Synthesis of magnolol and honokiol derivatives and their effect against hepatocarcinoma cells.
Synthesis of magnolol and honokiol derivatives and their effect against hepatocarcinoma cells.
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DOI：
10.1371/journal.pone.0192178
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发表时间：
2018
期刊：
影响因子：
3.7
通讯作者：
Delogu G
中科院分区：
文献类型：
--
作者：
Maioli M;Basoli V;Carta P;Fabbri D;Dettori MA;Cruciani S;Serra PA;Delogu G
肝细胞癌是最常见的恶性肿瘤之一，因其进展快，对常规化疗耐药，死亡率高。因此，寻找新的治疗线索是全球关注的问题。因此，对厚朴和厚朴的主要成分厚朴酚1和和厚朴酚2的一小部分衍生物进行了体外肿瘤肝细胞实验。通过对厚朴酚1和和厚朴酚2在合适的酯类衍生物中的羟基进行仔细的转化，采用亲药策略来提高化合物的生物活性。化合物10和11在浓度降至1μM时比亲代和厚朴酚2更有效，在80μM浓度下处理的成纤维细胞完全存活。和厚朴酚结构中丁酸酯和裸酚羟基的组合似乎在抗增殖活性中发挥了重要作用，确定了一条有趣的抗肝细胞癌的药理线索。
The hepatocellular carcinoma is one of the most common malignant tumour with high level of mortality rate due to its rapid progression and high resistance to conventional chemotherapies. Thus, the search for novel therapeutic leads is of global interest. Herein, a small set of derivatives of magnolol 1 and honokiol 2, the main components of Magnolia grandiflora and Magnolia obovata, were evaluated in in vitro assay using tumoral hepatocytes. The pro-drug approach was applied as versatile strategy to the improve bioactivity of the compounds by careful transformation of the hydroxyl groups of magnolol 1 and honokiol 2 in suitable ester derivatives. Compounds 10 and 11 resulted to be more potent than the parental honokiol 2 at concentration down to 1 μM with complete viability of treated fibroblast cells up to concentrations of 80 μM. The combination of a butyrate ester and a bare phenol-OH group in the honokiol structure seemed to play a significant role in the antiproliferative activity identifying an interesting pharmacological clue against hepatocellular carcinoma.
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