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2.
World J Gastroenterol ; 28(11): 1184-1186, 2022 Mar 21.
Artigo em Inglês | MEDLINE | ID: mdl-35431502

RESUMO

Gastroesophageal reflux disease (GERD) has a high prevalence worldwide. Li et al performed a well-designed study on the efficacy of modified Xiaochaihu decoction (MXD) for GERD, which showed that MXD is an optional therapy for GERD beyond proton pump inhibitors (PPIs). The herbal granule administration mode minimized the bias from traditional herbal formula in clinical trials. One limitation of that study was that it lacked records of side effects and rescue medication. As a chronic disease with recurrent symptoms, GERD rehabilitation requires prolonged observation of the clinical course with MXD therapy.


Assuntos
Medicamentos de Ervas Chinesas , Refluxo Gastroesofágico , Medicamentos de Ervas Chinesas/uso terapêutico , Refluxo Gastroesofágico/diagnóstico , Refluxo Gastroesofágico/tratamento farmacológico , Humanos , Medicina Tradicional Chinesa , Inibidores da Bomba de Prótons/uso terapêutico
3.
Mil Med Res ; 9(1): 20, 2022 04 26.
Artigo em Inglês | MEDLINE | ID: mdl-35473758

RESUMO

Granulomatous lobular mastitis (GLM) is a rare and chronic benign inflammatory disease of the breast. Difficulties exist in the management of GLM for many front-line surgeons and medical specialists who care for patients with inflammatory disorders of the breast. This consensus is summarized to establish evidence-based recommendations for the management of GLM. Literature was reviewed using PubMed from January 1, 1971 to July 31, 2020. Sixty-six international experienced multidisciplinary experts from 11 countries or regions were invited to review the evidence. Levels of evidence were determined using the American College of Physicians grading system, and recommendations were discussed until consensus. Experts discussed and concluded 30 recommendations on historical definitions, etiology and predisposing factors, diagnosis criteria, treatment, clinical stages, relapse and recurrence of GLM. GLM was recommended as a widely accepted definition. In addition, this consensus introduced a new clinical stages and management algorithm for GLM to provide individual treatment strategies. In conclusion, diagnosis of GLM depends on a combination of history, clinical manifestations, imaging examinations, laboratory examinations and pathology. The approach to treatment of GLM should be applied according to the different clinical stage of GLM. This evidence-based consensus would be valuable to assist front-line surgeons and medical specialists in the optimal management of GLM.


Assuntos
Mastite Granulomatosa , Mama/patologia , Consenso , Feminino , Mastite Granulomatosa/diagnóstico , Mastite Granulomatosa/patologia , Mastite Granulomatosa/terapia , Humanos , Recidiva
4.
Food Chem X ; 14: 100287, 2022 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-35313650

RESUMO

The present study investigated the effects of different extraction methods including water-water bath (W-WB), ethanol-water bath (E-WB), deep eutectic solvent (DES) combined with ultrasound-assisted extraction (DES-UAE), microwave-assisted extraction (DES-MAE), and enzyme-assisted extraction (DES-EAE) on flavonoids (total flavonoid content, flavonoid composition, and stability) in jujube. The highest total flavonoid content of 8.03 mg/g was obtained by the DES-MAE extraction. Fifteen types of flavonoids were identified from jujube. The amount of rutin produced by the E-WB and DES-UAE methods was 66.88 ± 1.58 µg/g and 45.23 ± 3.22 µg/g, respectively. The retention of flavonoids in DES-UAE extracts were 98.15 ± 0.51%, 64.25 ± 2.21% after 2 h of high temperature treatment at 90 °C and 21 days of dark storage, respectively. The flavonoids extracted by different methods were suitable for dark storage under different light contrasts, where the retention of flavonoids extracted by DES-UAE method was 86.44 ± 2.45%. In conclusion, DES-UAE would be an efficient method for flavonoid extraction from jujube.

5.
Quant Imaging Med Surg ; 11(7): 3133-3145, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34249640

RESUMO

BACKGROUND: Fluid responsiveness is an important topic for clinicians. We investigated whether changes in left ventricular outflow tract (LVOT) velocity time integral (VTI) during a Trendelenburg position (TP) maneuver can predict fluid responsiveness as a non-invasive marker in coronary artery bypass graft (CABG) surgery patients in the operating room. METHODS: This prospective, single-center observational study, performed in the operating room, enrolled 65 elective CABG patients. Hemodynamic data coupled with transesophageal echocardiography monitoring of the LVOT VTI and the peak velocity were collected at each step [baseline 1, TP, baseline 2 and fluid challenge (FC)]. Patients whose VTI increased ≥15% after FC (500 mL of Gelofusine infusion within 30 min) were considered responders. RESULTS: Twenty-eight (43.1%) patients were responders to fluid administration. VTI changes during the TP maneuver predicted fluid responsiveness with an area under the receiver operating characteristic curve (AUC) of 0.90 (95% CI, 0.79-0.96), with a sensitivity of 100%, and a specificity of 70% at a threshold of 10% (gray zone, 8-15%). The increase in VTI during the TP was correlated with the VTI changes induced by FC (r=0.61, P<0.0001). Changes in peak velocity and pulse pressure during the TP were poorly predictive of fluid responsiveness, with an AUC of 0.72 (95% CI: 0.60-0.82) and 0.66 (95% CI: 0.53-0.77), respectively. CONCLUSIONS: An increase in VTI induced by the TP could predict fluid responsiveness in CABG patients in the operating room. However, changes in peak velocity and pulse pressure stimulated by the TP could not reliably predict fluid responsiveness.

6.
Eur Heart J Suppl ; 23(Suppl B): B43-B45, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-35185402

RESUMO

To report the blood pressure (BP) data obtained in the May Measurement Month (MMM) 2019 in China. Study participants were recruited if ≥18 years of age and had ideally not had their BP measured for ≥1 year. BP was measured three times consecutively with a 1-min interval in the sitting position, using a validated electronic BP monitor. Trained volunteer investigators administered a questionnaire to collect information on lifestyle, medical history, and use of medications. The measurement was performed in 238 387 participants in 250 sites across 31 China provinces. The majority of screening took place in hospitals or clinics (78.7%), with 17.1% in outdoor public areas and 4.2% in other settings. The study participants included 127 853 women (53.6%) and had a mean (±SD) age of 48.9 ± 16.2 years. The mean (of readings two and three) systolic/diastolic BP was 121.8/73.8 mmHg. In all hypertensive patients (n = 66 181, 27.8%), the awareness, treatment, and control rates of hypertension were 51.5%, 48.4%, and 29.1%, respectively. Linear regression models showed differences in systolic and diastolic BP according to sex and age and several other major characteristics, such as previous stroke, myocardial infarction, and diabetes mellitus, antihypertensive medication use and known hypertension, previous hypertension in pregnancy and current pregnancy, alcohol intake and current smoking, and body mass index. The MMM 2019 campaign has been successful in measuring BP in a large member of participants in China.

7.
Ying Yong Sheng Tai Xue Bao ; 31(10): 3296-3304, 2020 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-33314818

RESUMO

The distribution pattern and interspecific associations of arbor seedlings were examined in two Tilia amurensis forest stands in Zhangguangcailing, with one without man-made interference (natural recovery secondary forest) and the other one being 20-year-old after selective cutting (selective cutting secondary forest). The results showed that the importance value of the seedlings of the soft broad-leaved (heliophile) and tolerant tree species was 7.9 and 64.5 in natural recovery secondary forest, and was 3.9 and 68.9 in selective cutting secondary forest, respectively. The spatial distribution pattern of arbor seedlings in natural recovery and selective cutting secondary forests showed clustered distribution at the scale of 0-18 m and 0-15 m, respectively. Most of tree species pairs were negatively correlated at large scale (14-45 m) in the natural recovery secondary forest, whereas tree species pairs at all the scales were mostly uncorrelated in the selective cutting secon-dary forest. Most of the tree pairs of T. amurensis seedlings (57%) with other tree species showed negatively correlation at large scale (31-45 m). In the natural recovery secondary forest, the proportion of negatively correlated tree pairs was higher than 60%. In selective cutting secondary forest, Acer mono seedlings were negatively correlated with other tree species at more scales (6-45 m). In the natural recovery secondary forest, the pairs of A. mono and other arbor seedlings were positively correlated at small scale (0-5 m), but not at large scale (31-45 m). Therefore, selective cutting accelerated the succession of the secondary forest of T. amurensis, which induced random distribution of the arbor seedlings at the large scale (31-45 m), promoted a more coordinated inter-specific relationship, and adjusted the spatial competition between T. amurensis seedlings. Both stands were under succession, and thus suitable artificial management should be carried out to promote tree regeneration and community restoration.


Assuntos
Pinus , Tilia , Adulto , China , Florestas , Humanos , Plântula , Árvores , Adulto Jovem
8.
J Clin Biochem Nutr ; 67(2): 146-152, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-33041511

RESUMO

Our study was to understand the autophagy induce by different ratios and concentrations of LA/DHA on Raw264.7 cell, and then to investigate the effect of Raw264.7 autophagy on the clearance of Staphylococcus aureus. Raw264.7 cells was treated by LA/DHA in different concentrations (50/100 µmol/L) and ratios (4:1, 6:1, 8:1, 1:4, 1:6 and 1:8) for 6/12/24 h, cell viability assay was assessed by Cell Counting Kit-8, LC3B, p62, P-mTOR, P-Akt, P-PI3K and BECN 1 were detected by the Western blot. LA/DHA could induce autophagy of Raw264.7 cells through the PI3K-Akt-mTOR signaling pathway, the strong effect on autophagy by the concentration is 100 µmol/L, the ratio is 6:1 of LA/DHA, and the treatment time is 24 h. Compared with the images in the control group obtained by merging red and green fluorescence channels, the treatment of LA, DHA in a ratio of 6:1 at a concentration of 100 µmol/L for 24 h significantly lead to a substantial number of autophagosomes (yellow) as well as autolysosomes (red), enhancing autophagy flux. Autophagy induce by LA/DHA can devour and damage intracellular and extracellular Staphylococcus aureus. These results indicate that LA/DHA cloud induce autophagy and enhance the phagocytosis and killing ability of macrophages to intracellular parasitic bacteria.

9.
Eur Heart J Suppl ; 22(Suppl H): H40-H42, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32884466

RESUMO

To further improve awareness, treatment, and control of hypertension, the May Measurement Month (MMM) campaign continued in 2018 in China. Study subjects were adults aged 18 years or more, ideally those who had not their blood pressure (BP) measured for at least a year. Blood pressure was measured three times consecutively with a 1-min interval in the sitting position, using automated BP monitors in 288 342 participants and transmitted to a central database by a smartphone app. Questionnaire data were collected with the same app. After imputation, the overall proportion of hypertension was 29.8%. Of those with hypertension, the rates of awareness, treatment, and control were 62.3%, 57.3%, and 35.9%, respectively. In analysis based on linear regression models, both systolic and diastolic BP were higher with cigarette smoking, alcohol intake, and overweight and obesity. Our study results suggest that hypertension management is improving in comparison with the data in MMM 2017 and the nationwide survey in 2012-15, and several known lifestyle factors are key to hypertension management.

10.
Ann Transl Med ; 7(14): 315, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31475185

RESUMO

BACKGROUND: The aim of this study was to evaluate whether a 20-second end-expiratory occlusion (EEO) test can predict fluid responsiveness in cardiac surgery patients in the operating theatre. METHODS: This prospective study enrolled 75 mechanically ventilated patients undergoing elective coronary artery bypass grafting surgery. Hemodynamic data coupled with transesophageal echocardiography monitoring of the velocity time integral (VTI) and the peak velocity (Vmax) at the left ventricular outflow tract were collected at each step (baseline 1, EEO, baseline 2 and fluid challenge). Patients were divided into fluid responders (increase in VTI ≥15%) and non-responders (increase in VTI <15%) after a fluid challenge (6 mL 0.9% saline per kg, given in 10 minutes). RESULTS: Fluid challenge significantly increased the VTI by more than 15% in 36 (48%) patients (responders). An increase in VTI greater than 5% during the EEO test predicted fluid responsiveness with a sensitivity of 81% and a specificity of 93%. The area under the receiver-operating characteristic curve (AUROC) of ΔVTI-EEO was 0.90 [95% confidence interval (CI): 0.83-0.97]. ΔVmax-EEO was poorly predictive of fluid responsiveness, with an AUC of 0.75 (95% CI: 0.63-0.86). CONCLUSIONS: Changes in VTI induced by a 20-second EEO can reliably predict fluid responsiveness in cardiac surgical patients in the operating theatre, whereas the changes in Vmax cannot.

11.
Artigo em Inglês | MEDLINE | ID: mdl-29599805

RESUMO

Acute lung injury (ALI) is a critical illness with no current effective treatment. Caveolin-1 indirectly activates inflammation-associated signaling pathways by inhibiting endothelial nitric oxide synthase (eNOS). This induces an imbalance between pro- and anti-inflammatory cytokine levels, which are involved in the pathogenesis of ALI. The compound Chinese prescription Qi-Dong-Huo-Xue-Yin (QDHXY) is efficacious for ALI treatment via an anti-inflammatory effect; however, the exact underlying mechanism is unknown. Therefore, we explored the protective effect of QDHXY against lipopolysaccharide- (LPS-) induced ALI in mice. Histopathological changes in mouse lung tissues were studied. Furthermore, alterations in the serum levels of pro- and anti-inflammatory cytokines were investigated. The levels of tumor necrosis factor- (TNF-)α, interleukin- (IL-) 6, IL-1ß, and interferon-γ-induced protein 10 in bronchoalveolar lavage fluid were measured. Additionally, the expression levels of myeloid differentiation factor 88 (MyD88), caveolin-1, and eNOS were assessed. QDHXY significantly reduced lung infiltration with inflammatory cells and the production of serum pro- and anti-inflammatory cytokines and inhibited the expression of TNF-α, IL-1ß, caveolin-1, and MyD88 but not eNOS. These indicate that QDHXY significantly improved the balance between pro- and anti-inflammatory cytokine levels, possibly by inhibiting the caveolin-1 signaling pathway. Therefore, QDHXY may be a potential treatment for ALI.

12.
Exp Ther Med ; 10(5): 1707-1719, 2015 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-26640541

RESUMO

Transthoracic needle biopsy is considered to be safe and effective for the diagnosis of focal lung lesions. The aim of the present study was to evaluate factors affecting the accuracy and safety of automated cutting needle lung biopsy (ACNB) using a new extrapleural locating (EPL) method. Computed tomography (CT)-guided needle biopsies were performed on 1,065 patients between March 2005 and May 2012 using the EPL method. The locating needle remained in the chest following extrapleural positioning, while the radiologist confirmed the puncture angle and distance between the locating needle and lesion. The biopsy instrument was advanced into the lung, and the core needle was subsequently fired into the lesion based on the direction indicated by the locating needle. Univariate and multivariate regression analyses were used to evaluate the diagnostic accuracy and safety of the procedure. The sensitivity, specificity, positive predictive value and negative predictive value of the extrapleural method were 91.9, 100, 100 and 82.9%, respectively, and the overall diagnostic accuracy was 94.2%. Significant risk factors affecting accuracy were younger age, atelectasis, hemoptysis and lesion depth (P<0.03). Multivariate logistic regression analysis revealed that the risk of malignant lesions receiving a false-negative diagnosis decreased for each additional year of subject age [odds ratio (OR), 0.97; P=0.027] and increased with each millimeter increase in lesion depth (OR, 1.03; P=0.008). Among the 1,106 lesions biopsied, 207 were associated with pneumothorax, 251 with hemorrhage and 58 with hemoptysis. Multivariate analysis revealed that lesion size and emphysema affected pneumothorax incidence, while age, lesion location and depth and emphysema significantly affected hemorrhage incidence (P<0.05). In conclusion, low-dose, CT-guided ACNB with the EPL method provides a safe and accurate diagnosis.

13.
Clin Imaging ; 39(5): 880-5, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25725947

RESUMO

OBJECTIVE: The present study was to evaluate the clinical value of dual-energy computed tomography (DECT) for detecting monosodium urate crystals in patients with gouty arthritis. METHODS: Two hundred and two patients, who experienced arthrocele and (or) joint pain, were enrolled into our study. DECT scans of upper or lower extremity were performed. One hundred and sixty one patients who conformed to the American College of Rheumatology classification standard were defined as the gout group. The rest (41) of the patients were regarded as the without-gout group. DE (80kV/140kV) datasets were reconstructed via DE gout software. Images were reviewed independently by two senior radiologists. RESULTS: In the gout group, DECT scans revealed a total of 379 areas of urate deposition in 121 patients. In the without-gout group, 3 areas of green urate deposition were detected. The sensitivity and specificity were 75.2% and 92.7%, respectively; when we increased the ratio to 1.32 and decreased the range to 3, the number of patients with green urate deposition increased, and the areas of urate deposition were more extensive. The sensitivity and specificity were 91.9% and 85.4%. DECT images could illustrate the palpable reduction in the tissue urate deposits compared to baseline images before and after treatment. CONCLUSIONS: DECT has comparable sensitivity and specificity for the detection of gouty arthritis in a clinical setting, and DECT can monitor the clinical treatment. However, DECT results should be interpreted carefully because there could be some false-negative or false-positive findings.


Assuntos
Artrite Gotosa/diagnóstico por imagem , Tomografia Computadorizada por Raios X/métodos , Ácido Úrico/análise , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Artralgia/diagnóstico por imagem , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Sensibilidade e Especificidade , Adulto Jovem
14.
Huan Jing Ke Xue ; 36(9): 3298-303, 2015 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-26717691

RESUMO

The orpiment[As2S3(s)] is an important secondary mineral in the geochemical process of arsenic in the environment. The study upon orpiment dissolution is important to investigate the migration and transformation of arsenic in the environment. The environmental pH and sulfur content have vital influence on species changing and stability of arsenic species in orpiment. Here we analyzed the stable arsenic species of anoxic orpiment dissolution in sulfidic and the absence of sulfide solutions at neutral condition with simulation test via X-ray absorption near edge spectroscopy(XANES) and extended X-ray absorption fine structure(EXAFS). The results showed that orpiment dissolution contained a mixture of arsenite and thioarsenite species at neutral condition, and arsenic species in sulfidic solutions is mainly thioarsenic, while arsenic species in the absence of sulfide solutions is oxythioarsenic. The results of Linear Combination of Fits showed that arsenic species were arsenite (88. 2%) and thioarsenite(11. 8%) in sulfidic solutions, and there were arsenite (56. 3%) and thioarsenite(43. 7%) in the absence of sulfide solutions. Our results confirmed that the formation of arsenite was related to the total sulfur to total arsenic ratios, and the form of thioarsenite species could be enriched by increasing of the total sulfur to total arsenic ratio.


Assuntos
Arsenicais/análise , Sulfetos/análise , Arsênio , Arsenitos , Meio Ambiente , Minerais , Enxofre , Espectroscopia por Absorção de Raios X
15.
Exp Ther Med ; 9(1): 262-266, 2015 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-25452813

RESUMO

In cases of pleural lesion, tissue samples can be obtained through thoracoscopy or closed needle biopsy for histopathological analysis. Cutting needle biopsy is a relatively recent addition to these techniques. The aim of this study was to evaluate the diagnostic accuracy and safety of computed tomography-guided cutting needle pleural biopsy (CT-CNPB), as well as the associated complications, in patients with pleural lesion. This study was a retrospective analysis of 92 percutaneous CT-CNPBs on 90 patients between March 2008 and May 2013. For group comparisons, χ2 tests were used to detect the risk factors for diagnostic accuracy (false-negative rate). Of the 92 CT-CNPBs, malignant lesions were diagnosed in 55 cases (mesothelioma in 12, metastatic pleural disease in 36, synoviosarcoma in one, indeterminate-origin disease in one and false-negative lesion in five) and benign pleural disease was diagnosed in 37 cases (inflammation in 15, tuberculosis in 10, granuloma in three, solitary fibrous tumor in two, hematoma in one, fungus in one and indeterminate-origin disease in five). The sensitivity of diagnostic malignant lesion was 90.9%, and the specificity and positive and negative predictive values were 100, 100 and 88.1%, respectively. The overall diagnostic accuracy was 94.6%. A specific diagnosis was achieved in 89.1% of malignant lesions and 86.4% of benign lesions. Univariate analysis of the risk factors affecting accuracy (false-negative rate) did not reveal any significant differences (all P>0.05). The complication rates were 6.5% for pneumothorax, 8.7% for hemorrhage and 1.1% for hemothorax. In conclusion, CT-CNPB is a safe and accurate diagnostic technique that can be recommended as the primary method of diagnosis in patients with pleural thickening or lesions observed by CT scan.

16.
Oncol Lett ; 8(6): 2669-2671, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25364446

RESUMO

Renal metastasis of a submandibular gland adenoid cystic carcinoma is clinically rare when it presents with an atypical imaging appearance of singular renal metastases. Whole-body positron emission tomography (PET)/computed tomography (CT) can determine whether the singular renal mass is benign or malignant and identify metastases in other parts of the body, particularly in uncommon sites. In the present case, the patient developed a rare partial metastasis to the right kidney three years after undergoing a surgery for submandibular gland adenoid cystic carcinoma. Based on the present case, whole-body PET/CT examination could provide an important basis for making treatment plans for singular renal metastases.

17.
Mol Clin Oncol ; 2(5): 761-766, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-25054043

RESUMO

Metastatic tumours presenting as soft tissue metastasis (STM) are relatively rare. STM represents metastasis to the muscle and subcutaneous tissues. The majority of the currently available clinical or radiological data on STM consist of isolated case reports or reviews. The aim of this study was to report the manifestations, origin and distribution of STM detected by 18F-fluorodeoxyglucose (FDG) positron emission tomography (PET)/computed tomography (CT) and to assess the value of 18F-FDG PET/CT in the characterisation of STM. We reviewed 17 cases of patients with STM who underwent 18F-FDG PET/CT scanning. The imaging and clinical data of these patients were retrospectively analysed. This method is very sensitive in the detection of STM and provides ample information for clinical tumour staging. PET is more sensitive compared to CT in detecting lesions in muscle, before the density and morphology of the soft tissues are altered, providing a clear view within the soft tissue. Due to the limitations in resolution, PET is less sensitive compared to CT in detecting lesions in the subcutaneous tissues. The aim of this study was to improve our knowledge of 18F-FDG PET/CT findings in the diagnosis of STM and determine its value in the staging of malignant tumours.

18.
Oncol Lett ; 7(6): 1970-1974, 2014 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-24932271

RESUMO

The current study presents a case of extraskeletal mesenchymal chondrosarcoma (ESMC) involving the vena cava that originally occurred in the retroperitoneum of a 61-year-old female. Following excision of the masses, pathological examination confirmed a diagnosis of primary ESMC. Mesenchymal chondrosarcomas are extremely rare in comparison to conventional chondrosarcomas and even more so when arising in an extraskeletal location. In the current report, the major characteristics of ESMC are discussed and a review of the current knowledge regarding this rare disease entity is presented.

19.
Oncol Lett ; 5(5): 1554-1558, 2013 May.
Artigo em Inglês | MEDLINE | ID: mdl-23761818

RESUMO

Elemene has been approved for the treatment of advanced cancer in China, however, it inhibits cell growth only at high concentrations and is an essential oil with poor water solubility and stability. The discovery of new ß-elemene derivatives is of increasing interest. We recently reported that the compound 13,14-bis(cis-3,5-dimethyl-1-piperazinyl)-ß-elemene (IIi), a novel ß-elemene derivative with a cis-2,6-dimethylpiperazine substitution, is a potent agent for inhibiting the proliferation of SGC-7901 and HeLa cells. In the present study, we further verified that IIi is cytotoxic to a wide spectrum of human cancer cells in culture, including those of breast, ovarian, lung, gastric, hepatocellular and colon cancer, as well as leukemia cell lines, with an average IC50 of 3.44 µmol/l. Notably, IIi showed significant cytotoxicity in two multidrug-resistant (MDR) cell lines, with an average resistance factor (RF) of 1.66. Moreover, in mice with S-180 sarcoma xenografts, the intraperitoneal administration of IIi inhibited tumor growth. The immunoblotting study showed that treatment with IIi decreases phosphorylated p70S6K1 and 4EBP1 levels in the human breast cancer MCF-7 and MDA-MB-468 cells. In the MCF-7 cells, IIi also significantly increased the expression of cleaved LC3. This indicated that IIi inhibits mTOR activity and induces autophagy. The mTOR inhibitory function and the potent antitumor activity, taken together with the appreciable anti-multidrug resistance action, shows IIi to be a novel potential antitumor agent, which merits further research and development.

20.
Acta Crystallogr Sect E Struct Rep Online ; 68(Pt 6): o1843, 2012 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-22719610

RESUMO

The title compound, C(23)H(18)ClN(3)O, exists in an enamine-keto form with the amino group involved in an intra-molecular N-H⋯O hydrogen bond. The five-membered ring is nearly planar, the largest deviation being 0.0004 (7) Å, and makes dihedral angles of 16.62 (6), 41.89 (5) and 71.27 (4)° with the phenyl rings. In the crystal, weak C-H⋯O hydrogen bonds link the mol-ecules into supra-molecular chains along the b axis.

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