Anticancer Activity of Artemisinin and its Derivatives

Plasmodium falciparumnHighlight:artemisinin andn its derivatives (ARTs) exhibit action against viruses and other parasites such as Schistosoma or Leishmania, but also against cancer (7)nHighlight:the presence of the endoperoxide bridge and production of reactive oxygen species (ROS) is suggested as an importantn feature not only in antimalarial action but also in the fight against cancer cellsnHighlight:sesquiterpenenHighlight:Qinghao (the Chinese name for Artemisia annua)nHighlight:The first isolation of artemisinin from the herb occurred in 1972 by a group led by Youyou TunHighlight:Nobel laureate in physiology or medicine awarded in 2015 for a discoveryn of artemisininnHighlight:semi-synthetic derivatives such as artemether, dihydroartemisinin,n arteether, and artesunatenHighlight:These compounds are considered to be about five times more effective to fightn Plasmodium parasite and also the cancer cellsnHighlight:ARTs being generally hydrophobic,nHighlight:Current in vivo and in vitro studies propose numerous possible mechanisms of action. The most described and cited are: 1) oxidative stress, 2) inductionn of apoptosis, 3) inhibition of angiogenesis, 4) arrest of cell cycle at G0/G1 and 5) ferroptosisnHighlight:strong induction of ROS and reducedn proliferationnHighlight:Increased apoptosis rates and significant antiproliferative effectnHighlight:antiproliferative effect of artesunate and Wnt/β-catenin pathwaynHighlight:down-regulation of VEGF expression and suppression of angiopoietin 1 secretion induced by artesunate were reportedn in a study with multiple myeloma cellsnHighlight:G1 cell cycle arrest and downregulated cyclin-dependent kinase-4 (CDK4) gene expression by disruption of nuclear factor-ĸB (NF-ĸB)n interactions with the CDK4 promoternHighlight:decreased expression of CDK4 and cyclin D1 and an increase in a tumour suppressor protein p16 expressionnHighlight:Artesunate caused G2/M cell cycle arrest in breast cancer cells by upregulating the expression of Beclin1, initiator of autophagynHighlight:G0/G1 cell cycle arrest affecting the expression of cell cycle regulatory enzymes, such as cyclin E, CDK2, CDK4 and p27nHighlight:dihydroartemisinin inhibited the translocation and DNA-binding activity of NF-ĸBnHighlight:decreased levels of GPx4 and Ras in dihydroartemisinin-treated HNSCC cells, as both GPx4 and Ras aren important regulators of ferroptosisnHighlight:resistant cancer cell lines become sensitive by adding artemisininn and its derivatives to the conventional treatment (chemosensitization)nHighlight:Significantn increase of apoptosis, decreased Ki-67 index, decreased NF-ĸB activity and its related gene products such as c-myc, cyclinn D1, Bcl-2, Bcl-xL were manifestednHighlight:Inhibition of gemcitabine-induced NF-ĸB activation is believed to be the main mechanismn dihydroartemisinin acts in synergism with gemcitabinenHighlight:ARTs, mainly dihydroartemisinin and artesunate, possess the chemo-sensitising effectsnHighlight:The most studiedn are patients with solid tumours: colorectal carcinoma, breast cancer, hepatocellular carcinoma and lung cancernHighlight:Phases 1 and 2 are in progressnHighlight:(artesunate) and metabolite (dihydroartemisinin)nHighlight:then concentrations of salivary and plasma dihydroartemisinin correlated and proposed a possible use of saliva samples in furthern pharmacokinetic investigationsnHighlight:adverse effects such as leucopenia, neutropenia, anemia and vertigo were observed possibly related to the artesunate add-onn therapynHighlight:adverse events of the auditory systemnHighlight:vertigonHighlight:multiple preclinical and clinical studiesnHighlight:ARTs effectively reduce the growth of solid tumours by inhibitionn of angiogenesis, induction of apoptosis and ferroptosis, production of reactive oxygen species and induction of cell-cyclen arrestn]]>

About Dr. Nathan Goodyear
About Dr. Nathan Goodyear

Dr. Nathan Goodyear, a medical doctor with years of experience in the field of integrative cancer care, has announced the launch of an online training program. This program, available on his new website, will provide individuals with access to video trainings led by Dr. Goodyear himself, covering a range of topics related to integrative cancer care. These trainings will include information on the latest research and techniques in the field, as well as guidance on how to incorporate these approaches into a patient’s overall cancer treatment plan. With this online program, Dr. Goodyear hopes to make his expertise and knowledge more widely accessible, and help more people understand the benefits of integrative cancer care.


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