scholarly journals Comparative Analysis of Experimental Pharmacokinetics of New Neurotropic Peptides

2019 ◽  
Vol 2 (1) ◽  
Author(s):  
S.S. Boyko ◽  
V.P. Zherdev ◽  
R.V. Shevchenko ◽  
O.G. Gribakina
Keyword(s):  
Structural Features ◽  
New Drugs ◽  
Active Metabolites ◽  
Experimental Animals ◽  
Active Peptides ◽  
Nootropic Drug ◽  
Enzymatic Action ◽  
Enzymatic Systems ◽  
Glycine Ethyl Ester ◽  
Pharmacologically Active

Experimental pharmacokinetics of new pharmacologically active peptides, modified analogues of endogenous neuropeptides, has been investigated in rats and rabbits. The study icluded 3 new drugs: (i) the nootropic drug noopept (phenylacetyl-prolyl-glycine ethyl ester); (ii) dilept (N-caproyl-L-prolyl-L-tyrosine methyl ester) – the antipsychotic with positive mnemotropic action; (iii) compound GB-115 – selective anxiolytic (phenylhexanoyl-prolyl-tryptophan amide). Differences in pharmacokinetics and biotransformation of the studied drugs depended on their structural features. The ether derivatives noopept and dilept underwent intensive metabolism by rat gastrointestinal esterases and peptidases with the formation of active metabolites. Being an amide, the compound GB-115 was more resistant to the enzymatic effects of peptidases and was detected for a longer period in the blood of experimental animals. In rabbits the studied compounds were less exposed to the enzymatic action by gastrointestinal peptidases, and were detected plasma of rabbits for a longer period. The higher stability of the compounds studied in rabbits may be attributed not only to the structural features of the studied dipeptides, but also to differences in the activity of the enzymatic systems of the gastrointestinal tract participating in their metabolism, as well as differences in the rate of hepatic and renal blood flow in rats and rabbits.

scholarly journals Citrus Peels as a Source of Bioactive Compounds with Industrial and Therapeutic Applications

2021 ◽  
Author(s):  
Doha Hussien Abou Baker ◽  
Eman Ahmed Ibrahim ◽  
Zeinab Abd El-Rhaman Salama
Keyword(s):  
Bioactive Compounds ◽  
Antioxidant Activities ◽  
Rich Source ◽  
New Drugs ◽  
Active Metabolites ◽  
Citrus Peel ◽  
The World ◽  
Good Starting Point ◽  
Pharmacologically Active ◽  
Agriculture Wastes

Agriculture wastes are considered a good starting point to discover for new drugs all over the world. In this context, Agriculture wastes contain millions of compounds to be screened to find bioactive compounds responsible for the activity to be used in drugs. Citrus agriculture is one of the most important commercial and industrial agricultural activities in the world. The peel waste of Citrus species is a rich source of bioactive compounds such as essential oils, flavones, polyphenols, and pigment. Citrus peel has been widely used in the medicine industry. The waste peel of citrus consider a rich source of pharmacologically active metabolites with antioxidant activities.

scholarly journals Natural Bioactive Thiazole-Based Peptides from Marine Resources: Structural and Pharmacological Aspects

Marine Drugs ◽  
2020 ◽  
Vol 18 (6) ◽  
pp. 329
Author(s):  
Rajiv Dahiya ◽  
Sunita Dahiya ◽  
Neeraj Kumar Fuloria ◽  
Suresh Kumar ◽  
Rita Mourya ◽  
...  
Keyword(s):  
Binding Sites ◽  
Wide Spectrum ◽  
Structural Features ◽  
Complex Nature ◽  
Special Focus ◽  
Structural Components ◽  
Active Peptides ◽  
Peptide Interactions ◽  
Allosteric Binding Sites ◽  
Pharmacologically Active

Peptides are distinctive biomacromolecules that demonstrate potential cytotoxicity and diversified bioactivities against a variety of microorganisms including bacteria, mycobacteria, and fungi via their unique mechanisms of action. Among broad-ranging pharmacologically active peptides, natural marine-originated thiazole-based oligopeptides possess peculiar structural features along with a wide spectrum of exceptional and potent bioproperties. Because of their complex nature and size divergence, thiazole-based peptides (TBPs) bestow a pivotal chemical platform in drug discovery processes to generate competent scaffolds for regulating allosteric binding sites and peptide–peptide interactions. The present study dissertates on the natural reservoirs and exclusive structural components of marine-originated TBPs, with a special focus on their most pertinent pharmacological profiles, which may impart vital resources for the development of novel peptide-based therapeutic agents.

scholarly journals Ketamine—50 years in use: from anesthesia to rapid antidepressant effects and neurobiological mechanisms

2021 ◽  
Vol 73 (2) ◽  
pp. 323-345
Author(s):  
Samuel Kohtala
Keyword(s):  
Traumatic Stress ◽  
Molecular Mechanisms ◽  
Post Traumatic Stress ◽  
Active Metabolites ◽  
The Past ◽  
Antidepressant Effects ◽  
Post Traumatic ◽  
Pharmacologically Active ◽  
Dose Dependent ◽  
Different Doses

AbstractOver the past 50 years, ketamine has solidified its position in both human and veterinary medicine as an important anesthetic with many uses. More recently, ketamine has been studied and used for several new indications, ranging from chronic pain to drug addiction and post-traumatic stress disorder. The discovery of the rapid-acting antidepressant effects of ketamine has resulted in a surge of interest towards understanding the precise mechanisms driving its effects. Indeed, ketamine may have had the largest impact for advancements in the research and treatment of psychiatric disorders in the past few decades. While intense research efforts have been aimed towards uncovering the molecular targets underlying ketamine’s effects in treating depression, the underlying neurobiological mechanisms remain elusive. These efforts are made more difficult by ketamine’s complex dose-dependent effects on molecular mechanisms, multiple pharmacologically active metabolites, and a mechanism of action associated with the facilitation of synaptic plasticity. This review aims to provide a brief overview of the different uses of ketamine, with an emphasis on examining ketamine’s rapid antidepressant effects spanning molecular, cellular, and network levels. Another focus of the review is to offer a perspective on studies related to the different doses of ketamine used in antidepressant research. Finally, the review discusses some of the latest hypotheses concerning ketamine’s action.

scholarly journals Diversity of Conopeptides and Conoenzymes from the Venom Duct of the Marine Cone Snail Conus bayani as Determined from Transcriptomic and Proteomic Analyses

Marine Drugs ◽  
2021 ◽  
Vol 19 (4) ◽  
pp. 202
Author(s):  
Rajesh Rajaian Pushpabai ◽  
Carlton Ranjith Wilson Alphonse ◽  
Rajasekar Mani ◽  
Deepak Arun Apte ◽  
Jayaseelan Benjamin Franklin
Keyword(s):  
Gene Family ◽  
Transcriptome Sequencing ◽  
Cone Snail ◽  
Active Peptides ◽  
Transcriptomic Data ◽  
Sequencing Technologies ◽  
Hunting Strategies ◽  
Divergent Gene ◽  
Pharmacologically Active ◽  
Highly Evolved

Marine cone snails are predatory gastropods characterized by a well-developed venom apparatus and highly evolved hunting strategies that utilize toxins to paralyze prey and defend against predators. The venom of each species of cone snail has a large number of pharmacologically active peptides known as conopeptides or conotoxins that are usually unique in each species. Nevertheless, venoms of only very few species have been characterized so far by transcriptomic approaches. In this study, we used transcriptome sequencing technologies and mass spectrometric methods to describe the diversity of venom components expressed by a worm-hunting species, Conus bayani. A total of 82 conotoxin sequences were retrieved from transcriptomic data that contain 54 validated conotoxin sequences clustered into 21 gene superfamilies including divergent gene family, 17 sequences clustered to 6 different conotoxin classes, and 11 conotoxins classified as unassigned gene family. Seven new conotoxin sequences showed unusual cysteine patterns. We were also able to identify 19 peptide sequences using mass spectrometry that completely overlapped with the conotoxin sequences obtained from transcriptome analysis. Importantly, herein we document the presence of 16 proteins that include five post-translational modifying enzymes obtained from transcriptomic data. Our results revealed diverse and novel conopeptides of an unexplored species that could be used extensively in biomedical research due to their therapeutic potentials.

Pharmacologically Active Peptides and Proteins from Bee Venom

Animal Toxins ◽  
2000 ◽  
pp. 127-151
Author(s):  
Peter N. Strong ◽  
Jonathan D. F. Wadsworth
Keyword(s):  
Bee Venom ◽  
Active Peptides ◽  
Pharmacologically Active

scholarly journals Are Platelet Aggregation Tests the Best Way to Assess New Drugs for Arterial Disease

2018 ◽  
Vol 1 (1) ◽  
pp. 01-03
Author(s):  
Mark I. M. Noble
Keyword(s):  
Platelet Aggregation ◽  
Platelet Function ◽  
Platelet Rich Plasma ◽  
New Drugs ◽  
In Vitro Test ◽  
In Vivo Efficacy ◽  
Experimental Animals ◽  
Stenosed Artery

Over many years, laboratory testing of platelet aggregability have been carried out in attempts to develop drugs that would prevent thrombosis in arteries. The problems encountered included the question of methodology. Blood samples have to be anticoagulated in order to study the platelets. Anti-coagulation with citrate and tests on derived platelet rich plasma did not correlate at all well with thrombus growth in the stenosed coronary arteries of experimental animals and citrate removes the calcium ions which are vital for platelet function. Anticoagulation with heparin also interfered with platelet function, so that now, hirudins are the preferred anticoagulant. However it was observed that if, instead of stimulating platelet aggregation with adrenaline or ADP, serotonin was applied to the preparation, very little aggregation took place in spite of serotonin 5HT2A antagonists being the most potent inhibitors of thrombus growth in experimental animals. Another indicator that primary platelet agggregation is not a predictor of in vivo efficacy was the finding that 5HT2A antagonism inhibited aggregate growth. In a stenosed artery the platelets are activated by increased shear stress and blood turbulence with release of platelet serotonin causing positive feedback activation of more platelets. At present, there does not seem to be a bench in vitro test that accurately predicts in vivo efficacy in stenosed artery occlusive thrombosis.

scholarly journals A Review of Terpenes from Marine-Derived Fungi: 2015–2019

Marine Drugs ◽  
2020 ◽  
Vol 18 (6) ◽  
pp. 321 ◽  
Author(s):  
Minghua Jiang ◽  
Zhenger Wu ◽  
Heng Guo ◽  
Lan Liu ◽  
Senhua Chen
Keyword(s):  
Enzyme Inhibitor ◽  
Biological Activities ◽  
Chemical Diversity ◽  
Active Metabolites ◽  
Marine Animals ◽  
Research Papers ◽  
Lead Compounds ◽  
Chemical Structures ◽  
The Past ◽  
Pharmacologically Active

Marine-derived fungi are a significant source of pharmacologically active metabolites with interesting structural properties, especially terpenoids with biological and chemical diversity. In the past five years, there has been a tremendous increase in the rate of new terpenoids from marine-derived fungi being discovered. In this updated review, we examine the chemical structures and bioactive properties of new terpenes from marine-derived fungi, and the biodiversity of these fungi from 2015 to 2019. A total of 140 research papers describing 471 new terpenoids of six groups (monoterpenes, sesquiterpenes, diterpenes, sesterterpenes, triterpenes, and meroterpenes) from 133 marine fungal strains belonging to 34 genera were included. Among them, sesquiterpenes, meroterpenes, and diterpenes comprise the largest proportions of terpenes, and the fungi genera of Penicillium, Aspergillus, and Trichoderma are the dominant producers of terpenoids. The majority of the marine-derived fungi are isolated from live marine matter: marine animals and aquatic plants (including mangrove plants and algae). Moreover, many terpenoids display various bioactivities, including cytotoxicity, antibacterial activity, lethal toxicity, anti-inflammatory activity, enzyme inhibitor activity, etc. In our opinion, the chemical diversity and biological activities of these novel terpenoids will provide medical and chemical researchers with a plenty variety of promising lead compounds for the development of marine drugs.

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