Different Temperature Treatments of Millet Grains Affect the Biological Activity of Protein Hydrolyzates and Peptide Fractions.

The objective of this study was to analyze millet protein hydrolyzates and peptide fractions with molecular mass under 3.0 kDa obtained from grains treated with different temperature values as inhibitors of angiotensin-converting enzyme (ACE), α-amylase, and α-glucosidase activity. The protein fractions were hydrolyzed in vitro in gastrointestinal conditions and the highest degree of hydrolysis was noted for globulin 7S obtained from control grains (98.33%). All samples were characterized by a high peptide bioaccessibility index, which was 23.89 for peptides obtained from globulin 11S after treatment with 100 °C. The highest peptide bioavailability index was noted for peptides obtained from globulin 11S after the treatment with 65 °C (2.12). The highest potential metabolic syndrome inhibitory effect was determined for peptide fractions obtained from the prolamin control (IC50 for ACE and α-amylase was 0.42 and 0.11 mg/mL, respectively) and after the 100 °C treatment (IC50 for ACE and α-glucosidase was 0.33 and 0.12 mg/mL, respectively) and from globulin 11S after the 65 °C treatment (IC50 0.38 and 0.05 for ACE and α-glucosidase, respectively). The effect of these samples on endothelial cell HECa10 was determined. The sequences of potential inhibitory peptides were identified as GEHGGAGMGGGQFQPV, EQGFLPGPEESGR, RLARAGLAQ, YGNPVGGVGH, and GNPVGGVGHGTTGT.

Use of phytochemomics to evaluate the bioavailability and bioactivity of antioxidant peptides of soybean ß-conglycinin.

This research investigates how in vitro digestion contributes to the release of antioxidant peptides crypted in soybean ß-conglycinin (7S) and its deglycosylated form (D7S). It also investigates the uptake of the bioactive peptides by human intestinal Caco-2 cells using a bicameral system, and their effect on the antioxidant cell defense. Phytochemomics is used as a tool for achieving this goal. The peptides are obtained by mimicking human physiological gastrointestinal digestion conditions. The antioxidant capacity of the peptides is tested by ABTS•(+) radical cation decolorization (2,2'-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS)) and oxygen radical absorbance capacity assays. The antioxidant power of the peptides recovered from the basolateral chamber is also evaluated by an analysis of biomarkers of cellular oxidative stress such as cell proliferation, alkaline phosphatase, and secretion of nitric oxide, lipid peroxidation, superoxide dismutase and catalase. Peptides from D7S were more active than those of 7S in the modulation of the cell proliferation, oxidative status and differentiation of Caco-2 cells treated with H2 O2 . Differences in the bioactivity of the peptides of both proteins can be explained by analysis of the structural data obtained by mass spectrophotometry. Our findings support the bioavailability of antioxidant peptides of 7S. The antioxidant properties of 7S soy protein were influenced by events such as glycosylation, digestion, and absorption. Deglycosylation seems to be an innovative strategy for improving the properties of 7S. Deglycosylation might enhance 7S antioxidant power and reduce its immunoreactivity. The combined use of advanced analytical techniques and biochemical analyses (phytochemomics) has been a key part of this study.

Study of the variables which influence the impregnation of globules, compressed tablets and tablet triturates used in homeopathy

Globules, compressed tablets and tablet triturates are solid dosage forms used in homeopathy. Divergences can be noted between the preparation techniques described in official compendiums as well as those applied in homeopathic pharmacies. The difficulty associated with standardization of the impregnation of these dosage forms occurs due to the lack of detail provided for the techniques in the literature, leaving it up to each pharmacy to decide on the exact method of preparation. The objective was to optimize the impregnation technique, through investigating the variables that influence the impregnation of globules, compressed tablets and tablet triturates, applying the statistical tool of factorial design. The independent variables were the dosage form, percentage and type of impregnation and drying temperature, and the dependent variables were the mass gain, disintegration time, friability and hardness. For the globules, the greatest mass gain was for 10% impregnation and drying at 20 ºC. For the tablet triturates and compressed tablets the greatest mass gain was for 15% impregnation and there was no difference between the results obtained using simple and triple impregnation or different drying temperatures. The results can contribute to improving the final product quality, besides aiding in the establishment of standardized techniques for the official compendiums.

Glóbulos, comprimidos e tabletes são formas farmacêuticas sólidas utilizadas em homeopatia. Constatam-se divergências entre técnicas de preparação descritas nos compêndios oficiais, bem como em farmácias homeopáticas. A dificuldade de padronização na impregnação destas formas farmacêuticas também ocorre devido à falta de detalhamento das técnicas na literatura existente, deixando para cada farmácia a escolha de como executá-las. O objetivo foi otimizar a técnica de impregnação, através do estudo de variáveis que interferem na impregnação de glóbulos, comprimidos e tabletes, aplicando como ferramenta estatística planejamento fatorial. As variáveis foram forma farmacêutica, percentual e tipo de impregnação e temperatura de secagem, sendo o ganho de massa, tempo de desintegração, friabilidade e dureza as variáveis dependentes. Para os glóbulos, observou-se maior ganho de massa quando impregnados a 10% e secagem realizada a 20 ºC. Para os tabletes e comprimidos, constatou-se maior ganho de massa quando impregnados a 15%, sendo que não houve diferença na impregnação simples ou tríplice nem nas diferentes temperaturas de secagem. Os resultados obtidos podem contribuir para a melhoria da qualidade do produto final, além de auxiliar no estabelecimento de técnicas padronizadas para os compêndios oficiais.

Bioresorbable polyelectrolyte amphiphiles as nanosized carriers for lipophilic drug solubilization and delivery.

Starting from drug carriers and drug-delivery systems described in the literature, this article examines more specifically those that are relevant to the field of nanocarriers composed of a degradable hydrophilic polyelectrolyte backbone with pendent hydrophobes arranged to form comb-like co-polymers. Advantage is taken of the nanosized, lipophilic pocket-bearing multimolecule aggregates formed in aqueous media by such amphiphilic polyelectrolytes to accommodate water-insoluble drug molecules according to a phenomenon named macromolecular microencapsulation. Comments are also made on the criteria to be fulfilled by nanosized polymeric drug carriers. These carriers require a size or molar mass high enough to avoid renal excretion and thus be retained in the body for longer periods of time than the free drug. Since they nevertheless have to be eliminated from the body (bioresorption), they must be degraded at the end of use. In situ degradation is an important criterion that is taken into account by using special polyelectrolytes that belong to the class of the so-called "artificial biopolymers". Artificial biopolymers are made of pro-metabolite units than generate metabolite upon degradation, thus resulting in metabolisation of degradation end-products if intermediates are not excreted before. Aggregates of amphiphilic polyanions derived from malic acid, citric acid, L-lysine and L-serine are presented to support the concept of macromolecular microencapsulation. Comparison is made with non-polyelectrolytic systems with similar structures.