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利用壳聚糖亲和层析提取抑酶肽的研究 被引量:3
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作者 范继业 张静 《河北工业科技》 CAS 2006年第3期149-151,共3页
采用化学改性的壳聚糖为载体,共价法偶联胰蛋白酶,制成抑酶肽亲和吸附剂,将其直接亲和层析牛肺提取液,分离、纯化高比活力的抑酶肽。抑酶肽抑制比活力为71 428 BAEE.mg-1,酶活性回收率为62.5%。该方法质量稳定,成本较低,吸附剂机械强度... 采用化学改性的壳聚糖为载体,共价法偶联胰蛋白酶,制成抑酶肽亲和吸附剂,将其直接亲和层析牛肺提取液,分离、纯化高比活力的抑酶肽。抑酶肽抑制比活力为71 428 BAEE.mg-1,酶活性回收率为62.5%。该方法质量稳定,成本较低,吸附剂机械强度高,抗污染能力较强,非特异性吸附较小,可反复使用,价格低廉,适于应用。 展开更多
关键词 固定化 亲和层析 抑酶肽 壳聚糖
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壳聚糖微球亲和层析提取抑酶肽的研究
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作者 范继业 张静 +2 位作者 高冬婷 王刚 刘然 《河北科技大学学报》 CAS 北大核心 2009年第2期92-94,98,共4页
建立了一种高效、实用的抑酶肽制备技术。采用牛肺为原料,利用改性壳聚糖载体,共价偶联胰蛋白酶,亲和层析牛肺提取液,2步制得高比活抑酶肽。抑酶肽抑制比活力为71428 BAEE/mg,酶活性回收率为73.5%。该方法质量稳定,成本较低,吸附剂机械... 建立了一种高效、实用的抑酶肽制备技术。采用牛肺为原料,利用改性壳聚糖载体,共价偶联胰蛋白酶,亲和层析牛肺提取液,2步制得高比活抑酶肽。抑酶肽抑制比活力为71428 BAEE/mg,酶活性回收率为73.5%。该方法质量稳定,成本较低,吸附剂机械强度高,抗污染能力较强,可反复使用,适宜应用。 展开更多
关键词 牛肺 亲和层析 抑酶肽 壳聚糖
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抑酶肽对失血性休克兔再灌注肺损伤的保护作用
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作者 莫志武 《中国热带医学》 CAS 2007年第6期1038-1039,共2页
目的探讨抑酶肽对失血性休克兔再灌注肺损伤的保护作用。方法36只白兔随机分为对照组、休克组和抑酶肽组,每组12只,分别于休克2h、复苏后2h取静脉血测定丙二醛(MDA)、超氧化物歧化酶(SOD)、肿瘤坏死因子α(TNF-α)、磷脂酶A2(PLA2)的含... 目的探讨抑酶肽对失血性休克兔再灌注肺损伤的保护作用。方法36只白兔随机分为对照组、休克组和抑酶肽组,每组12只,分别于休克2h、复苏后2h取静脉血测定丙二醛(MDA)、超氧化物歧化酶(SOD)、肿瘤坏死因子α(TNF-α)、磷脂酶A2(PLA2)的含量及肺组织的湿/干重比值。结果抑酶肽组的MDA含量明显低于休克组(P<0.05);SOD含量明显高于休克组(P<0.05);磷脂酶A2和肿瘤坏死因子α的含量明显低于休克组(P<0.05);肺组织的湿/干重比值也明显小于休克组(P<0.05)。结论早期持续小剂量运用抑酶肽可通过抑制氧自由基的产生,参与炎症反应的多个环节,从而减轻创伤失血性休克兔再灌注肺组织损伤。 展开更多
关键词 抑酶肽 失血性休克 急性肺损伤 丙二醛 超氧化物歧化 肿瘤坏死因子Α 磷脂A2
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蚓酶多肽抑菌营养液在设施蔬菜上的应用效果 被引量:2
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作者 王东升 谢晓艾 +3 位作者 王蓓 李伟明 刘庆叶 黄忠阳 《北方园艺》 CAS 北大核心 2020年第18期58-63,共6页
以黄瓜和番茄为试材,设常规施肥处理(CK)和常规施肥处理+喷施蚓酶多肽抑菌营养液(Te),研究了蚓酶多肽抑菌营养液对其植株生长、抗病能力、产量及果实品质的影响,以期为蚓酶多肽抑菌营养液对于农业设施蔬菜的使用效果提供参考依据。结果... 以黄瓜和番茄为试材,设常规施肥处理(CK)和常规施肥处理+喷施蚓酶多肽抑菌营养液(Te),研究了蚓酶多肽抑菌营养液对其植株生长、抗病能力、产量及果实品质的影响,以期为蚓酶多肽抑菌营养液对于农业设施蔬菜的使用效果提供参考依据。结果表明:在黄瓜上,与对照CK相比,喷施蚓酶多肽抑菌营养液显著提高了黄瓜的株高,有效促进了黄瓜的生长;从品质上看,Te处理显著提高了黄瓜的维生素C含量和降低了硝酸盐含量,说明蚓酶多肽抑菌营养液对于改善黄瓜品质有一定效果;从产量上看,Te与CK相比,增幅高达20.30%,说明蚓酶多肽抑菌营养液能显著提高黄瓜的产量。在番茄上,喷施蚓酶多肽抑菌营养液对于促进番茄生长无显著效果,但在青枯病抗病上明显优于对照CK,CK、Te的发病率分别为38.20%和0%,说明蚓酶多肽抑菌营养液能提高对番茄青枯病抗病能力,抑制其发病;从品质上看,Te处理有效提高了番茄的蛋白质含量并降低了有机酸含量,说明蚓酶多肽抑菌营养液能改善番茄品质;从产量上看,与CK相比,Te处理的增幅高达23.94%,说明喷施蚓酶多肽抑菌营养液能显著提高番茄产量。 展开更多
关键词 黄瓜 番茄 产量 菌营养液
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高浓度葡萄糖诱导红细胞磷脂酰丝氨酸暴露的机制研究
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作者 权国波 韩颖 +5 位作者 杨超 扈文博 刘敏霞 刘安 王艳 王捷熙 《中国实验血液学杂志》 CAS CSCD 2008年第5期1181-1184,共4页
本研究探讨高浓度葡萄糖诱导红细胞磷脂酰丝氨酸(PS)暴露的机制。将红细胞于葡萄糖缓冲液中孵育后用流式细胞术分析PS标记率和前向角值;检测caspase-3和caspase-8的活化情况;用流式细胞术和荧光显微镜观察亮抑酶肽对葡萄糖引起的红细胞P... 本研究探讨高浓度葡萄糖诱导红细胞磷脂酰丝氨酸(PS)暴露的机制。将红细胞于葡萄糖缓冲液中孵育后用流式细胞术分析PS标记率和前向角值;检测caspase-3和caspase-8的活化情况;用流式细胞术和荧光显微镜观察亮抑酶肽对葡萄糖引起的红细胞PS暴露的抑制效果。结果表明:葡萄糖可以诱导红细胞PS暴露,而且其效率和葡萄糖浓度密切相关。随着葡萄糖浓度的增加,红细胞的PS标记率呈逐步增加的趋势,当葡萄糖浓度为0.8mol/L时,红细胞的PS标记率在80%以上。然而,在葡萄糖引起的红细胞PS暴露过程中,caspase-3和caspase-8没有活化,而亮抑酶肽却可以很好地抑制红细胞PS暴露和使其体积缩小。随着亮抑酶肽浓度的增加,红细胞PS标记率呈逐步下降的趋势,而细胞体积却呈逐步增加的趋势。结论:高浓度葡萄糖可以导致严重的红细胞PS暴露,而且这种PS暴露和caspase无关,推测葡萄糖诱导的红细胞PS暴露是受一条对亮抑酶肽高度敏感的、未知的通路调控的。 展开更多
关键词 红细胞 磷脂酰丝氨酸 葡萄糖 抑酶肽
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The Topical Use of Aprotinin in Cardiac Surgery with Cardiopulmonary Bypass
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作者 陈亦江 王晓伟 陈广明 《Journal of Nanjing Medical University》 2003年第1期23-29,共7页
Objective To investigate the effects of the topical use of aprotinin on thebasis of comprehensive blood conservations in cardiopulmonary bypass (CPB). Methods In a prospectiveclinical trial, 20 patients were randomly ... Objective To investigate the effects of the topical use of aprotinin on thebasis of comprehensive blood conservations in cardiopulmonary bypass (CPB). Methods In a prospectiveclinical trial, 20 patients were randomly divided into 2 groups. Control group: placebo was usedtopically. Aprotinin group: aprotinin was poured into the pericardial cavity before closure of thesternotomy. Before and 24h after surgery, hemoglobin (Hb), hematocrit (Hct), bleeding time (BT),clotting time (CT) and prothrombin time (PT) were measured. Meanwhile, amounts of the mediastinaldrainage and the hemoglobin loss were observed at 0, 2, 6 and 24h after operation. The samples fromthe mediastinal drainage were also collected to measure D-Dimer (D-D), tissue type plasminogenactivator (t-PA) activity, plasminogen activator inhibitor (PAI) activity and protein C (PC).Results In Aprotinin group, D-D, t-PA activity and PC were significantly reduced, compared withthose in Control group (P<0.05, P<0.05, P<0.01). On the contrary, PAI activity was significantlyincreased, compared with that in Control group. Amounts of the mediastinal drainage and thehemoglobin loss were decreased by 43% and 52%, compared with those in Control group. Conclusion Ourresults suggest that the topical use of aprotinin can have better effects on the basis ofcomprehensive moderate blood conservation. 展开更多
关键词 cardiopulmonary bypass APROTININ topical use
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Purification and Characterization of Angiotensin I Converting Enzyme Inhibition Peptides from Sandworm Sipunculus nudus 被引量:5
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作者 SUN Xueping WANG Man +1 位作者 LIU Buming SUN Zhenliang 《Journal of Ocean University of China》 SCIE CAS CSCD 2017年第5期911-915,共5页
Three angiotensin I converting enzyme(ACE) inhibition peptides were isolated from sandworm Sipunculus nudus protein hydrolysate prepared using protamex. Consecutive purification methods, including size exclusion chrom... Three angiotensin I converting enzyme(ACE) inhibition peptides were isolated from sandworm Sipunculus nudus protein hydrolysate prepared using protamex. Consecutive purification methods, including size exclusion chromatography and reverse-phase high performance liquid chromatography(RP-HPLC), were used to isolate the ACE inhibition peptides. The amino acid sequences of the peptides were identified as Ile-Asn-Asp, Val-Glu-Pro-Gly and Leu-Ala-Asp-Glu-Phe. The IC_(50) values of the purified peptides for ACE inhibition activity were 34.72 μmol L^(-1), 20.55 μmol L^(-1) and 22.77 μmol L^(-1), respectively. These results suggested that S. nudus proteins contain specific peptides that can be released by enzymatic hydrolysis. This study may provide an experimental basis for further systematic research, rational development and clinical utilization of sandworm resources. 展开更多
关键词 hydrolysis converting purification exclusion Angiotensin Inhibition shrimp isolate purified Enzyme
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Changing the treatment of heart failure with reduced ejection fraction: clinical use of sacubitril-valsartan combination 被引量:4
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作者 Edgardo Kaplinsky 《Journal of Geriatric Cardiology》 SCIE CAS CSCD 2016年第11期914-923,共10页
Despite significant therapeutic advances, patients with chronic heart failure (HF) remain at high risk of morbidity and mortality. Sacubitill valsartan (previously known as LCZ696) is a new oral agent approved for... Despite significant therapeutic advances, patients with chronic heart failure (HF) remain at high risk of morbidity and mortality. Sacubitill valsartan (previously known as LCZ696) is a new oral agent approved for the treatment of symptomatic chronic heart failure in adults with reduced ejection fraction. It is described as the fast in class angiotensin receptor neprilysin inhibitor (ARNI) since it incorporates the neprilysin inhibitor, sacubitril and the angiotensin Ⅱ receptor antagonist, valsartan. Neprilysin is an endopeptidase that breaks down several vasoactive peptides including natriuretic peptides (NPs), bradykinin, endothelin and angiotensin II (Ang-II). Therefore, a natural consequence of its inhibition is an increase of plasmatic levels of both, NPs and Ang-Ⅱ (with opposite biological actions). So, a combined inhibition of these both systems (Sacubitril / valsartan) may enhance the benefits of NPs effects in HF (natriuresis, diuresis, etc) while Ang-Ⅱ receptor is inhibited (reducing vasoconstriction and aldosterone release). In a large clinical trial (PARADIGM-HF with 8442 patients), this new agent was found to significantly reduce cardiovascular and all cause mortality as well as hospitalizations due to HF (compared to enalapril). This manuscript reviews clinical evidence for sacubitril valsartan, dosing and cautions, future directions and its considered place in the therapy of HF with reduced ejection fraction. 展开更多
关键词 Heart failure LCZ696 NEPRILYSIN PARADIGM-HF Sacubitril VALSARTAN
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Cysteine peptidase and its inhibitor activity levels and vitamin E concentration in normal human serum and colorectal carcinomas 被引量:1
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作者 Robert Szwed Zygmunt Grzebieniak +2 位作者 Yousif Saleh Godwin Bwire Ekonjo Maciej Siewinski 《World Journal of Gastroenterology》 SCIE CAS CSCD 2005年第6期850-853,共4页
AIM: Cysteine peptidase (CP) and its inhibitor (CPI) are a matrix protease that may be associated with colorectal carcinoma invasion and progression, and vitamin E is also a stimulator of the immunological system. Our... AIM: Cysteine peptidase (CP) and its inhibitor (CPI) are a matrix protease that may be associated with colorectal carcinoma invasion and progression, and vitamin E is also a stimulator of the immunological system. Our purpose was to determine the correlation between the expression of cysteine peptidases and their endogenous inhibitors,and the level of vitamin E in sera of patients with colorectal cancer in comparison with healthy individuals.METHODS: The levels of cysteine peptidases and their inhibitors were determined in the sera of patients with primary and metastatic colorectal carcinoma and healthy individuals using fluorogenic substrate, and the level of vitamin E was determined by HPLC.RESULTS: The levels of cysteine peptidases and their inhibitors were significantly higher in the metastatic colorectal cancer patients than that in the healthy controls (P<0.05).The activity of CP increased 2.2-fold, CPI 2.8-fold and vitamin E decreased 3.4-fold in sera of patients with metastasis in comparison with controls. The level of vitamin E in healthy individuals was higher, whereas the activity of cysteine peptidases and their inhibitors associated with complexes was lower than that in patients with cancer of the digestive tract.CONCLUSION: These results suggest that the serum levels of CP and their inhibitors could be an indicator of the prognosis for patients with metastatic colorectal cancer. Vitamin E can be administered prophylactically to prevent digestive tract neoplasmas. 展开更多
关键词 Cysteine peptidases INHIBITORS Vitamin E Colorectal cancers
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A clinical study of aprotinin blood anesthesia used in the surgery of liver cancer
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作者 易斌 陶国才 +1 位作者 毕敏 刘怀琼 《Journal of Medical Colleges of PLA(China)》 CAS 2004年第4期241-244,共4页
Objective: To investigate the role of aprotinin blood anesthesia used in hepatotomy. Methods: Patients with liver cancer undergoing hepatotomy were divided into two groups. In experimental group (40 patients) a loadin... Objective: To investigate the role of aprotinin blood anesthesia used in hepatotomy. Methods: Patients with liver cancer undergoing hepatotomy were divided into two groups. In experimental group (40 patients) a loading dose with 1112 EPU aprotinin and maintained by 278 EPU/h was used until 2 h after operation. The control group (42 patients) was treated with 0.9% normal saline. The venous blood was withdrew for blood routine, thrombelastography and coagulable test at the time of preinduced, 1 h, 2 h and 4 h following the operation beginning, 6 h and 12 h after operation. The change of TEG and coagulable profile were monitored during the whole surgery. The volume of blood transfusion and hemorrhage between two groups were compared. Results: After the usage of aprotinin, the preoperative hypercoagulability of the experimental group was remitted and the coagulative state was kept relatively stable during the operation. However, hypercoagulability of the control group aggravated following the operation beginning and some of them switched to hypocoagulability. The volumes and rates of hemorrhage and transfusion were smaller in the experimental group than in the control group. Conclusion: Aprotinin can stabilize the coagulable state, reduce the volumes and rates of hemorrhage and transfusion, and is worth using in the surgery of operations of liver cancer. 展开更多
关键词 APROTININ THROMBELASTOGRAPHY liver neoplasm
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Effect of vitamin E and human placenta cysteine peptidase inhibitor on expression of cathepsins B and L in implanted hepatoma Morris 5123 tumor model in Wistar rats 被引量:2
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作者 Tadeusz Sebzda Piotr Hanczyc +3 位作者 Yousif Saleh Bernice F Akinpelumi Maciej Siewinski Jerzy Rudnicki 《World Journal of Gastroenterology》 SCIE CAS CSCD 2005年第4期587-592,共6页
AIM: To examine the effectiveness of human placental inhibitors, by injecting vitamin E to rats with transplanted Morris-5123 hepatoma, on the expression of cathepsins B and L in tumor, liver, lung and blood sera afte... AIM: To examine the effectiveness of human placental inhibitors, by injecting vitamin E to rats with transplanted Morris-5123 hepatoma, on the expression of cathepsins B and L in tumor, liver, lung and blood sera after transplantation of Morris 5123 hepatoma. METHODS: Animals were divided into 10 groups receiving three different concentrations of vitamin E and inhibitors along or in combination and compared with negative control (healthy rats) and positive control (tumor rats). Effectiveness of treatment was evaluated with regard to survival time, tumor response and determination of the activities of proteolytic enzymes and their inhibitors using flurogenic substrates. RESULTS: Cathepsins B and L activities were elevated by 16-fold in comparison with negative control tissues, and their endogenous inhibitor activity decreased by 1.2-fold before treatment. In several cases, tumors completely disappeared following vitamin E plus human placental cyteine protease inhibitor (CPI) compared with controls. The number of complete tumor responses was higher when 20 m/kg vitamin E plus 400 μg of CPI was used, i.e. 7/10 rats survived more than two mo. Cathepsins B and L were expressed significantly in tumor, liver, lung tissues and sera in parallel to the increasing of the endogenous inhibitor activity compared with the controls after treatment(P<0.0001) CONCLUSION: The data indicate formation of metastasis significantly reduced in treated rats, which might provide a therapeutic basis for anti-cancer therapy. 展开更多
关键词 Morris-5123 hepatoma Vitamin E Human placenta cysteine peptidase inhibitor Cathepsin B Cathepsin L
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Selective cyclooxygenase-2 inhibitor ameliorates cholecystokinin-octapeptide-induced acute pancreatitis in rats 被引量:8
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作者 Sang-Wan Seo Won-Seok Jung +6 位作者 Tai-Guang Piao Seung-Heon Hong Ki-Jung Yun Rae-Kil Park Min-Kyo Shin Ho-Joon Song Sung-Joo Park 《World Journal of Gastroenterology》 SCIE CAS CSCD 2007年第16期2298-2304,共7页
AIM: To investigate the effect of selective Cyclooxygenase-2 (COX-2) inhibitor 4-[5-(4-Chloro-phenyl)-3- (trifluoromethyl)- 1H-pyrazol- 1-yl] benzenesulfonamide (SC-236), on the cholecystokinin (CCK)-octape... AIM: To investigate the effect of selective Cyclooxygenase-2 (COX-2) inhibitor 4-[5-(4-Chloro-phenyl)-3- (trifluoromethyl)- 1H-pyrazol- 1-yl] benzenesulfonamide (SC-236), on the cholecystokinin (CCK)-octapeptideinduced acute pancreatitis (AP) in rats. METHODS: Wistar rat weighing 240 g to 260 g were divided into three groups. (1) Normal DMSO treated group, (2) SC-236 at 4 mg/kg treated group; SC-236 systemically administered via the intravenous (i.v.) catheter, followed by 75 μg/kg CCK octapeptide subcutaneously three times, after 1, 3 and 5 h. This whole procedure was repeated for 5 d. (3) Dimethyl sulfoxide (DMSO) treated group: an identical protocol was used in this group as in the SC-236 cohort (see 2. above). Repeated CCK octapeptide treatment resulted in a typical experimentally induced pancreatitis in the Wistar rats. RESULTS: SC-236 improved the severity of CCK- octapeptide-induced AP as measured by laboratory criteria [the pancreatic weight/body weight (p.w/ b.w) ratio, the level of serum amylase and lipase]. The SC-236 treated group showed minimal histologic evidence of pancreatitis and a significant reduction in myeloperoxidase activity. SC-236 also increased heat shock protein (HSP)-60 and HSP72 compared with the DMSO-treated group in the CCK-octapeptide-induced AP and also reduced the pancreatic levels of COX-2. Furthermore, SC-236 reduced proinflammatory cytokine synthesis and inhibited NF-KB activation compared with the DMSO-treated group in the CCK-octapeptide-induced AP. CONCLUSION: Our results suggested that COX-2 plays pivotal role in the development of AP and COX-2 inhibitors may play a beneficial role in preventing AP. 展开更多
关键词 SC-236 Acute pancreatitis Cholecystokinin octapeptide
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Efficacy and safety of saxagliptin in patients with type 2 diabetes mellitus:a meta-analysis of randomized controlled trials 被引量:2
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作者 姚莉 范芳芳 +2 位作者 胡兰 赵生俊 郑丽丽 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2016年第2期128-139,共12页
As a new oral hypoglycemic agent, saxagliptin belongs to the class of dipeptidyl peptidase-4 (DPP-4) inhibitors. However, it remains inconclusive whether saxagliptin is associated with increased risk of adverse even... As a new oral hypoglycemic agent, saxagliptin belongs to the class of dipeptidyl peptidase-4 (DPP-4) inhibitors. However, it remains inconclusive whether saxagliptin is associated with increased risk of adverse events (AE) and efficacy as add-on treatment. Therefore, we performed an up-to-date meta-analysis to compare the efficacy and safety of saxagliptin with placebo and other oral hypoglycemic agents in adult patients with type 2 diabetes mellitus (T2DM). Randomized clinical trials (RCTs) comparing saxagliptin with comparators were retrieved by selecting articles from Pubmed, Embase, Cochrane Library and Clinical Trials Registry Platform up to Oct. 2013. Weighted mean difference (WMD) was used to analyze the effect of hypoglycemic agents on HbAlc, weight and fasting plasma glucose (FPG). While the patients who achieved HbAlc〈7.0% and had AE were analyzed as relative risks (RR). A total of 18 articles from 16 RCTs and one clinic trial from the WHO International Clinical Trials Registry Platform met the included criterion. Clinically significant decrease from baseline HbAlc compared with placebo was certified for 2.5 mg/day saxagliptin (WMD = -0.45%, 95% CI, -0.48% to -0.42%) and 5 mg/d saxagliptin (WMD = -0.52%, 95% CI, -0.60% to -0.44%). Saxagliptin as add-on therapy was superior to thiazolidinediones, up-titrated glyburide, up-titrated metformin or metformin monotherapy in achieving HbA1c〈7.0%. Treatment with saxagliptin had negligible effect on weight, and it was considered weight neutral. Saxagliptin treatment did not increase the risk of hypoglycemia (RR = 1.28, 95% CI 0.72 to 2.27, P = 0.40) and serious adverse experiences (RR = 1.25, 95% CI 0.94 to 1.66, P = 0.13). No statistically significant differences were observed between saxagliptin and comparators in terms of the risk of infections. The present study showed that saxagliptin was effective in improving glycaemic control in T2DM with a low risk of hypoglycaemia and incidence of infections in either monotherapy or add-on treatment. This founding should be further certified by large-sample size and good-designed RCT. 展开更多
关键词 DPP-4 inhibitor SAXAGLIPTIN META-ANALYSIS Type 2 diabetes mellitus Fasting plasma glucose Glycosylated hemoglobin Randomized controlled trial HYPOGLYCAEMIA
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Study on the dipeptide vinyl sulfonamide derivatives as proteasome inhibitor
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作者 姚书扬 周玥 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2016年第6期408-418,共11页
On the basis of the Michael-addition mechanism of classical proteasome inhibitors, six dipeptide vinyl sulfonamide and dipeptide vinyl sulfonate derivatives were designed and synthesized. Moreover, an efficient method... On the basis of the Michael-addition mechanism of classical proteasome inhibitors, six dipeptide vinyl sulfonamide and dipeptide vinyl sulfonate derivatives were designed and synthesized. Moreover, an efficient method for the synthesis of g-amino vinyl sulfonamides, key intermediates to the target molecules, was developed via the Wittig-Horner reaction of peptide aldehyde with Wittig reagents derived from methanesulfonamides. 展开更多
关键词 Proteasome inhibitor Dipeptide vinyl sulfonamides Wittig-Horner reaction g-Amino vinyl sulfonamide
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Stability and cytotoxicity of angiotensin-I-converting enzyme inhibitory peptides derived from bovine casein 被引量:6
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作者 Wei WU Pan-pan YU +2 位作者 Feng-yang ZHANG Hong-xia CHE Zhan-mei JIANG 《Journal of Zhejiang University-Science B(Biomedicine & Biotechnology)》 SCIE CAS CSCD 2014年第2期143-152,共10页
This study investigated the effect of heat treatment combined with acid and alkali on the angiotensin-I- converting enzyme (ACE) inhibitory activity of peptides derived from bovine casein. The free amino group conte... This study investigated the effect of heat treatment combined with acid and alkali on the angiotensin-I- converting enzyme (ACE) inhibitory activity of peptides derived from bovine casein. The free amino group content, color, and cytotoxicity of the peptides were measured under different conditions. When heated at 100 ℃ in the pH range from 9.0 to 12.0, ACE inhibitory activity was reduced and the appearance of the peptides was significantly darkened. After thermal treatment in the presence of acid and alkali, the free amino group content of ACE inhibitory peptides decreased markedly. High temperature and prolonged heating also resulted in the loss of ACE inhibitory activity, the loss of free amino groups, and the darker coloration of bovine casein-derived peptides. However, ACE inhibitory peptides, within a concentration range of from 0.01 to 0.2 mg/ml, showed no cytotoxicity to Caco-2 and ECV-304 cell lines after heat treatment. This indicated that high temperature and alkaline heat treatment impaired the stability of bovine casein-derived ACE inhibitory peptides. 展开更多
关键词 Angiotensin-l-converting enzyme inhibitory peptide Heat treatment STABILITY CYTOTOXICITY
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Study of the prodrugs of peptide aldehydes as proteasome inhibitors
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作者 Li-Qiang Han Yu-An Zhang +4 位作者 Shu-Yang Yao Bo Xu Ze-Mei Ge Jing-Rong Cui Run-Tao Li 《Journal of Chinese Pharmaceutical Sciences》 CAS 2012年第1期21-27,共7页
To improve the stability of peptide aldehyde proteasome inhibitors, four peptide cycloacetal derivatives and two peptide heterocycle compounds were designed and synthesized. Their proteasome inhibition and in vitro an... To improve the stability of peptide aldehyde proteasome inhibitors, four peptide cycloacetal derivatives and two peptide heterocycle compounds were designed and synthesized. Their proteasome inhibition and in vitro anticancer activities were evaluated. The four peptide cycloacetal derivatives did not showed any activities, which demonstrated that this kind of cycloacetal derivatives might be suitable as prodrugs. The two peptide heterocycle compounds were found to show obvious activities at both enzyme and cell levels. These results provide us a new clue for the modification of peptide aldehyde proteasome inhibitors. 展开更多
关键词 Proteasome inhibitor ANTICANCER Peptide acetal derivative Prodrug principle
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