Skalny Anatoly, Aschner Michael, Paoliello Monica, Santamaria Abel, Nikitina Natalia, Rejniuk Vladimir, Jiang Yueming, Rocha João, Tinkov Alexey
IM Sechenov First Moscow State Medical University, Moscow 119146, Russia.
Peoples' Friendship University of Russia (RUDN University), Moscow 117198, Russia.
Arh Farm (Belgr). 2021;71(6):491-507. doi: 10.5937/arhfarm71-34359.
The objective of the present study was to review the existing data on the mechanisms involved in the endocrine disrupting activity of mancozeb (MCZ) in its main targets, including thyroid and gonads, as well as other endocrine tissues that may be potentially affected by MCZ. MCZ exposure was shown to interfere with thyroid functioning through impairment of thyroid hormone synthesis due to inhibition of sodium-iodine symporter (NIS) and thyroid peroxidase (TPO) activity, as well as thyroglobulin expression. Direct thyrotoxic effect may also contribute to thyroid pathology upon MCZ exposure. Gonadal effects of MCZ involve inhibition of sex steroid synthesis due to inhibition of P450scc (CYP11A1), as well as 3β-HSD and 17β-HSD. In parallel with altered hormone synthesis, MCZ was shown to down-regulate androgen and estrogen receptor signaling. Taken together, these gonad-specific effects result in development of both male and female reproductive dysfunction. In parallel with clearly estimated targets for MCZ endocrine disturbing activity, namely thyroid and gonads, other endocrine tissues may be also involved. Specifically, the fungicide was shown to affect cortisol synthesis that may be mediated by modulation of CYP11B1 activity. Moreover, MCZ exposure was shown to interfere with PPARγ signaling, being a key regulator of adipogenesis. The existing data also propose that endocrine-disrupting effects of MCZ exposure may be mediated by modulation of hypothalamus-pituitary-target axis. It is proposed that MCZ neurotoxicity may at least partially affect central mechanisms of endocrine system functioning. However, further studies are required to unravel the mechanisms of MCZ endocrine disrupting activity and overall toxicity.
本研究的目的是回顾现有数据,这些数据涉及代森锰锌(MCZ)在其主要靶标(包括甲状腺和性腺)以及其他可能受MCZ潜在影响的内分泌组织中的内分泌干扰活性机制。研究表明,MCZ暴露会通过抑制钠碘同向转运体(NIS)和甲状腺过氧化物酶(TPO)活性以及甲状腺球蛋白表达,损害甲状腺激素合成,从而干扰甲状腺功能。MCZ暴露时的直接甲状腺毒性作用也可能导致甲状腺病变。MCZ对性腺的影响包括抑制P450scc(CYP11A1)、3β-羟类固醇脱氢酶(3β-HSD)和17β-羟类固醇脱氢酶(17β-HSD),从而抑制性类固醇合成。与激素合成改变同时发生的是,MCZ被证明会下调雄激素和雌激素受体信号传导。综上所述,这些性腺特异性效应导致了男性和女性生殖功能障碍。除了MCZ内分泌干扰活性的明确估计靶标(即甲状腺和性腺)外,其他内分泌组织可能也会涉及。具体而言,已表明这种杀菌剂会影响皮质醇合成,这可能是由CYP11B1活性的调节介导的。此外,MCZ暴露被证明会干扰PPARγ信号传导,而PPARγ是脂肪生成的关键调节因子。现有数据还表明,MCZ暴露的内分泌干扰效应可能是由下丘脑-垂体-靶轴的调节介导的。有人提出,MCZ的神经毒性可能至少部分影响内分泌系统功能的中枢机制。然而,需要进一步研究来阐明MCZ内分泌干扰活性和总体毒性的机制。