Department of Biomedical Sciences, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, United States.
Department of Pathology, Joan C. Edwards School of Medicine, Marshall University, Huntington, WV, United States.
Adv Cancer Res. 2024;164:241-281. doi: 10.1016/bs.acr.2024.05.005. Epub 2024 May 31.
Capsaicin is the hot and pungent ingredient of chili peppers. It is a potent pain-relieving agent and is often present in over-the-counter analgesic lotions and creams. Several convergent studies reveal that capsaicin displays growth-suppressive activity in human cancers in vitro and in vivo. Apart from its growth-suppressive activity (as a single agent), capsaicin has been found to sensitize human cancer cells to the pro-apoptotic effects of chemotherapy and radiation. The first part of this book chapter discusses the anti-cancer activity of capsaicin in gynecological cancers in cell culture experiments and mouse models. Out of all gynecological cancers, the anti-cancer activity of capsaicin (and its analogs) has only been investigated in cervical cancers and ovarian cancers. The clinical development of capsaicin as a viable anti-cancer drug has remained challenging due to its poor bioavailability and aqueous solubility properties. In addition, the administration of capsaicin is associated with adverse side effects like gastrointestinal cramps, stomach pain, irritation in the gut, nausea diarrhea and vomiting. Two strategies have been investigated to overcome these drawbacks of capsaicin. The first is to encapsulate capsaicin in sustained release drug delivery systems. The second strategy is to design non-pungent capsaicin analogs which will retain the anti-tumor activity of capsaicin. The second part of this chapter provides an overview of the anti-neoplastic (and chemosensitization activity) of capsaicin analogs and capsaicin-based sustained release formulations in cervical and ovarian cancers. The design of selective non-pungent capsaicin analogs and capsaicin-based polymeric drug delivery systems may foster the hope of novel strategies for the treatment and management of gynecological cancers.
辣椒素是辣椒中产生辣味和刺激性的成分。它是一种有效的止痛剂，常用于非处方止痛乳液和乳膏中。几项趋同研究表明，辣椒素在体外和体内对人类癌症具有生长抑制活性。除了其生长抑制活性（作为单一药物）外，还发现辣椒素使人类癌细胞对化疗和放疗的促凋亡作用敏感。本章的第一部分讨论了辣椒素在细胞培养实验和小鼠模型中对妇科癌症的抗癌活性。在所有妇科癌症中，只有在宫颈癌和卵巢癌中研究了辣椒素（及其类似物）的抗癌活性。由于其生物利用度和水溶性差，辣椒素作为可行的抗癌药物的临床开发仍然具有挑战性。此外，辣椒素的给药与胃肠道痉挛、胃痛、肠道刺激、恶心、腹泻和呕吐等不良反应有关。已经研究了两种策略来克服辣椒素的这些缺点。第一种是将辣椒素包封在缓释药物递送系统中。第二种策略是设计非刺激性的辣椒素类似物，保留辣椒素的抗肿瘤活性。本章的第二部分概述了辣椒素类似物和基于辣椒素的缓释制剂在宫颈癌和卵巢癌中的抗肿瘤（和化疗增敏活性）。选择性非刺激性辣椒素类似物和基于辣椒素的聚合物药物递送系统的设计可能为妇科癌症的治疗和管理提供新策略的希望。
