2.Study of Leshibao Capsule on gastrointestinal function
Shiwei CHEN ; Hong ZHENG ; Hongmin ZHANG ; Qizhong ZHENG ;
Chinese Traditional Patent Medicine 1992;0(04):-
Objective: To study the function of Leshibao Capsule (Radix Ginseng, Rhizoma Atractylodis, Sea cucumber, etc.) on stomach and intestines. Methods: Gastrointestinal function was measured by small intestine driving test, gastric juice quantity, pepsin activity and gastric emptying time. Results: Leshibao Capsule could increase gastric juice, enhance pepsin activity. It could adjust function of gastrointestine in two ways that showed gastrointestinal movement fasted by neostigmine and inhibited gastrointestinal movement slowed by diphenoxylate and morphine hydrochloride. Conclusion: Leshibao Capsule can adjust gastrointestinal function and facilitate digestive function.
3.Diversity-oriented synthesis and its application in drug discovery.
Lei ZHANG ; Ming-yue ZHENG ; Hong LIU
Acta Pharmaceutica Sinica 2015;50(4):419-433
Diversity-oriented synthesis (DOS) aims to efficiently generate collections of small molecules with diverse appendages, functional groups, stereochemistry and skeletons, thus yielding diverse biological activities capable of modulating a wide variety of biological processes. In this review, we discussed the common strategies employed in DOS with specific examples from recent literature, including reagent-based approach, substrate-based approach, build-couple-pair strategy and privileged substructure-based DOS. The application of some DOS libraries in drug discovery is also presented.
Drug Design
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Drug Discovery
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Small Molecule Libraries
5.Effects of Icariin of experimental IgA nephropathy in rats
Hong ZHANG ; Nian LIU ; Zheng LI
Chinese Journal of Comparative Medicine 2017;27(1):73-78
Objective To investigate the effect of Icariin ( ICA) experimental IgA nephropathy in rats and to explore related mechanisms .Methods Experimental IgA nephropathy rat model was established and then model rat were treated with or without different doses of ICA .Then, urine RBC, Urine protein and urine NAG were analyzed; IgA precipitation was detected with immunofluorescence staining;the protein level of NF-κBp65 and MCP-1 were examined by immunohistochemical staining;the mRNA level of IL-4, IL-10 and IL-13 were determined by quantitative PCR .Results The concentrations of urine RBC, Urine protein and urine NAG were reduced after ICA treatment , as companied by a decrease of IgA precipitation .Moreover, ICA treatment also decreased the protein level of NF-κBp65 and MCP-1, and the mRNA level of IL-4, IL-10 and IL-13.Conclusions ICA exerts a certain degree of efficacy on the treatment of experimental IgA nephropathy through regulating NF-κBp65 and MCP-1 expression and the immunoregulation mechanism .
6.Anesthetic efficacy of epidural ropivacaine mixed with different doses of snfentanil for hysterectomy
Hong ZHENG ; Zhiqun XIA ; Qing ZHANG
Chinese Journal of Anesthesiology 1994;0(04):-
Objective To assess the efficacy of ropivacaine in combination with different doses of sufentanil for epidural anesthesia in patients undergoing hysterectomy. Methods Eighty ASA Ⅰ or Ⅱ patients aged 30-55 yrs weighing 40-70 kg undergoing elective hysterectomy were randomly divided into 4 groups ( n = 20 each) : ropivacaine group (R) and 3 ropivacaine-sufentanil groups (R-S1-3). The patients were unpremedicated. ECG, BP, HR and SpO2 were monitored during ansthesia. Each patient received an epidural catheter placed at L2,3 interspace. After correct placement of epidural catheter was confirmed 0.75% ropivacaine 13 ml and normal saline (NS) 2 ml were given through epidural catheter in group R whereas in the 3 R-S groups 0.75% ropivacaine 13 ml and sufentanil 10 (R-S1), 20 (R-S2) or 30 (R-S3) ?g in NS 2 ml were injected into epidural space. BP, HR and SpO2 were recorded every 3 min. The onset time, upper spread and duration of sensory block; onset and duration of motor block (Bromage scale); degree of abdominal muscle relaxation; level of sedation (OAA/S scale); anesthetic efficacy and side-effects were recorded. The dose-response curve constructed by probit regression analysis was established to calculate ED50 and ED95. Results The onset time, the time needed to reach the highest sensory level were significantly shorter and the duration of sensory block was significantly longer in the 3 R-S groups than in R group ( P
7.The inhibitory effect of capsaicin on streptozocin-induced apoptosis of rat retinal cells
Ting, ZHANG ; Ji-hong, YANG ; Zheng, GUO
Chinese Journal of Experimental Ophthalmology 2013;(1):34-38
Background Diabetes mellitus (DM) can provoke the apoptosis of retinal cells and downregulate the expression of calcitonin gene related peptide (CGRP) in the retina.Capsaicin promotes the release of CGRP and elicits protective effects on human organs.However,whether CGRP protects retinal cells in diabetic retinopathy (DR) is still unclear.Objective The study was designed to examine the effect of capsaicin on the apoptosis of retinal cells in diabetic rats and its relationship with CGRP.Methods Forty clean healthy adult male Sprague-Dawey rats were randomly divided into the diabetes group,capsaicin pretreated group,streptozocin (STZ)control group,capsaicin control group and plain control group,with 8 rats per group.The diabetic model was established by the intraperitoneal injection of 60 mg/kg in all rats except those of the plain control group.0.4 mL of a 1% capsaicin injected at 20 mg/kg was subcutaneously injected for 3 consecutive days prior to model establishment in the capsaicin pretreated group,after which 1.2 mL of STZ was intraperitoneally injected on the fourth day.Rats from the STZ control group were administered intraperitoneally 1.2 mL of 0.1 mol/L,pH 4.5,citrate buffer.The capsaicin control group received subcutaneous injections of 0.4 mL of 1% capsaicin at 20 mg/kg for 3 consecutive days,after which 1.2 mL of 0.1 mol/L,pH 4.5,citrate buffer was administered intraperitoneally.The rats were sacrificed at the tenth week after model establishment and retinal specimens were prepared for the apoptosis assay by TUNEL staining and the quantitative analysis of caspase-3 activity.Expression of CGRP in the retina and serum was detected using ELISA.The use of experimental animals followed the Regulations for the Administration of Affairs Concerning Experimental Animals by State Science and Technology Commission.Results Retinal cell apoptosis was mainly localized to the retinal ganglion cell (RGC) layer.The apoptosis rate of RGCs was (43.4±5.0)% in the DR model group and (30.0±5.1)% in the capsaicin pretreated group,showing a significant difference (t =5.930,P<0.01).Compared with the DR model group and capsaicin pretreated group,the apoptosis rates of the DR control group (12.4±9.9) % and the capsaicin control group (17.6-±6.1) % were significantly lower (t =8.800,t =4.925,P<0.01).The apoptosis rate of the plain control group was (16.2±6.9)%,exhibiting significant differences in comparison with the DR control group and capsaicin control group (t =-0.989,t =0.951,P>0.05).The specific activity of caspase-3 was (2.19±0.86) in the DR model group and (1.96±0.56) in the capsaicin pretreated group,presenting a significant difference (t =-0.515,P<0.05).Those of the DR control group and capsaicin control group were (1.47±0.14) and (0.74±0.27),respectively,with considerable decline in comparison with the DR model group and capsaicin pretreated group (t=2.142,t=2.797,P<0.05).The retinal and serum CGRP levels were (424.4±44.2)and (148.8±39.1) ng/L,respectively,displaying significantly lower levels than (543.2±74.4) and (237.5±78.7) ng/L (t =3.070,2.359,P<0.05) from the capsaicin pretreated group.Conclusions Apoptosis of retinal ganglion cells occurs in the STZ-induced diabetic rats.Pretreatment of capsaicin reduces retinal cell apoptosis,which may be associated with an increase of CGRP in the retina.
8.Protective effects of thioltransferase (TTase) on oxidative damaged human lens epithelial cells induced by ultraviolet radiation
Xiaoliang ZHENG ; Jie ZHANG ; Hong YAN
Recent Advances in Ophthalmology 2017;37(7):601-604
Objective To discuss the protective effects of thioltransferase (TTase) on oxidative damaged human lens epithelial cells (HLEC) induced by ultraviolet radiation.Methods HLEC were cultured in vitro and then randomly divided into 4 groups:Normal group:normal cultured HLEC;UV group:normal cultured HLEC + UV radiation (with 302 nm UV radiation irradiation intensity 55.56 μW · cm-2 for 15 minutes,totaling irradiation volume 500 J · m-2);TTase siRNA group:HLEC transfected with TTase siRNA;TTase siRNA + UV group:HLEC transfected with TTase siRNA + UV radiation(with 302 nm UV radiation irradiation intensity 55.56 μW · cm-2 for 15 minutes,totaling irradiation volume 500 J · m-2).TTase mRNA expression was measured by qRT-PCR,the cell proliferation was detected by LDH Assay Kit,and the TTase activity was measured.TTase expression was detected by Western blotting.The levels of TGSH,GSH and GSSG of HLEC were measured,and then GSSG/T-GSH ratio was calculated.Results Cell proliferation ability in UV group,TTase siRNA group and TTase siRNA + UV group were decreased by 21.0%,17.0% and 29.0% compared with normal group (all P < 0.05).TTase activity in UV group was 2.1 times of the normal group,TTlase siRNA group was 67.0% of the normal group,Tlase siRNA + UV group was 1.3 times of TTase siRNA group (all P < 0.05).TTase expression in UV group was 3.9 times of the normal group,TTase siRNA group was 35.0% of the normal group,TTase siRNA + UV group was 3.0 times of siRNA group (all P < 0.05).GSH content in UV group,TTase siRNA group and TTase siRNA + UV group were 68.4%,79.0%,61.7% of the normal group (all P < 0.05).GSSG content in UV group,TTase siRNA group and TTase siRNA + UV group were 2.3 times,1.4 times,3.7 times of the normal group (all P < 0.05).GSSG/T-GSH in UV group,TTase siRNA group and TTase siRNA + UV group were 3.1 times,1.7 times,5.2 times of the normal group (all P < 0.05).Conclusion TTase plays an important protective role in oxidative damaged HLEC induced by ultraviolet radiation.
9.Research progress of surgery for age-related macular degeneration with cataract
Xiao-Liang, ZHENG ; Jie, ZHANG ; Hong, YAN
International Eye Science 2017;17(9):1678-1681
Age-related macular degeneration (AMD) and cataract are the most common causes of low vision worldwide.Nowadays, there is still a controversy about whether cataract surgery should be taken in patients combined with AMD and when should the surgery be taken.The aim of this review is to assess the influence of cataract surgery on the occurrence and development of AMD, to analyze the risk factors, to explore the occasion of cataract surgery in patients with AMD, and joint with anti-vascular endothelial growth factor (VEGF) treatment, also including the development and application of intraocular lens.It helps to avoid and postpone the development and progression of macular degeneration after cataract surgery and get good visual outcome.
10.Diversity-oriented synthesis and its application in drug discovery.
Lei ZHANG ; Mingyue ZHENG ; Hong LIU
Acta Pharmaceutica Sinica 2015;50(4):419-33
Diversity-oriented synthesis (DOS) aims to efficiently generate collections of small molecules with diverse appendages, functional groups, stereochemistry and skeletons, thus yielding diverse biological activities capable of modulating a wide variety of biological processes. In this review, we discussed the common strategies employed in DOS with specific examples from recent literature, including reagent-based approach, substrate-based approach, build-couple-pair strategy and privileged substructure-based DOS. The application of some DOS libraries in drug discovery is also presented.