Preferred Language
Articles
/
bijps-381
Design, Synthesis, Characterization and Preliminary Anticancer Study for Methotrexate Silibinin Conjugates
...Show More Authors

The spectrum of clinical efficacy of Methotrexate (MTX) is broad in that MTX is used in the treatment of certain cancers, severe psoriasis and rheumatoid arthritis.Various mechanisms by which cancer cells grown in tissue culture become resistant to anticancer drugs. The use of multiple  drugs with different mechanisms of entry into cells and different cellular targets allows for effective chemotherapy and high cure rates. In an efforts to develop effective strategies that increase the therapeutic potential of anticancer drugs with less systemic toxicity ,are being directed  towards the investigation of dietary supplements and other phytotherapeutic agents for their synergistic efficacy in combination with anticancer drugs. A promising approach to improve the cancer cell selectivity of methotrexate is the chemical transformation into reversible derivatives which convert the conjugate to the parent drug by virtue of enzyme within cancer tissue. The present study includes the synthesis of  two derivatives of methotrexate which are :-Schiff base methotrexate-silibinin conjugate ( compound 5), and Methotrexate-silibinin conjugate (compound 6).The synthesis  of the target compounds was  accomplished following multistep reaction procedures. The chemical reactions were followed up and purity of the products was checked by TLC. The structures of the final compounds and their intermediates were characterized and identified by their melting points, infrared spectroscopy, 1H-NMR and elemental microanalysis(C H N S).The anticancer activity of these compounds was investigated by HEP-2 cell line(Larynx carcinoma), which showed  that compounds 5 and 6 have the higher activity than methotrexate or silibinin alone.These are promising data for the discovery of new anticancer agents in future. These compounds may deliver the parent drug  selectively  into the cancer cells to be hydrolyzed by enzymes that are elevated in  tumor tissues compared with normal tissues .

Keywords: Methotrexate, Silibinin, Cancer treatment resistance, Folate receptor, Cancer cell targeting.

Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Wed Apr 12 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis ,Characterization and Study Biological Activity of Some New 1, 3, 4-Thiadiazole and Pyrazolone Derivatives Containing Indole Ring
...Show More Authors

   This work involves synthesis and characterization of some new 1, 3, 4-thiadiazole or pyrazoline derivatives  heterocyclic containing indole ring. The new 2-amino-1, 3, 4thiadiazole derivatives[IV] and [V]a, b were synthesized by cyclization reaction of 2-methyl1H-indole-carbothiosemicarbazide[III] in H2SO4 acid or by reaction of indole-3-acetic acid or indole-3-butanoic acid with thiosemicarbazide in the presence of phosphorous oxychloride, respectively. Amide derivatives [VI]-[VIII] were synthesized by the reaction equimolar of 2amino-1, 3, 4-thiadiazoles and (acetyl chloride, benzoyl chloride, anisoyl chloride and heptanoyl chloride) in DMF and pyridine as accepter. The new pyrazolone  derivatives [XI]a, b were s

... Show More
View Publication Preview PDF
Publication Date
Wed Jul 01 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, Design, Docking and biological activity of new benzo hydrazide derivatives.
...Show More Authors

View Publication
Scopus (2)
Crossref (1)
Scopus Crossref
Publication Date
Thu Mar 30 2017
Journal Name
Journal Of Biotechnology Research Center
Study the Effects of Methotrexate with and without Vitamin A on Some Biochemical and Histological Parameters in Male Rabbits
...Show More Authors

The present study aims to evaluate the effects of methotrexate (MTX) with and without vitamin A (Vit. A) on some biochemical parameters and histological structure in male rabbits liver. Twenty male rabbits weighing 1250-1480 gm were divided into four equal number groups. The first group was given 2 ml distilled water as control group. The second group was given MTX (20 mg/kg), the third group was given Vit. A (5000 IU), while the fourth group was given MTX (20 mg/kg) +Vit. A (5000 IU) in alternative days. Following four weeks of treatment, lipid profile total cholesterol (TC), triglycerides (TG), high-density lipoprotein (HDL), [low-density lipoprotein (LDL) and very low-density lipoprotein (VLDL)]; in addition to thyroid hormones tr

... Show More
Publication Date
Wed Dec 14 2022
Journal Name
Bulletin Of The Chemical Society Of Ethiopia
Synthesis, characterization, theoretical study and biological evaluation of Schiff base and their La(III), Ce(IV) and UO2(II) complexes
...Show More Authors

ABSTRACT. A new three metal complexes of La(III), Ce(IV) and UO2(II) ions have been synthesized based on a Schiff base derived from the condensation of L-histidine and anisaldehyde. All prepared compounds were characterized by different spectroscopic techniques and Density-functional theory (DFT) calculations. The complexes were proposed to have an octahedral structure based on the investigated results. The optimized shape, numbering system, and dipole moment vector of Ligand and La, Ce, and UO2 (1:1) chelates were investigated. The Schiff base ligand and complexes exhibit moderate action against all of the bacteria tested, with P. aeruginosa, Klebsiella sp., and E. faecalis respectively being the order of inhibition.  

... Show More
View Publication
Crossref (2)
Crossref
Publication Date
Tue Mar 06 2007
Journal Name
Iraqi J Pharm Sci,
Effect of Silibinin in Lowering the Intraocular Pressure in Normotensive Rabbits: Interaction with Pilocarpine and Cyclopentolate
...Show More Authors

Previous data indicated the effectiveness of silibinin as intraocular pressure (IOP) - lowering agent. The present study was performed to evaluate the interaction of silibinin with pilocarpine or cyclopentolate in lowering IOP in normotensive rabbits. The effects of topically instilled silibinin hemisuccinate solution (0.75%) alone or adjunctly combined with 2% pilocarpine or 1% cyclopentolate on the IOP of normotensive rabbits were evaluated using indentation tonometry. The results showed that 0.75% solution of silibinin was found more potent than pilocarpine (2% drops) in lowering IOP of normotensive rabbits, while their combination results in longer duration of action. Moreover, the elevated IOP values produced by cyclopentolate (1%drops

... Show More
Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Effect of Silibinin in Lowering the Intraocular Pressure in Normotensive Rabbits: Interaction with Pilocarpine and Cyclopentolate
...Show More Authors

Previous data indicated the effectiveness of silibinin as intraocular pressure (IOP) - lowering agent.  The present study was performed to evaluate the interaction of silibinin with pilocarpine or cyclopentolate in lowering IOP in normotensive rabbits. The effects of topically instilled silibinin hemisuccinate solution (0.75%) alone or adjunctly combined with 2% pilocarpine or 1% cyclopentolate on the IOP of normotensive rabbits were evaluated using indentation tonometry. The results showed that 0.75% solution of silibinin was found more potent than pilocarpine (2% drops) in lowering IOP of normotensive rabbits, while their combination results in longer duration of action. Moreover, the elevated IOP values produced by cyclopentolate

... Show More
View Publication Preview PDF
Crossref
Publication Date
Mon Jan 01 2018
Journal Name
Journal Of Pharmacy Research
Design and in vitro characterization of bisacodyl as a hollow-type suppositories
...Show More Authors

Publication Date
Tue Dec 31 2019
Journal Name
Journal Of Economics And Administrative Sciences
The investment Decision Making According to the Preliminary Feasibility Study for the 100-Bed Teaching Hospital - Service Sector in Diwaniya Governorate (Case Study)
...Show More Authors

     The research aims to prepare a preliminary feasibility study that shows the importance of preliminary feasibility study in investment decision making, carrying out of the local demand of service provided in accordance with international standards and statement of investment opportunities available to the private sector in several investment methods. In order to reach the objectives of the study was adopted as a method of partial analysis at the level of economic unity through the study demand, supply, costs, economic and social profitability.

      The health sector in Iraq is one of the service sectors facing today a continuous deficiency

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Feb 28 2023
Journal Name
Research Journal Of Pharmacy And Technology
Synthesis and Characterization of Molecularly Imprinted Polymers for Metronidazole by using Allyl Chloride and Allyl Bromide as Monomers
...Show More Authors

Metronidazole-MIPs were prepared by using (MDZ) as the template as well as allylchloride (AYC) or allylbromide (AYB) as monomer, used (TMPTA) tri-methylol propane tri-acrylate or ethylene glycol di-methyl acrylate (EGDMA) as cross-linker and initiator used (BP) benzyl peroxide. By using different plasticizers (di butyl Phthalate (DBPH), Nitrobenzene (NB), oleic acid (OA) and paraffin) for MDZ-MIP1 and (Di-butyl sebecate (DBS), Di-methyl acrylate (DMA), Tributylphosphate(TBP) and Tris(ethylhexyl phosphate (TEHP) ) for MDZ-MIP2. Membranes of MIPs were prepared in PVC matrix. The characterizations of each electrode were determined The Slope range from (55.083 - 43.711) mV/decade, Limit of Detection (8 X 10 -4- 2 X 10-6) and Linearity

... Show More
View Publication
Scopus Crossref
Publication Date
Fri Nov 03 2023
Journal Name
Karbala International Journal Of Modern Science
Synthesis and characterization of zirconium oxide nanoparticles using Z. officinale and S. aromaticum plant extracts for antibacterial application
...Show More Authors

View Publication
Scopus (1)
Scopus Crossref