scholarly journals IN-VITRO ANTICANCER ACTIVITY AND DNA CLEVAGE OF BIOLOGICALLY ACTIVE VO(II) COMPLEX WITH ETHYL-4-AMINOBENZOATE AND OXALATE ION

2020 ◽  
Vol 12 (02) ◽  
pp. 934-939
Author(s):  
B. Sathiyamoorthy ◽  
K. Rajasekar ◽  
S. Balasubramaniyan ◽  
R. Selvarani ◽  
C. Veravel
Keyword(s):  
Anticancer Activity ◽  
Biologically Active ◽  
Oxalate Ion

scholarly journals SYNTHESIS AND CHARACTERIZATION OF CYCLOHEXANE-1,3-DIONE DERIVATIVES AND THEIR IN SILICO AND IN VITRO STUDIES ON ANTIMICROBIAL AND BREAST CANCER ACTIVITY

2019 ◽  
pp. 311-320 ◽  
Author(s):  
RAJA CHINNAMANAYAKAR ◽  
EZHILARASI MR ◽  
PRABHA B ◽  
KULANDHAIVEL M
Keyword(s):  
Breast Cancer ◽  
Antimicrobial Activity ◽  
Anticancer Activity ◽  
Mtt Assay ◽  
In Silico ◽  
Biologically Active ◽  
Diffusion Method ◽  
Breast Adenocarcinoma ◽  
In Silico Docking

Objective: The objective of this study was to evaluate in silico and in vitro anticancer activity for synthesized cyclohexane-1,3-dione derivatives. Methods: The new series of cyclohexane-1,3-dione derivatives were synthesized based on the Michael addition reaction. Further, the structures of the synthesized compounds were confirmed by Fourier-transform infrared spectroscopy, 1H nuclear magnetic resonance (NMR), and 13C NMR spectral data. Then, the in silico molecular docking studies were carried out using AutoDock tool version 1.5.6 and AutoDock version 4.2.5.1 docking program. The antimicrobial activity was carried out using the agar disk diffusion method, and the in vitro anticancer activity was performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay for the synthesized compound. Results: In silico docking study, compound 5c showed good binding score and binding interactions with selected bacterial proteins and breast cancer protein. Further, compound (5a-5h) was tested for their antimicrobial activity and compound 5c was only tested for anticancer activity (human breast adenocarcinoma 3,4-methylenedioxyamphetamine-MB-231 cell line). Compound 5c was found to be the most active one of all the tested compounds. In the MTT assay compound, 5c showed the LC50 value of 10.31±0.003 μg/ml. In antimicrobial activity, the minimum inhibitory concentration of compound 5c is 2.5 mg/ml. Conclusion: An efficient synthesis of biologically active cyclohexane-1, 3-dione derivatives has been developed.

scholarly journals Ruthenium(II) and Platinum(II) Complexes with Biologically Active Aminoflavone Ligands Exhibit In Vitro Anticancer Activity

2021 ◽  
Vol 22 (14) ◽  
pp. 7568
Author(s):  
Małgorzata Fabijańska ◽  
Maria M. Kasprzak ◽  
Justyn Ochocki
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Cisplatin Resistance ◽  
Annexin V ◽  
Biologically Active ◽  
Caspase 8 ◽  
Mitochondrial Potential ◽  
Apoptosis Pathway ◽  
Ruthenium Compounds

Continuing our studies on the mechanisms underlying the cytotoxicity of potential drugs, we have described several aspects of the in vitro anticancer activity of ruthenium(II) and platinum(II) complexes with bioactive, synthetic aminoflavone ligands. We examined the mechanism of proapoptotic activity of cis-dichlorobis(3-imino-2-methoxyflavanone)ruthenium(II), cis-dichlorobis(3-imino-2-ethoxyflavanone)ruthenium(II), and trans-dichlorobis(3-aminoflavone)platinum(II). Cisplatin was used as a reference compound. The cytotoxicity was investigated by MTT assay. The mechanism of proapoptotic activity of the tested compounds was investigated by evaluation of caspase-8 activity, cytometric analysis of annexin-V positive cells, and mitochondrial potential loss measurement. The results showed that ruthenium compounds break partially or completely the cisplatin resistance by activating the caspase 8-dependent apoptosis pathway and loss of mitochondrial membrane potential. Platinum compounds also have a cytostatic effect, but their action requires more exposure time. Potential mechanisms underlying drug resistance in the two pairs of cancer cell lines were investigated: total glutathione content, P-glycoprotein activity, and differences in the activity of DNA repair induced by nucleotide excision. Results showed that cisplatin-resistant cells have elevated glutathione levels relative to sensitive cells. Moreover, they indicated the mechanisms enabling cells to avoid apoptosis caused by DNA damage. Pg-P activity has no effect on the development of cisplatin resistance in the cell lines described.

scholarly journals Bis-Pyridazine Derivatives with Anticancer Activity

Proceedings ◽  
2019 ◽  
Vol 22 (1) ◽  
pp. 6
Author(s):  
Dorina ◽  
Ionel ◽  
Vasilichia ◽  
Violeta
Keyword(s):  
Lung Cancer ◽  
Growth Inhibition ◽  
Small Cell Lung Cancer ◽  
Anticancer Activity ◽  
Cell Lung Cancer ◽  
Small Cell ◽  
Biologically Active ◽  
Small Cell Lung ◽  
Pyridazine Derivatives

Over the last decades, pyridazine derivatives are considered “privileged structures” in medicinal chemistry, with special attention being given to pyridazinones derivatives, which were found to have a large range of biological activities, including anticancer. On the other hand, because of the huge difficulties in cancer treatment, there is an urgent need from the pharmaceutical industry for new anticancer drug candidates. As part of our ongoing efforts in searching for new biologically active entities with anticancer potential, we report here the design, synthesis, structure and in vitro anticancer activity of a new class of pyridazinones derivatives, namely bis-pyridazinones. The structures of the compounds were proven by elemental and spectral analysis: IR, LC-MS, 1H-NMR, 13C-NMR, two-dimensional experiments 2D-COSY, HMQC, and HMBC. A few of the compounds were accepted by the National Cancer Institute (USA) for anticancer screening and were evaluated for their in vitro cytotoxic activity against a panel of 60 human tumor cell lines, representing cancers of the brain, breast, colon, kidney, lung, ovary, prostate, as well as leukemia and melanoma. Three of the tested compounds have proven to be active against non-small cell lung cancer HOP 92 and NCI-H226, CNC cancer SNB-75, renal cancer A498 and UO-31, with a growth inhibition between 50–80 mM. Interestingly, one compound (unsubstituted bis-pyridazinones I) has a selective anticancer activity, being active only on non-small cell lung cancer HOP 92, with a growth inhibition of 51.45 mM. SAR correlation has been performed.

scholarly journals Sulfated polysaccharides from Phaeodactylum tricornutum: isolation, structural characteristics, and inhibiting HepG2 growth activity in vitro

PeerJ ◽  
2019 ◽  
Vol 7 ◽  
pp. e6409 ◽  
Author(s):  
Shengfeng Yang ◽  
Haitao Wan ◽  
Rui Wang ◽  
Daijun Hao
Keyword(s):  
Anticancer Activity ◽  
Hepg2 Cells ◽  
Phaeodactylum Tricornutum ◽  
Structural Characteristics ◽  
Sulfated Polysaccharide ◽  
Biologically Active ◽  
Sulfated Polysaccharides ◽  
Dependent Manner ◽  
Active Components

Microalgae, eukaryotic unicellular plants, are increasing in demand due to their use as nutraceutical and food supplements. They consisted different kinds of biologically active components such as polysaccharides. On the other hand, cancer is the leading cause of death globally. At present, there is no efficient method to cure it. Therefore, in this work, we extracted polysaccharides from Phaeodactylum tricornutum (PTP), characterized the chemical composition and structure, and investigated its anticancer activity on HepG2 cells. The results showed that PTP was a sulfated polysaccharide with a high Mw of 4,810 kDa, and xylose, fucose, glucose and galactose were the main monosaccharides. PTP has significant anticancer activity in a dose-dependent manner (up to 60.37% at 250 ug/mL) according to MTT assays. Furthermore, cycle analysis was carried out to explain its anticancer activity. The results showed that it exhibited anticancer effect mainly through the induction of apoptosis without affecting the cycle and mitosis of HepG2 cells. This might make it a potential drug for anticancer treatment in the future.

scholarly journals Examination of in Vitro Anticancer Activity of Crude Extracts Obtained from Two Bacterial Strains Isolated from Kodiyampalayam, Tamil Nadu

2019 ◽  
Vol 8 (3S2) ◽  
pp. 291-295
Keyword(s):  
Anticancer Activity ◽  
Tamil Nadu ◽  
Biological Activities ◽  
Biologically Active ◽  
Morphological Alteration ◽  
Nuclear Staining ◽  
Kb Cells ◽  
Morphological Studies ◽  
Oral Squamous Carcinoma

Extracts of natural products, especially microorganisms, have been a valuable source of various molecules in many drug discovery efforts and led to the discovery of many important drugs. The identification of microbial strains with promising biological activities and the purification of biomolecules responsible for activities led to the discovery of many biologically active molecules.Crude extracts of two marine bacterial isolates isolated from marine sediment samples, were studied for their in vitro anticancer activity against human oral squamous carcinoma (KB) cell line. Morphological studies and biochemical tests of the two bacterial extracts were also carried out. Cytotoxic, intracellular ROS, nuclear staining and apoptotic morphological alteration studies were carried out to assess the anticancer potential of each extract. The crude ethyl acetate extract of KP-9 isolate showed promising results by MTT assay with IC50 as low as 7.9 μg/ml while as KP-7 showed an IC50 value of 21.1μg/ml in KB cells. The crude extract of KP-9 augmented higher levels of ROS and displayed higher potential by inducing higher levels of nuclear and morphological alterations when compared with KP-7 bacterial extract in KB cells.

“In vitro” Neutralization with Oxalate Ion of the Anticoagulant Effect of Heparin

1961 ◽  
Vol 05 (02) ◽  
pp. 314-318 ◽  
Author(s):  
W. O Cruz ◽  
L Meis ◽  
C. P Dietrich
Keyword(s):  
Calcium Oxalate ◽  
Aluminium Hydroxide ◽  
Barium Sulfate ◽  
Anticoagulant Effect ◽  
Normal Plasma ◽  
Oxalate Ion

SummaryHeparinized blood or plasma coagulates if, after addition of oxalate, recalcification follows. Of the decalcifying agents only oxalate ion has been suitable for demonstrating this phenomenon. Oxalate seem to accomplish two different roles connected with this effect: a fundamental one, i. e., to sensitize a heparinlipoprotein complex to the action of an anti-heparin factor found in normal plasma or serum and a secondary one, related to its capacity to adsorb this antiheparin factor. The latter is removable by centrifugation. This anti-heparin oxalate factor, which is able to counteract the action of heparin after previous addition of oxalate, was found in sequestrened, Dowex 50 resin plasma or in serum, but is not active in citrated plasma. This factor was removed from plasma by adsorption with barium sulfate, aluminium hydroxide or calcium oxalate and was eluted from these adsorbants after incubation with saline.

Vitamin D as potential therapeutic anticancer agent

2018 ◽  
pp. 1-3
Keyword(s):  
Vitamin D ◽  
Anticancer Activity ◽  
Anticancer Agent ◽  
Antitumor Agents ◽  
Metastatic Potential ◽  
Anticancer Properties ◽  
Chemotherapy Agents

The role of vitamin D is implicated in carcinogenesis through numerous biological processes like induction of apoptosis, modulation of immune system inhibition of inflammation and cell proliferation and promotion of cell differentiation. Its use as additional adjuvant drug with cancer treatment may be novel combination for improved outcome of different cancers. Numerous preclinical, epidemiological and clinical studies support the role of vitamin D as an anticancer agent. Anticancer properties of vitamin D have been studied widely (both in vivo and in vitro) among various cancers and found to have promising results. There are considerable data that indicate synergistic potential of calcitriol and antitumor agents. Possible mechanisms for modulatory anticancer activity of vitamin D include its antiproliferative, prodifferentiating, and anti-angiogenic and apoptic properties. Calcitriol reduces invasiveness and metastatic potential of many cancer cells by inhibiting angiogenesis and regulating expression of the key molecules involved in invasion and metastasis. Anticancer activity of vitamin D is synergistic or additive with the antineoplastic actions of several drugs including cytotoxic chemotherapy agents like paclitaxel, docetaxel, platinum base compounds and mitoxantrone. Benefits of addition of vitamin D should be weighed against the risk of its toxicity.

Properties and Biotechnological Application of mutant Derivatives of Mini-intein PRP8 from Penicillium chrysogenum with Improved Control of C-terminal Processing

2019 ◽  
Vol 35 (6) ◽  
pp. 91-101
Author(s):  
F.A. Klebanov ◽  
S.E. Cheperegin ◽  
D.G. Kozlov
Keyword(s):  
Penicillium Chrysogenum ◽  
Protein Denaturation ◽  
Biologically Active ◽  
Cultivation Temperature ◽  
Target Proteins ◽  
E Coli ◽  
Complete Inactivation ◽  
Target Molecules ◽  
Proteins And Peptides

Mutant variants of mini-intein PRP8 from Penicillium chrysogenum (Int4b) with improved control of C-terminal processing were characterized. The presented variants can serve as a basis for self-removed polypeptide tags capable of carrying an affine label and allowing to optimize the process of obtaining target proteins and peptides in E. coli cells. They allow to synthesize target molecules in the composition of soluble and insoluble hybrid proteins (fusions), provide their afnne purification, autocatalytic processing and obtaining mature target products. The presented variants have a number of features in comparison with the known prototypes. In particular the mutant mini-intein Int4bPRO, containing the L93P mutation, has temperature-dependent properties. At cultivation temperature below 30 °C it allows the production of target molecules as part of soluble fusions, but after increasing of cultivation temperature to 37 °C it directs the most of synthesized fusions into insoluble intracellular aggregates. The transition of Int4bPRO into insoluble form is accompanied by complete inactivation of C-terminal processing. Further application of standard protein denaturation-renaturation procedures enable efficiently reactivate Int4bPRO and to carry out processing of its fusions in vitro. Two other variants, Int4b56 and Int4b36, containing a point mutation T62N or combination of mutations D144N and L146T respectively, have a reduced rate of C-terminal processing. Their use in E. coli cells allows to optimize the biosynthesis of biologically active target proteins and peptides in the composition of soluble fusions, suitable for afnne purification and subsequent intein-dependent processing without the use of protein denaturation-renaturation procedures. intein, fusion, processing, processing rate, gelonin The work was supported within the framework of the State Assignment no. 595-00003-19 PR.

Metabolomics of Healthy Berry Fruits

2019 ◽  
Vol 25 (37) ◽  
pp. 4888-4902 ◽  
Author(s):  
Gilda D'Urso ◽  
Sonia Piacente ◽  
Cosimo Pizza ◽  
Paola Montoro
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
In Vivo Studies ◽  
Bioactive Metabolites ◽  
Active Metabolites ◽  
Positive Effects ◽  
Cell Functions ◽  
Berry Fruits

The consumption of berry-type fruits has become very popular in recent years because of their positive effects on human health. Berries are in fact widely known for their health-promoting benefits, including prevention of chronic disease, cardiovascular disease and cancer. Berries are a rich source of bioactive metabolites, such as vitamins, minerals, and phenolic compounds, mainly anthocyanins. Numerous in vitro and in vivo studies recognized the health effects of berries and their function as bioactive modulators of various cell functions associated with oxidative stress. Plants have one of the largest metabolome databases, with over 1200 papers on plant metabolomics published only in the last decade. Mass spectrometry (MS) and NMR (Nuclear Magnetic Resonance) are the most important analytical technologies on which the emerging ''omics'' approaches are based. They may provide detection and quantization of thousands of biologically active metabolites from a tissue, working in a ''global'' or ''targeted'' manner, down to ultra-trace levels. In the present review, we highlighted the use of MS and NMR-based strategies and Multivariate Data Analysis for the valorization of berries known for their biological activities, important as food and often used in the preparation of nutraceutical formulations.

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