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Xinxing Tang

Bio: Xinxing Tang is an academic researcher. The author has contributed to research in topics: Dispersity & Solubility. The author has an hindex of 3, co-authored 4 publications receiving 68 citations.

Papers
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Journal ArticleDOI
TL;DR: S GLT2 inhibitors deuterated at sites susceptible to oxidative metabolism were found to have a slightly longer tmax and half-life, dose-dependent increase in urinary glucose excretion in rats, and slightly superior effects on UGE in dogs while retaining similar in vitro inhibitory activities against hSGLT2.
Abstract: SGLT2 inhibitors deuterated at sites susceptible to oxidative metabolism were found to have a slightly longer tmax and half-life (t1/2), dose-dependent increase in urinary glucose excretion (UGE) in rats, and slightly superior effects on UGE in dogs while retaining similar in vitro inhibitory activities against hSGLT2. In particular, deuterated compound 41 has the potential to be a robust long-acting antidiabetic agent.

56 citations

Patent
15 Jul 2009
TL;DR: In this article, compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT are provided. But they do not provide any methods of using these compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by sGLT inhibition.
Abstract: Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by SGLT inhibition.

14 citations

Patent
11 Oct 2014
TL;DR: Methods for preparing intermediates of SGLT2 inhibitors are provided in this paper, including crystalline forms and methods of crystallizing intermediates, and they are shown to work well in the presence of high temperature.
Abstract: Methods for preparing intermediates of SGLT2 inhibitors are provided, including crystalline forms and methods of crystallizing intermediates.

3 citations

Journal ArticleDOI
01 Dec 2022
TL;DR: In this paper , the optimal SDF was selected by comparing encapsulation efficiency, hydrodynamic diameter, polydispersity index and ζ-potential of the aggregates formed through interacting with Curcumin (Cur).
Abstract: There are interactions between dietary fiber and polyphenols in food, affecting the bioavailability of polyphenols. Soluble dietary fibers (SDF) were extracted from dietary fibers and characterized. The optimal SDF was selected by comparing encapsulation efficiency, hydrodynamic diameter, polydispersity index and ζ-potential of the aggregates formed through interacting with Curcumin (Cur). Finally, the optimized SDF was polymerized with Cur and curcuminoids respectively, and the differences of two aggregates were compared. Among five kinds of dietary fibers, a 60% ethanol-precipitated fenugreek SDF (FS60) belonging to a type of glucan was the best SDF tested for forming Cur-SDF aggregates. However, a better aggregation of FS60 on curcuminoids than Cur was observed. Furthermore, FS60 encapsulated Cur to form spherical nano-aggregates by hydrogen bonding and electrostatic force with ketone and phenolic hydroxyl groups of Cur. Due to the lack of one methoxy, demethoxycurcumin (DMC) had stronger spatial interaction with FS60. Curcuminoids-FS60 aggregates were composed of DMC-FS60 and Cur-FS60 nanoparticles. A small amount of DMC promoted the aggregation of Cur and FS60. The presence of Cur and DMC mutually promoted the hydrogen bond, making the system more stable. The curcuminoids-FS60 aggregates provide an opportunity to improve the solubility and bioavailability of Cur.

1 citations

Journal ArticleDOI
TL;DR: Specific molecular subtypes based on DNA methylation status are explored and subtype-specific characteristics using patient samples from the TCGA database are identified using an information entropy-based algorithm to represent the unique molecular characteristics of the subtype.
Abstract: Bladder cancer is a highly complex and heterogeneous malignancy. Tumor heterogeneity is a barrier to effective diagnosis and treatment of bladder cancer. Human carcinogenesis is closely related to abnormal gene expression, and DNA methylation is an important regulatory factor of gene expression. Therefore, it is of great significance for bladder cancer research to characterize tumor heterogeneity by integrating genetic and epigenetic characteristics. This study explored specific molecular subtypes based on DNA methylation status and identified subtype-specific characteristics using patient samples from the TCGA database with DNA methylation and gene expression were measured simultaneously. The results were validated using an independent cohort from GEO database. Four DNA methylation molecular subtypes of bladder cancer were obtained with different prognostic states. In addition, subtype-specific DNA methylation markers were identified using an information entropy-based algorithm to represent the unique molecular characteristics of the subtype and verified in the test set. The results of this study can provide an important reference for clinicians to make treatment decisions.

1 citations


Cited by
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Journal ArticleDOI
TL;DR: Advances in the application of hydrogen isotopes in the life sciences are described and 3 H, in particular, has seen an increase in utilization, especially in pharmaceutical drug discovery.
Abstract: Hydrogen isotopes are unique tools for identifying and understanding biological and chemical processes. Hydrogen isotope labelling allows for the traceless and direct incorporation of an additional mass or radioactive tag into an organic molecule with almost no changes in its chemical structure, physical properties, or biological activity. Using deuterium-labelled isotopologues to study the unique mass-spectrometric patterns generated from mixtures of biologically relevant molecules drastically simplifies analysis. Such methods are now providing unprecedented levels of insight in a wide and continuously growing range of applications in the life sciences and beyond. Tritium (3 H), in particular, has seen an increase in utilization, especially in pharmaceutical drug discovery. The efforts and costs associated with the synthesis of labelled compounds are more than compensated for by the enhanced molecular sensitivity during analysis and the high reliability of the data obtained. In this Review, advances in the application of hydrogen isotopes in the life sciences are described.

394 citations

Journal ArticleDOI
TL;DR: This Perspective provides an overview of the recent developments of deuteration, with a focus on deuterated clinical candidates, and highlights both opportunities and challenges of this strategy.
Abstract: The use of deuteration in medicinal chemistry has exploded in the past years, and the FDA has recently approved the first deuterium-labeled drug. Precision deuteration goes beyond the pure and simple amelioration of the pharmacokinetic parameters of a drug and might provide an opportunity when facing problems in terms of metabolism-mediated toxicity, drug interactions, and low bioactivation. The use of deuterium is even broader, offering the opportunity to lower the degree of epimerization, reduce the dose of coadministered boosters, and discover compounds where deuterium is the basis for the mechanism of action. Nevertheless, designing, synthesizing, and developing a successful deuterated drug is far from straightforward, and the translation from concept to practice is often unpredictable. This Perspective provides an overview of the recent developments of deuteration, with a focus on deuterated clinical candidates, and highlights both opportunities and challenges of this strategy.

341 citations

Journal ArticleDOI
TL;DR: This review offers a medium on which future drug design and development toward diabetes management may be modelled (i.e. optimization via structural derivatization), as many of the drug candidates highlighted show promise as an effective anti-diabetic chemotherapy.

200 citations

Journal ArticleDOI
TL;DR: This Review summarizes close to 500 primary publications and surveys published since 2000 about the syntheses and diverse bioactivities of C-glycopyranosyl (het)arenes displaying among others antioxidant, antiviral, antibiotic, antiadhesive, cytotoxic, and glycoenzyme inhibitory effects.
Abstract: This Review summarizes close to 500 primary publications and surveys published since 2000 about the syntheses and diverse bioactivities of C-glycopyranosyl (het)arenes. A classification of the preparative routes to these synthetic targets according to methodologies and compound categories is provided. Several of these compounds, regardless of their natural or synthetic origin, display antidiabetic properties due to enzyme inhibition (glycogen phosphorylase, protein tyrosine phosphatase 1B) or by inhibiting renal sodium-dependent glucose cotransporter 2 (SGLT2). The latter class of synthetic inhibitors, very recently approved as antihyperglycemic drugs, opens new perspectives in the pharmacological treatment of type 2 diabetes. Various compounds with the C-glycopyranosyl (het)arene motif were subjected to biological studies displaying among others antioxidant, antiviral, antibiotic, antiadhesive, cytotoxic, and glycoenzyme inhibitory effects.

151 citations

Journal ArticleDOI
TL;DR: This review summarises recent approaches and advancement in anti-diabetes treatment concerning characteristics, structure-activity relationships, functional mechanisms, expression regulation, and applications in medicine.

91 citations