2.Study on lipid-lowering traditional Chinese medicines based on pharmacophore technology and patent retrieval.
Xiao-qian HUO ; Yu-su HE ; Lian-sheng QIAO ; Zhi-yi SUN ; Yan-ling ZHANG
China Journal of Chinese Materia Medica 2014;39(24):4839-4843
The combined application of statins that inhibit HMG-CoA reductase and fibrates that activate PPAR-α can produce a better lipid-lowering effect than the simple application, but with stronger adverse reactions at the same time. In the treatment of hyperlipidemia, the combined administration of TCMs and HMG-CoA reductase inhibitor in treating hyperlipidemia shows stable efficacy and less adverse reactions, and provides a new option for the combined application of drugs. In this article, the pharmacophore technology was used to search chemical components of TCMs, trace their source herbs, and determine the potential common TCMs that could activate PPAR-α. Because there is no hyperlipidemia-related medication reference in modern TCM classics, to ensure the high safety and efficacy of all selected TCMs, we selected TCMs that are proved to be combined with statins in the World Traditional/Natural Medicine Patent Database, analyzed corresponding drugs in pharmacophore results based on that, and finally obtained common TCMs that can be applied in PPAR-α and combined with statins. Specifically, the pharmacophore model was based on eight receptor-ligand complexes of PPAR-α. The Receptor-Ligand Pharmacophore Generation module in the DS program was used to build the model, optimize with the Screen Library module, and get the best sub-pharmacophore, which consisted of two hydrogen bond acceptor, three hydrophobic groups and 19 excluded volumes, with the identification effectiveness index value N of 2. 82 and the comprehensive evaluation index CAI value of 1. 84. The model was used to screen the TCMD database, hit 5,235 kinds of chemical components and 1 193 natural animals and plants, and finally determine 62 TCMs. Through patent retrieval, we found 38 TCMs; After comparing with the virtual screening results, we finally got seven TCMs.
Acyl Coenzyme A
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metabolism
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Animals
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Databases, Factual
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Drugs, Chinese Herbal
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chemistry
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pharmacology
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Hydrophobic and Hydrophilic Interactions
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Hydroxymethylglutaryl-CoA Reductase Inhibitors
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chemistry
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pharmacology
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Lipid Metabolism
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drug effects
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Lipids
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blood
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Medicine, Chinese Traditional
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Models, Molecular
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Quantitative Structure-Activity Relationship
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Technology
4.Expression of IL-18 in the peripheral blood mononuclear cells of chronic hepatitis B patients
Weiqun WEN ; Lian ZHANG ; Zhangyong HU ; Mingxia ZHANG ; Hong XIAO ; Yi QIAN
Immunological Journal 2001;(2):125-127
Objective To investigated the possible roles of IL-18 in HBV infection, and the expression of IL-18 in the peripheral blood mononuclear cells (PBMC) of chronic hepatitis B. Methods In 15 cases of asymptomatic carriers, 30 cases of active and remissive phases of chronic hepatitis and 10 healthy individuals (as normal controls), IL-18 expression in PBMC were quantitatively analyzed with flow cytometric immunological method. The PBMC were separated routinely and stimulated with LPS (SIGMA) and Monensin (SIGMA) for 6 hours. Then the cells were harvested and fixed by PBS/4% paraformaldehyde. The treated cells were stored in liquid nitrogen for detection later. After immunologic stain, the expression of IL-18 in PBMC were examined by flow cytometry. Results ① IL-18 was the lowest in asymptomatic carriers. It was fewer in remissive phase than in normal controls (P<0.01).There was no difference between active phase and normal controls(P=0.25).②Within the group of active phase, IL-18 was significantly different between each grade of inflammatory activity(P<0.01),and correlated with serum ALT positively(r=0.63,P<0.01). Conclusion IL-18 may relate to disease activity and the inflammation of liver.
5.Research on needle-acupointomics.
Shu-Hua XIAO ; Lian-Hai WEI ; Yi GUO
Chinese Acupuncture & Moxibustion 2012;32(3):261-263
The concept of needle-acupointomics should be clarified initially in order to discuss the relative researches. The comprehension can be deepened through the aspects of researching methods, content and goals. Proper researching model and analysis method should be selected so as to bring the advantages of the ancient acupuncture literatures, case records and clinical experiences of famous physicians into full play. Only in this way can the domestic needle acupointomics studies achieve a breakthrough.
Acupuncture Points
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Acupuncture Therapy
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instrumentation
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methods
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Animals
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Biomedical Research
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Humans
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Needles
6.Astragaloside IV regulates STAT1/IκB/NF-κB signaling pathway to inhibit activation of BV-2 cells.
Yi-xin HE ; Hai-lian SHI ; Hong-shuai LIU ; Hui WU ; Bei-bei ZHANG ; Xiao-jun WU ; Zheng-tao WANG
China Journal of Chinese Materia Medica 2015;40(1):124-128
OBJECTIVEThe study was aimed to investigate the inhibitory effect and mechanism of astragaloside IV (ASI) on the activation of microglial cells.
METHODAfter pre-incubated with ASI for 2 h, microglial cells BV-2 were stimulated with interferon-γ (IFN-γ) for 1. 5 h and 24 h, respectively. Secretion of nitric oxide (NO) in the medium was measured by Griess method. Production of tumor necrosis factor alpha (TNF-α) was detected by ELISA approach. Cellular gene expressions of CD11b, TNF-α, interleukin 1β (IL-1β) and induced nitric oxide synthase (iNOS) were examined by quantitative-PCR analysis. Total and phosphorylation of STAT1, IκB and NF-κB was analyzed by Western blot method.
RESULTASI could significantly inhibit the increased secretion of TNF-α and NO from BV-2 cells upon IFN-γ stimulation (P < 0.001). Further study showed that ASI significantly down-regulated gene expression of IL-1β and TNF-α (P < 0.01, P < 0.05) and exhibited a trend to reduce that of iNOS. IFN-γ and ASI have no obvious effect on gene expression of CD11b. Moreover, ASI inhibited the phosphorylation of STAT1, IκB and NF-κB elicited by IFN-γ stimulation.
CONCLUSIONASI could restrain microglial activation through interfering STAT1/IκB/NF-κB signaling pathway, reducing gene expres- sion of IL-1β and TNF-α, and thus inhibiting the production of proinflammatory mediators such as NO and TNF-α.
Animals ; Astragalus Plant ; chemistry ; Drugs, Chinese Herbal ; pharmacology ; I-kappa B Proteins ; genetics ; metabolism ; Interferon-gamma ; genetics ; metabolism ; Mice ; NF-kappa B ; genetics ; metabolism ; Nitric Oxide ; metabolism ; Nitric Oxide Synthase Type II ; genetics ; metabolism ; STAT1 Transcription Factor ; genetics ; metabolism ; Saponins ; pharmacology ; Signal Transduction ; drug effects ; Triterpenes ; pharmacology
7.In vitro study of safety and co-efficiency of the transbronchial coagulation techniques
Chong BAI ; Yu-Chao DONG ; Xiao-Lian SONG ; Yi HUANG ; Hui SHI ; Zhen-Li HU ; Qiang LI
Chinese Medical Journal 2013;(1):124-128
Background The usual transbronchial coagulation techniques include microwave,argon plasma coagulation (APC),electrocautery and cryotherapy.However,there are serious clinical problems in the safety of each.By analyzing the experimental data and clinical observations,we observed the variable effects of different coagulation techniques via bronchofibroscopy,to look for an optimal interventional management of luminal bronchus diseases,and evaluate the safety and the equivalent point.Methods Four kinds of coagulation techniques under bronchoscopy were performed on the fresh bronchus of healthy sheep,and the pathologic changes in all groups were observed under the microscope.The different treatment parameters were as follows:microwave 60 W×1 second,3 seconds,5 seconds and 40 W×1 second,3 seconds,5 seconds; APC 40 W×1 second,3 seconds,5 seconds; electrocautery 40 W×1 second,3 seconds,5 seconds;cryotherapy 100 Ω×60 seconds,120 seconds.Results After treatment,ovine bronchial mucosa in all groups showed pathologic changes such as local necrosis and amotio of the mucosa lining epithelium,local submucosa coagulative necrosis or tissue defects,while inflammation in the surrounding tissue was not obvious.Under the same output power and action time,different methods had different outcomes.The damage by APC was the most superficial,microwave was the second,and electrocautery caused the worst damage.The study also found that effects of electrocautery at 40 W×3 seconds,microwave at 40 W×5 seconds or 60 W×3 seconds,APC at 40 W×5 seconds and cryotherapy at 100 Ω×120 seconds were the equivalent point conditions.The appearance included mucosa absence,partial submucosa absence,and collagen fiber coagulation in treatment areas.Conclusions Each coagulation technique has its own characteristic.It is very important to choose the appropriate power and action time of the suitable method according to the therapy requirement.
8.Determination of six constituents in Shiyifang Vinum by HPLC
Xian-Yi SHI ; Zhi-Ping WANG ; Fang LI ; Xue-Mei CAI ; Xiao-Yi CHEN ; Jie-Lian HUANG
Chinese Traditional Patent Medicine 2018;40(5):1088-1093
AIM To establish an HPLC method for the content determination of six constituents in Shiyifang Vinum (Notoginseng Radix et Rhizoma,Dipsaci Radix,Carthami Flos,etc.).METHODS The content determination of notoginsenoside R1,ginsenoside Rg1,ginsenoside Rb1 and asperosaponin Ⅵ was performed on a 30℃ thermostatic Inertsil(R) ODS-3 C18column (4.6 mm ×250 mm,5 μm),with the mobile phase comprising of acetonitrile-0.1% phosphoric acid flowing at 1.0 mL/min in a gradient manner,and the detection wavelength was set at 203 nm.The content determination of brucine and strychnine was conducted on a 30 ℃ thermostatic Geminni(R) C18 110(A) column (4.6 mm × 250 mm,5 μm),with the mobile phase comprising of acetonitrile-mixed solution of 0.01 mol/L sodium heptanesulfonate and 0.02 mol/L potassium dihydrogen phosphate flowing at 1.0 mL/min in an isocratic elution manner,and the detection wavelength was set at 260 nm.RESULTS Six constituents showed good linear relationships within their own ranges (r > 0.999 0),whose average recoveries were 98.52%-99.96% with the RSDs of 2.0%-2.3%.CONCLUSION This simple,accurate and reproducible method can be used for the quality control of Shiyifang Vinum.
9.Imaging analysis in acute upper urinary tract calculous obstruction
Yi-Hai SUN ; Xiao-Ping WAN ; Zhi-Bin LI ; LIAN-Hong ; Kai-Ling LUO ; Xiao-Zhuang SU
Journal of Clinical Urology 2000;15(11):491-492
Purpose:To study the diagnostic value of using ultrasonography(US)、plain film of the abdomen(KUB)、 intravenous urography (IVU) in acute ureteral calculous obstruction. Methods: The routine B-US、diuretic US、 KUB、 IVU were retrospectively analyzed in 352 cases of acute ureteral calculous obstruction.Results: Of all the patients, 83.2 % (293/352) 、 96.6 % (340/352)were diagnosed as hydronephrosis by routine B-US、 routine B-US plus diuretic US, respectively. The hydronephrotic diagnosis of 59 suspected patients were79.7% (47/59)using diuretic US. The ureteral calculous dignosis of US、KUB、US plus KUB were 76. 1 % (268/352 )、81.6(284/348)and 91.8(323/352),respectively. Conclusion:The routine B-US is an effective method todiagnose acute upper urinary tract obstruction,and routine B-US plus diuretic US is more valuable. B-US plusKUB is the first approach to diagnose ureteral calculi.
10.Construction of the nucleic vaccine pVVP3L-18HN and its antitumor effect on human laryngeal carcinoma.
Guo-fang GUAN ; Ning-yi JIN ; Zhi-qiang MI ; Xiao LI ; Hai LIAN ; Chun-shun JIN ; Li-li SUN ; Lian-ji WEN
Chinese Journal of Otorhinolaryngology Head and Neck Surgery 2005;40(8):566-570
OBJECTIVENucleic vaccine of pVVP3IL-18HN expressing apoptin gene, Newcastle disease virus HN gene and IL-18 gene were constructed to observe the combinative antitumor effect of the above three genes.
METHODSEukaryotic expression plasmid pVVP3IL-18HN was constructed by inserting apoptin gene and fragment comprising fused IL-18HN gene and IRES promoter into the downstream of CMV promoter of vector pVAX1. The expression of inserted gene was identified by RT-PCR, indirect immunofluorescence and Western-blot. The recombinant plasmid was introduced into Hep-2 cells by liposome, then suppression rate of Hep-2 of different time and different quantity was calculated according to MTT results.
RESULTThe recombinant plasmid of pVVP3IL-18HN suppressed Hep-2 successfully and its suppression rate was up to 61.9% with 20 microg/ml, incubation of 72 hours.
CONCLUSIONThe nucleic vaccine constructed pVVP3IL-18HN had antitumor effect on Hep-2. It may can be used to the therapy and research of laryngeal carcinoma.
Cancer Vaccines ; biosynthesis ; Gene Expression ; Genetic Vectors ; HN Protein ; genetics ; Hep G2 Cells ; Humans ; Interleukin-18 ; genetics ; Laryngeal Neoplasms ; immunology ; prevention & control ; Newcastle disease virus ; immunology ; Plasmids ; Transfection ; Vaccines, DNA ; biosynthesis