Leonurus japonicas Houtt., a medicinal herb with a history dating back to the ancient classical text Shennong Bencao Jing—where it was noted for properties associated with "light body and long life"—has long been valued in traditional medicine under the names Chinese Motherwort or Siberian Motherwort. Renowned as the "sacred medicine of gynecology," it is recognized for effects including activating blood circulation, regulating menstruation, promoting diuresis, reducing swelling, and clearing heat and detoxifying, making it a common choice in clinical settings for treating various gynecological diseases. Within this herb, leonurine stands out as a key alkaloid, endowed with multiple biological activities such as anti-oxidation, anti-inflammation, and anti-apoptosis. Given that cardiovascular and central nervous system diseases pose significant "major health threats" to human life and health globally, and considering the side effects of many existing drugs, a comprehensive exploration of leonurine’s potential therapeutic role in these areas becomes highly relevant. This work focuses on reviewing the potential molecular therapeutic effects of leonurine on diseases affecting the cardiovascular and central nervous systems, emphasizes the latest findings in current research progress, and centers on its therapeutic impacts across different disease conditions. Currently, leonurine is in the clinical experiment stage, and the insights compiled aim to offer guidance for future studies into its molecular mechanisms and its broader clinical application.