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全面评价黄酮醇抗氧化剂,α-糖苷异槲皮苷和槲皮苷,以评估其遗传毒性。

Comprehensive evaluation of the flavonol anti-oxidants, alpha-glycosyl isoquercitrin and isoquercitrin, for genotoxic potential.

机构信息

Toxicology Program, Integrated Laboratory Systems, Inc., PO Box 13501, Research Triangle Park, NC 27709, USA.

Global Scientific and Regulatory Affairs, San-Ei Gen F.F.I., Inc., 1-1-11 Sanwa-cho, Toyonaka, Osaka 561-8588, Japan.

出版信息

Food Chem Toxicol. 2018 Mar;113:218-227. doi: 10.1016/j.fct.2017.12.059. Epub 2018 Jan 6.

Abstract

Quercetin and its glycosides possess potential benefits to human health. Several flavonols are available to consumers as dietary supplements, promoted as anti-oxidants; however, incorporation of natural quercetin glycosides into food and beverage products has been limited by poor miscibility in water. Enzymatic conjugation of multiple glucose moieties to isoquercitrin to produce alpha-glycosyl isoquercitrin (AGIQ) enhances solubility and bioavailability. AGIQ is used in Japan as a food additive and has been granted generally recognized as safe (GRAS) status. However, although substantial genotoxicity data exist for quercetin, there is very little available data for AGIQ and isoquercitrin. To support expanded global marketing of food products containing AGIQ, comprehensive testing of genotoxic potential of AGIQ and isoquercitrin was conducted according to current regulatory test guidelines. Both chemicals tested positive in bacterial reverse mutation assays, and exposure to isoquercitrin resulted in chromosomal aberrations in CHO-WBL cells. All other in vitro mammalian micronucleus and chromosomal aberration assays, micronucleus and comet assays in male and female B6C3F1 mice and Sprague Dawley rats, and Muta™ Mouse mutation assays evaluating multiple potential target tissues, were negative for both chemicals. These results supplement existing toxicity data to further support the safe use of AGIQ in food and beverage products.

摘要

槲皮素及其糖苷类化合物对人类健康具有潜在益处。几种黄酮醇以膳食补充剂的形式提供给消费者,被宣传为抗氧化剂;然而,由于在水中的混溶性差,将天然槲皮素糖苷类化合物掺入食品和饮料产品中受到限制。用多个葡萄糖部分对异槲皮苷进行酶促结合,生成α-糖苷基异槲皮苷(AGIQ),可提高溶解度和生物利用度。AGIQ 在日本用作食品添加剂,并已获得公认安全(GRAS)地位。然而,尽管有大量关于槲皮素的遗传毒性数据,但关于 AGIQ 和异槲皮苷的可用数据非常少。为了支持含有 AGIQ 的食品在全球范围内的广泛销售,根据当前的监管测试指南,对 AGIQ 和异槲皮苷的遗传毒性潜力进行了全面测试。这两种化学物质在细菌回复突变试验中均呈阳性,并且异槲皮苷暴露会导致 CHO-WBL 细胞中的染色体畸变。其他所有体外哺乳动物微核和染色体畸变试验、雄性和雌性 B6C3F1 小鼠和 Sprague Dawley 大鼠的微核和彗星试验以及评估多个潜在靶组织的 Muta™ 小鼠突变试验,对于这两种化学物质均为阴性。这些结果补充了现有的毒性数据,进一步支持了在食品和饮料产品中安全使用 AGIQ。

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