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Archive > Volume 10 Issue 3 > 2018,10(3):323-330 Prev Next

7-O-氨基酸取代白楊素衍生物的合成及抗腫瘤活性

Original articles

Synthesis and anti-tumor activities of novel 7-O-amino acids chrysin derivatives

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    摘要:
    目的：設(shè)計(jì)并合成一系列白楊素衍生物，用MTT法測定化合物抗腫瘤活性，并研究其分子結(jié)構(gòu)與分子對接的構(gòu)效關(guān)系。方法：依次通過取代反應(yīng)，水解反應(yīng)，酯化反應(yīng)，皂化反應(yīng)等以高產(chǎn)率合成目標(biāo)產(chǎn)物，并用人胃癌細(xì)胞系MGC-803和人乳腺癌細(xì)胞株MCF-7通過標(biāo)準(zhǔn)的MTT法測定化合物活性。用Sybyl X-2.0版的Surflex Geom X程序計(jì)算分子對接結(jié)果。結(jié)果：合成了7-O-氨基酸白楊素衍生物6a-6l，并通過與母體白楊素以及陽性對照藥物5-氟尿嘧啶（5-FU）比較，評價其對腫瘤細(xì)胞的抑制作用。 在這些衍生物中，化合物5b（IC50 = 24.50 ± 2.26 μmol/L），5k（IC50 = 24.30 ± 2.19 μmol/L）和6f（IC50 = 24.61 ± 2.01 μmol/L）對MGC-803細(xì)胞具有更好的抑制活性?；衔?g（IC50 = 13.15±1.73μmol/ L）和5j（IC50 = 12.34 ± 1.25 μmol/L）對MCF-7細(xì)胞的抑制活性優(yōu)于白楊素和5-FU。 結(jié)合MTT實(shí)驗(yàn)結(jié)果，分子對接評分顯示出可信的一致性。結(jié)論：化合物5b，5d，5g，5j，5k和6f對特定腫瘤細(xì)胞具有良好的抗增殖作用。結(jié)合分子對接實(shí)驗(yàn)，化合物5g值得進(jìn)一步研究。

    Abstract:
    Objective To design and synthesize a series of chrysin derivatives and evaluate the antitumor activities with MTT assay, so as to investigate molecular structure-activity relationship with molecular docking. Methods Target products were synthesized with high yield by substitution reaction, hydrolysis reaction, esterification reaction, and saponification reaction in sequence, and activities of all compounds were evaluated with human gastric carcinoma cell lines MGC-803 and human breast carcinoma cell lines MCF-7 through standard MTT assay. Molecular docking results were calculated with Surflex Geom X programme of Sybyl X-2.0 version workstation. Results 7-O-amino acids chrysin derivatives 6a-6l were synthesized and their inhibitory effects were evaluated by comparing the material chrysin with positive control drug 5-fluorouracil (5-FU). Among these derivatives, compound 5b (IC50 = 24.50 ± 2.26 μmol/L), 5k (IC50 = 24.30 ± 2.19 μmol/L), and 6f (IC50 = 24.61 ± 2.01 μmol/L) showed better inhibitory activities against MGC-803 cell lines, and compound 5g (IC50 = 13.15 ± 1.73 μmol/L) and 5j (IC50 = 12.34 ± 1.25 μmol/L) showed better inhibitory activities against MCF-7 cell lines than chrysin and 5-FU. Molecular docking scores showed a credible consistency compared with MTT results. Conclusion Compounds 5b, 5d, 5g, 5j, 5k, and 6f showed good antiproliferative effects on specific tumor cells, and compound 5g should be researched further when according to molecular docking.

    關(guān)鍵詞:
    氨基酸白楊素衍生物;抗腫瘤;分子對接;合成

    Keywords:


    Project Supported:
    Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study (No. 2014-405) and Hunan Provincial Department of Education Project (14C1003)

    Clc Number:

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