Dietary feeding of Flavokawain A, a Kava chalcone, exhibits a satisfactory safety profile and its association with enhancement of phase II enzymes in mice.
Dietary feeding of Flavokawain A, a Kava chalcone, exhibits a satisfactory safety profile and its association with enhancement of phase II enzymes in mice.
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Flavokawain A（Kava Chalcone）的饮食喂养表现出令人满意的安全性及其与小鼠II期酶增强的关联。
DOI：
10.1016/j.toxrep.2014.02.002
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发表时间：
2014
影响因子：
--
通讯作者：
Zi, Xiaolin
中科院分区：
文献类型：
--
作者：
Li, Xuesen;Xu, Xia;Ji, Tao;Liu, Zhongbo;Gu, Mai;Hoang, Bang H;Zi, Xiaolin
Flavokawain A （FKA）是卡瓦植物中的一种主要查尔酮，近年来被证明具有良好的抗癌活性。对FKA的安全性进行系统的评估之前没有报道过。在本研究中，雄性FVB/N小鼠分别饲喂AIN-76A饲粮或AIN-76A饲粮中添加0.6% （6 g/kg食物）FKA或0.6%商业卡瓦根提取物（KRE） 3周。饲粮中饲喂FKA对食用量和体重没有影响。肝脏、肾脏、结肠、肺、心脏、脾脏和胸腺的组织病理学检查未发现氟氯卡引起的毒性迹象。生化血清分析和组织学检查证实fka治疗小鼠器官功能正常。细胞毒性分析显示，与阿霉素相比，FKA对骨髓和小肠上皮细胞的副作用最小。此外，口服FKA可提高小鼠肝脏、肺、前列腺和膀胱组织中谷胱甘肽s转移酶和醌还原酶的活性。相比之下，饲粮中添加0.6% KRE可提高肝脏/体重比，降低脾脏、胸腺和睾丸/体重比，并诱导肝脏组织结节增生。由此可见，饲粮中添加枸杞多糖对小鼠主要器官功能和体内平衡无不良影响，提示枸杞多糖具有用于人类癌症化学预防研究的潜力。
Flavokawain A (FKA), a major chalcone in the Kava plant, has recently demonstrated promising anti-cancer activities. A systematic evaluation of FKA's safety profile has not been reported before. In this study, male FVB/N mice were fed with an AIN-76A diet or AIN-76A diet supplemented with 0.6% (6 g/kg food) FKA or 0.6% commercial kava root extract (KRE) for three weeks. Dietary feeding of FKA did not affect food consumption and body weight. Histopathological examination of liver, kidney, colon, lung, heart, spleen, and thymus revealed no signs of FKA-induced toxicity. Biochemical serum analysis and histological examination confirmed normal organ function in FKA-treated mice. The cytotoxicity profile showed FKA had minimal side effects on bone marrow and small intestinal epithelial cells compared with Adriamycin. In addition, oral feeding of FKA increased activities of both glutathione S-transferase and quinone reductase in the liver, lung, prostate and bladder tissues of mice. In comparison, dietary feeding of 0.6% KRE increased liver/body weight ratio and decreased spleen, thymus, and testis/body weight ratios, as well as induced nodular proliferation in liver tissues. Therefore, dietary feeding FKA showed no adverse effects on major organ function and homeostasis in mice, suggesting the potential of FKA for chemoprevention study of human cancers.