Harperoids A-F, Complex Polyprenylated Acylphloroglucinols from Harrisonia perforata that Reverse Multidrug Resistance by Targeting ABC Transporter Function
文献类型：期刊论文
| 作者 | An, Pei-Pei2,3; Li, Ying1; Yu, Jin-Hai1; Zhou, Bin2; Yue, Jian-Min1,2,3 |
| 刊名 | JOURNAL OF ORGANIC CHEMISTRY
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| 出版日期 | 2026-02-20 |
| 卷号 | 91期号:7页码:2915-2927 |
| ISSN号 | 0022-3263 |
| DOI | 10.1021/acs.joc.5c03053 |
| 英文摘要 | Utilizing an LC/MS-MS-based feature-based molecular networking (FBMN) strategy, six undescribed PPAPs (1-6) characterized by an acetyl substituent at the C-1 position of their phloroglucinol scaffold, were efficiently isolated from the roots of Harrisonia perforata. Notably, compund 1 displays an unconventional 5/5/6/5 ring architecture, while compounds 5 and 6 represent the first case incorporating a benzofuran core and a geranyl-derived cyclohexanol unit. Their structures were unequivocally elucidated through comprehensive spectroscopic data analysis, TDDFT-ECD calculations, and X-ray crystallographic studies. Interestingly, compound 3 at 20 mu M exhibited negligible cytotoxicity but significantly potentiated the activity of paclitaxel against HCT-15 cells by 42.8-fold. Mechanistic studies further demonstrated that compound 3 did not significantly alter the expression levels of ATP-binding cassette (ABC) transporters, but potently inhibited the transport function of both ABCB1 and ABCG2. Molecular docking reveals that compound 3 stably binds to the central substrate-binding cavities of ABCB1 and ABCG2, with its binding primarily stabilized by hydrogen bonds and hydrophobic interactions. |
| WOS关键词 | PROMISING BIOLOGICAL-ACTIVITY ; CORE |
| 资助项目 | Chinese Academy of Sciences[XDB0830000] ; National Natural Science Foundation of China[22494691] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001685279400001 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/322836]  |
| 专题 | 国家级研究中心_原创新药研究全国重点实验室 |
| 通讯作者 | Zhou, Bin; Yue, Jian-Min |
| 作者单位 | 1.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 3.Lanzhou Univ, Coll Chem & Chem Engn, State Key Lab Appl Organ Chem, Lanzhou 730000, Peoples R China |
| 推荐引用方式 GB/T 7714 | An, Pei-Pei,Li, Ying,Yu, Jin-Hai,et al. Harperoids A-F, Complex Polyprenylated Acylphloroglucinols from Harrisonia perforata that Reverse Multidrug Resistance by Targeting ABC Transporter Function[J]. JOURNAL OF ORGANIC CHEMISTRY,2026,91(7):2915-2927. |
| APA | An, Pei-Pei,Li, Ying,Yu, Jin-Hai,Zhou, Bin,&Yue, Jian-Min.(2026).Harperoids A-F, Complex Polyprenylated Acylphloroglucinols from Harrisonia perforata that Reverse Multidrug Resistance by Targeting ABC Transporter Function.JOURNAL OF ORGANIC CHEMISTRY,91(7),2915-2927. |
| MLA | An, Pei-Pei,et al."Harperoids A-F, Complex Polyprenylated Acylphloroglucinols from Harrisonia perforata that Reverse Multidrug Resistance by Targeting ABC Transporter Function".JOURNAL OF ORGANIC CHEMISTRY 91.7(2026):2915-2927. |
入库方式： OAI收割
来源：上海药物研究所
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