Silybum marianum (SM), a well-known
plant used as both a medicine and a food, has been widely used to
treat various diseases, especially hepatic diseases. The seeds and
fruits of SM contain a flavonolignan complex called silymarin, the
active compounds of which include silybin, isosilybin, silychristin,
dihydrosilybin, silydianin, and so on. In this review, we thoroughly
summarize high-quality publications related to the pharmacological
effects and underlying mechanisms of SM. SM has antimicrobial, anticancer,
hepatoprotective, cardiovascular-protective, neuroprotective, skin-protective,
antidiabetic, and other effects. Importantly, SM also counteracts
the toxicities of antibiotics, metals, and pesticides. The diverse
pharmacological activities of SM provide scientific evidence supporting
its use in both humans and animals. Multiple signaling pathways associated
with oxidative stress and inflammation are the common molecular targets
of SM. Moreover, the flavonolignans of SM are potential agonists of
PPARγ and ABCA1, PTP1B inhibitors, and metal chelators. At the
end of the review, the potential and perspectives of SM are discussed,
and these insights are expected to facilitate the application of SM
and the discovery and development of new drugs. We conclude that SM
is an interesting dietary medicine for health enhancement and drug
discovery and warrants further investigation.