GYY4137 is a slow-release H2S donor with vasodilatory and antihypertensive activities. GYY4137 also exhibits anti-inflammatory and anticancer activities[1][2][3].In the concentration range of 400-800 μM, GYY4137 exhibited concentration-dependent killing of seven different human cancer cell lines (HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11, and U2OS) without affecting the survival of normal human lung fibroblasts (IMR90, WI-38)[2].In the concentration range of 0.1-0.5 mM, GYY4137 reduced LPS-induced production of nitrite (NO2), PGE2, TNF-α, and IL-6 in human synoviocytes (HFLS) and articular chondrocytes (HAC), decreased the levels and catalytic activities of inducible nitric oxide synthase (iNOS) and cyclo-oxygenase-2 (COX-2), and reduced LPS induced NF-κB activation[3].
GYY4137 动物研究
Animal study
Administered intraperitoneally at a dose of 100-300 mg/kg and administered once daily for 14 days, GYY4137 significantly reduced tumour volume in both animal models in a dose-dependent manner[2].In complete Forsythia adjuvant (CFA)-treated mice, GYY4137 (50 mg/kg, i.p.) increased knee swelling in the animals, whereas injection of GYY4137 6 hours after CFA produced an anti-inflammatory effect manifested by a decrease in synovial myeloperoxidase (MPO) and N-acetyl-β-D-glucosaminidase (NAG) activities, and a decrease in TNF-α, IL-1 β, IL-6 and IL-8 concentrations[3].GYY4137 significantly inhibited tumour growth in a subcutaneous HepG2 xenograft model by inhibiting STAT3 activation and the expression of its target genes[4].GYY4137 prevents nitrosative stress and α-synuclein nitration in a mouse model of MPTP-induced Parkinson's disease[5].
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