目的以肺泡巨噬细胞为研究对象,观察脂多糖(lipopolysaccharide,LPS)刺激下RBD-2(大鼠β防御素-2,Rat-βdefensins-2)在正常大鼠及糖尿病大鼠肺泡巨噬细胞表达的变化。方法以健康雄性SD大鼠制备糖尿病模型。32只大鼠随机分为四组:正常...目的以肺泡巨噬细胞为研究对象,观察脂多糖(lipopolysaccharide,LPS)刺激下RBD-2(大鼠β防御素-2,Rat-βdefensins-2)在正常大鼠及糖尿病大鼠肺泡巨噬细胞表达的变化。方法以健康雄性SD大鼠制备糖尿病模型。32只大鼠随机分为四组:正常对照组(A组)、糖尿病组(B组)、LPS组(C组)和糖尿病+LPS组(D组),每组均为8只。分离培养大鼠肺泡巨噬细胞,通过RT-PCR以及Western blotting分别检测RBD-2的RNA及蛋白质表达水平,同时通过Real Time PCR检测大鼠肺泡巨噬细胞的TLR-2以及TLR-4的mRNA的表达。结果大鼠糖尿病模型构建成功。RT-PCR以及Western blotting结果显示,与正常组相比,糖尿病组、正常组+LPS组、糖尿病+脂多糖组的RBD-2 mRNA以及蛋白质表达水平依次增加,差异显著(P<0.05)。Real Time PCR结果显示,与正常组相比,糖尿病组、正常组+LPS组、糖尿病+脂多糖组的TLR-4 mRNA的表达水平依次增加,差异显著(P<0.05),而TLR-2差异则不明显。结论 LPS刺激后糖尿病大鼠肺泡巨噬细胞RBD-2表达增加较糖尿病组更为显著,说明RBD-2变化对于增强糖尿病机体的非特异性免疫能力具有明显的帮助,同时糖尿病大鼠肺泡巨噬细胞RBD-2表达较正常组增高,说明处于糖尿病时期的大鼠机体处于炎症状态,并且这一通路的表达受体主要是TLR-4受体。展开更多
Virtual screening is a computational technique widely used for identifying small molecules which are most likely to bind to a protein target. In the present work, a molecular docking study is carried out to propose po...Virtual screening is a computational technique widely used for identifying small molecules which are most likely to bind to a protein target. In the present work, a molecular docking study is carried out to propose potential candidates for preventing the RBD/ACE2 attachment. These candidates are sixteen different flavonoids present in the peppermint leaf. Results showed that Luteolin 7-O-neohesperidoside is the peppermint flavonoid with a higher binding affinity regarding the RBD/ACE2 complex (about -9.18 Kcal/mol). On the other hand, Sakuranetin presented the lowest affinity (about -6.38 Kcal/mol). Binding affinities of the other peppermint flavonoids ranged from -6.44 Kcal/mol up to -9.05 Kcal/mol. The binding site surface analysis showed pocket-like regions on the RBD/ACE2 complex that yield several interactions (mostly hydrogen bonds) between the flavonoid and the amino acid residues of the proteins. This study can open channels for the understanding of the roles of flavonoids against COVID-19 infection.展开更多
To the Editor:The current coronavirus disease-19(COVID-19)pandemic spurs the development of antiviral drugs for SARS-CoV-2,as the number of patients with viral infections continues to rise globally in the context of w...To the Editor:The current coronavirus disease-19(COVID-19)pandemic spurs the development of antiviral drugs for SARS-CoV-2,as the number of patients with viral infections continues to rise globally in the context of widespread vaccination.Targeting the interaction between the receptor binding domain(RBD)of SARS-CoV-2 spike protein and the host cell ACE2 is a promising therapeutic strategy to effectively inhibit viral entry.展开更多
文摘目的以肺泡巨噬细胞为研究对象,观察脂多糖(lipopolysaccharide,LPS)刺激下RBD-2(大鼠β防御素-2,Rat-βdefensins-2)在正常大鼠及糖尿病大鼠肺泡巨噬细胞表达的变化。方法以健康雄性SD大鼠制备糖尿病模型。32只大鼠随机分为四组:正常对照组(A组)、糖尿病组(B组)、LPS组(C组)和糖尿病+LPS组(D组),每组均为8只。分离培养大鼠肺泡巨噬细胞,通过RT-PCR以及Western blotting分别检测RBD-2的RNA及蛋白质表达水平,同时通过Real Time PCR检测大鼠肺泡巨噬细胞的TLR-2以及TLR-4的mRNA的表达。结果大鼠糖尿病模型构建成功。RT-PCR以及Western blotting结果显示,与正常组相比,糖尿病组、正常组+LPS组、糖尿病+脂多糖组的RBD-2 mRNA以及蛋白质表达水平依次增加,差异显著(P<0.05)。Real Time PCR结果显示,与正常组相比,糖尿病组、正常组+LPS组、糖尿病+脂多糖组的TLR-4 mRNA的表达水平依次增加,差异显著(P<0.05),而TLR-2差异则不明显。结论 LPS刺激后糖尿病大鼠肺泡巨噬细胞RBD-2表达增加较糖尿病组更为显著,说明RBD-2变化对于增强糖尿病机体的非特异性免疫能力具有明显的帮助,同时糖尿病大鼠肺泡巨噬细胞RBD-2表达较正常组增高,说明处于糖尿病时期的大鼠机体处于炎症状态,并且这一通路的表达受体主要是TLR-4受体。
文摘Virtual screening is a computational technique widely used for identifying small molecules which are most likely to bind to a protein target. In the present work, a molecular docking study is carried out to propose potential candidates for preventing the RBD/ACE2 attachment. These candidates are sixteen different flavonoids present in the peppermint leaf. Results showed that Luteolin 7-O-neohesperidoside is the peppermint flavonoid with a higher binding affinity regarding the RBD/ACE2 complex (about -9.18 Kcal/mol). On the other hand, Sakuranetin presented the lowest affinity (about -6.38 Kcal/mol). Binding affinities of the other peppermint flavonoids ranged from -6.44 Kcal/mol up to -9.05 Kcal/mol. The binding site surface analysis showed pocket-like regions on the RBD/ACE2 complex that yield several interactions (mostly hydrogen bonds) between the flavonoid and the amino acid residues of the proteins. This study can open channels for the understanding of the roles of flavonoids against COVID-19 infection.
基金supported by the National Natural Science Foundation of China (22078314, 21878286, 21908216)Dalian Institute of Chemical Physics (DICPI202142, DICPI202006, DICPI201938, DICPZZBS201805, China)
文摘To the Editor:The current coronavirus disease-19(COVID-19)pandemic spurs the development of antiviral drugs for SARS-CoV-2,as the number of patients with viral infections continues to rise globally in the context of widespread vaccination.Targeting the interaction between the receptor binding domain(RBD)of SARS-CoV-2 spike protein and the host cell ACE2 is a promising therapeutic strategy to effectively inhibit viral entry.
