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PEPT1-mediated prodrug strategy for oral delivery of peramivir

Asian Journal of Pharmaceutical Sciences 2018年第6期13卷 555-565页

作者： Yongbing Sun Wei Gan Mingdao Lei Wei Jiang Meng Cheng Junwei He Qi Sun Wan Liu Lvjiang Hu Yi Jin Division of Pharmaceutics National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine Jiangxi University of Traditional Chinese Medicine Department of pharmacy Jiangxi Maternal and Child Health Hospital Research Center of Natural Resources of chinese Medicinal Materials and Ethnic medicine Jiangxi University of Traditional Chinese Medicine Affiliated Hospital of jiangxi university of traditional chinese medicine

Peramivir was a novel and highly potent neuraminidase(NA) inhibitor for the treatment of influenza A and B. However, it exhibited a very low oral bioavailability(only 3%) due to the high polarity(log P of-1.4) and the low membrane permeability across the intestine. To utilize the PEPT1-mediated prodrug strategy to improve the oral absorption and develop the oral alternative, seven amino acid ester prodrugs and seven amino acid amide prodrugs have been synthesized. The permeability of these prodrugs across Caco-2 cells were screened. Peramivr-(CH_2)_2-l-Val and Peramivir-l-Ile were of the highest permeability in ester prodrugs and amide prodrugs, respectively, and then they were selected for further studies. Glycylsarcosine(gly-sar) uptake by Caco-2 could be inbihited by Peramivir-(CH_2)_2-l-Val and Peramivir-l-Ile in a concentration-dependent manner, and the IC 50 was 1.34 ± 0.31 m M and 1.78 ± 0.48 m M, respectively. The direct uptake of Peramivir-(CH_2)_2-l-Val and Peramivirl-Ile in MDCK-PEPT1 cells were significantly higher than in MDCK mock cells, and could be markedly inhibited by gly-sar. The uptake of Peramivir-(CH_2)_2-l-Val and Peramivir-l-Ile(0.01 to 50 m M) in MDCK-hPEPT1 cells conformed to Michaelis–Menten Equation. The oral bioavailability of peramivir was 65.3% and 37.3% after the oral administration of Peramivir-(CH_2)_2-l-Val and Peramivir-l-Ile to rats, respectively. The oral absorption and bioactivation of Peramivir-(CH_2)_2-l-Val was rapid and extensive, and no Peramivir-(CH_2)_2-l-Val was found in plasma. Because the amide bond was relatively stable, Peramivir-l-Ile could not be totally converted to the parent drug in vivo. Peramivir-(CH_2)_2-l-Val with good oral profiles and rapid bioactivation might be a promising prodrug for the further clinic development. The present study also corroborated the idea that the PEPT1-mediated prodrug approach has enormous promise for improving the oral absorption of poorly absorbed drug.

关键词： Peramivir Prodrug Peptide transporter 1 Pharmacokinetics Oral bioavailability

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Anti-acute gastric ulcer resistance of Aurantii Fructus Immaturus juice processing Atractylodis Macrocephalae Rhizoma by regulating PTGS2,MAPK1,and KDR targets based on metabolomics and integrated network pharmacology analysis

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Science of traditional chinese medicine 2024年第2期2卷 121-137页

作者： Wanai Xu Jingyu Wu Danyang Yang Yuxun Chen Xiaoying Wu Rou Wen Liping Yan Chao Li Huan Yu school of pharmacy Jiangxi University of Chinese MedicineNanchangChina school of pharmacy Tianjin University of Traditional Chinese MedicineTianjinChina

Background:Currently,traditional methods of treating acute gastric ulcer(AGU)have many drawbacks,necessitating an alternative therapy with fewer adverse *** Macrocephalae Rhizoma(BZ)is known for strengthening the spleen and harmonizing the *** processed with Aurantii Fructus Immaturus juice(ZSZBZ),a classic decoction since the Han Dynasty,can enhance the efficacy of ***,the key active components and targets of action of ZSZBZ remain *** the study:This study aimed to investigate the bioactive chemical constituents of ZSZBZ against AGU and their possible mechanisms of action,elucidating the scientific content of ZSZBZ *** and methods:Initially,we examined rat stomach histopathology and conducted ELISA for oxidative stress and ***,we investigated underlying mechanisms using *** analysis of potent components and key targets in ZSZBZ was conducted through liquid chromatography-mass spectrometry analysis combined with network ***,key targets were analyzed by Western ***:ZSZBZ improved gastric histopathology,reversing high alcohol-induced oxidative stress(SOD,CAT)and inflammatory level(TNF-α,IL-6)*** is associated with ZSZBZ’s regulation of amino acid metabolism,energy metabolism,and inflammatory response-related metabolic pathways,along with key targets PTGS2,MAPK1,and *** significant increase in potency of ZSZBZ may be attributed to elevated levels of naringenin,hesperidin,hesperidin,and rhamnoceroside after ***:Combining metabolomics and network pharmacology,this study elucidated that ZSZBZ enhanced gastroprotection by modulating amino acid metabolism,antioxidant,and inflammation-related targets and pathways,providing insights into the bioactive compounds and potential mechanisms of herbal concoctions.

关键词： Metabolomics Network pharmacology Processing Atractylodes macrocephala Koidz Gastric ulcer

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Screening hepatoprotective effective components of Lonicerae japonica Flos based on the spectrum-effect relationship and its mechanism exploring

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Food Science and Human Wellness 2023年第1期12卷 283-294页

作者： Song Wang Lin Yang Ajiao Hou Songtao Liu Liu Yang Haixue Kuang Hai Jiang Key Laboratory of chinese Materia Medica Heilongjiang University of Chinese MedicineMinistry of EducationHarbin 150040China school of pharmacy Jiangxi University of Traditional Chinese MedicineNanchang 330004China

Lonicerae japonicae Flos(LF)is a kind of healthcare food with hepatoprotective *** study was designed to explore the spectrum-effect relationships between UPLC fingerprints and the hepatoprotective effects of *** of ten batches of LF were established by *** inhibitory levels of AST and ALT were used as pharmacological indexes,and secoxyloganin,isochlorogenic acid A and isochlorogenic acid C were screened as hepatoprotective active compounds by grey relational analysis(GRA)and partial least squares regression analysis(PLSR).Caspase-3 was obtained by network pharmacology as a key target of hepatoprotective active *** docking is used to explore the interaction between small molecules and *** work provided a general model of the combination of UPLC-PDA and hepatoprotective effect to study the spectrum-effect relationship of LF,which can be used to considerable methods and insight for the fundamental research of the material basis of similar healthcare food.

关键词： Lonicerae japonicae Flos Hepatoprotective effect Spectrum-effect relationship Molecular docking Mechanism

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Optimization of taste-masking on ibuprofen microspheres with selected structure features

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Asian Journal of Pharmaceutical Sciences 2019年第2期14卷 174-182页

作者： Wei Qin Yuanzhi He Zhen Guo Liu Zhang Li Wu Xianzhen Yin Shailendra Shakya Abi Maharjan Yan Tang Weifeng Zhu Jiwen Zhang Ministry of Education Jiangxi University of Traditional Chinese Medicine Shanghai Institute of Materia Medica Chinese Academy of Sciences school of pharmacy Shenyang Pharmaceutical University school of pharmacy University of Chinese Academy of Sciences

The microsphere was a primary particulate system for taste-masking with unique structural features defined by production process. In this article, ibuprofen lipid microspheres of octadecanol and glycerin monostearate were prepared to mask the undesirable taste of ibuprofen via three kinds of spray congealing processes, namely, air-cooling, water-cooling and citric acid solution-cooling. The stereoscopic and internal structures of ibuprofen microspheres were quantitatively analyzed by synchrotron radiation X-ray micro-computed tomography(SR-μCT) to establish the relationship between the preparation process and microsphere architectures. It was found that the microstructure and morphology of the microspheres were significantly influenced by preparation processes as the primary factors to determine the release profiles and taste-masking effects. The sphericity of ibuprofen microspheres congealed in citric acid solution was higher than that of other two and its morphology was more regular than that being congealed in air or distilled water, and the contact angles between congealing media and melted ibuprofen in octadecanol and glycerin monostearate well demonstrated the structure differences among microspheres of three processes which controlled the release characteristics of the microspheres. The structure parameters like porosity, sphericity, and radius ratio from quantitative analysis were correlated well with drug release behaviors. The results demonstrated that the exterior morphology and internal structure of microspheres had considerable influences on the drug release behaviors as well as taste-masking effects.

关键词： Ibuprofen microsphere Spray congealing Internal structure Synchrotron radiation X-ray micro-computed tomography

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Enhanced treatment for cerebral ischemia-reperfusion injury of puerarin loading liposomes through neutrophils-mediated targeted delivery

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Nano Research 2021年第12期14卷 4634-4643页

作者： Wei Liu Haowei Lu Xiaoyong Rao Xiang Li Hongdan Lu Feifei Li Yan He Riyue Yu Rongsheng Zhong Yao Zhang Xiaojian Luo Hongliang Xin National Pharmaceutical Engineering Center for Solid Preparation in chinese Herbal medicine Jiangxi University of Traditional Chinese MedicineNanchang330006China The Affiliated Hospital of jiangxi university of traditional chinese medicine Nanchang330006China Department of Pharmaceutics and Key Laboratory of Cardiovascular&Cerebrovascular medicine School of PharmacyNanjing Medical UniversityNanjing211166China Department of pharmacy Kangda College of Nanjing Medical UniversityLianyungang222000China

The recovery of blood circulation following cerebral infarction-associated thrombolysis brings new damage to the brain,which is cerebral ischemia-reperfusion injury(CIRI).Inflammation is the main pathological mechanism of *** inflammatory response triggered by cerebral ischemia-reperfusion provides neutrophils with a special opportunity to facilitate drug delivery to the site of ischemic penumbra through the chemotaxis of inflammatory factors by *** is an isoflavone derivative with a significant neuroprotective effect in *** the blood-brain barrier(BBB)impedes its therapeutic efficacy on CIRI within the *** by the pathological process,we have used neutrophils as carriers to enhance the BBB penetration of liposomes loaded with puerarin and improve the concentration of puerarin in the brain parenchyma in this *** results showed that puerarin-containing liposomes were released in response to inflammatory conditions associated with brain injury to enhance the neuroprotection effect at the ischemic penumbra.

关键词： cerebral ischemia-reperfusion injury neuroprotection neutrophils puerarin liposomes

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Novel wine in an old bottle:Preventive and therapeutic potentials of andrographolide in atherosclerotic cardiovascular diseases

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Journal of Pharmaceutical Analysis 2023年第6期13卷 563-589页

作者： Tingting Gou Minghao Hu Min Xu Yuchen Chen Rong Chen Tao Zhou Junjing Liu Li Guo Hui Ao Qiang Ye State Key Laboratory of Southwestern chinese medicine Resources Chengdu University of Traditional Chinese MedicineChengdu611137China school of pharmacy Chengdu University of Traditional Chinese MedicineChengdu611137China Innovative Institute of chinese medicine and pharmacy Chengdu University of Traditional Chinese MedicineChengdu611137China

Atherosclerotic cardiovascular disease(ASCVD)frequently results in sudden death and poses a serious threat to public health *** drugs approved for the prevention and treatment of ASCVD are usually used in combination but are inefficient owing to their side effects and single therapeutic ***,the use of natural products in developing drugs for the prevention and treatment of ASCVD has received great scholarly ***(AG)is a diterpenoid lactone compound extracted from Andrographis *** addition to its use in conditions such as sore throat,AG can be used to prevent and treat *** is different from drugs that are commonly used in the prevention and treatment of ASCVD and can not only treat obesity,diabetes,hyperlipidaemia and ASCVD but also inhibit the pathological process of atherosclerosis(AS)including lipid accumulation,inflammation,oxidative stress and cellular abnormalities by regulating various targets and ***,the pharmacological mechanisms of AG underlying the prevention and treatment of ASCVD have not been corroborated,which may hinder its clinical development and ***,this review summarizes the physiological and pathological mechanisms underlying the development of ASCVD and the in vivo and in vitro pharmacological effects of AG on the relative risk factors of AS and *** findings support the use of the old pharmacological compound(‘old bottle’)as a novel drug(‘novel wine’)for the prevention and treatment of ***,this review summarizes studies on the availability as well as pharmaceutical and pharmacokinetic properties of AG,aiming to provide more information regarding the clinical application and further research and development of AG.

关键词： Andrographolide Atherosclerosis Atherosclerotic cardiovascular disease Pharmacological effects Pharmacokinetics properties Toxicity

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New perspectives on the therapeutic potential of quercetin in non-communicable diseases:Targeting Nrf2 to counteract oxidative stress and inflammation

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Journal of Pharmaceutical Analysis 2024年第6期14卷 805-822页

作者： Li Zhang Li-Yue Xu Fei Tang Dong Liu Xiao-Lan Zhao Jing-Nan Zhang Jia Xia Jiao-Jiao Wu Yu Yang Cheng Peng Hui Ao State Key Laboratory of Southwestern chinese medicine Resources School of PharmacyChengdu University of Traditional Chinese MedicineChengdu611137China Innovative Institute of chinese medicine and pharmacy Chengdu University of Traditional Chinese MedicineChengdu611137China

Non-communicable diseases(NCDs),including cardiovascular diseases,cancer,metabolic diseases,and skeletal diseases,pose significant challenges to public health *** complex pathogenesis of these diseases is closely linked to oxidative stress and inflammatory *** factor erythroid 2-related factor 2(Nrf2),a critical transcription factor,plays an important role in regulating antioxidant and anti-inflammatory responses to protect the cells from oxidative damage and inflammation-mediated ***,Nrf2-targeting therapies hold promise for preventing and treating ***(Que)is a widely available flavonoid that has significant antioxidant and anti-inflammatory *** modulates the Nrf2 signaling pathway to ameliorate oxidative stress and *** modulates mitochondrial function,apoptosis,autophagy,and cell damage biomarkers to regulate oxidative stress and inflammation,highlighting its efficacy as a therapeutic agent against ***,we discussed,for the first time,the close association between NCD pathogenesis and the Nrf2 signaling pathway,involved in neurodegenerative diseases(NDDs),cardiovascular disease,cancers,organ damage,and bone ***,we reviewed the availability,pharmacokinetics,pharmaceutics,and therapeutic applications of Que in treating *** addition,we focused on the challenges and prospects for its clinical *** represents a promising candidate for the treatment of NCDs due to its Nrf2-targeting properties.

关键词： Quercetin Nrf2 Non-communicable diseases Antioxidant Anti-inflammatory Availability

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A metal ions-mediated natural small molecules carrier-free injectable hydrogel achieving laser-mediated photo-Fenton-like anticancer therapy by synergy apoptosis/cuproptosis/anti-inflammation

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Bioactive Materials 2023年第11期29卷 98-115页

作者： Wenmin Pi Linying Wu Jihui Lu Xiaoyu Lin Xuemei Huang Zhijia Wang Zhihua Yuan Hailing Qiu Jianglan Zhang Haimin Lei Penglong Wang school of chinese pharmacy Beijing University of Chinese MedicineBeijing102488China school of traditional chinese medicine Beijing University of Chinese MedicineBeijing102488China

Tumor microenvironment (TME) plays an important role in the tumorigenesis, proliferation, invasion and metastasis. Thereby developing synergistic anticancer strategies with multiple mechanisms are urgent. Copper is widely used in the treatment of tumor chemodynamic therapy (CDT) due to its excellent laser-mediated photo- Fenton-like reaction. Additionally, copper can induce cell death through cuproptosis, which is a new modality different from the known death mechanisms and has great promise in tumor treatment. Herein, we report a natural small molecules carrier-free injectable hydrogel (NCTD Gel) consisted of Cu2+-mediated self-assembled glycyrrhizic acid (GA) and norcantharidin (NCTD), which are mainly governed by coordination and hydrogen bonds. Under 808 nm laser irradiation, NCTD Gel can produce reactive oxygen species (ROS), consume glutathione (GSH) and overcome hypoxia in TME, leading to synergistically regulate TME via apoptosis, cuproptosis and anti-inflammation. In addition, NCTD Gel’s CDT display high selectivity and good biocompatibility as it relies on the weak acidity and H2O2 overexpression of TME. Notably, NCTD Gel’s components are originated from clinical agents and its preparation process is easy, green and economical, without any excipients. This study provides a new carrier-free hydrogel synergistic antitumor strategy, which has a good prospect in industrial production and clinical transformation.

关键词： Natural small molecular ternary carrier-free hydrogel Tumor microenvironment Cuproptosis Laser-mediated photo-fenton-like reaction

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Regulatory effects of Poria on substance and energy metabolism in cold-deficiency syndrome compared with heat-deficiency syndrome in rats

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chinese Journal of Natural medicines 2018年第12期16卷 936-945页

作者： HAN Xue-Ying WANG Ya-Nan DOU De-Qiang College of pharmacy Liaoning University of Traditional Chinese Medicine

Recent studies have revealed that the property of drug is mainly associated with the body's substance and energy metabolism. The present study aimed to evaluate the drug property of Poria, called Fuling(FL) in traditional chinese medicine(TCM), in terms of its effects on the substance and energy metabolism in rat models of cold-deficiency and heat-deficiency syndromes, compared with Aconiti Lateralis Radix Praeparaia, called Fuzi(FZ) in TCM, with hot property, and Anemarrhenae Rhizoma, called Zhimu(ZM) in TCM, with cold property, as reference drugs, respectively. The appearance score, toe and rectal temperatures of the animals treated were assessed at different time points. Several indices in vivo correlated with substance and energy metabolism(glucokinas, phosphoglycerate kinase, cytochrome c reductase, cytochrome c oxydase, and Na^+-K^+-ATPase), endocrine system(triiodothyronine, thyroxine, and 17-hydroxycorticosteroid), nervous system(acetylcholin esterase), and cyclic nucleotide system were determined. The changes in appearance score and indices in vivo suggested the successful establishment of cold-deficiency and heat-deficiency syndrome models. FZ reversed the decreased levels of indices(substance and energy metabolism and endocrine system) and alleviated the syndrome of cold-deficiency model, and ZM showed obviously therapeutic effect on heat-deficiency syndrome(appearance score, substance and energy metabolism, and endocrine system). FL could alleviate cold-deficiency syndrome and raise the decreased levels of glucokinas, phosphoglycerate kinase, cytochrome c reductase and triiodothyronine in cold-deficiency model, but had no significant effect on heat-deficiency syndrome. Drug property of FL was inferred as trending to "flat and warm", which still need further study. It was advisable to adopt both cold-deficiency and heat-deficiency models to study the drugs with "flat" property.

关键词： Poria Substance metabolism Energy metabolism Cold-deficiency syndrome Heat-deficiency syndrome

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Characterization and Comparison Analysis of WHO Monographs on Selected Medicinal Plants and Iso Standards of chinese Materia Medica

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chinese Journal of Integrative medicine 2023年第6期29卷 540-548页

作者： YANG Jing-yi SANG Zhen WANG Rui SHI Yan-hong HUANG Yi-ran school of pharmacy Shanghai University of Traditional Chinese MedicineShanghai(201203)China Institute of traditional chinese medicine International Standardization Shuguang Hospital Affliated to Shanghai University of Traditional Chinese MedicineShanghai(201203)China Institute of traditional chinese medicine International Standardization Shanghai University of Traditional Chinese MedicineShanghai(201203)China

Medicinal plants or chinese materia medica(CMM)are now attracting worldwide attention as they have increasingly prominent advantages over chemical drugs in disease treatment and *** the 1990s,World Health Organization(WHO)and International Organization for Standardization established the Technical Committee of traditional chinese medicine(ISO/TC 249)have carried out the development of quality standards on medicinal plants or CMMs respectively,and a considerable number of monographs and international standards have been *** the two international organizations adhere to different principles,the standards they develop naturally have different *** by market demand and international trade,ISO mainly takes quality,efficacy and safety into consideration when developing standards,while WHO pays more attention to clinical practice,quality control and medication *** to now,there is a lack of comparative analysis on the records,background,principles,basic content,and main requirements of quality standards on medicinal plants or CMMs respectively published by WHO and ***,based on international standards of CMM developed by ISO/TC 249 platform and WHO Monographs on Selected Medicinal Plants,this paper systematically compares the purposes,selected principles,standard-developing process,basic content,and main quality requirements to summarize their similarities and differences,and find their merits,aiming to serve as a reference to the development of international standards for CMMs that helps them go global.

关键词： chinese materia medica medicinal plants international standards International Organization for Standardization Technical Committee of traditional chinese medicine World Health Organization

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