scholarly journals Sintesis Dan Uji Aktivitas Antioksidan Senyawa Flavonol 2-(3,4,5-Dimetoksifenil)-3-Hidroksi-4h-Kromen-4-On

2019 ◽  
Vol 2 (2) ◽  
pp. 34-37
Author(s):  
Muhamad Rokhim ◽  
Adel Zamri ◽  
Hilwan Yuda Teruna
Keyword(s):  
Antioxidant Activity ◽  
Spectroscopic Data ◽  
Dpph Assay ◽  
Ic50 Values ◽  
Derivatives Of

Flavonols derivatives of 2'-hydroxycalone have been synthesized under basic condition (KOH). The structures of all compounds were characterized based on the interpretation of spectroscopic data including HPLC, UV, FTIR, NMR and HRMS. Antioxidant activity was evaluated using the DPPH assay which showed that the flavonol 2'-hydroxycalone derivative was potentially active as antioxidants with IC50 values <1000 µg / mL.

scholarly journals Synthesis, Test of Antioxidant and Anticancer Activities Flavonol 2- (3,4,5-Dimethoxyphenyli) -3-Hydroxy-4H-Chromen-4-On

2019 ◽  
Vol 17 (2) ◽  
pp. 16
Author(s):  
Muhamad Rokim ◽  
Adel Zamri ◽  
Hilwan Yuda Teruna
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Activity ◽  
Spectroscopic Data ◽  
Dpph Assay ◽  
Anticancer Activities ◽  
Ic50 Values ◽  
Derivatives Of ◽  
Mts Assay

Flavonols 2-(3,4,5-dimethoxyphenyli)-3-hydroxy-4h-chromen-4-on) derivatives of 2'-hydroxycalone have been synthesized under basic condition (KOH). The structures of all compounds were characterized based on the interpretation of spectroscopic data including UV, FTIR, NMR and HRMS. Antioxidant activity was evaluated using the DPPH assay and anticancer activity was evaluated using the MTS assay which showed that the flavonol 2'-hydroxycalone derivative was potentially active as antioxidants and anticancer with IC50 values <1000 µg / mL.

scholarly journals Secondary Metabolites with α-Glucosidase Inhibitory Activity from the Mangrove Fungus Mycosphaerella sp. SYSU-DZG01

Marine Drugs ◽  
2019 ◽  
Vol 17 (8) ◽  
pp. 483 ◽  
Author(s):  
Pei Qiu ◽  
Zhaoming Liu ◽  
Yan Chen ◽  
Runlin Cai ◽  
Guangying Chen ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Secondary Metabolites ◽  
Single Crystal ◽  
Absolute Configuration ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
X Ray Diffraction ◽  
X Ray ◽  
Ic50 Values ◽  
New Metabolites

Four new metabolites, asperchalasine I (1), dibefurin B (2) and two epicoccine derivatives (3 and 4), together with seven known compounds (5–11) were isolated from a mangrove fungus Mycosphaerella sp. SYSU-DZG01. The structures of compounds 1–4 were established from extensive spectroscopic data and HRESIMS analysis. The absolute configuration of 1 was deduced by comparison of ECD data with that of a known structure. The stereostructures of 2–4 were further confirmed by single-crystal X-ray diffraction. Compounds 1, 8 and 9 exhibited significant α-glucosidase inhibitory activity with IC50 values of 17.1, 26.7 and 15.7 μM, respectively. Compounds 1, 4, 6 and 8 showed antioxidant activity by scavenging DPPH· with EC50 values ranging from 16.3 to 85.8 μM.

scholarly journals STUDY ON CHEMICAL CONSTITUENTS AND BIOLOGICAL ACTIVITIES OF ALPINIA KWANGSIENSIS T. L. WU AND S. J. CHEN COLLECTED IN VIETNAM

2018 ◽  
Vol 56 (4A) ◽  
pp. 273
Author(s):  
Tran Thi Minh
Keyword(s):  
Staphylococcus Aureus ◽  
Antioxidant Activity ◽  
Bacillus Subtilis ◽  
Ethyl Acetate ◽  
Spectroscopic Data ◽  
Methanol Extract ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Ethyl Acetate Fraction ◽  
Ic50 Values

Three compounds named ester methyl-trans-p-coumarate (1), 7-hydroxy-6-methoxycoumarin (2), and (+)-gallocatechin (3) have been isolated from the ethyl acetate fraction of methanol extract of Alpinia kwangsiensis roots collected in Thai Nguyen province. Their structures were elucidated on the basis of spectroscopic data and by comparison with their spectral data reported in literature. This is the first isolation of three compounds from this species. The ethyl acetate fraction was found to be active against bacterias as Staphylococcus aureus and Bacillus subtilis with the IC50 values ranging at 74.65 mg/ml and 80.54 mg/ml, respectively. This fraction also showed antioxidant activity through DPPH test with the EC50 value 87.98 mg/ml.

scholarly journals Essential oil composition and antioxidant activity of two Juniperus communis L. varieties growing wild in Serbia

2016 ◽  
pp. 197-205 ◽  
Author(s):  
Nemanja Rajcevic ◽  
Tanja Dodos ◽  
Jelica Novakovic ◽  
Pedja Janackovic ◽  
Petar Marin
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Essential Oil ◽  
Essential Oils ◽  
Essential Oil Composition ◽  
Oil Composition ◽  
Dpph Assay ◽  
Juniperus Communis ◽  
Ic50 Values ◽  
Typical Variety

The genus Juniperus L. (Cupressaceae) consists of ca. 67 species and 34 varieties. Juniperus communis L. grows on dry hills or mountainous tracts and is widely distributed in the northern hemisphere. A typical variety J. communis L. var. communis was collected in Deliblatska pescara (Deliblato Sands) and variety J. communis L. var. saxatilis Pall. in Kopaonik Mountain. Needle essential oils were obtained using Clevenger apparatus and analyzed using GC/MS and GC/FID. Antioxidant activity of essential oils was evaluated using DPPH assay. A total of 78 compounds were detected and identified. Both oils are characterized by high abundance of monoterpenes. The main constituents of J. communis var. communis essential oil were sabinene (39.4%), ?-pinene (13.3%), myrcene (4.7%) and terpinen-4-ol (3.7%), while J. communis var. saxatilis essential oil had ?-pinene (34.9%), sabinene (20.3%), ?-3-carene (6.4%) and germacrene B (6.3%) as the most abundant components. DPPH test showed IC50 values 0.66 mg/ml for J. communis var. communis and 0.32 mg/ml for J. communis var. saxatilis. Although antioxidant activity was weaker than used standards (BHT and L-ascorbic acid) it is still significant.

scholarly journals ANTI-INFLAMMATORY AND ANTIOXIDANT ACTIVITY OF SYNTHESIZED MANNICH BASE DERIVATIVES OF (2E,6E)-2-[(4-HYDROXY-3-METHOXYPHENYL)METHYLIDENE]-6-(PHENYL METHYLIDENE)CYCLOHEXAN-1-ONE

2019 ◽  
pp. 246-250 ◽  
Author(s):  
HAYUN HAYUN ◽  
BAITHA PALANGGATAN MAGGADANI ◽  
ARINI KURNIA ◽  
AULIA HANIFAH ◽  
MEIDI YULIANDI ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Protein Denaturation ◽  
Antioxidant Activities ◽  
Diclofenac Sodium ◽  
Radical Scavenging ◽  
Mannich Bases ◽  
Inflammatory Activity ◽  
Ic50 Values ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: To further understand this compound, we synthesized and evaluated the antioxidant and anti-inflammatory activity of a series of itsMannich base derivatives.Methods: We synthesized the compounds via the previously reported Mannich reaction method. Their structures were elucidated by Fouriertransforminfrared,1H-NMR,13C-NMR, and high-resolution mass spectra. The derivatives’ anti-inflammatory and antioxidant activities were testedusing the inhibition of protein denaturation method and the 2,2-diphenyl-2-picrylhydrazyl free radical scavenging assay.Results: The IC50 values for the anti-inflammatory activity of the 2,6-dimethylmorpholine, pyrrolidine, 1-methylpiperazine, and dimethylamineMannich base derivatives 2a–d were 10.67, 10.72, 37.75, and 1.93 μM, respectively; for (2E,6E)-2-({4-hydroxy-3-methoxyphenyl}methylidene)-6-(phenylmethylidene)cyclohexan-1-one (1), diclofenac sodium, and curcumin, the IC50 values were 56.29, 1.52, and 8.43 μM, respectively. The IC50values for the antioxidant activity of compounds 2a–2d were 229.62, 57.29, 280.43, and 219.22 μM, respectively; for compound 1, quercetin, andcurcumin, the IC50 values were 144.22, 27.28, and 26.45 μM, respectively.Conclusion: Substituting Mannich bases into (2E,6E)-2-[(4-hydroxy-3-methoxyphenyl) methylidene]-6-(phenylmethylidene)cyclohexan-1-oneenhanced its anti-inflammatory activity, but lowered its antioxidant activity. Compound 2d, (2E,6E)-2-({3-[(dimethylamino)methyl]-4-hydroxy-5-methoxyphenyl}methylidene)-6-(phenyl methylidene)cyclohexan-1-one, exhibited potent anti-inflammatory activity comparable to diclofenacsodium and four times higher than curcumin. However, further investigation of this compound’s mechanism of action and toxicity is warranted.

Inhibition of Protein Tyrosine Phosphatase 1B by Lutein Derivatives isolated from Mexican Oregano (Lippia graveolens)

2018 ◽  
Vol 17 (3) ◽  
pp. 134-139
Author(s):  
R.M. Perez-Gutierrez
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Methanol Extract ◽  
Tyrosine Phosphatase ◽  
Positive Control ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Ic50 Value ◽  
Ic50 Values

Methanol extract from Lippia graveolens (Mexican oregano) was studied in order to identify inhibitory bioactives for protein tyrosine phosphatase 1B (PTP1B). Known flavone as lutein (1), and another flavone glycoside such as lutein-7-o-glucoside (2), 6-hydroxy-lutein-7-ohexoside (3) and lutein-7-o-ramnoide (4) were isolated from methanol extract of aerial parts of the Lippia graveolens. All isolates were identified based on extensive spectroscopic data analysis, including UV, IR, NMR, MS and compared with spectroscopic data previously reported. These flavones were evaluated for PTP1B inhibitory activity. Among them, compounds 1 and 3 displayed potential inhibitory activity against PTP1B with IC50 values of 7.01 ± 1.25 μg/ml and 18.4 μg/ml, respectively. In addition, compound 2 and 4 showed moderate inhibitory activity with an IC50 value of 23.8 ± 6.21 and 67.8 ± 5.80 μg/ml respectively. Among the four compounds, luteolin was found to be the most potent PTP1B inhibitor compared to the positive control ursolic acid, with an IC50 value of 8.12 ± 1.06 μg/ml. These results indicate that flavonoids constituents contained in Lippia graveolens can be considered as a natural source for the treatment of type 2 diabetes.

Phenolic Imidazole Derivatives with Dual Antioxidant/Antifungal Activity: Synthesis and Structure-Activity Relationship

2019 ◽  
Vol 15 (4) ◽  
pp. 341-351 ◽  
Author(s):  
Ana P. Bettencourt ◽  
Marián Castro ◽  
João P. Silva ◽  
Francisco Fernandes ◽  
Olga P. Coutinho ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antifungal Activity ◽  
Organic Molecules ◽  
Inhibitory Concentration ◽  
Yeast Species ◽  
Dpph Radical ◽  
Dpph Assay ◽  
Gram Negative ◽  
Structure Activity ◽  
Deoxyribose Degradation

Background: Previous publications show that the addition of a phenolic antioxidant to an antifungal agent, considerably enhances the antifungal activity. Objective: Synthesis of novel compounds combining phenolic units with linear or cyclic nitrogencontaining organic molecules with antioxidant/antifungal activity using methodologies previously developed in the group. Methods: Several N- [1,2-dicyano-2- (arylidenamino) vinyl]-O-alkylformamidoximes 3 were synthesized and cyclized to 4,5-dicyano-N- (N´-alcoxyformimidoyl)-2-arylimidazoles 4 upon reflux in DMF, in the presence of manganese dioxide or to 6-cyano-8-arylpurines 5 when the reagent was refluxed in acetonitrile with an excess of triethylamine. These compounds were tested for their antioxidant activity by cyclic voltammetry, DPPH radical (DPPH•) assay and deoxyribose degradation assay. The minimum inhibitory concentration (MIC) of all compounds was evaluated against two yeast species, Saccharomyces cerevisiae and Candida albicans, and against bacteria Bacillus subtilis (Gram-positive) and Escherichia coli (Gram negative). Their cytotoxicity was evaluated in fibroblasts. Results: Among the synthetised compounds, five presented higher antioxidant activity than reference antioxidant Trolox and from these compounds, four presented antifungal activity without toxic effects in fibroblasts and bacteria. Conclusion: Four novel compounds presented dual antioxidant/antifungal activity at concentrations that are not toxic to bacteria and fibroblasts. The active molecules can be used as an inspiration for further studies in this area.

Synthesis of Novel 1,2,3-Triazole Derivatives of Isocoumarins and 3,4-Dihydroisocoumarin with Potential Antiplasmodial Activity In Vitro

2020 ◽  
Vol 16 ◽  
Author(s):  
Lucas da Silva Santos ◽  
Matheus Fillipe Langanke de Carvalho ◽  
Ana Claudia de Souza Pinto ◽  
Amanda Luisa da Fonseca ◽  
Julio César Dias Lopes ◽  
...  
Keyword(s):  
Triazole Ring ◽  
Antiplasmodial Activity ◽  
World Health ◽  
Dipolar Cycloaddition ◽  
Terminal Alkynes ◽  
The World ◽  
Ic50 Values ◽  
Derivatives Of ◽  
Active Substances

Background: Malaria greatly affects the world health, having caused more than 228 million cases only in 2018. The emergence of drug resistance is one of the main problems in its treatment, demonstrating the urge for the development of new antimalarial drugs. Objective: Synthesis and in vitro antiplasmodial evaluation of triazole compounds derived from isocoumarins and a 3,4- dihydroisocoumarin. Method: The compounds were synthesized in 4 to 6-step reactions with the formation of the triazole ring via the Copper(I)-catalyzed 1,3-dipolar cycloaddition between isocoumarin or 3,4-dihydroisocoumarin azides and terminal alkynes. This key reaction provided compounds with an unprecedented connection of isocoumarin or 3,4-dihydroisocoumarin and the 1,2,3-triazole ring. The products were tested for their antiplasmodial activity against a Plasmodium falciparum chloroquine resistant and sensitive strains (W2 and 3D7, respectively). Results: Thirty-one substances were efficiently obtained by the proposed routes with an overall yield of 25-53%. The active substances in the antiplasmodial test displayed IC50 values ranging from 0.68-2.89 μM and 0.85-2.07 μM against W2 and 3D7 strains, respectively.

Synthesis, Cytotoxicity and Antioxidant Activity of New Analogs of RC-121 Synthetic Derivatives of Somatostatin

2019 ◽  
Vol 18 (10) ◽  
pp. 1417-1424 ◽  
Author(s):  
Emilia Naydenova ◽  
Diana Wesselinova ◽  
Svetlana Staykova ◽  
Ivan Goshev ◽  
Ljubomir Vezenkov
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Capacity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Colorectal Cancer Cell Line ◽  
Cervical Cancer Cell Line ◽  
Synthetic Derivatives ◽  
Derivatives Of

Background: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, - synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity. Objectives: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine). Methods: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (Human Colorectal Cancer Cell Line), MDA-MB-23 (Human Breast Cancer Cell Line), Hep G-2 (Human Hepatocellular Carcinoma Cell Line) and HeLa (cervical cancer cell line). The antioxidant capacities were tested by ORAC (Oxygen Radical Antioxidant Capacity) and HORAC (Hydroxyl Radical Averting Capacity) methods. Results: All substances expressed significantly higher antioxidant capacity by comparison with galic acid and Trolox. All substances showed considerable antioxidant capacity as well. Compound 2T (D-Phe-c(Cys-Tyr-DTrp- Dap-Tle-Cys)-Thr-NH2)had the highest antioxidant effect. The compound 4T (D-Phe-c(Cys-Tyr-D-Trp- Orn-Tle-Cys)-Thr-NH2) displayed antiproliferative effect on HeLa cells with IC50 30 µM. The peptide analog 3T (D-Phe-c(Cys-Tyr-D-Trp-Lys-Tle-Cys)-Thr-NH2) exerted the most pronounced inhibition on the cell vitality up to 53%, 56% and 65% resp. against MDA-MB-23, Hep G-2, HeLa in the higher tested concentration. Conclusion: The somatostatin analogs showed moderate influence on the vitality of different tumor cells and could be used in changing their pathology.

scholarly journals Quantification of Major Bioactive Constituents, Antioxidant Activity, and Enzyme Inhibitory Effects of Whole Coffee Cherries (Coffea arabica) and Their Extracts

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4306
Author(s):  
Boris Nemzer ◽  
Diganta Kalita ◽  
Nebiyu Abshiru
Keyword(s):  
Antioxidant Activity ◽  
Coffea Arabica ◽  
Digestive Enzymes ◽  
Chlorogenic Acids ◽  
Inhibitory Effects ◽  
Bioactive Constituents ◽  
Caffeoylquinic Acids ◽  
Dicaffeoylquinic Acid ◽  
Ic50 Values ◽  
Control Of Diabetes

Coffee cherry is a rich source of chlorogenic acids (CGAs) and caffeine. In this study we examined the potential antioxidant activity and enzyme inhibitory effects of whole coffee cherries (WCC) and their two extracts on α-amylase, α-glucosidase and acetylcholinesterase (AChE) activities, which are targets for the control of diabetes and Alzheimer’s diseases. Whole coffee cherry extract 40% (WCCE1) is rich in chlorogenic acid compounds, consisting of a minimum of 40% major isomers, namely 3-caffeoylquinic acids, 4-caffeoylquinic acids, 5-caffeoylquinic acids, 3,4-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid, 4,5-dicaffeoylquinic acid, 4-feruloylquinc acid, and 5-feruloylquinc acid. Whole coffee cherry extract 70% (WCCE2) is rich in caffeine, with a minimum of 70%. WCCE1 inhibited the activities of digestive enzymes α-amylase and α-glucosidase, and WCCE2 inhibited acetylcholinesterase activities with their IC50 values of 1.74, 2.42, and 0.09 mg/mL, respectively. Multiple antioxidant assays—including DPPH, ABTS, FRAP, ORAC, HORAC, NORAC, and SORAC—demonstrated that WCCE1 has strong antioxidant activity.

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