An asymmetric binuclear zinc(ii) complex with mixed iminodiacetate and phenanthroline ligands: synthesis, characterization, structural conversion and anticancer properties

2016 ◽  
Vol 3 (7) ◽  
pp. 959-968 ◽  
Author(s):  
Lubin Ni ◽  
Juan Wang ◽  
Chang Liu ◽  
Jinhong Fan ◽  
Yun Sun ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Chemotherapeutic Agent ◽  
Water Soluble ◽  
Structural Conversion ◽  
Anticancer Properties ◽  
Low Toxicity ◽  
Phenanthroline Ligands

A water-soluble asymmetric binuclear zinc(ii) complex with mixed iminodiacetate and 1,10-phenanthroline ligands exhibited promising anticancer activity and low toxicity, suggesting potential as a chemotherapeutic agent.

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.

Design of Lamivudine Loaded Nanoparticles for Oral Application by Nano Spray Drying Method: A New Approach to use an Antiretroviral Drug for Lung Cancer Treatment

2020 ◽  
Vol 23 (10) ◽  
pp. 1064-1079
Author(s):  
Ahmet Alper Öztürk ◽  
İrem Namlı ◽  
Kadri Güleç ◽  
Şennur Görgülü
Keyword(s):  
Lung Cancer ◽  
Cancer Treatment ◽  
Anticancer Activity ◽  
Cell Line ◽  
Anticancer Drugs ◽  
Release Kinetics ◽  
Prolonged Release ◽  
Lung Cancer Treatment ◽  
Anticancer Properties ◽  
Ft Ir

Aims: To prepare lamivudine (LAM)-loaded-nanoparticles (NPs) that can be used in lung cancer treatment. To change the antiviral indication of LAM to anticancer. Background: The development of anticancer drugs is a difficult process. One approach to accelerate the availability of drugs is to reclassify drugs approved for other conditions as anticancer. The most common route of administration of anticancer drugs is intravenous injection. Oral administration of anticancer drugs may considerably change current treatment modalities of chemotherapy and improve the life quality of cancer patients. There is also a potentially significant economic advantage. Objective: To characterize the LAM-loaded-NPs and examine the anticancer activity. Methods: LAM-loaded-NPs were prepared using Nano Spray-Dryer. Properties of NPs were elucidated by particle size (PS), polydispersity index (PDI), zeta potential (ZP), SEM, encapsulation efficiency (EE%), dissolution, release kinetics, DSC and FT-IR. Then, the anticancer activity of all NPs was examined. Results: The PS values of the LAM-loaded-NPs were between 373 and 486 nm. All NPs prepared have spherical structure and positive ZP. EE% was in a range of 61-79%. NPs showed prolonged release and the release kinetics fitted to the Weibull model. NPs structures were clarified by DSC and FT-IR analysis. The results showed that the properties of NPs were directly related to the drug:polymer ratio of feed solution. NPs have potential anticancer properties against A549 cell line at low concentrations and non-toxic to CCD 19-Lu cell line. Conclusion: NPs have potential anticancer properties against human lung adenocarcinoma cells and may induce cell death effectively and be a potent modality to treat this type of cancer. These experiments also indicate that our formulations are non-toxic to normal cells. It is clear that this study would bring a new perspective to cancer therapy.

scholarly journals Anticancer Activity of Triazolo-Thiadiazole Derivatives and Inhibition of AKT1 and AKT2 Activation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 493
Author(s):  
Dimitrios T. Trafalis ◽  
Sofia Sagredou ◽  
Panayiotis Dalezis ◽  
Maria Voura ◽  
Stella Fountoulaki ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Human Colon ◽  
Tumor Xenograft ◽  
Atp Binding Site ◽  
Anticancer Properties ◽  
Extensive Range ◽  
Dependent Inhibition ◽  
Ht 29

The fusion of 1,2,4-triazole and 1,3,4-thiadiazole rings results in a class of heterocycles compounds with an extensive range of pharmacological properties. A series of 1,2,4-triazolo[3,4-b]-1,2,4-thiadiazoles was synthesized and tested for its enzyme inhibition potential and anticancer activity. The results show that 1,2,4-triazolo[3,4-b]-1,2,4-thiadiazoles display potent anticancer properties in vitro against a panel of cancer cells and in vivo efficacy in HT-29 human colon tumor xenograft in CB17 severe combined immunodeficient (SCID) mice. Preliminary mechanistic studies revealed that KA25 and KA39 exhibit time- and concentration-dependent inhibition of Akt Ser-473 phosphorylation. Molecular modeling experiments indicated that 1,2,4-triazolo[3,4-b]-1,2,4-thiadiazoles bind well to the ATP binding site in Akt1 and Akt2. The low acute toxicity combined with in vitro and in vivo anticancer activity render triazolo[3,4-b]thiadiazoles KA25, KA26, and KA39 promising cancer therapeutic agents.

scholarly journals A Nitrocarbazole as a New Microtubule-Targeting Agent in Breast Cancer Treatment

2021 ◽  
Vol 11 (19) ◽  
pp. 9139
Author(s):  
Maria Stefania Sinicropi ◽  
Cinzia Tavani ◽  
Camillo Rosano ◽  
Jessica Ceramella ◽  
Domenico Iacopetta ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Breast Cancer Cell Lines ◽  
Cellular Functions ◽  
Anticancer Properties ◽  
Cycle Arrest ◽  
In Silico Studies ◽  
Ic50 Values ◽  
Mcf 7

Breast cancer is still considered a high-incidence disease, and numerous are the research efforts for the development of new useful and effective therapies. Among anticancer drugs, carbazole compounds are largely studied for their anticancer properties and their ability to interfere with specific targets, such as microtubule components. The latter are involved in vital cellular functions, and the perturbation of their dynamics leads to cell cycle arrest and subsequent apoptosis. In this context, we report the anticancer activity of a series of carbazole analogues 1–8. Among them, 2-nitrocarbazole 1 exhibited the best cytotoxic profile, showing good anticancer activity against two breast cancer cell lines, namely MCF-7 and MDA-MB-231, with IC50 values of 7 ± 1.0 and 11.6 ± 0.8 μM, respectively. Furthermore, compound 1 did not interfere with the growth of the normal cell line MCF-10A, contrarily to Ellipticine, a well-known carbazole derivative used as a reference molecule. Finally, in vitro immunofluorescence analysis and in silico studies allowed us to demonstrate the ability of compound 1 to interfere with tubulin organization, similarly to vinblastine: a feature that results in triggering MCF-7 cell death by apoptosis, as demonstrated using a TUNEL assay.

scholarly journals CURCUMIN, A NATURAL GOLDEN DRUG AND ITS ANTICANCER ASPECTS FROM SYNTHESIS TO DELIVERY: A REVIEW

2020 ◽  
pp. 70-84
Author(s):  
GEETA KRISHNAMURTHY ◽  
DEEPTI ROY ◽  
JYOTSNA KUMAR
Keyword(s):  
Side Effects ◽  
Anticancer Activity ◽  
Review Paper ◽  
Chemotherapeutic Agent ◽  
Wide Spectrum ◽  
Curcuma Longa ◽  
Structure Modification ◽  
Synthetic Drugs ◽  
Effective Drugs ◽  
Novel Delivery Systems

Cancer is a dreadful disease and, in most cases, leads to death even when it is being treated. Even though synthetic drugs are still in use for the treatment of cancer, the seriousness of the side effects of these drugs has boggled researcher’s mind to find more effective drugs which will help to overcome the side effects and have greater potency in trying to make the patient completely free of the disease. Recently, researchers turned their attention towards bio-components present in natural products. Curcumin, a polyphenol and the main constituent of a rhizome Curcuma longa, has geared significant interest due to its wide spectrum of therapeutics values, especially anticancer activity. Paper summarizes the chemistry and bio-metabolism of curcumin in the human body. Aim of this review article is to gather the dispersed efforts of researchers predominantly in improving the bioavailability of curcumin. In the present review, comprehensive literature on anticancer activity of Curcumin via combination therapy, structure modification, synthesis of analogues, novel delivery systems have been highlighted. Besides, the review paper explicated several challenges associated with Curcumin as an adjuvant chemotherapeutic agent and emphasizes more on clinical studies.

In-Vitro Antioxidant, Antibacterial and Anticancer properties of Leaf Extract Annona Muricata

2021 ◽  
Vol 8 (1) ◽  
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Activity ◽  
Antioxidant Activities ◽  
Extraction Procedure ◽  
Radical Scavenging ◽  
Antibacterial Activities ◽  
Diffusion Method ◽  
Annona Muricata ◽  
Anticancer Properties

Annona muricata is one of the important herbal plant that are widely used to treat antidiabetic, anti-inflammatory, insecticidal, antimalarial, anticancer, antibacterial and antioxidant activities. In the present study, extraction procedure was carried out in few step processes method. The extract contains high percentage of steroid, alkaloid, flavonoid, phenolic and saponin. The extract was used to study the antioxidant activity; antibacterial activities and anticancer activity by standard methods. The antioxidant activity was studied by using radical scavenging DPPH, FRAP and H2O2 method and disc diffusion method. The results of antibacterial activity of the following bacteria’s such as Pseudomonas, Staphylococcus, Bacillus, E.coli shows the maximum zone of inhibition against Staphylococcus aureus which is around 1.7 cm. The anticancer activity was carried out by MTT assay using Hep-G2 as cell line and results are reported in the paper.

scholarly journals Selenium Anticancer Properties and Impact on Cellular Redox Status

Antioxidants ◽  
2020 ◽  
Vol 9 (1) ◽  
pp. 80 ◽  
Author(s):  
Lolita Kuršvietienė ◽  
Aušra Mongirdienė ◽  
Jurga Bernatonienė ◽  
Jurgita Šulinskienė ◽  
Inga Stanevičienė
Keyword(s):  
Anticancer Activity ◽  
Antioxidant Activities ◽  
Chemotherapeutic Agents ◽  
Redox Activity ◽  
Biological Functions ◽  
Cellular Redox ◽  
Selenium Compounds ◽  
Anticancer Properties ◽  
Redox Active ◽  
The Impact

(1) Background: In this review, we provide information published in recent years on the chemical forms, main biological functions and especially on antioxidant and prooxidant activities of selenium. The main focus is put on the impact of selenoproteins on maintaining cellular redox balance and anticancerogenic function. Moreover, we summarize data on chemotherapeutic application of redox active selenium compounds. (2) Methods: In the first section, main aspects of metabolism and redox activity of selenium compounds is reviewed. The second outlines multiple biological functions, asserted when selenium is incorporated into the structure of selenoproteins. The final section focuses on anticancer activity of selenium and chemotherapeutic application of redox active selenium compounds as well. (3) Results: optimal dietary level of selenium ensures its proper antioxidant and anticancer activity. We pay special attention to antioxidant activities of selenium compounds, especially selenoproteins, and their importance in antioxidant defence. It is worth noting, that data on selenium anticancer properties is still contraversive. Moreover, selenium compounds as chemotherapeutic agents usually are used at supranutritional doses. (4) Conclusions: Selenium play a vital role for many organism systems due to its incorporation into selenoproteins structure. Selenium possesses antioxidant activity at optimal doses, while at supranutritional doses, it displays prooxidant activity. Redox active selenium compounds can be used for cancer treatment; recently special attention is put to selenium containing nanoparticles.

scholarly journals Photoactivated in Vitro Anticancer Activity of Rhenium(I) Tricarbonyl Complexes Bearing Water-Soluble Phosphines

2018 ◽  
Vol 57 (3) ◽  
pp. 1311-1331 ◽  
Author(s):  
Sierra C. Marker ◽  
Samantha N. MacMillan ◽  
Warren R. Zipfel ◽  
Zhi Li ◽  
Peter C. Ford ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Water Soluble ◽  
Water Soluble Phosphines
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