scholarly journals Synthesis and In Vitro Evaluation of Caffeoylquinic Acid Derivatives as Potential Hypolipidemic Agents

Molecules ◽  
2019 ◽  
Vol 24 (5) ◽  
pp. 964 ◽  
Author(s):  
Yu Tian ◽  
Xiao-Xue Cao ◽  
Hai Shang ◽  
Chong-Ming Wu ◽  
Xi Zhang ◽  
...  
Keyword(s):  
Oleic Acid ◽  
Chlorogenic Acid ◽  
Positive Control ◽  
Biological Evaluation ◽  
Lipid Lowering ◽  
Caffeoylquinic Acid ◽  
Hypolipidemic Agents ◽  
Derivatives Of ◽  
Lipid Lowering Effect

A series of novel caffeoylquinic acid derivatives of chlorogenic acid have been designed and synthesized. Biological evaluation indicated that several synthesized derivatives exhibited moderate to good lipid-lowering effects on oleic acid-elicited lipid accumulation in HepG2 liver cells. Particularly, derivatives 3d, 3g, 4c and 4d exhibited more potential lipid-lowering effect than the positive control simvastatin and chlorogenic acid. Further studies on the mechanism of 3d, 3g, 4c and 4d revealed that the lipid-lowering effects were related to their regulation of TG levels and merit further investigation.

scholarly journals Antioxidant Capacity of Proteins and Hydrolysates from the Liver of Newborn Piglets, and Their Inhibitory Effects on Steatosis in vitro

2020 ◽  
Vol 58 (4) ◽  
Author(s):  
Ruilin Zhang ◽  
Lasheng Yin ◽  
Jian Chen ◽  
Xuewu Zhang
Keyword(s):  
Oleic Acid ◽  
Hepg2 Cells ◽  
Early Stage ◽  
Lipid Lowering ◽  
Inhibitory Effects ◽  
Hepatic Disorder ◽  
Newborn Piglets ◽  
End Stage ◽  
Lipid Lowering Effect

Research background. Non-alcoholic steatohepatitis is a potentially progressive hepatic disorder that can lead to end-stage liver disease and hepatocellular carcinoma. The inhibitory effects of proteins and hydrolysates from the liver of newborn piglets on hepatic steatosis in oleic-acid-induced HepG2 cells were investigated in vitro. Experimental approach. The extracted proteins from the liver of newborn piglets (NPLP) were hydrolysed with papain, pepsin, trypsin and Alcalase. Based on comparison of different enzyme digestion condition, a protein hydrolysis protocol was established to obtain hydrolysates with lipid-lowering effect. Results and conclusions. NPLH-trypsin (trypsin-digested NPLP hydrolysate) exhibited strong antioxidant activity and possessed good inhibitory effects on lipogenesis and cholesterol accumulation in HepG2 cells at 150 μg/mL, with a triglyceride decrease of (43±3) % and cholesterol decrease of (31±5) %, comparing with 0.75 mM oleic acid induced model. The addition of NPLH-trypsin (300 μg/mL) decreased alanine aminotransferase and aspartate aminotransferase activities and increased superoxide dismutase activity. Novelty and scientific contribution. This study demonstrated that NPLH-trypsin have a potential preventive effect on NAFLD in its early stage, and NPLH-trypsin has potential use as the modulator of lipid overaccumulation disease in food supplements.

Design and synthesis of herboxidiene derivatives that potently inhibit in vitro splicing

2021 ◽  
Vol 19 (6) ◽  
pp. 1365-1377
Author(s):  
Arun K. Ghosh ◽  
Srinivasa Rao Allu ◽  
Guddeti Chandrashekar Reddy ◽  
Adriana Gamboa Lopez ◽  
Patricia Mendez ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design And Synthesis ◽  
In Vitro Splicing ◽  
Enantioselective Syntheses ◽  
Derivatives Of

Enantioselective syntheses of C-6 modified derivatives of herboxidiene and their biological evaluation in splicing inhibitory assay.

Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]

2017 ◽  
Vol 46 (21) ◽  
pp. 7005-7019 ◽  
Author(s):  
Benjamin W. J. Harper ◽  
Emanuele Petruzzella ◽  
Roman Sirota ◽  
Fernanda Fabiola Faccioli ◽  
Janice R. Aldrich-Wright ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Synthesis and biological evaluation in vitro and in vivo of functionalized Pt(iv) derivatives of Pt56MeSS.

scholarly journals Novel Ester and Acid Derivatives of the 1,5-Diarylpyrrole Scaffold as Anti-Inflammatory and Analgesic Agents. Synthesis and in Vitro and in Vivo Biological Evaluation

2010 ◽  
Vol 53 (2) ◽  
pp. 723-733 ◽  
Author(s):  
Mariangela Biava ◽  
Giulio C. Porretta ◽  
Giovanna Poce ◽  
Claudio Battilocchio ◽  
Fabrizio Manetti ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Analgesic Agents ◽  
Anti Inflammatory ◽  
Derivatives Of

Synthesis and Biological Evaluation of Novel 4-Phenylaminobenzofuro[2,3-d]pyrimidine Derivatives

2020 ◽  
Vol 42 (4) ◽  
pp. 564-564
Author(s):  
Ju liu Ju liu ◽  
Jun Li Jun Li ◽  
Jian tao Shi Jian tao Shi ◽  
Jie Li Jie Li ◽  
Xue chen Hao Xue chen Hao ◽  
...  
Keyword(s):  
Cell Lines ◽  
A549 Cells ◽  
Positive Control ◽  
Biological Evaluation ◽  
Dependent Manner ◽  
Pyrimidine Derivatives ◽  
Concentration Dependent Manner ◽  
Ic50 Value ◽  
Synthesis And Biological Evaluation

A series of novel 4-phenylaminobenzofuro[2,3-d]pyrimidine derivatives had been prepared and assessed for their in vitro antiproliferative activities against three lung cancer cell lines (A549, H460 and H1975). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activities. Among them, compound 8f exhibited remarkable inhibitory activity against A549 and H460 cell lines with IC50 value of 2.54 μM and 2.68 μM, respectively, which was comparable to that of the positive control sorafenib (IC50 = 2.69 μM for A549 and 3.71 μM for H460). AO/EB staining suggests that compound 8f could induce apoptosis in A549 cells. Furthermore, cell cycle analyses show that compound 8f increased G0/G1 A549 cells arrest in a concentration-dependent manner. The preliminary structure-activity relationships (SARs) studies indicated that mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring are positive on the antitumor activity.

scholarly journals 2-Amino-4-arylthiazole Derivatives as Anti-giardial Agents: Synthesis, Biological Evaluation and QSAR Studies

2015 ◽  
Vol 13 (1) ◽  
Author(s):  
Raul Mocelo-Castell ◽  
Carlos Villanueva-Novelo ◽  
David Cáceres-Castillo ◽  
Ruben M. Carballo ◽  
Ramiro F. Quijano-Quiñones ◽  
...  
Keyword(s):  
Positive Control ◽  
Biological Evaluation ◽  
Toxicity Tests ◽  
Data Set ◽  
Qsar Analysis ◽  
Qsar Studies ◽  
Modified Method ◽  
Acute Toxicity Tests ◽  
Low Toxicity

AbstractA series of seven 2-amino-4-arylthiazoles were prepared following Hantzsch’s modified method under microwave irradiation. A set of 50 derivatives was obtained and the in vitro activity against Giardia intestinalis was evaluated. The results on the biological activity revealed that, in general, the N-(5-bromo-4-aryl-thiazol-2-yl)-acetamide scaffold showed high bioactivity. In particular, compounds 6e (IC50 = 0.39 μM) and 6b (IC50 = 0.87 μM) were found to be more potent than the positive control metronidazole. Citoxicity and acute toxicity tests performed showed low toxicity and high selectivity of the most active compounds (6e SI = 139, 6b SI = 52.3). A QSAR analysis was applied to a data set of 37 obtained 2-amino-4-arylthiazoles derivatives and the best model described a strongly correlation between the anti-giardiasic activity and molecular descriptors as E2M, RDF115m, F10, MATS6v, and Hypnotic-80, with high statistical quality. This finding indicates that N-substituted aminothiazole scaffold should be investigated for the development of highly selective anti-giardial agent.

scholarly journals Phytochemical Characterization and Bioactive Properties of Cinnamon Basil (Ocimum basilicum cv. ‘Cinnamon’) and Lemon Basil (Ocimum × citriodorum)

Antioxidants ◽  
2020 ◽  
Vol 9 (5) ◽  
pp. 369 ◽  
Author(s):  
Chaimae Majdi ◽  
Carla Pereira ◽  
Maria Inês Dias ◽  
Ricardo C. Calhelha ◽  
Maria José Alves ◽  
...  
Keyword(s):  
Thiobarbituric Acid ◽  
Positive Control ◽  
Thiobarbituric Acid Reactive Substances ◽  
Oxidative Hemolysis ◽  
Gram Positive Bacteria ◽  
Bioactive Properties ◽  
Anti Inflammatory ◽  
Hydroethanolic Extract ◽  
Derivatives Of

The aim of this work was to contribute to the knowledge on the chemical composition and bioactive properties of two species of the Ocimum genus, namely O. basilicum cultivar ’Cinammon’ and O. × citriodorum. For this purpose, samples of these plants grown in Portugal were evaluated for their composition in phenolic and volatile compounds, and the infusion and hydroethanolic extracts were assessed for their in vitro antioxidant, antimicrobial, cytotoxic, and anti-inflammatory activities. In total, the two basil samples showed the presence of seven caffeic acid and derivatives (dimers, trimers, and tetramers) and five flavonoids, mainly glycoside derivatives of quercetin. Despite some qualitative and quantitative differences, in both samples rosmarinic acid was the major phenolic compound, and linalool the predominant volatile compound. In general, the tested extracts provided relevant bioactive properties since both basil species showed higher antioxidant activity in Thiobarbituric Acid Reactive Substances (TBARs) and Oxidative Hemolysis Inhibition (OxHLIA) assays when compared with the positive control Trolox. Despite O. × citriodorum extracts showing slightly better activity against some strains, both types of extracts evidenced similar antimicrobial activity, being more active against Gram-positive bacteria. The extracts also revealed interesting cytotoxicity, particularly the O. × citriodorum hydroethanolic extract which was also the only one exhibiting anti-inflammatory activity.

Study on the Lipid-Lowering Effect of Water-Soluble Chitosan Nanoparticles and Microspheres In Vitro

2011 ◽  
Vol 217-218 ◽  
pp. 306-310 ◽  
Author(s):  
Bing Gao ◽  
Si Hui Wu ◽  
Hong Liang Zhang ◽  
Yi Tao ◽  
Zheng Quan Su
Keyword(s):  
Binding Capacity ◽  
Food Additives ◽  
Chitosan Nanoparticles ◽  
Water Soluble ◽  
Lipid Lowering ◽  
Drying Methods ◽  
Particle Sizes ◽  
Particle Sizer ◽  
Lipid Lowering Effect

Objective: To prepare water-soluble chitosan(WSC) nanoparticles(WSC-NPs) and microspheres(WSC-MPs) , exam the morphology and particle sizes of them and study their effect on lowering lipids . Methods: WSC-NPs and WSC-MPs were prepared by ionic gelation process and spray-drying methods respectively. The effect of WSC-NPs and WSC-MPs on lowering lipids was evaluated by measuring its binding capacities of lipids in the conditions simulating human gastrointestinal tract in vitro. Also, the morphology and particle sizes of WSC-NPs and WSC-MPs were examined under scanning electron microscopy (SEM) and particle sizer. Resluts: WSC-NPs and WSC-MPs were nearly spherical in shape and the mean particles size varied from 200-400 nm and 3-7 μm respectively; The lipids-binding capacities of WSC-NPs and WSC-MPs were more effective compared with water-soluble chiosan. The lipids-binding capacity were enhenced when the particle size were decreased. Conclusion: WSC-NPs and WSC-MPs will be better fat-lowing food additives to replace water-soluble chitosan.

Synthesis and Biological Evaluation of Acetylcholinesterase Inhibitor Macakurzin C and Its Derivatives

Synlett ◽  
2015 ◽  
Vol 26 (08) ◽  
pp. 1131-1134 ◽  
Author(s):  
Hyoungsu Kim ◽  
Seung-Hoon Baek ◽  
Hongjun Jang
Keyword(s):  
Inhibitory Activity ◽  
Acetylcholinesterase Inhibitor ◽  
Biological Evaluation ◽  
Hydroxyl Groups ◽  
Structural Requirements ◽  
Ache Inhibitory Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

The derivatives of macakurzin C containing a modified D ring and protected C(3)/C(5)-hydroxyl groups were synthesized and their in vitro AChE inhibitory activity and neurotoxicity were evaluated to identify the structural requirements for the activities. The results indicated that C(3)-benzyl-protected derivative has a more potent AChE inhibitory activity (IC50, 2.6 μM) and a less neurotoxicity (GI50, >100 μM) than synthetic macakurzin C (IC50, 9.1 μM; GI50, 16.6 μM).

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