Kallifatidis Georgios, Hoy James J, Lokeshwar Bal L
Department of Medicine, Georgia Cancer Center and Medical College of Georgia, Augusta University, Augusta, GA 30912, USA.
Department of Medicine, Georgia Cancer Center and Medical College of Georgia, Augusta University, Augusta, GA 30912, USA; Biochemistry and Molecular Biology, Georgia Cancer Center and Medical College of Georgia, Augusta University, Augusta, GA 30912, USA; Research Service, Charlie Norwood VA Hospital and Medical Center, Augusta, GA 30912, USA.
Semin Cancer Biol. 2016 Oct;40-41:160-169. doi: 10.1016/j.semcancer.2016.06.003. Epub 2016 Jun 28.
Prostate cancer (PCa), a hormonally-driven cancer, ranks first in incidence and second in cancer related mortality in men in most Western industrialized countries. Androgen and androgen receptor (AR) are the dominant modulators of PCa growth. Over the last two decades multiple advancements in screening, treatment, surveillance and palliative care of PCa have significantly increased quality of life and survival following diagnosis. However, over 20% of patients initially diagnosed with PCa still develop an aggressive and treatment-refractory disease. Prevention or treatment for hormone-refractory PCa using bioactive compounds from marine sponges, mushrooms, and edible plants either as single agents or as adjuvants to existing therapy, has not been clinically successful. Major advancements have been made in the identification, testing and modification of the existing molecular structures of natural products. Additionally, conjugation of these compounds to novel matrices has enhanced their bio-availability; a big step towards bringing natural products to clinical trials. Natural products derived from edible plants (nutraceuticals), and common folk-medicines might offer advantages over synthetic compounds due to their broader range of targets, as compared to mostly single target synthetic anticancer compounds; e.g. kinase inhibitors. The use of synthetic inhibitors or antibodies that target a single aberrant molecule in cancer cells might be in part responsible for emergence of treatment refractory cancers. Nutraceuticals that target AR signaling (epigallocatechin gallate [EGCG], curcumin, and 5α-reductase inhibitors), AR synthesis (ericifolin, capsaicin and others) or AR degradation (betulinic acid, di-indolyl diamine, sulphoraphane, silibinin and others) are prime candidates for use as adjuvant or mono-therapies. Nutraceuticals target multiple pathophysiological mechanisms involved during cancer development and progression and thus have potential to simultaneously inhibit both prostate cancer growth and metastatic progression (e.g., inhibition of angiogenesis, epithelial-mesenchymal transition (EMT) and proliferation). Given their multi-targeting properties along with relatively lower systemic toxicity, these compounds offer significant therapeutic advantages for prevention and treatment of PCa. This review emphasizes the potential application of some of the well-researched natural compounds that target AR for prevention and therapy of PCa.
前列腺癌(PCa)是一种激素驱动的癌症,在大多数西方工业化国家男性中,其发病率居首位,癌症相关死亡率居第二位。雄激素和雄激素受体(AR)是前列腺癌生长的主要调节因子。在过去二十年中,前列腺癌在筛查、治疗、监测和姑息治疗方面的多项进展显著提高了诊断后的生活质量和生存率。然而,最初被诊断为前列腺癌的患者中,仍有超过20%会发展为侵袭性且难治性疾病。使用来自海洋海绵、蘑菇和可食用植物的生物活性化合物作为单一药物或现有治疗的辅助药物来预防或治疗激素难治性前列腺癌,在临床上尚未取得成功。在天然产物现有分子结构的鉴定、测试和修饰方面已经取得了重大进展。此外,将这些化合物与新型基质结合提高了它们的生物利用度;这是将天然产物推向临床试验的重要一步。与大多为单一靶点的合成抗癌化合物(如激酶抑制剂)相比,源自可食用植物的天然产物(营养保健品)和常见民间药物可能因其更广泛的靶点而具有优势。使用针对癌细胞中单个异常分子的合成抑制剂或抗体可能部分导致了难治性癌症的出现。靶向AR信号传导(表没食子儿茶素没食子酸酯[EGCG]、姜黄素和5α-还原酶抑制剂)、AR合成(毛冬青甲素、辣椒素等)或AR降解(桦木酸、二吲哚基二胺、萝卜硫素、水飞蓟宾等)的营养保健品是用作辅助治疗或单一疗法的主要候选药物。营养保健品靶向癌症发生和发展过程中涉及的多种病理生理机制,因此有潜力同时抑制前列腺癌的生长和转移进展(例如,抑制血管生成、上皮-间质转化(EMT)和增殖)。鉴于它们的多靶点特性以及相对较低的全身毒性,这些化合物为前列腺癌的预防和治疗提供了显著的治疗优势。本综述强调了一些针对AR进行前列腺癌预防和治疗的经过充分研究的天然化合物的潜在应用。