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Your search keyword '"Xie, Xiao-Yang"' showing total 2 results
Start Over Author "Xie, Xiao-Yang" Topic drug discovery
2 results on '"Xie, Xiao-Yang"'

1. Isolation, synthesis, and cytotoxicity evaluation of two impurities in nomegestrol acetate.

Author

Xie BC, Song SY, Xie XY, Sun YT, Zhang XY, Xu DH, and Huang YS

Subjects
Antineoplastic Agents, Hormonal chemistry, Antineoplastic Agents, Hormonal pharmacology, Cell Line, Tumor, Cell Survival drug effects, Drug Contamination, Humans, Megestrol chemistry, Megestrol pharmacology, Molecular Structure, Norpregnadienes chemistry, Norpregnadienes pharmacology, Progesterone Congeners chemistry, Progesterone Congeners pharmacology, Antineoplastic Agents, Hormonal chemical synthesis, Drug Discovery methods, Megestrol chemical synthesis, Norpregnadienes chemical synthesis, Progesterone Congeners chemical synthesis
Abstract

Nomegestrol acetate (NOMAc) is a synthetic progesterone analog and classified as a fourth-generation progestin. It has been approved in many countries for oral contraception, hormonal replacement therapy (HRT), and treatment of various gynecological disorders. There are several synthetic routes reported for the synthesis of NOMAc and they all share the very similar last three to five steps toward the conversion of 6-methylene to 6-methyl-6,7-unsaturated structure. Therefore the final product from different processing routes may have similar impurity profiles. In the analysis of NOMAc, we identified two impurities, impurity A (listed in EP 8.0) and impurity B (not specified in EP 8.0). Both impurities were further confirmed by synthesis. In addition, both impurities and NOMAc were evaluated for their in vitro cytotoxicities against L02 liver cells, mesenchymal stem cells, MCF-7 breast cancer cells, and C33A cervical cancer cells. These three analogs are not cytotoxic to the four cell lines at low concentrations (<20 μM). NOMAc and impurity A showed cytotoxicity to L02, MCF-7, and C33A cells at high concentrations, while impurity B did not show significant cytotoxicity to any of the cell lines tested., (© 2019 Deutsche Pharmazeutische Gesellschaft.)

Published
2019
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2. Sigma-2 Receptor as a Potential Drug Target

Author

Ma Wen-Hui, Xie Xiao-Yang, Huang Yun-Sheng, and Chen Ai-Fang

Subjects
Sigma-2 receptor, medicine.disease_cause, 01 natural sciences, Biochemistry, Neuroprotection, 03 medical and health sciences, Alzheimer Disease, Drug Discovery, medicine, Humans, Receptors, sigma, 0101 mathematics, Receptor, Protein kinase C, PI3K/AKT/mTOR pathway, 030304 developmental biology, Pharmacology, 0303 health sciences, Amyloid beta-Peptides, Chemistry, Organic Chemistry, Autophagy, Brain, 010101 applied mathematics, Pharmaceutical Preparations, Cancer research, Molecular Medicine, Signal transduction, Oxidative stress
Abstract

Sigma-2 receptor plays key roles in promoting tumor cell apoptosis, enhancing efficacy of anti-tumor drugs, blocking signal transduction controlled by Aβ oligomers, regulating Ca2+ homeostasis and protecting nerve cells. Studies indicated that sigma-2 receptor may be closely coupled with ROS, LDL, mTOR, RAS, PLC/PKC, lysosomal autophagy and mitochondrial super oxidative stress. In addition, the high expression of this receptor in proliferating cells and nerve cells indicates that sigma-2 receptor is an ideal molecular target for imaging and therapeutic development for cancer, Alzheimer's disease, schizophrenia and traumatic brain injury. Various sigma-2 agonists have shown promising anticancer activities, while sigma-2 antagonists have displayed neuroprotection and inhibition of Aβ oligomers in the brain of Alzheimer's disease patients. Thus, both sigma-2 agonists and antagonists are potentially useful therapeutics for the management of cancer and neurodegenerative disorders.

Published
2021
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