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1.
Int J Comput Assist Radiol Surg ; 18(5): 855-864, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-36602643

RESUMO

PURPOSE: Scalpels are typical tools used for cutting in surgery, and the surgical tray is one of the locations where the scalpel is present during surgery. However, there is no known method for the classification and segmentation of multiple types of scalpels. This paper presents a dataset of multiple types of scalpels and a classification and segmentation method that can be applied as a first step for validating segmentation of scalpels and further applications can include identifying scalpels from other tools in different clinical scenarios. METHODS: The proposed scalpel dataset contains 6400 images with labeled information of 10 types of scalpels, and a classification and segmentation model for multiple types of scalpels is obtained by training the dataset based on Mask R-CNN. The article concludes with an analysis and evaluation of the network performance, verifying the feasibility of the work. RESULTS: A multi-type scalpel dataset was established, and the classification and segmentation models of multi-type scalpel were obtained by training the Mask R-CNN. The average accuracy and average recall reached 94.19% and 96.61%, respectively, in the classification task and 93.30% and 95.14%, respectively, in the segmentation task. CONCLUSION: The first scalpel dataset is created covering multiple types of scalpels. And the classification and segmentation of multiple types of scalpels are realized for the first time. This study achieves the classification and segmentation of scalpels in a surgical tray scene, providing a potential solution for scalpel recognition, localization and tracking.


Assuntos
Aprendizado Profundo , Humanos , Processamento de Imagem Assistida por Computador/métodos
2.
Bioorg Chem ; 130: 106262, 2023 01.
Artigo em Inglês | MEDLINE | ID: mdl-36371821

RESUMO

Nine new flavonoids dimers, psocorylins R-Z (1-9), were isolated from the fruits of Psoralea corylifolia L. (Psoraleae Fructus), a traditional Chinese medicine. The structures of these compounds were elucidated via multiple spectroscopic techniques and X-ray diffraction. Psocorylins R (1) and S (2) were rare cyclobutane-containing chalcone dimers, and psocorylins T-Z (3-9) were established by CC or COC bond of two flavonoid monomers. The structural-types, flavonoids dimers, were isolated from the plant for the first time, enriching the chemical diversity. The cytotoxicity assay suggested that compounds 1, 2, 4, 5, 6 and 8 exhibited cytotoxic activities against MCF-7 cells. Furthermore, compounds 1 and 8 significantly increased intracellular ROS levels, decreased MMP and induced apoptosis of MCF-7 cells. They markedly upregulated the expression of Bax and cleaved caspase-3, and suppressed Bcl-2 and caspase-3 levels, indicating their mechanism of Bcl-2/Bax/Cleaved caspase-3 pathway. Hence, our findings not only promoted the chemical investigation of Psoraleae Fructus, but also provided potential bioactive natural products for anti-cancer.


Assuntos
Flavonoides , Psoralea , Humanos , Proteína X Associada a bcl-2 , Caspase 3/efeitos dos fármacos , Caspase 3/metabolismo , Fabaceae/química , Flavonoides/química , Flavonoides/farmacologia , Frutas/química , Células MCF-7/efeitos dos fármacos , Células MCF-7/metabolismo , Polímeros , Proteínas Proto-Oncogênicas c-bcl-2/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Psoralea/química
3.
Comput Methods Biomech Biomed Engin ; 26(13): 1523-1531, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36382359

RESUMO

Saliva blood mixed liquid (SBML) appears in oral surgery, such as scaling and root planning, and it affects surgical vision and causes discomfort to the patient. However, removing SBML, i.e. frequent aspiration of the mixed liquid, is a routine task involving heavy workload and interruption of oral surgery. Therefore, it is valuable to alternate the manual mode by autonomous robotic technique. The robotic system is designed consisting of an RGB-D camera, a manipulator, a disposable oral aspirator. An algorithm is developed for detection of SBML. Path planning method is also addressed for the distal end of the aspirator. A workflow for removing SBML is presented. 95% of the area of the SBML in the oral cavity was removed after liquid aspiration among a group of ten SBML aspiration experiments. This study provides the first result of the autonomous aspirating robot (AAR) for removing SBML in oral surgery, demonstrating that SBML can be removed by the autonomous robot, freeing stomatology surgeon from tedious work.


Assuntos
Procedimentos Cirúrgicos Bucais , Robótica , Humanos , Saliva
4.
Curr Pharm Des ; 29(43): 3467-3477, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38163971

RESUMO

BACKGROUND: Growth differentiation factor-10 (GDF-10), a member of the TGF-ß superfamily, plays a crucial role in cell proliferation and differentiation. In some tumors, GDF-10 can act as a tumor suppressor to inhibit tumor progression, but its role in posterior squamous cell carcinoma has not been reported yet. METHODS: The aim of this study was to investigate the effect of GDF-10 on the epithelial-mesenchymal transition of laryngeal squamous cell carcinoma, and to provide new ideas for future targets in the treatment of laryngeal squamous carcinoma. RESULTS: The effect of GDF-10 on tumor growth was detected; bioinformatics analysis was performed to predict the downstream targets of GDF-10, and RT-PCR and western blot were performed to detect the expression levels of target genes and proteins, respectively. CONCLUSION: Our findings support that GDF-10 can inhibit the proliferation, migration, and invasion, and promote apoptosis of laryngeal carcinoma AMC-HN-8 cells. GDF-10 inhibits the EMT of laryngeal carcinoma through LRP4 and thus inhibits the progression of laryngeal carcinoma.


Assuntos
Carcinoma de Células Escamosas , Neoplasias Laríngeas , Humanos , Neoplasias Laríngeas/tratamento farmacológico , Neoplasias Laríngeas/genética , Neoplasias Laríngeas/metabolismo , Fator 10 de Diferenciação de Crescimento/genética , Fator 10 de Diferenciação de Crescimento/metabolismo , Carcinoma de Células Escamosas/tratamento farmacológico , Carcinoma de Células Escamosas/genética , Fator de Crescimento Transformador beta/metabolismo , Transição Epitelial-Mesenquimal/genética , Linhagem Celular Tumoral , Movimento Celular , Proliferação de Células , Regulação Neoplásica da Expressão Gênica
5.
Medicine (Baltimore) ; 101(46): e31216, 2022 Nov 18.
Artigo em Inglês | MEDLINE | ID: mdl-36401416

RESUMO

BACKGROUND: Deep venipuncture catheterization is widely used in clinical anesthesia. However, it is worth thinking about how to improve the rate of successful catheter insertion, and relieve patients' discomfort. This paper aimed to compare the clinical advantages between trocar and steel needle. METHODS: Total 503 adult patients were recruited and randomly assigned. The control group was punctured with steel needle, and the experimental group was punctured with trocar needle. Clinical and followed-up information was recorded. Pearson's chi-squared and spearman test were performed to analyze the correlation between intervention and relative parameters. Univariate logistic regression was performed to verify the odds ratio of trocar needle compared with steel needle. RESULTS: Pearson's chi-square test and Spearman's correlation test showed a significant correlation between puncture success, puncture comfort, successful catheter insertion, puncture time, thrombosis, catheter fever, bleeding, infection and interventions (P < .05). Univariate logistic regression showed that there existed better puncture comfort (odds ratio [OR] = 6.548, 95% confidence interval [CI]: 4.320-9.925, P < .001), higher successful catheter insertion (OR = 6.060, 95% CI: 3.278-11.204, P < .001), shorter puncture time (OR = 0.147, 95% CI: 0.093-0.233, P < .001), lesser thrombosis (OR = 0.194, 95% CI: 0.121-0.312, P < .001), lesser catheter fever (OR = 0.263, 95% CI: 0.158-0.438, P < .001), lesser bleeding (OR = 0.082, 95% CI: 0.045-0.150, P < .001) and lesser infection (OR = 0.340, 95% CI: 0.202-0.571, P < .001) in trocar group compared with steel needle group. CONCLUSION: Trocar application in deep venipuncture catheterization can improve successful catheter insertion, relieve pain and discomfort of patients, reduce incidence of complications, and provide better security for patients.


Assuntos
Cateterismo Venoso Central , Trombose , Humanos , Adulto , Flebotomia/efeitos adversos , Cateterismo Venoso Central/efeitos adversos , Aço , Hemorragia/etiologia , Trombose/etiologia , Instrumentos Cirúrgicos
6.
Chem Biodivers ; 19(7): e202200218, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35689671

RESUMO

Three new alkamides, achilleamide B-D (1-3) along with five known alkamides (4-8) were isolated from the aerial parts of Achillea alpina L. Structures were elucidated by spectroscopic analysis. Modified Mosher's method and electronic circular dichroism (ECD) calculations were introduced for the absolute configuration of 3. The neuroprotective effects of all the compounds were evaluated by 6-hydroxydopamine (6-OHDA)-induced cell death in human neuroblastoma SH-SY5Y cells, with concentration for 50 % of maximal effect (EC50 ) values of 3.16-24.75 µM, and the structure-activity relationship was conducted.


Assuntos
Achillea , Neuroblastoma , Fármacos Neuroprotetores , Achillea/química , Humanos , Estrutura Molecular , Fármacos Neuroprotetores/química , Componentes Aéreos da Planta/química
7.
Front Pharmacol ; 12: 771976, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34970143

RESUMO

Bile acid (BA) metabolism is an attractive therapeutic target in nonalcoholic fatty liver disease (NAFLD). We aimed to investigate the effect of ilexsaponin A1 (IsA), a major bioactive ingredient of Ilex, on high-fat diet (HFD)-induced NAFLD in mice with a focus on BA homeostasis. Male C57BL/6J mice were fed an HFD to induce NAFLD and were treated with IsA (120 mg/kg) for 8 weeks. The results showed that administration of IsA significantly decreased serum total cholesterol (TC), attenuated liver steatosis, and decreased total hepatic BA levels in HFD-induced NAFLD mice. IsA-treated mice showed increased BA synthesis in the alternative pathway by upregulating the gene expression levels of sterol 27-hydroxylase (CYP27A1) and cholesterol 7b-hydroxylase (CYP7B1). IsA treatment accelerated efflux and decreased uptake of BA in liver by increasing hepatic farnesoid X receptor (FXR) and bile salt export pump (BSEP) expression, and reducing Na+-taurocholic acid cotransporting polypeptide (NTCP) expression. Alterations in the gut microbiota and increased bile salt hydrolase (BSH) activity might be related to enhanced fecal BA excretion in IsA-treated mice. This study demonstrates that consumption of IsA may prevent HFD-induced NAFLD and exert cholesterol-lowering effects, possibly by regulating the gut microbiota and BA metabolism.

8.
Med Sci Monit ; 27: e929824, 2021 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-34153024

RESUMO

BACKGROUND A cardioprotective effect of salvianolic acid A (SalA) has been described, but it is unknown whether SalA can protect cardiomyocytes against doxorubicin (Dox)-induced cardiotoxicity. This study aimed to investigate whether SalA could inhibit Dox-induced apoptosis in H9C2 cells and to uncover the potential mechanism. MATERIAL AND METHODS H9C2 cardiomyocytes exposed to Dox were treated with SalA or not, and then cell viability, apoptosis, and the expression of nuclear factor-kappaB (NF-kappaB) signaling were detected by Cell Counting Kit-8, TUNEL staining, and western blot assays, respectively. Nuclear factor kappa B subunit 1 (NFKB1) was overexpressed in H9C2 cells, and then alterations in cell viability and apoptosis in H9C2 cells co-treated with Dox and SalA were investigated. RESULTS SalA (2, 10, and 50 µM) had no effect on H9C2 cell viability, while Dox reduced cell viability in a concentration-dependent manner. In addition, SalA rescued Dox-decreased cell viability. Dox also triggered apoptosis as evidenced by an increased ratio of TUNEL-positive cells, enhanced expression of pro-apoptotic proteins, and reduced expression of anti-apoptotic protein BCL-2, which were all partially blocked by SalA co-treatment. The proteins involved in NF-kappaB signaling including IkappaBalpha, IKKalpha, IKKß, and p65 were activated by Dox but inactivated by SalA co-treatment. Moreover, Dox increased NFKB1 mRNA and nuclear expression, which was blocked by SalA. NFKB1 could bind to plasmacytoma variant translocation 1 (PVT1) and upregulate PVT1 expression. Mechanistically, the overexpression of NFKB1 blocked the inhibitory effect of SalA on Dox-induced cell viability impairment and apoptosis. CONCLUSIONS We demonstrated that SalA may exert a protective effect against Dox-induced H9C2 injury and apoptosis via inhibition of NFKB1 expression, thereby downregulating lncRNA PVT1.


Assuntos
Ácidos Cafeicos/farmacologia , Cardiotoxicidade/prevenção & controle , Lactatos/farmacologia , Miócitos Cardíacos/efeitos dos fármacos , NF-kappa B/efeitos dos fármacos , Plasmocitoma/metabolismo , RNA Longo não Codificante/efeitos dos fármacos , Animais , Células Cultivadas , Modelos Animais de Doenças , Regulação para Baixo/efeitos dos fármacos , Doxorrubicina/administração & dosagem , Ratos , Transdução de Sinais/efeitos dos fármacos
9.
Zhongguo Zhong Yao Za Zhi ; 46(8): 2094-2103, 2021 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-33982525

RESUMO

The absorption is the key to the resulted efficacy of orally administered drugs and the small intestine is the main site to absorb the orally administered drug. In this paper, internationally recognized human colon adenocarcinoma cell line(Caco-2) monola-yer model which can simulate small intestinal epithelial cell was used to comparatively study the absorption and transportation diffe-rences of total coumarins and main individual coumarin in Angelica dahurica 'Yubaizhi' by separately using 6-and 12-well plates. It was found that apparent permeability coefficient(P_(app)) values of oxypeucedanin hydrate, byakangelicin and phellopterin were at the quantitative degree of 1 × 10~(-5) cm·s~(-1) when the individual administration was conducted independently, indicating that they were well-absorbed compounds. P_(app) ratio of their bi-directional transportation was close to 1, indicating that they can be absorbed across Caco-2 monolayer by passive diffusion mechanism without carrier mediation during the transportation. The similar trend of transportation was also observed for imperatorin, isoimperatorin and bergapten. The P_(app) values of oxypeucedanin hydrate, byakangelicin and bergapten were at quantitative degree of 1 × 10~(-5) cm·s~(-1) when the administration of total coumarins in Angelica dahurica 'Yubaizhi' was conducted, indicating that they were well-absorbed compounds. The results were consistent with those of independent administration of individual coumarins. Whereas, the P_(app) values of imperatorin, phellopterin and isoimperatorin in the total coumarins decreased, indicating that the interaction between compounds may exist although the P_(app) value ratio of bi-directional transportation was between 0.5 and 1.5. The results laid the foundation for intestinal absorption study of Angelica dahurica 'Yubaizhi' coumarins in compound Chinese medicine.


Assuntos
Angelica , Medicamentos de Ervas Chinesas , Células CACO-2 , Cumarínicos , Humanos , Absorção Intestinal , Raízes de Plantas
10.
Zool Res ; 42(1): 14-27, 2021 01 18.
Artigo em Inglês | MEDLINE | ID: mdl-33420764

RESUMO

Double sex and mab-3-related transcription factor 1 (Dmrt1), which is expressed in goat male germline stem cells (mGSCs) and Sertoli cells, is one of the most conserved transcription factors involved in sex determination. In this study, we highlighted the role of Dmrt1 in balancing the innate immune response in goat mGSCs. Dmrt1 recruited promyelocytic leukemia zinc finger (Plzf), also known as zinc finger and BTB domain-containing protein 16 (Zbtb16), to repress the Toll-like receptor 4 (TLR4)-dependent inflammatory signaling pathway and nuclear factor (NF)-κB. Knockdown of Dmrt1 in seminiferous tubules resulted in widespread degeneration of germ and somatic cells, while the expression of proinflammatory factors were significantly enhanced. We also demonstrated that Dmrt1 stimulated proliferation of mGSCs, but repressed apoptosis caused by the immune response. Thus, Dmrt1 is sufficient to reduce inflammation in the testes, thereby establishing the stability of spermatogenesis and the testicular microenvironment.


Assuntos
Células-Tronco Germinativas Adultas/metabolismo , Imunidade Inata/fisiologia , Transdução de Sinais/fisiologia , Receptor 4 Toll-Like/metabolismo , Fatores de Transcrição/metabolismo , Animais , Células Cultivadas , Regulação da Expressão Gênica/efeitos dos fármacos , Técnicas de Silenciamento de Genes , Cabras , Inflamação/metabolismo , Lipopolissacarídeos/toxicidade , Masculino , NF-kappa B , Túbulos Seminíferos , Células de Sertoli/metabolismo , Receptor 4 Toll-Like/genética , Fatores de Transcrição/genética
11.
Phytochemistry ; 176: 112394, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32361500

RESUMO

Seventeen undescribed heterodimers of meroterpene phenol, psocorylins A-Q, were isolated from the fruits of Psoralea corylifolia. Their another monomeric unit derived from flavonone, chalcone, coumarin and isoflavone, respectively. Psocorylins A-E were rare natural spiroketals with the skeleton of 1,4,8-trioxaspiro[4.5]decane deriving from flavonone, and their plausible biosynthetic pathways were proposed. These structures were established by spectroscopic methods. Their absolute configurations were assigned via single-crystal X-ray diffraction, electronic circular dichroism (ECD) calculations and Rh2(OCOCF3)4-induced ECD spectra. Psocorylins B-E, F, M and Q exhibited potent cytotoxic activities against different kinds of tumor cells with IC50 values less than 10 µM.


Assuntos
Frutas , Psoralea , Estrutura Molecular , Fenol , Fenóis
12.
Clin Respir J ; 14(5): 447-452, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-31916391

RESUMO

INTRODUCTION: Rapid on-site evaluation (ROSE) has the potential to increase endobronchial ultrasound transbronchial lung biopsy with guide sheath (EBUS-GS-TBLB) accuracy in the diagnosis of peripheral lung cancer. However, studies have reported controversial results. OBJECTIVES: The aim of the study was to evaluate the diagnosis value of EBUS-GS-TBLB combination with ROSE in peripheral lung cancer. METHODS: A total of 138 patients undergoing EBUS-GS-TBLB and ultimately diagnosed with lung cancer were allocated into the ROSE group and non-ROSE group. The result of the diagnostic yields, number of biopsy sites, the complication, cytopathological diagnostic cost and procedure times of EBUS-GS-TBLB with ROSE and without ROSE were compared. RESULTS: The diagnostic yields of TBLB were 87.8% and 78.1% in ROSE group and non-ROSE group, respectively (P < .05). The number of biopsy, procedure times and the percentage of the complication in ROSE group was significantly lower than in non-ROSE group (P < .05, respectively). The cytopathological diagnostic cost of ROSE group was lower compared with non-ROSE group (P < .05). CONCLUSIONS: EBUS-GS-TBLB combined with ROSE could be helpful to diagnose peripheral lung cancer, and could reduce the number of biopsy, procedure times, cytopathological diagnostic cost and complication.


Assuntos
Endossonografia/métodos , Biópsia Guiada por Imagem/instrumentação , Biópsia Guiada por Imagem/estatística & dados numéricos , Neoplasias Pulmonares/patologia , Adulto , Idoso , Broncoscopia/métodos , China/epidemiologia , Feminino , Humanos , Biópsia Guiada por Imagem/economia , Pulmão/patologia , Neoplasias Pulmonares/diagnóstico por imagem , Masculino , Pessoa de Meia-Idade , Estudos Prospectivos , Fatores de Tempo , Tomografia Computadorizada por Raios X/métodos
13.
Zhongguo Zhong Yao Za Zhi ; 45(23): 5762-5769, 2020 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-33496117

RESUMO

This paper discussed the synergistic anti-tumor effect of Shuangdan Capsules combined with 5-fluorouracil(5-FU) on human liver cancer cell line Huh-7 and tumor bearing mice. The effects of Shuangdan Capsules combined with 5-FU on the activity and vascular endothelial growth factor(VEGF) receptor protein expression of Huh-7 cells were investigated, and the effects of drug combination on tube formation of HUVEC cell were also verified. In addition, the mice model of Huh-7 was established to observe the anti-tumor effect of drug combination and the distribution of tumor blood flow in tumor bearing mice by using molecular imaging. HPLC analysis showed that Shuangdan Capsules mainly consisted of danshensusodium, protocatechuic aldehyde, paeoniflorin, rosmarinic acid, alkannic acid, salvianolic acid B, and paeonol. In MTT experiment, the inhibition rate of Shuangdan Capsules(20 mg·L~(-1)) and 5-FU(1 µmol·L~(-1)) on Huh-7 cells was 60%, and the CI value was 0.59, suggesting that these two drugs had synergistic anti-hepatoma cells effect. The expression of VEGF receptor in Huh-7 cells was inhibited by the combination of these two drugs. In addition, the process of HUVEC was slow, and the number, length and area of the lumen branches decreased significantly. In vivo, Shuangdan Capsules combined with 5-FU inhibited the growth and prolongation of survival of Huh-7 cells in subcutaneous transplanted tumor nude mice; serum expression of CD31 and VEGF in nude mice were decreased, while caspase-3 was increased. Meanwhile, the drug combination significantly inhibited the expressions of MMP2 and VEGF in tumor tissues. Ultrasound showed that Shuangdan Capsules combined with 5-FU also inhibited tumor angiogenesis and reduced blood flow of tumor tissue. The results showed that Shuangdan Capsules combined with 5-FU may inhibit tumor angiogenesis by inhibiting VEGF and MMP2 expressions, thereby blocking tumor growth.


Assuntos
Carcinoma Hepatocelular , Neoplasias Hepáticas , Animais , Cápsulas , Linhagem Celular Tumoral , Proliferação de Células , Medicamentos de Ervas Chinesas , Fluoruracila , Xenoenxertos , Camundongos , Camundongos Nus , Fator A de Crescimento do Endotélio Vascular , Ensaios Antitumorais Modelo de Xenoenxerto
14.
Molecules ; 24(22)2019 Nov 12.
Artigo em Inglês | MEDLINE | ID: mdl-31718071

RESUMO

Psoralen (P) and isopsoralen (IP) are the main active ingredients in the dried fruit of Psoralen corylifolia L. (PC), with a wide range of pharmacology activities. The intestinal bacteria biotransformation plays a central role in the metabolism of the complex ingredients in traditional Chinese medicine (TCM). Our study aimed to investigated the metabolic profile of P and IP in the intestinal condition, co-cultured with human fecal bacteria anaerobically. Four bio-transforming products were obtained, including 6,7-furano-hydrocoumaric acid (P-1) and 6,7-furano-hydro- coumaric acid methyl ester (P-2), which transformed from P, and 5,6-furano-hydrocoumaric acid (IP-1) and 5,6-furano-hydrocoumaric acid methyl ester (IP-2), which were transformed from IP. It is worth mentioning that IP-2 is a new compound that has not been published. Their structures were analyzed based on their spectroscopic data. Moreover, a highly sensitive ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method was used to characterize the metabolic pathways of P, IP, and their bio-transforming products in the reaction samples. In addition, the dampening effects against the oxidative stress of P, IP, and their bio-transforming products by human intestinal flora were estimated in vitro via the human colorectal cells (HCT116) and heterogeneous human epithelial colorectal adenocarcinoma cells (Caco-2) cell lines. The results showed that the metabolites have stronger activity than P and IP, which possibly provides a basis for elucidating the treating mechanisms of PC extract against inflammatory bowel disease.


Assuntos
Biotransformação , Ficusina/metabolismo , Furocumarinas/metabolismo , Microbioma Gastrointestinal , Cromatografia Líquida de Alta Pressão , Ficusina/química , Furocumarinas/química , Humanos , Limite de Detecção , Metabolômica/métodos , Estrutura Molecular , Estresse Oxidativo , Espectrometria de Massas em Tandem , Fatores de Tempo
15.
Molecules ; 24(20)2019 Oct 17.
Artigo em Inglês | MEDLINE | ID: mdl-31627460

RESUMO

The dried vine stems of Spatholobus suberectus are commonly used in traditional Chinese medicine for treating gynecological and cardiovascular diseases. In this study, five new compounds named spasuberol A (2), homovanillyl-4-oxo-nonanoate (5), spasuberol C (6), spasuberoside A (14), and spasuberoside B (15), together with ten known compounds (1, 3, 4, 7-13), were isolated from the dried vine stems of S. suberectus. Their chemical structures were analyzed using spectroscopic assays. This is the first study interpreting the detailed structural information of 4. The anti-inflammatory activity of these compounds was evaluated by reducing nitric oxide overproduction in RAW264.7 macrophages stimulated by lipopolysaccharide. Compounds 1 and 8-10 showed strong inhibitory activity with half maximal inhibitory concentration (IC50) values of 5.69, 16.34, 16.87, and 6.78 µM, respectively, exhibiting higher activity than the positive drug l-N6-(1-iminoethyl)-lysine (l-NIL) with an IC50 value of 19.08 µM. The IC50 values of inhibitory activity of compounds 2 and 4-6 were 46.26, 40.05, 45.87, and 28.29 µM respectively, which were lower than l-NIL, but better than that of positive drug indomethacin with an IC50 value of 55.44 µM. Quantitative real-time polymerase chain reaction analysis revealed that assayed compounds with good anti-inflammatory activity, such as 1, 6, 9, and 10 at different concentrations, can reduce the messenger RNA (mRNA) expression of some pro-inflammatory cytokines such as tumor necrosis factor α (TNF-α), nitric oxide synthase (iNOS), and cyclooxygenase 2 (COX-2). The anti-inflammatory activity and the possible mechanism of the compounds mentioned in this paper were studied preliminarily.


Assuntos
Anti-Inflamatórios/farmacologia , Fabaceae/química , Expressão Gênica/efeitos dos fármacos , Glicosídeos/farmacologia , Lipopolissacarídeos/antagonistas & inibidores , Óxido Nítrico/antagonistas & inibidores , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Ciclo-Oxigenase 2/genética , Ciclo-Oxigenase 2/metabolismo , Glicosídeos/química , Glicosídeos/isolamento & purificação , Humanos , Indometacina/farmacologia , Concentração Inibidora 50 , Lipopolissacarídeos/farmacologia , Lisina/análogos & derivados , Lisina/farmacologia , Medicina Tradicional Chinesa , Camundongos , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Óxido Nítrico Sintase Tipo II/genética , Óxido Nítrico Sintase Tipo II/metabolismo , Extratos Vegetais/química , Caules de Planta/química , Células RAW 264.7 , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismo
16.
J Agric Food Chem ; 67(29): 8243-8252, 2019 Jul 24.
Artigo em Inglês | MEDLINE | ID: mdl-31271289

RESUMO

Elemicin, an alkenylbenzene constituent of natural oils of several plant species, is widely distributed in food, dietary supplements, and medicinal plants. 1'-Hydroxylation is known to cause metabolic activation of alkenylbenzenes leading to their potential toxicity. The aim of this study was to explore the relationship between elemicin metabolism and its toxicity through comparing the metabolic maps between elemicin and 1'-hydroxyelemicin. Elemicin was transformed into a reactive metabolite of 1'-hydroxyelemicin, which was subsequently conjugated with cysteine (Cys) and N-acetylcysteine (NAC). Administration of NAC could significantly ameliorate the elemicin- and 1'-hydroxyelemicin-induced cytotoxicity of HepG2 cells, while depletion of Cys with diethyl maleate (DEM) increased cytotoxicity. Recombinant human CYP screening and CYP inhibition experiments revealed that multiple CYPs, notably CYP1A1, CYP1A2, and CYP3A4, were responsible for the metabolic activation of elemicin. This study revealed that metabolic activation plays a critical role in elemicin cytotoxicity.


Assuntos
Pirogalol/análogos & derivados , Ativação Metabólica , Biotransformação , Sobrevivência Celular/efeitos dos fármacos , Sistema Enzimático do Citocromo P-450/metabolismo , Células Hep G2 , Humanos , Hidroxilação , Estrutura Molecular , Pirogalol/química , Pirogalol/metabolismo , Pirogalol/toxicidade
17.
J Org Chem ; 84(20): 12904-12912, 2019 Oct 18.
Artigo em Inglês | MEDLINE | ID: mdl-31294555

RESUMO

The functionalization of aliphatic C-H bonds is both a major challenge and a desirable goal in organic synthesis. Here, we describe the successful arylation of unactivated alkanes with heteroarenes by using iridium polypyridyl complexes as the photocatalyst and persulfate as the HAT catalyst precursor under visible-light irradiation. This reaction features good functional group tolerance and broad scope with regard to both alkane and heteroarene substrates (37 examples), which allows direct access to alkyl-substituted N-heteroarenes, a key structural motif in natural products and bioactive molecules.

18.
J Agric Food Chem ; 67(15): 4328-4336, 2019 Apr 17.
Artigo em Inglês | MEDLINE | ID: mdl-30912427

RESUMO

Myristicin is widely distributed in spices and medicinal plants. The aim of this study was to explore the role of metabolic activation of myristicin in its potential toxicity through a metabolomic approach. The myristicin- N-acetylcysteine adduct was identified by comparing the metabolic maps of myristicin and 1'-hydroxymyristicin. The supplement of N-acetylcysteine could protect against the cytotoxicity of myristicin and 1'-hydroxymyristicin in primary mouse hepatocytes. When the depletion of intracellular N-acetylcysteine was pretreated with diethyl maleate in hepatocytes, the cytotoxicity induced by myristicin and 1'-hydroxymyristicin was deteriorated. It suggested that the N-acetylcysteine adduct resulting from myristicin bioactivation was closely associated with myristicin toxicity. Screening of human recombinant cytochrome P450s (CYPs) and treatment with CYP inhibitors revealed that CYP1A1 was mainly involved in the formation of 1'-hydroxymyristicin. Collectively, this study provided a global view of myristicin metabolism and identified the N-acetylcysteine adduct resulting from myristicin bioactivation, which could be used for understanding the mechanism of myristicin toxicity.


Assuntos
Compostos de Benzil/metabolismo , Compostos de Benzil/toxicidade , Dioxolanos/metabolismo , Dioxolanos/toxicidade , Hepatócitos/efeitos dos fármacos , Pirogalol/análogos & derivados , Acetilcisteína/química , Acetilcisteína/metabolismo , Ativação Metabólica , Derivados de Alilbenzenos , Animais , Compostos de Benzil/química , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Citocromo P-450 CYP1A1/metabolismo , Dioxolanos/química , Hepatócitos/citologia , Humanos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Pirogalol/química , Pirogalol/metabolismo , Pirogalol/toxicidade
19.
Open Med (Wars) ; 13: 544-550, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30426092

RESUMO

INTRODUCTION: The fascin-1 protein is a cytoskeleton-like protein, which can prompt structural changes in cell membranes and affect the integrity of intercellular relations to promote invasion and metastasis of tumor cells. In this study, we researched the expression of fascin-1 in glioma. MATERIAL AND METHODS: The fascin-1 protein and mRNA were detected by immunohistochemistry and reverse transcription polymerase chain reaction (RT-PCR). Then, we analyzed the relationship between the expression of fascin-1 protein and the clinical pathological characteristics of patients with glioma. Finally, the fascin-1 protein expression status and prognosis of glioma patients were investigated. RESULTS: The fascin-1 protein was mainly located in the cytoplasm of cells from glioma. The high expression rate of fascin-1 protein in glioma tissue was higher than that of normal brain tissue. At same time, we found that high fascin-1 protein expression was significantly correlated with World Health Organization (WHO) grading of glioma patients. The results survival analysis suggested high expression of fascin-1 protein in glioma patients with a shorter survival time. Multivariate analysis showed that high expression of fascin-1 protein was an independent predictor of the prognosis of patients with glioma. CONCLUSIONS: High expression of the fascin-1 protein indicates poor prognosis for glioma patients.

20.
BMC Cancer ; 18(1): 925, 2018 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-30257641

RESUMO

BACKGROUND: Cervical cancer incidence and mortality is high in Uyghur ethnics. Their life style and dietary habit were different from other ethnics living together. Study on the role of trace elements in HPV infection and cervical lesion of Uyghur minority is needed for future intervention and prevention work. METHODS: In total, 833 Uyghur women were randomly selected from the screening site and hospital. The concentrations of the trace elements As, Fe, Cd, Ni, Cu, Zn, Mn, and Se were determined by atomic absorption spectrophotometry and inductively coupled plasma atomic emission spectroscopy. Univariate analysis was performed with chi-squared test between the HPV-positive and HPV-negative groups and between the case group and the control group. Multivariate analysis was performed with logistic regression. RESULTS: An As concentration ≥ 0.02 mg/kg was a risk factor for HPV infection (OR > 1, P < 0.05), and Ni concentration ≥ 0.1232 mg/kg and Se concentration ≥ 0.02 mg/kg were protective factors (OR < 1, P < 0.05). Concentrations of Fe ≥ 6.9153 mmol/L and As ≥0.02 mg/kg were risk factors for CIN2+ (OR > 1, P < 0.05), and concentrations of Ni ≥0.0965 mg/kg and Se ≥0.02 mg/kg were protective factors (OR < 1, P < 0.05). CONCLUSIONS: Low serum concentrations of Se and Ni and a high serum concentration of As might be related to HPV infection and CIN2+ in Uyghur women in rural China.


Assuntos
Arsênio/sangue , Infecções por HIV/epidemiologia , Níquel/sangue , Selênio/sangue , Neoplasias do Colo do Útero/epidemiologia , Adulto , China/etnologia , Feminino , Infecções por HIV/sangue , Humanos , Modelos Logísticos , Pessoa de Meia-Idade , População Rural , Espectrofotometria Atômica , Oligoelementos/sangue , Neoplasias do Colo do Útero/sangue , Adulto Jovem
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