Agrobacterium rhizogenes–mediated hairy root culture of Aerva lanata (L.) Juss. ex Schult for enhanced production of 10-methoxycanthin-6-one and its multi-target therapeutic activities
摘要
The rising requirement for plant-derived bioactive molecules has driven interest in sustainable production. In the present investigation, biosynthetic enhancement of pharmacologically relevant secondary metabolites was achieved using Aerva lanata, a therapeutic species with established ethnopharmacological relevance but limited utilization. Comparative evaluation of five Agrobacterium rhizogenes strains identified R1000 as the most effective, producing a transformation frequency of 86.2 ± 0.2% in leaf explants. The resulting hairy roots displayed rapid proliferation and compact growth in Murashige and Skoog liquid medium containing 50.0% of the standard macro- and micronutrient levels, resulting in enhanced biomass production and elevated metabolite levels. Hairy root cultures induced via Agrobacterium rhizogenes showed higher levels of levels of methylaervine (10-methoxycanthin-6-one) reaching 72.9 ± 0.2 µg mL⁻1 in leaf-derived transformed roots, outperforming callus (47.7 ± 0.4 µg mL⁻1) and node-derived roots (41.0 ± 1.0 µg mL⁻1). The elicited compounds separated by chromatography techniques showed notable therapeutic effectiveness across the biochemical assays performed. The methylaervine exhibited potent α-amylase inhibitory activity (IC₅₀: 34.4 ± 0.6 µg mL⁻1), effective pancreatic lipase inhibition (IC₅₀: 7.0 ± 0.3 µg mL⁻1), and robust anti-inflammatory activity based on protein denaturation inhibition (IC₅₀: 42.1 ± 0.9 µg mL⁻1). In comparison with the crude extracts, the purified compound methylaervine exhibited consistently greater biochemical activity, highlighting the enhanced pharmacological potential of metabolites obtained from hairy root cultures. Enzyme inhibition studies demonstrated effectiveness against pancreatic lipase and α-amylase, along with minimal hemolytic activity, indicating potential anti-diabetic, anti-obesity, and anti-inflammatory applications. To date, there are no published reports on multi-target inhibitory properties of methylaervine, making this the first systematic evaluation of its activity across these biological targets. Overall, this study presents a scalable, sustainable, and high-yielding biological production system for methylaervine and related phytochemicals, with potential applications in the biopharmaceutical, nutraceutical, and functional food industries.