Table 1: The main effects of artemisinin derivatives.

NameMain functionsMechanismAdverse events

ArteetherAntiparasitesPlasmodiumInducing iron-dependent free radicals’ generationAnorexia
Cardiovascular symptom
Immunosuppressive activity neurotoxicity
SchistosomaReducing glycogen content and alkaline phosphatase activity
Toxoplasma gondiiUnknown
AnticancerTumor of the central nervous systemInducing iron-dependent cell death
AntifungiCryptococcus neoformansUnknown

Artelinic acidAntiparasitesPlasmodiumUnknownAnemia
Vascular irritation

Artemether AntiparasitesPlasmodiumIncreasing production of reactive oxygen intermediates and reactive nitrogen intermediates Anemia
Clastogenic potential
Distal tubular ectasia
Endocrine disruption
Fetal growth retardation
Flattened epithelium in the kidney
Haemolytic anemia
Hepatocellular hypertrophy
High liver weight
Immunosuppressive activity
Increases in hemoglobin levels
Meningeal inflammation
Prolonged QT interval
Reduction in fetal body weight
Reduced oxytocin-induced contraction of uterine tissues
Slight damage to the proprius layer lamina of intestinal villi
Suppression of humoral responses
Transient focal vesicle degeneration of the liver
Acanthamoeba castellaniiBe used as a hosphoglycerate dehydrogenase inhibitor
Schistosoma(1) Affecting both carbohydrate and protein metabolism of schistosomes;
(2) By inhibition of GST and SOD enzymes, leading to increased schistosome susceptibility to oxidant attacks
Toxoplasma gondiiBy affecting the glucose-6-phosphatase of T. gondii, resulting in the energy metabolism of the parasite
AnticancerPituitary macroadenomaUnknown
GliomaInhibiting the migration, invasiveness, expression of MMP-2/MMP-9 and p-Akt significantly while also promoting the apoptosis of tumor cells
Anti-inflammationNeuroinflammationInducing Nrf2 expression which results in the anti-inflammatory effect

ArtemisininAntiparasitesPlasmodiumGenerating highly reactive carbon-centered radicals via endoperoxide cleavage Anemia
Cholestatic liver injury
Genital system injury
Immunosuppressive activity
Toxoplasma gondii(1) Inhibiting the intracellular growth of T. gondii in vitro by imposing oxidative stress within the cells
(2) Perturbing calcium homeostasis in T. gondii
TrypanosomaInhibiting calcium-dependent ATPase activity in T. cruzi membranes
AnticancerBrain tumor(1) Bringing about reactive oxygen species-mediated action
(2) Inducing iron-dependent cell death
Anti-inflammationAlzheimer’s diseaseSuppressing NF-κB activity and NALP3 inflammasome activation
AntifungiC. neoformansUnknown
C. albicansUnknown
AntivirusCytomegalovirusModulating cell cycle through CDKs and pRb
Herpes virusUnknown
OthersSchizophreniaReducing levels of antibodies to gliadin
Neurite outgrowthActivating ERK and p38 MAPK signaling pathways
Vascular(1) Inhibiting VSMC migration through down-regulation of ERK1/2 and MMP9 phosphorylation
(2) Inhibiting the inflammation of VSMCs induced by TNF-α through ROS-mediated NF-κB signal pathway

ArtesunateAntiparasitesPlasmodium(1) Inhibiting the activity of the cytochrome oxidase
(2) Increasing oxidant stress on the infected red cells
Cardiovascular system
Contragestational action
Immunosuppressive activity
SchistosomaReducing expression of schistosome thioredoxin glutathione reductase and cytochrome c peroxidase
Toxoplasma gondiiDistorting in tachyzoites’ shape, peeling, erosions and discontinuity in areas of surface membrane
AnticancerGliomaInducing oxidative DNA lesions and DNA double-strand breaks
NeuroblastomaInducing apoptosis and reactive oxygen species in neuroblastoma cells
SchwannomaInducing cell death dependent on necroptosis
NeurofibromatosisBinding to and degrading translationally controlled tumor protein
Growth hormone adenomaInhibiting proliferation and inducing apoptosis by caspase-dependent pathways
Anti-inflammationNeuroinflammatoryInfluencing NF-kB, p38 MAPK and Nrf2/ARE-dependent signal pathway
AntivirusCytomegalovirusInterfering with the NF-κB pathway by targeting RelA/p65
Ebola virusUnknown
Epstein-Barr virusBlocking viral immediate early protein synthesis
Herpes virusUnknown
PolyomavirusLeading to cytostatic effects on the host cell
OthersSubarachnoid hemorrhageProtecting BBB via S1P1/PI3K pathway after subarachnoid hemorrhage
Vascular(1) Inhibiting VSMCs proliferation by disturbing DNA replication, inducing cell apoptosis and blocking cell cycle in G0/G1 phase
(2) Inducing apoptosis of endothelial cells via an iron/ROS-dependent p38 MAPK-mitochondrial pathway
(3) Inhibiting NF-κB nuclear translocation and the subsequent expression of ICAM-1

DihydroartemisininAntiparasitesPlasmodium(1) Generating highly reactive carbon-centered radicals via endoperoxide cleavage
(2) Causing the pigment of P. berghei to clump
Contragestational effects
Erythroid cell differentiation
Immunosuppressive activity
Suppression of humoral responses
Naegleria fowleriUnknown
SchistosomaCausing damage to the genital system of worms
Toxoplasma gondiiUnknown
AnticancerNeuroblastomaDamaging mitochondrial cristae and endoplasmic reticulum
Glioma(1) Inhibiting the Raf/ERK/MEK, ADAM17, PI3K/AKT pathways and activating caspase-3
(2) Increasing the reactive oxygen species and inhibiting hypoxia inducible factor-1α activation
OthersNeurite outgrowthActivating ERK and p38 MAPK signaling pathways
Vascular(1) Inhibiting VEGF-induced EC migration via a p38 MAPK-independent pathway
(2) Repressing the NF-κB pathway

Toxoplasma gondiiUnknown

AnticancerTumor of the central nervous systemInducing iron-dependent cell death

ArtemisoneAntiparasitesPlasmodiumResulting in antimalarial activities by the Fe2+-mediated decomposition, PfATP6 bindingEmbryotoxicity
Cardiac ventricular septal defects
Vascular variation
Toxoplasma gondiiUnknown

Artefenomel (OZ439)AntiparasitesPlasmodiumActivating hemoglobin degradationUnknown

Arterolane (OZ277)AntiparasitesPlasmodiumActivating hemoglobin degradationEmbryotoxicity

Arteanuin BAnticancerTumor of the central nervous systemInducing iron-dependent cell deathUnknown
OthersVascularInhibiting immune mediators of angiogenesis

SM735Anti-inflammationImmunosuppressive activityInhibiting the proliferation of splenocytes, proinflammatory cytokine production, T cell-mediated delayed-type hypersensitivity (DTH) and B-cell-mediated QHS reactionsUnknown

SM905Anti-inflammationImmunosuppressive activityInhibiting T cell activation, NO and proinflammatory cytokine production by suppressing and Ras activation, MAPK and NF-kappaB pathwaysUnknown

SM933Anti-inflammationAutoimmune encephalomyelitisInvolving the NF-kB and the Rig-G/JAB1 signaling pathwaysUnknown

SM934Anti-inflammationAutoimmune encephalomyelitis
Immunosuppressive activity
Inducing Treg differentiation and expansion
Inhibiting T cell activation

Artemisinin dimer 1AnticancerTumor of the central nervous systemInducing iron-dependent cell deathUnknown

Artemisinin dimer 2AnticancerTumor of the central nervous systemInducing iron-dependent cell deathUnknown

Artemisinin dimer hemisuccinateAnticancerTumor of the central nervous systemInducing iron-dependent cell deathUnknown

Artesunate derivativeAnticancerTumor of the central nervous systemInducing iron-dependent cell deathUnknown



10-Aminoethylether derivatives of artemisininAntiparasitesPlasmodiumUnknownUnknown