Review
Biochemistry & Molecular Biology
Annagiulia Di Trana, Diletta Berardinelli, Eva Montanari, Paolo Berretta, Giuseppe Basile, Marilyn A. Huestis, Francesco Paolo Busardo
Summary: Adulteration is a common practice in drug production, where active ingredients are intentionally added to alter drug effects and increase profits. The types of adulterants used vary over time. Constant monitoring of adulterants is crucial to protect drug consumers' health.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Psychiatry
Michal Ordak, Aleksandra Zmyslowska, Milosz Bielski, Daniel Rybak, Maja Tomaszewska, Katarzyna Wyszomierska, Aleksandra Kmiec, Natalia Garlicka, Maria Zalewska, Michal Zalewski, Tadeusz Nasierowski, Elzbieta Muszynska, Magdalena Bujalska-Zadrozny
Summary: This study reviewed 51 case reports of NPS use between 2010 and 2019, showing that most cases involved synthetic cannabinoids and cathinones. The primary pharmacotherapy used was benzodiazepines, with some patients also receiving neuroleptics and muscle relaxants.
FRONTIERS IN PSYCHIATRY
(2021)
Review
Chemistry, Analytical
Felix Zapata, Jose Manuel Matey, Gemma Montalvo, Carmen Garcia-Ruiz
Summary: This work reviews fundamental concepts about drugs, focusing on new psychoactive substances (NPS) and their classifications. A revised classification based on chemical composition is proposed to merge recent chemical groupings of NPS from various institutions, aiming to be useful for forensic practitioners/researchers.
MICROCHEMICAL JOURNAL
(2021)
Review
Pharmacology & Pharmacy
Rita Roque-Bravo, Rafaela Sofia Silva, Rui F. Malheiro, Helena Carmo, Felix Carvalho, Diana Dias da Silva, Joao Pedro Silva
Summary: Synthetic cannabinoids, a chemically diverse group of new psychoactive substances that target the endocannabinoid system, have more intense effects than cannabis and are increasingly being used recreationally. However, the rise in intoxications and deaths associated with synthetic cannabinoids poses a major public health concern and challenge for policy makers.
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY
(2023)
Article
Chemistry, Analytical
Graeme Cochrane, Jennifer K. Field, Matthew C. Hulme, Nicolas Gilbert, Ryan E. Mewis, Melvin R. Euerby, Oliver B. Sutcliffe
Summary: In this study, Supercritical Fluid Chromatography (SFC-UV) was used to rapidly analyze 31 novel, regioisomeric diphenidine-derived psychoactive substances. The polarity of the stationary phases had a significant impact on the retention time and elution order of the compounds. SFC demonstrated good retention for hydrophilic compounds that were poorly retained on a C18 reverse phase column.
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2022)
Article
Neurosciences
Giovanni Martinotti, Stefania Schiavone, Attilio Negri, Chiara Vannini, Luigia Trabace, Domenico De Berardis, Mauro Pettorruso, Stefano L. Sensi, Massimo Di Giannantonio
Summary: The study found that after taking psychoactive drugs, there is a widespread prevalence of suicide ideation, with differences in suicide ideation intensity among different drug categories. High levels of suicidality do not specifically correlate with major symptoms of ongoing psychiatric background.
Article
Biochemistry & Molecular Biology
Idowu Kehinde, Pritika Ramharack, Manimbulu Nlooto, Michelle Gordon
Summary: This study used computational tools to analyze the inhibitory potential of four phytochemical compounds against drug-metabolizing proteins. The study found that epigallocatechin gallate and kaempferol-7-glucoside showed strong inhibitory activities and could potentially increase the concentration of drugs in patients.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Psychology, Clinical
Caroline Zangani, Edoardo Giuseppe Ostinelli, Barbara Giordano, Armando D'Agostino, Giovanni Martinotti, Massimo Clerici, Orsola Gambini, Fabrizio Schifano
Summary: This study in Italy identified that male gender, homosexual sexual orientation, use of emergency services due to alcohol, and previous contact with mental health services are risk factors for lifetime use of NPS. Improving preventive strategies and providing simplified access to information on NPS, especially for individuals at higher risk of misuse, could help slow down the spread of NPS and prevent substance use consequences.
INTERNATIONAL JOURNAL OF MENTAL HEALTH AND ADDICTION
(2021)
Article
Psychiatry
George Savulich, Owen Bowden-Jones, Robert Stephenson, Annette B. Bruhl, Karen D. Ersche, Trevor W. Robbins, Barbara J. Sahakian
Summary: Research on NPS/polydrug users shows that recreational NPS users exhibit higher levels of risk-taking behavior and emotion-laden cognition, while treatment-seekers show poorer learning and memory abilities. Those seeking treatment are more susceptible to influences related to impulsivity and emotional control.
FRONTIERS IN PSYCHIATRY
(2021)
Article
Chemistry, Analytical
Franks Kamgang Nzekoue, Marco Agostini, Michele Verboni, Caterina Renzoni, Lucia Alfieri, Simone Barocci, Massimo Ricciutelli, Giovanni Caprioli, Simone Lucarini
Summary: A rapid LC-MS/MS method was developed and validated for the targeted analysis of 98 NPS from hair matrix, showing good precision, linearity, selectivity, and sensitivity, as well as reduced matrix effect and acceptable recovery. The method is suitable for quantifying NPS in hair matrix and could be employed in routine analyses in analytical laboratories.
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2021)
Review
Medical Laboratory Technology
Lea Wagmann, Cathy M. Jacobs, Markus R. Meyer
Summary: This review discusses the methods for detecting new psychoactive substances (NPSs) using mass spectrometry and highlights the advantages and disadvantages of using common biological matrices for screening in a clinical toxicology setting. The results show that blood and urine are the most commonly used biological matrices, but other options are also available.
THERAPEUTIC DRUG MONITORING
(2022)
Article
Chemistry, Analytical
Jennifer K. Field, Christine Hinz, Christopher M. Titman, Matthew C. Hulme, Rhona M. Cowan, Jack B. Ainsworth-McMillan, Nicolas Gilbert, Robert J. Lee, Jack Marron, Andrew Costello, Ryan E. Mewis, Melvin R. Euerby, Oliver B. Sutcliffe
Summary: This study presents the development of a rapid gradient UHPLC method with targeted MS/MS for the detection and confirmation of the identity of 33 substituted diphenidine derivatives in solid drug samples. The study also investigates the influence of substituents on the elution order and the retention mechanism of diphenidines under reverse-phase UHPLC conditions. The developed method was proven to be specific through the assessment of common adulterants, and it was successfully applied to confirm the identity of psychoactive components in seized bulk samples.
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2022)
Article
Chemistry, Analytical
Jiajia Li, Yong Wang, Anran Liu, Songqin Liu
Summary: A highly sensitive, rapid and highly selective method for the detection of synthetic cannabinoids (SCs) in human serum was developed. Magnetic molecularly imprinted polymer (MIP) nanocomposites were prepared through self-polymerization of dopamine and template molecules. With these magnetic MIP nanoparticles, six SCs could be rapidly and effectively extracted from human blood and their concentrations accurately determined by HPLC-MS analysis. The proposed method is characterized by high sensitivity and selectivity, and has great potential for application in practical sample analysis.
Article
Medicine, Legal
Olivia A. Lin, Pei-Jiun Chuang, Y. Jane Tseng
Summary: This study conducted a systematic review on controlled drug regulations and analyzed the numbers of new psychoactive substances (NPS) reported in six East and Southeast Asian countries in comparison to US and UK from 2009 to 2020. The findings showed that the US and UK reported more NPS compared to Japan, China, Singapore, South Korea, Malaysia, and Taiwan. Legislative mechanisms including specific listing, generic control, analogue control, and temporary bans were evaluated. Countries that adopted a combination of legislative mechanisms were able to identify higher numbers of NPS for regulatory control.
REGULATORY TOXICOLOGY AND PHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Magnus A. B. Axelsson, Hanna Lovgren, Robert Kronstrand, Henrik Green, Moa Andresen Bergstrom
Summary: This study retrospectively identified a variety of new psychoactive substances, including some substances notified by the EU and Sweden in 2019, through analysis of clinical sample data. The research found that the use of NPS is more common in men and polydrug users, with legal NPS being more prevalent than illegal ones.
BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY
(2022)
Article
Biochemical Research Methods
Cathy M. Jacobs, Michael Kunz, Felix Mahfoud, Lea Wagmann, Markus R. Meyer
Summary: Volumetric absorptive microsampling (VAMS), an emerging microsampling technique, has been developed and validated for assessing adherence of antihypertensive drugs. The study demonstrated that VAMS-based strategy is suitable for evaluating adherence of all classes of antihypertensive drugs used in hypertension management guidelines.
ANALYTICAL AND BIOANALYTICAL CHEMISTRY
(2023)
Article
Biochemical Research Methods
Cathy M. Jacobs, Lea Wagmann, Markus R. Meyer
Summary: Taxus baccata contains poisonous taxine alkaloids that block calcium and sodium channels. This study analyzed human blood and urine to confirm ingestion of yew needles. The developed procedures successfully detected and tentatively identified several alkaloids.
DRUG TESTING AND ANALYSIS
(2023)
Article
Biochemical Research Methods
Matthias J. Richter, Lea Wagmann, Pierce Kavanagh, Simon D. Brandt, Markus R. Meyer
Summary: This study aims to identify the in vitro Phase I and II metabolites of QMMSB and QMiPSB for use as screening targets in toxicology. It was found that ester hydrolysis is an important step in the metabolism of these compounds, with the carboxylic acid product being detected only in negative ionization mode. The involvement of human monooxygenases and human carboxylesterases was also examined.
DRUG TESTING AND ANALYSIS
(2023)
Article
Chemistry, Analytical
Frederike Nordmeier, Adrian A. Doerr, Stefan Potente, Nadja Walle, Matthias W. Laschke, Michael D. Menger, Peter H. Schmidt, Markus R. Meyer, Nadine Schaefer
Summary: The interpretation of analytical results in forensic postmortem cases is often challenging, especially due to possible postmortem redistribution phenomena. A controlled toxicokinetic study on pigs was performed to examine the tissue distribution and possible redistribution of synthetic opioids U-47700 and tramadol. The study found that these substances are only slightly prone to redistribution, and central blood might be the best matrix for quantification.
JOURNAL OF ANALYTICAL TOXICOLOGY
(2023)
Article
Chemistry, Analytical
Cathy M. Jacobs, Lea Wagmann, Fabian Frankenfeld, Markus R. Meyer
Summary: This study reports a case of suicide by ingesting a high dose of chloroquine in combination with other drugs. Blood and urine toxicology screening and follow-up analyses were performed, revealing the presence of various drugs. The concentration of chloroquine and its metabolites were monitored over a period of 3 weeks, providing information on the excretion progress of chloroquine.
JOURNAL OF ANALYTICAL TOXICOLOGY
(2023)
Article
Chemistry, Analytical
Matthias J. Richter, Lea Wagmann, Simon D. Brandt, Markus R. Meyer
Summary: The study identified in vitro metabolites of synthetic cannabinoid receptor agonists 2F-QMPSB and SGT-233, and found suitable targets for toxicological screenings. Different enzymes and human carboxylesterases were involved in their metabolism. Various CYP isoforms played important roles in the metabolism of these compounds.
JOURNAL OF ANALYTICAL TOXICOLOGY
(2023)
Article
Pharmacology & Pharmacy
Hyunki Cho, Young Jun Kim, Jung-Woo Chae, Markus R. Meyer, Sang Kyum Kim, Chang Seon Ryu
Summary: This in-vitro study examined the drug metabolism and pharmacokinetics of Plpro inhibitors GRL0617 and HY-17542. The inhibitors underwent phase I and phase I + II metabolism in human liver microsomes, with CYP3A4 and CYP3A5 responsible for the predominant reactions. GRL0617 inhibited major drug-metabolizing enzymes, while HY-17542 was metabolized to GRL0617 through non-CYP reactions. The short half-lives of these Plpro inhibitors suggest the need for preclinical metabolism studies to determine therapeutic doses.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Aljoscha Gabelmann, Claus-Michael Lehr, Holger Grohganz
Summary: Addressing antimicrobial resistance requires new approaches in various disciplines of pharmaceutical sciences. The fluoroquinolone levofloxacin (LEV) plays an important role in the therapy of lung infections. However, its effectiveness is limited by its severe side effects involving tendinopathy, muscle weakness and psychiatric disturbance. Therefore, there is a need for the development of an effective formulation of LEV with reduced systemic drug concentrations, thereby also reducing the consumption and excretion of antibiotics or metabolites.
Article
Chemistry, Multidisciplinary
Aghiad Bali, Mohamed A. M. Kamal, Glorjen Mulla, Brigitta Loretz, Claus-Michael Lehr
Summary: With the emerging problem of antimicrobial resistance, new concepts for anti-infective drugs are emerging to de-weaponize bacteria rather than killing them. However, new biological barriers such as the biofilm matrix and bacterial cell envelope are creating challenges to maximize bacterial bioavailability. Functional materials and innovative delivery systems are needed to overcome these barriers, improve bacterial bioavailability, and enhance the effectiveness of anti-infective molecules.
ADVANCED FUNCTIONAL MATERIALS
(2023)
Article
Biochemistry & Molecular Biology
Yingwen Wu, Ben G. E. Zoller, Mohamed Ashraf Mostafa Kamal, Sven-Kevin Hotop, Claus-Michael Lehr, Mark Broenstrup, Petra Dersch, Martin Empting
Summary: Polymicrobial infections can cause acute and chronic diseases in the gastrointestinal and respiratory tracts. This study aims to modulate microbial communities by targeting the posttranscriptional regulator system called carbon storage regulator A (CsrA). A luciferase reporter gene assay combined with a qPCR expression gene assay has been successfully developed to evaluate the cellular effects of CsrA-regulated mechanisms. The assay enables the monitoring of downstream targets of CsrA and the evaluation of non-bactericidal/non-bacteriostatic compounds targeting CsrA/RsmA.
Article
Engineering, Chemical
Petra Obioma Nnamani, Edith Obioma Diovu, Ikechukwu Emmanuel Peter, Akachukwu Marytheresa Onwuka, Chiamaka Victory Ogbuanwu, Obiora Emmanuel Abonyi, Brigitta Loretz, Claus-Michael Lehr
Summary: This study investigated the characteristics and anti-inflammatory potency of herbal lipospheres formulated from Pentaclethra macrophylla. The results showed that the lipospheres had desirable particle size and morphology, and effectively inhibited edema in arthritis. These findings suggest that the herbal lipospheres have potential as a drug with better delivery system and reduced side effects.
Meeting Abstract
Peripheral Vascular Disease
Felix Goetzinger, Mathias Hohl, Dominic Norman Millenaar, Lucas Douglass Lauder, Joerg Reichrath, Markus Robert Meyer, Michael Boehm, Christian Ukena, Felix Mahfoud
JOURNAL OF HYPERTENSION
(2023)
Letter
Biochemistry & Molecular Biology
Caroline Diener, Martin Hart, Claudia Fecher-Trost, Jessica Knittel, Stefanie Rheinheimer, Markus R. Meyer, Jens Mayer, Veit Flockerzi, Andreas Keller, Eckart Meese
Summary: One widely accepted concept in biology is the potentiated cooperative effect of multiple miRNAs on the same target, despite insufficient experimental evidence. The quantity and quality of required side constraints of cooperative binding remain largely unknown. In this study, we selected 15 joint target genes, representing various 3'UTR binding site constellations, and found different cooperative scenarios between miR-21-5p and miR-155-5p. Surprisingly, our experiments provided stronger evidence for cooperative miRNA effects than originally postulated, highlighting the need to refine the definition of targetomes specified for single miRNAs to account for their cooperative effects.
CELLULAR & MOLECULAR BIOLOGY LETTERS
(2023)
Article
Biochemical Research Methods
Fabian Frankenfeld, Lea Wagmann, Cathy M. Jacobs, Markus R. Meyer
Summary: This study developed two separate methods for the quantitative analysis of selected drugs of abuse and cognitive enhancers in influent wastewater. The methods allowed for fast and accurate analysis of samples, and quantification of multiple analytes in wastewater.
DRUG TESTING AND ANALYSIS
(2023)
Meeting Abstract
Cardiac & Cardiovascular Systems
J. Hoevelmann, C. A. Viljoen, J. M. Schaar, M. Boehm, M. R. Meyer, K. Sliwa
EUROPEAN JOURNAL OF HEART FAILURE
(2023)
Article
Pharmacology & Pharmacy
Paola Orlandi, Marta Banchi, Francesca Vaglini, Marco Carli, Stefano Aringhieri, Arianna Bandini, Carla Pardini, Cristina Viaggi, Michele Lai, Greta Ali, Alessandra Ottani, Eleonora Vandini, Patrizia Guidi, Margherita Bernardeschi, Veronica La Rocca, Giulio Francia, Gabriella Fontanini, Mauro Pistello, Giada Frenzilli, Daniela Giuliani, Marco Scarselli, Guido Bocci
Summary: This study investigates the role of MC4R in melanoma and the use of the selective antagonist ML in combination with vemurafenib. The results show that ML can inhibit melanoma cell proliferation and induce apoptosis through the inhibition of ERK1/2 phosphorylation and reduction of BCL-XL expression. The combination of vemurafenib and ML exhibits a synergistic effect in vitro and inhibits tumor growth in vivo without causing adverse effects.
BIOCHEMICAL PHARMACOLOGY
(2024)
Article
Pharmacology & Pharmacy
Conor J. Bloxham, Katina D. Hulme, Fabrizio Fierro, Christian Fercher, Cassandra L. Pegg, Shannon L. O'Brien, Simon R. Foster, Kirsty R. Short, Sebastian G. B. Furness, Melissa E. Reichelt, Masha Y. Niv, Walter G. Thomas
Summary: Bitter taste receptors (T2Rs) are a type of G protein-coupled receptors that allow humans to detect aversive and toxic substances. This study characterized the functional properties of previously identified T2Rs in human cardiac tissues and their naturally occurring polymorphisms. The results showed differences in signaling among different T2R variants, and revealed a potential association between the T2R50 Tyr203 variant and cardiovascular disease.
BIOCHEMICAL PHARMACOLOGY
(2024)
Article
Pharmacology & Pharmacy
Lu Chen, Huanying Shi, Wenxin Zhang, Yongjun Zhu, Haifei Chen, Zimei Wu, Huijie Qi, Jiafeng Liu, Mingkang Zhong, Xiaojin Shi, Tianxiao Wang, Qunyi Li
Summary: This study demonstrates that Carfilzomib exhibits potent anti-tumor activity against esophageal squamous cell carcinoma (ESCC) by triggering mitochondrial apoptosis and reprogramming cellular metabolism. It has been identified that activating transcription factor 3 (ATF3) plays a crucial role as a cellular target in ESCC cells treated with Carfilzomib. Overexpression of ATF3 effectively counteracts the effects of Carfilzomib on ESCC cell proliferation, apoptosis, and metabolic reprogramming. Furthermore, ATF3 mediates the anti-tumor activity of Carfilzomib, suggesting its potential as a therapeutic agent for ESCC.
BIOCHEMICAL PHARMACOLOGY
(2024)
Review
Pharmacology & Pharmacy
Xing Zhang, Xiang Li, Ran Xia, Hong-Sheng Zhang
Summary: This review summarizes recent progress on the mechanisms of ferroptosis resistance in cancer and highlights the role of redox status and metabolism. Combination therapy for ferroptosis has great potential in treating resistant malignant tumors.
BIOCHEMICAL PHARMACOLOGY
(2024)