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Abstracts. PHYTOPHARM 2017
STRUCTURAL ANALYSIS OF HOMOPIPECOLIC ACID DERIVATIVES OF SPINY RESTHARROW ROOT
© Nora Gampe, Andrâs Darcsi, Szabolcs Béni, Lâszlô Kursinszki
Semmelweis University, Department of Pharmacognosy, Budapest, Hungary
The root of spiny restharrow (Ononis spinosa L.) is used as a diuretic remedy in traditional medicine and the drug is official in both the Hungarian and the European Pharmacopoeia. The most important secondary metabolites in restharrow root are isoflavonoids. These molecules can be found in the form of glucosides, glucoside malonates and rarely, glucoside acetates [1]. During thorough HPLC-MS/MS investigations characteristic peaks of nitrogen containing isoflavonoid derivatives could be observed. Beforehand neither alkaloids nor nitrogen containing other secondary metabolites have been identified in the extract of restharrow root. Based on product ion spectra and literature information, the structure of the isoflavonoid moiety could be identified unambiguously, however, the elucidation of the nitrogen containing part could not be executed using mass spectrometry exclusively. For the preparative isolation of the molecules of interest
the aqueous-methanolic extract was purified on weak cation-exchange cartridges. The eluted fraction was further separated by preparative HPLC. With the help of 1D and 2D NMR experiments six isoflavonoid glucoside piperidine-2-ylacetate (homopipecolic acid) could be identified. Moreover, the homologous pyrrolidine-2-ylacetate (homoproline) esters were also detected and tentatively identified in the extract based on the MS/MS spectra. The biosynthetic origin of these heterocyclic compounds is yet unknown in the Fabaceae family and their derivatives are firstly isolated from higher plants [2]. Acknowledgement: OTKA-PD-109373
References:
1. Gampe N, Darcsi A, Lohner S, Béni S, Kursinszki L. 2016. J. Pharm. Biomed. Anal. 123:74-81.
2. Nilsu T, Thorroad S, Ruchirawat S, Thasana N. 2016. Planta Med. 82(11/12):1046-1050.
CARDIOPROTECTIVE EFFECT OF SALVIANIC ACID A IN DB/DB MICE WITH ELEVATED HOMOCYSTEINE LEVEL
© Lei GAO1, Christopher WK LAI1, Adelheid Brantner2, Gerald Wölkart2
1 Department of Health Technology and Informatics, the Hong Kong Polytechnic University, Hung Hom, HKSAR, China;
2 Institute of Pharmaceutical Sciences, Department of Pharmacology and Toxicology, University of Graz, Graz
Cardiovascular disease (CVD) is the top death cause plays a dominant role. Hyper-homocysteine (HHcy), as an independent risk factor of CVD, can also be aggravated in diabetic patients. Salvianic acid A (SAA) is a major active ingredient extracted from a typical traditional Chinese medicine (TCM) applied in treatment of CVD.
The overall aim of this project is to investigate the therapeutic effect of SAA on HHcy and cardiovascular dysfunction in a transgenic diabetic animal model, db/ db mice. In this study, the functional and morphological changes of heart of db/db mice were examined with echocardiography. The endothelial function was determined using myograph system. And related biomarkers involved in homocysteine metabolism were also analyzed.
The result suggested that SAA administration suspended left ventricular hypertrophy of diabetes group (2.9% increase of left ventricular mass compared with baseline) compared with diabetes group without treatment (49.0% increase of left ventricular mass compared with
in people with diabetes, in which endothelial dysfunction baseline), and ameliorated endothelial dysfunction in diabetes with HHcy (improve endothelial-dependent vasorelaxation at the acetylcholine concentration of 10-6M by 42.8% compared with HHcy group without SAA). The acute vasorelaxant effects of SAA and its similarity was also tested in ex vivo assay. The serum homocysteine level in group with SAA treatment was significantly reduced (40.8% compared with HHcy group without SAA). These observed beneficial cardiovascular effects of SAA are probably due to improved redox status induced by the antioxidant effect of SAA itself, and to a lesser extent by the increased production of glutathione (23.2% increase of glutathione in HHcy group with SAA treatment compared with HHcy group without SAA) via activated transsulfuration pathway. The authors would like to thank the Eurasia Pacific Uninet for the scholarship support.
Obzory po kliniceskoj farmacologii i lekarstvennoj terapii [Reviews of clinical pharmacology and drug therapy]
vol. 15/2017/suppLeMEnT 1
