Artemisinin shown to kill cancer cells, especially when bound to iron

Artemisinin, a Chinese herbal compound from the plant Artemisia annua or sweet wormwood, has been shown to have significant action against cancers from brain cancer to breast cancer, especially when bound to iron. It is also proven to treat malaria, yeasts, pathogens and parasites.

Artemisinin can kill cancer cells, especially when it is bound to iron

As long ago as 2004, researchers at the University of Washington Professor Henry Lai and Dr Narendra P. Singh, were showing that artemisinin could cause cancer cell death (1). (Updated from an original article in 2011, revised in 2017 and again in 2023 by Chris Woollams)

Then followed a number of studies published in journals like Life Sciences, Cancer Letters and Anticancer Drugs, artemisinin, one of three natural compounds in the plant Artemisia annua and often called wormwood, can kill off cancer cells at a rate of 12,000 cancer cells for every healthy cell (2). In the studies, the researchers used leukemia, breast and prostate cancer cell lines. Leaves from the plant are even eaten as salad in China. Artemisinin is not toxic to healthy cells. 

In a 2008 study (3) Professor Henry Lai and the team of researchers from the University of Washington tagged artemisinin with iron (transferrin), which transports iron in the plasma and collects in cells as ferritin and showed that this could significantly reduce the growth of breast cancer tumours in vivo.

“By itself, artemisinin is about 100 times more selective in killing cancer cells as opposed to normal cells. But the tagged compound was 34,000 times more potent,” said Lai.

“We call it a Trojan horse because the cancer cell recognizes transferrin as a natural, harmless protein. So the cell picks up the compound without knowing that a bomb (artemisinin) is hidden inside.”

Transferrin is a glycoprotein and a method of transporting iron in the plasma. Once the iron reaches cells, it is stored as ferritin.

The 'bound' compound is currently being licensed by the University of Washington to Artemisia Biomedical Inc., a company that Lai, Sasaki and Narendra Singh, UW, associate professor of bioengineering, founded in Newcastle, Washington for development and commercialization of artemisinin.

“Although, human trials are at least several years away, Artemisinin is readily available today”, Sasaki said. However, already the researchers are concerned that the product they sold the license for, is being developed all too slowly! However, one of the researchers is trying to bring you an iron-based artemisinin anti-cancer protocol today - you can see how Dr Singh uses artemisinin and iron HERE.

Artemisinin and anti-cancer properties

Artemisinin has been shown to cause cancer cell death in many cancer cell lines. Artemisinin compounds have also been shown to have anti-angiogenic, anti-inflammatory, anti-metastasis, and growth inhibition effects. The problem seems that artemisinin on its own doesn't have the potency that being bound to iron gives it. As a result, the team are developing more potent and target-selective artemisinin-compounds. These include artemisinin dimers and trimers, and artemisinin hybrid compounds (4).

The artemisinin/iron bound compound seems to have significant benefits with many cancers and even brain tumours when used with 5-aminolevulinic acid, or 5-ALA. And this included drug-resistant glioblastoma, GBM (10).  The research showed that it attacked a single cellular pathway, that for porphyrin (heme) biosynthesis in vitro and in vivo.  5- is a fluorescent compound usually used before brain tumour surgery to light up the cancer so that the surgeon can remove as many cancer cells as possible with removing too many healthy cells. 

Sometimes researchers have used the artemisinin with linoleic acid. A 2021 study using both colorectal cancer cells and metastatic colorectal cancer cells, with artemisinin (ART) or Dihydroartemisinin (DHA), showed significant late cancer cell death especially as the linoleic acid levels increased. No effect was seen with healthy cells. When holotransferin was added (the iron carrier) the cancer cell death intensified. Researchers stated that levels used were perfectly achievable in human subjects with colorectal and metastatic colorectal cancer., 

Cancer cells contain very high levels of ferritin iron in their lysosomes and the more transferrin receptors in a tumour pulling the iron in, the more aggressive the cancer is. Chlorophyll (plant iron) is the cheap way of providing the iron for the artemisinin to ultimately attack. When the artemisinin attacks the iron it causes free-radicals to be produced and a degradation of the lysosomes which then leak into the cancer cell and kill it. This is not 'apoptosis' but 'ferroptosis'. Many scientists have felt since 2012 that ferroptosis is full of potential as a way of killing cancer cells but the theories have never really made their way into practice. This 'potential' was still being stated in 2022 research looking into preventing chemo-drug resistance (6). Maybe Henry Li and his team found the way to do it with artemisinin almost 20 years ago?!.

What helps artemisinin against cancer, what hinders?

Beware: Lysosome degradation caused by artemisinin, is inhibited by N acetyl cysteine, NAC, bafilomycin (antibiotic), and deferoxamine mesylate (an iron chelator). Protective enzyme AIMFP-2, or FSP1, acts independently of oxidative systems such as IVC, Glutathione or CoQ10 (7).

Resveratrol, turmeric, allicin, berberine, vitamin D, melatonin, butyrate and stilbines all increase artemisinin's activity, as does IVC (8).

And artemisinin can enhance the action of chemotherapy drugs (9).

The final word - “Artemisinin is currently FDA approved for the treatment of malaria, it’s very safe and easy to use. It’s inexpensive and works on all cancers” added Sasaki.

Go To: A review on Artemisinin

"If you are thinking of buying artemisinin, or sweet wormwood, you may like to see what Natural Selection has to offer by "CLICKING HERE " .

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References

1. Artemisinin induces apoptosis in human cancer cells; Narendra P. Singh, Henry Lai; Anticancer Res. 2004 Jul-Aug;24(4):2277-80
2. Scientists develop new cancer-killing compound from salad plant; Henry Lai et al; Oct 13 2008 UW News; 
3. Artemisinin-transferrin conjugate retards growth of breast tumors in the rat; Henry Lai et al; Anticancer Res; 2009 Oct;29(10):3807-10.
4. Development of artemisinin compounds for cancer treatment; Henry C Lai, Narendra P Singh, Tomikazu Sasaki; Invest New Drugs; 2013 Feb;31(1):230-46.
5. Artesunate induces cell death in human cancer cells via enhancing lysosomal function and lysosomal degradation of ferritin; Nai-Di Yang et al.  Journal of Biological Chemistry; 2014 Nov 28;289(48):33425-41.
6. Ferroptosis in cancer therapy: a novel approach to reversing drug resistance; Chen Zhang et al; Mol Cancer. 2022 Feb 12;21(1):47.  
7. AIFM2 blocks ferroptosis independent of ubiquinol metabolism; Enyong Dai et al; Biochem Biophys Res Commun. 2020 Mar 19;523(4):966-971.
8. Anti-malarials are anti-cancers and vice versa - one arrow two sparrows; Chanakya Nath Kundu et al; Acta Trop. 2015 Sep;149:113-27.  
9. Effects of antioxidants and pro-oxidants on cytotoxicity of dihydroartemisinin to Molt-4 human leukemia cells; Thomas Gerdhardt et al; Anticancer Res, 2015 Apr;35(4):1867-71.
10. A whole-genome scan for Artemisinin cytotoxicity reveals a novel therapy for human brain tumors; Jasmin Taubenschmid-Stowers et al; Embo Mol Med 2023
11. The Real Cytotoxic Effect of Artemisinins on Colon Cancer Cells in a Physiological Cell Culture Setting. How Composition of the Culture Medium Biases Experimental Findings; Dagmara Otto-lusarczyk, Magdalena Mielczarek-Puta, Wojciech Grabon; Pharmaceuticals (Basel). 2021 Sep 26;14(10):976.