Garlicnin B1, an Active Cyclic Sulfide from Garlic, Exhibits Potent Anti-Inflammatory and Anti-Tumor Activities

• Published in: Antioxidants Vol. 12; no. 4; p. 869
• Main Authors: Gao, Shanghui, Yang, Kai, Nohara, Toshihiro, Ikeda, Tsuyoshi, Zhou, Jian-Rong, Yokomizo, Kazumi, Fang, Jun
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 01.04.2023; MDPI
• Subjects: anti-cancer; anti-inflammation; Antitumor agents; Azoxymethane; Cancer therapies; Cellulose; Chromatography; Colitis; Colon cancer; Cytotoxicity; Dextran; Dextran sulfate; Dosage; Drugs; Garlic; garlicnin B1; Hydrogen peroxide; Identification and classification; Inflammatory bowel disease; Inflammatory diseases; Natural products; NMR; Nuclear magnetic resonance; Nutritional aspects; Reactive oxygen species; Sarcoma; Spectrum analysis; Sulfides; Tumor necrosis factor-TNF; Tumors; Japan; United States > US; natural products; garlicnin B1; anti-inflammation; anti-cancer; reactive oxygen species
• ISSN: 2076-3921; 2076-3921
• DOI: 10.3390/antiox12040869

This study aimed to investigate the pharmacological activities of garlicnin B1, a cyclic sulfide compound found abundantly in garlic and structurally similar to onionin A1, which has been shown to possess strong anti-tumor effects. In vitro studies demonstrated that garlicnin B1 significantly reduced intracellular reactive oxygen species triggered by hydrogen peroxide in colon cancer cells. In a mouse colitis model induced by dextran sulfate sodium, garlicnin B1 at a low dose (5 mg/kg) remarkably ameliorated the symptoms and pathological progression. Additionally, garlicnin B1 exhibited considerable tumoricidal activity with an IC50 value of ~20 μM, as observed in cytotoxicity assays. In vivo experiments using the mouse sarcoma S180 transplanted model and the azoxymethane (AOM) or DSS-induced colon cancer model showed that garlicnin B1 effectively suppressed tumor growth in a dose-dependent manner, with marked inhibition at 80 mg/kg. These results suggest that garlicnin B1 has diverse functions that could be achieved by carefully manipulating the dosing regimen. We anticipate that garlicnin B1 has the potential to be used beneficially in the future for the treatment of cancer and inflammatory diseases, although further studies are warranted to elucidate its mechanisms of action.