Thiamethoxam

Thiamethoxam is a highly effective and broad-spectrum neonicotinoid insecticide that controls pests through contact, ingestion, and systemic action^[1]. Thiamethoxam is rapidly absorbed by plants and translocated acropetally within the xylem, providing lasting control against sap-sucking pests such as aphids, planthoppers, and whiteflies^[2]. In animals, Thiamethoxam exhibits neurotoxicity, hepatotoxicity, and can cause impaired development of reproductive cells^[3-4].

In vitro, treatment of differentiated human neuroblastoma SH-SY5Y cells with Thiamethoxam (354.5-781.1mg/L) for 96 hours resulted in cytotoxicity, significantly increased intracellular generation of reactive oxygen and nitrogen species, and promoted apoptosis^[5]. Incubation of MCF-7 and GH3 cells with Thiamethoxam (1–300mg/L) for 6 days led to reduced cell viability^[6].

In vivo, oral administration of Thiamethoxam (78.15mg/kg and 156.3mg/kg) to 10–11-week-old male Wistar rats for 58 days (5 days per week) significantly reduced body weight gain and the weight of reproductive organs such as testes and epididymides, while also decreasing sperm count, motility, and increasing abnormality rates^[7]. Thiamethoxam (156mg/kg and 312mg/kg) administered orally to female Wistar rats for 30 days significantly reduced body weight gain and induced oxidative stress in ovarian and uterine tissues, leading to vacuolation of ovarian luteal cells, degeneration of oocytes, and necrosis of the uterine circular muscle layer accompanied by numerous apoptotic cells^[8].

References:
[1] Ruan CC, Liu Z, Li X, et al. Isolation and characterization of a new ginsenoside from the fresh root of Panax Ginseng. Molecules. 2010 Mar 30;15(4):2319-25.
[2] Liu GY, Bu X, Yan H, et al. 20S-protopanaxadiol-induced programmed cell death in glioma cells through caspase-dependent and -independent pathways. J Nat Prod. 2007 Feb;70(2):259-64.
[3] Zhao Y, Bu L, Yan H, et al. 20S-protopanaxadiol inhibits P-glycoprotein in multidrug resistant cancer cells. Planta Med. 2009 Aug;75(10):1124-8.
[4] Wang Y, Mi X, Du Y, et al. Design, Synthesis, and Anti-Inflammatory Activities of 12-Dehydropyxinol Derivatives. Molecules. 2023 Jan 30;28(3):1307.
[6] Liu Y, Guo X, Wu L, et al. Lipid rafts promote liver cancer cell proliferation and migration by up-regulation of TLR7 expression. Oncotarget. 2016 Sep 27;7(39):63856-63869.
[7] Yu Y, Zhou Q, Hang Y, et al. Antiestrogenic effect of 20S-protopanaxadiol and its synergy with tamoxifen on breast cancer cells. Cancer. 2007 Jun 1;109(11):2374-82.
[8] Li C, Ma C, Zhao R, et al. Analysis of potential targets of 20S-protopanaxadiol on diabetic nephropathy based on network pharmacology, molecular docking, and experimental validation. Ren Fail. 2025 Dec;47(1):2526688.

Thiamethoxam是一种高效、广谱的新烟碱类杀虫剂，通过触杀、胃毒和内吸作用有效防治害虫^[1]。Thiamethoxam能够被植物快速吸收并在木质部向顶传导，从而对刺吸式害虫如蚜虫、飞虱和粉虱等产生持久防控效果^[2]。Thiamethoxam对动物而言具有神经毒性、肝毒性，还会引起生殖细胞发育障碍^[3-4]。

在体外，Thiamethoxam（354.5-781.1mg/L）处理分化的人神经母细胞瘤SH-SY5Y细胞96小时，Thiamethoxam对SH-SY5Y细胞具有毒性，并显著增加细胞内活性氧和活性氮的生成，促进细胞凋亡^[5]。Thiamethoxam（1-300mg/L）孵育MCF-7细胞、GH3细胞6天，Thiamethoxam引起细胞活力下降^[6]。

在体内，Thiamethoxam（78.15mg/kg及156.3mg/kg）经口灌胃处理10–11周龄雄性Wistar大鼠，每周5天，持续58天，Thiamethoxam显著降低体重增长、睾丸及附睾等生殖器官重量，并导致精子数量减少、活力下降及畸形率升高^[7]。Thiamethoxam（156mg/kg及312mg/kg）经口灌胃处理雌性Wistar大鼠30天，显著降低体重增长并诱导卵巢与子宫组织氧化应激，引起卵巢黄体细胞空泡化、卵母细胞退化及子宫环状肌层坏死伴大量凋亡细胞^[8]。