From Ethnopharmacology to Drug Discovery: The Therapeutic Potential of <i>Anisomeles indica</i>

BACKGROUND: Anisomeles indica (Lamiaceae) is a traditional medicinal plant widely used in the treatment of inflammatory and systemic disorders. Increasing evidence suggests that it represents a rich source of bioactive natural products with broad pharmacological potential. AIMS: This review aims to systematically summarize the phytochemistry, pharmacological activities, safety profiles, and recent advances in drug discovery of Anisomeles indica, with a particular focus on its major diterpenoid constituent, ovatodiolide (OVA). MATERIALS AND METHODS: A comprehensive literature search was conducted across multiple databases, including PubMed, Web of Science, Scopus, and CNKI, covering studies related to ethnopharmacology, phytochemistry, pharmacology, toxicology, and pharmacokinetics of Anisomeles indica and its constituents. RESULTS: Phytochemical studies have identified diverse constituents, particularly macrocyclic diterpenoids such as OVA, which exhibit extensive biological activities including anti-inflammatory, anti-cancer, antiviral, antibacterial, antioxidant, and immunomodulatory effects. Mechanistically, these effects involve key signaling pathways such as NF-κB, STAT3, PI3K/Akt/mTOR, β-catenin, and TGF-β signaling. Despite promising bioactivities, OVA is limited by rapid clearance and poor oral bioavailability. To overcome these limitations, medicinal chemistry efforts have led to the development of optimized derivatives, such as NMP-diepoxyovatodiolide and ACT004, which demonstrate improved pharmacokinetics, enhanced safety, and robust efficacy in preclinical models. DISCUSSION: The pharmacological diversity of Anisomeles indica arises from its complex chemical composition and multi-target mechanisms. However, challenges remain, including variability in extract composition, insufficient clinical validation, and suboptimal pharmacokinetic properties of key compounds. CONCLUSION: Anisomeles indica represents a promising source of multifunctional therapeutic agents. Continued efforts in standardization, mechanistic validation, and clinical translation, together with the development of pharmacokinetically optimized derivatives, are essential to fully realize its potential as a platform for next-generation drug discovery.