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The authors regret for the changes in Fig. 6 as follow: [Figure presented] Fig. 6. HPLC-ELSD chromatograms of ten Anoectochilus, four Goodyera and one Ludisia species on AQ-C
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Objective: To establish multi-class bioactive constituents’ determination of ten Anoectochilus, four Goodyera and one Ludisia species, and provide reference for the improvement of their quality control. Methods: HPLC-ELSD and phenol–sulphuric acid methods were used for the quantitative determination of lactone glycosides (kinsenoside and its diastereoisomer, goodyeroside A) and polysaccharides, respectively, while an efficient iHPLC–MS/MS method was established for rapid determination of other minor constituents in ten Anoectochilus species and five related species. Results: The contents of kinsenoside, goodyeroside A, polysaccharides and flavonoids varied notably almost in all tested samples, including both wild plants and tissue cultures. In particular, kinsenoside was the major lactone glycoside in A. roxburghii, A. formosanus, A. xingrenensis, A. nandanensis, A. brevilabris and A. burmannicus, whereas goodyeroside A was the predominant constituent in A. lylei, A. longilobus, A. elatus, A. zhejiangensis, G. schlechtendaliana, G. biflora, G. yangmeishanensi, G. repens and Ludisia discolor. Conclusion: Our present study suggested that A. lylei, A. longilobus, A. elatus, A. zhejiangensis, Ludisia discolor and Goodyera species cannot be used as alternatives for A. roxburghii, and goodyeroside A may be reasonably used as a diagnostic marker for distinguishing A. roxburghii from A. lylei, A. longilobus, A. elatus and A. zhejiangensis, Goodyera and Ludisia species. The established method thus could be potentially used for the quality evaluation and control of Anoectochilus and some related species.
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Aim To study the anti-diabetic effects of natural product gastrodin ( GSTD ) in KK-Ay mice. Methods C57BL/6J mice were used as normal con-trol, while KK-Ay diabetic mice were divided into five groups, namely the untreated group, GSTD 10 mg· kg-1, 20 mg·kg-1, 50 mg·kg-1 groups, and the metformin ( Met) 200 mg·kg-1 group, respectively, with 10 mice in each group. GSTD and Met were ad-ministered intragastrically for eight weeks. Before ex-periment and once a week during the experiment, the fasting blood glucose ( FBG) levels were determined. During the 7th week of drug treatment, oral glucose tolerance test ( OGTT ) and insulin tolerance test ( ITT) were conducted. Before the end of experiment, 24 h urine samples were collected for the assay of rela-tive parameters. At the end of experiment, blood sam-ples were collected for the assay of glycosylated hemo-globin ( GHb) ; serums were isolated for the determina-tion of insulin concentration and other biochemical in-dexes. After sacrifice, the livers, kidneys, and pan-creases of the mice were harvested for pathological ex-amination; the contents of advanced glycation end product ( AGE) and triglyceride ( TG) in renal tissues were assayed by kits. Results GSTD at all doses sig-nificantly reduced FBG, urine glucose, GHb, serum insulin level, and the insulin resistance index in KK-Ay diabetic mice. In addition, GSTD greatly inhibited body weight gain and improved glucose tolerance and insulin tolerance ( P <0.05 or P <0.01 vs untreated group ) . The pathological examination showed that GSTD significantly increased the glycogen content of liver tissues, reduced islet volume and improved its pathological changes. In addition, the glomerulosclero-sis induced by diabetes was greatly ameliorated by GSTD. Meanwhile, GSTD greatly reduced serum crea-tine ( Scr) , 24 h urine amount, 24 h urine total pro-tein and microalbumin ( mAlb) , as well as renal AGE and TG contents in KK-Ay mice ( P <0.05 or P <0.01 vs untreated group) . The anti-diabetic effect of GSTD at 50 mg·kg-1 was comparable to that of 200 mg·kg-1 of Met. Conclusions When used to treat KK-Ay diabetic mice, GSTD has potent activities in lowering blood glucose, improving insulin resistance and ameliorating diabetic nephropathy. However, the detailed mechanisms of GSTD in modulating glucose metabolism and increasing insulin sensitivity still need further investigation.
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Cathepsin K (CTSK) is considered a critical pharmaceutical target in the treatment of osteoporosis. CTSK exerts proteolytic activities against regulatory proteins besides its collagenase function, which may account for some of the adverse reactions when blocked by active site-directed inhibitors. Exosite inhibitors that can discriminate between the therapeutic collagenase and other biological activities of CTSK specifically inhibit the collagenase activity of CTSK without interfering with the other proteolytic activities of the protease. Active recombinant CTSK was expressed in Pichia pastoris, and purified by n-butyl sepharose and SP sepharose column chromatography. Herba Ecliptae is a common traditional Chinese medicine in the treatment of bone diseases. Collagenase assay and benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin (Z-FR-MCA) substrate assay based on CTSK are applied to verify the exosite inhibitors. n-Butanol extract of Herba Ecliptae are the most active fraction and eclalbasaponin IX isolated from n-butanol fraction is the potential exosite inhibitor of CTSK.
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<p><b>BACKGROUND</b>Previous studies reported interleukin-27 (IL-27), interferon-γ (IFN-γ), or adenosine deaminase (ADA) alone plays a helpful role in diagnosing tuberculous pleural effusion (TPE). The present study aims at comparing the diagnostic accuracy of pleural IL-27, IFN-γ, and ADA, and investigate the diagnostic accuracy of the combination of IL-27, IFN-γ, or/and ADA for differentiating TPE from pleural effusions with the other etiologies.</p><p><b>METHODS</b>The concentrations of IL-27, IFN-γ and ADA were simultaneously determined in pleural fluids and sera from 40 patients with TPE; 26 with malignant pleural effusion, seven with infectious pleural effusion, and eight with transudative pleural effusion by enzyme linked immunosorbent assay and colorimetric method. The corresponding biochemical indexs were also simultaneously determined.</p><p><b>RESULTS</b>The concentrations of pleural IL-27 and IFN-γ in the tuberculous group were significantly higher than those in the malignant, infectious, and transudative groups. The concentrations of ADA in TPE were significantly higher than those in MPE or transudative effusions, while much lower than those in infectious effusions. Among these three biomarkers, IL-27 was the most effective for TPE diagnosis, with the cut off value of 900.8 ng/L. IL-27 had a high sensitivity of 95% and specificity of 97.6% for differential diagnosis of TPE from non-TPEs. Combinations of IL-27, IFN-γ and ADA measurements further increased the sensitivity or specificity up to 100%.</p><p><b>CONCLUSIONS</b>Compared to non-TPEs, IL-27, IFN-γ and ADA all simultaneously increased in TPE; and among these three rapid detection methods, IL-27 appeared to be the best for distinguishing tuberculous from non-TPEs, especially from MPE. Combinations of the three markers (IL-27, IFN-γ and ADA) yielded the highest sensitivity and specificity. These findings suggest that the applications of a new biomarker, IL-27, alone or with IFN-γ and ADA, may contribute to more efficient diagnosis strategies in the management of tuberculous pleurisy.</p>
Subject(s)
Aged , Female , Humans , Male , Middle Aged , Adenosine Deaminase , Blood , Metabolism , Interferon-gamma , Blood , Metabolism , Interleukin-27 , Blood , Metabolism , Pleural Effusion , Blood , Metabolism , Tuberculosis, Pleural , Blood , Diagnosis , MetabolismABSTRACT
A series of novel quinolinone acid-containing compounds were designed and synthesized. Their structures were confirmed with 1H NMR and MS. The target compounds were tested for anti-HIV-1 integrase activities in vitro with enzyme linked immunosorbent assay (ELISA). The result showed that D-2, D-4 and D-7 have anti-integrase activity with IC50 < 100 micromol L(-1).
Subject(s)
HIV Integrase , Metabolism , HIV Integrase Inhibitors , Chemistry , Pharmacology , Inhibitory Concentration 50 , Quinolones , Chemistry , Pharmacology , Structure-Activity RelationshipABSTRACT
<p><b>BACKGROUND</b>Triggering receptors expressed on myeloid cells (TREM) proteins are a family of cell surface receptors expressed broadly by cells of the myeloid lineage. The aim of this study was to investigate the clinical significance of soluble TREM-1 (sTREM-1) in pleural effusions, and to determine the effects of pneumonia on pleural sTREM-1 concentrations.</p><p><b>METHODS</b>Pleural fluid was collected from 109 patients who presented to the respiratory institute (35 with malignant pleural effusion, 31 with tuberculous pleural effusion, 21 with bacterial pleural effusion, and 22 with transudate). The concentrations of sTREM-1, tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta) were determined in effusion and serum samples by enzyme linked immunosorbent assay (ELISA).</p><p><b>RESULTS</b>The concentrations of sTREM-1 in bacterial pleural effusion were significantly higher than those in malignant, tuberculous, and transudative groups (all P < 0.001). An sTREM-1 cutoff value of 768.1 ng/L had a sensitivity of 86% and a specificity of 93%. Pleural sTREM-1 levels were positively correlated with levels of TNF-alpha and IL-1beta. Patients with complicating bacterial pneumonia did not have elevated concentration of sTREM-1 in pleural effusion when compared with patients without pneumonia.</p><p><b>CONCLUSIONS</b>Determination of pleural sTREM-1 may improve the ability of clinicians to differentiate pleural effusion patients of bacterial origin from those with other etiologies. The occurrence of bacterial pneumonia did not affect pleural sTREM-1 concentrations.</p>