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Cephalothin as a Carrier of 6-Mercaptopurine for Targeting Cancer Tissues
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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

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Publication Date
Fri Jul 01 2022
Journal Name
Archives Of Razi Institute
Prognostic Value of Intracellular Transcription of Factors HIF-1α and p53 and Their Relation to Estradiol and TNM Parameters of Breast Cancer Tissues in Women with Invasive Ductal Carcinoma in Thi-Qar Province, Iraq
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Breast cancer is the most common malignancy affecting women's health, with an increasing incidence worldwide. This study aimed to measure the intracellular concentration of the hypoxia-inducible factor 1 α (HIF-1α), tumor suppression protein p53, and estradiol (E2) in tumor tissues of adult females with breast cancer and their relation to tumor grade, tumor size, and lymph node metastases (LNM). The study was conducted on 65 adult female participants with breast mass admitted to the operating theater in Al-Hussein Teaching Hospital and Al-Habboby Teaching Hospital in Nasiriyah, Iraq, from January to November 2021. Fresh breast tumor tissues were collated and homogenized for intracellular biochemical analysis using the enzyme-linked immuno

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Publication Date
Sat Jul 01 2023
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Diagnostic and Predictive Values of IL-6 in a Group of Iraqi Patients with Rheumatoid Arthritis
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الخلفية: التهاب المفاصل الرَثَيَانِي أو الداء الرثياني أو الالتهاب المفصلي الروماتويدي هو مرض مزمن، من الأمراض الانضدادية التي تؤدي بالجهاز المناعي لمهاجمة المفاصل، مسببة التهابات وتدميرًا لها. ومن الممكن أيضًا أن يدمر جهاز المناعة أعضاء أخرى في الجسم مثل الرئتين والجلد. وفي بعض الحالات، يسبب المرض الإعاقة، مؤدية إلى فقدان القدرة على الحركة والإنتاجية. ويتم تشخيص المرض بواسطة تحاليل دم مخبرية مثل تحلي

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Publication Date
Sun Mar 31 2024
Journal Name
Association Of Arab Universities Journal Of Engineering Sciences
Using Solid Waste as A Substitute for Raw Materials in Construction: A Review.
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The main challenge is to protect the environment from future deterioration due to pollution and the lack of natural resources. Therefore, one of the most important things to pay attention to and get rid of its negative impact is solid waste. Solid waste is a double-edged sword according to the way it is dealt with, as neglecting it causes a serious environmental risk from water, air and soil pollution, while dealing with it in the right way makes it an important resource in preserving the environment. Accordingly, the proper management of solid waste and its reuse or recycling is the most important factor. Therefore, attention has been drawn to the use of solid waste in different ways, and the most common way is to use it as an alternative

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Publication Date
Thu Mar 05 2020
Journal Name
Revista Brasileira De Farmacognosia
Zerumbone-Loaded Nanostructured Lipid Carrier Gel Facilitates Wound Healing in Rats
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Publication Date
Wed Oct 07 2020
Journal Name
Indian Journal Of Forensic Medicine & Toxicology
CA 27-29: A Valuable Marker for Breast Cancer Management in Correlation with CA 15-3
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Publication Date
Sun Dec 22 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Ex-vivo Ex-Vivo Absorption Study of a Novel Dabigatran Etexilate Loaded Nanostructured Lipid Carrier Using Non-Everted Intestinal Sac Model
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Abstract

The purpose of our study was to develop Dabigatran Etexilate loaded nanostructured lipid carriers (DE-NLCs) using Glyceryl monostearate and Oleic acid as lipid matrix, and to estimate the potential of the developed delivery system to improve oral absorption of low bioavailability drug, different Oleic acid ratios effect on particle size, zeta potential, entrapment efficiency and loading capacity were studied, the optimized DE-NLCs shows a particle size within the nanorange, the zeta potential (ZP) was 33.81±0.73mV with drug entrapment efficiency (EE%) of  92.42±2.31% and a loading capacity (DL%) of 7.69±0.17%. about 92% of drug was released in 24hr in a controlled manner, the ex-vivo intestinal p

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Publication Date
Sat Jun 30 2012
Journal Name
Al-kindy College Medical Journal
Correlation of Concentrations of Certain Trace Elements in Normal and Diseased Human Tissues
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Background Over the past decade there has been a growing awareness of, and interest in, the trace element concentration differences between normal and diseased tissues. Significant changes in tissue concentrations of Zinc (Zn) and Copper (Cu) have been previously reported in inflammation and cancer of certain human tissues.
Aim:(1)To correlate between Zn and Cu concentrations and the histological picture of normal and certain inflamed human tissues, namely the gall bladder (GB) the vermiform appendix (VA), visceral adipose tissue (VAT) and subcutaneous adipose tissue (SAT). (2) to detect whether there is a difference in the above-mentioned parameters between VAT and SAT. (3) to obtain recordings for trace element levels in human tissu

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Publication Date
Sat Mar 25 2017
Journal Name
Biomedical And Pharmacology Journal
Detection of Cytomegalovirus and Epstein Barr Virus in Placental Tissues of Aborted Women
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Introduction The abortions reasons in several circumstances yet are mysterious, nevertheless the bacterial toxicities signify a main reason in abortion, where germs seems to be the utmost elaborate pathogens (Khameneh et.al., 2014) and (Oliver and Overton ,2014). Between numerous germs, Humano

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Publication Date
Wed Jan 02 2019
Journal Name
Journal Of Global Pharma Technology
Nanocrystal Technology as a Tool for Improving Dissolution of Poorly Soluble Drugs
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Many approaches have been developed over time to counter the bioavailability limitations of poorly soluble drugs. With advances in nanotechnology in recent decades, this issue has been approached through the formulation of drugs as nanocrystals. Nanocrystals consist of pure drug(s) and a minimum of surface active agent(s) required for stabilization. They are carrier-free submicron colloidal drug delivery systems with a mean particle size typically in the range of 200 - 500 nm. By reducing particle size to nanoscale, the surface area available for dissolution is increased, and thus bioavailability is enhanced. Drug nanocrystals constitute a versatile formulation approach to enhance the pharmacokinetic and pharmacodynamic properties of poorly

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Publication Date
Wed Jun 28 2023
Journal Name
The Iraqi Journal Of Veterinary Medicine
Haemoglobin Epsilon as a Biomarker for the Molecular Detection of Canine ‎Lymphoma
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Lymphoma is a cancer arising from B or T lymphocytes that are central immune system ‎components. It is one of the three most common cancers encountered in the canine; ‎lymphoma affects middle-aged to older dogs and usually stems from lymphatic tissues, ‎such as lymph nodes, lymphoid tissue, or spleen. Despite the advance in the management of ‎canine lymphoma, a better understanding of the subtype and tumor aggressiveness is still ‎crucial for improved clinical diagnosis to differentiate malignancy from hyperplastic ‎conditions and to improve decision-making around treating and what treatment type to use. ‎This study aimed to evaluate a potential novel biomarker related to iron metabolism,

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