RESUMEN
Liriogerphines A-D (1-4, respectively), an unprecedented class of hybrids of germacranolide-type sesquiterpenoids and aporphine-type alkaloids, were isolated from the rare medicinal plant Liriodendron chinense. Their structures were elucidated by comprehensive spectroscopic analyses combined with electronic circular dichroism calculations and X-ray crystallographic data. Biosynthetically, an aza-Michael addition reaction is proposed to be involved in the assemblies of this class of hybrids. Compound 4 exhibited cytotoxicity against leukemia cells via inducing apoptosis and inhibiting Bcl-2 expression.
Asunto(s)
Alcaloides , Antineoplásicos , Liriodendron , Sesquiterpenos , Alcaloides/química , Alcaloides/farmacología , China , Estructura Molecular , Sesquiterpenos/química , Sesquiterpenos/farmacología , ÁrbolesRESUMEN
The ethanolic extracts of the dried flower buds of two Caprifoliaceae plants, Lonicera japonica and Abelia × grandiflora, showed considerable inhibitory activities against adenosine triphosphate (ATP)-citrate lyase (ACL), a new promising drug target for the treatment of metabolic disorders. Bioassay-guided purification in conjunction with HPLC-PDA profiling led to the isolation and characterization of thirty-five (1-35) and fourteen (1'-14') structurally diverse compounds from the above two plant extracts, respectively. Compounds 1-9 and 1'-6' are previously undescribed glycosides. Their structures were elucidated on the basis of spectroscopic data, electronic circular dichroism (ECD), and single crystal X-ray diffraction analyses. In particular, lonicejaposide A (1) has an unprecedented skeleton generated through the coupling of C-7 in secologanin with C-2'' in phenylacetaldehyde via an aldol condensation. Abeliflorosides A (1') and B (2') are hitherto unknown glycosides of triterpene and bisiridoid conjugates constructed through the formation of a 1,3-dioxane moiety. All the isolates were evaluated for their inhibitory activities against ACL. Compounds 9, 25-28, 31, 1', 2', and 14' displayed significant inhibitory effects, with IC50 values ranging from 0.1 to 14.2 µM. The interactions of selected compounds possessing different structure features (e.g., 9, 25, 31, and 2') with ACL were thereafter performed by employing molecular docking studies. In addition, compound 2', the most complex triterpene-bisiridoid conjugate glycoside reported herein, also inhibited acetyl-CoA carboxylase 1 (ACC1), with an IC50 value of 7.9 µM. The dried material of the flower buds of L. japonica (honeysuckle) is a well-known traditional oriental medicine (i.e., Flos Lonicerae Japonicae, FLJ) and has long been used in large quantities. The above findings not only provide new insights for the development of multipurpose utilization of FLJ in healthcare community, but also provide profitable clues indicating that the flower buds of A. × grandiflora might be a potential alternative to FLJ in the traditional Chinese medicine market.
Asunto(s)
Caprifoliaceae , Lonicera , Triterpenos , Adenosina Trifosfato , Flores/química , Glicósidos/química , Lonicera/química , Simulación del Acoplamiento Molecular , Complejos Multienzimáticos , Oxo-Ácido-LiasasRESUMEN
Clonorosins A (1) and B (2), two novel indole alkaloids featuring unprecedented 6/5/6/6/5 and 6/5/5 cores, together with seven known indole-linked 2,5-diketopiperazine alkaloids (3-9), were isolated from the soil-derived fungus Clonostachys rosea YRS-06. The new structures were proposed through HR-MS, NMR, and ECD spectroscopic data. They were established by comparing the calculated NMR, ECD, and specific rotation data with the experimental. To assist in determining the absolute configuration of the chiral carbon in the side chain of 2,5-diketopiperazine derivatives, flexible analogues 3i-3iv were synthesized and analyzed. 1 was active against Fusarium oxysporum with an MIC value of 50 µg/mL. 7 and 8 showed excellent activity against human HeLa and HepG2 cells with IC50 values of 0.12-0.60 µM.
Asunto(s)
Antibacterianos/farmacología , Hypocreales/química , Alcaloides Indólicos/farmacología , Antibacterianos/aislamiento & purificación , Productos Biológicos/aislamiento & purificación , Productos Biológicos/farmacología , Células HeLa , Células Hep G2 , Humanos , Alcaloides Indólicos/aislamiento & purificación , Estructura Molecular , Microbiología del SueloRESUMEN
During a phytochemical investigation of the unripe fruits of Rubus chingii Hu (i.e., Fructus Rubi, a traditional Chinese medicine named "Fu-Pen-Zi"), a number of highly oxygenated terpenoids were isolated and characterized. These included nine ursane-type (1, 2, and 4-10), five oleanane-type (3, 11-14), and six cucurbitane-type (15-20) triterpenoids, together with five ent-kaurane-type diterpenoids (21-25). Among them, (4R,5R,8R,9R,10R,14S,17S,18S,19R,20R)-2,19α,23-trihydroxy-3-oxo-urs-1,12-dien-28-oic acid (rubusacid A, 1), (2R*,4S*,5R*,8R*,9R*,10R*,14S*,17S*, 18S*,19R*,20R*)-2α,19α,24-trihydroxy-3-oxo-urs-12-en-28-oic acid (rubusacid B, 2), (5R,8R,9R,10R, 14S,17R,18S,19S)-2,19α-dihydroxy-olean-1,12-dien-28-oic acid (rubusacid C, 3), and (3S,5S,8S,9R, 10S,13R,16R)-3α,16α,17-trihydroxy-ent-kaur-2-one (rubusone, 21) were previously undescribed. Their chemical structures and absolute configurations were elucidated on the basis of spectroscopic data and electronic circular dichroism (ECD) analyses. Compounds 1 and 3 are rare naturally occurring pentacyclic triterpenoids featuring a special α,ß-unsaturated keto-enol (diosphenol) unit in ring A. Cucurbitacin B (15), cucurbitacin D (16), and 3α,16α,20(R),25-tetrahydroxy-cucurbita-5,23- dien-2,11,22-trione (17) were found to have remarkable inhibitory effects against NF-κB, with IC50 values of 0.08, 0.61, and 1.60 µM, respectively.
Asunto(s)
Candida albicans/efectos de los fármacos , Diterpenos , Frutas/química , Rubus/química , Triterpenos , Diterpenos/química , Diterpenos/farmacología , Células HEK293 , Humanos , Estructura Molecular , FN-kappa B/metabolismo , Fitoquímicos/química , Fitoquímicos/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Triterpenos/química , Triterpenos/farmacologíaRESUMEN
Metals from the natural environment have potential hypertension effects. However, relevant studies on this topic are few. A total of 1358 adults aged 18-74 years from Chizhou, Maanshan, and Tongling of Anhui Province participated in the baseline study from 2014 to 2015. The follow-up study was performed from 2016 to 2017. Inductively coupled plasma optical emission spectrometry (7000 DV) was used to measure urinary Cr, Mn, Fe, Cu, and Zn of residents. Urinary concentrations of Cd determined via TAS-900 atomic absorption spectrophotometry at 228.8 nm wavelength. A total of 275 hypertension cases were identified. After adjusting for sociodemographic factors and risk factors for hypertension, four metals (Cd, Cr, Cu, and Mn) were significantly associated with hypertension in the single-metal model. Upon including all metals in the same model, the hazard ratios of the highest quartiles Cd and Cu compared with the reference group were 1.42 (95% confidence interval [CI] 1.09-2.02) and 1.56 (95% CI 1.16-2.09) for cases of hypertension. Our findings suggested that high levels of Cd and Cu might increase the incidence of hypertension. Further studies involving larger population should be conducted to confirm these findings.
Asunto(s)
Hipertensión/inducido químicamente , Hipertensión/epidemiología , Metales Pesados/orina , Adulto , Anciano , China/epidemiología , Exposición a Riesgos Ambientales/efectos adversos , Femenino , Estudios de Seguimiento , Humanos , Hipertensión/orina , Incidencia , Masculino , Metales Pesados/análisis , Metales Pesados/toxicidad , Persona de Mediana Edad , Factores de Riesgo , Contaminantes del Suelo/análisis , Espectrofotometría AtómicaRESUMEN
Four undescribed palmarumycin-type spirodioxynaphthalenes (phyligustricins A-D) and a known biogenetic precursor (palmarumycin BG1) were isolated from a solid fermentation of Phyllosticta ligustricola HDF-L-2, an endophyte associated with the endangered Chinese conifer Pseudotsuga gaussenii. The structures were elucidated by spectroscopic methods, single-crystal X-ray diffraction analyses, and electronic circular dichroism calculations. Both phyligustricins A and B have an unprecedented spirodioxynaphthalene-derived skeleton containing an extra 4H-furo [3,2-c]pyran-4-one moiety, while phyligustricins C and D are p-hydroxy-phenethyl substituted spirodioxynaphthalenes. The plausible biosynthetic relationships of the isolates were briefly proposed. Phyligustricins C and D and palmarumycin BG1 showed considerable antibacterial activity against Staphylococcus aureus, each with an MIC value of 16 µg/mL. Palmarumycin BG1 displayed significant inhibitory effects against ACL and ACC1, with IC50 values of 1.60 and 8.00 µM, respectively.
Asunto(s)
Ascomicetos , Pseudotsuga , Ascomicetos/química , Antibacterianos/farmacología , Antibacterianos/químicaRESUMEN
A phytochemical investigation on the stems of Glycosmis puberula var. craibii led to the isolation of a new indole alkaloid (named glycosmiscrol A, 1), together with four known compounds (2-5). The new structure was elucidated by detailed analysis of comprehensive spectroscopic methods. All isolated compounds were evaluated for their antiproliferative activities against five human cancer cell lines: HL-60, SMMC-7721, A-549, MCF-7 and SW480 in vitro. Compounds 1-5 showed significant antiproliferative effects with IC50 values ranging from 0.16 to 8.58 µM.
Asunto(s)
Antineoplásicos Fitogénicos , Rutaceae , Antineoplásicos Fitogénicos/farmacología , Línea Celular Tumoral , Humanos , Alcaloides Indólicos/farmacología , Estructura Molecular , Tallos de la PlantaRESUMEN
A number of previously undescribed (1-7) and structurally related known (8-17) isobenzofuran-type polyketides were obtained from the fermentation of Penicillium commune P-4-1, an endophytic fungus isolated from the fresh trunk bark of the critically endangered conifer Abies beshanzuensis. Beshanzoides A-D (1-4, resp.) feature a cycloheptanone-containing isobenzofuran ring system hitherto unknown, which might be biosynthesized via two steps of aldol reactions starting from a common co-occurring isobenzofuran-type polyketide as the precursor. The new structures were elucidated by spectroscopic methods, electronic circular dichroism data, and single crystal X-ray diffraction analyses. Beshanzoide E (5) showed antimicrobial activity (MIC: 16 µg mL-1) against Staphylococcus aureus, whereas (±)-strobide A (10) inhibited (MIC: 16 µg mL-1) Candida albicans. Cyclopaldic acid (12) and 3-O-methyl-cyclopaldic acid (13) exhibited inhibitory effects against acetyl-CoA carboxylase 1 (ACC1) with IC50 values of 0.96 and 11.77 µM, respectively. Compound 12 also inhibited (IC50: 7.56 µM) ATP-citrate lyase (ACL).
RESUMEN
A preliminary phytochemical investigation of the stems of the endangered plant Ulmus elongata led to the isolation of a new coumarin derivative (named ulmuselactone A, 1) and eight known compounds (2-9). The new structure was elucidated by detailed analysis of comprehensive spectroscopic methods, and its absolute configuration was established by comparing experimental and calculated electronic circular dichroism (ECD) spectra. The isolated compounds were evaluated for their antibacterial activities.
Asunto(s)
Ulmus , Antibacterianos/farmacología , Cumarinas/farmacología , Fitoquímicos , Extractos VegetalesRESUMEN
We report here that macrocyclic H-bonded pyridone pentamers, containing five properly and convergently spaced electron-rich O-atoms that decorate a rigid cavity of 2.85â Å across, exhibit an extraordinarily high yet pH-independent capacity and selectivity in Cs+ removal. In particular, with [host]=240â µM and [Cs+ ]=15â µM, a single extraction efficiently removes more than 91% of Cs+ ions from artificial sea water, containing various competitive metal ions at a total concentration of 0.68â M ([total Mn+ ]/[Cs+ ]=4.5×104 ]). To our best knowledge, these pyridone pentamers represent the best small organic molecule-based extractants that target Cs+ ions.
RESUMEN
OBJECTIVE: As a widespread toxic metal, arsenic had potential effect for hypertensive. We evaluated the association between urinary arsenic and the incidence of hypertension in adult residents along the Yangtze River of China. METHODS: We conducted the study of 1358 adults 18 to 74 years of age from Chizhou, Maanshan, and Tongling of Anhui province, who participated in the baseline study in 2014 to 2015. Inductively coupled plasma optical emission spectrometry was used to measure urinary as of residents, and follow-up extended through 2016 to 2017. RESULTS: We identified 275 hypertension events. The hazard ratios (HRs) of highest quartile arsenic compared with lowest quartile was 1.49 for hypertension events (95% confidence interval [CI]â=â1.05 to 2.12), and HRs (≥P20 vs Asunto(s)
Arsénico/toxicidad
, Exposición a Riesgos Ambientales/efectos adversos
, Contaminantes Ambientales/toxicidad
, Hipertensión/inducido químicamente
, Ríos
, Salud Rural/estadística & datos numéricos
, Adolescente
, Adulto
, Anciano
, Arsénico/orina
, China/epidemiología
, Exposición a Riesgos Ambientales/análisis
, Exposición a Riesgos Ambientales/estadística & datos numéricos
, Contaminantes Ambientales/orina
, Femenino
, Estudios de Seguimiento
, Humanos
, Hipertensión/diagnóstico
, Hipertensión/epidemiología
, Incidencia
, Masculino
, Persona de Mediana Edad
, Modelos de Riesgos Proporcionales
, Estudios Prospectivos
, Factores de Riesgo
, Adulto Joven
RESUMEN
Fusarium, a large genus of filamentous fungi, is widely distributed in soil and plants. Fusarium is a prolific source of novel chemical constituents with various bioactivities. In search for antibiotics from soil and endophytic fungi, the secondary metabolites of Fusarium avenaceum SF-1502 and Fusarium proliferatum AF-04 were investigated. An alkaloid (1), a depsipeptide (6), and five sesquiterpenoids (7-11) were isolated from the extracts of the soil fungus F. avenaceum SF-1502. Three alkaloids (2-4), a depsipeptide (5), three sesquiterpenoids (9, 11, and 12), a sesterterpene (13), and four 1,4-naphthoquinones (14-17) were also separated from the extract of the green Chinese onion derived fungus F. proliferatum AF-04. Fusaravenin (1) represents the first example of a natural naphthoisoxazole-type zwitter-ionic alkaloid, a naphthoisoxazole formic acid connected with a morpholino carbon skeleton. Cyclonerotriol B (7) is a new cyclonerane sesquiterpene. Another new sesquiterpene, 3ß-hydroxy-ß-acorenol (12), possesses an acorane framework. The known compounds 9 and 11 were found from both fungi. The structures of the new compounds were determined via extensive HR-ESI-MS and comparison between experimental and calculated NMR results. The biological properties of 1-5 and 7-17 were evaluated against eight anthropogenic bacteria, while 1 and 7-11 were also screened for inhibitory effects against four plant pathogen bacteria. The known compounds 8, 9, and 14-17 showed potent antibacterial activities toward some of the tested anthropogenic bacteria.
Asunto(s)
Alcaloides/aislamiento & purificación , Depsipéptidos/aislamiento & purificación , Fusarium/química , Naftoquinonas/aislamiento & purificación , Sesquiterpenos/aislamiento & purificación , Microbiología del Suelo , Alcaloides/química , Alcaloides/farmacología , Antibacterianos , Depsipéptidos/química , Depsipéptidos/farmacología , Espectroscopía de Resonancia Magnética , Modelos Moleculares , Estructura Molecular , Naftoquinonas/química , Naftoquinonas/farmacología , Sesquiterpenos/química , Sesquiterpenos/farmacología , Espectrometría de Masa por Ionización de ElectrosprayRESUMEN
BACKGROUND: This study was to investigate the association of fasting serum glucose (FSG), thyroid-stimulating hormone (TSH), and thyroid hormones with papillary thyroid cancer (PTC). METHODS: A total of 649 participants were included in this case-control study. The associations of FSG, TSH, free triiodothyronine (FT3) and free thyroxine (FT4) with PTC were estimated using an unconditional logistic regression. RESULTS: Compared with the lowest quintile of TSH levels, odds ratios (ORs) and 95% confidence intervals (CIs) for association between PTC risk and highest quintile of TSH levels were 1.67 (95% CI, 0.99-2.83). However, this risk correlation was more significant in PTC cases with ≤1.0 cm tumor size (adjusted OR, 1.95; 95% CI, 1.08-3.54; adjusted P-trend, 0.05). The PTC risk was also inversely associated with the serum FT3 level in all participants (adjusted P-trend, 0.001), but positively associated with the serum FT4 (adjusted P-trend, 0.001) and FSG (adjusted P-trend, 0.01) levels. Among the participants without diabetes, the individuals with high FSG levels and abnormal TSH concentration had an increased PTC risk (adjusted OR, 3.38; 95% CI, 1.78-6.42). CONCLUSION: The current study provides evidence for the association of FSG, TSH, and thyroid hormones (FT3 and FT4) with PTC risk. However, larger relative studies are needed.
Asunto(s)
Glucemia/análisis , Cáncer Papilar Tiroideo/epidemiología , Hormonas Tiroideas/sangre , Neoplasias de la Tiroides/epidemiología , Tirotropina/sangre , Estudios de Casos y Controles , Ayuno , Femenino , Humanos , Masculino , Persona de Mediana Edad , Riesgo , Cáncer Papilar Tiroideo/patología , Neoplasias de la Tiroides/patologíaRESUMEN
Extracts of the aerial parts of Scorzonera divaricata afforded sulfoscorzonin D (1) and sulfoscorzonin E (2), two novel pyrrolidine inner salt alkaloids with a sulfated guaiane sesquiterpene lactone nucleus, along with 22 known compounds. Especially, sulfoscorzonin D containing a unusual monoterpene moiety is very rare. The structures of new compounds were established using spectroscopic analysis including one- and two-dimensional NMR and HRESIMS. The cytotoxicities of compounds 1-4 and 10 against three tumor cell lines (K562, Hela, and HepG2) were evaluated using the MTT assay. Compounds 2 and 10 exhibited moderate cytotoxic activity. The biological properties of 1-3, 5-8, 10-14, and 16-24, were screened against nine different gram-positive and gram-negative bacteria. Compounds 1, 5-8, 10, and 18, showed potent antibacterial activities. CHEMICAL COMPOUNDS STUDIED IN THIS ARTICLE: Glucozaluzanin C (PubChem CID: 442320); 1ß,4α-dihydroxy-5α,6ß,7α,11ßH-eudermn-12; 6-olide (CID: 11119093); oleanolic acid (CID: 10494); lup-20(29)-ene-3ß,28-diol (CID: 72326); (22E)-5α,8α-epidioxyergosta-6,22-dien-3ß-ol (CID: 5469431); ergosta-3ß,5α, 6ß-trialcohol (CID: 44558918); stigma-5-en-3-O-ß-glucoside (CID: 5742590); vomifoliol (CID: 12444927); trans-caffeic acid (CID: 689043); trans-p-hydroxy coumaric acid (CID: 637542); 4-hydroxy-3-methoxyphenyl ferulate (CID: 11500646); 7,3',4'-trihydroxyflavonol (CID: 5281614); tricin (ID: 5281702); luteolin (CID: 5280445); diosmetin (CID: 5281612); 5,7-dihydroxy-8-methoxyflavone (CID: 5281703); 5,7-dihydroxy-6-methoxyflavone (CID: 5320315); methyl-3,4-dihydroxy benzoate (CID: 287064); m-hydroxy benzoic acid (CID: 7420); 7-hydroxy-coumarin (CID: 5281426); and scopoletin (CID: 5280460).
Asunto(s)
Alcaloides/aislamiento & purificación , Componentes Aéreos de las Plantas/química , Scorzonera/química , Sesquiterpenos de Guayano/aislamiento & purificación , Antibacterianos/aislamiento & purificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Línea Celular Tumoral , Humanos , Estructura MolecularRESUMEN
Carpesium humile Winkl is an endemic Chinese species and no previous phytochemical studies have been reported for this species. Two new germacranolides (1 and 2) and a new phytane diterpene (5), together with five known compounds (two sesquiterpenoids and three diterpenoids), were isolated from the aerial parts of C. humile. Their structures were elucidated on the basis of extensive spectroscopic analysis. The conformations and absolute configurations of 1 and 2 were established by combinative analysis of NMR, CD exciton chirality, and X-ray crystallography data. Four germacranolides (1-4) showed strong cytotoxic activities, with broad spectrum activities against six human cancer (HepG2, HeLa, HL60, SGC7901, Lewis, and MDA231) cell lines in vitro using MTT assay, with IC50 values from 3.09 to 7.71⯵g/mL. Diterpenes (5, 6, and 8) also displayed good cytotoxic activities for selected cancer cell lines, with IC50 values in the range 5.46-8.08⯵g/mL.
Asunto(s)
Antineoplásicos Fitogénicos/aislamiento & purificación , Asteraceae/química , Diterpenos/aislamiento & purificación , Sesquiterpenos de Germacrano/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Línea Celular Tumoral , Diterpenos/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Estructura Molecular , Componentes Aéreos de las Plantas/química , Sesquiterpenos de Germacrano/farmacologíaRESUMEN
OBJECTIVE: To investigate the association among aldehyde dehydrogenase-2 (ALDH2) gene polymorphisms, alcohol flushing and efficacy of nitroglycerin (GTN) in patients with coronary heart disease. METHODS: One hundred and forty two patients with coronary heart disease, who were confirmed by coronary angiography and consistent with the criteria of selection were enrolled in this study. The patients were divided into two groups according to flushing or not after drinking wine: non-flushing group (n = 88) and flushing group (n = 54). The genotypes of ALDH2 were determined with polymerase chain reaction and direct sequencing. The efficacy of nitroglycerin on angina pectoris attacks for all the patients were obtained by observation and inquiry. Basal clinical data and nitroglycerin efficacy between the two groups were compared. RESULTS: The rate of efficacious response to GTN and ALDH2*1 genotype in non-flushing group were significantly higher than those in the flushing group (89.8% vs 37.0%, P < 0.01; 93.2% vs 44.4%, P < 0.01). The number of patients with angina pectoris attacks ameliorated by GTN in 5 minutes in the non-flushing group were remarkably higher than that in the flushing group (67.1% vs 20.4%, P < 0.01). The rate of efficacious response to GTN was significantly higher in the patients with ALDH2*1 genotype than the patients with ALDH2*2 genotype (81.1% vs 36.1%, P < 0.01) and the efficacious response to GTN in 5 minutes was higher in the patients with ALDH2*1 genotype than those with ALDH2*2 genotype (57.5% vs 11.1%, P < 0.01). CONCLUSIONS: There is relationship among ALDH2 gene polymorphisms, alcohol flushing and efficacy of nitroglycerin. The rate of efficacious response to GTN is significantly higher in non-flushing patients; this may be explained by the effect of gene polymorphisms.
Asunto(s)
Aldehído Deshidrogenasa/genética , Angina de Pecho/tratamiento farmacológico , Angina de Pecho/genética , Nitroglicerina/uso terapéutico , Polimorfismo Genético , Anciano , Consumo de Bebidas Alcohólicas , Aldehído Deshidrogenasa Mitocondrial , Angina de Pecho/metabolismo , Genotipo , Humanos , Masculino , Persona de Mediana Edad , Óxido Nítrico/metabolismo , Resultado del Tratamiento , Vasodilatadores/uso terapéuticoRESUMEN
The fungus Clonostachys rosea is widely distributed all over the world. The destructive force of this fungus, as a biological control agent, is very strong to lots of plant pathogenic fungi. As part of the ongoing search for antibiotics from fungi obtained from soil samples, the secondary metabolites of C. rosea YRS-06 were investigated. Through efficient bioassay-guided isolation, three new bisorbicillinoids possessing open-ended cage structures, tetrahydrotrichodimer ether (1) and dihydrotrichodimer ether A and B (2 and 3), and 12 known compounds were obtained. Their structures were determined via extensive NMR, HR-ESI-MS, and CD spectroscopic analyses and X-ray diffraction data. Compounds 1-3 are rare bisorbicillinoids with a γ-pyrone moiety. The biological properties of 1-15 were evaluated against six different Gram-positive and Gram-negative bacteria. Bisorbicillinoids, 2-5, and TMC-151 C and E, 14 and 15, showed potent antibacterial activity.
Asunto(s)
Antibacterianos/aislamiento & purificación , Antibacterianos/farmacología , Agentes de Control Biológico , Hypocreales/metabolismo , Microbiología del Suelo , Antibacterianos/química , Bacterias/efectos de los fármacos , Agentes de Control Biológico/química , Agentes de Control Biológico/aislamiento & purificación , Hidrocarburos Aromáticos con Puentes , Dicroismo Circular , Hypocreales/química , Espectroscopía de Resonancia Magnética , Estructura Molecular , Suelo , Espectrometría de Masa por Ionización de Electrospray , Difracción de Rayos XRESUMEN
The focus of this review is placed on the chemical structures from the species of the genus Talaromyces reported with reference to their biological activities. 221 secondary metabolites, including 43 alkaloids and peptides, 88 esters, 31 polyketides, 19 quinones, 15 steroid and terpenoids, and 25 other structure type compounds, have been included, and 66 references are cited.
RESUMEN
Alcohol consumption has an important effect on coronary atherosclerotic heart disease (CAD). Acetaldehyde dehydrogenase 2 (ALDH2) is a key enzyme in alcohol metabolism. A G-to-A missense mutation of ALDH2 gene, which causes a Glu > Lys(504) substitution, was recently shown to be associated with carotid atherosclerosis; however, its relationship with coronary atherosclerosis has not been well studied. We, therefore, investigated this relationship in Han Chinese. There are two ALDH2 alleles (1 and 2) and their combination: 1/1 (GG, typical homozygote), 1/2 (GA, heterozygote) and 2/2 (AA, atypical homozygote) in the population. Successive Han Chinese, including 89 with myocardial infarction (MI) and 142 with unstable angina, were recruited, and underwent coronary angiography and gene sequencing. Coronary atherosclerosis severity was expressed by the number of lesioned coronary arteries (>or=50% diameter stenosis) and Gensini score, calculated based on the luminal narrowing degree and its geographic importance, as assessed by angiography. Based on their ALDH2 genotypes, the 231 patients were divided into wild-type (1/1, n = 145) and mutation groups (1/2 and 2/2, n = 86). There were no significant differences in basic clinical data between the two groups; however, the mutation group had significantly higher rates of diabetes mellitus and MI, and lower prevalence of alcohol consumption than wild-type group. Yet, the two groups were not significantly different in coronary atherosclerosis severity. Multiple regression analysis has shown that the ALDH2 genotype 1/2 or 2/2 is an independent risk factor for MI, but is not associated with coronary atherosclerosis severity in Han Chinese.