bluuebunny/crossref_metadata_2025_split huggingface dataset:
Effects of Fasting andPhoenix dactyliferaon the Expression of Major Drug- Metabolizing Enzymes in the Mouse Livers
Authors: Balasmeh Ruba , Jarrar Yazun , Al-Sheikh Iyad , Alshaiah Hamza , Jarrar Qais , Alani Raad , Abudahab Sara 
Published: August 2022

Aims:This study aimed to investigate the effects of consuming Phoenix dactylifera and fasting on the mRNA expression of major hepatic drug-metabolizing enzymes in mice.Methods:Phoenix dactylifera ethanolic extract was analyzed using LC-MS/MS. We used forty-two male Balb/c mice, which were treated with low (300 mg/kg) and high (2583 mg/kg) doses of Phoenix dactylifera and fasted for 24 hours, two weeks, and one month. Then, we analyzed the expression of cyp3a11, cyp2c29, cyp2d9, and ugt2b1 using real-time polymerase chain reaction assay. In addition, we assessed the relative liver weights of the mice and the hepatic phathohistological alterations.Results:We found that Phoenix dactylifera ethanolic extract contained 38 phytochemical compounds, mainly kaempherol, campesterol, lutein, apigenin, genistein, and isoquercetin. Fasting significantly upregulated the mRNA expression of several drug-metabolizing enzymes in a time-dependent manner and we showed that consuming the low dose of Phoenix dactylifera significantly upregulated the expression of drug-metabolizing enzymes more than the high dose. The results of the histological examinations and relative liver weight showed that fasting and consuming of Phoenix dactylifera did not cause any toxicological alterations in the liver of the mice.Conclusion:It is concluded from this study that fasting and consuming of Phoenix dactylifera upregulated the mRNA expression of major drug-metabolizing enzymes in mouse livers. These findings may explain, at least partly, the variation of drug response during fasting in the month of Ramadan and would direct future clinical studies in optimizing the dosing of pharmacotherapeutic regimen.
Peptide-based Nanomaterials: Self-assembly and Applications
Authors: Zou Qian Li , Yong Jin , Tan Lina , Huan Ren , Wu Li Fang , Bao Yanni , Ma Yu Chen 
Published: August 2022

Abstract:
The self-assembly behavior of polypeptides is common in nature. Compared with monopeptides, polypeptide-based self-assembled nanomaterials with ordered structures have good thermal stability, mechanical stability, semi-conductivity, piezoelectric and optical properties. In recent years, the self-assembly of polypeptides has become a hot topic in the material science and biomedical field. By reasonably adjusting the molecular structure of the polypeptide and changing the external environment of the polypeptide, the polypeptide can be self-assembled or triggered by non-covalent bonding forces such as hydrogen bond, hydrophobicity, and π - π accumulation to form specific polypeptide assemblies such as nanoparticles, hydrogels, nanofibers, and micelles. Due to good biocompatibility and controllable degradability, polypeptide-based self-assembled nanomaterials have been widely used in the fields of nanotechnology, imaging technology, biosensor, and biomedical science. As a new drug delivery system, the polypeptide-drug conjugate has the advantages of low toxicity, high efficiency, enhanced drug stability, and avoiding side effects. This paper reviews the research progress of polypeptide-drug self-assembly nanostructure in recent years. Several structural models of polypeptide self-assembly technology and the mechanism of polypeptide self-assembly are introduced. Then the assembly form of polypeptide-drug self-assembly and the application of self-assembly compound therapy is described.
Less Known but Clinically Relevant Comorbidities of Atrial Fibrillation: A Narrative Review
Authors: Koraćević Goran , Stojković Milan , Stojanović Milovan , Zdravković Marija , Simić Dragan , Šalinger-Martinović Sonja , Đorđević Dragan , Damjanović Miodrag , Đorđević-Radojković Danijela , Koraćević Maja 
Published: August 2022

Background:The important risk factors for atrial fibrillation (AF) in the general population are not always equally important in specific and relatively prevalent diseases.Objective:The main goal of this narrative review is to focus attention on the presence and the relationship of AF with several important diseases, such as cancer or sepsis, in order to: 1) stimulate further research in the field, and 2) draw attention to this relationship and search for AF in clinical practice.Methods:We searched PubMed, SCOPUS, Elsevier, Wiley, Springer, Oxford Journals, Cambridge, SAGE, and Google Scholar for less-known comorbidities of AF. The search was limited to publications in English. No time limits were applied.Results:AF is widely represented in cardiovascular and other important diseases, even in those in which AF is rarely mentioned. In some specific clinical subsets of AF patients (e.g., patients with sepsis or cancer), the general risk factors for AF may not be so important. Patients with new-onset AF have a several-fold increase in relative risk of cancer, deep vein thrombosis, and pulmonary thromboembolism (PTE) during the follow-up.Conclusion:AF presence, prognosis, and optimal therapeutic approach are insufficiently recognised in several prevalent diseases, including life-threatening ones. There is a need for a better search for AF in PTE, pulmonary oedema, aortic dissection, sepsis, cancer and several gastrointestinal diseases. Improved AF detection would influence treatment and improve outcomes.
Highly Efficient Synthesis of Imidazolecarboxylate Salts via Sequential Nucleophilic Addition-Intramolecular Cyclization Reactions
Authors: Azizian Javad , Nazarahari Maryam 
Published: August 2022

Abstract:In this work, we used a highly efficient and easy approach for synthesizing imidazolecarboxylate salt through the reaction between α-amidino carboxylic acids and α-halo ketones with as readily available starting materials in the presence of KHCO3 at THF under reflux. Targeted synthesis of this type of imidazole bearing the carboxylic acid group in a single structure, in addition to the biological properties enriched as a ligand, is very popular in the manufacture of catalysts. The salient features of this protocol include eco-friendly, high atom-economical, easy and mild conditions that led to the production of all products with high yields. Furthermore, all products were purified without the need for column chromatography through the GAP chemistry (group-assisted purification chemistry) technique.
Comprehensive Insight into Synthetic Strategies of Enigmol and Its Analogs
as Therapeutic Agents
Authors: Kaur Parleen , Singh Vasundhara 
Published: August 2022

Abstract:
1-Deoxysphingolipids are a class of sphingolipids which lacks the primary hydroxyl group
(C1-OH). Hence, it does not get converted/degraded to complex corresponding products like sphingosine-1-phosphate (SIP), a pro-mitotic. Enigmol, an orally bioavailable 1-deoxyphingolipid has shown
potential against various different types of cancer cells along with impressive cytotoxic/antiproliferative properties. Due to its unique structural properties, Enigmol and its analogs have
attracted considerable attention from synthetic organic chemists. This review provides an overview of
all the synthetic approaches being followed for the synthesis of Enigmol and its structural analogs.
Potential Role of Bilirubin in Preventing Retinopathy of Prematurity
Authors: Zakerihamidi Maryam , Boskabadi Hassan , Shoeibi Naser , Bagheri Fatemeh , Pourbadakhshan Nafiseh , Moradi Ali 
Published: August 2022

Background:One of the most common problems in preterm neonates is retinopathy of prematurity (ROP). It has been shown antioxidants may be effective in preventing the development and progression of ROP. Considering the antioxidant properties of bilirubin, we decided to investi-gate the bilirubin level in neonates with ROP and compare it with healthy neonates.Methods:This case-control study was performed on VLBW neonates admitted to the NICU of Ghaem Hospital in Mashhad between 2014 and 2020 for a Jaundice evaluation. Complete neonate’s characteristics, maternal history and laboratory results were collected in a questionnaire. Then the neonates were examined for ROP by a fellowship of the retina of an ophthalmologist at 32 weeks or four weeks after birth. The highest bilirubin levels during their hospitalization were also recorded.Results:Of 427 neonates examined, 121 (37.7%) had a normal eye examination, and 266 (62.3%) had ROP. The mean weight, gestational age and bilirubin were 1455.8 ± 431.4 grams, 31.6 ± 2.3 weeks and 8.8 ± 2.4 mg/dl, respectively. There was a significant difference between controls and neonates with ROP with regard to birth weight, duration of intermittent positive pressure ventilation (IPPV), duration of oxygen therapy, first and fifth minute Apgar scores, the maximum level of bili-rubin and gestational age (P < 0.05). It was observed that the maximum level of bilirubin was lower in neonates with higher stages of ROP.Conclusion:According to the results of this study, higher levels of bilirubin in neonates may be a protective factor against ROP. Moreover, increased levels of bilirubin are associated with reduced severity of ROP. Therefore, prophylaxis phototherapy in premature infants may need to be recon-sidered.
MicroRNA 155, Factor XIII and Type 2 Diabetes Mellitus and Coronary
Heart Disease
Authors: Ntanyane Phasha Marry-Ann , Soma Prashilla , Rooy Mia-Jeanne Van , Phulukdaree Alisa 
Published: August 2022

Abstract:
There is a rise in the number of individuals diagnosed with type 2 diabetes mellitus
(T2DM) in South Africa. Cardiovascular disease is among the macrovascular complication of type
2 diabetes mellitus and accounts for the high mortality rate in patients with T2DM. The disease is
characterized by insulin resistance, hyperglycaemia, oxidative stress, inflammation, hypofibrinolysis
and hypercoagulation. The impairment of fibrinolysis, hyperactivation of coagulation and the
inflammatory pathways result in an increased risk of developing coronary heart disease. Factor
XIII-A is one of the key coagulation factors that play a crucial role in the last stage of the coagulation
cascade, and it has been shown to play a critical role in the development of thrombotic diseases.
In addition, several studies show the influence of FXIII-A polymorphisms on thrombotic diseases.
The influence of genetic variations such as single nucleotide variants and gene expression
regulators (micro-RNAs) are important factors involved in the hyperactivation of coagulation and
hypofibrinolysis. Thus, this review aims to summarise key aspects of coagulation, FXIII-A expression,
potential FXIII-A genetic variations and epigenetic mediators (micro-RNA-155) in T2DM
and patients with coronary artery disease.
Design, Synthesis and Biological Evaluation of Novel N-Alkyl-4-Methyl-2,2- Dioxo-1H-2λ6,1-Benzothiazine-3-Carboxamides as Promising Analgesics
Authors: Georgiyants Victoriya , Ukrainets Igor , Burian Anna , Voloshchuk Natali , Taran Illia , Shishkina Svitlana , Severina Hanna , Grinevich Lina , Sim Galina , Burian Kateryna 
Published: August 2022

Introduction:An analysis of the literature on the painkillers long used in traditional medicine, which are isolated from plant materials, has shown that many of them are alkylamides of various carboxylic acids. This fact served as the basis for the study of a large group of N-alkyl-4- methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamides as potential new analgesics. The objects of the study were synthesized in the traditional way involving the initial conversion of 4-methyl- 2,2-dioxo-1H-2λ6,1- benzothiazine-3-carboxylic acid to imidazolide, in which imidazolide was used as an acylating agent. The method is simple to implement and, as a rule, gives high yields of final alkylamides. However, in reaction with sterically hindered tert-butylamine, along with the “normal” product, an unexpected formation of N-tert-butyl-4-methyl-1-(4-methyl-2,2-dioxo-1H-2λ6,1- benzothiazine-3-carbonyl)-2,2-dioxo-2λ6,1-benzothiazine-3-carboxamide was observed, which was characterized by X-ray diffraction analysis as a monosolvate with N,N-dimethylformamide. These synthetic problems can be avoided using a more powerful acylating agent, 4-methyl-2,2-dioxo-1H- 2λ6,1- benzothiazine-3-carbonyl chloride.Background:A large group of new N-alkyl-4-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3- carboxamides was synthesized.Objective:On the basis of molecular docking, some derivatives of N-alkyl-4-methyl-2,2-dioxo-1H- 2λ6,1-benzothiazine-3-carboxamides have been designed. Their preliminary structure-activity relationships (SAR) have been studied. The most rational approaches to the synthesis of lead compounds have been developed. The most active compounds have shown high anti-inflammatory and analgesic activities.Methods:The structure of all compounds prepared has been confirmed by the data of elemental analysis, 1H- and 13C NMR spectroscopy, and electrospray ionization liquid chromato-mass spectrometry. For rational drug design, optimization of further pharmacological screening and prediction of a possible mechanism of pharmacological action, molecular docking has been performed. For the determination of activity, pharmacological studies have been carried out.Results:Pharmacological tests have determined that the transition from N-aryl(heteroaryl) alkylamides to “pure” N-alkylamides we carried out is accompanied by a significant reduction and even complete loss of anti-inflammatory effect with remaining analgesic activity.Conclusion:According to the studies, compounds from N-alkyl-4-methyl-2,2-dioxo-1H-2λ6,1- benzothiazine-3-carboxamides are potential anti-inflammatory and analgesic agents.
Recent Insights on Synthetic Methods and Pharmacological Potential in
Relation with Structure of Benzothiazoles
Authors: Yadav Ranjeet Kumar , Kumar Rajnish , Singh Himanshu , Mazumdar Avijit , Salahuddin  , Chauhan Bharti , Abdullah Mohd. Mustaqeem 
Published: August 2022

Abstract:
Benzothiazole is a bicyclic heterocyclic compound that contains benzene fused with 1, 3-
thiazole ring. Several researches established the potential of benzothiazoles as important moiety in
various adverse pharmacological conditions. Benzothiazole and its derivatives have been in use and
marketed as anti-microbial, anti-inflammatory, anti-diabetic, anti-oxidant, anti-convulsant, antitumor,
etc. The variations in pharmacological potentials of benzothiazole and its derivatives have
been rational with their chemical structure. Nowadays, hybridization of two or more pharmacophores
to synthesize a single molecule with potent pharmacological action is used. This helps to
synergize pharmacological properties, make interaction possible with many targets, or minimize the
adverse effects associated with them. Several synthetic approaches have been reported for benzothiazole
and its derivatives. In this present review, we focused on recently adopted synthetic approaches
for the synthesis of the benzothiazole nucleus and its derivatives. The structure-activity relationship
in relation to different pharmacological activities has also been highlighted to provide a good
understanding to the researchers for future research on benzothiazoles.
Synthesis and In vitro Efficacy of Tetracyclic Benzothiazepines Against
Blood-Stage Plasmodium falciparum and Liver-Stage P. berghei
Authors: Gutteridge Clare E. , Sadowski Brett W. , Hughes Stephen M. , Friedlander J. Alan , Gaidry Alicia D. , Baxter Michael C. , Smith Matthew B. , Rodrigo Leighton G. , O'Neil Michael T. , Gerena Lucia , Lee Patricia J. , Sathunuru Ramadas , Gettayacamin Montip 
Published: August 2022

Objective:
A series of novel, substituted tetracyclic benzothiazepines were designed and prepared in an effort to optimize potency of this chemical class against drug-resistant strains of the malaria parasite.

Method:
Tetracyclic benzothiazepines bearing structural modification at seven distinct positions within the structure were synthesized, in Knoevenagel condensation reactions followed by sequential intermolecular thio-Michael and then intramolecular imine formation reactions. Following purification and chemical characterization, the novel compounds were tested for in vitro efficacy against blood-stage P. falciparum and liver-stage P. berghei, and also for in vivo efficacy against P. berghei.

Results:
Benzothiazepines bearing structural modification at the sulfur atom and at the three carbocycles within the molecule were successfully synthesized. The majority of analogs inhibited blood-stage P. falciparum with submicromolar IC50 values. The potency of an 8-methoxy-substituted analog 12 exceeded that of chloroquine in all three P. falciparum strains tested. The parent benzothiazepine 1 possessed liver-stage activity, inhibiting P. berghei sporozoites infecting HepG2 cells with an IC50 of 106.4 nM and an IC90 of 408.9 nM, but failed to enhance the longevity of P. berghei infected mice compared to the controls. Compounds displayed modest toxicity toward HepG2 cells, and were tolerated by mice at the highest dose tested, 640 mg/kg/dose once daily for three days.

Conclusion:
The tetracyclic benzothiazepine described, which inhibits P. berghei infected hepatic cells with an IC50 of 106.4 nM, would appear to warrant further investigation. Optimization of ADME properties may be required, since the most active analogs are probably excessively lipophilic.
Assay of Trace Copper Ion in Water Resources Using a Photo-sensing
Diode Circuit
Authors: Cho In Hea , Choi Kwang Jin , Choi Jong Wan , Lee Kyung , Ly Suw Young , Kwak Ah Young , Youb Lee Joo 
Published: August 2022

Background:
Trace copper play an important role in plant growth and is a biological component of various enzymes involved in both photosynthesis and plant respiration, in this study.

Objective:
Electrochemical voltammetric bio assay of trace copper ion was detected by using photo-sensing diode circuits (PSD) with a working sensors for ppb levels trace detection in agricultural water by stripping and cyclic voltammetry.

Results:
Optimum voltammetric conditions were examined. The system used was simple and inexpensive circuits of our fabricated systems, but low detection limit was attained at 40.0 ugL⁻¹.
Here can be attained to low detection limits better then common diagnostic analyzers.

Conclusion:
The developed technique can be used in determining trace amounts of copper, especially in detecting copper ions in agricultural water resources.
Technical Advances in the Chiral Separation of Anti-diabetic Drugs Using Analytical and Bio-analytical Methods: A Comprehensive Review
Authors: Spandana Tatineni , Beeraka Narasimha Murthy , Hemanth Vikram Poola R , Goli Veera Venkata Nishanth , Devi Sri Chiriki , Gurupadayya Bannimath 
Published: August 2022

Abstract:Chirality seems to be a pivotal technique in the field of science. Research teams are quite well versed in empirical separation, however, at the same time, they are clueless about the evolution of chiral separation. As per the guidelines of the United States Food and Drug Administration (US FDA), chiral drugs must be untangled before they are sold to the public. Stereogenic separation has gained prominence during the last 10 decades due to the disparate biological function of enantiomers in the stereogenic environment. Chiral drugs exhibit a wide range of bioavailability, distribution, and pharmacodynamic properties concomitantly they exert divergent pharmacological and toxicological properties. Enantiomeric chiral products could be considered safe and potent in combating various diseases including metabolic diseases like diabetes. Several studies have delineated the development of a novel analytical and bioanalytical method to detect/segregate/quantify chiral chemical components in medicinal chemistry. The same physicochemical characteristics of enantiomers have been proven to be beneficial to the estrangement of stereogenic compounds. Furthermore, the advancement of bioanalytical methods is also critical to shedding light on the destiny of distinct enantiomers in the biological environment. HPLC (High-Performance Liquid Chromatography) and CE (Capillary Electrophoresis) have been the most commonly employed separation techniques. But the technical advances are required to enhance the efficiency of detection and quantification of chiral molecules on a large scale. The current review delineates the need for the chiral separation of stereogenic antidiabetic drug compounds with technical advances. Furthermore, this research is focused on the enantioseparation of chiral antidiabetic drugs and a brief overview of the analytical and bioanalytical methods conducted on distant chiral antidiabetic drugs to improve the efficiency of chiral separation.
A Molecular Approach of Caloric Restriction and Vitamins for Cancer Prevention
Authors: Rubio Carmen , Romo-Parra Héctor , Gatica Fernando , Rodríguez-Quintero Paola , Morales Zayra 
Published: August 2022

Abstract:
Each year, cancer claims the lives of around 10.0 million people worldwide. Food components have been
shown to alter numerous intracellular signaling events that frequently go awry during carcinogenesis. Many studies
suggest that dietary behaviors involving the consumption of antioxidant-rich foods, as well as caloric restriction, may
play an important role in cancer prevention. Gene expression patterns, such as genetic polymorphisms, can influence
the response to food components by altering their specific action on targets, as well as absorption, metabolism, and
distribution, among other things. This review discusses two significant cancer prevention techniques: a vitamin-rich
diet and caloric restriction. It also discusses the possible molecular interactions between the two dietary strategies and
the first clues of a probable synergy that would come from combining caloric restriction with antioxidant use. Caloric
restriction diets have positive effects on life expectancy and enable avoidance of age-related illnesses. As a result, this
manuscript is based on the degenerative nature of cancer and intends to shed light on the biochemical features of not
just calorie restriction but also vitamins. Both are thought to have an effect on oxidative stress, autophagy, and signaling
pathways involved in energy metabolism and mitochondrial functions.
Bioactive Polysaccharides from Microalgae: A Close Look at the Biomedical Applications
Authors: Depra Mariany C. , Dias Rosangela R. , Maroneze Mariana M. , Nascimento Tatiele C. , Severo Ihana A. , Zepka Leila Q. , Jacob-Lopes Eduardo 
Published: August 2022

Abstract:There is a current tendency towards bioactive natural products that can be used in different areas such as food, pharmaceutical, and biomedical. In the last decades, polysaccharides have attracted increasing interest because of their potent nontoxic effects, therapeutic properties, and diversified range of applications. Polysaccharides are complex and heterogeneous macromolecules constituted of different monosaccharides and, in some cases, of glucuronic acid and sulphate groups. Polysaccharides with biological activity can be derived from plants, animals and microorganisms, especially microalgae. Microalgae are considered one of the most promising sources of these compounds that have already proved to have several important biological properties. In this sense, our objective is to elucidate the use of bioactive polysaccharides from microalgae in biomedical applications, emphasizing the biological activity of these compounds. Furthermore, the microalgal biomass production systems and polysaccharides extraction methods were presented and discussed.