Description
Dehydrocostus lactone (DHL) is a sesquiterpene lactone originally found in species of Saussurea. DHL exhibits antibiotic, antioxidative, anti-angiogenic, anticancer chemotherapeutic, and chemopreventive activities. DHL displays antibacterial activity against species of Mycobacterium. In osteoblasts, DHL increases levels of NADPH, thioredoxin reductase, and phospho-CREB and decreases levels of nitrotyrosin, preventing mitochondrial dysfunction induced by antimycin A. In macrophages treated with LPS, DHL decreases expression of iNOS and TNF-α. Additionally, DHL activates cAMP-activated cystic fibrosis transmembrane conductance regulator (CFTR) Cl- channels in thyroid cells. In vitro and in vivo, this compound downregulates expression of cyclin D1, Akt, mTOR, and inhibits phosphorylation of GSK-3β, inducing G0/G1 phase cell cycle arrest and preventing capillary tube formation. In soft tissue sarcoma cell lines, DHL decreases expression of CDK2, p27, CDK1/cdc2, cyclin B1, and matrix metalloproteinases 2 and 9 (MMP2/9), inducing G2/M phase cell cycle arrest and inhibiting cell proliferation.
References
Wang X, Zhang YF, Yu B, et al. Dehydrocostuslactone, a sesquiterpene lactone activates wild-type and ΔF508 mutant CFTR chloride channel. J Asian Nat Prod Res. 2013;15(8):855-66. PMID: 23799322.
Lohberger B, Rinner B, Stuendl N, et al. Sesquiterpene lactones downregulate G2/M cell cycle regulator proteins and affect the invasive potential of human soft tissue sarcoma cells. PLoS One. 2013 Jun 14;8(6):e66300. PMID: 23799090.
Wang CY, Tsai AC, Peng CY, et al. Dehydrocostuslactone suppresses angiogenesis in vitro and in vivo through inhibition of Akt/GSK-3β and mTOR signaling pathways. PLoS One. 2012;7(2):e31195. PMID: 22359572.
Seo MS, Choi EM. The effects of dehydrocostus lactone on osteoblastic MC3T3-E1 cells in redox changes and PI3K/Akt/CREB. Immunopharmacol Immunotoxicol. 2012 Oct;34(5):810-4. PMID: 22324303.
Choi EM. Dehydrocostus lactone prevents mitochondrial dysfunction in osteoblastic MC3T3-E1 cells. Eur J Pharmacol. 2011 Aug 16;664(1-3):1-7. PMID: 21596031.
Luna-Herrera J, Costa MC, González HG, et al. Synergistic antimycobacterial activities of sesquiterpene lactones from Laurus spp. J Antimicrob Chemother. 2007 Mar;59(3):548-52. PMID: 17218447.
Lee HJ, Kim NY, Jang MK, et al. A sesquiterpene, dehydrocostus lactone, inhibits the expression of inducible nitric oxide synthase and TNF-alpha in LPS-activated macrophages. Planta Med. 1999 Mar;65(2):104-8. PMID: 10193198.
