Xin-Hua Lu

Hebei Normal University, Chentow, Hebei, China

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Publications (11)17.49 Total impact

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    ABSTRACT: Protein tyrosine phosphatase 1B (PTP1B) is implicated as a negative regulator of insulin receptor (IR) signaling and a potential drug target for the treatment of type II diabetes and other associated metabolic syndromes. Therefore, small molecular inhibitors of PTP1B can be considered as an attractive approach for the design of new therapeutic agents of type II diabetes diseases. In a continuing search for new protein phosphatase inhibitors from fungi, we have isolated a new compound, named penostatin J (1), together with three known ones, penostatin C (2), penostatin A (3), and penostatin B (4), from cultures of the entomogenous fungus Isaria tenuipes. The structure of penostatin J (1) was elucidated by extensive spectroscopic analysis. We also demonstrate for the first time that penostatin derivatives exhibit the best PTP1B inhibitory action. These findings suggest that penostatin derivatives are a potential novel kind of PTP1B inhibitors.
    Molecules 01/2014; 19(2):1663-1671. · 2.43 Impact Factor
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    ABSTRACT: Eighteen polyketides (1-18) including six citrinin derivatives, two phenol derivatives, one cyclopentenone, two naphthol derivatives, and seven tetralone derivatives were isolated from the culture broth of a marine-derived fungal strain Xylariaceae sp. SCSGAF0086. Five of these compounds (1, 2, 8, 9, and 10) were new, and their structures were determined by spectroscopic methods. Compounds 4, 6, 7, and 17 showed enzyme-inhibitory activities towards several tested enzymes, and 6 and 7 showed strong antifouling activity against Bugula neritina larvae settlement. This is the first time that the antifouling and enzyme-inhibitory activities of these compounds has been reported.
    Marine Drugs 01/2013; 11(5):1718-1727. · 3.98 Impact Factor
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    ABSTRACT: To study the chemical constituents of Bauhinia glauca subsp. pernervosa, eleven phenolic acids were isolated from a 95% ethanol extract by using a combination of various chromatographic techniques including column chromatography over silica gel, ODS, MCI, Sephadex LH-20, and semi-preparative HPLC. By spectroscopic techniques including 1H NMR, 13C NMR, 2D NMR, and HR-ESI-MS, these compounds were identified as isopropyl O-beta-(6'-O-galloyl)-glucopyranoside (1), ethyl O-beta-(6'-O-galloyl)-glucopyranoside (2), 3, 4, 5-trimethoxyphenyl-(6'-O-galloyl)-O-beta-D-glucopyranoside (3), 3, 4, 5-trimethoxyphenyl-beta-D-glucopyranoside (4), gallic acid (5), methyl gallate (6), ethyl gallate (7), protocatechuic acid (8), 3, 5-dimethoxy-4-hydroxybenzoic acid (9), erigeside C (10) and glucosyringic acid (11). Among them, compound 1 is a new polyhydroxyl compound; compounds 2, 10, and 11 were isolated from the genus Bauhinia for the first time, and the other compounds were isolated from the plant for the first time. Compounds 6 and 8 showed significant protein tyrosine phosphatase1B (PTP1B) inhibitory activity in vitro with the IC50 values of 72.3 and 54.1 micromol x L(-1), respectively.
    Yao xue xue bao = Acta pharmaceutica Sinica 08/2011; 46(8):946-50.
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    ABSTRACT: Mycophenolic acid (MPA) has been known for decades to be an anticancer and immunosuppressive agent and has significant anticancer properties, but its underlying molecular mechanisms are poorly characterized. Peroxisome proliferator-activated receptor gamma (PPARγ) has a central role in adipocyte differentiation, and MPA has been shown to be a potent PPARγ agonist. Whether PPARγ activation has a putative role in the anticancer efficacy of MPA via induction of adipocyte-like differentiation has not been elucidated. In the present study, MPA was demonstrated to dose-dependently activate PPARγ transcription in the GAL4-hPPARγ (LBD) chimeric receptor assay and PPRE-luc reporter gene assay with an EC(50) of 5.2-9.3 μM. Treatment of the breast cancer cell lines MDA-MB-231 and MCF-7 with MPA resulted in differentiation of adipose tissue that was characterized by accumulation of intracellular lipids, enlargement of cell volume, and permanent withdrawal from the cell cycle at the G1/G0 stage. At a molecular level, the expression of three adipocyte differentiation markers (PPARγ, adipsin D, and aP2) was remarkably induced in differentiated breast cancer cells. However, RNA interference experiments showed that PPARγ-knockdown cannot completely reverse the differentiated state of MDA-MB-231 cells after MPA treatment. These data suggest that the effects of MPA on adipocyte-like terminal differentiation of breast cancer cells are (at least in part) due to PPARγ activation, which is a novel anticancer mechanism of MPA.
    European journal of pharmacology 02/2011; 658(1):1-8. · 2.59 Impact Factor
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    ABSTRACT: Four novel oxepin-containing pyrimidines, namely oxepinamides D–G (1–4), were isolated from cultures of Aspergillus puniceus F02Z-1744. The structures of 1–4 were elucidated by analyzing their spectroscopic data generated by 1D and 2D NMR and MS methods. The configurations of 1 and 2 were established based on single-crystal X-ray crystallographic analysis. All four compounds 1–4 showed transcriptional activation on Liver X Receptor α (LXRα) with EC50 values of 10.6, 12.8, 13.6, and 12.1 μM, respectively.
    European Journal of Organic Chemistry 12/2010; 2011(4):802-807. · 3.34 Impact Factor
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    ABSTRACT: Nuclear receptors are a superfamily of ligand-activated transcription factors that play key roles in many biological processes, and have become one class of the most important targets in drug discovery. Mammalian one-hybrid system has been used to develop a cell-based functional transactivation high-throughput screening (HTS) assay for detecting nuclear receptors ligands. In the present study, we proved that different promoters used in the reporter vector had significant different impacts on the performance of HTS assays. The assay using the SV40 promoter in the reporter vector showed the characteristics of much higher signal/noise ratios, acceptable Z' factors (>0.6), low coefficient variation (<12.5%) and higher hits rate, which could be more robust, reproducible, and sensitive. In contrast, utilizing a TATA box promoter in the assay resulted in higher variance and low sensitivity. In addition, it was found that the assay using SV40 had longer signal decay time and was easier to be miniaturized in 384-well format. It has been confirmed that the choice of a promoter is a critical factor in developing a reporter gene HTS assay. However, the SV40 promoter used in the present study has been shown to be more adaptable than the minimal promoter TATA box in the Mammalian one-hybrid HTS assays for detecting nuclear receptor agonists.
    Analytical and Bioanalytical Chemistry 03/2010; 396(5):1721-30. · 3.66 Impact Factor
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    ABSTRACT: To study the chemical constituents of Angelica sinensis. The constituents were separated by chromatographic methods, and their structures were identified on the basis of spectroscopic analysis. Eight compounds were isolated and identified as levistolide A (1), senkyunolide O (2), (3Z, 3Z')-6.8', 7.3'-diligustilide (3), tokinolide B (4), isotokinolide B (5), (3'Z)-(3R, 8S, 3a'R, 6'S)-3, 3a': 8, 6'-biligustilide (6), E, E'-3. 3', 8. 8'-diligustilide (7) and E, E'-3. 3', 8. 8'-isodiligustilide (8), which are all diligustilides. Compound 7 was obtained from the plant for the first time; compounds 6 and 8 are new compounds.
    Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 11/2008; 33(19):2196-201.
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    ABSTRACT: Human leukocyte elastase is an important selection target of inflammation and cancer. In this paper, a high throughput screening model was established for screening human leukocyte elastase inhibitors from thousands of strains of actinomycetes. As a result, a strain, N01WA-735 with potent suppression activity was isolated. Firstly, the strain N01WA-735 was identified as Streptomyces according to morphology and biochemical analysis. The Streptomyces N01WA-735 was processed by solvent extraction, silica column chromatography, Sephadex LH-20 column chromatography and crystallization to get a pure active compound named N01WA-735E. Its chemical structure was elucidated as the same as that of the compound named BE-52440A by physicochemical properties and spectral data of UV, MS, 1H-NMR and 13C-NMR respectively. The compound showed a strong inhibitory activity against human leukocyte elastase with IC50 of 3.02 micromol/L. The compound is reported as a human leukocyte elastase inhibitor for the first time.
    Sheng wu gong cheng xue bao = Chinese journal of biotechnology 12/2007; 23(6):1112-5.
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    ABSTRACT: A high throughput screening was carried out in order to search for inhibitors of acetylcholinesterase (AChE) from microorganism metabolites. An actinomycete strain was found to produce active compounds named N98-1272 A, B and C with IC50 of 15.0, 11.5, 12.5 microM, respectively. Structural studies revealed that the three compounds are identical to the known antibiotics, Manumycin C, B and A. Kinetic analyses showed that N98-1272 C (Manumycin A) acted as a reversible noncompetitive inhibitor of acetylcholinesterase, with a Ki value of 7.2 microM. The cyclohexenone epoxide part of the structure plays a crucial role in the inhibitory activity against AChE. Compared with Tacrine, N98-1272 A, B, and C exhibit much better selectivity toward AChE over BuChE.
    Journal of Enzyme Inhibition and Medicinal Chemistry 03/2007; 22(1):43-9. · 1.50 Impact Factor
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    ABSTRACT: To investigate the chemical constituents of Potentilla multifida. Various chromatographic techniques were employed for isolation and purification of the constituents. The structures were elucidated by spectral analysis. Four megastigmane glycosides were isolated from P. multifida and their structures were identified as citroside A (1), icariside B1 (2), (6S,7E,9R)-roseoside (3), (6S,7E,9R)-vomifoliol-9-O-beta-D-xylopyranosyl-(1-->6)-O-beta-D-glucopyranoside (4), respectively. All compounds were obtained from the genus Potentilla for the first time.
    Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 08/2005; 30(13):983-6.
  • Xin-hua Lu, Hong Liang, Yu-ying Zhao
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    ABSTRACT: To find out substance basis of pharmacological activities of Angelica sinensis. Chromatographic methods were used to isolate the chemical components, and spectroscopic methods were used to identify their structures. Five compounds were isolated from the ethanol extract of the roots of Angelica sinensis. Their structures were identified as: (Z)-ligustilide, (Z)-6,7-epoxyligustilide, (Z)-6,7-cis-dihydroxyligustilide, (E)-6,7-cis-dihydroxy-ligustilide and 11-angeloylsenkyunolide F. 11-angeloylsenkyunolide F was obtained from Angelica sinensis for the first time.
    Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 06/2003; 28(5):423-5.

Publication Stats

21 Citations
17.49 Total Impact Points

Institutions

  • 2010–2011
    • Hebei Normal University
      Chentow, Hebei, China
    • Hebei Medical University
      Chentow, Hebei, China
  • 2005–2011
    • Peking University
      • School of Pharmaceutical Sciences
      Beijing, Beijing Shi, China
  • 2008
    • Peking University Health Science Center
      Peping, Beijing, China
  • 2007
    • Peking Union Medical College Hospital
      Peping, Beijing, China