Open Access Articles | Tissue Distribution of Active Principles from Alpiniae Oxyphyllae Fructus Extract: An Experimental Study in Rats

 

Journal Name: Current Pharmaceutical Analysis

            Author(s): Qi Wen, Hai-Long Li, Shi-Ying Mai, Yin-Feng Tan*, Feng Chen*.

 

Graphical Abstract:

 

Abstract:

Background: Alpiniae Oxyphyllae Fructus (Yizhi in Chinese) have been widely used as an herbal medicine for the treatment of diuresis, enuresis and diarrhea in China. Many studies have deciphered some potential underlying mechanisms for its anti-diarrheal effects. However, tissue distribution of Yizhi constituents is warranted because pharmacological receptors are frequently located in tissues. Moreover, it is also interesting to know about the potential correlation between behavior in drug distribution and the observed pharmacological response. The aim of this study is to investigate tissue distribution behaviors of Yizhi constituents after oral administration of Yizhi extract to rats, focusing on 10 active principles.

Methods: Twenty four male Sprague Dawley rats were given orally the Yizhi extract and fourteen tissue samples were collected after being killed by bleeding from the abdominal aorta under ether anesthesia at different time-points. The resulting tissues were excised and homogenized. Based on our previous reports, liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) was used to quantify the target analytes, as well as phase II metabolites, in the various biosamples.

Results: Almost all the targeted Yizhi active principles and some glucuronidated metabolites were qualitatively measured in rat stomach, small intestine, large intestine, as well as liver. Nootkatone, yakuchinone A and tectochrysin were observed in the rat brain. In other rat tissues, these analytes had lower exposure or could not be detected. Consistently, quantitative analysis revealed that the Yizhi active principles dominantly distributed into gastrointestinal tissues followed by liver, the overall exposure levels ranking as follows: stomach > small intestine > large intestine > liver. Tissue concentrationtime profiles of the test active principles in rat stomach, small intestine, and large intestine were bimodal with two concentration peaks occurring at 0.5 and 4h after oral administration, respectively. The exposure levels in rat kidney and bladder were quite low.

Conclusion: The active principles of Yizhi were specially distributed into gastrointestinal tissues after oral administration of its ethanol extract to rats. The tissue distribution behaviors partly supported its anti-diarrheal effects from a pharmacokinetic opinion. This paper will be useful as the starting point for studying the pharmacological activities of this traditional herb. To read out more, please visit: http://www.eurekaselect.com/165218/article

Open Access Articles | An Integrated Computational Approach for Plant-Based Protein Tyrosine Phosphatase Non-Receptor Type 1 Inhibitors

 

Journal Name: Current Computer-Aided Drug Design

Author(s): Shabana Bibi, Katsumi Sakata*.

 

 

Graphical Abstract:

 

Abstract:

Background: Protein tyrosine phosphatase non-receptor type 1 is a therapeutic target for the type 2 diabetes mellitus. According to the International Diabetes Federation 2015 report, one out of 11 adults suffers from diabetes mellitus globally.

Objective: Current anti-diabetic drugs can cause life-threatening side-effects. The present study proposes a pipeline for the development of effective and plant-derived anti-diabetic drugs that may be safer and better tolerated.

Methods: Plant-derived protein tyrosine phosphatase non-receptor type 1 inhibitors possessing antidiabetic activity less than 10µM were used as a training set. A common feature pharmacophore model was generated. Pharmacophore-based screening of plant-derived compounds of the ZINC database was conducted using ZINCpharmer. Screened hits were assessed to evaluate their drug-likeness, pharmacokinetics, detailed binding behavior, and aggregator possibility based on their physiochemical properties and chemical similarity with reported aggregators.

Results: Through virtual screening and in silico pharmacology protocol isosilybin (ZINC30731533) was identified as a lead compound with optimal properties. This compound can be recommended for laboratory tests and further analyses to confirm its activity as protein tyrosine phosphatase nonreceptor type 1 inhibitor.

Conclusion: The present study has identified plant-derived anti-diabetic virtual lead compound with the potential to inhibit protein tyrosine phosphatase non-receptor type 1, which may be helpful to enhance insulin production. This computer-aided study could facilitate the development of novel pharmacological inhibitors for diabetes treatment. To read out more, please visit: http://www.eurekaselect.com/151386/article

MOST ACCESSED ARTICLE – Natural Product Inhibitors of Topoisomerases: Review and Docking Study

Journal Name: Current Protein & Peptide Science

Author(s): Luciana Scotti*, Francisco Jaime Bezerra Mendonca, Frederico Favaro Ribeiro,Josean Fechine Tavares, Marcelo Sobral da Silva, Jose Maria Barbosa Filho, Marcus Tullius Scotti.

 

 

Graphical Abstract:

 

Abstract:

Since ancient times, natural products have been used in treating various diseases effectively and safely. Nowadays, these natural compounds are submitted to sophisticated methodologies from isolation, computing, analytical, and even serving as pharmacophore suggestions for synthesis. The substances extracted from marine species, plants, and microorganisms present activities beneficial to our health, including protection against malignant tumors. The topoisomerase enzymes play an important role in DNA metabolism, and searching for enzyme inhibitors is an important target in the search for new anticancer drugs. This review discusses this problem, reporting research involving alkaloids, terpenes, flavonoids, xanthones, coumarins, acetogenins, and in addition, includes a docking study with our Brazilian diterpenes to topoisomerases I and II. The better compound, the trachylobane 1, forms one hydrogen bond when submitted to docking with Topo I (with the ASP533 residue) and two with residues in Topo II (THR213 and TYR188). The difference observed in the energy of formation can be attributed to hydrogen-bond interactions.

The difference observed in the energy of formation can be attributed to hydrogen-bond interactions.

 

READ MORE HERE: http://www.eurekaselect.com/149155

MOST ACCESSED ARTICLE – Polyphenols: Potential Use in the Prevention and Treatment of Cardiovascular Diseases

Journal Name: Current Pharmaceutical Design

Author(s): Rosaria Vincenza Giglio, Angelo Maria Patti, Arrigo F.G. Cicero, Giuseppe Lippi, Manfredi Rizzo*, Peter P. Toth, Maciej Banach.

 

 

 

Abstract:

Background: Polyphenols are bioactive compounds that can be found mostly in foods like fruits, cereals, vegetables, dry legumes, chocolate and beverages such as coffee, tea and wine. They are extensively used in the prevention and treatment of cardiovascular disease (CVD) providing protection against many chronic illnesses. Their effects on human health depend on the amount consumed and on their bioavailability. Many studies have demonstrated that polyphenols have also good effects on the vascular system by lowering blood pressure, improving endothelial function, increasing antioxidant defences, inhibiting platelet aggregation and low-density lipoprotein oxidation, and reducing inflammatory responses.

Methods: This review is focused on some groups of polyphenols and their effects on several cardiovascular risk factors such as hypertension, oxidative stress, atherogenesis, endothelial dysfunction, carotid artery intima-media thickness, diabetes and lipid disorders.

Results: It is proved that these compounds have many cardio protective functions: they alter hepatic cholesterol absorption, triglyceride biosynthesis and lipoprotein secretion, the processing of lipoproteins in plasma, and inflammation. In some cases, human long-term studies did not show conclusive results because they lacked in appropriate controls and in an undefined polyphenol dosing regimen.

Conclusion: Rigorous evidence is necessary to demonstrate whether or not polyphenols beneficially impact CVD prevention and treatment.

 

READ MORE HERE: http://www.eurekaselect.com/159482

TESTIMONIAL BY FEDERICA POLLASTRO!

Contributed Article: “Cannabis Phenolics And Their Bioactivities“

Dark chocolate and blood pressure

The goal of this study was to assess the effect of dark chocolate intake on cardiovascular parameters like blood pressure and heart rate values in a normotensive population. http://bit.ly/1FeQgnW

This article is from the journal Current Drug Delivery

Recent Issues of the Following Journals have been Published!

The Natural Products Journal, 4 Issue 1

Editor-in-Chief:

Francesco Epifano

Università “G. D’Annunzio”

Chieti-Pescara, Chieti Scalo (CH)
Italy

Aims & Scope

The Natural Products Journal a peer reviewed journal, aims to publish all the latest and outstanding developments in natural products.

The Natural Products Journal publishes original research articles, reviews, letters and guest edited issues on all aspects of research and development in the field including: isolation, purification, structure elucidation, synthesis and bioactivity of chemical compounds found in nature.

www.eurekaselect.com

 Abstracted & Indexed in:

Chemical Abstracts, J-Gate, PubsHub.

http://www.eurekaselect.com/123357/issue/1

For details, visit: http://benthamscience.com/journal/index.php?journalID=npj

Clinical Immunology, Endocrine & Metabolic Drugs, 1 Issue 1

Editor-in-Chief:

Emilio Jirillo

Professor of Immunology, University of Bari
Bari
Italy 

Aims & Scope

Clinical Immunology, Endocrine & Metabolic Drugspublishes original research, expert reviews, drug clinical trials and thematic issues in all core areas of translational and clinical immunology, endocrine & metabolic drug research.

The journal publishes pre-clinical and clinical studies on the development of new immunology, endocrine & metabolic agents. Clinical studies of new reported immunology, endocrine & metabolic drugs include Phase 1 – IV clinical trial studies, their designs, research methodologies, and analyses. The journal is essential reading to clinicians, toxicologists, medicinal chemists, and pharmacologists.

http://www.eurekaselect.com/123473/issue/1

For more details, visit: http://benthamscience.com/journal/index.php?journalID=ciemd

CNS & Neurological Disorders – Drug Targets , 13 Issue 5

Editor-in-Chief:

Stephen D. Skaper

Department of Pharmaceutical and Pharmacological Sciences
University of Padova
Padova
Italy

Aims & Scope

CNS & Neurological Disorders – Drug Targets aims to cover all the latest and outstanding developments on the medicinal chemistry, pharmacology, molecular biology, genomics and biochemistry of contemporary molecular targets involved in neurological and central nervous system (CNS) disorders e.g. disease specific proteins, receptors, enzymes, genes.

CNS & Neurological Disorders – Drug Targets publishes guest edited thematic issues written by leaders in the field covering a range of current topics of CNS & neurological drug targets. The journal also accepts for publication original research articles, letters, reviews and drug clinical trial studies.

As the discovery, identification, characterization and validation of novel human drug targets for neurological and CNS drug discovery continues to grow; this journal is essential reading for all pharmaceutical scientists involved in drug discovery and development.

www.eurekaselect.com

Abstracted & Indexed in:

Science Citation Index Expanded, MEDLINE, PubMed, BIOSIS, BIOSIS Previews, BIOSIS Reviews Reports and Meetings, Chemical Abstracts, EMBASE/Excerpta Medica, PsycINFO, Current Contents^®/Clinical Medicine, Journal Citation Reports/Science Edition, Scopus, Neuroscience Citation Index^®, MediaFinder^®-Standard Periodical Directory, Genamics JournalSeek, PubsHub, J-Gate.

http://www.eurekaselect.com/123446/issue/5

For more information, visit: http://benthamscience.com/journal/index.php?journalID=cnsnddt

Current Organic Chemistry, 18 Issue 10

Editor-in-Chief:

Atta-ur-Rahman

FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: coc@benthamscience.org 

Aims & Scope

Current Organic Chemistry aims to provide in-depth reviews on the current progress in the fields of asymmetric synthesis, organo-metallic chemistry, bioorganic chemistry, heterocyclic chemistry, natural product chemistry and analytical methods in organic chemistry. The frontier reviews provide the current state of knowledge in these fields and are written by chosen experts who are internationally known for their eminent research contributions. The Journal also accepts high quality research papers, highlights and letters besides thematic issues in these fields. Current Organic Chemistry should prove to be of great interest to organic chemists in academia and industry who wish to keep abreast with recent developments in key fields of organic chemistry.

www.eurekaselect.com

Abstracted & Indexed in:

Science Citation Index, Science Citation Index Expanded, Journal Citation Reports/Science Edition, Current Contents^®(Physical, Chemical and Earth Sciences), Chemistry Citation Index^®, Chemical Abstracts, Science Citation Index Expanded, Scopus, PubsHub, Genamics JournalSeek,Research Alert, SciSearch, Engineering Village/Chimica, MediaFinder^®-Standard Periodical Directory, J-Gate.

http://www.eurekaselect.com/123455/issue/10

For details, visit: http://benthamscience.com/journal/index.php?journalID=coc