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1.
SLAS Technol ; 29(5): 100185, 2024 Aug 28.
Artículo en Inglés | MEDLINE | ID: mdl-39209116

RESUMEN

The study of motor muscle control mechanisms can improve rehabilitation therapy and human-computer interaction technology. The limitations of traditional electroencephalography (EEG) limit the comprehensive understanding of motor muscle control mechanisms. Therefore, this study aims to explore the mechanism of motor muscle control based on optical EEG images, in order to expand the understanding of the process of motor control. The study selected optical EEG imaging technology as the main data acquisition tool. Optical EEG images have higher spatiotemporal resolution and can provide more detailed neural activity information. This technology combines optical imaging with EEG images to obtain spatiotemporal information of brain activity in a short period of time. The device is composed of multiple optical sensors and can measure blood oxygen concentration and neuronal activity in the cerebral cortex. Preprocess EEG image data using image processing and signal processing techniques, then use computational methods and algorithms to detect activated regions, and evaluate their relationships using correlation analysis and statistical methods. By comparing EEG image data and motor muscle activity data under different motor tasks. The research results show that optical EEG imaging technology can provide more detailed information on brain neural activity and accurately capture the activity patterns of different motor muscles. These results provide new perspectives and methods for further studying the control mechanisms of motor muscles.

2.
Nat Prod Bioprospect ; 14(1): 26, 2024 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-38691189

RESUMEN

Seven undescribed compounds, including three flavones (1-3), one phenylpropanoid (19), three monoaromatic hydrocarbons (27-29), were isolated from the twigs of Mosla chinensis Maxim together with twenty-eight known compounds. The structures were characterized by HRESIMS, 1D and 2D NMR, and ECD spectroscopic techniques. Compound 20 displayed the most significant activity against A/WSN/33/2009 (H1N1) virus (IC50 = 20.47 µM) compared to the positive control oseltamivir (IC50 = 6.85 µM). Further research on the anti-influenza mechanism showed that compound 20 could bind to H1N1 virus surface antigen HA1 and inhibit the early attachment stage of the virus. Furthermore, compounds 9, 22, 23, and 25 displayed moderate inhibitory effects on the NO expression in LPS inducing Raw 264.7 cells with IC50 values of 22.78, 20.47, 27.66, and 30.14 µM, respectively.

3.
Chem Biodivers ; 21(6): e202400399, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38634752

RESUMEN

Four undescribed prenylated flavonoids, sophoratones A-D (1-4), and 17 known flavonoids, were obtained from the aerial parts of Sophora tonkinensis. Their structures with absolute configurations were elucidated by detailed interpretation of NMR spectroscopy, mass spectrometry, and ECD calculations. Meanwhile, the ability of these compounds to inhibit the release of nitric oxide (NO) by a lipopolysaccharide induced mouse in RAW 264.7 cells was assayed. The results indicated that some compounds exhibited clear inhibitory effects, with IC50 ranging from 19.91±1.08 to 35.72±2.92 µM. These results suggest that prenylated flavonoids from the aerial parts of S. tonkinensis could potentially be used as a latent source of anti-inflammatory agents.


Asunto(s)
Flavonoides , Lipopolisacáridos , Óxido Nítrico , Componentes Aéreos de las Plantas , Sophora , Sophora/química , Animales , Ratones , Flavonoides/farmacología , Flavonoides/aislamiento & purificación , Flavonoides/química , Células RAW 264.7 , Componentes Aéreos de las Plantas/química , Óxido Nítrico/antagonistas & inhibidores , Óxido Nítrico/metabolismo , Óxido Nítrico/biosíntesis , Lipopolisacáridos/farmacología , Lipopolisacáridos/antagonistas & inhibidores , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Relación Estructura-Actividad , Antiinflamatorios no Esteroideos/farmacología , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/aislamiento & purificación , Estructura Molecular , Relación Dosis-Respuesta a Droga , Supervivencia Celular/efectos de los fármacos
4.
Molecules ; 28(5)2023 Feb 22.
Artículo en Inglés | MEDLINE | ID: mdl-36903293

RESUMEN

The phytochemical investigation of the roots of the traditional Chinese medicinal plant Sophora flavescens led to the isolation of two novel prenylflavonoids with an unusual cyclohexyl substituent instead of the common aromatic ring B, named 4',4'-dimethoxy-sophvein (17) and sophvein-4'-one (18), and 34 known compounds (1-16, 19-36). The structures of these chemical compounds were determined by spectroscopic techniques, including 1D-, 2D-NMR, and HRESIMS data. Furthermore, evaluations of nitric oxide (NO) production inhibitory activity against lipopolysaccharide (LPS)-treated RAW264.7 cells indicated that some compounds exhibited obvious inhibition effects, with IC50 ranged from 4.6 ± 1.1 to 14.4 ± 0.4 µM. Moreover, additional research demonstrated that some compounds inhibited the growth of HepG2 cells, with an IC50 ranging from 0.46 ± 0.1 to 48.6 ± 0.8 µM. These results suggest that flavonoid derivatives from the roots of S. flavescens can be used as a latent source of antiproliferative or anti-inflammatory agents.


Asunto(s)
Flavonoides , Sophora , Flavonoides/química , Sophora flavescens , Sophora/química , Antiinflamatorios/farmacología , Raíces de Plantas/química , Extractos Vegetales/farmacología , Espectroscopía de Resonancia Magnética
5.
J Asian Nat Prod Res ; 25(1): 27-35, 2023 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-35503565

RESUMEN

Two new iridoid glycosides, named productasperulosidic acid butyl ester (1) and E-6-O-3-hydroxy-p-methoxycinnamoyl scandoside methyl ester (2), along with nine known ones (3-11), were isolated from Hedyotis diffusa Willd. The structures of them were elucidated by extensive 1D, 2D NMR and HR-ESI-MS spectral data. Compounds 1-11 showed no significant cytotoxic activity against HeLa cells.


Asunto(s)
Medicamentos Herbarios Chinos , Hedyotis , Humanos , Glicósidos Iridoides , Hedyotis/química , Células HeLa , Estructura Molecular , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/química
6.
International Eye Science ; (12): 2065-2069, 2023.
Artículo en Chino | WPRIM (Pacífico Occidental) | ID: wpr-998491

RESUMEN

AIM: To investigate the efficacy of epithelial-off accelerated corneal cross-linking(CXL)in the treatment of advanced keratoconus.METHODS: A retrospective study was performed on data collected from 32 patients(43 eyes)with advanced keratoconus who underwent epithelial-off accelerated CXL at Ningxia Eye Hospital from April 2020 to December 2021. Slit-lamp, intraocular pressure, uncorrected visual acuity(UCVA), corrected visual acuity, specular microscope, Pentacam and Corvis ST were tested before and at 1, 3 and 6mo after surgery. Preoperative and postoperative corneal condition, UCVA, best corrected visual acuity(BCVA)and the values of corneal endothelial, maximum keratometry(Kmax), thinnest corneal thickness(TCT), anterior and posterior surfaces of the cornea K1, K2, biomechanically corrected intraocular pressure(bIOP), applanation time 1(A1T), applanation length 1(A1L), applanation velocity 1(A1V), applanation time 2(A2T), applanation length 2(A2L), applanation velocity 2(A2V), highest concavity deformation amplitude(HCDA), radius at highest curvature(HCR), highest concavity peak distance(HCPD)and stiffness parameter at first applanation(SP-A1)were recorded.RESULTS: There were differences between UCVA(LogMAR; 1.06±0.49, 0.78±0.39)and BCVA(LogMAR; 0.48±0.34, 0.38±0.29)before and at 6mo after surgery(P<0.05), but there were no differences in corneal endothelial cells(2917.39±288.38 vs. 2959.19±336.27 cells/mm2, P=0.477). There were differences among Kmax, TCT, anterior surface K1 and K2 and posterior surface K1 before and after surgery(P<0.05), and all increased at 1mo after surgery then returned to preoperative level at 3mo after surgery, while there was no difference in the posterior K2. Furthermore, there were statistical significance in A1T, HCPD and SP-A1 before and after surgery(P<0.05), while there were no statistical significance in A1L, A1V,A2T, A2L, A2V, HCDA, HCR and bIOP(P>0.05).CONCLUSION: Epithelial-off accelerated CXL can prevent the progression of keratoconus within half year after surgery, and it has certain safety.

7.
Genet Res (Camb) ; 2022: 1273153, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35855056

RESUMEN

Background: Exercise is a regular behavioral activity that not only helps to lose weight but also reduces the risk of cardiovascular and cerebrovascular diseases. Diabetes is a common disease that plagues human health. It is shown that regular exercise can improve the insulin sensitivity of diabetic patients and have an important function in adjuvant therapy. Methods: We downloaded the GSE101931 dataset from the Gene Expression Omnibus (GEO) database, 10 samples were obtained from the GSE101931 dataset, including 5 before exercise and 5 postexercise samples, and GEO2R was used to screen the differentially expressed genes (DEGs) exhibited by a heat map. Then, the enrichment analysis of DEGs in Gene Ontology (GO) function was analyzed by Metascape, and the Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway of DEGs was also analyzed by gene set enrichment analysis (GSEA). Next, the protein-protein interaction (PPI) network maps were drawn, and the hub genes were identified through Metascape. Finally, the expressions of the hub genes in the dataset were analyzed. Results: Totally, 116 upregulated DEGs and 1017 downregulated DEGs were identified from these data. These DEGs were mainly enriched in the platelet-derived growth factor receptor signaling pathway and mRNA processing. Then, the GSEA analysis showed that 6 KEGG pathways were associated with postexercise prediabetic samples, namely, ABC transporters, focal adhesion, MAPK signaling pathway, prion diseases, melanogenesis, and gap junction. Afterward, three hub genes (HSPA8, STIP1, and HSPH1) were highly expressed after exercise through the box plot analysis. Conclusion: A myriad of research results confirms that there is a certain connection between exercise and diabetes, which provides a favorable basis for emerging exercise into the treatment of diabetic patients.


Asunto(s)
Biología Computacional , Diabetes Mellitus , Biomarcadores , Biología Computacional/métodos , Diabetes Mellitus/genética , Ejercicio Físico , Perfilación de la Expresión Génica/métodos , Regulación Neoplásica de la Expresión Génica , Redes Reguladoras de Genes , Humanos , Transcriptoma/genética
8.
Phytomedicine ; 93: 153779, 2021 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-34638030

RESUMEN

BACKGROUND: Gansui-Banxia Decoction (GSBXD) is a classic formula of traditional Chinese medical (TCM) sage Zhang Zhongjing to treat stagnation of evil heat and obstruction of qi. At present GSBXD is wildly used to treat cancerous ascites, pleural effusion, peritoneal effusion, pericardial effusion, cranial cavity effusion and several types of cancers, such as hepatocellular carcinoma (HCC) and esophageal cancer. Myeloid-derived suppressor cells (MDSCs) are a kind of immature and heterogeneous cells which can suppress lymphocytes activation by forming a suppressive environment. MDSCs accumulation in peripheral blood and tumors are closely related to the cancer stage and low survival rate of clinical patients. The antitumor immune effect of GSBXD has not received widespread attention. PURPOSE: To investigate the effects of GSBXD on MDSCs accumulation and the mediators including AKT/STAT3/ERK signaling pathways. METHODS: The chemical components of GSBXD were analyzed by UHPLC-MS, and the putative pathways of GSBXD based on Network pharmacology were predicted. Mice were vaccinated with Hepatoma 22 (H22) to establish tumor growth model, which were then administrated with GSBXD ethanol extraction (0.49 mg/kg/day, 1.75 mg/kg/day), sorafenib (60 mg/kg) or saline for 14 days. The cell morphology was evaluated by hematoxylin and eosin (H&E) staining, and immunity cells were determined through flowcytometry analysis. The levels of cytokines production in blood were evaluated by using ELISA kits. STAT3, ERK and AKT/mTOR signaling transduction associated proteins were determined by Western blot. RESULTS: GSBXD could inhibit tumor growth and splenomegaly in H22 tumor model mice. Importantly, GSBXD reduced MDSCs accumulation and differentiation, and inhibited proliferation of F4/80+ CD11b+ macrophages and apoptosis of T cells and B cells, and increased the percentage of CD 3- NK1.1+ NK cells. To better understand the active component of GSBXD, the ethanol-extraction powdered GSBXD was prepared and analyzed by UHPLC-MS. Combined with these main chemical compounds, we predicted that the anti-tumor effect of GSBXD mainly mediated PI3K-AKT and RAS-MAPK signal pathways based on Network Pharmacology. Western blot analysis of tumor tissues and MDSCs cells demonstrated that phosphorylation of AKT, ERK and STAT3 were significantly reduced, specially the activation of ERK. The levels of IL-1ß and IFN-γ were significantly decreased by ELISA analysis. CONCLUSION: GSBXD exhibited antitumor immune activity by reducing the accumulation of MDSCs in vivo, which is possible via down-regulation of AKT/STAT3/ERK signaling pathway and suppression of IL-1ß and IFN-γ.


Asunto(s)
Carcinoma Hepatocelular , Neoplasias Hepáticas , Células Supresoras de Origen Mieloide , Animales , Carcinoma Hepatocelular/tratamiento farmacológico , Línea Celular Tumoral , Humanos , Ratones , Ratones Endogámicos C57BL , Células Supresoras de Origen Mieloide/metabolismo , Fosfatidilinositol 3-Quinasas/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Factor de Transcripción STAT3 , Transducción de Señal
9.
Chem Biodivers ; 18(12): e2100693, 2021 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-34713556

RESUMEN

The bioactivity-guided isolation on the Scutellaria barbata extract resulted in the purification of four undescribed neo-clerodane diterpenoids, scuttenlines A-D (1-4), alone with 20 known diterpenoids (5-24). The chemical structures of them were elaborated by extensive spectroscopic means, including 1D, 2D-NMR and HR-MS. The anti-inflammatory potential ability of 1-24 was screened in lipopolysaccharide-stimulated mouse RAW 264.7 cells. Scuttenline C (IC50 =1.9 µM) and 18 (IC50 =3.7 µM) exhibited potent activity to inhibit NO production.


Asunto(s)
Antiinflamatorios/farmacología , Diterpenos de Tipo Clerodano/farmacología , Componentes Aéreos de las Plantas/química , Extractos Vegetales/farmacología , Scutellaria/química , Animales , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Diterpenos de Tipo Clerodano/química , Diterpenos de Tipo Clerodano/aislamiento & purificación , Lipopolisacáridos/antagonistas & inhibidores , Lipopolisacáridos/farmacología , Ratones , Conformación Molecular , Óxido Nítrico/antagonistas & inhibidores , Óxido Nítrico/biosíntesis , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Células RAW 264.7
10.
Bioorg Chem ; 115: 105178, 2021 10.
Artículo en Inglés | MEDLINE | ID: mdl-34303897

RESUMEN

Four undescribed ent-kaurane diterpenoids, wilkaunoids A - D (1-4), and three undescribed abietane diterpenoids, wilabinoids A - C (13-15), along with thirteen known ones (5-12 and 16-20), were isolated from Tripterygium wilfordii. Their structures were elucidated by extensive spectroscopic methods, electroniccirculardichroism calculation, and X-ray diffraction analysis. Compounds 1 and 2 were a pair of C-19 epimers of ent-kaurane diterpenoids, featuring a rare 19,20-epoxy-19,20-dimethoxy-kaurane fragment. Compound 3 possessed a rare naturally occurring 1,3-dioxacyclohexane moiety. Compounds 13 and 15 represented the first example of abietane diterpenoids with an isovalerate substitution from the genus of Tripterygium. The possible biosynthetic pathways of 1-3 were postulated. The effect of 1-20 on nitric oxide production was examined in lipopolysaccharide-stimulated RAW 264.7 cells. Abietane diterpenoid quinones 7-13 (IC50: 1.9-10.2 µM) exhibited the significant activity to inhibit nitric oxide production versus positive control (NG-monomethyl-l-arginine acetate salt, IC50 = 24.9 µM). The structure activity relationship of 7-13 in inhibiting nitric oxide production was then discussed. The most potent 7 and 8 were found to significantly suppress the expression of cyclooxygenase-2 and inducible nitric oxide synthase proteins, showing a good anti-inflammatory potential. The findings provided some valuable insights for the discovery and structural modification of abietane diterpenoids towards anti-inflammatory lead compounds.


Asunto(s)
Abietanos/farmacología , Antiinflamatorios/farmacología , Diterpenos de Tipo Kaurano/farmacología , Tripterygium/química , Abietanos/química , Animales , Antiinflamatorios/química , Diterpenos de Tipo Kaurano/química , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Ratones , Óxido Nítrico/metabolismo , Células RAW 264.7
11.
Chem Biodivers ; 18(4): e2001066, 2021 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-33656782

RESUMEN

Three new matrine-type alkaloids, 8ß-hydroxyoxysophoridine (1), 9ß-hydroxysophoridine (2), 9ß-hydroxyisosophocarpine (3), together with one known analog, 11,12-dehydromatrine (4), were isolated from the seeds of Sophora alopecuroides L. The structures of new compounds were elucidated using extensive spectroscopic techniques including the experimental and calculated ECD data. The anti-inflammatory activities of all the isolates on NO production in RAW 264.7 cells stimulated by lipopolysaccharide were evaluated. Among them, 8ß-hydroxyoxysophoridine (1) showed a significant inhibitory effect with an IC50 value of 18.26 µM.


Asunto(s)
Alcaloides/farmacología , Antiinflamatorios/farmacología , Óxido Nítrico/antagonistas & inhibidores , Extractos Vegetales/farmacología , Semillas/química , Sophora/química , Alcaloides/química , Alcaloides/aislamiento & purificación , Animales , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Lipopolisacáridos/antagonistas & inhibidores , Lipopolisacáridos/farmacología , Ratones , Óxido Nítrico/biosíntesis , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Células RAW 264.7
12.
Front Genet ; 12: 637755, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33613651

RESUMEN

BACKGROUND: Exercise has a positive impact on patients with osteosarcoma, improving function, reducing disability, maintaining independence and quality of life. Exercise may also directly affect the effectiveness of cancer treatment. Cell division cycle-associated protein 4 (CDCA4) is reported to function importantly during numerous human cancers development. Nevertheless, the details toward CDCA4 function are still to be investigated. METHODS: This study comprehensively analyzed the GSE74194 database and obtained aerobic exercise-related genes. Protein-protein interaction network (PPI) and Gene Ontology (GO) analysis were performed on the differentially expressed genes (DEGs). Quantitative reverse transcription polymerase chain reaction (qRT-PCR) and tumor genome atlas (TCGA) data mining were applied to measure aerobic exercise-related gene CDCA4 level in osteosarcoma tissue. We conducted lots of functional experiments to uncover CDCA4 function and its corresponding mechanism in osteosarcoma. RESULTS: We screened a total of 547 DEGs related to aerobic exercise, of which 373 were up-regulated and 174 were down-regulated. PPI analysis revealed 90 genes that might play key roles. GO analysis showed that aerobic exercise-related DEGs were significantly enriched during the mitotic cell cycle, cell division, mitotic nuclear division and sister chromatid segregation, nuclear division, microtubule cytoskeleton organization involved protein, microtubule-based process, spindle organization, G2/M transition of mitotic cell cycle. Our results indicated that CDCA4 was increased in osteosarcoma tissues and cell lines, and its level had association with high mortality of osteosarcoma patients. Further studies revealed that absence of CDCA4 largely hindered osteosarcoma cancer cell proliferation, invasion, and migration. CONCLUSION: Comprehensive bioinformatics analysis improves our understanding of the underlying molecular mechanisms of aerobic exercise on osteosarcoma. This provides evidence for the effect of aerobic exercise on CDCA4 expression. Our data suggested that CDCA4 could facilitate osteosarcoma development, and gave a hint that CDCA4 was a candidate target in the treatment of osteosarcoma, aerobic exercise might help the treatment and prognosis of patients with osteosarcoma.

13.
Metallomics ; 12(7): 1131-1141, 2020 07 22.
Artículo en Inglés | MEDLINE | ID: mdl-32453319

RESUMEN

Hepatocellular carcinoma (HCC) poses a serious threat to people's health worldwide. Artesunate (ART), one of the classical antimalarial drugs, has recently been shown to exert significant cytotoxicity in various cancers, but its bioavailability is low. Cyclometalated iridium(iii) complexes have emerged as a promising class of anticancer therapeutic agents. Herein, through conjugation of two of them, three novel Ir(iii)-ART conjugates, [Ir(C-N)2(bpy-ART)](PF6) (bpy = 2,2'-bipyridine, C-N = 2-phenylpyridine (ppy, Ir-ART-1), 2-(2-thienyl)pyridine (thpy, Ir-ART-2), and 2-(2,4-difluorophenyl)pyridine (dfppy, Ir-ART-3)) have been synthesized, and their potential as anti-HCC agents was evaluated. We demonstrate that Ir-ART-1-3 display higher cytotoxicity against HCC cell lines than normal liver cells, and they can especially locate to mitochondria of HepG2 cells and induce a series of mitochondria-mediated apoptosis events. Moreover, Ir-ART-1-3 can regulate the cell cycle and inhibit metastasis of HepG2 cells. Finally, in vivo antitumor evaluation also demonstrates the inhibitory activity of Ir-ART-1 on tumor growth. Taken together, these Ir(iii)-ART conjugates have the potential to become drug candidates for future anti-HCC treatments.


Asunto(s)
Antineoplásicos/uso terapéutico , Carcinoma Hepatocelular/metabolismo , Neoplasias Hepáticas/metabolismo , Apoptosis/efectos de los fármacos , Artesunato/química , Artesunato/farmacología , Carcinoma Hepatocelular/genética , Complejos de Coordinación/química , Complejos de Coordinación/uso terapéutico , Células Hep G2 , Humanos , Iridio/química , Iridio/farmacología , Neoplasias Hepáticas/genética
14.
Preprint en Inglés | medRxiv | ID: ppmedrxiv-20114124

RESUMEN

Children are strikingly underrepresented in COVID-19 case counts1-3. In the United States, children represent 22% of the population but only 1.7% of confirmed SARS-CoV-2 cases1. One possibility is that symptom-based viral testing is less likely to identify infected children, since they often experience milder disease than adults1,4-7. To better assess the frequency of pediatric SARS-CoV-2 infection, we serologically screened 1,775 residual samples from Seattle Children's Hospital collected from 1,076 children seeking medical care during March and April of 2020. Only one child was seropositive in March, but seven were seropositive in April for a period seroprevalence of {approx} 1%. Most seropositive children (6/8) were not suspected of having had COVID-19. The sera of seropositive children had neutralizing activity, including one that neutralized at a dilution >1:18,000. Therefore, an increasing number of children seeking medical care were infected by SARS-CoV-2 during the early Seattle outbreak despite few positive viral tests.

15.
Phytochemistry ; 175: 112373, 2020 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-32305684

RESUMEN

Twelve ent-isopimarane diterpenoids, including six undescribed ones, eupnerias J-O, were isolated from the stem barks of Euphorbia neriifolia L. Structurally, eupnerias J-M were the first examples of 18 (or 19)-norditerpenoid with ent-isopimarane skeleton from E. neriifolia. The absolute configuration of eupneria J was established based on the X-ray diffraction analysis and the experimental and calculated electronic circular dichroism (ECD), while the absolute configuration of eupnerias K-N were determined by the experimental and calculated ECD. In addition, the absolute configuration of the known compound, 3ß-hydroxysandaracopimaric acid, was determined by comparing its ECD spectrum with eupneria J, and renamed as eupneria P. Furthermore, eupneria J and eurifoloid H showed significant anti-HIV-1 activities with IC50 values of 0.31 and 6.70 µg/mL, respectively, and ent-isopimara-8(14),15-dien-3ß,12ß-diol possessed obvious anti-influenza virus activity against A/Puerto Rico/8/1934, with an IC50 at 3.86 µg/mL.


Asunto(s)
Diterpenos , Euphorbia , VIH-1 , Abietanos , Dicroismo Circular , Estructura Molecular
16.
Nat Prod Res ; 34(13): 1853-1861, 2020 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-30691300

RESUMEN

Six new compounds, including three terpenoids (1-3) and three lignans (4-6), were isolated from the 95% EtOH extract of the twigs of Tripterygium hypoglaucum. Their structures were determined on the basis of extensive spectroscopic analysis. 9'-O-benzoyl-lariciresinol (4) showed weak cytotoxicity against HepG2/Adr cells, with an IC50 value of 30.1 µM in vitro.


Asunto(s)
Lignanos/aislamiento & purificación , Terpenos/aislamiento & purificación , Tripterygium/química , Antineoplásicos/aislamiento & purificación , Antineoplásicos/farmacología , Furanos/aislamiento & purificación , Furanos/farmacología , Células Hep G2/efectos de los fármacos , Humanos , Concentración 50 Inhibidora , Lignanos/química , Lignanos/farmacología , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/farmacología , Análisis Espectral , Terpenos/química
17.
Acta Pharmaceutica Sinica B ; (6): 850-860, 2020.
Artículo en Inglés | WPRIM (Pacífico Occidental) | ID: wpr-828839

RESUMEN

Organic anion transporting polypeptide 1B1 and 1B3 (OATP1B1/3) as important uptake transporters play a fundamental role in the transportation of exogenous drugs and endogenous substances into cells. Rat OATP1B2, encoded by the gene, is homologous to human OATP1B1/3. Although OATP1B1/3 is very important, few animal models can be used to study its properties. In this report, we successfully constructed the S knockout (KO) rat model using the CRISPR/Cas9 technology for the first time. The novel rat model showed the absence of OATP1B2 protein expression, with no off-target effects as well as compensatory regulation of other transporters. Further pharmacokinetic study of pitavastatin, a typical substrate of OATP1B2, confirmed the OATP1B2 function was absent. Since bilirubin and bile acids are the substrates of OATP1B2, the contents of total bilirubin, direct bilirubin, indirect bilirubin, and total bile acids in serum are significantly higher in KO rats than the data of wild-type rats. These results are consistent with the symptoms caused by the absence of OATP1B1/3 in Rotor syndrome. Therefore, this rat model is not only a powerful tool for the study of OATP1B2-mediated drug transportation, but also a good disease model to study hyperbilirubinemia-related diseases.

18.
Front Genet ; 11: 637320, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-33679872

RESUMEN

Malignant melanoma represents a sort of neoplasm deriving from melanocytes or cells developing from melanocytes. The balance of energy and energy-associated body composition and body mass index could be altered by exercise, thereby directly affecting the microenvironment of neoplasm. However, few studies have examined the mechanism of genes induced by exercise and the pathways involved in melanoma. This study used three separate datasets to perform comprehensive bioinformatics analysis and then screened the probable genes and pathways in the process of exercise-promoted melanoma. In total, 1,627 differentially expressed genes (DEGs) induced by exercise were recognized. All selected genes were largely enriched in NF-kappa B, Chemokine signaling pathways, and the immune response after gene set enrichment analysis. The protein-protein interaction network was applied to excavate DEGs and identified the most relevant and pivotal genes. The top 6 hub genes (Itgb2, Wdfy4, Itgam, Cybb, Mmp2, and Parp14) were identified, and importantly, 5 hub genes (Itgb2, Wdfy4, Itgam, Cybb, and Parp14) were related to weak disease-free survival and overall survival (OS). In conclusion, our findings demonstrate the prognostic value of exercise-induced genes and uncovered the pathways of these genes in melanoma, implying that these genes might act as prognostic biomarkers for melanoma.

19.
Chem Biodivers ; 16(12): e1900495, 2019 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-31755643

RESUMEN

Fifteen diterpenoids (1-15), including three undescribed ones with ent-atisane skeleton, eupnerias G-I (1-3), were obtained from Euphorbia neriifolia. Compounds 1-3 were established through comprehensive spectroscopic analysis. Compounds 4 and 5 exhibited obvious anti-HIV-1 effect, and their EC50 were 6.6±3.2 and 6.4±2.5 µg mL-1 , respectively. Compound 6 exhibited moderate cytotoxicity on HepG2 and HepG2/Adr cells with IC50 at 13.70 and 15.57 µm, respectively. In addition, compound 15 exhibited significant cytotoxicity on HepG2 cell lines (IC50 =0.01 µm), while it did not show any cytotoxicity against HepG2/Adr cell lines.


Asunto(s)
Fármacos Anti-VIH/química , Diterpenos/química , Euphorbia/química , Fármacos Anti-VIH/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Diterpenos/farmacología , Resistencia a Antineoplásicos/efectos de los fármacos , Euphorbia/metabolismo , VIH-1/efectos de los fármacos , Humanos , Conformación Molecular , Relación Estructura-Actividad
20.
ACS Appl Mater Interfaces ; 11(24): 21668-21674, 2019 Jun 19.
Artículo en Inglés | MEDLINE | ID: mdl-31117433

RESUMEN

Photosensitive precursors are developed for the printing of 2D and 3D conductive structures via blue laser projection printing. With the assistance of a photosensitizer, metal nanoparticles can be efficiently photosynthesized under laser irradiation of low light intensity (45-290 mW cm-2). By projecting well-defined laser patterns on the precursor, corresponding 2D metal structures with the finest line of about 50 µm can be formed on various substrates including flexible polymer thin films, curved substrates, and ground glass. Moreover, complex 3D objects with nanoparticles embedded in the polymeric matrix are constructed via 3D printing combining photoreduction of the metal precursor and photopolymerization of resin. The as-prepared structures exhibit promising conductivities after sintering (in the order of magnitude of 106 S m-1). A possible mechanism of photochemical synthesis of metal nanoparticles upon exposure to blue laser is proposed. The high efficiency and low cost of the technique, the complexity of the structures prepared, and the applicability to various substrates and metals (including silver, gold, and palladium) promise practical applications of this approach in the printed electronics industry.

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