Hormonal Interactions in the Effects of Halogenated Aromatic Hydrocarbons On the Developing Brain

1998 ◽  
Vol 14 (1-2) ◽  
pp. 185-208 ◽  
Author(s):  
Neil J. Maclusky ◽  
Theodore J. Brown ◽  
Susan Schantz ◽  
Byung Woun Seo ◽  
Richard E. Peterson
Keyword(s):  
Low Dose ◽  
Biological Activities ◽  
Developing Brain ◽  
Adrenocortical Function ◽  
Environmental Toxicants ◽  
Halogenated Aromatic Hydrocarbons ◽  
Wide Range ◽  
The Central Nervous System ◽  
Dioxin Exposure ◽  
Underlying Mechanisms

Halogenated arylhydrocarbons (HAHs) exert a wide range of effects on the developing brain. These effects result in altered patterns of neuroendocrine function and behavior in adulthood, as well as changes in cognitive function. The underlying mechanisms have not yet been clearly defined. This paper briefly reviews the effects of HAHs on brain development, and proposes the hypothesis that interactions between different hormone-sensitive systems may contribute to the broad spectrum of responses observed after fetal or early postnatal HAH exposure. Physiological interactions between the effects of sex steroids, corticosteroids, and thyroid hormone are known to influence the development of the central nervous system (CNS). Since the biosynthesis and/or action of each of these hormones is sensitive to developmental HAH exposure, it is suggested that convergent effects of HAHs on different endocrine pathways may underlie some of the disruptive effects of these chemicals on CNS differentiation. Data are presented indicating that the disruptive effects of low dose dioxin exposure on sexual differentiation of the rat brain are probably not mediated through blockade of estrogen responses, butmay instead involve subtle developmental changes in other endocrine systems, perhaps also affecting the feedback control of adrenocortical function. The potential for interactive endocrine effects illustrates the need for a fuller understanding of the range of biological activities of HAHs in the brain, so that the potential risks of low dose developmental exposure to these environmental toxicants can be predicted with greater certainty.

scholarly journals Advances in Studies on the Pharmacological Activities of Fucoxanthin

Marine Drugs ◽  
2020 ◽  
Vol 18 (12) ◽  
pp. 634
Author(s):  
Han Xiao ◽  
Jiarui Zhao ◽  
Chang Fang ◽  
Qi Cao ◽  
Maochen Xing ◽  
...  
Keyword(s):  
Biological Activities ◽  
Intestinal Flora ◽  
Small Molecular Weight ◽  
Pharmacological Activities ◽  
Beneficial Effects ◽  
Wide Range ◽  
Cell Components ◽  
Underlying Mechanisms ◽  
Organ Fibrosis ◽  
Active Can

Fucoxanthin is a natural carotenoid derived mostly from many species of marine brown algae. It is characterized by small molecular weight, is chemically active, can be easily oxidized, and has diverse biological activities, thus protecting cell components from ROS. Fucoxanthin inhibits the proliferation of a variety of cancer cells, promotes weight loss, acts as an antioxidant and anti-inflammatory agent, interacts with the intestinal flora to protect intestinal health, prevents organ fibrosis, and exerts a multitude of other beneficial effects. Thus, fucoxanthin has a wide range of applications and broad prospects. This review focuses primarily on the latest progress in research on its pharmacological activity and underlying mechanisms.

Pathology of Angiostrongylus cantonensis infection in two model avian hosts

Parasitology ◽  
2020 ◽  
pp. 1-4
Author(s):  
Barbora Fecková ◽  
Priyanka Djoehana ◽  
Barbora Putnová ◽  
Michaela Valašťanová ◽  
Michaela Petríková ◽  
...  
Keyword(s):  
Low Dose ◽  
Natural Infection ◽  
Clinical Signs ◽  
French Polynesia ◽  
Angiostrongylus Cantonensis ◽  
High Dose ◽  
Wide Range ◽  
The Central Nervous System ◽  
Gross Lesions ◽  
Natural Pest Control

Abstract Angiostrongylus cantonensis causes severe neurological disorders in a wide range of warm-blooded animals, including several avian species. A laboratory isolate of A. cantonensis originating from French Polynesia, genotyped as clade 2, was used to assess the effect of experimental infection in chicken and Japanese quail. Low dose groups of birds were infected orally by 100 L3 larvae, high dose groups by 1500 L3 larvae and the birds in the third group were fed three infected snails, mimicking a natural infection. Clinical signs during the first week after infection, haematology, biochemistry, gross lesions and histology findings were used to assess the pathology of the infection. Some of the infected birds showed peripheral eosinophilia, while mild neurological signs were seen in others. No larvae were observed in serial sections of the central nervous system of infected birds 1 week after infection and no major gross lesions were observed during necropsy; histopathology did not reveal lesions directly attributable to A. cantonensis infection. Our results suggest that galliform birds are not highly susceptible to A. cantonensis infection and open a question of the importance of Galliformes in endemic areas as natural pest control, lowering the number of hosts carrying the infective larvae.

(Hetero)Aryloxyaminopropanols with N-Phenylpiperazine Structural Fragment – Review of Cardiovascular Activity

2020 ◽  
Vol 20 (17) ◽  
pp. 1719-1731
Author(s):  
Pavlina Marvanova ◽  
Tereza Padrtova ◽  
Petr Mokry
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Biological Activities ◽  
Cardiovascular Effects ◽  
Structural Fragment ◽  
Cardiovascular Activity ◽  
Phosphodiesterase Inhibition ◽  
Cardiovascular Agents ◽  
Wide Range ◽  
The Central Nervous System

Aryloxyphenylpiperazinylpropanols are a group of compounds exhibiting a wide range of biological activities, affecting the central nervous system and many cardiovascular mechanisms among them. As cardiovascular agents, aryloxyphenylpiperazinylpropanols work as antihypertensives, antiarrhythmics, cardiotonics or antiaggregants. The mechanism of action is almost always an α1-adrenolytic or combined α1- and β-adrenolytic effect, but sometimes other mechanisms (e.g., Ca2+ antagonism or phosphodiesterase inhibition) antagonism or phosphodiesterase inhibition) can positively participate. In some cases, compounds with a small modification of the connecting chain also exhibit the desired cardiovascular effects. Several studies dealt with chirality of aryloxyphenylpiperazinylpropanols and determined the differences between the particular activities of racemic and enantiomeric compounds.

scholarly journals Xanthine scaffold: available synthesis routes to deliver diversity by derivatization

2020 ◽  
Vol 17 ◽  
Author(s):  
Rita Petrucci ◽  
Marta Feroci ◽  
Leonardo Mattiello ◽  
Isabella Chiarotto
Keyword(s):  
Low Dose ◽  
Biological Activities ◽  
Biologically Active ◽  
Sustainable Chemistry ◽  
Chemical Transformations ◽  
Purine Base ◽  
Wide Range ◽  
Synthesis Routes ◽  
New Compounds ◽  
Coffee Species

: The functionalization of the skeletal systems of heterocycles represents a significant goal for new compounds development. The heterocyclic molecule xanthine (3,7-dihydro-1H-purine-2,6-dione) is a purine base with a bicyclic ring skeleton and four different nitrogen atoms, three of them are -NH groups. The principal derivatives are the well known natural methylxanthines (e.g. caffeine, theophylline and theobromine) that have prominent physiological effects at very low dose. The natural methylated xanthines, theophylline, theobromine and caffeine, are present in different plants such as the tea, cocoa and coffee species. For this reason natural xanthines can be considered as bio-based and renewable starting materials; their use in organic synthesis is strongly recommended in order to carry out sustainable chemistry. Essentially, the xanthine scaffold led to the preparation of numerous compounds very attractive in the pharmaceutical field, and these drugs are commercialized for a wide range of biological activities. The scope of this Mini Review is to consider the use of natural xanthines as starting material in chemical transformations carried out in organic solvents, without the intent to be exhaustive of all the synthetically chemical applications. More information on the chemical and electrochemical reactivity of this structural core in organic solvent can be useful for the scientific community. The effectiveness of natural xanthines can be improved by modifying the structures of these already biologically active compounds.

Antidiabetic Potential of Naturally Occurring Sesquiterpenes: A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Anupam Maurya ◽  
Sweta Mohan ◽  
Subash C. Verma
Keyword(s):  
Herbal Medicine ◽  
Side Effect ◽  
Biological Activities ◽  
Blood Stream ◽  
Synthetic Drugs ◽  
Wide Range ◽  
The World ◽  
Suitable Treatment ◽  
Underlying Mechanisms ◽  
The Many

: Diabetes Mellitus (DM) is endocrine disease, which causes 3rd leading death in human; additionally, it’s one of the major key concerns over the globe. The high levels of the glucose in blood stream is as well characterized hyperglycemia, which lead to serious damage to heart, blood vessels kidney, eyes, and nerve. The best treatment of the DM is still not available; many scientists all over the world are trying hard to seek out suitable treatment of DM. Though, numerous synthetic drugs are developed for the treatment of diabetes, but their utility has been hampered because of several side effect and poor efficacy. Among the various approaches for the treatment of DM, an herbal medicine, enriched extracts and natural derived molecules are most effective. The herbal medicine and plants contain many bioactive phytochemicals such as terpenoids, alkaloids, flavonoids & phenolics etc. The plant derived molecules and their suitable structure modification have given many leads or drugs to the world which are used in the treatment of many diseases e.g. sesquiterpene; artemisinin and their derivatives artemether & artesunate as an antimalarial drug. Sesquiterpenes are available in human diet, and largely taken as components of the many folk medicines and dietary supplements. Sesquiterpenes have wide range of biological activities such as anti-cancer, anti-inflammatory, anti-nociceptive, immunomodulatory, antidiabetic and antimicrobial which make them potential targets for development of new therapeutics and their usage for medical purposes. The natural products have attracted attention of world due to their large number biological activities, high safety and less side effect. The review mainly focuses on sesquiterpenes such as β-Caryophyllene, dysidine, farnesol & eremanthin etc., a class of terpenoids that may play important role in treatment or prevention of this morbid disorder diabetes, including their underlying mechanisms for the blood glucose-lowering property.

scholarly journals New Insights into the Stereochemical Requirements of the Bombesin BB1 Receptor Antagonists Binding

2020 ◽  
Vol 13 (8) ◽  
pp. 197
Author(s):  
Bahareh Rasaeifar ◽  
Patricia Gomez-Gutierrez ◽  
Juan J. Perez
Keyword(s):  
Biological Activities ◽  
Docking Study ◽  
Experimental Information ◽  
Peptide Ligands ◽  
Peripheral Tissues ◽  
Starting Point ◽  
Wide Range ◽  
The Family ◽  
The Central Nervous System ◽  
G Protein Coupled

Members of the family of bombesinlike peptides exert a wide range of biological activities both at the central nervous system and in peripheral tissues through at least three G-Protein Coupled Receptors: BB1, BB2 and BB3. Despite the number of peptide ligands already described, only a few small molecule binders have been disclosed so far, hampering a deeper understanding of their pharmacology. In order to have a deeper understanding of the stereochemical features characterizing binding to the BB1 receptor, we performed the molecular modeling study consisting of the construction of a 3D model of the receptor by homology modeling followed by a docking study of the peptoids PD168368 and PD176252 onto it. Analysis of the complexes permitted us to propose prospective bound conformations of the compounds, consistent with the experimental information available. Subsequently, we defined a pharmacophore describing minimal stereochemical requirements for binding to the BB1 receptor that was used in silico screening. This exercise yielded a set of small molecules that were purchased and tested, showing affinity to the BB1 but not to the BB2 receptor. These molecules exhibit scaffolds of diverse chemical families that can be used as a starting point for the development of novel BB1 antagonists.

scholarly journals Costunolide—A Bioactive Sesquiterpene Lactone with Diverse Therapeutic Potential

2019 ◽  
Vol 20 (12) ◽  
pp. 2926 ◽  
Author(s):  
Dae Yong Kim ◽  
Bu Young Choi
Keyword(s):  
Nitric Oxide ◽  
Intracellular Signaling ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Sesquiterpene Lactones ◽  
Activator Protein 1 ◽  
Transcription Activator ◽  
Proinflammatory Mediators ◽  
Wide Range ◽  
Underlying Mechanisms

Sesquiterpene lactones constitute a major class of bioactive natural products. One of the naturally occurring sesquiterpene lactones is costunolide, which has been extensively investigated for a wide range of biological activities. Multiple lines of preclinical studies have reported that the compound possesses antioxidative, anti-inflammatory, antiallergic, bone remodeling, neuroprotective, hair growth promoting, anticancer, and antidiabetic properties. Many of these bioactivities are supported by mechanistic details, such as the modulation of various intracellular signaling pathways involved in precipitating tissue inflammation, tumor growth and progression, bone loss, and neurodegeneration. The key molecular targets of costunolide include, but are not limited to, intracellular kinases, such as mitogen-activated protein kinases, Akt kinase, telomerase, cyclins and cyclin-dependent kinases, and redox-regulated transcription factors, such as nuclear factor-kappaB, signal transducer and activator of transcription, activator protein-1. The compound also diminished the production and/expression of proinflammatory mediators, such as cyclooxygenase-2, inducible nitric oxide synthase, nitric oxide, prostaglandins, and cytokines. This review provides an overview of the therapeutic potential of costunolide in the management of various diseases and their underlying mechanisms.

scholarly journals Puerarin Suppresses the Self-Renewal of Murine Embryonic Stem Cells by Inhibition of REST-MiR-21 Regulatory Pathway

2015 ◽  
Vol 37 (2) ◽  
pp. 527-536 ◽  
Author(s):  
Mengmeng Yin ◽  
Yin Yuan ◽  
Yurong Cui ◽  
Xian Hong ◽  
Hongyan Luo ◽  
...  
Keyword(s):  
Biological Activities ◽  
Embryonic Stem ◽  
The Self ◽  
Cardiac Differentiation ◽  
Regulatory Pathway ◽  
Self Renewal ◽  
Wide Range ◽  
Underlying Mechanisms ◽  
Mes Cells

Background/Aims: Puerarin shows a wide range of biological activities, including affecting the cardiac differentiation from murine embryonic stem (mES) cells. However, little is known about its effect and mechanism of action on the self-renewal of mES cells. This study aimed to determine the effect of puerarin on the self-renewal and pluripotency of mES cells and its underlying mechanisms. Methods: RT-PCR and real-time PCR were used to detect the transcripts of core transcription factors, specific markers for multiple lineages, REST and microRNA-21 (miR-21). Colony-forming assay was performed to estimate the self-renewal capacity of mES cells. Western blotting and wortmannin were employed to explore the role of PI3K/Akt signaling pathway in the inhibitory action of puerarin on REST transcript. Transfected mES cells with antagomir21 were used to confirm the role of miR-21 in the action of puerarin on cell self-renewal. Results: Puerarin significantly decreased the percentage of the self-renewal colonies, and suppressed the transcripts of Oct4, Nanog, Sox2, c-Myc and REST. Besides, PECAM, NCAM and miR-21 were up-regulated both under the self-renewal conditions and at day 4 of differentiation. The PI3K inhibitor wortmannin successfully reversed the mRNA expression changes of REST, Nanog and Sox2. Transfection of antagomir21 efficiently reversed the effects of puerarin on mES cells self-renewal. Conclusion: Inhibition of REST-miR-21 regulatory pathway may be the key mechanism of puerarin-induced suppression of mES cells self-renewal.

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

Synthesis, Characterization and Antiproliferative Activity Assessment of a Novel 1H-5-mercapto-1,2,4 Triazole Derivative

2017 ◽  
Vol 68 (4) ◽  
pp. 745-747 ◽  
Author(s):  
Marius Mioc ◽  
Sorin Avram ◽  
Vasile Bercean ◽  
Mihaela Balan Porcarasu ◽  
Codruta Soica ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Vascular Endothelial ◽  
Triazole Derivative ◽  
Activity Assessment ◽  
Wide Range ◽  
Specific Receptors ◽  
Endothelial Growth Factor ◽  
Selection Of

Angiogenesis plays an important function in tumor proliferation, one of the main angiogenic promoters being the vascular endothelial growth factor (VEGF) which activates specific receptors, particularly VEGFR-2. Thus, VEGFR-2 has become an essential therapeutic target in the development of new antitumor drugs. 1,2,4-triazoles show a wide range of biological activities, including antitumor effect, which was documented by numerous reports. In the current study the selection of 5-mercapto-1,2,4-triazole structure (1H-3-styryl-5-benzylidenehydrazino-carbonyl-methylsulfanil-1,2,4-triazole, Tz3a.7) was conducted based on molecular docking that emphasized it as suitable ligand for VEGFR-2 and EGFR1 receptors. Compound Tz3a.7 was synthesized and physicochemically and biologically evaluated thus revealing a moderate antiproliferative activity against breast cancer cell line MDA-MB-231.

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