An Integrated Strategy for Rapid Screening of Multi-target Lead Compoundsfor the Treatment of Alzheimer's Disease from Traditional ChineseMedicines by UHPLC Combined with High-throughput Screening:A Case Study on Salviae miltiorrhizae Radix et Rhizoma / Minmin Zhang, Siduo Zhou, Wei Liu, Huijiao Yan, Xiao Wang, Heng-qiang Zhao
Background: Salviae miltiorrhizae Radix et Rhizoma (Red Sage root) is widely usedin traditional Chinese medicine (TCM) for the treatment of Alzheimers disease (AD) withdemonstrated curative effects, based on the concept of "one drug with multiple therapeutic targets,"which appears to be a good strategy for AD treatment. Objective: This study aimed to develop of high-throughput screening (HTS) method for multitherapeutictarget components found in complex TCMs, which are active against AD, using RedSage root as the case study. Methods: Acetylcholinesterase (AChE) inhibitors (AChEIs) from Red Sage root extracts werepre-screened by ultrafiltration-HPLC (UF-HPLC) analysis, in which AChE was added to the extractand then ultrafiltered to remove non-binding compounds. Potential AChEIs were identifiedby HPLC analysis of compounds bound to AChE. A microplate-based HTS was then used toquantify the AChE inhibitory activity and antioxidant activity of the pre-screened compounds. Results: Pre-screening found ten potential inhibitors, which were identified by ESI-TOF/MS; sixof these were purified by semi-preparative HPLC: Oleoyl neocryptotanshinone (1), DihydrotanshinoneⅠ (2), Cryptotanshinone (3), Tanshinone Ⅰ (4), Tanshinone ⅡA (5) and Miltirone (6).All six compounds had good AChE inhibitory activity and weak DPPH scavenging capacity. Conclusion: This study provides a platform and technology support for the rapid discovery ofmulti-target components, potentially active against AD, from complex TCMs and with strong potentialfor adaptation to the discovery of treatments for other diseases.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:18 |
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| Enthalten in: |
Current pharmaceutical analysis - 18(2022), 3, Seite 9 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Zhang, Minmin [VerfasserIn] |
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| Links: |
FID Access [lizenzpflichtig] |
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| Umfang: |
1 Online-Ressource (9 p) |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
KFL011170328 |
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| 245 | 1 | 0 | |a An Integrated Strategy for Rapid Screening of Multi-target Lead Compoundsfor the Treatment of Alzheimer's Disease from Traditional ChineseMedicines by UHPLC Combined with High-throughput Screening:A Case Study on Salviae miltiorrhizae Radix et Rhizoma |c Minmin Zhang, Siduo Zhou, Wei Liu, Huijiao Yan, Xiao Wang, Heng-qiang Zhao |
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| 520 | |a Background: Salviae miltiorrhizae Radix et Rhizoma (Red Sage root) is widely usedin traditional Chinese medicine (TCM) for the treatment of Alzheimers disease (AD) withdemonstrated curative effects, based on the concept of "one drug with multiple therapeutic targets,"which appears to be a good strategy for AD treatment. Objective: This study aimed to develop of high-throughput screening (HTS) method for multitherapeutictarget components found in complex TCMs, which are active against AD, using RedSage root as the case study. Methods: Acetylcholinesterase (AChE) inhibitors (AChEIs) from Red Sage root extracts werepre-screened by ultrafiltration-HPLC (UF-HPLC) analysis, in which AChE was added to the extractand then ultrafiltered to remove non-binding compounds. Potential AChEIs were identifiedby HPLC analysis of compounds bound to AChE. A microplate-based HTS was then used toquantify the AChE inhibitory activity and antioxidant activity of the pre-screened compounds. Results: Pre-screening found ten potential inhibitors, which were identified by ESI-TOF/MS; sixof these were purified by semi-preparative HPLC: Oleoyl neocryptotanshinone (1), DihydrotanshinoneⅠ (2), Cryptotanshinone (3), Tanshinone Ⅰ (4), Tanshinone ⅡA (5) and Miltirone (6).All six compounds had good AChE inhibitory activity and weak DPPH scavenging capacity. Conclusion: This study provides a platform and technology support for the rapid discovery ofmulti-target components, potentially active against AD, from complex TCMs and with strong potentialfor adaptation to the discovery of treatments for other diseases | ||
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| 700 | 1 | |a Liu, Wei |e verfasserin |4 aut | |
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| 700 | 1 | |a Wang, Xiao |e verfasserin |4 aut | |
| 700 | 1 | |a Zhao, Heng-qiang |e verfasserin |4 aut | |
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