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 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.

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.

scholarly journals Front Cover: Synthesis, Crystallization Studies, and in vitro Characterization of Cinnamic Acid Derivatives as Sm HDAC8 Inhibitors for the Treatment of Schistosomiasis (ChemMedChem 15/2018)

ChemMedChem ◽  
2018 ◽  
Vol 13 (15) ◽  
pp. 1488-1488
Author(s):  
Theresa Bayer ◽  
Alokta Chakrabarti ◽  
Julien Lancelot ◽  
Tajith B. Shaik ◽  
Kristin Hausmann ◽  
...  
Keyword(s):  
Cinnamic Acid ◽  
Cinnamic Acid Derivatives ◽  
Front Cover ◽  
In Vitro Characterization ◽  
Hdac8 Inhibitors

scholarly journals Antimicrobial activity of selected aminoglycoside and fluoroquinolone eye drops against Staphylococcus aureus isolated from the conjunctiva of a bacterial conjunctivitis patient

2021 ◽  
Vol 2 (2) ◽  
pp. 151-157
Author(s):  
Chigozie John Ekenze ◽  
Oyinyechi Lilian Umunnakwe ◽  
Timothy Olugbenga Ogundeko ◽  
Chioma Lilian Owunna ◽  
Florence Akuchi Mbatuegwu ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Bacterial Infections ◽  
In Vitro Study ◽  
Inhibition Zone ◽  
Aureus Strain ◽  
Eye Drops ◽  
Bacterial Conjunctivitis ◽  
Antimicrobial Sensitivity ◽  
Zones Of Inhibition

A comparative in vitro study was conducted to ascertain the efficacy of 4 selected antibiotic eye drops against Staphylococcus aureus strain isolated from the conjunctiva of a patient diagnosed of bacterial conjunctivitis, and were assayed on the basis of the zone of inhibition. One and two drops volume of the test drugs were inoculated (administered). Results for average inhibition zone for 1 and 2 drops volume was Levofloxacin (26.88 mm), Ciprofloxacin (25.0 mm), Tobramycin (12.5 mm), Gentamicin (7.5 mm) and Levofloxacin (33.12 mm), Ciprofloxacin (30.6 mm), Tobramycin (19.3 mm) and Gentamicin (17.5 mm) respectively with two drops having higher effect than one for Levofloxacin˃ Ciprofloxacin˃ Tobramycin˃ Gentamicin by way of order of susceptibility. The difference in the average zones of inhibition produced by equal volumes of gentamicin and tobramycin and that between ciprofloxacin and levofloxacin both not statistically significant (p˃0.05). Fluoroquinolones showed greater zones of inhibition than the aminoglycosides significantly with levofloxacin more efficacious than ciprofloxacin. One drop prescription is thus recommended. However, if two drops must be prescribed perhaps due to severity of symptoms as the clinician may deem necessary, the drugs should be administered in divided doses. Antimicrobial sensitivity test should be conducted in cases of ocular bacterial infections caused by Staphylococcus aureus while treatment with fluoroquinolone especially levofloxacin eye drops as the first line treatment is also suggested.

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.

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