School Of Basic And Applied Sciences

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    Evaluation of chemical composition and groundwater and anticancer properties of citrullus colocynthis
    (Central University of Punjab, 2014) Kaur, Jatinder; Bhardwaj, Pankaj
    Colocynth (Citrullus colocynthis (L.)) is medicinal plant of family Cucurbitaceae which is the native of Turkey. This plant has been used as anti-inflammatory agent, for the treatment of jaundice, skin infections, and urinary diseases from ancient times. It is anti-diabetic, anti-microbial, anti-parasitic, antifungal and anti-oxidant in nature and thought to possess anti-cancer properties also. There is no proper study available regarding its anticancer nature. The aim of the study was to estimate the chemical composition of C. colocynthis fruit and the effect of different extracts prepared from C. colocynthis pulp and seeds on various cancer cell lines. These extracts were found to contain number of secondary metabolites which may further have useful and healing properties. When cancer cells were treated with different prepared extracts, the cell viability of various cancer cells was reduced effectively. Effect of p53 gene was also analysed by using intact p53 as well as p53 mutant cell lines. Antioxidant activity of C. colocynthis was also determined by performing H2DCFDA. Assessment of various antioxidant enzymes such as Catalase, SOD, and Glutathione reductase was also done and found to be present in this fruit. We also analysed the protective effect of C. colocynthis by first treating the cells with pesticides and then with colocynthis extracts. Results indicate that C. colocynthis neutralized the harmful effect of pesticides. The results obtained are encouraging and confirm the value of the use of C. colocynthis as an anticancer agent for fighting against various cancers. It may be helpful to find the exact component responsible for the protective action of C. colocynthis.
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    Design and synethesis of APE1 inhibitors as putative anticancer agents
    (Central University of Punjab, 2014) Kaur, Gagandeep; Kumar, Raj
    Success in chemotherapy has not been attained completely yet and has remained a worried issue from years. Various reasons drive this failure, but the much talked about is failure due to emergence of resistance to chemotherapeutic drugs due to various factors. One of the major reasons here we have targeted is the resistance developed against DNA damaging chemotherapy due to over activation of APE1 enzyme evolved in BER pathway, which is the major repair pathway responsible for 95% of the DNA repair. Design and synthesis of APE1 inhibitors using rational approach fulfilling the pharmacophoric requirements has been carried out in this research work. Molecular modelling studies were performed to confirm that designed compounds fit well into the repair active cavity. 14 compounds have been designed and synthesized having pyrazolo-quinazolines core structure. The anticancer potential of the 8 representative compounds was evaluated against rat C-6 glial cell line at different concentrations. All synthesized compounds showed good anticancer activity against rat C-6 glial cell lines. The inhibitory potential of the compounds obtained from the MTT assay results helped us to formulate the SAR studies. Further ROS measurement was also carried out using DCFDA assay. Compounds showing good MTT results were also found to be potential antioxidants which conclude their mechanism of anticancer activity through APE1 inhibition. The active compounds may be taken further for lead optimisation and mechanistic interventions for their in vitro binding studies on APE1 in future.
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    Recent developments of C-4 substituted coumarin derivatives as anticancer agents
    (Elsevier Masson SAS, 2016) Dandriyal, Jyoti; Singla, Ramit; Kumar, Manvendra; Jaitak, Vikas
    Cancer is a prominent cause of death in global. Currently, the numbers of drugs that are in clinical practice are having a high prevalence of side effect and multidrug resistance. Researchers have made an attempt to expand a suitable anticancer drug that has no MDR and side effect. Coumarin scaffold became an attractive subject due to their broad spectrum of pharmacological activities. Coumarin derivatives extensively explored for anticancer activities as it possesses minimum side effect along with multi-drug reversal activity. Coumarin derivatives can act by various mechanisms on different tumor cell lines depending on substitution pattern of the core structure of coumarin. Substitution on coumarin nucleus leads to the search for more potent compounds. In this review, we have made an effort to give a synthetic strategy for the preparation of C-4 substituted coumarin derivatives as anticancer agents based on their mechanism of action and also discuss the SAR of the most active compound. ? 2016 Elsevier Masson SAS. All rights reserved.
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    Coumarins as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies
    (Elsevier Masson SAS, 2015) Thakur, Anuradha; Singla, Ramit; Jaitak, Vikas
    Abstract Coumarins are fused benzene and pyrone ring systems which prompt biological investigation to assess their potential therapeutic significance. It possesses immeasurable anticancer potential with minimum side effects depending on the substitutions on the basic nucleus. Coumarins have a tremendous ability to regulate diverse range of cellular pathways that can be explored for selective anticancer activity. This is the first standalone review that emphasis on the assorted retrosynthetic approaches, important targets for molecularly targeted cancer therapy and structure activity relationship studies that highlight the chemical groups responsible for evoking the anticancer potential of coumarin derivatives reported from 2011 to 2014. ? 2015 Elsevier Masson SAS.