Geraniin

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.

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.

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.

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.

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.

In the management of solid tumors, ionizing radiation is a critical therapeutic modality, particularly when surgical intervention is impractical due to patient-related factors, such as compromised health or elevated mortality risk. However, its non-selective action can cause serious side effects that negate the therapeutic benefits. Efforts have thus been made to identify pharmacological agents that can selectively protect normal tissues from exposure to ionizing radiation. Seven decades of study, however, have shown that the desired success has not been achieved in obtaining an ideal radioprotective agent. Moreover, even at optimal doses, the FDA-approved drug, amifostine (also known as WR-2721 [S-2- (3-aminopropyl-amino) ethyl phosphorothioic acid], exhibits significant toxicity. An ideal radioprotective agent can also be beneficial in environments where individuals are exposed to prolonged, low-dose radiation. Considering this, there is a pressing need to develop methods of shielding cells and patients from the deleterious effects of radiation, and a non-toxic radioprotective drug can be useful in both clinical and occupational contexts. Studies have shown that the fruits of Emblica officinalis and its cardinal phytochemicals, such as gallic acid, ellagic acid, quercetin, geraniin, corilagin, and kaempferol, have been demonstrated to mitigate radiationinduced side effects. Research has also demonstrated that fruits can reduce the severity of radiationinduced mucositis in head and neck cancer patients undergoing curative treatment. Currently, there are no clinically effective non-toxic medications that are beneficial in mitigating radiation-induced ill effects. In lieu of this, for the first time, this review compiles the positive effects of fruits, phytochemicals, and their byproducts, chyawanprash and triphala, on radiation-induced damage, the mechanisms by which these effects occur, and the gaps that must be filled in order for future research to help people and the agricultural and nutraceutical industries.