Angiotensin I converting enzyme (ACE) plays an important physiological role in the regulation of hypertension. In this study, we applied virtual screening to discover a novel angiotensin I converting enzyme inhibito...Angiotensin I converting enzyme (ACE) plays an important physiological role in the regulation of hypertension. In this study, we applied virtual screening to discover a novel angiotensin I converting enzyme inhibitory peptides from milk casein. One potential hit was identified based on docking scores, subsequently confirmed by activity studies in vitro (IC50=20.85 μmol L-1). The proposed peptide in this study contains a unique sequence, Lys-Val-Leu-Ile-Leu-Ala. Moreover, we performed the docking studies to understand the binding mode between the enzyme and peptide hit.展开更多
Drying technology of angiotensin converting enzyme (ACE) inhibitory peptides derived from bovine casein was investigated. No significance was observed on ACE inhibitory activity of products prepared by spay drying a...Drying technology of angiotensin converting enzyme (ACE) inhibitory peptides derived from bovine casein was investigated. No significance was observed on ACE inhibitory activity of products prepared by spay drying and freeze drying (P〉0.05). Spay drying was the best drying process for practical industry production. The inlet temperature ranged from 140℃ to 160℃ and the exit temperature ranged from 70 ℃ to 90 ℃ during the spay drying process. Under the optimal conditions, scale-up of angiotensin converted enzyme inhibitory peptide from 1 L to 10 L and the experiment was successively conducted. Peptide yield was 29% and half inhibitory concentration (IC50) was 0.53 g. L^-1.展开更多
To explore the relation of angiotensin-converting enzyme (ACE) and angiotensin Ⅱ type 1 receptor (AT1R) gene polymorphism with coronary heart disease (CHD) and the severity of coronary artery stenosis, 130 CHD ...To explore the relation of angiotensin-converting enzyme (ACE) and angiotensin Ⅱ type 1 receptor (AT1R) gene polymorphism with coronary heart disease (CHD) and the severity of coronary artery stenosis, 130 CHD patients who underwent coronary angiography were examined for the number of affected coronary vessels (≥75% stenosis) and coronary Jeopardy score. The insertion/deletion of ACE gene polymorphism and AT1R gene polymorphism (an A→C transversion at nucleotide position 1166) were detected by using polymerase chain reaction (PCR) and restriction fragment length polymorphism (RFLP) in CHD patients and 90 healthy serving as controls. The resuits showed that DD genotype and of ACE were more frequent in CHD patients than that in control group (38.5% vs 14.4%, P〈0.001). The frequency of the ATIR A/C genotypes did not differ between the patients and the controls (10% vs 13.1%, P〉0.05). The relative risk associated with the ACE-DD was increased by AT1R-AC genotype. Neither the number of affected coronary vessels nor the coronary score differed among the ACE I/D genotypes (P〉0.05). But the number of affected coronary vessels and the coronary score were significantly greater in the patients with the AT1R-AC genotype than in those with the AA genotype (P〈0.05). In conclusion, DD genotype may be risk factor for CHD and MI in Chinese people, and is not responsible for the development of the coronary artery stenosis. The AT1R-C allele may increase the relative risk associated with the ACE-DD genotype, and may be involved in the development of the stenosis of coronary artery.展开更多
Objective To investigate the relationship of an insertion/deletion (I/D) polymorphism of the angiotension converting enzyme (ACE) gene to obstructive sleep apnea syndrome (OSAS) patients and the control subjects.Met...Objective To investigate the relationship of an insertion/deletion (I/D) polymorphism of the angiotension converting enzyme (ACE) gene to obstructive sleep apnea syndrome (OSAS) patients and the control subjects.Methods Genomic DNA was extracted from blood samples and amplified by polymerase chain reaction (PCR). PCR primers flanked the polymorphic region in intro 16 of the ACE gene. Results OSAS patients had significantly higher frequencies of I/I genotype and insertion allele of the ACE gene as compared with the control subjects in Chinese population. The OSAS patients with I/I genotype had significantly longer apnea time, lower minimum SaO2 and greater AHI than the OSAS patients with I/D genotype. Conclusion These results indicate that the I/I genotype and I allele are a risk factor for OSAS in Chinese.展开更多
Chemical feature based pharmacophore models were generated for an angiotensin converting enzyme(ACE) inhibitory peptide using the Discovery Studio 2.0 pharmacophore modeling approach. The pharmacophore hypothesis sele...Chemical feature based pharmacophore models were generated for an angiotensin converting enzyme(ACE) inhibitory peptide using the Discovery Studio 2.0 pharmacophore modeling approach. The pharmacophore hypothesis selected has five features(one negative ionizable region,one hydrogen bond donor,one hydrogen bond acceptor and two hydrophobic functional groups). Additionally,ACE inhibitory hexapeptide previously obtained from silkworm pupae protein was optimized to target the ACE based on the selected pharmacophore. The results suggest that tri-peptide(thr-val-phe) may be structural determinant of ACE activity. Docking studies further provided confidence for the validity of the selected pharmacophore model to perform structure optimization of the ACE inhibitory peptide.展开更多
该研究将富硒能力较强的纳豆芽孢杆菌作为发酵菌种,鹰嘴豆为原料,以血管紧张素转化酶(angiotensin I converting enzyme,ACE)抑制率为指标,采用单因素试验和响应面优化法对纳豆芽孢杆菌富硒后产ACE抑制肽的最佳条件进行优化。同时采用...该研究将富硒能力较强的纳豆芽孢杆菌作为发酵菌种,鹰嘴豆为原料,以血管紧张素转化酶(angiotensin I converting enzyme,ACE)抑制率为指标,采用单因素试验和响应面优化法对纳豆芽孢杆菌富硒后产ACE抑制肽的最佳条件进行优化。同时采用超高效液相色谱-电喷雾电离-串联质谱(ultra performance liquid chromatography electrospray ionization tandem mass spectrometry,UPLC-ESI-MS/MS)法对鹰嘴豆纳豆富硒后硒代氨基酸进行定性定量分析。结果表明,L-硒代胱氨酸是鹰嘴豆纳豆富硒后主要的硒代氨基酸,纳豆芽孢杆菌富硒后产ACE抑制肽的最佳条件为接种量2%、液料比18∶1(mL/g)、发酵温度40℃,ACE抑制率可达89.24%。对比试验的结果显示,纳豆芽孢杆菌不富硒发酵鹰嘴豆产ACE抑制肽活性为66.35%,表明富硒纳豆芽孢杆菌发酵鹰嘴豆对ACE活性有良好的抑制作用。展开更多
Background Angiotensin-converting enzyme inhibitors (ACEI) and angiotensin II type 1 receptor blockers (ARB) can inhibit tumor growth by inhibition of angiogenesis. This study was designed to study the anticancer ...Background Angiotensin-converting enzyme inhibitors (ACEI) and angiotensin II type 1 receptor blockers (ARB) can inhibit tumor growth by inhibition of angiogenesis. This study was designed to study the anticancer effects of ACEI and ARB on tumor growth and lymphangiogenesis in an implanted gastric cancer mouse model. Methods A model of gastric cancer was established by subcutaneously inoculating human gastric cancer cell line SGC-7901 into 60 nude mice. One week later, all mice were randomly divided into 5 groups. A control group received physiologic saline once daily for 21 days. Mice in the 4 treatment groups received one of the following agents by gavage once daily for 21 days: perindopril, 2 mg/kg; captopril, 5 mg/kg; Iosartan, 50 mg/kg; or valsartan, 40 mg/kg. Twenty-one days after treatment, all the mice were sacrificed and the tumors were removed. Tumor sections were processed, and immunohistochemical methods were used to observe the expressions of vascular endothelial growth factor C (VEGF-C), matrix metalloproteinase 7 (MMP-7), and lymphatic microvessel density (LMVD). Results Tumor volume was significantly inhibited in all ACEI and ARB groups, compared with the control group (all P 〈0,01). LMVD in the ACEI and ARB groups was also significantly lower than that of the control group (all P 〈0.01). In the ACEI groups, the expressions of VEGF-C and MMP-7 were both significantly decreased, compared with the control group (all P 〈0.05). In the ARB groups, expression of VEGF-C was significantly decreased compared with the control group (all P 〈0.05). However, no significant difference was found in the expression of MMP-7 between ARB groups and the control group. Conclusion In a mouse model, ACEI and ARB might inhibit gastric cancer tumor growth by suppressing lymphangiogenesis.展开更多
基金supported by the National High Technology Research and Development Program of China(863 Program, 2008AA10Z313)the Foundation for Sciand Tech Research Project of Zhejiang Province, China(2006C12096)Natural Science Foundation of Zhejiang Province, China (Y3090026)
文摘Angiotensin I converting enzyme (ACE) plays an important physiological role in the regulation of hypertension. In this study, we applied virtual screening to discover a novel angiotensin I converting enzyme inhibitory peptides from milk casein. One potential hit was identified based on docking scores, subsequently confirmed by activity studies in vitro (IC50=20.85 μmol L-1). The proposed peptide in this study contains a unique sequence, Lys-Val-Leu-Ile-Leu-Ala. Moreover, we performed the docking studies to understand the binding mode between the enzyme and peptide hit.
基金Supported by Scientific Research Foundation for Young Scholars of Heilongjiang Province of China (QC07C25)The National High Technology Research and Development Program of China (2008AA10Z315)
文摘Drying technology of angiotensin converting enzyme (ACE) inhibitory peptides derived from bovine casein was investigated. No significance was observed on ACE inhibitory activity of products prepared by spay drying and freeze drying (P〉0.05). Spay drying was the best drying process for practical industry production. The inlet temperature ranged from 140℃ to 160℃ and the exit temperature ranged from 70 ℃ to 90 ℃ during the spay drying process. Under the optimal conditions, scale-up of angiotensin converted enzyme inhibitory peptide from 1 L to 10 L and the experiment was successively conducted. Peptide yield was 29% and half inhibitory concentration (IC50) was 0.53 g. L^-1.
文摘To explore the relation of angiotensin-converting enzyme (ACE) and angiotensin Ⅱ type 1 receptor (AT1R) gene polymorphism with coronary heart disease (CHD) and the severity of coronary artery stenosis, 130 CHD patients who underwent coronary angiography were examined for the number of affected coronary vessels (≥75% stenosis) and coronary Jeopardy score. The insertion/deletion of ACE gene polymorphism and AT1R gene polymorphism (an A→C transversion at nucleotide position 1166) were detected by using polymerase chain reaction (PCR) and restriction fragment length polymorphism (RFLP) in CHD patients and 90 healthy serving as controls. The resuits showed that DD genotype and of ACE were more frequent in CHD patients than that in control group (38.5% vs 14.4%, P〈0.001). The frequency of the ATIR A/C genotypes did not differ between the patients and the controls (10% vs 13.1%, P〉0.05). The relative risk associated with the ACE-DD was increased by AT1R-AC genotype. Neither the number of affected coronary vessels nor the coronary score differed among the ACE I/D genotypes (P〉0.05). But the number of affected coronary vessels and the coronary score were significantly greater in the patients with the AT1R-AC genotype than in those with the AA genotype (P〈0.05). In conclusion, DD genotype may be risk factor for CHD and MI in Chinese people, and is not responsible for the development of the coronary artery stenosis. The AT1R-C allele may increase the relative risk associated with the ACE-DD genotype, and may be involved in the development of the stenosis of coronary artery.
文摘Objective To investigate the relationship of an insertion/deletion (I/D) polymorphism of the angiotension converting enzyme (ACE) gene to obstructive sleep apnea syndrome (OSAS) patients and the control subjects.Methods Genomic DNA was extracted from blood samples and amplified by polymerase chain reaction (PCR). PCR primers flanked the polymorphic region in intro 16 of the ACE gene. Results OSAS patients had significantly higher frequencies of I/I genotype and insertion allele of the ACE gene as compared with the control subjects in Chinese population. The OSAS patients with I/I genotype had significantly longer apnea time, lower minimum SaO2 and greater AHI than the OSAS patients with I/D genotype. Conclusion These results indicate that the I/I genotype and I allele are a risk factor for OSAS in Chinese.
基金Supported by the Program 111 of Ministry of Education of China and the Program "National Science and Technology Support Plan of Eleventh Five Year Program-ming" of China (Grant No. 2006BAD05A01)
文摘Chemical feature based pharmacophore models were generated for an angiotensin converting enzyme(ACE) inhibitory peptide using the Discovery Studio 2.0 pharmacophore modeling approach. The pharmacophore hypothesis selected has five features(one negative ionizable region,one hydrogen bond donor,one hydrogen bond acceptor and two hydrophobic functional groups). Additionally,ACE inhibitory hexapeptide previously obtained from silkworm pupae protein was optimized to target the ACE based on the selected pharmacophore. The results suggest that tri-peptide(thr-val-phe) may be structural determinant of ACE activity. Docking studies further provided confidence for the validity of the selected pharmacophore model to perform structure optimization of the ACE inhibitory peptide.
文摘该研究将富硒能力较强的纳豆芽孢杆菌作为发酵菌种,鹰嘴豆为原料,以血管紧张素转化酶(angiotensin I converting enzyme,ACE)抑制率为指标,采用单因素试验和响应面优化法对纳豆芽孢杆菌富硒后产ACE抑制肽的最佳条件进行优化。同时采用超高效液相色谱-电喷雾电离-串联质谱(ultra performance liquid chromatography electrospray ionization tandem mass spectrometry,UPLC-ESI-MS/MS)法对鹰嘴豆纳豆富硒后硒代氨基酸进行定性定量分析。结果表明,L-硒代胱氨酸是鹰嘴豆纳豆富硒后主要的硒代氨基酸,纳豆芽孢杆菌富硒后产ACE抑制肽的最佳条件为接种量2%、液料比18∶1(mL/g)、发酵温度40℃,ACE抑制率可达89.24%。对比试验的结果显示,纳豆芽孢杆菌不富硒发酵鹰嘴豆产ACE抑制肽活性为66.35%,表明富硒纳豆芽孢杆菌发酵鹰嘴豆对ACE活性有良好的抑制作用。
基金This study was supported by a grant from the Guangdong Province Natural Science Foundation (No. 5001766).
文摘Background Angiotensin-converting enzyme inhibitors (ACEI) and angiotensin II type 1 receptor blockers (ARB) can inhibit tumor growth by inhibition of angiogenesis. This study was designed to study the anticancer effects of ACEI and ARB on tumor growth and lymphangiogenesis in an implanted gastric cancer mouse model. Methods A model of gastric cancer was established by subcutaneously inoculating human gastric cancer cell line SGC-7901 into 60 nude mice. One week later, all mice were randomly divided into 5 groups. A control group received physiologic saline once daily for 21 days. Mice in the 4 treatment groups received one of the following agents by gavage once daily for 21 days: perindopril, 2 mg/kg; captopril, 5 mg/kg; Iosartan, 50 mg/kg; or valsartan, 40 mg/kg. Twenty-one days after treatment, all the mice were sacrificed and the tumors were removed. Tumor sections were processed, and immunohistochemical methods were used to observe the expressions of vascular endothelial growth factor C (VEGF-C), matrix metalloproteinase 7 (MMP-7), and lymphatic microvessel density (LMVD). Results Tumor volume was significantly inhibited in all ACEI and ARB groups, compared with the control group (all P 〈0,01). LMVD in the ACEI and ARB groups was also significantly lower than that of the control group (all P 〈0.01). In the ACEI groups, the expressions of VEGF-C and MMP-7 were both significantly decreased, compared with the control group (all P 〈0.05). In the ARB groups, expression of VEGF-C was significantly decreased compared with the control group (all P 〈0.05). However, no significant difference was found in the expression of MMP-7 between ARB groups and the control group. Conclusion In a mouse model, ACEI and ARB might inhibit gastric cancer tumor growth by suppressing lymphangiogenesis.