Table S1. Qualitative Comparison of Constituents in AF and AFI. No. Tr
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Small Molecule–Mediated Reprogramming of the Epithelial–Mesenchymal Transition
bioRxiv preprint doi: https://doi.org/10.1101/106591; this version posted February 16, 2017. The copyright holder for this preprint (which was not certified by peer review) is the author/funder. All rights reserved. No reuse allowed without permission. Small molecule–mediated reprogramming of the epithelial–mesenchymal transition prevents fibrosis Running title: Reversion of fibrosis by chromones Han-Soo Kim,1,2* Jun-Hwan Kim,1,3* Ji Yong Lee,2 Young-Min Yoon,3 Ik-Hwan Kim,4 Ho- Sup Yoon5 and Byung-Soo Youn3# 1Institute for BioMedical Convergence, Catholic Kwandong University-International St. Mary’s Hospital, Incheon 22711, Republic of Korea , 2Department of Biomedical Sciences, Catholic Kwandong University College of Medicine, Gangneung-si, Gangwon-do 25601, Republic of Korea. 3#705 Ace High-end Tower 9th 233,Gasandigital-1-ro, Geumcheon- gu, Seoul, 08501, Republic of Korea, 4Department of Biotechnology, Korea University. Seoul 02841and 5Department of Genetic Engineering, College of Life Sciences, Kyung Hee University, Yongin-si, Gyeonggi-do 446-701, Republic of Korea and 5School of Biological Sciences, Nanyang Technological University, 60 Nanyang Drive, 637551, Singapore *These contributes equally to this work. #Corresponding author: Byung-Soo Youn, PhD, OsteoNeuroGen, Inc. Ace High-end Tower 9th 233, Gasandigital-1-ro, Geumcheon-gu, Seoul, 08501, Republic of Korea Email: [email protected], Tel) 822- 6267 2737 Fax) 822-6267-2740 １ bioRxiv preprint doi: https://doi.org/10.1101/106591; this version posted February 16, 2017. The copyright holder for this preprint (which was not certified by peer review) is the author/funder. All rights reserved. No reuse allowed without permission. -
Supplementary Materials Evodiamine Inhibits Both Stem Cell and Non-Stem
Supplementary materials Evodiamine inhibits both stem cell and non-stem-cell populations in human cancer cells by targeting heat shock protein 70 Seung Yeob Hyun, Huong Thuy Le, Hye-Young Min, Honglan Pei, Yijae Lim, Injae Song, Yen T. K. Nguyen, Suckchang Hong, Byung Woo Han, Ho-Young Lee - 1 - Table S1. Short tandem repeat (STR) DNA profiles for human cancer cell lines used in this study. MDA-MB-231 Marker H1299 H460 A549 HCT116 (MDA231) Amelogenin XX XY XY XX XX D8S1179 10, 13 12 13, 14 10, 14, 15 13 D21S11 32.2 30 29 29, 30 30, 33.2 D7S820 10 9, 12 8, 11 11, 12 8 CSF1PO 12 11, 12 10, 12 7, 10 12, 13 D3S1358 17 15, 18 16 12, 16, 17 16 TH01 6, 9.3 9.3 8, 9.3 8, 9 7, 9.3 D13S317 12 13 11 10, 12 13 D16S539 12, 13 9 11, 12 11, 13 12 D2S1338 23, 24 17, 25 24 16 21 D19S433 14 14 13 11, 12 11, 14 vWA 16, 18 17 14 17, 22 15 TPOX 8 8 8, 11 8, 9 8, 9 D18S51 16 13, 15 14, 17 15, 17 11, 16 D5S818 11 9, 10 11 10, 11 12 FGA 20 21, 23 23 18, 23 22, 23 - 2 - Table S2. Antibodies used in this study. Catalogue Target Vendor Clone Dilution ratio Application1) Number 1:1000 (WB) ADI-SPA- 1:50 (IHC) HSP70 Enzo C92F3A-5 WB, IHC, IF, IP 810-F 1:50 (IF) 1 :1000 (IP) ADI-SPA- HSP90 Enzo 9D2 1:1000 WB 840-F 1:1000 (WB) Oct4 Abcam ab19857 WB, IF 1:100 (IF) Nanog Cell Signaling 4903S D73G4 1:1000 WB Sox2 Abcam ab97959 1:1000 WB ADI-SRA- Hop Enzo DS14F5 1:1000 WB 1500-F HIF-1α BD 610958 54/HIF-1α 1:1000 WB pAkt (S473) Cell Signaling 4060S D9E 1:1000 WB Akt Cell Signaling 9272S 1:1000 WB pMEK Cell Signaling 9121S 1:1000 WB (S217/221) MEK Cell Signaling 9122S 1:1000 -
Graphical Abstract CG 18-1-MS
Send Orders for Reprints to [email protected] 3 Current Genomics, 2017, 18, 3-26 REVIEW ARTICLE ISSN: 1389-2029 eISSN: 1875-5488 Impact Factor: 2.43 Established Human Cell Lines as Models to Study Anti-leukemic Effects of Flavonoids BENTHAM SCIENCE Katrin Sak* and Hele Everaus Department of Hematology and Oncology, University of Tartu, Tartu, Estonia Abstract: Despite the extensive work on pathological mechanisms and some recent advances in the treatment of different hematological malignancies, leukemia continues to present a significant challenge being frequently considered as incurable disease. Therefore, the development of novel therapeutic agents with high efficacy and low toxicity is urgently needed to improve the overall survival rate of pa- A R T I C L E H I S T O R Y tients. In this comprehensive review article, the current knowledge about the anticancer activities of Received: May 11, 2015 flavonoids as plant secondary polyphenolic metabolites in the most commonly used human established Revised: November 20, 2015 Accepted: November 27, 2015 leukemia cell lines (HL-60, NB4, KG1a, U937, THP-1, K562, Jurkat, CCRF- CEM, MOLT-3, and MOLT-4) is compiled, revealing clear anti-proliferative, pro-apoptotic, cell cycle arresting, and differ- DOI: 10.2174/138920291766616080316 entiation inducing effects for certain compounds. Considering the low toxicity of these substances in 5447 normal blood cells, the presented data show a great potential of flavonoids to be developed into novel anti-leukemia agents applicable also in the malignant cells resistant to the current conventional che- motherapeutic drugs. Keywords: Antiproliferation, Apoptosis, Cell cycle arrest, Cytotoxicity, Differentiation, Flavonoids, Leukemia, Human cell lines. -
Shilin Yang Doctor of Philosophy
PHYTOCHEMICAL STUDIES OF ARTEMISIA ANNUA L. THESIS Presented by SHILIN YANG For the Degree of DOCTOR OF PHILOSOPHY of the UNIVERSITY OF LONDON DEPARTMENT OF PHARMACOGNOSY THE SCHOOL OF PHARMACY THE UNIVERSITY OF LONDON BRUNSWICK SQUARE, LONDON WC1N 1AX ProQuest Number: U063742 All rights reserved INFORMATION TO ALL USERS The quality of this reproduction is dependent upon the quality of the copy submitted. In the unlikely event that the author did not send a com plete manuscript and there are missing pages, these will be noted. Also, if material had to be removed, a note will indicate the deletion. uest ProQuest U063742 Published by ProQuest LLC(2017). Copyright of the Dissertation is held by the Author. All rights reserved. This work is protected against unauthorized copying under Title 17, United States C ode Microform Edition © ProQuest LLC. ProQuest LLC. 789 East Eisenhower Parkway P.O. Box 1346 Ann Arbor, Ml 48106- 1346 ACKNOWLEDGEMENT I wish to express my sincere gratitude to Professor J.D. Phillipson and Dr. M.J.O’Neill for their supervision throughout the course of studies. I would especially like to thank Dr. M.F.Roberts for her great help. I like to thank Dr. K.C.S.C.Liu and B.C.Homeyer for their great help. My sincere thanks to Mrs.J.B.Hallsworth for her help. I am very grateful to the staff of the MS Spectroscopy Unit and NMR Unit of the School of Pharmacy, and the staff of the NMR Unit, King’s College, University of London, for running the MS and NMR spectra. -
Study on Structure Activity Relationship of Natural Flavonoids Against Thrombin by Molecular Docking Virtual Screening Combined with Activity Evaluation in Vitro
molecules Article Study on Structure Activity Relationship of Natural Flavonoids against Thrombin by Molecular Docking Virtual Screening Combined with Activity Evaluation In Vitro 1,2, 3,4, 3,4 1 1,2 Xiaoyan Wang y, Zhen Yang y, Feifei Su , Jin Li , Evans Owusu Boadi , Yan-xu Chang 1,2,* and Hui Wang 3,4,* 1 Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China 2 Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China 3 Tianjin Key Laboratory of Chinese Medicine Pharmacology, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China 4 College of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China * Correspondence: [email protected] (Y.-x.C.); [email protected] (H.W.); Tel./Fax: +86-22-59596163 (Y.-x.C.) These authors contributed equally to this work. y Received: 20 December 2019; Accepted: 18 January 2020; Published: 20 January 2020 Abstract: Thrombin, a key enzyme of the serine protease superfamily, plays an integral role in the blood coagulation cascade and thrombotic diseases. In view of this, it is worthwhile to establish a method to screen thrombin inhibitors (such as natural flavonoid-type inhibitors) as well as investigate their structure activity relationships. Virtual screening using molecular docking technique was used to screen 103 flavonoids. Out of this number, 42 target compounds were selected, and their inhibitory effects on thrombin assayed by chromogenic substrate method. The results indicated that the carbon-carbon double bond group at the C2, C3 sites and the carbonyl group at the C4 sites of flavones were essential for thrombin inhibition, whereas the methoxy and O-glycosyl groups reduced thrombin inhibition. -
Study on Structure Activity Relationship of Natural Flavonoids
1 of 15 1 Study on Structure Activity Relationship of Natural 2 Flavonoids against Thrombin by Molecular Docking 3 Virtual Screening combined with Activity Evaluation 4 in vitro 5 Xiaoyan Wang1, 2 # , Zhen Yang3, 4 #, Feifei Su3, 4, Jin Li1, Evans Owusu Boadi 1, 2 , Yan-xu Chang1, 2*, 6 Hui Wang3, 4* 7 1 Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese 8 Medicine, Tianjin, 300193, China; 9 2 Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional 10 Chinese Medicine, Tianjin, 300193, China; 11 3 Tianjin Key Laboratory of Chinese medicine Pharmacology, Tianjin University of Traditional Chinese 12 Medicine, Tianjin, 300193, China 13 4 College of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, 14 China 15 16 * Corresponding author: [email protected] (H.W.); [email protected] (Y.C) 17 Tel. /FAX: +86-22-59596163(S.F. &Y.C.) 18 # These authors contributed equally to this work. 19 20 21 22 Table S1 the docking score of 103 Compounds (In descending order of “-CDOCKER_energy”) 23 Figure S1 the Molecular structures of 42 flavonoids 24 25 26 27 28 Table S1 the docking score of 103 Compounds (In descending order of “-CDOCKER_energy”) 29 - -CDOCKER_ CDOCKER_IN energy TERACTION_ No. CAS compound (kcal/mol) energy (kcal/mol) 1 1257-08-5 (-)-Epicatechin gallate 52.0751 54.6293 2 83104-87-4 (-)-EGCG-3''-O-Me 51.2391 50.5546 3 20315-25-7 Proanthocyanidin B1 42.3509 55.9285 4 27200-12-0 Dihydromyricetin 40.3383 -
Flavonoids: Structure–Function and Mechanisms of Action and Opportunities for Drug Development
Toxicological Research Toxicol Res. eISSN 2234-2753 https://doi.org/10.1007/s43188-020-00080-z pISSN 1976-8257 INVITED REVIEW Flavonoids: structure–function and mechanisms of action and opportunities for drug development Stephen Safe1 · Arul Jayaraman2 · Robert S. Chapkin3 · Marcell Howard1 · Kumaravel Mohankumar1 · Rupesh Shrestha4 Received: 10 November 2020 / Accepted: 4 December 2020 © Korean Society of Toxicology 2021 Abstract Flavonoids are polyphenolic phytochemicals produced in fruits, nuts and vegetables and dietary consumption of these structurally diverse compounds is associated with multiple health benefts including increased lifespan, decreased cardio- vascular problems and low rates of metabolic diseases. Preclinical studies with individual favonoids demonstrate that these compounds exhibit anti-infammatory and anticancer activities and they enhance the immune system. Their efectiveness in both chemoprevention and chemotherapy is associated with their targeting of multiple genes/pathways including nuclear receptors, the aryl hydrocarbon receptor (AhR), kinases, receptor tyrosine kinases and G protein-coupled receptors. However, despite the remarkable preclinical activities of favonoids, their clinical applications have been limited and this is due, in part, to problems in drug delivery and poor bioavailability and these problems are being addressed. Further improvements that will expand clinical applications of favonoids include mechanism-based precision medicine approaches which will identify critical mechanisms of action -
Therapeutic Single Compounds for Osteoarthritis Treatment
pharmaceuticals Review Therapeutic Single Compounds for Osteoarthritis Treatment Hyemi Lee 1,2,3,† , Xiangyu Zhao 4,†, Young-Ok Son 4,5,6,* and Siyoung Yang 1,2,3,* 1 Department of Biomedical Sciences, Ajou University Graduate School of Medicine, Suwon 16499, Korea; [email protected] 2 Department of Pharmacology, Ajou University School of Medicine, Suwon 16499, Korea 3 Degenerative InterDiseases Research Center, Ajou University School of Medicine, Suwon 16499, Korea 4 Department of Animal Biotechnology, Faculty of Biotechnology and Interdisciplinary Graduate Program in Advanced Convergence Technology and Science, Jeju National University, Jeju 63243, Korea; [email protected] 5 Bio-Health Materials Core-Facility Center, Jeju National University, Jeju 63243, Korea 6 Practical Translational Research Center, Jeju National University, Jeju 63243, Korea * Correspondence: [email protected] (Y.-O.S.); [email protected] (S.Y.); Tel.: +82-64-754-3331 (Y.-O.S.); +82-31-219-5065 (S.Y.) † These authors are contributed equally. Abstract: Osteoarthritis (OA) is an age-related degenerative disease for which an effective disease- modifying therapy is not available. Natural compounds derived from plants have been traditionally used in the clinic to treat OA. Over the years, many studies have explored the treatment of OA using natural extracts. Although various active natural extracts with broad application prospects have been discovered, single compounds are more important for clinical trials than total natural extracts. Moreover, although natural extracts exhibit minimal safety issues, the cytotoxicity and function of all single compounds in a total extract remain unclear. Therefore, understanding single compounds with the ability to inhibit catabolic factor expression is essential for developing therapeutic agents for OA. -
Dr. Duke's Phytochemical and Ethnobotanical Databases List of Chemicals for Cataracts
Dr. Duke's Phytochemical and Ethnobotanical Databases List of Chemicals for Cataracts Chemical Activity Count (+)-ALPHA-VINIFERIN 2 (+)-CATECHIN 5 (+)-CORYDALINE 1 (+)-EUDESMA-4(14),7(11)-DIENE-3-ONE 1 (+)-GALLOCATECHIN 1 (+)-GLAUCINE 1 (+)-HERNANDEZINE 1 (+)-ISOCORYDINE 1 (+)-PSEUDOEPHEDRINE 1 (+)-SYRINGARESINOL 1 (+)-SYRINGARESINOL-DI-O-BETA-D-GLUCOSIDE 1 (-)-16,17-DIHYDROXY-16BETA-KAURAN-19-OIC 1 (-)-ALPHA-BISABOLOL 1 (-)-BETONICINE 1 (-)-BISPARTHENOLIDINE 1 (-)-BORNYL-CAFFEATE 2 (-)-BORNYL-FERULATE 2 (-)-BORNYL-P-COUMARATE 2 (-)-DANSHEXINKUN 1 (-)-EPIAFZELECHIN 1 (-)-EPICATECHIN 3 (-)-EPICATECHIN-3-O-GALLATE 1 (-)-EPIGALLOCATECHIN 2 (-)-EPIGALLOCATECHIN-3-O-GALLATE 1 (-)-EPIGALLOCATECHIN-GALLATE 4 (-)-HYDROXYJASMONIC-ACID 1 (-)-STYLOPINE 1 Chemical Activity Count (-)-TETRAHYDROCOLUMBAMINE 1 (1'S)-1'-ACETOXYCHAVICOL-ACETATE 2 (15:1)-CARDANOL 1 (2R)-(12Z,15Z)-2-HYDROXY-4-OXOHENEICOSA-12,15-DIEN-1-YL-ACETATE 1 (3'R,4'R)-3'-EPOXYANGELOYLOXY-4'-ACETOXY-3',4'-DIHYDROSESELIN 1 (7R,10R)-CAROTA-1,4-DIENALDEHYDE 1 (E)-4-(3',4'-DIMETHOXYPHENYL)-BUT-3-EN-OL 2 1,2,3,6-TETRA-O-GALLYOL-BETA-D-GLUCOSE 1 1,2,6-TRI-O-GALLOYL-BETA-D-GLUCOSE 1 1,3,6-TRIHYDROXY-2,7-DIMETHOXY-XANTHONE 1 1,6,7-TRIHYDROXY-2,3-DIMETHOXY-XANTHONE 1 1,7-BIS(3,4-DIHYDROXYPHENYL)HEPTA-4E,6E-DIEN-3-ONE 1 1,7-BIS-(4-HYDROXYPHENYL)-1,4,6-HEPTATRIEN-3-ONE 1 1,8-CINEOLE 3 1-HYDROXY-3,6,7-TRIMETHOXY-XANTHONE 1 1-METHOXY-2,3-METHYLENEDIOXY-XANTHONE 1 1-O-(2,3,4-TRIHYDROXY-3-METHYL)-BUTYL-6-O-FERULOYL-BETA-D-GLUCOPYRANOSIDE 1 10-ACETOXY-8-HYDROXY-9-ISOBUTYLOXY-6-METHOXYTHYMOL 2 10-DEHYDROGINGERDIONE -
( 12 ) United States Patent
US010722444B2 (12 ) United States Patent ( 10 ) Patent No.: US 10,722,444 B2 Gousse et al. (45 ) Date of Patent : Jul. 28 , 2020 (54 ) STABLE HYDROGEL COMPOSITIONS 4,605,691 A 8/1986 Balazs et al . 4,636,524 A 1/1987 Balazs et al . INCLUDING ADDITIVES 4,642,117 A 2/1987 Nguyen et al. 4,657,553 A 4/1987 Taylor (71 ) Applicant: Allergan Industrie , SAS , Pringy (FR ) 4,713,448 A 12/1987 Balazs et al . 4,716,154 A 12/1987 Malson et al. ( 72 ) 4,772,419 A 9/1988 Malson et al. Inventors: Cécile Gousse , Dingy St. Clair ( FR ) ; 4,803,075 A 2/1989 Wallace et al . Sébastien Pierre, Annecy ( FR ) ; Pierre 4,886,787 A 12/1989 De Belder et al . F. Lebreton , Annecy ( FR ) 4,896,787 A 1/1990 Delamour et al. 5,009,013 A 4/1991 Wiklund ( 73 ) Assignee : Allergan Industrie , SAS , Pringy (FR ) 5,087,446 A 2/1992 Suzuki et al. 5,091,171 A 2/1992 Yu et al. 5,143,724 A 9/1992 Leshchiner ( * ) Notice : Subject to any disclaimer , the term of this 5,246,698 A 9/1993 Leshchiner et al . patent is extended or adjusted under 35 5,314,874 A 5/1994 Miyata et al . U.S.C. 154 (b ) by 0 days. 5,328,955 A 7/1994 Rhee et al . 5,356,883 A 10/1994 Kuo et al . (21 ) Appl . No.: 15 /514,329 5,399,351 A 3/1995 Leshchiner et al . 5,428,024 A 6/1995 Chu et al . -
Natural Antioxidant and Anti-Inflammatory Compounds In
antioxidants Review Natural Antioxidant and Anti-Inflammatory Compounds in Foodstuff or Medicinal Herbs Inducing Heme Oxygenase-1 Expression 1,2, 3, 4, Dongyup Hahn y, Seung Ho Shin y and Jong-Sup Bae * 1 School of Food Science and Biotechnology, College of Agriculture and Life Sciences, Kyungpook National University, Daegu 41566, Korea; [email protected] 2 Department of Integrative Biology, Kyungpook National University, Daegu 41566, Korea 3 Department of Food and Nutrition, Institute of Agriculture and Life Science, Gyeongsang National University, Jinju 52828, Korea; [email protected] 4 College of Pharmacy, CMRI, Research Institute of Pharmaceutical Sciences, BK21 Plus KNU Multi-Omics based Creative Drug Research Team, Kyungpook National University, Daegu 41566, Korea * Correspondence: [email protected] These authors contributed equally to this work. y Received: 29 October 2020; Accepted: 24 November 2020; Published: 27 November 2020 Abstract: Heme oxygenase-1 (HO-1) is an inducible antioxidant enzyme that catalyzes heme group degradation. Decreased level of HO-1 is correlated with disease progression, and HO-1 induction suppresses development of metabolic and neurological disorders. Natural compounds with antioxidant activities have emerged as a rich source of HO-1 inducers with marginal toxicity. Here we discuss the therapeutic role of HO-1 in obesity, hypertension, atherosclerosis, Parkinson’s disease and hepatic fibrosis, and present important signaling pathway components that lead to HO-1 expression. We provide an updated, comprehensive list of natural HO-1 inducers in foodstuff and medicinal herbs categorized by their chemical structures. Based on the continued research in HO-1 signaling pathways and rapid development of their natural inducers, HO-1 may serve as a preventive and therapeutic target for metabolic and neurological disorders. -
(12) Patent Application Publication (10) Pub. No.: US 2012/0208890 A1 Gousse Et Al
US 20120208890A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2012/0208890 A1 Gousse et al. (43) Pub. Date: Aug. 16, 2012 (54) STABLE HYDROGEL COMPOSITIONS of application No. 127956,542, filed on Nov.30, 2010, INCLUDING ADDITIVES which is a continuation-in-part of application No. 12/714,377, filed on Feb.26, 2010, which is a continu (75) Inventors: Cecile Gousse, Dingy Saint Clair ation-in-part of application No. 12/687,048, filed on (FR); Pierre F. Lebreton, Annecy Jan. 13, 2010. (FR); Nicolas Prost, Mornant (FR): Sumit Paliwal, Goleta, CA (US); Publication Classification Dennis Van Epps, Goleta, CA (US) (51) Int. C. (73) Assignee: ALLERGAN, INC. Irvine, CA A6IR 8/4I (2006.01) (US) A61O 19/08 (2006.01) A6IR 8/42 (2006.01) (21) Appl. No.: 13/350,518 (52) U.S. Cl. ......................................... 514/626; 514/653 (22) Filed: Jan. 13, 2012 (57) ABSTRACT Related U.S. Application Data The present specification generally relates to hydrogel com (63) Continuation-in-part of application No. 13/005,860, positions and methods of treating a soft tissue condition using filed on Jan. 13, 2011, which is a continuation-in-part Such hydrogel compositions. Patent Application Publication Aug. 16, 2012 Sheet 1 of 7 US 2012/0208890 A1 lication Publication ug. 16, 2012 Sheet 2 of 7 co & S. N SESo 9 CD s Y NI C O O CN ve ve D an an 5 S. 5 3. 9. S. Patent Application Publication Aug. 16, 2012 Sheet 3 of 7 US 2012/0208890 A1 00Z?000).00800900700Z0 O.GZ?eSÅep~ Patent Application Publication Aug.