Background: Cyclea peltata (Lam.) Hook. f. and Thoms., an ethnomedicinal herb with antitoxin and anti-herpes activities, is used to cure smallpox, wounds, diabetic disorders of the skin, and its use as a cooling agent. In the present study, an attempt has been made to screen different alkaloids present in Cyclea peltata roots using LC-ESI-MS/MS and to evaluate the in vitro cytotoxic activity of alkaloids. Methods: The detection of alkaloids in C. peltata root extract was carried out by performing MRM-based assay using liquid chromatography-mass spectrometry. The cytotoxic effect of the acetone crystalized fraction was performed against human pancreatic cancer using MIA PaCa-2 cells. Results: The study revealed the presence of tetrandrine and fangchinoline as the major BBI alkaloids in the roots of this herb, along with cycleacurine, isochondrodendrine, cycleahomine and tetrandrine mono-N-2’-oxide. Furthermore, the present study also detected two precursors of BBI alkaloids such as d-Coclaurine, (-)-N-methylcoclaurine. The study also showed a significant (p<0.05) cytotoxic effect of the acetone crystalized fraction with an IC50 value of 59.85 μg/ml. Conclusion: C. peltata root is the major source of tetrandrine and fangchinoline with potent cytotoxic effect.
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