Kumar Anil, Rajput Dharmendra Singh, Gupta Mandeep Kumar, Kumar Vivek, Singh Harpreet, Mishra Arun Kumar, Chopra Shivani, Chopra Hitesh
Faculty of Medical and Paramedical Sciences, Madhyanchal Professional University, Bhopal-462044, Madhya Pradesh, India.
Moradabad Educational Trust Group of Institutions Faculty of Pharmacy, Moradabad-244001, Uttar Pradesh, India.
EXCLI J. 2025 Mar 7;24:407-429. doi: 10.17179/excli2024-7941. eCollection 2025.
Hepatocellular Carcinoma (HCC) is one of the most common and fatal types of liver cancer worldwide; in this sense, Diethylnitrosamine (DEN) has been established as a potent carcinogen affecting the development and progression of this disease. The present work focused on determining whether phosphodiesterase (PDE) enzymes, especially PDE5, may serve as targets in the therapeutic treatment of DEN-induced HCC. PDE5 inhibitors, widely used as therapeutic drugs for cardiovascular diseases and erectile dysfunction, have recently been found to be promising in preclinical cancer models through the modulation of key signaling pathways implicated in the progression of tumors, such as the cGMP-PKG, JNK, and MAPK pathways. These pathways are very important for cell proliferation, apoptosis and metastasis, and their dysregulation contributes to the aggressive nature of HCC. This study assessed the potential of PDE5 inhibitors to suppress proliferation, induce apoptosis, and alter the tumor microenvironment, thus potentially improving standard chemotherapy and immunotherapy interventions. By inhibiting certain PDE isoforms with these drugs, an anticancer response might occur as part of a complex mechanism that acts on both cancer cells and the microenvironment favorable for tumor growth. A preliminary review indicated that PDE inhibitors may be a promising therapeutic approach for overcoming some of the shortcomings of current treatments, particularly the development of resistance and the toxic effects of these treatments. Additional clinical investigations are necessary to determine the safety profile, appropriate amount of Osage, and long-term efficacy of these agents in the treatment of HCC, particularly in DEN-induced animal models. This study contributes to the expanding body of evidence supporting the use of PDE inhibitors in cancer treatment.
肝细胞癌(HCC)是全球最常见且致命的肝癌类型之一;从这个意义上讲,二乙基亚硝胺(DEN)已被确认为一种强效致癌物,会影响这种疾病的发生和发展。目前的工作重点是确定磷酸二酯酶(PDE),尤其是PDE5,是否可作为DEN诱导的HCC治疗的靶点。PDE5抑制剂被广泛用作心血管疾病和勃起功能障碍的治疗药物,最近在临床前癌症模型中发现,通过调节与肿瘤进展相关的关键信号通路,如cGMP - PKG、JNK和MAPK通路,具有潜在的治疗前景。这些通路对细胞增殖、凋亡和转移非常重要,其失调会导致HCC的侵袭性。本研究评估了PDE5抑制剂抑制增殖、诱导凋亡以及改变肿瘤微环境的潜力,从而有可能改善标准化化疗和免疫治疗干预。通过用这些药物抑制某些PDE亚型,可能会引发抗癌反应,这是一种作用于癌细胞和有利于肿瘤生长的微环境的复杂机制的一部分。初步综述表明,PDE抑制剂可能是一种有前景的治疗方法,可克服当前治疗的一些缺点,特别是耐药性的产生和这些治疗的毒副作用。需要进一步的临床研究来确定这些药物在治疗HCC中的安全性、合适剂量以及长期疗效,特别是在DEN诱导的动物模型中。本研究为支持在癌症治疗中使用PDE抑制剂的证据不断增加做出了贡献。