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Full-Text Articles in Medicine and Health Sciences
Development Of Phenotypic Drug Discovery Models For Tropical Parasitic Diseases, Surendra Kumar Jain
Development Of Phenotypic Drug Discovery Models For Tropical Parasitic Diseases, Surendra Kumar Jain
Electronic Theses and Dissertations
Malaria and visceral leishmaniasis are major killer parasitic diseases. These diseases though occur primarily in tropical countries; economic burden and overall health impacts of malaria and leishmaniasis are global. The emergence of drug-resistant and more-virulent strains of the pathogens has further amplified the problems. New drug discovery approaches primarily rely on in vitro and in vivo models of the disease. The pathogens causing leishmaniasis and malaria are intracellular. Leishmania parasite grows as amastigotes in macrophages cells, and malaria parasite grows within the hepatocytes or erythrocytes. The intracellular forms of the pathogens are responsible for the pathophysiology of the diseases. New …
Lipid & Surfactant Based Systems For Improved Delivery Of Poorly Soluble Apis, Sri Satyasai Nagendra Babu Punyamurthula
Lipid & Surfactant Based Systems For Improved Delivery Of Poorly Soluble Apis, Sri Satyasai Nagendra Babu Punyamurthula
Electronic Theses and Dissertations
A large number of pharmaceutical compounds belong to class II and IV of biopharmaceutical classification of drug (BCS). Class II compounds are limited by their poor aqueous solubility, while class IV compounds suffer from poor solubility and permeability. This translates to poor absorption and low plasma levels post oral administration. Lipids comprise of fatty acids and their derivatives and are considered a biocompatible option for drug delivery. In the studies discussed in following chapters, lipid based drug delivery systems (LBDDS) have been utilized in improving the handling, ease of formulation, solubility and bioavailability of three compounds. In the first study, …
Discovery, Isolation, And Identification Of Antimalarials From Fungal Endophytes, Andrekeus Lee
Discovery, Isolation, And Identification Of Antimalarials From Fungal Endophytes, Andrekeus Lee
Electronic Theses and Dissertations
We examined fungal endophytes for their ability to inhibit bacterial, fungal and protozoal pathogens. Once antimalarial activity was discovered and confirmed, we sought to isolate and identify the active constituent(s) of our extracts. Bioassay-guided fractionation techniques were used to isolate our active compound, the structure of which was elucidated using 1H- and 13C-NMR. 2D-NMR and LC-MS analyses helped confirm that our endophytes were indeed producing artemisinin. Growth versus production studies were conducted to optimize our growth and extraction conditions while several other variables, like temperature and culture medium, were evaluated in an effort to improve our yields. Artemisinin production under …
New Synthetic Methodologies For The Construction And Optimization Of Natural Products, Amir E. Wahba
New Synthetic Methodologies For The Construction And Optimization Of Natural Products, Amir E. Wahba
Electronic Theses and Dissertations
Toxicity associated with bioactive natural products is considered as a major obstacle in the process of drug discovery. Manzamine A (MA) is one such candidate that requires optimization to overcome the toxicity problem. The manzamine alkaloids represents a unique class of natural products that have shown a diverse range of bioactivities including antimicrobial, antiparasitic, cytotoxicity, anti-inflammatory, pesticidial, and was shown to possess activity against HIV-1 and AIDS opportunistic infections. The greatest potential for the manzamine alkaloids appears to be against malaria and neuroinflammation. Experimental and modeling studies suggested that the planer ?-carboline moiety can act as DNA intercalator and hence …