examined their TG-lowering effects with a commercial triglyceride assay kit. Real-time PCR and Western blotting were used to confirm genes and proteins of interest, respectively. Among those BBR metabolites, M2 exhibited the more potential effects on TG-lowering and AMP-activated protein kinase (AMPK) activation in Hep G2 cells as compared with BBR. Moreover, BBR and M2 inhibited gene expressions of acetyl-CoA carboxylase (ACC), fatty acid synthase (FAS), glycerol-3-phosphate acyltransferase (GPAT) and 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR), but motivated gene expression of medium chain acyl-CoA dehydrogenase (mCAD) significantly. The results suggested that the TG-lowering effects of BBR and M2 might be partially mediated by the up-regulation of lipolysis gene expressions and down-regulation of lipogenesis gene expressions through activation of the AMPK signaling pathway. BBR and its metabolites might be in vivo active forms of oral doses of BBR, and M2 might be a promising drug candidate against hyperlipidemia.
    Journal of ethnopharmacology 07/2013; DOI:10.1016/j.jep.2013.07.025 · 2.32 Impact Factor

Publication Stats

999 Citations
246.10 Total Impact Points


  • 1998–2015
    • Shenyang Pharmaceutical University
      • • School of Traditional Chinese Medicines
      • • School of Traditional Chinese Materia Medica
      • • Department of Natural Products Chemistry
      Feng-t’ien, Liaoning, China
  • 2014
    • Tianjin University of Traditional Chinese Medicine
      T’ien-ching-shih, Tianjin Shi, China
  • 2012–2014
    • Shandong University
      Chi-nan-shih, Shandong Sheng, China
  • 2013
    • University of Jinan (Jinan, China)
      Chi-nan-shih, Shandong Sheng, China
  • 2011
    • National Institutes of Health
      • Branch of Radiation Oncology
      Bethesda, MD, United States