Triflumuron

Triflumuron is a synthetic insecticide from the active ingredient group of chitin biosynthesis inhibitors with IC₅₀ value of 1.48 ± 1.44μM, and with EI₅₀ values of 5.28 and 1.59μg/L against Culex quinquefasciatus and Aedes albopictus, respectively. Triflumuron interferes with chitin synthesis and the moulting cycle, disrupting chitin deposition in the insect cuticle after ingestion^[1][2][3].

In vitro, Triflumuron(1μM to 1mM) was tested for its ability to inhibit hyaluronan (HA) secretion in NIH3T3 fibroblast cells. The results showed that Triflumuron effectively reduced HA deposition in the cell culture media, with a half-maximal inhibitory concentration (IC₅₀) of 1.48 ± 1.44μM^[1]. Triflumuron (50‐300μM) treated human renal embryonic cells (HEK 293) and hepatocytes (Hep G2) reduced significantly the cell viability and increased the reactive oxygen species generation, malondialdehyde levels, and mitochondrial membrane potential in both cell lines. Triflumuron was also demonstrated as an inductor of DNA damages quantified by the comet assay^[4].

In vivo, single intraperitoneal injection of Triflumuron (250, 350, 500mg/kg) in Balb/C mice induced oxidatie stress and elevated protein carbonyl levels in both liver and kidney extracts. The results also showed a significant increase in superoxide dismutase (SOD), glutathione peroxidase (GPX), glutathione S-transferase (GST) activity in liver and kidney after Triflumuron administration^[5]. Triflumuron (250, 350, 500mg/kg) was administered intraperitoneally to Balb/C male mice for 24h. The results indicated that Triflumuron has genotoxic effects on mice bone marrow cells, causing DNA damage, micronuclei formation, and chromosome aberrations in a dose-dependent manner^[6].

References:
[1] Tsitrina A A, Krasylov I G, Maltsev D I, et al. Inhibition of hyaluronan secretion by novel coumarin compounds and chitin synthesis inhibitors. Glycobiology. 2021 Sep 9;31(8):959-974.
[2] Belinato T A, Martins A J, Lima J B P, Valle D. Effect of triflumuron, a chitin synthesis inhibitor, on Aedes aegypti, Aedes albopictus and Culex quinquefasciatus under laboratory conditions. Parasit Vectors. 2013 Apr 4:6:83.
[3] Batra C P, Mittal P K, Adak T, Ansari M A. Efficacy of IGR compound Starycide 480 SC (Triflumuron) against mosquito larvae in clear and polluted water. J Vector Borne Dis.2005 Sep;42(3):109-16.
[4] Timoumi R, Amara I, Salem I B, Abid-Essefi S. Triflumuron induces cytotoxic effects on hepatic and renal human cell lines. J Biochem Mol Toxicol. 2020 Aug;34(8):e22504.
[5] Timoumi R, Amara I, Neffati F, et al. Acute triflumuron exposure induces oxidative stress responses in liver and kidney of Balb/C mice. Environ Sci Pollut Res Int. 2019 Feb;26(4):3723-3730.
[6] Timoumi R, Amara I, Ayed Y. et al. Triflumuron induces genotoxicity in both mice bone marrow cells and human Colon cancer cell line. Toxicol Mech Methods. 2020 Jul;30(6):438-449.

Triflumuron是一种几丁质合成抑制剂类的合成杀虫剂，其IC₅₀值为1.48 ± 1.44μM，在对抗Culex quinquefasciatus和Aedes albopictus时的EI₅₀值分别为5.28和1.59μg/L。Triflumuron通过干扰昆虫蜕皮过程中的几丁质沉积来发挥作用^[1][2][3]。

体外实验中，Triflumuron（1μM-1mM）被用于测试其抑制NIH3T3成纤维细胞分泌透明质酸（HA）的能力，结果显示其IC₅₀值为1.48 ± 1.44μM^[1]。此外经Triflumuron（50-300μM）处理的人类肾胚胎细胞（HEK 293）和肝细胞（Hep G2）的细胞活性显著降低，同时活性氧（ROS）生成、丙二醛（MDA）水平以及线粒体膜电位均有所增加，且通过彗星实验发现其可诱导DNA损伤^[4]。

体内实验中，Balb/C小鼠单次腹腔注射Triflumuron（250、350、500mg/kg）后，肝脏和肾脏提取物中的氧化应激水平和蛋白质羰基水平升高，且在Triflumuron给药后，肝脏和肾脏中的超氧化物歧化酶（SOD）、谷胱甘肽过氧化物酶（GPX）和谷胱甘肽S转移酶（GST）活性显著增加^[5]。此外Balb/C雄性小鼠腹腔注射Triflumuron（250、350、500mg/kg）24小时后，结果表明Triflumuron对小鼠骨髓细胞具有遗传毒性，以剂量依赖性方式导致DNA损伤、微核形成和染色体畸变^[6]。