Isomangiferin

Isomangiferin is an orally active xanthone C-glucoside, and its chemical structure is similar to Mangiferin (HY-N0290). Isomangiferin is an effective VEGFR-2 kinase inhibitor, which can induces cell apoptosis, inhibit the growth, metastasis and angiogenesis of breast cancer. Isomangiferin exerts anti-inflammatory effects by inhibiting the HMGB1/NLRP3/NF-κB signaling pathway, thereby improving the renal function indicators of diabetic mice. Isomangiferin exhibits inhibitory effects on various bacteria and herpes simplex virus type 1 (HSV-1). Isomangiferin promotes the migration and osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs) and reduces cell apoptosis and the production of ROS by activating the AMPK/ACC pathway, thereby facilitating fracture healing^{[1][2][3][4][5]}. In Vitro:Isomangiferin inhibits HSV-1 that exceeds Acyclovir (HY-17422), Idoxuridine (HY-B0307), and Cyclocytidine (HY-N0093) in log by 0.27-0.50 in log determination and exhibits the average plaque reduction rate of 69.5%^[1].
Isomangiferin shows better antibacterial potential than Mangiferin against all the tested strain including B. subtilis, S. aureus, K. pneumoniae, S. Setubal, E. coli with MICs ≤ 250 μg/mL^[2].
Isomangiferin shows poor cytotoxicity towards Brine shrimp nauplii with a LD₅₀ of 768.92 mg/mL^[2].
Isomangiferin (2.5-10 μM, 24 h) promotes osteogenic differentiation and migration of H₂O₂-treated bone marrow mesenchymal stem cells (BMSCs), reduces apoptosis and reactive oxygen species production, and activates the AMP-activated protein kinase/acetyl-CoA carboxylase (AMPK/ACC) pathway^[3].
Isomangiferin (1 μM, 48 h) decreases the viability of breast cancer cells (MDA-MB-231, T47D, MCF7, SKBR3, 4T1) with IC₅₀s of approximately 1 μM, , while the IC₅₀ for the MCF-10A cells exceeded 100 μM^[5].
Isomangiferin (1 μM, 5 days) inhibits microvessel sprouting and vascular tubulogenesis of endothelial cells^[5].
Isomangiferin (0-5 μM, 1-36 h) inhibits migration and invasion and induces breast cancer cell apoptosis and impairs cell adhesion in MDA-MB-231 cells through VEGFR-2-mediated signaling pathway^[5].
In Vivo:Isomangiferin (10-20 mg/kg, p.o., once daily for 12 weeks) provides protection against renal injury via inhibiting HMGB1/NLRP3/ NF-κB signaling in a diabetic mouse model^[4].
Isomangiferin (10 mg/kg, i.p., once daily for a month) inhibits breast cancer growth and blocks the VEGFR-2 pathway in the xenograft model^[5].