|
Celastrol
Celastrol (tripterine) is a chemical compound isolated from the root extracts of ''Tripterygium wilfordii'' (Thunder god vine) and '' Tripterygium regelii'' (Regel's threewingnut). Celastrol is a pentacyclic nortriterpen quinone and belongs to the family of quinone methides. In mice, celastrol is an NR4A1 agonist that alleviates inflammation and induces autophagy. Also in mice, celastrol increase expression of IL1R1, which is the receptor for the cytokine interleukin-1 (IL-1). IL1R1 knock-out mice exposed to celastrol exhibit no leptin-sensitizing or anti-obesity effect. In ''in vitro'' and ''in vivo'' animal experiments, celastrol exhibits antibacterial, antioxidant, anti-inflammatory, anticancer, and insecticidal activities. It has been shown to have obesity-controlling effects in mice by inhibiting negative regulators of leptin. Celastrol has also shown to possess (by inhibition of NF-κB in the hypothalamus) anti-diabetic effects on diabetic nephropathy and improve who ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tripterygium Wilfordii
''Tripterygium wilfordii'', or ''léi gōng téng'' (Mandarin) (, Japanese: ''raikōtō''), sometimes called thunder god vine but more properly translated thunder duke vine, is a vine used in traditional Chinese medicine. ''Tripterygium wilfordii'' has been promoted for use in rheumatoid arthritis and psoriasis; however, due to safety concerns this use is not recommended. Evidence is insufficient to deem it effective as a method of birth control for humans. A 2021 study published in Nature Communications found that one chemical isolated from the herb, triptonide, was an effective male birth control in mice and non-human primates, while others chemicals present in the herb have been previously shown to cause severe liver toxicity. Extracts of the bark T. wilfordii have been used as an insecticide in China for centuries, as documented in Wu Qijun’s 1848 Illustrated Catalogues of Plants. Health effects The United Kingdom government does not recommend the use of ''Tripterygium'' du ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quinone Methide
A quinone methide is a type of conjugated organic compound that contain a cyclohexadiene with a carbonyl and an exocyclic methylidene or extended alkene unit. It is analogous to a quinone, but having one of the double bonded oxygens replaced with a carbon. The carbonyl and methylidene are usually oriented either ortho or para to each other. There are some examples of transient synthetic meta quinone methides. Properties Quinone methides are cross-conjugated rather than aromatic. Nucleophilic addition at the exo-cyclic double bond will result in rearomatisation, making such reactions highly favourable. As a result, quinone methides are excellent, electrophilic Michael acceptors, react quickly with nucleophiles and can be easily reduced. They are able to act as radical scavengers via a similar process, a behaviour exploited by certain polymerisation inhibitors. Quinone methides are more polar than quinones, and therefore more chemically reactive. Simple unhindered quinone methide ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nuclear Receptor 4A1
The nuclear receptor 4A1 (NR4A1 for "nuclear receptor subfamily 4 group A member 1") also known as Nur77, TR3, and NGFI-B is a protein that in humans is encoded by the ''NR4A1'' gene. Nuclear receptor 4A1 (NR4A1) is a member of the ''NR4A'' nuclear receptor family of intracellular transcription factors. NR4A1 is involved in cell cycle mediation, inflammation and apoptosis. Nuclear receptor 4A1 plays a key role in mediating inflammatory responses in macrophages. In addition, subcellular localization of the NR4A1 protein appears to play a key role in the survival and death of cells. Expression is inducible by phytohemagglutinin in human lymphocytes and by serum stimulation of arrested fibroblasts. Translocation of the protein from the nucleus to mitochondria induces apoptosis. Multiple alternatively spliced variants, encoding the same protein, have been identified. Structure The ''NR4A1'' gene contains seven exons. An amino terminal transactivation domain is encoded in exon ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CHUK
Inhibitor of nuclear factor kappa-B kinase subunit alpha (IKK-α) also known as IKK1 or conserved helix-loop-helix ubiquitous kinase (CHUK) is a protein kinase that in humans is encoded by the ''CHUK'' gene. IKK-α is part of the IκB kinase complex that plays an important role in regulating the NF-κB transcription factor. However, IKK-α has many additional cellular targets, and is thought to function independently of the NF-κB pathway to regulate epidermal differentiation. Function NF-κB response IKK-α is a member of the serine/threonine protein kinase family and forms a complex in the cell with IKK-β and NEMO. NF-κB transcription factors are normally held in an inactive state by the inhibitory proteins IκBs. IKK-α and IKK-β phosphorylate the IκB proteins, marking them for degradation via ubiquitination and allowing NF-κB transcription factors to go into the nucleus. Once activated, NF-κB transcription factors regulate genes that are implicated in many ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quinone Methides
The quinones are a class of organic compounds that are formally "derived from aromatic compounds uch as benzene or naphthalene">benzene.html" ;"title="uch as benzene">uch as benzene or naphthalene] by conversion of an even number of –CH= groups into –C(=O)– groups with any necessary rearrangement of double bonds, resulting in "a fully Conjugated system, conjugated cyclic diketone, dione structure". The archetypical member of the class is 1,4-benzoquinone or cyclohexadienedione, often called simply "quinone" (thus the name of the class). Other important examples are 1,2-benzoquinone (''ortho''-quinone), 1,4-naphthoquinone and 9,10-anthraquinone. The name is derived from that of quinic acid (with the suffix "-one" indicating a ketone), since it is one of the compounds obtained upon oxidation of quinic acid. Quinic acid, like quinine is obtained from cinchona bark, called quinaquina in the indigenous languages of Peruvian tribes. Properties Quinones are oxidized derivativ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
The Journal Of Antibiotics
''The Journal of Antibiotics'' is a peer-reviewed medical journal published by the Nature Publishing Group Nature Portfolio (formerly known as Nature Publishing Group and Nature Research) is a division of the international scientific publishing company Springer Nature that publishes academic journals, magazines, online databases, and services in scien ... for the Japan Antibiotics Research Association. The journal seeks to endorse studies on antibiotics and associated types of biologically substances. In June 2020, the journal published a pioneer systematic review on Ivermectin and COVID-19 by Fatemeh Heiday and Reza Gharebaghi which later identified as highly cited in this field. References External links * Microbiology journals Nature Research academic journals Monthly journals Publications established in 1948 English-language journals Academic journals associated with learned and professional societies {{med-journal-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monoterpene
Monoterpenes are a class of terpenes that consist of two isoprene units and have the molecular formula C10H16. Monoterpenes may be linear (acyclic) or contain rings (monocyclic and bicyclic). Modified terpenes, such as those containing oxygen functionality or missing a methyl group, are called monoterpenoids. Monoterpenes and monoterpenoids are diverse. They have relevance to the pharmaceutical, cosmetic, agricultural, and food industries. Biosynthesis Monoterpenes are derived biosynthetically from units of isopentenyl pyrophosphate, which is formed from acetyl-CoA via the intermediacy of mevalonic acid in the HMG-CoA reductase pathway. An alternative, unrelated biosynthesis pathway of IPP is known in some bacterial groups and the plastids of plants, the so-called MEP-(2-methyl-D-erythritol-4-phosphate) pathway, which is initiated from C5 sugars. In both pathways, IPP is isomerized to DMAPP by the enzyme isopentenyl pyrophosphate isomerase. Geranyl pyrophosphate is the precurso ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thymol
Thymol (also known as 2-isopropyl-5-methylphenol, IPMP), , is a natural monoterpenoid phenol derivative of ''p''-Cymene, isomeric with carvacrol, found in oil of thyme, and extracted from ''Thymus vulgaris'' (common thyme), ajwain, and various other plants as a white crystalline substance of a pleasant aromatic odor and strong antiseptic properties. Thymol also provides the distinctive, strong flavor of the culinary herb thyme, also produced from ''T. vulgaris''. Thymol is only slightly soluble in water at neutral pH, but it is extremely soluble in alcohols and other organic solvents. It is also soluble in strongly alkaline aqueous solutions due to deprotonation of the phenol. Its dissociation constant ( p''K''a) is . Thymol absorbs maximum UV radiation at 274 nm. Chemical synthesis Thymol is produced by the alkylation of ''m''-cresol and propene: : History Ancient Egyptians used thyme for embalming. The ancient Greeks used it in their baths and burned it as ince ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Klebsiella Pneumoniae
''Klebsiella pneumoniae'' is a Gram-negative, non-motile, encapsulated, lactose-fermenting, facultative anaerobic, rod-shaped bacterium. It appears as a mucoid lactose fermenter on MacConkey agar. Although found in the normal flora of the mouth, skin, and intestines, it can cause destructive changes to human and animal lungs if aspirated, specifically to the alveoli resulting in bloody, brownish or yellow colored jelly like sputum. In the clinical setting, it is the most significant member of the genus ''Klebsiella'' of the Enterobacteriaceae. ''K. oxytoca'' and ''K. rhinoscleromatis'' have also been demonstrated in human clinical specimens. In recent years, ''Klebsiella'' species have become important pathogens in nosocomial infections. It naturally occurs in the soil, and about 30% of strains can fix nitrogen in anaerobic conditions. As a free-living diazotroph, its nitrogen-fixation system has been much-studied, and is of agricultural interest, as ''K. pneumoniae'' has been ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carbapenem-resistant Enterobacteriaceae
Carbapenem-resistant Enterobacteriaceae (CRE) or carbapenemase-producing Enterobacteriaceae (CPE) are Gram-negative bacteria that are resistant to the carbapenem class of antibiotics, considered the drugs of last resort for such infections. They are resistant because they produce an enzyme called a carbapenemase that disables the drug molecule. The resistance can vary from moderate to severe. Enterobacteriaceae are common commensals and infectious agents. Experts fear CRE as the new "superbug". The bacteria can kill up to half of patients who get bloodstream infections. Tom Frieden, former head of the Centers for Disease Control and Prevention has referred to CRE as "nightmare bacteria". Examples of enzymes found in certain types of CRE are KPC (''Klebsiella pneumoniae'' carbapenemase) and NDM (New Delhi Metallo-beta-lactamase). KPC and NDM are enzymes that break down carbapenems and make them ineffective. Both of these enzymes, as well as the enzyme VIM (Verona Integron-Mediated ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carbapenemase
Beta-lactamases, (β-lactamases) are enzymes () produced by bacteria that provide multi-resistance to beta-lactam antibiotics such as penicillins, cephalosporins, cephamycins, monobactams and carbapenems (ertapenem), although carbapenems are relatively resistant to beta-lactamase. Beta-lactamase provides antibiotic resistance by breaking the antibiotics' structure. These antibiotics all have a common element in their molecular structure: a four-atom ring known as a beta-lactam (β-lactam) ring. Through hydrolysis, the enzyme lactamase breaks the β-lactam ring open, deactivating the molecule's antibacterial properties. Beta-lactam antibiotics are typically used to target a broad spectrum of gram-positive and gram-negative bacteria. Beta-lactamases produced by gram-negative bacteria are usually secreted, especially when antibiotics are present in the environment. Structure The structure of a ''Streptomyces'' serine β-lactamase (SBLs) is given by . The alpha-beta fold ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
HSF1
Heat shock factor 1 (HSF1) is a protein that in humans is encoded by the ''HSF1'' gene. HSF1 is highly conserved in eukaryotes and is the primary mediator of transcriptional responses to proteotoxic stress with important roles in non-stress regulation such as development and metabolism. Structure Human HSF1 consists of several domains which regulate its binding and activity. DNA-Binding Domain (DBD) This N-terminal domain of approximately 100 amino acids is the most highly conserved region in the HSF protein family and consists of a helix-turn-helix loop. The DBD of each HSF1 monomer recognizes the sequence nGAAn on target DNA. Repeated sequences of the nGAAn pentamer constitute heat shock elements (HSEs) for active HSF1 trimers to bind. Oligomerization Domain (Leucine Zipper Domains) The two regions responsible for oligomerization between HSF1 monomers are leucine zipper (LZ) domains 1-3 and 4 (these regions are also commonly referred to as HR-A/B and HR-C). LZ1-3 is s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
