| Novel synovial targeting peptide-sinomenine conjugates as a potential strategy for the treatment of rheumatoid arthritis | |
| Zhang, Tianyue1,2; Ouyang, Xu1,2; Gou, Sanhu1,2; Zhang, Yun1,2; Yan, Na1; Chang, Linlin1,2; Li, Beibei1,2; Zhang, Fangyan1,2; Liu, Hui1,2; Ni, Jingman1,2,3 | |
| 2022-04-05 | |
| Online publication date | 2022-03 |
| Source Publication | INTERNATIONAL JOURNAL OF PHARMACEUTICS Impact Factor & Quartile |
| ISSN | 0378-5173 |
| EISSN | 1873-3476 |
| Volume | 617 |
| page numbers | 12 |
| Abstract | Sinomenine (SIN) is an effective anti-inflammatory agent, but its therapeutic efficacy is limited by its short halflife and the high dosage required. Tissue-specific strategies have the potential to overcome these limitations. The synovial homing peptide (CKSTHDRLC) was identified to have high synovial endothelium targeting affinity. In this work, two peptide-drug conjugates (PDCs), conjugate (L) and conjugate (C), were synthesized, in which SIN was covalently connected to the linear and cyclic synovial homing peptide, respectively, via a 6-aminocaproic acid linker. An evaluation of biostability showed that conjugate (C) was more stable in mouse serum and inflammatory joint homogenate than conjugate (L). The two conjugates gradually released free SIN. Interestingly, conjugate (L) self-cyclized via a disulfide bridge in a biological environment, which significantly impacted its biostability. It had an almost equipotent half-life in serum but faster degradation in the inflammatory joint than conjugate (C). Therefore, conjugate (C) exhibited better therapeutic efficacy and tissue targeting. All the results indicated that PDCs particularly in its cyclic form might be more efficient for targeted deliver and represent a potential strategy for the treatment of rheumatoid arthritis. |
| Keyword | Peptide-drug conjugates Sinomenine Rheumatoid arthritis Target delivery |
| Publisher | ELSEVIER |
| DOI | 10.1016/j.ijpharm.2022.121628 |
| Indexed By | SCIE |
| Language | 英语 |
| WOS Research Area | Pharmacology & Pharmacy |
| WOS Subject | Pharmacology & Pharmacy |
| WOS ID | WOS:000773658400004 |
| Original Document Type | Article |
| PMID | 35245636 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | https://ir.lzu.edu.cn/handle/262010/480234 |
| Collection | 兰州大学 |
| Corresponding Author | Liu, Hui; Ni, Jingman |
| Affiliation | 1.Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China; 2.Lanzhou Univ, Sch Basic Med Sci, Key Lab Preclin Study New Drugs Gansu Prov, Lanzhou 730000, Peoples R China; 3.Macau Univ Sci & Technol, State Key Lab Qual Res Chinese Med, Ave Wai Long, Taipa 999078, Macao, Peoples R China |
| Recommended Citation GB/T 7714 | Zhang, Tianyue,Ouyang, Xu,Gou, Sanhu,et al. Novel synovial targeting peptide-sinomenine conjugates as a potential strategy for the treatment of rheumatoid arthritis[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2022,617. |
| APA | Zhang, Tianyue.,Ouyang, Xu.,Gou, Sanhu.,Zhang, Yun.,Yan, Na.,...&Ni, Jingman.(2022).Novel synovial targeting peptide-sinomenine conjugates as a potential strategy for the treatment of rheumatoid arthritis.INTERNATIONAL JOURNAL OF PHARMACEUTICS,617. |
| MLA | Zhang, Tianyue,et al."Novel synovial targeting peptide-sinomenine conjugates as a potential strategy for the treatment of rheumatoid arthritis".INTERNATIONAL JOURNAL OF PHARMACEUTICS 617(2022). |
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