Norwich Medical School, University of East Anglia, Norwich NR4 7UQ, UK.
Free Radic Biol Med. 2021 May 1;167:125-140. doi: 10.1016/j.freeradbiomed.2021.02.044. Epub 2021 Mar 10.
Natural isothiocyanates (ITCs) are phytochemicals abundant in cruciferous vegetables with the general structure, R-NCS. They are bioactive organosulfur compounds derived from the hydrolysis of glucosinolates by myrosinase. A significant number of isothiocyanates have been isolated from different plant sources that include broccoli, Brussels sprouts, cabbage, cauliflower, kale, mustard, wasabi, and watercress. Several ITCs have been demonstrated to possess significant pharmacological properties including: antioxidant, anti-inflammatory, anti-cancer and antimicrobial activities. Due to their chemopreventive effects on many types of cancer, ITCs have been regarded as a promising anti-cancer therapeutic agent without major toxicity concerns. However, their clinical application has been hindered by several factors including their low aqueous solubility, low bioavailability, instability as well as their hormetic effect. Moreover, the typical dietary uptake of ITCs consumed for promotion of good health may be far from their bioactive (or cytotoxic) dose necessary for cancer prevention and/or treatment. Nanotechnology is one of best options to attain enhanced efficacy and minimize hormetic effect for ITCs. Nanoformulation of ITCs leads to enhance stability of ITCs in plasma and emphasize on their chemopreventive effects. This review provides a summary of the potential bioactivities of ITCs, their mechanisms of action for the prevention and treatment of cancer, as well as the recent research progress in their nanodelivery strategies to enhance solubility, bioavailability, and anti-cancer efficacy.
天然异硫氰酸酯（ITCs）是十字花科蔬菜中丰富的植物化学物质，具有一般结构 R-NCS。它们是生物活性有机硫化合物，来源于黑芥子硫苷酶对硫苷的水解。从不同的植物来源中分离出了大量的异硫氰酸酯，包括西兰花、球芽甘蓝、白菜、花椰菜、羽衣甘蓝、芥菜、山葵和豆瓣菜。许多 ITC 已被证明具有显著的药理学特性，包括：抗氧化、抗炎、抗癌和抗菌活性。由于它们对许多类型癌症的化学预防作用，ITCs 被认为是一种有前途的抗癌治疗剂，而没有重大毒性问题。然而，由于其低水溶解度、低生物利用度、不稳定性以及它们的毒物兴奋效应，其临床应用受到了阻碍。此外，为促进健康而摄入的 ITC 的典型饮食摄取量可能远远低于预防和/或治疗癌症所需的生物活性（或细胞毒性）剂量。纳米技术是提高 ITCs 疗效和最小化毒物兴奋效应的最佳选择之一。ITCs 的纳米制剂可提高 ITCs 在血浆中的稳定性，并强调其化学预防作用。本文综述了 ITCs 的潜在生物活性、它们在预防和治疗癌症中的作用机制，以及最近在纳米递药策略方面的研究进展，以提高溶解度、生物利用度和抗癌疗效。
