Kashyap Dharambir, Sharma Ajay, Sak Katrin, Tuli Hardeep Singh, Buttar Harpal Singh, Bishayee Anupam
Department of Histopathology, Postgraduate Institute of Medical Education and Research, Chandigarh 160 012, Punjab, India.
Department of Chemistry, Career Point University, Tikker-Kharwarian, Hamirpur 176 041, Himachal Pradesh, India.
Life Sci. 2018 Feb 1;194:75-87. doi: 10.1016/j.lfs.2017.12.005. Epub 2017 Dec 7.
A wide variety of chronic diseases, such as neurodegenerative and cardiovascular disorders, diabetes mellitus, osteoarthtitis, obesity and various cancers, are now being treated with cost effective phytomedicines. Since synthetic medicines are very expensive, concerted efforts are being made in developing and poor countries to discover cost effective medicines for the treatment of non-communicable diseases (NCDs). Understanding the underlying mechanisms of bioactive medicines from natural sources would not only open incipient avenues for the scientific community and pharmaceutical industry to discover new drug molecules for the therapy of NCDs, but also help to garner knowledge for alternative therapeutic approaches for the management of chronic diseases. Fisetin is a polyphenolic molecule of flavonoids class, and belongs to the bioactive phytochemicals that have potential to block multiple signaling pathways associated with NCDs such as cell division, angiogenesis, metastasis, oxidative stress, and inflammation. The emerging evidence suggests that fisetin may be useful for the prevention and management of several types of human malignancies. Efforts are being made to enhance the bioavailability of fisetin after oral administration to prevent and/or treat cancer of the liver, breast, ovary and other organs. The intent of this review is to highlight the in vitro and in vivo activities of fisetin and to provide up-to-date information about the molecular interactions of fisetin with its cellular targets involved in cancer initiation, promotion and progression as well as to focus on strategies underway to increase the bioavailability and reduce the risk of deleterious effects, if any, associated with fisetin administration.
多种慢性疾病，如神经退行性疾病和心血管疾病、糖尿病、骨关节炎、肥胖症以及各种癌症，目前正在使用具有成本效益的植物药进行治疗。由于合成药物非常昂贵，发展中国家和贫困国家正在共同努力，以发现治疗非传染性疾病（NCDs）的具有成本效益的药物。了解天然来源生物活性药物的潜在机制，不仅将为科学界和制药行业开辟新的途径，以发现用于治疗非传染性疾病的新药物分子，还将有助于积累有关慢性疾病管理替代治疗方法的知识。非瑟酮是黄酮类的多酚分子，属于具有潜在能力阻断与非传染性疾病相关的多种信号通路的生物活性植物化学物质，如细胞分裂、血管生成、转移、氧化应激和炎症。新出现的证据表明，非瑟酮可能对预防和管理几种类型的人类恶性肿瘤有用。正在努力提高非瑟酮口服后的生物利用度，以预防和/或治疗肝癌、乳腺癌、卵巢癌和其他器官的癌症。本综述的目的是强调非瑟酮的体外和体内活性，并提供有关非瑟酮与其参与癌症起始、促进和进展的细胞靶点分子相互作用的最新信息，以及关注正在进行的提高生物利用度和降低与非瑟酮给药相关的有害影响风险（如有）的策略。
