- Poonam Shukla
- Mavurapu Satyanarayana
- Prem C. Verma
- Jaya Tiwari
- Atma P. Dwivedi
- Rohit Srivastava
- Neha Rehuja
- Swayam P. Srivastava
- Sudeep Gautam
- Akhilesh K. Tamrakar
- Hari N. Kushwaha
- Nagsen Gautam
- Shio K. Singh
- Mukesh Srivastava
- Chandishwar Nath
- Ram Raghubir
- Arvind K. Srivastava
- Ram Pratap
- Dhananjay Mani Tripathi
- Shashi
- Hadi Hasan
- Ganesh K. Singh
- Madhvi Tiwari
- Shashi Dwivedi
- Deependra Kr. Anand
- Rahul Singh
- Shashi
A B C D E F G H I J K L M N O P Q R S T U V W X Y Z All
Dwivedi, Anil K.
- Chalcone-Based Aryloxypropanolamine as a Potential Antidiabetic and Antidyslipidaemic Agent
Authors
1 Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226 031, IN
2 Division of Biochemistry, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226 031, IN
3 Division of Pharmaceutics, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226 031, IN
4 Division of Pharmacokinetics and Pharmaco-Dynamics, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226 031, IN
5 Division of Biometry and Statistics, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226 031, IN
6 Division of Toxicology, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226 031, IN
7 Division of Pharmacology, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226 031, IN
8 Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226 031
Source
Current Science, Vol 112, No 08 (2017), Pagination: 1675-1689Abstract
The hybrid congener 3 derived from hydroxychalcone and pharmacophore oxypropanolamine for adrenergic receptor, along with its enantiomers 9a and 9b were selected from a series of compounds for detailed studies of their antidiabetic profile in sucrose-challenged, low-dosed, streptozotocin-induced diabetic rats and in db/db mice, and antidyslipidaemic profile in high fat diet-induced dyslipidaemic hamsters. The test compounds exhibited significant and consistent antidiabetic and antidyslipidaemic activities in the above models. The pharmacodynamic studies of two metabolites, 10 and 11, were undertaken. Metabolite 10 having greater bioavailability in plasma was synthesized and found to exhibit significant antidiabetic activity. The parent compound together with its active metabolites exhibited significant oral bioavailability, thus establishing compound 3 as a potential lead molecule for further studies.Keywords
Antidiabetic and Antidyslipidaemic Activity, Chalcone, Diabetes Mellitus, Metabolites, Rodents.Full Text
References
- Stone, B. G. and Van Thiel, D. H., Diabetes mellitus and the liver. Semin. Liver Dis., 1985, 5, 8–28.
- Consoli, A., Nurjhan, N., Capani, F. and Gerich, J., Predominant role of gluconeogenesis in increased hepatic glucose production in NIDDM. Diabetes, 1989, 38, 550–557.
- Spirito, P., Bellone, P., Harris, K. M., Bernabo, P. and Maron, B., Magnitude of left ventricular hypertrophy and risk of sudden death in hypertrophic cardiomyopathy. N. Eng. J. Med., 2000, 342, 1778–1785.
- Jaques, W. E., The incidence of portal cirrhosis and fatty metamorphosis in patients dying with diabetes mellitus. N. Engl. J. Med., 1953, 249, 442–445.
- Maedler, K. et al., Glucose- and interleukin-1-beta-induced betacell apoptosis requires Ca2+ influx and extracellular signalregulated kinase (ERK) 1/2 activation and is prevented by a sulfonylurea receptor 1/inwardly rectifying K+ channel 6.2 (SUR/Kir6.2) selective potassium channel opener in human islets. Diabetes, 2004, 53, 1706–1713.
- De Matteis, R., Arch, J. R., Petroni, M. L., Ferrari, D., Cinti, S. and Stock, M. J., Immunohistochemical identification of the β3-adrenoceptor in intact human adipocytes and ventricular myocardium: effect of obesity and treatment with ephedrine and caffeine. Int. J. Obes. Relat. Metab. Disord., 2002, 26, 1442–1450.
- Grujic, D., Susulic, V. S., Harper, M. E., Himms-Hagen, J., Cunningham, B. A., Corkey, B. E. and Lowell, B. B., β3-Adrenergic receptors on white and brown adipocytes mediate β3-selective agonist-induced effects on energy expenditure, insulin secretion, and food intake. A study using transgenic and gene knockout mice. J. Biol. Chem., 1997, 272, 17686–17693.
- Fisher, M. H. et al., A selective human β3-adrenergic receptor agonist increases metabolic rate in rhesus monkeys. J. Clin. Invest., 1998, 101, 2387–2393.
- Weyer, C., Tataranni, P. A., Snitker, S., Danforth, E. and Ravussin, E., Increase in insulin action and fat oxidation after treatment with CL 316,243, a highly selective β3-adrenoceptor agonist in humans. Diabetes, 1998, 47, 1555–1561.
- Yoshida, T., Sakane, N., Wakabayashi, Y., Umekawa, T. and Kondo, M., Anti-obesity and anti-diabetic effects of CL 316,243, a highly specific β3-adrenoceptor agonist, in yellow KK mice. Life Sci., 1994, 54, 491–498.
- Arch, J. R. S., β3-adrenoreceptor ligands and pharmacology of the β3-adrenoreceptor. In The β3-Adrenoceptor (ed. Strosberg. A. D.), Taylor and Francis, London, 2000, pp. 48–76.
- Verma, A. K. and Pratap, R., The biological potential of flavones. Nat. Prod. Rep., 2010, 27, 1571–1593.
- Pratap, R. et al., Oxy substituted chalcones as antihyperglycaemic and antidyslipidaemic agents. US7807712 B2, 2010.
- Satyanarayana, M., Tiwari, P., Tripathi, B. K., Srivastava, A. K. and Pratap, R., Synthesis and antihyperglycaemic activity of chalcone based aryloxypropanolamines. Bioorg. Med. Chem., 2004, 12, 883–889.
- Verma, A. K. et al., Flavone-based novel antidiabetic and antidyslipidaemic agents. J. Med. Chem., 2012, 55, 4551–4567.
- Srivsatava, R., Srivastava, S. P., Jaiswal, N., Mishra, A., Maurya, R. and Srivastava, A. K., Antidiabetic and antidyslipidaemic activities of Cuminum cyminum L. in validated animal models. Med. Chem. Res., 2010, 20, 1656–1666.
- Mishra, A., Srivastava, R., Srivastava, S. P., Gautam, S., Tamrakar, A. K., Maurya, R. and Srivastava, A. K., Antidiabetic activity of heart wood of Pterocarpus marsupium Roxb. and analysis of phytoconstituents. Indian J. Exp. Biol., 2013, 51, 363–374.
- Gupta, S., Varshney, K., Srivastava, R., Rahuja, N., Rawat, A. K., Srivastava, A. K. and Saxena, A. K., Identification of novel urea derivatives as PTP1B inhibitors: synthesis, biological evaluation and structure–activity relationships. Med. Chem. Commun., 2013, 4, 1382–1387.
- Shukla, P., Srivastava, S. P., Srivastava, R., Rawat, A. K., Srivastava, A. K. and Pratap, R., Synthesis and antidyslipidaemic activity of chalcone fibrates. Bioorg. Med. Chem. Lett., 2011, 21, 3475–3478.
- Miura, T., Itoh, C., Iwamoto, N., Kato, M., Kawai, M., Park, S. R. and Suzuki, I., Hypoglycemic activity of the fruit of the Momordica charantia in type 2 diabetic mice. J. Nutr. Sci. Vitaminol., 2001, 47, 340–344.
- Okine, L. K. N., Nyarko, A. K., Osei-Kwabena, N., Oppong, I. V., Barnes, F. and Ofosuhene, M., The antidiabetic activity of the herbal preparation ADD-199 in mice: a comparative study with two oral hypoglycaemic drugs. J. Ethnopharmacol., 2005, 97, 31– 38.
- Mythili, M. D., Vyas, R., Akila, G. and Gunasekaran, S., Effect of streptozotocin on the ultrastructure of rat pancreatic islets. Microsc. Res. Tech., 2004, 63, 274–281.
- Skyler, J. S., Jovanovic, L., Klioze, S., Reis, J. and Duggan, W., Inhaled Human Insulin Type 1 Diabetes Study Group, two-year safety and efficacy of inhaled human insulin (Exubera) in adult patients with type 1 diabetes. Diabetes Care, 2007, 30, 579–585; doi:10.2337/dc06-1863.
- Tamrakar, A. K., Jaiswal, N., Yadav, P. P., Maurya, R. and Srivastava, A. K., Pongamol from Pongamia pinnata stimulates glucose uptake by increasing surface GLUT4 level in skeletal muscle cells. Mol. Cell. Endocrinol., 2011, 339, 98–104.
- Izumi, T., Enomoto, S., Hoshiyama, K., Sasahara, K. and Sugiyama, Y., Pharmacokinetic stereoselectivity of troglitazone, an antidiabetic agent, in the KK mouse. Biopharm. Drug Dispos., 1997, 18, 305–324.
- Jamali, F., Mehvar, R. and Pasutto, F. M., Enantioselective aspects of drug action and disposition: therapeutic pitfalls. J. Pharm. Sci., 1989, 78, 695–715.
- Rauws, A. G. and Groen, K., Current regulatory (draft) guidance on chiral medicinal products: Canada, EEC, Japan, United States. Chirality, 1994, 6, 72–75.
- Kostiainen, R., Kotiaho, T., Kuuranne, T. and Auriola, S., Liquid chromatography/atmospheric pressure ionization-mass spectrometry in drug metabolism studies. J. Mass Spectrom., 2003, 38, 357– 372.
- Tiller, P. R. and Romanyshyn, L. A., Liquid chromatography/ tandem mass spectrometric quantification with metabolite screening as a strategy to enhance the early drug discovery process. Rapid Commun. Mass Spectrom., 2002, 16, 1225–1231.
- Gautam, N. et al., Liquid chromatography tandem mass spectrometry method for determination of antidiabetic chalcones derivative S001-469 in rat plasma, urine and feces: application to pharmacokinetic study. Drug Res., 2014, 64, 377–383.
- Bajrami, B., Zhao, L., Schenkman, J. B. and Rusling, J. F., Rapid LC-MS drug metabolite profiling using microsomal enzyme bioreactors in a parallel processing format. Anal. Chem., 2009, 81, 9921–9929.
- Anthropecology of Solid Waste and The Water Bodies
Authors
1 Pollution and Environmental Assay Research Laboratory (PEARL), Department of Botany, D.D.U. Gorakhpur University, Gorakhpur, IN
2 Laboratory of Environmental Chemistry and Complexes
Source
Indian Science Cruiser, Vol 24, No 2 (2010), Pagination: 20-24Abstract
Anthropecology is a new term coined in the year 2009, to explain the ecology of the system which is largely affected, rather directed by the multidimensional anthropogenic activities. The present civic society generates a large amount of solid waste. Further; the diversity in the quality of waste is also increasing these days. By increase in population, and the increase in demand of the agricultural produce, the globe is facing rapid reduction. In this situation a problem arises for the proper disposal of the present day solid waste. The most convenient solution which is left with us is dumping of these poisonous solid wastes in to the low lying areas, preferably the lakes. The literature deals with the ill-effects of this mal-practice, rather anthropecology of the solid waste and the perennial water bodies.
- Crude Agricultural Practices and Water Pollution
Authors
1 Pollution and Environmental Assay Research Laboratory (PEARL), Department of Botany, Deen Dayal Upadhyay Gorakhpur University, Gorakhpur - 273009, IN
2 Laboratory of Environmental Chemistry & Complexes, Department of Chemistry, Udai Pratap College, Varanasi-221002, IN
Source
Indian Science Cruiser, Vol 24, No 5 (2010), Pagination: 21-25Abstract
Agriculture is one of the most important activities. It is essential because belly of the globe is filled by grains only and not by the coins and currencies, whatever economic development we achieve. Thus, this is an activity of human which can be considered as the most important. Every coin has two faces; therefore, this practice of man has also its own drawback. In rural area the practice of agriculture is performed. It has been reported that the present day agriculture is not ecofriendly, it is highly mechanized and chemically managed. Large numbers of chemicals are being used in agriculture now days, in the form of insecticides, pesticides, rhodenticides, fungicides and the fertilizers. The fertilizers are rich in nitrates and phosphates. Due to crude agricultural practices these chemicals percolate through the soil surface and there are chances of groundwater pollution. The chemicals other than fertilizers are rich in a variety of heavy metals. Their percolation or runoff may lead to pollution of the water bodies directly and indirectly. DOT, BHC, aldrin, heptachlor and the other chlorinated hydrocarbons are extremely toxic and persistent. They would be causing problems, which may or may not be noticed, but ultimately it is the life of human which is affected.
- Ph D Degree in the Search of its Respect and Recognition in India
Authors
1 Pollution and Environmental Assay Research Laboratory (PEARL), Department of Botany, DDU Gorakhpur University, Gorakhpur, U.P. 273 009, IN
Source
Indian Science Cruiser, Vol 25, No 1 (2011), Pagination: 10-10Abstract
For recruitment of Lecturers m higher education National Eligibility Test (NET) was initiated in 1991. This was done by the UGC to avoid the then ambiguity in the Ph.D. By that time obtaining the Ph.D. degree was not tough, though this condition was prevailing in some of the arts subjects only. The degree of Ph.D. in science subjects has never been an easy task, possibly because of the involvement of the laboratory work. To promote the quality and the value of Ph.D. it was decided to conduct an entrance test before registration for the Ph.D. course. Syllabus and the pattern, including the minus markings were designed similar to that of NET in nearly all the Universities’. This test is not easy, as the records are available, showing only four to sixteen percent success rate.
- Invited Invasion of the Foreign Universities in India
Authors
1 Pollution and Environmental Assay Research Laboratory (PEARL), Department of Botany, DDU Gorakhpur University, Gorakhpur, U.P. - 273 009, IN
Source
Indian Science Cruiser, Vol 25, No 2 (2011), Pagination: 8-9Abstract
I don’t know, what is wrong with the policy makers. They are just following the experiment of ‘Trial and Errors” in higher education. This higher education is in the target of the government, presently. The Governments have made up their mind to break the back bone of the culture of Higher Education in India. This has been proved by certain activities of the Policy makers. Government has directed its policies to invite and place “Red Carpet Welcome” to the foreign Universities, saying that by competition, the quality of higher education in India will improve. I doubt, how long the handicapped Universities will stand with empty stomach and in Gemini posture before the foreign Universities, which will come well equipped with their policies to take over the Indians. The Policy of the government is just as to throw the Indian soldiers empty handed before their enemy.
- Hope, Scope and Need of Reforms in Higher Education
Authors
1 Pollution and Environmental Assay Research Laboratory (PEARL), Department of Botany, DDU Gorakhpur University, Gorakhpur, U.P. 273 009, IN
Source
Indian Science Cruiser, Vol 25, No 4 (2011), Pagination: 8-9Abstract
The policy makers are following the experiment of “Trial and Errors” in higher education. Though, there is enough to discuss, but I shall bring out only some of the hidden agenda of the policy makers. If such disputed agenda are approved, it will not only affect the present generation, but generations have to make sacrifice like our freedom fighters.
- Waste Water a Potential Resource for Irrigation
Authors
1 Pollution and Environmental Assay Research Laboratory (PEARL), Department of Botany, DDU Gorakhpur University, Gorakhpur-273009, U.P., IN
2 Laboratory of Environmental Chemistry and Complexes, Department of Chemistry, Udai Pratap Autonomy, P.G. College, Varanasi-221002, U.P.,, IN
Source
Indian Science Cruiser, Vol 26, No 3 (2012), Pagination: 49-53Abstract
Waste water is gaining popularity as a source of irrigation water in different countries around the world. This is especially true in India, where it has been in use for a long time. Its economic benefits and its importance as a coping strategy for the poor have had little recognition. The lack of alternative source of water has generated viable markets for wastewater. Increased disposable incomes have resulted from the catalytic use of waste water that was formerly not socially acceptable, i.e. the farmers considered it unhealthy and unclean. The use of waste water to grow food crops poses uncertain risks to the health of both, the consumers and to those who actually handle the waste water. It is useful in the discussion to differentiate between unplanned use of waste water resulting from poor sanitation and planned use which tries to address matters such as economic benefits but also institutional challenges and risks which require different management approaches and ideally different guidelines. This diversity makes the current WHO guidelines, which try to be global in nature, complex to understand and apply.
- The Murophyte
Authors
1 Pollution and Environmental assay Research Laboratory (PEARL), Department of Botany, Deen Dayal Upadhyay Gorakhpur University, Gorakhpur - 273009, IN
Source
Indian Science Cruiser, Vol 27, No 1 (2013), Pagination: 32-35Abstract
Murophytes are the plants growing over the buildings, walls and roofs. Plants can live in aquatic, terrestrial and organic environments. Their growth in these environments is influenced by many parameters, which regulate the morphological features of the plants. It is not only the morphological features, but the presence of a specific group of plants is also regulated. There are habitats in which the extreme condition leads to the selection of species with morphological and physiological adaptations enabling them to service. Walls constitute a specialized microhabitat; since they are built by man they are restricted to inhabited areas. Mural flora developed in historical periods in which civilized man constructed buildings. The oldest walls or those most characteristically covered in vegetation.
- Groundwater Pollution: Causes and Impact
Authors
1 Pollution and Environmental Assay Research Laboratory (PEA RL), Department of Botany, D.D.U. Gorakhpur University, Gorakhpur., IN
2 Pollution and Environmental Assay Research Laboratory (PE A R L), Department of Botany, D.D.U. Gorakhpur University, Gorakhpur., IN
3 Laboratory of Environmental Chemistry and Complexes, Department of Chemistry, U.P. College, Varanasi., IN