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标题:Screening for anti-proliferative and anti-inflammatory components from Rhamnus davurica Pall. using bio-affinity ultrafiltration with multiple drug targets.
时间:2020-03-27 00:02:33
DOI:10.1007/s00216-018-0953-6
PMID:29476234
作者:Guilin Chen;Jianlin Wu;Na Li
出版源: 《Analytical & Bioanalytical Chemistry》 ,2018 ,410 (15) :3587-3595
摘要:Rhamnus davurica Pall. (R. davurica) has been used as a traditional medicine for many years in China and abroad and shown a wide spectrum of biological activities. Previously, we reported the phytochemical fingerprinting profile of R. davurica, its distinct anti-proliferative activities against HT-29 and SGC-7901 cell lines, and the topoisomerase I (Top I) ligands based on bio-affinity ultrafiltration and HPLC-MS (UF-HPLC-MS). Nevertheless, among the 32 peaks detected in the fingerprinting profile, the common bioactive constituents responsible for the anti-inflammatory and anti-proliferative activities in the extracts remain elusive. To further explore the specific responsible components for their diversified activities and their potential action targets/mechanisms, the method based on bio-affinity UF-HPLC-MS using therapeutic targets like Top I and cyclooxygenase 2 (COX-2) was established to rapidly screen and identify the ligands binding to these known target enzymes. As a result, 12 components were revealed as potential Top I ligands along with 11 components as potential COX-2 ligands, where several components were revealed to possess both activities. Further validations of these bioactive components have also been conducted and confirmed their highlighted activities. This integrated method of UF-HPLC-MS exhibits high efficiency in rapidly screening for multi-target bioactive components responsible for multiple pharmacological effects from the complex natural products and could be very useful to explain the complex action mechanisms of herb medicines in a complex multi-component and multi-target mode at the molecular level.
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目录:
  • Screening...
    • Abstract
    • Introduction
    • Materials and methods
      • Materials, chemicals, and solvents
      • Sample preparation and screening for potential ligands with ultrafiltration
      • HPLC-ESI-MS/MS analysis
      • COX-2 inhibition assays
      • Anti-proliferation assays
    • Results and discussion
      • Screening for Top I and COX-2 ligands in R.’davurica using the UF-HPLC-MS method
      • Identification of Top I and COX-2 ligands in R.’davurica using HPLC-ESI-MS/MS
      • In’vitro bioactive validation of the representative compounds
      • The structure-activity relationships between flavonoids and enzymes
    • Conclusion
    • References

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