Parthenin

Parthenin is a pseudo-guaianolide sesquiterpene lactone found in Parthenium hysterophorus L. It has the capability to induce chromosomal aberrations in human peripheral blood lymphocytes, primarily causing chromatid breaks. Parthenin exhibits toxicity towards Salmonella typhimurium and Escherichia coli strains, although this toxicity is reduced in the presence of a metabolic activation system (S9). It acts as a feeding deterrent for sixth-instar larvae of the armyworm (Spodoptera litura) and shows insecticidal activity against adult Callosobruchus maculatus. Parthenin inhibits seed germination and seedling growth in Senna (Cassiatora) and has nematicidal effects on second-stage juveniles of the southern root-knot nematode (Meloidogyne incognita). The compound is also used in research related to cancer, malaria, amoebic infections, inflammatory diseases, and bacterial infections.

Parthenin, ranging from 0.19 to 19.06 μmole per plate, does not exhibit mutagenic effects on Salmonella typhimurium strains TA 1535, TA 1537, TA 98, and TA 100, but induces a slight revertant mutation response in strain TA 102 at 0.19 and 0.49 μmole per plate. At concentrations of 10-60 μM for 17 hours, Parthenin can cause dose-dependent chromosomal aberrations, primarily as chromatid breaks, in human peripheral blood lymphocytes, with a notable increase in polyploidy at 40 μM. When used at 100-1000 mg/L for 24-72 hours, Parthenin demonstrates moderate nematicidal activity against the second-stage juveniles (J2) of Meloidogyne incognita, with LC50 values of 862 mg/L after 48 hours and 512 mg/L after 72 hours. Parthenin shows significant antimalarial activity against multidrug-resistant Plasmodium falciparum and potential application against artemisinin-resistant strains. It exhibits amoebicidal activity against Entamoeba histolytica. Additionally, Parthenin exerts anti-inflammatory effects by reducing the expression of pro-inflammatory cytokines TNF-α, IL-1β, and IL-6 in mouse neutrophils. It possesses insecticidal activity against Plutella xylostella, Aphis craccivora, and Tribolium confusum, with varying efficacy across species. Furthermore, Parthenin displays antifungal activity against several plant pathogenic fungi by inhibiting sporangium germination, zoospore viability, and hyphal growth. At 1 μg/mL for 24 hours, Parthenin is cytotoxic to cultured bovine kidney cells, inhibiting the synthesis of RNA, DNA, and proteins by nearly 50%.

Parthenin administered intraperitoneally at doses of 4-31 mg/kg significantly increases the frequency of micronucleated reticulocytes in male and female Swiss albino mice 48 hours after administration at a dose of 31 mg/kg, with no significant effect observed at lower doses or after 72 hours. When topically applied to leaves, Parthenin exhibits moderate antifeedant activity against the sixth instar larvae of Spodoptera litura, with an ED50 of 287 mg/L in choice tests, achieving a 99% deterrence rate at a concentration of 10000 mg/L. Applied topically to the surface of Petri dishes, Parthenin shows very low insecticidal activity against adult Callosobruchus maculatus, with an LC50 of 568 mg/L after 72 hours of exposure. When used to soak seeds, Parthenin inhibits the germination and seedling growth of Cassia tora, with ID50 values of 364 mg/L for germination, 738 mg/L for hypocotyl length, and 427 mg/L for radicle length. Parthenin exhibits moderate repellent activity against Plutella xylostella (diamondback moth) with an LC50 of 1709.42 mg/L and high insecticidal activity against aphids with an LC50 of 947.87 mg/L. Additionally, Parthenin demonstrates insecticidal activity against stored grain pests and nematicidal activity against root-knot nematodes.