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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Lanthanide containing compounds for therapeutic care in bone resorption disorders
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Lanthanide containing compounds for therapeutic care in bone resorption disorders

机译：含镧系元素的化合物，可用于骨吸收疾病的治疗

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摘要

Lanthanide ions, Ln( III), are known functional mimics of Ca( II) ions and have been shown to affect the bone remodeling cycle. Exploiting this disruption to the bone remodeling cycle has potential for the treatment of bone density disorders, such as osteoporosis. In an effort to find new orally active agents for these disorders, a series of Ln( III) containing complexes incorporating small, non-toxic, bidentate pyrone and pyridinone ligands have been synthesized and characterized ( LnL(3), Ln = La, Eu, Gd, Tb, Yb, L = 3-oxy-2-methyl-4-pyrone (ma(-)), 3-oxy-2-ethyl-4-pyrone ( ema(-)), 3-oxy-1,2-dimethyl-4-pyridinone ( dpp(-)) and 3-oxy-2-methyl-4(1H)-pyridinone(mpp(-))). Preliminary biological analysis included cytotoxicity, cell uptake and bidirectional transport studies in Caco-2 cells and in vitro hydroxyapatite ( HA) binding studies. The proportion of intact compounds bound to HA was calculated based on determination of Ln( III) concentration by ICP-MS and by UV-vis spectrophotometric assay of the proligand in solution. The LnL(3) species were found to have IC50 values at least 6 times greater than that of cisplatin, >= 98% HA-binding capacity, and permeability coefficients in the moderate range. La( dpp)(3) was ascertained to be the lead compound for the treatment of bone density disorders with the highest percentage cell uptake of 9.07 +/- 2.33% and the highest preliminary P-app value of 3.54 +/- 2.86 x 10(-6) cm s(-1) compared to the other LnL(3) complexes tested.
机译：镧系元素离子Ln（III）是已知的Ca（II）离子功能模拟物，已显示会影响骨骼重塑周期。利用这种对骨骼重塑周期的破坏，具有治疗骨密度异常（例如骨质疏松症）的潜力。为了寻找用于这些疾病的新的口服活性剂，已合成并表征了一系列包含小，无毒，双齿吡喃酮和吡啶酮配体的Ln（III）配合物（LnL（3），Ln = La，Eu ，Gd，Tb，Yb，L = 3-氧-2-甲基-4-吡喃酮（ma（-）），3-氧-2-乙基-4-吡喃酮（ema（-）），3-氧-1 ，2-二甲基-4-吡啶酮（dpp（-））和3-氧-2-甲基-4（1H）-吡啶酮（mpp（-）））。初步的生物学分析包括Caco-2细胞的细胞毒性，细胞摄取和双向转运研究以及体外羟基磷灰石（HA）结合研究。基于ICP-MS和溶液中配体的紫外可见分光光度法测定Ln（III）浓度，计算与HA结合的完整化合物的比例。发现LnL（3）物种的IC50值至少是顺铂的IC50值的6倍以上，> = 98％的HA结合能力以及适中的渗透系数。 La（dpp）（3）被确定为治疗骨密度疾病的主要化合物，具有最高的细胞摄取百分比9.07 +/- 2.33％和最高的初始P-app值3.54 +/- 2.86 x 10 （-6）cm s（-1）与测试的其他LnL（3）复合物相比。

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