Research Title: Pharmacology of Adenosine Receptors

Author: Balakumar Chandrasekarn, Published Year: 2020

Faculty: Pharmacy

Abstract: Adenosine is an endogenous nucleoside molecule, regulating a myriad of physiological and pathological effects in almost all the organs systems including central nervous system (CNS), cardiovascular system (CVS), respiratory system, renal system, and immune system. Biological functions of adenosine are mediated by its interactions with four subtypes of G-protein-coupled receptors (GPCRs), namely A1, A2A, A2B, and A3 adenosine receptors (ARs) which are ubiquitously present throughout the body. However, ubiquitous distribution of ARs in both healthy and diseased tissues imposed a great challenge to the researchers in the discovery and development of ligands targeting a particular AR subtype in a specific tissue, devoid of undesirable side effects

Keywords: Adenosine · A1, A2A, A2B and A3 adenosine receptors · G-protein-coupled receptors (GPCRs) · Adenosine receptors signaling

Research Title: Drug-Receptor Interactions

Author: Balakumar Chandrasekarn, Published Year: 2020

Faculty: Pharmacy

Abstract: Conventional treatment of any disease can be achieved by the administration of drugs of natural and synthetic origin. The drug exhibits its pharmacological action by altering cellular signaling or the biochemical events associated with the respective target proteins such as receptors or enzymes. Functional groups/ pharmacophores of the drug interact with functional groups present in the receptor’s binding site, complementarily thereby producing effective binding interactions. Key interactions that occur between the drug and the receptor will decide the potency and intrinsic activity of the drug. Major interactions observed in the drug-receptor complexes are mostly of reversible type which consist of electrostatic interactions, ion-dipole and dipole-dipole interactions, hydrogen bonding, charge-transfer interactions, hydrophobic, and Van der Waals interactions. In this chapter, we have discussed the types of receptors, theories and types of drug-receptor interactions, the role of functional groups, and

Keywords: Drug-receptor complex · H-bonding · VdW interaction · Antagonist · Agonist

Research Title: A system for prediction, prevention, and diagnosis of heart related diseases at an early stage using deep learning

Author: Balakumar Chandrasekarn, Published Year: 2022

Faculty: Pharmacy

Abstract: A system for prediction, prevention, and diagnosis of heart related diseases at an early stage using deep learning

Keywords: A system; prediction; prevention; deep learning

Research Title: Computer aided drug design and green synthesis of novel pyrazole analogues as potential SARS-CoV-2 main protease inhibitors against anti COVID-19 protein targets.

Author: Balakumar Chandrasekarn, Published Year: 2021

Faculty: Pharmacy

Abstract: Computer aided drug design and green synthesis of novel pyrazole analogues as potential SARS-CoV-2 main protease inhibitors against anti COVID-19 protein targets.

Keywords: Computer aided drug design; green synthesis; pyrazole analogues

Research Title: In silico screening, physicochemical and pharmacokinetic analysis of novel sulfonamides as potential antimicrobial drugs docked with protein targets: PDB: 2VF5, 1KZN and 1JIJ

Author: Balakumar Chandrasekarn, Published Year: 2021

Faculty: Pharmacy

Abstract: In silico screening, physicochemical and pharmacokinetic analysis of novel sulfonamides as potential antimicrobial drugs docked with protein targets: PDB: 2VF5, 1KZN and 1JIJ

Keywords: In silico screening; physicochemical; pharmacokinetic

Research Title: N-substituted isatin hydrazones as antimycobacterial and antimicrobial agents

Author: Balakumar Chandrasekarn, Published Year: 2017

Faculty: Pharmacy

Abstract: N-substituted isatin hydrazones as antimycobacterial and antimicrobial agents

Keywords: isatin; hydrazones; antimycobacterial and antimicrobial agents

Research Title: Development of Polymeric-Based Formulation as Potential Smart Colonic Drug Delivery System

Author: Balakumar Chandrasekarn, Published Year: 2022

Polymers, 14

Faculty: Pharmacy

Abstract: Conventional oral formulations are mainly absorbed in the small intestine. This limits their use in the treatment of some diseases associated with the colon, where the drug has to act topically at the inflammation site. This paved the way for the development of a smart colonic drug delivery system, thereby improving the therapeutic efficacy, reducing the dosing frequency and potential side effects, as well as improving patient acceptance, especially in cases where enemas or other topical preparations may not be effective alone in treating the inflammation. In healthy individuals, it takes an oral medication delivery system about 5 to 6 h to reach the colon. A colonic drug delivery system should delay or prohibit the medication release during these five to six hours while permitting its release afterward. The main aim of this study was to develop a smart drug delivery system based on pH-sensitive polymeric formulations, synthesized by a free-radical bulk polymerization method, using different monomer and crosslinker concentrations. The formulations were loaded with 5-amino salicylic acid as a model drug and Capmul MCM C8 as a bioavailability enhancer. The glass transition temperature (Tg), tensile strength, Young’s modulus, and tensile elongation at break were all measured as a part of the dried films’ characterization. In vitro swelling and release studies were performed to assess the behavior of the produced formulations. The in vitro swelling and release evaluation demonstrated the potential ability of the developed system to retard the drug release at conditions mimicking the stomach and small intestine while triggering its release at conditions mimicking the colon, which indicates its promising applicability as a potential smart colonic drug delivery system

Keywords: 5-amino salicylic acid; smart delivery system; sustainable polymers; triggered drug delivery; ulcerative colitis

Research Title: Mucilage of Coccinia grandis as an Efficient Natural Polymer-Based Pharmaceutical Excipient

Author: Balakumar Chandrasekarn, Published Year: 2022

Polymers, 14

Faculty: Pharmacy

Abstract: Natural eco-friendly materials are recently employed in products to replace synthetic materials due to their superior benefits in preserving the environment. The herb Coccinia grandis is widely distributed in continents like Asia and Africa and used traditionally to treat fever, leprosy, asthma, jaundice, and bronchitis. Mucilage of Coccinia grandis was accordingly extracted, isolated by a maceration technique, and precipitated. The mucilage was evaluated for its physicochemical, binding, and disintegrant properties in tablets using paracetamol as a model drug. The crucial physicochemical properties such as flow properties, solubility, swelling index, loss on drying, viscosity, pH, microbial load, cytotoxicity was evaluated and the compatibility was analyzed using sophisticated instrumental methods (TGA, DTA, DSC, and FTIR). The binding properties of the mucilage was used at three different concentrations and compared with starch and PVP as examples of standard binders. The disintegrant properties of mucilage were used at two different concentrations and compared with standard disintegrants MCCP, SSG, and CCS. The tablets were punched and evaluated for their hardness, friability, assay, disintegration time, in vitro dissolution profiles. In vitro cytotoxicity studies of the mucilage were performed in a human embryonic kidney (HEK) cell line. The outcome of the study indicated that the mucilage had good performance compared with starch and PVP. Further, the mucilage acts as a better disintegrant than MCCP, SSG and CCS for paracetamol tablets. Use of a concentration of 3% or less demonstrated the ability of the mucilage to act as a super disintegrating agent and showed faster disintegration and dissolution, which makes it as an attractive, promising disintegrant in formulating solid dosage forms to improve the therapeutic efficacy and patient compliance. Moreover, the in vitro cytotoxicity evaluation results demonstrated that the mucilage is non-cytotoxic to human cells and is safe.

Keywords: binding agent; disintegrating agent; natural polymer; mucilage; Coccinia grandis

Research Title: Target protein degradation by protacs: A budding cancer treatment strategy

Author: Mohammad Bayan, Published Year: 2023

Pharmacology and Therapeutics, 250

Faculty: Pharmacy

Abstract: Cancer is one of the most common causes of death. So, its lethal effect increases with time. Near about hundreds of cancers are known in humans. Cancer treatment is done to cure or prolonged remission, and shrinkage of the tumor. Cytotoxic agents, biological agents/targeted drugs, hormonal drugs, surgery, radiotherapy/proton therapy, chemotherapy, immunotherapy, and gene therapy are currently used in the treatment of cancer but their cost is high and cause various side effects. Seeing this, some new targeted strategies such as PROTACs are the need of the time. Proteolysis targeting chimera (PROTAC) has become one of the most discussed topics regarding cancer treatment. Few of the PROTAC molecules are in the trial phases. PROTACs have many advantages over other strategies such as modularity, compatibility, sub-stoichiometric activity, acting on undruggable targets, molecular design, and acts on intracellular targets, selectivity and specificity can be recruited for any cancer, versatility, and others. PROTACs are having some unclear questions on their pharmacokinetics, heavy-molecular weight, etc. PROTACs are anticipated to bring about a conversion in current healthcare and will emerge as booming treatments. In this review article we summarize PROTACs, their mechanism of action, uses, advantages, disadvantages, challenges, and future aspects for the successful development of potent PROTACs as a drug strategy.

Keywords: PROTACs, Cancer, E3 Ligases, Protein Degradation, Ubiquitination.

Research Title: The Moderating Role of Liquidity in the Relationship between the Expenditures and Financial Performance of SMEs: Evidence from Jordan

Author: Fahd Mohammed Saleh Al-Duais, Published Year: 2023

Economies, 11(4)

Faculty: Business

Abstract: The current paper aims to investigate the moderating role of liquidity in the relationship between accounting and advertising expenditures and the financial performance of small and medium enterprises (SMEs) in Jordan. Furthermore, the present paper highlights the importance of managing expenditures and improving financial performance. Since the performance of Jordanian SMEs is extremely critical, furthermore, the present paper explores the possibility of empowering these businesses in order to achieve profitability. This paper is based on descriptive statistics, regression, and correlation analysis in order to analyze the data, collecting secondary data from 200 SMEs. The results demonstrate that accounting expenditures are key factors for financial performance, especially in SMEs. Moreover, SMEs are more sensitive to liquidity challenges, which significantly impact their short-term expenditure and consequently influence their financial performance. It is evident that accounting expenditures moderated by liquidity have a positive effect on the financial performance of SMEs. However, our findings indicate a negative effect regarding the relationship between advertising expenditures and financial performance. According to the results of this study, regulators may offer new regulations and legislation in the future to the Ministry of Finance and the Amman Stock Exchange.

Keywords: accounting expenditure; advertising expenditure; liquidity; small and medium enterprises (SMEs)