Hellmich Mark R, Szabo Csaba
Departments of Surgery and Anesthesiology, University of Texas Medical Branch, Galveston, TX, USA,
Handb Exp Pharmacol. 2015;230:233-41. doi: 10.1007/978-3-319-18144-8_12.
Recent studies revealed increased expression of various hydrogen sulfide (H2S)-producing enzymes in cancer cells of various tissue types, and new roles of H2S in the pathophysiology of cancer have emerged. This is particularly evident in cancers of the colon and ovaries, where the malignant cells both overexpress cystathionine-β-synthase (CBS) and produce increased amounts of H2S, which enhances tumor growth and spread by (a) stimulating cellular bioenergetics, (b) activating proliferative, migratory, and invasive signaling pathways, and (c) enhancing tumor angiogenesis. Importantly, in preclinical models of these cancers, either pharmacological inhibition or genetic silencing of CBS was shown to be sufficient to suppress cancer cell bioenergetics in vitro, inhibit tumor growth and metastasis in vivo, and enhance the antitumor efficacy of frontline chemotherapeutic agents, providing a strong rationale for the development of CBS-targeted inhibitors as anticancer therapies. However, the observation that inhibition of H2S biosynthesis exerts anticancer effects is contradicted by other studies showing that increasing H2S with exogenous donors also exerts antitumor actions. Herein, we present a brief review of the scientific literature documenting the function of H2S, H2S donors, and transsulfuration enzymes in cancers from various tissue types, and propose that the paradoxical actions of H2S can be resolved by considering the bell-shaped pharmacology of H2S, whereby lower (endogenous) H2S production tends to promote, while higher (generated from exogenously added H2S donors) tends to inhibit cancer cell proliferation. Finally, we suggest areas for future investigations to expand our knowledge of this nascent field.
最近的研究表明,各种组织类型的癌细胞中,多种产硫化氢(H₂S)酶的表达增加,H₂S在癌症病理生理学中的新作用也已显现。这在结肠癌和卵巢癌中尤为明显,其中恶性细胞既过度表达胱硫醚-β-合酶(CBS),又产生更多的H₂S,H₂S通过以下方式促进肿瘤生长和扩散:(a)刺激细胞生物能量学;(b)激活增殖、迁移和侵袭信号通路;(c)增强肿瘤血管生成。重要的是,在这些癌症的临床前模型中,CBS的药理学抑制或基因沉默均足以在体外抑制癌细胞生物能量学,在体内抑制肿瘤生长和转移,并增强一线化疗药物的抗肿瘤疗效,这为开发靶向CBS的抑制剂作为抗癌疗法提供了有力依据。然而,抑制H₂S生物合成具有抗癌作用这一观察结果与其他研究相矛盾,其他研究表明,外源性供体增加H₂S也具有抗肿瘤作用。在此,我们简要综述了科学文献中关于H₂S、H₂S供体和转硫酶在各种组织类型癌症中的功能,并提出可以通过考虑H₂S的钟形药理学来解决H₂S的矛盾作用,即较低(内源性)的H₂S生成倾向于促进,而较高(由外源性添加的H₂S供体产生)的H₂S倾向于抑制癌细胞增殖。最后,我们提出了未来研究的领域,以扩展我们对这个新兴领域的认识。