Synthetic analogues of memantine as neuroprotective and influenza viral inhibitors: in vitro and physicochemical studies

Amino Acids ◽  
2020 ◽  
Vol 52 (11-12) ◽  
pp. 1559-1580
Author(s):  
Aleksandra Tencheva ◽  
Rui Liu ◽  
Tatyana V. Volkova ◽  
Radoslav Chayrov ◽  
Yavor Mitrev ◽  
...  
Keyword(s):  
Synthetic Analogues ◽  
Physicochemical Studies ◽  
Viral Inhibitors

scholarly journals Ferulic Acid-NLC with Lavandula Essential Oil: A Possible Strategy for Wound-Healing?

Nanomaterials ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 898 ◽  
Author(s):  
Claudia Carbone ◽  
Carla Caddeo ◽  
Maria Aurora Grimaudo ◽  
Daniela Erminia Manno ◽  
Antonio Serra ◽  
...  
Keyword(s):  
Wound Healing ◽  
Ferulic Acid ◽  
Isopropyl Myristate ◽  
Beneficial Effects ◽  
Physicochemical Studies ◽  
Nanoparticles Stability ◽  
And Migration ◽  
Treatment Of Wounds ◽  
Drug Solution

Nowadays, an increasing interest in combinatorial drug delivery systems is emerging, highlighting the possibility of exploiting essential oils (EO) for topical applications. This work aimed at developing nanostructured lipid carriers (NLC) for the combined delivery of ferulic acid and Lavandula EO, whose beneficial effects in wound-healing processes have been widely reported. Homogeneous (polydispersity index, PDI < 0.2) nanoparticles with a small size (<150 nm) and a high encapsulation efficiency (>85%) were obtained. The co-presence of ferulic acid and Lavandula EO, as compared to synthetic isopropyl myristate-based NLC, increased nanoparticles’ stability, due to higher ordering chains, as confirmed by morphological and physicochemical studies. An enhanced cytocompatibility was observed when combining ferulic acid and Lavandula EO, as confirmed by in vitro studies on fibroblasts. Furthermore, the combined delivery of ferulic acid and Lavandula EO significantly promoted cell migration with higher effectiveness in respect to the free drug solution and the carrier without the EO. Taken all together, our results suggest a potential combined effect of the antioxidant ferulic acid and Lavandula EO co-delivered in lipid nanoparticles in promoting cell proliferation and migration, representing a promising strategy in the treatment of wounds.

Heparin-Induced Thrombocytopenia Platelet Aggregation Studies in the Presence of Heparin Fractions or Semi-Synthetic Analogues of Various Molecular Weights and Anticoagulant Activities

1986 ◽  
Vol 55 (01) ◽  
pp. 090-093 ◽  
Author(s):  
D Blockmans ◽  
H Bounameaux ◽  
J Vermylen ◽  
M Verstraete
Keyword(s):  
Molecular Weight ◽  
Platelet Aggregation ◽  
Platelet Rich Plasma ◽  
Anticoagulant Activity ◽  
Lag Phase ◽  
Synthetic Analogues ◽  
Heparin Induced Thrombocytopenia ◽  
Molecular Weights ◽  
Induced Aggregation

SummaryOne case of heparin-induced thrombocytopenia is reported. Aggregation was observed in the platelet-rich plasma of this patient in the presence of two commercial standard heparin preparations (from a final concentration of 0.025 IU/ml upwards), of two semi-synthetic heparin analogues (0.1 APTT U/ml) and of three low-molecular weight heparin (LMWH) fractions (0.1 anti-Xa U/ml) but not in the presence of five other LMWH fractions.The patient’s isolated platelets no longer aggregated in the presence of heparin but the phenomenon recurred after addition of the patient’s platelet poor plasma (PPP).Furthermore, addition of patient’s PPP to control platelets led to heparin-induced aggregation.The phenomenon was associated with thromboxane generation and could be blocked by in vitro addition of aspirin, PGI2, and PGD2 whereas the lag phase was dose-dependently prolonged by adenosine.It is concluded that platelet aggregation may be induced in some patients by standard heparin and by certain LMWH fractions or semi-synthetic analogues, independently of their molecular weight and anticoagulant activity.

In vitro antifungal evaluation and structure-activity relationship of diphenyl diselenide and synthetic analogues

Mycoses ◽  
2011 ◽  
Vol 54 (5) ◽  
pp. e572-e576 ◽  
Author(s):  
Érico Silva Loreto ◽  
Débora Alves Nunes Mario ◽  
Janio Morais Santurio ◽  
Sydney Hartz Alves ◽  
Cristina Wayne Nogueira ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Diphenyl Diselenide ◽  
Synthetic Analogues ◽  
Structure Activity ◽  
Relationship Of

Fungicidal properties, sterol binding, and proteolytic resistance of the synthetic peptide D4E1

1998 ◽  
Vol 44 (6) ◽  
pp. 514-520 ◽  
Author(s):  
A J De Lucca ◽  
J M Bland ◽  
C Grimm ◽  
T J Jacks ◽  
J W Cary ◽  
...  
Keyword(s):  
Synthetic Peptide ◽  
Fusarium Spp ◽  
Transgenic Expression ◽  
Cecropin A ◽  
Proteolytic Resistance ◽  
Plant Protease ◽  
Physicochemical Studies ◽  
Natural Peptide ◽  
Protease Degradation

The fungicidal properties of the synthetic peptide D4E1 were studied with nongerminated and germinating conidia of Aspergillus flavus, Aspergillus fumigatus, Aspergillus niger, Fusarium moniliforme, and Fusarium oxysporum. The minimal lethal concentrations (MLC) needed to kill 100% of germinating conidia ofA. fumigatus, A. flavus, and A. niger were 12.5, 12.5, and 25 µM, respectively. The MLC value for nongerminated and germinating conidia of both Fusarium spp. was 3.0 µM. Except for A. fumigatus, D4E1 was inactive against the nongerminated conidia of the Aspergillus spp. Physicochemical studies showed D4E1 complexed with ergosterol, a sterol present in conidial walls. Cholesterol, present in nongerminated conidia of F. moniliforme, had a greater affinity for D4E1 than did ergosterol. D4E1 was more resistant to fungal and plant protease degradation than the natural peptide, cecropin A. These in vitro results suggest D4E1 is a candidate for transgenic expression in plants to enhance host resistance to fungal infection.Key words: peptides, fungicidal, Aspergillus spp., Fusarium spp., sterols.

Physicochemical studies using amylose as an in vitro model for resistant starch

1995 ◽  
Vol 21 (1) ◽  
pp. 37-47 ◽  
Author(s):  
P. Cairns ◽  
L. Sun ◽  
V.J. Morris ◽  
S.G. Ring
Keyword(s):  
Resistant Starch ◽  
In Vitro Model ◽  
Physicochemical Studies ◽  
Vitro Model

scholarly journals The supramolecular structure is decisive for the immunostimulatory properties of synthetic analogues of a mycobacterial lipid in vitro

RSC Advances ◽  
2013 ◽  
Vol 3 (43) ◽  
pp. 20673-20683 ◽  
Author(s):  
Birte Martin-Bertelsen ◽  
Karen Smith Korsholm ◽  
Fabrice Rose ◽  
Pernille Nordly ◽  
Henrik Franzyk ◽  
...  
Keyword(s):  
Supramolecular Structure ◽  
Synthetic Analogues

scholarly journals Synthesis, Physicochemical Studies and Biological Properties of Mixed-Ligand Nickel(II) Complexes Containing β-Diketones With N-donor Ligands

2018 ◽  
Vol 10 (4) ◽  
pp. 11
Author(s):  
Helen Oluwatola Omoregie
Keyword(s):  
Conductivity Measurement ◽  
Antimicrobial Activities ◽  
Biological Properties ◽  
Molar Conductance ◽  
Bidentate Ligand ◽  
Mixed Ligand ◽  
Donor Ligands ◽  
Spectral Measurements ◽  
Physicochemical Studies

Some mixed ligand nickel(II) complexes of thenoyltrifluoroacetone (tta-H) with 2,2ꞌ-bipyridine (bipy), 1,10-phenanthroline (phen) and tetramethylethylenediamine (tmen) [Ni(tta)(N-N)(NO3)]; N-N= bipy, phen, or tmen] have been synthesized and characterized by molar conductance measurements, elemental analysis, mass spectrometry, spectral measurements and antimicrobial activities. Attempt to prepare the mixed ligand nickel(II) complexes containing acetylacetone (acacH), benzoylacetone (bzacH), dibenzoylmethane (dbm-H) and thenoyltrifluoroacetone (tta-H) with ethylenediamine associated with NO3 counter ion led to the formation of [Ni(&beta;-diketone)2en]. The &beta;-diketones enolized acting as bidentate ligand, coordinating to the metal with carbonyl and enolic oxygen, ethylenediamine (en) coordinates to the metal using N, N chromophores. The nickel complexes of the type [Ni(tta)(N-N)NO3)] are five-coordinate square pyramidal in geometry while those of the type [Ni(&beta;-diketone)2en] are six-coordinate octahedral geometry. The conductivity measurement in nitromethane revealed that the [Ni(tta)(N-N)NO3)] complexes are non-electrolyte. The complexes were screened for their in-vitro antimicrobial activity against six microorganisms. A comparison of the complexes with gentamicin showed that most of the complexes are resistant to tested organisms except [Ni(tta)2(en)].H2O, [Ni(bzac)2(en)] and [Ni(bta)2(en)] which compared favourably well in Staphylococcus aureus.

scholarly journals The influence of chromone based hydrazones on lipid peroxidation and bFGF concentration in the HL-60 cell line.

2013 ◽  
Vol 60 (2) ◽  
Author(s):  
Andrzej Łazarenkow ◽  
Marta Michalska ◽  
Anna Gorąca ◽  
Marek Mirowski ◽  
Jolanta Nawrot-Modranka ◽  
...  
Keyword(s):  
Lipid Peroxidation ◽  
Cell Line ◽  
Significant Influence ◽  
Biological Properties ◽  
Synthetic Analogues ◽  
Wide Range ◽  
Synthetic Derivatives ◽  
Derivatives Of

Natural and synthetic derivatives of benzo-γ-pyrones (i.e. flavones, chromones, and coumarins) and their synthetic analogues possess a wide range of biological properties in vitro and in vivo. In this paper we investigated the influence of two hydrazone compounds of chromones, 3-{[(2-dimethoxytiophosphoryl)-2-methylhydrazono]-methyl}-chromen-4-one (CH-3) and 2-amino-6-chloro-3-[(2-hydroxyethyl)-hydrazonomethyl]-chromen-4-one (A-12), on lipid peroxidation and bFGF concentration in the HL-60 cells. Both of the studied compounds had a significant influence on bFGF and TBARS in ranges -137.20 ~ 380.26% and -81.66 ~ -28.68%, respectively, in comparison with the control (counted as 0%).

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