sophoridine

Sophoridine (Dihydro-5-episophocarpine), a natural anticancer drug, has been used in China for decades. A series of novel N-substituted Sophoridinic acid derivatives were synthesized and evaluated for their cytotoxicity with 1 as the lead. The structure-activity relationship indicated that introduction of an aliphatic acyl on the nitrogen atom might significantly enhance the anticancer activity. Among the compounds, 6b bearing bromoacetyl side-chain afforded a potential effect against four human tumor cell lines (liver, colon, breast, and lung). The mechanism of action of 6b is to inhibit the activity of DNA topoisomerase I, followed by the S-phase arrest and then cause apoptotic cell death, similar to that of its parent 1.

L-Sophoridine (Matridin-15-one) , a natural product obtained from medicinal plants, which has a variety of pharmacological effects, including anti-Y effects, and selectively induces apoptotic cell death in a variety of human Y cells in vitro and in vivo; however, its mechanism of action needs to be further elaborated.

Oxysophoridine (Sophoridine N-oxide) has a protective effect on focal cerebral ischemic injury through antioxidant and anti-apoptotic mechanisms; it may be a potential neuroprotective agent for cerebral ischemia injury, that the effect may be due to its ability to inhibit oxidative stress and expression of the N-methyl-D-aspartate receptor subunit NR1.Oxysophoridine ameliorates cardiac damage in a rat model of AMI and that this cardioprotection may be linked with its anti-oxidative, anti-apoptotic and anti-inflammatory properties.