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对来自掌腱膜挛缩症患者的细胞进行潜在前药的筛选。

Screening of potential prodrugs on cells derived from Dupuytren's disease patients.

作者信息

Kraljevic Pavelic Sandra, Bratulic Sinisa, Hock Karlo, Jurisic Davor, Hranjec Marijana, Karminski-Zamola Grace, Zinic Biserka, Bujak Maro, Pavelic Kresimir

机构信息

Laboratory of Systems Biomedicine, Division of Molecular Medicine, Rudjer Boskovic Institute, Bijenicka Cesta 54, 10000 Zagreb, Croatia.

出版信息

Biomed Pharmacother. 2009 Sep;63(8):577-85. doi: 10.1016/j.biopha.2008.10.005. Epub 2008 Oct 31.

Abstract

Dupuytren's disease (DD) is a fibroproliferative disorder, the cure for which is still limited to surgical excision of the affected fascia, often leading to high recurrence rates. Due to this fact, non-surgical treatments are being investigated, among them those targeting molecular processes of proliferation and differentiation in Dupuytren's cell cultures. Drugs with antiproliferative action may be valuable in DD treatment. Through characterization of changes on DD-specific cells, we, therefore, decided to test the therapeutic potential of new cytostatic drugs for DD treatment and/or for reduction of post-operative recurrence rates. The N-sulfonylpyrimidine derivative, amidino-substituted benzimidazo[1,2-a]quinoline, and amidino dihydrothienothienyl[2,3-c]quinolone hydrochloride, known to affect proliferation processes, were tested for their antiproliferative activity on primary fibroblasts/myofibroblasts cell cultures derived from the palmar fascia of patients with DD. Only amidino dihydrothienothienyl[2,3-c]quinolone hydrochloride acted in a highly specific manner on cells derived from diseased fascia of DD patients and exhibited a low cytotoxic effect. This result might be a consequence of its specific activity on cytoskeleton changes occurring in differentiating cells. A similar short-term differential antiproliferative effect was observed by the N-sulfonylpyrimidine derivative that was, however, completely lost after 6- and 14-day treatments. The amidino-substituted benzimidazo[1,2-a]quinoline exerted a strong non-specific, dose-related antiproliferative activity on cell types.

摘要

掌腱膜挛缩症(DD)是一种纤维增生性疾病,其治疗方法目前仍局限于手术切除受影响的筋膜,这往往导致高复发率。鉴于此,人们正在研究非手术治疗方法,其中包括针对掌腱膜挛缩症细胞培养中增殖和分化分子过程的治疗方法。具有抗增殖作用的药物可能对掌腱膜挛缩症的治疗有价值。因此,通过对掌腱膜挛缩症特异性细胞变化的表征,我们决定测试新型细胞毒性药物对掌腱膜挛缩症治疗和/或降低术后复发率的治疗潜力。已知会影响增殖过程的N-磺酰基嘧啶衍生物、脒基取代的苯并咪唑[1,2-a]喹啉和盐酸脒基二氢噻吩并[2,3-c]喹诺酮,对来自掌腱膜挛缩症患者掌腱膜的原代成纤维细胞/肌成纤维细胞培养物进行了抗增殖活性测试。只有盐酸脒基二氢噻吩并[2,3-c]喹诺酮对掌腱膜挛缩症患者患病筋膜来源的细胞具有高度特异性作用,且细胞毒性较低。这一结果可能是其对分化细胞中发生的细胞骨架变化具有特异性活性的结果。N-磺酰基嘧啶衍生物也观察到了类似的短期差异抗增殖作用,然而,在6天和14天的治疗后,这种作用完全消失。脒基取代的苯并咪唑[1,2-a]喹啉对细胞类型具有强烈的非特异性、剂量相关的抗增殖活性。

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