title: Inhibitory effects of four plants flavonoids extracts on fatty acid synthase.
abstract: Fatty acid synthase (FAS) had been found overexpress and hyperactive in most cancers. Pharmacological inhibitors of FAS activity preferentially repress cancer cell proliferation and induce cancer cell apoptosis without affecting nonmalignant fibroblasts. These made FAS an excellent drug target for cancer therapy. The activity of FAS in 11 different kinds of cancer cells, including esophageal carcinoma (EC109, EC8712, H5E973), gastric carcinoma (N87, BGC823), lung carcinoma (A549, 95-D), hepatoma (HepG2), uterine cervix cancer (HeLa) and leukaemia (K562, U937) were compared using spectrophotometric method. We selected the cell line with the highest FAS activity as cell model to study the inhibitory effect of the flavonoids extracts on FAS. Four plants including Canavium album Raeuseh leaves, Bombax ceiba Linn, Brassica albograbra Bailey, and Citrus reticulata Blanco were selected for extracting flavonoids. The results showed significantly different FAS activity among different cancer cells. The FAS activity is the lowest in gastric cancer cell N87 (15.91 ± 3.61 U/mg protein) and the highest in lung cancer cell A549 (127.36 ± 10.14 U/mg protein). The cancer cell A549 was used as cell model to test the inhibitory effort of flavonoids extracts on FAS. Results showed that the flavonoids extracts of Citrus reticulata Blanco and Canavium album Raeuseh leaves have higher inhibitory effect on FAS activity compared with the universally used FAS inhibitor C75 and both extracts inhibit cancer cell proliferation when added to cultured cancer cells. These studies provided a good cell model for testing the inhibitory effect on FAS activity and suggested that Citrus reticulata Blanco rind and Canavium album Raeuseh leaves are good biomaterials for separating and purifying natural flavonoids FAS inhibitors and exploring their inhibitory mechanisms.
authors.affiliation: Department of Biology, Shantou University, Shantou 515063, China; Department of Biochemistry and Molecular Biology, Medical College of Shantou University, Shantou 515041, China.
authors.forename: Jun
authors.initials: J
authors.lastname: Chen
authors.affiliation: Department of Biology, Shantou University, Shantou 515063, China; Department of Biology, Hanshan Normal University, Chaozhou 521041, China.
authors.forename: Donghong
authors.initials: D
authors.lastname: Zhuang
authors.affiliation: Institute of Oncologic Pathology, Medical College of Shantou University, Shantou 515041, China.
authors.forename: Weijia
authors.initials: W
authors.lastname: Cai
authors.affiliation: Department of Biochemistry and Molecular Biology, Medical College of Shantou University, Shantou 515041, China.
authors.forename: Liyan
authors.initials: L
authors.lastname: Xu
authors.affiliation: Department of Biochemistry and Molecular Biology, Medical College of Shantou University, Shantou 515041, China.
authors.forename: Enmin
authors.initials: E
authors.lastname: Li
authors.affiliation: Department of Biology, Hanshan Normal University, Chaozhou 521041, China.
authors.forename: Yunying
authors.initials: Y
authors.lastname: Wu
authors.affiliation: Hachinohe National College of Technology, Tamonoki Hachinohe 0391192, Japan.
authors.forename: Kazuo
authors.initials: K
authors.lastname: Sugiyama
mesh_terms: D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D064429:Fatty Acid Synthases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D005419:Flavonoids / Q000494:pharmacology*; D006801:Humans; D009369:Neoplasms / Q000201:enzymology / Q000473:pathology; D010936:Plant Extracts / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D005419:Flavonoids; D010936:Plant Extracts; D064429:Fatty Acid Synthases