Multi-Target Therapeutics of Geraniin from Geranium wilfordii Maxim. and Related Species: Mechanisms and Applications.

Abstract

Ethnopharmacological relevance: Erodii Herba Geranii Herba (also called Laoguancao in China) is the dried aerial part of Geranium wilfordii Maxim., Geranium carolinianum L. or Erodium stephanianum Willd.. It has developed into a natural remedy known for its anti-inflammatory, analgesic and hepatoprotective properties, and widely recognized within traditional Chinese medicine (TCM) and its cultural context. Given the traditional applications of Erodii Herba Geranii Herba, which underscore its potential as a promising source of bioactive compounds for pharmaceutical development, geraniin-one of its principal active constituents-has attracted increasing attention for its prospective development and utilization. Previous studies have demonstrated that geraniin exhibits a broad spectrum of pharmacological activities, including metabolic regulation, organ protection mediated through anti-inflammatory and antioxidant mechanisms, as well as antitumor and antiviral effects. Nevertheless, a systematic review of these pharmacological activities and their underlying mechanisms remains lacking.

Aim of the study: This review focused on the pharmacological activities of geraniin and also summarized its availability, pharmacokinetics, and toxicity, thereby providing a solid theoretical foundation for its further development and practical utilization.

Material and methods: The literature included in this review was identified through searches conducted in the PubMed and China National Knowledge Infrastructure (CNKI) databases using the keywords "Geraniin", "Pharmacology", and "Pharmacokinetics". A total of 99 articles were retrieved, excluding review articles. The retrieved publications covered a period from 1974 to 2025.

Results: Geraniin demonstrated a range of pharmacological effects, including regulation of metabolism (glycolipid metabolism, blood pressure, and bone metabolism), protection of multiple organs (brain, cardiovascular, pulmonary, gastrointestinal, and renal systems), anti-tumor activity (against lung, breast, colorectal, and cervical cancers), and broad-spectrum antiviral properties. Notably, the multi-target actions of geraniin facilitated cross-disease modulation through involvement in the oxidative-inflammatory network (via NF-κB-Nrf2 and MAPK pathways) and the cell survival network (including PI3K/Akt and Wnt/β-catenin pathways), thereby underpinning its organ-protective effects, anti-tumor activity, and metabolic regulatory functions.

Conclusion: These attributes suggested that geraniin held promise as a multi-targeted therapeutic agent. Thus, this paper elucidated the possibility of exploiting the resources of geraniin as a pharmaceutical product.