Nanovesicular ultraflexible invasomes and invasomal gel for transdermal delivery of phytopharmaceuticals.

Tweetable abstract Invasomes and invasomal gel are ultraflexible, soft vesicular, phospholipid based nanocarriers with deeper skin penetration ability for transdermal applications of drugs and phytopharmaceuticals.

Synthesis, characterization, and radiosynthesis of fluorine-18-AVT-011 as a Pgp chemoresistance imaging marker.

P-glycoprotein (Pgp) is the most studied ATP-binding cassette (ABC) efflux transporter and contributes to chemoresistance. A few tracers have been developed to detect the in-vivo status of chemoresistance using positron emission tomography (PET) imaging. In our study, we have synthesized labeled AVT-011 with fluorine-18 (F) followed by in-vitro and in-vivo analysis.

Targeting G-Quadruplex DNA for Cancer Chemotherapy.

The self-association of DNA formed by Hoogsteen hydrogen bonding comprises several layers of four guanine or G-tetrads or G4s. The distinct feature of G4s, such as the G-tetrads and loops, qualify structure-selective recognition by small molecules and various ligands and can act as potential anticancer therapeutic molecules. The G4 selective ligands can influence gene expression by targeting a nucleic acid structure rather than sequence.

On effective cognitive state classification using novel feature extraction strategies.

Investigating new features for human cognitive state classification is an intiguing area of research with Electroencephalography (EEG) based signal analysis. We plan to develop a cost-effective system for cognitive state classification using ambulatory EEG signals. A novel event driven environment is created using external stimuli for capturing EEG data using a 14-channel Emotiv neuro-headset.

Stereoselective Synthesis of Spirooxindole Derivatives Using One-Pot Multicomponent Cycloaddition Reaction and Evaluation of Their Antiproliferative Efficacy.

A highly stereoselective, one-pot, multicomponent method has been developed to synthesize pyrrolizidine- and -methyl pyrrolidine-substituted spirooxindole derivatives. The [3 + 2] cycloaddition reaction involves the reaction between the dipole azomethine ylides, generated from the reaction between isatin and secondary amino acids such as L-proline or sarcosine, and α,β-unsaturated carbonyl compounds as the dipolarophile. The reaction condition was optimized to achieve excellent regio- and stereoselectivity.

Author Correction: Preparation of Lauroyl Grafted Alginate-Psyllium Husk Gel Composite Film with Enhanced Physicochemical, Mechanical and Antimicrobial Properties.

An amendment to this paper has been published and can be accessed via a link at the top of the paper.

Recent Progress of Adenosine Receptor Modulators in the Development of Anticancer Chemotherapeutic Agents.

Increased risks of peripheral toxicity and undesired adverse effects associated with chemotherapeutic agents are the major medical hurdles in cancer treatment that worsen the quality of life of cancer patients. Although several novel and target-specific anticancer agents have been discovered in the recent past, none of them have proved to be effective in the management of metastatic tumor. Therefore, there is a continuous effort for the discovery of safer and effective cancer chemotherapeutic agent.

Preparation of Lauroyl Grafted Alginate-Psyllium Husk Gel Composite Film with Enhanced Physicochemical, Mechanical and Antimicrobial Properties.

In this study, a lauroyl grafted hydrophobic glycolipid derivative of alginate has been successfully synthesized and characterized. This glycolipid has been incorporated into Psyllium husk gel-alginate composite films and compared with the films containing only Psyllim husk gel and Psyllim husk gel-alginate for its mechanical and physicochemical properties. Additionally, the composite film has also been evaluated for protein adsorption and antimicrobial property to verify its utility in biomedical applications.

Hybrids of Steroid and Nitrogen Mustard as Antiproliferative Agents: Synthesis, In Vitro Evaluation and In Silico Inverse Screening.

Hybrids of 16E-arylidene steroids and nitrogen mustard have been synthesized and evaluated for their in vitro cytotoxic activity to develop tissue specific antineoplastic agents from steroids. These hybrids displayed specificity towards leukemia cell lines, however somewhat reduced potency was observed in comparison with the earlier reported 16E-arylidene steroids. The in silico reverse screening experiments were employed to find out the probable pharmacological mechanism of these hybrids.

Synthesis of androstene oxime-nitrogen mustard bioconjugates as potent antineoplastic agents.

In the present study, synthesis and antineoplastic activity of phenylacetic acid and benzoic acid nitrogen mustard conjugates of various steroidal oximes are reported for the first time. The conjugation was achieved through a more stable oxime-ester linkage and the resulting newly synthesized conjugates were evaluated in vitro on various human cancer cell lines for cytotoxicity. The extent of their alkylating activity was investigated by the in vitro colorimetric 4-(p-nitrobenzyl)pyridine (NBP) assay.

FTIR assay method for UV inactive drug carisoprodol and identification of degradants by RP-HPLC and ESI-MS.

A new method of analysis has been developed for UV inactive drug carisoprodol using FTIR spectroscopy. These methods were validated for various parameters according to ICH guidelines. The proposed method has also been successfully applied for the determination of the drug concentration in a tablet formulation.

Radiosynthesis of [18F]-fluorobenzoate-doxorubicin Using Acylation Approach.

Background: Previously, we have labeled doxorubicin with [99Tc] and evaluated its potential as a SPECT agent to detect cancer in tumor bearing mice. In this study, we sought to radiolabel doxorubicin with [18F] using acylation method.

Methods: A quaternary salt of the precursor pentamethylbenzyl-4-(trimethylammonium trifluoromethanesulfonate) benzoate was synthesized and characterized by 1H-NMR.

Synthesis and antiproliferative activity of some androstene oximes and their O-alkylated derivatives.

In order to study the structure-activity relationship with respect to the cytotoxicity of steroidal oximes, several 6E-hydroximino-4-ene steroids and their O-alkylated derivatives were synthesized. The oxime ethers were solidified and purified by preparing their corresponding oxalate salts. The new derivatives as well as some previously synthesized ones were evaluated for in vitro antineoplastic activity against a panel of 60 cancer cell lines at 10 µM.

Synthesis and antileukemic activity of 16E-[4-(2-carboxy)ethoxybenzylidene]-androstene amides.

In order to determine the structural requirements for cytotoxicity against various tumor cell lines, a new series of 16E-arylidene androstene amides with varying degrees of unsaturation in ring A has been synthesized. Characterization and invitro cytotoxic studies of the newly synthesized compounds are discussed. The compounds on evaluation against various tumor cell lines exhibited significant growth inhibition on leukemia cell lines.