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2.
Saudi Med J ; 44(11): 1104-1112, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37926448

RESUMO

OBJECTIVES: To investigate the predictive significance of dynamic changes in the neutrophil to lymphocyte ratio (NLR) and platelet counts (PLTs) in patients with advanced gastric cancer (GC) during chemotherapy. METHODS: A total of 259 advanced GC patients receiving chemotherapy were enrolled and grouped by high or low NLR with a cut value of 2.5 and PLT with cut value of 300×109/L. The Kaplan-Meier survival model and the Log-rank test were carried out to determine the comparison on the overall survival differences. Cox regression analysis was employed to carry out both univariate and multivariate regression studies, aiming to explore potential prognostic factors acting independently. RESULTS: Higher pre-chemotherapy NLR exhibited an association with metastasis and advanced grade of Borrmann type, and higher NLR of pre- or post-chemotherapy GC patients was related with Borrmann type grade. Moreover, higher PLT counts are associated with advanced grades of Borrmann type. Interestingly, patients with lower post-chemotherapy NLR or decreasing NLR hold better overall response rate and disease control rate than those with higher NLR or increasing NLR. Furthermore, patients with high post-chemotherapy NLR alone or higher post-chemotherapy NLR plus higher post-chemotherapy PLT. CONCLUSION: Our study suggested that high post-chemotherapy NLR and post-chemotherapy PLT might be adverse prognostic markers in advanced GC patients undergoing chemotherapy.


Assuntos
Neutrófilos , Neoplasias Gástricas , Humanos , Prognóstico , Contagem de Plaquetas , Plaquetas/patologia , Estimativa de Kaplan-Meier , Linfócitos/patologia
3.
Onco Targets Ther ; 16: 885-890, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37927329

RESUMO

Metaplastic breast cancer (MBC) is a rare disease, and there was rarely reported the treatment after recurrence and metastasis. Here, we report the treatment of an adult patient who suffered from MBC with lung, lymph nodes and left pleura metastasis after radical surgery. The next-generation sequencing result demonstrated that it had tumor mutational burden (TMB) of 12.0 Muts/Mb and microsatellite stability. The patient received sintilimab, an immune checkpoint inhibitor, plus chemotherapy and achieved partial response (PR). This is a report of a good outcome of metastatic MBC achieving 24 months of progression-free survival (PFS) and 39 months of overall survival (OS) with a combination therapy of immune checkpoint inhibitor and chemotherapy. Immuno-chemotherapy may have antitumor activity for relapse MBC. TMB may serve as a potential predictor associated with PD-1 inhibitors in MBC and help clinicians make an optimum treatment strategy.

4.
Cancer Cell Int ; 23(1): 146, 2023 Jul 22.
Artigo em Inglês | MEDLINE | ID: mdl-37481519

RESUMO

PURPOSE: Colorectal cancer (CRC) is the third most common cancer in the world. The purpose of this study was to investigate the role of TNNT2 in the proliferation, migration and invasion of CRC cells and its expression in CRC tissues to better understand the regulatory role of TNNT2 in CRC. METHODS: Western blotting (WB) and qPCR were used to detect the expression of TNNT2 in colorectal cancer tissues and paracancerous tissues. CCK-8, colony formation, Transwell and other experiments were used to clarify the role of TNNT2 in the proliferation, migration and invasion of colorectal cancer cells. Changes in TNNT2, EGFR and HER2 mRNA transcription levels were detected by SYBR Real-Time PCR assay, and the effects of TNNT2 overexpression or knockdown on the expression of EGFR, HER2 and EMT-related proteins in CRC cells were determined by WB. TNNT2 and EGFR intreaction was carried out in HCT116 cells by coimmunoprecipitation experiments. RESULTS: The protein and mRNA expression level of TNNT2 in CRC tissues were higher than those in paracancerous tissues. The CCK-8 results suggested that overexpression of TNNT2 significantly promoted the proliferation of HCT116 and RKO cells, and TNNT2 konckdown gets the opposite result; and the colony formation results were the same as tthose of CCK-8 assay. Transwell invasion and migration experiments showed that overexpression of TNNT2 promoted the migration and invasion of HCT116 and PKO cells, and TNNT2 konckdown suppressed the migration and invasion of the these cells. The SYBR Green I real-time PCR method revealed that them RNA levels of TNNT2, EGFR and HER2 in the TNNT2 overexpression group were higher than those in RKO cells. WB showed that overexpressing TNNT2 increased the expression of EGFR and HER2 in HCT16 and RKO cells,decreased the expression of EMT marker E-cadherin, and increased the expression of Vimentin and N-cadherin. Konckdown of TNNT2 decreased the expression of EGFR and HER2, increased the expression of E-cadherin, and decreased the expression of Vimentin and N-cadherin in HCT16 and RKO cells. The immunocoprecipitation experiment showed that there was an interaction between EGFR and TNNT2. CONCLUSION: TNNT2 can promote the proliferation, invasion and metastasis of colorectal cancer cells. There is an interaction between TNNT2 and EGFR protein. TNNT2 can upregulate EGFR and HER2-related proteins in colorectal cancer cells and promote the occurrence of EMT. Therefore, TNNT2 can promote the invasion and metastasis of CRC cells through the EGFR/HER2/EMT signal axis, suggesting that TNNT2 is a potential target of CRC treatment.

5.
World J Surg Oncol ; 21(1): 198, 2023 Jul 07.
Artigo em Inglês | MEDLINE | ID: mdl-37420219

RESUMO

BACKGROUND: Immunocheckpoint inhibitor(ICI) is a major breakthrough in tumor treatment. It can activate the patient's own immune system and play an anti-tumor role, but not all patients can benefit from it. At present, there is still a lack of effective biomarkers to guide clinical application. The systemic immune inflammation(SII) index reflects the systemic inflammatory state and immune state of patients. Prognostic nutrition index(PNI) can be used to evaluate immune status of patients. Therefore, SII and PNI indexes may have some value in predicting the efficacy and prognosis of immunotherapy, but there is still a lack of relevant research. The purpose of our study was to explore the influence of SII and PNI index on the efficacy and prognosis of immunotherapy. METHODS: A total of 1935 patients treated with ICIs treatment in the Fourth Hospital of Hebei Medical University from November 2016 to October 2021 were retrospectively collected. 435 patients who met the inclusion criteria and did not meet the exclusion criteria. The imaging data, blood results of each patient were collected within 1 week before ICIs treatment. The neutrophil lymphocyte ratio(NLR), platelet lymphocyte ratio(PLR), monocyte lymphocyte ratio(MLR), PNI,systemic inflammatory response index(SIRI),neutrophil-eosinophil ratio(NER) was calculated. The patients were followed up by in-patient, out-patient reexamination and telephone contact, and the efficacy evaluation and survival status were recorded. The deadline of follow-up: January 2021. SPSS-24.0 software was employed for statistical analysis. RESULTS: Among the 435 patients receiving ICI treatment, 61,236 and 138 patients were evaluated respectively as partial response (PR), stable disease (SD) and progressive disease (PD). The overall response rate(ORR) and disease control rate (DCR) of this cohort were 14.0% and 68.3%, respectively. Median progression-free survival (mPFS) is 4.0 months, The overall survival (mOS) of this cohort is 6.8 months. Multivariate analysis showed that SIRI(Hazard Ratio, HR = 1.304, P = 0.014), PNI (HR = 0.771, P = 0.019), prealbumin (PAB) (HR = 0.596, P = 0.001), and PNI(HR = 0.657, P = 0.008) were independent risk factors for PFS and OS, respectively. CONCLUSIONS: Patients with high SIRI value and low PNI value before ICI treatment have shorter PFS. Patients with higher PNI value have better prognosis. Therefore, hematological indicators may become predictors of immunotherapy.


Assuntos
Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Humanos , Prognóstico , Inibidores de Checkpoint Imunológico/uso terapêutico , Estudos Retrospectivos , Carcinoma Pulmonar de Células não Pequenas/patologia , Neoplasias Pulmonares/patologia , Inflamação , Neutrófilos/patologia
6.
Artigo em Inglês | MEDLINE | ID: mdl-37282652

RESUMO

AIM: The present study is to investigate the association between T790M status and clinical characteristics of patients with EGFR-sensitive advanced non-small cell lung cancer (NSCLC) who progressed the initial epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) administration. METHODS: A total of 167 patients with EGFR-sensitive mutations advanced NSCLC who had successful genetic tests and progressed the initial EGFR-TKI treatment were included in this study retrospectively. The clinical and demographic characteristics of these patients were collected, which were manifested as pathological type, metastasis location, initial biopsy method, initial genetic test specimens, and baseline gene mutations status. Correlation analysis between T790M status and these characteristics was performed and prognostic analysis regarding the different subgroups was carried out accordingly. RESULTS: The prevalence of secondary T790M after resistance to initial EGFR-TKIs among the 167 patients was 52.7%. Correlation analysis indicated that the median progression-free Survival (PFS) to initial EGFR-TKIs >12 months were more likely to develop secondary T790M in univariate analysis. However, the conclusion failed to show statistically significant in multivariate analysis. Additionally, patients with intracranial progression of initial EGFR-TKIs therapy were associated with secondary EGFR-T790M. However, it should be noted that those whose best overall response was partial response (PR) during the EGFR-TKI therapy were relevant to secondary T790M. Furthermore, The median PFS of the initial EGFR-TKIs administration was longer among patients with T790M positive mutation and patients with PR reaction than those without T790M mutation and patients with stable disease (SD), respectively (median PFS: 13.6 vs 10.9 months, P=0.023) and (median PFS: 14.0 vs 10.1 months, P=0.001). CONCLUSION: This retrospective study highlighted the real-world evidence that the best efficacy and intracranial progression with initial EGFR-TKIs therapy among patients with advanced NSCLC might be the promising indicators to predict the occurrence of EGFR-T790M. Patients with PR reaction and T790M positive mutation conferred longer PFS of the initial EGFR-TKIs administration. Also, the conclusion should be confirmed in more patients with advanced NSCLC subsequently.

7.
Biomed Pharmacother ; 163: 114830, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37150036

RESUMO

Recently, cuproptosis has been demonstrated to be a new non-apototic cell death mode that is characterized by copper dependence and the regulation of mitochondrial respiration. Cuproptosis is distinct from known cell death modes such as apoptosis, necrosis, pyroptosis, or ferroptosis. Excessive copper induces cuproptosis by promoting protein toxic stress reactions via copper-dependent anomalous oligomerization of lipoylation proteins in the tricarboxylic acid (TCA) cycle and reducing iron-sulfur cluster protein levels. Ferredoxin1 (FDX1) promotes dihydrolipoyl transacetylase (DLAT) lipoacylation and abates iron-sulfur cluster proteins by reducing Cu2+ to Cu+, inducing cell death. Copper homeostasis depends on the copper transporter, and disturbances to this homeostasis cause cuproptosis. Recent evidence has shown that cuproptosis plays a significant role in the occurrence and development of many cardiovascular diseases, such as myocardial ischemia/reperfusion (I/R) injury, heart failure, atherosclerosis, and arrhythmias. Copper chelators, such as ammonium tetrathiomolybdate(VI) and DL-Penicillamine, may ease the above cardiovascular diseases by inhibiting the cuproptosis pathway. Oxidative phosphorylation inhibitors may inhibit cuproptosis by inhibiting protein stress response. In conclusion, cuproptosis plays an essential role in cardiovascular disease pathogenesis. Inhibition of cardiovascular cuproptosis is expected to become a potential treatment. Here, we will thoroughly review the molecular mechanisms involved in cuproptosis and its significance in cardiovascular disease.


Assuntos
Doenças Cardiovasculares , Insuficiência Cardíaca , Humanos , Cobre , Apoptose , Enxofre , Ferro
8.
Onco Targets Ther ; 16: 109-114, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36824323

RESUMO

Anaplastic lymphoma kinase (ALK) rearrangements have been reported in 3-7% of non-small-cell lung cancers (NSCLC). ALK has been reported to be fused with a variety of genes in NSCLC. Significant clinical activity was achieved by ALK inhibitors in patients with NSCLC harbouring ALK translocations. We reported on a 48-year-old male Chinese patient with advanced lung adenocarcinoma harboring a novel ALK-LIMS1 who showed no response to crizotinib. The tissue was assayed by immunohistochemistry (IHC) for ALK and showed diffuse expression of ALK. Next-generation sequencing (NGS) was performed on the peripheral blood and tissue. The previous tumor tissue showed diffuse expression of ALK. Tissue and the later peripheral blood revealed a ALK- LIMS1 fusion. The patient failed to benefit from crizotinib (250 mg, twice a day), with a progression-free survival of two months. We identified a new ALK-LIMS1 fusion from an advanced lung adenocarcinoma which was primary resistant to crizotinib. Our case suggested that the coexistence of mutations and the non-dominant clone, as well as the rearrangement of ALK fusion, did not result in expressed ALK kinase domain that might lead to no response to ALK-TKIs.

9.
Iran J Public Health ; 51(8): 1817-1826, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-36249096

RESUMO

Background: We aimed to analyze the predictive role of serum test and questionnaire in Early Gastric Cancer in The First Affiliated Hospital of Xingtai Medical College, Hebei Province from 2019 to 2020. Methods: In this prospective study, 280 medical examiners underwent questionnaire, serum test and gastroscopy. They were divided into Gastric cancer (GC) and Non-Gastric cancer (NGC) group. NGC group was divided into Low-grade intraepithelial neoplasia (LGIN), Chronic atrophic gastritis (CAG) and Non-chronic atrophic gastritis (NCAG) group. Results: Age, drinking, sex and Gastrin-17(G-17) was respectively independent risk factors for GC. Age, drinking and G-17 was independent risk factors for GC in men. G-17 of GC group was higher than that of LGIN and NCAG group (P<0.05). Pepsinogen I/II ratio (PGR) of GC was lower than that of NCAG group (P<0.05). There was no significant difference between Pepsinogen I (PGI) and Pepsinogen II (PGII) in the four groups. Helicobacter pylori-immunoglobulin G antibodies (H. pylori-IgG) of LGIN group was significantly higher than that of CAG and NCAG group in gastritis group (P<0.008). G-17≥42.95 pmol/L, age≥69years, male and drinking can predict GC. Conclusion: Older, drinking, men and high G-17 could respectively predict GC. Especially in men, older, drinking and high G-17 could affect the occurrence of GC. G-17, age, drinking and sex used respectively to screen high-risk populations for GC were more efficient than combined screening. GC had a higher serum G-17 and a lower PG than other gastric diseases.

10.
World J Clin Cases ; 10(21): 7324-7332, 2022 Jul 26.
Artigo em Inglês | MEDLINE | ID: mdl-36158017

RESUMO

BACKGROUND: Osteoporosis is a global disease affecting 6.6% of the total population. Osteoporosis complications include fractures, increased bone fragility, and reduced bone strength. The most commonly affected parts are the vertebral body, hip, and wrist. AIM: To examine the effect of alendronate sodium combined with InterTan for osteoporotic femoral intertrochanteric fractures on bone and fracture recurrence. METHODS: In total, 126 cases of osteoporotic femoral intertrochanteric fractures were selected and divided into two groups according to the 1:1 principle by the simple random method. They were admitted to the Department of Orthopedics, First Affiliated Hospital of Xingtai Medical College, from January 2018 to September 2020. The control group was treated with InterTan fixation combined with placebo, and the observation group with alendronate sodium based on InterTan fixation. Operation-related indicators, complications, and recurrent fractures were compared between the groups. Changes in bone metabolism markers, t value for hip bone mineral density, and Harris Hip Score were observed. RESULTS: Operation time, intraoperative blood loss, postoperative ambulation time, and complications were compared between the groups, and no significant difference was found. The fracture healing time was significantly shorter in the observation group than in the control group. ß-Collagen-specific sequence (ß-CTX) and total aminoterminal propeptide of type I procollagen (T-PINP) in the control group at 3 mo after operation were compared with those before operation, and the difference was not significant. Six months after the operation, the ß-CTX level decreased and T-PINP level increased. ß-CTX level at 3 and 6 mo in the observation group after operation was lower, and T-PINP level was higher, than that before operation. Compared with the control group, T-PINP level of the observation group was significantly higher and ß-CTX level was significantly lower at 3 and 6 mo after operation. The t value of hip bone mineral density was compared in the control group before and 1 mo after operation, and significant difference was not found. Compared with the control group, the t value of hip bone mineral density in the observation group was significantly higher at 1, 3, 6, and 12 mo after operation. Compared with the control group, the Harris score of the observation group was significantly higher at 1, 3, 6, and 12 mo after operation. The recurrence rate of fractures in the observation group within 12 mo was 0.00%, which was significantly lower than 6.35% in the control group. CONCLUSION: Alendronate sodium combined with InterTan in the treatment of osteoporotic femoral intertrochanteric fractures can increase bone mineral density, improve hip joint function, promote fracture healing, and reduce fracture recurrence.

11.
Anticancer Drugs ; 33(9): 975-978, 2022 10 01.
Artigo em Inglês | MEDLINE | ID: mdl-35946538

RESUMO

The reason that immune checkpoint inhibitors have not been widely applied to pancreatic cancer treatment is probably because of low immunogenicity or dense stromal fibrosis. Recently, only pembrolizumab was recommended for DNA mismatch repair deficiency or high microsatellite instability by National Comprehensive Cancer Network guideline. Pancreatic ductal adenocarcinoma (PDAC) accounts for more than 90% of pancreatic cancer, with a poor overall survival rate, the value of immunotherapy for PDAC needs more research. Here, we report a 56-year-old man suffered from PDAC with liver metastasis after radical surgery. The next-generation sequencing result demonstrated that it had remarkably high tumor mutational burden (TMB) of 49.92 Muts/Mb and microsatellite stability. Sintilimab (anti-PD-1) monotherapy was continuously administrated after failure of combined chemotherapy in second line, achieving stable disease within 22 months and few immunotherapy-related adverse events. To our knowledge, this is the first time to report a good outcome achieving 22 months with progression-free survival after PDAC metastasis with monotherapy of sintilimab. TMB may serve as a potential efficacy-related predictor in PDAC patients with sintilimab and help physicians make optimum clinical strategy.


Assuntos
Carcinoma Ductal Pancreático , Neoplasias Pancreáticas , Anticorpos Monoclonais Humanizados , Carcinoma Ductal Pancreático/tratamento farmacológico , Carcinoma Ductal Pancreático/genética , DNA , Humanos , Inibidores de Checkpoint Imunológico , Masculino , Pessoa de Meia-Idade , Mutação , Recidiva Local de Neoplasia , Neoplasias Pancreáticas/tratamento farmacológico , Neoplasias Pancreáticas/genética , Neoplasias Pancreáticas/patologia , Neoplasias Pancreáticas
12.
Drug Deliv ; 29(1): 342-350, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-35049388

RESUMO

PURPOSE: Colorectal cancer (CRC) is the third most frequently diagnosed cancer and this study aimed to develop a conatumumab decorated, irinotecan prodrug and quercetin co-loaded delivery system for combined and targeted colorectal cancer treatment. METHODS: A conatumumab (C) decorated, irinotecan prodrug (I-p) and quercetin (Q) co-encapsulated NLC (C I-p/Q NLC) was developed. In vitro and in vivo antitumor efficiency of NLC was evaluated on CRC cells and mice xenograft. RESULTS: The results showed that the HT-29 cells uptake of C I-p/Q NLC was over 70%. Reactive oxygen species (ROS) sensitive irinotecan prodrug formulation showed improved drug release ability in hypoxic conditions. C I-p/Q NLC showed significantly higher cytotoxicity than non-decorated NLC, single drug-loaded NLC and free drugs. In vivo studies in a CRC-bearing model corroborated the capability of nanoparticles for the inhibition of cancer, leading to a reduction of tumor growth without systemic toxicity. CONCLUSION: The conatumumab decorated, ROS sensitive prodrug contained combination nano-system is a promising platform for CRC therapy.


Assuntos
Anticorpos Monoclonais/farmacologia , Antineoplásicos/farmacologia , Irinotecano/farmacologia , Sistemas de Liberação de Fármacos por Nanopartículas/química , Quercetina/farmacologia , Animais , Anticorpos Monoclonais/administração & dosagem , Antineoplásicos/administração & dosagem , Sobrevivência Celular/efeitos dos fármacos , Química Farmacêutica , Portadores de Fármacos/química , Combinação de Medicamentos , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Sinergismo Farmacológico , Células HT29 , Humanos , Irinotecano/administração & dosagem , Lipídeos/química , Camundongos , Nanoestruturas , Tamanho da Partícula , Pró-Fármacos , Quercetina/administração & dosagem , Espécies Reativas de Oxigênio , Propriedades de Superfície , Ensaios Antitumorais Modelo de Xenoenxerto
13.
World J Surg Oncol ; 19(1): 64, 2021 Feb 26.
Artigo em Inglês | MEDLINE | ID: mdl-33637113

RESUMO

BACKGROUND: This paper aims to compare the efficacy and safety of recombinant human endostatin combined with chemotherapy in patients with squamous cell lung cancer (SqCLC). METHODS: We searched the Cochrane Library, PubMed, Embase, CNKI, Wanfang database, Metstr, VIP, and others and manually searched books and magazines until 2019 for articles about the efficacy and safety of recombinant human endostatin combined with chemotherapy in patients with SqCLC. A second search was conducted on the review literature. According to the criteria of the literature screen, the relevant randomized controlled trials (RCTs) and nonrandomized controlled trials (non-RCTs) of recombinant human endostatin combined with chemotherapy and chemotherapy alone in the treatment of SqCLC were included. After the data were extracted and analyzed, RevMan 5.3 software was used for meta-analysis for the outcome indicators. Then, heterogeneity tests and sensitivity analyses were carried out, and the publication bias of this study was tested in Stata 13.0 software. Six RCTs and eight non-RCTs were included. In total, 821 patients with SqCLC were included. RESULTS: The response rate (RR) was 2.12 (95% CI: 1.57-2.85, p < 0.00001). The disease control rate (DCR) was 2.38 (95% CI: 1.70-3.32, p < 0.00001). The difference between the two groups was statistically significant. Regarding safety, the incidence rates of the adverse reactions cardiotoxicity, leukopenia, thrombocytopenia, and gastrointestinal reactions were not significantly different between the two groups (OR = 1.70, 95% CI: 0.79-3.68; OR = 0.93, 95% CI: 0.61-1.42; OR = 1.08, 95% CI: 0.71-1.64; OR = 0.86, 95% CI: 0.56-1.30, respectively). CONCLUSION: The combined treatment had a better therapeutic effect than chemotherapy alone. It did not increase the incidence of adverse reactions in the course of treatment.


Assuntos
Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Endostatinas/uso terapêutico , Células Epiteliais , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Prognóstico
14.
Iran J Public Health ; 49(11): 2103-2110, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33680997

RESUMO

BACKGROUND: To study the anti-cancer effect of isoalantolactone, a sesquiterpene lactoneisolated from the roots of Inula heleniumon human gynecologic cancer cells. METHODS: A structure-activity relationship experiment was designed to identify the functional moiety of isoalantolactone for its significant anti-cancer activity. Five gynecologic cancer cell lines were treated with isoalantolactone. Cell proliferation was determined by MTT assay in vitro and cell apoptosis by flow cytometry. RESULTS: We found isoalantolactone strongly inhibited the cell proliferationofHEC-1, HAC-2, HOC-21, and HeLa cells. Its inhibitory effect was comparable to that of well-known chemotherapeutic agents, cisplatin and taxol. Furthermore, isoalantolactone induced apoptosis in HeLa cells via caspase. On the contrary, its 11, 13-dihydro derivatives had much weaker anti-proliferative activities than the parent compound. CONCLUSION: Isoalantolactone exhibited strong anti-proliferative activities and apoptosis-inducing effects on gynecologic cancer cells. The 11, 13-dehydro lactone moiety was critical for its anti-proliferative activity.

15.
Zhongguo Zhong Yao Za Zhi ; 40(24): 4840-6, 2015 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-27245032

RESUMO

The technique of liquisolid compress is a new technique developed in 1990s, which was considered to be the most promising technique to improve the dissolution of water-insoluble drugs. In this article, tanshinone II(A) and the extracts of the ester-solubility fractions were chosen as the model drugs to evaluate the effects of the liquisolid technique for enhancement of dissolution properties of tanshinone II(A). Several liquisolid tablets (LS) formulations containing different dosage of drugs and various liquid vehicle were pre-pared and for all the formulations, microcrystalline cellulose and silica were chosen as the carrier and coating materials to evaluate their flow properties, such as angle of repose, Carr's compressibility index and Hausner's ratio. The interaction between drug and excipients in prepared LS compacts were studied by differential scanning calorimetry(DSC) and X-ray powder diffraction (XRPD). The dissolution curves of tanshinone II(A) from liquisolid compacts were investigated to determine the technique's effect in improving the dissolution of tanshinone II(A) and its impacting factors. According to the results, the dissolution increased with the rise in the dissolution of the liquid-phase solvent. The R-value and drug dosage can significantly affect the drug release, but with less impact on active fractions. This indicated that liquisolid technique is a promising alternative for improvement of dissolution property of water-soluble drugs, and can make a synergistic effect with other ester-soluble constituents and bettern improve the release of tanshinone II(A). Therefore, the technique of liquisolid compress will have a better development prospect in traditional Chinese medicines.


Assuntos
Abietanos/química , Varredura Diferencial de Calorimetria , Solubilidade , Difração de Raios X
16.
Zhongguo Zhong Yao Za Zhi ; 38(14): 2302-5, 2013 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-24199559

RESUMO

The extraction of functional components from radix of Arnebia euchroma was optimized using orthogonal design based on the extraction yields of shikonin, and hydroxyl-naphthoquinone pigments. The data processing was carried out with the multiple guidelines grading method for optimizing the extraction condition. Compared with the traditional method (refluxing and ultrasonic extraction), the flash extraction method was more efficient The optimal conditions were as follows: 95% ethanol extract 3 times with 90 s for each. Under these conditions, the extraction yields of shikonin, and hydroxyl-naphthoquinone pigments were 93.16%, 93.89%, respectively, and the dry extract rate was 5.16%. In conclusion, the result showed that the flash extraction technology was appropriate, stable and feasible.


Assuntos
Boraginaceae/química , Medicamentos de Ervas Chinesas/química , Naftoquinonas/química , Pigmentos Biológicos/química , Extratos Vegetais/química
17.
Zhongguo Zhong Yao Za Zhi ; 38(22): 3880-7, 2013 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-24558869

RESUMO

To investigate the feasible application of the bioassay method in the evaluation of traditional Chinese medicine sustained-release preparations, develop a rapid drug-release evaluation method in vitro for multi-component preparations, and replace the biological activity determination method characterizing the overall behavior with the existing drug-release evaluation method for single component, in order to give better instruction for sustained-release preparations. HPLC was adopted to determine dissolution media, drug releasing rates, and accumulative releasing of active ingredients (salvianolic acid B, protocatechuic aldehyde and rosmarinic acid) of Salvia Miltiorrhiza hydrophilic gel matrix tablets. The ultraviolet spectroscopy was adopted to determine the antioxidant activity of release media, and evaluate the correlation between the drug-time curve of various drug components and the drug-time curve of the total antioxidant activity. The correlation coefficient between the drug-release curve of various components and the drug-time curve of the total antioxidant activity was higher than the critical value r 0.898 (P < 0.001). This indicated that the drug-release curve of the three phenolic acids and the drug-time curve of the total antioxidant activity had a good correlation in different conditions, such as dissolution media, release rates and component ratios. The bioassay method for determination was feasible, simple and convenient for preparation quality evaluation and prescription design in the place of in vitro dissolution.


Assuntos
Bioensaio/métodos , Preparações de Ação Retardada/química , Medicamentos de Ervas Chinesas/química , Salvia miltiorrhiza/química , Antioxidantes/química , Cinética , Solubilidade , Comprimidos/química
18.
Zhongguo Zhong Yao Za Zhi ; 38(19): 3373-7, 2013 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-24422411

RESUMO

To develop a HPLC method for determination of the concentration of scutellarin and scutellarin ethyl ester and their pharmacokinetics were also compared. 104 mg kg-1of scutellarin or 114. 5 mg kg-1 scutellarin ethyl ester were given at single dose by oral gavarge. Blood samples were collected from the jugular vein. Plasma concentration was measured by HPLC. The pharmacokinetic parameters were calculated with Winnonlin program. The plasma concentration-time profile of scutellarin and scutellarin ethyl ester were both fitted with non-compartment model and both were double peaks. The main pharmacokinetic parameters of scutellarin and scutellarin ethyl ester were as follows: Tmax Cmax and AUC0-t for scutellarin were (6 +/- 1.26) h, (321.55 +/-48.31) microg L-1 and (2 974 +/-753) h micro.g L-1; for scutellarin ethyl ester, Tmax, Cmax and AUC0-t were 0.5 h, (1 550.82 +/-219.75) +/- microg L- and (6 407 +/- 399) h microg L-1. The speed ingested into the blood of scutellarin ethyl ester was faster than scutellarin, and the bioavailability of scutellarin ethyl ester was two times higher than scutellarin.


Assuntos
Apigenina/farmacocinética , Flavonas/farmacocinética , Glucuronatos/farmacocinética , Glucuronídeos/farmacocinética , Animais , Cromatografia Líquida de Alta Pressão , Masculino , Ratos , Ratos Wistar
19.
Guang Pu Xue Yu Guang Pu Fen Xi ; 30(3): 595-8, 2010 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-20496667

RESUMO

The electroluminescence effect can be observed by the micro N-type wide-gap CBN semiconductor crystal under the condition of static eletric field. The micro N-type CBN crystal was fixed on the focus of the parabolic reflector of grating monochromator, and the maximum value of transmission ratio and the ideal signal-noise ratio can be obtained. Under the condition of static ectric-field intensity (4.7 x 10(6) V x cm(-1)), the blue-violet light-emitting spectrum of the CBN crystal was measured in the range from 350 to 450 nm. The construction of the CBN energy band, which was calculated with the First-principles method, the nonlinear relationship between current density and the ectric-field intensity that was measured and the phenomenon of electrical break-down were considered together to enable us to discuss the luminescence mechanism. Finally, the authors came up with the luminescence mechanism concerning electron migration from gamma energy valley to X energy valley. The large number of excited electrons we talked about were generated by polarization and breakdown of defect dipole before avalanche breakdown occurred.

20.
Guang Pu Xue Yu Guang Pu Fen Xi ; 28(7): 1569-72, 2008 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-18844162

RESUMO

UV absorption spectroscopy of artificial cubic boron nitride (cBN) single crystal flake, synthesized under high-temperature and high-pressure, was studied in the present paper. UV WINLAB spectrometer was used in the experiments, and MOLECULAR SPECTROSCOPY software was used for data analysis. The UV-cBN limit of 198 nm was showed in this test by a special fixture quartz sample. We calculated the energy gap by virtue of the formula: lambda0 = 1.24/E(g) (microm). The energy gap is 6. 26 eV. There are many viewpoints about the gap of cBN. By using the first-principles theory to calculate energy band structure and density of electronic states of cBN, an indirect transition due to electronics in valence band jumping into conduction band by absorbing photon can be confirmed. That leads to UV absorption. The method of calculation was based on the quantum mechanics of CASTEP in the commercial software package of Cerius2 in the Co. Accerlrys in the United States. The theory of CASTEP is based on local density approximation or gradient corrected LDA. The crystal parameter of cBN was input to the quantum mechanics of CASTEP in order to construct the crystal parameter model of cBN. We calculated the energy gap of cBN by the method of gradient corrected LDA. The method underestimates the value of nonconductor by about 1 to 2 eV. We gaot some opinions as follows: cBN is indirect band semiconductor. The energy gap is 4.76 eV, less than our experiment. The reason may be defect that we ignored in calculating process. It was reported that the results by first principles method of calculation of the band generally was less than the experimental results. This paper shows good UV characteristics of cBN because of the good agreement of experimental results with the cBN band width. That is a kind of development prospect of UV photo-electronic devices and high-temperature semiconductor devices.

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