title: Hydroquinone analog 4-[(Tetrahydro-2H-pyran-2‑yl) oxy] phenol induces C26 colon cancer cell apoptosis and inhibits tumor growth in vivo.
abstract: The 4[(Tetrahydro‑2H‑pyran‑2‑yl) oxy] phenol (XG‑d) hydroquinone analog, is found in Vaccinium vitis‑idaea  L. Although it is known for its antioxidant properties and high level of safety, its antitumor activity remains to be elucidated. In the present study, the anticancer effect of XG‑d was determined in vitro and in vivo. The cytotoxicity of XG‑d against C26 murine colon carcinoma cells was found to occur in a time‑ and concentration‑dependent manner, whereas little effect was observed in the two normal cell lines (HK‑2 and L02) investigated. Oral administration of XG‑d (100 mg/kg) had effects on the tumor growth of tumor‑bearing mice. Furthermore, marked apoptosis was observed using Hoechst 33258 staining and flow cytometric analysis with annexin V/propidium iodide double staining. XG‑d also downregulated the expression of B‑cell lymphoma 2 (Bcl‑2), increased the expression levels of Bcl‑2‑associated X protein and activated caspase‑9, caspase‑3 and poly(adenosine diphosphate‑ribose) polymerase. The present study demonstrated for the first time, to the best of our knowledge, that XG‑d inhibited cancer cell growth via the induction of apoptosis and was also able to inhibit tumor growth in vivo. These results demonstrated that XG‑d may be used as a potential natural agent for cancer therapy with low toxicity.
authors: Laboratory of Ethnopharmacology, Regenerative Medicine Research Center, West China Hospital, West China Medical School and Institute for Nanobiomedical Technology and Membrane Biology, Sichuan University, Chengdu, Sichuan 610041, P.R. China.
authors: Qigen
authors: Q
authors: Du
authors: Laboratory of Ethnopharmacology, Regenerative Medicine Research Center, West China Hospital, West China Medical School and Institute for Nanobiomedical Technology and Membrane Biology, Sichuan University, Chengdu, Sichuan 610041, P.R. China.
authors: Guang
authors: G
authors: Xin
authors: Laboratory of Ethnopharmacology, Regenerative Medicine Research Center, West China Hospital, West China Medical School and Institute for Nanobiomedical Technology and Membrane Biology, Sichuan University, Chengdu, Sichuan 610041, P.R. China.
authors: Hai
authors: H
authors: Niu
authors: Laboratory of Ethnopharmacology, Regenerative Medicine Research Center, West China Hospital, West China Medical School and Institute for Nanobiomedical Technology and Membrane Biology, Sichuan University, Chengdu, Sichuan 610041, P.R. China.
authors: Wen
authors: W
authors: Huang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity*; D017209:Apoptosis / Q000187:drug effects; D053148:Caspase 3 / Q000378:metabolism; D053453:Caspase 9 / Q000378:metabolism; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D003110:Colonic Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D005260:Female; D059585:G1 Phase Cell Cycle Checkpoints / Q000187:drug effects; D019073:HT29 Cells; D006801:Humans; D006873:Hydroquinones / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D051379:Mice; D008807:Mice, Inbred BALB C; D046529:Microscopy, Electron, Transmission; D010636:Phenols / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity*; D011065:Poly(ADP-ribose) Polymerases / Q000378:metabolism; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000378:metabolism; D011714:Pyrans / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity*; D029796:Vaccinium / Q000737:chemistry / Q000378:metabolism; D023041:Xenograft Model Antitumor Assays; D051028:bcl-2-Associated X Protein / Q000378:metabolism
chemical_list: C000603451:4-((tetrahydro-2H-pyran-2-yl)oxy)phenol; D000972:Antineoplastic Agents, Phytogenic; D006873:Hydroquinones; D010636:Phenols; D019253:Proto-Oncogene Proteins c-bcl-2; D011714:Pyrans; D051028:bcl-2-Associated X Protein; D011065:Poly(ADP-ribose) Polymerases; D053148:Caspase 3; D053453:Caspase 9; C031927:hydroquinone