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您的检索式：作者名="DONG Chune"
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| 1 | Development of composite PLGA microspheres containing exenatide-encapsulated lecithin nanoparticles for sustained drug release显示文摘This study aimed to prepare poly(D, L-lactic-co-glycolic acid) microspheres(PLGA-Ms)by a modified solid-in-oil-in-water(S/O/W) multi-emulsion technique in order to achieve sustained release with reduced initial burst and maintain efficient drug concentration for a prolonged period of time. Composite PLGA microspheres containing exenatideencapsulated lecithin nanoparticles(Ex-NPs-PLGA-Ms) were obtained by initial fabrication of exenatide-loaded lecithin nanoparticles(Ex-NPs) via the alcohol injection method,followed by encapsulation of Ex-NPs into PLGA microspheres. Compared to Ms prepared by the conventional water-in-oil-in-water(W/O/W) technique(Ex-PLGA-Ms), Ex-NPs-PLGAMs showed a more uniform particle size distribution, reduced initial burst release, and sustained release for over 60 d in vitro. Cytotoxicity studies showed that Ms prepared by both techniques had superior biocompatibility without causing any detectable cytotoxicity.In pharmacokinetic studies, the effective drug concentration was maintained for over 30 d following a single subcutaneous injection of two types of Ms formulation in rats, potentially prolonging the therapeutic action of Ex. In addition, administration of Ex-NPs-PLGA-Ms resulted in a more smooth plasma concentration-time profile with a higher area under the curve(AUC) compared to that of Ex-PLGA-Ms. Overall, Ex-NPs-PLGA-Ms prepared by the novel S/O/W method could be a promising sustained drug release system with reduced initial burst release and prolonged therapeutic efficacy. | Ni Dong Chune Zhu Junhuang Jiang Di Huang Xing Li Guilan Quan Yang Liu Wen Tan Xin Pan Chuanbin Wu | 2020 | Asian Journal of Pharmaceutical Sciences2020，15，3： | 7 |
| 2 | Micro-electro-mechanical systems (MEMS)-based micro-scale direct methanol fuel cell development显示文摘 | Yao Shi Chune Tang Xu Dong Hsieh Cheng Chieh | 2006 | Energy2006，31，5： | 1 |
| 3 | Enantioselective Chlorocyclization of Olefinic Amides with 1,3-Dichloro-5,5-Dimethylhydantoin(DCDMH) Catalyzed by(DHQD)2PHAL显示文摘 | ZHOU Qingjun GUO Chao LI Xiwang HE Pei YANG Guichun DONG Chune | 2018 | Wuhan University Journal of Natural Sciences2018，23，3： | 0 |
| 4 | Discovery of novel covalent selective estrogen receptor degraders against endocrine-resistant breast cancer显示文摘Endocrine-resistance remains a major challenge in estrogen receptorαpositive(ERα^(+))breast cancer(BC)treatment and constitutively active somatic mutations in ERαare a common mechanism.There is an urgent need to develop novel drugs with new mode of mechanism to fight endocrineresistance.Given aberrant ERαactivity,we herein report the identification of novel covalent selective estrogen receptor degraders(cSERDs)possessing the advantages of both covalent and degradation strategies.A highly potent cSERD 29c was identified with superior anti-proliferative activity than fulvestrant against a panel of ERa+breast cancer cell lines including mutant ERα.Crystal structure of ERα-29c complex alongside intact mass spectrometry revealed that 29c disrupted ERa protein homeostasis through covalent targeting C530 and strong hydrophobic interaction collied on H11,thus enforcing a unique antagonist conformation and driving the ERαdegradation.These significant effects of the cSERD on ERαhomeostasis,unlike typical ERαdegraders that occur directly via long side chains perturbing the morphology of H12,demonstrating a distinct mechanism of action(MoA).In vivo,29c showed potent antitumor activity in MCF-7 tumor xenograft models and low toxicity.This proof-of-principle study verifies that novel cSERDs offering new opportunities for the development of innovative therapies for endocrine-resistant BC. | Yubo Wang Jian Min Xiangping Deng Tian Feng Hebing Hu Xinyi Guo Yan Cheng Baohua Xie Yu Yang Chun-Chi Chen Rey-Ting Guo Chune Dong Hai-Bing Zhou | 2023 | Acta Pharmaceutica Sinica B2023，13，12： | 0 |
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