Sulfur-containing compounds (SCCs) derived from Allium vegetables, particularly garlic, exhibit diverse bioactivities relevant to human health. This chapter focuses on the physiological functions of diallyl trisulfide (DATS), a volatile compound formed during garlic processing. DATS modulates drug-metabolizing enzymes by downregulating CYP2E1 and inducing phase II enzymes such as glutathione S-transferase via the Nrf2-Keap1 signaling pathway, thereby mitigating hepatotoxicity. In colorectal cancer cells, DATS induces M-phase cell cycle arrest through the oxidative modification of cysteine residues on β-tubulin, which impairing microtubule polymerization and inhibiting cell proliferation. Furthermore, DATS suppresses platelet aggregation by oxidizing thiol groups on key platelet surface proteins, a mechanism similar to that of antiplatelet drugs. These findings highlight thiol modification as a central mechanism underlying the bioactivities of garlic-derived SCCs. In addition to their hepatoprotective, anticancer, and antithrombotic effects, SCCs have been reported to exert anti-inflammatory and lipid metabolism-regulating effects, although their molecular targets remain yet to be fully characterized. Further studies are required to further elucidate these mechanisms of action and evaluate their therapeutic potential in humans.