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.
The historical context of Leonurus japonicas Houtt. provides a foundational understanding of its long-standing relevance in traditional medicinal practices. Shennong Bencao Jing, one of the oldest and most authoritative classical medicinal texts, documented the herb’s unique properties, linking it to concepts of enhanced physical lightness and longevity—attributes that have contributed to its enduring reputation in herbal medicine. Over time, its recognition as Chinese Motherwort or Siberian Motherwort solidified its position, particularly in gynecological care, where its multifaceted effects address key concerns such as irregular menstruation, blood stasis-related issues, fluid retention, and inflammatory conditions. Clinicians have relied on it for generations to alleviate common gynecological ailments, a testament to its practical value and perceived efficacy in traditional therapeutic frameworks.
At the core of Leonurus japonicas Houtt.’s biological activity lies leonurine, an alkaloid that has emerged as a focal point of modern scientific inquiry due to its diverse beneficial properties. Anti-oxidation, a critical function in combating oxidative stress—a known driver of cellular damage and aging—enables leonurine to neutralize harmful free radicals and protect cells from oxidative harm. Its anti-inflammatory capacity is equally significant, as chronic inflammation underpins the development and progression of numerous diseases, from cardiovascular disorders to neurodegenerative conditions. Additionally, the anti-apoptotic activity of leonurine plays a vital role in preserving cellular viability, preventing excessive or inappropriate cell death that can disrupt tissue function and contribute to disease pathogenesis. These combined biological activities position leonurine as a promising candidate for therapeutic development, particularly in areas where existing treatments fall short due to side effects or limited efficacy.
The global burden of cardiovascular and central nervous system diseases underscores the urgency of identifying new, safer therapeutic agents. Cardiovascular diseases, including conditions such as hypertension, atherosclerosis, and heart failure, remain leading causes of mortality worldwide, with current medications often associated with adverse effects ranging from digestive disturbances to more severe complications. Similarly, central nervous system disorders, such as Alzheimer’s disease, Parkinson’s disease, and stroke, pose significant challenges to patient quality of life and healthcare systems, with treatments frequently focusing on symptom management rather than addressing underlying molecular mechanisms. In this context, leonurine’s potential to target these diseases at the molecular level offers a new avenue for exploration. By examining its interactions with key molecular pathways involved in disease progression—such as those regulating inflammation, oxidative stress, and cell survival—researchers aim to uncover how leonurine can modulate these processes to exert therapeutic effects.
Current research into leonurine’s role in cardiovascular and central nervous system diseases has yielded valuable insights, though much remains to be explored. Studies have begun to elucidate specific molecular targets of leonurine, such as enzymes, receptors, or signaling molecules that are dysregulated in disease states. For example, in cardiovascular contexts, leonurine may influence pathways involved in vascular relaxation, platelet aggregation, or myocardial cell protection, while in central nervous system disorders, it could impact processes like neuroinflammation, synaptic plasticity, or neuronal survival. These findings not only highlight leonurine’s potential but also underscore the need for further investigation to fully understand its molecular mechanisms of action, optimize dosage and delivery methods, and evaluate its long-term safety and efficacy in clinical settings.
As leonurine transitions into the clinical experiment stage, the compilation of existing research becomes increasingly important. This review serves as a synthesis of current knowledge, bringing together findings from diverse studies to provide a comprehensive overview of leonurine’s therapeutic potential. By identifying gaps in current understanding—such as the need for more in-depth studies on specific molecular pathways, or the exploration of leonurine’s interactions with other drugs—it offers direction for future research efforts. Additionally, it aims to inform clinical practice by highlighting the potential applications of leonurine, ultimately contributing to the development of safer, more effective treatments for cardiovascular and central nervous system diseases that burden global health..
DOI：10.1007/s11684-025-1138-2