School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, China.
Department of Radiology, Division of Translational Nanobiomaterials and Imaging, Leiden University Medical Center, Leiden, The Netherlands.
J Pharm Pharmacol. 2021 Mar 8;73(4):425-436. doi: 10.1093/jpp/rgaa018.
Hypericin is a polycyclic aromatic naphthodianthrone that occurs naturally. It is also an active ingredient in some species of the genus Hypericum. Emerging evidence suggests that hypericin has attracted great attention as a potential anticancer drug and exhibits remarkable antiproliferative effect upon irradiation on various tumour cells. This paper aims to summarise the anticancer effect and molecular mechanisms modulated by hypericin-medicated photodynamic therapy and its potential role in the cancer treatment.
Hypericin-medicated photodynamic therapy could inhibit the proliferation of various tumour cells including bladder, colon, breast, cervical, glioma, leukaemia, hepatic, melanoma, lymphoma and lung cancers. The effect is primarily mediated by p38 mitogen-activated protein kinase (MAPK), JNK, PI3K, CCAAT-enhancer-binding protein homologous protein (CHOP)/TRIB3/Akt/mTOR, TRAIL/TRAIL-receptor, c-Met and Ephrin-Eph, the mitochondria and extrinsic signalling pathways. Furthermore, hypericin-medicated photodynamic therapy in conjunction with chemotherapeutic agents or targeted therapies is more effective in inhibiting the growth of tumour cells.
During the past few decades, the anticancer properties of photoactivated hypericin have been extensively investigated. Hypericin-medicated photodynamic therapy can modulate a variety of proteins and genes and exhibit a great potential to be used as a therapeutic agent for various types of cancer.
金丝桃素是一种天然存在的多环芳香萘并二蒽酮，也是贯叶连翘属某些物种的一种活性成分。新出现的证据表明，金丝桃素作为一种潜在的抗癌药物引起了极大的关注，并对各种肿瘤细胞的照射表现出显著的抗增殖作用。本文旨在总结金丝桃素介导的光动力疗法的抗癌作用和分子机制及其在癌症治疗中的潜在作用。
金丝桃素介导的光动力疗法可以抑制包括膀胱癌、结肠癌、乳腺癌、宫颈癌、神经胶质瘤、白血病、肝癌、黑色素瘤、淋巴瘤和肺癌在内的各种肿瘤细胞的增殖。这种作用主要是通过 p38 丝裂原活化蛋白激酶 (MAPK)、JNK、PI3K、CCAAT 增强子结合蛋白同源蛋白 (CHOP)/TRIB3/Akt/mTOR、TRAIL/TRAIL 受体、c-Met 和 Ephrin-Eph、线粒体和外在信号通路来介导的。此外，金丝桃素介导的光动力疗法与化疗药物或靶向治疗联合使用，能更有效地抑制肿瘤细胞的生长。
在过去的几十年中，光激活金丝桃素的抗癌特性得到了广泛的研究。金丝桃素介导的光动力疗法可以调节多种蛋白质和基因，具有作为各种类型癌症治疗剂的巨大潜力。
