OPEN ACCESS ARTICLE – Serotonin Receptor Binding Characteristics of Geissoschizine Methyl Ether, an Indole Alkaloid in Uncaria Hook

Journal Name: Current Medicinal Chemistry

Author(s): Yasushi Ikarashi, Kyoji Sekiguchi, Kazushige Mizoguchi*.

 

Abstract:

Background: Geissoschizine methyl ether (GM) is one of the indole alkaloids in Uncaria hook, and an active ingredient of yokukansan (YKS) that improves behavioral and psychological symptoms of dementia (BPSD) in patients with several types of dementia. The pharmacological action of GM has been related to various serotonin (5-HT) receptor subtypes.

Objective: The aim of this article is to review the binding characteristics of GM to the 5-HT receptor subtypes in the brains using our own data and previous findings.

Method: Competitive receptor-binding and agonist/antagonist activity assays for several 5-HT receptor subtypes were performed. Moreover, the articles describing pharmacokinetics and brain distribution of GM were searched in PubMed.

Results: GM bound the following 5-HT receptor subtypes: 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5- HT4, 5-HT5A, 5-HT6, and 5-HT7. Among these receptors, GM had partial agonistic activity for 5-HT1A receptors and antagonistic activity for 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptors. Also, GM was metabolized by various CYP isoforms, mainly CYP3A4. Parent/unchanged GM was detected in both the blood and brain of rats after oral administration of YKS. In the brains, GM was presumed to bind to 5- HT1A, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptors on neuron-like large cells mainly in the frontal cortex.

Conclusion: These results suggest that GM is a pharmacologically important alkaloid that regulates various serotonergic activities or functions by binding to multiple 5-HT receptor subtypes. Thus, this review provides recent 5-HT receptor-related evidence that GM is partly responsible for pharmacological effects of YKS.

 

READ MORE HERE: http://www.eurekaselect.com/151003 

OPEN ACCESS ARTICLE – Does Ceruloplasmin Defend Against Neurodegenerative Diseases?

Journal Name: Current Neuropharmacology

Author(s): Bo Wang , Xiao-Ping Wang*.

 

 

Abstract:

Ceruloplasmin (CP) is the major copper transport protein in plasma, mainly produced by the liver. Glycosylphosphatidylinositol-linked CP (GPI-CP) is the predominant form expressed in astrocytes of the brain. A growing body of evidence has demonstrated that CP is an essential protein in the body with multiple functions such as regulating the homeostasis of copper and iron ions, ferroxidase activity, oxidizing organic amines, and preventing the formation of free radicals. In addition, as an acute-phase protein, CP is induced during inflammation and infection. The fact that patients with genetic disorder aceruloplasminemia do not suffer from tissue copper deficiency, but rather from disruptions in iron metabolism shows essential roles of CP in iron metabolism rather than copper. Furthermore, abnormal metabolism of metal ions and oxidative stress are found in other neurodegenerative diseases, such as Wilson’s disease, Alzheimer’s disease and Parkinson’s disease. Brain iron accumulation and decreased activity of CP have been shown to be associated with neurodegeneration. We hypothesize that CP may play a protective role in neurodegenerative diseases. However, whether iron accumulation is a cause or a result of neurodegeneration remains unclear. Further research on molecular mechanisms is required before a consensus can be reached regarding a neuroprotective role for CP in neurodegeneration. This review article summarizes the main physiological functions of CP and the current knowledge of its role in neurodegenerative diseases.

 

Read more here: http://www.eurekaselect.com/161925 

OPEN ACCESS ARTICLE – Ayahuasca: Psychological and Physiologic Effects, Pharmacology and Potential Uses in Addiction and Mental Illness

Journal Name: Current Neuropharmacology.

Author(s): Jonathan Hamill, Jaime Hallak, Serdar M. Dursun, Glen Baker*.

Abstract:

Ayahuasca, a traditional Amazonian decoction with psychoactive properties, is made from bark of the Banisteriopsis caapi vine (contains beta-carboline alkaloids) and leaves of the Psychotria viridis bush (supply the hallucinogen N,N-dimethyltryptamine (DMT)). Originally used by indigenous shamans for the purposes of spirit communication, magical experiences, healing, and religious rituals, across several South American countries ayahuasca has been incorporated into folk medicine and spiritual healing, and several Brazilian churches use it routinely to foster spiritual experience. More recently it is being used in Europe and North America, not only for religious or healing reasons, but also for recreation. Objective: To review ayahuasca’s behavioral effects, possible adverse effects, proposed mechanisms of action and potential clinical uses in mental illness. Method: We searched Medline, in English, using the terms ayahuasca, dimethytryptamine, Banisteriopsis caapi, and Psychotria viridis and reviewed the relevant publications. Results: The following aspects of ayahuasca are summarized: Political and legal factors; acute and chronic psychological effects; electrophysiological studies and imaging; physiological effects, safety and adverse effects; pharmacology; potential psychiatric uses. Conclusion: Many years of shamanic wisdom have indicated potential therapeutic uses for ayahuasca, and many present day studies suggest that it may be useful for treating various psychiatric disorders and addictions. The side effect profile appears to be relatively mild, but more detailed studies need to be done. Several prominent researchers feel that government regulations with regard to ayahuasca should be relaxed so that it could be provided more readily to recognized credible researchers to conduct comprehensive clinical trials.

 

Read more here: http://www.eurekaselect.com/159373

OPEN ACCESS ARTICLE – Regulation of Apoptosis by SYB in HepG2 Liver Cancer Cells is Mediated by the P53/Caspase 9 Axis – Anti-Cancer Agents in Medicinal Chemistry

Journal: Anti-Cancer Agents in Medicinal Chemistry

Author(s): Sharula, Zhongjun Wu*

Graphical Abstract:

 

Abstract:

Objective: To explore the function of miR-34a in promotion of apoptosis by SYB.

Methods: In this study, the most effective concentration of SYB was determined by measuring cell proliferation. Relative miR-34a mRNA levels were detected by quantitative RT-PCR. Apoptosis was assessed using Annexin- V/PI assays, whereas protein levels of p53, caspase 3, caspase 9, caspase 8 and Bcl2 were evaluated by western blotting.

Results: Minimum HepG2 cell growth was observed after 36h of exposure to 150 nmol/L SYB. miR-34a expression was highest 40min after the addition of SYB. SYB slightly decreased the abundance of Bcl-2, but increased the abundance of p53, caspase 3, caspase 9 and caspase 8. SYB failed to alter miR-34a expression when p53 was inhibited. Bcl-2 abundance remained low over time, whereas the abundance of caspase 3, caspase 9 and caspase 8 gradually increased. Inhibition of p53 promoted HepG2 cell growth in comparison with that of the control group. miR-34a was silenced to assess the role of miR-34a in the inhibitory effect of SYB on HepG2 cell growth. When p53 was silenced, protein abundance of Bcl2, caspase 3, caspase 8 and caspase 9 remained unchanged following the addition of SYB; moreover, HepG2 cell growth was increased.
Conlusion: SYB represents a promising therapeutic approach for liver cancer patients.

 

Open Access Article – Control of Risk Factors for Cardiovascular Disease among Multinational Patient Population in the Arabian Gulf – Current Vascular Pharmacology

Journal: Current Vascular Pharmacology

Author(s): Ibrahim Al-Zakwani, Wael Al-Mahmeed, Mohamed Arafah, Ali T. Al-Hinai, Abdullah Shehab, Omer Al-Tamimi, Mahmoud Al-Awadhi,Shorook Al-Herz, Faisal Al-Anazi, Khalid Al-Nemer, Othman Metwally, Akram Al-Khadra, Mohammed Fakhry, Hossam Elghetany, Abdel R. Medani,Afzal H. Yusufali, Obaid Al-Jassim, Omar Al-Hallaq, Fahad O.A.S. Baslaib, Haitham Amin, Raul D. Santos, Khalid Al-Waili, Khamis Al-Hashmi,Khalid Al-Rasadi.

Abstract:

We evaluated the control of cardiovascular disease (CVD) risk factors among patients with atherosclerotic cardiovascular disease (ASCVD) in the Centralized Pan-Middle East Survey on the undertreatment of hypercholesterolaemia (CEPHEUS) in the Arabian Gulf. Of the 4398 enrolled patients, overall mean age was 57 ± 11 years, 60% were males, 13% were smokers, 76% had diabetes, 71% had metabolic syndrome and 78% had very high ASCVD risk status. The proportion of subjects with body mass index <25 kg/m2, HbA1c <7% (in diabetics), low-density lipoprotein cholesterol (LDL-C) <2.6 mmol/L (100 mg/dL) and <1.8 mmol/L (70 mg/dL) for high and very high ASCVD risk cohorts, respectively and controlled blood pressure (<140/90 mmHg) was 14, 26, 31% and 60%, respectively. Only 1.4% of the participants had all of their CVD risk factors controlled with significant differences among the countries (P < .001). CVD risk goal attainment rates were significantly lower in those with very high ASCVD risk compared with those with high ASCVD risk status (P < .001). Females were also, generally, less likely to attain goals when compared with males (P < .001).

Read more here: http://www.eurekaselect.com/136029

EurekAlert! –Uric acid, gout and kidney disease: The chicken or the egg?

The increasing prevalence of both gout and chronic kidney disease has led to a growing interest in the association between hyperuricemia (an abnormally high level of uric acid in the blood) and kidney disease

The increasing prevalence of both gout and chronic kidney disease has led to a growing interest in the association between hyperuricemia (an abnormally high level of uric acid in the blood) and kidney disease.

A new thematic issue of The Open Urology & Nephrology Journal, titled ‘Current Perspectives in Hyperuricemia, Gout and the Kidney,’ reports on the interplay of various factors, particularly the role of the kidney in uric acid excretion on the one hand, and the possible impact of hyperuricemia on progression of renal disease on the other. The common patho-physiological link appears to be the chronic, low-grade, systemic inflammation that is intrinsic to both conditions, and that may explain some of the perplexing observations noted in these clinical conditions.


The special issue is edited by

Vandana Dua Niyyar

MD, Associate Professor of Medicine (Nephrology)

Emory University School of Medicine.

Read more here: http://www.eurekalert.org/pub_releases/2016-03/bsp-uag032816.php

Complimentary Bentham OPEN Membership

Bentham Science Publishers is dedicated to the sharing of knowledge and pushing the boundaries of science even further! We are offering our Complimentary Bentham OPEN Membership to students and researchers using libraries around the world.

Bentham  has under its umbrella the publication of more than 230 Open Access journals related to diverse fields and interests. These free-to-view online journals cover all major disciplines of science, technology, medicine and social sciences. Open access has a universal reach, providing an invaluable service to the global scientific community by making academic and professional research available and accessible to all. Bentham Science Open Access is a trusted name for professional, peer-reviewed publication for an efficient exchange of scientific information. Bentham follows a stringent editorial policy: the code of Ethical Approval of Studies and Informed Consent, Plagiarism Prevention, Copyrights, Standard Protocol on Approvals, etc. The Bentham Open Access policies and standards ensure a rigorous peer-review system that is up to the international open access publishing standards.

Bentham OPEN Membership  is a complimentary membership offered to International R & D organizations, institutes and universities. This opportunity will entitle authors from different member institutes to a special discount of 30% in the open access publication fee for submission of articles to Bentham OPEN journals. Additionally, input and contributions from associate institutes would also be recognized and a link to their respective Website would be displayed on the Bentham OPEN membership page. The member institution’s logo will also be published on the same page.

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For further information, please visit http://www.benthamscience.com/open/oaMembership.php .

Complimentary Bentham Open Membership
Bentham Open Membership

Bentham Open Membership

Bentham OPEN offers its ‘Complimentary Membership’ to International R & D organizations, institutes and universities. This opportunity will entitle authors from different member institutes to a special discount of 30% in the open access publication fee for submission of articles to Bentham OPEN journals. Additionally, input and contributions from associate institutes would also be recognized and a link to their respective Website would be displayed on the Bentham OPEN membership page. The member institution’s logo will also be published on the same page.

Complimentary Membership

Bentham Open Membership

Bentham Open Membership provides the following advantages:

• Possibility to explore 73 distinct disciplines by means of publishing in 239 open access journals.

• Free access to all provides prospects of higher citations.

• Author(s) own the copyrights to their published articles.

• High standard criteria for peer-review.

• Unbound right to read, download or print open access articles.

• Access to a range of articles in printed form such as short communications, full length research articles, reviews or conference proceedings.

• Simple steps from submission to publication, leading to fast turn-around.

• Possibility of archiving published articles.

The complimentary membership is valid for a span of one year and upon completion of the prescribed period, it is renewed by mutual interest and agreement.

Kindly contact us via e-mail at membership@benthamscience.org or oa@benthamscience.org.

Why not start a new open access journal of your own at Bentham Open?

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Whether you have an existing journal, represent a learned society’s journal or wish to start a new journal, Bentham Open is the foremost publisher to meet all your requirements. There can be no better way than making research freely available to a global audience by opting for open access publication with Bentham Open.
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