Department Of Pharmaceutical Sciences and Natural Products
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Item Recent Advances in Plant Metabolites Analysis, Isolation, and Characterization(Springer, 2018) Singla, Ramit; Jaitak, VikasMetabolites 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.Item Phytochemical investigation and biological evaluation of secondary metabolites from asparagus racemosus l through in-vitro and in-silico approach(Central University of Punjab, 2013) Singla, Ramit; Jaitak, VikasNature has been a source of medicinal products for millennia, and with many useful drugs developed from different natural resources, with majority of drugs are from plant origin. Asparagus racemosus belonging to family liliaceae, is one such important medicinal plant. This plant species is used traditionally in India and other parts of the world in epilepsy, Vaat disorders, brain tonic, hypertension, hepatoprotection, immunostimulant and antiabortifacient. In this context, the aim of the present study was to explore the roots of A.racemosus in terms of its medicinal values for instances antimutagenic, and advanced glycation end-product inhibitor. Antimutagenic activity of different extracts were evaluated using Ames test. A. racemosus methanolic extract (RME) and aqueous extract (RAE) have been found to have effective in the inhibition mutation induced by NPD and sodium azide. Among the two extracts, RAE and RME showed maximum inhibition of 49.2%, and 40.63% in Co-incubation mode respectively. The inhibition of BSA-glucose for the determination of antiglycation activity showed that the inhibition varied significantly among different extracts of A. racemosus. The highest inhibition measured by BSA-glucose was observed for (Ethyl acetate extract) REE (IC50 37.56 ± 1.65 ?g/mL) followed by (methanolic extract) RME (IC50 51.32 ± 1.48 ?g/mL). Isolation of molecules from methanol extract led to the characterisation of one molecule v namely nyasol out of total seven isolated molecules. The molecular docking study of isolated molecule Nyasol displayed strong binding affinity with estrogen receptor ? and estrogen receptor ?, indicating that Nyasol is beneficial in hormone responsive breast cancer. Moreover, in-silico study of already reported phytoestrogens from A.racemosus was also carried out using Glide docking to investigate interaction pattern with Human placental estrone sulphatases (1P49), human 17?-hydroxysteroid-dehydrogenase type 1 (1FDS), human glucose 6-phosphate dehydrogenase (2BH9) and tubulin protein receptors. The top docking score was obtained for rutin (estrogen receptor ?), 3,6,4'-trimethoxy-7-O-?-D-glucopyranosyl [1?4]-O-?-D-xylopyranoside glucopyranpsyl (HSP90), 8-Methoxy-5,6,4-trihydroxyisoflavone-7-O-?-D-glucopyranoside (human placental estrone sulphatase), Shatavarin X (17?-hydroxydehydrogenase`), Racemoside A (Glucose-6-phosphate dehydrogenase), Immunoside (Colchicine binding site of tubulin). The results indicated that phytoestrogens are likely potential candidate for controlling tumor progression with a special emphasis in breast cancer progression.Item 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, VikasIn 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.Item 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, SameerEssential 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.Item Synthesis of rebaudioside A from stevioside and their interaction model with hTAS2R4 bitter taste receptor(Elsevier Ltd, 2016) Singla, Ramit; Jaitak, VikasSteviol 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.Item 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 KumarIn 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.Item Molecular docking simulation study of phytoestrogens asparagus racemosus in breast cancer progression(International Journal Of Pharmaceutical Sciences And Research (IJPSR), 2015) Singla, Ramit; Jaitak, VikasPhytoestrogens are the xenoestrogens which are derived from the plant. This is the first report providing the deeper inside into the mechanism involved in restricting breast cancer progression with the help of docking simulation by phytoestrogen. Docking experiment bring to light that phytoestrogens prevents the binding of oestradiol with its receptor, thereby down regulating the signalling pathway and also acts as inhibitor of enzymes involved in the biosynthesis of endogenous oestradiol. In the present study, thirty phytoestrogen reported from A. racemosus were selected as ligand along with reference compounds using Maestro 9.3. Rutin, shatavarin I, 3, 6, 4' – trimethoxy-7-O-β-D- glucopyranosyl [1→4]-O-α-D-xylopyranoside glucopyranpsyl, 8-methoxy-5,6,4-trihydroxyisoflavone-7-O-β-D-glucopyranoside,shatavarin X, racemoside A, immunoside showed better interactions with their targets indicated from their respective dock score.Item Indole derivatives as anticancer agents for breast cancer therapy: A review(Bentham Science Publishers B.V., 2016) Sidhu, Jagpreet Singh; Singla, Ramit; Mayank; Jaitak, VikasBreast cancer (BC) is the second most common cause of cancer-related deaths in women throughout the world. Multiple drugs have been approved by US-FDA for breast related malignancies. Frequent emergence of resistances creates the severe need of newer moieties that are free from such problems. Drugs targeting breast cancer have been observed to be based on the multiple mechanisms of action, and various indole based anticancer agents have also been explored. Moreover, indoles have promising anti-cancer potential; there has been the emphasis on the synthesis of indole derivatives to overcome problems faced by existing therapeutic agents. Taking into consideration the above-mentioned facts we have analyzed in detail the possible role of indole based anticancer agents typically for breast related malignancies. This is the first exhaustive review that jointly covers various synthetic anticancer indole derivatives and related signaling pathways by which these derivatives have shown promising anti-breast cancer potential. ? 2016 Bentham Science Publishers.Item SHATAVARI (ASPARAGUS RACEMOSUS WILD): A REVIEW ON ITS CULTIVATION, MORPHOLOGY, PHYTOCHEMISTRY AND PHARMACOLOGICAL IMPORTANCE(web of Science (Thomson Reuters), 2014) Singla, Ramit; Jaitak, VikasAsparagus racemosus, a climbing Ayurvedic plant, is known for its numerous activities such as hyperlipidemia, hypertension, angina, dysmenorrhea, anxiety disorders, benign prostatic hyperplasia (BPH), leucorrhoea and urinary tract infections. This plant possesses a wide range of secondary metabolites inclusive of steroids, alkaloids, dihydrophenanthrene derivatives, flavonoids, furan derivatives and essential oils. Information from the literature suggests that, the major constituents of A. racemosus are steroidal saponins which are mainly responsible for different biological activities of A. racemosus. The review summarizes the information concerning the cultivation, morphology, phytochemistry, biological activities, safety profile, marketing status and conservation techniques of A. racemosus .Item Recent developments of C-4 substituted coumarin derivatives as anticancer agents(Elsevier Masson SAS, 2016) Dandriyal, Jyoti; Singla, Ramit; Kumar, Manvendra; Jaitak, VikasCancer 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.