Rajendran Peramaiyan, Rengarajan Thamaraiselvan, Nandakumar Natarajan, Palaniswami Rajendran, Nishigaki Yutaka, Nishigaki Ikuo
NPO-International Laboratory of Biochemistry, 1-166, Uchide, Nakagawa-ku, Nagoya 454-0926, Japan.
Department of Microbiology, Immunology and Genetics, Ben Gurion University of the Negev, Beer Sheva 84105, P.O.B. 653, Israel.
Eur J Med Chem. 2014 Oct 30;86:103-12. doi: 10.1016/j.ejmech.2014.08.011. Epub 2014 Aug 5.
Kaempferol (3,5,7-trihydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one) is a flavonoid found in many edible plants (e.g., tea, broccoli, cabbage, kale, beans, endive, leek, tomato, strawberries, and grapes) and in plants or botanical products commonly used in traditional medicine (e.g., Ginkgo biloba, Tilia spp, Equisetum spp, Moringa oleifera, Sophora japonica and propolis). Its anti-oxidant/anti-inflammatory effects have been demonstrated in various disease models, including those for encephalomyelitis, diabetes, asthma, and carcinogenesis. Moreover, kaempferol act as a scavenger of free radicals and superoxide radicals as well as preserve the activity of various anti-oxidant enzymes such as catalase, glutathione peroxidase, and glutathione-S-transferase. The anticancer effect of this flavonoid is mediated through different modes of action, including anti-proliferation, apoptosis induction, cell-cycle arrest, generation of reactive oxygen species (ROS), and anti-metastasis/anti-angiogenesis activities. In addition, kaempferol was found to exhibit its anticancer activity through the modulation of multiple molecular targets including p53 and STAT3, through the activation of caspases, and through the generation of ROS. The anti-tumor effects of kaempferol have also been investigated in tumor-bearing mice. The combination of kaempferol and conventional chemotherapeutic drugs produces a greater therapeutic effect than the latter, as well as reduces the toxicity of the latter. In this review, we summarize the anti-oxidant/anti-inflammatory and anticancer effects of kaempferol with a focus on its molecular targets and the possible use of this flavonoid for the treatment of inflammatory diseases and cancer.
山奈酚(3,5,7 - 三羟基 - 2 -(4 - 羟基苯基)- 4H - 1 - 苯并吡喃 - 4 - 酮)是一种存在于许多可食用植物(如茶、西兰花、卷心菜、羽衣甘蓝、豆类、苦苣、韭菜、番茄、草莓和葡萄)以及传统医学中常用的植物或植物产品(如银杏、椴树属植物、木贼属植物、辣木、槐树和蜂胶)中的黄酮类化合物。其抗氧化/抗炎作用已在多种疾病模型中得到证实,包括脑脊髓炎、糖尿病、哮喘和癌症发生模型。此外,山奈酚可作为自由基和超氧阴离子的清除剂,并能维持过氧化氢酶、谷胱甘肽过氧化物酶和谷胱甘肽 - S - 转移酶等多种抗氧化酶的活性。这种黄酮类化合物的抗癌作用是通过不同的作用方式介导的,包括抗增殖、诱导凋亡、细胞周期阻滞、活性氧(ROS)生成以及抗转移/抗血管生成活性。此外,发现山奈酚通过调节包括p53和STAT3在内的多个分子靶点、激活半胱天冬酶以及生成ROS来发挥其抗癌活性。山奈酚的抗肿瘤作用也在荷瘤小鼠中进行了研究。山奈酚与传统化疗药物联合使用比后者产生更大的治疗效果,同时降低了后者的毒性。在本综述中,我们总结了山奈酚的抗氧化/抗炎和抗癌作用,重点关注其分子靶点以及这种黄酮类化合物在治疗炎症性疾病和癌症方面的可能用途。