scholarly journals Anti-trypanosomal Phenolic Derivatives from Baccharis uncinella

2014 ◽  
Vol 9 (2) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Simone dos S. Grecco ◽  
Maria Júlia P. Félix ◽  
João Henrique G. Lago ◽  
Érika G. Pinto ◽  
André G. Tempone ◽  
...  
Keyword(s):  
Cinnamic Acid ◽  
Inhibitory Concentration ◽  
Acid Mixture ◽  
Chlorogenic Acids ◽  
Cinnamic Acid Derivatives ◽  
Etoh Extract ◽  
Aerial Parts ◽  
Bioassay Guided Fractionation ◽  
Ferulic Acids

Bioassay-guided fractionation of the EtOH extract of the aerial parts of Baccharis uncinella C. DC. (Asteraceae) led to identification of two cinnamic acid derivatives (caffeic and ferulic acids), two flavones (hispidulin and pectolinaringenin) and a mixture of three chlorogenic acids (3,4-, 3,5- and 4,5-O-dicaffeoylquinic acids), which displayed in vitro anti-trypanosomal activity. Pectolinaringenin, hispidulin and caffeic acid showed activity against trypomastigotes of Trypanosoma cruzi, exhibiting 50% inhibitory concentration (IC50) values of 52, 81 and 56 μg/mL, respectively, while the chlorogenic acid mixture showed an IC50 value of 61 μg/mL. The flavonoids and cinnamic acid derivatives were evaluated for cytotoxicity against NCTC cells resulting in a 50% cytotoxic concentration (CC50) ranging from 33.82 to 129.1 μg/mL while the chlorogenic acids did not display cytotoxicity (CC50 >150 μg/mL). This is the first report of anti-trypanosomal activity of compounds from B. uncinella.

scholarly journals Cinnamic Acid Derivatives and Their Biological Efficacy

2020 ◽  
Vol 21 (16) ◽  
pp. 5712 ◽  
Author(s):  
Ngonidzashe Ruwizhi ◽  
Blessing Atim Aderibigbe
Keyword(s):  
Cinnamic Acid ◽  
Neurological Disorders ◽  
Bacterial Infections ◽  
Antimalarial Activity ◽  
Aureus Strain ◽  
Cinnamic Acid Derivatives ◽  
Biological Efficacy ◽  
Bioactive Agents ◽  
Acid Functional Group

The role played by cinnamic acid derivatives in treating cancer, bacterial infections, diabetes and neurological disorders, among many, has been reported. Cinnamic acid is obtained from cinnamon bark. Its structure is composed of a benzene ring, an alkene double bond and an acrylic acid functional group making it possible to modify the aforementioned functionalities with a variety of compounds resulting in bioactive agents with enhanced efficacy. The nature of the substituents incorporated into cinnamic acid has been found to play a huge role in either enhancing or decreasing the biological efficacy of the synthesized cinnamic acid derivatives. Some of the derivatives have been reported to be more effective when compared to the standard drugs used to treat chronic or infectious diseases in vitro, thus making them very promising therapeutic agents. Compound 20 displayed potent anti-TB activity, compound 27 exhibited significant antibacterial activity on S. aureus strain of bacteria and compounds with potent antimalarial activity are 35a, 35g, 35i, 36i, and 36b. Furthermore, compounds 43d, 44o, 55g–55p, 59e, 59g displayed potent anticancer activity and compounds 86f–h were active against both hAChE and hBuChE. This review will expound on the recent advances on cinnamic acid derivatives and their biological efficacy.

scholarly journals Antidepressant Potential of Lotus corniculatus L. subsp. corniculatus: An Ethnobotany Based Approach

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1299
Author(s):  
Fatma Tuğçe Gürağaç Dereli ◽  
Haroon Khan ◽  
Eduardo Sobarzo-Sánchez ◽  
Esra Küpeli Akkol
Keyword(s):  
Antidepressant Activity ◽  
Tail Suspension Test ◽  
Lotus Corniculatus ◽  
Antidepressant Effect ◽  
In Vivo Test ◽  
Aerial Parts ◽  
Test Models ◽  
Bioassay Guided Fractionation

As a Turkish traditional medicinal plant, aerial parts of Lotus corniculatus L. subsp. corniculatus (Fabaceae) are used as a painkiller, antihemoroidal, diuretic and sedative. In this study, the antidepressant potential of the plant has been attempted to clarify. Extracts with water, n-Hexane, ethyl acetate, and methanol were prepared respectively from the aerial parts. Antidepressant activity of the extracts were researched by using three different in vivo test models namely a tail suspension test, antagonism of tetrabenazine-induced hypothermia, ptosis, and suppression of locomotor activity and forced swimming test on male BALB/c mice and in vitro monoamine oxidase (MAO)-A and B inhibition assays. The results were evaluated through comparing with control and reference groups, and then active compounds of the active extract have been determined. Bioassay-guided fractionation of active fraction led to the isolation of three compounds and structures of the compounds were elucidated by spectroscopic methods. The data of this study demonstrate that the MeOH extract of the aerial parts of the plant showed remarkable in vivo antidepressant effect and the isolated compounds medicarpin-3-O-glucoside, gossypetin-3-O-glucoside and naringenin-7-O-glucoside (prunin) from the active sub-fractions could be responsible for the activity. Further mechanistic and toxicity studies are planned to develop new antidepressant-acting drugs.

scholarly journals Germinated and Ungerminated Seeds Extract from TwoLupinusSpecies: Biological Compounds Characterization and In Vitro and In Vivo Evaluations

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Bogdan Andor ◽  
Corina Danciu ◽  
Ersilia Alexa ◽  
Istvan Zupko ◽  
Elena Hogea ◽  
...  
Keyword(s):  
Cinnamic Acid ◽  
Therapeutic Potential ◽  
Lupinus Albus ◽  
Biological Evaluation ◽  
Lupinus Angustifolius ◽  
Cinnamic Acid Derivatives ◽  
Natural Agents ◽  
Germinated Seeds

In recent years, nutraceuticals attracted a great amount of attention in the biomedical research due to their significant contribution as natural agents for prevention of various health issues. Ethanolic extracts from the ungerminated and germinated seeds ofLupinus albusL. andLupinus angustifoliusL. were analyzed for the content in isoflavones (genistein) and cinnamic acid derivatives. Additionally, the extracts were evaluated for antimicrobial, antiproliferative, and anti-inflammatory properties, using in vitro and in vivo tests. Germination proved to be a method of choice in increasing the amount of genistein and cinnamic acid derivatives in bothLupinus albusL. andLupinus angustifolius L.seeds. Biological evaluation of all vegetal extracts revealed a weak therapeutic potential for both ungerminated and germinated seeds.

Antiviral Activity of Cholesteryl Esters of Cinnamic Acid Derivatives

1998 ◽  
Vol 53 (9-10) ◽  
pp. 883-887 ◽  
Author(s):  
Angel S. Galabov ◽  
Lubomira Nikolaeva ◽  
Daniela Todorova ◽  
Tsenka Milkova
Keyword(s):  
Antiviral Activity ◽  
Cinnamic Acid ◽  
Cholesteryl Esters ◽  
Cinnamic Acid Derivatives ◽  
Steryl Esters ◽  
Causative Agents ◽  
Marked Activity ◽  
Taxonomic Groups

Cholesteryl 3”,4”-dimethoxycinnamate (7) and a new synthesized o-coumaroyl ester of 3β- (2’-hydroxyethoxy)-cholest-5-en (13) exhibited a marked activity against poliovirus type 1 (Mahoney). Compound 7 showed an approximately 20-fold greater selectivity in its antiviral activity than compound 13. These compounds were selected from thirteen steryl esters of cinnamic acid derivatives through an in vitro antiviral screening against viruses belonging to taxonomic groups with causative agents of important human infectious diseases to which chemotherapy is indicated, i.e. Picornaviridae, Orthomyxoviridae, Paramyxoviridae and Herpesviridae.

Influence of some cinnamic acid derivatives on changes of the tricarboxylic acid cycle enzymes activity in rats under brain ischemia conditions

2020 ◽  
Vol 20 (2) ◽  
pp. 27-32
Author(s):  
Andrey V. Voronkov ◽  
Dmitry I. Pozdnyakov ◽  
Similla L. Adjiahmetova ◽  
Nadezhda M. Chervonnaya ◽  
Victoria M. Rukovitsina ◽  
...  
Keyword(s):  
Cerebral Ischemia ◽  
Cinnamic Acid ◽  
Citrate Synthase ◽  
Tricarboxylic Acid Cycle ◽  
Tricarboxylic Acid ◽  
Reference Drug ◽  
Cinnamic Acid Derivatives ◽  
Acid Cycle ◽  
Activity Of Enzymes ◽  
Ferulic Acids

The aim of the study was to assess the effect of certain derivatives of cinnamic acids on changes of the tricarboxylic acid cycle enzymes activity under experimental cerebral ischemia. Materials and methods. Brain ischemia was modeled by irreversible right-sided coagulation of the middle cerebral artery. Test compounds: 4-hydroxy-3,5-ditretbutyl cinnamic acid, coumaric, coffee, synapic, cinnamic, 4-hydroxycinnamic and ferulic acids, as well as a reference drug succinic acid was administered at a dose of 100 mg / kg per os for 3 days after the reproduction of ischemia. Then, changes in the activity of aconitase, citrate synthase, and -ketoglutarate dehydrogenase were evaluated in the supernatant of the brain. Results. The use of all the studied compounds and the reference drug helped to restore the activity of enzymes of the tricarboxylic acid cycle. The most pronounced results were obtained when animals were treated by 4-hydroxy-3,5-ditretbutyl cinnamic acid, against the background of which the activity of citrate synthase was higher than in animals treated by succinic, coumaric, coffee, synapic and ferulic acids by 1.53 (p 0.05), 1.41 (p 0.05), 1.4 (p 0.05), 1.46 (p 0.05) and 1.41 (p 0.05) times, respectively. Also, with the administration of 4-hydroxy-3,5-ditretbutyl cinnamic acid, the activity of aconitase was higher compared to rats that were administered with succinic, coumaric, coffee, synapic and ferulic acids by 2.47 (p 0.05), 2.49 (p 0.05), 3.44 (p 0.05), 2.59 (p 0.05) and 1.9 (p 0.05) times, respectively. Conclusion. The administration of the studied in this work cinnamic acid derivatives helps to restore the activity of citrate synthase, aconitase, and -ketoglutarate dehydrogenase in rats under conditions of cerebral ischemia. The most pronounced changes in the activity of enzymes were obtained with the iadministration of 4-hydroxy-3,5-ditretbutyl cinnamic acid.

In-vitro Antibacterial Effects of Aqueous, Ethanolic, Methanolic, Acetone and Hydro Ethanolic Extracts of Achillea Millefolium on Standard Klebsiella, S. pyogenes, and Oral Bacterias Strains

2020 ◽  
Author(s):  
Negar Fallah ◽  
Sanaz Namazi ◽  
Negar Balmeh ◽  
Samira Mahmoudi ◽  
Fereshteh Mirzaei Poor
Keyword(s):  
Inhibitory Concentration ◽  
Minimum Bactericidal Concentration ◽  
Methanolic Extract ◽  
Growth Zone ◽  
Achillea Millefolium ◽  
Antibacterial Effects ◽  
Millipore Filter ◽  
Antimicrobial Effects ◽  
Aerial Parts

Introduction: So far, a lot of attempts have been carried out to find antimicrobial compounds. In this study, it was also tried to investigate the antibacterial effects of Achillea millefolium on standard Klebsiella, S. pyogenes, and oral bacterias strain. Material and Methods: The aerial parts of Achillea millefolium were used and the aqueous, ethanolic, methanolic, acetone and hydroethanolic extracts were prepared. After the preparation of standard strains of Klebsiella, S. pyogenes, and oral bacterias and sterilization of extracts by the Millipore filter, the antibacterial effects of these extracts on the mentioned microorganisms were assessed by minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and well diffusion at the concentration 50 mg/ml. The test was repeated three times for each bacterium. Results: It was exposed that aqueous extract of Achillea millefolium had the most distinguished antimicrobial effects against all studied strains and methanolic extract had antimicrobial effects only on S. pyogenes. MIC and MBC of effective extracts were the basic concentration (50mg/ml), and non-growth zone was not observed in other serial dilution in case of all bacteria. Conclusion: The Achillea millefolium can be admitted as an antibacterial medicinal herb. Thus, it can be concluded that after evaluating their effects in vitro, Achillea millefolium can be utilized as an alternative to the routine chemical drugs.

Synthesis, Crystallization Studies, and in vitro Characterization of Cinnamic Acid Derivatives as Sm HDAC8 Inhibitors for the Treatment of Schistosomiasis

ChemMedChem ◽  
2018 ◽  
Vol 13 (15) ◽  
pp. 1517-1529 ◽  
Author(s):  
Theresa Bayer ◽  
Alokta Chakrabarti ◽  
Julien Lancelot ◽  
Tajith B. Shaik ◽  
Kristin Hausmann ◽  
...  
Keyword(s):  
Cinnamic Acid ◽  
Cinnamic Acid Derivatives ◽  
In Vitro Characterization ◽  
Hdac8 Inhibitors

scholarly journals Hybridization of Curcumin Analogues with Cinnamic Acid Derivatives as Multi-Target Agents Against Alzheimer’s Disease Targets

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 4958 ◽  
Author(s):  
Eirini Chainoglou ◽  
Argyris Siskos ◽  
Eleni Pontiki ◽  
Dimitra Hadjipavlou-Litina
Keyword(s):  
Cinnamic Acid ◽  
Hydrophobic Interactions ◽  
Docking Studies ◽  
The Novel ◽  
Chromatography Method ◽  
Cinnamic Acid Derivatives ◽  
Curcumin Analogues ◽  
Antioxidant Agents ◽  
Good Oral Bioavailability

The synthesis of the new hybrids followed a hybridization with the aid of hydroxy-benzotriazole (HOBT) and 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDCI.HCL) in dry DMF or thionyl chloride between curcumin analogues and cinnamic acid derivatives. IR, 1H-NMR, 13C-NMR, LC/MS ESI+, and elemental analysis were used for the confirmation of the structures of the novel hybrids. The lipophilicity values of compounds were calculated theoretically and experimentally via the reversed chromatography method as RM values. The novel derivatives were studied through in vitro experiments for their activity as antioxidant agents and as inhibitors of lipoxygenase, cyclooxygenase-2, and acetyl-cholinesterase. All the compounds showed satisfying anti-lipid peroxidation activity of linoleic acid induced by 2,2′-azobis(2-amidinopropane) hydrochloride (AAPH). Hybrid 3e was the most significant pleiotropic derivative, followed by 3a. According to the predicted results, all hybrids could be easily transported, diffused, and absorbed through the blood–brain barrier (BBB). They presented good oral bioavailability and very high absorption with the exception of 3h. No inhibition for CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 was noticed. According to the Ames test, all the hybrids induced mutagenicity with the exception of 3d. Efforts were conducted a) to correlate the in vitro results with the most important physicochemical properties of the structural components of the molecules and b) to clarify the correlation of actions among them to propose a possible mechanism of action. Docking studies were performed on soybean lipoxygenase (LOX) and showed hydrophobic interactions with amino acids. Docking studies on acetylcholinesterase (AChE) exhibited: (a) hydrophobic interactions with TRP281, LEU282, TYR332, PHE333, and TYR336 and (b) π-stacking interactions with TYR336.

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