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https://www.readbyqxmd.com/read/28231528/identification-of-uv-absorbing-extractables-from-rubber-closures-used-in-containers-of-injectable-powder-and-safety-assessment-of-leachables-in-the-drug
#1
Yulei Wei, Ying Wu, Tingli Zhu, Zhiyan Li, Yilan Zhang
Rubber closures have been of great concern to regulatory authorities on account of their potential safety risks to patients. The aim of our work is to provide part of data about the compatibility of the injectable powder and its packaging materials for the drug registration. In this report, methodologies were established to study the system of the preparation. Firstly, three major extractables were isolated by semi-preparative HPLC method combined with silica gel-based chromatographic methods. NMR spectra including 1D NMR ((1)H, (13)C, DEPT135) and 2D NMR (COSY, HSQC, HMBC) were introduced to identify the extractables, besides HPLC, GC-MS, ESI-MS/MS and HRMS...
February 16, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28231523/synergistic-effects-between-a-copper-based-metal-casiope%C3%A3-na-iii-ia-and-cisplatin
#2
Silvia Graciela Davila-Manzanilla, Yeshenia Figueroa-de-Paz, Carmen Mejia, Lena Ruiz-Azuara
Additive, subadditive or superadditive interactions observed in combination therapy play an important role in several treatments, particularly for cancer. The isobolographic analysis allows to establish the pharmacological interactions that exist between two drugs that are administered together in equieffective doses. In order to identify if the combination of two compounds presents synergistic interaction, the antiproliferative activity of CasIII-ia with analogue compounds or cisplatin in different molar ratios was evaluated...
February 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28231520/medicinal-plants-used-as-anthelmintics-ethnomedical-pharmacological-and-phytochemical-studies
#3
REVIEW
Juan Carlos Romero-Benavides, Ana Lucía Ruano, Ronal Silva-Rivas, Paola Castillo-Veintimilla, Sara Vivanco-Jaramillo, Natalia Bailon-Moscoso
Intestinal parasites delay mental and physical development in children. Infection with these parasites can result in complications during pregnancy and alter the health of newborns, which has long-term effects on educational attainment and economic productivity. The appearance of resistance against classical drug treatments generates interest in the development of new deworming alternatives. We think that research of new plants species may reveal potential antiparasitic compounds. This review is focused on the use of plants and secondary metabolites against intestinal parasites...
February 16, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28231051/short-communication-challenges-relating-to-comparison-of-flavonoid-glycosides-dissolution-profiles-from-sutherlandia-frutescens-products
#4
Oluchi N Mbamalu, James Syce, Halima Samsodien
Unlike the case of conventional drug formulations, dissolution tests have hitherto not been required for herbal medicinal products commercially available in South Africa. This study investigated dissolution of the South African Sutherlandia frutescens using selected flavonoid glycosides as marker compounds. Dissolution of markers was assessed in three dissolution media at pH 1.2, 4.5 and 6.8, and samples were analysed using a validated HPLC method. The dissolution profile of each marker varied for the different materials investigated...
March 1, 2017: Acta Pharmaceutica
https://www.readbyqxmd.com/read/28230986/design-synthesis-and-evaluation-of-a-novel-series-of-oxadiazine-gamma-secretase-modulators-for-familial-alzheimer-s-disease
#5
Matthew G Bursavich, Bryce A Harrison, Raksha Acharya, Donald E Costa, Emily A Freeman, Hilliary E Hodgdon, Lori A Hrdlicka, Hong Jin, Sudarshan Kapadnis, Jeffrey S Moffit, Deirdre A Murphy, Scott Nolan, Holger Patzke, Cuyue Tang, Melody Wen, Gerhard Koenig, Jean-François Blain, Duane A Burnett
Herein we describe the design, synthesis and evaluation of a novel series of oxadiazine-based gamma secretase modulators obtained via isosteric amide replacement and critical consideration of conforma-tional restriction. Oxadiazine lead 47 possesses good in vitro potency with excellent predicted CNS drug-like properties and desirable ADME/PK profile. This lead compound demonstrated robust Aβ42 reductions and subsequent Aβ37 increases in both rodent brain and CSF at 30 mg/kg dosed orally.
February 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28230985/discovery-of-competitive-and-non-competitive-ligands-of-the-organic-cation-transporter-1-oct1-slc22a1
#6
Eugene C Chen, Natalia Khuri, Xiaomin Liang, Adrian Stecula, Huan-Chieh Chien, Sook Wah Yee, Yong Huang, Andrej Sali, Kathleen M Giacomini
Organic cation transporter 1 (OCT1) plays a critical role in the hepatocellular uptake of structurally diverse endogenous compounds and xenobiotics. Here, we identified competitive and noncompetitive OCT1 interacting ligands in a library of 1,780 prescription drugs by combining in silico and in vitro methods. Ligands were predicted by docking against a comparative model based a eukaryotic homolog. In parallel, high-throughput screening (HTS) was conducted using the fluorescent probe substrate ASP+ in cells overexpressing human OCT1...
February 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28230866/oridonin-induces-autophagy-via-inhibition-of-glucose-metabolism-in-p53-mutated-colorectal-cancer-cells
#7
Zhuo Yao, Fuhua Xie, Min Li, Zirui Liang, Wenli Xu, Jianhua Yang, Chang Liu, Hongwangwang Li, Hui Zhou, Liang-Hu Qu
The Warburg effect is an important characteristic of tumor cells, making it an attractive therapeutic target. Current anticancer drug development strategies predominantly focus on inhibitors of the specific molecular effectors involved in tumor cell proliferation. These drugs or natural compounds, many of which target the Warburg effect and the underlying mechanisms, still need to be characterized. To elucidate the anticancer effects of a natural diterpenoid, oridonin, we first demonstrated the anticancer activity of oridonin both in vitro and in vivo in colorectal cancer (CRC) cells...
February 23, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28230778/caffeic-acid-expands-anti-tumor-effect-of-metformin-in-human-metastatic-cervical-carcinoma-htb-34-cells-implications-of-ampk-activation-and-impairment-of-fatty-acids-de-novo-biosynthesis
#8
Malgorzata Tyszka-Czochara, Pawel Konieczny, Marcin Majka
The efficacy of cancer treatments is often limited and associated with substantial toxicity. Appropriate combination of drug targeting specific mechanisms may regulate metabolism of tumor cells to reduce cancer cell growth and to improve survival. Therefore, we investigated the effects of anti-diabetic drug Metformin (Met) and a natural compound caffeic acid (trans-3,4-dihydroxycinnamic acid, CA) alone and in combination to treat an aggressive metastatic human cervical HTB-34 (ATCC CRL-1550) cancer cell line...
February 21, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28230762/the-development-of-ck2-inhibitors-from-traditional-pharmacology-to-in-silico-rational-drug-design
#9
REVIEW
Giorgio Cozza
Casein kinase II (CK2) is an ubiquitous and pleiotropic serine/threonine protein kinase able to phosphorylate hundreds of substrates. Being implicated in several human diseases, from neurodegeneration to cancer, the biological roles of CK2 have been intensively studied. Upregulation of CK2 has been shown to be critical to tumor progression, making this kinase an attractive target for cancer therapy. Several CK2 inhibitors have been developed so far, the first being discovered by "trial and error testing". In the last decade, the development of in silico rational drug design has prompted the discovery, de novo design and optimization of several CK2 inhibitors, active in the low nanomolar range...
February 20, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28229078/systemic-therapy-of-cholangiocarcinoma
#10
REVIEW
Ruben R Plentz, Nisar P Malek
BACKGROUND: Cholangiocarcinoma (CC) is the second most common primary malignant liver disease. During the last decades, various novel therapies have been introduced in the field of oncology; nevertheless, the number of treatment options for CC is still limited. METHODS: In this article, current palliative chemotherapy concepts as well as new drug therapies are outlined. RESULTS: Gemcitabine and cisplatin are the standard treatment of care for patients with inoperable CC...
December 2016: Visceral Medicine
https://www.readbyqxmd.com/read/28228365/isoquinoline-alkaloids-from-coptis-japonica-stimulate-the-myoblast-differentiation-via-p38-map-kinase-and-akt-signaling-pathway
#11
Heyjin Lee, Le Thi Tuong, Ji Hye Jeong, Sang-Jin Lee, Gyu-Un Bae, Jae-Ha Ryu
To overcome the muscle atrophy, such as cachexia and sarcopenia, we tried to find myogenic agents from medicinal plants. From myogenic extract of Coptis japonica, we purified six isoquinoline alkaloids and evaluated their effects on transactivation of myoD and MHC expression in C2C12 cells during differentiation process. Among obtained compounds, magnoflorine most efficiently enhanced the myoblast differentiation by activating the p38 MAP kinase and Akt pathway, and also increased the number of multinucleated and cylinder-shaped myotubes...
February 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28228362/development-of-mbri-001-a-deuterium-substituted-plinabulin-derivative-as-a-potent-anti-cancer-agent
#12
Zhongpeng Ding, Hejuan Cheng, Shixiao Wang, Yingwei Hou, Jianchun Zhao, Huashi Guan, Wenbao Li
Plinabulin, a drug targeting microtubule of cancer cells, has been currently tried in its phase III clinical study. However, low efficacy caused by poor pharmacokinetic (PK) properties has been considered to be the main obstacle to approved by the Food and Drug Administration. Herein, we introduced a deuterium atom as an isostere in its structure to become a new compound named (MBRI-001, No. 9 in a series of deuterium-substituted compounds). The structure of MBRI-001 was characterized by HRMS, NMR, IR and a single crystal analysis...
February 3, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28228233/analyzing-complex-mixtures-of-drug-like-molecules-ion-mobility-as-an-adjunct-to-existing-liquid-chromatography-tandem-mass-spectrometry-methods
#13
Jasper Boschmans, Filip Lemière, Frank Sobott
The use of traveling wave ion mobility mass spectrometry (TWIMS) is evaluated in conjunction with, and as a possible alternative to, conventional LC-MS(/MS) methods for the separation and characterization of drug-like compounds and metabolites. As a model system we use an in vitro incubation mixture of the chemotherapeutic agent melphalan, which results in more than ten closely related hydrolysis products and chain-like oligomers. Ion mobility as a filtering tool results in the separation of ions of interest from interfering ions, based on charge state and shape/size...
February 14, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28228228/molecular-hybridization-conceded-exceptionally-potent-quinolinyl-oxadiazole-hybrids-through-phenyl-linked-thiosemicarbazide-antileishmanial-scaffolds-in-silico-validation-and-sar-studies
#14
Muhammad Taha, Nor Hadiani Ismail, Muhammad Ali, Umer Rashid, Syarul Imran, Nizam Uddin, Khalid Mohammed Khan
The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover a novel series of compounds 6-23 based on the concept of molecular hybridization. Most of the synthesized analogues exhibited potent leishmanicidal potential. The most potent compound (23, IC50=0.10±0.001μM) among the series was found ∼70 times more lethal than the standard drug. The current series 6-23 conceded in the development of fourteen (14) extraordinarily active compounds against leishmaniasis...
February 19, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28228097/alkaloid-extracts-from-combretum-zeyheri-inhibit-the-growth-of-mycobacterium-smegmatis
#15
Tafadzwa Nyambuya, Ruvimbo Mautsa, Stanley Mukanganyama
BACKGROUND: Current tuberculosis regimens have failed to combat the issue of drug resistance and ethno medicines may represent a possible source of antimycobacterial agents. Combretum species are well known in African traditional medicines and used for various ailments including pneumonia, venereal diseases like syphilis, mental problems, relief of sore throats and colds, fever, and chest coughs associated with tuberculosis. Alkaloids function as either hydrogen-acceptor or hydrogen-donor in hydrogen bonding critical for the interaction between targets thus, potentiating effects of curative agents on diseases...
February 23, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28228088/aryl-heteroaryl-substituted-celecoxib-derivatives-as-cox-2-inhibitors-synthesis-anti-inflammatory-activity-and-molecular-docking-studies
#16
Golla Madhava, Katla Venkata Ramana, Saddala Madhu Sudhana, Devineni Subba Rao, Kuntrapakam Hema Kumar, Valluru Lokanatha, Asupatri Usha Rani, Chamarthi Naga Raju
BACKGROUND: Cyclooxygenase (COX-2) inhibitors have been developed to provide better anti-inflammatory and analgesic efficacy than those of traditional NSAIDs. Several compounds having selective COX-2 inhibitors such as SC-558, Celecoxib, Rofecoxib, Valdecoxib and Etoricoxib are marketed as new generation NSAIDs and block the production of prostaglandins (PGs) in inflammatory cells. New anti-inflammatory dynamic agents with improved potency and safety profile are still needed. OBJECTIVE: As a part of our continuation research work towards the synthesis of anti-inflammatory agents, the synthesis of N-substituted aryl/heteroaryl-pyrazole-1yl benzene sulfonamide (Celecoxib) derivatives, and evaluated their anti-inflammatory activity in both methods in vitro and in vivo, and molecular docking study on COX-2 enzyme will be discussed in this study...
February 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28228080/marine-drugs-a-hidden-wealth-and-a-new-epoch-for-cancer-management
#17
Eram Shakeel, Deepika Arora, Qazi Mohammad Sajid Jamal, Salman Akhtar, Mohd Kalim Ahmad Khan, Mohammad A Kamal, Mohd Haris Siddiqui, Mohtashim Lohani, Jamal M Arif
Malignant tumors are the leading cause of death in humans. Due to tedious efforts and investigation made in the field of marine drug discovery, there is now a scientific bridge between marine and pharmaceutical sciences. However, at present only few marine drugs have been paved towards anticancer management, yet many more to be established. Marine organisms are profuse manufacturer of structurally inimitable bioactive metabolites that have unusual mechanisms of action and diverse biosynthetic pathways. Some of the compounds derived from marine organisms have antioxidant property and anticancer activities, but they are largely unexplored...
February 20, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28228070/nanoscale-delivery-systems-actual-and-potential-applications-in-the-natural-products-industry
#18
Antal Diana Simona, Ardelean Florina, Chis Aimée Rodica, Ollivier Evelyne, Serban Maria-Corina
BACKGROUND: Compounds and extracts derived from natural sources continue to stand in the spotlight of drug design owing to their versatile interaction with enzymes, receptors and metabolic pathways. Nanomedicine offers an operative tool for the efficient delivery of natural products, in terms of increased bioavailability, targeting, and controlled release while protecting active constituents against physico-chemical alterations. The interest of the scientific community in the field of nanosized delivery of natural compounds is demonstrated by the exponential growth of the publications in this field...
February 20, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28227433/microprinted-tumor-spheroids-enable-anti-cancer-drug-screening
#19
Pradip S Thakuri, Stephanie L Ham, Hossein Tavana, Pradip S Thakuri, Stephanie L Ham, Hossein Tavana, Stephanie L Ham, Hossein Tavana
Spheroids present a biologically relevant model of avascular tumors and a unique tool for discovery of anti-cancer drugs. Despite being used in research laboratories for several decades, spheroids are not routinely used for drug discovery primarily due to the difficulty of mass-producing uniformly-sized spheroids and intense labor involved in handling, drug treatment, and analyzing them. We overcome this barrier using a novel technology to robotically microprint spheroids in standard 384-well plates. An aqueous drop containing cancer cells is dispensed into a bath of a second, immiscible aqueous phase...
August 2016: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/28226337/immunoassay-based-drug-tests-are-inadequately-sensitive-for-medication-compliance-monitoring-in-patients-treated-for-chronic-pain
#20
Marion L Snyder, Corrine R Fantz, Stacy Melanson
BACKGROUND: Enzyme immunoassays (EIA) have notable limitations for monitoring therapeutic compliance in pain management. Chromatography coupled with mass spectrometry provides definitive results and superior sensitivity and specificity over traditional EIA testing. OBJECTIVE: To analyze and compare the sensitivity of EIA results together with known prescriptions to liquid chromatography-tandem mass spectrometry (LC-MS/MS) for monitoring drug use (and abuse) in patients treated for chronic pain...
February 2017: Pain Physician
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