Tribulus terrestris L. has traditionally been used in Mongolian medicine for its effects on kidney protection, promotion of urination, and boosting of physical energy. This study investigated the plant's historical use, chemical composition, biological effects, and medicinal significance. Methods: A literature review was conducted using classical medical texts, pharmacopoeias, and peer-reviewed articles from international research databases to explore the properties and uses of T. terrestris. Results: Traditional sources, such as book “Essence of spring water, root of the eight-part secret”(“Rashaan Shim Naiman Gishuun't Nuuts Uvdisiin Undes”), describe T. terrestris as having sweet and warm properties, mainly used for treating kidney diseases and wind-related disorders (khi). It has traditionally been used to relieve kidney ailments caused by cold, kidney rheumatism, urinary retention, leg and back pain, edema, and male reproductive weakness. Additionally, it is believed to promote urination and enhance the overall vitality. Modern research confirms that T. terrestris exhibits kidney-protective effects owing to its antioxidant, anti-inflammatory, and antimicrobial properties. It also has mild diuretic effects, supports sex hormone production, and enhances sexual functions. Furthermore, their antioxidant properties have potential anti-aging effects. Conclusion: Modern research confirms the traditional use of T. terrestris to support kidney health, promote urination, and boost physical energy intake.