Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg mL).

β,β-Dimethylacrylalkannin is a natural product isolated from Arnebia nobilis Reichb.f, increases collagen and involucrin content in skin cells.

Monomethyl lithospermate (Lithospermic acid monomethyl ester) has potential antiviral activity, alleviating ischemic stroke injury in vivo in middle cerebral artery occlusion mice by activating PI5K Akt signaling and protecting oxygen-glucose deprivation reoxygenation-induced SHSY-3Y cells in vitro. Monomethyl lithospermate could improve the viability of SHSY-5Y cells, inhibit mitochondrial membrane potential (MMOP) collapse, and inhibit cell apoptosis. Monomethyl lithospermate also reduced the level of oxidative stress in the brain tissue of middle artery occlusion (MCAO) rats and improved nerve damage in ischemic stroke (IS) rats.

(2-Methylbutyryl)shikonin is a natural product from Lithospermum erythrorhizon Sieb. et Zucc.

(-)-5-Epilithospermoside is proposed as a potential marker of botanical origin for phacelia honey.

Shikonofuran A, a natural product, is isolated from Lithosperrrium erythrorhizon Sieb.

Acetylshikonin can effectively inhibit tumor cells, it can be used to treat hepatocellular carcinoma cells expressing hepatitis B virus X protein (HBX) by inducing ER stress , an oncoprotein from hepatitis B virus. Acetylshikonin inhibits the production of eicosanoid, is due to the attenuation of cytosolic phospholipase A(2) membrane recruitment via the decrease in [Ca(2+)](i) and to the blockade of cyclooxygenase and 5-lipoxygenase activity.