Diphenyleneiodonium (DPI) chloride (DPIC), as a NADH/NADPH oxidase inhibitor, has possessing potent antimicrobial activity against Mtb and S. aureus[1].
In vitro efficacy test it shown that DPIC was equi-potently effective against drug-resistant clinical isolates of S. aureus with MIC of 0.5-1 mg/L as compared to S. aureus ATCC 29213. DPIC has no obvious potency against gram-negative bacteria with MIC ranging from 4-32 mg/L. DPIC also has potent antimicrobial activity against H37Rv with MIC of 0.39 μM or 0.12 mg/L[1]. In vitro, with 0.1 mM DPIC inhibits fungal spore germination and bacterial cell proliferation[2]. In vitro, treatment with 10 μM Diphenyleneiodonium chloride, DPI has strongest inhibition against neutrophil extracellular trap creation[3]. In vitro test it exhibited that treatment with 0.5-4 μM DPI in HCT116 cells decrease in G1 and increase in S phase cells. In addition, DPI treatment (0.5 μM DPI for 3 days) induces senescence of MCF-7 cells[4].
In vivo test it demonstrated that rat were administrated with 1 mg/kg DPI subcutaneously maybe protect against the functional and neurohistological damage of bupivacaine-blocked sciatic nerves in a high-fat diet/streptozotocin-induced DN model[5]. In vivo, treatment with 5 mg/kg DPI intraperitoneally in Sprague-Dawley rats, there was obvious reduction in the intracellular ROS, the number of inflammatory cells, and cytokines (TNF-α and IL-6) in BALF compared with LPS-treated rats[6].
References:
[1] Pandey M, et al. Diphenyleneiodonium chloride (DPIC) displays broad-spectrum bactericidal activity. Sci Rep. 2017 Sep 14;7(1):11521.
[2] Jung B, et al. Efficacy of Diphenyleneiodonium Chloride (DPIC) Against Diverse Plant Pathogens. Mycobiology. 2019 Jan 14;47(1):105-111.
[3] Ostafin M, et al. Different procedures of diphenyleneiodonium chloride addition affect neutrophil extracellular trap formation. Anal Biochem. 2016 Sep 15;509:60-66.
[4] Piszczatowska K, et al. Inhibition of NADPH Oxidases Activity by Diphenyleneiodonium Chloride as a Mechanism of Senescence Induction in Human Cancer Cells. Antioxidants (Basel). 2020 Dec 8;9(12):1248.
[5] Ji ZH, et al. Diphenyleneiodonium Mitigates Bupivacaine-Induced Sciatic Nerve Damage in a Diabetic Neuropathy Rat Model by Attenuating Oxidative Stress. Anesth Analg. 2017 Aug;125(2):653-661.
[6] Kim SK, et al. Protective effects of diphenyleneiodonium, an NADPH oxidase inhibitor, on lipopolysaccharide-induced acute lung injury. Clin Exp Pharmacol Physiol. 2019 Feb;46(2):153-162.
二苯碘铵 (DPI) 氯化物 (DPIC) 作为 NADH/NADPH 氧化酶抑制剂,对 Mtb 和 S. aureus 具有有效的抗菌活性[1]。
体外药效试验表明,DPIC对金黄色葡萄球菌的耐药临床分离株具有同等效力,MIC为0.5-1 mg/L,与金黄色葡萄球菌ATCC 29213相比,DPIC对金黄色葡萄球菌无明显效力MIC 范围为 4-32 mg/L 的革兰氏阴性菌。 DPIC 还对 H37Rv 具有有效的抗菌活性,MIC 为 0.39 μM 或 0.12 mg/L[1]。在体外,0.1 mM DPIC 抑制真菌孢子萌发和细菌细胞增殖[2]。在体外,用 10 μM Diphenyleneiodonium chloride 处理后,DPI 对中性粒细胞胞外陷阱产生的抑制作用最强[3]。体外试验表明,在 HCT116 细胞中用 0.5-4 μM DPI 处理后,G1 期细胞减少,S 期细胞增加。此外,DPI 处理（0.5 μM DPI 处理 3 天）可诱导 MCF-7 细胞衰老[4]。
体内试验表明,在高脂肪饮食/链脲佐菌素诱导的 DN 模型中,皮下给予大鼠 1 mg/kg DPI 可能会防止布比卡因阻断坐骨神经的功能和神经组织学损伤[5 ]。在体内,用 5 mg/kg DPI 腹腔注射 Sprague-Dawley 大鼠,与 LPS 处理相比,BALF 中的细胞内 ROS、炎症细胞数量和细胞因子（TNF-α 和 IL-6）明显减少大鼠[6].