scholarly journals Xanthine: Synthetic Strategy And Biological Activity

2021 ◽  
Vol 12 (6) ◽  
pp. 7438-7468
Keyword(s):  
Adenosine Receptors ◽  
Pharmacological Effects ◽  
Human Beings ◽  
Research Groups ◽  
Biological Profile ◽  
Xanthine Derivatives ◽  
Synthetic Strategy ◽  
Purine Alkaloids ◽  
Central Nervous System Penetration ◽  
Penetration Ability

Xanthine and its derivatives belong to the class of purine alkaloids. They are natural bases holding nitrogen atoms within the molecular structure, and they have an effective pharmacological alteration in both animals and human beings. Substituted xanthine, theophylline/caffeine being prototype, is one of the derivatives which have shown prominent binding to adenosine receptors as agonist or antagonist. Various mechanistic approaches are involved in exerting bronchospasmolytic, neuroprotective, hypoglycemic, MAO modulatory, along cardiac effects. Mostly, xanthine derivatives reduce inflammation and bronchospasm in asthmatic conditions. Other therapeutics effects are in the management of cancer, Alzheimer's disease, vasoconstriction, and also possess excellent central nervous system-penetration ability; thus, they can also be used as stimulants and anti-depressants. Their actions are relatively very weak, but their pharmacological effects are also associated with snarl-up adenosine-mediated functions. An assortment of the biological profile of the xanthine scaffold attracted many research groups over the years to explore this nucleus vividly. The present review is aimed to cover every aspect of the xanthine moiety reported in the earlier years. This review covers all the major biological roles and various synthetic strategies adopted to synthesize xanthine moiety and its derivatives.

Sex determination by discriminant function analysis using the human tibia in a Central Indian population

2019 ◽  
Vol 59 (3) ◽  
pp. 171-179 ◽  
Author(s):  
Preetika M Chatterjee ◽  
Kewal Krishan ◽  
RK Singh ◽  
Tanuj Kanchan
Keyword(s):  
Sex Determination ◽  
Discriminant Function ◽  
Discriminant Function Analysis ◽  
Function Analysis ◽  
Articular Surface ◽  
Transverse Diameter ◽  
Long Bones ◽  
Human Beings ◽  
Biological Profile ◽  
Nutrient Foramen

In human beings, sexual dimorphism can be well distinguished in almost every bone of the skeleton. Establishing a reliable biological profile is the foremost step in identifying human skeletal remains. Sex determination along with the estimation of age, stature and ancestry comprise the important parameters in establishing a biological profile. The pelvis and skull are considered the most reliable bones in sexing human remains. In the absence of the pelvis and skull, forensic scientists must rely upon other parts of the skeleton for sex assessment. Determination of sex from long bones based on morphological traits can be a challenging task, as there are a few morphological differences between the sexes for long bones. However, metric variations can prove to be helpful, as they are reproducible and more reliable. Metric analysis also has the added benefit of being less biased than nonmetric analysis. This study aimed to establish sex determination standards from tibiae using discriminant function analysis. A total of 17 measurements were taken on 162 dry tibiae (116 males and 46 females) of known sex and in the age range 20–60 years. Discriminant function analysis was performed to derive models for sexing of the tibiae. The breadth of the medial articular surface was observed to be the best parameter for sex prediction from metric measurements of the tibia. In stepwise analysis, only seven parameters – namely, the breadth of the medial articular surface, the condylo-malleolar length, the circumference at the nutrient foramen, the breadth of the lateral articular surface, the maximum length, the transverse diameter in the middle of the bone and the transverse diameter at the level of the nutrient foramen – were entered into the discriminant functions. Overall, the accuracy of sexing was observed to be 93.8% and 95% with the direct method and the stepwise method, respectively. This study provides a database and standards for sex estimation from tibiae based on discriminant function models. This investigation further concludes that tibiae can be used for sex determination in forensic examinations.

scholarly journals Pharmacological Overview of the BGP-15 Chemical Agent as a New Drug Candidate for the Treatment of Symptoms of Metabolic Syndrome

Molecules ◽  
2020 ◽  
Vol 25 (2) ◽  
pp. 429
Author(s):  
Ágota Pető ◽  
Dóra Kósa ◽  
Pálma Fehér ◽  
Zoltán Ujhelyi ◽  
Dávid Sinka ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Parp Inhibitor ◽  
Drug Candidate ◽  
Chemical Agent ◽  
Membrane Domains ◽  
Protective Effects ◽  
Pharmacological Effects ◽  
Research Groups ◽  
Insulin Sensitizer ◽  
Beneficial Effects

BGP-15 is a new insulin sensitizer drug candidate, which was developed by Hungarian researchers. In recent years, numerous research groups have studied its beneficial effects. It is effective in the treatment of insulin resistance and it has protective effects in Duchenne muscular dystrophy, diastolic dysfunction, tachycardia, heart failure, and atrial fibrillation, and it can alleviate cardiotoxicity. BGP-15 exhibits chemoprotective properties in different cytostatic therapies, and has also proven to be photoprotective. It can additionally have advantageous effects in mitochondrial-stress-related diseases. Although the precise mechanism of the effect is still unknown to us, we know that the molecule is a PARP inhibitor, chaperone co-inducer, reduces ROS production, and is able to remodel the organization of cholesterol-rich membrane domains. In the following review, our aim was to summarize the investigated molecular mechanisms and pharmacological effects of this potential API. The main objective was to present the wide pharmacological potentials of this chemical agent.

scholarly journals 3-Aryl-4-nitrobenzothiochromans S,S-dioxide: From Calcium-Channel Modulators Properties to Multidrug-Resistance Reverting Activity

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1056 ◽  
Author(s):  
Matteo Micucci ◽  
Maurizio Viale ◽  
Alberto Chiarini ◽  
Domenico Spinelli ◽  
Maria Frosini ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Multidrug Resistance ◽  
Tumor Cell ◽  
Organic Compounds ◽  
Ex Vivo ◽  
Pharmacological Properties ◽  
Tumor Cell Lines ◽  
Research Groups ◽  
Biological Profile ◽  
Biological Interest

Our research groups have been involved for many years in studies aimed at identifying new active organic compounds endowed with pharmacological properties. In this work, we focused our attention on the evaluation of cardiovascular and molecular drug resistance (MDR) reverting activities of some nitrosubstituted sulphur-containing heterocycles. Firstly, we have examined the effects of 4-nitro-3-(4-methylphenyl)-3,6-dihydro-2H-thiopyran S,S-dioxide 5, and have observed no activity. Then we have extended our investigation to the 3-aryl-4-nitrobenzothiochromans S,S-dioxide 6 and 7, and have observed an interesting biological profile. Cardiovascular activities were assessed for all compounds using ex vivo studies, while the MDR reverting effect was evaluated only for selected compounds using tumor cell lines. All compounds were shown to affect cardiovascular parameters. Compound 7i exerted the most effect on negative inotropic activity, while 6d and 6f could be interesting molecules for the development of more active ABCB1 inhibitors. Both 6 and 7 represent structures of large possible biological interest, providing a scaffold for the identification of new ABCB1 inhibitors.

scholarly journals Isolation, analysis and in vitro assessment of CYP3A4 inhibition by methylxanthines extracted from Pu-erh and Bancha tea leaves

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Kaloyan D. Georgiev ◽  
Maya Radeva-Ilieva ◽  
Stanila Stoeva ◽  
Iliya Zhelev
Keyword(s):  
Drug Interactions ◽  
Green Tea ◽  
Dependent Manner ◽  
Pharmacological Effects ◽  
Tea Leaves ◽  
Concentration Dependent Manner ◽  
Cyp3a4 Inhibition ◽  
Purine Alkaloids ◽  
In Vitro Assessment

Abstract Methylxanthines, purine alkaloids found in plants, are found in beverages (coffee, tea, cocoa) and foods (chocolate and other cocoa-containing foods) commonly consumed worldwide. Members of this family include caffeine, theophylline and theobromine. Methylxanthines have a variety of pharmacological effects, and caffeine and theophylline are used as pharmaceuticals. Methylxanthines are metabolized in the liver predominantly by the enzyme CYP1A2. Their co-administration with CYP1A2 inhibitors may lead to pharmacokinetic interactions. Little is known about the possible drug interactions between caffeine and substrates of other CYP450 enzymes. In our study, methylxanthine fractions inhibited CYP3A4 in a concentration-dependent manner. Concomitant consumption of green tea with CYP3A4 substrates could increase the possibility of interactions, and this requires further clarification. The inhibition of CYP3A4 is not only due to the presence of catechin derivatives but methylxanthines may also contribute to this effect.

Role and Function of Adenosine and its Receptors in Inflammation, Neuroinflammation, IBS, Autoimmune Inflammatory Disorders, Rheumatoid Arthritis and Psoriasis

2019 ◽  
Vol 25 (26) ◽  
pp. 2875-2891 ◽  
Author(s):  
Ashok K. Shakya ◽  
Rajashri R. Naik ◽  
Ihab M. ALMASRI ◽  
Avneet Kaur
Keyword(s):  
Rheumatoid Arthritis ◽  
Adenosine Receptors ◽  
G Protein Coupled Receptors ◽  
Physiological Effects ◽  
Xanthine Derivatives ◽  
Organ Systems ◽  
New Chemical Entities ◽  
And Function ◽  
G Protein Coupled ◽  
Role And Function

The physiological effects of endogenous adenosine on various organ systems are very complex and numerous which are elicited upon activation of any of the four G-protein-coupled receptors (GPCRs) denoted as A1, A2A, A2B and A3 adenosine receptors (ARs). Several fused heterocyclic and non-xanthine derivatives are reported as a possible target for these receptors due to physiological problems and lack of selectivity of xanthine derivatives. In the present review, we have discussed the development of various new chemical entities as a target for these receptors. In addition, compounds acting on adenosine receptors can be utilized in treating diseases like inflammation, neuroinflammation, autoimmune and related diseases.

scholarly journals Some thoughts on the physiology of caffeine in coffee: and a glimpse of metabolite profiling

2006 ◽  
Vol 18 (1) ◽  
pp. 243-251 ◽  
Author(s):  
Thomas W. Baumann
Keyword(s):  
Molecular Biology ◽  
Metabolite Profiling ◽  
Recent Progress ◽  
Physiological Role ◽  
Coffee Bean ◽  
Human Beings ◽  
Research Groups ◽  
Coffee Plant ◽  
Knowing That ◽  
Coffee Plants

Human beings enjoy the flavor and stimulating activity of a cup of coffee without knowing that by doing so, they are part of a 'food web' and receive signals coffee plants build to improve their struggle for life. This review is centered in the first part on the purine alkaloid caffeine and its physiological role in the coffee plant's life cycle. Many of the thoughts and ideas presented here are plain speculation, because the real research revealing the secrets of plant physiology such as e.g. the formation of the coffee bean with all its ingredients, has just started. The recent achievements in molecular biology made it possible to tackle and answer new questions regarding the regulation of secondary metabolism in the coffee plant organs at selected stages of their development. Brazilian research groups have much contributed to the recent progress in molecular biology and physiology of coffee. Among them was Maro R. Söndahl, in commemoration of whom this article has been written. Thus, the second part reports on the very first steps Maro and I made together into a very new field of coffee, that is metabolite profiling. The outcome was amazing and gives an idea of the great potential of this technique to map in future the complex network of the coffee metabolom.

Novel, Dual Target‐Directed Annelated Xanthine Derivatives Acting on Adenosine Receptors and Monoamine Oxidase B

ChemMedChem ◽  
2020 ◽  
Vol 15 (9) ◽  
pp. 772-786
Author(s):  
Kamil J. Kuder ◽  
Michał Załuski ◽  
Jakub Schabikowski ◽  
Gniewomir Latacz ◽  
Agnieszka Olejarz‐Maciej ◽  
...  
Keyword(s):  
Monoamine Oxidase ◽  
Adenosine Receptors ◽  
Monoamine Oxidase B ◽  
Xanthine Derivatives ◽  
Dual Target

A Brief Review of Transparent Wood: Synthetic Strategy, Functionalization, and Applications

2021 ◽  
Vol 18 ◽  
Author(s):  
Caichao Wan ◽  
Xinyi Liu ◽  
Qiongtao Huang ◽  
Wenjie Cheng ◽  
Jiahui Su ◽  
...  
Keyword(s):  
Renewable Resources ◽  
Building Materials ◽  
Channel Structure ◽  
Wall Structure ◽  
Human Beings ◽  
Environmental Friendliness ◽  
Synthetic Strategy ◽  
Research Activities ◽  
Cellular Wall ◽  
The Relationship

: Severe pressure from energy consumption and serious pollution from non-renewable resources have urged human beings to develop green and energy-efficient materials. Transparent wood, consisting of original wood channel structure filled with resins, has favorable environmental friendliness and high transparency and haze, which holds huge potential in various important fields. Herein, a brief review of the current research activities centering on the development of transparent wood is provided. This review begins with an introduction to the background of transparent wood. Next, the cellular wall structure of wood and the synthetic strategy of transparent wood (including decolorization and impregnation) are summarized. Furthermore, the functionalization of transparent wood through doping nanomaterials or modifying resins is highlighted, and the relationship between the physicochemical properties and the potential uses (like optoelectronics, building materials, and furniture decoration) of transparent wood are clarified. Finally, a brief overview of the prospects and challenges for transparent wood is provided.

scholarly journals Highly bioactive zeolitic imidazolate framework-8–capped nanotherapeutics for efficient reversal of reperfusion-induced injury in ischemic stroke

2020 ◽  
Vol 6 (12) ◽  
pp. eaay9751 ◽  
Author(s):  
Lizhen He ◽  
Guanning Huang ◽  
Hongxing Liu ◽  
Chengcheng Sang ◽  
Xinxin Liu ◽  
...  
Keyword(s):  
Ischemic Stroke ◽  
Rational Design ◽  
Artery Occlusion ◽  
Zeolitic Imidazolate Framework ◽  
Synthetic Strategy ◽  
Action Mechanisms ◽  
Neuroprotective Therapy ◽  
Penetration Ability ◽  
Cerebral Artery Occlusion

Rational design of potent antioxidative agent with high biocompatibility is urgently needed to treat ischemic reperfusion-induced ROS-mediated cerebrovascular and neural injury during ischemia strokes. Here, we demonstrate an in situ synthetic strategy of bioactive zeolitic imidazolate framework-8–capped ceria nanoparticles (CeO2@ZIF-8 NPs) to achieve enhanced catalytic and antioxidative activities and improved stroke therapeutic efficacy. This nanosystem exhibits prolonged blood circulation time, reduced clearance rate, improved BBB penetration ability, and enhanced brain accumulation, where it effectively inhibits the lipid peroxidation in brain tissues in middle cerebral artery occlusion mice and reduces the oxidative damage and apoptosis of neurons in brain tissue. CeO2@ZIF-8 also suppresses inflammation- and immune response–induced injury by suppressing the activation of astrocytes and secretion of proinflammatory cytokines, thus achieving satisfactory prevention and treatment in neuroprotective therapy. This study also sheds light on the neuroprotective action mechanisms of ZIF-8–capped nanomedicine against reperfusion-induced injury in ischemic stroke.

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