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Rhynchophylline Loaded-Mpeg-PLGA Nanoparticles Coated with Tween-80 for Preliminary Study in Alzheimer's Disease
International Journal of Nanomedicine Dovepress open access to scientific and medical research Open Access Full Text Article ORIGINAL RESEARCH Rhynchophylline Loaded-mPEG-PLGA Nanoparticles Coated with Tween-80 for Preliminary Study in Alzheimer’sDisease This article was published in the following Dove Press journal: International Journal of Nanomedicine Ruiling Xu1 Purpose: Alzheimer’s disease (AD) is a growing concern in the modern society. The current Junying Wang1 drugs approved by FDA are not very promising. Rhynchophylline (RIN) is a major active Juanjuan Xu1 tetracyclic oxindole alkaloid stem from traditional Chinese medicine uncaria species, which fi Xiangrong Song2 has potential activities bene cial for the treatment of AD. However, the application of Hai Huang 2 rhynchophylline for AD treatment is restricted by the low water solubility, low concentration in brain tissue and low bioavailability. And there is no study of brain-targeting therapy with Yue Feng 3 RIN. In this work, we prepared rhynchophylline loaded methoxy poly (ethylene glycol)–poly Chunmei Fu1 (dl-lactide-co-glycolic acid) (mPEG-PLGA) nanoparticles (NPS-RIN), which coupled with 1Key Laboratory of Drug-Targeting and Tween 80 (T80) further for brain targeting delivery (T80-NPS-RIN). Drug Delivery System of the Education Methods: Preparation and characterization of T80-NPS-RIN were followed by the detection Ministry and Sichuan Province, Sichuan Engineering Laboratory for Plant-Sourced of transportation across the blood–brain barrier (BBB) model in vitro, biodistribution and Drug and Sichuan Research Center for neuroprotective effects of nanoparticles. Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan Results: The results indicated T80-NPS-RIN could usefully assist RIN to pass through the University, Chengdu 610041, People’s BBB to the brain. -
European Chemistry Congress June 16-18, 2016 Rome, Italy
conferenceseries.com conferenceseries.com 513th Conference European Chemistry Congress June 16-18, 2016 Rome, Italy Posters Page 98 Adriana A Lopes et al., Chem Sci J 2016, 7:2(Suppl) http://dx.doi.org/10.4172/2150-3494.C1.003 conferenceseries.com European Chemistry Congress June 16-18, 2016 Rome, Italy Unnatural fluoro-oxindole alkaloids produced by Uncaria guianensis plantlets Adriana A Lopes, Bruno Musquiari, Suzelei de C França and Ana Maria S Pereira Universidade de Ribeirão Preto, Brazil atural products and their analogues have been sources of numerous important therapeutic agents. The medicinal plant NU. guianensis (Rubiaceae) cultured in vitro produce four oxindole alkaloids that displays anti-tumoral activity. Natural products can be modified by several approaches, one of which is precursor-directed biosynthesis (PDB). Thus, the aim of this work was apply precursor-directed biosynthesis approach to obtain oxindole alkaloids analogues using in vitro Uncaria guianensis. Plantletes were cultivated into culture medium supplemented with 1mM of 6-fluoro-tryptamine, the indol precursor of alkaloids biosynthesis. U. guianensis explants were maintained at 25±2°C, 55-60% relative humidity under the same photoperiod and light intensity. After 30 days, a methanolic extract from U. guianensis was obtained and analysed by HPLC- DAD analytical procedure. The chromatogram showed four natural alkaloids (mitraphylline, isomitraphylline, rhynchophylline and isorhynchophylline and four additional peaks. Semi-preparative HPLC allowed isolation and purification of these four oxindole alkaloids analogues and the identity of the peaks was confirmed from high-resolution MS data (HRESIMS/MS in positive mode). All data confirmed that Uncaria guianensis produced fluoro-oxindole alkaloids analogues. -
Immunolocalization of Cannabinoid Receptor Type 1 and CB2 Cannabinoid Receptors, and Transient Receptor Potential Vanilloid Channels in Pterygium
MOLECULAR MEDICINE REPORTS 16: 5285-5293, 2017 Immunolocalization of cannabinoid receptor type 1 and CB2 cannabinoid receptors, and transient receptor potential vanilloid channels in pterygium MARTHA ASSIMAKOPOULOU1, DIONYSIOS PAGOULATOS1, PINELOPI NTERMA1 and NIKOLAOS PHARMAKAKIS2 Departments of 1Anatomy, Histology and Embryology, and 2Ophthalmology, School of Medicine, University of Patras, GR-26504 Rio, Greece Received July 27, 2016; Accepted January 19, 2017 DOI: 10.3892/mmr.2017.7246 Abstract. Cannabinoids, as multi-target mediators, acti- CB2 (P>0.05). Additionally, CB1 and CB2 were significantly vate cannabinoid receptors and transient receptor potential highly expressed in primary pterygia (P=0.01), compared with vanilloid (TRPV) channels. There is evidence to support a recurrent pterygia. Furthermore, CB1 expression levels were functional interaction of cannabinoid receptors and TRPV significantly correlated with CB2 expression levels in primary channels when they are coexpressed. Human conjunctiva pterygia (P=0.005), but not in recurrent pterygia (P>0.05). demonstrates widespread cannabinoid receptor type 1 (CB1), No significant difference was detected for all TRPV channel CB2 and TRPV channel localization. The aim of the present expression levels between pterygium (primary or recurrent) study was to investigate the expression profile for cannabinoid and conjunctival tissues (P>0.05). A significant correlation receptors (CB1 and CB2) and TRPV channels in pterygium, between the TRPV1 and TRPV3 expression levels (P<0.001) an ocular surface lesion originating from the conjunctiva. was detected independently of pterygium recurrence. Finally, Semi‑serial paraffin‑embedded sections from primary and TRPV channel expression was identified to be significantly recurrent pterygium samples were immunohistochemically higher than the expression level of cannabinoid receptors in the examined with the use of specific antibodies. -
Note: the Letters 'F' and 'T' Following the Locators Refers to Figures and Tables
Index Note: The letters ‘f’ and ‘t’ following the locators refers to figures and tables cited in the text. A Acyl-lipid desaturas, 455 AA, see Arachidonic acid (AA) Adenophostin A, 71, 72t aa, see Amino acid (aa) Adenosine 5-diphosphoribose, 65, 789 AACOCF3, see Arachidonyl trifluoromethyl Adlea, 651 ketone (AACOCF3) ADP, 4t, 10, 155, 597, 598f, 599, 602, 669, α1A-adrenoceptor antagonist prazosin, 711t, 814–815, 890 553 ADPKD, see Autosomal dominant polycystic aa 723–928 fragment, 19 kidney disease (ADPKD) aa 839–873 fragment, 17, 19 ADPKD-causing mutations Aβ, see Amyloid β-peptide (Aβ) PKD1 ABC protein, see ATP-binding cassette protein L4224P, 17 (ABC transporter) R4227X, 17 Abeele, F. V., 715 TRPP2 Abbott Laboratories, 645 E837X, 17 ACA, see N-(p-amylcinnamoyl)anthranilic R742X, 17 acid (ACA) R807X, 17 Acetaldehyde, 68t, 69 R872X, 17 Acetic acid-induced nociceptive response, ADPR, see ADP-ribose (ADPR) 50 ADP-ribose (ADPR), 99, 112–113, 113f, Acetylcholine-secreting sympathetic neuron, 380–382, 464, 534–536, 535f, 179 537f, 538, 711t, 712–713, Acetylsalicylic acid, 49t, 55 717, 770, 784, 789, 816–820, Acrolein, 67t, 69, 867, 971–972 885 Acrosome reaction, 125, 130, 301, 325, β-Adrenergic agonists, 740 578, 881–882, 885, 888–889, α2 Adrenoreceptor, 49t, 55, 188 891–895 Adult polycystic kidney disease (ADPKD), Actinopterigy, 223 1023 Activation gate, 485–486 Aframomum daniellii (aframodial), 46t, 52 Leu681, amino acid residue, 485–486 Aframomum melegueta (Melegueta pepper), Tyr671, ion pathway, 486 45t, 51, 70 Acute myeloid leukaemia and myelodysplastic Agelenopsis aperta (American funnel web syndrome (AML/MDS), 949 spider), 48t, 54 Acylated phloroglucinol hyperforin, 71 Agonist-dependent vasorelaxation, 378 Acylation, 96 Ahern, G. -
PCHHAX Comparative Phytochemical and Pharmacological Study Of
Available online a t www.derpharma chemica.com ISSN 0975-413X Der Pharma Chemica, 2016, 8(1):67-83 CODEN (USA): PCHHAX (http://derpharmachemica.com/archive.html) Comparative phytochemical and pharmacological study of antitussive and antimicrobial effects of boswellia and thyme essential oils Kamilia F. Taha 1, Mona H. Hetta 2, Walid I. Bakeer 3, Nemat A. Z. Yassin 4, Bassant M. M. Ibrahim 4 and Marwa E. S. Hassan 1 1Phytochemistry Department, Applied Research Center of Medicinal Plants, National Organization for Drug Control and Research (NODCAR), Egypt 2Pharmacognosy Department, Fayoum University, Fayoum, Egypt 3Microbiology Department, Beni -Suef University, Egypt 4Pharmacology Department, National Research Centre, Dokki, Giza, Egypt _____________________________________________________________________________________________ ABSTRACT Essential oils are commonly used in herbal cough mixtures as antitussive and antimicrobial preparations, for instance Thyme oil is used in many cough preparations in the Egyptian market and also Boswellia oil is traditionally used as an antitussive. The aim of this study is to compare the antitussive and antimicrobial activity of essential oils of Boswellia carterii and Thymus vulgaris referring to their chemical components which were studied by using different methods of analysis (UV, HPTLC, HPLC, GC and GC/MS). HPLC technique was used for the first time for analysis of Boswellia oil. Results showed that the principal component of Boswellia oil was octyl acetate (35.1%), while the major constituent of Thyme oil was thymol (51%). Both oils were effective as antitussives but Thyme oil was more efficient (89.3%) than Boswellia oil (59%) and also as antimicrobial. It could be concluded that Thyme and Boswellia oils are effective as antitussives but less with Boswellia oil which could serve as an adjuvant in herbal cough mixture but cannot replace Thyme oil. -
Research Article Antidepressant-Like Activity of the Ethanolic Extract from Uncaria Lanosa Wallich Var. Appendiculata Ridsd in T
Hindawi Publishing Corporation Evidence-Based Complementary and Alternative Medicine Volume 2012, Article ID 497302, 12 pages doi:10.1155/2012/497302 Research Article Antidepressant-Like Activity of the Ethanolic Extract from Uncaria lanosa Wallich var. appendiculata Ridsd in the Forced Swimming Test and in the Tail Suspension Test in Mice Lieh-Ching Hsu,1 Yu-Jen Ko,1 Hao-Yuan Cheng,2 Ching-Wen Chang,1 Yu-Chin Lin,3 Ying-Hui Cheng,1 Ming-Tsuen Hsieh,1 and Wen Huang Peng1 1 School of Chinese Pharmaceutical Sciences and Chinese Medicine Resources, College of Pharmacy, China Medical University, No. 91 Hsueh-Shih Road, Taichung 404, Taiwan 2 Department of Nursing, Chung Jen College of Nursing, Health Sciences and Management, No. 1-10 Da-Hu, Hu-Bei Village, Da-Lin Township, Chia-Yi 62241, Taiwan 3 Department of Biotechnology, TransWorld University, No. 1221, Jen-Nang Road, Chia-Tong Li, Douliou, Yunlin 64063, Taiwan Correspondence should be addressed to Hao-Yuan Cheng, [email protected] and Wen Huang Peng, [email protected] Received 23 November 2011; Revised 30 January 2012; Accepted 30 January 2012 Academic Editor: Vincenzo De Feo Copyright © 2012 Lieh-Ching Hsu et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. This study investigated the antidepressant activity of ethanolic extract of U. lanosa Wallich var. appendiculata Ridsd (ULEtOH)for two-weeks administrations by using FST and TST on mice. In order to understand the probable mechanism of antidepressant-like activity of ULEtOH in FST and TST, the researchers measured the levels of monoamines and monoamine oxidase activities in mice brain, and combined the antidepressant drugs (fluoxetine, imipramine, maprotiline, clorgyline, bupropion and ketanserin). -
Ep 1553091 A1
Europäisches Patentamt *EP001553091A1* (19) European Patent Office Office européen des brevets (11) EP 1 553 091 A1 (12) EUROPEAN PATENT APPLICATION published in accordance with Art. 158(3) EPC (43) Date of publication: (51) Int Cl.7: C07D 263/32, C07D 417/14, 13.07.2005 Bulletin 2005/28 C07D 333/20, C07D 413/12, C07D 417/06 (21) Application number: 04726765.3 (86) International application number: (22) Date of filing: 09.04.2004 PCT/JP2004/005119 (87) International publication number: WO 2004/089918 (21.10.2004 Gazette 2004/43) (84) Designated Contracting States: • SAKAMOTO, Johei AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Takatsuki-shi, Osaka 569-1125 (JP) HU IE IT LI LU MC NL PL PT RO SE SI SK TR • NAKANISHI, Hiroyuki Designated Extension States: Takatsuki-shi, Osaka 569-1125 (JP) AL HR LT LV MK • NAKAGAWA, Yuichi Takatsuki-shi, Osaka 569-1125 (JP) (30) Priority: 09.04.2003 JP 2003105267 • OHTA, Takeshi 03.06.2003 JP 2003157590 Takatsuki-shi, Osaka 569-1125 (JP) • SAKATA, Shohei (71) Applicant: Japan Tobacco Inc. Takatsuki-shi, Osaka 569-1125 (JP) Tokyo 105-8422 (JP) • MORINAGA, Hisayo Takatsuki-shi, Osaka 569-1125 (JP) (72) Inventors: • IKEMOTO, Tomoyuki (74) Representative: Takatsuki-shi, Osaka 569-1125 (JP) von Kreisler, Alek, Dipl.-Chem. et al • TANAKA, Masahiro Deichmannhaus am Dom, Takatsuki-shi, Osaka 569-1125 (JP) Postfach 10 22 41 • YUNO, Takeo 50462 Köln (DE) Takatsuki-shi, Osaka 569-1125 (JP) (54) HETEROAROMATIC PENTACYCLIC COMPOUND AND MEDICINAL USE THEREOF (57) A 5-membered heteroaromatic ring compound represented by the formula [I] 1 2 4 5 7 wherein V is CH or N; W is S or O; R and R are each H etc.; X is -N(R )-, -O-, -S-, -SO2-N(R )-, -CO-N(R )- etc.; L is EP 1 553 091 A1 Printed by Jouve, 75001 PARIS (FR) (Cont. -
Transient Receptor Potential Channels and Metabolism
Molecules and Cells Minireview Transient Receptor Potential Channels and Metabolism Subash Dhakal and Youngseok Lee* Department of Bio and Fermentation Convergence Technology, Kookmin University, BK21 PLUS Project, Seoul 02707, Korea *Correspondence: [email protected] https://doi.org/10.14348/molcells.2019.0007 www.molcells.org Transient receptor potential (TRP) channels are nonselective Montell, 2007). These cationic channels were first charac- cationic channels, conserved among flies to humans. Most terized in the vinegar fly, Drosophila melanogaster. While TRP channels have well known functions in chemosensation, a visual mechanism using forward genetic screening was thermosensation, and mechanosensation. In addition to being studied, a mutant fly showed a transient response to being sensing environmental changes, many TRP channels constant light instead of the continuous electroretinogram are also internal sensors that help maintain homeostasis. response recorded in the wild type (Cosens and Manning, Recent improvements to analytical methods for genomics 1969). Therefore, the mutant was named as transient recep- and metabolomics allow us to investigate these channels tor potential (trp). In the beginning, researchers had spent in both mutant animals and humans. In this review, we two decades discovering the trp locus with the germ-line discuss three aspects of TRP channels, which are their role transformation of the genomic region (Montell and Rubin, in metabolism, their functional characteristics, and their 1989). Using a detailed structural permeation property anal- role in metabolic syndrome. First, we introduce each TRP ysis in light-induced current, the TRP channel was confirmed channel superfamily and their particular roles in metabolism. as a six transmembrane domain protein, bearing a structural Second, we provide evidence for which metabolites TRP resemblance to a calcium-permeable cation channel (Mon- channels affect, such as lipids or glucose. -
7Th World Congress on ADHD: from Child to Adult Disorder
ADHD Atten Def Hyp Disord (2019) 11(Suppl 1):S1–S89 https://doi.org/10.1007/s12402-019-00295-7 ABSTRACTS Ó Springer-Verlag GmbH Austria, part of Springer Nature 2019 7th World Congress on ADHD: From Child to Adult Disorder 25th–28th April, Lisbon Portugal Editors: Manfred Gerlach, Wu¨rzburg Peter Riederer, Wu¨rzburg Andreas Warnke, Wu¨rzburg Luis Rohde, Porto Alegre 123 S2 ABSTRACTS Introduction Dear Colleagues and Friends, We are pleased to have received more than 180 poster abstracts as well as more than 100 poster abstracts from young scientists and clinicians (\ 35 years) who applied for our Young Scientists’ Award. Of all abstracts submitted by our young colleagues, the Scientific Programme Committee has selected the best eight. The authors have been invited to give a presentation as part of our two Young Scientist Award Sessions and to receive a prize money in the amount of 500 Euros. With this approach, we intend to highlight the importance of original scientific contributions, especially from our young colleagues. In this volume, the abstracts of our two Young Scientist Award Sessions come first, followed by regular poster abstracts. These have been organized by topics: Aetiology, Autism Spectrum Disorders, Co-morbidity, Diagnosis, Electrophysiology, Epidemiology, Experimental Models, Genetics, Neuroimaging, Non-pharmacological Treatment, Pathophysiology, Pharmacological Treatment, Quality of Life/Caregiver Burden, Substance Use Disorders and Miscellaneous. Submitted abstracts have not been modified in any way. Please, do not just read the selected poster abstracts, we also encourage you to actively discuss and share your ideas with our young colleagues. Finally, we would like thank all our speakers, contributors and sponsors of our 7th World Congress on ADHD: from Childhood to Adult Disease, and welcome you to join—what we are sure will be—a very enjoyable and highly informative event. -
Download Product Insert (PDF)
PRODUCT INFORMATION Terpene Screening Library Item No. 9003370 • Batch No. 0611615 Panels are routinely re-evaluated to include new catalog introductions as the research evolves. Page 1 of 4 Plate Well Contents Item Number 1 A1 Unused 1 A2 Ursolic Acid 10072 1 A3 Forskolin 11018 1 A4 Betulin 11041 1 A5 Lupeol 11215 1 A6 Paxilline 11345 1 A7 β-acetyl-Boswellic Acid 11674 1 A8 Andrographolide 11679 1 A9 Bakuchiol 11684 1 A10 Betulinic Acid 11686 1 A11 β-Elemonic Acid 11712 1 A12 Unused 1 B1 Unused 1 B2 Oleanolic Acid 11726 1 B3 Neoandrographolide 11742 1 B4 Asiatic Acid 11818 1 B5 Madecassic Acid 11854 1 B6 Cafestol 13999 1 B7 Ingenol 14031 1 B8 Bilobalide 14272 1 B9 (−)-Huperzine A 14620 1 B10 Ginkgolide B 14636 1 B11 Cucurbitacin B 14820 1 B12 Unused 1 C1 Unused 1 C2 Cucurbitacin E 14821 1 C3 Polygodial 14979 1 C4 Zerumbone 15400 1 C5 Ingenol-3-angelate 16207 1 C6 Ferutinin 16554 1 C7 Limonin 16932 1 C8 Phytol 17401 1 C9 Dehydrocostus lactone 18485 1 C10 β-Elemene 19641 1 C11 Juvenile Hormone III 19646 1 C12 Unused WARNING CAYMAN CHEMICAL THIS PRODUCT IS FOR RESEARCH ONLY - NOT FOR HUMAN OR VETERINARY DIAGNOSTIC OR THERAPEUTIC USE. 1180 EAST ELLSWORTH RD SAFETY DATA ANN ARBOR, MI 48108 · USA This material should be considered hazardous until further information becomes available. Do not ingest, inhale, get in eyes, on skin, or on clothing. Wash thoroughly after handling. Before use, the user must review the complete Safety Data Sheet, which has been sent via email to your institution. -
(12) Patent Application Publication (10) Pub. No.: US 2015/0038576A1 Timokhina Et Al
US 20150.038576A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2015/0038576A1 Timokhina et al. (43) Pub. Date: Feb. 5, 2015 (54) COMPOSITIONS AND THEIR USE FOR A24F 47/00 (2006.01) SMOKING CESSATION AND OTHER A63L/2 (2006.01) TREATMENTS A63L/II (2006.01) (71) Applicant: SENTIENS, LLC, Charlotte, NC (US) A6M I5/00 (2006.01) A63L/25 (2006.01) (72) Inventors: Inna S. Timokhina, Potomac, MD (US); A63L/343 (2006.01) Reid von Borstel, Potomac, MD (US); (52) U.S. Cl DennisMSG Tan, Weddington,NEW, NC 'S(US): CPCAV e. we............... A24B 15/16 (2013.01); A61 K3I/125 s s (2013.01); A61 K3I/05 (2013.01); A61 K (73) Assignee: SENTIENS, LLC, Charlotte, NC (US) 3 1/343 (2013.01); A61 K31/12 (2013.01); A6 IK3I/II (2013.01); A61M 15/009 (21) Appl. No.: 14/449,533 (2013.01); A24F 47/008 (2013.01) USPC ........... 514/470; 13 1/270; 13 1/273: 514/692; (22) Filed: Aug. 1, 2014 514/731: 514/678; 514/701: 128/200.14; 128/202.21 Related U.S. Application Data (60) Provisional application No. 61/861,865, filed on Aug. 2, 2013. (57) ABSTRACT Publication Classification A composition includes a liquid. The liquid aerosolizes for (51) Int. Cl. delivery to a user by an airway. The liquid includes an agent A24B 15/16 (2006.01) that activates a TRPV3 channel. The agent includes a terpe A6 IK3I/05 (2006.01) noid compound. Patent Application Publication Feb. 5, 2015 US 2015/0038576 A1 covC s US 2015/0038576 A1 Feb. -
Camphor Elicits Up-Regulation of Hepatic and Pulmonary Pro
Pathophysiology 26 (2019) 305–313 Contents lists available at ScienceDirect Pathophysiology jo urnal homepage: www.elsevier.com/locate/pathophys Camphor elicits up-regulation of hepatic and pulmonary pro-inflammatory cytokines and chemokines via activation of NF-kB in rats a,∗ b a a Oluwatobi T. Somade , Babajide O. Ajayi , Nurudeen O. Tajudeen , Eniola M. Atunlute , a a Adewale S. James , Samuel A. Kehinde a Department of Biochemistry, College of Biosciences, Federal University of Agriculture, Abeokuta, Nigeria b Department of Biochemistry, Bowen University, Iwo, Nigeria a r t i c l e i n f o a b s t r a c t Article history: Consumption of camphor infusions is widely used as an aphrodisiac in preparation for sexual intercourse, Received 10 April 2019 to boost performance. There is dearth of information associating or relating its consumption to liver or Received in revised form 8 May 2019 lung inflammation. Therefore, we investigated the effect of various doses of camphor in an acute study, Accepted 28 July 2019 on hepatic and pulmonary levels of some pro-inflammatory cytokines and chemokines in male wistar rats. Following administration, 2000 and 4000 mg/kg body weight camphor significantly increase liver Keywords: and lung levels of tumor necrosis factor alpha (TNF-␣), interleukin 1 beta (IL-1) and interleukin 6 (IL-6) Camphor in a dose dependent manner compared with control, while interleukin 10 (IL-10) levels were significantly Chemokines Cytokines increased only by 1000 and 4000 mg/kg body weight camphor in liver and lung respectively, compared Hepatic with control. Also compared with control, camphor administration resulted in a significant increase in the Pro-inflammation expressions of hepatic and pulmonary nuclear factor kappa B (NFkB), cyclooxygenase 2 (COX-2), regulated Pulmonary upon activation normal T cell expressed and secreted (RANTES) or CCL5, and monocyte chemo-attractant protein 1 (MCP-1) in a dose dependent manner.