1. Xinjiang Key Laboratory of Molecular Biology and Endemic Diseases, Xinjiang Medical University, Urumqi 830011, China;
2. College of Life Science and Technology, Xinjiang University, Urumqi 830046, China
Abstract：The Pinobanksin-3-acetate (PB3A) is a natural flavonoid commonly present in propolis, honey, and many plants. The purpose of this study is to evaluate the anticancer activity of the PB3A on the human colon cancer in vitro. The effect of different concentrations of PB3A, 5-fluorouracil (5-FU) and a combination of PB3A and 5-FU for different durations on the proliferation of the cell line HCT-116 is analyzed by the MTT assay. The morphological changes of HCT-116 cells are observed by the inverted photo microscopy after treatment with different concentrations of PB3A for 24 h. The 24 h apoptotic rates of the HCT-116 cells induced with PB3A and 5-FU are determined by the FCM with Annexin V-FITC/PI double labeling. The results show that the PB3A has a significant inhibitory effect on the HCT-116 cell proliferation and in a time-and dose-dependent manner, and an additive or synergistic effect is shown with the common chemotherapy drug 5-FU. The PB3A could induce the typical changes of cell morphology in a dose-dependent manner. The FCM analysis shows that the PB3A could significantly increase the apoptosis rate in a dosedependent manner. The findings in this study suggest that the PB3A can play a potential anticancer role for the colon cancer in vitro, and it could induce the apoptosis.
 Awale S, Shrestha S P, Tezuka Y, et al. Neoflavonoids and related constituents from Nepalese propolis and their nitric oxide production inhibitory activity[J]. Journal of Natural Products, 2005, 68: 858-864.
 Ramanauskiene K, Inkeniene A M, Savickas A, et al. Analysis of the antimicrobial activity of propolis and lysozyme in semisolid emulsion system[J]. Acta Poloniae Pharmaceutica-Drug Research, 2009, 66:681-688.
 王玉芬. 蜂胶的研究进展[J]. 河北医药, 2002, 24(3): 227-228. Wang Yufen. Research Progress in Propolis[J]. Hebei Medical Journal, 2002, 24(3): 227-228.
 Fischer G, Cleff M B, Dummer L A, et al. Adjuvant effect of green propolis on humoral immune response of bovines immunized with bovine herpesvirus type 5[J]. Veterinary Immunology and Immunopathology, 2007, 116(1-2): 79-84.
 Bankova V. Recent trends and important developments in propolis research[J]. Evidence-based Complementary and Alternative Medicine, 2005, 2(1): 29-32.
 Inokuchi Y, Shimazawa M, Nakajima Y, et al. Brazilian green propolis protects against retinal damage in vitro and in vivo[J]. Evidence-based Complementary and Alternative Medicine, 2006, 3(1): 71-77.
 Onlen Y, Tamer C, Oksuz H, et al. Comparative trial of different antibacterial combinations with propolis and ciprofloxacin on Pseudomonas keratitis in rabbits[J]. Microbiological Research, 2007, 162(1): 62-68.
 Chen J, Long Y, Han M, et al. Water-soluble derivative of propolis mitigates scopolamine-induced learning and memory impairment in mice[J]. Pharmacology Biochemistry and Behavior, 2008, 90(3): 441-446.
 玄红专, 胡福良, 顾美儿. 蜂胶中咖啡酸苯乙酯的研究进展[J]. 食物研究与开发2006, 27(5): 14-15. Xuan Hongzhuan, Hu Fuliang, Gu Meier. Advance in the research of caffeic acid phenethyl ester in propolis[J]. Food Research and Development, 2006, 27(5): 14-15.
 Chen Y J, Shiao M S, Hsu M L, et al. Effect of caffeic acid phenethyl ester, an antioxidant from propolis, on inducing apoptosis in human leukemic HL-60 cells[J]. Journal of Agricultural and Food Chemistry, 2001, 49(11): 5615-5619.
 Wang D, Xiang D B, He Y J, et al. Effect of caffeic acid phenethyl ester on proliferation and apoptosis of colorectal cancer cells in vitro[J]. World Journal of Gastroenterology, 2005, 11(26): 4008-4012.
 Watabe M, Hishikawa K, Takayanagi A, et al. Caffeic acid phenethyl ester induces apoptosis by inhibition of NFkappaB and activation of Fas in human breast cancer MCF-7 cells[J]. The Journal of Biological Chemistry, 2004, 279(7): 6017-6026.
 Hung M W, Shiao M S, Tsai L C, et al. Apoptotic effect of caffeic acid phenethyl ester and its ester and amide analogues in human cervical cancer ME180 cells[J]. Anticancer research, 2003, 23(6C): 4773-4780.
 Awale S, Li F, Onozuka H, et al. Constituents of Brazilian red propolis and their preferential cytotoxic activity against human pancreatic PANC-1 cancer cell line in nutrient-deprived condition[J]. Bioorganic & Medicinal Chemistry Letters, 2008, 16(1): 181-189.
 Seda V H, Sorkun K, Gurhan S, et al. Propolis from Turkey induces apoptosis through activating caspases in human breast carcinoma cell lines[J]. Acta Histochemica, 2010, 112(6): 546-556.
 Valente M J, Baltazar A F, Henrique R, et al. Biological activities of Portuguese propolis: Protection against free radical-induced erythrocyte damage and inhibition of human renal cancer cell growth in vitro[J]. Food and Chemical Toxicology, 2011, 49(1): 86-92.
 阿布力克木·吾甫尔, 依米提·热合曼, 吐尔逊娜依·阿布都热依木, 等. 新疆蜂胶挥发油对结直肠癌HCT-116细胞增生、周期及凋亡的影响[J]. 世界华人消化杂志, 2011, 19(14): 1469-1475. Upur Ablikim, Rahman Yimit, Abdureyim Tursunay, et al. Effects of essential oils extracted from Xinjiang propolis on cell proliferation, cell cycle progression and apoptosis in human colorectal cancer cell line HCT-116[J]. Shijie Huaren Xiaohua Zazhi, 2011, 19(14): 1469-1475.
 Tiakavkina N A, Rulenko I A, Kolesnik I U A. Natural flavonoids as dietary antioxidants and biologically active additives[J]. Veprosy Pitania, 1996(2): 3338.
 Fang J M, Su W C, Cheng Y S. Flavonoids and stilbenes from armand pine[J]. Phytochemistry, 1988, 27(5): 1395-1397.
 Kumazawa S, Hamasaka T, Nakayama T. Antioxidant activity of propolis of various geographic origins[J]. Food Chemistry, 2004, 84(3): 329-339.
 Rapta P, Misík V, Stasko A, et al. Redox intermediates of flavonoids and caffeic acid esters from propolis: An EPR spectrometry and cyclic voltammetry study[J]. Free Radical Biology & Medicine, 1995, 18(5): 901-908.
 Valencia D, Alday E, Robles-Zepeda R, et al. Seasonal effect on chemical composition and biological activities of Sonoran propolis[J]. Food Chemistry, 2012, 131(2): 645-651.
 戴益琛, 宋于刚, 谢军培. 采用基因芯片技术筛选黑斑息肉综合征相关基因[J]. 世界华人消化杂志, 2008, 16(19): 2191-2194. Dai Yishen, Song Yugang, Xie Junpei, et al. Screening and annotation of genes associated with Peutz-Jeghers syndrome using gene chip technique[J]. Shijie Huaren Xiaohua Zazhi, 2008, 16(19): 2191-2194.
 Guo X, Xu B, Pandey S, et al. Disulfiram/copper complex inhibiting NFkappaB activity and potentiating cytotoxic effect of gemcitabine on colon and breast cancer cell lines[J]. Cancer Letters, 2010, 290(1):104-113.