Isoxanthohumol - Biologically active hop flavonoid
Isoxanthohumol - Biologically active hop flavonoid
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DOI：
10.1016/j.fitote.2015.03.007
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发表时间：
2015-06-01
期刊：
影响因子：
3.4
通讯作者：
Aniol, Miroslaw
中科院分区：
文献类型：
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作者：
Zolnierczyk, Anna Katarzyna;Maczka, Wanda Krystyna;Aniol, Miroslaw
除了黄腐酚 (XN) 和 8-异戊二烯柚皮素 (8PN) 之外，异黄腐酚 (IXN) 是啤酒花中发现的最重要的异戊二烯类黄酮之一。这种化合物的另一个天然来源是灌木苦参，用于中药。 IXN 的主要膳食来源是啤酒，该化合物是在麦芽汁煮沸过程中由 XN 产生的。在人体内，该化合物被 O-去甲基化为 8PN，这是已知最强的植物雌激素。这个过程发生在肝脏和肠道中，由当地微生物群介导。一些研究报告称，尽管啤酒中含有少量的啤酒花及其制剂，但这些化合物可能会影响人体的机能。 IXN 对乳腺癌 (MCF-7)、卵巢癌 (A-2780)、前列腺癌（DU145 和 PC-3）和结肠癌（HT-29 和 SW620）细胞的典型人类细胞系具有抗增殖活性。它通过人细胞色素 P450 (CYP1A2) 强烈抑制以下致癌物质的激活：2-氨基-3-甲基咪唑-[4,5-f]喹啉和黄曲霉毒素 B1 (AFB1)。它还抑制前列腺特异性抗原（PSA）的产生。 IXN 显着降低侵袭性乳腺癌 MDA-MB-231 中转化生长因子-β (TGF-β) 的表达。它干扰 JAK/STAT 信号通路并抑制单核细胞白血病细胞系 (MonoMac6) 中 prol 炎症基因的表达。它激活人脐静脉内皮细胞 (HUVEC) 和人主动脉平滑肌细胞 (HASMC) 的凋亡。此外，IXN 对疱疹病毒（HSV1 和 HSV2）和牛病毒性腹泻病毒（BVDV）具有抗病毒活性。 (C) 2015 Elsevier B.V. 保留所有权利。
Isoxanthohumol (IXN), apart from xanthohumol (XN) and 8-prenylnaringenin (8PN), is one of the most important prenylflavonoids found in hops. Another natural source of this compound is a shrub Sophora flavescens, used in traditional Chinese medicine. Main dietary source of IXN is beer, and the compound is produced from XN during wort boiling. In the human body, the compound is O-demethylated to 8PN, the strongest known phytoestrogen. This process takes place in the liver and in the intestine, where it is mediated by local microflora. It has been reported in some studies that even though beer contains small amounts of hops and its preparations, these compounds may affect the functioning of the human body. IXN exhibits an antiproliferative activity against human cell lines typical for breast cancer (MCF-7), ovarian cancer (A-2780), prostate cancer (DU145 and PC-3), and colon cancer (HT-29 and SW620) cells. It strongly inhibits the activation of the following carcinogens: 2-amino-3-methylimidazol-[4,5-f]quinoline and aflatoxin B1 (AFB1) via human cytochrome P450 (CYP1A2). It also inhibits the production of prostate specific antigen (PSA). IXN significantly reduces the expression of transforming growth factor-beta (TGF-beta) in the case of invasive breast cancer MDA-MB-231. It interferes with JAK/STAT signaling pathway and inhibits the expression of prol inflammatory genes in the monoblastic leukemia cell line (MonoMac6). It activates apoptosis in human umbilical vein endothelial cells (HUVEC) and human aortic smooth muscle cells (HASMCs). In addition, IXN shows an antiviral activity towards herpes viruses (HSV1 and HSV2) and bovine viral diarrhea virus (BVDV). (C) 2015 Elsevier B.V. All rights reserved.