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Fan P.,Shandong University | Zhang T.,Shandong Qidu Pharmaceutical Co. | Hostettmann K.,University of Geneva
Journal of Traditional and Complementary Medicine | Year: 2013

Polygonum cuspidatum Sieb. and Zucc. has been traditionally used as a member of many anti-inflammatory polyherbal formulations, but is now a widespread invasive neophyte in Europe and America. To discuss if the invasive variety is chemically identical to the native one in traditional medicine, the different constituents of the invasive variety compared to the native variety were isolated and their anti-inflammatory activity was tested. Resveratroloside and catechin-(4α→8)-catechin, the newly found constituents in the invasive variety, have similar nitric oxide (NO) inhibition potency as that of piceid (the major constituent of P. cuspidatum), but the newly found major constituent, i.e., piceatannol glucoside, showed no apparent effect. On the other hand, as a marker, the total content of resveratrol in the methanol root extract after glucosidase hydrolysis was measured and compared between the invasive and native varieties. The total content of resveratrol measured in the root extracts of the Swiss sample was about 2.5 times less than that of the Chinese one. This study brings attention to the point that when the invasive variety of P. cuspidatum is used in traditional medicine, the chemical difference should be kept in mind. Copyright © 2013 Committee on Chinese Medicine and Pharmacy, Taiwan.

Fu H.,Shandong University | Han L.,Shandong University | Hou X.,Shandong University | Dun Y.,Shandong University | And 3 more authors.
Bioorganic and Medicinal Chemistry | Year: 2015

We report the development of a novel series of saccharin-based N-hydroxybenzamides as histone deacetylases inhibitors. Among them, 6j exhibited potent HDACs inhibitory activity against Hela nuclear extract. Further biological evaluation found 6i showed similar antiproliferative activities in vitro compared with the approved SAHA. © 2015 Elsevier Ltd.

Wang X.-J.,Weifang Medical University | Duan Y.,Weifang Medical University | Li Z.-T.,Shandong Qidu Pharmaceutical Co. | Feng J.-H.,Shandong Academy of Sciences | And 4 more authors.
Asian Pacific Journal of Cancer Prevention | Year: 2014

Multi-target drug design, in which drugs are designed as single molecules to simultaneously modulate multiple physiological targets, is an important strategy in the field of drug discovery. QT-011, a tamibarotene-furoxan derivative, was here prepared and proposed to exert synergistic effects on antileukemia by releasing nitric oxide and tamibarotene. Compared with tamibarotene itself, QT-011 displayed stronger antiproliferative effects on U937 and HL-60 cells and was more effective evaluated in a nude mice U937 xenograft model in vivo. In addition, QT-011 could release nitric oxide which might contribute to the antiproliferative activity. Autodocking assays showed that QT-011 fits well with the hydrophobic pocket of retinoic acid receptors. Taken together, these results suggest that QT-011 might be a highly effective derivative of tamibarotene and a potential candidate compound as antileukemia agent.

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