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Pharmaceuticals, Volume 5, Issue 6 (June 2012), Pages 553-673

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Research

Jump to: Review

Open AccessArticle a-Anilinoketones, Esters and Amides: A Chemical Study
Pharmaceuticals 2012, 5(6), 591-612; doi:10.3390/ph5060591
Received: 14 May 2012 / Revised: 28 May 2012 / Accepted: 29 May 2012 / Published: 5 June 2012
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Abstract
A group of a-anilinoketones, 2-aminoalcohols, a-anilinoesters and a-anilinoamides were successfully synthesized and characterized by NMR spectroscopy and mass spectrometry. The yields were, in general, moderate to good (up to 75.4%), except for the a-anilinoesters (16.9–35.6%). The a-halocarbonyl starting materials showed different chemical [...] Read more.
A group of a-anilinoketones, 2-aminoalcohols, a-anilinoesters and a-anilinoamides were successfully synthesized and characterized by NMR spectroscopy and mass spectrometry. The yields were, in general, moderate to good (up to 75.4%), except for the a-anilinoesters (16.9–35.6%). The a-halocarbonyl starting materials showed different chemical reactivities. a-Haloketones and a-chloroacetates afforded monoalkylation, while small a-chloroamides afforded dialkylation. Finally, NMR spectroscopy revealed interesting structural features about the 2-aminoalcohols and diphenylamides. Full article
Open AccessArticle Phytochemical Composition, Antioxidant and Xanthine Oxidase Inhibitory Activities of Amaranthus cruentus L. and Amaranthus hybridus L. Extracts
Pharmaceuticals 2012, 5(6), 613-628; doi:10.3390/ph5060613
Received: 12 March 2012 / Revised: 22 May 2012 / Accepted: 24 May 2012 / Published: 15 June 2012
Cited by 8 | PDF Full-text (203 KB) | HTML Full-text | XML Full-text
Abstract
This paper describes a preliminary assessment of the nutraceutical value of Amaranthus cruentus (A. cruentus) and Amaranthus hybridus (A. hybridus), two food plant species found in Burkina Faso. Hydroacetonic (HAE), methanolic (ME), and aqueous extracts (AE) from the aerial parts were [...] Read more.
This paper describes a preliminary assessment of the nutraceutical value of Amaranthus cruentus (A. cruentus) and Amaranthus hybridus (A. hybridus), two food plant species found in Burkina Faso. Hydroacetonic (HAE), methanolic (ME), and aqueous extracts (AE) from the aerial parts were screened for in vitro antioxidant and xanthine oxidase inhibitory activities. Phytochemical analyses revealed the presence of polyphenols, tannins, flavonoids, steroids, terpenoids, saponins and betalains. Hydroacetonic extracts have shown the most diversity for secondary metabolites. The TLC analyses of flavonoids from HAE extracts showed the presence of rutin and other unidentified compounds. The phenolic compound contents of the HAE, ME and AE extracts were determined using the Folin–Ciocalteu method and ranged from 7.55 to 10.18 mg Gallic acid equivalent GAE/100 mg. Tannins, flavonoids, and flavonols ranged from 2.83 to 10.17 mg tannic acid equivalent (TAE)/100 mg, 0.37 to 7.06 mg quercetin equivalent (QE) /100 mg, and 0.09 to 1.31 mg QE/100 mg, respectively. The betacyanin contents were 40.42 and 6.35 mg Amaranthin Equivalent/100 g aerial parts (dry weight) in A. cruentus and A. hybridus, respectively. Free-radical scavenging activity expressed as IC50 (DPPH method) and iron reducing power (FRAP method) ranged from 56 to 423 µg/mL and from 2.26 to 2.56 mmol AAE/g, respectively. Xanthine oxidase inhibitory activities of extracts of A. cruentus and A. hybridus were 3.18% and 38.22%, respectively. The A. hybridus extract showed the best antioxidant and xanthine oxidase inhibition activities. The results indicated that the phytochemical contents of the two species justify their traditional uses as nutraceutical food plants. Full article
(This article belongs to the Section Medicinal Chemistry)
Open AccessArticle Physical Factors Affecting Plasmid DNA Compaction in Stearylamine-Containing Nanoemulsions Intended for Gene Delivery
Pharmaceuticals 2012, 5(6), 643-654; doi:10.3390/ph5060643
Received: 17 May 2012 / Revised: 9 June 2012 / Accepted: 13 June 2012 / Published: 18 June 2012
Cited by 3 | PDF Full-text (442 KB) | HTML Full-text | XML Full-text
Abstract
Cationic lipids have been used in the development of non-viral gene delivery systems as lipoplexes. Stearylamine, a cationic lipid that presents a primary amine group when in solution, is able to compact genetic material by electrostatic interactions. In dispersed systems such as [...] Read more.
Cationic lipids have been used in the development of non-viral gene delivery systems as lipoplexes. Stearylamine, a cationic lipid that presents a primary amine group when in solution, is able to compact genetic material by electrostatic interactions. In dispersed systems such as nanoemulsions this lipid anchors on the oil/water interface confering a positive charge to them. The aim of this work was to evaluate factors that influence DNA compaction in cationic nanoemulsions containing stearylamine. The influence of the stearylamine incorporation phase (water or oil), time of complexation, and different incubation temperatures were studied. The complexation rate was assessed by electrophoresis migration on agarose gel 0.7%, and nanoemulsion and lipoplex characterization was done by Dynamic Light Scattering (DLS). The results demonstrate that the best DNA compaction process occurs after 120 min of complexation, at low temperature (4 ± 1 °C), and after incorporation of the cationic lipid into the aqueous phase. Although the zeta potential of lipoplexes was lower than the results found for basic nanoemulsions, the granulometry did not change. Moreover, it was demonstrated that lipoplexes are suitable vehicles for gene delivery. Full article
(This article belongs to the Special Issue Gene Therapy)
Open AccessArticle Removal of Cholera Toxin from Aqueous Solution by Probiotic Bacteria
Pharmaceuticals 2012, 5(6), 665-673; doi:10.3390/ph5060665
Received: 7 May 2012 / Revised: 13 June 2012 / Accepted: 15 June 2012 / Published: 19 June 2012
Cited by 1 | PDF Full-text (205 KB) | HTML Full-text | XML Full-text
Abstract
Cholera remains a serious health problem, especially in developing countries where basic hygiene standards are not met. The symptoms of cholera are caused by cholera toxin, an enterotoxin, which is produced by the bacterium Vibrio cholerae. We have recently shown that [...] Read more.
Cholera remains a serious health problem, especially in developing countries where basic hygiene standards are not met. The symptoms of cholera are caused by cholera toxin, an enterotoxin, which is produced by the bacterium Vibrio cholerae. We have recently shown that human probiotic bacteria are capable of removing cyanobacterial toxins from aqueous solutions. In the present study we investigate the ability of the human probiotic bacteria, Lactobacillus rhamnosus strain GG (ATCC 53103) and Bifidobacterium longum 46 (DSM 14583), to remove cholera toxin from solution in vitro. Lactobacillus rhamnosus strain GG and Bifidobacterium longum 46 were able to remove 68% and 59% of cholera toxin from aqueous solutions during 18 h of incubation at 37 °C, respectively. The effect was dependent on bacterial concentration and L. rhamnosus GG was more effective at lower bacterial concentrations. No significant effect on cholera toxin concentration was observed when nonviable bacteria or bacterial supernatant was used. Full article
(This article belongs to the Special Issue Probiotics and Prebiotics)
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Review

Jump to: Research

Open AccessReview Gene Therapy for the Treatment of Parkinson’s Disease: The Nature of the Biologics Expands the Future Indications
Pharmaceuticals 2012, 5(6), 553-590; doi:10.3390/ph5060553
Received: 17 April 2012 / Revised: 18 May 2012 / Accepted: 23 May 2012 / Published: 4 June 2012
Cited by 3 | PDF Full-text (442 KB) | HTML Full-text | XML Full-text
Abstract
The pharmaceutical industry’s development of therapeutic medications for the treatment of Parkinson’s disease (PD) endures, as a result of the continuing need for better agents, and the increased clinical demand due to the aging population. Each new drug offers advantages and disadvantages [...] Read more.
The pharmaceutical industry’s development of therapeutic medications for the treatment of Parkinson’s disease (PD) endures, as a result of the continuing need for better agents, and the increased clinical demand due to the aging population. Each new drug offers advantages and disadvantages to patients when compared to other medical offerings or surgical options. Deep brain stimulation (DBS) has become a standard surgical remedy for the effective treatment of select patients with PD, for whom most drug regimens have failed or become refractory. Similar to DBS as a surgical option, gene therapy for the treatment of PD is evolving as a future option. In the four different PD gene therapy approaches that have reached clinical trials investigators have documented an excellent safety profile associated with the stereotactic delivery, viral vectors and doses utilized, and transgenes expressed. In this article, we review the clinically relevant gene therapy strategies for the treatment of PD, concentrating on the published preclinical and clinical results, and the likely mechanisms involved. Based on these presentations, we advance an analysis of how the nature of the gene therapy used may eventually expand the scope and utility for the management of PD. Full article
(This article belongs to the Special Issue Gene Therapy)
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Open AccessReview Influence of Maternal Bifidobacteria on the Development of Gut Bifidobacteria in Infants
Pharmaceuticals 2012, 5(6), 629-642; doi:10.3390/ph5060629
Received: 1 April 2012 / Revised: 29 May 2012 / Accepted: 5 June 2012 / Published: 18 June 2012
Cited by 7 | PDF Full-text (73 KB) | HTML Full-text | XML Full-text
Abstract
Intestinal microbiota plays an important role in human health by influencing metabolic activities that result in the creation of energy and absorbable nutrients, a barrier to the colonization of pathogens, and stimulation of the immune system. The development of fecal microbiota in [...] Read more.
Intestinal microbiota plays an important role in human health by influencing metabolic activities that result in the creation of energy and absorbable nutrients, a barrier to the colonization of pathogens, and stimulation of the immune system. The development of fecal microbiota in neonates is crucial because those bacteria are the first to colonize the sterile intestine of the neonates and, thus, have a significant effect on the host. Initial colonization is also relevant to the final composition of the permanent microbiota in adults. Bifidobacteria are predominant in the fecal microbiota of infants, and, therefore, they are important to an understanding of how commensal bifidobacteria is established in the intestine of infants. While the mother’s bifidobacteria are considered to significantly influence the infant’s bifidobacteria, it is not clear whether a specific bifidobacterial strain transmits vertically from mother to infant and what factors of the mother before delivery influence the establishment of intestinal bifidobacteria in infants. This review focuses on the impact of maternal bifidobacteria on the development of gut bifidobacteria in the infant and suggests that there is cumulative evidence regarding bifidobacterial transfer from the maternal gut or breast milk to the infant gut. Full article
(This article belongs to the Special Issue Probiotics and Prebiotics)
Open AccessReview The Potential Therapeutic Efficacy of Lactobacillus GG in Children with Food Allergies
Pharmaceuticals 2012, 5(6), 655-664; doi:10.3390/ph5060655
Received: 16 May 2012 / Revised: 4 June 2012 / Accepted: 6 June 2012 / Published: 19 June 2012
Cited by 8 | PDF Full-text (570 KB) | HTML Full-text | XML Full-text
Abstract
Food allergy (FA) continues to be a growing health concern for infants living in Western countries. The long-term prognosis for the majority of affected infants is good, with 80–90% naturally acquiring tolerance by the age of five years. However, recent studies suggest [...] Read more.
Food allergy (FA) continues to be a growing health concern for infants living in Western countries. The long-term prognosis for the majority of affected infants is good, with 80–90% naturally acquiring tolerance by the age of five years. However, recent studies suggest that the natural history of FA is changing, with an increasing persistence until later ages. The pathogenesis of FA as well as oral tolerance is complex and not completely known, although numerous studies implicate gut-associated immunity and enteric microflora, and it has been suggested that an altered composition of intestinal microflora results in an unbalanced local and systemic immune response to food allergens. In addition, there are qualitative and quantitative differences in the composition of gut microbiota between patients affected by FA and healthy infants. These findings prompted the concept that specific beneficial bacteria from the human intestinal microflora, designated probiotics, could restore intestinal homeostasis and prevent or alleviate allergy, at least in part by interacting with the intestinal immune cells. Full article
(This article belongs to the Special Issue Probiotics and Prebiotics)

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