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Linear-like polypeptide-based micelle with pH-sensitive detachable PEG to deliver dimeric camptothecin for cancer therapy
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作者 Ka Hong Wong zhaopei Guo +4 位作者 Di Jiang Xingzhi Zhou Lizhu Lin denggao zhao Meiwan Chen 《Asian Journal of Pharmaceutical Sciences》 SCIE CAS 2023年第1期97-107,共11页
Nano drug delivery systems have made significant progress in delivering anticancer drugs camptothecin(CPT).However,many challenges for CPT delivery remain,including low drug loading efficiency,premature drug leakage,a... Nano drug delivery systems have made significant progress in delivering anticancer drugs camptothecin(CPT).However,many challenges for CPT delivery remain,including low drug loading efficiency,premature drug leakage,and poor cellular internalization.Herein,we report a novel dual-sensitive polypeptide-based micelle with remarkably high drug loading of CPT for cancer therapy.This self-assembled micelle possesses the following essential components for CPT:(1)pH-sensitive PEG(OHC-PEG-CHO)for prolonging blood circulation and allowing biocompatibility by shielding the cationic micelles,which can be detached under the tumor acidic microenvironment and facilitates the cellular uptake;(2)polypeptide polylysine-polyphenylalanine(PKF)synthesized via ring-opening polymerization for micelle formation and CPT analogue loading;(3)dimeric CPT(DCPT)with redox-sensitive linker for increasing CPT loading and ensuring drug release at tumor sites.Interestingly,the linear-like morphology of PEG-PKF/DCPT micelles was able to enhance their cellular internalization when compared with the spherical blank PKF micelles.Also,the anticancer efficacy of DCPT against lung cancer cells was significantly improved by the micelle formation.In conclusion,this work provides a promising strategy facilitating the safety and effective application of CPT in cancer therapy. 展开更多
关键词 Dimeric camptothecin PH-SENSITIVE Redox-responsive Cancer therapy Self-assembled micelle
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5-Demethylnobiletin and its major metabolites:efficient preparation and mechanism of their anti-proliferation activity in HepG2 cells
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作者 Yanping Xin Ting Zheng +7 位作者 Man Zhang Ruiqiang Zhang Siyue Zhu Dongli Li denggao zhao Yanyan Ma Chi-Tang Ho Qingrong Huang 《Food Science and Human Wellness》 SCIE 2022年第5期1191-1200,共10页
5-Demethylnobile tin(5-DMN),a hydroxylated polymethoxyflavone(OH-PMF)identified in aged citrus peels,has demonstrated health benefiting effects in previous studies.5-DMN undergoes biotransformation in vivo,yielding 5,... 5-Demethylnobile tin(5-DMN),a hydroxylated polymethoxyflavone(OH-PMF)identified in aged citrus peels,has demonstrated health benefiting effects in previous studies.5-DMN undergoes biotransformation in vivo,yielding 5,3’-didemethylnobiletin(5,3’-DDMN),5,4’-didemethylnobiletin(5,4’-DDMN)and5,3’,4’-tridemethylnobiletin(5,3’,4’-TDMN).However,the anti-cancer effects of 5-DMN and its in vivo metabolites against HepG2 cells remain unclear.In this study,an efficient chemical synthetic method was developed to obtain 5-DMN and its 3 metabolites,and their molecular structures were confirmed by;H NMR and LC-MS.Cytotoxicity,cell cycle arrestment,apoptosis and caspase-3 expression were investigated to evaluate the anti-liver cancer effects of these OH-PMFs on HepG2 cells.The results showed that all 4 compounds inhibited the proliferation of HepG2 cells in a concentration-dependent manner.Their anti-proliferative activity was exerted through inducing G2/M phase arrestment,cell apoptosis and promoting expression of a key apoptotic protein called cleaved caspase-3.Our results indicated that 5,3’-DDMN and5,3’,4’-TDMN showed a stronger inhibitory activity on cell proliferation than 5-DMN,followed by 5,4’-DDMN.The expression of cleaved caspase-3 was the highest in cells treated with 5,4’-DDMN,implying that the apoptosis induced by other OH-PMFs might be mediated by other apoptotic execution proteins.Our research reveals the application potential and scientific evidence for the production and functionality of OH-PMFs. 展开更多
关键词 Hydroxylated polymethoxyflavones Chemical synthesis HEPG2 Cell cycle APOPTOSIS
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