(12) Patent Application Publication (10) Pub. No.: US 2016/0122430 A1 Gish Et Al
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Grape Seeds Proanthocyanidins: Advanced Technological Preparation and Analytical Characterization
antioxidants Article Grape Seeds Proanthocyanidins: Advanced Technological Preparation and Analytical Characterization Paolo Morazzoni 1, Paola Vanzani 2, Sandro Santinello 1, Antonina Gucciardi 2,3 , Lucio Zennaro 2, Giovanni Miotto 2,3,4,* and Fulvio Ursini 2,* 1 Distillerie Bonollo Umberto S.p.A., Nutraceutical Division, Mestrino, 35035 Padova, Italy; [email protected] (P.M.); [email protected] (S.S.) 2 Department of Molecular Medicine, University of Padova, 35129 Padova, Italy; [email protected] (P.V.); [email protected] (A.G.); [email protected] (L.Z.) 3 Proteomics Center, University of Padova and Azienda Ospedaliera di Padova, 35129 Padova, Italy 4 CRIBI Biotechnology Center, University of Padova, 35129 Padova, Italy * Correspondence: [email protected] (G.M.); [email protected] (F.U.); Tel.: +39-0498276130 (G.M.); +39-0498276104 (F.U.) Abstract: A “green” solvent-free industrial process (patent pending) is here described for a grape seed extract (GSE) preparation (Ecovitis™) obtained from selected seeds of Veneto region wineries, in the northeast of Italy, by water and selective tangential flow filtration at different porosity. Since a comprehensive, non-ambiguous characterization of GSE is still a difficult task, we resorted to using an integrated combination of gel permeation chromatography (GPC) and electrospray ionization high resolution mass spectrometry (ESI-HRMS). By calibration of retention time and spectroscopic quantification of catechin as chromophore, we succeeded in quantifying GPC polymers up to traces at Citation: Morazzoni, P.; Vanzani, P.; n = 30. The MS analysis carried out by the ESI-HRMS method by direct-infusion allows the detection Santinello, S.; Gucciardi, A.; Zennaro, of more than 70 species, at different polymerization and galloylation, up to n = 13. -
Inhibitory Activity of Synthesized Acetylated Procyanidin B1 Analogs Against Hela S3 Cells Proliferation
Molecules 2014, 19, 1775-1785; doi:10.3390/molecules19021775 OPEN ACCESS molecules ISSN 1420-3049 www.mdpi.com/journal/molecules Article Inhibitory Activity of Synthesized Acetylated Procyanidin B1 Analogs against HeLa S3 Cells Proliferation Syuhei Okamoto 1, Sayaka Ishihara 1, Taisuke Okamoto 1, Syoma Doi 1, Kota Harui 1, Yusuke Higashino 1, Takashi Kawasaki 2, Noriyuki Nakajima 3,* and Akiko Saito 1,* 1 Graduate School of Engineering, Osaka Electro-communication University (OECU), 18-8 Hatsu-cho, Neyagawa-shi, Osaka 572-8530, Japan; E-Mails: [email protected] (S.O.); [email protected] (S.I.); [email protected] (T.O.); [email protected] (S.D.); [email protected] (K.H.); [email protected] (Y.H.) 2 Department of Pharmaceutical Sciences, Ritsumeikan University, 1-1-1 Nojihigashi, Kusatsu, Shiga 525-8577, Japan; E-Mail: [email protected] 3 Biotechnology Research Center and Department of Biotechnology, Toyama Prefectural University, 5180 Kurokawa, Imizu, Toyama 939-0398, Japan * Authors to whom correspondence should be addressed; E-Mails: [email protected] (N.N.); [email protected] (A.S.); Tel.: +81-766-56-7500 (N.N.); Fax: +81-766-56-2498 (N.N.); Tel.: +81-72-824-1131 (A.S.); Fax: +81-72-824-0014 (A.S.). Received: 19 November 2013; in revised form: 22 January 2014 / Accepted: 28 January 2014 / Published: 4 February 2014 Abstract: Proanthocyanidins, also known as condensed tannins and/or oligomeric flavonoids, occur in many edible plants and have various interesting biological activities. Previously, we reported a synthetic method for the preparation of various procyanidins in pure form and described their biological activities. -
Seattle Genetics and Genmab Enter Into New Antibody-Drug Conjugate Collaboration
Seattle Genetics and Genmab Enter Into New Antibody-Drug Conjugate Collaboration Company Announcement • Additional collaboration combines Genmab’s proprietary antibodies and Seattle Genetics’ ADC technology • New ADC program will target AXL expressed on multiple tumor types Bothell, WA and Copenhagen, Denmark; September 10, 2014 – Seattle Genetics, Inc. (Nasdaq: SGEN) and Genmab A/S (OMX: GEN) today announced that the companies have entered into an additional antibody-drug conjugate (ADC) collaboration. Under the new agreement, Genmab will pay an upfront fee of $11 million for exclusive rights to utilize Seattle Genetics’ auristatin-based ADC technology with Genmab’s HuMax®-AXL, an antibody targeting AXL which is expressed on multiple types of solid cancers. Seattle Genetics is also entitled to receive more than $200 million in potential milestone payments and mid-to-high single digit royalties on worldwide net sales of any resulting products. In addition, prior to Genmab’s initiation of a Phase III study for any resulting products, Seattle Genetics has the right to exercise an option to increase the royalties to double digits in exchange for a reduction of the milestone payments owed by Genmab. Irrespective of any exercise of option, Genmab remains in full control of development and commercialization. “This collaboration with Genmab further extends the reach of our industry-leading ADC technology for use with novel oncology targets, while providing us with a compelling financial value proposition as the program advances,” said Natasha -
Determination of Total Procyanidins in Selected Chocolate and Confectionery Products Using DMAC
SPSFAM-FLAV-11 Based from Call for Methods 12-21-2011 PAYNE ET AL.: JOURNAL OF AOAC INTERNATIONAL VOL. 93, NO. 1, 2010 89 DIETARY SUPPLEMENTS Determination of Total Procyanidins in Selected Chocolate and Confectionery Products Using DMAC MARK J. PAYNE,WILLIAM JEFFREY HURST,andDAVI D A. STUART Hershey Center for Health and Nutrition, The Hershey Co., 1025 Reese Ave, Hershey, PA 17033 BOXIN OU and ELLEN FAN Brunswick Laboratories (USA), 50 Commerce Way, Norton, MA 02766 HONGPING JI and YAN KOU Brunswick Laboratories (China), 218 Xing Hu Rd, Suzhou Industrial Park, China 215125 A simple, specific, high-throughput colorimetric which the monomers are linked through C4÷C8 or, less method based on the reaction of frequently, C4÷C6 linkages. In the less common A-type 4-dimethylaminocinnamaldehyde (DMAC) with procyanidins, the monomers are connected through C2÷O÷C7 flavan-3-ols was developed to determine total or C2÷O÷C5 linkages. Procyanidins are widely distributed in procyanidins in selected cacao-based products. plants and are found in significant quantities in foods such as Extracts of defatted samples were dispensed into a fruits, spices, tea, wine, nuts, and cocoa (1). Of the many types of 96-well plate and reacted with DMAC. The polyphenols, flavan-3-ols, flavonols, and anthocyanidins are the absorbance of the reaction products was most abundant classes found in plants (2). The interest in measured at 640 nm and compared to polyphenol antioxidants has increased dramatically due to their commercially available procyanidin B2 as a ability to scavenge free radicals and their association with a standard. -
Proanthocyanidin Metabolism, a Mini Review
Nutrition and Aging 2 (2014) 111–116 111 DOI 10.3233/NUA-140038 IOS Press Proanthocyanidin Metabolism, a mini review Y.Y. Choy and A.L. Waterhouse∗ Viticulture and Enology, University of California, Davis, CA, USA Abstract. There is emerging evidence suggesting that consumption of beverage and food rich in polyphenol may offer protective effects against various neurodegenerative, cardiovascular diseases and cancers. Proanthocyanidins (PACs) are one of the most abundant polyphenol in human diets, but also one of the least absorbed polyphenol mostly due to their size and structure com- plexity. PACs or condensed tannins are oligomers and polymers of monomeric unit flavan-3-ol (+)-catechin or (−)-epicatechin. To date, the absorption and metabolism of PACs are still remains largely unknown. The aim of this mini review was to highlight the absorption and metabolism of PACs, their effect in the gut and sample preparation for analysis. Ultimately, the potential bioactivities derived from the interaction between PACs metabolites and the gut microbiota warrants further investigation. Keywords: Proanthocyanidins, phenolic acids, metabolism, colon 1. Introduction derived subunits. PACs that consists exclusively of (−)-epicatechin, (+)-catechin units, are known as pro- Polyphenols are among the ubiquitous constituents cyanidins because only cyanidin is released in acid, of foods of plant origins and are widely distributed and comprised the largest class of PACs, while those throughout the plant kingdom. Polyphenols can be with gallocatechin units release delphinidin. The size categorized into different groups such as flavonoids, or molecular weight of PACs can be expressed as phenolic acids, stilbenes and lignans. The flavonoids mean degree of polymerization (mDP). -
Homogeneous Antibody-Drug Conjugates Via Site-Selective Disulfide Bridging
Homogeneous antibody-drug conjugates via site-selective disulfide bridging Nafsika Forte, Vijay Chudasama, and James R. Baker* Department of Chemistry, University College London, London, UK; email: [email protected] Antibody-drug conjugates (ADCs) constructed using site-selective labelling methodologies are likely to dominate the next generation of these targeted therapeutics. To this end, disulfide bridging has emerged as a leading strategy as it allows the production of highly homogeneous ADCs without the need for antibody engineering. It consists of targeting reduced interchain disulfide bonds with reagents which reconnect the resultant pairs of cysteine residues, whilst simultaneously attaching drugs. The 3 main reagent classes which have been exemplified for the construction of ADCs by disulfide bridging will be discussed in this review; bissulfones, next generation maleimides and pyridazinediones, along with others in development. Introduction In the past decades, the potential of monoclonal antibodies (mAbs) in targeted therapy against cancer has been realized, with the market of therapeutic antibodies currently being the fastest growing sector in the pharmaceutical industry. While unmodified antibodies have demonstrated unprecedented activities in the clinic, their action can also be synergistically improved by arming them with cytotoxic drugs to create a new class of targeted therapy, i.e. antibody-drug conjugates (ADCs).1,2 This strategy has great potential to dramatically reduce the side-effects observed with standard chemotherapy, -
Antibody–Drug Conjugates: the Last Decade
pharmaceuticals Review Antibody–Drug Conjugates: The Last Decade Nicolas Joubert 1,* , Alain Beck 2 , Charles Dumontet 3,4 and Caroline Denevault-Sabourin 1 1 GICC EA7501, Equipe IMT, Université de Tours, UFR des Sciences Pharmaceutiques, 31 Avenue Monge, 37200 Tours, France; [email protected] 2 Institut de Recherche Pierre Fabre, Centre d’Immunologie Pierre Fabre, 5 Avenue Napoléon III, 74160 Saint Julien en Genevois, France; [email protected] 3 Cancer Research Center of Lyon (CRCL), INSERM, 1052/CNRS 5286/UCBL, 69000 Lyon, France; [email protected] 4 Hospices Civils de Lyon, 69000 Lyon, France * Correspondence: [email protected] Received: 17 August 2020; Accepted: 10 September 2020; Published: 14 September 2020 Abstract: An armed antibody (antibody–drug conjugate or ADC) is a vectorized chemotherapy, which results from the grafting of a cytotoxic agent onto a monoclonal antibody via a judiciously constructed spacer arm. ADCs have made considerable progress in 10 years. While in 2009 only gemtuzumab ozogamicin (Mylotarg®) was used clinically, in 2020, 9 Food and Drug Administration (FDA)-approved ADCs are available, and more than 80 others are in active clinical studies. This review will focus on FDA-approved and late-stage ADCs, their limitations including their toxicity and associated resistance mechanisms, as well as new emerging strategies to address these issues and attempt to widen their therapeutic window. Finally, we will discuss their combination with conventional chemotherapy or checkpoint inhibitors, and their design for applications beyond oncology, to make ADCs the magic bullet that Paul Ehrlich dreamed of. Keywords: antibody–drug conjugate; ADC; bioconjugation; linker; payload; cancer; resistance; combination therapies 1. -
2019, 17–28 Assessment of Antioxidants by Hplc-Ms in Grapevine Seeds
Acta Sci. Pol. Hortorum Cultus, 18(6) 2019, 17–28 https://czasopisma.up.lublin.pl/index.php/asphc ISSN 1644-0692 e-ISSN 2545-1405 DOI: 10.24326/asphc.2019.6.2 ORIGINAL PAPER Accepted: 4.03.2019 ASSESSMENT OF ANTIOXIDANTS BY HPLC-MS IN GRAPEVINE SEEDS Lenka Sochorova1, Borivoj Klejdus2, Mojmir Baron1, Tunde Jurikova3, Jiri Mlcek4, Jiri Sochor1, Sezai Ercisli5, Muhammed Kupe5 1 Department of Viticulture and Enology, Faculty of Horticulture, Mendel University in Brno, Valticka 337, CZ-691 44 Lednice, Czech Republic 2 Department of Chemistry and Biochemistry, Faculty of Agronomy, Mendel University in Brno, Zemedelska 1, CZ-613 00 Brno, Czech Republic 3 Department of Natural and Informatics Sciences, Faculty of Central European Studies, Constantine the Philosopher University in Nitra, Drazovska 4, 949 74 Nitra, Slovakia 4 Department of Food Analysis and Chemistry, Faculty of Technology, Tomas Bata University in Zlin, nam. T. G. Masaryka 5555, 760 01 Zlin Czech Republic 5 Department of Horticulture, Agricultural Faculty, Ataturk University, 25240 Erzurum, Turkey ABSTRACT It is well known, that grapevine seeds are rich in significant antioxidants. However, the issue of dealing with the analysis and comparison of antioxidant components in the seeds of Vitis vinifera L. in individual cultivars has not yet been sufficiently studied. The experiment was performed with extracts of three varieties (Blaufränkish, Italian Riesling and Cabernet Moravia) and three interspecific cultivars (Nativa, Marlen and Kofranka). Contents of nine major flavonoids (apigenin, astragalin, hyperoside, isorhamnetin, kaempferol, myricetin, quercetin, quercitrin and rutin) and two procyanidins (procyanidin A2 and procyanidin B1) were assessed by the HPLC/MS method. -
Targeting and Efficacy of Novel Mab806-Antibody-Drug Conjugates in Malignant Mesothelioma
pharmaceuticals Article Targeting and Efficacy of Novel mAb806-Antibody-Drug Conjugates in Malignant Mesothelioma 1,2,3, 1,3,4, 5 5 Puey-Ling Chia y, Sagun Parakh y, Ming-Sound Tsao , Nhu-An Pham , Hui K. Gan 1,2,3,4, Diana Cao 1, Ingrid J. G. Burvenich 1,2 , Angela Rigopoulos 1, Edward B. Reilly 6, Thomas John 1,2,3,4,* and Andrew M. Scott 1,2,4,7,* 1 Tumour Targeting Laboratory, Olivia Newton-John Cancer Research Institute, Melbourne, Victoria 3084, Australia; [email protected] (P.-L.C.); [email protected] (S.P.); [email protected] (H.K.G.); [email protected] (D.C.); [email protected] (I.J.G.B.); [email protected] (A.R.) 2 Faculty of Medicine, University of Melbourne, Melbourne, Victoria 3010, Australia 3 Department of Medical Oncology, Austin Health, Melbourne, Victoria 3084, Australia 4 School of Cancer Medicine, La Trobe University, Plenty Rd &, Kingsbury Dr, Bundoora, Victoria 3086, Australia 5 Princess Margaret Cancer Centre, University Health Network, Toronto, ON M5G 2C1, Canada; [email protected] (M.-S.T.); [email protected] (N.-A.P.) 6 AbbVie Inc., North Chicago, IL 60064, USA; [email protected] 7 Department of Molecular Imaging and Therapy, Austin Health, Melbourne, Victoria 3084, Australia * Correspondence: [email protected] (T.J.); [email protected] (A.M.S.); Tel.: +61-39496-5876 (A.M.S.); Fax: +61-39496-5334 (A.M.S.) These authors contributed equally to this work. y Received: 7 September 2020; Accepted: 28 September 2020; Published: 2 October 2020 Abstract: Epidermal growth factor receptor (EGFR) is highly overexpressed in malignant mesothelioma (MM). -
Docking Characterization and in Vitro Inhibitory Activity of Flavan-3-Ols and Dimeric Proanthocyanidins Against the Main Protease Activity of SARS-Cov-2
ORIGINAL RESEARCH published: 30 November 2020 doi: 10.3389/fpls.2020.601316 Docking Characterization and in vitro Inhibitory Activity of Flavan-3-ols and Dimeric Proanthocyanidins Against the Main Protease Activity of SARS-Cov-2 Yue Zhu and De-Yu Xie* Department of Plant and Microbial Biology, North Carolina State University, Raleigh, NC, United States We report to use the main protease (Mpro) of SARS-Cov-2 to screen plant flavan-3-ols and proanthocyanidins. Twelve compounds, (–)-afzelechin (AF), (–)-epiafzelechin (EAF), (+)-catechin (CA), (–)-epicatechin (EC), (+)-gallocatechin (GC), (–)-epigallocatechin Edited by: (EGC), (+)-catechin-3-O-gallate (CAG), (–)-epicatechin-3-O-gallate (ECG), Guodong Wang, Chinese Academy of Sciences, China (–)-gallocatechin-3-O-gallate (GCG), (–)-epigallocatechin-3-O-gallate (EGCG), Reviewed by: procyanidin A2 (PA2), and procyanidin B2 (PB2), were selected for docking simulation. pro Hiroshi Noguchi, The resulting data predicted that all 12 metabolites could bind to M . The affinity Nihon Pharmaceutical scores of PA2 and PB2 were predicted to be −9.2, followed by ECG, GCG, EGCG, University, Japan Ericsson Coy-Barrera, and CAG, −8.3 to −8.7, and then six flavan-3-ol aglycones, −7.0 to −7.7. Docking Universidad Militar Nueva characterization predicted that these compounds bound to three or four subsites (S1, Granada, Colombia S1′, S2, and S4) in the binding pocket of Mpro via different spatial ways and various *Correspondence: De-Yu Xie formation of one to four hydrogen bonds. In vitro analysis with 10 available compounds pro [email protected] showed that CAG, ECG, GCG, EGCG, and PB2 inhibited the M activity with an IC50 value, 2.98 ± 0.21, 5.21 ± 0.5, 6.38 ± 0.5, 7.51 ± 0.21, and 75.3 ± 1.29 µM, Specialty section: respectively, while CA, EC, EGC, GC, and PA2 did not have inhibitory activities. -
USDA Database for the Proanthocyanidin Content of Selected Foods
USDA Database for the Proanthocyanidin Content of Selected Foods Release 2 Prepared by Seema Bhagwat and David Haytowitz Nutrient Data Laboratory Beltsville Human Nutrition Research Center Agricultural Research Service U.S. Department of Agriculture September 2015 Slightly Revised December 2015 U.S. Department of Agriculture Agricultural Research Service Beltsville Human Nutrition Research Center Nutrient Data Laboratory 10300 Baltimore Avenue Building 005, Room 107, BARC-West Beltsville, Maryland 20705 Tel. 301-504-0630, FAX: 301-504-0632 E-Mail: [email protected] Web site: http://www.ars.usda.gov/nutrientdata/flav Table of Contents Release History ............................................................................................................. i Suggested Citation: ....................................................................................................... i Acknowledgements ...................................................................................................... ii Documentation ................................................................................................................ 1 Changes in the update of the proanthocyanidins database ......................................... 1 Data Sources ............................................................................................................... 1 Data Management ....................................................................................................... 2 Data Quality Evaluation............................................................................................... -
Adcetris, INN-Brentuximab Vedotin
19 July 2012 EMA/702390/2012 Committee for Medicinal Products for Human Use (CHMP) Assessment report Adcetris International non-proprietary name: brentuximab vedotin Procedure No. EMEA/H/C/002455 Note Assessment report as adopted by the CHMP with all information of a commercially confidential nature deleted. 7 Westferry Circus ● Canary Wharf ● London E14 4HB ● United Kingdom Telephone +44 (0)20 7418 8400 Facsimile +44 (0)20 7523 7455 E -mail [email protected] Website www.ema.europa.eu An agency of the European Union Product information Name of the medicinal product: Adcetris Applicant: Takeda Global Research and Development Centre (Europe) Ltd. 61 Aldwych London WC2B 4AE United Kingdom Active substance: brentuximab vedotin International Nonproprietary Name/Common Name: brentuximab vedotin Pharmaco-therapeutic group Monoclonal antibodies (ATC Code): (L01XC12) ADCETRIS is indicated for the treatment of adult Therapeutic indication(s): patients with relapsed or refractory CD30+ Hodgkin lymphoma (HL): 1. following autologous stem cell transplant (ASCT) or 2. following at least two prior therapies when ASCT or multi-agent chemotherpay are not a treatment option ADCETRIS is indicated for the treatment of adult patients with relapsed or refractory systemic anaplastic large cell lymphoma (sALCL). Pharmaceutical form(s): Powder for concentrate for solution for infusion Strength(s): 50 mg Route(s) of administration: Intravenous use Packaging: vial (glass) Package size(s): 1 vial Adcetris CHMP assessment report Page 2/102 Rev10.11 Table of contents 1. Background information on the procedure .............................................. 9 1.1. Submission of the dossier ...................................................................................... 9 1.2. Steps taken for the assessment of the product ....................................................... 10 2. Scientific discussion .............................................................................