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1.
Artigo em Inglês | MEDLINE | ID: mdl-34637265

RESUMO

Ambipolar photoresponsivity mainly originates from intrinsic or interfacial defects. However, these defects are difficult to control and will prolong the response speed of the photodetector. Here, we demonstrate tunable ambipolar photoresponsivity in a photodetector built from vertical p-WSe2/n-InSe heterostructures with photogating effect, exhibiting ultrahigh photoresponsivity from -1.76 × 104 to 5.48 × 104 A/W. Moreover, the photodetector possesses broadband photodetection (365-965 nm), an ultrahigh specific detectivity (D*) of 5.8 × 1013 Jones, an external quantum efficiency of 1.86 × 107%, and a rapid response time of 20.8 ms. The WSe2/InSe vertical architecture has promising potential in developing high-performance nano-optoelectronics.

2.
Trials ; 22(1): 697, 2021 Oct 13.
Artigo em Inglês | MEDLINE | ID: mdl-34645510

RESUMO

BACKGROUND: Magill forceps are frequently used to complete nasotracheal intubation (NTI). We aimed to identify a tube core that could conveniently facilitate the NTI process without using Magill forceps. METHODS: Sixty patients scheduled for oral and maxillofacial surgeries were enrolled in our study and divided into two groups (30 per group) with no differences with regard to demographic data. In the Magill forceps group (Group M), a wire-reinforced endotracheal catheter was inserted into the trachea using Magill forceps. However, in the tube core group (Group T), a tube core bent to the physiological curve of the nasal cavity and lubricated with aseptic paraffin oil was inserted into the endotracheal catheter and was then withdrawn after the endotracheal catheter was advanced through the glottis under direct vision. RESULTS: All NTIs were completed successfully, and Magill forceps were not used on any patient in Group T. There was a significant difference in total NTI time between the two groups (Group M, 59.7 (5.1) s vs Group T, 52.4 (3.1) s). Mild epistaxis was observed in 6 patients in Group M and 5 patients in Group T (6/30 vs 5/30, respectively). No damage to oral tissue or teeth was observed in either group. CONCLUSIONS: We conclude that using a tube core, consisting of a disposable sterilised stylet, is a convenient choice for NTI. TRIAL REGISTRATION: Patient enrolment was conducted after registration in the Chinese Clinical Trial Registry ( www.Chictr.org.cn , ChiCTR190002 7387). This trial was prospectively registered on 11 November 2019.

3.
ESC Heart Fail ; 2021 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-34612024

RESUMO

Myocardial fibrosis detected by cardiac magnetic resonance (CMR) has been reported in patients with desmin-related myopathy, although its characteristics remain unclear. Here, we describe a case of desmin-related restrictive cardiomyopathy wherein CMR imaging revealed myocardial oedema, ischaemia, and fibrosis in the left ventricle; the different types and processes of myocardial injury were detected by CMR. Middle wall left ventricular enhancement may be a feature of late gadolinium enhancement, and the lateral wall is often involved in cases of myocardial injury. CMR is useful for the early detection of cardiac involvement and the prediction of prognosis in patients diagnosed with desmin-related myopathy.

4.
Langmuir ; 2021 Oct 14.
Artigo em Inglês | MEDLINE | ID: mdl-34648714

RESUMO

Colloidal molecules (CMs), nonspherical clusters of a small number of particles, can be used as building blocks for self-assembly applications. Here, we propose a novel one pot method for CMs synthesis. First, poly(N-isopropylacrylamide-co-acrylic acid) (P(NIPAM-co-AA)) microgels were prepared by soap-free emulsion polymerization as seed particles, then monomer styrene and cross-linking agent divinylbenzene (DVB) were added, which could be polymerized by the remaining free radicals on the seed surface in situ. P(NIPAM-co-AA)-PS colloidal molecules with a series of morphologies such as popcorn-like, CO2-like, NH3-like, CH4-like and so on could be obtained. The effects of satellite colloid viscosity, interfacial tension, and polymer chain mobility on the number of satellite colloid have been investigated, and the formation mechanism of CMs is proposed based on morphology evolution investigation. Compared with the existing CM synthesis techniques, our method enables fabricating CMs from vinyl monomer in a facile and efficient way, and the scientific finding regarding the CMs formation will guide the CMs fabrication toward salable and reliable direction.

5.
J Int Med Res ; 49(9): 3000605211041269, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34525883

RESUMO

Oesophageal liposarcomas are particularly rare, accounting for 1.2-1.5% of all gastrointestinal liposarcomas. Surgical resection is the usual treatment. Endoscopic resection is minimally invasive but still controversial. This current case report describes a rare case of a large oesophageal liposarcoma in a 52-year-old male that presented with 10-year history of dysphagia for dry and solid food that was exacerbated by a recent common cold. Thoracoscopic and laparoscopic oesophagectomy was performed. He did not have any dysphagia or dyspnoea 1 week postoperatively. The excised specimen consisted of a polypoid mass measuring 21.0 cm × 5.1 cm. Histological examination confirmed that it was an oesophageal liposarcoma. At 1-year postoperatively, there was no sign of recurrence. Thoracoscopy and laparoscopy can be used to treat large oesophageal masses. Long-term follow-up is required as oesophageal liposarcomas tend to recur.


Assuntos
Neoplasias Esofágicas , Laparoscopia , Lipossarcoma , Neoplasias Esofágicas/diagnóstico por imagem , Neoplasias Esofágicas/cirurgia , Esofagectomia , Humanos , Lipossarcoma/diagnóstico por imagem , Lipossarcoma/cirurgia , Masculino , Pessoa de Meia-Idade , Recidiva Local de Neoplasia
6.
Anim Biosci ; 2021 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-34474533

RESUMO

Objective: In this study we aimed to evaluate the effect of dietary live yeast supplementation on ruminal pH pattern, fermentation characteristics and associated bacteria in beef cattle. Methods: This work comprised of in vitro and in vivo experiments. In vitro fermentation was conducted by incubating 0, 0.05, 0.075, 0.1, 0.125, and 0.15% active dried yeast (Saccharomyces cerevisiae, ADY) with total mixed ration substrate to determine its dose effect. According to in vitro results, 0.1% ADY inclusion level was assigned in in vivo study for continuously monitoring ruminal fermentation characteristics and microbes. Six ruminally cannulated steers were randomly assigned to 2 treatments (Control and ADY supplementation) as two-period crossover design (30-day). Blood samples were harvested before-feeding and rumen fluid was sampled at 0, 3, 6, 9 and 12 h post-feeding on 30 d. Results: After 24 h in vitro fermentation, pH and gas production were increased at 0.1% ADY where ammonia nitrogen and microbial crude protein also displayed lowest and peak values, respectively. Acetate, butyrate and total volatile fatty acids concentrations heightened with increasing ADY doses and plateaued at high levels, while acetate to propionate ratio was decreased accordingly. In in vivo study, ruminal pH was increased with ADY supplementation that also elevated acetate and propionate. Conversely, ADY reduced lactate level by dampening Streptococcus bovis and inducing greater Selenomonas ruminantium and Megasphaera elsdenii populations involved in lactate utilization. The serum urea nitrogen decreased, whereas glucose, albumin and total protein concentrations were increased with ADY supplementation. Conclusion: The results demonstrated dietary ADY improved ruminal fermentation dose-dependently. The ruminal lactate reduction through modification of lactate metabolic bacteria could be an important reason for rumen pH stabilization induced by ADY. ADY supplementation offered a complementary probiotics strategy in improving gluconeogenesis and nitrogen metabolism of beef cattle, potentially resulted from optimized rumen pH and fermentation.

7.
Zhongguo Zhong Yao Za Zhi ; 46(12): 2942-2948, 2021 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-34467684

RESUMO

To systematically search and sort out the clinical randomized controlled trial(RCT) on the prevention and treatment of acute cerebral infarction with traditional Chinese medicine(TCM) by using the method of evidence map, and to understand the evidence distribution of related studies. CNKI, Wanfang, VIP, CBM, PubMed, EMbase, Cochrane Library and Web of Science were retrieved from January 2016 to September 2020, and literatures related to the prevention and treatment of acute cerebral infarction with traditional Chinese medicine were included. Text description combined with table and bubble chart were used to analyze the distribution characteristics of evidence. A total of 1 102 clinical articles in recent five years were retrieved. The annual trend of clinical study publication, study size, TCM therapy category and main scheme, and study literature quality were analyzed. We find that TCM treatment of acute cerebral infarction has become a hot topic of clinical research, the number of literature showed a trend of increased year by year, various means of intervention of TCM in the treatment of the advantages of increasingly highlight. Follow-up clinical research should highlight the characteristics of TCM: in the analysis of outcome indicators; increase the neuropsychological patients after stroke and cognitive ability, and the theory of combined treatment of TCM disease when thoughts; At the same time, the quality of clinical research needs to be improved. At present, there is still a lack of unified standards for the production of evidence map. This study is the first to explore the application of evidence map to summarize and display the clinical research status of TCM treatment of acute cerebral infarction, and combine it with the setting of priority areas of TCM clinical research, so as to provide a reference basis for determining the priority topic selection of TCM treatment optimization research.


Assuntos
Isquemia Encefálica , Medicamentos de Ervas Chinesas , Acidente Vascular Cerebral , Infarto Cerebral/tratamento farmacológico , Medicamentos de Ervas Chinesas/uso terapêutico , Humanos , Medicina Tradicional Chinesa , Acidente Vascular Cerebral/tratamento farmacológico
8.
Artigo em Inglês | MEDLINE | ID: mdl-34491473

RESUMO

PURPOSE: Abdominal aortic aneurysm (AAA) rupture is one of the most common causes of mortality in cardiovascular diseases, but currently there is no approved drug for AAA treatment or prevention in the clinic. Naringenin (NGN) has been reported to have anti-AAA effects. However, water solubility and in vivo absorption of NGN are not satisfactory, which leads to its low bioavailability, thus affecting its pharmacological effects. In this project, the improving effects of isonicotinamide (INT) co-crystal and hydroxy propyl methyl cellulose (HPMC) or polyvinyl pyrrolidone (PVP) on the solubility, in vivo absorption, and anti-AAA effects of NGN were evaluated. METHODS: In the current study, co-crystals of naringenin-isonicotinamide (NGN-INT) were prepared, and effects of PVP or HPMC on precipitation rate, supersaturation, and bioavailability of NGN were explored. In addition, with or without HPMC supply, the effects of NGN-INT co-crystal on anti-AAA efficacy of NGN were investigated on an elastase-induced AAA mouse model, and the results were compared with the efficacy of the NGN crude drug. RESULTS: Our results demonstrate that NGN-INT formulation, compared to the NGN crude drug, enhanced the dissolution rate of NGN and significantly increased Cmax and AUC(0-∞) of NGN by 18 times and 1.97 times, respectively. Addition of PVP or HPMC in NGN-INT co-crystal further increased bioavailability of NGN in NGN-INT. The in vivo pharmacodynamic study showed that NGN-INT with HPMC significantly improved the inhibitory effects of NGN against AAA. CONCLUSION: NGN-INT significantly improved the absorption and aortic protective effects of NGN. The supersaturation-prolonging effect of HPMC further enhanced bioavailability and anti-AAA effects of NGN-INT.

9.
Sci Rep ; 11(1): 17797, 2021 Sep 07.
Artigo em Inglês | MEDLINE | ID: mdl-34493740

RESUMO

Hepatocellular carcinoma (HCC) is one of the most common malignant tumors and has extremely high morbidity and mortality. Although many existing studies have focused on the identification of biomarkers, little information has been uncovered regarding the PBMC RNA profile of HCC. We attempted to create a profile throughout using expression of peripheral blood mononuclear cell (PBMC) RNA using RNA-seq technology and compared the transcriptome between HCC patients and healthy controls. Seventeen patients and 17 matched healthy controls were included in this study, and PBMC RNA was sequenced from all samples. Sequencing data were analyzed using bioinformatics tools, and quantitative reverse transcription PCR (qRT-PCR) was used for selected validation of DEGs. A total of 1,578 dysregulated genes were found in the PBMC samples, including 1,334 upregulated genes and 244 downregulated genes. GO enrichment and KEGG studies revealed that HCC is closely linked to differentially expressed genes (DEGs) implicated in the immune response. Expression of 6 selected genes (SELENBP1, SLC4A1, SLC26A8, HSPA8P4, CALM1, and RPL7p24) was confirmed by qRT-PCR, and higher sensitivity and specificity were obtained by ROC analysis of the 6 genes. CALM1 was found to gradually decrease as tumors enlarged. Nearly the opposite expression modes were obtained when compared to tumor sequencing data. Immune cell populations exhibited significant differences between HCC and controls. These findings suggest a potential biomarker for the diagnosis of HCC. This study provides new perspectives for liver cancer development and possible future successful clinical diagnosis.

10.
Proc Natl Acad Sci U S A ; 118(37)2021 Sep 14.
Artigo em Inglês | MEDLINE | ID: mdl-34504019

RESUMO

Endothelial cell (EC) sensing of wall fluid shear stress (FSS) from blood flow governs vessel remodeling to maintain FSS at a specific magnitude or set point in healthy vessels. Low FSS triggers inward remodeling to restore normal FSS but the regulatory mechanisms are unknown. In this paper, we describe the signaling network that governs inward artery remodeling. FSS induces Smad2/3 phosphorylation through the type I transforming growth factor (TGF)-ß family receptor Alk5 and the transmembrane protein Neuropilin-1, which together increase sensitivity to circulating bone morphogenetic protein (BMP)-9. Smad2/3 nuclear translocation and target gene expression but not phosphorylation are maximal at low FSS and suppressed at physiological high shear. Reducing flow by carotid ligation in rodents increases Smad2/3 nuclear localization, while the resultant inward remodeling is blocked by the EC-specific deletion of Alk5. The flow-activated MEKK3/Klf2 pathway mediates the suppression of Smad2/3 nuclear translocation at high FSS, mainly through the cyclin-dependent kinase (CDK)-2-dependent phosphosphorylation of the Smad linker region. Thus, low FSS activates Smad2/3, while higher FSS blocks nuclear translocation to induce inward artery remodeling, specifically at low FSS. These results are likely relevant to inward remodeling in atherosclerotic vessels, in which Smad2/3 is activated through TGF-ß signaling.

11.
Cell Death Discov ; 7(1): 262, 2021 Sep 24.
Artigo em Inglês | MEDLINE | ID: mdl-34561425

RESUMO

LncRNAs play an important role in tumorigenesis and progression; however, the function and mechanisms of lncRNAs in esophageal cancer (EC) remain largely unclear. In this study, we screened the differentially expressed lncRNAs in EC by using RNA-seq and one of the most upregulated lncRNAs, lncRNA RP11-465B22.8, was further characterized. LncRNA RP11-465B22.8 was upregulated in EC tissues and high lncRNA RP11-465B22.8 expression was associated with poor survival of EC patients. Ectopic expression of lncRNA RP11-465B22.8 enhanced the proliferation, migration, and invasion of EC cells, whereas knockdown of lncRNA RP11-465B22.8 led to the opposite effects. Mechanistically, lncRNA RP11-465B22.8 sponged miR-765 to increase the expression of KLK4. Moreover, LncRNA RP11-465B22.8 could be delivered from EC cells to macrophages via exosomes and subsequently induced M2 macrophage-induced cell migration and invasion. Our findings revealed a novel lncRNA RP11-465B22.8/miR-765/KLK4 pathway in EC and indicated that lncRNA RP11-465B22.8 might be a potential target for EC therapy.

12.
Org Lett ; 23(19): 7666-7671, 2021 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-34543569

RESUMO

An unprecedented Sc(OTf)3-catalyzed C2-selective cyanation/defluorination cascade of perfluoroalkylated 3-indolylmethanols with TMSCN is described, which provides a novel and practical strategy for the synthesis of structurally diverse 3-(2-cyano)-indolyl substituted gem-difluoroalkenes and ß-fluoro-ß-perfluoroalkylalkenes. The reaction features excellent regio- and stereoselectivity and broad substrate scope. Notably, the obtained gem-difluoroalkenes and ß-fluoro-ß-perfluoroalkylalkenes could be easily transformed into 3-fluoro(perfluoroalkyl)-ß-carbolines with excellent efficiency simply by treating them with Grignard reagents or DIBAL-H under mild reaction conditions.

13.
Artigo em Inglês | MEDLINE | ID: mdl-34574441

RESUMO

Acupuncture can improve explosive force production and affect joint stiffness by affecting muscle activation levels. This study aims to explore the effects of true acupuncture (TA) compared with sham acupuncture (SA) on the explosive force production and stiffness of the knee joint in healthy male subjects. Twenty subjects were randomly divided into the TA group (n = 10) and SA group (n = 10) to complete isokinetic movement of the right knee joint at a speed of 240°/s before and after acupuncture. Futu (ST32), Liangqiu (ST34), Zusanli (ST36), Xuehai (SP10), and Chengshan (BL57) were selected for acupuncture. The intervention of SA is that needles with a blunt tip were pushed against the skin, giving an illusion of insertion. The results showed that acupuncture and the intervention time had a significant interaction effect on knee joint explosive force and joint stiffness (p < 0.05). The average maximum (max) torque, average work, average power, average peak power and total work of the TA group increased significantly after acupuncture (p < 0.05), while the SA group did not (p > 0.05). Therefore, true acupuncture can immediately improve the explosive force and joint stiffness of the male knee joint by inducing post-activation potentiation (PAP) and/or De-Qi.

14.
J Phys Chem Lett ; 12(39): 9525-9530, 2021 Oct 07.
Artigo em Inglês | MEDLINE | ID: mdl-34559971

RESUMO

Triplet-triplet annihilation (TTA) upconversion has shown promising potentials in the augmentation of solar energy conversion. However, challenging issues exist in improving TTA upconversion efficiencies in solid-states, one of which is the back energy transfer from upconverted singlet annihilators to sensitizers, resulting in decreasing upconversion emission. Here we present a light-harvesting molecular wire consisting of dendrons with 9,10-diphenylanthracene derivatives (DPAEH) at the periphery and p-phenylene ethynylene oligomers (PPE) as the wire core. The peripheral DPAEH antenna funnels singlet excitonic energy to the wire on a 12 ps time scale. Incorporating the molecular wire into the TTA upconversion solid consisting of the DPAEH annihilator and the porphyrin sensitizer evidently improves the upconversion quantum yield from 1.5% to 2.7% upon 532 nm excitation by suppressing the back energy transfer from the singlet annihilator to the sensitizer. This finding offers a potential route to use a singlet energy light-harvesting architecture for enhancing TTA upconversion.

15.
Tissue Cell ; 73: 101616, 2021 Aug 12.
Artigo em Inglês | MEDLINE | ID: mdl-34481230

RESUMO

In early pregnancy, hypoxia is a typical extrinsic factor that regulates EVT functions including proliferation, migration and invasion which are essential for a successful pregnancy. Human differentiated embryonic chondrocyte-expressed gene 1 (DEC1), a hypoxia-regulated gene, has been reported to be overexpressed in several types of cancers. Given that the placenta and the cancer share several similarities with respect to their capacity to proliferate and invade adjacent tissues, we focused on the role of DEC1 on trophoblast function in a physiologically hypoxic environment, which may be associated with unexplained recurrent spontaneous abortion (URSA).In our study, we measured the expression of HIF-1α and DEC1 in first-trimester villi through real-time-PCR (RT-PCR) and immunohistochemical analysis. in vitro, DEC1 expression was downregulated in trophoblast cells via DEC1-specific shRNA plasmid transfection. The expression of DEC1 and HIF-1α was detected via western blotting and RT-PCR analysis. The proliferation and migration of HTR-8/SVneo cells were assayed using CCK-8 and Transwell migration assays, respectively.Our results indicated that the expression of DEC1 was significantly reduced in villi of URSA compared to that in normal pregnant women. in vitro, hypoxia induced the expression of HIF-1ɑ and DEC1 and upregulated proliferation and migration of the HTR-8/SVneo cells. Knockdown of DEC1 inhibited proliferation and migration of HTR-8/SVneo cells exposure to hypoxia. Furthermore, inhibition of HIF1α expression resulted in a significant decrease in DEC1. These findings illustrate that hypoxia-induced DEC1 expression promotes trophoblast cell proliferation and migration through the HIF1α signaling pathway, which plays an important role during placentation.

16.
Zhonghua Wei Zhong Bing Ji Jiu Yi Xue ; 33(8): 999-1002, 2021 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-34590571

RESUMO

OBJECTIVE: To investigate the clinical values of the differences between hematocrit and serum albumin (HCT-ALB) for evaluating the severity of patients with acute paraquat (PQ) poisoning. METHODS: Patients with acute PQ poisoning admitted to the Second People's Hospital of Yunnan Province from January 2018 to December 2019 were enrolled, and healthy voluteers during the same period were selected as the control. The general information, poisoning dose and poisoning time of patients, as well as the HCT and serum ALB levels before blood product infusion, intravenous infusion, or hemopurification at admission were collected, and the HCT-ALB was calculated. According to the results of rapid semiquantitative test of PQ in urine at admission, the patients were divided into PQ low concentration group (0-10 mg/L) and PQ high concentration group (30-100 mg/L). The relationship between poisoning time, poisoning dose, HCT-ALB and the degree of acute PQ poisoning were analyzed, and Spearman method was used to analyze the grade correlation. RESULTS: A total of 295 patients with acute PQ poisoning were enrolled, including 118 cases in PQ low concentration group and 177 cases in PQ high concentration group, and another 200 healthy persons matched with PQ patients in gender and age (healthy control group). The poisoning time of PQ low concentration group was significantly longer than that of PQ high concentration group [hours: 11.0 (6.0, 60.0) vs. 8.0 (5.0, 20.5), P < 0.01], but the poisoning dose was significantly lower than that of PQ high concentration group [mL: 10.0 (5.8, 15.0) vs. 40.0 (20.0, 80.0), P < 0.01]. The HCT and HCT-ALB in PQ low and high concentration groups were significantly higher than those of the healthy control group [HCT: (43.14±4.41)%, (43.54±5.40)% vs. (42.14±2.15)%, HCT-ALB: 3.59±6.26, 5.94±7.80 vs. -7.26±3.55, all P < 0.01], but ALB was significantly lower than that of the healthy control group (g/L: 39.54±5.74, 37.60±7.15 vs. 49.40±3.41, both P < 0.01). With the increase of urine PQ concentration, the HCT and HCT-ALB further increased, and ALB further decreased. There were significant differences between PQ high concentration group and PQ low concentration group [HCT: (43.54±5.40)% vs. (43.14±4.41)%, HCT-ALB: 5.94±7.80 vs. 3.59±6.26, ALB (g/L): 37.60±7.15 vs. 39.54±5.74, all P < 0.05]. The poisoning severity of patients with acute PQ poisoning were negatively correlated with poisoning time and ALB (r values were -0.195 and -0.695, respectively, both P < 0.01), there were positively correlated with poisoning dose, HCT, and HCT-ALB (r values were 0.650, 0.256, 0.737, respectively, all P < 0.01), and the correlation between HCT-ALB and poisoning severity was the strongest. CONCLUSIONS: The HCT-ALB can reflect the poisoning severity of patients with acute PQ poisoning and indirectly reveal the pathological changes of microvessels in patients with acute PQ poisoning.


Assuntos
Paraquat , Envenenamento , China , Hematócrito , Humanos , Prognóstico , Albumina Sérica
17.
Artigo em Inglês | MEDLINE | ID: mdl-34500403

RESUMO

Lead compound is an important concept for modern drug discovery. In this study, a new concept of lead chemome and an efficient strategy to discover lead chemome were proposed. Compared with the concept of lead compound, lead chemome can provide not only the starting point for drug development, but also the direction for structure optimization. Two traditional Chinese medicines of Mahonia bealei and Mahonia fortunei were used as examples to illustrate the strategy. Based on natural chromatogram-effect correlation (NCEC), berberine, palmatine and jatrorrhizine were discovered as acetylcholinesterase (AchE) inhibitors. Taking the three compounds as template molecules, a lead chemome consisting of 10 structurally related natural compounds were generated through natural structure-effect correlation (NSEC). In the lead chemome, the IC50 values of jatrorrhizine, berberine, coptisine, palmatine and epiberberine are at nanomolar level, which are comparable to a widely used drug of galantamine. Pharmacophore modeling shows that the positive ionizable group and aromatic rings are important substructures for AchE inhibition. Molecular docking further shows that pi-cation interaction and pi-pi stacking are critical for compounds to maintain nanomolar IC50 values. The structure-activity information is helpful for drug design and structure optimization. This work also expanded the traditional understanding of "stem is the medicinal part of Mahonia bealei and Mahonia fortunei". Actually, all parts except the leaf of Mahonia bealei exhibited potent AchE-inhibitory activity. This study provides not only a strategy to discover lead chemome for modern drug development, but also a reference for the application of different parts of medicinal plants.

18.
Int J Pharm ; 609: 121138, 2021 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-34592395

RESUMO

Artesunate (ARS) is the only artemisinin-based intravenous drug approved for treatment of malaria in the clinic. ARS is rapidly metabolized in vivo to short lived (∼30-45 min) but fast acting, dihydroartemisinin (DHA). The short half-life of DHA necessitates multiple dose administration to circumvent the risk of recrudescence and development of artemisinin resistance. In this work, we report a stable, safe and potent alternative artemisinin-based injectable nanocomplex consisting of dimeric artesunate-choline conjugate (dACC) micelles coated with hyaluronic acid (HA). Firstly, dACC was synthesized by one-step esterification of two artesunate molecules with 3-(dimethylamino)-1,2-propanediol followed by quaternization. After that, dACC was self-assembled into cationic nanomicelles and further coated with anionic small molecular weight HA. The HA-coated dACC nanocomplex (dACC/HA nanocomplex) has a narrow size distribution of about 30 nm. Hemolytic toxicity and cytotoxicity studies revealed a favorable bio-safety profile. Finally, in vitro and in vivo studies showed the dACC/HA nanocomplex possess superior safety and antimalarial efficacy compared to ARS. Taken together, the dACC/HA nanocomplex is a promising injectable alternative to the traditional clinically used artesunate.

19.
J Environ Manage ; 298: 113487, 2021 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-34411801

RESUMO

Phosphate species can complex with nuclides and heavy metals from aqueous solutions strongly. The introduction of phosphate groups onto the surface of biochar sorbents (mostly <1.0 at.% of P) is highly desired. In this study, phosphate modified hydrochars (HTBs) were prepared through the hydrothermal carbonization of bamboo sawdust with various duration (2, 12, 24 h) in the presence of phytic acid (0-70 wt%). The results showed that the addition of PA with a low concentration of 10 wt% carbonized at 2 h generated hydrogen protons to etch the pristine sawdust, inducing the granulation of surfaces and a 5.5-fold enhancement of surface area. While HTBs carbonized with increasing PA concentrations (30-70 wt%) and longer duration (12 and 24 h) presented more carbonaceous particles with rising sizes from <100 nm to 2.5 µm, which should be due to the cross-linkage of dehydrated phosphate-containing organic carbon components to the matrix, enabling the resultful surface modification (maximum of 2.1 wt% of P). The uptake of U(VI), Pb(II) and Cd(II) on HTBs was investigated given various geochemical conditions including contact time, pH, ionic strength, humic acid and temperature. HTBs could capture U(VI), Pb(II) and Cd(II) efficiently from the ideal and simulated wastewaters, and be reused well after six recycles. This work opened a new strategy for the potential of phosphate-hydrochars in the aqueous remediation.


Assuntos
Cádmio , Ácido Fítico , Adsorção , Carvão Vegetal , Chumbo , Fosfatos
20.
Zhongguo Zhong Yao Za Zhi ; 46(14): 3722-3731, 2021 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-34402297

RESUMO

This study aims to explore the efficacy of Chinese medicine injections( CMIs) for promoting blood circulation and removing blood stasis for acute cerebral infarction from the perspectives of clinical medication and mechanism of action based on two complex network analysis methods. Firstly,the current 13 kinds of CMIs for acute cerebral infarction were obtained from 2019 List of medicines for national basic medical insurance,industrial injury insurance and maternity insurance with the method of network Meta-analysis. Secondly,with the use of network pharmacology,the mechanisms of top 2 CMIs with the highest therapeutic effect for acute cerebral infarction were explored from two levels including core target and network function enrichment. The result of network Meta-analysis showed Mailuoning Injection was superior to Danhong Injection in terms of total effectiveness rate for neurological deficit score and NIHSS score. The network pharmacology results showed that Mailuoning Injection had more core targets,interaction networks,enriched biological functions and more signaling pathways than Danhong Injection for cerebral infarction. Both two CMIs can play a role in treating cerebral infarction through core targets such as TP53 and NOS3,biological processes such as fibrinolysis,nitric oxide biosynthesis,nitric oxide-mediated signal transduction,negative regulation of apoptosis in endothelial cells and apoptosis process,as well as the signaling pathways such as PI3 K-Akt signaling pathway,HIF-1 signaling pathway and cell apoptosis signaling pathways. The results of pharmacological studies explained their differences in clinical efficacy to a certain extent. A research strategy based on curative effect should be advocated in efficacy evaluation of traditional Chinese medicine,where comparative research on clinical efficacy can be conducted firstly,and then mechanism research based on outstanding effective drugs to better provide references and basis for selection of similar competitive drugs for one disease in the clinical practice.


Assuntos
Medicamentos de Ervas Chinesas , Medicina Tradicional Chinesa , Infarto Cerebral/tratamento farmacológico , Medicamentos de Ervas Chinesas/uso terapêutico , Células Endoteliais , Feminino , Humanos , Injeções , Gravidez , Transdução de Sinais
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