keyword
https://read.qxmd.com/read/38226592/the-hybrid-antibiotic-thiomarinol-a-overcomes-intrinsic-resistance-in-escherichia-coli-using-a-privileged-dithiolopyrrolone-moiety
#1
JOURNAL ARTICLE
Rachel M Johnson, Kelin Li, Xiaoyan Chen, Gina L Morgan, Jeffrey Aubé, Bo Li
An impermeable outer membrane and multidrug efflux pumps work in concert to provide Gram-negative bacteria with intrinsic resistance against many antibiotics. These resistance mechanisms reduce the intracellular concentrations of antibiotics and render them ineffective. The natural product thiomarinol A combines holothin, a dithiolopyrrolone antibiotic, with marinolic acid A, a close analogue of mupirocin. The hybridity of thiomarinol A converts the mupirocin scaffold from inhibiting Gram-positive bacteria to inhibiting both Gram-positive and -negative bacteria...
January 16, 2024: ACS Infectious Diseases
https://read.qxmd.com/read/37538850/medical-cannabis-received-by-patients-according-to-qualifying-condition-in-a-us-state-cannabis-program-product-choice-dosing-and-age-related-trends
#2
JOURNAL ARTICLE
Xintian Lyu, Sílvia M Illamola, Susan E Marino, Ilo E Leppik, Stephen Dahmer, Paloma Lehfeldt, Jeannine M Conway, Rory P Remmel, Kyle Kingsley, Angela K Birnbaum
BACKGROUND: Little is known about the distribution of cannabidiol (CBD) and Δ9-tetrahydrocannabinol (THC) to patients participating in state medical cannabis programs. The Minnesota cannabis program requires third-party testing of products with limited formulations of cannabis for distribution to patients. OBJECTIVE: To characterize the distribution of cannabis products, their CBD/THC content, and dosing among patients with qualifying conditions. METHODS: This is a retrospective analysis of ∼50% of registered users receiving medical cannabis in Minnesota (June 16, 2016, to November 15, 2019)...
2023: Current Therapeutic Research, Clinical and Experimental
https://read.qxmd.com/read/36540233/rational-drug-design-of-cb2-receptor-ligands-from-2012-to-2021
#3
REVIEW
Yan-Ran Wu, Jia-Qin Tang, Wan-Nian Zhang, Chun-Lin Zhuang, Ying Shi
Cannabinoid receptors belong to the large family of G-protein-coupled receptors, which can be divided into two receptor types, cannabinoid receptor type-1 (CB1) and cannabinoid receptor type-2 (CB2). Marinol, Cesamet and Sativex are marketed CB1 drugs which are still in use and work well, but the central nervous system side effects caused by activation CB1, which limited the development of CB1 ligands. So far, no selective CB2 ligand has been approved for marketing, but lots of its ligands in the clinical stage and pre-clinical stage have positive effects on the treatment of some disease models and have great potential for development...
December 6, 2022: RSC Advances
https://read.qxmd.com/read/35337156/medical-cannabis-in-pediatric-oncology-friend-or-foe
#4
REVIEW
Megan Malach, Igor Kovalchuk, Olga Kovalchuk
The antineoplastic effects of cannabis have been known since 1975. Since the identification of the components of the endogenous cannabinoid system (ECS) in the 1990s, research into the potential of cannabinoids as medicine has exploded, including in anti-cancer research. However, nearly all of this research has been on adults. Physicians and governing bodies remain cautious in recommending the use of cannabis in children, since the ECS develops early in life and data about cannabis exposure in utero show negative outcomes...
March 16, 2022: Pharmaceuticals
https://read.qxmd.com/read/34342433/inhibition-of-isoleucyl-trna-synthetase-by-the-hybrid-antibiotic-thiomarinol
#5
JOURNAL ARTICLE
Rachel A Johnson, Andrew N Chan, Ryan D Ward, Caylie A McGlade, Breanne M Hatfield, Jason M Peters, Bo Li
Hybrid antibiotics are an emerging antimicrobial strategy to overcome antibiotic resistance. The natural product thiomarinol A is a hybrid of two antibiotics: holothin, a dithiolopyrrolone (DTP), and marinolic acid, a close analogue of the drug mupirocin that is used to treat methicillin-resistant Staphylococcus aureus (MRSA). DTPs disrupt metal homeostasis by chelating metal ions in cells, whereas mupirocin targets the essential enzyme isoleucyl-tRNA synthetase (IleRS). Thiomarinol A is over 100-fold more potent than mupirocin against mupirocin-sensitive MRSA; however, its mode of action has been unknown...
August 3, 2021: Journal of the American Chemical Society
https://read.qxmd.com/read/33804793/cannabis-cannabidiol-oils-and-tetrahydrocannabinol-what-do-veterinarians-need-to-know
#6
REVIEW
Nancy De Briyne, Danny Holmes, Ian Sandler, Enid Stiles, Dharati Szymanski, Sarah Moody, Stephan Neumann, Arturo Anadón
As cannabis-derived products have become more available, veterinarians are seeing more cases of toxicosis. In addition, animal owners are having an increasing interest in using these products for their pets. This review looks at the situation in Europe and North America, the different types of cannabis and cannabis-derived products with historical examples of use in animals, and the cannabis industry. The existing regulatory framework for use in humans and animals as medicines and/or supplements was examined...
March 20, 2021: Animals: An Open Access Journal From MDPI
https://read.qxmd.com/read/33564897/-three-years-of-cannabis-as-medicine-preliminary-results-of-the-survey-accompanying-the-prescription-of-medical-cannabis-in-germany
#7
JOURNAL ARTICLE
Gabriele Schmidt-Wolf, Peter Cremer-Schaeffer
In Germany, physicians who prescribe medical cannabis flowers or cannabis-based medicines (narcotic prescription) at the expense of the statutory health insurance are obliged to take part in a noninterventional accompanying survey that runs until 31 March 2022.At the time of this interim evaluation, 11 May 2020, there were 10,010 complete datasets collected. The most frequently treated symptoms were pain (73%), followed by spasticity (10%), and anorexia/wasting (6%). Dronabinol (i.e., prescription drug or Marinol®) was most frequently (65%) prescribed, followed by cannabis flowers (18%), Sativex® (13%), cannabis extract (4%, with increasing frequency), and nabilone (0...
February 9, 2021: Bundesgesundheitsblatt, Gesundheitsforschung, Gesundheitsschutz
https://read.qxmd.com/read/30689342/dark-classics-in-chemical-neuroscience-%C3%AE-9-tetrahydrocannabinol
#8
REVIEW
Samuel D Banister, Jonathon C Arnold, Mark Connor, Michelle Glass, Iain S McGregor
Cannabis ( Cannabis sativa) is the most widely used illicit drug in the world, with an estimated 192 million users globally. The main psychoactive component of cannabis is (-)- trans-Δ9 -tetrahydrocannabinol (Δ9 -THC), a compound with a diverse range of pharmacological actions. The unique and distinctive intoxication caused by Δ9 -THC primarily reflects partial agonist action at central cannabinoid type 1 (CB1 ) receptors. Δ9 -THC is an approved therapeutic treatment for a range of conditions, including chronic pain, chemotherapy-induced nausea and vomiting, and multiple sclerosis, and is being investigated in indications such as anorexia nervosa, agitation in dementia, and Tourette's syndrome...
May 15, 2019: ACS Chemical Neuroscience
https://read.qxmd.com/read/27557472/linking-in-vitro-lipolysis-and-microsomal-metabolism-for-the-quantitative-prediction-of-oral-bioavailability-of-bcs-ii-drugs-administered-in-lipidic-formulations
#9
JOURNAL ARTICLE
Paloma Benito-Gallo, Maria Marlow, Vanessa Zann, Peter Scholes, Pavel Gershkovich
Lipidic formulations (LFs) are increasingly utilized for the delivery of drugs that belong to class II of the Biopharmaceutics Classification System (BCS). The current work proposes, for the first time, the combination of in vitro lipolysis and microsomal metabolism studies for the quantitative prediction of human oral bioavailability of BCS II drugs administered in LFs. Marinol and Neoral were selected as model LFs, and their observed oral bioavailabilities (Fobserved ) were obtained from published clinical studies in humans...
October 3, 2016: Molecular Pharmaceutics
https://read.qxmd.com/read/27435265/cannabinoids-inflammation-and-fibrosis
#10
REVIEW
Robert B Zurier, Sumner H Burstein
Cannabinoids apparently act on inflammation through mechanisms different from those of agents such as nonsteroidal anti-inflammatory drugs (NSAIDs). As a class, the cannabinoids are generally free from the adverse effects associated with NSAIDs. Their clinical development thus provides a new approach to treatment of diseases characterized by acute and chronic inflammation and fibrosis. A concise survey of the anti-inflammatory actions of the phytocannabinoids Δ9 -tetrahydrocannabinol (THC), cannabidiol, cannabichromene, and cannabinol is presented...
November 2016: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://read.qxmd.com/read/27109234/chronic-%C3%AE-9-tetrahydrocannabinol-administration-reduces-ige-b-cells-but-unlikely-enhances-pathogenic-sivmac251-infection-in-male-rhesus-macaques-of-chinese-origin
#11
JOURNAL ARTICLE
Qiang Wei, Li Liu, Zhe Cong, Xiaoxian Wu, Hui Wang, Chuan Qin, Patricia Molina, Zhiwei Chen
Delta9-tetrahydrocannabinol (Δ(9)-THC) is the major psychoactive component of the cannabis plant. Δ(9)-THC has been used in the active ingredient of Marinol as an appetite stimulant for AIDS patients. Its impact on progression of HIV-1 infection, however, remains debatable. Previous studies indicated that Δ(9)-THC administration enhanced HIV-1 infection in huPBL-SCID mice but seemingly decreased early mortality in simian immunodeficiency virus (SIV) infected male Indian-derived rhesus macaques. Here, we determine the chronic effect of Δ(9)-THC administration using 0...
September 2016: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://read.qxmd.com/read/27007804/various-acylglycerols-from-common-oils-exert-different-antitumor-activities-on-colorectal-cancer-cells
#12
JOURNAL ARTICLE
Rebeca P Ramos-Bueno, María J González-Fernández, José L Guil-Guerrero
Colorectal cancer is one of the leading causes of death in Western countries; therefore, the implementation of healthy dietary habits in order to prevent its occurrence is a desirable action. We show here that both free fatty acids (FFAs) and some acylglycerols induce antitumoral actions in the colorectal cancer cell line HT-29. We tested several C18 polyunsaturated fatty acid-enriched oils (e.g., sunflower and Echium) as well as other oils, such as arachidonic acid-enriched (Arasco®) and docosahexaenoic acid-enriched (Marinol® and cod liver oil), in addition to coconut and olive oils...
2016: Nutrition and Cancer
https://read.qxmd.com/read/26443472/medical-marijuana-patient-counseling-points-for-health-care-professionals-based-on-trends-in-the-medical-uses-efficacy-and-adverse-effects-of-cannabis-based-pharmaceutical-drugs
#13
REVIEW
Jayesh R Parmar, Benjamin D Forrest, Robert A Freeman
The purpose of this report is to present a review of the medical uses, efficacy, and adverse effects of the three approved cannabis-based medications and ingested marijuana. A literature review was conducted utilizing key search terms: dronabinol, nabilone, nabiximols, cannabis, marijuana, smoke, efficacy, toxicity, cancer, multiple sclerosis, nausea, vomiting, appetite, pain, glaucoma, and side effects. Abstracts of the included literature were reviewed, analyzed, and organized to identify the strength of evidence in medical use, efficacy, and adverse effects of the approved cannabis-based medications and medical marijuana...
July 2016: Research in Social & Administrative Pharmacy: RSAP
https://read.qxmd.com/read/26162535/a-state-of-the-art-review-of-the-management-and-treatment-of-taste-and-smell-alterations-in-adult-oncology-patients
#14
REVIEW
Trina Thorne, Karin Olson, Wendy Wismer
PURPOSE: The purpose of this review was to examine studies of interventions for the prevention and management of taste and smell alterations (TSA) experienced by adult oncology patients. METHODS: Articles published between 1993 and 2013 were identified by searching CINAHL, MEDLINE and Food Science & Technology Abstracts (FSTA) and were included if they were in English and focused on adult oncology patients. Only interventions within the scope of nursing practice were reviewed...
September 2015: Supportive Care in Cancer
https://read.qxmd.com/read/25957748/comparing-treatment-effects-of-oral-thc-on-simulated-and-on-the-road-driving-performance-testing-the-validity-of-driving-simulator-drug-research
#15
JOURNAL ARTICLE
J L Veldstra, W M Bosker, D de Waard, J G Ramaekers, K A Brookhuis
RATIONALE: The driving simulator provides a safe and controlled environment for testing driving behaviour efficiently. The question is whether it is sensitive to detect drug-induced effects. OBJECTIVE: The primary aim of the current study was to investigate the sensitivity of the driving simulator for detecting drug effects. As a case in point, we investigated the dose-related effects of oral ∆(9)-tetrahydrocannabinol (THC), i.e. dronabinol, on simulator and on-the-road driving performance in equally demanding driving tasks...
August 2015: Psychopharmacology
https://read.qxmd.com/read/25666611/fatty-acid-binding-proteins-fabps-are-intracellular-carriers-for-%C3%AE-9-tetrahydrocannabinol-thc-and-cannabidiol-cbd
#16
JOURNAL ARTICLE
Matthew W Elmes, Martin Kaczocha, William T Berger, KwanNok Leung, Brian P Ralph, Liqun Wang, Joseph M Sweeney, Jeremy T Miyauchi, Stella E Tsirka, Iwao Ojima, Dale G Deutsch
Δ(9)-Tetrahydrocannabinol (THC) and cannabidiol (CBD) occur naturally in marijuana (Cannabis) and may be formulated, individually or in combination in pharmaceuticals such as Marinol or Sativex. Although it is known that these hydrophobic compounds can be transported in blood by albumin or lipoproteins, the intracellular carrier has not been identified. Recent reports suggest that CBD and THC elevate the levels of the endocannabinoid anandamide (AEA) when administered to humans, suggesting that phytocannabinoids target cellular proteins involved in endocannabinoid clearance...
April 3, 2015: Journal of Biological Chemistry
https://read.qxmd.com/read/24835149/dithiolopyrrolones-biosynthesis-synthesis-and-activity-of-a-unique-class-of-disulfide-containing-antibiotics
#17
REVIEW
Bo Li, Walter J Wever, Christopher T Walsh, Albert A Bowers
Covering: up to 2014. Dithiolopyrrolone (DTP) group antibiotics were first isolated in the early half of the 20th century, but only recently has research been reawakened by insights gained from the synthesis and biosynthesis of this structurally intriguing class of molecules. DTPs are characterized by an electronically unique bicyclic structure, which contains a compact disulfide bridge between two ene-thiols. Points of diversity within the compound class occur outside of the bicyclic core, at the two amide nitrogens...
July 2014: Natural Product Reports
https://read.qxmd.com/read/24691713/a-unified-strategy-for-the-synthesis-of-the-c1-c14-fragment-of-marinolic-acids-mupirocins-pseudomonic-acids-and-thiomarinols-total-synthesis-of-pseudomonic-acid-methyl-monate-c
#18
JOURNAL ARTICLE
Y Sridhar, P Srihari
A flexible stereoselective approach to the common C1-C14 skeleton present in natural products of the pseudomonic acid family is described. The strategy has been extended and the total synthesis of pseudomonic acid methyl monate C was achieved. The key synthetic reactions utilized include Achmatowicz rearrangement, Johnson-Claisen rearrangement, Julia-Kocienski olefination, and Horner-Wadsworth-Emmons olefination reaction.
May 14, 2014: Organic & Biomolecular Chemistry
https://read.qxmd.com/read/24197528/effects-of-dietary-borage-oil-enriched-in-%C3%AE-linolenic-acid-18-3-n-6-or-marine-fish-oil-enriched-in-eicosapentaenoic-acid-20-5-n-3-on-growth-mortalities-liver-histopathology-and-lipid-composition-of-juvenile-turbot-scophthalmus-maximus
#19
JOURNAL ARTICLE
J G Bell, D R Tocher, F M Macdonald, J R Sargent
A marine fish oil, Marinol K (MO) and borage oil (BO) were used to formulate diets relatively rich in eicosapentaenoic acid [EPA; 20:5(n-3)] and γ-linolenic acid [GLA; 18:3(n-6)], respectively. The diets were fed to duplicate groups of juvenile turbot (Scophthalmus maximus) of initial weight 1.4 g for a period of 12 weeks. No differences were observed in final weights either between duplicate tanks or between dietary treatments. Mortalities in the MO-fed group were significantly greater than in the BO-fed group...
October 1995: Fish Physiology and Biochemistry
https://read.qxmd.com/read/23421098/-marihuana-and-cannobinoids-as-medicaments
#20
REVIEW
Marek Tkaczyk, Ewa Florek, Wojciech Piekoszewski
Biological activity of cannabinoids is caused by binding to two cannabinoid receptors CB1 and CB2. Psychoactive is not only tetrahydrocannabinol (THC) but also: cannabidiol, cannabigerol or cannabichromen. Formerly, the usefulness of hemp was assessed in the relation to temporary appeasement of the symptoms of some ailments as nausea or vomiting. Present discoveries indicates that cannabis-based drugs has shown ability to alleviate of autoimmunological disorders such as: Multiple sclerosis (MS), Rheumatoid arthritis (RA) or inflammatory bowel disease...
2012: Przegla̧d Lekarski
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