Small molecules drug conjugate mutual prodrug design (SMDC) composed of folate and lethal agent conjugate, rigidly bonded via hydrophilic bridge and self immolative disulfide bond ; represent new interesting approaches for cancer treatment , the component of SMDC intended for targeting folate receptor , along with greater conservation of component until reaching the target tumor tissue . The designing and synthesis of compound VI and VIII derived from 6-Mercaptopurine (6-MP) and Methotrexate ( MTX) conjugate altogether as mutual prodrugs were processed forward successfully by multistep reaction procedures , and by Thin Layer Chromatography (TLC) for preliminary detection of products and their intermediates, along with their purity. The structures of two final compounds and their intermediates were proclaimed by melting point measurement, infrared spectrometry and ¹HNMR analysis given results greatly correspond with theoretical proposed chemical structure of synthesized compounds. Furthermore, cytotoxic activity evaluation on cell line level had been done for two final compounds against human breast tumor cell (MCF-7) and human ovarian tumor cell (SKO-3) types of cancer cell line and the results were confirmed which show greater cytotoxic tumor activity of two final compounds, while compound VI possess optimal activity proportional with increased number of 6-MP molecules.
Background: Antibiotic resistance is a problem leading to difficulty in treating microbial infections thatmay occur due to many causes. For the important pharmacist role as a reference for the information and theability to access to medications, they are vital members in lowering the development of antibiotic resistance,and also they support the proper use and control of antibioticsmisuse. Our goal is comparing the knowledge,attitude, practice of undergraduate and postgraduate pharmacy students and their perceptions about thecausing factors of antibiotic resistance in Iraq.Method: A cross sectional study was conducted involving the final year bachelor and postgraduate (masterand Philosophical doctor) students from different private
... Show MoreBackground: The anticancer impact of Epigallocatechin gallate (EGCG) the highly active polyphenol of green tea was abundantly studied. Though, the exact mechanism of its cytotoxicity is still under investigation. Objectives: Hence, the current study designed to investigate the molecular target of EGCG in HepG2 cells on thirteen autophagy- and/or apoptosis- related genes. Methods: The apoptosis detection analyses such as flow cytometry and dual apoptosis assay were used. The genes expression profile was explored by the real-time quantitative-PCR. Results: EGCG increases G0/G1 cell cycle arrest and the real-time apoptosis markers proteins leading to stimulate apoptos
... Show MoreBackground: Central serous chorioretinopathy (CSCR) is an idiopathic condition aggravated by exogenous or endogenous glucocorticoids. Vascular deregulation in the choroid is a new hypothesis regarding central serous chorioretinopathy occurrence. The inhibition of choroidal mineralocorticoid receptors has a great role in shortening the duration of CSCR by inhibiting choroidal vasodilatation and leak.
Objective: To assess the effect of oral spironolactone on subretinal fluid, central macular thickness and visual acuity in patients with acute CSCR compared to observation.
Subjects and Methods: a hospital based, randomized clinical trial carried out at outpatient clinic in Ibn-Alhaitham Teaching E
... Show MoreCurcumin (Cur) possesses remarkable pharmacological properties, including cardioprotective, neuroprotective, antimicrobial, and anticancer activities. However, the utilization of Cur in pharmaceuticals faces constraints owing to its inadequate water solubility and limited bioavailability. To overcome these hurdles, there has been notable focus on exploring innovative formulations, with nanobiotechnology emerging as a promising avenue to enhance the therapeutic effectiveness of these complex compounds. We report a novel safe, effective method for improving the incorporation of anticancer curcumin to induce apoptosis by reducing the expression levels of miR20a and miR21. The established
New series of Schiff bases 2(a-j) and corresponding beta-lactam derivatives 3(a-j) were synthesized from cefalexin (1) as starting material. The compound (1) was reacted with different aldehydes and ketones to give Schiff bases derivatives 2(a-j). The synthesized Schiff bases were cyclized by chloroacetyl chloride in the presence of triethylamine to form beta-lactam derivatives 3(a-j). The compounds were characterized by deremination melting point, FT-IR and 1H NMR. The beta-lactam derivatives were screened in vitro antibacterial against some bacterial species
A research include of synthesized five member ring, which has been synthesized by condensation of 2-(1-(4- hydroxyphenyl) ethylidene)hydrazine-1-carbothioamide[I] with α-chloro ethylacetate in sodium acetate (fused) to form ethyl 2-(4-(1-((4-oxo-2-thioxopyrrolidin-3-ylidene)hydrazono) ethyl)phenoxy)acetate [II]. After that reacted [II]with hydrazine hydrate to resulting compound [III]. Compound [III] was refluxed with 4-aminobenzoicacid in excess of phosphorus oxy chloride give compound [IV],the later compound [IV] interact with acetyl acetone or ethylacetoacetate give to pyrazole and pyrazoline derivatives[V],[VI]. While when reacted with different aromatic aldehydes and one ketone consistence Schiff base derivatives [VII]a-e . The FTIR a
... Show MoreA research include of synthesized five member ring, which has been synthesized by condensation of 2-(1-(4- hydroxyphenyl) ethylidene)hydrazine-1-carbothioamide[I] with α-chloro ethylacetate in sodium acetate (fused) to form ethyl 2-(4-(1-((4-oxo-2-thioxopyrrolidin-3-ylidene)hydrazono) ethyl)phenoxy)acetate [II]. After that reacted [II]with hydrazine hydrate to resulting compound [III]. Compound [III] was refluxed with 4-aminobenzoicacid in excess of phosphorus oxy chloride give compound [IV],the later compound [IV] interact with acetyl acetone or ethylacetoacetate give to pyrazole and pyrazoline derivatives[V],[VI]. While when reacted with different aromatic aldehydes and one ketone consistence Schiff base derivatives [VII]a-e . The FTIR a
... Show MoreBackground: Bone regeneration in dehiscence and fenestration defect can be improved with the use of platelet rich fibrin (PRF) that provides a scaffold for new bone regeneration. This study was conducted to assess the effectiveness of PRF as a graft material and membrane in dehiscence and fenestration defects. Materials and Methods: This prospective clinical study included patients who received dental implants that demonstrated peri-implant defects which were augmented using Leukocyte- PRF (L-PRF) or Advanced-PRF (A-PRF). Twenty four weeks postoperatively the defect resolution and the density of regenerated bone were assessed by CBCT and re-entry surgery. The assessment also included measurement of primary and secondary implant stability
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