Chitta Suresh - Academia.edu (original) (raw)
Papers by Chitta Suresh
Proper cell cycle progression is critical for maintaining genomic stability. Mitosis is particula... more Proper cell cycle progression is critical for maintaining genomic stability. Mitosis is particularly tightly regulated as deregulated mitosis would lead to improper segregation of chromosomes. Checkpoints including G2/M checkpoint, kinetochore and spindle checkpoint have therefore evolved to ensure proper onset of mitosis and correct
PubMed, Jul 1, 2011
The main aim of present investigation was to develop sustained release matrix tablets of Gliclazi... more The main aim of present investigation was to develop sustained release matrix tablets of Gliclazide using fruit mucilage from the plant Ficus glomerata. Varying ratios of drug and polymer viz. 1:0.25, 1:0.5, 1:0.75, 1:1.0 and 1:1.25 were selected for the study. The flow properties of powdered mucilage and physical properties of matrix tablets were performed. The swelling behavior and release rate characteristics were studied. The in vitro drug release data was analyzed by zero order, first order, Higuchi plot, Peppas plot and Hixon-Crowell Models. It was observed that as the proportion of mucilage increased the release of drug from the matrix tablets was retarded. Stability studies were conducted at 40±2ºC and RH 75±5% for 3 months indicates that Gliclazide was stable in the matrix tablets. The Differential Scanning Calorimetric (DSC) and Fourier Transform Infrared (FTIR) study revealed that there was no negative chemical interaction between drug and the mucilage used. From the dissolution study, it was concluded that dried Ficus glomerata mucilage can be used as an excipient for making sustained release matrix tablets.
Journal of Computational Biology and Bioinformatics Research, Jan 31, 2011
The structure of thrombin protein Oncorhynchus mykiss had not yet been resolved by NMR or X-ray d... more The structure of thrombin protein Oncorhynchus mykiss had not yet been resolved by NMR or X-ray diffraction method. In the present work, we have modeled the structure of protein using Modeller 9v1, taking human thrombin protein as the template. Furthermore, the antithrombin protein was docked with the best model generated by R-dock and Z-dock module of INSIGHT II and the nine potential amino acids involved in anchoring of antithrombin with thrombin were identified as: Leu3,
Journal of Biomolecular Structure & Dynamics, Feb 20, 2017
Pseudomonas aeruginosa (P.aeruginosa) is an opportunistic microorganism causing diseases both in ... more Pseudomonas aeruginosa (P.aeruginosa) is an opportunistic microorganism causing diseases both in animals and humans. In case of human pathology, the role of P.aeruginosa is one of the major concerns in intensive care septicemia. Presently the drug resistance strains of P.aeruginosa are arising mainly by developing multiple mechanisms due to its natural and acquired resistance to many of the antimicrobial agents commonly used in clinical practice. As a result, there is a direneed to invent new drugs so that they may restrict the outbreak of multidrug resistant strains. Virtual high-throughput insilico screening, which helps to identify the chemical ligands that bind to the enzymes, is an important tool in drug discovery and the drugs discovered in this way are clinically tested. In this study, Methyl isocitrateLyase (MICL), which is essential for the survival of the bacterium and which doesn't show any similarity with the humans, was selected to evaluate the functions of high-affinity inhibitors (PPI-analogs) that are identified using the virtual screening approach. By adopting the computational analysis tools structural, functional and inhibitor interactions of MICL against P.aeruginosa were identified. The PPIA-32 is found to be the best binding interactions with MICL. PPIA-32 reduces the binding affinity for substrate to residues required for MICL enzyme activity and also RMSD simulations shows the most stable nature of PPA32-MICL(complex) than that of MICL alone, thereby effectively inhibiting the growth of virulent P.aeruginosa. To our suprise the same phenomenon is also identified with other Gram negative bacteria like E. coli,Klebsiella pneumonia, Salmonella typhi.
The main objective of the present study was to develop matrix-moderated transdermal systems of Di... more The main objective of the present study was to develop matrix-moderated transdermal systems of Diltiazem HCl using various proportions of Ficus reticuleta fruit mucilage. Physical evaluation was performed such as moisture content, moisture uptake, tensile strength, flatness and folding endurance. In-vitro penetration studies were performed in a Keshary-Chien diffusion cell. The matrix-type transdermal systems were prepared using Diltiazem HCl with Ficus reticuleta fruit mucilage by the solvent evaporation technique. The interactions between Diltiazem HCl and Ficus reticuleta fruit mucilage were performed. The transdermal patches were subjected to various physicochemical parameters viz. mechanical properties, permeation studies and skin irritation studies. The prepared patches possessed satisfactory pre-formulary and formulary characteristics. In vitro permeation studies were performed using a Keshary-Chien diffusion cell across hairless Albino rat skin. The non-ionic surfactants Span 80, Glycerin, Propylene glycol in the formulation played a role as permeability enhancer. The patches were seemingly free of potentially hazardous skin irritation. The experimental results shows that the release of drug from the patch delayed in controlled manner as the proportion of Ficus reticuleta increased. It was concluded that Diltiazem HCl can be developed as a transdermal patches with Ficus reticuleta fruit mucilage
Journal of Pharmacy Research, 2010
Heliyon, Feb 1, 2021
Tobacco products are widely consumed around the world in smoking and smokeless tobacco (SLT) form... more Tobacco products are widely consumed around the world in smoking and smokeless tobacco (SLT) forms. Analysis of smokeless tobacco consumption suggested that the effects of nicotine and tobacco-specific N-nitrosamines, the main ingredients of smokeless tobacco are attractive to study because its consumption often results in biochemical changes of plasma parameters and markers of oxidative stress development. Smokeless tobacco users generally consume the most commonly available SLT products like khaleja brand of gutkha and mahak chaini brand of khaini 3-5 times per day. We found a significant increase in plasma glucose levels, total cholesterol, triglycerides, and a significant decrease in high-density lipoprotein (HDL) cholesterol indicative of atherosclerosis risk. We also found that the plasma peroxynitrites (ONOO À), nitric oxide (NO), lipid peroxidation (LPO), and protein carbonyls (PCO) levels were significantly elevated. Plasma nicotine and cotinine levels were significantly elevated in study subjects, suggesting that nicotine could be responsible for the oxidative and nitrosative stress indirectly inducing cardiovascular risk. There was a strong correlation of nicotine with reactive oxygen species (ROS), reactive nitrogen species (RNS), cholesterol, and creatinine in exposed smokeless tobacco (gutkha) consumers. These data demonstrate SLT users are at high cardiovascular risk due to nicotine-induced free radicals and oxidative damage.
Asian Pacific Journal of Cancer Prevention, Dec 1, 2019
campaigns about smokeless tobacco products results in the decrease of 34.1% of consumers was reve... more campaigns about smokeless tobacco products results in the decrease of 34.1% of consumers was revealed by Global Adult Tobacco Survey-2016-17 in the India (Shah et al., 2018). The total 356 million people are the habitual users of smokeless tobacco across the globe (Mehrotra et al., 2019). The greater satisfaction and psychological reward was highly observed in regular snus users compared to occasional users (Zandonai et al., 2018). The state wide tobacco control and prevention efforts that address the different types of smokeless tobacco products consumption among adults (Hu et al., 2019).
The main objective of the present investigation was to design matrix tablets of Diclofenac sodium... more The main objective of the present investigation was to design matrix tablets of Diclofenac sodium using Hibiscus rosa-sinensis leaves mucilage and to study its release retardant activity in prepared sustained release formulations. Hibiscus rosa-sinensis leaves were evaluated for physicochemical properties. Different matrix tablets of Diclofenac sodium Hibiscus rosa-sinensis leaves mucilage were formulated. The matrix tablets found to have better uniformity of weight, hardness, friability and drug content with low deviated values. The swelling behavior, release rate characteristics and the in-vitro dissolution study proved that the dried Hibiscus rosa-sinensis leaves mucilage can be used as a matrix forming material for preparing sustained release matrix tablets. The kinetics of drug release from selected DHR-5 formulation followed zero order. It was concluded that Hibiscus rosa-sinensis leaves mucilage can be used as an effective matrix forming polymer, to sustain the release of Diclofenac sodium from the formulation.
Omics A Journal of Integrative Biology, Nov 1, 2013
Nature has been a provenance of medicinal agents for thousands of years. Resveratrol (RESL) is a ... more Nature has been a provenance of medicinal agents for thousands of years. Resveratrol (RESL) is a naturally occurring polyphenolic compound in food stuffs such as peanuts, seeds, berries, grapes, and beverages (red wine). RESL has received significant attention due to a plethora of in vitro and in vivo reports on its cancer chemopreventive and therapeutic properties. In the present study, diacetate RESL derivative (RESL43) was synthesized. The RESL43 displayed potent cytotoxicity and triggered apoptosis in U937 cells as evidenced by poly (ADP-ribose) polymerase (PARP) cleavage, DNA fragmentation, morphological changes, and activation of FasR and FasL genes. The electrophoretic mobility shift assay revealed the suppression NFkB activity in U937 cells after treatment with RESL43 in corroboration with the deactivation of NFkB dependent genes such as IL-8, TNFR, and TNFa. Furthermore, molecular docking and dynamics studies have shown that RESL and RESL43 might exert their inhibitory activity on NFkB by altering the intramolecular binding abilities between DNA and NFkB. Taken together, RESL43 can have greater putative activity than parental RESL in a context of cancer chemoprevention and therapeutics. We suggest that the diacetate resveratrol derivative RESL43 warrants further evaluation in preclinical and clinical bridging studies in the near future.
Bioorganic & Medicinal Chemistry Letters, Nov 1, 2012
A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives were synthesi... more A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives were synthesized via converting the readily available 4-hydroxy coumarin to the corresponding ethyl 2-(2-oxo-2H-chromen-4-yloxy)propanoate followed by hydrolysis and then reacting with different substituted amines. The molecular structures of two representative compounds, that is, 3 and 5l were confirmed by single crystal X-ray diffraction study. All the compounds synthesized were evaluated for their cyclooxygenase (COX) inhibiting properties in vitro. The compound 5i showed balanced selectivity towards COX-2 over COX-1 inhibition and good docking scores when docked into the COX-2 protein.
Bioorganic & Medicinal Chemistry, 2012
A facile and catalyst free synthesis of 6H-1-benzopyrano[4,3-b]quinolin-6-ones has been accomplis... more A facile and catalyst free synthesis of 6H-1-benzopyrano[4,3-b]quinolin-6-ones has been accomplished via the reaction of 4-chloro-2-oxo-2H-chromene-3-carbaldehyde with various aromatic amines in the presence of ultrasound. Some of these compounds were converted to the corresponding 2-(3-(hydroxymethyl)quinolin-2-yl)phenols and further structure elaboration of a representative quinoline derivative is presented. Molecular structure of two representative compounds was confirmed by single crystal X-ray diffraction study. Many of these compounds were evaluated for their anti-proliferative properties in vitro against four cancer cell lines and several compounds were found to be active. Further in vitro studies indicated that inhibition of sirtuins could be the possible mechanism of action of these molecules.
Biomedicine & Pharmacotherapy, Dec 1, 2018
The use of phytochemicals in control of human diseases have been considerable public and scientif... more The use of phytochemicals in control of human diseases have been considerable public and scientific interest in current days. Syringic acid (SA), a phenolic compound often found in fruits and vegetables and which is synthesized via shikimic acid pathway in plants. It shows a wide range of therapeutic applications in prevention of diabetes, CVDs, cancer, cerebral ischemia; as well as it possess anti-oxidant, antimicrobial, anti-inflammatory, antiendotoxic, neuro and hepatoprotective activities. It has an effective free radical scavenger and alleviates the oxidative stress markers. The therapeutic property of SA is attributed by the presence of methoxy groups onto the aromatic ring at positions 3 and 5. The strong antioxidant activity of SA may confer its beneficial effects for human health. SA has the potential to modulate enzyme activity, protein dynamics and diverse transcription factors involved in diabetes, inflammation, cancer and angiogenesis. In vivo experimental data and histopathological studies on SA activity has delineated its possible therapeutic mechanisms. Besides usage in biomedical field, SA has greater industrial applications in bioremediation, photocatalytic ozonation, and laccase based catalysis. The present review deals about SA natural sources, biosynthesis, bioavailability, biomedical applications (in vivo and in vito. The review addresses basic information about molecular mechanisms, therapeutic and industrial potential of SA.
Bioinformation, 2006
Lysyl tRNA synthetases facilitate amino acylation and play a crucial role in the essential cellul... more Lysyl tRNA synthetases facilitate amino acylation and play a crucial role in the essential cellular process of translation. They are grouped into two distinct classes (class I and class II). Class I lysyl tRNA synthetase is considered as a drug target for syphilis caused by Treponema pallidum. Comparative genome analysis shows the absence of its sequence homolog in eukaryotes. The structure of class I lysyl tRNA synthetase from Treponema pallidum is unknown and the difficulties in the in vitro culturing of Treponema makes it non-trivial. We used the structural template of class I lysyl tRNA synthetase from the archaea Pyrococcus horikoshii for modeling the Treponema pallidum lysyl tRNA synthetase structure. Thus, we propose the usefulness of the modeled class I lysyl tRNA synthetase for the design of suitable inhibitors towards the treatment of syphilis.
International Journal of Applied Research in Natural Products, Mar 15, 2011
Bioorganic & Medicinal Chemistry Letters, Mar 1, 2012
Molecular iodine facilitated the reaction of 5,5-dimethyl-1,3-cyclohexanedione with aromatic alde... more Molecular iodine facilitated the reaction of 5,5-dimethyl-1,3-cyclohexanedione with aromatic aldehydes in iso-propanol affording a variety of 1,8-dioxo-octahydroxanthenes in high yields. Most of the compounds synthesized showed good anti-proliferative properties in vitro against three cancer cell lines and 9-(2-hydroxyphenyl)-3,3,6,6-tetramethyl-3,4,5,6,7,9-hexahydro-1H-xanthene-1,8(2H)-dione possessing a 2-hydroxy phenyl group at C-9 position was found to be promising. Further structure elaboration of the same compound and the crystal structure analysis and hydrogen bonding patterns of another compound that is, 9-(4-methoxyphenyl)-3,3,6,6-tetramethyl-3,4,5,6,7,9-hexahydro-1H-xanthene-1,8 (2H)-dione prepared by using this methodology is presented.
Journal of Pharmacy Research, 2010
Toxicology Reports, 2020
This is a PDF file of an article that has undergone enhancements after acceptance, such as the ad... more This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.
Journal of Analytical & Pharmaceutical Research, 2018
Smokeless tobacco may able to induce microalbuminuria. The present study investigates the relatio... more Smokeless tobacco may able to induce microalbuminuria. The present study investigates the relation between nicotine and cotinine with renal function in gutkha and khaini users. Methods: The levels of nicotine and cotinine were estimated by HPLC methods and other urine variables were detected by spectrophotometric methods. Current smokeless tobacco users have shown that significantly elevated levels of nicotine, cotinine, and epinephrine excretion in the urine than non-tobacco users. Renal function was assessed by glomerular filtration rate (GFR), levels of urea, and creatinine. Among the kidney function measures that we examined, microalbuminuria, decreased glomerular filtration rate, and creatinine clearance were found associated with gutkha and khaini users. Significantly decreased proteinuria, urea and increased levels of uric acid and creatinine excretion with the concomitant increase in plasma total proteins, urea, and decreased uric acid levels were observed in the group I and group II users compared to group III users. The products of smokeless tobacco are regarded as good predictors of assessing the free radical levels in the cells. The active markers of nitroxidative stress have been elevated progressively with the uptake of nicotine and exposure. The nicotine and cotinine were significantly positive correlated with renal markers (creatinine, urea, and GFR), nitric oxide, malondialdehyde, and epinephrine. Increased excretion of nicotine and epinephrine indicated that the renal related complications may occur. The smokeless tobacco products were significantly and directly proportional to the levels of kidney dysfunction.
Journal of Drug Delivery and Therapeutics, 2012
In present study, an attempt has been made to evaluate the effect of natural gums on the release ... more In present study, an attempt has been made to evaluate the effect of natural gums on the release profile of drug from matrix system for once daily sustained release tablets formulations. Aceclofenac NSAIDs was used as a model drug to evaluate it release characteristics from different matrices. Matrix tablets of Aceclofenac were prepared by direct compression process using natural gums (xanthan gum and karaya gum) in different ratios drug: gum ratios of FX, FK and FXK (FX and FK in 1:1 ratios). The tablets were evaluated for physical characteristic like hardness, weight variation, friability, swelling index and drug content, in-vitro release of drug was performed in Phosphate buffer pH 7.4 for 24 hours. All the physical characteristic of fabricated tablet was within acceptable limits. The release of Aceclofenac from a gelatinous swollen mass, which controls the diffusion of drug molecules through the polymeric materials in to aqueous medium. The FXK matrices show prices controlled release than FX and FK matrices because of burst effect and fast release in case of FX and FK matrices respectively and there was no chemical interaction between drug and polymers in FXK formulation as confirmed by FTIR studies. The release mechanism was explained with zero order, first order, higuchi and korsmeyer equations via swelling and non fickian diffusion mechanism. The FXK matrices leads to more prices result than FX and FK alone by utilization of synergistic interaction between two biopolymers and uniformity in the hydration layer in dissolution media.
Proper cell cycle progression is critical for maintaining genomic stability. Mitosis is particula... more Proper cell cycle progression is critical for maintaining genomic stability. Mitosis is particularly tightly regulated as deregulated mitosis would lead to improper segregation of chromosomes. Checkpoints including G2/M checkpoint, kinetochore and spindle checkpoint have therefore evolved to ensure proper onset of mitosis and correct
PubMed, Jul 1, 2011
The main aim of present investigation was to develop sustained release matrix tablets of Gliclazi... more The main aim of present investigation was to develop sustained release matrix tablets of Gliclazide using fruit mucilage from the plant Ficus glomerata. Varying ratios of drug and polymer viz. 1:0.25, 1:0.5, 1:0.75, 1:1.0 and 1:1.25 were selected for the study. The flow properties of powdered mucilage and physical properties of matrix tablets were performed. The swelling behavior and release rate characteristics were studied. The in vitro drug release data was analyzed by zero order, first order, Higuchi plot, Peppas plot and Hixon-Crowell Models. It was observed that as the proportion of mucilage increased the release of drug from the matrix tablets was retarded. Stability studies were conducted at 40±2ºC and RH 75±5% for 3 months indicates that Gliclazide was stable in the matrix tablets. The Differential Scanning Calorimetric (DSC) and Fourier Transform Infrared (FTIR) study revealed that there was no negative chemical interaction between drug and the mucilage used. From the dissolution study, it was concluded that dried Ficus glomerata mucilage can be used as an excipient for making sustained release matrix tablets.
Journal of Computational Biology and Bioinformatics Research, Jan 31, 2011
The structure of thrombin protein Oncorhynchus mykiss had not yet been resolved by NMR or X-ray d... more The structure of thrombin protein Oncorhynchus mykiss had not yet been resolved by NMR or X-ray diffraction method. In the present work, we have modeled the structure of protein using Modeller 9v1, taking human thrombin protein as the template. Furthermore, the antithrombin protein was docked with the best model generated by R-dock and Z-dock module of INSIGHT II and the nine potential amino acids involved in anchoring of antithrombin with thrombin were identified as: Leu3,
Journal of Biomolecular Structure & Dynamics, Feb 20, 2017
Pseudomonas aeruginosa (P.aeruginosa) is an opportunistic microorganism causing diseases both in ... more Pseudomonas aeruginosa (P.aeruginosa) is an opportunistic microorganism causing diseases both in animals and humans. In case of human pathology, the role of P.aeruginosa is one of the major concerns in intensive care septicemia. Presently the drug resistance strains of P.aeruginosa are arising mainly by developing multiple mechanisms due to its natural and acquired resistance to many of the antimicrobial agents commonly used in clinical practice. As a result, there is a direneed to invent new drugs so that they may restrict the outbreak of multidrug resistant strains. Virtual high-throughput insilico screening, which helps to identify the chemical ligands that bind to the enzymes, is an important tool in drug discovery and the drugs discovered in this way are clinically tested. In this study, Methyl isocitrateLyase (MICL), which is essential for the survival of the bacterium and which doesn't show any similarity with the humans, was selected to evaluate the functions of high-affinity inhibitors (PPI-analogs) that are identified using the virtual screening approach. By adopting the computational analysis tools structural, functional and inhibitor interactions of MICL against P.aeruginosa were identified. The PPIA-32 is found to be the best binding interactions with MICL. PPIA-32 reduces the binding affinity for substrate to residues required for MICL enzyme activity and also RMSD simulations shows the most stable nature of PPA32-MICL(complex) than that of MICL alone, thereby effectively inhibiting the growth of virulent P.aeruginosa. To our suprise the same phenomenon is also identified with other Gram negative bacteria like E. coli,Klebsiella pneumonia, Salmonella typhi.
The main objective of the present study was to develop matrix-moderated transdermal systems of Di... more The main objective of the present study was to develop matrix-moderated transdermal systems of Diltiazem HCl using various proportions of Ficus reticuleta fruit mucilage. Physical evaluation was performed such as moisture content, moisture uptake, tensile strength, flatness and folding endurance. In-vitro penetration studies were performed in a Keshary-Chien diffusion cell. The matrix-type transdermal systems were prepared using Diltiazem HCl with Ficus reticuleta fruit mucilage by the solvent evaporation technique. The interactions between Diltiazem HCl and Ficus reticuleta fruit mucilage were performed. The transdermal patches were subjected to various physicochemical parameters viz. mechanical properties, permeation studies and skin irritation studies. The prepared patches possessed satisfactory pre-formulary and formulary characteristics. In vitro permeation studies were performed using a Keshary-Chien diffusion cell across hairless Albino rat skin. The non-ionic surfactants Span 80, Glycerin, Propylene glycol in the formulation played a role as permeability enhancer. The patches were seemingly free of potentially hazardous skin irritation. The experimental results shows that the release of drug from the patch delayed in controlled manner as the proportion of Ficus reticuleta increased. It was concluded that Diltiazem HCl can be developed as a transdermal patches with Ficus reticuleta fruit mucilage
Journal of Pharmacy Research, 2010
Heliyon, Feb 1, 2021
Tobacco products are widely consumed around the world in smoking and smokeless tobacco (SLT) form... more Tobacco products are widely consumed around the world in smoking and smokeless tobacco (SLT) forms. Analysis of smokeless tobacco consumption suggested that the effects of nicotine and tobacco-specific N-nitrosamines, the main ingredients of smokeless tobacco are attractive to study because its consumption often results in biochemical changes of plasma parameters and markers of oxidative stress development. Smokeless tobacco users generally consume the most commonly available SLT products like khaleja brand of gutkha and mahak chaini brand of khaini 3-5 times per day. We found a significant increase in plasma glucose levels, total cholesterol, triglycerides, and a significant decrease in high-density lipoprotein (HDL) cholesterol indicative of atherosclerosis risk. We also found that the plasma peroxynitrites (ONOO À), nitric oxide (NO), lipid peroxidation (LPO), and protein carbonyls (PCO) levels were significantly elevated. Plasma nicotine and cotinine levels were significantly elevated in study subjects, suggesting that nicotine could be responsible for the oxidative and nitrosative stress indirectly inducing cardiovascular risk. There was a strong correlation of nicotine with reactive oxygen species (ROS), reactive nitrogen species (RNS), cholesterol, and creatinine in exposed smokeless tobacco (gutkha) consumers. These data demonstrate SLT users are at high cardiovascular risk due to nicotine-induced free radicals and oxidative damage.
Asian Pacific Journal of Cancer Prevention, Dec 1, 2019
campaigns about smokeless tobacco products results in the decrease of 34.1% of consumers was reve... more campaigns about smokeless tobacco products results in the decrease of 34.1% of consumers was revealed by Global Adult Tobacco Survey-2016-17 in the India (Shah et al., 2018). The total 356 million people are the habitual users of smokeless tobacco across the globe (Mehrotra et al., 2019). The greater satisfaction and psychological reward was highly observed in regular snus users compared to occasional users (Zandonai et al., 2018). The state wide tobacco control and prevention efforts that address the different types of smokeless tobacco products consumption among adults (Hu et al., 2019).
The main objective of the present investigation was to design matrix tablets of Diclofenac sodium... more The main objective of the present investigation was to design matrix tablets of Diclofenac sodium using Hibiscus rosa-sinensis leaves mucilage and to study its release retardant activity in prepared sustained release formulations. Hibiscus rosa-sinensis leaves were evaluated for physicochemical properties. Different matrix tablets of Diclofenac sodium Hibiscus rosa-sinensis leaves mucilage were formulated. The matrix tablets found to have better uniformity of weight, hardness, friability and drug content with low deviated values. The swelling behavior, release rate characteristics and the in-vitro dissolution study proved that the dried Hibiscus rosa-sinensis leaves mucilage can be used as a matrix forming material for preparing sustained release matrix tablets. The kinetics of drug release from selected DHR-5 formulation followed zero order. It was concluded that Hibiscus rosa-sinensis leaves mucilage can be used as an effective matrix forming polymer, to sustain the release of Diclofenac sodium from the formulation.
Omics A Journal of Integrative Biology, Nov 1, 2013
Nature has been a provenance of medicinal agents for thousands of years. Resveratrol (RESL) is a ... more Nature has been a provenance of medicinal agents for thousands of years. Resveratrol (RESL) is a naturally occurring polyphenolic compound in food stuffs such as peanuts, seeds, berries, grapes, and beverages (red wine). RESL has received significant attention due to a plethora of in vitro and in vivo reports on its cancer chemopreventive and therapeutic properties. In the present study, diacetate RESL derivative (RESL43) was synthesized. The RESL43 displayed potent cytotoxicity and triggered apoptosis in U937 cells as evidenced by poly (ADP-ribose) polymerase (PARP) cleavage, DNA fragmentation, morphological changes, and activation of FasR and FasL genes. The electrophoretic mobility shift assay revealed the suppression NFkB activity in U937 cells after treatment with RESL43 in corroboration with the deactivation of NFkB dependent genes such as IL-8, TNFR, and TNFa. Furthermore, molecular docking and dynamics studies have shown that RESL and RESL43 might exert their inhibitory activity on NFkB by altering the intramolecular binding abilities between DNA and NFkB. Taken together, RESL43 can have greater putative activity than parental RESL in a context of cancer chemoprevention and therapeutics. We suggest that the diacetate resveratrol derivative RESL43 warrants further evaluation in preclinical and clinical bridging studies in the near future.
Bioorganic & Medicinal Chemistry Letters, Nov 1, 2012
A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives were synthesi... more A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives were synthesized via converting the readily available 4-hydroxy coumarin to the corresponding ethyl 2-(2-oxo-2H-chromen-4-yloxy)propanoate followed by hydrolysis and then reacting with different substituted amines. The molecular structures of two representative compounds, that is, 3 and 5l were confirmed by single crystal X-ray diffraction study. All the compounds synthesized were evaluated for their cyclooxygenase (COX) inhibiting properties in vitro. The compound 5i showed balanced selectivity towards COX-2 over COX-1 inhibition and good docking scores when docked into the COX-2 protein.
Bioorganic & Medicinal Chemistry, 2012
A facile and catalyst free synthesis of 6H-1-benzopyrano[4,3-b]quinolin-6-ones has been accomplis... more A facile and catalyst free synthesis of 6H-1-benzopyrano[4,3-b]quinolin-6-ones has been accomplished via the reaction of 4-chloro-2-oxo-2H-chromene-3-carbaldehyde with various aromatic amines in the presence of ultrasound. Some of these compounds were converted to the corresponding 2-(3-(hydroxymethyl)quinolin-2-yl)phenols and further structure elaboration of a representative quinoline derivative is presented. Molecular structure of two representative compounds was confirmed by single crystal X-ray diffraction study. Many of these compounds were evaluated for their anti-proliferative properties in vitro against four cancer cell lines and several compounds were found to be active. Further in vitro studies indicated that inhibition of sirtuins could be the possible mechanism of action of these molecules.
Biomedicine & Pharmacotherapy, Dec 1, 2018
The use of phytochemicals in control of human diseases have been considerable public and scientif... more The use of phytochemicals in control of human diseases have been considerable public and scientific interest in current days. Syringic acid (SA), a phenolic compound often found in fruits and vegetables and which is synthesized via shikimic acid pathway in plants. It shows a wide range of therapeutic applications in prevention of diabetes, CVDs, cancer, cerebral ischemia; as well as it possess anti-oxidant, antimicrobial, anti-inflammatory, antiendotoxic, neuro and hepatoprotective activities. It has an effective free radical scavenger and alleviates the oxidative stress markers. The therapeutic property of SA is attributed by the presence of methoxy groups onto the aromatic ring at positions 3 and 5. The strong antioxidant activity of SA may confer its beneficial effects for human health. SA has the potential to modulate enzyme activity, protein dynamics and diverse transcription factors involved in diabetes, inflammation, cancer and angiogenesis. In vivo experimental data and histopathological studies on SA activity has delineated its possible therapeutic mechanisms. Besides usage in biomedical field, SA has greater industrial applications in bioremediation, photocatalytic ozonation, and laccase based catalysis. The present review deals about SA natural sources, biosynthesis, bioavailability, biomedical applications (in vivo and in vito. The review addresses basic information about molecular mechanisms, therapeutic and industrial potential of SA.
Bioinformation, 2006
Lysyl tRNA synthetases facilitate amino acylation and play a crucial role in the essential cellul... more Lysyl tRNA synthetases facilitate amino acylation and play a crucial role in the essential cellular process of translation. They are grouped into two distinct classes (class I and class II). Class I lysyl tRNA synthetase is considered as a drug target for syphilis caused by Treponema pallidum. Comparative genome analysis shows the absence of its sequence homolog in eukaryotes. The structure of class I lysyl tRNA synthetase from Treponema pallidum is unknown and the difficulties in the in vitro culturing of Treponema makes it non-trivial. We used the structural template of class I lysyl tRNA synthetase from the archaea Pyrococcus horikoshii for modeling the Treponema pallidum lysyl tRNA synthetase structure. Thus, we propose the usefulness of the modeled class I lysyl tRNA synthetase for the design of suitable inhibitors towards the treatment of syphilis.
International Journal of Applied Research in Natural Products, Mar 15, 2011
Bioorganic & Medicinal Chemistry Letters, Mar 1, 2012
Molecular iodine facilitated the reaction of 5,5-dimethyl-1,3-cyclohexanedione with aromatic alde... more Molecular iodine facilitated the reaction of 5,5-dimethyl-1,3-cyclohexanedione with aromatic aldehydes in iso-propanol affording a variety of 1,8-dioxo-octahydroxanthenes in high yields. Most of the compounds synthesized showed good anti-proliferative properties in vitro against three cancer cell lines and 9-(2-hydroxyphenyl)-3,3,6,6-tetramethyl-3,4,5,6,7,9-hexahydro-1H-xanthene-1,8(2H)-dione possessing a 2-hydroxy phenyl group at C-9 position was found to be promising. Further structure elaboration of the same compound and the crystal structure analysis and hydrogen bonding patterns of another compound that is, 9-(4-methoxyphenyl)-3,3,6,6-tetramethyl-3,4,5,6,7,9-hexahydro-1H-xanthene-1,8 (2H)-dione prepared by using this methodology is presented.
Journal of Pharmacy Research, 2010
Toxicology Reports, 2020
This is a PDF file of an article that has undergone enhancements after acceptance, such as the ad... more This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.
Journal of Analytical & Pharmaceutical Research, 2018
Smokeless tobacco may able to induce microalbuminuria. The present study investigates the relatio... more Smokeless tobacco may able to induce microalbuminuria. The present study investigates the relation between nicotine and cotinine with renal function in gutkha and khaini users. Methods: The levels of nicotine and cotinine were estimated by HPLC methods and other urine variables were detected by spectrophotometric methods. Current smokeless tobacco users have shown that significantly elevated levels of nicotine, cotinine, and epinephrine excretion in the urine than non-tobacco users. Renal function was assessed by glomerular filtration rate (GFR), levels of urea, and creatinine. Among the kidney function measures that we examined, microalbuminuria, decreased glomerular filtration rate, and creatinine clearance were found associated with gutkha and khaini users. Significantly decreased proteinuria, urea and increased levels of uric acid and creatinine excretion with the concomitant increase in plasma total proteins, urea, and decreased uric acid levels were observed in the group I and group II users compared to group III users. The products of smokeless tobacco are regarded as good predictors of assessing the free radical levels in the cells. The active markers of nitroxidative stress have been elevated progressively with the uptake of nicotine and exposure. The nicotine and cotinine were significantly positive correlated with renal markers (creatinine, urea, and GFR), nitric oxide, malondialdehyde, and epinephrine. Increased excretion of nicotine and epinephrine indicated that the renal related complications may occur. The smokeless tobacco products were significantly and directly proportional to the levels of kidney dysfunction.
Journal of Drug Delivery and Therapeutics, 2012
In present study, an attempt has been made to evaluate the effect of natural gums on the release ... more In present study, an attempt has been made to evaluate the effect of natural gums on the release profile of drug from matrix system for once daily sustained release tablets formulations. Aceclofenac NSAIDs was used as a model drug to evaluate it release characteristics from different matrices. Matrix tablets of Aceclofenac were prepared by direct compression process using natural gums (xanthan gum and karaya gum) in different ratios drug: gum ratios of FX, FK and FXK (FX and FK in 1:1 ratios). The tablets were evaluated for physical characteristic like hardness, weight variation, friability, swelling index and drug content, in-vitro release of drug was performed in Phosphate buffer pH 7.4 for 24 hours. All the physical characteristic of fabricated tablet was within acceptable limits. The release of Aceclofenac from a gelatinous swollen mass, which controls the diffusion of drug molecules through the polymeric materials in to aqueous medium. The FXK matrices show prices controlled release than FX and FK matrices because of burst effect and fast release in case of FX and FK matrices respectively and there was no chemical interaction between drug and polymers in FXK formulation as confirmed by FTIR studies. The release mechanism was explained with zero order, first order, higuchi and korsmeyer equations via swelling and non fickian diffusion mechanism. The FXK matrices leads to more prices result than FX and FK alone by utilization of synergistic interaction between two biopolymers and uniformity in the hydration layer in dissolution media.