Carbon monoxide (CO) is now well recognized a pivotal endogenous signaling molecule in mammalian lives. The proof-of-concept employing chemical carriers of exogenous CO as prodrugs for CO release, also known as CO-releasing molecules (CO-RMs), has been appreciated. The major advantage of CO-RMs is that they are able to deliver CO to the target sites in a controlled manner. There is an increasing body of experimental studies suggesting the therapeutic potentials of CO and CO-RMs in different cancer models. This review firstly presents a short but crucial view concerning the characteristics of CO and CO-RMs. Then, the anticancer activities of CO-RMs that target many cancer hallmarks, mainly proliferation, apoptosis, angiogenesis, and invasion and metastasis, are discussed. However, their anticancer activities are varying and cell-type specific. The aerobic metabolism of molecular oxygen inevitably generates various oxygen-containing reactive metabolites termed reactive oxygen species (ROS) which play important roles in both physiology and pathophysiology. Although ROS act as a double-edged sword in cancer, both sides of which may potentially have been exploited for therapeutic benefits. The main focus of the present review is thus to identify the possible signaling network by which CO-RMs can exert their anticancer actions, where ROS play the central role. Another important issue concerning the potential effect of CO-RMs on the aerobic glycolysis (the Warburg effect) which is a feature of cancer metabolic reprogramming is given before the conclusion with future prospects on the challenges of developing CO-RMs into clinically pharmaceutical candidates in cancer therapy.

一氧化碳 (CO) 现在被公认为哺乳动物生活中的关键内源性信号分子。使用外源性 CO 的化学载体作为 CO 释放的前药（也称为 CO 释放分子 (CO-RM)）的概念验证已受到赞赏。CO-RM 的主要优点是它们能够以受控方式将 CO 输送到目标站点。越来越多的实验研究表明 CO 和 CO-RM 在不同癌症模型中的治疗潜力。本综述首先对 CO 和 CO-RM 的特征提出了一个简短但至关重要的观点。然后，讨论了针对许多癌症标志的 CO-RM 的抗癌活性，主要是增殖、凋亡、血管生成和侵袭和转移。然而，它们的抗癌活性各不相同，并且具有细胞类型特异性。分子氧的有氧代谢不可避免地产生各种含氧活性代谢物，称为活性氧 (ROS)，它们在生理学和病理生理学中都起着重要作用。尽管 ROS 在癌症中扮演着双刃剑的角色，但其双方都可能被利用来获得治疗益处。因此，本综述的主要重点是确定可能的信号网络，通过该网络，CO-RM 可以发挥其抗癌作用，其中 ROS 发挥核心作用。另一个重要问题是关于 CO-RM 对有氧糖酵解（Warburg 效应）的潜在影响，这是癌症代谢重编程的一个特征，然后给出了关于将 CO-RM 开发为癌症临床候选药物的挑战的未来前景治疗。