EDITOR’S CHOICE ARTICLE –Preparation, Characterization and In vitro Biological Activity of Soyasapogenol B Loaded onto Functionalized Multi-walled Carbon Nanotubes

Journal Name: Current Bioactive Compounds

Author(s): Ahmed A. Haroun*, Hala A. Amin, Sameh H. Abd El-Alim.




Graphical Abstract:




Background: Using Multi-Walled Carbon Nanotubes (MWCNTs) as a drug delivery system, can avoid the need for solvents and preventing drug precipitation in aqueous solution. Soyasapogenol B (SSB) acts as an important therapeutic agent owing to its numerous reported biological activities. Hence, this work deals with preparation and characterization of SBB loaded onto functionalized MWCNTs with tetraethyl orthosilicate (TEOS) and/or chitosan.

Method: SSB was immobilized onto functionalized MWCNTs using miniemulsion technique. Moreover, niosomes were utilized to encapsulate the prepared systems. The formulations were analyzed by Fourier Transform Infrared Spectroscopy (FTIR), Transmission Electron Microscope (TEM) and particle size distribution analysis. In vitro release profiles of loaded SSB particles were carried out and kinetics of release were also studied. In vitro cytotoxicity of the prepared materials was examined and evaluated by SRB assay using different human cell lines such as normal melanocytes (HFB4), and carcinoma breast and liver (MCF7 and HepG2, respectively) in comparison with the standard doxorubicin.

Results: SSB loaded materials exhibited successful encapsulation in niosomes, resulting in sustainable in drug release. Study of kinetics of release revealed presence of several complex factors affecting SSB release. Mathematical processing of the in vitro release data showed that the release of SSB from niosomal formulations obeyed more than one model. The second order and Higuchi’s models were the most fitting models in case of presence of chitosan or TEOS, respectively. While, all formulations exhibited low cytotoxic properties on all tested cell lines.

Conclusion: FTIR, particle size and TEM analysis confirmed that SSB was successfully loaded onto functionalized MWCNTs. Moreover, the different niosome formulations based on functionalized MWCNTs were prepared with sustainable SSB release in. The cytotoxicity could be minimized in case of chitosan and TEOS functionalization.


For more details, please visit: http://www.eurekaselect.com/151456/article

Major Article Contributions by some of the Indian Authors of Bentham Science Publishers in the Journal: Medicinal Chemistry

Journal Name: Medicinal Chemistry

Article Title QSAR Study on a Series of Aryl Carboxylic Acid Amide Derivatives as Potential Inhibitors of Dihydroorotate Dehydrogenase (DHODH)

Author(s): Vivek K. Vyas and Manjunath Ghate

Abstract: QSAR study was performed on a series of aryl carboxylic acid amide derivatives (62 analogs) to establish structural features required for human dihydroorotate dehydrogenase (hDHODH) inhibition. Statistical significant QSAR models were developed for the prediction of hDHODH inhibitory activity by applying MLR analysis (r2 = 0.851 and q2 = 0.795), PCR analysis (r2 = 0.713 and q2 = 0.667) and PLS analysis (r2 = 0.848 and q2 = 0.802). QSAR study emphasized the importance of topological, estate number, hydrophobic and alignment independent descriptors for the prediction of hDHODH inhibitory activity. SaasCcount descriptor suggested the presence of carbon atoms in five member aryl ring system. Positive impact of alignment independent descriptors reveals the presence of carbonyl oxygen and chloro group in this series of compounds. DistTopo signifies basic connectivity of atoms in the molecules. High degree of predictability of the proposed QSAR models offers a great potential for the design and development of potent hDHODH inhibitors.

For more Details, visit: http://benthamscience.com/journal/abstracts.php?journalID=mc&articleID=106309

Article Title: QSAR and Docking Based Semi-synthesis and in vitro Evaluation of 18 β-glycyrrhetinic Acid Derivatives Against Human Lung Cancer Cell Line A-549

Author(s): Dharmendra Kumar Yadav, Komal Kalani, Feroz Khan and Santosh Kumar Srivastava

Abstract: For the prediction of anticancer activity of glycyrrhetinic acid (GA-1) analogs against the human lung cancer cell line (A-549), a QSAR model was developed by forward stepwise multiple linear regression methodology. The regression coefficient (r2) and prediction accuracy (rCV2) of the QSAR model were taken 0.94 and 0.82, respectively in terms of correlation. The QSAR study indicates that the dipole moments, size of smallest ring, amine counts, hydroxyl and nitro functional groups are correlated well with cytotoxic activity. The docking studies showed high binding affinity of the predicted active compounds against the lung cancer target EGFR. These active glycyrrhetinic acid derivatives were then semi-synthesized, characterized and in-vitro tested for anticancer activity. The experimental results were in agreement with the predicted values and the ethyl oxalyl derivative of GA-1 (GA-3) showed equal cytotoxic activity to that of standard anticancer drug paclitaxel.

For more details, visit: http://benthamscience.com/journal/abstracts.php?journalID=mc&articleID=116645

Article Title: Synthesis, Leptospirocidal Activity and QSAR Analysis of Novel Quinoxaline Derivatives

Author(s): Ayarivan Puratchikody, Ramalakshmi Natarajan, Mukesh Doble, Shanmugam Hema Iswarya and Raj Vijayabharathi

Abstract: A simple and efficient method has been developed for the synthesis of series of N-Mannich bases of (E)-3- (phenylimino/4-chlorophenylimino)-2,3-dihydro-1-[(N-substituted piperazinyl) methyl]quinoxaline-2-(1H)-one 3a-f and 4a-f. The requisite 2a and 2b were obtained by reactionbetween quinoxaline-2,3-dione 1 and aniline / p-chloroaniline. These compounds underwent NMannich reaction with various substituted piperazines to yield (title compounds 3a-f and 4a-f respectively. Structures of synthesized compounds were confirmed by spectral studies (IR, 1H NMR, 13C NMR and Mass) and elemental analysis. All the synthesized compounds were screened for in vitro leptospirocidal activty against Leptospira interrogans. The potent compounds 4a, 4b and 4c which showed maximum activity during in vitro studies were subjected to in vivo studies. The inhibitory activity of enzymes carboxypeptidase and transpeptidase, in leptospirosis by the synthesized compounds were determined. 3D-QSAR studies model developed showed the need for more hydrophobic and less steric groups as substituent groups to enhance the in vitro activity.

For more details, Visit: http://benthamscience.com/journal/abstracts.php?journalID=mc&articleID=106312

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