Fisetin, a major component derived from mulberry (Morus australis Poir.) leaves, prevents vascular abnormal contraction.

Mulberry (Morus australis Poir.) leaves have long been consumed in the form of tea or tincture especially in Asia, owing to their high antioxidant and blood pressure-regulating properties. Although it is thought that vascular abnormal contraction may be involved in the blood pressure-suppressing effect, the effect of mulberry on vascular abnormal contraction is still unknown. Therefore, we investigated mulberry leaves as a potential source of bioactive compounds that prevent vascular abnormal contraction. Mulberry leaves were divided into fresh leaves and tea leaves and further classified according to the age of the tree: more or less than 20 years old, into roasted and unroasted. Mulberry fruits were also evaluated. We assessed the preventive effect of mulberry extracts on vascular abnormal contraction. Extracts from mulberry leaves of trees more than 20 years old showed a strong preventive effect on vascular abnormal contraction of human coronary artery smooth muscle cells. Therefore, to identify the active components in mulberry leaves, we fractionated the active fractions by gel filtration chromatography and reversed-phase high-performance liquid chromatography. The active fraction was further analyzed by mass spectrometry and nuclear magnetic resonance; an active component of the mulberry leaf extract was fisetin. In addition, our results indicated that the hydroxyl group at the C-3 position of fisetin is crucial for its activity. These results prove that fisetin is effective in preventing vascular abnormal contraction. Overall, mulberry leaves and fisetin are expected to be used in a wide range of fields such as functional foods, nutraceuticals, and drug targets.