scholarly journals Synthesis, Characterization, and Interaction with Biomolecules of Platinum(II) Complexes with Shikimic Acid-Based Ligands

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Yan Peng ◽  
Min-Min Zhang ◽  
Zhen-Feng Chen ◽  
Kun Hu ◽  
Yan-Cheng Liu ◽  
...  
Keyword(s):  
Shikimic Acid ◽  
Covalent Binding ◽  
Carbon Chain ◽  
Water Soluble ◽  
Cytotoxic Activities ◽  
Experimental Conditions ◽  
H Nmr ◽  
Mtt Method ◽  
Low Cytotoxicity

Starting from the active ingredient shikimic acid (SA) of traditional Chinese medicine and NH2(CH2)nOH, (n=2–6), we have synthesized a series of new water-soluble Pt(II) complexes PtLa–eCl2, where La–eare chelating diamine ligands with carbon chain covalently attached to SA (La–e= SA-NH(CH2)nNHCH2CH2NH2; La,n=2; Lb,n=3; Lc,n=4; Ld,n=5; Le,n=6). The results of the elemental analysis, LC-MS, capillary electrophoresis, and1H,13C NMR indicated that there was only one product (isomer) formed under the present experimental conditions, in which the coordinate mode of PtLa–eCl2was two-amine bidentate. Theirin vitrocytotoxic activities were evaluated by MTT method, where these compounds only exhibited low cytotoxicity towards BEL7404, which should correlate their low lipophilicity. The interactions of the five Pt(II) complexes with DNA were investigated by agarose gel electrophoresis, which suggests that the Pt(II) complexes could induce DNA alteration. We also studied the interactions of the Pt(II) complexes with5′-GMP with ESI-MS and1H NMR and found that PtLbCl2, PtLcCl2, and PtLdCl2could react with5′-GMP to form mono-GMP and bis-GMP adducts. Furthermore, the cell-cycle analysis revealed that PtLbCl2, PtLcCl2cause cell G2-phase arrest after incubation for 72 h. Overall, these water-soluble Pt(II) complexes interact with DNA mainly through covalent binding, which blocks the DNA synthesis and replication and thus induces cytotoxicity that weakens as the length of carbon chain increases.

scholarly journals Immunomodulatory Action of Triterpene Glycosides Isolated from the Sea Cucumber Actinocucumis typica. Structure-Activity Relationships

2014 ◽  
Vol 9 (6) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Evgeny A. Pislyagin ◽  
Dmitry L. Aminin ◽  
Alexandra S. Silchenko ◽  
Sergey A. Avilov ◽  
Pelageya V. Andryjashchenko ◽  
...  
Keyword(s):  
Peritoneal Macrophages ◽  
Triterpene Glycosides ◽  
Cytotoxic Activities ◽  
Ros Formation ◽  
Low Toxicity ◽  
Low Cytotoxicity ◽  
Immunomodulatory Action ◽  
Mouse Peritoneal Macrophages ◽  
Stimulation Of

Stimulation of lysosomal activity and ROS formation in mouse peritoneal macrophages by five triterpene glycosides, typicosides A1 (1), A2 (2), B1 (3), C1 (4) and C2 (5) has been studied and compared with their cytotoxic activities. Glycosides 1–3 possess moderate activities, but the most cytotoxic glycoside 5 is not active. Typicoside C1 (4), with low toxicity, was proved to be the most active concerning stimulation of ROS formation. This is the first example of a triterpene glycoside from sea cucumbers with low cytotoxicity, but which demonstrates a strong immunostimulatory effect on mouse peritoneal macrophages in vitro.

Synthesis and in vitro Biological Activity of New 4,6-Disubstituted 3(2H)-Pyridazinone-acetohydrazide Derivatives

2012 ◽  
Vol 67 (5-6) ◽  
pp. 257-265
Author(s):  
Murat Sukuroglu ◽  
Tijen Onkol ◽  
Fatma Kaynak Onurdağ ◽  
Gulsen Akalın ◽  
M. Fethi Şahin
Keyword(s):  
Biological Activity ◽  
Antimicrobial Activities ◽  
Cytotoxic Activities ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
E Coli ◽  
Preliminary Results ◽  
H Nmr ◽  
Pyridazinone Derivatives

New 3(2H)-pyridazinone derivatives containing a N’-benzyliden-acetohydrazide moiety at position 2 were synthesized. The structures of these newly synthesized compounds were confi rmed by IR, 1H NMR, and MS data. These compounds were tested for their antibacterial, antifungal, antimycobacterial, and cytotoxic activities. The compounds 2-[4-(4-chlorophenyl)- 6-(morpholin-4-yl)-3-oxo-(2H)-pyridazin-2-yl]-N’-(4-tert-butylbenzyliden)acetohydrazide and 2-[4-(4-chlorophenyl)-6-(morpholin-4-yl)-3-oxo-(2H)-pyridazin-2-yl]-N’-(4-chlorobenzyliden) acetohydrazide exhibited activity against both Gram-positive and Gram-negative bacteria. Most of the compounds were active against E. coli ATCC 35218. The preliminary results of this study revealed that some target compounds exhibited promising antimicrobial activities

The Method of Coating Fe3O4 with Carbon Nanoparticles to Modify Biological Properties of Oxide Measured in Vitro

2017 ◽  
Vol 100 (4) ◽  
pp. 905-915 ◽  
Author(s):  
Tomasz Niemiec ◽  
Mariusz Dudek ◽  
Natalia Dziekan ◽  
Sławomir Jaworski ◽  
Aleksandra Przewozik ◽  
...  
Keyword(s):  
Chemical Properties ◽  
Chemical Vapor ◽  
Medical Application ◽  
Processing Parameters ◽  
Biological Properties ◽  
Experimental Conditions ◽  
Low Cytotoxicity ◽  
Vitro Model ◽  
Physical And Chemical

Abstract The coating of nanoparticles on materials for medical application [e.g., the coating of Fe3O4 nanopowder (IONP) with a carbon nanolayer] serves to protect and modify the selected biological, physical, and chemical properties of the coated material. Increases in chemical stability, changes in biocompatibility, and a modified surface structure are examples of the effects caused by the formation of carbon coatings. In the current study, Fe3O4 nanoparticles were coated with a carbon nanolayer (IONP@C) in a plasmochemical reactor (using radio-frequency plasma-enhanced chemical vapor deposition methods) under various experimental conditions. Based on data from X-ray diffraction, Raman, and IR spectroscopy, the best processing parameters were determined in order to produce a carbon coating that would not change the structure of the IONP. The materials with the best cover, i.e., a uniform carbon nanolayer, were used in cytotoxic tests to investigate their biological properties using the human HepG2 hepatocarcinoma cell line and chicken embryo red blood cells as an in vitro model. The obtained results proved the low cytotoxicity of Fe3O4 micropowder and IONP in contrast to IONP@C, which reduced cell viability, increased hemolysis, and generally was more toxic than bare Fe3O4.

scholarly journals Abietane Diterpenoids Isolated from Clerodendrum bracteatum and Their Antioxidant and Cytotoxic Activities

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4870
Author(s):  
Pingting Li ◽  
Lingling Li ◽  
Qin Zhu ◽  
Mingfeng Xu
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Cytotoxic Activities ◽  
Dpph Radical ◽  
Mtt Method ◽  
Extensive Analysis ◽  
Abietane Diterpenoids ◽  
New Compounds ◽  
Dpph Radical Scavenging

Two new abietane diterpenoids (1,2), along with five known diterpenoids (3–7), were first isolated and purified from the stems of Clerodendrum bracteatum. The structures of the new compounds were established by extensive analysis of mass spectrometric and 1-D, 2-D NMR spectroscopic data. Their antioxidant activities were determined on DPPH radical scavenging and ABTS. The in vitro cytotoxic activities of the compounds were evaluated against the HL-60 and A549 cell lines by the MTT method.

Labeling Cells with Silver/Dendrimer Nanocomposites

2004 ◽  
Vol 845 ◽  
Author(s):  
Wojciech Lesniak ◽  
Xiangyang Shi ◽  
Anna Bielinska ◽  
Katarzyna Janczak ◽  
Kai Sun ◽  
...  
Keyword(s):  
Aqueous Solution ◽  
Uv Light ◽  
Toxicity Testing ◽  
Water Soluble ◽  
Cell Labeling ◽  
Single Particles ◽  
Experimental Conditions ◽  
Silver Nanocomposite ◽  
Positively Charged

ABSTRACTWe have developed water-soluble, biocompatible, fluorescent, and photostable silver/dendrimer nanocomposites that have a potential to be used for in vitro cell labeling. A PAMAM_E5.NH2 dendrimer was used as a template to prepare first a silver-dendrimer complex in an aqueous solution at biologic pH=7.4. Conversion into nanocomposite was achieved by irradiating the solution of the [(Ag+)25-PAMAM_E5.NH2] complex by UV light to reduce the bound Ag+ to zero-valent Ag0 atoms, which were simultaneously trapped in the dendrimer network. Results indicate that the {(Ag0)25-PAMAM_E5.NH2} silver/dendrimer nanocomposite forms positively charged single particles of 4–5 nm under the experimental conditions used. The dendrimer nanocomposite proved to be fluorescent. Toxicity testing of {(Ag0)25-PAMAM_E5.NH2} nanocomposite revealed a behavior similar to the template dendrimer. Intracellular internalization of the silver nanocomposite and cell labeling capabilities was confirmed by confocal microscopy.

scholarly journals Development of water-soluble prodrugs of the bisdioxopiperazine topoisomerase IIβ inhibitor ICRF-193 as potential cardioprotective agents against anthracycline cardiotoxicity

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Hana Bavlovič Piskáčková ◽  
Hana Jansová ◽  
Jan Kubeš ◽  
Galina Karabanovich ◽  
Nela Váňová ◽  
...  
Keyword(s):  
Plasma Concentrations ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Drug Candidate ◽  
Anthracycline Cardiotoxicity ◽  
Cardioprotective Effects ◽  
Low Cytotoxicity ◽  
Anthracycline Toxicity

AbstractThe bisdioxopiperazine topoisomerase IIβ inhibitor ICRF-193 has been previously identified as a more potent analog of dexrazoxane (ICRF-187), a drug used in clinical practice against anthracycline cardiotoxicity. However, the poor aqueous solubility of ICRF-193 has precluded its further in vivo development as a cardioprotective agent. To overcome this issue, water-soluble prodrugs of ICRF-193 were prepared, their abilities to release ICRF-193 were investigated using a novel UHPLC-MS/MS assay, and their cytoprotective effects against anthracycline cardiotoxicity were tested in vitro in neonatal ventricular cardiomyocytes (NVCMs). Based on the obtained results, the bis(2-aminoacetoxymethyl)-type prodrug GK-667 was selected for advanced investigations due to its straightforward synthesis, sufficient solubility, low cytotoxicity and favorable ICRF-193 release. Upon administration of GK-667 to NVCMs, the released ICRF-193 penetrated well into the cells, reached sufficient intracellular concentrations and provided effective cytoprotection against anthracycline toxicity. The pharmacokinetics of the prodrug, ICRF-193 and its rings-opened metabolite was estimated in vivo after administration of GK-667 to rabbits. The plasma concentrations of ICRF-193 reached were found to be adequate to achieve cardioprotective effects in vivo. Hence, GK-667 was demonstrated to be a pharmaceutically acceptable prodrug of ICRF-193 and a promising drug candidate for further evaluation as a potential cardioprotectant against chronic anthracycline toxicity.

scholarly journals In VitroAntiparasitic and Apoptotic Effects of Antimony Sulfide Nanoparticles onLeishmania infantum

2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
Saied Soflaei ◽  
Abdolhossein Dalimi ◽  
Fatemeh Ghaffarifar ◽  
Mojtaba Shakibaie ◽  
Ahmad Reza Shahverdi ◽  
...  
Keyword(s):  
Antimony Sulfide ◽  
Mtt Method ◽  
Amastigote Stage ◽  
Viable Cells ◽  
Promastigote Form ◽  
Low Cytotoxicity ◽  
Cytotoxicity Effects ◽  
Apoptotic Effects ◽  
Dose Dependent

Visceral leishmaniasis is one of the most important sever diseases in tropical and subtropical countries. In the present study the effects of antimony sulfide nanoparticles onLeishmania infantum in vitrowere evaluated. Antimony sulfide NPs (Sb2S5) were synthesized by biological method fromSerratia marcescensbacteria. Then the cytotoxicity effects of different concentrations (5, 10, 25, 50, and 100 μg/mL) of this nanoparticle were assessed on promastigote and amastigote stages ofL. infantum. MTT method was used for verification results of promastigote assay. Finally, the percentages of apoptotic, necrotic, and viable cells were determined by flow cytometry. The results indicated the positive effectiveness of antimony sulfide NPs on proliferation of promastigote form. The IC50(50% inhibitory concentration) of antimony sulfide NPs on promastigotes was calculated 50 μg/mL. The cytotoxicity effect was dose-dependent means by increasing the concentration of antimony sulfide NPs, the cytotoxicity curve was raised and the viability curve of the parasite dropped simultaneously. Moreover, the IC50of antimony sulfide NPs on amastigote stage was calculated 25 μg/mL. On the other hand, however, antimony sulfide NPs have a low cytotoxicity effect on uninfected macrophages but it can induce apoptosis in promastigote stage at 3 of 4 concentrations.

scholarly journals Facile synthesis, characterization, and cytotoxicity study of new 3-(indol-2-yl)bicyclotetrazatridecahexaens

2017 ◽  
Vol 95 (8) ◽  
pp. 858-862 ◽  
Author(s):  
Kamal Sweidan ◽  
Dima A. Sabbah ◽  
Sanaa Bardaweel ◽  
Ghassan Abu Sheikha ◽  
Tariq Al-Qirim ◽  
...  
Keyword(s):  
Condensation Reaction ◽  
Hct116 Cell ◽  
Chloroacetic Acid ◽  
Human Colon ◽  
Cytotoxic Activities ◽  
Human Skin Fibroblast ◽  
Normal Human Skin ◽  
H Nmr ◽  
Elemental Analyses

A new series of thiosemicarbazone-based indole derivatives 12–15 has been prepared by condensation reaction of indole-2-carboxamide derivatives 8–11 with thiosemicarbazide. The former compounds underwent intracyclization in the presence of chloroacetic acid and sodium acetate to afford a set of new 3-(indol-2-yl)bicyclotetrazatridecahexaens 16–19. These newly synthesized compounds have been characterized by means of FTIR, 1H NMR, 13C NMR, and HRMS and by elemental analyses. Cytotoxic activities of the prepared compounds along with LY294002 were evaluated in vitro against normal human skin fibroblast, human colon carcinoma (HCT116), and leukemia (K562) cell lines; results revealed that the series inhibits only HCT116 cell line. In addition, results showed that compound 18 exerts moderate potency in HCT116 with an IC50 value of 54 μmol/L and significantly induces apoptosis.

scholarly journals Water-soluble Constituents of the Heartwood of Streblus asper

2012 ◽  
Vol 7 (5) ◽  
pp. 1934578X1200700
Author(s):  
Jun Li ◽  
Mao-Tong Tang ◽  
Qiang Wu ◽  
Hong Chen ◽  
Xiao-Tao Niu ◽  
...  
Keyword(s):  
Optical Rotation ◽  
2D Nmr ◽  
Water Soluble ◽  
Coupling Constants ◽  
Meoh Extract ◽  
H Nmr ◽  
Streblus Asper ◽  
C Nmr ◽  
Soluble Part

A new lignan, (7′ R,8′ R)- threo-strebluslignanol-2- O-β-D-glucopyranoside, along with 8 known compounds (2–9) were isolated from the water-soluble part of the MeOH extract of the heartwood of Streblus asper. Their structures were elucidated through various spectroscopic methods, including 1D NMR (1H NMR, 13C NMR), 2D NMR (HMQC, HMBC, and NOESY), and HRMS. The stereochemistry at the chiral centers was determined using the CD spectrum, as well as analyses of coupling constants and optical rotation data. In the preliminary bioassay, the isolated compounds did not show anti-HBV activities in vitro using the HBV transfected HepG2.2.15 cell line.

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