Isorhapontigenin

Isorhapontigenin is an orally active polyphenol. Isorhapontigenin can be isolated from grapes. Isorhapontigenin induces Autophagy, upregulates the PPAR-α/PGC-1α/CPT-1A signaling pathway, inhibits the release of IL-6 and CXCL8, suppresses the transcriptional activity of NF-κB, and reduces the production of ROS. Isorhapontigenin enhances the activity and stability of PPARγ, upregulates FOXO1 protein, and inhibits MMP-2. Isorhapontigenin exerts anti-inflammatory and antioxidant effects. Isorhapontigenin alleviates Acetaminophen (HY-66005)-induced liver injury and ameliorates diabetes. Isorhapontigenin exhibits anticancer activity against bladder cancer^{[1][2][3][4][5][6]}. In Vitro:Isorhapontigenin (1.25-40 μM; 24 h) induces autophagy in a dose-dependent manner in UMUC3, T24T, and HeLa cells, and this autophagy contributes to its inhibition of anchorage-independent growth of UMUC3 cells^[1].
Isorhapontigenin (10 μM; 12 h) attenuates Acetaminophen (HY-66005)-induced FAO dysregulation in AML12 cells, upregulating PPAR-α/PGC-1α/CPT-1A signaling^[2].
Isorhapontigenin (1-100 μM; 1 h pre-incubation + 24 h stimulation, 1 h pre-incubation + 10-60 min stimulation) inhibits IL-6 and CXCL8 release from primary human airway epithelial cells (healthy and COPD) and A549 cells, with IC₅₀ values for IL-6 of 17.3-19.7 μM, and suppresses NF-κB, AP-1, and PI3K/Akt/FoxO3A signaling pathways^[3].
Isorhapontigenin (5-15 μM; 12 h pretreatment + 12 h LPS stimulation) exerts anti-inflammatory and antioxidant effects on LPS-challenged RAW264.7 cells by reducing pro-inflammatory mediator and ROS production^[4].
Isorhapontigenin (25 μM; 0-12 h) increases PPARγ activity and stability in 3T3-L1 cells by reducing inhibitory phosphorylation and decelerating proteasomal degradation^[5].
Isorhapontigenin (2.5-20 μM; 6-18 h) induces dose- and time-dependent upregulation of FOXO1 protein expression in UMUC3 and T24T human invasive bladder cancer cells^[6]. In Vivo:Isorhapontigenin (150 mg/kg) markedly inhibits xenograft tumor growth in nude mice injected with T24T cells^[1].
Isorhapontigenin (25-50 mg/kg; i.g.; once
daily for three consecutive days or 1 h after APAP administration) alleviates Acetaminophen (HY-66005)-induced liver injury in mice^[2].
Isorhapontigenin (51.6 mg/kg; p.o.; daily; 7 days) effectively ameliorates LPS-induced acute lung injury in mice by reducing inflammation and oxidative stress^[4].
Isorhapontigenin (25 mg/kg; i.p.; daily; 5 weeks) improves diabetes in mice via regulating the activity and stability of PPARγ in adipocytes^[5].