scholarly journals Syntheses, Characterization, Resolution, and Biological Studies of Coordination Compounds of Aspartic Acid and Glycine

2017 ◽  
Vol 2017 ◽  
pp. 1-15 ◽  
Author(s):  
Temitayo Aiyelabola ◽  
Ezekiel Akinkunmi ◽  
Isaac Ojo ◽  
Efere Obuotor ◽  
Clement Adebajo ◽  
...  
Keyword(s):  
Aspartic Acid ◽  
Coordination Compounds ◽  
Biological Activities ◽  
Enantiomeric Purity ◽  
Cytotoxic Agents ◽  
Cytotoxic Activities ◽  
Biological Studies ◽  
Racemic Mixtures ◽  
Resolving Agents ◽  
Metal Ligand

Enantiomerically enriched coordination compounds of aspartic acid and racemic mixtures of coordination compounds of glycine metal-ligand ratio 1 : 3 were synthesized and characterized using infrared and UV-Vis spectrophotometric techniques and magnetic susceptibility measurements. Five of the complexes were resolved using (+)-cis-dichlorobis(ethylenediamine)cobalt(III) chloride, (+)-bis(glycinato)(1,10-phenanthroline)cobalt(III) chloride, and (+)-tris(1,10-phenanthroline)nickel(II) chloride as resolving agents. The antimicrobial and cytotoxic activities of these complexes were then determined. The results obtained indicated that aspartic acid and glycine coordinated in a bidentate fashion. The enantiomeric purity of the compounds was in the range of 22.10–32.10%, with (+)-cis-dichlorobis(ethylenediamine)cobalt(III) complex as the more efficient resolving agent. The resolved complexes exhibited better activity in some cases compared to the parent complexes for both biological activities. It was therefore inferred that although the increase in the lipophilicity of the complexes may assist in the permeability of the complexes through the cell membrane of the pathogens, the enantiomeric purity of the complexes is also of importance in their activity as antimicrobial and cytotoxic agents.

scholarly journals Synthesis Characterization and Biological Activities of Coordination Compounds of 4-Hydroxy-3-nitro-2H-chromen-2-one and Its Aminoethanoic Acid and Pyrrolidine-2-carboxylic Acid Mixed Ligand Complexes

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Temitayo Aiyelabola ◽  
Ezekiel Akinkunmi ◽  
Efere Obuotor ◽  
Idowu Olawuni ◽  
David Isabirye ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Coordination Compounds ◽  
Biological Activities ◽  
Amino Nitrogen ◽  
Mixed Ligand ◽  
Mixed Ligand Complexes ◽  
Molar Ratio ◽  
Cytotoxic Activities ◽  
Carboxylate Oxygen ◽  
Edx Analyses

Coordination compounds of 4-hydroxy-3-nitro-2H-chromen-2-one and their mixed ligand complexes with aminoethanoic acid and pyrrolidine-2-carboxylic acid were synthesized by the reaction of Cu(II) and Zn(II) salts in molar ratio 1 : 2 for the coumarin complexes and 1 : 1 : 1 for the mixed ligand complexes, in basic media. The compounds formed were characterized using infrared, Uv-vis spectrophotometric analyses, mass spectrometry, magnetic susceptibility measurements, and EDX analyses. It was concluded that 4-hydroxy-3-nitro-2H-chromen-2-one coordinated as a monobasic ligand for all the complexes; it also coordinated via the carbonyl moiety in the case of the Cu(II) mixed ligand complexes. Similarly it was proposed that the amino acids also coordinated in a bidentate fashion via their amino nitrogen and carboxylate oxygen atoms. The synthesized compounds were screened for their antimicrobial and cytotoxic activities. The complexes exhibited marginal antimicrobial activity but good cytotoxic activity.

scholarly journals Synthesis, Characterization, and Antimicrobial Activities of Coordination Compounds of Aspartic Acid

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
T. O. Aiyelabola ◽  
D. A. Isabirye ◽  
E. O. Akinkunmi ◽  
O. A. Ogunkunle ◽  
I. A. O. Ojo
Keyword(s):  
Mass Spectrometry ◽  
Aspartic Acid ◽  
Coordination Compounds ◽  
Antimicrobial Activities ◽  
Stoichiometric Ratio ◽  
Gram Negative Bacteria ◽  
Acidic Media ◽  
Geometrical Structures ◽  
Gram Negative ◽  
Metal Ligand

Coordination compounds of aspartic acid were synthesized in basic and acidic media, with metal ligand M : L stoichiometric ratio 1 : 2. The complexes were characterized using infrared, electronic and magnetic susceptibility measurements, and mass spectrometry. Antimicrobial activity of the compounds was determined against three Gram-positive and three Gram-negative bacteria and one fungus. The results obtained indicated that the availability of donor atoms used for coordination was a function of the pH of the solution in which the reaction was carried out. This resulted in varying geometrical structures for the complexes. The compounds exhibited a broad spectrum of activity and in some cases better activity than the standard.

scholarly journals Chemical and Biological Studies of Leaf Extract of Dendrophthoe falcata Linn.

2018 ◽  
Vol 16 (2) ◽  
pp. 215-219 ◽  
Author(s):  
Md Rajdoula Rafe ◽  
Monira Ahsan ◽  
Choudhury Mahmood Hasan ◽  
Mohammad Mehedi Masud
Keyword(s):  
Brine Shrimp ◽  
Methanol Extract ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Radical Scavenging ◽  
Cytotoxic Activities ◽  
Significant Activity ◽  
Brine Shrimp Lethality ◽  
Biological Studies ◽  
Dendrophthoe Falcata

Dendrophthoe falcata (Family Loranthaceae) is used extensively in rural area as a component of ethno-medicine for the treatment of various diseases. In this study, the crude extracts and the fractions obtained from D. falcata were investigated for potential chemical constituents and some biological activities. For medicinal properties the antioxidant, brine shrimp lethality and thrombolytic activities have been investigated. The structures of the isolated three compounds were solved by extensive analyses of their high resolution 1HNMR spectroscopic data. They were identified as Lupeol, 3-β-acetoxy-12-ene-11-one and β-sitosterol. For bioactivities, the petroleum ether, dichloromethane, chloroform and aqueous soluble fractions abbreviated as PESF, DCMSF, CSF and AQSF respectively. Brine shrimp lethality bioassay was used to evaluate potential cytotoxic activities, where all fractions showed significant activity with lower LC50. Most significant activity has been observed for methanol extract (LC50= 4.477 µg/ml). AQSF revealed maximum activity in DPPH free radical scavenging assay (IC50 = of 43.49 μg/ml). In assay for thrombolytic activity, the methanol extract and its chloroform soluble fraction demonstrated significant efficacy with 32.65% and 32.36% clot lysis, respectively.Dhaka Univ. J. Pharm. Sci. 16(2): 215-219, 2017 (December)

scholarly journals Comparative Analyses of Metabolomic Fingerprints and Cytotoxic Activities of Soft Corals from the Colombian Caribbean

Marine Drugs ◽  
2019 ◽  
Vol 17 (1) ◽  
pp. 37 ◽  
Author(s):  
Liliana Santacruz ◽  
Olivier Thomas ◽  
Carmenza Duque ◽  
Mónica Puyana ◽  
Edisson Tello
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
High Resolution Mass Spectrometry ◽  
Biological Activities ◽  
Analytical Techniques ◽  
Living Organism ◽  
Cytotoxic Agents ◽  
Cytotoxic Activities ◽  
Tumor Cell Lines ◽  
Soft Corals

Soft corals (Cnidaria, Anthozoa, Octocorallia) are a diverse group of marine invertebrates that inhabit various marine environments in tropical and subtropical areas. Several species are recognized as prolific sources of compounds with a wide array of biological activities. Recent advances in analytical techniques, supported by robust statistical analyses, have allowed the analysis and characterization of the metabolome present in a single living organism. In this study, a liquid chromatography-high resolution mass spectrometry metabolomic approach was applied to analyze the metabolite composition of 28 soft corals present in the Caribbean coast of Colombia. Multivariate data analysis was used to correlate the chemical fingerprints of soft corals with their cytotoxic activity against tumor cell lines for anticancer purpose. Some diterpenoids were identified as specific markers to discriminate between cytotoxic and non-cytotoxic crude extracts of soft corals against tumor cell lines. In the models generated from the comparative analysis of PLS-DA for tumor lines, A549 and SiHa, the diterpene 13-keto-1,11-dolabell-3(E),7(E),12(18)-triene yielded a high score in the variable importance in projection. These results highlight the potential of metabolomic approaches towards the identification of cytotoxic agents against cancer of marine origin. This workflow can be useful in several studies, mainly those that are time consuming, such as traditional bioprospecting of marine natural products.

N6-substituted adenosines. Cytokinin and antitumor activities

2011 ◽  
Vol 76 (11) ◽  
pp. 1361-1378 ◽  
Author(s):  
Svetlana V. Kolyachkina ◽  
Vitali I. Tararov ◽  
Cyril S. Alexeev ◽  
Dmitry M. Krivosheev ◽  
Georgy A. Romanov ◽  
...  
Keyword(s):  
Click Reaction ◽  
Human Cancer ◽  
Biological Activities ◽  
Alkyl Halides ◽  
Cytotoxic Agents ◽  
Cytotoxic Activities ◽  
Human Cancer Cell ◽  
Antitumor Activities ◽  
Cell Assays ◽  
Adenosine Derivatives

A series of N6-adenosine derivatives were synthesized by alkylation of N6-acetyl-2′,3′,5′-tri-O-acetyladenosine (1) with alkyl halides and alcohols. It was shown that propargyl derivative 2a is a good substrate for copper(I) catalyzed Huisgen [3+2] cycloaddition with azides. This click-reaction can be used for preparation of the libraries of 1,2,3-triazolyl modified adenosines. Biological activities of N6-adenosines were studied in two plant and six human cancer cell assays. The remarkable parallel between cytokinin and cytotoxic activities was found. The most cytokinin active compounds 3c–3e at the same time appeared to be the most potent cytotoxic agents.

Bioactive Secondary Metabolites from Endophytic Fungi

2020 ◽  
Vol 27 (11) ◽  
pp. 1836-1854 ◽  
Author(s):  
Elena Ancheeva ◽  
Georgios Daletos ◽  
Peter Proksch
Keyword(s):  
Secondary Metabolites ◽  
Endophytic Fungi ◽  
Host Plants ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Special Focus ◽  
Plant Metabolites ◽  
Direct Production ◽  
Bioactive Secondary Metabolites ◽  
Fungal Genes

Background: Endophytes represent a complex community of microorganisms colonizing asymptomatically internal tissues of higher plants. Several reports have shown that endophytes enhance the fitness of their host plants by direct production of bioactive secondary metabolites, which are involved in protecting the host against herbivores and pathogenic microbes. In addition, it is increasingly apparent that endophytes are able to biosynthesize medicinally important “phytochemicals”, originally believed to be produced only by their host plants. Objective: The present review provides an overview of secondary metabolites from endophytic fungi with pronounced biological activities covering the literature between 2010 and 2017. Special focus is given on studies aiming at exploration of the mode of action of these metabolites towards the discovery of leads from endophytic fungi. Moreover, this review critically evaluates the potential of endophytic fungi as alternative sources of bioactive “plant metabolites”. Results: Over the past few years, several promising lead structures from endophytic fungi have been described in the literature. In this review, 65 metabolites are outlined with pronounced biological activities, primarily as antimicrobial and cytotoxic agents. Some of these metabolites have shown to be highly selective or to possess novel mechanisms of action, which hold great promises as potential drug candidates. Conclusion: Endophytes represent an inexhaustible reservoir of pharmacologically important compounds. Moreover, endophytic fungi could be exploited for the sustainable production of bioactive “plant metabolites” in the future. Towards this aim, further insights into the dynamic endophyte - host plant interactions and origin of endophytic fungal genes would be of utmost importance.

Recent Developments on Synthesis of Indole Derivatives Through Green Approaches and Their Pharmaceutical Applications

2020 ◽  
Vol 24 (22) ◽  
pp. 2665-2693
Author(s):  
Dipayan Mondal ◽  
Pankaj Lal Kalar ◽  
Shivam Kori ◽  
Shovanlal Gayen ◽  
Kalpataru Das
Keyword(s):  
Biological Activities ◽  
Synthetic Methods ◽  
Pharmaceutical Chemistry ◽  
Indole Derivatives ◽  
Biological Studies ◽  
Recent Developments ◽  
Pharmaceutical Industries ◽  
Green Methodology ◽  
Conventional Methods ◽  
High Yields

Indole moiety is often found in different classes of pharmaceutically active molecules having various biological activities including anticancer, anti-viral, anti-psychotic, antihypertensive, anti-migraine, anti-arthritis and analgesic activities. Due to enormous applications of indole derivatives in pharmaceutical chemistry, a number of conventional synthetic methods as well as green methodology have been developed for their synthesis. Green methodology has many advantages including high yields, short reaction time, and inexpensive reagents, highly efficient and environmentally benign over conventional methods. Currently, the researchers in academia as well as in pharmaceutical industries have been developing various methods for the chemical synthesis of indole based compounds via green approaches to overcome the drawbacks of conventional methods. This review reflects the last ten years developments of the various greener methods for the synthesis of indole derivatives by using microwave, ionic liquids, water, ultrasound, nanocatalyst, green catalyst, multicomponent reaction and solvent-free reactions etc. (please see the scheme below). Furthermore, the applications of green chemistry towards developments of indole containing pharmaceuticals and their biological studies have been represented in this review.

Synthesis and Evaluation of Aromatic Surfactants as Potential Antibacterial and Cytotoxic Agents

2019 ◽  
Vol 16 (6) ◽  
pp. 478-484
Author(s):  
Kenia Barrantes ◽  
Mary Fuentes ◽  
Luz Chacón ◽  
Rosario Achí ◽  
Jorge Granados-Zuñiga ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Hela Cells ◽  
Cytotoxic Agents ◽  
Cytotoxic Activities ◽  
Hydroxybenzoic Acid ◽  
Derivatives Of

Two ether and one ester derivatives of the 4-nitro-3-hydroxybenzoic acid were synthesized and characterized. The in vitro antimicrobial and cytotoxic activities of the three novel compounds were also evaluated. The aromatic derivatives showed antibacterial activity against one of the four microorganisms tested and two compounds (C8 and NOBA) had a lower IC50 in HeLa cells.

Naphthoquinone-based hydrazone hybrids: synthesis and potent activity against cancer cell lines

2020 ◽  
Vol 16 ◽  
Author(s):  
Délis Galvão Guimarães ◽  
Arlan de Assis Gonsalves ◽  
Larissa Araújo Rolim ◽  
Edigênia Cavalcante Araújo ◽  
Victória Laysna dos Anjos Santos ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Biological Activities ◽  
Supporting Electrolyte ◽  
Cancer Cell Lines ◽  
Molecular Structures ◽  
Cytotoxic Activities ◽  
Electrochemical Studies ◽  
Ic50 Values

Background: Natural naphthoquinones have shown diversified biological activities including antibacterial, antifungal, antimalarial, and cytotoxic activities. However, they are also compounds with acute cytotoxicity, immunotoxicity, carcinogenesis, and cardio- and hepatotoxicity, then the modification at their redox center is an interesting strategy to overcome such harmful activity. Objective: In this study, four novel semisynthetic hydrazones, derived from the isomers α- and β-lapachones (α and β, respectively) and coupled with the drugs hydralazine (HDZ) and isoniazid (ACIL), were prepared, evaluated by electrochemical methods and assayed for anticancer activity. Method: The semisynthetic hydrazones were obtained and had their molecular structures established by NMR, IR, and MS. Anticancer activity was evaluated by cell viability determined by reduction of 3-(4,5-dimethyl-2-thiazol)-2,5-diphenyl-2H-tetrazolium bromide (MTT). The electrochemical studies, mainly cyclic voltammetry, were performed, in aprotic and protic media. Result: The study showed that the compounds 2, 3, and 4 were active against at least one of the cancer cell lines evaluated, being compounds 3 and 4 the most cytotoxic. Toward HL-60 cells, compound 3 was 20x more active than β-lapachone, and 3x more cytotoxic than doxorubicin. Furthermore, 3 showed an SI value of 39.62 for HL-60 cells. Compound 4 was active against all cancer cells tested, with IC50 values in the range 2.90–12.40 μM. Electrochemical studies revealed a profile typical of self-protonation and reductive cleavage, dependent on the supporting electrolyte. Conclusion: These results therefore indicate that compounds 3 and 4 are strong candidates as prototypes of new antineoplastic drugs.

Design, Synthesis, Anti-Proliferative Evaluation and Cell Cycle Analysis of Hybrid 2-Quinolones

2019 ◽  
Vol 19 (9) ◽  
pp. 1132-1140
Author(s):  
Heba A.E. Mohamed ◽  
Hossa F. Al-Shareef
Keyword(s):  
Cell Cycle ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Flow Cytometric Analysis ◽  
Annexin V ◽  
Cytotoxic Activities ◽  
Significant Group ◽  
Design Synthesis ◽  
Standard Drug ◽  
Wide Range

Background: Quinolones are a significant group of nitrogen heterocyclic compounds that exist in therapeutic agents, alkaloids, and synthetic small molecules that have important biological activities. A wide range of quinolones have been used as antituberculosis, antibacterial, anti-malarial, antifungal, anticonvulsant, anticancer agents and urease inhibitors. Methods: Ethyl 3,3-disubstituted-2-cyano propionates containing hybride quinolones derivatives were synthesized by the reaction of 1-amino-7-hydroxy-4-methylquinolin-2(1H)-one and its dibromo derivative with α, β-unsaturated carbonyl in ethanol. Results: A novel series of hybrid 2-quinolone derivatives was designed and synthesized. The compounds structures were confirmed using different spectroscopic methods and elemental analysis. The cytotoxic activities of all the compounds were assessed against HepG2 cell line in comparison with doxorubicin as a standard drug. Conclusion: Most compounds revealed superior anti-proliferative activity than the standard. Compound 4b, is the most active compound (IC50 = 0.39mM) compared with doxorubicin (IC50 = 9.23mM). DNA flow cytometric analysis of compound 4b showed cell cycle arrest at G2/M phase with a concomitant increase of cells in apoptotic phase. Dual annexin-V/ propidium iodide staining assay of compound 4b revealed that the selected candidate increased the apoptosis of HepG-2 cells more than control.

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