Thursday, November 29, 2018

Phytochemical Analysis and Antioxidant Property of Selected Medicinal Plants Native to Cambodia:(DDIPIJ)-Lupine Publishers



Cambodian medicinal plants have been used to treat different diseases such as cardiovascular diseases, inflammation, cancers, diabetes and AIDS. This study aimed at conducting the Phytochemical analysis and in vitro antioxidant activities of whole plant of BryophyIIumpinnatum (Lam.) Kurz, barks of Dillenia ovata Wall. ex Hook. f. & Thomson, rhizomes of Drynariafortunei (Kunze ex Mett.) J. Sm. and barks of Lophopetalumwallichii Kurz. native to Cambodia. All the plants were extracted with ethanolby maceration extraction method. The Phytochemical analysis for alkaloids, phenolic compounds, tannins, flavonoids, coumarins, steroids, terpenoids, cardiac glycosides, essential oils, saponins and resins by using the standard methods. The in vitro antioxidant property was evaluated by assessing the DPPH' radical scavenging ability. The preliminary Phytochemical evaluation of these species exhibited that the ethanolic extracts of B. pinnatum (whole plant), D. ovata (barks), D.fortunei (rhizomes) and L.waIIichii (barks) contain alkaloids, phenolic compounds, tannins, flavonoids, terpenoids, cardiac glycosides, saponins and resins. Moreover, the ethanolic extracts of B. pinnatum whole plant, D. ovata barks, and D.fortunei rhizomes possess coumarins and steroids, and of L.waIIichii barks have essential oils. The in vitro antioxidant activity of the species B. pinnatum whole plant, D. ovata barks, D.fortunei rhizomes and L.waIIichii barks have prominent antioxidant activities. This study suggests the potential source of natural antioxidant in B. pinnatum, D. ovata, D.fortunei and L.waIIichii native to Cambodia. Further research is highly recommended on the isolation of the antioxidant compounds from these species.

http://www.lupinepublishers.com/drug-designing-journal/abstracts/phytochemical-analysis-and-antioxidant-property-of-selected-medicinal-plants-native-to-cambodia.ID.000109.php
http://www.lupinepublishers.com/drug-designing-journal/fulltext/phytochemical-analysis-and-antioxidant-property-of-selected-medicinal-plants-native-to-cambodia.ID.000109.php

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Monday, November 26, 2018

Preparation of Polyelectrolyte Hydrogels and Study Their Controlled Release of Gabapentin:(DDIPIJ)-Lupine Publishers



The semi interpenetrating network hydrogels (Z1-Z15) were prepared from different ratio of sodium alginate and linear poly (acrylamide-co-diallyl dimethyl ammonium chloride) then they mixed with the acrylamide and bisacrylamide as cross linking agent and polymerized via redox polymerization to form the semi-IPNs. All prepared semi-IPNs were loaded with three different amounts from Gabapentin as drug model. The swelling characteristics were studied for all semi- IPN hydrogels by determining the swelling ratio (Q).The release of Gabapentin was followed by using U.V. spectroscopy at (202 , 201 and 204) nm at constant temperature (37°C) in distilled water , simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) respectly. The results of Gabapentin released indicated that all semi-IPNs have the ability to release drug to environment and the amount of Gabapentin released about 50% during two hours. Higuchi equation was used to determine the Higuchi constant which is very useful to forecasting the amount of Gabapentin released theoretically.


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Thursday, November 22, 2018

An Overview on Pharmaceutical Supply Chain: A Next Step towards Good Manufacturing Practice:(DDIPIJ)-Lupine Publishers



The top priority in any health system is delivering of medicine as a strategic product. In the present context of a health-conscious society, management of pharmaceutical supply chains has become more complex because it involves the life-saving interest of human being and requires the participation of different stakeholders such as pharmaceutical manufacturers, wholesalers, distributors, customers, information service providers and regulatory agencies. Limited research is available in the area of pharmaceutical supply chains. Pharmaceutical companies, a most important player of the drug supply chain, are subject to many risks. These risks interrupt the quantity and quality of supply of medicine and their delivery to the accurate place and customers and at the correct time.


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Monday, November 19, 2018

Breaking into Merck's CCK Patents: the Starting Point of PNB Vesper Life Science to Design and Develop Cholecystokinin(CCK)-Antagonists as Targeted Chemotherapeutics:(DDIPIJ)-Lupine Publishers



Early anti-cancer research was dominated by the development of alkylating agents, followed by the discovery of a variety of anti-metabolites, which were useful anti-viral agents at the same time. Current anti-cancer drugs are designed towards molecular targets in order to reduce their toxicity and to enhance the selectivity on the cancer cells. Within an increasingly growing number of molecular targets, the cholecystokinin, as a neuro modulator, became an important anti-cancer target, especially when it was shown that cholecystokinin regulates the invasiveness of human pancreatic cancer cell lines via the protein kinase C pathway. The low potency and the lack of subtype receptor selectivity of those early non-peptide CCK-antagonists, was improved in the following generations of CCK antagonists. These potent and selective antagonists have shown disappointing results in clinical trials due to a poor bioavailability. Initially cholecystokinin was discussed as growth factor, not only in pancreatic cancer, but also for lung, breast, colon and brain cancer, followed by a detailed discussion of over 20 different chemical classes having been developed to date, mainly for the area of neuroscience. Loxiglumide, CI-988, Devazepide, L-365,260 and YM022 are highlighted including in vivo studies and clinical trials. Moreover, CCK antagonists were found useful in the enhancement of the analgesic effects of morphine and the anti-neo plastic effect of cis-platinium. Clinical trials are ongoing. It is concluded that non peptidal cholecystokinin receptor antagonists are modern, non-toxic anti-cancer agents.


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Wednesday, November 14, 2018

From Merck’s CCK- Antagonists Via 4-Amino-2(5H)- Furanones towards 5-Hydroxy-Pyrrol-2-Ones: Design, Synthesis and Evaluation of PNB-001 & PNB-081 as Experimental Therapeutic Agents in Pain Management:(DDIPIJ)-Lupine Publishers



Arylated 5-hydroxy–pyrrol-2-ones were prepared in 2 synthetic steps from muco-chloric acid and were optimised as CCK1 / CCK2 selective ligands using radio labelled binding assays. A potent CCK1 selective ligand was identified (PNB-081: CCK1=20nM) as well as a potent CCK2 ligand (PNB-001, IC50= 22nM) during a systematic SAR optimisation. The antagonism was confirmed for both ligands by using isolated tissue preparations with CCK5 and CCK8S. Subsequent in vivo evaluation revealed analgesic activity for the gastrin CCK2 antagonist PNB-001, in the hotplate and tail immersion test at 0.5mg /kg by IP administration in mice. The cholecystokinin antagonist PNB-081 potentiated the analgesic effect of morphine and reversed opiate tolerance in mice from doses >1 mg/kg by oral administration.


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Monday, November 12, 2018

On the Second Harmonic Index of Titania Nanotubes:(DDIPIJ)-Lupine Publishers



Topological indices which are graph invariants derived from molecular graphs of molecules are used in QSPR researches for modeling physicochemical properties of molecules. Topological indices are important tools for determining the underlying topology of a molecule in view of theoretical chemistry. The second harmonic index has been defined recently. In this study we compute the second harmonic index of Titania nanotubes.

Friday, November 9, 2018

Do You Know Your New Molecular Entity (NME)?:(DDIPIJ)-Lupine Publishers


During the last decades, life science startup companies have relatively rapidly increased their presence in the pharmaceutical landscape. Pharmaceutical development has evolved because technology (analytical and process development) and clinical development (hybrid design in phase 1, including patients in phase 1B) have evolved in parallel allowing in certain cases to decrease the time to regulatory filings (IND, CTA, NDA, NDA 505 (b)(2),..), which seemed attractive for startup companies. However, new molecular entities have become more complex since polypeptides, proteins, and monoclonal antibodies drug products take more and more place in many therapeutic areas (more than 50% in the 50 best seller drugs) along with the more conventional small molecules. But it is not the end of small molecules; research institutes, startup companies are still busy working hard to develop more powerful small molecules, since the physiopathology has also evolved and helped finding some new targets to enhance their efficacy and decrease their lack of selectivity. Startup companies are mostly driven by high level scientists and few of them are familiar with the drug development process, including its early phases. Scientists do know their NMEs from a scientific point of view however, much less and, sometimes, not at all in terms of potential drug product candidates.



Drug Designing & Intellectual Properties International Journal (DDIPIJ)- (ISSN: 2637-4706)- Lupine Publishers



Drug Designing & Intellectual Properties International Journal (DDIPIJ) is an international peer reviewed open access journal presenting original research and contributions and scientific advances in the field of drug design and development. Drug Designing & Intellectual Properties International Journal welcomes research articles, review articles, letter to the editors, editorials, case reports and innovations relating to all aspects of drug design and development and related sciences. Intellectual property (IP) pertains to any original creation of the human intellect such as artistic, literary, scientific creation. Several types properties of intellectual property protection like patent, copy right, trademark, etc. Patent is recognition for invention, which satisfies the criteria of global innovation, non obviousness. 

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