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1. Medicinal chemistry perspectives of 1,2,3,4-tetrahydroisoquinoline analogs – biological activities and SAR studies

Author:
Faheem,; Karan Kumar, Banoth; Chandra Sekhar, Kondapalli Venkata Gowri; Chander, Subhash; Kunjiappan, Selvaraj; Murugesan, Sankaranarayanan
Source:
RSC advances 2021 v.11 no.20 pp. 12254-12287
ISSN:
2046-2069
Subject:
mechanism of action,   etc   ; bioactive properties; heterocyclic compounds;     Show all 3 Subjects
Abstract:
... Isoquinoline alkaloids are a large group of natural products in which 1,2,3,4-tetrahydroisoquinolines (THIQ) form an important class. THIQ based natural and synthetic compounds exert diverse biological activities against various infective pathogens and neurodegenerative disorders. Due to these reasons, the THIQ heterocyclic scaffold has garnered a lot of attention in the scientific community which ...
DOI:
10.1039/d1ra01480c

2. Recent advances in protein metalation: structural studies

Author:
Merlino, Antonello
Source:
Chemical communications 2021 v.57 no.11 pp. 1295-1307
ISSN:
1364-548X
Subject:
mechanism of action,   etc   ; ligands; oxidation; toxicity;     Show all 4 Subjects
Abstract:
... Protein metalation is a process that determines the formation of adducts upon reaction of metal compounds with proteins. Protein metalation plays a crucial role in different fields, determining the mechanism of action and toxicity of metal-based drugs and the basis for the rational design of artificial metalloenzymes and protein-based metallodrug-delivery systems. Recent advances in structural stu ...
DOI:
10.1039/d0cc08053e

3. Comparison of consistency and complementarity of reporting biosimilar quality attributes between regulatory and scientific communities: An adalimumab case study

Author:
Alsamil, Ali M.; Giezen, Thijs J.; Egberts, Toine C.; Leufkens, Hubert G.; Gardarsdottir, Helga
Source:
Biologicals 2021 v.69 pp. 30-37
ISSN:
1045-1056
Subject:
mechanism of action,   etc   ; bioactive properties; case studies;     Show all 3 Subjects
Abstract:
... Biosimilar approval relies on the comparability of quality attributes (QAs), for which information can be derived from regulatory or scientific communities. Limited information is known about whether these sources are consistent with or complementary to each other. The consistency and complementarity of QA reporting in biosimilarity assessments for adalimumab biosimilars approved by the European M ...
DOI:
10.1016/j.biologicals.2020.12.003

4. Development and validation of dual-cardiotoxicity evaluation method based on analysis of field potential and contractile force of human iPSC-derived cardiomyocytes / multielectrode assay platform

Author:
Lee, Seul-Gi; Kim, Jin; Oh, Min-Seok; Ryu, Bokyeong; Kang, Kyu-Ree; Baek, Jieun; Lee, Jin-Moo; Choi, Sun-Ok; Kim, C-Yoon; Chung, Hyung Min
Source:
Biochemical and biophysical research communications 2021 v.555 pp. 67-73
ISSN:
0006-291X
Subject:
mechanism of action,   etc   ; cardiomyocytes; cardiotoxicity; electrophysiology; humans; pharmacology; research;     Show all 7 Subjects
Abstract:
... A recent in vitro cardiovascular safety pharmacology test uses cardiomyocytes derived from human induced pluripotent stem cells (hiPSCs) to overcome the limitations of the classical test systems, such as species differences and local channel analysis. The Comprehensive in vitro Proarrhythmia Assay (CiPA) is a new proarrhythmia screening paradigm proposed by a CiPA steering expert group, which esse ...
DOI:
10.1016/j.bbrc.2021.03.039

5. Lysins breaking down the walls of Gram-negative bacteria, no longer a no-go

Author:
Gutiérrez, Diana; Briers, Yves
Source:
Current opinion in biotechnology 2021 v.68 pp. 15-22
ISSN:
0958-1669
Subject:
mechanism of action,   etc   ; bacteriophages; biotechnology; clinical examination; peptidoglycans;     Show all 5 Subjects
Abstract:
... Phage lysins are one of the most advanced classes of antibacterials under clinical evaluation and have a new mode of action based on peptidoglycan degradation. Lysins were initially excluded from use against Gram-negative pathogens because of their impermeable outer membrane, but are now increasingly developed as effective antibacterials against these critical priority pathogens. Generally, three ...
DOI:
10.1016/j.copbio.2020.08.014

6. Nanoparticles as antimicrobial and antiviral agents: A literature-based perspective study

Author:
Sharmin, Shabnam; Rahaman, Md. Mizanur; Sarkar, Chandan; Atolani, Olubunmi; Islam, Mohammad Torequl; Adeyemi, Oluyomi Stephen
Source:
Heliyon 2021 v.7 no.3 pp. e06456
ISSN:
2405-8440
Subject:
mechanism of action,   etc   ; antibiotic resistance; surface area; therapeutics;     Show all 4 Subjects
Abstract:
... The scientific explorations of nanoparticles for their inherent therapeutic potencies as antimicrobial and antiviral agents due to increasing incidences of antibiotic resistance have gained more attention in recent time. This factor amongst others necessitates the search for newer and more effective antimicrobial agents. Several investigations have demonstrated the prospects of nanoparticles in th ...
DOI:
10.1016/j.heliyon.2021.e06456

7. Sublingual Immunotherapy: How Sublingual Allergen Administration Heals Allergic Diseases; Current Perspective about the Mode of Action

Author:
Gotoh, Minoru; Kaminuma, Osamu
Source:
Pathogens 2021 v.10 no.2
ISSN:
2076-0817
Subject:
mechanism of action,   etc   ; T-lymphocytes; allergens; immunotherapy; macrophages; tongue;     Show all 6 Subjects
Abstract:
... Owing to the successful application of sublingual immunotherapy (SLIT), allergen immunotherapy (AIT) has become one of the leading treatments for allergic diseases. Similar to the case with other AITs, such as subcutaneous and oral immunotherapies, not only the alleviation of allergic symptoms, but also the curing of the diseases can be expected in patients undergoing SLIT. However, how and why su ...
DOI:
10.3390/pathogens10020147

8. Current Applications and Future Perspectives of Fluorescence Light Energy Biomodulation in Veterinary Medicine

Author:
Marchegiani, Andrea; Spaterna, Andrea; Cerquetella, Matteo
Source:
Veterinary sciences 2021 v.8 no.2
ISSN:
2306-7381
Subject:
mechanism of action,   etc   ; dogs; energy; fluorescence; veterinary medicine;     Show all 5 Subjects
Abstract:
... The purpose of this review is to determine the state of the art of the mode of action and potential applications of fluorescence photobiomodulation in veterinary medicine. After a summary of the assets that have led the translation of such light-based therapies from bench side into clinical use, recent advances in canine dermatology using this brand-new approach are presented, and future scenarios ...
DOI:
10.3390/vetsci8020020

9. A Future Perspective on Phototriggered Isomerizations of Transition Metal Sulfoxides and Related Complexes

Author:
Vittardi, Sebastian B.; Thapa Magar, Rajani; Breen, Douglas J.; Rack, Jeffrey J.
Source:
Journal of the American Chemical Society 2021 v.143 no.2 pp. 526-537
ISSN:
1520-5126
Subject:
mechanism of action,   etc   ; isomerization; ligands; osmium; ruthenium; sulfoxides;     Show all 6 Subjects
Abstract:
... Photochromic molecules are examples of light-activated bistable molecules. We highlight the design criteria for a class of ruthenium and osmium sulfoxide complexes that undergo phototriggered isomerization of the bound sulfoxide. The mode of action in these complexes is an excited-state isomerization of the sulfoxide from S-bonded to O-bonded. We discuss the basic mechanism for this transformation ...
DOI:
10.1021/jacs.0c08820

10. Plant-virus infection inhibitors: The great potential of Caryophyllales species

Author:
Lembo Duarte, Lígia Maria; Vaz Alexandre, Maria Amélia; Rodrigues Chaves, Alexandre Levi; Alves Cursino dos Santos, Déborah Yara; Oliveira de Souza, Ana Claudia; Bernacci, Luis Carlos
Source:
Physiological and molecular plant pathology 2021 v.113 pp. 101597
ISSN:
0885-5765
Subject:
mechanism of action,   etc   ; Caryophyllales; models; plant pathology; viruses;     Show all 5 Subjects
Abstract:
... Caryophyllales is one of the largest orders in eudicots and comprises 39 families with approximately 12,500 species. Although extracts from species of this order have been considered potential inhibitors of plant virus infection since the early 20th century, few species have actually been investigated. In this review, we present an exhaustive analysis of published papers that investigate this inhi ...
DOI:
10.1016/j.pmpp.2020.101597

11. Lipid membranes induce structural conversion from amyloid oligomers to fibrils

Author:
Gu, Lei; Guo, Zhefeng
Source:
Biochemical and biophysical research communications 2021 v.557 pp. 122-126
ISSN:
0006-291X
Subject:
mechanism of action,   etc   ; amyloid; electron paramagnetic resonance spectroscopy; lipids; neurons; pathogenesis; research; therapeutics; toxicity;     Show all 9 Subjects
Abstract:
... Formation of amyloid oligomers and fibrils underlies the pathogenesis of a number of neurodegenerative diseases such as Alzheimer’s. One mechanism of action by which Aβ aggregates cause neuronal toxicity is through interactions with cellular membranes. Aβ aggregates have been shown to disrupt membrane integrity via pore formation, membrane thinning, or lipid extraction. At the same time, lipid mem ...
DOI:
10.1016/j.bbrc.2021.03.174

12. Gut microbiota-mediated pesticide toxicity in humans: Methodological issues and challenges in the risk assessment of pesticides

Author:
Utembe, Wells; Kamng’ona, Arox Wadson
Source:
Chemosphere 2021 v.271 pp. 129817
ISSN:
0045-6535
Subject:
mechanism of action,   etc   ; biomarkers; digestive system; humans; intestinal microorganisms; pesticides; pharmacokinetics; risk assessment; toxicity;     Show all 9 Subjects
Abstract:
... Many in vivo and in vitro studies have shown that pesticides can disrupt the functioning of gut microbiota (GM), which can lead to many diseases in humans. While the tests developed by the Organization of Economic Cooperation and Development (OECD) are expected to capture most apical effects resulting from GM disruptions, exclusion of GM in the risk assessment might mischaracterize hazards or over ...
DOI:
10.1016/j.chemosphere.2021.129817

13. The G-patch activators Pfa1 and PINX1 exhibit different modes of interaction with the Prp43 RNA helicase

Author:
Mouffok, Saïda; Capeyrou, Régine; Belhabich-Baumas, Kamila; Joret, Clément; Henras, Anthony K.; Humbert, Odile; Henry, Yves
Source:
RNA biology 2021 v.18 no.4 pp. 510-522
ISSN:
1555-8584
Subject:
mechanism of action,   etc   ; RNA; RNA helicases; active sites; adenosinetriphosphatase; biogenesis; ribosomes; yeasts;     Show all 8 Subjects
Abstract:
... Prp43 is a DEAH-box RNA helicase involved in both splicing and ribosome biogenesis. Its activities are directly stimulated by several co-activators that share a G-patch domain. The substrates of Prp43, its mechanism of action and the modes of interaction with and activation by G-patch proteins have been only partially characterized. We investigated how Pfa1 and PINX1, two G-patch proteins involved ...
DOI:
10.1080/15476286.2020.1818458

14. Fungal glycosides: Structure and biological function

Author:
Hussain, Hidayat; Mamadalieva, Nilufar Z.; Ali, Iftikhar; Elizbit,; Green, Ivan R.; Wang, Daijie; Zou, Liang; Simal-Gandara, Jesus; Cao, Hui; Xiao, Jianbo
Source:
Trends in food science & technology 2021 v.110 pp. 611-651
ISSN:
0924-2244
Subject:
mechanism of action,   etc   ; bioavailability; cytotoxicity; food science; fungi; glycosides; glycosylation; secondary metabolites; spoilage; sugars; technology; therapeutics;     Show all 12 Subjects
Abstract:
... Natural products acquire vast and intriguing structural diversity and have been recognized as a tremendously diverse source of new lead compounds. Numerous bioactive secondary metabolites are present in the form of glycosylated molecules in which the sugar parts are normally associated with the interaction along with molecular recognition of the cellular target.The presence of sugar entities are c ...
DOI:
10.1016/j.tifs.2021.02.029

15. Recent updates on the chemistry, bioactivities, mode of action, and industrial applications of plant essential oils

Author:
Ni, Zhi-Jing; Wang, Xin; Shen, Yi; Thakur, Kiran; Han, Jinzhi; Zhang, Jian-Guo; Hu, Fei; Wei, Zhao-Jun
Source:
Trends in food science & technology 2021 v.110 pp. 78-89
ISSN:
0924-2244
Subject:
mechanism of action,   etc   ; antioxidants; flavor; food preservation; medicine; odors; shelf life; therapeutics;     Show all 8 Subjects
Abstract:
... Since time immemorial, natural active compounds including essential oils (EOs) and their components have been used due to their flavor and fragrance. Out of 3000 known varieties, 300 are commercially utilized for the food and pharmaceutical industries.In recent years, studies on EOs have enormously increased owing to their remarkable biological activities and health benefits. As a result, their ph ...
DOI:
10.1016/j.tifs.2021.01.070

16. Triterpene glycosides and phenylpropane derivatives from Staurogyne concinnula possessing anti-angiogenic activity

Author:
Vo, Thanh-Hoa; Lin, Yu-Chi; Liaw, Chia-Ching; Pan, Wen-Pin; Cheng, Jing-Jy; Lee, Ching-Kuo; Kuo, Yao-Haur
Source:
Phytochemistry 2021 v.184 pp. 112666
ISSN:
0031-9422
Subject:
mechanism of action,   etc   ; biological assessment; butanol; ethanol; integrins; plant biochemistry; screening; signal transduction; triterpenoid saponins;     Show all 9 Subjects
Abstract:
... After anti-angiogenic activity screening, the potential n-butanol layer partitioned from the ethanol extract of Staurogyne concinnula was conducted. Further purification by Diaion HP20 column and preparative HPLC chromatography, four undescribed triterpenoid saponin derivatives, along with the known baptisiasaponin I, and four known phenylpropanoid glycosides were isolated and characterized from n ...
DOI:
10.1016/j.phytochem.2021.112666

17. The natural compound rutaecarpine promotes white adipocyte browning through activation of the AMPK-PRDM16 axis

Author:
Liu, Xiaomin; Zhang, Yuwei; Chu, Yi; Zhao, Xuemei; Mao, Liufeng; Zhao, Shiting; Lin, Shaoqiang; Hui, Xiaoyan; Gu, Ping; Xu, Yong; Loomes, Kerry; Tang, Shibing; Nie, Tao; Wu, Donghai
Source:
Biochemical and biophysical research communications 2021 v.545 pp. 189-194
ISSN:
0006-291X
Subject:
mechanism of action,   etc   ; Western blotting; drugs; noninsulin-dependent diabetes mellitus; obesity; research; sequence analysis; white adipocytes;     Show all 8 Subjects
Abstract:
... The prevalence of obesity is increasing globally and is associated with many metabolic disorders, such as type 2 diabetes and cardiovascular diseases. In recent years, a number of studies suggest that promotion of white adipose browning represents a promising strategy to combat obesity and its related metabolic disorders. The aim of this study was to identify compounds that induce adipocyte browni ...
DOI:
10.1016/j.bbrc.2021.01.080

18. A signal-on fluorescent aptasensor based on gold nanoparticles for kanamycin detection

Author:
Sun, Yimeng; Qi, Tong; Jin, Yan; Liang, Lijuan; Zhao, Jianlong
Source:
RSC advances 2021 v.11 no.17 pp. 10054-10060
ISSN:
2046-2069
Subject:
mechanism of action,   etc   ; aptasensors; detection limit; fluorescence; fluorescent dyes; fluorometry; gold; kanamycin; nanogold; nucleic acids; oligonucleotides;     Show all 11 Subjects
Abstract:
... This study describes the development, verification and practical application of an aptasensor for the fluorometric detection of kanamycin. Using the nucleic acid aptamer with FAM fluorescent group as the conjugate, using gold nanoparticles as the fluorescence dynamic quenching source, a fluorescence sensor was fabricated through the signal-on method for the micro-detection of kanamycin. The nuclei ...
DOI:
10.1039/d0ra10602j

19. Caffeic Acid and Its Derivatives: Antimicrobial Drugs toward Microbial Pathogens

Author:
Khan, Fazlurrahman; Bamunuarachchi, Nilushi Indika; Tabassum, Nazia; Kim, Young-Mog
Source:
Journal of agricultural and food chemistry 2021 v.69 no.10 pp. 2979-3004
ISSN:
1520-5118
Subject:
mechanism of action,   etc   ; amides; caffeic acid; food chemistry; glycosides; pathogenesis; photoirradiation; sugars; water solubility;     Show all 9 Subjects
Abstract:
... Caffeic acid is a plant-derived compound that is classified as hydroxycinnamic acid which contains both phenolic and acrylic functional groups. Caffeic acid has been greatly employed as an alternative strategy to combat microbial pathogenesis and chronic infection induced by microbes such as bacteria, fungi, and viruses. Similarly, several derivatives of caffeic acid such as sugar esters, organic ...
DOI:
10.1021/acs.jafc.0c07579

20. Nitric oxide and l-arginine have mixed effects on mammalian feeding in condition of a high motivation to feed

Author:
Hazut, Noa; Rapps, Kayla; Weller, Aron; Susswein, Abraham J.
Source:
Appetite 2021 v.158 pp. 105011
ISSN:
0195-6663
Subject:
mechanism of action,   etc   ; arginine; drinking water; hunger; motivation; nervous system; neurotransmitters; nitric oxide; rats; satiety;     Show all 10 Subjects
Abstract:
... Feeding inhibition caused by satiation in rats is partially mediated by the unconventional neurotransmitter nitric oxide (NO). Thus, in satiated rats blocking NO production increases feeding, and treatment with the NO precursor l-arginine or with an NO donor reduces feeding beyond that caused by satiation. Do NO and l-arginine also inhibit feeding when feeding motivation is high? When feeding moti ...
DOI:
10.1016/j.appet.2020.105011