Non-food bioactive products: Semisynthesis, biological activities, and mechanisms of action of oximinoether derivatives of matrine from Sophora flavescens

2019 ◽  
Vol 131 ◽  
pp. 134-141 ◽  
Author(s):  
Shaochen Li ◽  
Zhiqiang Sun ◽  
Bingchuan Zhang ◽  
Min Lv ◽  
Hui Xu
Keyword(s):  
Biological Activities ◽  
Mechanisms Of Action ◽  
Sophora Flavescens ◽  
Derivatives Of

Advances on Monosaccharides and Oligosaccharides: Structural Modifications and Bioactivities

2021 ◽  
Vol 21 ◽  
Author(s):  
Shaochen Li ◽  
Min Lv ◽  
Shaoyong Zhang ◽  
Hui Xu
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Biological Activities ◽  
Building Blocks ◽  
Biological Properties ◽  
Mechanisms Of Action ◽  
Biological Processes ◽  
Structural Modifications ◽  
Structure Activity ◽  
Derivatives Of

: Derivatives of monosaccharides and oligosaccharides play the important roles in biological processes. Monosaccharides are the single carbohydrate building blocks, such as glucose, xylose, and fructose. Oligosaccharides are composed of 2–10 monosaccharides including disaccharides and trisaccharides. Moreover, monosaccharides, oligosaccharides and their derivatives are vital molecules with various biological properties including anticancer activity, antiviral activity, insecticidal activity, antimicrobial activity, and antioxidant activity. This review covers a survey of structural modifications, biological activities, and mechanisms of action of monosaccharides, oligosaccharides and their derivatives. Additionally, their structure–activity relationships are also concluded.

Synthesis, characterization and biological activities of 1,3,4-oxadiazole derivatives of nalidixic acid and their copper complexes

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Nalidixic Acid ◽  
Copper Complexes ◽  
Biological Activities ◽  
Bidentate Coordination ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Oxadiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
Derivatives Of ◽  
Substituted 1

A series of novel 1, 3, 4-oxadiazole analogues was synthesized from cyclization of hydrazones of substituted 1-ethyl-1,4-dihydro-7-methyl-4-oxo-1,8-naphthyridine-3-carbohydrazides were prepared from nalidixic acid. The structures of synthesized oxadiazole derivatives and their copper complexes were elucidated on the basis of FTIR, elemental analyses, 1H-NMR and atomic absorption spectral analysis. It was observed from spectral data that metal ligand ratio was 1:1 in all copper complexes and they were bidentate, coordination was found to be done through oxygen of 4-oxo group and nitrogen of oxadiazole ring. The synthesized compounds were further evaluated with biological activities and compared with parent hydrazones. Copper complexes possess antibacterial and antifungal activities better than the oxadiazoles while they have better antioxidant activity then copper complexes. Parent hydrazones were better in all biological activities than synthesized oxadiazoles.

scholarly journals Synthesis, Antiproliferative Activity and Radical Scavenging Ability of 5-O-Acyl Derivatives of Quercetin

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1608
Author(s):  
Stephen Lo ◽  
Euphemia Leung ◽  
Bruno Fedrizzi ◽  
David Barker
Keyword(s):  
Antiproliferative Activity ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Breast Cancer Cell Lines ◽  
Scavenging Activity ◽  
Plant Materials ◽  
Wide Range ◽  
Derivatives Of ◽  
Acyl Derivatives

Quercetin is a flavonoid that is found in many plant materials, including commonly eaten fruits and vegetables. The compound is well known for its wide range of biological activities. In this study, 5-O-acyl derivatives of quercetin were synthesised and assessed for their antiproliferative activity against the HCT116 colon cancer and MDA-MB-231 breast cancer cell lines; and their radical scavenging activity against the 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical species. Four derivatives were found to have improved the antiproliferative activity compared to quercetin whilst retaining radical scavenging activity.

scholarly journals Advances in Phenazines over the Past Decade: Review of Their Pharmacological Activities, Mechanisms of Action, Biosynthetic Pathways and Synthetic Strategies

Marine Drugs ◽  
2021 ◽  
Vol 19 (11) ◽  
pp. 610
Author(s):  
Junjie Yan ◽  
Weiwei Liu ◽  
Jiatong Cai ◽  
Yiming Wang ◽  
Dahong Li ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Pharmacological Activity ◽  
Biological Activities ◽  
Natural Compounds ◽  
Mechanisms Of Action ◽  
Biosynthetic Pathways ◽  
Pharmacological Activities ◽  
Chemical Structures ◽  
The Past ◽  
Synthetic Derivatives

Phenazines are a large group of nitrogen-containing heterocycles, providing diverse chemical structures and various biological activities. Natural phenazines are mainly isolated from marine and terrestrial microorganisms. So far, more than 100 different natural compounds and over 6000 synthetic derivatives have been found and investigated. Many phenazines show great pharmacological activity in various fields, such as antimicrobial, antiparasitic, neuroprotective, insecticidal, anti-inflammatory and anticancer activity. Researchers continued to investigate these compounds and hope to develop them as medicines. Cimmino et al. published a significant review about anticancer activity of phenazines, containing articles from 2000 to 2011. Here, we mainly summarize articles from 2012 to 2021. According to sources of compounds, phenazines were categorized into natural phenazines and synthetic phenazine derivatives in this review. Their pharmacological activities, mechanisms of action, biosynthetic pathways and synthetic strategies were summarized. These may provide guidance for the investigation on phenazines in the future.

scholarly journals Astaxanthin attenuates neurotoxicity in a mouse model of Parkinson’s disease

2017 ◽  
Vol 7 (8) ◽  
pp. 562 ◽  
Author(s):  
B. Grimmig ◽  
L. Daly ◽  
C. Hudson ◽  
K.R. Nash ◽  
P.C. Bickford
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Microglial Activation ◽  
Biological Activities ◽  
Control Diet ◽  
Dietary Supplementation ◽  
Mechanisms Of Action ◽  
Immunohistochemical Detection ◽  
Dopaminergic Cell ◽  
The Central Nervous System

Background: Astaxanthin (AXT) is a natural carotenoid with diverse biological activities. Although it is best known as a potent antioxidant, recent work suggests additional mechanisms of action that have the potential to oppose the ongoing pathophysiology of Parkinson’s disease (PD). For example, AXT has a putative role in modulating microglial activity and preserving mitochondrial function, thereby implicating this compound as a neuroprotective agent. Both oxidative stress and inflammation are involved in the progression of many neurodegenerative diseases. Therefore, we examined the efficacy for AXT to reduced neurotoxicity in a toxic model of PD in mice. Methods: In this study, we used a 4-week dietary supplementation of algae derived AXT to reduce 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) induced dopaminergic cell death.Results: AXT treated mice were protected against the loss of tyrosine hydroxylase (TH) staining in the substantia nigra (SN) after MPTP exposure compared to the control diet. This effect of preserved TH immunoreactivity was also observed in the striatum. Furthermore, AXT administration was able to interrupt the neuroinflammatory process known to contribute to neurodegeneration in this model.Conclusions: We demonstrate that AXT neuroprotection was associated with attenuated microglial activation as indicated by reduced immunohistochemical detection of IBA-1 in the SN and striatum of AXT treated mice. Altogether, these studies suggest that AXT has neuroprotective property in the central nervous system against MPTP neurodegeneration.Keywords: Astaxanthin, Neuroprotection, Neurodegeneration, Neuroinflammation, Parkinson’s disease

Immobilisation on polystyrene of diazirine derivatives of mono- and disaccharides: biological activities of modified surfaces

2001 ◽  
Vol 9 (11) ◽  
pp. 2943-2953 ◽  
Author(s):  
Y Chevolot ◽  
J Martins ◽  
N Milosevic ◽  
D Léonard ◽  
S Zeng ◽  
...  
Keyword(s):  
Biological Activities ◽  
Modified Surfaces ◽  
Derivatives Of

Identification of promising objects for the synthesis of thiosulphonate derivatives of benzoquinone and hydroquinone

2021 ◽  
Vol 4 (2) ◽  
pp. 47-53
Author(s):  
N. Y. Monka ◽  
◽  
N. E. Stadnytska ◽  
I. R. Buchkevych ◽  
K. O. Kaplia ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Experimental Studies ◽  
New Drugs ◽  
Reduced Form ◽  
Free Form ◽  
Wide Range ◽  
On Line ◽  
Living Organisms ◽  
Derivatives Of

Benzoquinone and its reduced form hydroquinone belong to phenolic compounds and are found in living organisms in free form or in glycosides. They are active substances of some medicinal plants and have a pharmacological effect on the human body. Accordingly, their derivatives are important objects for chemical synthesis and development of new drugs. This article presents the findings of the structural design of substances with benzoquinone or hydroquinone fragment and sulfur-containing compound. By use of appropriate on-line programs a predictive screening of the biological activity and cytotoxicity of thiosulfonate derivatives of benzoquinone and hydroquinone has been conducted. It has been found that they have immense methodological potential to be synthesized by substances with a wide range of biological activities and a high value of probable activity, which substantiates the feasibility of conducting experimental studies on their biological activity, particularly anticancer.

Therapeutic Journey of Andrographis paniculata (Burm.f.) Nees from Natural to Synthetic and Nanoformulations

2021 ◽  
Vol 21 ◽  
Author(s):  
Sharuti Mehta ◽  
Anil Kumar Sharma ◽  
Rajesh K. Singh
Keyword(s):  
Biological Activities ◽  
Andrographis Paniculata ◽  
Herbaceous Plant ◽  
Target Tissue ◽  
Active Components ◽  
Essential Information ◽  
Compound Plant ◽  
Therapeutic Activities ◽  
Synthetic Derivatives ◽  
Derivatives Of

: Andrographis paniculata (Burm.f.) Nees (Acanthaceae) is a herbaceous plant and commonly called 'King of Bitters'. It has gained attraction as a potential hepatoprotective agent and a natural molecule with various biological activities viz. anticancer, immunomodulatory, anti-inflammatory, antibacterial, neuroprotective, and so on. The andrographolide is one of the main diterpenoids responsible for the drug's bitter taste and various therapeutic activities. The poor cellular permeability, solubility and short biological half-life of its pure components limit its distribution to the target tissue. To conquer this obstacle, various researchers worldwide have been working on designing the synthetic derivatives of its active components and nanoformulations to improve the drug's efficiency and selectivity to develop more active leads for biomedical applications. This article discussed the recent research on synthetic derivatives, including their possible therapeutic applications and structure-activity relationship (SAR). Additionally, this article also presents the essential information concerning the various nanoformulations developed to increase the delivery of pure compound/plant extract to the target site, thereby improving the drug's efficacy for multiple ailments.

scholarly journals PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS

2017 ◽  
Vol 10 (6) ◽  
pp. 237 ◽  
Author(s):  
Ishwar Bhat K ◽  
Abhishek Kumar
Keyword(s):  
Acetic Acid ◽  
Cytotoxic Activity ◽  
Glacial Acetic Acid ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agents

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