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Foods (Basel, Switzerland) Feb 2023The increase in meat consumption could adversely affect the environment. Thus, there is growing interest in meat analogs. Soy protein isolate is the most common primary...
The increase in meat consumption could adversely affect the environment. Thus, there is growing interest in meat analogs. Soy protein isolate is the most common primary material to produce low- and high-moisture meat analogs (LMMA and HMMA), and full-fat soy (FFS) is another promising ingredient for LMMA and HMMA. Therefore, in this study, LMMA and HMMA with FFS were manufactured, and then their physicochemical properties were investigated. The water holding capacity, springiness, and cohesiveness of LMMA decreased with increasing FFS contents, whereas the integrity index, chewiness, cutting strength, degree of texturization, DPPH free radical scavenging activity, and total phenolic content of LMMA increased when FFS contents increased. While the physical properties of HMMA decreased with the increasing FFS content, its DPPH free radical scavenging activity and total phenolic contents increased. In conclusion, when full-fat soy content increased from 0% to 30%, there was a positive influence on the fibrous structure of LMMA. On the other hand, the HMMA process requires additional research to improve the fibrous structure with FFS.
PubMed: 36900528
DOI: 10.3390/foods12051011 -
Cell Structure and Function Oct 1999This minireview summarizes the syntheses of various purinenucleotide analogues and their effects on microtubule (Mt) assembly. 27 analogues were so far synthesized and,... (Review)
Review
This minireview summarizes the syntheses of various purinenucleotide analogues and their effects on microtubule (Mt) assembly. 27 analogues were so far synthesized and, together with 3 analogues commercially available (ITP, XTP and dGTP), their effects on Microtubule assembly were investigated. The positions C2, C6, C8, and ribose moiety of purine nucleotides were modified or substituted. It was found that the microenvironments of the purine base and ribose moiety are important for the nucleotides to support Mt assembly. Introduction of amino group into position C2 of ATP, formation of 2-amino ATP, caused Mt assembly substantially. 2-Amino deoxy ATP and deoxy GTP are more potent than GTP in supporting assembly. The introduction of reactive thiol group into C6 (6-SH-GTP) largely reduces the activity of the analogue to support assembly. However, sequestering reactivity of the thiol group by association with methyl group largely recovers the ability of the analogue to promote assembly. Free rotation of the glycosidic linkage was found to be also innevitable in promoting assembly, as the introduction of sulfur atom between C8 of the purine base and C2' of the ribose moiety (formation of 8,2'-S-cyclo purine nucleotides) caused total inhibition. Purinenucleoside triphosphate supports assembly better than GTP but the deoxy-type analogues are totally inhibitory. 2-Amino-8-hydroxy ATP and other analogues support assembly much better than does GTP. However, their diphosphate analogues are totally incapable of supporting assembly. Introduction of a bulky fluorescent probes into C3' can be made to visualize the fluorescent signal in assembled Mts. Together with the suggestions proposed from electron chrystallography of zinc-induced tubulin sheets, interactions of the purine base and ribose moieties with surrounding amino acid residues are discussed.
Topics: Adenosine Diphosphate; Adenosine Triphosphate; Cyclization; Fluorescent Dyes; Guanosine Diphosphate; Guanosine Triphosphate; Microtubules; Molecular Structure; Protein Binding; Purine Nucleotides; Spectrometry, Fluorescence; Spectrophotometry, Ultraviolet; Structure-Activity Relationship; Tubulin; ortho-Aminobenzoates
PubMed: 15216887
DOI: 10.1247/csf.24.305 -
Postgraduate Medical Journal Jul 1996The long-acting analogues of somatostatin have an established place in the medical treatment of patients with neuroendocrine tumours. They act through binding with... (Review)
Review
The long-acting analogues of somatostatin have an established place in the medical treatment of patients with neuroendocrine tumours. They act through binding with specific, high-affinity membrane receptors. Somatostatin analogue therapy is an effective and safe treatment for most growth hormone and thyrothropin-secreting pituitary adenomas. The potential therapeutic consequences of the presence of somatostatin receptors on clinically 'nonfunctioning' pituitary tumours are still uncertain. Somatostatin analogues are not useful in the treatment of patients with prolactinomas, or adrenocorticotropin (ACTH)-secreting adenomas. However, the somatostatin analogue octreotide suppressed pathological ACTH release in some patients with Nelson's syndrome and ACTH and cortisol secretion in several patients with Cushing's syndrome caused by ectopic ACTH secretion. Somatostatin analogues are effective in the sympatomatic treatment of most (metastatic) pancreatic islet cell tumours and most (metastatic) carcinoids. In some of these patients, they also induce tumour stabilisation or reduction. In some patients with (metastatic) medullary thyroid carcinomas, continuous treatment with very high doses of octreotide can be of temporary relief. The clinical effectiveness of somatostatin analogues in patients with small cell lung cancer is currently under investigation. Long-term therapy with somatostatin analogues of catecholamine-secreting (malignant) paragangliomas and phaeochromocytomas has not shown clinical benefits.
Topics: Antineoplastic Agents; Apudoma; Hormone Antagonists; Humans; Neuroendocrine Tumors; Octreotide; Peptides, Cyclic; Pituitary Neoplasms; Receptors, Somatostatin; Somatostatin
PubMed: 8935599
DOI: 10.1136/pgmj.72.849.403 -
Alimentary Pharmacology & Therapeutics Jan 2010The discovery of somatostatin (SST) and the synthesis of a variety of analogues constituted a major therapeutic advance in the treatment of gastroenteropancreatic... (Review)
Review
BACKGROUND
The discovery of somatostatin (SST) and the synthesis of a variety of analogues constituted a major therapeutic advance in the treatment of gastroenteropancreatic neuroendocrine (carcinoid) tumours (GEP-NETs). They currently provide the most efficient treatment to achieve symptomatic relief and have recently been demonstrated to inhibit tumour growth.
AIM
To review 35 years of experience regarding the clinical application and efficacy of SST analogues.
METHODS
The PubMed database (1972-2009) was searched using somatostatin as a search term with combinations of terms including 'treatment'; 'neuroendocrine'; 'carcinoid'; 'tumor'; 'octreotide'; 'lanreotide' and 'pasireotide'.
RESULTS
In a review of 15 studies including 481 patients, the slow-release formulations Sandostatin LAR and Somatuline SR/Autogel achieved symptomatic relief in 74.2% (61.9-92.8%) and 67.5% (40.0-100%), biochemical response in 51.4% (31.5-100%) and 39.0% (17.9-58%), and tumour response in 69.8% (47.0-87.5%) and 64.4% (48.0-87.0%) respectively. Novel SST analogues like SOM230 (pasireotide) that exhibit pan SST receptor activity and analogues with high affinity to specific somatostatin receptor (sstr) subtypes may further advance the field, but efficacy studies are lacking.
CONCLUSION
As more precise understanding of NET cell biology evolves and molecular biological tools advance, more accurate identification of individual tumours sstr profile will probably facilitate a more precise delineation of SST analogue treatment.
Topics: Antineoplastic Agents; Carcinoid Tumor; Gastrointestinal Neoplasms; Hormones; Humans; Pancreatic Neoplasms; Receptors, Somatostatin; Somatostatin; Treatment Outcome
PubMed: 19845567
DOI: 10.1111/j.1365-2036.2009.04174.x -
The Netherlands Journal of Medicine Dec 2012GLP-1 analogues have been proven to be effective in the treatment of type 2 diabetes mellitus. They stimulate insulin production and secretion, and suppress glucagon... (Review)
Review
GLP-1 analogues have been proven to be effective in the treatment of type 2 diabetes mellitus. They stimulate insulin production and secretion, and suppress glucagon secretion, depending on the blood glucose level. They also have an effect on the brain, enhancing satiety, and on the gut, where they delay gastric emptying. Theoretically, in type 2 diabetes mellitus patients, the combination of a GLP-1 analogue with insulin seems attractive, because of the weight loss perceived in users of GLP-1 analogues in contrast to the weight gain seen in most patients starting insulin therapy, leading to even more insulin resistance. There are only a few randomised controlled trials which have studied this combination and several uncontrolled studies, which will be reviewed here.
Topics: Blood Glucose; Diabetes Mellitus, Type 2; Drug Therapy, Combination; Glucagon; Glucagon-Like Peptide 1; Humans; Insulin; Insulin Resistance; Treatment Outcome
PubMed: 23230012
DOI: No ID Found -
Foods (Basel, Switzerland) Feb 2023Fish products are consumed by human beings as a high-quality protein source. However, overfishing, and pollution puts out an urgent call to seek a new strategy to... (Review)
Review
Fish products are consumed by human beings as a high-quality protein source. However, overfishing, and pollution puts out an urgent call to seek a new strategy to substitute fish protein for secure eco-sustainability. Plant-based fish analogs, which mimic the structure, texture, and flavor of fish meat products, are a rapid-growing segment of the food products. The purpose of this review is to discuss the feasibility and potential strategies for developing plant-based fish analog. The nutritional properties, especially the protein quality of plant-based fish analogs, were discussed. Furthermore, a thorough comparison was made between fish and terrestrial animal muscle structures, including both macroscopical and microscopical structures. Potential processing technologies for producing plant-based fish analogs from plant proteins and approaches for the characterization of the fish analog structures were elaborated. Comparing all the current processing techniques, extrusion is the predominately used technique in the current industry. At the same time, 3D-printing and electrospinning have shown the prominent potential of mimicking fish muscle structure as bottom-up approaches. Finally, key challenges and future research were discussed for the potential commercialization of plant-based fish analogues. The primary focus of this review covers the innovative works that were indexed in the Web of Science Core Collection in the past five years.
PubMed: 36766143
DOI: 10.3390/foods12030614 -
Journal of Experimental Child Psychology Oct 2022Prior research presents a mixed picture regarding the circumstances under which children transfer learning of problem solutions from fantastical stories to real-world...
Prior research presents a mixed picture regarding the circumstances under which children transfer learning of problem solutions from fantastical stories to real-world problems. Two experiments examined 3- to 5-year-old children's transfer of learning from fantastical storybooks that systematically varied in the fantastical abilities of storybook characters. In both experiments, participants heard stories about a character solving physical problems, and then participants attempted to solve analogous real-world problems. In Experiment 1, children heard stories that varied the fantastical abilities and practices of the protagonist; characters either did or did not have the ability to violate physical laws and did or did not use magic to help in solving a problem. Children were more likely to transfer problem solutions from the stories in which characters were presented as having the ability to violate real-world physical laws. In Experiment 2, the fantastical abilities of the characters varied by whether the characters were described as real, as pretend but living in a world where no physical laws could be violated, as pretend and living in a world where some physical laws could be violated, or as pretend and living in a world where many physical laws could be violated. Other than varying the characters' abilities, all characters used realistic solutions to solve the problem. Again, transfer was higher for children who heard about characters with the ability to violate real-world laws. The findings suggest that fantastical stories in which characters have the ability to do impossible things but use realistic solutions to problems can be effective in teaching children how to solve physical problems.
Topics: Child Development; Child, Preschool; Fantasy; Humans; Transfer, Psychology
PubMed: 35679778
DOI: 10.1016/j.jecp.2022.105474 -
BMC Biology Sep 2020Resistance to front-line antimalarials (artemisinin combination therapies) is spreading, and development of new drug treatment strategies to rapidly kill Plasmodium spp....
BACKGROUND
Resistance to front-line antimalarials (artemisinin combination therapies) is spreading, and development of new drug treatment strategies to rapidly kill Plasmodium spp. malaria parasites is urgently needed. Azithromycin is a clinically used macrolide antibiotic proposed as a partner drug for combination therapy in malaria, which has also been tested as monotherapy. However, its slow-killing 'delayed-death' activity against the parasite's apicoplast organelle and suboptimal activity as monotherapy limit its application as a potential malaria treatment. Here, we explore a panel of azithromycin analogues and demonstrate that chemical modifications can be used to greatly improve the speed and potency of antimalarial action.
RESULTS
Investigation of 84 azithromycin analogues revealed nanomolar quick-killing potency directed against the very earliest stage of parasite development within red blood cells. Indeed, the best analogue exhibited 1600-fold higher potency than azithromycin with less than 48 hrs treatment in vitro. Analogues were effective against zoonotic Plasmodium knowlesi malaria parasites and against both multi-drug and artemisinin-resistant Plasmodium falciparum lines. Metabolomic profiles of azithromycin analogue-treated parasites suggested activity in the parasite food vacuole and mitochondria were disrupted. Moreover, unlike the food vacuole-targeting drug chloroquine, azithromycin and analogues were active across blood-stage development, including merozoite invasion, suggesting that these macrolides have a multi-factorial mechanism of quick-killing activity. The positioning of functional groups added to azithromycin and its quick-killing analogues altered their activity against bacterial-like ribosomes but had minimal change on 'quick-killing' activity. Apicoplast minus parasites remained susceptible to both azithromycin and its analogues, further demonstrating that quick-killing is independent of apicoplast-targeting, delayed-death activity.
CONCLUSION
We show that azithromycin and analogues can rapidly kill malaria parasite asexual blood stages via a fast action mechanism. Development of azithromycin and analogues as antimalarials offers the possibility of targeting parasites through both a quick-killing and delayed-death mechanism of action in a single, multifactorial chemotype.
Topics: Antimalarials; Azithromycin; Malaria; Malaria, Falciparum; Malaria, Vivax; Plasmodium falciparum; Plasmodium knowlesi; Plasmodium vivax
PubMed: 32993629
DOI: 10.1186/s12915-020-00859-4 -
Alimentary Pharmacology & Therapeutics Aug 2003Somatostatin and its analogue octreotide have been used for two decades to treat oesophageal variceal haemorrhage. The drug was introduced because of its capacity to... (Review)
Review
Somatostatin and its analogue octreotide have been used for two decades to treat oesophageal variceal haemorrhage. The drug was introduced because of its capacity to decrease portal venous pressure without major side effects. In clinical trials assessing the efficacy of somatostatin and long-acting analogues in arresting variceal haemorrhage, conflicting results have been obtained. Furthermore, in haemodynamic studies evaluating the effects of somatostatin and analogues in patients with cirrhosis, divergent effects were observed. The main reason for these differences is probably related to different affinities of the drugs for different somatostatin receptor subtypes. The effects of somatostatin and analogues are mediated via five different G-protein coupled receptors (somatostatin receptor subtypes 1-5), which regulate the activity of ion channels (Ca2+, K+, Na+ and Cl-) and enzymes (adenyl cyclase, phospholipase C, phospholipase A2, phosphoinositide 3-kinase and guanylate cyclase) responsible for the synthesis or degradation of intracellular second messengers including cyclic AMP, inositol 1,4,5-trisphosphate, diacylglycerol and cyclic GMP. Despite universal use of somatostatin, the cellular and biochemical mechanisms of its effects in portal hypertension are relatively poorly studied and remain incompletely understood. In this review, we summarize relevant signal transduction of somatostatin and analogues, the haemodynamic effects of the drugs and the possible mechanisms by which these effects are mediated.
Topics: Blood Flow Velocity; Blood Pressure; Hormones; Humans; Hypertension, Portal; Receptors, Somatostatin; Somatostatin
PubMed: 12940922
DOI: 10.1046/j.1365-2036.2003.01657.x -
PloS One 2023This study involves the in-vitro and in-vivo anti-TB potency and in-vivo safety of Transitmycin (TR) (PubChem CID:90659753)- identified to be a novel secondary...
This study involves the in-vitro and in-vivo anti-TB potency and in-vivo safety of Transitmycin (TR) (PubChem CID:90659753)- identified to be a novel secondary metabolite derived from Streptomyces sp (R2). TR was tested in-vitro against drug resistant TB clinical isolates (n = 49). 94% of DR-TB strains (n = 49) were inhibited by TR at 10μg ml-1. In-vivo safety and efficacy studies showed that 0.005mg kg-1 of TR is toxic to mice, rats and guinea pigs, while 0.001mg kg-1 is safe, infection load did not reduce. TR is a potent DNA intercalator and also targets RecA and methionine aminopeptidases of Mycobacterium. Analogue 47 of TR was designed using in-silico based molecule detoxification approaches and SAR analysis. The multiple targeting nature of the TR brightens the chances of the analogues of TR to be a potent TB therapeutic molecule even though the parental compound is toxic. Analog 47 of TR is proposed to have non-DNA intercalating property and lesser in-vivo toxicity with high functional potency. This study attempts to develop a novel anti-TB molecule from microbial sources. Though the parental compound is toxic, its analogs are designed to be safe through in-silico approaches. However, further laboratory validations on this claim need to be carried out before labelling it as a promising anti-TB molecule.
Topics: Animals; Guinea Pigs; Mice; Rats; Mycobacterium tuberculosis; Intercalating Agents; Laboratories; Product Labeling; Research Design; Streptomyces
PubMed: 36867599
DOI: 10.1371/journal.pone.0282454