Antiproliferative and cytotoxic effects of prenylated flavonoids from hops (Humulus lupulus) in human cancer cell lines
Antiproliferative and cytotoxic effects of prenylated flavonoids from hops (Humulus lupulus) in human cancer cell lines
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DOI：
10.1016/s0278-6915(99)00019-8
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发表时间：
1999-04-01
影响因子：
4.3
通讯作者：
Buhler, DR
中科院分区：
文献类型：
--
作者：
Miranda, CL;Stevens, JF;Buhler, DR
从啤酒花(Humulus Lupulus)中提取黄腐酚(XN)、2‘，4’，6‘，4-四羟基-3’-戊烯基查尔酮(TP)；2‘，3’，6‘，4-四羟基-3’-香叶基查尔酮(TG)；脱氢环黄腐酚(DX)、脱氢环黄腐酚水合物(DH)和异黄腐酚(IX)。XN、DX和IX对所有癌细胞的生长均有剂量依赖性的抑制作用(0.1~100亩L)。经过两天的治疗。XN、DX和IX对MCF-7细胞生长的半数抑制浓度(IC50)分别为13.3、15.7和15.3mU/L。治疗4天后，XN、DX和IX的ICS分别为3.47、6.87和4.69亩M。HT-29细胞比MCF-7细胞对这些黄酮类化合物具有更强的耐药性。在A-2780细胞中，XN作用2天和4天的IC50值分别为0.52和5.2mU，具有较强的抗增殖作用。100 mM时，所有的啤酒花黄酮类化合物在三种细胞系中都具有细胞毒性。细胞计数证实XN和IX对MCF-7细胞生长有抑制作用。XN和IX对MCF-7细胞DNA合成有抑制作用。作为抗增殖剂，XN(查尔酮)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作用。(C)1999爱思唯尔科学有限公司。保留所有权利。
Sis flavonoids [xanthohumol (XN), 2',4',6',4-tetrahydroxy-3'-prenylchalcone (TP); 2',3',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 mu l) decrease in growth of all cancer cells. After a 2-day treatment. the concentrations at which the growth of MCF-7 cells was inhibited bq 50% (IC50) were 13.3, 15.7 and 15.3 mu M for XN, DX and IX, respectively. After a 4-day treatment, the ICS, for XN, DX and IX were 3.47, 6.87 and 4.69 mu M, 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 mu M after 2 and 4 days of exposure, respectively. At 100 mu M. 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. (C) 1999 Elsevier Science Ltd. All rights reserved.