Screening and isolation of a natural dopamine D1 receptor antagonist using cell-based assays

Yu, Sungryul; Park, Jeong‐Soo; Paredes, Verenice; Song, Myoung‐Chong; Baek, Nam‐In; Lee, Sang‐Ik; Lim, Jong-Soon; Cho, Nam-Young; Yoon, Jaeseung; Baek, Kwanghee

doi:10.1016/j.jbiotec.2009.12.005

Cited by 5 publications

(3 citation statements)

References 20 publications

(25 reference statements)

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“…The single compounds from the fruits or anomalous fruits of Gleditsia sinensis have been isolated as triterpene (echinocystic acid), flavonoid (aromadendrin), polyphenol (ellagic acid glycosides), and triterpenoid saponins (gleditsioside A-K, N-Q, and Z) [31-40]. Their identified pharmacological activities were antagonistic against dopamine D1 receptor (gleditsioside F) [33], protective against acute myocardial ischemia (echinocystic acid) [32] or type 2 diabetes mellitus (aromadendrin) [35], antiallergic in mast cells (saponins) [41], and cytotoxic to leukemic cells (gleditsioside E) [38]. The single compounds from the Gleditsia sinensis thorns were isolated as a lupane acid with anti-HIV activity [42], and triterpenoid (D:C-friedous-7-en-3-one) and sterols with antimutagenic activity [43].…”

Section: Discussionmentioning

confidence: 99%

Ethanol extract of Gleditsia sinensis thorn suppresses angiogenesis in vitro and in vivo

Park

et al. 2012

BMC Complement Altern Med

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BackgroundGleditsia sinensis thorns have been widely used in traditional Korean medicine for the treatment of several diseases, including obesity, thrombosis, and tumor-related diseases. The aim of the study is to determine the antiangiogenic effect of Gleditsia sinensis thorns in vitro and in vivo in a bid to evaluate its potential as an anticancer drug.MethodsEthanol extract of Gleditsia sinensis thorns (EEGS) were prepared and used for in vitro and in vivo assays. In vitro antiangiogenic effect of EEGS was determined in HUVEC primary cells by cell migration and tube formation assays. In vivo antiangiogenic effect of EEGS was determined by measuring vessel formation and vascular endothelial cells migrating into the implanted matrigels in nude mice. The angiogenesis-related proteins of which expression levels were altered by EEGS were identified by proteomic analysis.ResultsEEGS exerted a dose-dependent antiproliferative effect on HUVEC cells without significant cytotoxicity. Angiogenic properties, such as cell migration and tube formation, were significantly inhibited by EEGS in a dose-dependent manner. New vessel formation was also suppressed by EEGS, as determined by the directed in vivo angiogenesis assays in nude mice. EEGS reduced the expression of proangiogenic proteins, endothelin 1 and matrix metallopeptidase 2, in HUVEC cells.ConclusionsOur findings suggest that EEGS can inhibit angiogenesis by down-regulating proangiogenic proteins, and therefore it should be considered as a potential anticancer drug targeting tumor-derived angiogenesis.

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Section: Discussionmentioning

confidence: 99%

Ethanol extract of Gleditsia sinensis thorn suppresses angiogenesis in vitro and in vivo

Park

et al. 2012

BMC Complement Altern Med

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“…The challenge in these procedures lies in the difficulty of correctly matching the dereplicated bioactive compounds in particular fractions with their chemical structure [8, 9]. Typical examples include fractionation of intact proteins before matrix-assisted laser-desorption ionization (MALDI) MS analysis [10], and many types of biochemical assay formats that are conducted after fractionation of bioactive mixtures, such as natural extracts [11, 12], metabolic mixtures [13], and environmental mixtures [14–17]. The main drawback is that the high resolution obtained from the separation step (chromatographic peaks of seconds to tens of seconds) is often lost in the low-resolution fractionation process (fractions in the minute range are common).…”

Section: Introductionmentioning

confidence: 99%

Advances in mass spectrometry-based post-column bioaffinity profiling of mixtures

Kool¹,

Giera²,

Irth³

et al. 2010

Anal Bioanal Chem

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In the screening of complex mixtures, for example combinatorial libraries, natural extracts, and metabolic incubations, different approaches are used for integrated bioaffinity screening. Four major strategies can be used for screening of bioactive mixtures for protein targets—pre-column and post-column off-line, at-line, and on-line strategies. The focus of this review is on recent developments in post-column on-line screening, and the role of mass spectrometry (MS) in these systems. On-line screening systems integrate separation sciences, mass spectrometry, and biochemical methodology, enabling screening for active compounds in complex mixtures. There are three main variants of on-line MS based bioassays: the mass spectrometer is used for ligand identification only; the mass spectrometer is used for both ligand identification and bioassay readout; or MS detection is conducted in parallel with at-line microfractionation with off-line bioaffinity analysis. On the basis of the different fields of application of on-line screening, the principles are explained and their usefulness in the different fields of drug research is critically evaluated. Furthermore, off-line screening is discussed briefly with the on-line and at-line approaches.Schematic view of an on-line bioaffinity analysis or HRS setup with MS based bioassay detection

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“…T raditionally, bioactive mixtures are fractionated prior to offline bioactivity profiling. one can think of natural extracts 1,2 and metabolic mixtures 3 in which the fractionation process is followed by reconcentration, addition of biochemical reagents, incubation, and finally microplate reader analysis. analysis of bioactives in mixtures is important in, for example, the pharmaceutical area to assess their medicinal and/or adME(t) potential.…”

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confidence: 99%

High-Resolution Bioactivity Profiling of Mixtures toward the Acetylcholine Binding Protein Using a Nanofractionation Spotter Technology

Kool¹,

Heus²,

Kloe

et al. 2011

SLAS Discovery

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this study describes the evaluation, validation, and use of contactless postcolumn fractionation of bioactive mixtures with acetylcholine binding protein (aChBP) affinity analysis with help of a spotter technology. the high-resolution fractionation tailors the fractionation frequency to the chromatographic peaks. Postcolumn reagents for aChBP bioaffinity profiling are mixed prior to droplet ejection into 1536-well plates. after an incubation step, microplate reader analysis is used to determine bioactive compounds in a mixture. For ligands tested, a good correlation was found for iC 50 s determined in flow injection analysis mode when compared with traditional radioligand binding assays. after the evaluation and validation, bioaffinity profiling of actual mixtures was performed. the advantage of this "atline" technology using postcolumn bioaffinity analysis when compared to continuous flow online postcolumn bioaffinity profiling is the possibility to choose postcolumn incubation times freely without compromising resolution due to diffusion effects. (Journal of Biomolecular Screening. 2011;16:917-924)

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Screening and isolation of a natural dopamine D1 receptor antagonist using cell-based assays

Cited by 5 publications

References 20 publications

Ethanol extract of Gleditsia sinensis thorn suppresses angiogenesis in vitro and in vivo

Ethanol extract of Gleditsia sinensis thorn suppresses angiogenesis in vitro and in vivo

Advances in mass spectrometry-based post-column bioaffinity profiling of mixtures

High-Resolution Bioactivity Profiling of Mixtures toward the Acetylcholine Binding Protein Using a Nanofractionation Spotter Technology

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