Biosynthesis and Therapeutic Applications of Picrosides in Medicinal Plants
Summary
Picrosides are iridoid glycosides predominantly found in species of the genus Picrorhiza and related taxa. Biosynthesis commences with the non-mevalonate (MEP) pathway yielding monoterpenoid precursors, which converge with shikimate-derived phenylpropanoids to form the cyclopentanoid iridoid scaffold. Subsequent hydroxylation, glycosylation and acylation steps, often mediated by family 1 glycosyltransferases, generate the characteristic picroside I and II variants. Tissue-specific expression of key enzymes and intercellular metabolite transport shape the spatial complexity of picroside accumulation. Therapeutically, picrosides exhibit anti-inflammatory, hepatoprotective, neuroprotective, antidiabetic and anticancer activities. Advances in analytical methods and metabolic engineering are beginning to unlock sustainable production routes and to refine pharmacokinetic profiles in preparation for clinical translation.
Research from Nature Portfolio
Recent studies have demonstrated that supplying immediate precursors—cinnamic acid and catalpol—to shoot cultures profoundly enhances picroside-I accumulation. Co-feeding of both precursors elicited a more than fourfold increase in product yield, indicating synergistic activation of both phenylpropanoid and iridoid branches. Limitation of flux by individual precursor scarcity was shown to induce feedback inhibition on rate-limiting enzymes, pinpointing metabolic bottlenecks. These findings provide a blueprint for future metabolic-engineering strategies aimed at boosting picroside yields in vitro and reducing pressure on wild populations.
Biosynthesis and Therapeutic Applications of Picrosides in Medicinal Plants publication trend
The graph below shows the total number of articles in biosynthesis and therapeutic applications of picrosides in medicinal plants across all publications each year (not limited to Nature Index journals).
Technical terms
Picroside: An iridoid glycoside characterised by a cyclopentanoid monoterpenoid core linked to glucose and aromatic acids.
Iridoid glycoside: A class of plant secondary metabolites derived from monoterpenoid pathways, often with sugar moieties.
MEP pathway: The methylerythritol phosphate route in plastids that synthesises isoprenoid precursors for monoterpenes.
Phenylpropanoid pathway: A route originating from phenylalanine that yields aromatic compounds such as cinnamic and ferulic acids.
Glycosyltransferase: An enzyme that attaches sugar units to aglycones, modulating solubility and bioactivity of natural products.
Metabolic flux: The rate of flow of metabolites through a biosynthetic pathway, which can be altered by precursor availability or enzyme activity.
References
- Integrative analysis of metabolite and transcriptome reveals the biosynthetic pathway and candidate genes for iridoid glycoside biosynthesis in Neopicrorhiza scrophulariiflora (Pennell) D.Y.Hong. Frontiers in Plant Science (2025).
- Exogenous feeding of immediate precursors reveals synergistic effect on picroside-I biosynthesis in shoot cultures of Picrorhiza kurroa Royle ex Benth. Scientific Reports (2016).
- Modular Design of Picroside-II Biosynthesis Deciphered through NGS Transcriptomes and Metabolic Intermediates Analysis in Naturally Variant Chemotypes of a Medicinal Herb, Picrorhiza kurroa. Frontiers in Plant Science (2017).
- Simultaneous Determination of Five Iridoids of Picrorhiza scrophulariiflora in Rat Plasma Using UHPLC-ESI-MS/MS. Molecules (2023).
- Molecular Characterization of UGT94F2 and UGT86C4, Two Glycosyltransferases from Picrorhiza kurrooa: Comparative Structural Insight and Evaluation of Substrate Recognition. PLOS ONE (2013).
- Picrorhiza kurroa Enhances β-Cell Mass Proliferation and Insulin Secretion in Streptozotocin Evoked β-Cell Damage in Rats. Frontiers in Pharmacology (2017).
- Neuroprotective Properties of Picroside II in a Rat Model of Focal Cerebral Ischemia. International Journal of Molecular Sciences (2010).
- HPTLC Analysis of Bioactivity Guided Anticancer Enriched Fraction of Hydroalcoholic Extract of Picrorhiza kurroa. BioMed Research International (2015).
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