Miranda C L, Stevens J F, Helmrich A, Henderson M C, Rodriguez R J, Yang Y H, Deinzer M L, Barnes D W, Buhler D R
Department of Environmental and Molecular Toxicology, Oregon State University, Corvallis 97331, USA.
Food Chem Toxicol. 1999 Apr;37(4):271-85. doi: 10.1016/s0278-6915(99)00019-8.
Six flavonoids [xanthohumol (XN), 2',4',6',4-tetrahydroxy-3'-prenylchalcone (TP); 2',4',6',4-tetrahydroxy-3'-geranylchalcone (TG); dehydrocycloxanthohumol (DX); dehydrocycloxanthohumol hydrate (DH); and isoxanthohumol (IX)] from hops (Humulus lupulus) were tested for their antiproliferative activity in human breast cancer (MCF-7), colon cancer (HT-29) and ovarian cancer (A-2780) cells in vitro. XN, DX and IX caused a dose-dependent (0.1 to 100 microM) decrease in growth of all cancer cells. After a 2-day treatment, the concentrations at which the growth of MCF-7 cells was inhibited by 50% (IC50) were 13.3, 15.7 and 15.3 microM for XN, DX and IX, respectively. After a 4-day treatment, the IC50 for XN, DX and IX were 3.47, 6.87 and 4.69 microM, respectively. HT-29 cells were more resistant than MCF-7 cells to these flavonoids. In A-2780 cells, XN was highly antiproliferative with IC50 values of 0.52 and 5.2 microM after 2 and 4 days of exposure, respectively. At 100 microM, all the hop flavonoids were cytotoxic in the three cell lines. Growth inhibition of XN- and IX-treated MCF-7 cells was confirmed by cell counting. XN and IX inhibited DNA synthesis in MCF-7 cells. As antiproliferative agents, XN (chalcone) and IX (flavanone isomer of XN) may have potential chemopreventive activity against breast and ovarian cancer in humans.
对啤酒花（Humulus lupulus）中的六种黄酮类化合物[黄腐酚（XN）、2',4',6',4 - 四羟基 - 3'- 异戊烯基查耳酮（TP）、2',4',6',4 - 四羟基 - 3'- 香叶基查耳酮（TG）、脱氢环黄腐酚（DX）、脱氢环黄腐酚水合物（DH）和异黄腐酚（IX）]进行了体外抗人乳腺癌（MCF - 7）、结肠癌（HT - 29）和卵巢癌（A - 2780）细胞增殖活性的测试。XN、DX和IX导致所有癌细胞的生长呈剂量依赖性（0.1至100微摩尔）下降。经过2天的处理，XN、DX和IX抑制MCF - 7细胞生长50%（IC50）的浓度分别为13.3、15.7和15.3微摩尔。经过4天的处理，XN、DX和IX的IC50分别为3.47、6.87和4.69微摩尔。HT - 29细胞比MCF - 7细胞对这些黄酮类化合物更具抗性。在A - 2780细胞中，XN具有高度抗增殖活性，暴露2天和4天后的IC50值分别为0.52和5.2微摩尔。在100微摩尔时，所有啤酒花黄酮类化合物在这三种细胞系中均具有细胞毒性。通过细胞计数证实了XN和IX处理的MCF - 7细胞的生长抑制。XN和IX抑制了MCF - 7细胞中的DNA合成。作为抗增殖剂，XN（查耳酮）和IX（XN的黄烷酮异构体）可能对人类乳腺癌和卵巢癌具有潜在的化学预防活性。
