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Chinese Chemical Letters 2022年第11期33卷 4948-4951页

作者： Lingyu Hang chengying shen Baode shen Hailong Yuan Department of Pharmacy Air Force Medical CenterPLABeijing 100142China College of Pharmacy Jiangxi University of Chinese MedicineNanchang 330004China Department of Pharmacy Jiangxi Provincial People's HospitalNanchang 330006China

Intravenous nanosuspensions are attracted growing attention as a viable strategy for development of intravenous formulations of poorly water-soluble drugs.However,only few information about the biological fate of intravenous nanosuspensions is currently known,especially amorphous nanosuspensions are not reported yet.In this study,the in vivo fate of herpetrione(HPE)amorphous nanosuspensions following intravenous administration was explored by using an aggregation-caused quenching(ACQ)probe and HPLC methods.The ACQ probe is physically embedded into HPE nanoparticles via anti-solvent method to form HPE hybrid nanosuspensions(HPE-HNSs)for bioimaging.HPE-HNSs emit strong and stable fluorescence,but fluorescence quenches immediately upon the dissolution of HPE-HNSs,confirming the selfdiscrimination of HPE-HNSs.Following intravenous administration of HPE-HNSs,integral HPE-HNSs and HPE show similar degradation and biodistribution,with rapid clearance from blood circulation and obvious accumulation in liver and lung.Due to the slower dissolution and enhanced recognition by reticuloendothelial system,450 nm HPE-HNSs accumulate more in liver,lung and spleen than that of 200 nm HPE-HNSs.These results demonstrate that integral HPE-HNSs determine the in vivo performance of HPEHNSs.This study provides insight into the in vivo fate of intravenous amorphous nanosuspensions.

关键词： Amorphous nanosuspensions Herpetrione In vivo fate Intravenous delivery Aggregation-caused quenching

Effects of novel Fufang Biejia Ruangan Tablets with sheep placenta as substitute for Hominis Placenta on CCl4-induced liver fibrosis

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Chinese Herbal Medicines 2022年第1期14卷 104-110页

作者： Baode shen Li Deng Yuan Liu Ruisheng Li chengying shen Xiao Liu Yinchao Li Hailong Yuan Department of Pharmacy Air Force Medical CenterPLABeijing 100142China College of Pharmaceutical Sciences Zhengzhou UniversityZhengzhou 450001China Research Center for Clinical and Translational Medicine The Fifth Medical Center of ChinesePLA General HospitalBeijing 100039China School of Chemistry Biology and Material ScienceEast China University of TechnologyNanchang 330013China

Objective:Fufang Biejia Ruangan Tablet(FBRT) is widely used for the treatment of liver fibrosis.However,Hominis Placenta(HP),as an important adjuvant of FBRT,has been restricted for medicinal using due to the limited availability,ethical controversy and safety issues.The present study aimed to investigate the therapeutic effects of novel FBRT(N-FBRT) with sheep placenta(SP) as substitute for HP on liver fibrosis and explore its possible mechanisms.Different dosages of SP in N-FBRT were also evaluated.Methods:Rats were subcutaneously injected with CCl_(4)to induce liver fibrosis and then treated with NFBRT and FBRT.The anti-hepatic fibrosis effect was determined based on biomarkers analysis of liver function and hepatic fibrosis,and the liver pathology was visualized by H&E staining and Masson staining.The oxidative stress and inflammatory cytokines were also detected.Immunohistochemical staining of a-SMA,real time PCR and Western blotting were performed to evaluate hepatic stellate cells(HSCs)activation and TGF-β1/Smad signaling pathway.Results:N-FBRT and FBRT could ameliorate CCl_(4)-induced liver fibrosis and improve liver function,as evidenced by lowering serum biomarkers levels of liver function and hepatic fibrosis,and decreasing hepatic Hyp content and collagen deposition,and improving the hepatic morphology and architecture changes.Moreover,the anti-liver fibrosis effect was better when the dosage of SP used in N-FBRT was 1/2 of HP in FBRT.Administration of N-FBRT markedly alleviated oxidative stress and inflammatory cytokines,and inhibited a-SMA expression.Furthermore,the mRNA expression of Col Ⅰ,Col Ⅲ,a-SMA and TGF-β1,and proteins expression of a-SMA,TGF-β1,Smad2/3 and p-Smad2/3 were significantly down-regulated by N-FBRT treatment.Conclusion:SP can be used as substitute for HP to prepare N-FBRT for the treatment of liver fibrosis and the anti-liver fibrosis effect of N-FBRT is achieved by eliminating oxidative stress and inflammation,and inhibiting HSCs activation and ECM production by blocking TGF-β1/S

关键词： Fufang Biejia Ruangan Tablet Hominis Placenta liver fibrosis sheep placenta substitute TGF-β1/Smad signaling pathway

The contribution of absorption of integral nanocrystals to enhancement of oral bioavailability of quercetin

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Acta Pharmaceutica Sinica B 2021年第4期11卷 978-988页

作者： Baode shen chengying shen Weifeng Zhu Hailong Yuan Department of Pharmacy Air Force Medical CenterPLABeijing 100142China Key Lab of Modern Preparation of Traditional Chinese Medicine(TCM) Ministry of EducationJiangxi University of TCMNanchang 330004China

In this study,self-discriminating hybrid nanocrystals was utilized to explore the biological fate of quercetin hybrid nanocrystals(QT-HNCs)with diameter around 280 nm(QT-HNCs-280)and550 nm(QT-HNCs-550)following oral and intravenous administration and the contribution of integral nanocrystals to oral bioavailability enhancement of QT was estimated by comparing the absolute exposure of integral QT-HNCs and total QT in the liver.Results showed that QT-HNCs could reside in vivo as intact nanocrystals for as long as 48 h following oral and intravenous administration.A higher accumulation of integral QT-HNCs in liver and lung was observed for both oral and intravenous administration of QT-HNCs.The particle size affects the absorption and biodistribution of integral QT-HNCs and total QT.As compared to QT-HNCs-550,QT-HNCs-280 with smaller particle size is more easily absorbed,but dissolves faster in vivo,leading to higher distribution of QT(146.90 vs.117.91 h·mg/mL)but lower accumulation of integral nanocrystals(6.82 e10 vs.15.27 e10 h·[p/s]/[μW/cm2])in liver following oral administration.Due to its slower dissolution and enhanced recognition by RES,QT-HNCs-550 with larger diameter shows higher liver distribution for both of QT(1015.80 h·mg/mL)and integral nanocrystals(259.63 e10 h·[p/s]/[μW/cm2])than those of QT-HNCs-280(673.82&77.66 e10 h·[p/s]/[μW/cm2])following intravenous administration.The absolute exposure of integral QT-HNCs in liver following oral administration of QT-HNCs are 8.78%for QT-HNCs-280 and 5.88%for QT-HNCs-550,while the absolute exposure of total QT for QT-HNCs-280 and QT-HNCs-550 are 21.80%and 11.61%,respectively.Owing to imprecise quantifcation method,a surprisingly high contribution of integral QT-HNCs to oral bioavailability enhancement of QT(40.27%for QT-HNCs-280 and 50.65%for QT-HNCs-550)was obtained.These results revealed signifcant difference in absorption and biodistrbution between integral nanocrystals and overall drugs following oral and intravenous administration of QT-HNCs,and provided a

关键词： Nanocrystals Biological fate Quercetin Pharmacokinetics Biodistribution Oral bioavailability Contribution Drug delivery

In vivo dissolution of poorly water-soluble drugs:Proof of concept based on fluorescence bioimaging

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Acta Pharmaceutica Sinica B 2021年第4期11卷 1056-1068页

作者： Yinqian Yang Yongjiu Lv chengying shen Tingting Shi Haisheng He Jianping Qi Xiaochun Dong Weili Zhao Yi Lu Wei Wu Key Laboratory of Smart Drug Delivery of MOE School of PharmacyFudan UniversityShanghai 201203China Center for Medical Research and Innovation Shanghai Pudong HospitalFudan University Pudong Medical CenterShanghai 201399China

In vitro-in vivo correlation(IVIVC)of solid dosage forms should be established basically between in vitro and in vivo dissolution of active pharmaceutical ingredients.Nevertheless,in vivo dissolution profles have never been accurately portrayed.The current practice of IVIVC has to resort to in vivo absorption fractions(Fa).In this proof-of-concept study,in vivo dissolution of a model poorly watersoluble drug fenofbrate(FNB)was investigated by fuorescence bioimaging.FNB crystals were frst labeled by near-infrared fuorophores with aggregation-caused quenching properties.The dyes illuminated FNB crystals but quenched immediately and absolutely once been released into aqueous media,enabling accurate monitoring of residual drug crystals.The linearity established between fuorescence and crystal concentration justifed reliable quantifcation of FNB crystals.In vitro dissolution was frst measured following pharmacopoeia monograph protocols with well-documented IVIVC.The synchronicity between fuorescence and in vitro dissolution of FNB supported using fuorescence as a measure for determination of dissolution.In vitro dissolution correlated well with in vivo dissolution,acquired by either live or ex vivo imaging.The newly established IVIVC was further validated by correlating both in vitro and in vivo dissolution with Faobtained from pharmacokinetic data.

关键词： In vivo dissolution Fenofibrate Fluorescence Aggregation-caused quenching Bioimaging IVIVC

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黄芩汤的抗须癣毛癣菌活性及作用机制研究

中国药房 2024年第3期35卷 311-315页

作者：沈成英罗忠章佩邓冯沂申宝德胡建新江西省人民医院(南昌医学院第一附属医院)药学部南昌330006 南昌大学药学院南昌330006 江西省人民医院(南昌医学院第一附属医院)临床医学研究所南昌330006 江西中医药大学现代中药制剂教育部重点实验室南昌330004

研究黄芩汤(HQD)的抗须癣毛癣菌活性及作用机制。方法通过测定最小抑菌浓度(MIC)、最小杀菌浓度(MFC)、菌丝长度、孢子萌发率、生物量和观察菌丝超微结构评价HQD的抗须癣毛癣菌活性;通过山梨醇保护实验检测HQD对须癣毛癣菌细胞壁的影响... 详细信息

研究黄芩汤(HQD)的抗须癣毛癣菌活性及作用机制。方法通过测定最小抑菌浓度(MIC)、最小杀菌浓度(MFC)、菌丝长度、孢子萌发率、生物量和观察菌丝超微结构评价HQD的抗须癣毛癣菌活性;通过山梨醇保护实验检测HQD对须癣毛癣菌细胞壁的影响;通过测定麦角固醇含量和角鲨烯环氧酶(SE)、羊毛甾醇14α-去甲基化酶(CYP51)的活性考察HQD对须癣毛癣菌细胞膜的影响;通过测定线粒体中苹果酸脱氢酶(MDH)、琥珀酸脱氢酶(SDH)及ATP酶(包括钠钾ATP酶、钙镁ATP酶和总ATP酶)的活性考察HQD对须癣毛癣菌线粒体的影响。结果 HQD对须癣毛癣菌具有显著的抑菌活性,MIC、MFC值分别为3.13、25 mg/mL。经HQD干预后,须癣毛癣菌菌丝长度均显著缩短(P<0.05);孢子萌发率、生物量、细胞膜中麦角固醇含量和SE、CYP51活性以及线粒体中MDH、SDH、各种ATP酶的活性均显著降低(P<0.05);细胞结构受到了一定程度的破坏,但细胞壁的完整性没有受影响。结论 HQD具有显著的抗须癣毛癣菌活性,其作用机制与降低细胞膜中麦角固醇含量和SE、CYP51活性以及线粒体相关酶活性有关。

关键词：黄芩汤须癣毛癣菌抗真菌活性作用机制细胞膜线粒体

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江苏省农药登记试验监管工作的实践与思考

农药科学与管理 2024年第4期45卷 1-6页

作者：陆澄滢任森沈迎春江苏省农药总站江苏南京210017

本文针对江苏省农药登记试验单位现状,分析了目前试验单位存在的问题,如关键岗位人员变化大、软硬件设施不足、机构管理不规范等。结合江苏工作实践,对农药登记试验行业发展提出若干建议。相关主管部门和登记试验单位应引起足够重视并... 详细信息

本文针对江苏省农药登记试验单位现状,分析了目前试验单位存在的问题,如关键岗位人员变化大、软硬件设施不足、机构管理不规范等。结合江苏工作实践,对农药登记试验行业发展提出若干建议。相关主管部门和登记试验单位应引起足够重视并积极应对,切实提高农药登记试验规范化水平。

关键词：农药登记试验单位监管思考

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266份木薯种质资源农艺性状分析评价

热带作物学报 2024年第4期45卷 712-721页

作者：黄渝岚李艳英周佳劳承英周灵芝韦本辉李素平申章佑广西农业科学院经济作物研究所广西南宁530007

以木薯种质资源为对象,对其8个主要农艺性状数据进行统计学分析。结果表明:8个农艺性状数据呈正态分布,变异系数范围为7.2%~46.9%,其中淀粉产量的变异系数达46.9%,薯干率的变异系数最小,为7.2%。相关分析结果表明,不同性状之间存在一定... 详细信息

以木薯种质资源为对象,对其8个主要农艺性状数据进行统计学分析。结果表明:8个农艺性状数据呈正态分布,变异系数范围为7.2%~46.9%,其中淀粉产量的变异系数达46.9%,薯干率的变异系数最小,为7.2%。相关分析结果表明,不同性状之间存在一定的显著正相关,其中单株鲜薯质量与茎径呈极显著正相关。进一步利用主成分分析方法将8个农艺性状简化为3个主成分,发现2年的累计贡献率分别达92.55%、93.67%。第一主成分是单株鲜薯质量、鲜薯产量、淀粉产量、薯干产量,第二主成分是淀粉含量和薯干率。通过聚类分析表明,在欧式距离为6.0处,可将各年份的资源分为4个类群,其中第Ⅱ类群(单株鲜薯质量、鲜薯产量、淀粉产量、薯干产量)表现优异,可优先作为高产优质木薯新品种选育的亲本材料。

关键词：木薯种质资源农艺性状相关性分析主成分分析聚类分析

维普期刊数据库博看期刊

粉垄耕作与绿肥还田对土壤酶活性和甘蔗产量的影响

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福建农业学报 2024年第4期39卷 409-417页

作者：周灵芝黄渝岚周佳劳承英申章佑李艳英韦本辉张宪王锋李素平广西壮族自治区农业科学院经济作物研究所

【目的】探明不同耕作和绿肥还田方式对长期连作蔗地土壤养分、酶活性和甘蔗产量的影响。【方法】采用随机区组设计，设置4个处理：传统旋耕甘蔗单作（TCK）、粉垄耕作甘蔗单作（FLCK）、粉垄耕作甘蔗/大豆还田甘蔗根部（FLG）和大豆还... 详细信息

【目的】探明不同耕作和绿肥还田方式对长期连作蔗地土壤养分、酶活性和甘蔗产量的影响。【方法】采用随机区组设计，设置4个处理：传统旋耕甘蔗单作（TCK）、粉垄耕作甘蔗单作（FLCK）、粉垄耕作甘蔗/大豆还田甘蔗根部（FLG）和大豆还田宽行（FLK）。测定土壤有机质、速效养分含量和脲酶、蔗糖酶、酸性磷酸酶、过氧化氢酶活性及甘蔗产量品质。【结果】（1）耕作方式和绿肥还田对土壤养分和酶活性影响显著。与TCK相比，所有处理的根部和宽行土壤有机质含量显著提高（P<0.05），增幅40.6%～76.7%。FLG、FLK和FLCK处理根部土壤碱解氮和有效磷含量比TCK显著提高，增幅16.1%～41.8%。（2）所有处理的土壤脲酶、蔗糖酶、酸性磷酸酶和过氧化氢酶活性比TCK提高（FLG处理宽行土壤脲酶活性除外）0.7%～166.7%。（3）FLG、FLK和FLCK处理的2年平均产量显著高于TCK，增幅13.1%～30.5%;FLG和FLK处理的2年平均产量显著高于FLCK，增幅9.9%～15.3%；其中以FLG处理平均产量最高，为86 043 kg·hm-2。FLG、FLK和FLCK处理的蔗糖分、锤度、重力纯度、视纯度和转光度均比TCK高。（4）甘蔗产量与土壤脲酶活性显著正相关，与土壤蔗糖酶、酸性磷酸酶、过氧化氢酶活性、有机质、碱解氮和有效磷含量极显著正相关。【结论】利用粉垄耕作结合绿肥还田可以提高连作蔗地土壤养分、土壤酶活性和甘蔗产质量；结合田间操作的便捷性，本地区生产推荐应用粉垄耕作结合绿肥还田到宽行的模式。

关键词：粉垄耕作绿肥还田土壤养分土壤酶活性甘蔗产量

基于COI条形码的市售蝉蜕及其混淆品DNA分子鉴定研究

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中草药 2024年第6期55卷 2057-2065页

作者：张欢欢徐金娣周静贾聪玲吴啟南郭梦斐沈纪晨伍城颖李松林毛茜南京中医药大学附属中西医结合医院中药质量研究室江苏南京210028 江苏省中医药研究院/中国中医科院江苏分院中药代谢组研究室江苏南京210028 南京中医药大学药学院江苏南京210023

目的利用COI序列对中药材蝉蜕Cicadae Periostracum及其混淆品进行DNA条形码鉴定研究,为蝉蜕药材的快速准确鉴定提供新的技术手段。方法收集全国市售蝉蜕药材、基地自采蝉蜕及其混淆品总45份样本,同时采集江苏徐州黑蚱养殖基地不同树种... 详细信息

目的利用COI序列对中药材蝉蜕Cicadae Periostracum及其混淆品进行DNA条形码鉴定研究,为蝉蜕药材的快速准确鉴定提供新的技术手段。方法收集全国市售蝉蜕药材、基地自采蝉蜕及其混淆品总45份样本,同时采集江苏徐州黑蚱养殖基地不同树种中蝉卵样品5份作为对照。提取DNA,进行PCR扩增及双向测序,测序结果采用DNAMAN和SnapGene进行拼接校对,运用MEGA11.0进行比对分析,计算种内及种间Kimura 2-Parameter(K2P)遗传距离并构建邻接法(neighbor-joining,NJ)系统发育树。结果黑蚱种内遗传距离远小于种间最小遗传距离,NJ树结果显示,黑蚱蝉蜕样品全部聚集为独立的一支,支持率为99%。混淆品样品分别聚集为单独的一支,支持率均大于90%,表明基于COI序列的DNA条形码技术可以有效鉴别蝉蜕药材真伪。结论应用COI序列作为DNA条形码能够准确有效地鉴别蝉蜕及其混淆品。

关键词：蝉蜕混淆品 DNA条形码 COI序列分子鉴定

Daily administration times of Canhuang tablet based on a pharmacodynamic/pharmacokinetic model in jaundiced rats

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Journal of Traditional Chinese Medicine 2015年第1期35卷 84-89页

作者： Bai Jinxia Han Jin Chen Hongge shen Baode Xu He Dai Ling shen chengying Yuan Hailong Department of Pharmacy 302 Hospital of PLA Pharmacy College Chengdu University of Traditional Chinese Medicine

OBJECTIVE: To study the daily administration times of Canhuang tablet(CHT) for treating jaundice in rats based on a pharmacodynamic/ pharmacokinetic model.METHODS: Rats were modeled by 4% 1-Naphthylisothiocyanate(75 mg/kg, p.o.). After 48 h, CHT was given(p.o.) at 0.75 g/kg once a day, 0.375 g/kg twice a day, and 0.25 g/kg three times a day. Blood was collected from the orbital sinus at different intervals. Levels of liver enzymes and bilirubin were detected using these blood samples. Bile was collected and determined after the first administration of CHT. High-performance liquid chromatography was used to determine the concentration of berberine in bile simultaneously. Time-effect and time-dose curves were then obtained.RESULTS: Compared with rats taking CHT twiceand three times a day, the total amount of bile within 10 h of rats taking CHT once a day were 1.32-and 1.47-fold higher, respectively. There was good consistency between the pharmacokinetics of berberine and the pharmacodynamics of the effect on liver enzymes and bilirubin in vivo. The pharmacokinetic analyses showed that rats administered CHT once daily maintained a higher concentration of berberine in bile for a longer period than rats administered CHT two- and three-times daily.CONCLUSION: In jaundiced rats, taking CHT once a day is better than taking CHT twice or three times a day. These data may provide a reference for the clinical application of CHT.

关键词：动力学模型时间间隔日常管理药效学大鼠黄疸平板电脑高效液相色谱法