Preferred Language
Articles
/
bijps-563
Cephalothin as a Carrier of 6-Mercaptopurine for Targeting Cancer Tissues
...Show More Authors

A lower extracellular pH is one of the few well-documented physiological differences between tumour and normal tissues. On the other hand, elevated glutathione (GSH) level has been detected in many tumours compared with healthy surrounding tissues. The compound II: 3-(9H-purin-6-yl-thio) carbonothionyl methyl-8-oxo-7-(2-thiophen-2-yl) acetamido-5-thia-1-azabicyclo-4-octo-ene-carboxylic acid was a cephalothin derivative contain 6-mercaptopurine (6-MP). Compound II react with general base catalysis in slightly acidic pH or with sulfhydryl nucleophiles to release the chemotherapeutic drug 6-MP. The generation of compound II was accomplished following multistep reaction procedures. The structure of compound II and its intermediate was confirmed by their melting point, infrared spectroscopy, CHN and NMR analysis. The hydrolysis of compound II in aqueous buffer solution of pH 6 and in the presence of GSH at pH 7.4 was studied. The partition coefficient (PC) of compound II was also determined. Compound II has acceptable rate of hydrolysis at slightly acidic medium pH 6 (t1/2 = 56.34 min.) and 80% of compound II had been converted to 6-MP within 30 min in the presence of GSH. And the compound has acceptable stability at pH 7.4(t0.5=639.65 min.) and the rate of hydrolysis was effected by change the buffer concentration.  This compound can selectively deliver 6-MP into the tumour tissues which have acidic pH or elevated GSH level. Compound II had an improved PC value of 12.23 compared to 1.22 for free drug 6-MP confirming higher lipophilicity.

Key words: 6-mercaptopurine, cancer, prodrug, targeting

Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Fri Jun 07 2024
Journal Name
Asian Pacific Journal Of Cancer Prevention
The Effect of NF-κB Deactivation on Cancer Cell Response to ALA Mediated Photodynamic Therapy
...Show More Authors

due to the presence of chemoresistance and the risk of tumor recurrence and metastasis. There is a pressing necessity to develop efficient treatments to improve response for treatment and increase prolong survival of breast cancer patients. Photodynamic therapy (PDT) has attracted interest for its features as a noninvasive and relatively selective cancer treatment. This method relies on light-activated photosensitizers that, upon absorbing light, generate reactive oxygen species (ROS) with powerful cell-killing outcomes. Nuclear factor kappa B (NF-κB), a transcription factor, plays a key role in cancer development by regulating cell proliferation, differentiation, and survival. Inhibiting NF-κB can sensitize tumor cells to chemotherapeuti

... Show More
View Publication
Scopus (2)
Scopus Crossref
Publication Date
Sun Dec 09 2018
Journal Name
Baghdad Science Journal
Synthesis, Characterization of Poly Heterocyclic Compounds, and Effect on Cancer Cell (Hep-2) In vitro.
...Show More Authors

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

... Show More
View Publication Preview PDF
Scopus (3)
Scopus Clarivate Crossref
Publication Date
Thu Aug 13 2020
Journal Name
Asia Pacific Journal Of Molecular Biology And Biotechnology
The anticancer molecular mechanism of Carnosol in human cervical cancer cells: An in vitro study
...Show More Authors

Carnosol, a phenolic diterpene, is one of the effective anticancer agents naturally occurring in rosemary, sage, parsley, and oregano. The chemoresistance problem increased with the routinely used chemotherapy. Therefore, the efforts to find a substitute with safe and low cost have become crucial worldwide. The current study attempts to inspect the anticancer molecular mechanisms of Carnosol on modulating up- and down- regulation of multiple genetic carcinogenesis pathways. The cytotoxicity of Carnosol on Hela cells was evaluated by MTS assay. Flow cytometry was used to assess apoptosis and cell cycle arrest. The apoptotic morphological changes were obvious by dual apoptosis assay. The differential gene expression after treatment wi

... Show More
View Publication
Scopus Crossref
Publication Date
Sat May 01 2021
Journal Name
Journal Of Physics: Conference Series
Antioxidant, cytotoxicity and phytochemical analysis of Larinus maculates F. cocoon aqueous extract against lung cancer
...Show More Authors
Abstract<p>Cocoon of larva <italic>Larinus maculates</italic> F. from Curculionidae family (<italic>Echinops</italic> species), locally in Iraq known as Tihan, is one of traditional folk medicine used in the treatment of diversity respiratory system and fever. This study was carried out to assess the bioactive component and the antioxidant capability of aqueous beetle cocoon extract (<italic>Larinus maculates</italic> F.) along with its possible cytotoxic activity against A549 lung cancer cell line. For phytochemical analysis gas chromatography-mass spectrometry (GC-MS) was used, and to detected free scavenging activity 2, 2-diphenyl-1 picrylhydrazyl (DPPH) was used</p> ... Show More
View Publication
Scopus (1)
Scopus Crossref
Publication Date
Sun Aug 28 2016
Journal Name
World Journal Of Pharmacy And Pharmaceutical Sciences
AN INSIGHT ON THE IDENTIFICATION OF CANCER STEM CELLS USING NOVEL IMMUNOLOGICAL AND MOLECULAR STRATEGIES
...Show More Authors

Cancer stem cells (CSCs) are defined as a population of cells present in tumours, which can undergo self-renewal and differentiation. Identification and isolation of these CSCs using putative surface markers have been a priority of research in cancer. With this background we selected pancreatic normal and tumor cells for this study and passaged them into animal tissue culture medium. Further staining was done using alkaline phosphatase and heamatoxilin staining. Blue to purple colored zones in undifferentiated pluripotent stem cells and clear coloration in the chromatin material indicated pancreatic cells. Further studies on the cell surface marker CD 44 were done using ELISA. For this, the protein was extracted from cultivated normal and t

... Show More
View Publication Preview PDF
Publication Date
Fri Jan 31 2025
Journal Name
Aip Conference Proceedings
Classification of oral cavity cancer using linear discriminant analysis (LDA) and principal component analysis (PCA)
...Show More Authors

View Publication
Scopus (1)
Crossref (1)
Scopus Crossref
Publication Date
Mon Apr 01 2024
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Impact of Clinical Pharmacist Intervention on Chemotherapy Knowledge, Attitude, and Practice among Breast Cancer Women
...Show More Authors

الخلفية: إن سمية الدواء والآثار الجانبية للعلاج الكيميائي تؤثر سلبا على مرضى سرطان الثدي. الأهداف: لتقييم فعالية التدخلات الصيدلانية في تحسين معرفة مرضى سرطان الثدي ومواقفهم وممارساتهم فيما يتعلق بالعلاج الكيميائي لسرطان الثدي.

View Publication Preview PDF
Crossref (6)
Crossref
Publication Date
Wed Jan 04 2023
Journal Name
Radiochimica Acta
Verification of radon, radium, polonium concentrations and lung cancer rates in blood of female hookah smokers
...Show More Authors
Abstract<p>Hookah smoking has become very popular in Iraq among women and men. Hookah tobacco contains natural radioactive elements, such as radon, radium, and uranium, as well as toxic elements, such as polonium, which are released during the combustion of tobacco and are inhaled by smoking. Most reviews focus on hookah tobacco, and only a few have investigated the blood of hookah smokers. In this study, a CR-39 detector was used to measure radon, radium, and polonium concentrations and conduct risk assessments in female hookah smokers of different ages. The results show that the concentrations of radon-222, polonium-218, and polonium-214 varied between 61.62 and 384.80, 5.45–33.64 on the wal</p> ... Show More
View Publication
Scopus (6)
Crossref (4)
Scopus Clarivate Crossref
Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
The inhibition effect of crude juice of olive Olea europeae on cancer cell line Rhabdomyosarcoma (RD)
...Show More Authors

The inhibition effect of crude juice of green and black olive on cancer cell line (RD) in vitro has been studied by depending on micro titration system . Eleven different concentration starting from (916-960) mg/ml of crude juice respectively ,for three periods of exposure(24-48-72)hours. The resulted showed that the inhibition effect dependent on type of olive fruit juice ,concentration of dose ,time of exposure and the high concentration of both type of olive juice increased the growth of cell line while other concentration caused decrease in different rates ,moreover the black juice was more effective than green and 48 hours' time exposure was the best for inhibition.

View Publication Preview PDF
Crossref
Publication Date
Tue Mar 01 2022
Journal Name
Iraqi Journal Of Agricultural Sciences
CORRELATION OF TMPRSS2-ERG GENE FUSION STATUS WITH CLINICOPATHOLOGICAL CHARACTERISTICS IN PROSTATE CANCER OF IRAQI PATIENTS
...Show More Authors