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Abstract A large population of immune compromised people is susceptible to opportunistic mycoses. Infections caused by Candida species, particularly Candida albicans, is a major cause of morbidity and mortality among the patients. Biofilm... more
Abstract A large population of immune compromised people is susceptible to opportunistic mycoses. Infections caused by Candida species, particularly Candida albicans, is a major cause of morbidity and mortality among the patients. Biofilm related infections of C. albicans pose a challenge to successful antifungal treatment because of their resistance to available drugs. Plants and plant derived products represent a rich platform for the discovery of pharmaceutically important molecules. The study evaluated activity of methanol and petroleum ether extracts of fruits of Helicteres isora Linn. against planktonic and biofilm growth of Candida albicans. Methanol extract of H. isora L. (MEHI) showed complete prevention of planktonic growth at 2 mg/ml, while petroleum ether extract (PEEHI) had no effect up to 4 mg/ml concentration. Decrease in biofilm formation was analyzed in presence of 1 mg/ml MEHI, and 2 mg/ml concentration of it prevented biofilm formation significantly (p< 0.05). In comparison, PEEHI exhibited negligible activity against biofilm. Results demonstrate anti-biofilm activity of methanol extract of H. isora L. fruit, in C. albicans.
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Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the... more
Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately ...
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It has been established that sulfoxide with sulfones have distinct pharmacological effects. Commodity compounds like sulfoxide and sulfones find widespread use in many chemical disciplines. This is why organic chemists find the synthesis... more
It has been established that sulfoxide with sulfones have distinct pharmacological effects. Commodity compounds like sulfoxide and sulfones find widespread use in many chemical disciplines. This is why organic chemists find the synthesis of sulfoxide and sulfones so interesting. In the process of oxidation, sulphides can transform into sulfoxides or sulfones. Comprehensive oxidation to the sulfones is significantly simpler than mild oxidation to the sulfoxide, but both can be achieved by the use of highly selective technologies.
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Background Most of the edible portions like peel and skin of some fruits is discarded while consuming it, though they are rich in several health beneficial phytochemicals or nutrients. Many reports from literature are about fruit pulp of... more
Background Most of the edible portions like peel and skin of some fruits is discarded while consuming it, though they are rich in several health beneficial phytochemicals or nutrients. Many reports from literature are about fruit pulp of (Sapota) Manilkara zapota (L) P. Royen having high radical scavenging and antioxidant potential, but the studies relating to peel extracts are scanty. Regardless of its commendable phytoconstituents which could have free radical scavenging potential, this fruit peel is as yet still needed to be assessed for in vitro antidiabetic prospects. Hence, the present study aims at evaluating in vitro free radical scavenging and α-glucosidase enzyme hindrance abilities of this fruit peel. Results With a maximum considerable % extractive yield (18.90%) in 70% ethanol, this study has demonstrated that 70% ethanolic extract of Manilkara Zapota (L.) P. Royen Fruit Peel (MZFP) has the highest in vitro free radical scavenging potential as compared to extracts of ot...
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Background A perusal of the literature suggested that Manilkara zapota (L.) P. Royen stem bark (MZSB) is enriched with several bioactive phytoconstituents but had not been yet screened for its in vitro and in vivo antidiabetic potentials.... more
Background A perusal of the literature suggested that Manilkara zapota (L.) P. Royen stem bark (MZSB) is enriched with several bioactive phytoconstituents but had not been yet screened for its in vitro and in vivo antidiabetic potentials. Thus, the present study aimed to investigate the effects of 70% ethanolic extract of Manilkara zapota (L) P. Royen stem bark (EMZSB) in DPPH- and H2O2-scavenging assay, in vitro α-glucosidase inhibition assay, ameliorating diabetes and its complications in alloxan-induced diabetes in Wistar rats. Results With a maximum extractive yield of 9.16% w/w, EMZSB has shown the presence of various phytochemicals like flavonoids, phenolic compounds, tannins, anthraquinone glycosides, steroids, terpenoids, and alkaloids. EMZSB has elucidated a considerable in vitro free radical scavenging potential by DPPH and H2O2 assays when compared with absolute ethanolic extract of Manilkara zapota (L) P. Royen stem bark (AEMZSB), while ascorbic acid was taken as the sta...
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This study aims to evaluate the effects of Manilkara zapota (L) P. Royen fruit peel extract (EMZFP) and its fractions in ameliorating diabetes and its complications in alloxan and STZ-NA induced diabetes in Wistar rats. Antidiabetic... more
This study aims to evaluate the effects of Manilkara zapota (L) P. Royen fruit peel extract (EMZFP) and its fractions in ameliorating diabetes and its complications in alloxan and STZ-NA induced diabetes in Wistar rats. Antidiabetic effects of EMZFP were assessed in alloxan (150 mg kg-1) induced diabetes in differently grouped rats (n=6). Diabetic rats were treated with EMZFP 150, 300, and 600 mg kg-1 while, glimepiride (0.09 mg kg-1) was used as a reference standard. Treated animals were assessed for various biological parameters i.e. blood glucose, serum lipids, nephroprotective markers, cardiovascular risk indices, liver glycogen, neuropathy, body weight, and histopathology of kidneys. However, for evaluating antidiabetic effects of fractions (chloroform, acetone, ethyl acetate, and remaining ethanol fraction) of EMZFP, diabetes was induced by streptozotocin (60 mg kg-1)–nicotinamide (120 mg kg-1/ml) in differently grouped male rats (n=6). Diabetic rats were treated with EMZFP fractions 200 mg kg-1 however; glibenclamide (10 mg kg-1) was a reference standard and evaluated for blood glucose, serum lipids, cardiovascular risk indices, and diabetic neuropathy. EMZFP 300 and 600 mg kg-1/day demonstrated significant antihyperglycemic effects with augmentation in glycogen content, perfection in serum lipid profile, cardiovascular risk indices, body weight enhancement, nephroprotective effects, beneficial in peripheral neuropathy, and histopathological evidence of reversal of glomerulosclerosis. EMZFP-Et and EMZFP-EA fractions depicted a significant improvement in blood glucose, serum lipid profile, cardiovascular risk indices, and peripheral neuropathy. EMZFP and its Et and EA fractions ameliorated diabetes and its complications by improving glycemic control and associated biochemical alteration. • Manilkara Zapota (L.) P. Royen fruit peel 70% ethanolic extract exert antidiabetic effects • EMZFP significantly ameliorated diabetic biochemical parameters and its complications. • EMZFP-Et and EMZFP-EA fractions exert potential antihyperglycemic, hypolipidemic effects and significantly improved cardiovascular risk indices, and peripheral neuropathy. • Studied MZFP can be used as promising natural herbal source of antidiabetic principles.
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Background Luffa cylindrica (L.) is a commonly used vegetable in different parts of Asia. Its fruits are generally used as a vegetable, but pharmacological activities of the leaves were unrevealed. The study evaluated the... more
Background Luffa cylindrica (L.) is a commonly used vegetable in different parts of Asia. Its fruits are generally used as a vegetable, but pharmacological activities of the leaves were unrevealed. The study evaluated the antihyperlipidemic activity and in vitro antioxidant potential of methanolic extract of Luffa cylindrica (L.) leaves (MELCL). The antihyperlipidemic potential was investigated in Triton X-100-induced hyperlipidemic rats. Animals were pre-treated with Triton X-100 (400 mg/kg). The Triton X-100-treated animals were then treated with MELCL at the doses of 100 and 200 mg/kg using 5% CMC, as a vehicle, per oral (p.o) for 7 days. Antioxidant activity was studied by examining the DPPH and hydrogen peroxide radical scavenging potential of the extract. Results The plasma sample of rats was analyzed, and it was found that MELCL shows significant (p
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Worldwide cancer is the leading cause of death; leukocytes within tumors and at the sites of chronic inflammation provided the first indication of a possible link between inflammation and cancer. Inflammation plays a crucial role at... more
Worldwide cancer is the leading cause of death; leukocytes within tumors and at the sites of chronic inflammation provided the first indication of a possible link between inflammation and cancer. Inflammation plays a crucial role at different stages of tumor growth via. transcription factors and inflammatory mediators such as TNF, IL’s, chemokines COX-2, STAT3and NF-κB. Nuclear factor-kappa B (NF-κB) has been one of the most extensively investigated transcription factors for its role in cancers. The NF-κB signaling pathways are vital in the initiation and progression of cancer which can act as a node of pharmacological interference in the management of tumor. However, NF-κB is an essential player in the immune response against various cancer developments; hence inhibition of NF-κB seems to be always important in the treatment of various malignancies. The application of an NF-κB inhibitor may prove useful in anticancer therapy by converting anti-apoptosis effect of NF-κB into apoptot...
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A novel series of N-(substituted pyridine-2-yl)-N-(quinoline-2-yl) malonamide derivatives (AK1-AK24) has been rationally designed, synthesized and biologically screened for in vitro anti HIV activity by using reverse transcriptase assay... more
A novel series of N-(substituted pyridine-2-yl)-N-(quinoline-2-yl) malonamide derivatives (AK1-AK24) has been rationally designed, synthesized and biologically screened for in vitro anti HIV activity by using reverse transcriptase assay kit (Roche). Out of the synthesized compounds, compound AK1, AK2 and AK3 show potent reverse transcriptase (RT) inhibitor activity and compounds AK4 to AK9, AK11, AK12, AK13 and AK14 show RT inhibitory activity comparable with standard rilpivirine. In docking studies, those compounds show higher G-Score which indicates higher percentage of inhibition of reverse transcriptase during in vitro screening. In silico pharmacokinetic studies imply that synthesized derivatives have no CYP450 inhibition, no BBB penetration and good oral absorption. Virtual toxicity studies performed by using Toxtree-v 2.6.6 in various computational animal models show high LD50 values and the compounds are found to be non-carcinogenic.
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Polymer-drug conjugates have demonstrated several advantages over the corresponding parent drugs, including fewer side effects, enhanced therapeutic efficacy, ease of drug administration, and improved patient compliance. Polymer-drug... more
Polymer-drug conjugates have demonstrated several advantages over the corresponding parent drugs, including fewer side effects, enhanced therapeutic efficacy, ease of drug administration, and improved patient compliance. Polymer-drug conjugates are nano-sized hybrid constructs that covalently combine a bioactive agent with a polymer to ensure not only its efficient delivery to the required intracellular compartment but also its availability within a specific period of time. Polymer-drug conjugates such as HMPA Copolymer-Doxorubicin (PK1), HMPA Copolymer-Doxorubicin-Galactosamine (PK2), HMPA CopolymerCamptothecin, HMPA Copolymer-Platinate (AP5346), PEG-Camptothecin (Pegamotecan) and PEG-SN38 (EZN2208) have main role in treatment of a wide variety of human pathologies, from diabetes, heart failure, and brain stroke. Future generation of polymer-drug conjugates will have to meet a number of challenges, including the development of novel polymers with modulated rates of degradation, ver...
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A novel series of substituted 2-Amino-4,6-diarylpyr imidines (DAPY’s)as Non-nucleoside reverse transcri ptase inhibitors (NNRTIs) were designed, synthesized and evaluated for in vitro reverse transcriptase (RT) i nhibition activity. Out... more
A novel series of substituted 2-Amino-4,6-diarylpyr imidines (DAPY’s)as Non-nucleoside reverse transcri ptase inhibitors (NNRTIs) were designed, synthesized and evaluated for in vitro reverse transcriptase (RT) i nhibition activity. Out of the reported compounds, 4a 4i, 4j and 4n showed potent anti-HIV activity as compared to stan dard rilpivirine. The other compounds displayed moderate activity against HIV-1. Binding affinities of the d signed NCEs were studied on reverse transcriptase enzyme using docking studies and showed possible horseshoe confo rmati n as required for the DAPY category of RT inhibitors. A correlation was found between the anti-HIV activity and the electrostatic energy interaction with Lys 101 resid ue.
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Antitubercular drug discovery is a challenging strain in the recent era. Quinazolines are an important chemical compounds having diverse significant biological activities. Three dimensional Quantitative structure-activity relationships (... more
Antitubercular drug discovery is a challenging strain in the recent era. Quinazolines are an important chemical compounds having diverse significant biological activities. Three dimensional Quantitative structure-activity relationships ( 3D QSAR) represent an attempt to correlate three dimensional structural features of compounds with biological activities. The pharmacophore identification and QSAR studies on C-2 and C-4 substituted quinazoline series was carried out by partial least-squares (PLS) method to identify the potential framework of the molecules responsible for the antitubercular activity. The QSAR models were developed considering training and test set approaches further validated for statistical significance and predictive ability by internal and external validation. The results of 3D QSAR model demonstrate the high degree of statistical importance and excellent predictive capability. The hydrogen bond accepter, hydrogen bond donor, positively charged, aromatic carbon, ...
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Calotropis procera (commonly known as Swallow wort) is described in the Ayurvedic literature for the treatment of inflammation and arthritic disorders. Therefore, in the present work, the antiarthritic activity of potential fractions of... more
Calotropis procera (commonly known as Swallow wort) is described in the Ayurvedic literature for the treatment of inflammation and arthritic disorders. Therefore, in the present work, the antiarthritic activity of potential fractions of Swallow wort leaf was evaluated and compared with standards (indomethacin and ibuprofen). This study was designed in Wistar rats for the investigation of antiarthritic activity and acute toxicity of Swallow wort. Arthritis was induced in Wistar rats by injecting 0.1 mL of Freund’s complete adjuvant (FCA) on the 1st and 7th days subcutaneously into the subplantar region of the left hind paw. Evaluation of our experimental findings suggested that antiarthritic activity of methanol fraction of Swallow wort (MFCP) was greater than ethyl acetate fraction of Swallow wort (EAFCP), equal to standard ibuprofen, and slightly lower than standard indomethacin. MFCP significantly reduced paw edema on the 17th, 21st, 24th, and 28th days. It also showed significant...
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Momordica charantia L. is growing in many tropical and subtropical regions; the fruits of bitter melon are also gradually becoming popular for treating diabetes and associated diseases. Over 248 compounds belonging to the lipids,... more
Momordica charantia L. is growing in many tropical and subtropical regions; the fruits of bitter melon are also gradually becoming popular for treating diabetes and associated diseases. Over 248 compounds belonging to the lipids, phenolics and terpenoids class are reported by diverse studies. However, M. charantia L. appears to be an inimitable species that synthesizes a diverse range of natural products in the fruits, leaves, stems and roots. The cucurbitane types of triterpenes exist in the various tissues of the plant in their aglycone as well as glycosylated forms. The bitter melon seems to exert their lipid lowering and antiobesity effects via several mechanisms like PPARs, LXRs, SREBPs, and Sirts mediated fat metabolism in various tissues, prevent adipocyte hypertrophy and visceral fat accumulation. M. charantia L. has been comprehensively studied worldwide for its therapeutic properties to treat a number of diseases like diabetes, dyslipidaemia, obesity, and certain cancers. ...
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In present work, carboxymethylcellulose (CMC) - polyethylene glycol (PEG) hydrogel films were prepared using citric acid as a non-toxic crosslinking agent, for the controlled delivery of model hydrophobic drug (ketoconazole). The carboxyl... more
In present work, carboxymethylcellulose (CMC) - polyethylene glycol (PEG) hydrogel films were prepared using citric acid as a non-toxic crosslinking agent, for the controlled delivery of model hydrophobic drug (ketoconazole). The carboxyl content of the hydrogel films were determined by acid-base titration. The films were characterized by solid state 13C NMR, ATR-FTIR, TGA and DSC, and evaluated for swelling behavior, drug loading, drug release, hemocompatibility, in vitro cytotoxicity and implantation test. An increase in the amount of PEG caused increase in the carboxyl content and swellability of the hydrogel films. The solid state 13C NMR, ATR-FTIR and thermal analysis confirmed the formation of ester crosslinks in between CMC and PEG in the hydrogel films. The release of KTZ was found to be retarded due to presence of grafted PEG in the hydrogel films. The hydrogel films exhibited excellent hemocompatibility and cytocompatibility. Implantation test revealed that the hydrogel films caused minimum inflammation. From the overall results, citric acid crosslinked CMC-PEG hydrogel films were found to be suitable for enhanced loading and controlled release of the poorly soluble drugs.
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The objective of this study was to synthesize and characterize citric acid crosslinked carboxymethyl tamarind gum (CMTG) hydrogels films. The hydrogel films were characterized by Attenuated total reflectance-Fourier transform infrared... more
The objective of this study was to synthesize and characterize citric acid crosslinked carboxymethyl tamarind gum (CMTG) hydrogels films. The hydrogel films were characterized by Attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy, solid state (13)C-nuclear magnetic resonance ((13)C NMR) spectroscopy and differential scanning calorimeter (DSC). The prepared hydrogel films were evaluated for the carboxyl content and swelling ratio. The model drug moxifloxacin hydrochloride was loaded into hydrogels films and drug release was studied at pH 7.4. The hemolysis assay was used to study the biocompatibility of hydrogel films. The results of ATR-FTIR, solid state (13)C NMR and DSC confirmed the formation of ester crosslinks between citric acid and CMTG. The total carboxyl content of hydrogel film was found to be decreased when amount of CMTG was increased. The swelling of hydrogel film was found to be decreased with increase in curing temperature and time. CMTG h...
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ABSTRACT In-vitro anthelmintic activity of methanol and petroleum ether extracts of Helicteres isora fruits were determined by the evaluation of time for paralysis and death (min.) against Indian earthworms Pheretima posthuma. Various... more
ABSTRACT In-vitro anthelmintic activity of methanol and petroleum ether extracts of Helicteres isora fruits were determined by the evaluation of time for paralysis and death (min.) against Indian earthworms Pheretima posthuma. Various concentrations of extracts were tested in the bioassay (10, 20, and 50 mg/ml). Albendazole at concentration 20 mg/ml was included as standard reference while normal saline (0.9 % NaCl) solution as control. Antioxidant activity was determined by 2, 2-diphenyl-1-picryl hydrazyl (DPPH) and Hydrogen peroxide (H2O2) radicals scavenging assays. The both methanol and petroleum ether extracts showed dose dependent anthelmintic activity. The DPPH free radical scavenging activity was obtained with the methanol extract (IC50 42.95 µg/ml), while petroleum ether extract showed less free radical scavenging activity (IC50 89.81 μg/ml) as compared to standard ascorbic acid (IC50 23.75 µg/ml). Hydrogen peroxide decomposition activity of methanol and petroleum ether extracts were showed in a concentration dependent manner with an IC50 36.61 µg/ml and 74.40 µg/ml respectively, while IC50 value for ascorbic acid was 9.64 ìg/ml. Methanol extracts showed potent anthelmintic and antioxidant activity than petroleum ether extracts.
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Research Interests: Chemistry, Organic Chemistry, Escherichia coli, Nitric oxide, Animals, and 15 moreBacteria, Staphylococcus aureus, Drug Design, Pseudomonas aeruginosa, Antibacterial activity, Anti-Bacterial Agents, Rats, Carboxylic Acids, Pseudomonas Aeruginosa, Anti Inflammatory Activity, Bioorganic and medicinal Chemistry, Pyrazoles, Pyrazole, Molecular Structure, and Pharmacology and pharmaceutical sciences(Bacteria, Staphylococcus aureus, Drug Design, Pseudomonas aeruginosa, Antibacterial activity, Anti-Bacterial Agents, Rats, Carboxylic Acids, Pseudomonas Aeruginosa, Anti Inflammatory Activity, Bioorganic and medicinal Chemistry, Pyrazoles, Pyrazole, Molecular Structure, and Pharmacology and pharmaceutical sciences)
(Bacteria, Staphylococcus aureus, Drug Design, Pseudomonas aeruginosa, Antibacterial activity, Anti-Bacterial Agents, Rats, Carboxylic Acids, Pseudomonas Aeruginosa, Anti Inflammatory Activity, Bioorganic and medicinal Chemistry, Pyrazoles, Pyrazole, Molecular Structure, and Pharmacology and pharmaceutical sciences)
Background Biofilms formed by Candida albicans are resistant towards most of the available antifungal drugs. Therefore, infections associated with Candida biofilms are considered as a threat to immunocompromised patients. Combinatorial... more
Background Biofilms formed by Candida albicans are resistant towards most of the available antifungal drugs. Therefore, infections associated with Candida biofilms are considered as a threat to immunocompromised patients. Combinatorial drug therapy may be a good strategy to combat C. albicans biofilms. Methods Combinations of five antifungal drugs- fluconazole (FLC), voriconazole (VOR), caspofungin (CSP), amphotericin B (AmB) and nystatin (NYT) with cyclosporine A (CSA) were tested in vitro against planktonic and biofilm growth of C. albicans. Standard broth micro dilution method was used to study planktonic growth, while biofilms were studied in an in vitro biofilm model. A chequerboard format was used to determine fractional inhibitory concentration indices (FICI) of combination effects. Biofilm growth was analyzed using XTT-metabolic assay. Results MICs of various antifungal drugs for planktonic growth of C. albicans were lowered in combination with CSA by 2 to 16 fold. Activity ...