A Review on Phytochemistry, and Pharmacological Activities of Lithospermum officinale L.

Review Article

Abstract

Lithospermum officinale L. (Boraginaceae) is used across Eurasian and regional ethnomedicinal systems for the management of urolithiasis, nephritic complications, gastrointestinal spasms, acute cutaneous trauma, and eruptive fevers. The therapeutic efficacy of this perennial herb is due to specialized secondary metabolites concentrated within subterranean roots and calcified nutlets. The main bioactive fractions consist of lipophilic monomeric and dimeric naphthoquinones (shikonin, acetylshikonin, and alkannin isomers), polyphenolic cinnamic acid derivatives (lithospermic acid, rosmarinic acid, and chlorogenic acid), flavonoids, and seed-derived polyunsaturated fatty acids characterized by unusual concentrations of stearidonic and -linolenic acids. Experimental in vitro and in vivo pharmacological evaluations indicate targeted antioxidant, anti-inflammatory, antimicrobial, burn-wound restorative, and antithyrotropic properties. The capacity of crude extracts and isolated rosmarinic acid to attenuate microglial neuroinflammation, paired with the vascular and re-epithelialization properties of naphthoquinones in cutaneous models, corroborates ancestral empirical uses. The identification of hepatotoxic 1,2-dehydropyrrolizidine alkaloids presents clear safety limitations that necessitate qualitative standardization. Resolving biomass yield fluctuations and metabolite-divergence profiles across the Lithospermeae tribe demands the integration of pharmaphylogenetic taxonomy with fungal endophyte bioprospecting. Exploiting mutualistic endophytes provides a viable biotechnological platform for producing enantiomerically pure naphthoquinones independently of natural populations