AI Article Synopsis
- Bunge, a traditional Chinese medicine, is investigated for its active component targeting TRPC1, a key protein in treating myocardial injury.* -
- The study employed pharmacology databases and various assays to identify rosmarinic acid (RosA) as a potent compound, showing strong binding to TRPC1 and reducing its levels in heart cells.* -
- Results indicate that RosA may serve as a promising clinical candidate for therapy related to myocardial injuries, particularly by mitigating Ca2+ influx injuries in heart cells.*
Article Abstract
Context: Bunge (Lamiaceae) is a traditional Chinese medicine (TCM) for the treatment of 'thoracic obstruction'. Transient receptor potential canonical channel 1 (TRPC1) is a important target for myocardial injury treatment.
Objective: This work screens the active component acting on TRPC1 from .
Materials And Methods: TCM Systems Pharmacology Database and Analysis Platform (TCMSP) was used to retrieve compounds for preliminary screening by referring to Lipinski's rule of five. Then, the compound group was comprehensively scored by AutoDock Vina based on TRPC1 protein. Surface plasmon resonance (SPR) was used to determine the affinity of the optimal compound to TRPC1 protein. Western blot assay was carried out to observe the effect of the optimal compound on TRPC1 protein expression in HL-1 cells, and Fura-2/AM detection was carried out to observe the effect of the optimal compound on calcium influx in HEK293 cells.
Results: Twenty compounds with relatively good characteristic parameters were determined from 202 compounds of . Rosmarinic acid (RosA) was obtained based on the molecular docking scoring function. RosA had a high binding affinity to TRPC1 protein (KD value = 1.27 µM). RosA (50 μM) could reduce the protein levels (417.1%) of TRPC1 after oxygen-glucose deprivation/reperfusion (OGD/R) in HL-1 cells and it could inhibit TRPC1-mediated Ca influx injury (0.07 ΔRatio340/380) in HEK293 cells.
Discussion And Conclusions: We obtained the potential active component RosA acting on TRPC1 from , and we speculate that RosA may be a promising clinical candidate for myocardial injury therapy.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9828776 | PMC |
| http://dx.doi.org/10.1080/13880209.2022.2160769 | DOI Listing |
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