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Shikonin used in Traditional Chinese Medicine for centuries is now targeting cancer

Naturally occurring anti-cancer compounds

By Marina T AlamanouPublished 2 years ago 3 min read
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Shikonin used in Traditional Chinese Medicine for centuries is now targeting cancer
Photo by 五玄土 ORIENTO on Unsplash

“I’m in good shape. My cancer means I have lost a lot of organs and I’m a lot lighter. I have devoted myself to yoga and I’m doing handstands.”

By Eve Ensler, an American playwright, performer, feminist, and activist

Shikonin is an active naphthoquinone, which is derived from the dried root of Lithospermum erythrorhizon (commonly called purple gromwell, red gromwell, red-root gromwell and redroot lithospermum), Arnebia euchroma (commonly known as Pink Arnebia) and Arnebia guttata. It possesses anti-oxidative, anti-inflammatory and anti-cancer activities and in traditional medicine, shikonin is used against bacterial disease and inflammation.

In 1985 a high-tech Japanese product, a biolipstick, with purely biological colorants such as shikonin was a big hit on the cosmetics market, since within a few days 2 million items were sold in Japan. The red colorant in the biolipstick was a truly biological product, and at the time it took 3–7 years before the plant Lithospermum erythrorhizon had collected a maximum of 2% of the active substance shikonin in its roots. So, the biolipstick was promoted not only for having a colorant biologically created, but also for protecting against bacteria and having anti-inflammatory properties.

Shikonin as an anti-caner agent it is effective in treating different kinds of cancers, including breast (source), prostate, ovarian and thyroid cancers, Ewing sarcoma and myelomonocytic lymphoma (Source: "Naturally occurring anti-cancer compounds: shining from Chinese herbal medicine").

Shikonin exerts anti-cancer effects mainly by inducing

  • apoptosis,
  • necroptosis,
  • autophagy,
  • cell cycle arrest, and
  • by inhibiting cell proliferation, growth and metastasis.

It has been reported that shikonin inhibits cell growth by inducing cell cycle arrest and promoting apoptosis in human non-small-cell lung carcinoma, gallbladder, esophageal cancer and epidermoid carcinoma cell lines.

It can also induce necroptosis (an alternative mode of regulated cell death mimicking features of apoptosis and necrosis) via autophagy (Source) in human non-small-cell lung carcinoma cells; and through ROS overproduction in human naso-pharyngeal carcinoma and glioma cells. Moreover, shikonin induces autophagy in human melanoma, pancreatic cancer and hepatocellular carcinoma cells and can suppress metastasis in human non-small-cell lung carcinoma cells.

Shikonin is also shown to modulate the function of the immune system.

By Drew Harbour on Unsplash

For example, it can enhance the proliferation of NK cells (a type of cytotoxic lymphocyte critical to the innate immune system that belong to the rapidly expanding family of innate lymphoid cells) and their cytotoxicity to human colorectal cancer cells. And can also bind directly to heterogeneous nuclear ribonucleoprotein A1 (hnRNPs are RNA binding proteins) to induce immunogenic cell death (any type of cell death eliciting an immune response) in human breast cancer cells.

Anti-cancer synergistic effects of combined treatments with shikonin.

Shikonin can enhance the pro-apoptotic effect of taxol (Paclitaxel, sold under the brand name Taxol among others, is a chemotherapy medication) in human breast cancer cells, and this combination improves mice survival and inhibits tumour growth in breast cancer xenograft mice.

Shikonin can also potentiate the anti-cancer effects of gemcitabine (brand name including Gemzar, is a chemotherapy medication) through NF-kB suppression (a master regulator that mediates a crosstalk between inflammation and cancer at multiple levels) in human pancreatic cancer cells.

And can also promote the efficacy of adriamycin (Doxorubicin, sold under the brand name Adriamycin among others, is a chemotherapy medication) in lung cancer and osteosarcoma cells, and can enhance sensitisation to cisplatin (a chemotherapy medication) in colorectal cancer cells.

Moreover, the combined treatment of shikonin and paclitaxel reverses multidrug resistance (MDR), a phenomenon by which after exposure to a chemotherapeutic agent cancer cells develop resistance and simultaneous cross-resistance to a wide range of functionally and structurally unrelated chemotherapeutic drugs, in human ovarian cancer cells.

So far, the single or combined therapies with shikonin have shown promising anti-cancer effects both in vitro and in vivo, and pre-clinical data have confirmed its therapeutic use in cancer treatment, consequently, clinical trials will be carried out to further confirm its safety and efficacy in humans.

For example, when a shikonin mixture was used for 19 cases of later-stage lung cancer who were not the candidates for operation, radiotherapy and chemotherapy, the clinical observation showed that shikonin mixture could inhibit the growth of lung cancer (by 25% in diameter) and improved the immune function of the body. Moreover, it had no harmful effects on peripheral blood picture, heart, kidney and liver. The conclusion was that the shikonin mixture is safe and effective for later-stage lung cancer.

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Marina T Alamanou

Life Science Consultant #metaphysicalcells

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