scholarly journals Synthesis and Characterization of Substituted Starch Grafted Methyl Nadic Anhydride and Substituted with 4-Aminoantipyrine

2019 ◽  
pp. 103-113
Author(s):  
Firyal M. Ali ◽  
Mohammed A. Farhan
Keyword(s):  
Structural Modification ◽  
In Vitro Study ◽  
Extended Period ◽  
Controlled Drug Release ◽  
Controlled Delivery ◽  
Ceric Ammonium Nitrate ◽  
Grafted Copolymer ◽  
Zero Time

In this research the structural modification of starch was carried out with methyl nadic anhydride (M1) as a spacer by using ceric ammonium nitrate (CAN) as an initiator, and grafted copolymer was substituted with amino drug such as 4-aminoantipyrine (M1B), this design of carries for controlled delivery of therapeutic agent which could release the entrapped drug over an extended period of time, due to its nontoxic, biodegradable and slow digesting nature, the new drug copolymer was characterized by FTIR, 1H-NMR and UV Spectroscopes. The prepared drug copolymer was analyzed in different pH values at (37°C) as in vitro study and controlled drug release was compared at zero time and after four days.

scholarly journals Chemical Derivatization and Characterization of Novel Antitrypanosomals for African Trypanosomiasis

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4488
Author(s):  
Aboagye Kwarteng Dofuor ◽  
Temitayo Samson Ademolue ◽  
Cynthia Mmalebna Amisigo ◽  
Kwaku Kyeremeh ◽  
Theresa Manful Gwira
Keyword(s):  
Structural Modification ◽  
Spectroscopic Analysis ◽  
Microscopic Analysis ◽  
The Novel ◽  
Chemical Derivatization ◽  
African Trypanosomiasis ◽  
Chemical Structures ◽  
Normal Ratio

The search for novel antitrypanosomals and the investigation into their mode of action remain crucial due to the toxicity and resistance of commercially available antitrypanosomal drugs. In this study, two novel antitrypanosomals, tortodofuordioxamide (compound 2) and tortodofuorpyramide (compound 3), were chemically derived from the natural N-alkylamide tortozanthoxylamide (compound 1) through structural modification. The chemical structures of these compounds were confirmed through spectrometric and spectroscopic analysis, and their in vitro efficacy and possible mechanisms of action were, subsequently, investigated in Trypanosoma brucei (T. brucei), one of the causative species of African trypanosomiasis (AT). The novel compounds 2 and 3 displayed significant antitrypanosomal potencies in terms of half-maximal effective concentrations (EC50) and selectivity indices (SI) (compound 1, EC50 = 7.3 μM, SI = 29.5; compound 2, EC50 = 3.2 μM, SI = 91.3; compound 3, EC50 = 4.5 μM, SI = 69.9). Microscopic analysis indicated that at the EC50 values, the compounds resulted in the coiling and clumping of parasite subpopulations without significantly affecting the normal ratio of nuclei to kinetoplasts. In contrast to the animal antitrypanosomal drug diminazene, compounds 1, 2 and 3 exhibited antioxidant absorbance properties comparable to the standard antioxidant Trolox (Trolox, 0.11 A; diminazene, 0.50 A; compound 1, 0.10 A; compound 2, 0.09 A; compound 3, 0.11 A). The analysis of growth kinetics suggested that the compounds exhibited a relatively gradual but consistent growth inhibition of T. brucei at different concentrations. The results suggest that further pharmacological optimization of compounds 2 and 3 may facilitate their development into novel AT chemotherapy.

scholarly journals A GREEN APPROACH FOR THE SYNTHESIS OF DRUG DELIVERY SYSTEM, MESOPOROUS SILICA GRAFTED ACRYLAMIDE –β- CYCLODEXTRIN COMPOSITE, FOR THE CONTROLLED RELEASE OF CURCUMIN

2018 ◽  
Vol 11 (9) ◽  
pp. 372
Author(s):  
Manohar D Mullassery ◽  
Noeline B Fernandez ◽  
Surya R ◽  
Diana Thomas
Keyword(s):  
Drug Delivery ◽  
Controlled Delivery ◽  
X Ray Diffraction ◽  
In Vitro Biocompatibility ◽  
Green Approach ◽  
Solvent Free Conditions ◽  
Good Biocompatibility ◽  
Biocompatibility Study

Objective: The scope of the present study was the preparation and characterization of a novel composite acrylamide β-cyclodextrin grafted 3-aminopropyltriethoxysilane bentonite (AMCD-g-APSB), for the controlled delivery of curcumin (CUR).Methods: AMCD-g-APSB, was synthesized by solvent-free conditions using microwave irradiation. The structure and surface morphology of the composite was established using Fourier transform infrared spectroscopy, X-ray diffraction, scanning electron microscopy, thermal analysis, etc.Results: The swelling percentage of the composite depends on both time and pH of the medium. The maximum swelling of the composite occurred at a pH of 7.4. The maximum drug encapsulation was occurring at a pH 3. About 96.5% of drug was loaded at pH 3. In vitro biocompatibility study was performed, and the result showed good biocompatibility of the composite in the concentration range 2.5–50 μg/ml.Conclusions: Drug delivery study of the composite proved that CUR could be successfully released in a controlled manner in the colon without much loses of the drug in the stomach.

Synthesis and characterization of novel PUFA esters exhibiting potential anticancer activities: An in vitro study

2011 ◽  
Vol 46 (10) ◽  
pp. 4878-4886 ◽  
Author(s):  
Azmat Ali Khan ◽  
Mahboob Alam ◽  
Saba Tufail ◽  
Jamal Mustafa ◽  
Mohammad Owais
Keyword(s):  
In Vitro Study ◽  
Vitro Study ◽  
Synthesis And Characterization ◽  
Anticancer Activities

In vivo and in vitro trimethadione oxidation activity of the liver from various animal species including mouse, hamster, rat, rabbit, dog, monkey and human

1999 ◽  
Vol 18 (1) ◽  
pp. 12-16 ◽  
Author(s):  
E Tanaka ◽  
A Ishikawa ◽  
T Horie
Keyword(s):  
Animal Species ◽  
In Vitro Study ◽  
Metabolic Clearance ◽  
Oxidation Activity ◽  
In Vitro Characterization ◽  
Demethylase Activity ◽  
Total Body

Trimethadione (TMO) has the properties required of a probe drug for the evaluation of hepatic drug-oxidizing capacity and, in this study, we have summarized the in vivo and in vitro metabolism of TMO in various animal species including mouse, hamster, rat, rabbit, dog, monkey and human. In the in vivo study, the plasma TMO level was measured after intravenous or oral (human) administration of TMO at a dose of 4 mg/kg to various animal species. The rate of TMO metabolic clearance in these animal species in vivo was in the order mouse > hamster >rat>rabbit>dog>monkey>human. In the in vitro study, species differences were observed in the cytochrome P450 (P450) content and drug-oxidizing enzyme activity. The content of P450 was monkey> mouse>dog>rabbit>hamster>rat>human. On the other hand, TMO N-demethylation was in the order mouse >hamster >rat >rabbit>dog>monkey>human. There was a good correlation between the mean total body clearance of TMO ( in vivo)andthemeanTMON-demethylase activity ( in vitro) (y=1.7×+0.11, r=0.965, P<0.001). These results show that TMO is a probe agent with metabolic and pharmacokinetic characteristics making it attractive for the in vivo and in vitro characterization of metabolic activity in various animal species.

Fabrication, characterization, and in vitro study of zinc substituted hydroxyapatite/silk fibroin composite coatings on titanium for biomedical applications

2017 ◽  
Vol 32 (3) ◽  
pp. 399-409 ◽  
Author(s):  
Zhenyu Zhong ◽  
Jun Ma
Keyword(s):  
Silk Fibroin ◽  
Composite Coatings ◽  
In Vitro Study ◽  
Biological Behavior ◽  
Apatite Formation ◽  
Hydroxyapatite Coatings ◽  
High Bone ◽  
Biomimetic Hydroxyapatite

Zinc substituted hydroxyapatite/silk fibroin composite coatings were deposited on titanium substrates at room temperature by electrophoretic deposition. Microscopic characterization of the synthesized composite nanoparticles revealed that the particle size ranged 50–200 nm, which increased a little after zinc substitution. The obtained coatings maintained the phase of hydroxyapatite and they could induce fast apatite formation in simulated body fluid, indicating high bone activity. The cell culturing results showed that the biomimetic hydroxyapatite coatings could regulate adhesion, spreading, and proliferation of osteoblastic cells. Furthermore, the biological behavior of the zinc substituted hydroxyapatite coatings was found to be better than the bare titanium without coatings and hydroxyapatite coatings without zinc, increasing MC3T1-E1 cell differentiation in alkaline phosphatase expression.

scholarly journals Insights into Cadmium-Induced Carcinogenesis through an In Vitro Study Using C3H10T1/2Cl8 Cells: The Multifaceted Role of Mitochondria

2021 ◽  
Vol 22 (19) ◽  
pp. 10837
Author(s):  
Monica Oldani ◽  
Anna Maria Villa ◽  
Marta Manzoni ◽  
Pasquale Melchioretto ◽  
Paolo Parenti ◽  
...  
Keyword(s):  
Confocal Microscopy ◽  
Oxidative Phosphorylation ◽  
Cell Transformation ◽  
In Vitro Study ◽  
Atp Synthesis ◽  
Cadmium Treatment ◽  
Mouse Embryo Fibroblasts

In this paper, we report the metabolic characterization of two foci, F1 and F3, obtained at the end of Cell Transformation Assay (CTA), performed by treating C3H10T1/2Cl8 mouse embryo fibroblasts with 1 μM CdCl2 for 24 h. The elucidation of the cadmium action mechanism can be useful both to improve the in vitro CTA and to yield insights into carcinogenesis. The metabolism of the two foci was investigated through Seahorse and enzyme activity assays; mitochondria were studied in confocal microscopy and reactive oxygen species were detected by flow cytometry. The results showed that F1 focus has higher glycolytic and TCA fluxes compared to F3 focus, and a more negative mitochondrial membrane potential, so that most ATP synthesis is performed through oxidative phosphorylation. Confocal microscopy showed mitochondria crowded in the perinuclear region. On the other hand, F3 focus showed lower metabolic rates, with ATP mainly produced by glycolysis and damaged mitochondria. Overall, our results showed that cadmium treatment induced lasting metabolic alterations in both foci. Triggered by the loss of the Pasteur effect in F1 focus and by mitochondrial impairment in F3 focus, these alterations lead to a loss of coordination among glycolysis, TCA and oxidative phosphorylation, which leads to malignant transformation.

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