Department of Pharmacognosy, Adesh Institute of Pharmacy and Biomedical Sciences, Adesh University, Bathinda, Punjab 151101, India.
College of Osteopathic Medicine, Lake Erie College of Osteopathic Medicine, 5000 Lakewood Ranch Boulevard, Bradenton, FL 34211, USA.
Phytomedicine. 2022 Oct;105:154356. doi: 10.1016/j.phymed.2022.154356. Epub 2022 Jul 25.
Emerging studies indicate that hypericin has diverse pharmacological actions and exhibits potential for treatment of various types of cancer.
The current review evaluates the pharmacological activity, associated molecular mechanism, and therapeutic application of hypericin as an anticancer agent according to the most recent state of knowledge with special emphasis on clinical trials and safety profile.
This review follows The Preferred Reporting Items for Systematic Reviews criteria. Various databases, including PubMed, Scopus and Science Direct, were used to search and collect relevant literature. The major keywords used included the following: cancer, distribution, property, signaling pathway, pharmacological effect, treatment, prevention, in vitro and in vivo studies, toxicity, bioavailability, and clinical trials.
One hundred three articles met the established inclusion and exclusion criteria. Hypericin has shown anticancer activity against the expansion of several cell types including breast cancer, cervical cancer, colorectal cancer, colon cancer, hepatocellular carcinoma, stomach carcinoma, leukemia, lung cancer, melanoma, and glioblastoma cancer. Hypericin exerts its anticancer activity by inhibiting pro-inflammatory mediators, endothelial growth factor, fibroblast growth factor, cell adhesion, angiogenesis, and mitochondrial thioredoxin. It has also been shown to cause an increase in the levels of caspase-3 and caspase-4, arrest the cell cycle at metaphase leading to cancer cell apoptosis, and affect various protein and gene expression patterns.
Hypericin exhibits significant inhibitory activity against various types of in vitro and in vivo cancer models. However, well-designed, high quality, large-scale and multi-center randomized clinical studies are required to establish the safety and clinical utility of hypericin in cancer patients.
新兴研究表明金丝桃素具有多种药理作用，并显示出治疗各种类型癌症的潜力。
本综述根据最新知识评估金丝桃素作为抗癌剂的药理活性、相关分子机制和治疗应用，特别强调临床试验和安全性概况。
本综述遵循系统评价的首选报告项目标准。使用包括 PubMed、Scopus 和 Science Direct 在内的各种数据库搜索和收集相关文献。使用的主要关键词包括：癌症、分布、特性、信号通路、药理作用、治疗、预防、体外和体内研究、毒性、生物利用度和临床试验。
符合既定纳入和排除标准的有 103 篇文章。金丝桃素已显示出对多种细胞类型（包括乳腺癌、宫颈癌、结直肠癌、结肠癌、肝细胞癌、胃癌、白血病、肺癌、黑色素瘤和神经胶质瘤）的抗癌活性。金丝桃素通过抑制促炎介质、内皮生长因子、成纤维细胞生长因子、细胞黏附、血管生成和线粒体硫氧还蛋白来发挥其抗癌活性。它还被证明可以增加 caspase-3 和 caspase-4 的水平，使细胞周期在中期停滞导致癌细胞凋亡，并影响各种蛋白质和基因表达模式。
金丝桃素对各种体外和体内癌症模型均表现出显著的抑制活性。然而，需要进行设计良好、高质量、大规模和多中心的随机临床试验，以确定金丝桃素在癌症患者中的安全性和临床实用性。
