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| 1 | Disulfiram thermosensitive in-situ gel based on solid dispersion for cataract显示文摘To improve the corneal permeability and water-solubility of disulfiram(DSF), which is an ocular drug for cataract, P188 was selected as a matrix to prepare solid dispersion of DSF(DSF SD) by hot melt method. The DSF SD was characterized by DSC, XRD, and IR, and the results suggested that DSF was amorphous in DSF SD. The DSF SD was added to borate buffer solution(BBS) contained 20% poloxamer P407 and 1.2% poloxamer P188 to form in-situ gel. In vitro and in vivo experiments revealed that DSF SD combined with in-situ gel(DSF SD/in-situ gel) increased the residence time and the amount of DSF penetrated through the corneal. The pharmacodynamics studies exhibited DSF SD/in-situ gel delayed the development of selenium-induced cataract at some content. These results investigated that DSF SD/in-situ gel as a drug delivery system can improve DSF ocular permeability. | Chunjuan Zhang Tonghua Xu Donglei Zhang Wei He Siling Wang Tongying Jiang | 2018 | Asian Journal of Pharmaceutical Sciences2018，13，6： | 3 |
| 2 | Drug repositioning of disulfiram induces endometrioid epithelial ovarian cancer cell death via the both apoptosis and cuproptosis pathways显示文摘Various therapeutic strategies have been developed to overcome ovarian cancer.However,the prognoses resulting from these strategies are still unclear.In the present work,we screened 54 small molecule compounds approved by the FDA to identify novel agents that could inhibit the viability of human epithelial ovarian cancer cells.Among these,we identified disulfiram(DSF),an old alcohol-abuse drug,as a potential inducer of cell death in ovarian cancer.Mechanistically,DSF treatment significantly reduced the expression of the anti-apoptosis marker Bcell lymphoma/leukemia-2(Bcl-2)and increase the expression of the apoptotic molecules Bcl2 associated X(Bax)and cleaved caspase-3 to promote human epithelial ovarian cancer cell apoptosis.Furthermore,DSF is a newly identified effective copper ionophore,thus the combination of DSF and copper was used to reduce ovarian cancer viability than DSF single treatment.Combination treatment with DSF and copper also led to the reduced expression of ferredoxin 1 and loss of Fe-S cluster proteins(biomarkers of cuproptosis).In vivo,DSF and copper gluconate significantly decreased the tumor volume and increased the survival rate in a murine ovarian cancer xenograft model.Thus,the role of DSF revealed its potential for used as a viable therapeutic agent for the ovarian cancer. | YAPING GAN TING LIU WEIFENG FENG LIANG WANG LI LI YINGXIA NING | 2023 | Oncology Research2023，31，3： | 2 |
| 3 | Disulfiram-loaded lactoferrin nanoparticles for treating inflammatory diseases显示文摘Sepsis is a dysregulated immune response to infection and potentially leads to life-threatening organ dysfunction,which is often seen in serious Covid-19 patients.Disulfiram(DSF),an old drug that has been used to treat alcohol addiction for decades,has recently been identified as a potent inhibitor of the gasdermin D(GSDMD)-induced pore formation that causes pyroptosis and inflammatory cytokine release.Therefore,DSF represents a promising therapeutic for the treatment of inflammatory disorders.Lactoferrin(LF)is a multifunctional glycoprotein with potent antibacterial and anti-inflammatory activities that acts by neutralizing circulating endotoxins and activating cellular responses.In addition,LF has been well exploited as a drug nanocarrier and targeting ligands.In this study,we developed a DSF-LF nanoparticulate system(DSF-LF NP)for combining the immunosuppressive activities of both DSF and LF.DSF-LF NPs could effectively block pyroptosis and inflammatory cytokine release from macrophages.Treatment with DSF-LF NPs showed remarkable therapeutic effects on lipopolysaccharide(LPS)-induced sepsis.In addition,this therapeutic strategy was also applied to treat ulcerative colitis(UC),and substantial treatment efficacy was achieved in a murine colitis model.The underlying mode of action of these DSF-LF-NPs may contribute to efficiently suppressing macrophage-mediated inflammatory responses and ameliorating the complications caused by sepsis and UC.As macrophage pyroptosis plays a pivotal role in inflammation,this safe and effective biomimetic nanomedicine may offer a versatile therapeutic strategy for treating various inflammatory diseases by repurposing DSF. | An-te Ou Jia-xin Zhang Yue-fei Fang Rong Wang Xue-ping Tang Peng-fei Zhao Yu-ge Zhao Meng Zhang Yong-zhuo Huang | 2021 | Acta Pharmacologica Sinica2021，42，11： | 2 |
| 4 | Tumor-responsive copper-activated disulfiram for synergetic nanocatalytic tumor therapy显示文摘Exploring alternative biomedical use of traditional drugs in different disease models is highly important as it can reduce the cost of drug development and overcome several critical issues of traditional chemodrugs such as low chemotherapeutic efficiency,severe side effect,and drug resistance.Disulfiram(DSF),a clinically approved alcohol-aversion drug,was recently demonstrated tofeature tumor-growth suppression effect along with the co-administration of Cu^(2+)species,but direct Cu^(2+)administration mode might cause severe toxicity originating from low Cu^(2+)accumulation into the tumor and nonspecific Cu^(2+)distribution-induced cytotoxicity.Based on the intriguing drug-delivery performance of nanoscale metal-organic frameworks(MOFs),we herein construct HKUST nMOFs as the Cu^(2+)self-supplying nanocarriers for efficient delivery of the D SF drug.The mildly acidic condition of tumor microenvironment initially triggered the release of Cu ions from HKUST nMOFs,which further reacted with the encapsulated DSF toform toxic Cu(DDTC)2(activation)for tumor chemotherapy.Especially,during the Cu(DDTC)2 complexation,Cu^(+)species were formed concomitantly,triggering the intratumoral nanocatalytic therapy for the generation of reactive oxygen species to synergistically destroying the tumor cells/tissue.As a result,synergetic tumor-responsive chemotherapy and nanocatalytic therapy are enabled by DSF@HKU ST nanodrugs,as demonstrated by the dominant anticancer efficacy with satisfied biocompatibility both in vitro and in vivo.The present work offers a sophisticated strategy for tumor-responsive nontoxic-to-toxic therapeutic with high biocompatibility. | Hao Chen Xi Li Minfeng Huo Liying Wang Yu Chen Wei Chen Bailiang Wang | 2021 | Nano Research2021，14，1： | 1 |
| 5 | Disulfiram联合Cu对耐药白血病细胞的作用及与JNK通路的关系显示文摘目的研究disulfiram(DS)联合Cu(DS/Cu)对耐药白血病细胞株HL60/ADM的逆转耐药作用及与JNK通路的关系。方法MTT法检测DS/Cu对HL60/ADM细胞的增殖抑制作用;选取DS/Cu对HL-60/ADM无明显杀伤作用的IC20值作为逆转浓度,MTT法检测IC20浓度DS/Cu联合不同浓度ADM处理24h后的IC50值;流式细胞仪检测阿霉素、DS/Cu单药及DS/Cu与阿霉素联合处理HL-60/ADM24h凋亡细胞比例的变化;Westernblotting检测c-jun表达的变化。结果DS/Cu对HL60/ADM细胞具有显著的增殖抑制作用,处理24hIC50为(1.11±0.025)μmol/L。HL-60/ADM细胞经IC20浓度(0.63μmol/L)DS/Cu处理24h后,ADM的IC50值从(7.69±1.87)降到(0.48±0.021)μg/mL,逆转倍数为15.95倍(P=0.003)。0.63μmol/L的DS/Cu、1.25μg/mL的阿霉素单药及上述浓度的DS/Cu联合阿霉素作用HL60/ADM细胞24h后,联合组凋亡细胞比例较DS/Cu或阿霉素单药组均显著增多(P<0.05)。Westernblotting显示阿霉素联合DS/Cu作用24h后c-jun表达水平显著增加。结论DS/Cu在体外对HL60/ADM细胞具有杀伤作用,IC20浓度的DS/Cu能够有效逆转HL60/ADM细胞的耐药,活化JNK通路是其机制之一。 | 史鹏程 徐兵 张妍琰 萧平难 陈国枢 周淑芸 | 2010 | 广东医学2010，31，4： | 1 |
| 6 | Disulfiram, an aldehyde dehydrogenase inhibitor, works as a potent drug against sepsis and cancer via NETosis, pyroptosis, apoptosis, ferroptosis, and cuproptosis显示文摘Regulated cell death(RCD)is essential for maintaining cell homeostasis and preventing diseases.Besides classical apoptosis,several novel nonapoptotic forms of RCD including NETosis,pyroptosis,ferroptosis,and cuproptosis have been reported and are increasingly being implicated in various cancers and inflammation.Disulfiram(DSF),an aldehyde dehydrogenase inhibitor,has been used clinically for decades as an anti-alcoholic drug.New studies have shown that DSF possesses potent anti-inflammatory and anti-cancer effects by regulating these new types of RCD.Here,we summarize the mechanisms and discuss the potential application of DSF in the treatment of cancers and inflammatory diseases. | Dingrui Nie Cunte Chen Yangqiu Li Chengwu Zeng | 2022 | Blood Science2022，4，3： | 0 |
| 7 | Dye-sensitized photo-oxidation of disulfiram显示文摘Dye-sensitized photo-oxidation of disulfiram has been carried out under various reaction conditions including change in solvents and sensitizers. The product has been isolated and characterized by its physical, chemical and spectral data. To confirm the participation of singlet-oxygen in the reaction, the experiment has also been carried out in the presence of various singlet oxygen scavengers. | CHOBISA C.S.BHARDWAJ Rajesh PUNJABI Pinki B.AMETA Suresh C. | 1995 | Chinese Journal of Chemistry1995，13，5： | 0 |
| 8 | Disulfiram及联合Cu对急性淋巴细胞白血病Molt4细胞增殖、凋亡及MDR1基因表达的影响显示文摘目的为进一步了解Disulfiram(DS)及DS联合Cu(DS/Cu)对急性淋巴细胞白血病Molt4细胞增殖、凋亡及多药耐药1(MDR1)基因水平表达的影响。方法用MTT法检测不同浓度(0.125、0.250、0.500、1.000、2.000、4.000μmol/mL)DS和DS/Cu对Molt4细胞的增殖抑制作用;用Annexin-ⅴ-FITC/PI流式细胞术检测不同浓度DS和DS/Cu作用Molt4细胞24h后凋亡细胞比例;实时荧光定量PCR检测不同浓度DS和DS/Cu对Molt4细胞MDR1基因表达水平的影响。结果不同浓度的DS对Molt4细胞有一定的抑制增殖作用,且呈剂量依赖性,IC50为(1.370±0.263)μmol/mL。DS/Cu联合后对Molt4细胞增殖抑制作用显著增强,IC50降为(0.560±0.443)μmol/mL,DS/Cu对Molt4细胞的抑制作用显著高于DS单药(P=0.005)。DS单药及DS/Cu对Molt4细胞均有诱导凋亡的作用,但DS/Cu对诱导Molt4细胞凋亡的比例显著高于DS单药(P=0.01)。DS单药对Molt4细胞MDR1基因表达水平无明显影响,而DS/Cu能显著降低Molt4细胞MDR1基因表达水平(P<0.001)。结论 DS对Molt4细胞有一定的抑制增殖、诱导凋亡作用,但对Molt4细胞MDR1表达水平无明显影响。DS/Cu不仅对Molt4细胞抑制增殖、诱导凋亡作用显著增强,还可显著下调Molt4细胞MDR1基因表达水平。 | 张妍琰 史鹏程 陈国枢 郭绪涛 萧平难 周淑芸 徐兵 | 2010 | 生物医学工程与临床2010，14，3： | 0 |
| 9 | A nanosystem of copper(II)-disulfiram for cancer treatment with high efficacy and few side effects显示文摘Developing chemotherapy drugs with high efficacy and few side effects has been a bottleneck problem that requires an efficient solution.The active cancer treatment ingredient disulfiram(DSF),inspired by the copper(II)diethyldithiocarbamate complex(CuET),can be used in a one-pot synthesis method to construct a CuET delivery nanosystem(CuET-ZIFCu@HA).Due to the high biocompatibility,targeting of CD44 overexpressed cancer cells,and acid response of zeolitic imidazolate framework(ZIF)materials of hyaluronic acid(HA),we realized that CuET-ZIFCu@HA could become an effective and highly selective cancer treatment.Both in vivo and in vitro experiments have demonstrated that CuET-ZIFCu@HA has robust anti-tumor properties without evident side effects.This research provided a promising strategy for DSF nanosystems that involves simple preparation and high efficacy,both of which are key to reusing DSF in cancer treatment. | Liping ZHAO Xiaoxia WANG Mingxia JIANG Xinghan WU Mogen ZHANG Xiuwen GUAN Jinlong MA Weifen ZHANG | 2021 | Frontiers of Materials Science2021，15，4： | 0 |
| 10 | Substance use disorders among older adults: A review of randomized controlled pharmacotherapy trials显示文摘Substance use disorders(SUDs)are a growing problem among older adults.Acamprosate,disulfiram,and naltrexone are United States Food and Drug Administration(referred to as FDA)approved for the treatment of alcohol use disorder,and buprenorphine is approved for the treatment of opiate use disorder among adults.However,the data on the use of these medications for the treatment of SUDs among older adults are unclear from randomized controlled trials(referred to as RCTs).A review of the literature indicates that there are only two RCTs that evaluated the use of pharmacologic agents for SUDs among older adults(≥50 years).One trial evaluated the use of naltrexone when compared to placebo for the treatment of alcohol use disorder among individuals,50-70 years in age.The other trial evaluated the use of naltrexone or placebo as adjuncts with sertraline in the treatment of alcohol use disorder among individuals older than 55 years in age.Both trials indicated that the use of naltrexone reduced the rates of relapse among older adults with alcohol use disorder.However,we did not identify any RCTs that studied the use of buprenorphine,acamprosate,or disulfiram for SUDs among older adults.Based on available evidence,it would be safe to conclude that limited data indicate some efficacy for naltrexone in the treatment of alcohol use disorder among older adults.However,data from controlled trials on the use of other medications that are FDA approved for the treatment of SUDs among younger adults are nonexistent among older adults with SUDs. | Rajesh R Tampi Aarti Chhatlani Hajra Ahmad Kripa Balaram Joel Dey Ricardo Escobar Thejasvi Lingamchetty | 2019 | World Journal of Psychiatry2019，9，5： | 0 |
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