<p class="first" id="d900142e148">Shikonin is the major bioactive component extracted
from the roots of Lithospermum
erythrorhizon which is also known as "Zicao" in Traditional Chinese Medicine (TCM).
Recent studies have shown that shikonin demonstrates various bioactivities related
to the treatment of cancer, inflammation, and wound healing. This review aimed to
provide an updated summary of recent studies on shikonin. Firstly, many studies have
demonstrated that shikonin exerts strong anticancer effects on various types of cancer
by inhibiting cell proliferation and migration, inducing apoptosis, autophagy, and
necroptosis. Shikonin also triggers Reactive Oxygen Species (ROS) generation, suppressing
exosome release, and activate anti-tumor immunity in multiple molecular mechanisms.
Examples of these effects include modulating the PI3K/AKT/mTOR and MAPKs signaling;
inhibiting the activation of TrxR1, PKM2, RIP1/3, Src, and FAK; and regulating the
expression of ERP57, MMPs, ATF2, C-MYC, miR-128, and GRP78 (Bip). Next, the anti-inflammatory
and wound-healing properties of shikonin were also reviewed. Furthermore, several
studies focusing on shikonin derivatives were reviewed, and these showed that, with
modification to the naphthazarin ring or side chain, some shikonin derivatives display
stronger anticancer activity and lower toxicity than shikonin itself. Our findings
suggest that shikonin and its derivatives could serve as potential novel drug for
the treatment of cancer and inflammation.
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