The use of cooled dialysate temperatures first came about in the early 1980s as a way to curb the incidence of intradialytic hypotension （IDH）. IDH was then, and it remains today, the most common complication affect...The use of cooled dialysate temperatures first came about in the early 1980s as a way to curb the incidence of intradialytic hypotension （IDH）. IDH was then, and it remains today, the most common complication affecting chronic hemodialysis patients. It decreases quality of life on dialysis and is an independent risk factor for mortality. Cooling dialysate was first employed as a technique to incite peripheral vasoconstriction on dialysis and in turn reduce the incidence of intradialytic hypotension. Although it has become a common practice amongst in-center hemodialysis units, cooled dialysate results in up to 70% of patients feeling cold while on dialysis and some even experience shivering. Over the years, various studies have been performed to evaluate the safety and effcacy of cooled dialysate in comparison to a standard, more thermoneutral dialysate temperature of 37℃. Although these studies are limited by small sample size, they are promising in many aspects. They demonstrated that cooled dialysis is safe and equally efficacious as thermoneutral dialysis. Although patients report feeling cold on dialysis, they also report increased energy and an improvement in their overall health following cooled dialysis. They established that cooling dialysate temperatures improves hemodynamic tolerability during and after hemodialysis, even in patients prone to IDH, and does so without adversely affecting dialysis adequacy. Cooled dialysis also reduces the incidence of IDH and has a protective effect over major organs including the heart and brain. Finally, it is an inexpensive measure that decreases economic burden by reducing necessary nursing intervention for issues that arise on hemodialysis such as IDH. Before cooled dialysate becomes standard of care for patients on chronic hemodialysis, larger studies with longer follow-up periods will need to take place to confrm the encouraging outcomes mentioned here.展开更多
Objective: To investigate the pharmacological basis of its uses of Phyla nodiflora(P. nodiflora) for the treatment of anomalies predominantly by smooth muscle containing tissues such as gastrointestinal/vascular/bronc...Objective: To investigate the pharmacological basis of its uses of Phyla nodiflora(P. nodiflora) for the treatment of anomalies predominantly by smooth muscle containing tissues such as gastrointestinal/vascular/broncho spasm and cardiovascular modulation.Methods: The crude hydroalcoholic extract of P. nodiflora(Pn.Cr) and its fractions were evaluated on isolated rabbit jejunum, rat trachea, aorta and atrium. To access the contractile or relaxant effects of testing materials, the tissues were mounted in isolated organ bath and responses were recorded with transducers coupled with data acquisition system.BALB/c mice were challenged with castor oil for the assessment of in-vivo antidiarrheal activity. Normotensive rats were used for in-vivo hypotensive study.Results: Hydroalcoholic extract of Pn.Cr at variable concentrations inhibited the natural spontaneous rhythm and 80 mmol/L K^+ mediated contractions in isolated segment of jejunum with EC_(50) values of 3.18 and 1.91 mg/mL respectively. Verapamil, a Ca^(2+) channel blocker, demonstrated akin pattern in jejunum and therefore possibly suggesting calcium blocking activity. On isolated rat tracheal tissue, Pn.Cr showed relaxation of high-K^+and carbachol mediated contractions(EC_(50) values: 1.24 and 2.42 mg/mL). Pn.Cr treatment relaxed the rat aortic ring in a cumulative doses with high-K^+ and phenylephrine-induced contractions(EC_(50) values 0.25 and 0.92 mg/mL). Activity based fractionation of Pn.Cr showed that dichloromethane fraction was more potent for relaxing the tissues spasm compared to aqueous fraction. In-vivo experiments, significant protection by Pn.Cr(P < 0.05) was observed in castor oil-induced diarrhea(50–500 mg/kg)whereas hypotensive effect in anesthetized rats was seen at the dose range of 1–10 mg/kg of Pn.Cr(P < 0.05).Conclusion: This study suggests the blockage of calcium channel in the smooth muscles as a pharmacological application to make usage of P. nodiflora in the management of diarrhea, asthma and hypotensive effect.展开更多
Plant of Bambusa vulgaris is used in traditional medicine practice for the management of many pathologies including hypertension. The effect of the aqueous extract of the leaves of Bambusa vulgaris on blood pressure w...Plant of Bambusa vulgaris is used in traditional medicine practice for the management of many pathologies including hypertension. The effect of the aqueous extract of the leaves of Bambusa vulgaris on blood pressure was evaluated in normotensive male rabbits. Blood pressure was measured by the invasive method. Thus, aqueous extract of Bambusa vulgaris leaves had been injected intravenously at doses ranging from 1 mg/kg to 30 mg/kg in rabbits anesthetized with thiopental. The effects of this extract on blood pressure were also evaluated in rabbits having previously received different doses of atropine. The aqueous extract of Bambusa vulgaris leaves induced a dose-dependent hypotension which is not canceled in the presence of atropine. The results obtained show that the extract has blood pressure lowering effect which may be mediated by muscarinic-type cholinergic receptors.展开更多
Nociceptin (NC) and its 4 fragments have been synthesized by solid phase peptide synthesis. Their hypotensive activity and mechanism, MVD assay and structure-activity relationship have been investigated. Results show ...Nociceptin (NC) and its 4 fragments have been synthesized by solid phase peptide synthesis. Their hypotensive activity and mechanism, MVD assay and structure-activity relationship have been investigated. Results show that NC(1-13)NH2 is the smallest fragment that shares the same activity with NC. The truncation of C-terminal not only leads the decrease展开更多
以燕麦、荞麦为原料,通过半固态酶解法制备谷物多肽并以液态酶解作为对照组研究其抗氧化、降血压能力。通过凯氏定氮法测定酶解产物中多肽含量,通过总抗氧化能力(Ferric ion reducing antioxidant power,FRAP法)、羟自由基清除能力及体...以燕麦、荞麦为原料,通过半固态酶解法制备谷物多肽并以液态酶解作为对照组研究其抗氧化、降血压能力。通过凯氏定氮法测定酶解产物中多肽含量,通过总抗氧化能力(Ferric ion reducing antioxidant power,FRAP法)、羟自由基清除能力及体外血管紧张素转换酶(Angiotensin I converting enzyme,ACE)活性抑制实验测定酶解产物抗氧化及降血压能力。结果表明,以酶解产物中多肽含量、抗氧化和ACE抑制活性为指标确定了燕麦、荞麦半固态酶解最佳工艺参数分别为:酶解时间3 h,酶添加量为3.75%;酶解时间为1 h,酶添加量为2.50%,在此条件下,燕麦、荞麦所得酶解产物中多肽含量为7.03%和6.35%。1 mg/mL燕麦、荞麦多肽(半固态酶解组)羟自由基清除率为61.34%、69.33%,总抗氧化能力相当于(0.53±0.03)mmol/L和(0.48±0.01)mmol/L的FeSO4,ACE抑制率为80.27%、77.60%。半固态酶解组的多肽含量及抗氧化、ACE抑制能力均显著高于液态酶解组。采用半固态酶解工艺,既可以提高谷物肽含量,又可提高其抗氧化、ACE抑制活性,为谷物高值化加工和功能性食品配料领域的应用提供理论支持。展开更多
该文以降压靶标膜ATP敏感钾通道(ATP-sensitive potassium channel,KATP)为研究对象,构建其基于配体和基于受体结构的药效团模型,并分别筛选中药化学成分数据库(traditional Chinese medicine database,TCMD),利用分子对接评价筛选结果...该文以降压靶标膜ATP敏感钾通道(ATP-sensitive potassium channel,KATP)为研究对象,构建其基于配体和基于受体结构的药效团模型,并分别筛选中药化学成分数据库(traditional Chinese medicine database,TCMD),利用分子对接评价筛选结果,发现具有潜在KATP开放作用的中药降压活性成分。其中,基于配体的药效团模型(ligand based pharmacophore,LBP)以对人源KATP具有开放活性的48个化合物为研究对象,利用Hypogen模块进行构建,最优模型由1个氢键受体、1个氢键供体、1个疏水基团、1个芳香环和5个排除体积组成,预测训练集化合物活性相关系数为0.876 4,测试集相关系数为0.705 8,辨识有效性指数N为3.304,综合评价指数CAI为2.616;以KATP同源模建模型(PM0079770)为研究对象,构建基于受体的药效团模型(structure-based pharmacophore,SBP),最优模型具有6个氢键受体、8个氢键供体、7个疏水基团和18个排除体积,辨识有效性指数N为2.200,综合评价指数CAI为2.017。分别用2个最优模型对TCMD数据库进行筛选,对候选化合物进行Lipinski五规则及ADMET性质预测研究,LBP模型命中171个化合物,SBP模型命中178个化合物。利用分子对接技术分别对上述2组潜在中药活性成分进行评价,按照打分值由大到小的排序,分别选取对接pose个数的前3%为潜在活性化合物。得到由LBP模型虚拟筛选得到的10个化合物、由SBP模型虚拟筛选得到的2个化合物,共12个具有潜在KATP开放活性的中药成分。该研究为发现新的KATP开放剂提供了思路。展开更多
Desmodium velutinum (D. velutinum) is a plant of the family Fabaceae used in traditional Congolese medicine for the treatment of high blood pressure (HBP) or hypertension (HT). The present work evaluated the hypotensi...Desmodium velutinum (D. velutinum) is a plant of the family Fabaceae used in traditional Congolese medicine for the treatment of high blood pressure (HBP) or hypertension (HT). The present work evaluated the hypotensive activity and determined the phytochemical profile of the aqueous extract and fractions of Desmodium velutinun (Willd) D. C. (Fabaceae) in the rat. The hypotensive effect of the aqueous extract and different fractions (F1, F2, F3 and F4) was evaluated at the dose of 2.5 mg/kg in normotensive rats anesthetized with 15% urethane at 1.5 g/kg, i.p. (intraperitoneally). Our results showed that the F3 fraction after administration caused a significant decrease in blood pressure and heart rate which remained higher than that of the aqueous extract and fractions (F1, F2 and F4). The richness in polyphenolic and flavonoid compounds as well as the separating capacity of the eluent used within the F3 fraction clearly justifies the beneficial effects of the latter on blood pressure and heart rate compared with the extract and fractions (F1, F2 and F4). In a second part we carried out the qualitative (thin-layer chromatography) and quantitative (total polyphenols and flavonoids determination) analysis. The chemical compounds remained dominated by the polyphenolic and flavonoid groups, the content of total polyphenols and total flavonoids meets the following increasing order: (extract, F1, F2, F3 and F4). The results obtained could certify the use of Desmodium velutinun in traditional Congolese medicine.展开更多
文摘The use of cooled dialysate temperatures first came about in the early 1980s as a way to curb the incidence of intradialytic hypotension （IDH）. IDH was then, and it remains today, the most common complication affecting chronic hemodialysis patients. It decreases quality of life on dialysis and is an independent risk factor for mortality. Cooling dialysate was first employed as a technique to incite peripheral vasoconstriction on dialysis and in turn reduce the incidence of intradialytic hypotension. Although it has become a common practice amongst in-center hemodialysis units, cooled dialysate results in up to 70% of patients feeling cold while on dialysis and some even experience shivering. Over the years, various studies have been performed to evaluate the safety and effcacy of cooled dialysate in comparison to a standard, more thermoneutral dialysate temperature of 37℃. Although these studies are limited by small sample size, they are promising in many aspects. They demonstrated that cooled dialysis is safe and equally efficacious as thermoneutral dialysis. Although patients report feeling cold on dialysis, they also report increased energy and an improvement in their overall health following cooled dialysis. They established that cooling dialysate temperatures improves hemodynamic tolerability during and after hemodialysis, even in patients prone to IDH, and does so without adversely affecting dialysis adequacy. Cooled dialysis also reduces the incidence of IDH and has a protective effect over major organs including the heart and brain. Finally, it is an inexpensive measure that decreases economic burden by reducing necessary nursing intervention for issues that arise on hemodialysis such as IDH. Before cooled dialysate becomes standard of care for patients on chronic hemodialysis, larger studies with longer follow-up periods will need to take place to confrm the encouraging outcomes mentioned here.
基金funded by Bahauddin Zakariya University,Multan,Pakistan(No.DR&EL/D-443)
文摘Objective: To investigate the pharmacological basis of its uses of Phyla nodiflora(P. nodiflora) for the treatment of anomalies predominantly by smooth muscle containing tissues such as gastrointestinal/vascular/broncho spasm and cardiovascular modulation.Methods: The crude hydroalcoholic extract of P. nodiflora(Pn.Cr) and its fractions were evaluated on isolated rabbit jejunum, rat trachea, aorta and atrium. To access the contractile or relaxant effects of testing materials, the tissues were mounted in isolated organ bath and responses were recorded with transducers coupled with data acquisition system.BALB/c mice were challenged with castor oil for the assessment of in-vivo antidiarrheal activity. Normotensive rats were used for in-vivo hypotensive study.Results: Hydroalcoholic extract of Pn.Cr at variable concentrations inhibited the natural spontaneous rhythm and 80 mmol/L K^+ mediated contractions in isolated segment of jejunum with EC_(50) values of 3.18 and 1.91 mg/mL respectively. Verapamil, a Ca^(2+) channel blocker, demonstrated akin pattern in jejunum and therefore possibly suggesting calcium blocking activity. On isolated rat tracheal tissue, Pn.Cr showed relaxation of high-K^+and carbachol mediated contractions(EC_(50) values: 1.24 and 2.42 mg/mL). Pn.Cr treatment relaxed the rat aortic ring in a cumulative doses with high-K^+ and phenylephrine-induced contractions(EC_(50) values 0.25 and 0.92 mg/mL). Activity based fractionation of Pn.Cr showed that dichloromethane fraction was more potent for relaxing the tissues spasm compared to aqueous fraction. In-vivo experiments, significant protection by Pn.Cr(P < 0.05) was observed in castor oil-induced diarrhea(50–500 mg/kg)whereas hypotensive effect in anesthetized rats was seen at the dose range of 1–10 mg/kg of Pn.Cr(P < 0.05).Conclusion: This study suggests the blockage of calcium channel in the smooth muscles as a pharmacological application to make usage of P. nodiflora in the management of diarrhea, asthma and hypotensive effect.
文摘Plant of Bambusa vulgaris is used in traditional medicine practice for the management of many pathologies including hypertension. The effect of the aqueous extract of the leaves of Bambusa vulgaris on blood pressure was evaluated in normotensive male rabbits. Blood pressure was measured by the invasive method. Thus, aqueous extract of Bambusa vulgaris leaves had been injected intravenously at doses ranging from 1 mg/kg to 30 mg/kg in rabbits anesthetized with thiopental. The effects of this extract on blood pressure were also evaluated in rabbits having previously received different doses of atropine. The aqueous extract of Bambusa vulgaris leaves induced a dose-dependent hypotension which is not canceled in the presence of atropine. The results obtained show that the extract has blood pressure lowering effect which may be mediated by muscarinic-type cholinergic receptors.
文摘Nociceptin (NC) and its 4 fragments have been synthesized by solid phase peptide synthesis. Their hypotensive activity and mechanism, MVD assay and structure-activity relationship have been investigated. Results show that NC(1-13)NH2 is the smallest fragment that shares the same activity with NC. The truncation of C-terminal not only leads the decrease
文摘该文以降压靶标膜ATP敏感钾通道(ATP-sensitive potassium channel,KATP)为研究对象,构建其基于配体和基于受体结构的药效团模型,并分别筛选中药化学成分数据库(traditional Chinese medicine database,TCMD),利用分子对接评价筛选结果,发现具有潜在KATP开放作用的中药降压活性成分。其中,基于配体的药效团模型(ligand based pharmacophore,LBP)以对人源KATP具有开放活性的48个化合物为研究对象,利用Hypogen模块进行构建,最优模型由1个氢键受体、1个氢键供体、1个疏水基团、1个芳香环和5个排除体积组成,预测训练集化合物活性相关系数为0.876 4,测试集相关系数为0.705 8,辨识有效性指数N为3.304,综合评价指数CAI为2.616;以KATP同源模建模型(PM0079770)为研究对象,构建基于受体的药效团模型(structure-based pharmacophore,SBP),最优模型具有6个氢键受体、8个氢键供体、7个疏水基团和18个排除体积,辨识有效性指数N为2.200,综合评价指数CAI为2.017。分别用2个最优模型对TCMD数据库进行筛选,对候选化合物进行Lipinski五规则及ADMET性质预测研究,LBP模型命中171个化合物,SBP模型命中178个化合物。利用分子对接技术分别对上述2组潜在中药活性成分进行评价,按照打分值由大到小的排序,分别选取对接pose个数的前3%为潜在活性化合物。得到由LBP模型虚拟筛选得到的10个化合物、由SBP模型虚拟筛选得到的2个化合物,共12个具有潜在KATP开放活性的中药成分。该研究为发现新的KATP开放剂提供了思路。
文摘Desmodium velutinum (D. velutinum) is a plant of the family Fabaceae used in traditional Congolese medicine for the treatment of high blood pressure (HBP) or hypertension (HT). The present work evaluated the hypotensive activity and determined the phytochemical profile of the aqueous extract and fractions of Desmodium velutinun (Willd) D. C. (Fabaceae) in the rat. The hypotensive effect of the aqueous extract and different fractions (F1, F2, F3 and F4) was evaluated at the dose of 2.5 mg/kg in normotensive rats anesthetized with 15% urethane at 1.5 g/kg, i.p. (intraperitoneally). Our results showed that the F3 fraction after administration caused a significant decrease in blood pressure and heart rate which remained higher than that of the aqueous extract and fractions (F1, F2 and F4). The richness in polyphenolic and flavonoid compounds as well as the separating capacity of the eluent used within the F3 fraction clearly justifies the beneficial effects of the latter on blood pressure and heart rate compared with the extract and fractions (F1, F2 and F4). In a second part we carried out the qualitative (thin-layer chromatography) and quantitative (total polyphenols and flavonoids determination) analysis. The chemical compounds remained dominated by the polyphenolic and flavonoid groups, the content of total polyphenols and total flavonoids meets the following increasing order: (extract, F1, F2, F3 and F4). The results obtained could certify the use of Desmodium velutinun in traditional Congolese medicine.
