Germacrone

Germacrone is a sesquiterpene compound with multiple biological activities. Germacrone inhibits the H1N1 and H3N2 influenza A virus and the influenza B virus. Germacrone blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone inhibits 5α-reductase and has anti-androgenic effect. Germacrone has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone also has antioxidant activity^{[1][2][3][4][5]}. IC50 & Target:Influenza virus^[1] In Vitro:Germacrone (0-2.0 μM, 48 h) inhibits the neuraminidase activity of A/PR/8/34(H1N1) (EC₅₀: 6.03/2.66 μM), A/human/Hubei/1/2009(H1N1) (EC₅₀: 5.59/2.9 μM), A/human/Hubei/3/2005(H3N2) (EC₅₀: 3.82/2.15 μM), Influenza B virus (EC₅₀: 6.30/2.33 μM), and A/WSN/33/S31N(H1N1) (EC₅₀: 7.12/4.78 μM) virus strains in MDCK cells and A549 cells^[1].
Germacrone (0-400 μM, 24-72 h) inhibits the proliferation of breast cancer cell lines MDA-MB-231 cells and MCF-7 cells in a dose-dependent manner^[2].
Germacrone (0-400 μM, 24 h) increases the release of LDH (66.85%; 72.76%) but decreases the mitochondrial membrane potential (ΔΨm) in MDA-MB-231 cells and MCF-7 cells^[2].
Germacrone (0-200 μM, 24 h) induces cell cycle arrest in G0/G1 phase (71.24%; 77.08%) and G2/M phase (15.89%; 12.36%) in MDA-MB-231 cells and MCF-7 cells in a dose-dependent manner^[2].
Germacrone (0-200 μM, 24 h) induces apoptosis in MDA-MB-231 cells^[2].
Germacrone (0-200 μM, 24 h) increases the release of mitochondrial cytochrome c and activates the caspases pathway^[2].
Germacrone (0.5 mg/mL, 30 min) inhibits the activity of rat liver 5α-reductase (65.7%, IC₅₀: 0.42 mg/mL)^[5].
Germacrone (0.01-10 μM, 96 h) inhibits testosterone-induced LNCaP cell growth in a concentration-dependent manner^[5].
In Vivo:Germacrone (50-100 mg/kg, i.v., once a day for 6 days) inhibits viral activity in 5 LD₅₀ influenza virus (A/Puerto Rico/8/34) infected mice^[1].
Germacrone (20 mg/kg, p.o., once a day for 3 weeks) reduces the levels of Th1 cytokines (TNF-α and IFN-γ) and increases Th2 cytokines (IL-4) in serum, synovial tissue and spleen of mice in collagen-induced arthritis (CIA) model^[3].
Germacrone (20 mg/kg, p.o., once a day for 3 weeks) inhibits NF-κB activation in synovial tissue of mice in CIA model^[3].
Germacrone (5-20 mg/kg, i.p.) improves neurological dysfunction and neurological injury in controlled cortical impact (CCI) model mice; inhibits the activity of microglia, the expression of proinflammatory factors TNF-α, IL-1β, IL-6 and oxidative stress in CCI mice; also inhibits NF-κB and induces Nrf2 pathway to exert anti-inflammatory and antioxidant effects^[4].
Germacrone (3-100 μg, topical administration, 4 weeks) inhibits testosterone-stimulated lumbar gland growth in castrated male rats (79-82%)^[5].