scholarly journals Phenolic constituents from twigs of Aleurites fordii and their biological activities

2021 ◽  
Vol 17 ◽  
pp. 2329-2339
Author(s):  
Kyoung Jin Park ◽  
Won Se Suh ◽  
Da Hye Yoon ◽  
Chung Sub Kim ◽  
Sun Yeou Kim ◽  
...  
Keyword(s):  
Biological Activities ◽  
Structural Elucidation ◽  
Phenolic Glycoside ◽  
Chemical Methods ◽  
Phenolic Constituents ◽  
New Compounds

Three new neolignan glycosides (1–3), a new phenolic glycoside (15), and a new cyanoglycoside (16) were isolated and characterized from the twigs of Aleurites fordii together with 14 known analogues (4–14 and 17–19). The structural elucidation of the new compounds was performed through the analysis of their NMR, HRMS, and ECD spectra and by chemical methods. All isolated compounds were tested for their antineuroinflammatory and neuroprotective activities.

A common mechanism links activities of butyrate in the colon

2017 ◽  
Author(s):  
Mohit S. Verma ◽  
Michael J. Fink ◽  
Gabriel L Salmon ◽  
Nadine Fornelos ◽  
Takahiro E. Ohara ◽  
...  
Keyword(s):  
Stem Cells ◽  
Histone Deacetylases ◽  
Biological Activities ◽  
Short Chain Fatty Acids ◽  
Common Mechanism ◽  
Epithelial Stem Cells ◽  
Degree Of Unsaturation ◽  
Structure Activity ◽  
Starting Point ◽  
New Compounds

Two biological activities of butyrate in the colon (suppression of proliferation of colonic epithelial stem cells and inflammation) correlate with inhibition of histone deacetylases. Cellular and biochemical studies of molecules similar in structure to butyrate, but different in molecular details (functional groups, chain-length, deuteration, oxidation level, fluorination, or degree of unsaturation) demonstrated that these activities were sensitive to molecular structure, and were compatible with the hypothesis that butyrate acts by binding to the Zn<sup>2+</sup> in the catalytic site of histone deacetylases. Structure-activity relationships drawn from a set of 36 compounds offer a starting point for the design of new compounds targeting the inhibition of histone deacetylases. The observation that butyrate was more potent than other short-chain fatty acids is compatible with the hypothesis that crypts evolved (at least in part), to separate stem cells at the base of crypts from butyrate produced by commensal bacteria.

Click Reactions in Chemistry of Triterpenes - Advances Towards Development of Potential Therapeutics

2018 ◽  
Vol 25 (5) ◽  
pp. 636-658 ◽  
Author(s):  
Jan Pokorny ◽  
Lucie Borkova ◽  
Milan Urban
Keyword(s):  
Biological Activities ◽  
Synthetic Approach ◽  
Clinical Use ◽  
New Approach ◽  
Click Reactions ◽  
Drug Candidates ◽  
The Past ◽  
Low Toxicity ◽  
New Compounds ◽  
Potential Therapeutics

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.

A Mini Review on the Chemical Synthesis of Resveratrol

2020 ◽  
Vol 17 (5) ◽  
pp. 546-558
Author(s):  
Hong Huang ◽  
Ruonan Liu ◽  
Wenhua Ou
Keyword(s):  
Cardiovascular Disease ◽  
Chemical Synthesis ◽  
Neurodegenerative Diseases ◽  
Biological Activities ◽  
Polyphenolic Compound ◽  
Chemical Methods

Resveratrol is a polyphenolic compound and has been shown to possess numerous biological activities, which could possibly be applied to the prevention and/or treatment of cancer, cardiovascular disease, and neurodegenerative diseases. This review summarizes the progress of different chemical methods in the preparation of resveratrol.

scholarly journals Phytochemistry and Biological Activities of Iris Species Growing in Iraqi Kurdistan and Phenolic Constituents of the Traditional Plant Iris postii

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 264
Author(s):  
Hawraz Ibrahim M. Amin ◽  
Faiq H. S. Hussain ◽  
Soran K. Najmaldin ◽  
Zaw Min Thu ◽  
Mohammed Farhad Ibrahim ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Chromatographic Separations ◽  
Traditional Use ◽  
Methanolic Extracts ◽  
Aerial Parts ◽  
Traditional Remedies ◽  
Phenolic Constituents ◽  
Total Antioxidant

A dozen Iris species (Iridaceae) are considered traditional remedies in Kurdistan, especially for treating inflammations. Phytochemical studies are still scarce. The information reported in the literature about Iris species growing in Kurdistan has been summarized in the first part of this paper, although, except for Iris persica, investigations have been performed on vegetal samples collected in countries different from Kurdistan. In the second part of the work, we have investigated, for the first time, the contents of the methanolic extracts of Iris postii aerial parts and rhizomes that were collected in Kurdistan. Both extracts exhibited a significant dose-dependent free radical scavenging and total antioxidant activities, comparable to those of ascorbic acid. Medium-pressure liquid chromatographic separations of the two extracts afforded l-tryptophan, androsin, isovitexin, swertisin, and 2″-O-α-l-rhamnopyranosyl swertisin from the aerial parts, whereas ε-viniferin, trans-resveratrol 3,4′-O-di-β-d-glucopyranoside, and isotectorigenin were isolated from the rhizomes. This is the first finding of the last three metabolites from an Iris species. The various remarkable biological activities of isolated compounds scientifically sustain the traditional use of I. postii as a medicinal plant.

scholarly journals Recent Findings in Azaphilone Pigments

2021 ◽  
Vol 7 (7) ◽  
pp. 541
Author(s):  
Lúcia P. S. Pimenta ◽  
Dhionne C. Gomes ◽  
Patrícia G. Cardoso ◽  
Jacqueline A. Takahashi
Keyword(s):  
Water Solubility ◽  
Biological Activities ◽  
Low Cost ◽  
Scale Up ◽  
Structural Diversity ◽  
Downstream Processing ◽  
Global Market ◽  
Yield Improvement ◽  
Potential Applications ◽  
New Compounds

Filamentous fungi are known to biosynthesize an extraordinary range of azaphilones pigments with structural diversity and advantages over vegetal-derived colored natural products such agile and simple cultivation in the lab, acceptance of low-cost substrates, speed yield improvement, and ease of downstream processing. Modern genetic engineering allows industrial production, providing pigments with higher thermostability, water-solubility, and promising bioactivities combined with ecological functions. This review, covering the literature from 2020 onwards, focuses on the state-of-the-art of azaphilone dyes, the global market scenario, new compounds isolated in the period with respective biological activities, and biosynthetic pathways. Furthermore, we discussed the innovations of azaphilone cultivation and extraction techniques, as well as in yield improvement and scale-up. Potential applications in the food, cosmetic, pharmaceutical, and textile industries were also explored.

scholarly journals Novel silver(I) compounds with 1-adamantanamine

2018 ◽  
Vol 83 (6) ◽  
pp. 699-705 ◽  
Author(s):  
Dejan Jeremic ◽  
Milena Djordjevic ◽  
Srdjan Miletic ◽  
Ljubica Andjelkovic ◽  
Dusan Sladic ◽  
...  
Keyword(s):  
Electron Donor ◽  
Aliphatic Amine ◽  
Biological Activities ◽  
Spectroscopic Characterization ◽  
Antibacterial Activities ◽  
Monodentate Ligand ◽  
Donor Ligand ◽  
Minimum Inhibitory Concentrations ◽  
New Compounds

In this work, three novel silver(I) complexes with an almost completely rigid and bulky monodentate ligand, 1-adamantanamine, were synthesized. The aliphatic amine, 1-adamantanamine, is the sole electron donor ligand in these complexes. In addition to spectroscopic characterization, the basic biological activities of the new compounds were investigated and their minimum inhibitory concentrations were determined. The antifungal and antibacterial activities indicate that these compounds could potentially be applied as new therapeutics.

scholarly journals Salvia officinalis, Rosmarinic and Caffeic Acids Attenuate Neuropathic Pain and Improve Function Recovery after Sciatic Nerve Chronic Constriction in Mice

2019 ◽  
Vol 2019 ◽  
pp. 1-17 ◽  
Author(s):  
Zineb El Gabbas ◽  
Kenza Bezza ◽  
Jawad Laadraoui ◽  
Mehdi Ait Laaradia ◽  
Aaziz Kebbou ◽  
...  
Keyword(s):  
Neuropathic Pain ◽  
Sciatic Nerve ◽  
Functional Recovery ◽  
Thermal Sensation ◽  
Biological Activities ◽  
Hematological Parameters ◽  
Thermal Hyperalgesia ◽  
Salvia Officinalis ◽  
Histopathological Analysis ◽  
Phenolic Constituents

The leaves of Salvia officinalis L. have a traditional reputation for the management of pain in Morocco. This study was conducted to investigate the curative effects of Salvia officinalis (SO) and its major constituents Rosmarinic (ROS) and Caffeic acids (CAF) on peripheral neuropathic pain in mice. Chronic constriction injury (CCI) was induced in mice, and neuropathic pain behaviors tests were evaluated by mechanical, chemical, thermal sensation tests and functional recovery of the sciatic nerve at different time intervals, i.e., (day 0, 1, 7, 14, and 21). Ethanolic extract of SO (100 and 200 mg/kg, p.o.), ROS (10 and 20 mg/kg, i.p.), CAF (30 and 40 mg/kg, i.p.), and CLOM (5 mg/kg, i.p., a positive control) was given for 21 days after surgery. Hematological and biochemical parameters were also measured as well as histopathological analysis. CCI produced significant development in mechanical and thermal hyperalgesia, cold allodynia, and rise in the sciatic functional index in mice. Chronic treatments with SO extract, ROS, CAF, and CLOM for 3 weeks significantly increased mechanical sensibility, cold, and thermal withdrawal latency and enhanced functional recovery of the injured nerve. The same treatments remarkably ameliorated hematological parameters and did not alter biochemical levels. The histopathological findings had revealed the protective effect of SO, ROS, and CAF against the CCI-induced damage. Our data support the use of SO in folk medicine to alleviate pain. Their main phenolic constituents could be promising antineuropathic compounds, which may be attributed to their biological activities including anti-inflammatory, antioxidant, and neuroprotective effects. SO leaves may be a good candidate to treat neuropathic pain.

scholarly journals Haematoxylon campechianum Extract Ameliorates Neuropathic Pain via Inhibition of NF-κB/TNF-α/NOX/iNOS Signalling Pathway in a Rat Model of Chronic Constriction Injury

Biomolecules ◽  
2020 ◽  
Vol 10 (3) ◽  
pp. 386 ◽  
Author(s):  
Mansour Sobeh ◽  
Mona F. Mahmoud ◽  
Samar Rezq ◽  
Mohamed A.O. Abdelfattah ◽  
Islam Mostafa ◽  
...  
Keyword(s):  
Neuropathic Pain ◽  
Sciatic Nerve ◽  
Brain Stem ◽  
Rat Model ◽  
Structural Changes ◽  
Chronic Constriction Injury ◽  
Biological Activities ◽  
Ethanol Extract ◽  
Phenolic Constituents ◽  
Anti Inflammatory

In this study, the phytochemical composition and the possible prophylactic effects of an aqueous ethanol extract of Haematoxylon campechianum flowers (HCF) on peripheral neuropathic pain in a chronic constriction injury (CCI) rat model are investigated. Rats with induced CCI were subjected to neuropathic pain behaviour tests and evaluated by chemical, thermal, and mechanical sensation tests and functional recovery of the brain stem and sciatic nerve at 7- and 14-day intervals. The effect of the extract on acute pain and inflammation is also investigated. The extract exerted both peripheral and central analgesic and anti-inflammatory properties in addition to antipyretic effects that are clear from targeting COX, LOX and PGE. It was found that CCI produced significant thermal and mechanical hyperalgesia, cold allodynia and deleterious structural changes in both sciatic nerve and brain stem. Treatments with HCF extract significantly improved cold and thermal withdrawal latency, mechanical sensibility and ameliorated deleterious changes of sciatic nerve and brain stem at different dose levels. The extract also ameliorated oxidative stress and inflammatory markers in brain stem and sciatic nerve. It suppressed the apoptotic marker, p53, and restored myelin sheath integrity. The effects of HCF extract were more potent than pregabalin. Fifteen secondary metabolites, mainly gallotannins and flavonoids, were characterized in the extract based on their retention times and MS/MS data. The identified phenolic constituents from the extract could be promising candidates to treat neuropathic pain due to their diverse biological activities, including antioxidant, anti-inflammatory and neuroprotective properties.

Four New Compounds from the Australian Brown Alga Cystophora brownii

1998 ◽  
Vol 51 (12) ◽  
pp. 1157 ◽  
Author(s):  
Baohong Bian ◽  
Ian A. van Altena
Keyword(s):  
Brown Alga ◽  
Two Dimensional ◽  
Chemical Methods ◽  
New Compounds

Two new steroids, (20S)-3β,20-dihydroxyergosta-5,24(28)-dien-16-one (7) and 3β-hydroxyergosta-5,24(28)-dien-16-one (9), and two new diastereoisomeric meroditerpenes, compounds (10) and (11), † have been isolated from the brown alga Cystophora brownii (Cystoseiraceae). Their structures were elucidated by one- and two-dimensional n.m.r. and other spectrometric and chemical methods.

scholarly journals Cytochalasins from Xylaria sp. CFL5, an Endophytic Fungus of Cephalotaxus fortunei

2020 ◽  
Author(s):  
Kai-Liang Ma ◽  
Shi-Hui Dong ◽  
Hang-Ying Li ◽  
Wen-Jun Wei ◽  
Yong-Qiang Tu ◽  
...  
Keyword(s):  
Endophytic Fungus ◽  
Spectroscopic Data ◽  
Biological Activities ◽  
Optical Rotation ◽  
Ags Cells ◽  
Mhc Ii ◽  
Chemical Structures ◽  
Data Analyses ◽  
Binding Inhibition ◽  
New Compounds

Abstract Three previously undescribed cytochalasins, named xylariasins A‒C (1‒3), together with six known ones (4‒9) were isolated from Xylaria sp. CFL5, an endophytic fungus of Cephalotaxus fortunei. The chemical structures of all new compounds were elucidated on the basis of extensive spectroscopic data analyses and electronic circular dichroism calculation, as well as optical rotation calculation. Biological activities of compounds 1, 4‒9 were evaluated, including cytotoxic, LAG3/MHC II binding inhibition and LAG3/FGL1 binding inhibition activities. Compounds 6 and 9 possessed cytotoxicity against AGS cells at 5 μM, with inhibition rates of 94% and 64%, respectively. In addition, all tested isolates, except compound 6, exhibited obvious inhibitory activity against the interaction of both LAG3/MHC II and LAG3/FGL1. Compounds 1, 5, 7, and 8 inhibited LAG3/MHC II with IC50 values ranging from 2.37 to 4.74 μM. Meanwhile, the IC50 values of compounds 1, 7, and 8 against LAG3/FGL1 were 11.78, 4.39, and 7.45 μM, respectively. Graphic Abstract

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