2-Phenoxy-4H-spiro { naphtho[2,3-e] [ 1,4,2]oxazaphosphinane-5,10-dione, 1′-cyclo- hexane}2-oxide （C22H20NO5P） was synthesized by the Mannich-type reaction of 2-amino-3- hydroxy-l,4-naphthoquinone with phenyl phosp...2-Phenoxy-4H-spiro { naphtho[2,3-e] [ 1,4,2]oxazaphosphinane-5,10-dione, 1′-cyclo- hexane}2-oxide （C22H20NO5P） was synthesized by the Mannich-type reaction of 2-amino-3- hydroxy-l,4-naphthoquinone with phenyl phosphorodichloridite and cyclohexanone, and structurally characterized by single-crystal X-ray diffraction analysis. It crystallizes in monoclinic, space group P2 1/n with a = 7.9133（11）, b = 13.0269（18）, c = 19.091（3） ,A,β = 101.906（2）°, V= 1925.6（5） ,A^3, Z= 4, Mr = 409.36, Dr = 1.412 g/cm^3, F（000） = 856,μ = 0.178 mm^-1, S = 1.015, the final R = 0.0381 and wR = 0.0906 for 2718 observed reflections with 1 〉 2σ（I） and 262 variable parameters. This compound may be used as DNA-intercalator. Its cytotoxic activities were also tested in vitro on four human tumor cell lines.展开更多
OBJECTIVE: To investigate the effect of Shenfuqiangxin capsule and the underlying mechanism on cardio-renal syndrome(CRS) in rats induced by infrarenal aortic-clamping after renal ischaemia.METHODS: Male Wistar rats u...OBJECTIVE: To investigate the effect of Shenfuqiangxin capsule and the underlying mechanism on cardio-renal syndrome(CRS) in rats induced by infrarenal aortic-clamping after renal ischaemia.METHODS: Male Wistar rats underwent infrarenal aortic-clamping after renal ischaemia or sham operation. The surviving CRS rats were divided randomly into three groups: CRS group(CRS + 10 m L·kg-1·d-1pure water by gavage), SFQX group(CRS + 13.2 g crude drug·kg- 1·d- 1Shenfuqiangxin by gavage),and handleregionpeptide(HRP)group(CRS+10mg/kg HRP by vein). Sham operation rats were given10 m L·kg-1·d-1pure water. Treatments were given8 weeks after surgery, which lasted for 4 weeks. Therats were detected for heart structure and function by transthoracic echocardiography. PPR m RNA was detected by Reverse Transcription Polymerase Chain Reaction(RT-PCR). To determine whether the mitogen-activated protein kinase(MAPK) signal pathway is included in the heart and kidney protective function of Shenfuqiangxin capsule, MAPK related proteins such as posophorylated C-Jun amino terminal kinase(p-JNK), posophorylated extracellular signal-regulated kinase ?(p-ERK1/2), posophorylated p38(p-p38) were examined by Western Blot.Apoptosis in heart and kidney tissues were detected by d UTP Nick End Labeling staining.RESULTS: Shenfuqiangxin capsule alleviated myocardial apoptosis and inhibited PRR m RNA expression and p-JNK, p-ERK1/2, p-p38 proteins expression in CRS rats.CONCLUSION: All the results suggest that Shenfuqiangxin capsule improves the injured heart and kidney function maybe through inhibition of MAPK response pathway.展开更多
文摘2-Phenoxy-4H-spiro { naphtho[2,3-e] [ 1,4,2]oxazaphosphinane-5,10-dione, 1′-cyclo- hexane}2-oxide （C22H20NO5P） was synthesized by the Mannich-type reaction of 2-amino-3- hydroxy-l,4-naphthoquinone with phenyl phosphorodichloridite and cyclohexanone, and structurally characterized by single-crystal X-ray diffraction analysis. It crystallizes in monoclinic, space group P2 1/n with a = 7.9133（11）, b = 13.0269（18）, c = 19.091（3） ,A,β = 101.906（2）°, V= 1925.6（5） ,A^3, Z= 4, Mr = 409.36, Dr = 1.412 g/cm^3, F（000） = 856,μ = 0.178 mm^-1, S = 1.015, the final R = 0.0381 and wR = 0.0906 for 2718 observed reflections with 1 〉 2σ（I） and 262 variable parameters. This compound may be used as DNA-intercalator. Its cytotoxic activities were also tested in vitro on four human tumor cell lines.
基金Natural Science Foundation-funded Project:Study on Mechanism of Invigorate Qi Warm Yang Activate Blood And Promote Dieresis Treatment Adjusted By MAPK Mediated by(P)RR(No.30973795)Sponsored by the the National Natural Science Foundation of China(No.81202801)
文摘OBJECTIVE: To investigate the effect of Shenfuqiangxin capsule and the underlying mechanism on cardio-renal syndrome(CRS) in rats induced by infrarenal aortic-clamping after renal ischaemia.METHODS: Male Wistar rats underwent infrarenal aortic-clamping after renal ischaemia or sham operation. The surviving CRS rats were divided randomly into three groups: CRS group(CRS + 10 m L·kg-1·d-1pure water by gavage), SFQX group(CRS + 13.2 g crude drug·kg- 1·d- 1Shenfuqiangxin by gavage),and handleregionpeptide(HRP)group(CRS+10mg/kg HRP by vein). Sham operation rats were given10 m L·kg-1·d-1pure water. Treatments were given8 weeks after surgery, which lasted for 4 weeks. Therats were detected for heart structure and function by transthoracic echocardiography. PPR m RNA was detected by Reverse Transcription Polymerase Chain Reaction(RT-PCR). To determine whether the mitogen-activated protein kinase(MAPK) signal pathway is included in the heart and kidney protective function of Shenfuqiangxin capsule, MAPK related proteins such as posophorylated C-Jun amino terminal kinase(p-JNK), posophorylated extracellular signal-regulated kinase ?(p-ERK1/2), posophorylated p38(p-p38) were examined by Western Blot.Apoptosis in heart and kidney tissues were detected by d UTP Nick End Labeling staining.RESULTS: Shenfuqiangxin capsule alleviated myocardial apoptosis and inhibited PRR m RNA expression and p-JNK, p-ERK1/2, p-p38 proteins expression in CRS rats.CONCLUSION: All the results suggest that Shenfuqiangxin capsule improves the injured heart and kidney function maybe through inhibition of MAPK response pathway.
