Open Access Articles – A Sensitive Chromatographic Method for Hyaluronate Quantification Applied to Analyze the Desorption Behavior on Contact Lenses

Journal Name: Current Pharmaceutical Analysis

Author(s): Wan-Hsin ChangPei-Yi LiuYuan-Ting Jiang*Yuan-Hao Howard Hsu*.

Abstract:

Background: Sodium hyaluronate (NaHA) is generally supplemented in products related to contact lenses for increasing comfort during wearing. The quantity of sodium hyaluronate and the material of lenses affect the retention of sodium hyaluronate on the contact lenses.

Methods: We developed a convenient and sensitive but unconventional chromatographic method to quantify sodium hyaluronate and analyze its release behavior from contact lenses. The reverse-phase chromatography eluted sodium hyaluronate with high molecular masses in the shortest time and could separate salt and small compounds from sodium hyaluronate.

Results: This method could accurately quantify sodium hyaluronate with diverse molecular sizes. Because sodium hyaluronate was eluted in a narrow time frame, sensitivity was significantly enhanced, and the limit of detection of this method was 0.45 μg/mL. According to this quantitation method, the attached quantity of sodium hyaluronate is related to the water content of the material. Furthermore, a material test indicated that the release efficiency of sodium hyaluronate depends on the material of lenses. Nonionic Polymacon had a longer half-life in the sodium hyaluronate release curve than negative Methafilcon A and silicone hydrogel.

Conclusion: This hyaluronate quantification method is a fast, sensitive and accurate method, making it suitable for the in vitro hyaluronate research without further derivatization. To read out more, please visit: http://www.eurekaselect.com/170419/article

Open Access Articles | 3D Cascaded Convolutional Networks for Multi-vertebrae Segmentation

 

Journal Name: Current Medical Imaging
Formerly: Current Medical Imaging Reviews

 

Author(s): Liu Xia, Liu Xiao, Gan Quan, Wang Bo*.

 

 

 

Graphical Abstract:

 

image_2020_04_08T07_24_19_625Z

 

Abstract:

Background: Automatic approach to vertebrae segmentation from computed tomography (CT) images is very important in clinical applications. As the intricate appearance and variable architecture of vertebrae across the population, cognate constructions in close vicinity, pathology, and the interconnection between vertebrae and ribs, it is a challenge to propose a 3D automatic vertebrae CT image segmentation method.

Objective: The purpose of this study was to propose an automatic multi-vertebrae segmentation method for spinal CT images.

Methods: Firstly, CLAHE-Threshold-Expansion was preprocessed to improve image quality and reduce input voxel points. Then, 3D coarse segmentation fully convolutional network and cascaded finely segmentation convolutional neural network were used to complete multi-vertebrae segmentation and classification.

Results: The results of this paper were compared with the other methods on the same datasets. Experimental results demonstrated that the Dice similarity coefficient (DSC) in this paper is 94.84%, higher than the V-net and 3D U-net.

Conclusion: Method of this paper has certain advantages in automatically and accurately segmenting vertebrae regions of CT images. Due to the easy acquisition of spine CT images. It was proven to be more conducive to clinical application of treatment that uses our segmentation model to obtain vertebrae regions, combining with the subsequent 3D reconstruction and printing work. To read out more, please visit: http://www.eurekaselect.com/168045/article

Open Access Articles | Antitumor Activity of Cyclodextrin-based Supramolecular Platinum Prodrug In vitro and In vivo

Journal Name: Letters in Drug Design & Discovery

Author(s): Yu-Hui Zhang, Jie Wang, Siqintana Xin, Li-Juan Wang, Xianliang Sheng*.

 

 

 

 

Graphical Abstract:

 

Abstract:

Background: Considering the limitations of cisplatin in clinical application, there is ongoing research to fabricate new platinum-containing prodrug which are highly effective to tumor cells and have low toxicity to normal cells.

Methods: In this study, a cyclodextrin-based supramolecular platinum prodrug that is 6,6’-ophenylenediseleno- bridged bis (β-cyclodextrin)s (CD) and its potassium tetrachloroplatinate(II) complex was reported. The cytotoxicity experiments were performed to evaluate the anticancer activities of supramolecular prodrug in vitro by means of MTT assay. The practical application of supramolecular prodrug in tumor treatment in vivo were evaluated using BALB/c nude mice model bearing Hela cancer cells.

Results: Compared with commercial anticancer drug cisplatin, the resultant cyclodextrin-based platinum prodrug exhibited comparative anticancer effect but with much lower toxicity side effects in vitro and in vivo.

Conclusion: The cyclodextrin-based supramolecular platinum prodrug displayed antitumor activity comparable to the commercial antitumor drug cisplatin but with lower side effects both in vitro and in vivo, implying that the two adjacent cyclodextrin cavities not merely act as desired solubilizer, but also endowed the prodrug with cell permeability through the interaction of cyclodextrin with phospholipids and cholesterol on cell membrane. To read out more, please visit: http://www.eurekaselect.com/172707/article

Open Access Articles | Tissue Distribution of Active Principles from Alpiniae Oxyphyllae Fructus Extract: An Experimental Study in Rats

 

Journal Name: Current Pharmaceutical Analysis

            Author(s): Qi Wen, Hai-Long Li, Shi-Ying Mai, Yin-Feng Tan*, Feng Chen*.

 

Graphical Abstract:

 

Abstract:

Background: Alpiniae Oxyphyllae Fructus (Yizhi in Chinese) have been widely used as an herbal medicine for the treatment of diuresis, enuresis and diarrhea in China. Many studies have deciphered some potential underlying mechanisms for its anti-diarrheal effects. However, tissue distribution of Yizhi constituents is warranted because pharmacological receptors are frequently located in tissues. Moreover, it is also interesting to know about the potential correlation between behavior in drug distribution and the observed pharmacological response. The aim of this study is to investigate tissue distribution behaviors of Yizhi constituents after oral administration of Yizhi extract to rats, focusing on 10 active principles.

Methods: Twenty four male Sprague Dawley rats were given orally the Yizhi extract and fourteen tissue samples were collected after being killed by bleeding from the abdominal aorta under ether anesthesia at different time-points. The resulting tissues were excised and homogenized. Based on our previous reports, liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) was used to quantify the target analytes, as well as phase II metabolites, in the various biosamples.

Results: Almost all the targeted Yizhi active principles and some glucuronidated metabolites were qualitatively measured in rat stomach, small intestine, large intestine, as well as liver. Nootkatone, yakuchinone A and tectochrysin were observed in the rat brain. In other rat tissues, these analytes had lower exposure or could not be detected. Consistently, quantitative analysis revealed that the Yizhi active principles dominantly distributed into gastrointestinal tissues followed by liver, the overall exposure levels ranking as follows: stomach > small intestine > large intestine > liver. Tissue concentrationtime profiles of the test active principles in rat stomach, small intestine, and large intestine were bimodal with two concentration peaks occurring at 0.5 and 4h after oral administration, respectively. The exposure levels in rat kidney and bladder were quite low.

Conclusion: The active principles of Yizhi were specially distributed into gastrointestinal tissues after oral administration of its ethanol extract to rats. The tissue distribution behaviors partly supported its anti-diarrheal effects from a pharmacokinetic opinion. This paper will be useful as the starting point for studying the pharmacological activities of this traditional herb. To read out more, please visit: http://www.eurekaselect.com/165218/article

Open Access Articles | An Integrated Computational Approach for Plant-Based Protein Tyrosine Phosphatase Non-Receptor Type 1 Inhibitors

 

Journal Name: Current Computer-Aided Drug Design

Author(s): Shabana Bibi, Katsumi Sakata*.

 

 

Graphical Abstract:

 

Abstract:

Background: Protein tyrosine phosphatase non-receptor type 1 is a therapeutic target for the type 2 diabetes mellitus. According to the International Diabetes Federation 2015 report, one out of 11 adults suffers from diabetes mellitus globally.

Objective: Current anti-diabetic drugs can cause life-threatening side-effects. The present study proposes a pipeline for the development of effective and plant-derived anti-diabetic drugs that may be safer and better tolerated.

Methods: Plant-derived protein tyrosine phosphatase non-receptor type 1 inhibitors possessing antidiabetic activity less than 10µM were used as a training set. A common feature pharmacophore model was generated. Pharmacophore-based screening of plant-derived compounds of the ZINC database was conducted using ZINCpharmer. Screened hits were assessed to evaluate their drug-likeness, pharmacokinetics, detailed binding behavior, and aggregator possibility based on their physiochemical properties and chemical similarity with reported aggregators.

Results: Through virtual screening and in silico pharmacology protocol isosilybin (ZINC30731533) was identified as a lead compound with optimal properties. This compound can be recommended for laboratory tests and further analyses to confirm its activity as protein tyrosine phosphatase nonreceptor type 1 inhibitor.

Conclusion: The present study has identified plant-derived anti-diabetic virtual lead compound with the potential to inhibit protein tyrosine phosphatase non-receptor type 1, which may be helpful to enhance insulin production. This computer-aided study could facilitate the development of novel pharmacological inhibitors for diabetes treatment. To read out more, please visit: http://www.eurekaselect.com/151386/article

Open Access Articles | Sexual Roles, Risk Sexual Behaviours, and HIV Prevalence among Men who Have Sex with Men Seeking HIV Testing in Changsha, China

Journal Name: Current HIV Research

Author(s): Yunxiao Lei, Kaili Zhang, Xueling Xiao, Chulei Tang, Xianhong Li, Honghong Wang*.

Graphical Abstract:

Abstract:

Background: HIV infection is prevalent among men who have sex with men (MSM), and sexual roles may be important factors related to it. This study aims to describe the sexual roles, risky sexual behaviors and HIV prevalence among MSM, and to determine associated factors for HIV prevalence.

Methods: A convenient sampling method was used to recruit participants in a non-government organization in Changsha, China. The participants were asked to complete a 38-item self-administered questionnaire regarding demographic characteristics and risky sexual behaviours before collecting blood samples for HIV testing. Chi-square tests and logistic regression analysis were conducted with the Statistical Package for the Social Sciences Version 18.0 and other indexes were statistically described.

Results: A total of 601 MSMs who came to a local non-government organization for voluntary counseling and testing completed a pencil-and-paper survey and were tested for HIV. The overall HIV prevalence of this sample was 13.3%, and that of the bottoms (16.3%) was similar to the versatiles (15.9%) but higher than the tops (6.1%). Bivariate analyses showed that there were significant differences in age, marital status, monthly income, sexual orientation, age at first sex, sex of the first sex partner, sex with a woman in the last 6 months, oral sex with a man in the last 6 months and role of oral sex among 3 subgroups of MSM (p < 0.05). Multivariate analyses indicated that MSMs who played the role of either the bottoms or the versatiles were more likely to be HIV positive than the tops. While MSMs who used condoms in anal sex in the last 6 months, had sex with a woman in the last 6 months or had oral sex with a man in the last 6 months were less likely to be HIV positive.

Conclusion: Different sexual roles are associated with high-risk sexual behaviors among MSMs and their HIV infection status. Further research should target preventive interventions, and improve the effectiveness of the intervention according to the characteristics of the subgroups to reduce the HIV transmission among Chinese MSM.

 

Read out more at: http://www.eurekaselect.com/163672

Bentham Open Access Article:

8-21-2014 9-46-29 AM

The Article, “Metastasis-Initiating Cells in Renal Cancer” of the journal: Current Signal Transduction Therapy, is now open for all to view and access.

For more details, visit: http://www.eurekaselect.com/120236/article

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