Sulfacetamide sodium monohydrate is a sulfonamide antibiotic. It has been investigated for the treatment of rosacea and pityriasis versicolor.

DHPS:9.5 μM

Sulfacetamide sodium monohydrate 抑制拟南芥DHPS，IC50为9.5 μM，pKa=5.4[1]。Sulfacetamide sodium monohydrate 对T-47D细胞具有抗增殖效应，这一效应独立于凋亡和细胞周期阻滞。Sulfacetamide sodium monohydrate 降低了p53/DRAM通路的表达，促进 Akt/mTOR 通路的上调，促进细胞保护性自噬。在48小时后，Sulfacetamide sodium monohydrate 对 T-47D 细胞的LD50为41 mM。Sulfacetamide处理的细胞使ATG5表达水平上升，增加在自噬通路中自噬体形成。在sulfathiazole 和 Sulfacetamide sodium monohydrate 诱导细胞自噬单不伴随细胞凋亡，且未在细胞周期的任何明确阶段发生阻滞作用。Sulfacetamide sodium monohydrate 通过DAPK独立通路触发T-47D细胞的自噬[2]。Sulfacetamide sodium monohydrate 是一种抗菌静止剂，对多种对磺胺药敏感的革兰氏阴性菌和革兰氏阳性菌活跃，包括链球菌、葡萄球菌、大肠杆菌、肺炎克雷伯菌、绿脓假单胞菌、沙门菌属、粪肠杆菌和诺卡菌属，这些细菌通常在皮肤的继发感染中被分离出来。Sulfacetamide还抑制了磷酸甘露糖异构酶（也称为磷酸甘露糖异构酶（PMI）），这被认为是鞭毛虫能量代谢的关键酶[3]。

小鼠口服 Sulfacetamide sodium monohydrate 的LD50为16,500 mg/kg。其副作用包括红斑、中度肿胀、恶心、呕吐和头痛。接受磺胺滴眼液治疗眼部感染的艾滋病毒阳性患者会出现史蒂文斯-约翰逊综合征。然而，所有这些副作用都与口服或通过皮肤、粘膜和结膜吸收大量化合物有关，而局部使用则不会产生强烈的副作用。

Cells are cultured in RPMI medium 1640, supplemented with 10% FBS and 1% penicillin/streptomycin, in a humidified atmosphere of 5% carbon dioxide in air at 37°C. According to MTT assay, the LC50 of sulfathiazole and sulfacetamide after 48 h is determined as 6.5 mM and 41 mM, respectively. Doxorubicin and sodium salt of sulfadrugs are dissolved in culture medium to the final desired concentration based on the determined LC50 and filtered. Cells (at 80% confluency) are incubated with freshly prepared drugs for 48h in a humidified incubator before being trypsinized and washed with phosphate-buffer saline 3 times and stored at ?70°C. For cell viability assay, cells are seeded in at least triplicate wells for each concentration of drug per time at 1 × 104 cells/well in a 96-well plate. After 24h of seeding, the cells has grown to ~80% confluency. The medium is changed to that containing drugs at concentrations ranging from 0.0-50 mM. The concentration range for doxorubicin is 0-6 μM. After 24, 48 and 72 h, each well is filled with 25 μl MTT stock solution (4 mg/ml or 100 μg/well) and incubated for 3 h at 37°C. Formazan crystals are dissolved in 100 μl of dimethyl sulfoxide (DMSO) and quantified using a microplate reader at 570 nm. The MTT assays are performed at least 3 times for each drug and the percentage of surviving cells relative to control (untreated sample) is calculated.(Only for Reference)