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Engineered microneedles arrays for wound healing

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Engineered Regeneration

Engineered Regeneration 2022年第3期3卷 232-240页

作者： Shun Yao Yuan Luo Yongan Wang State Key Laboratory of toxicology and Medical Countermeasures Beijing Institute of Pharmacology and ToxicologyBeijing 100850China

Wound healing is the regenerative process of original skin structure after destructing by different damage sources.Due to their transdermal delivery capability and high specific surface area,microneedles arrays(MAs)have been recognized as encouraging biomaterials for wound healing.In this review,we have outlined the engineered MAs used for tissue regeneration and wound healing.Engineered MAs were first classified by design methodologies such as bionic design,intelligent-responsive design,actively-triggered design,matrix materials innovation,and composite smart design.Then,the MAs were divided into two categories based on the different loading substances:drug-loaded MAs and living component-loaded MAs.Finally,we have summed up the important elements of the preceding discussions and forecasted their future evolution.

关键词： Engineered design Microneedles arrays Wound healing

Effect of thienorphine on intestinal transit and isolated guinea-pig ileum contraction

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World Journal of Gastroenterology 2013年第9期19卷 1444-1450页

作者： Pei-Lan Zhou Yu-Lei Li Ling-Di Yan Zheng Yong Gang Yu Hua-Jin Dong Hui Yan Rui-Bin Su Ze-Hui Gong Beijing Institute of Pharmacology and Toxicology

AIM: To evaluate the effect of thienorphine on small intestinal transit in vivo and on guinea-pig ileum (GPI) contraction in vitro . METHODS: The effects of thienorphine on intestinal transit were examined in mice and in isolated GPI. Buprenorphine and morphine served as controls. The distance traveled by the head of the charchol and the total length of the intestine were measured in vivo . Gastrointestinal transit was expressed as a percentage of the distance traveled by the head of the marker relative to the total length of the small intestine. The isolated GPI preparations were connected to an isotonic force transducer and equilibrated for at least 1 h before exposure to drugs. Acetylcholine was used for muscle stimulation. RESULTS: Thienorphine (0.005-1.0 mg/kg, ig ) or bu-prenorphine (0.005-1.0 mg/kg, sc ) dose-dependently significantly inhibited gut transit compared with saline. Thienorphine inhibited gut transit less than buprenorphine. The maximum inhibition by thienorphine on the intestinal transit was 50%-60%, whereas the maximum inhibition by morphine on gut transit was about 100%. Thienorphine also exhibited less inhibition on acetylcholine-induced contraction of GPI, with a maximum inhibition of 65%, compared with 93% inhibition by buprenorphine and 100% inhibition by morphine. Thienorphine induced a concentration-dependent decrease in the basal tonus of spontaneous movement of the GPI, the effect of which was weaker than that with buprenorphine. The duration of the effect of thienorphine on the GPI was longer than that with buprenorphine. CONCLUSION: Thienorphine had less influence, but a longer duration of action on GPI contraction and moderately inhibited intestinal transit.

关键词： Thienorphine Buprenorphine Guinea-pig ileum Gut transit Contraction

Novel small molecule retrograde transport blocker confers post-exposure protection against ricin intoxication

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Acta Pharmaceutica Sinica B 2020年第3期10卷 498-511页

作者： Xu Zhao Haixia Li Jia Li Kunlu Liu Bo Wang Yuxia Wang Xingzhou Li Wu Zhong National Engineering Research Center for the Emergency Drug Beijing Institute of Pharmacology and ToxicologyBeijing 100850China State Key Laboratory of toxicology and Medical Countermeasures Beijing Institute of Pharmacology and ToxicologyBeijing 100850China

Ricin is a highly toxic type 2 ribosome-inactivating protein(RIP)which is extracted from the seeds of castor beans.Ricin is considered a potential bioterror agent and no effective antidote for ricin exists so far.In this study,by structural modification of a retrograde transport blocker Retro-2cyc1,a series of novel compounds were obtained.The primary screen revealed that compound 27 has an improved antiricin activity compare to positive control.In vitro pre-exposure evaluation in Madin-Darby Canine Kidney(MDCK)cells demonstrated that 27 is a powerful anti-ricin compound with an EC50 of 41.05 nmol/L against one LC(lethal concentration,5.56 ng/mL)of ricin.Further studies surprisingly indicated that 27 confers post-exposure activity against ricin intoxication.An in vivo study showed that 1 h post-exposure administration of 27 can improve the survival rate as well as delay the death of ricin-intoxicated mice.A drug combination of 27 with monoclonal antibody mAb4 C13 rescued mice from one LD(lethal dose)ricin challenge and the survival rate of tested animals is 100%.These results represent,for the first time,indication that small molecule retrograde transport blocker confers both in vitro and in vivo post-exposure protection against ricin and therefore provides a promising candidate for the development of anti-ricin medicines.

关键词： Ricin toxin Ribosome-inactivating proteins Retrograde transport Post-exposure antidote Ricin antibody

Quantification of flupirtine maleate polymorphs using X-ray powder diffraction

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Chinese Chemical Letters 2016年第11期27卷 1666-1672页

作者： Yu-Mei Zhao Zhi-Bing Zheng Song Li Laboratory of Computer-Aided Drug Design & Discovery Beijing Institute of Pharmacology and Toxicology Laboratory of Structure Identification Beijing Institute of Pharmacology and Toxicology State Key Laboratory of toxicology and Medical Countermeasures Beijing Institute of Pharmacology and Toxicology

Flupirtine maleate, a pharmaceutical compound for treating psychotic disease in clinics, has seven polymorphs. Form A, with better crystal stability and bioavailability, has been widely used as the pharmaceutical crystal form. Unfortunately, it is usually found in a polymorphic mixture with form B. In this study, pure crystal forms of A and B were prepared and characterized by X-ray powder diffraction （XRPD）, Fourier transform infrared spectroscopy （FT-IR） and thermal analysis. An XRPD-based method for the quantitative determination of the amount of the flupirtine maleate polymorphs form A and form B was also established through a systematic optimization of instrumental parameters. The results of the analytical methodology validation showed that the XPRD method had a broad quantitative range of 0- 100% （w/w）, good linear relationship, with R2= 0.999, excellent repeatability and precision and low limits of detection （LoD） of 0.15% （w/w） and quantification （LoQ） of 0.5% （w/w）. The results also showed that the single-peak method was not as good as the whole pattern in reducing the influence of the preferred orientation, but this can be compensated for by a systematic optimization of instrumental parameters and validating the analytical methodology to reduce errors and obtain a good, repeatable, sensitive, and accurate method. This XRPD method can be used to analyze mixtures of flupirtine maleate polymorphs （forms A and B） quantitatively and control the quality of the bulk drug.

关键词： Flupirtine maleate X-ray powder diffraction Quantitative analysis of polymorphs Preferred orientation Transmission

Pteridic acid hydrate and pteridic acid C produced by Streptomyces pseudoverticillus YN17707 induce cell cycle arrest

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Chinese Journal of Natural Medicines 2015年第6期13卷 467-470页

作者： HAN Bing LI Wen-Xin CUI Cheng-Bin Beijing institute of Biomedicine Beijing Institute of Pharmacology and Toxicology

The present study aimed at identifying cell cycle inhibitors from the fermentation broth of Streptomyces pseudoverticillus YN17707. Activity-guided isolation was performed on ts FT210 cells. Compounds were isolated through various chromatographic methods and elucidated by spectroscopic analyses. Flow cytometry was used to evaluate the cell cycle inhibitory activities of the fractions and compounds. Two compounds were obtained and identified as pteridic acid hydrate(1) and pteridic acid C(2), which arrested the ts FT210 cells at the G0/G1 phase with the MIC values being 32.8 and 68.9 μmol·L-1, respectively. These results provide a basis for future development of Compounds 1 and 2 as novel cell cycle inhibitors for cancer therapy.

关键词： Cell cycle inhibitor Streptomyces pseudoverticillus Spirocyclic polyketide Pteridic acid Flow cytometry

Design and synthesis of cyclic acylguanidines as BACE1 inhibitors

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Chinese Chemical Letters 2015年第10期26卷 1327-1330页

作者： Jia-Kuo Liu Wei Gu Xiao-Rui Cheng Jun-Ping Cheng Wen-Xia Zhou Ai-Hua Nie Beijing Institute of Pharmacology and Toxicology

Based on the lead compound 1 reported in literature, a series of novel BACE1 inhibitors were designed and synthesized, among which compound 11 exhibited a 14-fold improvement in potency over the lead compound 1. This ... 详细信息

关键词： Alzheimer’s disease BACE1 inhibitor Cyclic acylguanidine

Size,shape,charge and“stealthy”surface:Carrier properties affect the drug circulation time in vivo

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Asian Journal of Pharmaceutical Sciences 2021年第4期16卷 444-458页

作者： Jinwei Di Xiang Gao Yimeng Du Hui Zhang Jing Gao Aiping Zheng State Key Laboratory of toxicology and Medical Countermeasures Beijing Institute of Pharmacology and ToxicologyBeijing 100850China

The present review sets out to discuss recent developments of the effects and mechanisms of carrier properties on their circulation time.For most drugs,sufficient in vivo circulation time is the basis of high bioavailability.Drug carrier plays an irreplaceable role in helping drug avoid being quickly recognized and cleared by mononuclear phagocyte system,to give drug enough time to arrive at targeted organ and tissue to play its therapeutic effect.The physical and chemical properties of drug carriers,such as size,shape,surface charge and surface modification,would affect their in vivo circulation time,metabolic behavior and biodistribution.The final circulation time of carriers is determined by the balance between macrophage recognitions,blood vessel penetration and urine excretion.Therefore,when designing the drug delivery system,we should pay much attention to the properties of drug carriers to get enough in vivo circulation time to arrive at target site eventually.This article mainly reviews the effect of carrier size,size,surface charge and surface properties on its circulation time in vivo,and discusses the mechanism of these properties affecting circulation time.This review has reference significance for the research of long-circulation drug delivery system.

关键词： Drug carrier Circulation time Physical and chemical properties Macrophages Phagocytosis

Characteristics of the traditional Liu-Wei-Di-Huang prescription reassessed in modern pharmacology

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Chinese Journal of Natural Medicines 2019年第2期17卷 103-121页

作者： CHENG Xiao-Rui QI Chun-Hui WANG Tong-Xing ZHOU Wen-Xia ZHANG Yong-Xiang Academy of Military Medical Science Institute of Pharmacology and Toxicology State Key Laboratory of toxicology and Medical Countermeasures

Liu-Wei-Di-Huang(LW) is a Yin nourishing and kidney tonifying prescription in traditional Chinese medicine with promising pharmacological characteristics that can be further exploited and developed in modern medicine. We provide a comprehensive and detailed literature report on the clinical and experimental pharmacology of LW,including its quality control parameters, phytochemistry, pharmacokinetics, and toxicology. Our literature review indicates that the LW prescription possesses a unique combination of pharmacological characteristics that can be safely used for treating very different diseases. Quality control and pharmacokinetic parameters of LW are mostly based on its major bioactive phytochemical constituents. We postulate that modulating or rebalancing the neuroendocrine immunomodulation network in the body is the underlying mechanism of the multiple pharmacological activities displayed by LW.

关键词： Liu-Wei-Di-Huang Traditional Chinese medicine pharmacology Phytochemistry Pharmacokinetics toxicology

Multifocal structured illumination optoacoustic microscopy

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Light(Science & Applications) 2020年第1期9卷 568-576页

作者： Zhenyue Chen Ali Ozbek Johannes Rebling Quanyu Zhou Xose Luis Dean-Ben Daniel Razansky institute for Biomedical Engineering and Institute of Pharmacology and Toxicology University of Zurich and ETH ZurichZurichSwitzerland

Optoacoustic(OA)imaging has the capacity to effectively bridge the gap between macroscopic and microscopic realms in biological imaging.High-resolution OA microscopy has so far been performed via point-by-point scanning with a focused laser beam,thus greatly restricting the achievable imaging speed and/or field of view.Herein we introduce multifocal structured illumination OA microscopy(MSIOAM)that attains real-time 3D imaging speeds.For this purpose,the excitation laser beam is shaped to a grid of focused spots at the tissue surface by means of a beamsplitting diffraction grating and a condenser and is then scanned with an acousto-optic deflector operating at kHz rates.In both phantom and in vivo mouse experiments,a 10mm wide volumetric field of view was imaged with 15 Hz frame rate at 28μm spatial resolution.The proposed method is expected to greatly aid in biological investigations of dynamic functional,kinetic,and metabolic processes across multiple scales.

关键词： illumination beam excitation