From ancient herb to modern drug: Artemisia annua and artemisinin for cancer therapy
Abstract
Artemisia annua L. is used throughout Asia and Africa as tea and press juice to treat malaria and related symptomes (fever, chills). Its active ingredient, artemisinin (ARS), has been developed as antimalarial drug and is used worldwide. Interestingly, the bioactivity is not restricted to malaria treatment. We and others found that ARS-type drugs also reveal anticancer in vitro and in vivo. In this review, we give a systematic overview of the literature published over the past two decades until the end of 2016. Like other natural products, ARS acts in a multi-specific manner against tumors. The cellular response of ARS and its derivatives (dihydroartemisinin, artesunate, artemether, arteether) towards cancer cells include oxidative stress response by reactive oxygen species and nitric oxide, DNA damage and repair (base excision repair, homologous recombination, non-homologous end-joining), various cell death modes (apoptosis, autophagy, ferroptosis, necrosis, necroptosis, oncosis), inhibition of angiogenesis and tumor-related signal transduction pathways (e.g. Wnt/β-catenin pathway, AMPK pathway, metastatic pathways, and others) and signal transducers (NF-κB, MYC/MAX, AP-1, CREBP, mTOR etc). ARS-type drugs are at the stairways to the clinics. Several published case reports and pilot phase I/II trials indicate clinical anticancer activity of these compounds. Because of unexpected cases of hepatotoxicity, combinations of ARS-type drugs with complementary and alternative medicines are not recommended, until controlled clinical trials will prove the safety of non-approved combination treatments.
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Artemisinin and its derivatives are effective against various types of cancers and tumors, some viruses including SARS-CoV-2, tuberculosis, and many other parasites including Schistosoma sp., Leishmania sp., Borrelia burgdorferi, and Trypanosoma sp.
“Artemisinin and its derivatives are not only effective against malaria, but also against various types of cancers and tumors (Efferth 2017), some viruses (Efferth et al. 2008; Efferth 2018) including SARS-CoV-2 (Nair et al. 2021), tuberculosis (Martini et al. 2020; Zheng et al. 2017), and many other parasites including Schistosoma sp. (Munyangi et al. 2018), Leishmania sp. (Mesa et al. 2017), Borr”
From Enhancing artemisinin content in and delivery from Artemisia annua: a review of alternative, classical, and transgenic approaches (2021) · cites this paper as Efferth 2017
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“Artemisinin and its derivatives are not only effective against malaria, but also against various types of cancers and tumors (Efferth 2017), some viruses (Efferth et al.”
Background
- Authors
- Efferth, T.
- Affiliations
- Johannes Gutenberg University Mainz (DE)
- Corresponding author
- Efferth, Thomas
- ORCID
- Efferth, Thomas
- Venue
- Seminars in Cancer Biology
- Publisher
- Elsevier BV
- Published
- 2017-10
- Volume
- 46
- Pages
- 65-83
- ISSN
- 1044-579X (ISSN-L)
- OpenAlex
- W2593768764
- Cited by
- 632
- References
- 262
- Citations by year
- 2026: 42 · 2025: 70 · 2024: 93 · 2023: 94 · 2022: 94 · 2021: 74 · 2020: 80 · 2019: 46 · 2018: 25 · 2017: 13
- FWCI
- 4.56
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Seminars in Cancer Biology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Sesquiterpenes and Asteraceae Studies
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Phytochemical compounds biological activities
- Health Sciences › Medicine › Complementary and alternative medicine › Natural Compounds in Disease Treatment
- Keywords
- Artemisia annua, artemisinin, artemisinin derivatives, dihydroartemisinin, artesunate, artemether, arteether, anticancer activity, oxidative stress, reactive oxygen species, DNA damage and repair, cell death mode, ferroptosis, angiogenesis inhibition, Wnt/β-catenin signaling, AMPK signaling, metastasis, NF-κB, hepatotoxicity, complementary and alternative medicine, cancer therapy
- MeSH terms
- Humans, Neoplasm Proteins, Neoplasms, Gene Expression Regulation, Neoplastic, Oxidative Stress, Artemisia annua, Artemisinins
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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