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Identification of Anxiolytic Potential of Niranthin:In-vivo and Computational Investigations

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Natural Products and Bioprospecting 2021年第2期11卷 223-233页

作者： Atul R.Chopade Prakash M.Somade Pratik P.Somade Suraj N.Mali Department of Pharmacology Rajarambapu College of PharmacyKasegaonSangliMaharashtra 415404India dept.of physiology Krishna Institute of Medical SciencesKaradMaharashtraIndia Government College of Pharmacy KaradMaharashtraIndia

Anxiety is an unpleasant state,which can critically decrease the quality of life is often accompanied by nervous behaviour and *** is a lignan isolated from various Phyllanthus *** literature survey on niranthin highlights wide ranges of the therapeutic *** a present study,based on our previous investigations,we evaluated pure,isolated and characterized niranthin as an anxiolytic *** niranthin[6-[(2R,3R)-3-[(3,4-dimethoxyphenyl)methyl]-4-methoxy-2-(methoxymethyl)butyl]-4-methoxy-1,3-benzodioxole]was purchased from commercial source and further subjected for assessment of its anxiolytic potentials using popular animal models including Elevated plus-maze model/test(EPM)and Light&Dark Exploration test(L&D).GABA-A receptor mediation was evaluated by pretreating the mice with the GABA-A receptor antagonist Flumazenil before the EPM *** docking simulation studies(pdb id:4COF)carried out by Vlife QSAR software showed that niranthin(docking score:−62.1714 kcal/mol)have shown comparatively best docking score compared to the standard drug Diazepam(docking score:−63.1568 kcal/mol).To conclude,Niranthin has probable potential in the management of anxiety *** in-silico and in-vivo analysis(indirectly)indicated the plausible role of GABA mediation for anxiolytic ***,these studies are preliminary,future in depth experimental explorations will be required to use Niranthin as anti-anxiety drug in near future.

关键词： Pharmacology Phytoconstituents Niranthin Lignan Anxiolytic activity EPM models

Hitting a moving target:inhibition of the nuclear export receptor XPO1/CRM1 as a therapeutic approach in cancer

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Cancer Drug Resistance 2018年第3期1卷 139-163页

作者： Maria Sendino Miren Josu Omaetxebarria Jose Antonio Rodríguez Department of Genetics Physical Anthropology and Animal PhysiologyUniversity of the Basque Country(UPV/EHU)Leioa48940Spain. Department of biochemistry and Molecular Biology University of the Basque Country(UPV/EHU)Leioa 48940Spain

Cellular homeostasis crucially relies on the correct nucleocytoplasmic distribution of a vast number of proteins and RNA molecules,which are shuttled in and out of the nucleus by specialized transport *** nuclear export receptor XPO1,also called CRM1,mediates the translocation of hundreds of proteins and several classes of RNA to the cytoplasm,and thus regulates critical signaling pathways and cellular *** normal function of XPO1 appears to be often disrupted in malignant cells due to gene mutations or,most commonly,aberrant *** to its important physiological roles and its frequent alteration in human tumors,XPO1 is a promising target for cancer ***1 inhibitors have undergone extensive testing as therapeutic agents in preclinical models of cancer,with promising *** of these inhibitors,Selinexor,is currently being evaluated in multiple clinical trials of different types of solid tumors and hematological ***,we review several key aspects of XPO1 function,as well as the mechanisms that may lead to its alteration in cancer,and provide an update on the status of XPO1 inhibitors being developed as drugs for cancer therapy,including the definitive results of the first clinical trials with Selinexor that have been recently published.

关键词： XPO1 CRM1 nucleocytoplasmic transport Selinexor

Circadian Expression of Clock Gene and Bmall Gene in Peripheral Lymphocytes of Human

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Circadian Expression of Clock Gene and Bmall Gene in Periphe...

2009全国时间生物医学学术会议

作者：王洁薜建傅春玲 dept of physiology Medical School School of Radiation Medicine & Public Health Soochow University

This study was conducted to investigate the circadian expression of Clock gene and Bmall gene in the peripheral lymphocytes of healthy young adults under the natural environmental conditions with a 16 h light(07:00-23:00):8 h-dark(23:00-07:00)*** 5 days prior to laboratory admission, ten healthy male volunteers aged from24-30 had lived according to the rules,then they were sampled for the peripheral blood lymphocytes every 4 hours in a circadian *** total RNA was extracted from each sample and the quantitative real time reverse transcription polymerase chain reaction(RT-PCR) was used to determine the temporal changes in mRNA level of Clock geneand Bmall gene during different zeitgeber times(ZT).The data parameters were obtained andanalyzed by both the cosine function software and the amplitude F test to reveal the circadian *** the LD(16:8)condition,both the Clock and Bmall genemRNA levels in the peripheral lymphocytes of healthy young adults showed a significantly circadian oscillation(P<0.05),with the peak at ZT13 and trough at ZT1 of Clock gene,peak at ZT12 and trough at ZT24 of B mall *** findings suggest that the transcription of Clock geneand Bmall gene in the peripheral lymphocytes of human shows the remarkably circadian rhythmic changes.

关键词： Clock gene Bmall gene circadian rhythm peripheral lymphocytes human

Value of the adenosine test for diagnosis of dual AV nodal physiology in patients with AV nodal reentrant tachycardia

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Journal of Zhejiang University-Science A(Applied Physics & Engineering) 2002年第5期3卷 133-136页

作者：周斌全胡申江鲁端王建安 dept. of Cardiology Sir Run Run Shaw Hospital Medical College Zhejiang University Hangzhou China dept. of Cardiology First Affiliated Hospital Medical College Zhejiang University Hangzhou China

Objectives: This study was aimed at assessing the value of the adenosine test for noninvasive diagnosis of dual AV nodal physiology(DAVNP) in patients with AV nodal reentrant tachycardia (AVNRT). Methods: 53 patients with paroxysmal supraventricular tachycardia (PSVT) were given incremental doses of adenosine intravenously during sinus rhythm before electrophysiological study. The adenosine test was repeated on a subset of 18 patients with AVNRT after radiofrequency catheter ablation. Results: Sudden increments of PR interval of more than 60 msec between two consecutive beats were observed in 26(83.9%) of 31 patients with typical AVNRT and 2 (9.1%) of 22 patients with AVRT and AT ( P <0.01). The maximal PR increment between 2 consecutive beats in the AVNRT group(105±45ms) was significantly greater than that in the AVRT and AT group (20±13ms) ( P <0.01).In postablation adenosine test, DAVNP was eliminated in all 8 patients who underwent slow pathway abolition that EPS showed the slow pathway disappeared and 4 of 10 patients who underwent slow pathway modification that EPS showed the slow pathway persisted. Six of 10 patients who exhibited persistent duality showed a marked reduction in the number of beats conducted in the slow pathway after adenosine injection( P <0.01).Conclusions: Administration of adenosine during sinus rhythm may be a useful bedside test for diagnosis of DAVNP in high percentage of patients with typical AVNRT and additionally for evaluating the effects of radiofrequency ablation.

关键词： Adenosine Dual AV nodal Electrophysiology Tachycardia AV nodal reentrant

Oral mucosal conditions and some related factors in 140 Uygur centenarians

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Chinese medical Journal 2000年第4期113卷 70-72页

作者：邱洪晟刘漪白生义李翠芳冯咪咪 Urumqi Gen. Hosp. Lanzhou Mil. Regn. PLA Urumqi 830000 China Department of physiology Xinjiang Medical University Urumqi 830054 China Hlth. Sect. of Hetian Mil. Subarea PLA Hetian 848000 China Clin. Rear-Serv. dept. Xinjiang M. PLA Urumqi 830002 China

Objective To investigate the condition of the oral mucosae in Xinjiang Uygur centenarians and explore some related factors Methods The oral mucosae and mucosal exfoliative cells of 140 Xinjiang Uygur centenarians were examined Saliva and blood were collected from some centenarians Salivary immunoglobulins (IgA, IgM, IgG), complements (C 3 and C 4), nitrous oxide (NO), 10 trace elements, serum sex hormones, thyroid hormones and osteocalcin (OST) were analysed using immunoglobulin, complement and NO kits, an ionochromatophotometer, and the kits for sex hormones and thyroid hormones, and fluorescence enzyme linked immunosorbent assay, respectively Results Most centenarians (64 29%) had normal labial, buccal, palatal and gingival mucosae The abnormal changes in mucosae were mainly vascular nevus patches and senile plaques Their mucosal exfoliative cells showed similar characteristics to those in elderly Han The centenarians who had normal mucosae had higher level of the trace element molybdenum (Mo) in their saliva than who had abnormal mucosae ( P <0 01) Conclusion The oral mucosal condition of Uygur centenarians was generally good The abnormal changes in oral mucosae of the centenarians were lesions not harmful to health and may be related to the lower level of Mo in their saliva

关键词： centenarians oral mucosae salivary trace elements

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Permeability transition pore. AQP8 and mitochondrial water transport

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Permeability transition pore. AQP8 and mitochondrial water t...

第十五届国际药理学大会

作者： G.Calamita P.Gena M.Svelto dept General and Environmental physiology University of BariItaly dept General and Environmental physiology University of BariItaly dept General and Environmental physiology University of BariItaly

＜正＞ Although movement of water into and out of the mitochondrion is central for its shape and activity the molecular pathways of mitochondrial water transport remain mostly elusive. By stopped flow light scattering we found striking high water permeability of isolated rat liver mitochondria and low activation energy characterizing the related osmotic transport. Experiments with mitochondria using cyclosporin A （CsA）, an inhibitor of the opening of the permeability transition pore （PTP） acting as a mitochondrial coordinator of pro-apoptosis, and Hg + + , an ion blocking AQP8, the aquaporin water channel located in the inner mitochondrial membrane, indicated major roles for PTP and AQP8 in mediating the mitochondrial water transport. Targeting of these two water conductive pathways may be instrumental to act on the mitochondrial volume, a function that could be used to modulate cell death in an innovative therapeutic perspective.

关键词： Mitochondria apoptosis FTP aquaporin

Commentary:Can FXR serve as a potential target for COVID-19 prevention?

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Acta Pharmaceutica Sinica B 2023年第4期13卷 1786-1788页

作者： Juan Pang Jia Nuo Feng Wenhua Ling Tianru Jin Division of Nutrition School of Public HealthSun Yat-sen UniversityGuangzhou 510080China Banting and Best Diabetes Centre Faculty of MedicineUniversity of TorontoTorontoON M5G 2C4Canada dept.of physiology University of TorontoTorontoON M5G 1X8Canada Division of Advanced Diagnostics Toronto General Hospital Research InstituteUniversity Health NetworkTorontoON M5G 2C4Canada

A research article has been accepted by Nature very recently entitled:FXR inhibition may protect from SARS-CoV-2 infection by reducing *** is a multiple-author study by 80 scientists from 40 different research units in UK,Germany,Greece,USA,Austria,Sweden,and Norway,with Teresa Brevini as the 1st author and one of the senior authors^(1).The pre-print of this study was posted online back to June 7,2021(bioRxiv).

关键词： COVID-19 ACE2 FXR Bile acid

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Hepatic hormone FGF21 and its analogues in clinical trials

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Chronic Diseases and Translational Medicine 2022年第1期8卷 19-25页

作者： Weijuan Shao Tianru Jin Division of Advanced Diagnostics Toronto General Hospital Research InstituteUniversity Health NetworkTorontoOntarioCanada Department of physiology Faculty of MedicineUniversity of TorontoTorontoOntarioCanada Banting and Best Diabetes Center Faculty of MedicineUniversity of TorontoTorontoOntarioCanada

Fibroblast growth factor 21(FGF21)is a fasting or stress inducible metabolic hormone produced mainly in the *** plays important roles in regulating both glucose and lipid homeostasis via interacting with a heterodimeric receptor complex comprising FGF receptor 1(FGFR1)andβ-klotho(KLB).For the past decade,great effort has been made on developing FGF21 derivatives or specific FGF21 receptor agonists into therapeutic agents for various metabolic disorders including type 2 diabetes(T2D),obesity,and more importantly,nonalcoholic fatty liver disease(NAFLD).Here we have reviewed FGF21 gene and protein structures,its expression pattern,cellular signaling cascades that mediate FGF21 production and *** have then summarized the six clinical trials utilizing four FGF21 ***,two recent literatures on the development of GLP-1 and FGF21 dual agonists were presented briefly.

关键词： dual agonists fibroblast growth factor 21 lipid metabolism metabolic diseases

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CHARACTERIZATION AND DEVELOPMENTAL EXPRESSION OF TESTIS-SPECIFIC mRNA OF ADENOSINE DEAMINASE.

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CHARACTERIZATION AND DEVELOPMENTAL EXPRESSION OF TESTIS-SPEC...

第二次北京生育调节国际学术研讨会

作者： Ilpo Huhtaniemi Piojio Pakarinen dept.of physiology Turku University20520 TurkuFinland dept.of physiology Turku University20520 TurkuFinland

＜正＞During spermatogenesis,germ cells pass through series developmental phases before becoming matural *** process involves extensive biochemical and morphological restructuring *** activation of several genes has been reported at precise stages of differentiation,indicating their important physiological roles for the spermatogenesis.

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