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[PMID]:29334634
[Au] Autor:Hansson A; Knych H; Stanley S; Berndtson E; Jackson L; Bondesson U; Thevis M; Hedeland M
[Ad] Endereço:Division of Analytical Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala University, Box 574, SE-75123, Uppsala, Sweden. Electronic address: Annelie.Hansson@farmkemi.uu.se.
[Ti] Título:Equine in vivo-derived metabolites of the SARM LGD-4033 and comparison with human and fungal metabolites.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1074-1075:91-98, 2018 Feb 01.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:LGD-4033 has been found in human doping control samples and has the potential for illicit use in racehorses as well. It belongs to the pharmacological class of selective androgen receptor modulators (SARMs) and can stimulate muscle growth, much like anabolic steroids. However, SARMs have shown superior side effect profiles compared to anabolic steroids, which arguably makes them attractive for use by individuals seeking an unfair advantage over their competitors. The purpose of this study was to investigate the metabolites formed from LGD-4033 in the horse in order to find suitable analytical targets for doping controls. LGD-4033 was administered to three horses after which plasma and urine samples were collected and analyzed for metabolites using ultra high performance liquid chromatography coupled to a high resolution mass spectrometer. In horse urine, eight metabolites, both phase I and phase II, were observed most of which had not been described in other metabolic systems. Six of these were also detected in plasma. The parent compound was detected in plasma, but not in non-hydrolyzed urine. The longest detection times were observed for unchanged LGD-4033 in plasma and in urine hydrolyzed with ß-glucuronidase and is thus suggested as the analytical target for doping control in the horse. The metabolite profile determined in the horse samples was also compared to those of human urine and fungal incubate from Cunninghamella elegans. The main human metabolite, dihydroxylated LGD-4033, was detected in the horse samples and was also produced by the fungus. However, it was a not a major metabolite for horse and fungus, which highlights the importance of performing metabolism studies in the species of interest.
[Mh] Termos MeSH primário: Cunninghamella/metabolismo
Nitrilos/análise
Nitrilos/metabolismo
Pirrolidinas/análise
Pirrolidinas/metabolismo
[Mh] Termos MeSH secundário: Animais
Cavalos
Seres Humanos
Limite de Detecção
Nitrilos/química
Pirrolidinas/química
Extração em Fase Sólida
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4-(2-(2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl)-2-(trifluoromethyl)benzonitrile); 0 (Nitriles); 0 (Pyrrolidines)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180116
[St] Status:MEDLINE


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[PMID]:28591186
[Au] Autor:Guinea J; Escribano P; Vena A; Muñoz P; Martínez-Jiménez MDC; Padilla B; Bouza E
[Ad] Endereço:Clinical Microbiology and Infectious Diseases Department, Hospital General Universitario Gregorio Marañón, Universidad Complutense de Madrid, Madrid, Spain.
[Ti] Título:Increasing incidence of mucormycosis in a large Spanish hospital from 2007 to 2015: Epidemiology and microbiological characterization of the isolates.
[So] Source:PLoS One;12(6):e0179136, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:We studied 19 cases of proven/probable mucormycosis diagnosed from 2007 to 2015 in our hospital and assessed the microbiological characteristics of the isolates. We recorded the incidence of mucormycosis and clinical and microbiological data of infected patients. Isolates were identified to molecular level and tested for their antifungal susceptibility to azoles, amphotericin B, and liposomal amphotericin B according to the CLSI M-38 A2 procedure. The incidence of mucormycosis in cases/100,000 hospital admissions during 2007-2015 increased significantly with respect to that reported in 1988-2006 (3.3 vs. 1.2; P<0.05). Patients mainly had hematological malignancies (52.6%) and/or trauma/surgical wounds (52.6%) and had received antifungal agents before the diagnosis of mucormycosis in 68% of cases. Diagnosis was by isolation (n = 17/19) and/or direct staining (n = 17/18) of Mucorales fungi in clinical samples. Identification was by panfungal PCR in patients with negative results in culture and in direct staining. The microorganisms identified were Lichtheimia spp. (42%), Rhizopus spp. (21%), Cunninghamella bertholletiae (16%), and others (21%). Liposomal amphotericin B was always more active than the other drugs against all the microorganisms except C. bertholletiae. All patients received antifungal treatment with 1 or more antifungal agents, mainly liposomal amphotericin B (17/19). Mortality was 47.4%, although this was significantly lower in the 11 patients in whom debridement was performed (18% vs. 87.5%) (P = 0.015). The incidence of mucormycosis has risen in recent years. The proportion of cases with soft tissue involvement was high, and Lichtheimia was the most frequently involved species. The highest antifungal activity was observed with liposomal amphotericin B.
[Mh] Termos MeSH primário: Neoplasias Hematológicas/epidemiologia
Mucormicose/tratamento farmacológico
Mucormicose/epidemiologia
Ferida Cirúrgica/epidemiologia
[Mh] Termos MeSH secundário: Adulto
Idoso
Anfotericina B/uso terapêutico
Antifúngicos/uso terapêutico
Azóis/uso terapêutico
Pré-Escolar
Cunninghamella/isolamento & purificação
Cunninghamella/patogenicidade
Feminino
Neoplasias Hematológicas/complicações
Neoplasias Hematológicas/microbiologia
Neoplasias Hematológicas/cirurgia
Seres Humanos
Masculino
Meia-Idade
Mucormicose/complicações
Mucormicose/microbiologia
Rhizopus/isolamento & purificação
Rhizopus/patogenicidade
Ferida Cirúrgica/complicações
Ferida Cirúrgica/tratamento farmacológico
Ferida Cirúrgica/microbiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antifungal Agents); 0 (Azoles); 0 (liposomal amphotericin B); 7XU7A7DROE (Amphotericin B)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170913
[Lr] Data última revisão:
170913
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170608
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0179136


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[PMID]:28576722
[Au] Autor:Zhan Y; Wu Y; Xu F; Bai Y; Guan Y; Williamson JS; Liu B
[Ad] Endereço:Guangxi Colleges and Universities Key Laboratory of Biomedical Sensing and Intelligent Instrument, School of Life and Environmental Sciences, Guilin University of Electronic Technology, Guilin 541004, People's Republic of China; State Key Laboratory of Bioreactor Engineering, East China University o
[Ti] Título:A novel dihydroxylated derivative of artemisinin from microbial transformation.
[So] Source:Fitoterapia;120:93-97, 2017 Jul.
[Is] ISSN:1873-6971
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Microbial transformation of artemisinin (1) by Cunninghamella elegans was investigated. Four isolated products were identified as 6ß-hydroxyartemisinin (2), 7α-hydroxyartemisinin (3), 7ß-hydroxyartemisinin (4), and 6ß,7α-dihydroxyartemisinin (5). The structures were elucidated by spectroscopic and X-ray crystallographic analysis. Product 5 is a novel compound and being reported here for the first time. It features two hydroxyl groups in its structure, and this is the first report on dihydroxylation of the artemisinin skeleton. Quantitative structure-activity relationship and molecular modeling studies indicate the modification of artemisinin skeleton will increase antimalarial activity and water solubility. The chemical syntheses of artemisinin derivatives at C6 or C7 position are impossible due to the lack of functional groups. 6ß,7α-Dihydroxyartemisinin is hydroxylated at both 6ß- and 7α-positions of artemisinin skeleton at the same time. Therefore, this new compound would be a good scaffold for further structural modification in the search for more potent antimalarial drugs.
[Mh] Termos MeSH primário: Antimaláricos/química
Artemisininas/química
Cunninghamella/metabolismo
[Mh] Termos MeSH secundário: Biotransformação
Hidroxilação
Modelos Moleculares
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antimalarials); 0 (Artemisinins)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170731
[Lr] Data última revisão:
170731
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170604
[St] Status:MEDLINE


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[PMID]:28531555
[Au] Autor:Zawadzka K; Bernat P; Felczak A; Lisowska K
[Ad] Endereço:Department of Industrial Microbiology and Biotechnology, Faculty of Biology and Environmental Protection, University of Lodz, 12/16 Banacha Street, 90-237, Lodz, Poland.
[Ti] Título:Microbial detoxification of carvedilol, a ß-adrenergic antagonist, by the filamentous fungus Cunninghamella echinulata.
[So] Source:Chemosphere;183:18-26, 2017 Sep.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Beta adrenergic antagonists like carvedilol are typical environmental pollutants detected in wastewater and surface water. Human metabolism of carvedilol is well investigated, while its environmental fates are still unknown. In recent years, there have been appearing reports on high toxicity of ß-blockers toward aquatic organisms. In this paper the ability of the filamentous fungus C. echinulata to eliminate the ß-blocker has been described for the first time. An 83% loss of carvedilol was observed after 120 h incubation of the tested fungus with the compound, where hydroxylated carvedilol metabolites were identified as the major biotransformation products. Carvedilol degradation by C. echinulata was proceeded by hydroxylation and conjugation reactions similar to its mammalian metabolism. Glucose conjugate was found in the fungi cultures, whereas glucuronide conjugates were detected in mammals. The impact of carvedilol on the functionality of fungal cells was also evaluated. A 2-fold decrease in the PC/PE ratio was noticed in the C. echinulata cell membrane after the exposition to carvedilol compared to control mycelium incubated without the ß-blocker. The change can denote perturbation of fungal cell membrane integration by carvedilol. Moreover, 2.8-fold lower toxicity of postcultures supernatants toward D. magna were shown in contrast to abiotic control.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos beta/análise
Carbazóis/análise
Cunninghamella/metabolismo
Propanolaminas/análise
Poluentes Químicos da Água/análise
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos beta/metabolismo
Antagonistas Adrenérgicos beta/toxicidade
Animais
Biotransformação
Carbazóis/metabolismo
Carbazóis/toxicidade
Cunninghamella/efeitos dos fármacos
Daphnia/efeitos dos fármacos
Seres Humanos
Hidroxilação
Inativação Metabólica
Propanolaminas/metabolismo
Propanolaminas/toxicidade
Poluentes Químicos da Água/metabolismo
Poluentes Químicos da Água/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-Antagonists); 0 (Carbazoles); 0 (Propanolamines); 0 (Water Pollutants, Chemical); 0K47UL67F2 (carvedilol)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170927
[Lr] Data última revisão:
170927
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170523
[St] Status:MEDLINE


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[PMID]:28321075
[Au] Autor:Ino K; Nakase K; Nakamura A; Nakamori Y; Sugawara Y; Miyazaki K; Monma F; Fujieda A; Sugimoto Y; Ohishi K; Masuya M; Katayama N
[Ad] Endereço:Department of Hematology and Oncology, Mie University Hospital, Japan.
[Ti] Título:Management of Pulmonary Mucormycosis Based on a Polymerase Chain Reaction (PCR) Diagnosis in Patients with Hematologic Malignancies: A Report of Four Cases.
[So] Source:Intern Med;56(6):707-711, 2017.
[Is] ISSN:1349-7235
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Pulmonary mucormycosis (PM) is a life-threatening fungal infection in patients with hematologic malignancies, and early and accurate diagnostic modalities are urgently needed. We conducted a polymerase chain reaction (PCR) assay targeting these fungi in peripheral blood from four patients with hematologic malignancies who were strongly suspected of having PM. In these four patients, the Rhizopus species was identified in two patients, and the Cunninghamella and Absidia species in one each. Based on these molecular findings, all of the patients were successfully treated via targeted therapy with liposomal amphotericin B. In this report, a PCR analysis proved very useful for managing PM in patients with hematologic malignancies.
[Mh] Termos MeSH primário: Anfotericina B/uso terapêutico
Antifúngicos/uso terapêutico
Cunninghamella
Pneumopatias Fúngicas/tratamento farmacológico
Mucormicose/tratamento farmacológico
[Mh] Termos MeSH secundário: Adulto
Idoso
Feminino
Neoplasias Hematológicas/complicações
Seres Humanos
Pneumopatias Fúngicas/complicações
Pneumopatias Fúngicas/diagnóstico
Masculino
Meia-Idade
Mucormicose/complicações
Mucormicose/diagnóstico
Reação em Cadeia da Polimerase
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antifungal Agents); 0 (liposomal amphotericin B); 7XU7A7DROE (Amphotericin B)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170516
[Lr] Data última revisão:
170516
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170322
[St] Status:MEDLINE
[do] DOI:10.2169/internalmedicine.56.7647


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[PMID]:28234904
[Au] Autor:Siddiqui M; Ahmad MS; Wahab AT; Yousuf S; Fatima N; Naveed Shaikh N; Rahman AU; Choudhary MI
[Ad] Endereço:H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.
[Ti] Título:Biotransformation of a potent anabolic steroid, mibolerone, with Cunninghamella blakesleeana, C. echinulata, and Macrophomina phaseolina, and biological activity evaluation of its metabolites.
[So] Source:PLoS One;12(2):e0171476, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Seven metabolites were obtained from the microbial transformation of anabolic-androgenic steroid mibolerone (1) with Cunninghamella blakesleeana, C. echinulata, and Macrophomina phaseolina. Their structures were determined as 10ß,17ß-dihydroxy-7α,17α-dimethylestr-4-en-3-one (2), 6ß,17ß-dihydroxy-7α,17α-dimethylestr-4-en-3-one (3), 6ß,10ß,17ß-trihydroxy-7α,17α-dimethylestr-4-en-3-one (4), 11ß,17ß-dihydroxy-(20-hydroxymethyl)-7α,17α-dimethylestr-4-en-3-one (5), 1α,17ß-dihydroxy-7α,17α-dimethylestr-4-en-3-one (6), 1α,11ß,17ß-trihydroxy-7α,17α-dimethylestr-4-en-3-one (7), and 11ß,17ß-dihydroxy-7α,17α-dimethylestr-4-en-3-one (8), on the basis of spectroscopic studies. All metabolites, except 8, were identified as new compounds. This study indicates that C. blakesleeana, and C. echinulata are able to catalyze hydroxylation at allylic positions, while M. phaseolina can catalyze hydroxylation of CH2 and CH3 groups of substrate 1. Mibolerone (1) was found to be a moderate inhibitor of ß-glucuronidase enzyme (IC50 = 42.98 ± 1.24 µM) during random biological screening, while its metabolites 2-4, and 8 were found to be inactive. Mibolerone (1) was also found to be significantly active against Leishmania major promastigotes (IC50 = 29.64 ± 0.88 µM). Its transformed products 3 (IC50 = 79.09 ± 0.06 µM), and 8 (IC50 = 70.09 ± 0.05 µM) showed a weak leishmanicidal activity, while 2 and 4 were found to be inactive. In addition, substrate 1 (IC50 = 35.7 ± 4.46 µM), and its metabolite 8 (IC50 = 34.16 ± 5.3 µM) exhibited potent cytotoxicity against HeLa cancer cell line (human cervical carcinoma). Metabolite 2 (IC50 = 46.5 ± 5.4 µM) also showed a significant cytotoxicity, while 3 (IC50 = 107.8 ± 4.0 µM) and 4 (IC50 = 152.5 ± 2.15 µM) showed weak cytotoxicity against HeLa cancer cell line. Compound 1 (IC50 = 46.3 ± 11.7 µM), and its transformed products 2 (IC50 = 43.3 ± 7.7 µM), 3 (IC50 = 65.6 ± 2.5 µM), and 4 (IC50 = 89.4 ± 2.7 µM) were also found to be moderately toxic to 3T3 cell line (mouse fibroblast). Interestingly, metabolite 8 showed no cytotoxicity against 3T3 cell line. Compounds 1-4, and 8 were also evaluated for inhibition of tyrosinase, carbonic anhydrase, and α-glucosidase enzymes, and all were found to be inactive.
[Mh] Termos MeSH primário: 17-Cetosteroides/metabolismo
Antineoplásicos/metabolismo
Antiprotozoários/metabolismo
Cunninghamella/metabolismo
Nandrolona/análogos & derivados
Saccharomycetales/metabolismo
Congêneres da Testosterona/metabolismo
[Mh] Termos MeSH secundário: 17-Cetosteroides/química
17-Cetosteroides/isolamento & purificação
17-Cetosteroides/farmacologia
Animais
Antineoplásicos/química
Antineoplásicos/isolamento & purificação
Antineoplásicos/farmacologia
Antiprotozoários/química
Antiprotozoários/isolamento & purificação
Antiprotozoários/farmacologia
Biotransformação
Anidrases Carbônicas/química
Sobrevivência Celular/efeitos dos fármacos
Cromatografia Líquida de Alta Pressão
Cunninghamella/química
Cunninghamella/efeitos dos fármacos
Glucuronidase/antagonistas & inibidores
Glucuronidase/química
Células HeLa
Seres Humanos
Hidroxilação
Leishmania major/efeitos dos fármacos
Leishmania major/crescimento & desenvolvimento
Camundongos
Estrutura Molecular
Monofenol Mono-Oxigenase/química
Células NIH 3T3
Nandrolona/química
Nandrolona/metabolismo
Nandrolona/farmacologia
Saccharomycetales/química
Saccharomycetales/efeitos dos fármacos
Congêneres da Testosterona/química
Congêneres da Testosterona/isolamento & purificação
Congêneres da Testosterona/farmacologia
alfa-Glucosidases/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (17-Ketosteroids); 0 (Antineoplastic Agents); 0 (Antiprotozoal Agents); 0 (Testosterone Congeners); 6PG9VR430D (Nandrolone); 9OGY4BOR8D (mibolerone); EC 1.14.18.1 (Monophenol Monooxygenase); EC 3.2.1.20 (alpha-Glucosidases); EC 3.2.1.31 (Glucuronidase); EC 4.2.1.1 (Carbonic Anhydrases)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170225
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0171476


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[PMID]:28216250
[Au] Autor:Chen Y; Tian JL; Wu JS; Sun TM; Zhou LN; Song SJ; You S
[Ad] Endereço:School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China.
[Ti] Título:Biotransfomation of cyperenoic acid by Cunninghamella elegans AS 3.2028 and the potent anti-angiogenic activities of its metabolites.
[So] Source:Fitoterapia;118:32-37, 2017 Apr.
[Is] ISSN:1873-6971
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Cyperenoic acid (1) is one of the major sesquiterpenes isolated from Croton crassifolius, which exhibited potent anti-angiogenic activity. Traditional structural modification of 1 is difficult to perform by chemical technology due to the remarkable stability of the patchoulane skeleton. In order to overcome chemical synthesis difficulties and obtain structurally diverse derivations, microbial transformation of 1 by using Cunninghamella elegans AS 3.2028 was studied for the first time. Five new hydroxylated products 2-6 were obtained. Furthermore, cytotoxicity and anti-angiogenic activities of all the biotransformation products were evaluated by MTT assay and ELISA in HepG2 and MCF-7 cells. These results indicated that hydroxylated modification products 2-4 significantly inhibited VEGF release, which suggest the potential use of hydroxylated modification products for cancer therapy.
[Mh] Termos MeSH primário: Inibidores da Angiogênese/metabolismo
Croton/química
Cunninghamella/metabolismo
Sesquiterpenos/metabolismo
[Mh] Termos MeSH secundário: Biotransformação
Células Hep G2
Seres Humanos
Células MCF-7
Raízes de Plantas/química
Sesquiterpenos/isolamento & purificação
Fator A de Crescimento do Endotélio Vascular/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Angiogenesis Inhibitors); 0 (Sesquiterpenes); 0 (VEGFA protein, human); 0 (Vascular Endothelial Growth Factor A); 0 (cyperenoic acid)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170425
[Lr] Data última revisão:
170425
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170221
[St] Status:MEDLINE


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[PMID]:27988088
[Au] Autor:Dube AK; Kumar MS
[Ad] Endereço:Narsee Monjee Institute of Management Studies, Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, Vile Parle (W), Mumbai, Maharashtra, India.
[Ti] Título:Biotransformation of bromhexine by Cunninghamella elegans, C. echinulata and C. blakesleeana.
[So] Source:Braz J Microbiol;48(2):259-267, 2017 Apr - Jun.
[Is] ISSN:1678-4405
[Cp] País de publicação:Brazil
[La] Idioma:eng
[Ab] Resumo:Fungi is a well-known model used to study drug metabolism and its production in in vitro condition. We aim to screen the most efficient strain of Cunninghamella sp. among C. elegans, C. echinulata and C. blakesleeana for bromhexine metabolites production. We characterized the metabolites produced using various analytical tools and compared them with mammalian metabolites in Rat liver microsomes (RLM). The metabolites were collected by two-stage fermentation of bromhexine with different strains of Cunninghamella sp. followed by extraction. Analysis was done by thin layer chromatography, high performance thin layer chromatography, Fourier transform infrared spectroscopy, high performance liquid chromatography and Liquid chromatography-mass spectrometry. The role of Cytochrome P3A4 (CYP3A4) enzymes in bromhexine metabolism was studied. Fungal incubates were spiked with reference standard - clarithromycin to confirm the role of CYP3A4 enzyme in bromhexine metabolism. Three metabolites appeared at 4.7, 5.5 and 6.4min retention time in HPLC. Metabolites produced by C. elegans and RLM were concluded to be similar based on their retention time, peak area and peak response of 30.05%, 21.06%, 1.34%, and 47.66% of three metabolites and bromhexine in HPLC. The role of CYP3A4 enzyme in metabolism of bromhexine and the presence of these enzymes in Cunninghamella species was confirmed due to absence of peaks at 4.7, 5.4 and 6.7min when RLM were incubated with a CYP3A4 enzyme inhibitor - clarithromycin.
[Mh] Termos MeSH primário: Bromoexina/metabolismo
Cunninghamella/metabolismo
[Mh] Termos MeSH secundário: Animais
Biotransformação
Cromatografia Líquida de Alta Pressão
Cromatografia em Camada Delgada
Citocromo P-450 CYP3A/metabolismo
Espectrometria de Massas
Microssomos/metabolismo
Ratos
Espectroscopia de Infravermelho com Transformada de Fourier
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
EC 1.14.14.1 (Cytochrome P-450 CYP3A); Q1J152VB1P (Bromhexine)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170714
[Lr] Data última revisão:
170714
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161219
[St] Status:MEDLINE


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[PMID]:27918992
[Au] Autor:Hansson A; Thevis M; Cox H; Miller G; Eichner D; Bondesson U; Hedeland M
[Ad] Endereço:Division of Analytical Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala University, Box 574, SE-75123, Uppsala, Sweden. Electronic address: Annelie.Hansson@farmkemi.uu.se.
[Ti] Título:Investigation of the metabolites of the HIF stabilizer FG-4592 (roxadustat) in five different in vitro models and in a human doping control sample using high resolution mass spectrometry.
[So] Source:J Pharm Biomed Anal;134:228-236, 2017 Feb 05.
[Is] ISSN:1873-264X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:FG-4592 is a hypoxia-inducible factor (HIF) stabilizer, which can increase the number of red blood cells in the body. It has not been approved by regulatory authorities, but is available for purchase on the Internet. Due to its ability to improve the oxygen transportation mechanism in the body, FG-4592 is of interest for doping control laboratories, but prior to this study, little information about its metabolism was available. In this study, the metabolism of FG-4592 was investigated in a human doping control sample and in five in vitro models: human hepatocytes and liver microsomes, equine liver microsomes and S9 fraction and the fungus Cunninghamella elegans. By using liquid chromatography coupled to a Q-TOF mass spectrometer operated in MS and MSMS modes, twelve different metabolites were observed for FG-4592. One monohydroxylated metabolite was detected in both the human and equine liver microsome incubations. For the fungus Cunninghamella elegans eleven different metabolites were observed of which the identical monohydroxylated metabolite had the highest response. This rich metabolic profile and the higher levels of metabolites produced by Cunninghamella elegans demonstrates its usefulness as a metabolite producing medium. In the doping control urine sample, one metabolite, which was the result of a direct glucuronidation, was observed. No metabolites were detected in neither the human hepatocyte nor in the equine liver S9 fraction incubates.
[Mh] Termos MeSH primário: Cunninghamella/metabolismo
Doping nos Esportes
Glicina/análogos & derivados
Prolina Dioxigenases do Fator Induzível por Hipóxia/metabolismo
Isoquinolinas/metabolismo
Detecção do Abuso de Substâncias/métodos
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Animais
Cunninghamella/química
Doping nos Esportes/prevenção & controle
Glicina/análise
Glicina/metabolismo
Hepatócitos/química
Hepatócitos/metabolismo
Cavalos
Seres Humanos
Prolina Dioxigenases do Fator Induzível por Hipóxia/análise
Isoquinolinas/análise
Extração Líquido-Líquido/métodos
Microssomos Hepáticos/química
Microssomos Hepáticos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (FG-4592); 0 (Isoquinolines); EC 1.14.11.29 (Hypoxia-Inducible Factor-Proline Dioxygenases); TE7660XO1C (Glycine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170523
[Lr] Data última revisão:
170523
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161206
[St] Status:MEDLINE


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[PMID]:27666872
[Au] Autor:Liu Z; Lu YH; Feng X; Zou YX; Diao Z; Chu ZY
[Ad] Endereço:a College of Food Science and Technology , Shanghai Ocean University , Shanghai 201306 , China.
[Ti] Título:Microbial transformation of hederagenin by Cunninghamella echinulate, Mucor subtilissimus, and Pseudomonas oleovorans.
[So] Source:J Asian Nat Prod Res;19(7):712-718, 2017 Jul.
[Is] ISSN:1477-2213
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The pentacyclic triterpenoid hederagenin (1) was subjected to biotransformation by Cunninghamella echinulate CGMCC 3.2000, Mucor subtilissimus CGMCC 3.2454 and Pseudomonas oleovorans CGMCC 1.1641. Three metabolites were obtained. On the basis of nuclear magnetic resonance and high-resolution mass spectral analyses, their structures were characterized as 3ß, 23-dihydroxyolean-12-en-28-oic acid 28-O-ß-D-glucopyranosyl ester (2), 3ß, 15α, 23-trihydroxyolean-12-en-28-oic acid (3), 1ß, 3ß, 23-trihydroxyolean-12-en-28-oic acid (4), and metabolite (3) was a new compound. This was the first report on the biotransformation of hederagenin.
[Mh] Termos MeSH primário: Cunninghamella/metabolismo
Mucor/metabolismo
Ácido Oleanólico/análogos & derivados
Pseudomonas oleovorans/metabolismo
[Mh] Termos MeSH secundário: Biotransformação
Estrutura Molecular
Ressonância Magnética Nuclear Biomolecular
Ácido Oleanólico/química
Saponinas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Saponins); 6SMK8R7TGJ (Oleanolic Acid); RQF57J8212 (hederagenin)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170809
[Lr] Data última revisão:
170809
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160927
[St] Status:MEDLINE
[do] DOI:10.1080/10286020.2016.1232252



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