钩吻素子

Koumine (0.5, 1 and 2 mg/mL) dose- and time-dependently inhibits the proliferation of MCF-7 cells, with an IC ₅₀ of 124 µg/mL at 72 h. Koumine induces apoptosis, causes cell cycle arrest at G2/M phase.
Koumine (0.5, 1 and 2 mg/mL) up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in a dose-dependent manner in MCF-7 Cells.
Koumine (25, 50, 100, and 200 μM) decreases the protein and mRNA levels of microglia M1 polarization factors in LPS-induced BV2 cells.

Koumine is less toxic, with the median lethal dose (LD ₅₀ ) of 300.0 mg/kg on Wistar rats. Koumine (0.6, 3, or 15 mg/kg/per, p.o.) exhibits antirheumatic properties in rats with adjuvant-induced arthritis (AIA) and collagen-induced arthritis (CIA).
Koumine inhibits the increase in cytokines in joint tissue and TNF-α level in serum at 15 mg/kg, and suppresses the increase in the serum level of IL-1β at 3 and 15 mg/kg.
Koumine (0.28, 7 mg/kg, s.c.) significantly reduces neuropathic pain after nerve injury. Koumine suppresses the increased Iba-1 protein level.