scholarly journals Synthesis, Characterization of Poly Heterocyclic Compounds, and Effect on Cancer Cell (Hep-2) In vitro.

2018 ◽  
Vol 15 (4) ◽  
pp. 415-524
Author(s):  
Baghdad Science Journal
Keyword(s):  
Cancer Cells ◽  
Diazonium Salt ◽  
Biological Effects ◽  
Acid Synthesis ◽  
Amine Hydrochloride ◽  
Spectrophotometric Methods ◽  
Heterocyclic Derivatives ◽  
Ft Ir ◽  
Reaction Compound

A synthesis series of new heterocyclic derivatives (A2-A7) (pyrrole, pyridazine, oxazine and imidazol) derived from 4-acetyl-2,5-dichloro-1-(3,5-dinitrophenyl)-1H-pyrrole-3-carboxylate(A1) have been synthesised. Synthesis of compound (A2) by the reaction of starting material (A1) with hydroxyl amine hydrochloride in the presence of pyridine. Compound (A2) was reacted with hydrazine hydrate in dry benzene to give (A3) derivative. The compound )A3( deals with sodium nitrite to give diazonium salt, and the reaction diazonium salt with ethyl acetoacetate to produce compound (A4). To a mixture of compound (A4) and hydroxyl amine with sttired to yield (A5).Compound (A6) was prepared by reaction compound (A4) with thiosemicarbazide in presence of drops of acetic acid. Synthesis of 1compound (A7) by reaction compound (A6) with ethyl chloro acetate. The reactions have been monitored by TLC and the synthesized compounds were characterized using spectrophotometric methods FT-IR, 1H NMR.The biological effects of the prepared compounds on the cancer cells were studied in vitro. The results indicated that these Synthesized compounds (A1–A7) inhibited1 the cancer1 cells1 efficiently, the compound (A6) was activity inhibited on the cancer cells.

scholarly journals Sulforaphene induces apoptosis and inhibits the invasion of esophageal cancer cells through MSK2/CREB/Bcl-2 and cadherin pathway in vivo and in vitro

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Chengjuan Zhang ◽  
Junxia Zhang ◽  
Qiong Wu ◽  
Benling Xu ◽  
Guoguo Jin ◽  
...  
Keyword(s):  
Esophageal Cancer ◽  
Cancer Cells ◽  
Cell Apoptosis ◽  
Biological Effects ◽  
Migration And Invasion ◽  
Global Changes ◽  
Fcm Analysis ◽  
Esophageal Cancer Cells

Abstract Background As a novel type of isothiocyanate derived from radish seeds from cruciferous vegetables, sulforaphene (SFE, 4-methylsufinyl-3-butenyl isothiocyanate) has various important biological effects, such as anti-oxidative and anti-bacterial effects. Recently, sulforaphene has attracted increasing attention for its anti-tumor effects and its ability to suppress the development of multiple tumors through different regulatory mechanisms. However, it has not yet been widely investigated for the treatment of esophageal cancer. Methods We observed an increased apoptosis in esophageal cancer cells on sulforaphene treatment through flow cytometry (FCM) analysis and transmission electron microscopy (TEM). Through mass spectrometry (MS) analysis, we further detected global changes in the proteomes and phosphoproteomes of esophageal cancer cells on sulforaphene treatment. The molecular mechanism of sulforaphene was verified by western blot,the effect and mechanism of SFE on esophageal cancer was further verified by patient-derived xenograft mouse model. Results We identified multiple cellular processes that were changed after sulforaphene treatment by proteomics. We found that sulforaphene could repress the phosphorylation of CREB through MSK2, leading to suppression of Bcl-2 and further promoted cell apoptosis. Additionally, we confirmed that sulforaphene induces tumor cell apoptosis in mice. Interestingly, we also observed the obvious inhibition of cell migration and invasion caused by sulforaphene treatment by inhibiting the expression of cadherin, indicating the complex effects of sulforaphene on the development of esophageal cancer. Conclusions Our data demonstrated that sulforaphene induced cell apoptosis and inhibits the invasion of esophageal cancer through a mechanism involving the inhibition of the MSK2–CREB–Bcl2 and cadherin pathway. Sulforaphene could therefore serve as a promising anti-tumor drug for the treatment of esophageal cancer.

scholarly journals Pectin-Tannic Acid Nano-Complexes Promote the Delivery and Bioactivity of Drugs in Pancreatic Cancer Cells

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 285 ◽  
Author(s):  
Sumeet S. Chauhan ◽  
Advait B. Shetty ◽  
Elham Hatami ◽  
Pallabita Chowdhury ◽  
Murali M. Yallapu
Keyword(s):  
Drug Delivery ◽  
Pancreatic Cancer ◽  
Cancer Cells ◽  
Tannic Acid ◽  
Pancreatic Cancer Cells ◽  
Drug Treatments ◽  
Ft Ir ◽  
Size And Morphology ◽  
Targeting Ability

Pancreatic cancer (PanCa) is a lethal disease. Conventional chemotherapies for PanCa offer severe systemic toxicities. Thus, the development of a successful nanomedicine-based therapeutic regimen with augmented therapeutic efficacy is highly sought. Naturally occurring pectin and modified pectin-based drug delivery systems exhibit remarkable self-targeting ability via galactose residues to various cancer cells. Herein, we developed and used an innovative approach of highly stable nanocomplexes based on modified pectin and tannic acid (MPT-NCs). The nanocomplex formation was enabled by strong intermolecular interactions between pectin and tannic acid under very mild conditions. These nanocomplexes were characterized by particle size and morphology (DLS, TEM, and SEM), FT-IR spectroscopy, and zeta potential measurements. Additionally, MPT-NCs were capable of encapsulating anticancer drugs (5-fluorouracil, gemcitabine, and irinotecan) through tannic acid binding. The in vitro bioactivity of these drug MPT-NCs were evaluated in pancreatic cancer adenocarcinoma (PDAC) cell lines (HPAF-II and PANC-1). A dose-dependent internalization of nanocomplexes was evident from microscopy and flow cytometry analysis. Both proliferation and colony formation assays indicated the anticancer potential of pectin drug nanocomplexes against PDAC cells compared to that of free drug treatments. Together, the pectin-based nanocomplexes could be a reliable and efficient drug delivery strategy for cancer therapy.

scholarly journals Efeitos da Fotobiomodulação em Células Tumorais in vitro: Revisão da Literatura

2021 ◽  
Vol 24 (5-esp.) ◽  
pp. 645-649
Author(s):  
Jéssica Lucio da Silva ◽  
Ana Flávia Spadaccini Silva-de-Oliveira ◽  
Danielle Gregorio ◽  
Rodrigo Antonio Carvalho Andraus ◽  
Luciana Prado Maia
Keyword(s):  
Cancer Cells ◽  
Biological Effects ◽  
In Vitro Study ◽  
Light Therapy ◽  
Good Prognosis ◽  
Cochrane Library ◽  
Control Group ◽  
Treatment Protocols ◽  
The Ideal

Atualmente, novos métodos de tratamento contra o câncer estão sendo investigados para a obtenção de um bom prognóstico e menor índice de efeitos colaterais, e uma das terapias atuais sob investigação é a Fotobiomodulação (FBM). Sabe-se que a proliferação de células normais e tumorais pode ser estimulada ou inibida pela FBM, e esse processo vai depender dos parâmetros utilizados. O objetivo deste estudo foi conduzir uma revisão da literatura, a fim de avaliar os efeitos biológicos de diferentes parâmetros da FBM sobre cultura de células tumorais (osteossarcoma). Realizou-se busca na literatura através das bases de dados PubMed/MEDLINE, Cochrane Library e EMBASE. Os estudos mostraram que a FBM pode ser utilizada em células cancerígenas de forma a diminuir a sua proliferação, contudo, a falta de padronização dos protocolos de irradiação a laser para investigações in vitro não permite estabelecer os parâmetros ideais para esse fim. Com base nos achados relatados se pode sugerir que a FBM, em parâmetros específicos, pode promover a bioestimulação ou até mesmo a inibição das células cancerígenas, sendo necessários mais estudos para determinar os protocolos de tratamento ideais e, por isso, deve ser usada com cautela na prática clínica.   Palavras-chave: Terapia com Luz de Baixa Intensidade. Terapia a Laser. Osteossarcoma.   Abstract Currently new  treatment methods against cancer have been investigated to obtain a good prognosis and a lower rate of side effects, and one of the current therapies under investigation is Photobiomodulation (PBM). It is known that the  normal and tumor cells proliferation can be stimulated or inhibited by PBM, and this process will depend on the parameters used. The objective of this study was to conduct a literature review in order to assess the biological effects of different  PBM parameters on tumor cell culture (osteosarcoma). Literature search was performed through the PubMed/MEDLINE, Cochrane Library and EMBASE databases. Inclusion criteria were: to be an in vitro study with cancer cells, and to have at least one treatment group with PBM and a control group (without treatment). Studies have shown that PBM can be used in cancerous lesions in order to decrease the proliferation of these cells, however, the lack of standardization of laser irradiation protocols for in vitro investigations does not allow to establish the ideal parameters for this purpose. Based on the reported findings, it can be suggested that PBM in specific parameters may promote biostimulation or even inhibition of cancer cells. More studies are necessary to determine the ideal treatment protocols, and, because of this, it should be used with caution in clinical practice.   Keywords: Low Intensity Light Therapy. Laser therapy. Osteosarcoma  

scholarly journals Scorpion Venom-Functionalized Quercetin Phytosomes for Breast Cancer Management: In Vitro Response Surface Optimization and Anticancer Activity against MCF-7 Cells

Polymers ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 93
Author(s):  
Nabil A. Alhakamy ◽  
Usama A. Fahmy ◽  
Shaimaa M. Badr Eldin ◽  
Osama A. A. Ahmed ◽  
Hibah M. Aldawsari ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Biological Effects ◽  
Scorpion Venom ◽  
Cancer Management ◽  
Promising Therapeutic Approach ◽  
Mcf 7

Breast cancer is a dangerous type of cancer in women. Quercetin (QRT), a naturally occurring flavonoid, has wide biological effects including antioxidant, anticarcinogenic, anti-inflammatory, antiallergic, and antiviral activities. The anticancer activity is considered the most valuable effect of QRT against several types of cancer, including prostate, liver, lung, colon, and breast cancer. Scorpion venom peptides (SV) has been found to induce apoptosis and aggravate cancer cells, making it a promising anticancer agent. QRT, SV, and Phospholipon® 90H (PL) were incorporated in a nano-based delivery platform to assess QRT’s cellular uptake and antiproliferative efficacy against a lung cancer cell line derived from human breast cancer cells MCF-7. Several nanovesicles were prepared and optimized, using four-factor Box–Behnken, in an experimental design. The optimized phytosomes showed vesicle size and zeta potential values of 116.9 nm and 31.5 mV, respectively. The IC50 values revealed that MCF-7 cells were significantly more sensitive to the optimized QRT formula than the plain formula and raw QRT. Cell cycle analysis revealed that optimized QRT formula treatment resulted in significant cell cycle arrest at the S phase. The results also indicated that treatment with QRT formula significantly increased caspase-9, Bax, Bcl-2, and p53 mRNA expression, compared with the plain formula and QRT. In terms of the inflammatory markers, the QRT formula significantly reduced the activity of TNF-α and NF-κB, in comparison with the plain formula and QRT only. Overall, the findings from the study proved that a QRT formulation could be a promising therapeutic approach for the treatment of breast cancer.

scholarly journals Synthesis, Characterization and Evaluate the Biological Activity of Novel Heterocyclic Derivatives from Azomethine Compounds

2019 ◽  
Vol 35 (4) ◽  
pp. 1360-1367
Author(s):  
Rasim Farraj Muslim ◽  
Suheb Eaid Saleh
Keyword(s):  
Biological Activity ◽  
Aromatic Amines ◽  
Aromatic Aldehydes ◽  
The Novel ◽  
Heterocyclic Derivatives ◽  
Primary Aromatic Amines ◽  
Ft Ir ◽  
Bacteria And Fungi ◽  
Azomethine Compounds

This research includes synthesis of new seventh-membered heterocyclic derivatives as 1,3-oxazepine-dione derived from azomethine compounds. Azomethine compounds R1-R4 were synthesized by the reaction of aromatic aldehydes with primary aromatic amines. The novel of 1,3-oxazepine-dione derivatives R5-R9 were obtained from the treatment of azomethine compounds with anhydrides. The synthesized compounds were checked by TLC technique, spectral methods (FT-IR, H1-NMR) and measurements of some its physical properties. The biological activity of the heterocyclic derivatives was investigated against bacteria and fungi in vitro.

scholarly journals Characterization and Anticancer Effects of Folate Targeted Inotodiol Liposome From Inonotus Obliquus (Chaga Mushroom)

2021 ◽  
Author(s):  
Yangpeng Lu ◽  
Xudong Gao ◽  
Zhongqin Chen ◽  
Zihan Xue ◽  
Yanan Jia ◽  
...  
Keyword(s):  
Particle Size ◽  
Cancer Cells ◽  
Targeted Delivery ◽  
Inonotus Obliquus ◽  
Research Attention ◽  
Ζ Potential ◽  
Anticancer Effects ◽  
Ft Ir ◽  
Mcf 7

Abstract Inotodiol, one tetracyclic triterpenoid isolated from inonotus obliquus (Chaga mushroom) possess excellent anticancer, antioxidant and anti-inflammatory activities, however it has not been applied to medical use due to its low solubility and low bioavailability. Liposome as a good nanodrug carrier with EPR and good biocompatibility has received much research attention. To improve the solubility and bioavailability of IOP, we prepared inotodiol liposomes (IOP-Lps) and folic-acid targeting IOP liposome (FA-IOP-Lps) by ultrasonic method, and their particle size, morphology, zeta potential, entrapment efficiency (EE) and drug loading rate (DL) were characterized by DLS, TEM, FT-IR and HPLC respectively. Their in vitro cytotoxicity of human cervical cancer cells HeLa, human liver cancer cells HepG2 and human breast cancer cells MCF-7 were assessed using the MTT assay. The results showed that IOP-Lps and FA-IOP-Lps possess significant anticancer effects. The results of TEM, FT-IR and DLS confirmed the formation of liposome. The particle size of IOP-Lps were 201.07±6.47 nm and ζ-potential of -50.2±0.5 mV, FA-IOP-Lps 224.33±1.86 nm and ζ-potential of -51.2±0.3 mV, the EE of IOP-Lps and FA-IOP-Lps were 79.14% and 77.33%, respectively. IOP-Lps and FA-IOP-Lps could selectively kill HeLa, HepG2 and MCF-7 cancer cells while nontoxic to normal L02 cells. This is the first study to give out in vitro information of inotodiol’ s anticancer effects based on nanocarriers. Besides, this drug delivery system is of good sustained release and targeted delivery effects to promote the utilization of both inotodiol and other natural hydrophobic compounds in target treatment of cancers.

Novel organotin(iv) complexes derived from 4-fluorophenyl-selenoacetic acid: synthesis, characterization and in vitro cytostatic activity evaluation

2017 ◽  
Vol 41 (13) ◽  
pp. 5639-5650 ◽  
Author(s):  
Ya-Ru Qiu ◽  
Ru-Fen Zhang ◽  
Shao-Liang Zhang ◽  
Shuang Cheng ◽  
Qian-Li Li ◽  
...  
Keyword(s):  
Single Crystal ◽  
Elemental Analysis ◽  
Acid Synthesis ◽  
Cytostatic Activity ◽  
X Ray Diffraction ◽  
X Ray ◽  
Activity Evaluation ◽  
Ft Ir

A cluster of novel organotin(iv) complexes were designed, synthesized, and characterized by elemental analysis, FT-IR, and NMR (1H, 13C, and 119Sn) spectroscopy as well as single-crystal X-ray diffraction.

Studying Adsorption and Cellular Toxicity of Boron Nitride Nanostructure versus Melphalan Anti-ovarian Cancer Drug

2021 ◽  
Vol 21 ◽  
Author(s):  
Min Fu ◽  
Reza Tayebee ◽  
Satar Saberi ◽  
Narjes Nourbakhsh ◽  
Effat Esmaeili ◽  
...  
Keyword(s):  
Boron Nitride ◽  
Cancer Cells ◽  
Density Functional ◽  
Polarizable Continuum Model ◽  
Cancer Drug ◽  
X Ray Diffraction ◽  
Average Growth ◽  
Cellular Toxicity ◽  
Ft Ir

Background: Inclusion of anticancer drugs into biocompatible nanoparticulate carriers decreases the general toxicity and improves the efficacy of clinical treatments due to the reduction of soluble circulating free drug. Methods: In addition, removal of emerging drug contaminants from wastewaters is a necessity that should be seriously attended. Boron nitride (BN) is choice in drug delivery because of many surprising properties. Here, boron nitride nanoparticles are prepared, characterized by Fourier-transform infrared spectroscopy (FT-IR) and x-ray diffraction (XRD) and used in the delivery of melphalan anti-cancer drug. Results: Then, density functional theory (DFT) calculations are carried out to study adsorption of this drug on the surface of pure boron nitride fullerene via familiar hybrid functionals B3LYP and B3PW91. In addition, the polarizable continuum model (PCM) calculations show that BN is stable in water. Conclusion: Finally, the in vitro cellular toxicity and viability of BN nanoparticles was examined on ES-2 cancer cells. The inhibitory dose IC50 of the material confirmed an acceptable cytotoxicity and nanoparticles affected the average growth of ES-2 cancer cells.

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