8,794
Views
45
CrossRef citations to date
0
Altmetric
Review Article

Natural fatty acid synthase inhibitors as potent therapeutic agents for cancers: A review

, , , , &
Pages 1919-1925 | Received 05 Jun 2015, Accepted 24 Oct 2015, Published online: 10 Feb 2016

References

  • Aras A, Khokhar AR, Qureshi MZ, Silva MF, Sobczak-Kupiec A, Pineda EA, Hechenleitner AA, Farooqi AA. (2014). Targeting cancer with nano-bullets: curcumin, EGCG, resveratrol and quercetin on flying carpets. Asian Pac J Cancer Prev. 15:3865–71.
  • Bitencourt TA, Komoto TT, Massaroto BG, Miranda CE, Beleboni RO, Marins M, Fachin AL. (2013). Trans-chalcone and quercetin down-regulate fatty acid synthase gene expression and reduce ergosterol content in the human pathogenic dermatophyte Trichophyton rubrum. BMC Complem Altern Med. 13:2–6.
  • Carvalho MA, Zecchin KG, Seguin F, Bastos DC, Agostini M, Rangel AL, Veiga SS, Raposo HF, Oliveira HCF, Loda M, et al. (2008). Fatty acid synthase inhibition with orlistat promotes apoptosis and reduces cell growth and lymph node metastasis in a mouse melanoma model. Int J Cancer. 123:2557–65.
  • Chen J, Zhuang DH, Cai WJ, Xu L, Li E, Wu Y, Sugiyama K. (2009). Inhibitory effects of four plants flavonoids extracts on fatty acid synthase. J Environ Sci. 21:S131–4.
  • Chiang CT, Way TD, Tsai SJ, Lin JK. (2007). Diosgenin, a naturally occurring steroid, suppresses fatty acid synthase expression in HER2-overexpressing breast cancer cells through modulating Akt, mTOR and JNK phosphorylation. Febs Lett. 581:5735–42.
  • Daker M, Ahmad M, Khoo AS. (2012). Quercetin-induced inhibition and synergistic activity with cisplatin - a chemotherapeutic strategy for nasopharyngeal carcinoma cells. Cancer Cell Int. 12:34–42.
  • Du GJ, Zhang ZY, Wen XD, Yu C, Calway T, Yuan CS, Wang CZ. (2012). Epigallocatechin gallate (EGCG) is the most effective cancer chemopreventive polyphenol in green tea. Nutrients. 4:1679–91.
  • Fan HJ, Tian WX, Ma XF. (2014). Curcumin induces apoptosis of HepG2 cells via inhibiting fatty acid synthase. Target Oncol. 9:279–86.
  • Gayathri R, Priya DK, Gunassekaran GR, Sakthisekaran D. (2009). Ursolic acid attenuates oxidative stress-mediated hepatocellular carcinoma induction by diethylnitrosamine in male Wistar rats. Asian Pac J Cancer Prev. 10:933–8.
  • Harris DM, Li LY, Chen M, Lagunero FT, Go VL, Boros LG. (2012). Diverse mechanisms of growth inhibition by luteolin, resveratrol, and quercetin in MIA PaCa-2 cells: a comparative glucose tracer study with the fatty acid synthase inhibitor C75. Metabolomics. 8:201–10.
  • Ilze V, Alvaro MV, Josias HH. (2011). Natural products in anti-obesity therapy. Nat Prod Rep. 28:1493–533.
  • Jiang HZ, Ma QY, Fan HJ, Liang WJ, Huang SZ, Dai HF, Wang PC, Ma XF, Zhao YX. (2012). Fatty acid synthase inhibitors isolated from Punica granatum L. J Braz Chem Soc. 223:889–93.
  • Jiang HZ, Quan XF, Tian WX, Hu JM, Wang PC, Huang SZ, Cheng ZQ, Liang WJ, Zhou J, Ma XF, et al. (2010). Fatty acid synthase inhibitors of phenolic constituents isolated from Garcinia mangostana. Bioorg Med Chem Lett. 20:6045–7.
  • Jimenez-Estrada M, Chilpa RR, Apan TR, Lledias F, Hansberg W, Arrieta D, Aguilar FJ. (2006). Anti-inflammatory activity of cacalol and cacalone sesquiterpenes isolated from Psacalium decompositum. J Ethnopharmacol. 105:34–8.
  • Joana R, Adriana B, Glòria O, Cufí S, Haro D, Marrero PF, Puig T. (2012). Different fatty acid metabolism effects (-)-epigallocatechin-3-gallate and C75 in adenocarcinoma lung cancer. BMC Cancer. 12:280
  • Kma L. (2013). Synergistic effect of resveratrol and radiotherapy in control of cancers. Asian Pac J Cancer Prev. 14:6197–208.
  • Knowles LM, Yang C, Osterman A, Smith JW. (2008). Inhibition of fatty-acid synthase induces caspase-8-mediated tumor cell apoptosis by up-regulating DDIT4. J Biol Chem. 283:31378–84.
  • Lee JS, Sul JY, Park JB, Lee MS, Cha EY, Song IS, Kim JR, Chang ES. (2013). Fatty acid synthase inhibition by amentoflavone suppresses HER2/neu (erbB2) oncogene in SKBR3 human breast cancer cells. Phytother Res. 27:713–20.
  • Liang Y, Tian W, Ma X. (2009). Chemical components of Polygonummultiflorum Thunb. J Shenyang Pharm Univ. 26:536–8. (in Chinese).
  • Liang Y, Tian W, Ma X. (2013). Inhibitory effects of grape skin extract and resveratrol on fatty acid synthase. BMC Complement Altern Med. 13:361–9.
  • Liu HW, Li JK, Zhao WH, Bao L, Song XH, Xia Y, Wang X, Zhang C, Wang XZ, Yao XS, et al. (2009). Fatty acid synthase inhibitors from Geum japonicum Thunb. Chem Biodivers. 6:402–10.
  • Liu W, Furuta E, Shindo K, Watabe M, Xing F, Pandey PR, Okuda H, Pai SK, Murphy LL, Cao D, et al. (2011). Cacalol, a natural sesquiterpene, induces apoptosis in breast cancer cells by modulating Akt-SREBP-FAS signaling pathway. Breast Cancer Res Treat. 128:57–68.
  • Martinez-Villaluenga C, Rupasinghe SG, Schuler MA, Gonzalez de Mejia E. (2010). Peptides from purified soybean beta-conglycinin inhibit fatty acid synthase by interaction with the thioesterase catalytic domain. FEBS J. 277:1481–93.
  • McFadden JM, Medghalchi SM, Thupari JN, Pinn ML, Vadlamudi A, Miller KI, Kuhajda FP, Townsend CA. (2005). Application of a flexible synthesis of (5R)-thiolactomycin to develop new inhibitors of type I fatty acid synthase. J Med Chem. 48:946–61.
  • Menendez JA, Lupu R. (2004). Fatty acid synthase-catalyzed de novo fatty acid biosynthesis: from anabolic-energy-storage pathway in normal tissues to jack-of-all-trades in cancer cells. Arch Immunol Ther Exp. 52:414–26.
  • Menendez JA, Vazquez-Martin A, Colomer R, Brunet J, Carrasco-Pancorbo A, Garcia-Villalba R, Fernandez-Gutierrez A, Segura-Carretero A. (2007). Olive oil's bitter principle reverses acquired autoresistance to trastuzumab (Herceptin) in HER2-overexpressing breast cancer cells. BMC Cancer. 7:80.
  • Menendez JA, Vazquez-Martin A, Oliveras-Ferraros C, Garcia Villalba R, Carrasco-Pancorbo A, Fernandez-Gutierrez A, et al. (2008). Analyzing effects of extra-virgin olive oil polyphenols on breast cancer-associated fatty acid synthase protein expression using reverse-phase protein microarrays. Int J Mol Med. 22:433–9.
  • Migita T, Ruiz S, Fornari A, Fiorentino M, Priolo C, Zadra G, Inazuka F, Grisanzio C, Palescandolo E, Shin E, et al. (2009). Fatty acid synthase: a metabolic enzyme and candidate oncogene in prostate cancer. J Natl Cancer Inst. 101:519–32.
  • Murata S, Yanagisawa K, Fukunaga K, Oda T, Kobayashi A, Sasaki R, Ohkohchi N. (2010). Fatty acid synthase inhibitor cerulenin suppresses liver metastasis of colon cancer in mice. Cancer Sci. 101:1861–5.
  • Oh J, Hwang IH, Hong CE, Lyu SY, Na M. (2013). Inhibition of fatty acid synthase by ginkgolic acids from the leaves of Ginkgo biloba and their cytotoxic activity. J Enzyme Inhib Med Chem. 28:565–8.
  • Ou YC, Li JR, Kuan YH, Raung SL, Wang CC, Hung YY, Pan PH, Lu HC, Chen CJ. (2014). Luteolin sensitizes human 786-O renal cell carcinoma cells to TRAIL-induced apoptosis. Life Sci. 100:110–7.
  • Oyagbemi AA, Saba AB, Ibraheem AO. (2009). Curcumin: from food spice to cancer prevention. Asian Pac J Cancer Prev. 10:963–7.
  • Pandey PR, Liu W, Xing F, Fukuda K, Watabe K. (2012). Anti-cancer drugs targeting fatty acid synthase (FAS). Recent Pat Anticancer Drug Discov. 7:185–97.
  • Pandey PR, Okuda H, Watabe M, Pai SK, Liu W, Kobayashi A, Xing F, Fukuda K, Hirota S, Sugai T, et al. (2011). Resveratrol suppresses growth of cancer stem-like cells by inhibiting fatty acid synthase. Breast Cancer Res Treat. 130:387–98.
  • Pappenberger G, Benz J, Gsell B, Hennig M, Ruf A, Stihle M, Thoma R, Rudolph MG. (2010). Structure of the human fatty acid synthase KS–MAT didomain as a framework for inhibitor design. J Mol Blol. 397:508–19.
  • Pizer ES, Thupari J, Han WF, Pinn ML, Chrest FJ, Frehywot GL, Townsend CA, Kuhajda FP. (2000). Malonyl-coenzyme-A is a potential mediator of cytotoxicity induced by fatty-acid synthase inhibition in human breast cancer cells and xenografts. Cancer Res. 60:213–8.
  • Quan XF, Wang Y, Ma XF, Liang Y, Tian WX, Ma QY, Jiang HZ, Zhao YX. (2012). α-Mangostin induces apoptosis and suppresses differentiation of 3T3-L1 cells via inhibiting fatty acid synthase. Plos One. 7:e33376
  • Rojas C, Pan-Castillo B, Valls C, Pujadas G, Garcia-Vallve S, Arola L, Mulero M. (2014). Resveratrol enhances palmitate-induced ER stress and apoptosis in cancer cells. Plos One. 9:e113929
  • Shishodia S, Aggarwal BB. (2006). Diosgenin inhibits osteoclastogenesis, invasion, and proliferation through the downregulation of Akt, I kappa B kinase activation and NF-kappa B-regulated gene expression. Oncogene. 25:1463–73.
  • Terasa P, Joanar R, Pedro FM, Haro D, Brunet J, Colomer R. (2008). Green tea catechin inhibits fatty acid synthase without stimulating carnitine palmitoyl transferase-1 or inducing weight loss in experimental animals. Anticancer Res. 28:3671–6.
  • Tian WX. (2006). Inhibition of fatty acid synthase by polyphenols. Curr Med Chem. 13:967–77.
  • Tian WX, Ma XF, Zhang SY, Sun YH, Li BH. (2011). Fatty acid synthase inhibitors from plants and their potential application in the prevention of metabolic syndrome. Clin Oncol Cancer Res. 8:1–9.
  • Torihata A, Hanai R, Gong X, Shen Y, Kuroda C. (2007). Chemical and genetic differentiation of Ligularia tsangchanensis in Yunnan and Sichuan provinces of China. . Chem Biodivers. 4:500–7.
  • Wang S, Moustaid-Moussa N, Chen L, Mo H, Shastri A, Su R, Bapat P, Kwun I, Shen CL. (2014). Novel insights of dietary polyphenols and obesity. J Nutr Biochem. 25:1–18.
  • Zeng XF, Li WW, Fan HJ, Wang XY, Ji P, Wang ZR, Ma S, Li LL, Ma XF, Yang SY. (2011). Discovery of novel fatty acid synthase (FAS) inhibitors based on the structure of ketoaceyl synthase (KS) domain. Bioorg Med Chem Lett. 21:4742–4744.
  • Zeng YW, Yang JZ, Pu XY, Du J, Yang T, Yang SM, Zhu WH. (2013). Strategies of functional food for cancer prevention in human beings. Asian Pac J Cancer Prev. 14:585–592.
  • Zhao J, Xun XB, Ye F, Ye F, Tian WX. (2011). Suppression of fatty acid synthase, differentiation and lipid accumulation in adipocytes by curcumin. Mol Cell Biochem. 351:19–28.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.