SUMATHY ARUNACHALAM - Academia.edu (original) (raw)

Papers by SUMATHY ARUNACHALAM

Research Journal of Pharmacy and Technology, Sep 28, 2009

The retrospective study was aimed to analyze the patient history to identity the risk factors inv... more The retrospective study was aimed to analyze the patient history to identity the risk factors involved in the hypertension, to identify the co-morbidities, past and present illness, to monitor the prescription and trends in the treatment of hypertension and to estimate the cost of anti hypertensive prescribed to the patient’s. The total number of patients included in the study was 60. The prevalence of hypertension was predominantly more with male patients than in female patients. The average age (57 years) of the population clearly indicates the elderly patients were affected more. It was alarming that 30 % of the total study population was identified as the first time hypertensive in the overall population. 26.7% of the study population was found to be mild hypertensive, around 23.3% of the study population was isolated systolic hypertensive and rest of the population was moderate and severe hypertension.

International research journal of pharmacy, Jul 28, 2014

According to data of the World Health Organization, Tuberculosis (TB) caused by Mycobacterium tub... more According to data of the World Health Organization, Tuberculosis (TB) caused by Mycobacterium tuberculosis, is considered to be the most chronic communicable disease in the World especially in Asia and Africa. This situation was made worse by the emergence of multi drug resistant TB (MDR-TB) and the increasing number of HIV-positive TB cases. Mycobacterium tuberculosis FabH, an essential enzyme in the mycolic acid biosynthetic pathway, is an attractive target for novel anti-tubercolosis agents. A series of pyrazolone linked with isonicotinic acid hydrazide were computationally designed and energy minimized. The molecular properties were calculated from suitable computational tools. These ligands were investigated for drug like properties by calculating Lipinski's rule of five using molinspiration. These compounds were docked into the active site of FabH, (PDB code-1HZP) using Argus lab docking software which showed good binding energy for the enzyme, when compared with the binding energies of standard drug isoniazid -6.17kcal/mol.) Among all the designed ligands, the ligand II and V showed more binding energy values (−8.68 and -8.86Kcal/mol) and the designed ligand are synthesized and evaluvate the TB activity by using alamar blue assay method. From the research work we found that pyrazolone linked with isonicotinic acid hydrazidehave significant role in the anti tubercular activity. The invitroactivity also suggest that the derivativesobtained from the presence of nitro (ligand II) and amino group (ligand v) in the substituted acid having appreciableactivity.

Asian journal of pharmaceutical and health sciences, 2016

International research journal of pharmacy, Nov 28, 2013

Binding interactions of drugs using docking studies is an important component of computer aided d... more Binding interactions of drugs using docking studies is an important component of computer aided drug design. Structure-based lead optimization approaches are a major role in the drug-discovery process. XO(xanthine oxidase) is the key enzyme that catalyzes the oxidation of hypoxanthine to xanthine and then to uric acid. Hyperuricemia is an underlying cause of gout& cardiovascular diseases. Allopurinol, a widely used XO inhibitor and commonly used drug to treat gout. However, a significant portion of the population suffers from adverse effects of allopurinol like gastrointestinal upset and skin rashes. Therefore use of allopurinol-like drugs with minimum side effects is the ideal drug of choice against gout.

Global journal of pharmacy & pharmaceutical sciences, Jul 21, 2017

General procedures Synthesis of 2-aryl-3-amino-4(3H) quinazolinone from anthranilic acid: Anthran... more General procedures Synthesis of 2-aryl-3-amino-4(3H) quinazolinone from anthranilic acid: Anthranilic acid (0.1mol, 13.71gm) was dissolved in 30ml of dry pyridine by stirring slowly at room temperature. The solution was cooled to 0 °C and a solution of an aromatic acid chloride (4-Chlorobenzoyl chloride) (0.02mole) in 30ml of dry pyridine was added slowly with constant stirring [4,5]. After this addition the reaction mixture was further stirred for half an hour at room temperature and set aside for 1h.

Der Pharma Chemica

Aim:Kinase suppressor of Ras (KSR) is a conserved component of the Ras pathway that acts as a mol... more Aim:Kinase suppressor of Ras (KSR) is a conserved component of the Ras pathway that acts as a molecular scaffold to promote signal transmission from Raf-1 to MEK and MAPK. Method: Study has been carried out through Computational analysis on inhibition of conserved cysteine-rich C1 domain of KSR protein receptor and MAPK downstream signaling pathway interruption through molecular docking studies by polyphenolic compounds. Result:The ligands investigated were found to occupy the potential areas of active site of ksr with satisfactory binding energies. Ligands like 2'-Hydroxygenistein showed lowest binding energy value of -6.36 kcal/mol. Further, Binding site analysis shows the ligands has the high fidelity towards target site with maximum potential. Conclusion:Investigational ligands has occupied the potential area of interaction of Raf binding sites, in such perspective these ligands can be targeted for interruption in MAPK signaling pathway for neoplasia

Terpenoids and flavonoids were evaluated for Acetylcholinesterase inhibition using in-silico and ... more Terpenoids and flavonoids were evaluated for Acetylcholinesterase inhibition using in-silico and in-vitro methods. Insilico docking method is carried out using AutoDock 4.2 tools and in-vitro AChE inhibition was based on Ellman method. The protein structure (amino acid sequence)of human AChE is similar to AChE from electric eelwas used for the evaluation. The crystal structure of AChE was downloaded from RCSB protein data bank. Terpenoids used for docking study were Ambrein, Geraniol, Limonene. Linalool, and ferulic acid whose lowest binding energy(kcal/mol) was found to be -9.54 kcal/mol, - 5.22 kcal/mol, -5.46 kcal/mol, -5.16 kcal/mol, -5.17 kcal/mol and their supporting IC50 values obtained through in-vitro enzyme inhibition studies were 91 µg/ml ± 0.12, 200 µg/ml ± 0.21, 195 µg/ml ± 0.43, 200 µg/ml ± 0.24, 185 µg/ml ± 0.56 respectively. Flavonoids used for the docking studies were Quercetin, Curcumin, Myricetin, Kaempferol, and Luteolin whoselowest binding energy was found to be...

Dipeptidylpeptidase-4 is an enzyme involved in the inhibition of GLP-1 (Incretin),which is necess... more Dipeptidylpeptidase-4 is an enzyme involved in the inhibition of GLP-1 (Incretin),which is necessary for the stimulation of insulin release. It is one of the enzyme targets for the treatment of type-2 diabetes mellitus. Ethanolic and aqueous extracts of Pergularia demia were investigated for activity using ellman method. Successive concentrations (50mg/ml,100mg/ml,200 mg/ml,400 mg/ml,800 mg/ml)of ethanolic and aqueous extracts were prepared and investigated for their inhibitory activity towards dipeptidylpeptidase-4 as per Kojima et al., method. It was found that both extracts exhibited significant activity towards DPP-4 inhibition. Diprotein-A was used as the standard and distilled water used as the control.

Tropical Journal of Pharmaceutical Research, Feb 16, 2023

Purpose: To synthesize novel pyrazolone fused thiazolidinone analogues and evaluate their efficie... more Purpose: To synthesize novel pyrazolone fused thiazolidinone analogues and evaluate their efficiency as potent HER2 and EGFR inhibitors in human breast adenocarcinoma cells for anti-cancer activity. Method: In this study, several pyrazolone fused thiazolidinone analogues were synthesized, and characterized by elemental analysis, IR, 1 H-NMR, 13 C-NMR, and mass spectroscopy, as well as tested for their in vitro cytotoxicity against breast cancer cell line (MCF-7) by MTT assay. A correlation study of the cytotoxicity was performed to obtain the Docking score using Schrodinger (Maestro) Version 9.6 Glide XP software. Result: A total of 10 compounds were synthesised and analysed for their physiochemical, spectral, and cytotoxic activity against breast cancer cell lines (MCF-7). Among the synthesised compounds, compound 4B5 showed significantly higher (p < 0.05) anticancer properties against MCF-7 cell lines with docking score of-6.614, and half-maximal concentration (IC50) value of 001.17 M compared to other synthesized compounds of the same categories. Conclusion: Novel pyrazolone-fused thiazolidinone analogues have been successfully synthesized. The synthesised compounds possess anti-cancer activity against the MCF-7 cell lines. This could potentially lead to the development of new anti-breast cancer agents.

Copyright © 2011 Palanisamy Sivanandy et al. This is an open access article distributed under the... more Copyright © 2011 Palanisamy Sivanandy et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. The aim of this study was to evaluate the efficacy and safety of thrombolytic therapy. Our study enrolled 23 patients out of which 2 patients died due to ICH; we also found that only 39 % of patients reached hospital within stroke window, and for those treated, mean NIHSS during admission was 14.0, but drastic improvement was shown after 24 hours of treatment, that is, 9.89 (P < 0.0001), and at discharge, it was 5.1 (P <0.0001) which showed a clear impact of the treatment, and around 60 % of patients were discharged within an mRS score of 1 and 2. Hence, it was found that thrombolytic therapy was beneficial, efficacious, and safe if used within 3 to 4.5 hours. 1.

Journal of Pharmaceutical Research International

Background: Cancer is the world's second leading cause of death, accounting for an estimate o... more Background: Cancer is the world's second leading cause of death, accounting for an estimate of more than 10 million deaths annually. The most common type of cancers in women are breast, endometrial, cervical, ovarian, colorectal, lung, and skin cancers.Among these, breast cancer is the most common in women of all ages. Human epidermal growth factor receptor 2 breast cancer is widely seen in women which test positive for the protein HER2. This protein is present in one-fifth of every breast cancer cell, which promotes the growth of cancer cells. There are several compounds available for the treatment of HER2 breast cancer in the market with varying promise in their efficacy and safety on HER2 treatment. Objective: To design synthesis and evaluation of core scaffold pyrazolone fused thiazolidinone derivatives as anticancer agents. Methods: In this study, the core scaffold pyrazolone fused thiazolidinone derivatives were designed, synthesized, and analyzed for the anticancer activi...

World Journal of Pharmaceutical and life sciences, Apr 8, 2005

World Journal of Pharmacy and Pharmaceutical Sciences, 2017

Pyrimidine and pyrazole shows various pharamacological activities. Pyrimidine is a heterocyclic a... more Pyrimidine and pyrazole shows various pharamacological activities. Pyrimidine is a heterocyclic aromatic organic compound containing two nitrogen atoms at positions 1 and 3 of the six-membered ring which shows wide range of biological activities. [1] Pyrimidines are synthetically versatile substrates, where they can be used for the synthesis of a large variety of heterocyclic compounds and as raw material for drug synthesis. It was therefore the objective of this review to systematically evaluate the pharmacological properties of various substituted pyrimidine and collate these findings to be used as a guide for future structure-activity relationship and mode of action studies. [2] Pyrazoles are an important class of five membered heterocyclic compounds; are widely found as the core structure in a large variety of compounds that possess important agrochemical and pharmaceutical activities. [3] The main aim of this review is the comparative study of pyrazole and pyrimidine.

Journal of Pharmacy Research

Glycogen synthase kinase 3β (GSK3β) is a serine/threonine kinase that has enzymatic activity regu... more Glycogen synthase kinase 3β (GSK3β) is a serine/threonine kinase that has enzymatic activity regulated by many signaling pathways and by distinct multiproteincomplexes. Glycogen synthase kinase-3β (GSK-3β) has been investigated for its potential binding affinity with selective anthraquinones like aesculin, aesculetin, anthragallol, damnacanthal, lucidin, morindone, nordamnacanthal and Rubiadin. Insilico docking studies showed that almost every ligands with better binding affinity and a satisfactory inhibition constant. Among them damnacanthal, nordamnacanthal, Anthragallol and morindone showed lowest free energy of binding through interaction with potential areas of amino acids exposed at the active site crucial for enzyme inhibition. These ligands can be targeted towards the inhibition of Glycogen synthase kinase-3β (GSK-3β) involved in specific neoplastic disoders like prostate cancer, oral cancer etc.

Polyphenolic compounds posses vast number of biological activities and they are the inclusions of... more Polyphenolic compounds posses vast number of biological activities and they are the inclusions of phytoconstituents of plant kingdom. Synthetic drugs usedin the treatment of neurodegenerative disorders like Alzheimer’s disease is of only symptomatic and for not permanent cure over the progression of the disease. Beta secretase-1(BACE1) is aspartic protease makes improper cleavage of amyloid precursor protein (APP) found on the membrane of the neuronal cells and produces the accumulation of beta amyloid proteins of insoluble fractions. Polyphenolic compounds like catechin3gallate, hesperidin, hesperitin etc., were found to possess lowest binding energy with best conformation, when comparing with the standard reference ligands. In this insilico docking studies, it revealed that targeting BACE1 inhibition, through Polyphenolic compounds can create number of lead molecules for better therapeutic concern in future

Oriental Pharmacy and Experimental Medicine, 2014

ABSTRACT Rho Kinases regulate a wide range of biological processes, including reorganization of t... more ABSTRACT Rho Kinases regulate a wide range of biological processes, including reorganization of the actin cytoskeleton, transcriptional regulation, vesicle trafficking, morphogenesis, neutrophil activation, phagocytosis and activation of the NADPH oxidase, mitogenesis, apoptosis and tumorigenesis. Rho associated coiled coil kinase-II (ROCK-II) is one of the isoform of Rho associated coiled coil kinase. ROCK-II is distributed mostly in the brain and heart.Insilico docking studies was carried out in targeting the crystal structure of ROCK-II with some rare selective flavonoids. Fasudil, well known ROCK-II inhibitor was used as a reference ligand. Amentoflavone and some selective flavonoids were showed lowest binding energy with corresponding dissociation constant (kd) values on comparing with reference ligands. It has been found out that these compounds possess inhibitory activity against ROCK-II through computational analysis.

The aim of this study was to evaluate the efficacy and safety of thrombolytic therapy. Our study ... more The aim of this study was to evaluate the efficacy and safety of thrombolytic therapy. Our study enrolled 23 patients out of which 2 patients died due to ICH; we also found that only 39% of patients reached hospital within stroke window, and for those treated, mean NIHSS during admission was 14.0, but drastic improvement was shown after 24 hours of treatment, that is, 9.89 (P < 0.0001), and at discharge, it was 5.1 (P < 0.0001) which showed a clear impact of the treatment, and around 60% of patients were discharged within an mRS score of 1 and 2. Hence, it was found that thrombolytic therapy was beneficial, efficacious, and safe if used within 3 to 4.5 hours.

Asian Journal of Pharmaceutical and Health Sciences, 2021