Astragaloside IV (AS-IV), is the primary active compound found in Astragalus membranaceus, a functional food for tonifying Qi. Modern extraction technologies, such as ultrasonic extraction, microwave extraction, and enzymatic-assisted extraction, have been utilized to extract AS-IV from Astragalus membranaceus, which could improve the extraction efficiency of AS-IV. Extensive scientific researches have revealed that AS-IV has a broad spectrum of pharmacological benefits, including anti-inflammatory, anti-fibrotic, anti-oxidative stress, anti-diabetic, and cardioprotective properties. The multiple effects are achieved through regulating the diverse cellular signaling pathways (MAPK, HIF-1α and NF-κB, etc.), which provides a comprehensive strategy for treating various diseases. Due to the multiple effects of AS-IV, this compound has essential therapeutic effects in treating heart failure, myocarditis, cardiac fibrosis and ischemic stroke. Nevertheless, AS-IV possessed short half-life and low bioavailability, which limited the clinical application. Drug delivery systems should be conducted to enhance the absorption rate and AS-IV. Given these diverse and promising effects, AS-IV stands out as a promising candidate for the development of novel therapeutic agents.