Exploring the Cardioprotective Spectrum-Effect Relationship of Apocynum venetum L. Using a Zebrafish Model

Area of Science:

• Phytochemistry and Pharmacology
• Natural Product Chemistry

Background:

• Apocynum venetum L. leaves possess traditional medicinal uses and demonstrated cardioprotective potential.
• The specific active compounds and their mechanisms underlying the cardioprotective effects remain largely unelucidated.

Purpose of the Study:

• To identify the primary cardioprotective constituents within the n-butanol fraction of Apocynum venetum leaves.
• To elucidate the mechanisms of action of these identified compounds using chemical profiling, zebrafish models, and cell-based assays.

Main Methods:

• Chemical profiling using HPLC and UPLC-QE-Orbitrap-MS/MS to characterize extract subfractions.
• Assessment of cardioprotective effects in zebrafish myocardial injury models.
• Spectrum-effect relationship analysis (GRA, OPLS) and molecular assays (transcriptomics, qRT-PCR, molecular docking, H9c2 cell assays) to identify and validate active compounds and explore mechanisms.

Main Results:

• Spectrum-effect analysis identified chlorogenic acid (CGA) and 4-caffeoylquinic acid (4-CQA) as major cardioprotective constituents.
• CGA demonstrated significant cardioprotective effects in zebrafish, linked to PPARα-related metabolic pathways.
• Synergistic cardioprotective effects were observed when CGA was combined with myricetin 3-O-glucoside in H9c2 cells.

Conclusions:

• Chlorogenic acid (CGA) and 4-caffeoylquinic acid (4-CQA) are identified as key cardioprotective compounds in Apocynum venetum leaf extracts.
• The findings support the potential for synergistic interactions among constituents, particularly CGA-dominated combinations.
• This study provides a scientific basis for the traditional use of Apocynum venetum and guides future pharmacological research into its cardioprotective properties.