coptisine

Coptisine is an isoquinoline alkaloid of the protoberberine group, commonly isolated from Coptis chinensis (Chinese goldthread) and related plants in the Ranunculaceae family. It is one of several major alkaloids found in the rhizomes of these species, often alongside berberine, palmatine and jatrorrhizine. In traditional medicine, plant preparations containing coptisine have been used for fever, infections and digestive complaints, but coptisine is typically present as part of a mixture rather than as a stand-alone drug.

Chemically, coptisine is a planar, polycyclic cationic alkaloid with a permanently charged nitrogen atom, contributing to the characteristic properties of protoberberine alkaloids. It occurs naturally in plant extracts and can be isolated through standard alkaloid extraction methods. The compound has also been prepared in laboratory settings, and several total synthesis routes have been described in the chemical literature.

Biological activity reported in scientific studies includes antimicrobial, anti-inflammatory and cytotoxic effects observed in vitro, with some in vivo data in animals. Proposed mechanisms involve modulation of signaling pathways such as NF-kB and interactions with cellular targets that affect proliferation and apoptosis. However, clinical evidence is lacking, and results are often limited to laboratory or animal models. Pharmacokinetic data indicate limited oral bioavailability and solubility, a common trait among protoberberine alkaloids, which can complicate therapeutic use.

Safety and regulatory status: there are no approved therapeutic uses for coptisine. It is primarily of interest as a research compound and as a constituent of traditional plant extracts; high concentrations can be cytotoxic and potential interactions with drug-metabolizing enzymes warrant cautious investigation.