利用PL3归巢肽和细胞穿透肽提高抗肿瘤靶向性

Q3 Pharmacology, Toxicology and Pharmaceutics
Dhafir Masheta, Shafq Al-azzawi
{"title":"利用PL3归巢肽和细胞穿透肽提高抗肿瘤靶向性","authors":"Dhafir Masheta, Shafq Al-azzawi","doi":"10.18413/rrpharmacology.9.10028","DOIUrl":null,"url":null,"abstract":"Introduction: Tumor-homing peptides have gained great attention as tools for the development of non-invasive and targeting drug delivery systems (DDS) to minimize drug systemic toxicity and enhance bioavailability. This study aims to improve antitumor targeting in prostate cancer via uploading a drug to a DDS comprised of a cell penetrating peptide decorated with a tumor-homing peptide, PL3.\nMaterial and Methods: The DDS was constructed via solid-phase peptide synthesis and then characterized via mass spectrum and high performance liquid chromatography. A cell viability assessment to evaluate its cytotoxicity on both tumor (prostate cancer cells) and normal cells was conducted, while a confocal laser scanning microscope and flow-cytometer were employed to investigate internalization. To inspect the effectiveness of the drug-loaded DDS, a biochemical enzyme inhibition assay on the target enzyme dihydrofolate reductase (DHFR) was performed. ‎\nResults and Discussion:‏ The findings supported the succeeded synthesis and loading of the drug into this carrier system and demonstrated its high efficacy in cytotoxic effect and inhibiting DHFR with considerable cellular uptake in prostate cancer cells.\nConclusion: The drug was delivered to the target prostate cancer cells by the PL3-functionalized DDS, limiting its localization to tumor cells rather than normal cells. Therefore, the study results highlighted the significance of the DDS in tumor therapy interventions.\nGraphical Abstact","PeriodicalId":21030,"journal":{"name":"Research Results in Pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2023-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Improving antitumor targeting via using PL3 homing peptide and cell-penetrating peptide\",\"authors\":\"Dhafir Masheta, Shafq Al-azzawi\",\"doi\":\"10.18413/rrpharmacology.9.10028\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Introduction: Tumor-homing peptides have gained great attention as tools for the development of non-invasive and targeting drug delivery systems (DDS) to minimize drug systemic toxicity and enhance bioavailability. This study aims to improve antitumor targeting in prostate cancer via uploading a drug to a DDS comprised of a cell penetrating peptide decorated with a tumor-homing peptide, PL3.\\nMaterial and Methods: The DDS was constructed via solid-phase peptide synthesis and then characterized via mass spectrum and high performance liquid chromatography. A cell viability assessment to evaluate its cytotoxicity on both tumor (prostate cancer cells) and normal cells was conducted, while a confocal laser scanning microscope and flow-cytometer were employed to investigate internalization. To inspect the effectiveness of the drug-loaded DDS, a biochemical enzyme inhibition assay on the target enzyme dihydrofolate reductase (DHFR) was performed. ‎\\nResults and Discussion:‏ The findings supported the succeeded synthesis and loading of the drug into this carrier system and demonstrated its high efficacy in cytotoxic effect and inhibiting DHFR with considerable cellular uptake in prostate cancer cells.\\nConclusion: The drug was delivered to the target prostate cancer cells by the PL3-functionalized DDS, limiting its localization to tumor cells rather than normal cells. Therefore, the study results highlighted the significance of the DDS in tumor therapy interventions.\\nGraphical Abstact\",\"PeriodicalId\":21030,\"journal\":{\"name\":\"Research Results in Pharmacology\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2023-06-06\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Research Results in Pharmacology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.18413/rrpharmacology.9.10028\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Research Results in Pharmacology","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.18413/rrpharmacology.9.10028","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
引用次数: 0

摘要

导论:肿瘤归巢肽作为开发非侵入性和靶向药物传递系统(DDS)的工具,以最大限度地减少药物的全身毒性和提高生物利用度,受到了广泛的关注。本研究旨在通过将药物上传给由细胞穿透肽修饰的肿瘤归巢肽PL3组成的DDS,提高前列腺癌的抗肿瘤靶向性。材料与方法:采用固相多肽合成法构建DDS,并通过质谱和高效液相色谱对其进行表征。采用细胞活力评估法评估其对肿瘤(前列腺癌细胞)和正常细胞的细胞毒性,并采用共聚焦激光扫描显微镜和流式细胞仪研究其内化作用。为了检验载药DDS的有效性,进行了对靶酶二氢叶酸还原酶(DHFR)的生化酶抑制实验。结果和讨论:该研究结果支持了该药物的成功合成和装载到该载体系统中,并证明了其在前列腺癌细胞中具有细胞毒作用和抑制DHFR的高效,并且具有相当大的细胞摄取。结论:该药物通过pl3功能化的DDS传递到靶前列腺癌细胞中,限制了其定位于肿瘤细胞而非正常细胞。因此,本研究结果强调了DDS在肿瘤治疗干预中的重要意义。图形摘要
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Improving antitumor targeting via using PL3 homing peptide and cell-penetrating peptide
Introduction: Tumor-homing peptides have gained great attention as tools for the development of non-invasive and targeting drug delivery systems (DDS) to minimize drug systemic toxicity and enhance bioavailability. This study aims to improve antitumor targeting in prostate cancer via uploading a drug to a DDS comprised of a cell penetrating peptide decorated with a tumor-homing peptide, PL3. Material and Methods: The DDS was constructed via solid-phase peptide synthesis and then characterized via mass spectrum and high performance liquid chromatography. A cell viability assessment to evaluate its cytotoxicity on both tumor (prostate cancer cells) and normal cells was conducted, while a confocal laser scanning microscope and flow-cytometer were employed to investigate internalization. To inspect the effectiveness of the drug-loaded DDS, a biochemical enzyme inhibition assay on the target enzyme dihydrofolate reductase (DHFR) was performed. ‎ Results and Discussion:‏ The findings supported the succeeded synthesis and loading of the drug into this carrier system and demonstrated its high efficacy in cytotoxic effect and inhibiting DHFR with considerable cellular uptake in prostate cancer cells. Conclusion: The drug was delivered to the target prostate cancer cells by the PL3-functionalized DDS, limiting its localization to tumor cells rather than normal cells. Therefore, the study results highlighted the significance of the DDS in tumor therapy interventions. Graphical Abstact
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
Research Results in Pharmacology
Research Results in Pharmacology Medicine-Pharmacology (medical)
CiteScore
1.50
自引率
0.00%
发文量
32
审稿时长
12 weeks
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信