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本文引用的文献

1
Nitrogen Permease Regulator-Like-2 Exhibited Anti-Tumor Effects And Enhanced The Sensitivity Of Colorectal Cancer Cells To Oxaliplatin And 5-Fluorouracil.类氮通透酶调节蛋白-2具有抗肿瘤作用,并增强了结肠癌细胞对奥沙利铂和5-氟尿嘧啶的敏感性。
Onco Targets Ther. 2019 Oct 18;12:8637-8644. doi: 10.2147/OTT.S219562. eCollection 2019.
2
Bias-adjusted Kaplan-Meier survival curves for marginal treatment effect in observational studies.观察性研究中边缘治疗效应的偏差调整Kaplan-Meier生存曲线。
J Biopharm Stat. 2019;29(4):592-605. doi: 10.1080/10543406.2019.1633659. Epub 2019 Jul 9.
3
Development of Moxifloxacin Hydrochloride loaded gel for the treatment of periodontitis: drug release study and antibacterial activity.用于治疗牙周炎的载盐酸莫西沙星凝胶的研制:药物释放研究及抗菌活性
J Oral Biol Craniofac Res. 2019 Jul-Sep;9(3):190-200. doi: 10.1016/j.jobcr.2019.04.001. Epub 2019 Apr 12.
4
Normal Body Temperature: A Systematic Review.正常体温:一项系统评价。
Open Forum Infect Dis. 2019 Apr 9;6(4):ofz032. doi: 10.1093/ofid/ofz032. eCollection 2019 Apr.
5
Comparison of the anesthetic effects of 2,2,2-tribromoethanol on ICR mice derived from three different sources.三种不同来源的ICR小鼠对2,2,2-三溴乙醇麻醉效果的比较。
Lab Anim Res. 2018 Dec;34(4):270-278. doi: 10.5625/lar.2018.34.4.270. Epub 2018 Dec 31.
6
Tolmetin sodium-loaded thermosensitive mucoadhesive liquid suppositories for rectal delivery; strategy to overcome oral delivery drawbacks.载有痛灭定钠的热敏型粘膜粘附性直肠用液体栓剂;克服口服给药缺陷的策略。
Drug Dev Ind Pharm. 2019 Feb;45(2):252-264. doi: 10.1080/03639045.2018.1534858. Epub 2018 Oct 31.
7
Effects of a Peganum harmala (Zygophyllaceae) preparation for root canal disinfection.苦豆子(蒺藜科)制剂对根管消毒的影响。
Phytother Res. 2018 Apr;32(4):672-677. doi: 10.1002/ptr.6015. Epub 2018 Jan 24.
8
Harmine suppresses the proliferation and migration of human ovarian cancer cells through inhibiting ERK/CREB pathway.哈尔敏通过抑制 ERK/CREB 通路抑制人卵巢癌细胞的增殖和迁移。
Oncol Rep. 2017 Nov;38(5):2927-2934. doi: 10.3892/or.2017.5952. Epub 2017 Sep 13.
9
Synthesis, characterisation and phase transition behaviour of temperature-responsive physically crosslinked poly (N-vinylcaprolactam) based polymers for biomedical applications.用于生物医学应用的温敏型物理交联聚(N-乙烯基己内酰胺)基聚合物的合成、表征及相转变行为。
Mater Sci Eng C Mater Biol Appl. 2017 Oct 1;79:130-139. doi: 10.1016/j.msec.2017.03.241. Epub 2017 Mar 29.
10
Preparation, pharmacokinetics and pharmacodynamics of ophthalmic thermosensitive in situ hydrogel of betaxolol hydrochloride.盐酸倍他洛尔眼用热敏原位凝胶的制备、药代动力学及药效学
Biomed Pharmacother. 2016 Oct;83:107-113. doi: 10.1016/j.biopha.2016.06.024. Epub 2016 Jun 23.

通过热敏凝胶负载去氢骆驼蓬碱改善结直肠癌治疗的抗肿瘤效果

Improving anti-tumor outcomes for colorectal cancer therapy through thermosensitive gel loading harmine.

作者信息

Li Zhenzhen, Chen Liqing, He Chenghui, Han Ying, Han Mingfeng, Zhang Yingying, Qi Lingling, Xing Xuezhong, Huang Wei, Gao Zhonggao, Xing Jianguo

机构信息

Key Laboratory of Xinjiang Endemic Phytomedicine Resources of Ministry of Education, School of Pharmacy, Shihezi University Shihezi 832003, China.

State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Department of Pharmaceutics, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College Beijing 100050, China.

出版信息

Am J Transl Res. 2020 May 15;12(5):1658-1671. eCollection 2020.

PMID:32509167
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7270021/
Abstract

Colorectal cancer is a common malignant tumor that seriously endangers human health. Harmine (HM), a natural product, has been shown to have a significant inhibitory effect on various cancers. However, systemic injection of HM can cause central nervous toxicity, which limits its clinical application. Local administration of HM overcomes this problem to a certain extent. In this study, we prepared an thermosensitive HM gel preparation (HM gel), and used it to treat colon cancer with reduced toxic side effects and prolonged residence time of HM at the tumor site. We employed a central composite design and response surface methodology to optimize the formulation, and evaluated the physicochemical properties, rectal retention capacity, and and antitumor effects of HM gel on colon 26 tumor cells. The results showed that HM gel had a significant inhibitory effect on the growth of colon 26 cells . In an orthotopic tumor-bearing mouse model, HM gel exhibited an obvious inhibitory effect on tumor growth and metastasis, and significantly prolonged the survival period. In conclusion, HM gel exhibited significant anti-tumor effects on colon cancer, and therefore presents a promising formulation for the treatment of colorectal cancer.

摘要

结直肠癌是一种严重危害人类健康的常见恶性肿瘤。哈尔明碱(HM)是一种天然产物,已被证明对多种癌症具有显著的抑制作用。然而,全身注射HM会引起中枢神经毒性,这限制了其临床应用。局部给药HM在一定程度上克服了这个问题。在本研究中,我们制备了一种热敏性HM凝胶制剂(HM凝胶),并用其治疗结肠癌,降低了毒副作用,延长了HM在肿瘤部位的滞留时间。我们采用中心复合设计和响应面法优化配方,并评估了HM凝胶的理化性质、直肠滞留能力以及对结肠26肿瘤细胞的抗肿瘤作用。结果表明,HM凝胶对结肠26细胞的生长具有显著的抑制作用。在原位荷瘤小鼠模型中,HM凝胶对肿瘤生长和转移表现出明显的抑制作用,并显著延长了生存期。总之,HM凝胶对结肠癌表现出显著的抗肿瘤作用,因此是一种有前途的结直肠癌治疗制剂。