Galium odoratum, commonly known as sweet woodruff, is a perennial herbaceous plant that contains coumarin and is recognized for its medicinal properties. In this study, the influence of sunlight exposure on the phytochemical composition and anti-inflammatory potential of G. odoratum extracts is assessed. The extracts from cultivated and wild-grown plants were analyzed via chromatographic and mass spectrometric methods. In addition, the total phenolic content, antioxidant activity, and effects on macrophage polarization were assessed. The results revealed that while coumarin levels remain stable regardless of environmental conditions, phenolic content and antioxidant activity increase significantly under sun-grown conditions, with chlorogenic acid and rutin identified as major contributing compounds. Additionally, the extracts exhibited anti-inflammatory activity, effectively reducing the M1 macrophage population involved in inflammatory responses. These findings suggest that controlled sunlight exposure can enhance the bioactive profile of G. odoratum. This research highlights the critical role of environmental management in optimizing the medicinal properties of G. odoratum, providing a foundation for its future use in natural therapeutic applications.