Department Of Pharmaceutical Sciences and Natural Products

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Author: search.filters.author.Jaitak, VikasHas files: Yes

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    Tetrazoles as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies
    (Elsevier, 2020) Dhiman, N; Kaur, K; Jaitak, Vikas
    Cancer is a leading cause of death worldwide. Even after the availability of numerous drugs and treatments in the market, scientists and researchers are focusing on new therapies because of their resistance and toxicity issues. The newly synthesized drug candidates are able to demonstrate in vitro activity but are unable to reach clinical trials due to their rapid metabolism and low bioavailability. Therefore there is an imperative requisite to expand novel anticancer negotiators with tremendous activity as well as in vivo efficacy. Tetrazole is a promising pharmacophore which is metabolically more stable and acts as a bioisosteric analogue for many functional groups. Tetrazole fragment is often castoff with other pharmacophores in the expansion of novel anticancer drugs. This is the first systematic review that emphasizes on contemporary strategies used for the inclusion of tetrazole moiety, mechanistic targets along with comprehensive structural activity relationship studies to provide perspective into the rational design of high-efficiency tetrazole-based anticancer drug candidates. - 2020 Elsevier Ltd
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    Stevia rebaudiana targeting α-amylase: An in-vitro and in-silico mechanistic study
    (Taylor and Francis, 2019) Singla, R; Singla, N; Jaitak, Vikas
    Diabetes mellitus (DM) is the fastest growing metabolic disorder in the world. Recently, more attention is paid to the study of natural products due to side effects of synthetic drugs. Stevia rebaudiana (Bertoni) is considered an encouraging starting point for the antidiabetic lead development. In the present study, the in vitro α-amylase inhibitory activity of the extracts of S. rebaudiana is investigated. In order to understand the molecular mechanism and future pharmacophore development, in silico study of secondary metabolites isolated from S. rebaudiana was carried out. Results indicated that water extract shows highest α-amylase inhibitory activity as compared to other extracts. Moreover, compound 20 (rebaudioside A) which has been previously reported and isolated from water extract showed the impressive binding profile with α-amylase. Therefore, our study suggests that S. rebaudiana could be used in the development of therapeutic drugs for the treatment of diabetes. © 2017, © 2017 Informa UK Limited, trading as Taylor & Francis Group.
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    Recent Advances in Plant Metabolites Analysis, Isolation, and Characterization
    (Springer, 2018) Singla, Ramit; Jaitak, Vikas
    Metabolites from natural sources either from terrestrial or marine sources serve as unmatched resources for new drug leads or diverse chemical identity. Due to ever-rising requirement for new pharmacophore in high-throughput screening and discovery for therapeutic drugs from metabolites, there has been motivated interest particularly in edible plants around the globe. Bioactive compounds are indispensable component present in different forms of botanicals, nutraceuticals, and herbal preparations used for the various medicinal applications. The prime focus in present chapter is to enlighten and discus diverse analytical methodologies which have been applied during extraction, isolation, and characterization of active constituents in botanicals, nutraceutical, and herbal preparations.
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    Identification of novel indole based heterocycles as selective estrogen receptor modulator
    (Academic Press Inc., 2018) Singla, Ramit; Prakash, Kunal; Bihari Gupta, Kunj; Upadhyay, Shishir; Dhiman, Monisha; Jaitak, Vikas
    In the present study, we have designed and synthesized indole derivatives by coalescing the indole nucleus with chromene carbonitrile and dihydropyridine nucleus. Two compounds 5c and 6d were selected from series I and II after sequential combinatorial library generation, docking, absorption, distribution, metabolism and excretion (ADME) filtering, anti-proliferative activity, cytotoxicity, and ER-? competitor assay kit by utilizing estrogen receptor-? (ER-?) dominant T47D BC cells line and PBMCs (Peripheral Blood Mononuclear Cells). Cell imaging experiment suggested that both the compounds successfully cross cellular biomembrane and accumulate in nuclear, cytoplasmic and plasma membrane region. Semiquantitative RT-PCR and Western blotting experiments further supported that both compounds reduced the expression of mRNA and receptor protein of ER-? thereby preventing downstream transactivation and signaling pathway in T47D cells line. Current findings imply that 5c and 6d represent novel ER-? antagonists and may be used in the development of chemotherapy for the management of BC. ? 2018 Elsevier Inc.
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    Polymeric Encapsulates of Essential Oils and Their Constituents: A Review of Preparation Techniques, Characterization, and Sustainable Release Mechanisms
    (Taylor and Francis Inc., 2016) Vishwakarma, G.S.; Gautam, N.; Babu, J.N.; Mittal, S.; Jaitak, Vikas
    Natural polymer based encapsulation of essential oil (EO) is one of the emerging and challenging area of research in perfumery, cosmetics, flavoring agents, preservatives, therapeutics, etc. The knowledge of formulation techniques and physico-chemical properties of the polymers are the basic requirements for the successful encapsulations of essential oils (EOs). This current review article is focused on a comparative account of various formulation techniques based on their applicability. For the first time, it also reviews various physico-chemical techniques used in the analysis of EO encapsulates to determine their stability, structure, surface morphology, and encapsulation efficiency. Further, the mechanisms involved in the release of EOs from encapsulates, along with various factors affecting their release, have also been discussed. ? 2016 Taylor & Francis Group, LLC.
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    Antimicrobial and repellent activity of the essential oils of two lamiaceae cultivated in Western Himalaya
    (Bentham Science Publishers B.V., 2015) Stappen, Iris; Ali, Abbas; Tabanca, Nurhayat; Khan,Ikhlas A.; Wanner, J�rgen; Gochev, Velizar K.; Singh, Virendra; Lal, Brij; Jaitak, Vikas; Kaul, Vijay K.; Schmidt, Erich; Jirovetz, Leopold; Stappen, I.; Ali, A.; Tabanca, N.; Khan, I.A.; Wanner, J.; Gochev, V.K.; Singh, V.; Lal, B.; Jaitak, V.; Kaulh, V.K.; Schmidt, E.; Jirovetz, L.
    The essential oils of two Lamiaceae cultivated in Western Himalaya were examined on their antimicrobial, biting deterrent as well as larvicidal activity. Additionally their odors are described and their chemical compositions analyzed by GC-MS are given. The main component of Nepeta cataria oil was 4a?,7?,7a?-nepetalactone (85%), whereas camphor (27%) and 1,8-cineol (27%) were dominant in the oil of Rosmarinus officinalis. The studied essential oils demonstrated high to moderately antimicrobial activity against reference strains, clinical and food spoilage isolates of Bacillus cereus, Staphylococcus aureus, Escherichia coli, Salmonella abony and Candida albicans (MIC 160-640 ?g/ml) and indicated low activity against Pseudomonas aeruginosa and P. fluorescens. Both oils showed biting deterrent activity above solvent control but lower than DEET. Nepeta catarica essential oil exhibited high toxicity with LD50 value of 20.2 whereas R. officinalis oil showed only 50% mortality at the highest tested dose of 125 ppm against 1-day old Aedes aegypti larvae at 24-hour post treatment. ? 2015 Bentham Science Publishers.
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    An in-silico approach on essential oil molecules as apoptosis inducer in cancer chemotherapy
    (Innovations in Pharmaceuticals and Pharmacotherapy, 2017) Bhalla, Yashika; Singla, Ramit; Jaitak, Vikas; Sapra, Sameer
    Essential oils (EOs) are very engrossing natural plant products and apart from this they possess various biological properties. It has been reported that these essential oil molecules are able to inhibit tumor cell proliferation and induce tumor cell death by inhibiting multiple cancer-specific targets including the suppression of anti-apoptotic pathways i.e., BCL-2, BCL-XL, MCL-1, and NFκb. This study was conducted with the objective of exploring the anticancer activity of herbs and spices, with special reference to its potential to inhibit anti-apoptotic pathways by studying their interaction pattern with the selective inhibitors of the particular receptors. Hence a comparative in-silico study was done in which the essential oil molecules were docked with specific anti-apoptotic receptors with respect to the particular known inhibitor of that receptor therefore the binding affinity of the essential oil molecule with that of the receptor site was analyzed. It has been observed that the phytochemicals like capsaicin have an impressive binding affinity for NFκb receptor, BCL-2 as compared to its standard inhibitors, which shows that the phytochemical has stronger binding affinity for receptor. These docking results hereby apparently tells us that the binding affinity of the essential oil molecules are either comparable or more than that of the specific inhibitors of the receptors hence in future drug molecules can be synthesized keeping in view the strong binding affinity of these molecules with the receptors.
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    Synthesis of rebaudioside A from stevioside and their interaction model with hTAS2R4 bitter taste receptor
    (Elsevier Ltd, 2016) Singla, Ramit; Jaitak, Vikas
    Steviol glycosides (SG's) from Stevia rebaudiana (Bertoni) have been used as a natural low-calorie sweeteners. Its aftertaste bitterness restricts its use for human consumption and limits its application in food and pharmaceutical products. In present study, we have performed computational analysis in order to investigate the interaction of two major constituents of SG's against homology model of the hTAS2R4 receptor. Molecular simulation study was performed using stevioside and rebaudioside A revealed that, sugar moiety at the C-3?? position in rebaudioside A causes restriction of its entry into the receptor site thereby unable to trigger the bitter reception signaling cascade. Encouraged by the current finding, we have also developed a greener route using ?-1,3-glucanase from Irpex lacteus for the synthesis of de-bittered rebaudioside A from stevioside. The rebaudioside A obtained was of high quality with percent conversion of 62.5%. The results here reported could be used for the synthesis of rebaudioside A which have large application in food and pharmaceutical industry. ? 2016 Elsevier Ltd. All rights reserved.
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    Photoprotective, antioxidant screening and new ester from dry root extracts of Potentilla atrosanguinea (Himalayan cinquefoil)
    (Elsevier, 2016) Kaur, Rajbir; Singla, Ramit; Jaitak, Vikas; Gupta, Vinay Kumar
    In vitro photoprotective and antioxidant activities of dried aqueous-methanolic (H2O/MeOH) crude extract and ethyl acetate (EtOAc), n-butanol (n-BuOH) as well as aqueous (H2O) fractions of roots of western Himalayan plant Potentilla atrosanguinea (Himalayan cinquefoil) were evaluated. The ability of protection against UVB region followed the trend EtOAc>n-BuOH>H2O/MeOH>H2O. Total phenol content of crude H2O/MeOH extract was found to be 429.808mg GAE/g. The H2O/MeOH crude extract showed highest antioxidant of DPPH radical scavenging, superoxide anion radical scavenging and cupric ion reducing of 90.04, 78.86 and 88.64% respectively at 200?g/mL. One new compound methyl pentatetraconta-30,32,34,36,38,40,42-heptaenoate (PA-1) along with a known pentadecylbutyrate (PA-2) was isolated by column chromatography. Results indicated the importance of root extracts as photoprotective agents in sunscreen preparation in the pharmaceutical industry and considered as a natural source of antioxidants. ? 2015 South African Association of Botanists.
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    Chemical Composition and Biological Activity of Essential Oils from Wild Growing Aromatic Plant Species of Skimmia laureola and Juniperusmacropoda from Western Himalaya
    (NPC (Natural Product Communication), 2015) Stappena,Iris; Tabanca, Nurhayat; Ali, Abbas; Wedge, David E.; Wanner, J�rgen; Kaul, Vijay K.; Lal, Brij; Jaitak, Vikas; Gochev, Velizar K.; Schmidt, Erich; Jirovetz, Leopold
    The Himalayan region is very rich in a great variety of medicinal plants. In this investigation the essential oils of two selected species are described for their antimicrobial and larvicidal as well as biting deterrent activities. Additionally, the odors are characterized. Analyzed by simultaneous GC-MS and GC-FID, the essential oils’ chemical compositions are given. The main components of Skimmia laureola oil were linalool and linalyl acetate whereas sabinene was found as the main compound for Juniperus macropoda essential oil. Antibacterial testing by agar dilution assay revealed highest activity of S. laureola oil against all tested bacteria, followed by J. macropoda oil . Antifungal activity was evaluated against the strawberry anthracnose causing plant pathogens Colletotrichum acutatum , C. fragariae and C . gloeosporioides . Juniperus macropoda essential oil indicated higher antifungal activity against all three pathogens than S. laureola oil. Both essential oils showed biting deterrent activity above solvent control but low larvicidal activity.