Botany - Research Publications

Permanent URI for this collectionhttps://kr.cup.edu.in/handle/32116/32

Browse

Author: search.filters.author.Jaitak, Vikas

Search Results

Now showing 1 - 3 of 3
  • Thumbnail Image
    Item
    Natural products as multidrug resistance modulators in cancer
    (Elsevier, 2019) Kumar, Amit; Jaitak, Vikas
    Cancer is a prominent cause of death globally. Currently, many drugs that are in clinical practice are having a high prevalence of side effect and multidrug resistance. Risk of tumors acquiring resistance to chemotherapy (multidrug resistance) remains a significant hurdle to the successful treatment of various types of cancer. Membrane-embedded drug transporters, generally overexpressed in cancer, are the leading cause among multiple mechanisms of multidrug resistance (MDR). P-glycoprotein (P-gp) also MDR1/ABCB1, multidrug resistance associated protein 1 (MRP1/ABCC1), MRP2 and breast cancer resistance protein (BCRP/ABCG2) are considered to be a prime factor for induction of MDR. To date, several chemical substances have been tested in a number of clinical trials for their MDR modulatory activity which are not having devoid of any side effects that necessitates to find newer and safer way to tackle the current problem of multidrug resistance in cancer. The present study systematically discusses the various classes of natural products i.e flavonoids, alkaloids, terpenoids, coumarins (from plants, marine, and microorganisms) as potential MDR modulators and/or as a source of promising lead compounds. Recently a bisbenzyl isoquinoline alkaloid namely tetrandrine, isolated from Chinese herb Stephania tetrandra (Han-Fang-Chi) is in clinical trials for its MDR reversal activity. © 2019 Elsevier Masson SAS
  • No Thumbnail Available
    Item
    Gene and metabolite profiling reveals flowering and survival strategies in Himalayan Rhododendron arboreum
    (Elsevier, 2019) Choudhary, Shurti; Thakur, Sapna; Jaitak, Vikas; Bhardwaj, Pankaj
    Rhododendron arboreum inhabits the Himalayan climate otherwise detrimental to many species, though the underlying survival mechanism remains unclear. Such temperate species have an inherent endurance towards freezing temperature which is prerequisite for an initiation and transition to flowering phase. Orchestrating the molecular architecture is vital towards managing distinct abiotic signals. To determine the molecular factors directing growth, development, and tolerance under environmental extremes in the species, the high-throughput transcriptome and metabolome data from vegetative as well as cold-acclimatized flowering season tissues were generated. Firstly, the de novo assembly pertaining to the foliar and floral tissues comprising of 157,427 unigenes was examined for a comparative analysis. 4149 of 12,577 transcripts observed with a significant fluctuating expression corresponded to seasonal retorts. Following the interactive network, 525 genes were distinguished as the epicenters of sense, response, and tolerance. Secondly, liquid chromatography coupled to mass spectrometry was adopted to profile the extent of metabolite richness across the tissues of two seasons. Taking into account the formula-based mappings offered by MetaboSearch tool, 421 unique ions obtained were annotated to 173 KEGG compounds, especially secondary metabolites. Moreover, by integrating the transcript and metabolite annotations, it was found that right from active metabolism, signaling, development, and their regulations, supplementary response to abiotic/biotic stimuli was induced. A multifaceted response displayed during flowering not only sponsored the climatic encounters but brought the shift from vegetative to reproductive growth. Overall, this comprehensive approach following transcriptome and non-targeted metabolome elucidated the contribution of genetic and metabolic factors in environmental responses
  • No Thumbnail Available
    Item
    In silico screening and molecular interaction studies of tetrahydrocannabinol and its derivatives with acetylcholine binding protein
    (Bentham Science Publishers B.V., 2018) Panigrahi, P.P.; Singla, Ramit; Bansal, A.; Comar, Junior M.; Jaitak, Vikas; Yennamalli, R.M; Singh, T.R.
    Background: Alzheimer’s disease (AD) is the fourth largest cause of death among people over 65 years of age. Accumulation of β-amyloid and cholinergic deficiency are two prominent pathological descriptions for AD. Objective: Depletion of acetylcholine at the site of its action is thought to be the prime cause of AD. It has been reported that tetrahydrocannabinol (THC) exhibits anticholinesterase activity and it has been proposed as a suitable candidate for treating neurological disorders such as AD. Methods: Using an in silico approach, including virtual screening, THC and its derivatives were docked against acetylcholine binding protein (AChBP) using AutoDock. The top-ranked molecules were studied in detail using an induced fit docking approach followed by characterization of their binding affinity, toxicity and ADME properties using TOPKAT and QikProp. Results: THC_JUIT25, a novel derivative of THC, showed maximum binding affinity and was observed as a promising candidate for performing receptor-ligand interaction studies using molecular dynamics simulation. Conclusion: In this study, we propose a novel THC derivative as a potential lead molecule in the drug development strategy for treating AD.