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Identification of 2-aminothiazoyl piperidine derivatives as a new class of adjuvants potentiating the activity of colistin against Acinetobacter baumannii

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Chinese Chemical Letters 2023年第2期34卷 468-474页

作者： Yuce Chen Zhen Li Yu Yin Ping Yang Yijin Kong Zhong Li Daijie Chen Xiaoyong Xu Shanghai Key Laboratory of Chemical Biology School of PharmacyEast China University of Science and TechnologyShanghai 200237China School of Pharmacy Shanghai JiaoTong UniversityShanghai 200240China

The rapid prevalence of antibiotic resistance has led to a significant global health problem. Although colistin is the last resort antibiotic, it is limited by dose dependent toxicity. A critical approach to solve this problem is to use an antibiotic adjuvant, which is able to potentiate the activity of antibiotic and reduce the dosage of antibiotic. Herein, we reported a novel 2-aminothiazoyl piperidine adjuvant, which enhanced the activity of colistin against Acinetobacter baumannii(A. baumannii). Two pilot libraries of 40compounds were prepared and their adjuvant activities were evaluated. The most potential compound11j enabled to cause16-fold reduction in the minimum inhibitory concentration(MIC) of colistin at 8μg/m L. Besides, time-kill curves exhibited that compound 11j had significant adjuvant activity to kill the bacteria. The predicted ADMET analysis showed that 2-aminothiazoyl piperidine derivatives had good drug-likeness and acceptable physicochemical properties. Furthermore, membrane permeability experiments demonstrated that compound 11j was beneficial for colistin to destroy the outer membrane of bacteria. Also, the comparative molecular similarity indices analysis(Co MSIA) and the density functional theory(DFT) calculations were conducted. The results drawn from these analyses indicated that the novel scaffold provided helpful information for the finding of new adjuvant lead.

关键词： 2-Aminothiazole piperidine Antibiotic adjuvant Acinetobacter baumannii Colistin

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Flavonoids rather than alkaloids as the diagnostic constituents to distinguish Sophorae Flavescentis Radix from Sophorae Tonkinensis Radix et Rhizoma: an HPLC fingerprint study

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Chinese Journal of Natural Medicines 2018年第12期16卷 951-960页

作者： DING Pei-Lan HE Chang-Ming CHENG Zhi-Hong CHEN Dao-Feng Department of Pharmacognosy School of Pharmacy Fudan University

Sophorae Flavescentis Radix(Sophora flavescens Ait., SFR) and Sophorae Tonkinensis Radix et Rhizoma(S. tonkinensis Gapnep., STR) are two commonly used traditional Chinese medicines from Sophora(Leguminosae) plants, which are believed to possess similar bioactive components with entirely different clinical applications. In order to find out the characteristic chemical constituents potentially leading to the unique medicinal properties claimed for each of the two closely related TCMs, an HPLC fingerprint method was developed for analyses of the alkaloid and flavonoid constituents of SFR and STR, respectively, which were further evaluated and compared through similarity calculation and hierarchical clustering analysis(HCA). The results from the present study showed that the alkaloid fingerprints of the two herbs were similar, with many components co-existing in both drugs and various batches of samples from different species being mixed together in the HCA dendrogram. However, their flavonoid constituents were totally different with specific fingerprints being yielded for each herb, and further HCA analysis showed that the tested samples could almost be clearly divided into two groups based on their origins of species. The results from the present study indicated that the flavonoid constituents could serve as the differentially diagnostic constituents of SFR and STR and might potentially attributed to their distinct therapeutic effects.

关键词： Sophoraflavescens Sophora tonkinensis Alkaloids Flavonoids HPLC fingerprint Hierarchical clustering analysis

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3D-QSAR Studies of the Pteridine Analogues as iNOS Inhibitors

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Chinese Journal of Structural Chemistry 2018年第9期37卷 1371-1378页

作者：张磊张青青唐锋张骥王京姚其正 School of Pharmacy Zunyi Medical University School of Pharmacy China Pharmaceutical University school of Basic Science China Pharmaceutical University

Inducible nitric oxide synthase（iNOS）, which can produce nitric oxide（NO） in the induction of cytokines and other factors, has an important impact onthe physiological functions of the body for the transmission of information. However,continuous generation of NOwill produce a lot of great damages to organisms. Therefore, iNOS inhibitors with good inhibitory activity and selectivity have beenimportant means of treating a variety of diseases. Based on the public-alignment of pteridine, 3D-QSAR（Three-Dimensional Quantitative Structure-Activity Relationship） models of pteridine analogues as iNOS inhibitors were established by the 3D-QSAR protocol of Discovery Studio 3.0. Pteridine molecules divided in different groups obtained four approximate models, indicating good stability of such models, in which A3 is preferable（q2 = 0.672, r2 = 0.996, rpred2 . = 0.888, q2 denotes the cross-validation coefficient, r2 denotes the non-cross-validation coefficient）. This study should be significant for the future structure design and modification of pteridine analogues as iNOS inhibitors.

关键词： 3D-QSAR pteridineanalogue iNOS inhibitor

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Determination of 6258-70,a new semi-synthetic taxane,in rat plasma and tissues:Application to the pharmacokinetics and tissue distribution study

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Journal of Pharmaceutical Analysis 2016年第4期6卷 219-225页

作者： Simin Zhao Yuanyuan Zhang Ping Ju Liqiang Gu Rui Zhuang Longshan Zhao Xing Tang Kaishun Bi Xiaohui Chen School of Pharmacy Shenyang Pharmaceutical University

Cancer is the leading cause of death all over the world.Among the chemotherapy drugs,taxanes play an important role in cancer treatment.6258-70 is a new semi-synthetic taxane which has a broad spectrum of antitumor activity.A fast and reliable high performance liquid chromatography-tandem mass spectrometry（HPLC-MS/MS） method was developed for quantification of 6258-70 in rat plasma and tissues in this paper.After extraction by liquid-liquid extraction method with methyl tert-butyl ether,the samples were separated on a Kinetex C_（18） column（50 mm × 2.1 mm,2.6 μm,Phenomenex,USA） within3 min.The method was fully validated with the matrix effect between 87.7%and 99.5%and the recovery ranging from 80.3%to 90.1%.The intra- and inter-day precisions were less than 9.5%and the accuracy ranged from-3.8%to 6.5%.The reliable method was successfully applied to the pharmacokinetics and tissue distribution studies of 6258-70 after intravenous administration in rats.The pharmacokinetic results indicated that the pharmacokinetic behavior of 6258-70 in rats was in accordance with linear features within tested dosage of 1 to 4 mg/kg,and there was no significant difference between the two genders.The tissue distribution study showed that 6258-70 had an effective penetration,spread widely and rapidly and could cross blood-brain barrier.The results of pharmacokinetics and tissue distribution may provide a guide for future study.

关键词： 6258-70 HPLC-MS/MS Pharmacokinetics Tissue distribution

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Effects of degree of substitution on stearic acid-modified Bletilla striata polysaccharides nanoparticles and interactions between nanoparticles and bovine serum albumin

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Chinese Chemical Letters 2018年第12期29卷 1861-1864页

作者： Guangyuan Zhang Ji Wu Yuran Liu Long Huang Jin Qiao Xin Liu Jingyan Wei Qingxiang Guan School of Pharmacy Jilin University

Three kinds of stearic acid（SA）-modified Bletilla striata polysaccharides（BSPs-SA） conjugates with different degrees of substitution（DS） values of SA moiety were synthesized. The impacts of the DS values on the properties of BSPs-SA self-aggregated nanoparticles were determined. The interactions between bovine serum albumin（BSA） and the BSPs-SA nanoparticles were characterized using spectroscopic observations. The cytotoxicity was measured through 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyl tetrazolium bromide（MTT） method. The critical aggregation concentration and the average particle sizes reduced from 16.81 μg/mL to 3,09 μg/mL and 192.70 nm to 125.29 nm when the DS values of SA segment increased from 4.98% to 12.94%, respectively. The cumulative release percentage of docetaxel in BSPs-SA nanoparticles decreased whereas encapsulation efficiency and loading capacity increased along with the DS increase of SA moiety. The fluorescence and ultraviolet results demonstrated that the conformation of BSA did not show significant change after incubating with BSPs-SA nanoparticles.Besides, the mass ratio of BSA/BSPs-SA affected their affinity intensity. The inhibition capability of cell proliferation of docetaxel-loaded BSPs-SA nanoparticles against 4 T1 was superior to that of Duopafei;.BSPs-SA nanoparticles may become a promising nanocarrier for anticancer drugs by adjusting the DS values of the hydrophobic SA groups.

关键词： Bletilla striata Nanoparticles Bovine serum albumin Interaction Degree of substitution

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Editorial for Molecular Imaging and Theranostics

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Acta Pharmaceutica Sinica B 2018年第3期8卷 318-319页

作者： Wei Lu School of Pharmacy Fudan University

Molecular imaging has become a hot research area since the early of this century.It utilizes the molecular interaction between the imaging probes and the particular targets to image the change of the area of interest.Molecular imaging opens up the possibility of early diagnosis as well as monitoring treatment response and outcomes that tailors individualized therapies.Researches have been focused on the development of imaging probes for various

关键词： Editorial for Molecular Imaging and Theranostics

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Synthesis of a reduction-sensitive Bletilla striata polysaccharide amphiphilic copolymer

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Chinese Chemical Letters 2018年第6期29卷 831-833页

作者： Dandan Sun Miao Wang Danyang Ji Jin Qiao Tong He Xin Liu Qingxiang Guan School of Pharmacy Jilin University

Recently, much special attention has been focused on the development of amphiphilic copolymers.Herein, a reduction-sensitive stearic acid grafted-Bletilla striata polysaccharide copolymer（BSP-ss-SA）was synthesized and characterized. BSP-ss-SA copolymer could spontaneously form micelles with an average particle size of（106 ？ 4.36） nm. Particle sizes were dramatically larger under 10 mmol/L dithiothreitol（DTT） than that in absence of 10 mmol/L DTT. Docetaxel loading content and encapsulation efficiency of micelles were 5.94 wt% and 72.75 wt%, respectively. The docetaxel release rate in vitro in micelles could be remarkably accelerated in pH 7.4 phosphate buffer solution（PBS） containing 10 mmol/L DTT compared with that of micelles（0 mmol/L DTT）. Furthermore, MTT results demonstrated the anticancer activities in vitro of docetaxel-loaded BSP-ss-SA micelles on HepG2 were superior to that of docetaxel injection. BSP-ss-SA copolymer might be a promising nanocarrier for cancer chemotherapy drugs.

关键词： Bletilla striata Amphiphilic polymer Micelle Reduction sensitivity Anticancer activity

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Difluoromethyl phenoxathiinium salt: A new general and versatile difluoromethylating reagent with divergent ·CFH, CFH,and :CFreactivities

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Science China Chemistry 2023年

作者： Yuan-Qing Gu Hong-Xin Long Dan-Dan Zhang Mei-Feng Ruan Guo-Kai Liu School of Pharmacy Shenzhen University Medical School Shenzhen University

Development of practical and versatile electrophilic difluoromethylating reagent is still a grand challenge so far due to its inherent instability or low reactivity. Herein, we report the design and synthesis of difluoromethyl phenoxathiinium tetrafluoroborate(PT-CF2H+BF4-) as a novel difluoromethylating reagent, which proves to be a bench-stable, general, powerful and versatile reagent with divergent ·CF2H, CF2H+, and :CF2reactivities. Making use of this reagent, we demonstrated a vast array of difluoromethyl radical transfer reactions via diverse pathways involving photocatalyst-free visible-light induction, visible-light photoredox catalysis and visible-light mediation single electron transfer of EDA complex. Moreover, the green and highly effective CF2H+and :CF2transfer reactions were also readily accomplished.

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Oral uptake and persistence of the FnAb-8 protein characterized by in situ radio-labeling and PET/CT imaging

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Asian Journal of Pharmaceutical Sciences 2020年第6期15卷 752-758页

作者： Qian Wang Wangxi Hai Sanyuan Shi Jinliang Peng Yuhong Xu School of Pharmacy and Chemistry DaLi UniversityDali 671000China School of Pharmacy Shanghai Jiao Tong UniversityShanghai 200240China

The absorption of peptides and proteins delivered orally is minimum because of the intestine epithelial barrier.There are few known active transport mechanisms for macromolecules including the neonatal Fc Receptor(FcRn)for the absorption and secretion of IgGs in infant and adult intestine.We had previously described the FnAb-8 protein that could bind to h FcRn tightly at pH 6.0 but barely at pH 7.4.In this study,we examined its uptake,biodistribution and pharmacokinetics after peroral administration in both wild-type and human FcRn transgenic(Tg)mice.FnAb-8 was modified to contain trans-cyclooctene(TCO)which could interact with18 F labeled tetrazine in situ via the bioorthogonal inverseelectron-demand Diels-Alder reaction.We showed that FnAb-8 had a tendency to distribute and persist in the Tg mice intestine for an extended duration of time.It could also be absorbed into the circulation and distributed systemically over a long period of time up to 172 h.The improvement in oral uptake and concentration in the intestine tissue may be valuable for designing oral delivery of biopharmaceuticals,especially for diseases involving the gastric intestinal tissue.

关键词： FcRn IEDDA Oral uptake

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Small molecules for combating multidrug-resistant superbug Candida auris infections

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Acta Pharmaceutica Sinica B 2022年第11期12卷 4056-4074页

作者： Jie Tu Na Liu Yahui Huang Wanzhen Yang Chunquan Sheng School of Pharmacy Second Military Medical UniversityShanghai 200433China

Candida auris is emerging as a major global threat to human health. C. auris infections are associated with high mortality due to intrinsic multi-drug resistance. Currently, therapeutic options for the treatment of C. auris infections are rather limited. We aim to provide a comprehensive review of current strategies, drug candidates, and lead compounds in the discovery and development of novel therapeutic agents against C. auris. The drug resistance profiles and mechanisms are briefly summarized. The structures and activities of clinical candidates, drug combinations, antifungal chemosensitizers, repositioned drugs, new targets, and new types of compounds will be illustrated in detail, and perspectives for guiding future research will be provided. We hope that this review will be helpful to prompting the drug development process to combat this fungal pathogen.

关键词： Candidaauris Antifungal agents Drug resistance Virulence factors Antifungal targets

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