2. Synthesis and antitumor evaluation of desmosdumotin C derivatives on B-ring
Chinese Pharmaceutical Journal 2013;48(11):924-929
OBJECTIVE: To synthesize desmosdumotin C derivatives on B-ring with antitumor activity. METHODS: The target compounds were synthesized from 2, 4, 6-trihydroxyacetophenone via methylation, O-methylation and aldol reaction. Their antiproliferative activities were tested against six human tumor cell lines. RESULTS: Fourteen target compounds were synthesized, nine of which were new compounds. All of them were characterized using 1H-NMR, 13C-NMR and MS. CONCLUSION: Preliminary pharmacological test showed that all the title compounds except 1i exhibited potent antitumor activities. 1h and 1n were better than desmosdumotin C in vitro. Introducing two fluoro atom on B-ring would benefit its activity against some tumor cells.
3.Protective effect of magnesium isoglycyrrhizinate on the liver of hepatic arterial chemoembolization
Hongling LI ; Shibo LI ; Zhe′en ZHANG ;
Chinese Journal of Primary Medicine and Pharmacy 2016;23(19):2885-2889
Objective To investigate the protective effect of magnesium isoglycyrrhizinate on the liver of hepatic arterial chemoembolization.Methods 68 patients with hepatic arterial chemoembolization were selected as research subjects,they were divided into magnesium isoglycyrrhizinate group and control group.All patients were routinely given hepatoprotective drug treatment from seven days before surgery until three days after surgery,magnesium isoglycyrrhizinate group was given magnesium isoglycyrrhizinate treatment on the basis of hepatoprotective treatment. Detected and compared the alanine aminotransferase,aspartate aminotransferase,total bilirubin,total protein,albumin and cholinesterase levels before and after liver cancer before and after surgery.Results The alanine aminotrans-ferase,aspartate aminotransferase levels at 3 days after surgery[(60.2 ±25.8)and (71.5 ±29.6)IU /L]were higher than before surgery in the control group[(34.7 ±18.6)and (49.5 ±20.4)IU /L](t =7.264 and 5.974,all P <0.05).The alanine aminotransferase,aspartate aminotransferase levels at 3 days after surgery had no differences with before surgery in the magnesium isoglycyrrhizinate group (P >0.05).The alanine aminotransferase,aspartate amin-otransferase and total bilirubin levels before surgery in magnesium isoglycyrrhizinate group had no differences with the control group (P >0.05).The alanine aminotransferase,aspartate aminotransferase levels at 3 days after surgery in the magnesium isoglycyrrhizinate group[(44.8 ±22.8)and (57.3 ±24.8)IU /L]were higher than those in the control group[(60.2 ±25.8)and (71.5 ±29.6)IU /L](t =6.385 and 7.358,all P <0.05).The albumin and cholinesterase levels at 3 days after surgery in the magnesium isoglycyrrhizinate group and the control group[(28.4 ± 4.7)g/L,(8.0 ±4.8)kU /L and (29.3 ±3.5)g/L,(6.9 ±4.3)kU /L]were lower than before surgery[(34.2 ± 4.3)g/L,(9.3 ±5.4)kU /L and (33.7 ±3.9)g/L,(9.0 ±5.8)kU /L](t =11.834,6.247 and 10.276,8.743,all P <0.05).The albumin and cholinesterase levels before surgery in the magnesium isoglycyrrhizinate group had no differences with the control group (P >0.05).The albumin and cholinesterase levels at 3 days after surgery in the magnesium isoglycyrrhizinate group[(28.4 ±4.7)g/L,(8.0 ±4.8)kU /L]were lower than those of control group [(29.3 ±3.5 )g/L,(6.9 ±4.3)kU /L](t =8.436 and 6.947,all P <0.05 ).The incidence rates of adverse reactions of the magnesium isoglycyrrhizinate group (upper abdominal pain incidence rate was 35.3%,fever incidence rate was 29.4%,nausea and vomiting incidence rate was 52.9%)were lower than those of the control group(55.9%,88.2%,76.5%)(χ2 =7.246,6.472,6.274,all P <0.05).Conclusion Hepatic arterial chemoem-bolization has some damage to liver function of liver cancer patients.Magnesium isoglycyrrhizinate can reduce liver damage,improve liver synthetic function,and has a protective effect on liver.
5.Roles and their mechanisms of neuroglobin in cerebral ischemia
Liu LIU ; Danfang LI ; En XU
International Journal of Cerebrovascular Diseases 2014;22(1):62-66
Neuroglobin (Ngb) is an oxygen-carrying globin that specifically expresses in brain tissue.It is involved in energy metabolism,mitochondrial function,as well as cell survival and proliferation of signaling pathway regulation.Under physiological conditions,Ngb presents as a form of ferrous deoxy hexacoordination,which has stronger oxygen affinity.During ischemia and hypoxia,the expression of Ngb is upregulated in brain tissue and interacts through a variety of proteins of its downstream,and plays a protective role for the damaged brain tissue.
7.Influence of plant growth regulater on yield and quality of Salvia miltiorrhiza.
China Journal of Chinese Materia Medica 2014;39(11):1992-1994
The study is aimed to investigate the effect of plant growth regulators on yield and quality of the Salvia miltiorrhiza. The plant growth regulators was spraying on Salvia plants in July or August in field experiment, then the yield, ingredient content and the antioxidant activity were determined. The results showed that plant growth regulator 'Zhuanggenling' could increase the yield of Salvia with root-planting by 38.45%. Plant growth regulator 'Duoxiaozuo' could increase the yield of Salvia with seedling planting by 14.19%. Both plant growth regulator significantly reduced the antioxidant activity of Salvia in vitro, but they had no significant effect on active ingredient contents.
Diterpenes, Abietane
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analysis
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Phenanthrenes
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analysis
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Plant Extracts
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analysis
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Plant Growth Regulators
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pharmacology
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Salvia miltiorrhiza
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chemistry
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drug effects
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growth & development
8.MiR-150 improves cardiac fibrosis after myocardial infarction by targeting c-Myb
Xiaocui ZHOU ; Tao WANG ; En LI
The Journal of Practical Medicine 2017;33(7):1078-1082
Objective To evaluate the role and mechanism of miR-150 in cardiac fibrosis after MI.Methods A rat model of MI was established by up-regulating miR-150 through overexpressing miR-150 lentivirus.Real-time PCR and Western blot were applied in detecting the expression of collagen 1 α 1 and α-SMA protein in infarction area border.Masson coloration was applied in measuring fibrosis.Cardiac fibroblasts were isolated and cultured.UTR was used to report the carrier and lentivirus.And c-Myb siRNA was used to verify the relationship between c-Myb and microRNA-150.Results In vivo,MiR-150 was down-regulated in myocardium border zone in 14 day and 28 day after infarction (P < 0.001,P < 0.05),and overexpressing miR-150 promoted myocardial fibrosis (P < 0.001),and inhibited the expression of collagen1α 1 and α-SMA (P < 0.01,P < 0.05).In vitro,c-Myb was the direct target gene of miR-150,and inhibited the expression of c-Myb resulting in the down regulation of collagen1α 1 and α-SMA,suggesting that the role of miR-150 was achieved by regulating c-Myb.Conclusions MiR-150 was down-regulated in myocardium border zone,and myocardial fibrosis can be improved by targeting c-Myb.
9.Study on changes of TNF-α and IL-1 in spleen cells of mice induced by recombinant BCG-Sj26GST vaccine of schistosoma japonicum
Chinese Journal of Endemiology 2001;20(3):172-174
Objective To study the effects of recombinant BCG-Sj26GST vaccine of schistosoma japonicum of TNF-α and IL-1 produced by spleen cells of mice.Methods In experiment 1,BALB/C mice were immnized subcutaneously by 106 and 108 CFU vaccine respectively,challenged with Sj cercariae on 8 w of immunization and killed on 6 w of infection to separate spleens,PBS served as control;in experiment 2,after immunized subcutaneously and intravenously by 106 CFU vaccine respectively,4 mice were killed to separate sleens on 0,4,8,10,14 and 16 w of immunization,spleen cells were stimulated by Sj26 or mitogens,the level of TNF-α in supernatant of spleen cells were detected by ELISA,that of IL-1 by fibroblast proliferative response.Results Levels of TNF-α and IL-1 increased obviously by immunization with the vaccine against challenge with Sj cercariae;dynamic observation showed that TNF-α and IL-1 in the subcutaneous group reached the highest level on 4~8 w;that in the intravenous group on 16 w and 4~8 w respectively.Conclusions Recombinant BCG-Sj26GST vaccine of schistosoma japonicum may promote spleen cell of mice to secrete TNF-α and IL-1 early,these cytokines may play an important role in protective immunity against schistosomiasis.
10. Pharmacokinetic study of total glucosides of paeony in rats with acute liver injury and normal rats
Chinese Pharmaceutical Journal 2012;47(7):534-538
OBJECTIVE: To compare the pharmacokinetics of total glucosides of paeony (TGP) in rats with acute liver injury and normal rats, thus to provide evidence for determining dosage regimen in clinic. METHODS: Acute liver injury rat model was established by single CCl4 intraperitoneal injection. Three dosages of TGP were orally administered to normal and model rats. The concentrations of Pae and Alb in plasma at different time after dosing were determined with HPLC method. The pharmacokinetic parameters were calculated based on mean plasma concentration-time curves of Pae and Alb. RESULTS: In model rat group, the t1/2 of Pae and Alb at high, medium, and low dosage (0.047, 0.141, 0.282 g · mL-1) were 5.02, 4.52, 4.91 h and 5.22, 5.04, 5.05 h, respectively. The ρmax of Pae and Alb of TGP at different dosages were 22.54, 14.52, 5.49 μg · mL-1, and 9.02, 5.04, 2.34 μg · mL-1, respectively. The AUC0-t of Pae and Alb of TGP at different dosages were (146.55 ± 7.52), (84.14 ± 7.84), (31.62 ± 2.97) μg · h · mL-1, and (56.56 ±8.70), (32.18 ± 3.49), (13.48 ±1.66) μg · h · mL-1, respectively. The tmax of paeoniflorin(Pae) and albiflorin(Alb) of TGP at different dosages were both 2 h. In rats of normal group, the t1/2 of Pae and Alb of TGP at different dosages respectively were 3.95, 3.69, 3.95 h, and 3.74, 3.98, 3.79 h, respectively. The ρmax were 19.16, 11.60, 4.46 μg · mL-1, and 7.16, 4.00, 1.93 μg · mL-1, respectively. The AUC0-t were (116.26.6 ± 19.99), (67.74 ± 12.79), (25.01 ±2.62) μg · h · mL-1, and (45.03 ±5.84), (27.26 ±3.57), (10.59 ± 1.86) μg · h · mL-1, respectively. The tmax were both 2.5 h. CONCLUSION: Compared with normal group, the ρmax and AUC0-t of TGP in model group significantly increased, tmax decreased, and t1/2 prolonged; tmax and t1/2 had no difference among three dosages, and ρmax. and AUC0-t had correlation with dosage. Copyright 2012 by the Chinese Pharmaceutical Association.