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首页> 外文期刊>RSC Advances >Triple-negative breast cancer suppressive activities, antioxidants and pharmacophore model of new acylated rhamnopyranoses from Premna odorata
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Triple-negative breast cancer suppressive activities, antioxidants and pharmacophore model of new acylated rhamnopyranoses from Premna odorata

机译：来自Premna Odorata的新酰化鼻窦抑制活性，抗氧化剂和药效模型

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摘要

Phytochemical investigation of Premna odorata Blanco "Lamiaceae" young stems afforded four new acylated rhamnopyranoses 1-4, along with fourteen known compounds 5-19. The structures of the new compounds were confirmed using extensive 1D, 2D NMR, and HRESIMS analysis. The isolated compounds were tested for their cell proliferation and migration inhibition activities against the invasive human triple-negative breast cancer cells MDA-MB-231 and MCF-7, and the normal human breast cell line MCF-10A. In addition, free radical scavenging activities using 2,2 '-diphenyl-1-picrylhydrazyl (DPPH) were studied. Compound 1 was the most active as an antiproliferative agent, showing a high to moderate antiproliferative effect with an IC50 value of 4.95 and 17.7 mu M against MCF-7 and MDA-MB-231, respectively. The antiproliferative activities of compounds 1-5 against the normal breast cell line MCF-10A were moderate to low with IC50 values of 13.91 to 27.70 mu M. On the other hand, compounds 1 and 10 suppressed MDA-MB-231 cell migration in the wound-healing assay at 10 mu M concentration. Meanwhile, compounds 1-5 exhibited the highest value of DPPH radical scavenging activities with an IC50 value range of 17.5-20.43 +/- 0.5 mu g mL(-1). The pharmacophore model generated using Molecular Operating Environment (MOE) for compounds 1-5 showed three hydrogen bond acceptors (HBAs), one hydrogen bond donor (HBD), one aromatic ring (Aro), and one hydrophobic (Hyd.) group. The central HBA feature lies at a distance of 4.36 angstrom and 6.38 angstrom from the remaining two HBA features. Also, the HBD feature maintains a distance of 2.74 angstrom from the aromatic feature. Acylated rhamnopyranoses can be considered good scaffolds for developing new anti-breast cancer and antioxidant compounds.
机译：Premna Odorata Blanco“LamiCeae”幼虫的植物化学研究得到了四种新的酰化萘吡喃吡喃物1-4，以及14个已知的化合物5-19。使用广泛的1D，2D NMR和Hresims分析确认新化合物的结构。对其细胞增殖和迁移抑制活性进行测试，针对侵入性人的三阴性乳腺癌细胞MDA-MB-231和MCF-7，以及正常人乳腺细胞系MCF-10a进行测试。此外，研究了使用2,2'-二苯基-1-富铬基（DPPH）的自由基清除活性。化合物1是最活性的抗增殖剂，显示出高于中等的抗增殖效果，分别与MCF-7和MDA-MB-231的IC50值为4.95和17.7μm。对正常乳房细胞系MCF-10a的化合物1-5的抗增殖活性与IC 50值为13.91至27.70μm的中等，另一方面，化合物1和10抑制了MDA-MB-231细胞迁移伤口愈合测定以10μm浓度。同时，化合物1-5表现出DPPH激进清除活性的最高值，IC 50值范围为17.5-20.43 +/-0.5μg（-1）。使用用于化合物1-5的分子运行环境（MOE）产生的药物光电模型显示了三种氢键受体（HBA），一种氢键供体（HBD），一种芳族环（ARO）和一种疏水性（REV。）组。中央HBA特征位于4.36埃·埃斯特朗斯和6.38埃的距离，剩余的两个HBA特征。此外，HBD特征从芳族特征维持2.74埃的距离。酰基化的鼻吡喃物可以被认为是用于开发新的抗乳腺癌和抗氧化剂化合物的良好支架。

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  • 来源
    《RSC Advances》 |2020年第18期|共15页
  • 作者

    Elmaidomy Abeer H.; Mohammed Rabab; Owis Asmsaa I.; Hetta Mona H.; AboulMagd Asmaa M.; Siddique Abu Bakar; Abdelmohsen Usama Ramadan; Rateb Mostafa E.; El Sayed Khalid A.; Hassan Hossam M.;

  • 作者单位

    Beni Suef Univ Fac Pharm Dept Pharmacognosy Bani Suwayf 62514 Egypt;

    Beni Suef Univ Fac Pharm Dept Pharmacognosy Bani Suwayf 62514 Egypt;

    Beni Suef Univ Fac Pharm Dept Pharmacognosy Bani Suwayf 62514 Egypt;

    Fayoum Univ Dept Pharmacognosy Fac Pharm Al Fayyum 63514 Egypt;

    Nahda Univ Dept Pharmaceut Chem Fac Pharm Bani Suwayf 62514 Egypt;

    Univ Louisiana Coll Pharm Sch Basic Pharmaceut &

    Toxicol Sci Monroe LA 71201 USA;

    Menia Univ Dept Pharmacognosy Fac Pharm Al Minya 61519 Egypt;

    Beni Suef Univ Fac Pharm Dept Pharmacognosy Bani Suwayf 62514 Egypt;

    Univ Louisiana Coll Pharm Sch Basic Pharmaceut &

    Toxicol Sci Monroe LA 71201 USA;

    Beni Suef Univ Fac Pharm Dept Pharmacognosy Bani Suwayf 62514 Egypt;

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  • 正文语种 eng
  • 中图分类 化学;
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