Background

Boron and boron containing compounds are known for their biological and protective roles being non-toxic and non-mutagenic in low concentrations. Male rats were exposed to halogenated boroxine (HB), dipotassium-trioxohydroxytetrafluorotriborate K₂[B₃O₃F₄OH], a potential new boron-containing therapeutic, aiming to determine concentrations with no adverse effects on selected serum biochemical parameters and histomorphological features.

Methods

HB was prepared by reacting potassium hydrofluoride (KHF₂) with boric acid in molar ratios 2:3 at room temperature and its primary structure contains 4 fluorine atoms substituted in 6-membered ring. In concentrations of 10, 25, 35 and 45 mg/kg, HB was administered intraperitoneally as a single dose. Biochemical parameters were observed 24 and 96 h following the treatment. Effects of HB on biochemical blood parameters were also observed 24 h following continuous nine days application in concentrations of 10 mg/kg intraperitoneally and 50 mg/kg per os. Histomorphological observation of kidneys, liver, spleen, lungs and heart was performed for all treated animals.

Results

Administration of single high dose of HB (35 mg/kg–45 mg/kg) effected high levels of urea and creatinine, which indicated renal injury that appeared to be temporary. Possible cause of concern is pancreatic injury indicated by elevated levels of serum amylase in the groups of animals that received the highest dosages of the substance. Histopathological examination of selected tissues revealed mild to moderate lesions in the kidneys and livers associated with administration of HB.

Conclusion

Observation of biochemical serum parameters or histopathology of examined tissues revealed no adverse effects of HB either after the administration of single dose lower than 35 mg/kg or following repeated administration at 10 mg/kg. These dosages should be further considered for potential therapeutic applications.

中文翻译：

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用潜在含硼治疗剂 K2[B3O3F4OH] 治疗的 Swiss Wistar 大鼠的生化和组织形态学发现。

背景

硼和含硼化合物以其生物和保护作用而闻名，在低浓度下无毒且无致突变性。雄性大鼠暴露于卤化硼烷 (HB)、三氧羟基四氟_三硼酸二钾 K ₂ [B ₃ O ₃ F ₄ OH]，这是一种潜在的新型含硼治疗剂，旨在确定对所选血清生化参数和组织形态学特征没有不利影响的浓度.

方法

HB 是通过氢氟化钾 (KHF ₂ ) 与硼酸在室温下以 2:3 的摩尔比反应制备的，其一级结构包含 4 个在 6 元环中取代的氟原子。HB 以 10、25、35 和 45 mg/kg 的浓度作为单剂量腹膜内给药。在治疗后 24 和 96 小时观察生化参数。还观察到在以下的10个浓度毫克/公斤连续9天应用24小时生化参数的血HB的影响和腹膜内50mg / kg的口服。对所有治疗动物进行肾脏、肝脏、脾脏、肺和心脏的组织形态学观察。

结果

单次高剂量 HB (35 mg/kg–45 mg/kg) 的给药会影响高水平的尿素和肌酐，这表明肾损伤似乎是暂时的。可能令人担忧的原因是胰腺损伤，表现为接受最高剂量该物质的动物组中血清淀粉酶水平升高。选定组织的组织病理学检查显示肾脏和肝脏中与 HB 给药相关的轻度至中度病变。

结论

观察血清生化参数或检查组织的组织病理学显示，在单次给药低于 35 mg/kg 或以 10 mg/kg 重复给药后，HB 没有不良反应。对于潜在的治疗应用，应进一步考虑这些剂量。