Pteryxin

Pteryxin ((+)-Pteryxin) is an orally active multi-target inhibitor that targets NF-κB, MAPK, NLRP3 inflammasome, and Nrf2/ARE pathways. Pteryxin is also a BChE inhibitor (IC₅₀=12.96 μg/mL) with a low inhibitory efficiency on AChE. Pteryxin inhibits the Ca²⁺-calcineurin-NFATc1 pathway by blocking NF-κB/MAPK signaling, inhibiting NLRP3 inflammasome activation, and reducing ROS generation, and activates Nrf2-mediated antioxidant enzyme expression. Pteryxin has anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin can be used in the study of inflammatory diseases, osteoporosis, diabetes, and Alzheimer's disease^{[1][2][3][4][5]}. IC50 & Target:IC50: 12.96 μg/mL (BChE)^[5] In Vitro:MTT cell viability assay:
Pteryxin (5-20 μM; 24 h) has no significant toxicity to RAW264.7 macrophages and BMMs osteoclast precursor cells^[1][2].
ELISA inflammatory factor detection:
[1].
WB protein analysis:
Pteryxin (5-20 μM; 24 h) concentration-dependently downregulates the expression of iNOS, COX-2, p-p38/p-ERK/p-JNK, p-p65 and NLRP3/ASC/Caspase-1 p20 proteins in RAW264.7 cells, and inhibits the expression of NFATc1/c-FOS/CTSK proteins in BMMs cells^[1][2].
IF immunofluorescence:
Pteryxin (20 μM; 24 h) blocks NF-κB p65 nuclear translocation and NLRP3/ASC speck formation in RAW264.7 cells, and reduces F-actin ring area and NFATc1 nuclear localization in BMMs cells^[1][2].
qPCR gene expression:
Pteryxin (5-20 μM; 24 h) upregulates antioxidant genes such as HO-1, GCLC, and Trxr1 in MIN6 islet cells, and downregulates Acp5/Mmp9/Dc-stamp^[2][3] in BMMs cells^[2][3].
In Vivo:Acute lung injury (ALI) model:
Pteryxin (5/10 mg/kg; intraperitoneal injection; once a day; 3 days) significantly attenuates LPS (5 mg/kg, i.t.)-induced lung inflammation in C57BL/6 mice, reduces lung wet/dry weight ratio, myeloperoxidase (MPO) activity, inflammatory cell infiltration in bronchoalveolar lavage fluid (BALF), and IL-6/TNF-α levels^[1].
Osteoporosis (OVX) model:
Pteryxin (10 mg/kg; oral; once a day; 8 weeks) significantly inhibits bone loss in ovariectomized C57BL/6 female mice, increases bone mineral density and trabecular number, reduces osteoclast number, and downregulates serum TRACP-5b and CTX-1 levels^[2].
Diabetic nephropathy (DN) model:

Pteryxin (20 mg/kg; gavage; once daily; 12 weeks) improves STZ-induced renal function in db/db mice, reduced urine protein, serum creatinine and urea nitrogen, alleviates glomerular mesangial proliferation and fibrosis, and inhibits renal NF-κB activation and TGF-β1 expression^[3].