Background:This study evaluates the efficacy of gabexate mesylate thermosensitive in-situ gel(GMTI) in the treatment of beagle grade Ⅲ pancreatic trauma(PT) with the assistance of contrast-enhanced ultrasound(CEUS) a...Background:This study evaluates the efficacy of gabexate mesylate thermosensitive in-situ gel(GMTI) in the treatment of beagle grade Ⅲ pancreatic trauma(PT) with the assistance of contrast-enhanced ultrasound(CEUS) and investigates its mechanism of action.Methods:A grade Ⅲ PT model consisting of 15 beagle dogs with severed main pancreatic ducts was created and treated with cephalic vein injection of gabexate mesylate(GM)(1.54mL/10kg,TID) and peripancreatic injection of GMTI(4.63 mL/10 kg,QD) guided by CEUS within 24h post-surgery.Ascites and serum levels of amylase(AMY),lipase(LPS),C-reactive protein(CRP),interleukin(IL)-6,tumor necrosis factor(TNF)-α,and urinary trypsinogen activating peptide(TAP) were detected by ELISA.Histopathological changes in the canine pancreas were observed by Hematoxylin and Eosin staining.Results:CEUS accurately displayed pancreatic lesions and guided catheterisation.Compared to the control group,the ascites was significantly reduced after treatment(p<0.01).AMY and LPS ascites significantly decreased on post-operative 1st and 2nd day(p<0.01).The levels of AMY,LPS,CRP,IL-6,and TNF-α in serum were decreased(p<0.05 or p <0.01).Urinary TAP was decreased 1 and 2 days after treatment(p<0.05or p<0.01,respectively).In the control group,pancreatic tissue necrosis was evident in the wound area.Normal glandular cell structures and fibrous tissue hyperplasia were observed in the wound area after GMTI treatment.The GMTI group performed better than the GM group in improving pancreatic histology and reducing AMY levels in the early post-operative period.Conclusion:Guided by CEUS,daily peripancreatic injections of GMTI in Beagles effectively inhibit pancreatic enzyme activity and aid in the adjuvant treatment of pancreatic trauma.展开更多
Objective:To evaluate the therapeutic effect of Tianma Gouteng Decoction combined with Betahistine Mesylate in patients with posterior circulation ischemic vertigo(PCI).Methods:Eighty-two patients with PCI who visited...Objective:To evaluate the therapeutic effect of Tianma Gouteng Decoction combined with Betahistine Mesylate in patients with posterior circulation ischemic vertigo(PCI).Methods:Eighty-two patients with PCI who visited the hospital from February 2024 to February 2025 were selected as samples and randomly divided into two groups.Group A received Tianma Gouteng Decoction combined with Betahistine Mesylate,while Group B received only Betahistine Mesylate.The efficacy,syndrome scores,hemodynamics,and quality of life indicators were compared between the two groups.Results:The efficacy of PCI treatment in Group A was higher than that in Group B(P<0.05).The syndrome scores in Group A were lower than those in Group B(P<0.05).The peak systolic velocity(PSV)of the basilar artery and left and right vertebral arteries in Group A were higher than those in Group B(P<0.05).The quality of life(SF-36)score in Group A was higher than that in Group B(P<0.05).Conclusion:Tianma Gouteng Decoction combined with Betahistine Mesylate is effective and feasible in the treatment of PCI,with improved hemodynamic indicators and reduced disease scores.展开更多
A 39-year-old male underwent distal gastrectomy for a high grade gastrointestinal stromal tumor(GIST) . Computed tomography(CT) and magnetic resonance imaging(MRI) 107 mo after the operation,revealed a cystic mass(14 ...A 39-year-old male underwent distal gastrectomy for a high grade gastrointestinal stromal tumor(GIST) . Computed tomography(CT) and magnetic resonance imaging(MRI) 107 mo after the operation,revealed a cystic mass(14 cm in diameter) and a solid mass(9 cm in diameter) in the right and left lobes of the liver,respectively. A biopsy specimen of the solid mass showed a liver metastasis of GIST. The patient received imatinib mesylate(IM) treatment,400 mg/day orally. Following the IM treatment for a period of 35 mo,the patient underwent partial hepatectomy(S4 + S5) . The effect of IM on the metastatic lesions was interpreted as pathologic complete response(CR) . Pathologically verified cases showing therapeutic efficacy of IM have been rarely reported.展开更多
Nafamostat mesylate,an apparent soi-disant panacea of sorts,is widely used to anticoagulate patients undergoing hemodialysis or cardiopulmonary bypass,mitigate the inflammatory response in patients diagnosed with acut...Nafamostat mesylate,an apparent soi-disant panacea of sorts,is widely used to anticoagulate patients undergoing hemodialysis or cardiopulmonary bypass,mitigate the inflammatory response in patients diagnosed with acute pancreatitis,and reverse the coagulopathy of patients experiencing the commonly preterminal disseminated intravascular coagulation in the Far East.The serine protease inhibitor nafamostat mesylate exhibits significant neuroprotective effects in the setting of neurovascular ischemia.Nafamostat mesylate generates neuroprotective effects by attenuating the enzymatic activity of serine proteases,neuroinflammatory signaling cascades,and the endoplasmic reticulum stress responses,downregulating excitotoxic transient receptor membrane channel subfamily 7 cationic currents,modulating the activity of intracellular signal transduction pathways,and supporting neuronal survival brain-derived neurotrophic factor/TrkB/ERK1/2/CREB,nuclear factor kappa B.The effects collectively reduce neuronal necrosis and apoptosis and prevent ischemia mediated disruption of blood-brain barrier microarchitecture.Investigational clinical applications of these compounds may mitigate ischemic reperfusion injury in patients undergoing cardiac,hepatic,renal,or intestinal transplant,preventing allograft rejection,and treating solid organ malignancies.Neuroprotective effects mediated by nafamostat mesylate support the wise conduct of randomized prospective controlled trials in Western countries to evaluate the clinical utility of this compound.展开更多
Gastrointestinal stromal tumors （GISTs） occur most frequently in the stomach.Diagnosis of gastric GIST is not always clear before surgery.Flexible endoscopy may suggest the nature of the lesion （a bulky tumor with ...Gastrointestinal stromal tumors （GISTs） occur most frequently in the stomach.Diagnosis of gastric GIST is not always clear before surgery.Flexible endoscopy may suggest the nature of the lesion （a bulky tumor with preserved mucosa）; however,biopsy is rarely diagnostic.Therefore,diagnostic medication with safe drugs may provide a feasible way under such conditions after an informed consent is obtained.Based on the excellent efficacy of imatinib mesylate （IM） in the treatment of GIST,we successfully applied it in the diagnostic medication of two patients with clinically suspected gastric stromal tumors.In conclusion,the diagnostic medication with IM can be an alternative option for patients with suspected GIST that can not be confirmed pathologically.展开更多
AIM： Most gastrointestinal stromal tumors （GISTs） express constitutively activated mutant isoforms of kit kinase or platelet-derived growth factor receptor alpha （PDGFRA）, which are potential therapeutic targets ...AIM： Most gastrointestinal stromal tumors （GISTs） express constitutively activated mutant isoforms of kit kinase or platelet-derived growth factor receptor alpha （PDGFRA）, which are potential therapeutic targets for imatinib mesylate （Glivec）. Partial response occurred in almost two thirds of GIST patients treated with Glivec. However, complete response （CR） after Glivec therapy was sporadically reported. Here we illustrated advanced GIST patients with CR after Glivec treatment. METHODS： Between January 2001 and June 2005, 42 advanced GIST patients were treated with Glivec. Patients were administered 400 mg of Glivec in 100-mg capsules, taken orally daily with food. The response of the tumor to Glivec was evaluated after one month, three months, and every three months thereafter or whenever medical need was indicated. Each tumor of patients was investigated for mutations of kit or PDGFRA. RESULTS： The median follow-up time of the 42 ad-vanced GIST patients treated with Glivec was 16.9 months （range, 1.0- 47.0 months）. Overall, 3 patients had complete response CR （7.1%）, 26 partial response （67.8%）, 5 stationary disease （11.9%）, and 3 progressive disease （11.9%）. The median duration of Glivec administration for the three patients was 36 months （range, 23-36 months）. The median time to CR after Glivec treatment was 20 months （range, 9-26 months）. Deletion and insertion mutations of c-kit exon 11 and insertion mutation of c-kit exon 9 were found in two cases and one case, respectively. CONCLUSION： Complete response （CR） can be achieved in selected advanced GIST patients treated with Glivec. The median time to CR after Glivec treatment was 20 months. Deletion and insertion mutations of kit exon 11 and insertion mutation of kit exon 9 contribute to the genetic features in these selected cases.展开更多
The binding of pefloxacin mesylate （PFLX） to bovine lactoferrin （BLf） and human serum albumin （HSA） in dilute aqueous solution was studied using fluorescence spectra and absorbance spectra. The binding constant ...The binding of pefloxacin mesylate （PFLX） to bovine lactoferrin （BLf） and human serum albumin （HSA） in dilute aqueous solution was studied using fluorescence spectra and absorbance spectra. The binding constant K and the binding sites n were obtained by fluorescence quenching method. The binding distance r and energy-transfer efficiency E between pefloxacin mesylate and bovine lactoferrin as well as human serum albumin were also obtained according to the mechanism of Forster-type dipole-dipole nonradiative energy-transfer. The effects of pefloxacin mesylate on the conformations of bovine lactoferrin and human serum albumin were also analyzed using synchronous fluorescence spectroscopy.展开更多
Gastrointestinal stromal tumors (GISTs) are rare tumors, which represent approximately 1% of the neoplasms of the gastrointestinal tract. These tumors rarely give extra-abdominal metastases. However, their clinical ou...Gastrointestinal stromal tumors (GISTs) are rare tumors, which represent approximately 1% of the neoplasms of the gastrointestinal tract. These tumors rarely give extra-abdominal metastases. However, their clinical outcome is potentially adverse. In some rare cases, co- existance of GISTs with other malignancies has been reported. Here we present a case of a 74-year old male with GIST, which was managed by surgical resection. Fourteen months later, the patient presented with liver metastases and imatinib mesylated was administered. During treatment, the patient reported skeletal pain and plane X-rays revealed osteolytic bone lesions. Further investigation revealed the presence of multiple myeloma. To the best of our knowledge, this is the first report of the co-existence of multiple myeloma (MM) with GIST.展开更多
AIM: To evaluate and characterize the patterns of disease progression of metastatic or unresectable gastrointestinal stromal tumor (GIST) treated with imatinib mesylate, and to determine the prognostic significance as...AIM: To evaluate and characterize the patterns of disease progression of metastatic or unresectable gastrointestinal stromal tumor (GIST) treated with imatinib mesylate, and to determine the prognostic significance associated with disease progression. METHODS: Clinical data and computed tomography (CT) images were retrospectively reviewed in 17 GIST patients who were treated with imatinib mesylate from October 2002 to October 2006. Apart from using size measurement for evaluation of tumor response [Response Evaluation Criteria in Solid Tumors (RECIST) criteria], patterns of CT changes during treatment were evaluated and correlated with clinical data. RESULTS: There were eight non-responders and nine responders. Five patterns of CT change during treatment were found: focal progression (FP), generalized progression (GP), generalized cystic change (GC), new cystic lesion (NC) and new solid lesion (NS). At the end of study, all non-responders showed GP, whereas responders showed cystic change (GC and NC) and response according to RECIST criteria. Overall survival was significantly better in patients with cystic change or response within the RECIST criteria compared with GP patients (P = 0.0271). CONCLUSION: Various patterns of CT change in patients with GIST who responded to imatinib mesylate were demonstrated, and might determine the prognosis of the disease. A combination of RECIST criteria and pattern of CT change are proposed for response evaluation in GIST.展开更多
BACKGROUND Recent studies on dialysis anticoagulation therapy in patients with renal failure have shown that Nafamostat mesylate,a broad-spectrum potent serine protease inhibitor,has strong anticoagulation and anti-fi...BACKGROUND Recent studies on dialysis anticoagulation therapy in patients with renal failure have shown that Nafamostat mesylate,a broad-spectrum potent serine protease inhibitor,has strong anticoagulation and anti-fiber activity.AIM To evaluate the efficacy and safety of Nafamostat mesylate in patients with end-stage renal failure.METHODS Seventy-five patients with end-stage renal failure who received hemodialysis at our hospital between January 2020 and August 2021 were selected and divided into the observation group(Nafamostat mesylate for injection,n=33)and control group(heparin sodium injection,n=32).General patient data,indicators of clinical efficacy,dialyzer hemocoagulation parameters,coagulation function indices,and hemoglobin concentration and platelet count before and after treatment,and the occurrence of adverse reactions after treatment were compared between the two groups.RESULTS The two groups showed no significant differences in general patient data(P>0.05).The post-treatment effectiveness rate in the control group was lower than that in the observation group(P<0.05).The two groups showed no significant difference in the number of patients in grade I(P>0.05),while the number of patients in grade 0 was lower in the control group,and the number of patients in grades II and III was higher in the control group(P<0.05).The post-treatment prothrombin time,activated partial thromboplastin time,thrombin time,and international normalized ratio values in the control group were higher than those in the observation group,while the fibrinogen level in the control group was lower than that in the observation group(P<0.05).The two groups showed no significant difference in the platelet count and hemoglobin level before and after treatment(P>0.05).The total number of post-treatment adverse reactions in the observation group was lower than that in the control group(P<0.05).CONCLUSION Treatment of patients showing end-stage renal failure with Nafamostat mesylate can significantly improve therapeutic efficacy and has high safety and clinical value.展开更多
Objective:To evaluate the effect of imatinib mesylate on cell viability,anti cancer effect through modulation of KAI1/CD82 gene expression in breast cancer MCF-7 cell line.Methods:The effects of imatinib mesylate on c...Objective:To evaluate the effect of imatinib mesylate on cell viability,anti cancer effect through modulation of KAI1/CD82 gene expression in breast cancer MCF-7 cell line.Methods:The effects of imatinib mesylate on cell viability in MCF-7 cell line were assessed using MTT assay and IC_(50)value was determined.GAPDH and KAI1/CD82 were selected as reference and target genes,respectively.Quantitative real time PCR technique was applied for investigation of KAI1/CD82 gene expression in human breast cancer MCF-7 cells.Subsequently,the quantity of KAI1 compared to GAPDH gene expressions were analyzed using the formula;2^(-DDCt).Results:Imatinib was showed to have a dose-dependent inhibitory effect on the viability of MCF-7 cells.CD82/GAPDH gene expression ratios were 1.322±0.030(P>0.05),2.052±0.200(P<0.05),2.151±0.270(P<0.05)for 10,20 and 40 mmol/L of imatinib concentrations.Conclusions:Based on the present data,imatinib mesylate might modulate metastasis by up-regulating KAI1/CD82 gene expression in human breast MCF-7 cancer cell line.展开更多
治疗转移性乳腺癌新药甲磺酸阿贝西尼(abemaciclib mesylate)是周期蛋白依赖激酶(CDK)4/6抑制药,由美国礼来公司(Eli Lilly and company)研发,曾用名为Bemaciclib,用于治疗激素受体(HR)阳性(HR+)及人表皮生长因子受体2(HER2)阴性(HER2-)...治疗转移性乳腺癌新药甲磺酸阿贝西尼(abemaciclib mesylate)是周期蛋白依赖激酶(CDK)4/6抑制药,由美国礼来公司(Eli Lilly and company)研发,曾用名为Bemaciclib,用于治疗激素受体(HR)阳性(HR+)及人表皮生长因子受体2(HER2)阴性(HER2-),经内分泌治疗后乳腺癌已进展或转移的成人晚期患者。阿贝西尼于2015年10月9日获得美国食品药品管理局(FDA)突破性疗法的认定,给予在HR+/HER2-乳腺癌患者中优先评审资格,2017年9月28日批准上市,商品名为Verzenio。该文对甲磺酸阿贝西尼的非临床和临床药理毒理学、临床研究、不良反应、适应证、剂量与用法、用药注意事项及知识产权状态和国内外研究进展等进行介绍。展开更多
Gastrointestinal stromal tumor （GIST） is the most common mesenchymal malignancy of the gastrointestinal tract.GISTs may coexist with different types of cancer,either synchronous or metachronous （1）.Most GISTs deve...Gastrointestinal stromal tumor （GIST） is the most common mesenchymal malignancy of the gastrointestinal tract.GISTs may coexist with different types of cancer,either synchronous or metachronous （1）.Most GISTs develop in a sporadic fashion,but familial occurrence,such as neurofibromatosis and Carney-triad,has also been reported （2）.The overall frequency of second tumors in different series varied from 4.5% to 33%.The most frequent types of GIST-associated cancers were gastrointestinal carcinomas （47%）,lymphoma/leukemia （7%）,carcinomas of prostate （9%）,breast （7%）,kidney （6%）,lung （5%）,female genital tract （5%）,carcinoid tumors （3%）,soft tissue and bone sarcomas （3%）,malignant melanoma （2%） and seminoma （1%） （1,3-5）.展开更多
Continuous renal replacement therapy (CRRT) is the preferred dialysis modality in critical care settings for patients with hemodynamic instability. Nafamostat mesylate (NM) is an anticoagulant commonly used (mainly in...Continuous renal replacement therapy (CRRT) is the preferred dialysis modality in critical care settings for patients with hemodynamic instability. Nafamostat mesylate (NM) is an anticoagulant commonly used (mainly in Japan) during CRRT in patients with high bleeding risk. In this study, we evaluated the pharmacokinetics of NM during CRRT. Patients undergoing CRRT therapy and using NM as the anticoagulant in the intensive care unit were enrolled in the study. Blood was collected from the CRRT circuit just after blood removal, just before and after the membrane for CRRT, and from the filtrates after the membrane. NM concentrations were measured using high-performance liquid chromatography. NM was detected in the intracorporeal circulation during CRRT in some cases, and liver enzymes were severely elevated in almost all of the cases. Coagulation time was prolonged even before the initiation of NM administration in these cases and may be associated with liver damage. This study suggests that NM dosage should take into account liver damage assessed by elevated liver enzymes.展开更多
A simple and straightforward method for the determination of dolasetron mesylate(DM) in aqueous solution was developed based on the fluorescence quenching of 3-Mercaptopropionic acid(MPA) capped Cd S quantum dots(QDs)...A simple and straightforward method for the determination of dolasetron mesylate(DM) in aqueous solution was developed based on the fluorescence quenching of 3-Mercaptopropionic acid(MPA) capped Cd S quantum dots(QDs).The structure,morphology,and optical properties of synthesized QDs were characterized by using UV-Vis absorption spectroscopy,fluorescence spectroscopy,transmission electron microscopy(TEM) and dynamic light scattering(DLS) measurements.Under the optimum conditions,the MPA-Cd S QDs fluorescence probe offered good sensitivity and selectivity for detecting DM.The probe provided a highly specific selectivity and a linear detection of DM in the range of 2–40 μg/m L with detection limit(LOD) 1.512 μg/m L.The common excipients did not interfere in the proposed method.The fluorescence quenching mechanism of Cd S QDs is also discussed.The developed sensor was applied to the quantification of DM in urine and human serum sample with satisfactory results.展开更多
Objective： Cancer stromal fibroblasts are important members of the cancer microenvironment. In this study, we determined the effect of sunitinib, a small molecule tyrosine kinase inhibitor, on the primary human colon...Objective： Cancer stromal fibroblasts are important members of the cancer microenvironment. In this study, we determined the effect of sunitinib, a small molecule tyrosine kinase inhibitor, on the primary human colonic fibroblasts. Methods： Cell cycle analysis and cell proliferation assays were performed to evaluate the inhibitory effect of sunitinib in vitro. Western-blot analysis was performed to evaluate variations in the levels of phosphorylated plateletderived growth factor receptor β （PDGFR-β）, Akt, and ERK proteins. Co-injection of SW620 cells and colonic fibreblasts in nude mice was employed to test anti-growth efficacy in vivo. Results： Sunitinib was found to effectively inhibit the growth of primary colonic fibroblasts. Low-dose sunitinib blocked the PDGF-BB-induced cell proliferation and PDGFR-β signaling. Co-injection of SW620 cells and colonic fibroblasts in nude mice generated greater tumor volumes than single injection of SW620 cells. Sunitinib treatment inhibited the SW620 cell＋colonic fibroblast tumor growth more effectively than treatment of 5-fluorouracil. Conclusions： Sunitinib mesylate inhibited the proliferation of primary human colonic fibroblasts through target-inhibited PDGFR signaling in vitro and in vivo.展开更多
Nafamostat mesylate is a serine protease inhibitor used in the treatment of acute pancreatitis.The impurities in nafamostat mesylate,the active pharmaceutical ingredient(API),were profiled via high performance liquid ...Nafamostat mesylate is a serine protease inhibitor used in the treatment of acute pancreatitis.The impurities in nafamostat mesylate,the active pharmaceutical ingredient(API),were profiled via high performance liquid chromatography tandem ion trap coupled with time-of-flight mass spectrometer(HPLC-IT-TOF/MS).The chromatography was performed on an ACE-3 C18 column(200 mm4.6 mm,3 mm)using methanol and 0.1%formic acid in purified water as mobile phase at a flow rate of 1.0 mL/min.The ions were detected by IT-TOF/MS with a full-scan mass analysis from m/z 100 to 800.In total,eleven impurities were detected in nafamostat mesylate API.The impurity profile was estimated based on the HPLC-IT-TOF/MS data,including accurate masses,MSn fingerprints of fragmentation pathways and a series of double-charged ions.Finally,seven impurities were identified and reported for the first time.The results will provide technical support for the quality control and clinical safety of nafamostat mesylate.展开更多
The structures of solid dosage forms determine their release behaviors and are critical attributes for the design and evaluation of the solid dosage forms.Here,the 3D structures of doxazosin mesylate sustained-release...The structures of solid dosage forms determine their release behaviors and are critical attributes for the design and evaluation of the solid dosage forms.Here,the 3D structures of doxazosin mesylate sustained-release tablets were parallelly assessed by micro-computed tomography(micro-CT).There were no significant differences observed in the release profiles between the RLD and the generic formulation in the conventional dissolution,but the generic preparation released slightly faster in media with ethanol during an alcohol-induced dose-dumping test.With their 3D structures obtained via micro-CT determination,the unique release behaviors of both RLD and the generic were investigated to reveal the effects of internal fine structure on the release kinetics.The structural parameters for both preparations were similar in conventional dissolution test,while the dissolutions in ethanol media showed some distinctions between RLD and generic preparations due to their static and dynamic structures.Furthermore,the findings revealed that the presence of ethanol accelerated dissolution and induced changes in internal structure of both RLD and generic preparations.Moreover,structure parameters like volume and area of outer contour,remaining solid volume and cavity volumewere not equivalent between the two formulations in 40%ethanol.In conclusion,the structure data obtained from this study provided valuable insights into the diverse release behaviors observed in various modified-release formulations in drug development and quality control.展开更多
文摘Background:This study evaluates the efficacy of gabexate mesylate thermosensitive in-situ gel(GMTI) in the treatment of beagle grade Ⅲ pancreatic trauma(PT) with the assistance of contrast-enhanced ultrasound(CEUS) and investigates its mechanism of action.Methods:A grade Ⅲ PT model consisting of 15 beagle dogs with severed main pancreatic ducts was created and treated with cephalic vein injection of gabexate mesylate(GM)(1.54mL/10kg,TID) and peripancreatic injection of GMTI(4.63 mL/10 kg,QD) guided by CEUS within 24h post-surgery.Ascites and serum levels of amylase(AMY),lipase(LPS),C-reactive protein(CRP),interleukin(IL)-6,tumor necrosis factor(TNF)-α,and urinary trypsinogen activating peptide(TAP) were detected by ELISA.Histopathological changes in the canine pancreas were observed by Hematoxylin and Eosin staining.Results:CEUS accurately displayed pancreatic lesions and guided catheterisation.Compared to the control group,the ascites was significantly reduced after treatment(p<0.01).AMY and LPS ascites significantly decreased on post-operative 1st and 2nd day(p<0.01).The levels of AMY,LPS,CRP,IL-6,and TNF-α in serum were decreased(p<0.05 or p <0.01).Urinary TAP was decreased 1 and 2 days after treatment(p<0.05or p<0.01,respectively).In the control group,pancreatic tissue necrosis was evident in the wound area.Normal glandular cell structures and fibrous tissue hyperplasia were observed in the wound area after GMTI treatment.The GMTI group performed better than the GM group in improving pancreatic histology and reducing AMY levels in the early post-operative period.Conclusion:Guided by CEUS,daily peripancreatic injections of GMTI in Beagles effectively inhibit pancreatic enzyme activity and aid in the adjuvant treatment of pancreatic trauma.
文摘Objective:To evaluate the therapeutic effect of Tianma Gouteng Decoction combined with Betahistine Mesylate in patients with posterior circulation ischemic vertigo(PCI).Methods:Eighty-two patients with PCI who visited the hospital from February 2024 to February 2025 were selected as samples and randomly divided into two groups.Group A received Tianma Gouteng Decoction combined with Betahistine Mesylate,while Group B received only Betahistine Mesylate.The efficacy,syndrome scores,hemodynamics,and quality of life indicators were compared between the two groups.Results:The efficacy of PCI treatment in Group A was higher than that in Group B(P<0.05).The syndrome scores in Group A were lower than those in Group B(P<0.05).The peak systolic velocity(PSV)of the basilar artery and left and right vertebral arteries in Group A were higher than those in Group B(P<0.05).The quality of life(SF-36)score in Group A was higher than that in Group B(P<0.05).Conclusion:Tianma Gouteng Decoction combined with Betahistine Mesylate is effective and feasible in the treatment of PCI,with improved hemodynamic indicators and reduced disease scores.
文摘A 39-year-old male underwent distal gastrectomy for a high grade gastrointestinal stromal tumor(GIST) . Computed tomography(CT) and magnetic resonance imaging(MRI) 107 mo after the operation,revealed a cystic mass(14 cm in diameter) and a solid mass(9 cm in diameter) in the right and left lobes of the liver,respectively. A biopsy specimen of the solid mass showed a liver metastasis of GIST. The patient received imatinib mesylate(IM) treatment,400 mg/day orally. Following the IM treatment for a period of 35 mo,the patient underwent partial hepatectomy(S4 + S5) . The effect of IM on the metastatic lesions was interpreted as pathologic complete response(CR) . Pathologically verified cases showing therapeutic efficacy of IM have been rarely reported.
文摘Nafamostat mesylate,an apparent soi-disant panacea of sorts,is widely used to anticoagulate patients undergoing hemodialysis or cardiopulmonary bypass,mitigate the inflammatory response in patients diagnosed with acute pancreatitis,and reverse the coagulopathy of patients experiencing the commonly preterminal disseminated intravascular coagulation in the Far East.The serine protease inhibitor nafamostat mesylate exhibits significant neuroprotective effects in the setting of neurovascular ischemia.Nafamostat mesylate generates neuroprotective effects by attenuating the enzymatic activity of serine proteases,neuroinflammatory signaling cascades,and the endoplasmic reticulum stress responses,downregulating excitotoxic transient receptor membrane channel subfamily 7 cationic currents,modulating the activity of intracellular signal transduction pathways,and supporting neuronal survival brain-derived neurotrophic factor/TrkB/ERK1/2/CREB,nuclear factor kappa B.The effects collectively reduce neuronal necrosis and apoptosis and prevent ischemia mediated disruption of blood-brain barrier microarchitecture.Investigational clinical applications of these compounds may mitigate ischemic reperfusion injury in patients undergoing cardiac,hepatic,renal,or intestinal transplant,preventing allograft rejection,and treating solid organ malignancies.Neuroprotective effects mediated by nafamostat mesylate support the wise conduct of randomized prospective controlled trials in Western countries to evaluate the clinical utility of this compound.
基金supported by WU JIEPING Medical Foundation(No.WJP-320.6700.09010)
文摘Gastrointestinal stromal tumors （GISTs） occur most frequently in the stomach.Diagnosis of gastric GIST is not always clear before surgery.Flexible endoscopy may suggest the nature of the lesion （a bulky tumor with preserved mucosa）; however,biopsy is rarely diagnostic.Therefore,diagnostic medication with safe drugs may provide a feasible way under such conditions after an informed consent is obtained.Based on the excellent efficacy of imatinib mesylate （IM） in the treatment of GIST,we successfully applied it in the diagnostic medication of two patients with clinically suspected gastric stromal tumors.In conclusion,the diagnostic medication with IM can be an alternative option for patients with suspected GIST that can not be confirmed pathologically.
文摘AIM： Most gastrointestinal stromal tumors （GISTs） express constitutively activated mutant isoforms of kit kinase or platelet-derived growth factor receptor alpha （PDGFRA）, which are potential therapeutic targets for imatinib mesylate （Glivec）. Partial response occurred in almost two thirds of GIST patients treated with Glivec. However, complete response （CR） after Glivec therapy was sporadically reported. Here we illustrated advanced GIST patients with CR after Glivec treatment. METHODS： Between January 2001 and June 2005, 42 advanced GIST patients were treated with Glivec. Patients were administered 400 mg of Glivec in 100-mg capsules, taken orally daily with food. The response of the tumor to Glivec was evaluated after one month, three months, and every three months thereafter or whenever medical need was indicated. Each tumor of patients was investigated for mutations of kit or PDGFRA. RESULTS： The median follow-up time of the 42 ad-vanced GIST patients treated with Glivec was 16.9 months （range, 1.0- 47.0 months）. Overall, 3 patients had complete response CR （7.1%）, 26 partial response （67.8%）, 5 stationary disease （11.9%）, and 3 progressive disease （11.9%）. The median duration of Glivec administration for the three patients was 36 months （range, 23-36 months）. The median time to CR after Glivec treatment was 20 months （range, 9-26 months）. Deletion and insertion mutations of c-kit exon 11 and insertion mutation of c-kit exon 9 were found in two cases and one case, respectively. CONCLUSION： Complete response （CR） can be achieved in selected advanced GIST patients treated with Glivec. The median time to CR after Glivec treatment was 20 months. Deletion and insertion mutations of kit exon 11 and insertion mutation of kit exon 9 contribute to the genetic features in these selected cases.
基金Project (No. 20173050) supported by the National Natural ScienceFoundation of China
文摘The binding of pefloxacin mesylate （PFLX） to bovine lactoferrin （BLf） and human serum albumin （HSA） in dilute aqueous solution was studied using fluorescence spectra and absorbance spectra. The binding constant K and the binding sites n were obtained by fluorescence quenching method. The binding distance r and energy-transfer efficiency E between pefloxacin mesylate and bovine lactoferrin as well as human serum albumin were also obtained according to the mechanism of Forster-type dipole-dipole nonradiative energy-transfer. The effects of pefloxacin mesylate on the conformations of bovine lactoferrin and human serum albumin were also analyzed using synchronous fluorescence spectroscopy.
文摘Gastrointestinal stromal tumors (GISTs) are rare tumors, which represent approximately 1% of the neoplasms of the gastrointestinal tract. These tumors rarely give extra-abdominal metastases. However, their clinical outcome is potentially adverse. In some rare cases, co- existance of GISTs with other malignancies has been reported. Here we present a case of a 74-year old male with GIST, which was managed by surgical resection. Fourteen months later, the patient presented with liver metastases and imatinib mesylated was administered. During treatment, the patient reported skeletal pain and plane X-rays revealed osteolytic bone lesions. Further investigation revealed the presence of multiple myeloma. To the best of our knowledge, this is the first report of the co-existence of multiple myeloma (MM) with GIST.
文摘AIM: To evaluate and characterize the patterns of disease progression of metastatic or unresectable gastrointestinal stromal tumor (GIST) treated with imatinib mesylate, and to determine the prognostic significance associated with disease progression. METHODS: Clinical data and computed tomography (CT) images were retrospectively reviewed in 17 GIST patients who were treated with imatinib mesylate from October 2002 to October 2006. Apart from using size measurement for evaluation of tumor response [Response Evaluation Criteria in Solid Tumors (RECIST) criteria], patterns of CT changes during treatment were evaluated and correlated with clinical data. RESULTS: There were eight non-responders and nine responders. Five patterns of CT change during treatment were found: focal progression (FP), generalized progression (GP), generalized cystic change (GC), new cystic lesion (NC) and new solid lesion (NS). At the end of study, all non-responders showed GP, whereas responders showed cystic change (GC and NC) and response according to RECIST criteria. Overall survival was significantly better in patients with cystic change or response within the RECIST criteria compared with GP patients (P = 0.0271). CONCLUSION: Various patterns of CT change in patients with GIST who responded to imatinib mesylate were demonstrated, and might determine the prognosis of the disease. A combination of RECIST criteria and pattern of CT change are proposed for response evaluation in GIST.
文摘BACKGROUND Recent studies on dialysis anticoagulation therapy in patients with renal failure have shown that Nafamostat mesylate,a broad-spectrum potent serine protease inhibitor,has strong anticoagulation and anti-fiber activity.AIM To evaluate the efficacy and safety of Nafamostat mesylate in patients with end-stage renal failure.METHODS Seventy-five patients with end-stage renal failure who received hemodialysis at our hospital between January 2020 and August 2021 were selected and divided into the observation group(Nafamostat mesylate for injection,n=33)and control group(heparin sodium injection,n=32).General patient data,indicators of clinical efficacy,dialyzer hemocoagulation parameters,coagulation function indices,and hemoglobin concentration and platelet count before and after treatment,and the occurrence of adverse reactions after treatment were compared between the two groups.RESULTS The two groups showed no significant differences in general patient data(P>0.05).The post-treatment effectiveness rate in the control group was lower than that in the observation group(P<0.05).The two groups showed no significant difference in the number of patients in grade I(P>0.05),while the number of patients in grade 0 was lower in the control group,and the number of patients in grades II and III was higher in the control group(P<0.05).The post-treatment prothrombin time,activated partial thromboplastin time,thrombin time,and international normalized ratio values in the control group were higher than those in the observation group,while the fibrinogen level in the control group was lower than that in the observation group(P<0.05).The two groups showed no significant difference in the platelet count and hemoglobin level before and after treatment(P>0.05).The total number of post-treatment adverse reactions in the observation group was lower than that in the control group(P<0.05).CONCLUSION Treatment of patients showing end-stage renal failure with Nafamostat mesylate can significantly improve therapeutic efficacy and has high safety and clinical value.
基金Supported by East Tehran Branch,Islamic Azad University(Grant No.923064)
文摘Objective:To evaluate the effect of imatinib mesylate on cell viability,anti cancer effect through modulation of KAI1/CD82 gene expression in breast cancer MCF-7 cell line.Methods:The effects of imatinib mesylate on cell viability in MCF-7 cell line were assessed using MTT assay and IC_(50)value was determined.GAPDH and KAI1/CD82 were selected as reference and target genes,respectively.Quantitative real time PCR technique was applied for investigation of KAI1/CD82 gene expression in human breast cancer MCF-7 cells.Subsequently,the quantity of KAI1 compared to GAPDH gene expressions were analyzed using the formula;2^(-DDCt).Results:Imatinib was showed to have a dose-dependent inhibitory effect on the viability of MCF-7 cells.CD82/GAPDH gene expression ratios were 1.322±0.030(P>0.05),2.052±0.200(P<0.05),2.151±0.270(P<0.05)for 10,20 and 40 mmol/L of imatinib concentrations.Conclusions:Based on the present data,imatinib mesylate might modulate metastasis by up-regulating KAI1/CD82 gene expression in human breast MCF-7 cancer cell line.
文摘治疗转移性乳腺癌新药甲磺酸阿贝西尼(abemaciclib mesylate)是周期蛋白依赖激酶(CDK)4/6抑制药,由美国礼来公司(Eli Lilly and company)研发,曾用名为Bemaciclib,用于治疗激素受体(HR)阳性(HR+)及人表皮生长因子受体2(HER2)阴性(HER2-),经内分泌治疗后乳腺癌已进展或转移的成人晚期患者。阿贝西尼于2015年10月9日获得美国食品药品管理局(FDA)突破性疗法的认定,给予在HR+/HER2-乳腺癌患者中优先评审资格,2017年9月28日批准上市,商品名为Verzenio。该文对甲磺酸阿贝西尼的非临床和临床药理毒理学、临床研究、不良反应、适应证、剂量与用法、用药注意事项及知识产权状态和国内外研究进展等进行介绍。
文摘Gastrointestinal stromal tumor （GIST） is the most common mesenchymal malignancy of the gastrointestinal tract.GISTs may coexist with different types of cancer,either synchronous or metachronous （1）.Most GISTs develop in a sporadic fashion,but familial occurrence,such as neurofibromatosis and Carney-triad,has also been reported （2）.The overall frequency of second tumors in different series varied from 4.5% to 33%.The most frequent types of GIST-associated cancers were gastrointestinal carcinomas （47%）,lymphoma/leukemia （7%）,carcinomas of prostate （9%）,breast （7%）,kidney （6%）,lung （5%）,female genital tract （5%）,carcinoid tumors （3%）,soft tissue and bone sarcomas （3%）,malignant melanoma （2%） and seminoma （1%） （1,3-5）.
文摘Continuous renal replacement therapy (CRRT) is the preferred dialysis modality in critical care settings for patients with hemodynamic instability. Nafamostat mesylate (NM) is an anticoagulant commonly used (mainly in Japan) during CRRT in patients with high bleeding risk. In this study, we evaluated the pharmacokinetics of NM during CRRT. Patients undergoing CRRT therapy and using NM as the anticoagulant in the intensive care unit were enrolled in the study. Blood was collected from the CRRT circuit just after blood removal, just before and after the membrane for CRRT, and from the filtrates after the membrane. NM concentrations were measured using high-performance liquid chromatography. NM was detected in the intracorporeal circulation during CRRT in some cases, and liver enzymes were severely elevated in almost all of the cases. Coagulation time was prolonged even before the initiation of NM administration in these cases and may be associated with liver damage. This study suggests that NM dosage should take into account liver damage assessed by elevated liver enzymes.
基金the UGC,New Delhi,India for providing the major research project(F.No.42-368/2013(SR))Department of Science and Technology(DST),New Delhi,India for financial assistance to the Department of Chemistry,Shivaji University,Kolhapur,India under FIST level-I Program(SR/FST/CST-008/2011)
文摘A simple and straightforward method for the determination of dolasetron mesylate(DM) in aqueous solution was developed based on the fluorescence quenching of 3-Mercaptopropionic acid(MPA) capped Cd S quantum dots(QDs).The structure,morphology,and optical properties of synthesized QDs were characterized by using UV-Vis absorption spectroscopy,fluorescence spectroscopy,transmission electron microscopy(TEM) and dynamic light scattering(DLS) measurements.Under the optimum conditions,the MPA-Cd S QDs fluorescence probe offered good sensitivity and selectivity for detecting DM.The probe provided a highly specific selectivity and a linear detection of DM in the range of 2–40 μg/m L with detection limit(LOD) 1.512 μg/m L.The common excipients did not interfere in the proposed method.The fluorescence quenching mechanism of Cd S QDs is also discussed.The developed sensor was applied to the quantification of DM in urine and human serum sample with satisfactory results.
基金supported by the National Natural Science Foundation of China(Nos.81071801 and 81272455)the Zhejiang Provincial Natural Science Foundation of China(No.R2100071)
文摘Objective： Cancer stromal fibroblasts are important members of the cancer microenvironment. In this study, we determined the effect of sunitinib, a small molecule tyrosine kinase inhibitor, on the primary human colonic fibroblasts. Methods： Cell cycle analysis and cell proliferation assays were performed to evaluate the inhibitory effect of sunitinib in vitro. Western-blot analysis was performed to evaluate variations in the levels of phosphorylated plateletderived growth factor receptor β （PDGFR-β）, Akt, and ERK proteins. Co-injection of SW620 cells and colonic fibreblasts in nude mice was employed to test anti-growth efficacy in vivo. Results： Sunitinib was found to effectively inhibit the growth of primary colonic fibroblasts. Low-dose sunitinib blocked the PDGF-BB-induced cell proliferation and PDGFR-β signaling. Co-injection of SW620 cells and colonic fibroblasts in nude mice generated greater tumor volumes than single injection of SW620 cells. Sunitinib treatment inhibited the SW620 cell＋colonic fibroblast tumor growth more effectively than treatment of 5-fluorouracil. Conclusions： Sunitinib mesylate inhibited the proliferation of primary human colonic fibroblasts through target-inhibited PDGFR signaling in vitro and in vivo.
基金This work was financially supported by the National Major Science and Technology Projects of China(2017ZX09101001)the Double First-Class University Project(CPU2018GY33).
文摘Nafamostat mesylate is a serine protease inhibitor used in the treatment of acute pancreatitis.The impurities in nafamostat mesylate,the active pharmaceutical ingredient(API),were profiled via high performance liquid chromatography tandem ion trap coupled with time-of-flight mass spectrometer(HPLC-IT-TOF/MS).The chromatography was performed on an ACE-3 C18 column(200 mm4.6 mm,3 mm)using methanol and 0.1%formic acid in purified water as mobile phase at a flow rate of 1.0 mL/min.The ions were detected by IT-TOF/MS with a full-scan mass analysis from m/z 100 to 800.In total,eleven impurities were detected in nafamostat mesylate API.The impurity profile was estimated based on the HPLC-IT-TOF/MS data,including accurate masses,MSn fingerprints of fragmentation pathways and a series of double-charged ions.Finally,seven impurities were identified and reported for the first time.The results will provide technical support for the quality control and clinical safety of nafamostat mesylate.
基金This work was supported by the Key Programfor International Science and Technology Cooperation Projects of China(2020YFE0201700)State Drug Administration key laboratory project(2024HYZX04).
文摘The structures of solid dosage forms determine their release behaviors and are critical attributes for the design and evaluation of the solid dosage forms.Here,the 3D structures of doxazosin mesylate sustained-release tablets were parallelly assessed by micro-computed tomography(micro-CT).There were no significant differences observed in the release profiles between the RLD and the generic formulation in the conventional dissolution,but the generic preparation released slightly faster in media with ethanol during an alcohol-induced dose-dumping test.With their 3D structures obtained via micro-CT determination,the unique release behaviors of both RLD and the generic were investigated to reveal the effects of internal fine structure on the release kinetics.The structural parameters for both preparations were similar in conventional dissolution test,while the dissolutions in ethanol media showed some distinctions between RLD and generic preparations due to their static and dynamic structures.Furthermore,the findings revealed that the presence of ethanol accelerated dissolution and induced changes in internal structure of both RLD and generic preparations.Moreover,structure parameters like volume and area of outer contour,remaining solid volume and cavity volumewere not equivalent between the two formulations in 40%ethanol.In conclusion,the structure data obtained from this study provided valuable insights into the diverse release behaviors observed in various modified-release formulations in drug development and quality control.
