Sophocarpine (monohydrate)

Sophocarpine monohydrate is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine monohydrate upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine monohydrate inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine monohydrate can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine monohydrate has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage^[1][2][3][4]. In Vitro:Sophocarpine monohydrate (0.5-4 mM; 24-48 h) inhibits cell viability, proliferation and migration, induces cell cycle G0/G1 arrest and apoptosis, upregulates PTEN and downregulates PI3K/Akt signaling pathways in glioblastoma cells (U251, C6)^[1].
Sophocarpine monohydrate (0.4 mM; 24-72 h) inhibits cell proliferation and migration, downregulates MEK/ERK phosphorylation and VEGF-A/C/D secretion, and reduces N-cadherin and MMP-9 expression in colorectal cancer cells (HCT116, SW620)^[2].
Sophocarpine monohydrate (50-100 μg/mL; 24 h) inhibits LPS-induced NO, TNF-α, and IL-6 production in RAW 264.7 macrophages, downregulates iNOS and COX-2 protein expression, and inhibits NF-κB activation and p38 and JNK phosphorylation in RAW 264.7 macrophages^[3].
Sophocarpine monohydrate (1-5 μM; 24 h pretreatment + 12 h DOX cotreatment) reduces ROS levels in H9C2 cardiomyocytes, upregulates Nrf2/HO-1 signaling, inhibits DOX (HY-15142A)-induced Bax and cleaved-caspase-3 expression, and upregulates Bcl-2 in H9C2 cardiomyocytes^[4].
In Vivo:Sophocarpine (35 mg/kg; intraperitoneal injection; once every 2 days; 2 weeks) monohydrate inhibits tumor growth, upregulates PTEN expression, downregulates Akt phosphorylation, and induces tumor cell apoptosis in BALB/c nude mouse subcutaneous and orthotopic glioma transplantation models^[1].
Sophocarpine (10-30 mg/kg; intraperitoneal injection; twice a week; 4 weeks) monohydrate improves cardiac function, reduces CK, CK-MB, and LDH levels, and alleviates oxidative stress and cardiomyocyte apoptosis in a DOX (HY-15142A)-induced cardiac injury model in C57BL/6J mice^[4].