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Biogenic Nanoparticles Based Drugs Derived from Medicinal Plants
Published in Richard L. K. Glover, Daniel Nyanganyura, Rofhiwa Bridget Mulaudzi, Maluta Steven Mufamadi, Green Synthesis in Nanomedicine and Human Health, 2021
Charles Oluwaseun Adetunji, Olugbenga Samuel Michael, Wilson Nwankwo, Osikemekha Anthony Anani, Juliana Bunmi Adetunji, Akinola Samson Olayinka, Muhammad Akram
Another scenario is where a drug discovery program is launched to develop new eco-friendly, safe, potent and highly efficacious drug intended to overcome the weaknesses of the available chemotherapeutic agents such a program cannot register any reasonable progress without deployment of large datasets for analysis, modelling and testing/simulation of necessary drug characteristics and component biochemical reactions. Specialized AI systems would be able to streamline and operate on these datasets. Targets would be identified including the candidate molecules. These systems would also help predict synthesis routes, cellular interaction and half-life of the prototype drug.
The pharmacology of pain control
Published in Nan Stalker, Pain Control, 2018
The prototype drug within this group is aspirin and all the chemical components which share the above pharmacological properties, irrespective of their chemical structure, were once referred to as aspirin-like drugs. These drugs are now more commonly known as non-steroidal anti-inflammatory drugs (NSAIDs). Examples of these drugs are aspirin, indomethacin, diflunisal, sulindac, diclofenac, ibuprofen and naproxen.
Molecular Properties of Radiotracer Receptors
Published in Lelio G. Colombetti, Principles of Radiopharmacology, 1979
Another way to obtain information regarding receptors is by indirect means or by the study of structure-activity relationships (SAR). A prototype drug that elicits a known biological effect is chosen. Substitution groups are added or subtracted at various positions on the molecule. This class of modified radiotracers are known as a congeneric series. By testing these radiotracers and relating their biological activity or potency to their molecular configuration, information about the radiotracer-receptor combination may be gained. In addition, information about the receptor may also be obtained.
Single and multiple dose pharmacokinetics and safety of ZSP1273, an RNA polymerase PB2 protein inhibitor of the influenza A virus: a phase 1 double-blind study in healthy subjects
Published in Expert Opinion on Investigational Drugs, 2021
Yue Hu, Haijun Li, Min Wu, Hong Zhang, Yanhua Ding, Yun Peng, Xiaojiao Li, Zhenxiang Yu
To explore the drug metabolism and excretion, we analyzed the plasma, bile, urine, and stool samples of the rats following the administration of ZSP1273. Besides prototype drug, a total of eight metabolites were identified. According to the preclinical experiments, single dose oral administration of ZSP1273 to Sprague–Dawley (SD) rats produced metabolites M456a/b, M616a/b/c/d, and M632a/b, among which M616a was the main metabolite. After oral administration of ZSP1273 in dogs, two metabolites (M11 and M18) were detected in the plasma with less than 1% contents. Overall, the SD rat and dog models demonstrated that the main metabolic pathways of ZSP1273 are mono-oxidation combined with glucuronic acid. Following the oral administration of ZSP1273, the rats and dogs excreted metabolites mainly through feces along with some excretion through urine. In this study, the main metabolic pathways of the drug in healthy subjects included gluconylation, mono-oxidation, mono-oxidation and gluconylation, whereas the content of metabolites in the plasma was less than 10%. The ZSP1273 was mainly excreted through feces by prototype drugs. The excretion from urine by glucuronic conjugate was very little, with a mean cumulative excretion rate of 0.0435%. Accordingly, the metabolism and excretion characteristics of ZSP1273 in healthy volunteers are basically consistent with the preclinical data.
Pharmacokinetics, tissue distribution and excretion of a novel long-acting human insulin analogue – recombinant insulin LysArg in rats
Published in Xenobiotica, 2021
Tao Cui, Yazhuo Li, Zihong Wei, Xingyan Zhang, Wei Li, Wei Zhou, Jiangjie Lu, Jing Li, Xiulin Yi, Yong Zeng, Changxiao Liu, Fengying Yan
Radioassay was a highly sensitive method for the determination of macromolecules such as proteins and peptides. Because compounds into the body would be degraded, the total radioactivity could not represent the prototype drug. How to measure the prototype drug was the crucial problem to be solved in the measurement method. It was generally believed that the method of re-measuring radioisotope using TCA precipitation approach could partially exclude the decomposition products and free-125I, and the results were close to the concentration of the prototype drug in reality. In the activity verification experiment of 125I-insulin LysArg, radiochemical purit was determined as 97.82%, and maximum binding rate with insulin antibody was determined as 74.83%. Therefore, the trends of its pharmacokinetic behaviors by RA and TCA-RA methods are roughly the same and half-life was similar. In addition to the conventional RA and TCA-RA methods, a set of HPLC-RA experiment was performed. At the identical dose (2 U/kg), the results from HPLC-RA method were very close to these results from TCA-RA method, indicating that insulin LysArg was stable in plasma and less degraded.
Comprehensive metabolism study of swertiamarin in rats using ultra high-performance liquid chromatography coupled with Quadrupole-Exactive Orbitrap mass spectrometry
Published in Xenobiotica, 2021
Beibei Ma, Tianyu Lou, Tingting Wang, Ruiji Li, Jinhui Liu, Shangyue Yu, Yudong Guo, Zhibin Wang, Jing Wang
So far, there have been a number of research reports on data sets processing technology. These methods primarily include mass defect filter (MDF), isotope pattern filtering (IPF), extracted ion chromatogram (EIC), diagnostic product ion (DPI), and neutral loss filtering (NLF) (Gao et al.2020, Gavard et al.2020, Stavrianidi 2020, Wang et al.2020c). They had played an irreplaceable role in the past analytical research, but their common limitation was that they only focussed on a series of metabolic processes directly related to the prototype drug, which led to the omission of a large number of biotransformation reactions of intermediate metabolites. For example, in the current studies on the metabolism of swertiamarin, only a few common metabolites have been found, such as erythrocentaurin (ECR), gentianine, gentiandiol, aglycone, and its isomerisation products (Wang et al.2012, 2014, Shi et al.2020).