CHEMICAL ENGINEERING JOURNAL
·
2024
·
IF 13.3
Linwei Chen,Qin Wang,Yong Jiang,Liu Xu,Nina Wei,Chang Lu,Chenqi Chang,Dandan Song,Yutong Wang,Li Wu,Weidong Li,Xiaobin Jia,Kaijun Zhao,Haibing Hua,Rui Chen,Zhipeng Chen
Cisplatin is a broad-spectrum antitumour agent, but its toxic side effects are severe. In clinical practice, cisplatin is typically administered intravenously, leading to unavoidable systemic toxicity, whereas oral administration of cisplatin is ineffective. In order to enhance the oral effectiveness of cisplatin and decrease its toxicity, a novel peptide was developed to act as an orally delivering carrier for platinum-based nanomedicine. This peptide naturally exhibited inhibitory effects on endothelial cells and angiogenesis. After being modified into a circular structure, its stability and tissue penetration ability were enhanced. Interestingly, it also demonstrated the ability to undergo self-assembly in aqueous environments and form tube-like nanomedicine when cisplatin was added. Oral administration of these nanotubes has shown remarkable structural stability, permeability across mucosal membranes, and a high selective uptake of cancer cells, resulting in a synergistic antitumour effect through the combined action of inhibiting blood vessel formation and suppressing cell proliferation in gastric cancer (GC). Our research has successfully demonstrated that Pt-chelated peptides possess the self-assembling potential to construct platinum-based nanomedicine for the oral treatment of GC.
研究领域:
肿瘤学
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药剂学
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纳米医学
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Na Li,Kaiyue Liu,Yue Zhang,Zhenzhen Hui,Ping Wang,Shuyang Sun,Chao Du
This study aimed to identify novel peptides with α-glucosidase inhibitory activity from Meretrix meretrix Linnaeus hydrolysates (MMLHs) following simulated gastrointestinal digestion (SGD) and to elucidate their inhibitory mechanisms. The molecular weight distribution of MMLHs progressively decreased during SGD, with hydrolysates from the intestinal digestion phase (MMLHs-I) exhibiting the strongest α-glucosidase inhibition (IC 50 : 0.14 ± 0.02 mg/mL). A total of 127 peptides were identified in MMLHs-I, among which 58 were unique compared to those from the gastric digestion phase. In silico screening and molecular docking identified six novel peptides—FAGDDAPR, VPLF, YRRL, WDH, PPLA, and WSG—with significant α-glucosidase inhibitory activity, displaying IC 50 values of 0.90, 1.30, 1.90, 1.20, 1.00, and 1.80 mg/mL, respectively. Among them, FAGDDAPR and PPLA exhibited the highest bioactivity. Kinetic analysis and fluorescence quenching assays demonstrated that both peptides acted as mixed-type inhibitors, forming stable complexes with α-glucosidase. Their inhibitory effects were primarily driven by hydrogen bonding and hydrophobic interactions, which hindered substrate binding and induced conformational changes in the enzyme. These findings suggest that peptides derived from MMLHs through gastrointestinal digestion possess potential antidiabetic properties, highlighting their promise as functional food ingredients for mitigating hyperglycemic damage.
研究领域:
食品科学
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生物化学
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产品关联
DOI
PubMed
高影响因子
International Journal of Peptide Research and Therapeutics
·
2024
·Vol. 30
·期 5
·1-13
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IF 2
Liu Ziyang,Wei Yuping,Zhang Man,Zhu Xingyan,Liu Kun
Angiotensin-converting enzyme-2 (ACE2) is a important cell surface receptor of SARS-CoV-2 S protein. The initial stage of SARS-COV-2 cell infection involves the binding of the S protein to ACE2. Hence, this work presents an innovative strategy to designing ACE2-based peptide inhibitors by considering the surface property and morphology of the S protein RBD. The aim is to develop a short peptide inhibitor that can effectively inhibit S protein-ACE2 interaction Through computational analysis and molecular simulation, the surface properties and morphology of S protein receptor-binding structural domain (RBD) were investigated, while the key residues of ACE2 ligand-binding structural domain (LBD) were identified based on their contributions and non-covalent interactions. Then, peptide inhibitors, consisting of ACE2 key residues, were developed by fitting to the surface characteristics and topographical features of the S protein RBD. Molecular simulation showed that two novel short peptides, IEPFF (I5) and WIEPFF (W6) had high affinity for S protein RBD but a low affinity for the cell membrane. Cellular adsorption studies demonstrated that both I5 and W6 effectively blocked ACE2-S protein binding without significant cytotoxicity. Flow cytometry analysis revealed that both I5 and W6 effectively inhibited S protein binding to the ACE2, resulting in a significant reduction (75 and 79%, respectively) in fluorescence intensity after 30 min of incubation at a concentration of 200 μM. Both I5 and W6 were excellent potential anti SARS-COV-2 drugs. This work provides an innovative perspective for the development of functional peptides for the prevention and management of SARS-COV-2.
研究领域:
生物化学
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分子生物学
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病毒学
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药学
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计算生物学
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产品关联
DOI
高影响因子
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