1. Department of Radiology, BenQ Medical Center, Nanjing Medical University, Nanjing 210019, China.
Theranostics. 2013 Aug 10;3(9):667-76. doi: 10.7150/thno.6650. eCollection 2013.
Hypericin has been widely studied as a potent photosensitizer for photodynamic therapy in both preclinical and clinical settings. Recently, hypericin has also been discovered to have a specific avidity for necrotic tissue. This affinity is also observed in a series of radiolabeled derivatives of hypericin, including [(123)I]iodohypericin, [(124)I]iodohypericin, and [(131)I]iodohypericin. Hypericin, along with other necrosis-avid contrast agents, has been investigated for use in noninvasively targeting necrotic tissues in numerous disorders. Potential clinical applications of hypericin include the identification of acute myocardial infarction, evaluation of tissue viability, assessment of therapeutic responses to treatments, and interventional procedures for solid tumors. The mechanisms of necrosis avidity in hypericin remain to be fully elucidated, although several hypotheses have been suggested. In particular, it has been proposed that the necrosis avidity of hypericin is compound specific; for instance, cholesterol, phosphatidylserine, or phosphatidylethanolamine components in the phospholipid bilayer of cellular membranes may be the major targets for its observed selectivity. Further investigations are needed to identify the specific binding moiety that is responsible for the necrosis avidity of hypericin.
金丝桃素作为一种有效的光敏剂，在临床前和临床环境中被广泛研究用于光动力疗法。最近，金丝桃素也被发现对坏死组织具有特异性亲和力。这种亲和力也存在于一系列金丝桃素的放射性标记衍生物中，包括 [(123)I]碘代金丝桃素、[(124)I]碘代金丝桃素和 [(131)I]碘代金丝桃素。金丝桃素与其他坏死亲和对比剂一起，已被用于在多种疾病中无创靶向坏死组织。金丝桃素的潜在临床应用包括急性心肌梗死的识别、组织活力的评估、对治疗反应的评估以及实体肿瘤的介入治疗。尽管提出了几种假设，但金丝桃素中坏死亲和力的机制仍有待充分阐明。特别是，有人提出金丝桃素的坏死亲和力是化合物特异性的；例如，细胞膜磷脂双层中的胆固醇、磷脂酰丝氨酸或磷脂酰乙醇胺成分可能是其观察到的选择性的主要靶标。需要进一步的研究来确定负责金丝桃素坏死亲和力的特定结合部分。
