Methoxy-3-Veratryl-5,6-Dihydrobenzoglyoxalocoline T
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Evodiae Fructus on Targeted Distribution of Berberine in Rats
Int J Clin Exp Med 2018;11(8):7701-7709 www.ijcem.com /ISSN:1940-5901/IJCEM0073795 Original Article Effects of Evodiae Fructus on targeted distribution of berberine in rats Rui-Feng Liang, Wen-Jing Ge, Hui-Sen Wang, She-Feng Zhang, Xue-Xia Zhang, Geng-Sheng Li Institute of Chinese Materia Medica, Henan Provincial Academy of Traditional Chinese Medicine, Zhengzhou 450003, Henan Province, China Received September 20, 2017; Accepted May 24, 2018; Epub August 15, 2018; Published August 30, 2018 Abstract: According to Traditional Chinese Medicine (TCM) theories, Evodiae Fructus (EF) was considered as a meridian guiding drug (MGD) in Zuojin Pill and could enhance the effectiveness of prescription. However, the sci- entific evidence for this effect is still unclear. In this study, the meridian guiding mechanism of EF was investigated. Rats were randomly divided into four groups, control group (water), low dose of EF (250 mg/kg), medium dose of EF (500 mg/kg) and high dose of EF (1000 mg/kg). Water or EF was given to the rats by intragastric administra- tion for 7 days. After the last administration, berberine (80 mg/kg) was administered to rats by gavage. Then the blood and tissues of interest were collected at predetermined time points. Concentrations of berberine in different tissues were analysed by ultra-performance liquid-chromatography tandem mass spectrometry (UPLC-MS/MS) and the target parameters including relative targeting efficiency (RTE), relative uptake efficiency (RUE) and maximum relative concentration (RCmax) were calculated. Compared with control group, various doses of EF could improve the targeting efficiency of berberine in liver. -
Combined Effects of Celecoxib and Cepharanthine on Human Colorectal Cancer Cells in Vitro
Journal of Applied Pharmaceutical Science Vol. 9(04), pp 117-125, April, 2019 Available online at http://www.japsonline.com DOI: 10.7324/JAPS.2019.90415 ISSN 2231-3354 Combined effects of celecoxib and cepharanthine on human colorectal cancer cells in vitro Parawee Lerdwanangkun1, Piyanuch Wonganan1, Robin James Storer2, Wacharee Limpanasithikul1* 1Department of Pharmacology, Faculty of Medicine, Chulalongkorn University, Bangkok, Thailand. 2Office of Research Affairs, Faculty of Medicine, Chulalongkorn University, Bangkok, Thailand. ARTICLE INFO ABSTRACT Received on: 11/09/2018 Colorectal cancer is one of the most common cancers worldwide. We investigated the combined effects of celecoxib Accepted on: 22/01/2019 (CLX)–cepharanthine (CEP) on HT-29 human colorectal cancer cells. CLX at 5, 10, 20, or 40 µM in combination Available online: 18/04/2019 with CEP at 1.25, 2.5, or 5 µM displayed synergistic cytotoxic effects with a combination index <1. Combinations of 20 or 40 µM of CLX with 1.25 or 2.5 µM of CEP increased HT-29 cell accumulation at the G1 phase of the cell cycle. The combined treatments increased the levels of p21 mRNA and decreased the levels of cyclin-A2 mRNA. Their Key words: combined effect triggered significant apoptosis of HT-29 cells when compared with the effect of each drug alone. The Celecoxib, cepharanthine, apoptotic effects of the drugs were correlated with increases in the levels of mRNA for BAX and decreases in the colorectal cancer, apoptosis, levels of mRNA for Bcl-xL. The results from this study revealed that at concentrations that were sub-IC individually, cell cycle. -
Specifications of Approved Drug Compound Library
Annexure-I : Specifications of Approved drug compound library The compounds should be structurally diverse, medicinally active, and cell permeable Compounds should have rich documentation with structure, Target, Activity and IC50 should be known Compounds which are supplied should have been validated by NMR and HPLC to ensure high purity Each compound should be supplied as 10mM solution in DMSO and at least 100µl of each compound should be supplied. Compounds should be supplied in screw capped vial arranged as 96 well plate format. -
(12) Patent Application Publication (10) Pub. No.: US 2010/0221245 A1 Kunin (43) Pub
US 2010O221245A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2010/0221245 A1 Kunin (43) Pub. Date: Sep. 2, 2010 (54) TOPICAL SKIN CARE COMPOSITION Publication Classification (51) Int. Cl. (76) Inventor: Audrey Kunin, Mission Hills, KS A 6LX 39/395 (2006.01) (US) A6II 3L/235 (2006.01) A638/16 (2006.01) Correspondence Address: (52) U.S. Cl. ......................... 424/133.1: 514/533: 514/12 HUSCH BLACKWELL SANDERS LLP (57) ABSTRACT 4801 Main Street, Suite 1000 - KANSAS CITY, MO 64112 (US) The present invention is directed to a topical skin care com position. The composition has the unique ability to treat acne without drying out the user's skin. In particular, the compo (21) Appl. No.: 12/395,251 sition includes a base, an antibacterial agent, at least one anti-inflammatory agent, and at least one antioxidant. The (22) Filed: Feb. 27, 2009 antibacterial agent may be benzoyl peroxide. US 2010/0221 245 A1 Sep. 2, 2010 TOPCAL SKIN CARE COMPOSITION stay of acne treatment since the 1950s. Skin irritation is the most common side effect of benzoyl peroxide and other anti BACKGROUND OF THE INVENTION biotic usage. Some treatments can be severe and can leave the 0001. The present invention generally relates to composi user's skin excessively dry. Excessive use of some acne prod tions and methods for producing topical skin care. Acne Vul ucts may cause redness, dryness of the face, and can actually garis, or acne, is a common skin disease that is prevalent in lead to more acne. Therefore, it would be beneficial to provide teenagers and young adults. -
United States Patent (19) 11 Patent Number: 5,627,195 Hu 45 Date of Patent: May 6, 1997
USOO5627195A United States Patent (19) 11 Patent Number: 5,627,195 Hu 45 Date of Patent: May 6, 1997 54 TREATMENT FOR OCULAR Ferrante, et al., Tetrandrine, a Plant Alkaloid, Inhibits the NFLAMMATON Production of Tumour Necrosis Factor-Alpha (Cachectin) by Human Monocytes, Clin, exp. Immunol. 80:232–235 75 Inventor: Shixing Hu, Cambridge, Mass. (1990). Kondo, et al., Inhibitory Effect of Bisbenzylisoquinoline 73) Assignee: Massachusetts Eye and Ear Alkaloids on the Quick Death of Mice Treated with BCG/ Infirmary, Boston, Mass. LPS, Chem. Pharm. bull. 38(10):287-2889 (1990). Ph.D. dissertation of Shixing Hu, Sun Yat-Sen University of 21 Appl. No.: 420,244 Medical Sciences, Guang Zhou, Guang Dong China, 1989. 22 Filed: Apr. 11, 1995 Seow, et al. In Vitro Immunosuppressive Properties of Teh Plant Alkaloid Tetrandrine. Int. Archs Allergy appl. Immun. [51] Int. Cl. ... A61K 31/445 85:410-415 (1988). 52 514/321: 514/912 Rao. et al., Modulation of Lens-Induced Uvetis by Super 58 Field of Search ...................................... 54/321, 912 oxide Dismutase, Opthlalmic Res. 18:41-46 (1986). Abal et al., Clinical Evaluation of Berberine in Mycotic 56 References Cited Infections, Ind. J. Ophthalm. 34:91-2 (1986). FOREIGN PATENT DOCUMENTS Mohan, et al. Berberine: An Indigenous Drug in Experi mental Herpetic Uveitis. Ind.J. Ophthalm. 31:65-68 (1983). 46-21396 6/1971 Japan. Yao Hsueh Tung Pao 1983; 18:31-36 The Natural Sources 3-44323 2/1991 Japan. and Biological Activities of Bisbenzylisoquinoline (BBI) 4–99723 3/1992 Japan. Alkaloids. OTHER PUBLICATIONS Babbar, et al., Effect of Berberine Chloride Eye Drops on Marshall, et al. -
(12) United States Patent (10) Patent No.: US 8,784.852 B2 Kunin (45) Date of Patent: Jul
US008784852B2 (12) United States Patent (10) Patent No.: US 8,784.852 B2 Kunin (45) Date of Patent: Jul. 22, 2014 (54) TOPICAL SKIN CARE COMPOSITION Katiyar SK, Ahmad N. Mukhtar H. Green Tea and Skin, Abstract from Arch Dermatol, 2000 Aug. pp. 989-994, Volume-Issue 136(8). (76) Inventor: Audrey Kunin, Mission Hills, KS (US) Hiipakka RA, Zhang HZ, Dai W. Dai Q, Liao S., Structure-activity relationships for inhibition of human 5alphareductases by (*) Notice: Subject to any disclaimer, the term of this polyphenols., Abstract from Biochem Pharmacol., Mar. 15, 2002, pp. patent is extended or adjusted under 35 1165-1176, Volume-Issue 63(6). Wenchieh Chen, Diane Thiboutot, Christos C Zouboulis, Cutaneous U.S.C. 154(b) by 437 days. Androgen Metabolism: Basic Research and Clinical Perspectives, Abstract from Journal of Investigative Dermatology, 2002, pp. 992 (21) Appl. No.: 12/395,251 1007, vol. 119. Daniel B. Yarosh, Jason W. Galvin, Stephanie L. Nay, Arely V. Pena, (22) Filed: Feb. 27, 2009 Matthew T. Canning, David A. Brown, Anti-inflammatory activity in skin by biomimetic of Evodia rutaecarpa extract from traditional (65) Prior Publication Data Chinese medicine, Journal of Dermatological Science, 2006, pp. US 2010/0221245 A1 Sep. 2, 2010 13-21, vol. 42. Gustavo Moura-Letts, León F. Villegas, Ana Marcalo, Abraham J Vaisberg, Gerald B. Hammond. In Vivo Wound-Healing Activity of (51) Int. Cl. Oleanolic Acid Derived from the Acid Hydrolysis of Anredera dif A6 IK 8/02 (2006.01) fusa, Abstract from J. Nat. Prod., 2006, pp. 978-979, Volume-Issue A 6LX3/075 (2006.01) 69(6). -
(12) United States Patent (10) Patent No.: US 9,636.405 B2 Tamarkin Et Al
USOO9636405B2 (12) United States Patent (10) Patent No.: US 9,636.405 B2 Tamarkin et al. (45) Date of Patent: May 2, 2017 (54) FOAMABLE VEHICLE AND (56) References Cited PHARMACEUTICAL COMPOSITIONS U.S. PATENT DOCUMENTS THEREOF M (71) Applicant: Foamix Pharmaceuticals Ltd., 1,159,250 A 1 1/1915 Moulton Rehovot (IL) 1,666,684 A 4, 1928 Carstens 1924,972 A 8, 1933 Beckert (72) Inventors: Dov Tamarkin, Maccabim (IL); Doron 2,085,733. A T. 1937 Bird Friedman, Karmei Yosef (IL); Meir 33 A 1683 Sk Eini, Ness Ziona (IL); Alex Besonov, 2,586.287- 4 A 2/1952 AppersonO Rehovot (IL) 2,617,754. A 1 1/1952 Neely 2,767,712 A 10, 1956 Waterman (73) Assignee: EMY PHARMACEUTICALs 2.968,628 A 1/1961 Reed ... Rehovot (IL) 3,004,894. A 10/1961 Johnson et al. (*) Notice: Subject to any disclaimer, the term of this 3,062,715. A 1 1/1962 Reese et al. tent is extended or adiusted under 35 3,067,784. A 12/1962 Gorman pa 3,092.255. A 6/1963 Hohman U.S.C. 154(b) by 37 days. 3,092,555 A 6/1963 Horn 3,141,821 A 7, 1964 Compeau (21) Appl. No.: 13/793,893 3,142,420 A 7/1964 Gawthrop (22) Filed: Mar. 11, 2013 3,144,386 A 8/1964 Brightenback O O 3,149,543 A 9/1964 Naab (65) Prior Publication Data 3,154,075 A 10, 1964 Weckesser US 2013/0189193 A1 Jul 25, 2013 3,178,352. -
Simple Ion Transfer at Liquid| Liquid Interfaces
Hindawi Publishing Corporation International Journal of Electrochemistry Volume 2012, Article ID 462197, 34 pages doi:10.1155/2012/462197 Review Article Simple Ion Transfer at Liquid|Liquid Interfaces L.J.SanchezVallejo,J.M.Ovejero,R.A.Fernandez,´ and S. A. Dassie Instituto de Investigaciones en Fisicoqu´ımica de Cordoba´ (INFIQC), CONICET y Departamento de Fisicoqu´ımica, Facultad de Ciencias Qu´ımicas, Universidad Nacional de Cordoba,´ Ciudad Universitaria, Cordoba´ X5000HUA, Argentina Correspondence should be addressed to S. A. Dassie, [email protected] Received 17 February 2012; Accepted 14 March 2012 Academic Editor: Shen-Ming Chen Copyright © 2012 L. J. Sanchez Vallejo 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. The main aspects related to the charge transfer reactions occurring at the interface between two immiscible electrolyte solutions (ITIES) are described. The particular topics to be discussed involve simple ion transfer. Focus is given on theoretical approaches, numerical simulations, and experimental methodologies. Concerning the theoretical procedures, different computational simu- lations related to simple ion transfer are reviewed. The main conclusions drawn from the most accepted models are described and analyzed in regard to their relevance for explaining different aspects of ion transfer. We describe numerical simulations implemen- ting different approaches for solving the differential equations associated with the mass transport and charge transfer. These nume- rical simulations are correlated with selected experimental results; their usefulness in designing new experiments is summarized. Finally, many practical applications can be envisaged regarding the determination of physicochemical properties, electroanalysis, drug lipophilicity, and phase-transfer catalysis. -
Analytical Reference Standards
Cerilliant Quality ISO GUIDE 34 ISO/IEC 17025 ISO 90 01:2 00 8 GM P/ GL P Analytical Reference Standards 2 011 Analytical Reference Standards 20 811 PALOMA DRIVE, SUITE A, ROUND ROCK, TEXAS 78665, USA 11 PHONE 800/848-7837 | 512/238-9974 | FAX 800/654-1458 | 512/238-9129 | www.cerilliant.com company overview about cerilliant Cerilliant is an ISO Guide 34 and ISO 17025 accredited company dedicated to producing and providing high quality Certified Reference Standards and Certified Spiking SolutionsTM. We serve a diverse group of customers including private and public laboratories, research institutes, instrument manufacturers and pharmaceutical concerns – organizations that require materials of the highest quality, whether they’re conducing clinical or forensic testing, environmental analysis, pharmaceutical research, or developing new testing equipment. But we do more than just conduct science on their behalf. We make science smarter. Our team of experts includes numerous PhDs and advance-degreed specialists in science, manufacturing, and quality control, all of whom have a passion for the work they do, thrive in our collaborative atmosphere which values innovative thinking, and approach each day committed to delivering products and service second to none. At Cerilliant, we believe good chemistry is more than just a process in the lab. It’s also about creating partnerships that anticipate the needs of our clients and provide the catalyst for their success. to place an order or for customer service WEBSITE: www.cerilliant.com E-MAIL: [email protected] PHONE (8 A.M.–5 P.M. CT): 800/848-7837 | 512/238-9974 FAX: 800/654-1458 | 512/238-9129 ADDRESS: 811 PALOMA DRIVE, SUITE A ROUND ROCK, TEXAS 78665, USA © 2010 Cerilliant Corporation. -
(12) United States Patent (10) Patent No.: US 8,158,152 B2 Palepu (45) Date of Patent: Apr
US008158152B2 (12) United States Patent (10) Patent No.: US 8,158,152 B2 Palepu (45) Date of Patent: Apr. 17, 2012 (54) LYOPHILIZATION PROCESS AND 6,884,422 B1 4/2005 Liu et al. PRODUCTS OBTANED THEREBY 6,900, 184 B2 5/2005 Cohen et al. 2002fOO 10357 A1 1/2002 Stogniew etal. 2002/009 1270 A1 7, 2002 Wu et al. (75) Inventor: Nageswara R. Palepu. Mill Creek, WA 2002/0143038 A1 10/2002 Bandyopadhyay et al. (US) 2002fO155097 A1 10, 2002 Te 2003, OO68416 A1 4/2003 Burgess et al. 2003/0077321 A1 4/2003 Kiel et al. (73) Assignee: SciDose LLC, Amherst, MA (US) 2003, OO82236 A1 5/2003 Mathiowitz et al. 2003/0096378 A1 5/2003 Qiu et al. (*) Notice: Subject to any disclaimer, the term of this 2003/OO96797 A1 5/2003 Stogniew et al. patent is extended or adjusted under 35 2003.01.1331.6 A1 6/2003 Kaisheva et al. U.S.C. 154(b) by 1560 days. 2003. O191157 A1 10, 2003 Doen 2003/0202978 A1 10, 2003 Maa et al. 2003/0211042 A1 11/2003 Evans (21) Appl. No.: 11/282,507 2003/0229027 A1 12/2003 Eissens et al. 2004.0005351 A1 1/2004 Kwon (22) Filed: Nov. 18, 2005 2004/0042971 A1 3/2004 Truong-Le et al. 2004/0042972 A1 3/2004 Truong-Le et al. (65) Prior Publication Data 2004.0043042 A1 3/2004 Johnson et al. 2004/OO57927 A1 3/2004 Warne et al. US 2007/O116729 A1 May 24, 2007 2004, OO63792 A1 4/2004 Khera et al. -
Accepted Version
Article Metabolomics identifies a biomarker revealing in vivo loss of functional ß-cell mass before diabetes onset LI, Lingzi, et al. Abstract Identification of pre-diabetic individuals with decreased functional ß-cell mass is essential for the prevention of diabetes. However, in vivo detection of early asymptomatic ß-cell defect remains unsuccessful. Metabolomics emerged as a powerful tool in providing read-outs of early disease states before clinical manifestation. We aimed at identifying novel plasma biomarkers for loss of functional ß-cell mass in the asymptomatic pre-diabetic stage. Non-targeted and targeted metabolomics were applied on both lean ß-Phb2-/- mice (ß-cell-specific prohibitin-2 knockout) and obese db/db mice (leptin receptor mutant), two distinct mouse models requiring neither chemical nor diet treatments to induce spontaneous decline of functional ß-cell mass promoting progressive diabetes development. Non-targeted metabolomics on ß-Phb2-/- mice identified 48 and 82 significantly affected metabolites in liver and plasma, respectively. Machine learning analysis pointed to deoxyhexose sugars consistently reduced at the asymptomatic pre-diabetic stage, including in db/db mice, showing strong correlation with the gradual loss of ß-cells. [...] Reference LI, Lingzi, et al. Metabolomics identifies a biomarker revealing in vivo loss of functional ß-cell mass before diabetes onset. Diabetes, 2019, vol. 68, no. 12, p. 2272-2286 PMID : 31537525 DOI : 10.2337/db19-0131 Available at: http://archive-ouverte.unige.ch/unige:126176 -
Anticancer Effects of Cepharanthine on Human Colon Cancer Cells ฤทธิ์ต้านมะเร็งของเซฟราเรนทีนต่อเซลล์มะเร็งล�ำไส้ใหญ่ของมนุษย์
68 วารสารวิจัย มข. (บศ.) 15 (3) : ก.ค. - ก.ย. 2558 Anticancer Effects of Cepharanthine on Human Colon Cancer Cells ฤทธิ์ต้านมะเร็งของเซฟราเรนทีนต่อเซลล์มะเร็งล�าไส้ใหญ่ของมนุษย์ Arkornnut Rattanawong (อากรณัท รัตนวงษ์)* Dr.Wacharee Limpanasithikul (ดร.วัชรี ลิมปนสิทธิกุล)** Dr.Piyanuch Wonganan (ดร.ปิยนุช วงศ์อนันต์)1*** ABSTRACT Cyclooxygenase (COX-2) has been found to be overexpressed in various tumors including colorectal cancer. Cepharanthine (CEP), a biscoclaurine alkaloid isolated from Stephania cepharantha Hayata, exhibits anticancer activity against several different types of cancer including oropharynx cancer, leukemia, hepatocarcinoma and cholangiocarcinoma. In this study, we investigated the anticancer effects of diclofenac, celecoxib, berberine, CEP and 5-fluorouracil against a COX-2 positive human colon cancer cell line, HT-29. Of all compounds tested, CEP was the most effective agents for controlling the growth of the cancer cells. CEP could significantly induce colon cancer cell apoptosis and effectively inhibit COX-2 mRNA expression. These findings demonstrated that CEP could potentially be used as a novel anticancer agent for COX-2-positive colon cancer cells. บทคัดย่อ มะเร็งหลายชนิดรวมทั้งมะเร็งล�าไส้ใหญ่มีการแสดงออกของ COX-2 ที่มากผิดปกติ จากการศึกษา ก่อนหน้านี้พบว่า cepharanthine (CEP) ซึ่งเป็นสารในกลุ่ม biscoclaurine alkaloid ที่พบได้ในราก ของต้น Stephania cepharantha Hayata มีฤทธิ์ต้านมะเร็งหลายชนิดเช่น มะเร็งช่องปากและล�าคอ มะเร็งเม็ดเลือดขาว มะเร็งตับ และมะเร็งท่อน�้าดี วัตถุประสงค์ของการทดลองนี้เพื่อศึกษาฤทธิ์ต้านมะเร็ง