RESUMEN
Ferulasinkins A-D (1-4), four new norlignans, were isolated from the resins of Ferula sinkiangensis, a medicinal plant of the Apiaceae family. All of them were obtained as racemic mixtures, chiral HPLC was used to produce their (+)- and (-)-antipodes. The structures of these new compounds, including their absolute configurations, were elucidated by spectroscopic and computational methods. This isolation provides new insight into the chemical profiling of F. sinkiangensis resins beyond the well-investigated structure types such as sesquiterpene coumarins and disulfides. Compounds 2a and 3a were found to significantly inhibit the invasion and migration of triple-negative breast cancer (TNBC) cell lines via CCK-8 assay. On the other hand, the wound-healing assay also demonstrated that compounds 4a and 4b could promote the proliferation of human umbilical vein endothelial cells (HUVECs). Notably, the promoting effects of 4a and 4b were observed as more significant versus a positive control using basic fibroblast growth factor (bFGF).
Asunto(s)
Ferula , Sesquiterpenos , Cumarinas/química , Cumarinas/farmacología , Células Endoteliales , Ferula/química , Humanos , Estructura Molecular , Resinas de Plantas , Sesquiterpenos/química , Sesquiterpenos/farmacologíaRESUMEN
Among numerous heterometallic chalcogenidoantimonates, relatively a few amine-directed Ge-Sb-S compounds have been synthesized. Presented here are the solvothermal syntheses, crystal structures, and ion-exchange, optical, and photocatalytic properties of two novel amine-directed Ge-Sb-S compounds, namely, [CH3NH3]20Ge10Sb28S72·7H2O (1) and [(CH3CH2CH2)2NH2]3Ge3Sb5S15·0.5(C2H5OH) (2). The structure of 1 features an unprecedented two-dimensional Ge-Sb-S double-layer composed of two twofold rotational symmetry-related thick [Ge8Sb28S72]n(28n-) single layers adhered via vertex-sharing [GeS4] tetrahedra. Compound 2 features a unique [Ge3Sb5S15]n(3n-) slab perforated with large elliptic-like windows. Remarkably, compound 1 exhibited excellent Cs(+) ion-exchange property despite the presence of excess competitive cations, such as Na(+), K(+), Mg(2+), and Ca(2+) ions. In addition, compound 1 displayed visible-light-driven photocatalytic activity for degradation of rhodamine B.
RESUMEN
Three unusual oleanane-derived triterpenoids, stytontriterpenes A-C (1-3), were isolated from the resin of Styrax tonkinensis together with an oleanane-lactone (stytontriterpene D, 4). Their structures and absolute configurations were characterised using a combination of spectroscopic analysis, electronic circular dichroism, and theoretical calculations. 1 and 2 belong to nor-oleanane with rare spiro D/E rings and 3 contains one infrequent C32 scaffold. 1 considerably suppressed the number of adhered leukemic monocytes (THP-1) to human umbilical vein endothelial cells and attenuated the upregulations of mRNA and protein levels of intracellular adhesion molecule-1 and vascular cell adhesion molecule-1 at 5 µM, suggesting that 1 might be a promising anti-vascular inflammatory chemical for atherosclerosis therapy. Plausible biosynthetic pathways for 1-4 are also proposed.
Asunto(s)
Aterosclerosis , Triterpenos , Humanos , Styrax/química , Triterpenos/química , Resinas de Plantas/química , Células Endoteliales de la Vena Umbilical Humana , Aterosclerosis/tratamiento farmacológico , Aterosclerosis/metabolismoRESUMEN
CONTEXT: Since AMP-activated protein kinase (AMPK) activation in skeletal muscle of obese rodents stimulates fatty acid oxidation, it is reasonable to hypothesize that pharmacological activation of AMPK might be of therapeutic benefit in obesity. OBJECTIVE: To investigate the effects of the traditional Korean anti-obesity drug GGEx18, a mixture of three herbs, Laminaria japonica Aresch (Laminariaceae), Rheum palmatum L. (Polygonaceae), and Ephedra sinica Stapf (Ephedraceae), on obesity and the involvement of AMPK in this process. MATERIALS AND METHODS: After high fat diet-induced obese mice were treated with GGEx18, we studied the effects of GGEx18 on body weight, fat mass, skeletal muscle lipid accumulation, and the expressions of AMPK, peroxisome proliferator-activated receptor ά (PPARα), and PPARα target genes. The effects of GGEx18 and/or the AMPK inhibitor compound C on lipid accumulation and expression of the above genes were measured in C2C12 skeletal muscle cells. RESULTS: Administration of GGEx18 to obese mice for 9 weeks significantly (p < 0.05) decreased body and adipose tissue weights compared with obese control mice (p < 0.05). Lipid accumulation in skeletal muscle was inhibited by GGEx18. GGEx18 significantly (p < 0.05) increased skeletal muscle mRNA levels of AMPKα1 and AMPKα2 as well as PPARα and its target genes. Consistent with the in vivo data, GGEx18 inhibited lipid accumulation, and similar activation of genes was observed in GGEx18-treated C2C12 cells. However, compound C inhibited these effects in C2C12 cells. DISCUSSION AND CONCLUSION: These results suggest that GGEx18 improves obesity through skeletal muscle AMPK and AMPK-stimulated expression of PPARα and its target enzymes for fatty acid oxidation.
Asunto(s)
Proteínas Quinasas Activadas por AMP/metabolismo , Fármacos Antiobesidad/farmacología , Ephedra sinica , Laminaria , Músculo Esquelético/efectos de los fármacos , Obesidad/tratamiento farmacológico , PPAR alfa/metabolismo , Preparaciones de Plantas/farmacología , Rheum , Proteínas Quinasas Activadas por AMP/antagonistas & inhibidores , Proteínas Quinasas Activadas por AMP/genética , Adiposidad/efectos de los fármacos , Animales , Fármacos Antiobesidad/química , Línea Celular , Dieta Alta en Grasa , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Regulación de la Expresión Génica/efectos de los fármacos , Metabolismo de los Lípidos/efectos de los fármacos , Masculino , Ratones , Ratones Endogámicos C57BL , Músculo Esquelético/enzimología , Obesidad/enzimología , Obesidad/etiología , Obesidad/genética , Obesidad/fisiopatología , PPAR alfa/genética , Extractos Vegetales , Preparaciones de Plantas/química , Plantas Medicinales , Inhibidores de Proteínas Quinasas/farmacología , Pirazoles/farmacología , Pirimidinas/farmacología , ARN Mensajero/metabolismo , Transducción de Señal/efectos de los fármacos , Factores de Tiempo , Pérdida de Peso/efectos de los fármacosRESUMEN
Two new triterpenoids, 3-oxotirucalla-7,9(11),24-trien-21-oic acid (1) and 18Hα,3ß,20ß-ursanediol (2), along with 15 known triterpenes, α-amyrin, α-boswellic acid, ß-boswellic acid, acetyl α-boswellic acid, acetyl ß-boswellic acid, 9,11-dehydro-ß-boswellic acid, 9,11-dehydro-α-boswellic acid, acetyl 11α-methoxy-ß-boswellic acid, 11-keto-ß-boswellic acid, acetyl 11-keto-ß-boswellic acid, acetyl α-elemolic acid, 3ß-hydroxytirucalla-8,24-dien-21-oic acid, elemonic acid, 3α-hydroxytirucalla-7,24-dien-21-oic acid, and 3α-hydroxytirucall-24-en-21-oic acid, were isolated from the resin of Boswellia carterii Birdw.
Asunto(s)
Boswellia/química , Medicamentos Herbarios Chinos/aislamiento & purificación , Triterpenos/aislamiento & purificación , Medicamentos Herbarios Chinos/química , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Resinas de Plantas/química , Estereoisomerismo , Triterpenos/químicaRESUMEN
INTRODUCTION: This case report is presented to improve our understanding of the atypical immunophenotype of hairy cell leukemia. PATIENT CONCERNS: A 58-year-old woman presented to our department with fatigue for >10âdays. DIAGNOSIS: The patient was diagnosed with an increased proportion of abnormal lymphocytes in peripheral blood and bone marrow smear, positive for CD11c, CD19, CD20, CD22, CD25, CD123, CD200, and Kappa, partial expression of CD23, but no expression of CD103, positive for BRAF V600E mutation. INTERVENTIONS AND OUTCOMES: Cladribine combined with rituximab achieved complete remission of minor residual disease negativity. CONCLUSION: Hairy cell leukemia is rare, and the diagnosis and differential diagnosis should be made by combining the patient's medical history, clinical manifestations, immunophenotype, gene detection, and other means. Purine nucleoside analogs are the first-line treatments.
Asunto(s)
Antineoplásicos/uso terapéutico , Cladribina/uso terapéutico , Leucemia de Células Pilosas/tratamiento farmacológico , Rituximab/uso terapéutico , Antígenos CD , Femenino , Humanos , Inmunofenotipificación , Cadenas alfa de Integrinas , Leucemia de Células Pilosas/diagnóstico , Persona de Mediana Edad , Neoplasia Residual , Receptores de IgE , Resultado del TratamientoRESUMEN
From the dried root and rhizomes of Atalantia buxifolia afford 11 compounds, one new compound 1 and ten known compounds 2-11 were isolated and identified. The novel compound 1 was alkaloid glycoside. Its mother nuclear was the acridone, which was relatively rare. The structure of compound 1 was established identified by spectrum and elucidated as ß-D-Glu-4,5-dimethoxy-1,6-dihydroxy-10-methyl-acridone. The compound 1 enriched the compound library and laid the material foundation for the subsequent study of pharmacological activities.
Asunto(s)
Alcaloides/química , Rutaceae/química , Acridonas/química , Alcaloides/aislamiento & purificación , Glicósidos/química , Espectroscopía de Resonancia Magnética , Estructura Molecular , Raíces de Plantas/química , Rizoma/químicaRESUMEN
Three new phenolic compounds, acutacoside C (1), acutacoside D (2) and acutacoside E (3) were isolated from the aerial part of Argyreia acuta. The oligosaccharide chain was composed of two glucoses and three rhamnoses, and the aglycone was (11S)-hydroxyhexadecanoic acid (jalapinolic acid). The core of the three compounds was operculinic acid B, which was rare in resin glycosides. Their structures were established by a combination of spectroscopic and chemical methods. Compounds 1-3 have been evaluated for inhibitory activity against α-glucosidase, which all showed weak inhibitory activities.
Asunto(s)
Convolvulaceae/química , Inhibidores de Glicósido Hidrolasas/farmacología , Glicósidos/aislamiento & purificación , Resinas de Plantas/aislamiento & purificación , Glicósidos/química , Glicósidos/farmacología , Componentes Aéreos de las Plantas/química , Resinas de Plantas/química , Resinas de Plantas/farmacologíaRESUMEN
Two new compounds of acutacosides 1 and 2, pentasaccharide resin glycosides were isolated from the aerial parts of Argyreia acuta. The core of the two compounds was operculinic acid A, and they were esterfied at the same position, just one substituent group was linked at C-2 of Rha. The absolute configuration of the aglycone in the two compounds was established by Mosher's method, which was (11S)-hydroxyhexadecanoic acid (jalapinolic acid). Their structures were established by a combination of spectroscopic and chemical methods.
Asunto(s)
Convolvulaceae/química , Oligosacáridos/química , Resinas de Plantas/química , Glicósidos/química , Espectroscopía de Resonancia Magnética , Oligosacáridos/aislamiento & purificación , Componentes Aéreos de las Plantas/química , Extractos Vegetales/química , Plantas Medicinales/químicaRESUMEN
OBJECTIVE: To establish a method used for optimization of harvesting time and determine the best time for harvesting Rumex gmelini. METHOD: An HPLC method was applied to determinate the contents of seven active constituents(resveratrol, polydatin, chrysophanol 1-glucoside, nepodin, emodin, chrysophanol and physcion)of R. gmelini at different development stage. The result was analyzed by principal component analysis. RESULT: The accumulation of active constituents showed a regular pattern. CONCLUSION: The best harvesting time of R. gmelini is early July.
Asunto(s)
Emodina/análisis , Plantas Medicinales/química , Análisis de Componente Principal , Rumex/química , Antraquinonas/análisis , Emodina/análogos & derivados , Glucósidos/análisis , Raíces de Plantas/química , Plantas Medicinales/crecimiento & desarrollo , Análisis de Componente Principal/métodos , Control de Calidad , Resveratrol , Rumex/crecimiento & desarrollo , Estaciones del Año , Estilbenos/análisisRESUMEN
Reactions of [Mn6O2(piv)10(py)2.5(piv)1.5], Ln(NO3)3·6H2O and N-mdeaH2 in MeCN in the presence of Me3SiCl generated a family of octanuclear Mn/Ln complexes [Mn6(III)Mn(II)Ln(N-mdea)3(N-mdeaH)(piv)8O2(OH)3(NO3)(H2O)]·xCH3CN·xH2O [Ln = Gd (1), Dy (2), Er (3), pivH = pivalic acid, N-mdeaH2 = N-methyl diethanolamine]. Each complex possesses a [Mn6(III)Mn(II)Ln(µ3-O)2(µ3-OH)3](16+) core containing two butterfly-like subunits of [Mn3Ln(µ3-OH)2] and [Mn4(µ3-O)2] sharing a common vertex, and an outer Mn atom ligated to one of the subunits through a µ3-OH(-) ligand. The core topology represents a new Mn/Ln core type. The magnetic susceptibility study of 1-3 indicates the presence of dominant antiferromagnetic interactions within the complexes. For complex 1, which contains an isotropic Gd(III) atom, fitting of the obtained M/(NµB) vs. H/T data gave S = 4, g = 1.90, and D = -0.31 cm(-1). The results were further supported by ac data. Complex exhibits out-of-phase ac susceptibility signals, indicating it may be a SMM.
RESUMEN
Exploration of the complex Ni2(MBD)4 (MBD = 2-mercaptobenzimidazole) (C1) having different coordinated Ni atoms as a photocatalyst for hydrogen evolution is made. For comparison, the bimetallic Ni2(MBT)4 (MBT = 2-mercaptobenthiazole) (C2) complex with the same coordinated Ni atoms was synthesized. Both of the complexes have been successfully constructed for photo-induced hydrogen production using organic dyes as photosensitizers and triethanolamine (TEOA) as the effective electron donor by visible light (>400 nm) in acetonitrile-water solution. The time-dependence of H2 generation and DFT computational studies demonstrate that the complex C1 is more active than C2 for H2 evolution. The mechanisms of photocatalytic hydrogen generation for C1 and C2 involve different protonation sites resulting from the differences between the two structures.
RESUMEN
Two [FeFe] hydrogenase mimics, [Fe(2)(µ-pdt)(CO)(5)L1] (L1 = PPh(2)SPhNH(2)) (Ph = phenyl) (2) and [Fe(2)(µ-pdt)(CO)(5)L2] (L2 = PPh(2)PhNH(2)) (3), and two molecular photocatalysts, [(CO)(5)(µ-pdt)Fe(2)PPh(2)SPhNHCO(bpy)(ppy)(2)Ir]PF(6) (bpy = bipyridine, ppy = 2-phenylpyridine) (2a) and [(CO)(5)(µ-pdt)Fe(2)PPh(2)PhNHCO(bpy)(ppy)(2)Ir](PF(6)) (3a), have been designed and synthesized, anchoring Ir(ppy)(2)(mbpy)PF(6) (mbpy = 4-methyl-4'-carbonyl-2,2'-bipyridine) (PS) to one of the iron centers of complexes 2 and 3 by forming amide bonds. Molecular dyads 2a, 3a and the intermolecular systems 2, 3 with PS have also been successfully constructed for photoinduced H(2) production using triethylamine (TEA) as a sacrificial electron donor by visible light (>400 nm) in CH(3)CN-H(2)O solution. The time-dependence of H(2) generation and spectroscopic studies suggest that the activity of H(2) evolution can be tuned by addition of a S atom to the phosphane ligand. The highest turnover numbers (TON) of hydrogen evolution obtained are 127, using 2a as a photocatalyst in a supramolecular system, and 138, based on catalyst 2 in a multi-component system. Density functional theory (DFT) computational studies demonstrate that the S atom in the second coordination sphere makes complex 2 accept an electron more easily than 3 and improves the activity in light-induced hydrogen production.
Asunto(s)
Hidrógeno/química , Hidrogenasas/química , Iridio/química , Proteínas Hierro-Azufre/química , Compuestos Organometálicos/química , Fármacos Fotosensibilizantes/química , Catálisis , Hidrogenasas/metabolismo , Proteínas Hierro-Azufre/metabolismo , Modelos Moleculares , Estructura Molecular , Procesos Fotoquímicos , Teoría CuánticaRESUMEN
This study was purposed to clarify the difference of microRNA (miRNA) expression in the peripheral blood cells of patients with primary immune thrombocytopenia (ITP) and normal controls. Exqion miRCURY(TM) microarray was used to investigate differentially expressed miRNA of peripheral blood cells obtained from affected ITP patients and the healthy controls. Cluster analysis was used to identify miRNA expression profile between the ITP patients and the healthy controls. Real-time PCR was used for validation. The results showed that a total of 159 miRNA were found to be differentially expressed in ITP patients compared to the controls, with 79 up-regulated and 80 down-regulated. Based on these differentially expressed miRNA, a tree with clear distinction between the controls and ITP patients was generated by cluster analysis. Real-time PCR confirmed microarray analysis results. It is concluded that differentially expressed miRNA were found in the peripheral blood cells from ITP patients, which may be potential novel biomarkers for ITP as well as help to elucidate pathogenic mechanisms of ITP.
Asunto(s)
MicroARNs/metabolismo , Trombocitopenia/sangre , Trombocitopenia/genética , Adulto , Estudios de Casos y Controles , Análisis por Conglomerados , Femenino , Perfilación de la Expresión Génica , Humanos , Masculino , MicroARNs/genética , Persona de Mediana Edad , Análisis de Secuencia por Matrices de Oligonucleótidos , Trombocitopenia/metabolismoRESUMEN
OBJECTIVE: To clone and express the gene of Hgp44 in adhesin domains of gingipains from Porphyromonas gingivalis (Pg) and to purify the protein. METHODS: The genomic DNA of Pg was isolated from PgATCC33277. The Hgp44 gene fragment was amplified by polymerase chain reaction (PCR) and then inserted into the cloning vector pMD18-T and sequenced. The correct fragment was linked with a prokaryotic expression vector pET-22b to construct the recombinant expression plasmid pET22b-Hgp44. The pET22b-Hgp44 confirmed by enzyme digestion was transformed into competent Escherchia coli (Ec) BL21 (DE3) cells. Expression of fusion protein was induced by isopropyl-ß-D-thiogalactoside (IPTG), and purified by immobilized metal-chelating affinity chromatography (IMAC) using a Ni(2+) matrix column. SDS-polyaerylamide gel electrophoresis (SDS-PAGE) and Western blotting analysis were used to examine the fusion protein. RESULTS: A 1 100 bp fragment was successfully amplified and verified by the agarose gel electrophoresis and sequencing. The generated recombinant expression vectors pET22b-Hgp44 were verified by enzyme digestion and agarose gel electrophoresis. The expression of fusion protein in Ec BL21 (DE3) cells was examined by SDS-PAGE and Western blotting analyses, and the data showed that the protein was 44 000 in size and expressed mostly in the form of inclusion body. The purification of fusion protein was achieved using Ni(2+) affinity chromatography. About 3.5 mg/L fusion protein was obtained. CONCLUSIONS: Hgp44 was successfully expressed in the prokaryotic expression system and purified by IMAC using a Ni(2+) matrix column.