Hai-Ning Lv

Peking University, Peping, Beijing, China

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Publications (18)53.53 Total impact

  • [Show abstract] [Hide abstract]
    ABSTRACT: Coumarin and its derivatives are fragrant natural compounds isolated from the genus Murraya that are flowering plants widely distributed in East Asia, Australia and the Pacific Islands. Murraya plants have been widely used as medicinal herbs for relief of pains such as headache, rheumatic pain, toothache and snake bites. However, little is known about their analgesic components and the molecular mechanism underlying pain relief. Here, we report the bioassay-guided fractionation and identification of a novel coumarin derivative, named muralatin L, that can specifically activate the nociceptor transient receptor potential vanilloid 1 (TRPV1) channel and reverse the inflammatory pain in mice through channel desensitization. Muralatin L was identified from active extract of M. alata against TRPV1 transiently expressed in HEK-293T cells in fluorescent calcium FlexStation assay. Activation of TRPV1 current by muralatin L and its selectivity were further confirmed by whole-cell patch clamp recordings of TRPV1 expressing HEK-293T cells and dorsal root ganglion neurons isolated from mice. Furthermore, muralatin L could reverse inflammatory pain induced by formalin and acetic acid in mice, but not in TRPV1 knockout mice. Taken together, our findings show that muralatin L specifically activates TRPV1 and reverses inflammatory pain, thus highlighting the potential of coumarin derivatives from Murraya plants for pharmaceutical and medicinal applications such as pain therapy.
    Journal of Biological Chemistry 10/2015; DOI:10.1074/jbc.M115.654392 · 4.57 Impact Factor
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    ABSTRACT: This work aims to evaluate the anti-neuroinflammatory effects of natural sesquiterpene dimer caruifolin D from Artemisia absinthium L., which is an edible vegetable or traditional medicinal food in East Asia due to its sedation, anti-asthma and antipruritic effects. In this study, we reported that caruifolin D significantly inhibited the productions of various neuroinflammatory mediators from microglia in response to bacterial lipopolysaccharide stimulation. Moreover, anti-inflammatory mechanism study showed that caruifolin D markedly suppressed the production of intracellular reactive oxygen species, which was an important player involved in neuroinflammation, leading to inhibitory effects on the activations of protein kinase C (PKC) and c-Jun N-terminal kinase (JNK), which were two major neuroinflammatory signaling pathways in the brains. Furthermore, caruifolin D protected neurons against microglia-mediated neuronal inflammatory damages by up-regulating neuronal viability and maintaining healthy neuronal morphology. Taken together, these results expanded our knowledge about the anti-neuroinflammatory and neuroprotective mechanism of Artemisia absinthium L., and also suggested that caruifolin D was a major anti-inflammatory component from Artemisia absinthium L., which might be developed as a drug candidate for neuroinflammation-related diseases.
    European journal of pharmacology 10/2015; DOI:10.1016/j.ejphar.2015.10.011 · 2.53 Impact Factor
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    ABSTRACT: TNF receptor-associated factor 6 (TRAF6) is a key hub protein involved in Toll-like receptor-dependent inflammatory signaling pathway, and it recruits additional proteins to form multiprotein complexes capable of activating downstream NF-ΰ B inflammatory signaling pathway. Ubiquitin-proteasome system (UPS) plays a crucial role in various protein degradations, such as TRAF6, leading to inhibitory effects on inflammatory response and immunologic function. However, whether ubiquitination-dependent TRAF6 degradation can be used as a novel anti-inflammatory drug target still remains to be explored. FMHM, a bioactive natural small molecule compound extracted from Chinese herbal medicine Radix Polygalae, suppressed acute inflammatory response by targeting ubiquitin protein and inducing UPS-dependent TRAF6 degradation mechanism. It was found that FMHM targeted ubiquitin protein via Lys48 site directly induced Lys48 residue-linked polyubiquitination. This promoted Lys48 residue-linked polyubiquitin chain formation on TRAF6, resulting in increased TRAF6 degradation via UPS and inactivation of downstream NF-ΰ B inflammatory pathway. Consequently, FMHM down-regulated inflammatory mediator levels in circulation, protected multiple organs against inflammatory injury in vivo, and prolong the survival of endotoxemia mouse models. Therefore, FMHM can serve as a novel lead compound for the development of TRAF6 scavenging agent via ubiquitination-dependent mode, which represents a promising strategy for treating inflammatory diseases.
    Scientific Reports 10/2015; 5:14715. DOI:10.1038/srep14715 · 5.58 Impact Factor
  • Hai-Ning Lv · Ran Wen · Ying Zhou · Ke-Wu Zeng · Jun Li · Xiao-Yu Guo · Peng-Fei Tu · Yong Jiang ·
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    ABSTRACT: Two new structurally unique trimeric carbazole alkaloids, murratrines A and B (1, 2), and 11 new carbazole dimers, murradines A-K (3-13), and four known analogues (14-17) were isolated from the leaves and stems of Murraya tetramera. The structures and relative configurations of 1-13 were elucidated on the basis of comprehensive 1D and 2D NMR spectroscopy, high-resolution mass spectrometry, and electronic circular dichroism (ECD) data analysis. Murratrines A and B (1, 2) both contain an unprecedented carbazole trimeric skeleton, and murradines A and D (3, 6) are the first natural C-1-C-3'-methyl-linked and C-6-C-3'-methyl-linked dimeric carbazole alkaloids, respectively. Compounds 4, 10, 14, 15, and 17 exhibited inhibition of nitric oxide production stimulated by lipopolysaccharide in BV-2 microglial cells with IC50 values in the range of 11.2-19.3 μM.
    Journal of Natural Products 09/2015; DOI:10.1021/acs.jnatprod.5b00527 · 3.80 Impact Factor
  • Hai-ning Lv · Guang-zhi Ding · Yun-bao Liu · Jing Qu ·
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    ABSTRACT: Endophytic fungi Penicillium dangeardii, isolated from Lysidice rhodostegia Hance root, was fermented and the secondary metabolites were studied. By means of Sephadex LH-20 column chromatography, ODS column chromatography and PHPLC over the fermented culture, 5 compounds were isolated. By using ESI-MS and NMR, the structures of the compounds were determined as N-[9-(β- D-ribofuranosyl)-9H-purin-6-yl]-L-aspartic acid (1), 3-caffeoylquinic acid (2), 4-caffeoylquinic acid (3), and 5-caffeoylquinic acid (4), 3-hydroxy-benzoic acid-4-O-β-D-glucopyranoside (5).
    Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 05/2015; 40(9):1759-61. DOI:10.4268/cjcmm20150925
  • Fang Xia · Hai-ning Lv · Yong Jiang · Peng-fei Tu ·
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    ABSTRACT: This study is to develop a sensitive method by using reversed-phase high performance liquid chromatography coupled with UV detector (HPLC-UV) to simultaneously determine four bioactive compounds, iriflophenone 3-C-beta-D-glucoside, iriflophenone 3,5-C-beta-D-diglucoside, mangiferin, and iriflophenone 2-O-alpha-L-rhamnoside in the leaves of Aquilaria sinensis. An Agilent Zorbax SB-C, column (4, 6 mm x 250 mm, 5 microm) was used, and the gradient elution was performed with mobile phase of 0.1% aqueous phosphoric acid and acetonitrile at a flow rate of 1 mL x min(-1). The detection wavelength was 280 nm, and the column temperature was 25 degrees C. The four marker compounds were well separated with good linearity (R2 > 0.9990), precision, stability and repeatabili y. The-recovery rates were in the range of 98.80%-101.39%. For 15 branch of the leaves, the contents of iriflophenone 3-C-beta-D-gluoside, iriflophenone 3,5-C-beta-D-diglucoside, mangiferin, and iriflophenone 2-O-alpha-L-rhamnoside were between 0.41-14.48, 0.72-3.85, 4.30-29.07, 0.24-5.06 mg, respectivley. This method is precise, accurate and reliable, which provides an efficient way for the quality control of the leaves of A. sinensis. This will promote the comprehensive usage of this plant.
    Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 04/2015; 40(7):1342-6.
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    ABSTRACT: MC13 is a novel coumarin compound found in Murraya, an economic crop whose leaves are widely used as condiment (curry) in cuisine. The aims of the present study were to investigate the neuroprotective effects of MC13 on microglia-mediated inflammatory injury model as well as potential molecular mechanism. Cell viability and apoptosis assay demonstrated that MC13 was not toxic to neurons and significantly protected neurons from microglia-mediated inflammatory injury upon lipopolysaccharide (LPS) stimulation. Results showed that MC13 markedly inhibited LPS-induced production of various inflammatory mediators, including nitrite oxide (Griess method), TNF-α and IL-6 (ELISA assay) in a concentration-dependent manner. Mechanism study showed that MC13 could suppress the activation of NF-κB, which was the central regulator for inflammatory response, and also decreased the interaction of TGF-β-activated kinase 1 (TAK1)-binding protein (TAB2) with TAK1 and TNF receptor associated factor (TRAF6), leading to the decreased phosphorylation levels of NF-κB upstream regulators such as IκB and IκB kinase (IKK). MC13 also significantly down-regulated the phosphorylation levels of ERK and p38 MAPKs, which played key roles in microglia-mediated inflammatory response. Furthermore, MC13 inhibited Jak2-dependent Stat1/3 signaling pathway activation by blocking Jak2 phosphorylation, Stat1/3 phosphorylation and nuclear translocation. Taken together, our results demonstrated that MC13 protected neurons from microglia-mediated neuroinflammatory injury by inhibiting TRAF6-TAK1-NF-κB, p38/ERK MAPKs and Jak2-Stat1/3 pathways. Finally, MC13 might interact with LPS and interfere LPS-binding to cell membrane surface. These findings suggested that coumarin might act as a potential medicinal agent for treating neuroinflammation as well as inflammation-related neurodegenerative diseases. This article is protected by copyright. All rights reserved
    Journal of Cellular Biochemistry 02/2015; 116(7). DOI:10.1002/jcb.25084 · 3.26 Impact Factor
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    ABSTRACT: Two new rare 8-methylbenzo[h]coumarins, muralatins A and B (1, 2), nine new C-8-substituted coumarins, muralatins C-K (3-11), and 22 known analogues (12-33) were isolated from the leaves of Murraya alata. The absolute configurations of compounds 5, 11, 23, 24, 27, 30, and 33 were assigned via comparison of their specific rotations, by Mosher's method, and by single-crystal X-ray diffraction and electronic circular dichroism (ECD) data of the in situ formed transition metal complexes. A putative biosynthesis pathway to 1 and 2 is proposed, and the chemical synthesis of 1 was accomplished through electrocyclization of 5,7-dimethoxy-8-[(Z)-3-methylbut-1,3-dienyl)]coumarin (12). Compounds 1, 2, 8, 12, and 31 showed inhibition of nitric oxide production in lipopolysaccharide-induced RAW 264.7 macrophages with IC50 values of 6.0-14.5 μM.
    Journal of Natural Products 01/2015; 78(2). DOI:10.1021/np500861u · 3.80 Impact Factor
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    ABSTRACT: Nine new prenylbisabolane diterpenoids, claoxylones A-I (1-9), were isolated from the branches and leaves of Claoxylon polot. This is the first example of prenylbisabolane diterpenoids with furan and tetrahydrofuran rings. Their structures and relative configurations were established by spectroscopic and conformational analysis, and the absolute configurations were determined by single-crystal X-ray diffraction and electronic circular dichroism (ECD) analysis. Compounds 1-9 exhibited antiviral activity against Coxsackie B3 virus, with IC50 values of 6.0-33.3 mu M.
    Tetrahedron 10/2014; 70(41):7476–7483. DOI:10.1016/j.tet.2014.08.021 · 2.64 Impact Factor
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    ABSTRACT: Ten compounds, including seven sesquiterpenes, two phenols and one phenylpropanoid, were isolated from the roots of Illicium majus by means of silica gel, ODS, Sephadex LH-20, and preparative HPLC. On analysis of MS and NMR spectroscopic data , their structures were established as cycloparviflorolide (1), cycloparvifloralone (2), tashironin (3), tashironin A (4), anislactone A(5), anislactone B (6), pseudomajucin (7), syringaldehyde (8), methyl-4-hydroxy-3, 5-dimethoxybenzoate (9), and (E)-3-methoxy-4,5-methylenedioxycinnamic alchol (10), respectively. Compounds 1-4 and 8-10 were first isolated from this plant. In the in vitro assays, at a concentration of 1.0 x 10(-5) mol x L(-1), compounds 5 and 6 were active against LPS induced NO production in microglia with a inhibition rate of 75.31% and 53.7%, respectively.
    Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 07/2014; 39(14):2689-92. DOI:10.4268/cjcmm20141419
  • Hai-Ning Lv · Xiao-Yu Guo · Peng-Fei Tu · Yong Jiang ·
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    ABSTRACT: Murrayae Folium et Cacumen (MFC) is a traditional Chinese medicine (TCM) derived from the leaves and twigs of two aromatic species of Rutaceae: Murraya paniculata (L.) Jack and M. exotica L. It has long been used as a folk medicine in South China for the treatment of a variety of disorders, particularly for inflammatory lesions and pains. In the present study, a detailed chemical examination as well as a comparative analysis of the essential oil composition of M. paniculata and M. exotica was conducted by gas chromatography-mass spectrometry (GC-MS). A total of 141 volatile components were identified from the essential oil of these two plants. Sesquiterpenes were found to be the predominant constituents, accounting for 92.8% of the oil from M. paniculata and 87.9% of that from M. exotica. A comparative analysis of the essential oil composition of these two plants revealed a high level of similarity in their main constituents, such as the co-occurrence of E-caryophyllene, spathulenol and delta-elemene, which gave the chemical evidence for their equal medicinal application as MFC in TCMs. Moreover, in combination with literature reports, E-caryophyllene was theoretically deduced as one of the pharmacologically effective components of MFC that is responsible for treating inflammatory lesions and for local anaesthesia.
    Natural product communications 10/2013; 8(10):1473-5. · 0.91 Impact Factor
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    ABSTRACT: Five new diterpenoids (1-5), five new sesquiterpenoids (6-10), and three known compounds (11-13) were isolated from the roots of Illicium majus. Their structures were elucidated by extensive spectroscopic analysis. The absolute configuration of 1 was assigned by X-ray crystallography, whereas those of the 1,2-diol moieties in 3 and 4 were determined using Snatzke's method. The abietane acids 1, 2, 11, 12, and 13 displayed antiviral activity against the Coxsackie B3 virus, with IC50 values of 3.3-51.7 μM/mL.
    Journal of Natural Products 09/2013; 76(10). DOI:10.1021/np400638r · 3.80 Impact Factor
  • Ying Ning · Jian Sun · Hai-Ning Lv · Peng-Fei Tu · Yong Jiang ·
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    ABSTRACT: Phytochemical investigation was carried out on the seeds of Vigna umbellata. The 70% ethanol extract of the seeds of V. umbellata was subjected to silica gel, Sephadex LH-20, ODS column chromatographies and preparative HPLC. The structures of the isolated compounds were elucidated on the basis of NMR and ESI-MS spectroscopic data Eight compounds were obtained and identified as carboxyatractyligenin (1), 2beta-O-beta-D-glucopyranosyl-15alpha-hydroxy-kaur-16-ene-18,19-dicarboxylic acid (2), 2beta-O-(beta-D-glucopyranosyl) atractyligenin (3), 3R-O-[beta-L-arabinopyranosyl-(1-6) -beta-D-glucopyranosyl] oct-1-ene-3-ol (4), (6S, 7E, 9R) -roseoside (5), liriodendrin (6), resveratrol (7) and maltol (8). Compounds 1-7 were isolated from Vigna genus for the first time, and compound 8 was isolated from V. umbellata for the first time.
    Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 06/2013; 38(12):1938-41. DOI:10.4268/cjcmm20131219
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    ABSTRACT: Mollolide A (1), a diterpenoid featuring a new 1,10:2,3-disecograyanane skeleton, was isolated from the roots of Rhododendron molle. Its structure was elucidated through extensive MS, IR, and NMR spectroscopy analyses. The absolute configuration was determined by single-crystal X-ray diffraction of its p-bromobenzoate derivative (1b). Compound 1 exhibits a significant analgesic effect at a dose of 20 mg/kg and antiviral activity against the Coxsackie B3 virus with an IC50 value of 27.7 μM.
    Organic Letters 05/2013; 15(12). DOI:10.1021/ol401254e · 6.36 Impact Factor
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    ABSTRACT: Two new alkaloids, lycojaponicumins D (1) and E (2), were isolated from the club moss Lycopodium japonicum. Their structures were elucidated by spectroscopic methods, calculated ECD, CD experiments and X-ray diffraction analysis. Lycojaponicumin D (1) possesses an unprecedented 5/7/6/6 tetracyclic skeleton formed by an unusual C3-C13 linkage, which is first reported in Lycopodium alkaloids. The plausible biogenetic pathway of 1 is proposed.
    Organic Letters 11/2012; 14(22). DOI:10.1021/ol302701y · 6.36 Impact Factor
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    ABSTRACT: Six new cardenolides, periforosides D-E (1-2), periforgenin C (3) and periforosides F-H (4-6), as well as 10 previously identified cardenolides (7-16) were isolated from the ethanol extract of the stems of Periploca forrestii. The structures of the new compounds were determined using extensive spectroscopic analyses including HRESI-MS, 1D and 2D NMR data. Evaluation of the cytotoxic activity of all the isolated compounds in five different human cancer cell lines indicated that compounds 2-6, 8, 9 and 12-16 have potent activity.
    Steroids 12/2011; 77(5):375-81. DOI:10.1016/j.steroids.2011.12.013 · 2.64 Impact Factor
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    ABSTRACT: Phenanthroindolizidine alkaloids are a family of plant-derived compounds with significant antineoplastic activity as well as other effects like antiamebicidal, antiviral, and anti-inflammatory activities. The specific biomolecular targets of these compounds have not yet been clearly identified. S-(+)-Deoxytylophorinidine (CAT) is a new phenanthroindolizidine alkaloid, originally extracted from the roots of Tylophora atrofolliculata and Tylophora ovata. Potent anticancer activity was observed in vitro and in vivo. Neurotoxicity of CAT was also studied and it was far less serious than that of vinblastine. Interactions between this compound and DNA had been studied in detail in our laboratory previously, and we further studied its interactions with RNA.
    Journal of Asian natural products research 05/2011; 13(5):400-8. DOI:10.1080/10286020.2011.566868 · 0.91 Impact Factor
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    ABSTRACT: Three new phloroglucinols, named lysidicins F-H (1-3), were isolated from the roots of Lysidice rhodostegia. These compounds have a unprecedented benzyl benzo[b]furo[3,2-d]furan skeleton, and lysidicin F (1) is the first example of natural product with trans-fused furan rings. Their structures were established on the basis of extensive spectroscopic analysis, and the absolute configurations of them were determined by computational methods. A possible biosynthetic pathway for 1-3 was also postulated.
    Organic Letters 05/2010; 12(10):2390-3. DOI:10.1021/ol100735f · 6.36 Impact Factor

Publication Stats

54 Citations
53.53 Total Impact Points


  • 2015
    • Peking University
      • School of Pharmaceutical Sciences
      Peping, Beijing, China
  • 2010-2014
    • Peking Union Medical College Hospital
      Peping, Beijing, China
  • 2013
    • Peking University Health Science Center
      Peping, Beijing, China
  • 2012-2013
    • Chinese Academy of Medical Sciences
      Peping, Beijing, China