2020 Vol. 10, No. 6

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Review paper
Challenges for cysteamine stabilization, quantification, and biological effects improvement
Carla Atallah, Catherine Charcosset, Hélène Greige-Gerges
2020, 10(6): 499-516. doi: 10.1016/j.jpha.2020.03.007
Abstract:
The aminothiol cysteamine, derived from coenzyme A degradation in mammalian cells, presents several biological applications. However, the bitter taste and sickening odor, chemical instability, hygroscopicity, and poor pharmacokinetic profile of cysteamine limit its efficacy. The use of encapsulation...
The current status of anti-GPCR drugs against different cancers
Sana Usman, Maria Khawer, Shazia Rafique, Zara Naz, Komal Saleem
2020, 10(6): 517-521. doi: 10.1016/j.jpha.2020.01.001
Abstract:
G protein coupled receptors (GPCRs) have emerged as the most potential target for a number of drug discovery programs ranging from control of blood pressure, diabetes, cure for genetic diseases to treatment of cancer. A panel of different ligands including hormones, peptides, ions and small molecule...
Three-dimensional aspects of formulation excipients in drug discovery: a critical assessment on orphan excipients, matrix effects and drug interactions
Vijayabhaskar Veeravalli, Hanumanth Srikanth Cheruvu, Pratima Srivastava, Lakshmi Mohan Vamsi Madgula
2020, 10(6): 522-531. doi: 10.1016/j.jpha.2020.02.007
Abstract:
Formulation/pharmaceutical excipients play a major role in formulating drug candidates, with the objectives of ease of administration, targeted delivery and complete availability. Many excipients used in pharmaceutical formulations are orphanized in preclinical drug discovery. These orphan excipient...
Original article
Use of subcutaneous tocilizumab to prepare intravenous solutions for COVID-19 emergency shortage: Comparative analytical study of physicochemical quality attributes
Natalia Navas, Jesús Hermosilla, Anabel Torrente-López, José Hernández-Jiménez, Jose Cabeza, Raquel Pérez-Robles, Antonio Salmerón-García
2020, 10(6): 532-545. doi: 10.1016/j.jpha.2020.06.003
Abstract:
COVID-19, a disease caused by the novel coronavirus SARS-CoV-2, has produced a serious emergency for global public health, placing enormous stress on national health systems in many countries. Several studies suggest that cytokine storms (interleukins) may play an important role in severe cases of C...
Discovery of human coronaviruses pan-papain-like protease inhibitors using computational approaches
Mubarak A. Alamri, Muhammad Tahir ul Qamar, Muhammad Usman Mirza, Safar M. Alqahtani, Matheus Froeyen, Ling-Ling Chen
2020, 10(6): 546-559. doi: 10.1016/j.jpha.2020.08.012
Abstract:
The papain-like protease (PLpro) is vital for the replication of coronaviruses (CoVs), as well as for escaping innate-immune responses of the host. Hence, it has emerged as an attractive antiviral drug-target. In this study, computational approaches were employed, mainly the structure-based virtual ...
Vancomycin pretreatment attenuates acetaminophen-induced liver injury through 2-hydroxybutyric acid
Ningning Zheng, Yu Gu, Ying Hong, Lili Sheng, Linlin Chen, Feng Zhang, Jie Hou, Weidong Zhang, Zean Zhang, Wei Jia, Houkai Li
2020, 10(6): 560-570. doi: 10.1016/j.jpha.2019.11.003
Abstract:
Liver injury caused by acetaminophen (AP) overdose is a leading public health problem. Although AP-induced liver injury is well recognized as the formation of N-acetyl-p-benzoquinone (NAPQI), a toxic metabolite of AP, resulting in cell damage, emerging evidence indicates that AP-induced liver injury...
Isoflavones' effects on pharmacokinetic profiles of main iridoids from Gardeniae Fructus in rats
Ruirui Chang, Jialin Liu, Yusha Luo, Taohong Huang, Qiang Li, Jun Wen, Weidong Chen, Tingting Zhou
2020, 10(6): 571-580. doi: 10.1016/j.jpha.2019.11.004
Abstract:
Gardeniae Fructus (GF) and Semen Sojae Praeparatum (SSP) are both medicine food homologies and widely used in Chinese clinical prescriptions together. The research investigated the pharmacokinetics of four iridoids in normal rats and isolfavones-fed rats, which were administered with isolfavones fro...
Metabonomic analysis of plasma biochemical changes in pyrexia rats after treatment with Gegenqinlian decoction, aspirin and itraconazole by UHPLC-FT-ICR-MS
Ting Liu, Ruiyun Li, Yue Cui, Zhiguo Yu, Yunli Zhao
2020, 10(6): 581-587. doi: 10.1016/j.jpha.2019.11.007
Abstract:
A metabonomic approach involving an ultrahigh-performance liquid chromatography combined with Fourier transform ion cyclotron resonance mass spectrometry (UHPLC-FT-ICR-MS) was used to investigate the changes in the endogenous metabolites in the plasma of rats with yeast-induced pyrexia treated with ...
Comparative analysis of constitutes and metabolites for traditional Chinese medicine using IDA and SWATH data acquisition modes on LC-Q-TOF MS
Dian Kang, Qingqing Ding, Yangfan Xu, Xiaoxi Yin, Huimin Guo, Tengjie Yu, He Wang, Wenshuo Xu, Guangji Wang, Yan Liang
2020, 10(6): 588-596. doi: 10.1016/j.jpha.2019.11.005
Abstract:
Identification of components and metabolites of traditional Chinese medicines (TCMs) employing liquid chromatography-quadrupole time-of-flight mass spectrometry (LC-Q-TOF MS) techniques with information-dependent acquisition (IDA) approaches is increasingly frequent. A current drawback of IDA-MS is ...
Offline two-dimensional liquid chromatography coupled with ion mobility-quadrupole time-of-flight mass spectrometry enabling four-dimensional separation and characterization of the multicomponents from white ginseng and red ginseng
Tiantian Zuo, Chunxia Zhang, Weiwei Li, Hongda Wang, Ying Hu, Wenzhi Yang, Li Jia, Xiaoyan Wang, Xiumei Gao, Dean Guo
2020, 10(6): 597-609. doi: 10.1016/j.jpha.2019.11.001
Abstract:
Inherent complexity of plant metabolites necessitates the use of multi-dimensional information to accomplish comprehensive profiling and confirmative identification. A dimension-enhanced strategy, by offline two-dimensional liquid chromatography/ion mobility-quadrupole time-of-flight mass spectromet...
Single-run reversed-phase HPLC method for determining sertraline content, enantiomeric purity, and related substances in drug substance and finished product
Alessia Rosetti, Rosella Ferretti, Leo Zanitti, Adriano Casulli, Claudio Villani, Roberto Cirilli
2020, 10(6): 610-616. doi: 10.1016/j.jpha.2020.11.002
Abstract:
A direct enantio-, diastereo-, and chemo-selective high-performance liquid chromatographic method was developed for determining the content, enantiomeric purity, and related substances of the chiral antidepressant drug sertraline HCl in a single chromatographic run. The separation was achieved on a ...
Original Article
Development of a UHPLC-MS/MS method for the quantification of ilaprazole enantiomers in rat plasma and its pharmacokinetic application
Fengting Ou, Ying Zhou, Jinxiu Lei, Su Zeng, Fuhai Wu, Ning Zhang, Lushan Yu
2020, 10(6): 617-623. doi: 10.1016/j.jpha.2019.09.002
Abstract:
In Korea and China, ilaprazole is a widely used proton pump inhibitor in the treatment of gastric ulcers. In this study, a specific and sensitive LC-MS/MS method has been developed and validated for the quantification of ilaprazole enantiomers in the rat plasma, using R-lansoprazole as the internal ...