Shikonin and its derivatives: a patent review

Abstract

At present, screening for anticancer shikonin derivatives is based on cellular level to find compounds with stronger cytotoxicity. Though several compounds have been discovered with striking cytotoxicity in vitro, however, no selectivity was observed and undoubtedly, the further outcomes have been disappointing because of their great damage to normal cells. Meanwhile, the presumed mechanisms of action are also established in terms of their cytotoxicity. From a pharmacological point of view, most of the shikonin derivatives are at an early stage of their development, and thus it is difficult to determine the exact effectiveness in cancer treatment. With research in this field going deeper, it can be expected that, despite the difficulties, shikonin derivatives as potential anticancer agents will soon follow.

TIPE2 Mediates the Suppressive Effects of Shikonin on MMP13 in Osteosarcoma Cells

“…High-dose Shikonin induces cancer cell necroptosis in OS, while delivery of high-dose Shikonin locally into the OS may be challenging and could have potent side-effects [23][24][25]. Thus, in our previous study and here, we analyzed the effects of low-dose Shinkonin on the invasiveness of OS, as well as the underlying mechanisms.…”

“…Shikonin is a purified constituent from a Chinese medicinal herb Lithospermum erythrorhixon [23][24][25]. Shikonin has demonstrated anti-tumor potent, in which it induces cancer cell apoptosis and necroptosis [23][24][25].…”

“…Shikonin has demonstrated anti-tumor potent, in which it induces cancer cell apoptosis and necroptosis [23][24][25]. Recently, we reported that high-dose of Shikonin had prompt but profound anti-tumor effect on both primary and metastatic OS, through inducing RIP1 and RIP3-dependent cancer cell necroptosis [26].…”

Shikonin inhibits invasiveness of osteosarcoma through MMP13 suppression

“…Shikonin has been found to have anti-tumor effect through inducing cancer cell apoptosis and necroptosis [32][33][34]. Recently, we reported that high dose of shikonin had prompt but profound anti-tumor effect on both primary and metastatic OS, through inducing RIP1-and RIP3-dependent cancer cell necroptosis [35].…”

“…Shikonin is an effective constituent that was purified from Lithospermum erythrorhizon, a Chinese medicinal herb [32][33][34]. Shikonin has been found to have anti-tumor effect through inducing cancer cell apoptosis and necroptosis [32][33][34].…”