Cited by 632Sesquiterpenes and Asteraceae StudiesPhytochemical compounds biological activitiesNatural Compounds in Disease Treatment

From ancient herb to modern drug: Artemisia annua and artemisinin for cancer therapy

Efferth, Thomas·2017·Seminars in Cancer Biology

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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Crossref · 10.1016/j.semcancer.2017.02.009

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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”

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Authors
Efferth, T.
Affiliations
Johannes Gutenberg University Mainz (DE)
Corresponding author
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

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