Kanehira Tsutomu, Takekoshi Susumu, Nagata Hidetaka, Matsuzaki Kentaro, Kambayashi Yasuhiro, Osamura Robert Y, Homma Takao
Department of Applied Chemistry, Tokai University Graduate School of Engineering, Hiratsuka, Kanagawa 259-1292, Japan.
Life Sci. 2003 Nov 21;74(1):87-97. doi: 10.1016/j.lfs.2003.06.033.
Kinobeon A was originally isolated from cultured cells of safflower (Carthamus tinctorius L., Compositae). It had never previously been directly isolated from safflower or other plants, animals or microorganisms. In this report, we demonstrate the anti-oxidative effects of kinobeon A and compare the results with those two known natural antioxidants, lignan (nordihydroguaiaretic acid) and quercetin. The NADPH-induced microsomal lipid peroxidation system was employed to assess anti-oxidative effects of kinobeon A. Addition of kinobeon A to the system significantly decreased the formation of thiobarbituric acid reactive substances (TBARS) in a dose-dependent manner with effects similar to those of lignan and quercetin. Formation of TBARS was completely inhibited at 10 microM of kinobeon A. Employing the xanthine/xanthine oxidase/nitroblue tetrazolium system and the KO2/XTT system, the superoxide anion scavenging activity of kinobeon A was greater than that of lignan or quercetin. IC50 values calculated for kinobeon A in these two systems were 1 microM and 0.8 microM, respectively. Kinobeon A exerted cytoprotective effects following oxidative treatments with hydrogen peroxide, cumene hydroperoxide, menadione and xanthine oxidase (XOD). Addition of kinobeon A to the systems markedly enhanced survival ratios of Madin-Darby bovine kidney cells, while their survival significantly decreased with the oxidative treatment alone. Kinobeon A exhibited stronger effect on the cell viability than lignan or quercetin when menadion or XOD were used as inducing reagents of oxidative stress. The present study demonstrates for the first time that kinobeon A prevents oxidative stresses and could be a useful cytoprotective reagent.
基诺苯A最初是从红花（菊科植物红花，学名Carthamus tinctorius L.）的培养细胞中分离出来的。此前从未直接从红花或其他植物、动物或微生物中分离得到过。在本报告中，我们展示了基诺苯A的抗氧化作用，并将结果与两种已知的天然抗氧化剂——木脂素（去甲二氢愈创木酸）和槲皮素进行比较。采用NADPH诱导的微粒体脂质过氧化系统来评估基诺苯A的抗氧化作用。向该系统中添加基诺苯A可显著降低硫代巴比妥酸反应性物质（TBARS）的形成，且呈剂量依赖性，其效果与木脂素和槲皮素相似。当基诺苯A的浓度为10微摩尔时，TBARS的形成被完全抑制。利用黄嘌呤/黄嘌呤氧化酶/硝基蓝四唑系统和KO2/XTT系统，基诺苯A的超氧阴离子清除活性高于木脂素或槲皮素。在这两个系统中计算得出的基诺苯A的IC50值分别为1微摩尔和0.8微摩尔。在用过氧化氢、氢过氧化异丙苯、甲萘醌和黄嘌呤氧化酶（XOD）进行氧化处理后，基诺苯A发挥了细胞保护作用。向这些系统中添加基诺苯A可显著提高马-达二氏牛肾细胞的存活率，而单独进行氧化处理时细胞存活率则显著降低。当使用甲萘醌或XOD作为氧化应激诱导剂时，基诺苯A对细胞活力的影响比木脂素或槲皮素更强。本研究首次证明基诺苯A可预防氧化应激，可能是一种有用的细胞保护剂。
