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Lenalidomide acesulfamate: Crystal structure, solid state characterization and dissolution performance EI Scopus SCIE
期刊论文 | 2019 , 1175 , 852-857 | Journal of Molecular Structure
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Abstract :

Lenalidomide (LEN) is a first line drug in the treatment of multiple myeloma, myelodysplastic syndromes, and mantle cell lymphoma. While, this compound holds poor water solubility, leading to unsatisfied bioavailability. To improve the solubility of LEN, a molecular salt with an artificial sweetener, acesulfame (AH), was obtained in this study. The LEN-AH salt was fully characterized by single-crystal and powder X-ray diffraction (XRD), 13C solid state nuclear magnetic resonance (NMR), differential scanning calorimetry (DSC), as well as dynamic vapour sorption (DVS). The crystal structure of LEN-AH clearly reveals the intermolecular proton transfer from NH group of AH to NH2 of LEN. The ionization state of LEN-AH was further confirmed by its feature 13C chemical shifts. The maximum solubility value of LEN was significantly enhanced after salt formation. And the supersaturation state of LEN solution can be maintained at a higher level with the presence of 0.1% PVP-K30. © 2018 Elsevier B.V.

Keyword :

Artificial sweeteners Intermolecular interactions Lenalidomide Myelodysplastic syndromes Single-crystal and powder Solid state characterization Solid-state nuclear magnetic resonance Solubilization

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GB/T 7714 Chen, Xin , Li, Duanxiu , Wang, Jianming et al. Lenalidomide acesulfamate: Crystal structure, solid state characterization and dissolution performance [J]. | Journal of Molecular Structure , 2019 , 1175 : 852-857 .
MLA Chen, Xin et al. "Lenalidomide acesulfamate: Crystal structure, solid state characterization and dissolution performance" . | Journal of Molecular Structure 1175 (2019) : 852-857 .
APA Chen, Xin , Li, Duanxiu , Wang, Jianming , Deng, Zongwu , Zhang, Hailu . Lenalidomide acesulfamate: Crystal structure, solid state characterization and dissolution performance . | Journal of Molecular Structure , 2019 , 1175 , 852-857 .
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Development and evaluation of hollow mesoporous silica microspheres bearing on enhanced oral delivery of curcumin. PubMed SCIE
期刊论文 | 2019 , 45 (2) , 273-281 | Drug development and industrial pharmacy
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Abstract :

The aim of this work is to develop curcumin-loaded hollow mesoporous silica microspheres (HMSMs@curcumin) to improve the poor oral bioavailability of curcumin. Hollow mesoporous silica microspheres (HMSMs) were synthesized in facile route using a hard template. HMSMs and HMSMs@curcumin were characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), nitrogen adsorption/desorption measurements, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) and X-ray diffraction (XRD). In addition, to demonstrate the potential application of the HMSMs@curcumin, cytotoxicity, in vitro release behavior and in vivo pharmacokinetics of curcumin loaded in these HMSMs were investigated by using of Caco-2 cells and Sprague-Dawley (SD) rats, respectively. These mono-dispersed HMSMs exhibited high drug loading ratio and encapsulation efficiency due to the mesoporous shell and hollow core. The excellent characteristics of HMSMs such as mono-dispersed morphology, smooth surface, uniform, ordered and size-narrowing mesopores resulted in a good in vitro release profile of curcumin from HMSMs@curcumin. Moreover, an impressive improvement in the oral absorption of curcumin and prolonged systemic circulation time were achieved in the in vivo animal studies. In addition, the good biocompatibility of developed HMSMs with Caco-2 cells was confirmed based on the in vitro cytotoxicity assay. In conclusion, this system demonstrated a great potential for efficiently delivery of curcumin in vitro and in vivo, suggesting a good prospect for its application in clinic for therapeutic drug delivery in future.

Keyword :

Cytotoxicity Hollow mesoporous silica microspheres (HMSMs) Curcumin In vivo drug delivery In vitro drug release

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GB/T 7714 Gao Yang , Ding Shujiang , Huang Xiaoyan et al. Development and evaluation of hollow mesoporous silica microspheres bearing on enhanced oral delivery of curcumin. [J]. | Drug development and industrial pharmacy , 2019 , 45 (2) : 273-281 .
MLA Gao Yang et al. "Development and evaluation of hollow mesoporous silica microspheres bearing on enhanced oral delivery of curcumin." . | Drug development and industrial pharmacy 45 . 2 (2019) : 273-281 .
APA Gao Yang , Ding Shujiang , Huang Xiaoyan , Fan Zhaoyang , Sun Jianmei , Hai Yang et al. Development and evaluation of hollow mesoporous silica microspheres bearing on enhanced oral delivery of curcumin. . | Drug development and industrial pharmacy , 2019 , 45 (2) , 273-281 .
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Prices, availability and affordability of insulin products: a cross-sectional survey in Shaanxi Province, western China. PubMed Scopus SCIE
期刊论文 | 2019 , 24 (1) , 43-52 | Tropical medicine & international health : TM & IH
WoS CC Cited Count: 1
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Abstract :

To evaluate price, availability and affordability of insulin products in Shaanxi Province, western China.We used a simplified and adapted WHO/Health Action International method to obtain the availability and prices of insulin products and 5 oral anti-diabetic medicines as comparators in public general hospitals and private retail outlets. In addition, we investigated the price components of 8 selected insulin products by tracing the supply chain.All three kinds of insulin products, prandial, basal and premixed insulin, are 100% available in public hospitals, and have fairly high availability in the private sector (62.5% to 68.8%). The prices of most insulin products were higher than international reference prices in both sectors (ranging from 0.95 times to 2.33 times). All insulin products were unaffordable as they would cost 3.5 to 17.1 days' wage of the lowest-paid government workers in Shaanxi. The manufacturer's markup (selling price), which comprised more than 60% of the final price of all insulin products surveyed, was the largest price component.Although availability of insulin products was high in public general hospitals and private retail pharmacies, their high price made them unaffordable to diabetes patients, especially low-income patients. The government should increase insurance compensation for those who need these life-saving medicines or decrease the cost of insulin products through negotiation with suppliers. This article is protected by copyright. All rights reserved.

Keyword :

price components insulin China affordability availability

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GB/T 7714 Li Zongjie , Feng Qinqin , Kabba John Alimamy et al. Prices, availability and affordability of insulin products: a cross-sectional survey in Shaanxi Province, western China. [J]. | Tropical medicine & international health : TM & IH , 2019 , 24 (1) : 43-52 .
MLA Li Zongjie et al. "Prices, availability and affordability of insulin products: a cross-sectional survey in Shaanxi Province, western China." . | Tropical medicine & international health : TM & IH 24 . 1 (2019) : 43-52 .
APA Li Zongjie , Feng Qinqin , Kabba John Alimamy , Yang Caijun , Chang Jie , Jiang Minghuan et al. Prices, availability and affordability of insulin products: a cross-sectional survey in Shaanxi Province, western China. . | Tropical medicine & international health : TM & IH , 2019 , 24 (1) , 43-52 .
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Silencing of LncRNA steroid receptor RNA activator attenuates polycystic ovary syndrome in mice Scopus SCIE PubMed
期刊论文 | 2019 , 157 , 48-56 | Biochimie
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© 2018 Elsevier B.V. and Société Française de Biochimie et Biologie Moléculaire (SFBBM) Background: Polycystic ovary syndrome (PCOS) is the most common endocrine disorder in women of reproductive age and has a prevalence of 1 in 15 women worldwide. This study aims to investigate the role of lncRNA SRA in the pathological processes of polycystic ovary syndrome (PCOS). Methods: Twenty five-day old female C57BL/6 mice received subcutaneous injection of 60 mg/kg dehydroepiandrosterone for 20 days to induce PCOS. Lentivirus containing lncRNA SRA-specific shRNA was subcapsularly injected into the ovaries of PCOS mice. Granulosa cell was primary cultured to explore the mechanism of DHEA-induced inflammatory responses. H&E staining was used to examine the histological changes of ovaries. ELISA was used to assess serum insulin level and proinflammatory cytokines and angiogenetic factors contents in ovary tissue. The expression levels of LncRNA SRA and proteins involved in the NF-κB signaling pathway were detected through Quantitative real-time PCR and Western blot. The nuclear translocation of NF-κB was observed by immunofluorescence and the activity of NF-κB-DNA binding was detected using EMSA. Results: Silencing of lncRNA SRA changed insulin release, attenuated ovary injury and reduced the production of angiogenetic factors in the PCOS mice. In addition, shRNA targeting lncRNA SRA inhibited DHEA-induced pro-inflammatory cytokines production and NF-κB nuclear translocation in the ovary of PCOS mice and primary granulosa cells. Conclusion: Silencing of lncRNA Steroid Receptor RNA Activator (SRA) attenuates polycystic ovary syndrome (PCOS) in mice. LncRNA SRA plays important roles in the development of PCOS.

Keyword :

Angiogenesis Granulosa cell Inflammation LncRNA SRA PCOS

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GB/T 7714 Li, Yan , Zhao, Wanqiu , Wang, Haixu et al. Silencing of LncRNA steroid receptor RNA activator attenuates polycystic ovary syndrome in mice [J]. | Biochimie , 2019 , 157 : 48-56 .
MLA Li, Yan et al. "Silencing of LncRNA steroid receptor RNA activator attenuates polycystic ovary syndrome in mice" . | Biochimie 157 (2019) : 48-56 .
APA Li, Yan , Zhao, Wanqiu , Wang, Haixu , Chen, Chen , Zhou, Dongmei , Li, Shengnan et al. Silencing of LncRNA steroid receptor RNA activator attenuates polycystic ovary syndrome in mice . | Biochimie , 2019 , 157 , 48-56 .
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Biodegradable Gelatin Methacryloyl Microneedles for Transdermal Drug Delivery. PubMed SCIE
期刊论文 | 2019 , 8 (3) , e1801054 | Advanced healthcare materials
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Abstract :

Biocompatible and bioresponsive microneedles (MNs) are emerging technology platforms for sustained drug release with a potential to be a key player in transdermal delivery of therapeutics. In this paper, an innovative biodegradable MNs patch for the sustained delivery of drugs using a polymer patch, which can adjust delivery rates based on its crosslinking degree, is reported. Gelatin methacryloyl (GelMA) is used as the base for engineering biodegradable MNs. The anticancer drug doxorubicin (DOX) is loaded into GelMA MNs using the one molding step. The GelMA MNs can efficiently penetrate the stratum corneum layer of a mouse cadaver skin. Mechanical properties and drug release behavior of the GelMA MNs can be adjusted by tuning the degree of crosslinking. The efficacy of the DOX released from the GelMA MNs is tested and the anticancer efficacy of the released drugs against melanoma cell line A375 is demonstrated. Since GelMA is a versatile material in engineering tissue scaffolds, it is expected that the GelMA MNs can be used as a platform for the delivery of various therapeutics.

Keyword :

transdermal drug delivery microneedle sustained release gelatin methacryloyl

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GB/T 7714 Luo Zhimin , Sun Wujin , Fang Jun et al. Biodegradable Gelatin Methacryloyl Microneedles for Transdermal Drug Delivery. [J]. | Advanced healthcare materials , 2019 , 8 (3) : e1801054 .
MLA Luo Zhimin et al. "Biodegradable Gelatin Methacryloyl Microneedles for Transdermal Drug Delivery." . | Advanced healthcare materials 8 . 3 (2019) : e1801054 .
APA Luo Zhimin , Sun Wujin , Fang Jun , Lee KangJu , Li Song , Gu Zhen et al. Biodegradable Gelatin Methacryloyl Microneedles for Transdermal Drug Delivery. . | Advanced healthcare materials , 2019 , 8 (3) , e1801054 .
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Determining the optimal cutoff point for lymph node density and its impact on overall survival in children with Wilms' tumor SCIE PubMed
期刊论文 | 2019 , 11 , 759-766 | CANCER MANAGEMENT AND RESEARCH
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Abstract :

Objective: Previous studies showed that the lymph node density (LND) was a predictor of survival in Wilms' tumor (WT). However, the optimal LND cutoff point is controversial due to methodological shortcomings of previous studies, and no studies have shown the effect of LND on survival in children with WT. The purpose of this study was to remedy this situation. Methods: We identified 376 children with WT. LND cutoff point was determined using the median value, the X-tile program, the survival-tree algorithm, and the time-dependent ROC curve analysis. Survival functions were estimated by the Kaplan-Meier method. We used Cox regression analysis to determine the impact of LND on survival. Smooth curve fitting between relative mortality risk and LND was performed. Results: The LND cutoff point was 0.44, 0.65, 0.65, and 0.64 according to the median value, the X-tile program, the survival-tree algorithm, and the time-dependent ROC curve analysis, respectively. The 5-, 10-, and 20-year overall survival rates were 86.9%, 86.9%, and 84.7%, respectively, in the <0.44 group and 81.3%, 80.3%, and 80.3%, respectively, in the >= 0.44 group. Survival did not differ significantly between the two groups (P=0.185). The 5-, 10-, and 20-year overall survival rates were 87.8%, 87.8%, and 86.0%, respectively, in the <0.65 or <0.64 group and 76.5%, 75.1%, and 75.1%, respectively, in the >= 0.65 or >= 0.64 group. Children with the high LND had a significantly worse survival (P=0.011) if 0.64 or 0.65 was used for the stratification. LND was a significant predictor for overall survival in the multivariate Cox regression analysis (HR=1.797; 95% CI, 1.043-3.097; P=0.035). Smooth curve fitting suggested that the risk of mortality tended to be ascending with the increase in LND in general. Conclusion: The three methods including the X-tile program, the survival-tree algorithm, and the time-dependent receiver operating characteristic (ROC) curve analysis are equivalent in their ability to stratify patients and clearly better than the median method. The results showed that the optimal LND cutoff point was around 0.65 and the LND was a reliable predictor of overall survival in children with WT.

Keyword :

lymph node density cutoff point survival Wilms' tumor

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GB/T 7714 Pan, Zhenyu , Bu, Qingting , You, Haisheng et al. Determining the optimal cutoff point for lymph node density and its impact on overall survival in children with Wilms' tumor [J]. | CANCER MANAGEMENT AND RESEARCH , 2019 , 11 : 759-766 .
MLA Pan, Zhenyu et al. "Determining the optimal cutoff point for lymph node density and its impact on overall survival in children with Wilms' tumor" . | CANCER MANAGEMENT AND RESEARCH 11 (2019) : 759-766 .
APA Pan, Zhenyu , Bu, Qingting , You, Haisheng , Yang, Jin , Liu, Qingqing , Lyu, Jun . Determining the optimal cutoff point for lymph node density and its impact on overall survival in children with Wilms' tumor . | CANCER MANAGEMENT AND RESEARCH , 2019 , 11 , 759-766 .
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Species delimitation and interspecific relationships of the endangered herb genus Notopterygium inferred from multilocus variations. PubMed
期刊论文 | 2019 , 133 , 142-151 | Molecular phylogenetics and evolution
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Abstract :

Species identification and discrimination is the basis of biodiversity research. In general, it is considered that numerous nucleotide variations (e.g., whole chloroplast genomes) can identify species with higher resolution than a few loci, e.g., partial chloroplast or nuclear gene fragments. In this study, we tested this hypothesis by sampling population genetics samples of the endangered herb genus Notopterygium. We sequenced the complete plastomes, five nuclear gene regions, three chloroplast DNA fragments, and a nuclear internal transcribed spacer (nrITS) region for 18 populations sampled throughout most of the geographic ranges of all six Notopterygium species. Species identification analysis showed that four DNA barcodes (matK, rbcL, trnS-trnG, and nrITS) and/or combinations of these markers achieved Notopterygium species discrimination at higher resolution than the general plastomes and nuclear gene sequences. In particular, nrITS had the highest discriminatory power among all of the individual markers. Molecular data sets and morphological evidence indicated that all six Notopterygium species could be reclassified unambiguously to four putative species clades. N. oviforme and N. franchetii had the closest relationship. Molecular dating showed that the origin and divergence of Notopterygium species was significantly associated with geological and climatic fluctuations during the middle of the Pliocene. In conclusion, our results suggest that a few nucleotide variations can achieve species discrimination with higher resolution than numerous plastomes and general nuclear gene fragments when discerning related Notopterygium species.

Keyword :

Chloroplast genome Notopterygium DNA barcode Nuclear marker Species identification

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GB/T 7714 Yang Jiao , Feng Li , Yue Ming et al. Species delimitation and interspecific relationships of the endangered herb genus Notopterygium inferred from multilocus variations. [J]. | Molecular phylogenetics and evolution , 2019 , 133 : 142-151 .
MLA Yang Jiao et al. "Species delimitation and interspecific relationships of the endangered herb genus Notopterygium inferred from multilocus variations." . | Molecular phylogenetics and evolution 133 (2019) : 142-151 .
APA Yang Jiao , Feng Li , Yue Ming , He Yan-Ling , Zhao Gui-Fang , Li Zhong-Hu . Species delimitation and interspecific relationships of the endangered herb genus Notopterygium inferred from multilocus variations. . | Molecular phylogenetics and evolution , 2019 , 133 , 142-151 .
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Dehydroandrographolide inhibits IgE-mediated anaphylactic reactions via calcium signaling pathway. PubMed SCIE
期刊论文 | 2019 , 366 , 46-53 | Toxicology and applied pharmacology
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The classical mast cells degranulation pathway is mediated by FcεRI aggregation and varies in strength among subjects. Dehydroandrographolide (DA) is one of principal components of Andrographis paniculata (Burm.f.) Nees (family: Acanthaceae) and considered the main contributors of its therapeutic properties, such as anti-tumor. In this study, inhibition of IgE-mediated anaphylactic reactions and anti-inflammatory potential of DA were investigated. The anti-anaphylactic activity of DA was investigated using skin swelling and extravasation assays in vivo and mast cell degranulation assay in vitro. The release of cytokines was measured using ELISA kits. Human Phospho-Kinase Array kit and western blotting were used to explore the related molecular signaling pathways. DA inhibited IgE-mediated mast cell activation, including degranulation and release of cytokines in vitro. Moreover, DA reduced the degree of swelling and Evans blue exudation of mice paw in a dose-dependent manner by inhibiting mast cell degranulation. DA obviously reduced the concentrations of histamine, TNF-α, MCP-1, IL-8, IL-13, and IL-4 in mice serum and inhibited IgE-mediated anaphylactic reactions as a potential P-PLCγ inhibitor. Our study reveals that DA can inhibit allergic responses in vivo and in vitro, and it may be regarded as a novel P-PLCγ inhibitor for preventing mast cell-immediate and delayed allergic diseases.

Keyword :

Mast cells IgE-mediated anaphylactic reactions Dehydroandrographolide P-PLCγ inhibitor Degranulation

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GB/T 7714 Che Delu , Hou Yajing , Zeng Yingnan et al. Dehydroandrographolide inhibits IgE-mediated anaphylactic reactions via calcium signaling pathway. [J]. | Toxicology and applied pharmacology , 2019 , 366 : 46-53 .
MLA Che Delu et al. "Dehydroandrographolide inhibits IgE-mediated anaphylactic reactions via calcium signaling pathway." . | Toxicology and applied pharmacology 366 (2019) : 46-53 .
APA Che Delu , Hou Yajing , Zeng Yingnan , Li Chaomei , Zhang Yongjing , Wei Di et al. Dehydroandrographolide inhibits IgE-mediated anaphylactic reactions via calcium signaling pathway. . | Toxicology and applied pharmacology , 2019 , 366 , 46-53 .
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Antidiabetic and hepatoprotective activity of the roots of Calanthe fimbriata Franch. PubMed SCIE
期刊论文 | 2019 , 111 , 60-67 | Biomedecine & pharmacotherapie
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Calanthe fimbriata is a Tujia ethnic medicine with various medicinal value and it is traditionally used for the treatment of gastric ulcer, chronic hepatitis, pharyngitis, and so on.The current study was conducted to evaluate the antidiabetic activity of C. fimbriata methanol extract (CfME) in oral glucose tolerance test (OGTT) mice and in streptozotocin (STZ)-induced diabetic mice.Experimental diabetes was induced by intraperitoneal injection of STZ (60 mg/kg) for three consecutive days in mice. OGTT in mice and α-glucosidase inhibition assay were also adopted to investigate the activity and elucidate the mechanism of action. Gliclazide and metformin were used as standard drugs in OGTT mice and in STZ-induced diabetic mice experiments, respectively. Blood glucose, total cholesterol (TC), triglyceride (TG), alanine aminotransferase (ALT), aspartate aminotransferase (AST), and hepatic glycogen were measured in plasma or in livers.CfME exerted potently antihyperglycemic activity in OGTT mice and in STZ-induced diabetic mice and decreased ALT, AST and TG levels, improved hepatomegaly, and increased hepatic glycogen content, however, CfME failed to modify the normal blood glucose in normoglycemic mice and exhibited weakly inhibitory activity on intestinal α-glucosidase.The present study demonstrated that CfME exerted potently antidiabetic activity by restoring the liver function to increase the synthesis of hepatic glycogen and by improving insulin resistance of peripheral tissues to enhance the uptake and utilization of glucose.

Keyword :

STZ-induced diabetic mice Diabetes Mechanism of action Hepatoprotection Calanthe fimbriata

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GB/T 7714 Peng Yajie , Gao Yang , Zhang Xiaoqing et al. Antidiabetic and hepatoprotective activity of the roots of Calanthe fimbriata Franch. [J]. | Biomedecine & pharmacotherapie , 2019 , 111 : 60-67 .
MLA Peng Yajie et al. "Antidiabetic and hepatoprotective activity of the roots of Calanthe fimbriata Franch." . | Biomedecine & pharmacotherapie 111 (2019) : 60-67 .
APA Peng Yajie , Gao Yang , Zhang Xiaoqing , Zhang Changlong , Wang Xinrui , Zhang Haimin et al. Antidiabetic and hepatoprotective activity of the roots of Calanthe fimbriata Franch. . | Biomedecine & pharmacotherapie , 2019 , 111 , 60-67 .
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Synthesis of budesonide conjugates and their anti-inflammatory effects: a preliminary study SCIE
期刊论文 | 2019 , 13 , 681-694 | DRUG DESIGN DEVELOPMENT AND THERAPY
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Purpose: Budesonide (Bud) is a nonhalogenated glucocorticoid with high anti-inflammatory potency and low systemic side effects. However, the poor water solubility of Bud affects its dissolution and release behavior, thus influencing its anti-inflammatory effect. This study was aimed at synthesizing and evaluating novel conjugates of Bud, hoping to increase the anti-inflammatory activity of Bud by improving its water solubility. Materials and methods: Seven novel Bud conjugates (3a-3g) were designed and synthesized in this study. Besides, the equilibrium solubility, cell viability, in vitro and in vivo anti-inflammatory activity, and the hydrolysis behavior of the conjugates in different pH solutions, rat and human plasma, and rat lung homogenate were studied in detail. Results: As compared to Bud, the equilibrium solubility of 3a, 3c, and 3e was significantly increased; 3a, 3b, and 3c significantly inhibited the interleukin-6 production in lipopolysaccharide-induced A549 cells; 3a and 3e could significantly decrease the xylene-induced ear edema; and 3a and 3c were gradually and slowly hydrolyzed into Bud in the alveolar fluid and lung homogenate and broken down quickly in plasma. Conclusion: The amino acid ester compounds budesonide-21-glycine ester (3a) and budesonide-21-alanine ester (3c) were selected as potential conjugates of Bud. This study would provide a theoretical and an experimental basis for the in vivo process of glucocorticoids and the treatment of inflammatory diseases.

Keyword :

budesonide anti-inflammatory effect equilibrium solubility glucocorticoid hydrolysis behavior

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GB/T 7714 Yan, Yan , Wang, Pengchong , Li, Ruiying et al. Synthesis of budesonide conjugates and their anti-inflammatory effects: a preliminary study [J]. | DRUG DESIGN DEVELOPMENT AND THERAPY , 2019 , 13 : 681-694 .
MLA Yan, Yan et al. "Synthesis of budesonide conjugates and their anti-inflammatory effects: a preliminary study" . | DRUG DESIGN DEVELOPMENT AND THERAPY 13 (2019) : 681-694 .
APA Yan, Yan , Wang, Pengchong , Li, Ruiying , Sun, Ying , Zhang, Rui , Huo, Chuanchuan et al. Synthesis of budesonide conjugates and their anti-inflammatory effects: a preliminary study . | DRUG DESIGN DEVELOPMENT AND THERAPY , 2019 , 13 , 681-694 .
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