Ultrafiltration LC-ESI-MSn screening of 5-lipoxygenase inhibitors from selected Chinese medicinal herbs Saposhnikovia divaricata, Smilax glabra, Pueraria lobata and Carthamus tinctorius

Zhao, Anqi; Li, Li; Li, Bo; Zheng, Min; Tsao, Rong

doi:10.1016/j.jff.2016.04.011

Cited by 25 publications

(18 citation statements)

References 19 publications

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“…The enhancement factor (Table 2) was introduced to further understand the relative binding strength of each compound [17, 20]. This factor is proportional to the LC peak area of the ligand bound to the target enzyme; thus the higher factor means more bound compound.…”

Section: Resultsmentioning

confidence: 99%

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Rapid Screening of Potential Phosphodiesterase Inhibitors from the Roots of Ilex pubescens Hook. et Arn. Using a Combination of Ultrafiltration and LC–MS

Liu

Lin

Chen

et al. 2017

Evidence-Based Complementary and Alternative Medicine

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The cyclic nucleotide phosphodiesterase (PDE) plays an important role in regulating the levels of second messenger molecules cAMP and cGMP. Various PDE inhibitors have been successfully developed into drugs for targeted diseases. In addition, PDE inhibitors can also be found in different foods and natural medicines. In this study, ultrafiltration liquid chromatography–diode-array detector–electrospray ionization–ion-trap–time-of-flight–mass spectrometry (ultrafiltration LC–DAD–ESI–IT–TOF–MS) was applied to screen PDE inhibitors from the roots of Ilex pubescens Hook. et Arn. As a result, 11 major compounds were identified in I. pubescens roots, with nine compounds as potential PDE inhibitors, among which five were further confirmed to be active against PDEI and PDE5A dose-dependently in vitro, with ilexsaponin A1 and ilexsaponin B2 being the strongest. HPLC quantification of these bioactive compounds suggested that they are major components in the plant. The results demonstrate that ultrafiltration LC–DAD–ESI–IT–TOF–MS is an efficient method for rapid screening of PDE inhibitors from natural medicines.

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Section: Resultsmentioning

confidence: 99%

“…The enhancement factor (%) = ( A 1 / A 2 ) × 100% was used for calculating the binding of a ligand to PDEI, where A 1 and A 2 are the amounts of compound bound to PDEI and the total amount of compound in incubation, respectively [17, 20]. …”

Section: Methodsmentioning

confidence: 99%

Rapid Screening of Potential Phosphodiesterase Inhibitors from the Roots of Ilex pubescens Hook. et Arn. Using a Combination of Ultrafiltration and LC–MS

Liu

Lin

Chen

et al. 2017

Evidence-Based Complementary and Alternative Medicine

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show abstract

“…To further characterize the relative binding capacity of the individual compounds and how each contributed to the overall activity of the extract, we calculated an enhancement factor . This factor as is based on the peak area or binding by a particular compound to the target enzyme; thus higher values indicate greater binding, or potentially higher potency of inhibition, by the compound.…”

Section: Resultsmentioning

confidence: 99%

Ultrafiltration‐LC–MS combined with semi‐preparative HPLC for the simultaneous screening and isolation of lactate dehydrogenase inhibitors from Belamcanda chinensis

Tang

et al. 2016

J of Separation Science

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Stroke represents the fourth leading cause of death in the USA and the second leading cause of death worldwide. Lactate dehydrogenase inhibitors are widely used in the treatment of ischemic stroke and natural products are considered a promising source of novel lactate dehydrogenase inhibitors. In this study, we used PC12 cells to determine the protective effect of extracts from the herb Belamcanda chinensis following toxic challenge. Using ultrafiltration high-performance liquid chromatography coupled with photo-diode array detection and electrospray ionization mass spectrometry, we screened and identified isoflavonoids from Belamcanda chinensis extracts. Semi-preparative high-performance liquid chromatography was then applied to separate and isolate the active constituents. Using these methods, we identified six major compounds in Belamcanda chinensis as lactate dehydrogenase inhibitors: tectoridin, iristectorin A, iridin, tectorigenin, irigenin, and irisflorentin, which were then isolated to >92% purity. This is the first report that Belamcanda chinensis extracts contain potent lactate dehydrogenase inhibitors. Our results demonstrate that the systematic isolation of bioactive components from Belamcanda chinensis guided by ultrafiltration high-performance liquid chromatography coupled with photo-diode array detection and electrospray ionization mass spectrometry represents a feasible and efficient technique that could be extended for the identification and isolation of other enzyme inhibitors.

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“…Throughoutt he years, some small organic compounds have been shown to inhibit the activity of IL-5. [64] In 1999, Sophora japonica L.,aplant of the Leguminosae family,w as found to have an inhibitory effect in IL-5 bioassays;s ome isoflavones, namely sophoricoside (35), genistein ( 36), orobol( 37), and genistin ( 38) ( Figure 22), were identified as the active principles. [64] These isoflavones are unrelated to the structural unit of IL-5, in contrast to the IL-5 antagonists isothiazolones, and are the first natural products to show inhibitory activity against IL-5b ioactivity.…”

Section: Interleukin-5 Inhibitorsmentioning

confidence: 99%

Chromones: A Promising Ring System for New Anti‐inflammatory Drugs

2016

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The quest for safer anti-inflammatory drugs is still the focus of several medicinal chemistry programs. Chromones (4H-chromen-4-ones) are a group of naturally occurring compounds ubiquitous in plants, and the chromone core has proven to be a privileged scaffold in medicinal chemistry. Herein we provide an overview of the relevance of chromones as anti-inflammatory agents, specifically as inhibitors of cyclooxygenase (COX), 5-lipoxygenase (5-LOX), interleukin-5 (IL-5), and nitric oxide ( NO) production. Numerous structure-activity relationships and mechanisms of action are discussed. This review is therefore intended to provide a foundation for the design and synthesis of novel chromone-based compound libraries for further development into safer and more efficient anti-inflammatory agents.

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Ultrafiltration LC-ESI-MSn screening of 5-lipoxygenase inhibitors from selected Chinese medicinal herbs Saposhnikovia divaricata, Smilax glabra, Pueraria lobata and Carthamus tinctorius

Cited by 25 publications

References 19 publications

Rapid Screening of Potential Phosphodiesterase Inhibitors from the Roots of Ilex pubescens Hook. et Arn. Using a Combination of Ultrafiltration and LC–MS

Rapid Screening of Potential Phosphodiesterase Inhibitors from the Roots of Ilex pubescens Hook. et Arn. Using a Combination of Ultrafiltration and LC–MS

Ultrafiltration‐LC–MS combined with semi‐preparative HPLC for the simultaneous screening and isolation of lactate dehydrogenase inhibitors from Belamcanda chinensis

Chromones: A Promising Ring System for New Anti‐inflammatory Drugs

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