Mini Reviews in Medicinal Chemistry, 2016, 20.

Phytochemicals for the Management of Melanoma

Harish Chandra Pal, Katherine Marchiony Hunt, Ariana Diamond, et al

Department of Dermatology, University of Alabama at Birmingham, Volker Hall, Room 501, 1670 University Blvd., Birmingham, AL, 35294, USA

Melanoma claims approximately 80% of skin cancer-related deaths. Its life-threatening nature is primarily due to a propensity to metastasize. The prognosis for melanoma patients with distal metastasis is bleak, with median survival of six months even with the latest available treatments. The most commonly mutated oncogenes in melanoma are BRAF and NRAS accounting approximately 60% and 20% of cases, respectively. In malignant melanoma, accumulating evidence suggests that multiple signaling pathways are constitutively activated and play an important role in cell proliferation, cell survival, epithelial to mesenchymal transition, metastasis and resistance to therapeutic regimens. Phytochemicals are gaining considerable attention because of their low toxicity, low cost, and public acceptance as dietary supplements. Cell culture and animals studies have elucidated several cellular and molecular mechanisms by which phytochemicals act in the prevention and treatment of metastatic melanoma. Several promising phytochemicals, such as, fisetin, epigallocatechin-3-gallate, resveratrol, curcumin, proanthocyanidins, silymarin, apigenin, capsaicin, genistein, indole-3-carbinol, and luteolin are gaining considerable attention and found in a variety of fresh fruits, vegetables, roots, and herbs. In this review, we will discuss the preventive potential, therapeutic effects, bioavailability and structure activity relationship of these selected phytochemicals for the management of melanoma.

荷兰《药物化学中的迷你点评》, 2016, 20.

治疗黑色素瘤的植物化学物质

Harish Chandra Pal, Katherine Marchiony Hunt, Ariana Diamond, et al

阿拉巴马大学伯明翰，福尔克 · 霍尔，501，1670 大学大道，伯明翰，铝，35294，美国皮肤科

黑色素瘤占据大约80％的皮肤癌相关死亡。其危及生命的性质主要是由于转移的倾向。远端转移的黑素瘤患者的预后是暗淡的，甚至使用最新可用的治疗，中值存活期也在六个月。黑色素瘤中最常见的突变致癌基因是BRAF和NRAS，分别占约60％和20％的病例。在恶性黑色素瘤中，积累的证据表明多种信号通路被组成型激活，并在细胞增殖，细胞存活，上皮间质转化，转移和对治疗方案的抗性中发挥重要作用。植物化学品由于它们的低毒性，低成本和作为膳食补充剂的公众接受而获得相当大的关注。细胞培养和动物研究已阐明几种细胞和分子机制，植物化学物质通过其在预防和治疗转移性黑素瘤中起作用。几种有希望的植物化学物质，例如非瑟酮，表没食子儿茶素-3-没食子酸酯，白藜芦醇，姜黄素，原花青素，水飞蓟素，芹菜素，辣椒素，染料木素，吲哚-3-甲醇和木犀草素获得相当的关注并且发现于各种新鲜水果，蔬菜，根和草本。在这次审查，我们将讨论这些选定的植物化学物质的管理的黑色素瘤的预防潜力，治疗效果，生物利用度和结构活性关系。