What is artemisinin?

“Artemisinin is a potent therapeutic substance found in sweet wormwood”

Artemisinin is a therapeutic substance found in sweet wormwood (Artemisia annua L.). that was used to treat malaria in traditional Chinese medicine for over 2000 years. When Chinese was experimenting with thousands of herbal extracts’ ability to treat malaria during the Vietnamese war, they found that the extract from the sweet wormwood leaves showed some promising result. [1]

Later this discovery was published after the war and artemisinin-derived medicine is widely used as an anti-malarial drug in the world. As malarial parasites started to develop resistant toward hydroxychloroquine and chloroquine, WHO recommended artemisinin derived drugs in combination with traditional drugs to be used to treat malaria patients. but its therapeutic abilities are being reemphasized as new efficacies of the substance is being discovered. 

Artemisinin efficacies

“Artemisinin can bolster your immune system, fight cancer, treat malaria and more”

• Most well-known Antimalarial Effect
  • Artemisinin is one of the best antimalarial substance that was ever discovered. WHO strongly recommends using artemisinin derived drugs to be used to treat malaria in combination with other traditional antimalarial drugs such as quinine, hydroxychloroquine, and chloroquine.
  • Artemisinin reacts with heme and iron which is highly abundant in the malaria parasite ( falciparum). The reaction is known to produce free radicals which lead to the death of the parasite only. [2]
• Antiviral effect 
  • Promising antiviral effects of artemisinin and its derivatives are being added by researchers [3]
  • HCMV (human cytomegalovirus)
    • Problem: This virus is also known as beta-herpesvirus. HCMV is a very common virus prevalence in 55-100% according to the British Society for immunology. Although negligible in a healthy host, it can be severe or even fatal to immunocompromised individuals or newborns. Many HCMV patients with severe symptoms are treated with current anticytomegaloviral drugs. However, these drugs are limited by toxicity, low efficiency with oral administration, and drug resistance.
    • Artemisinin: Similar effects found on malarial parasites were observed in HCMV. Researchers have shown that artemisinin and its derivatives have an antiviral effect even on GCV-resistant HCMV opening a new way for HCMV treatment [4][5].
  • All subfamilies of Herpesviruses (ɑ, β, and 𝛾)
    • These viruses are also known as Epstein-Barr virus, herpes simplex virus 1, human herpesvirus 6A. Studies are showing a promising inhibitory effect on these viruses with artemisinin and artesunate. [6]
  • Hepatitis B Virus (HBV)
    • Symptoms: There are two types of Hepatitis B Virus infections: acute and chronic. Acute infection is most likely to go away when the body heals itself, but the chronic infection may need lifelong treatment. Without the treatment, it might lead to cirrhosis, liver cancer, liver failure, and other conditions in kidneys or blood vessels. It is due to a lack of ability to fight off the diseases.
    • Despite the availability of an effective vaccine against HBV, the treatment of already infected patients has yet been fully developed. The current treatment of HBV with lamivudine shows toxicity and drug-resistance in some strains of HBV. Among many natural substances tested, artesunate (artemisinin derivative) has shown the most promising result. Although not as effective as current lamivudine treatment in test tubes, due to its high oral-bioavailability and non-toxic characteristic, it is a good candidate for synergetic treatment with the current method. [7]
  • Hepatitis C Virus (HCV)
    • Current drugs for HCV treatment also possess the same problem as HBV drugs. Artemisinin and its derivative artesunate have been tested for its efficacy in inhibiting HCV and show promising results. One of the studies shows 65% inhibition of HCV and even higher with another substance that exists in our body, hemin. [8]

• Anticancer effect
  • Artemisinin’s anticancer properties have come into the limelight of the medical community. It shows anticancer properties against various types of cancer cell lines including pancreatic cancer cells, retinoblastoma, leukemia, and more. There are numerous modes that artemisinin kills cancer cells. One is similar to the antimalarial effect. Cancer cells generally express a high level of iron and increased metabolism of heme which are known as targets for artemisinin. Moreover, it interacts with the cell system and makes the cancer cells to kill itself (apoptosis). There was a report of a few cases where the treatment of artesunate (artemisinin derivative) showing a significant reduction of tumor cells and in some cases complete clearances. [9][10][11] 

• Immunoregulatory Effect
  • Our immune system protects our body from outside pathogens through an inflammatory response. However, constant on-status of the inflammatory response can attack our own cells leading to various diseases such as type 1 diabetes, rheumatoid arthritis, and organ transplant rejection. Having an anti-inflammatory effect can help these various autoimmune diseases. Artemisinin down-regulates chemicals in cells that activate our immune system. This immunosuppressive activity prevents our immune systems from attacking our own cells. [12][13]

 

Resistance to artemisinin?

“There haven’t been any artemisinin-resistance reported”

Every drug that is injected or orally administrated is eventually secreted outside of our body, but it varies hugely by drugs. The time it takes for half of the drug entered the human bloodstream to be secreted is called the half-life. Compare to many other drugs, the half-life of artemisinin is extremely short. In a day or two, most of the artemisinin will be gone from our bloodstream. For parasites or viruses to develop resistance to drugs, it should be exposed to the drug for certain periods, but artemisinin would be already gone. That is why while malaria easily gained resistance to traditional anti-malarial drugs but haven’t acquired it on artemisinin yet. [2]

 

Is it dangerous? 

 “Toxicity of artemisinin is extreme low despites its efficacy”

Artemisinin and its derivatives are approved and recommended by the WHO. Side effects of artemisinin are mostly negligible unless exposed to a high dose for a long period. Artemisinin is currently widely used as an antimalarial drug and has undergone clinical trials with tens of thousands of patients. There are only a few reports of toxicity. Most of the side-effects were transient after stop administering artemisinin and other neurotoxic symptoms were concluded to be unrelated with the artemisinin. [2][14][15]