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Carbonic anhydrase 3

Abdur Rauf, Ghias Uddin, Bina S Siddiqui, Ajmal Khan, Umar Farooq, Farhan A Khan, Syed Majid Bukhari, Sher Bahadar Khan
Two new dimeric naphthoquinones, 5',8'-dihydroxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (1; Di-naphthodiospyrol D) and 5',8'-dihydroxy-5,8-dimethoxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (2; Di-naphthodiospyrol E), along with known naphthoquinones diospyrin (3) and 8-hydroxy diospyrin (4) were isolated from the chloroform fraction of extract of Diospyros lotus roots. Their structures were elucidated by advanced spectroscopic analyses, including HSQC, HMBC, NOESY, and J-resolved NMR experiments...
November 2017: Chinese Journal of Natural Medicines
Ebru Akkemik, Baki Cicek, Yasemin Camadan, Umit Calisir, Zekai Onbasioglu
Carbonic anhydrases (CAs) play an important function in various physiological and pathological processes. Therefore, many researchers work in this field in order to design and synthesize new drugs. Both inhibitors and activators of CAs, which are associated with the diagnosis and treatment of many diseases, are very important. The emergence of the use of CA activators in the treatment of Alzheimer has led many scholars to work on this issue. In this study, CA activators and inhibitors are determined. The crown ethers compounds (1, 2, 3, 6, 7, 8, and 9) were found to cause activation on enzyme activities of hCA I and II...
January 12, 2018: Journal of Biochemical and Molecular Toxicology
Eva Havránková, Jozef Csöllei, Daniela Vullo, Vladimír Garaj, Pavel Pazdera, Claudiu T Supuran
A new series of s-triazine derivatives incorporating sulfanilamide, homosulfanilamide, 4-aminoethyl-benzenesulfonamide and piperazine or aminoalcohol structural motifs is reported. Molecular docking was exploited to select compounds from virtual combinatorial library for synthesis and subsequent biological evaluation. The compounds were prepared by using step by step nucleophilic substitution of chlorine atoms from cyanuric chloride (2,4,6-trichloro-1,3,5-triazine). The compounds were tested as inhibitors of physiologically relevant carbonic anhydrase (CA, EC 4...
January 3, 2018: Bioorganic Chemistry
Serdar Burmaoglu, Ali O Yilmaz, Parham Taslimi, Oztekin Algul, Deryanur Kilic, Ilhami Gulcin
A series of novel phloroglucinol derivatives were designed, synthesized, characterized spectroscopically and tested for their inhibitory activity against selected metabolic enzymes, including α-glycosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I and II (hCA I and II). These compounds displayed nanomolar inhibition levels and showed Ki values of 1.14-3.92 nM against AChE, 0.24-1.64 nM against BChE, 6.73-51.10 nM against α-glycosidase, 1.80-5.10 nM against hCA I, and 1...
January 11, 2018: Archiv der Pharmazie
Andrea Angeli, Sonia Del Prete, Sameh M Osman, Fatmah A S Alasmary, Zeid AlOthman, William A Donald, Clemente Capasso, Claudiu T Supuran
The activation of a β-class carbonic anhydrase (CAs, EC from Mycobacterium tuberculosis, encoded by the gene Rv3273 (mtCA 3), was investigated using a panel of natural and non-natural amino acids and amines. mtCA 3 was effectively activated by D-DOPA, L-Trp, dopamine and serotonin, with KAs ranging between 8.98 and 12.1 µM. L-His and D-Tyr showed medium potency activating effects, with KAs in the range of 17.6-18.2 µM, whereas other amines and amino acids were relatively ineffective activators, with KAs in the range of 28...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Abdul M Baig, R Zohaib, S Tariq, H R Ahmad
AIM: This study intended to trace the evolution of acid-base buffers and water homeostasis in eukaryotes. Acanthamoeba castellanii  was selected as a model unicellular eukaryote for this purpose. Homologies of proteins involved in pH and water regulatory mechanisms at cellular levels were compared between humans and A. castellanii. MATERIALS & METHODS: Amino acid sequence homology, structural homology, 3D modeling and docking prediction were done to show the extent of similarities between carbonic anhydrase 1 (CA1), aquaporin (AQP), band-3 protein and H+ pump...
January 11, 2018: Future Microbiology
Alexander M Clifford, Alyssa M Weinrauch, Greg G Goss
Hagfish are capable of tolerating extreme hypercapnia (> 30 Torr) by mounting substantial plasma [HCO3-] (hypercarbia) to compensate for CO2-mediated acidosis. The goal of this study was to characterize the mechanistic hypercarbia-recovery strategies in the highly CO2 tolerant hagfish. We exposed hagfish to hypercapnia (30 Torr) for 48 h and allowed a 24 h recovery period in normocapnic seawater. Within 8 h of the recovery period, the compensatory plasma [HCO3-] load (~ 70 mmol L-1) was rapidly offloaded...
December 30, 2017: Journal of Comparative Physiology. B, Biochemical, Systemic, and Environmental Physiology
Parham Taslimi, Afsun Sujayev, Fikret Turkan, Emin Garibov, Zübeyir Huyut, Vagif Farzaliyev, Sevgi Mamedova, İlhami Gulçin
The conversion reactions of pyrimidine-thiones with nucleophilic reagent were studied during this scientific research. For this purpose, new compounds were synthesized by the interaction between 1,2-epoxy propane, 1,2-epoxy butane, and 4-chlor-1-butanol and pyrimidine-thiones. These pyrimidine-thiones derivatives (A-K) showed good inhibitory action against acetylcholinesterase (AChE), and human carbonic anhydrase (hCA) isoforms I and II. AChE inhibition was in the range of 93.1 ± 33.7-467.5 ± 126.9 nM. The hCA I and II were effectively inhibited by these compounds, with Ki values in the range of 4...
December 28, 2017: Journal of Biochemical and Molecular Toxicology
Andrea Angeli, Niccolò Chiaramonte, Dina Manetti, Maria Novella Romanelli, Claudiu T Supuran
Four human (h) carbonic anhydrase isoforms (CA, EC, hCA I, II, IV, and VII, were investigated for their activation profile with piperazines belonging to various classes, such as N-aryl-, N-alkyl-, N-acyl-piperazines as well as 2,4-disubstituted derivatives. As the activation mechanism involves participation of the activator in the proton shuttling between the zinc-coordinated water molecule and the external milieu, these derivatives possessing diverse basicity and different scaffolds were appropriate for being investigated as CA activators (CAAs)...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Lam Phung, Ivonne V Lollett, Raquel Goldhardt, Janet L Davis, Larry Young, Dana Ascherman, Anat Galor
Purpose: To report on a case of a young female with progressing dry eye symptoms and evolving autoimmune markers consistent with a presentation of early Sjogren's syndrome (SS). Observations: A 32 year-old female presented with chronic dry eye symptoms refractory to artificial tears. Slit lamp examination revealed punctate epithelial erosions, decreased tear break-up time, and decreased tear lake bilaterally. Initial tests for ocular surface inflammation (InflammaDry, Quidel, San Diego) and systemic autoantibodies (antinuclear antibodies, anti-SSA/Ro and anti-SSB/La) were negative...
December 2017: American Journal of Ophthalmology Case Reports
Laura Lucarini, Lucia Magnelli, Nicola Schiavone, Alfonso Crisci, Alessio Innocenti, Luca Puccetti, Fabio Cianchi, Sara Peri, Claudiu T Supuran, Laura Papucci, Emanuela Masini
Carbonic anhydrase (CA, EC IX is regarded as a tumour hypoxia marker and CA inhibitors have been proposed as a new class of antitumor agents, with one such agent in Phase II clinical trials. The expression of some CAs, in particular the isoforms CA IX and CA XII, has been correlated with tumour aggressiveness and progression in several cancers. The aim of this study was to evaluate the possibility that CA IX could represent a marker related to clear cell Renal Cell Carcinoma (ccRCC). Bcl-2 and Bax, and the activity of caspase-3, evaluated in tissue biopsies from patients, were congruent with resistance to apoptosis in ccRCCs with respect to healthy controls, respectively...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Xinxin Song, Shan Zhu, Yangchun Xie, Jiao Liu, Lingyi Sun, Dexing Zeng, Pengcheng Wang, Xiaochao Ma, Guido Kroemer, David L Bartlett, Timothy R Billiar, Michael Lotze, Herbert Zeh, Rui Kang, Daolin Tang
BACKGROUND & AIMS: Maintenance of acid-base homeostasis is required for normal physiology, metabolism, and development. It is not clear how cell death is activated in response to changes in pH. We performed a screen to identify agents that induce cell death in a pH-dependent manner (we call this alkaliptosis) in pancreatic ductal adenocarcinoma cancer (PDAC) cells and tested their effects in mice. METHODS: We screened a library of 254 compounds that interact with G protein-coupled receptors (GPCRs) to identify those with cytotoxic activity against a human PDAC cell line (PANC1)...
December 14, 2017: Gastroenterology
Jie Yang, Chan Xu, Hao Chen, Mi Huang, Xinhua Ma, Shihao Deng, Yun Huang, Yanzhang Wen, Xinzhou Yang, Ping Song
Extracts and components of Taxodium ascendens Brongn, an excellent afforestation tree, have exhibited several activities, including antibacterial activity and inhibitory activity on carbonic anhydrase II. However, the anti-hepatocellular carcinoma (anti-HCC) activity of extracts from the leaves of T. ascendens (TALE) remains unclear. In the present study, six diterpenoid compounds were isolated from a TALE extract. Here, the pro-apoptotic activities and the molecular mechanisms of TALE and the compounds 1-6 on HepG2 and Hep3B HCC cells were evaluated...
November 24, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Carolina A Freire, Anieli C Maraschi, Alessandra F Lara, Enelise M Amado, Viviane Prodocimo
Some Macrobrachium shrimps (Caridea, Palaemonidae) are diadromous; freshwater adults are truly euryhaline, while larvae need saline water for development. Branchial Na+/K+-ATPase (NKA) and carbonic anhydrase (CA) are involved in NaCl absorption in freshwater. This study aimed at verifying the time course of the osmoregulatory response of adult Macrobrachium acanthurus to high salinity brackish water (20‰), from the first 30min to 5days. The goal was to detect possible transition from hyper- to hyporegulation, the putative involvement of branchial NKA and CA, or the induction of muscular HSP70 expression...
December 10, 2017: Comparative Biochemistry and Physiology. Part B, Biochemistry & Molecular Biology
Laura Forker, Piers Gaunt, Stefano Sioletic, Patrick Shenjere, Robert Potter, Darren Roberts, Joely Irlam, Helen Valentine, David Hughes, Ana Hughes, Lucinda Billingham, Rob Grimer, Beatrice Seddon, Ananya Choudhury, Martin Robinson, Catharine M L West
BACKGROUND: Despite high metastasis rates, adjuvant/neoadjuvant systemic therapy for localised soft tissue sarcoma (STS) is not used routinely. Progress requires tailoring therapy to features of tumour biology, which need exploration in well-documented cohorts. Hypoxia has been linked to metastasis in STS and is targetable. This study evaluated hypoxia prognostic markers in the phase III adjuvant radiotherapy VorteX trial. METHODS: Formalin-fixed paraffin-embedded tumour biopsies, fresh tumour/normal tissue and blood were collected before radiotherapy...
December 12, 2017: British Journal of Cancer
Adriano Mollica, Giorgia Macedonio, Azzurra Stefanucci, Simone Carradori, Atilla Akdemir, Andrea Angeli, Claudiu T Supuran
It has been proven that specific isoforms of human carbonic anhydrase (hCA) are able to fine-tune physiological pathways connected to signal processing, and that decreased CAs expression negatively influences cognition, leading to mental retardation, Alzheimer's disease, and aging-related cognitive dysfunctions. For this reason, a small library of natural and synthetic nitrogen containing cyclic derivatives was assayed as activators of four human isoforms of carbonic anhydrase (hCA I, II, IV and VII). Most of the compounds activated hCA I, IV and VII in the micromolar range, with KAs ranging between 3...
December 9, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Jing Sun, Lina Wei, Yanzi Wang, Zhiping Zhao, Wenfang Liu
In recent years, the application of carbonic anhydrase (CA) in CO2 removal has attracted great interest. However, obtaining high enzyme recovery activity is difficult in existing immobilization techniques. In this work, water plasma-treated poly(vinylidene fluoride) (PVDF) membranes were modified via 3-aminopropyl triethoxy silane (KH550) or γ-(2, 3-epoxypropoxy) propyl trimethoxy silane (KH560), and then CA was attached. The immobilization process was optimized and the catalytic properties of PVDF-attached CA were characterized...
December 9, 2017: Biotechnology and Applied Biochemistry
Jacelyn J Shu, Till S Harter, Phillip R Morrison, Colin J Brauner
Recent findings indicate that some teleost fishes may be able to greatly enhance hemoglobin-oxygen (Hb-O2) unloading at the tissues under conditions that result in catecholamine release. The putative mechanism relies on the high pH sensitivity of teleost hemoglobin (Hb), intracellular red blood cell (RBC) pH regulation via β-adrenergic Na+/H+ exchanger (β-NHE) activity, and plasma-accessible carbonic anhydrase at the tissues that short-circuits RBC pH regulation. Previous studies have shown that in rainbow trout, this system may double Hb-O2 unloading to red muscle compared to a situation without short-circuiting...
December 7, 2017: Journal of Comparative Physiology. B, Biochemical, Systemic, and Environmental Physiology
Takahiro Ogawa, Shohei Hattori, Kazuki Kamezaki, Hiromi Kato, Naohiro Yoshida, Yoko Katayama
Carbonyl sulfide (COS) is one of the major sources of stratospheric sulfate aerosols, which affect the global radiation balance and ozone depletion. COS-degrading microorganisms are ubiquitous in soil and important for the global flux of COS. We examined the sulfur isotopic fractionation during the enzymatic degradation of COS by carbonyl sulfide hydrolase (COSase) from Thiobacillus thioparus THI115. The isotopic fractionation constant (34ε value) was -2.2±0.2‰. Under experimental conditions performed at parts per million by volume level of COS, the 34ε value for intact cells of T...
December 2, 2017: Microbes and Environments
Alexander Sapegin, Stanislav Kalinin, Andrea Angeli, Claudiu T Supuran, Mikhail Krasavin
4-Chloro-3-nitrobenzenesulfonamide reacted cleanly at room-temperature with a range of bis-electrophilic phenols bearing an NH-acidic functionality (secondary carboxamide or pyrazole) in the ortho-position. This produced a novel class of [1,4]oxazepine-based primary sulfonamides which exhibited strong inhibition of therapeutically relevant human carbonic anhydrases. 2-Chloronitrobenzene did not enter a similar cyclocondensation process, even under prolonged heating. Thus, the primary sulfonamide functionality plays a dual role by enabling the [1,4]oxazepine ring construction and acting as a enzyme prosthetic zinc-binding group when the resulting [1,4]oxazepine sulfonamides are employed as carbonic anhydrase inhibitors...
November 21, 2017: Bioorganic Chemistry
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