1.Effective Forms, Additive Effect, and Toxicities Scattering Effect of Pharmacodynamic Substances of TCMs Some Reflections Evoked by the Study on the Metabolic Disposition of Traditional Chinese Medicines (TCM)
Feng XU ; Donghui YANG ; Mingying SHANG ; Xuan WANG ; Shaoqing CAI
World Science and Technology-Modernization of Traditional Chinese Medicine 2014;(4):688-703
The blood concentrations of the pharmacodynamic substances of traditional Chinese medicines (TCMs) are usually very low. How can they exert pharmacological actions, in which forms (original form, metabolite or the both) do they exert the actions. To answer these questions, we proposed a new concept ofEffective Formsof pharmacodynamic substances of TCMs and a hypothesis of additive effect of multiple constituents of TCMs. The hypothesis includes that the aggregate or summation of Effective Forms of pharmacodynamic substances of TCMs is the core material base of the effi-cacy of TCMs, and the additive effect of the blood concentrations of different Effective Forms is one part of the action mechanism. The additive effect of the different Effective Forms of a TCMs means an additive effect of numerous con-stituents or/and metabolites on a same target, and therefore the efficacy brought by the addition of the concentrations of all these compounds, which different from the synergy effect of multi-constituents on multi-targets. Studies on the disposition of TCMs showed that a constituent can be biotransformed to many metabolites (up to more than 50 metabolites);different constituents can produce the same metabolites;many metabolites (up to 10 compounds for each metabolite) are isomers or homologues; some constituents can be converted to each other in vivo; and some metabolites are bioactive. These com-pounds having the similar structure are likely to have the same pharmacological effects on the same target, which could provide experimental evidences for the concept ofEffective Formsand the hypothesis ofAdditive Effect. We suggest that the Effective Forms and Additive Effects of the pharmacodynamic substances of TCMs should be extensively investi-gated in the future, and the results of such researches will help us further understand the pharmacodynamic substances and action mechanism of TCMs, and give a new explanation 'Toxicities Scattering Effect' for 'Why the toxicities of TCMs are low', and propose a new strategy for quality control of TCMs.
2.Research progress in the competing endogenous RNA in gastric cancer pathogenesis
Wenwen LIU ; Feng WANG ; Yan ZHANG ; Shaoqing JU
Chinese Journal of Laboratory Medicine 2017;40(8):637-640
Recent studies demonstrate that the long non-coding RNAs (lncRNAs), pseudogenes, circular RNAs (circRNAs) and so on can be used as competitive endogenous RNAs (ceRNAs), binding to microRNAs (miRNAs), to regulate the expression level of their targets.This novel interplay optimizes traditional liner miRNA→RNA pattern and has become a research hotspot in the scientific community.Dysregulation of ceRNA interplay will influence the body′s normal life activities, leading to the occurrence of diseases, and even tumor formation.This article briefly introduces the key components of ceRNA crosstalk and its research progress in gastric cancer pathogenesis, so as to provide a new thought for cancer research, clinical diagnosis and therapeutics.
3.A comparative study of two commonly used preoperative imaging-aided design methods for superficial circumflex iliac artery perfo-rator flap
Zhuowei TIAN ; Huihong ZHOU ; Shaoqing FENG ; Jian SUN ; Yue HE
Chinese Journal of Clinical Oncology 2015;42(16):807-812
Objective:To evaluate the accuracy of the application of color Doppler sonography (CDS) and computer tomography angiography (CTA) in preoperative perforator identification and flap design and provide theoretical support for the restoration of oral maxillofacial defect with free superficial circumflex iliac artery perforator flap (SCIAPF). Methods: (1) Preoperative CDS and CTA techniques were performed to map the SCIA perforators of 29 adult patients diagnosed with malignant tumor in the oral maxillofacial head and neck regions. These patients were scheduled for concurrent reconstruction surgery. (2) A diagnostic test was designed to com-pare the CDS and CTA techniques. Results:(1) A total of 18 patients underwent flap preparation. SCIA was not found in one of the pa-tients during surgery, but was observed intra-operatively in the other 17 patients. The average SCIA diameter was 0.69 ± 0.20 mm. (2) The diagnostic test showed a CDS sensitivity of 75.0%, a CDS specificity of 82.4%, and an area under the ROC curve of 0.79. The CTA sensitivity was 75.0%, the specificity was 94.2%, and the area under the ROC curve was 0.85. The diameters measured by CDS and CTA were compared with the diameter measured intra-operatively. Significant differences were observed among the three diame-ters (P<0.05). The average diameter measured by CDS was 0.84 ± 0.14 mm. The average diameter measured by CTA was 1.01 ± 0.19 mm. Conclusion:CDS and CTA are relatively reliable technologies for preoperative detection of perforator vessel. The use of CDS and CTA technology mapping for SCIAPF can provide accurate information about the perforator, including the position of the perforator and the relationship between the peripheral tissues and the caliber of the vessel.
4.Research progress on long non-coding RNA in gastric cancer
Xi LUO ; Feng WANG ; Xianjuan SHEN ; Shaoqing JU
Chinese Journal of Laboratory Medicine 2016;39(8):578-580
Long non-coding RNAs are a novel class of non-protein coding RNA molecules with more than 200 nucleotides in length.Recently, mounting evidence has been demonstrated that lncRNAs play crucial roles in epigenetic modification and gene expression regulation. This review aims to summarize current knowledge of lncRNAs in the carcinogenesis, clinical diagnosis, drug resistance and prognosis prediction of gastric cancer.
5.Effects of siRNA targeting APRIL gene on cell growth and migration of a mouse colorectal cancer cell line
Weifeng DING ; Yonghong QIAO ; Feng WANG ; Jingchun WANG ; Guihua WANG ; Shaoqing JU ; Yueguo WANG ; Huimin WANG
Chinese Journal of Microbiology and Immunology 2011;31(2):103-107
Objective To construct and screen siRNA targeting a proliferation-inducing ligand (APRIL) gene in a mouse colorectal cancer celline, CT-26. To investigate the effects to the cell growth and migrant capacity of CT-26 after knockdown APRIL gene, lay the foundation for molecular targeted therapy to colorectal cancer. Methods Four pairs of APRIL siRNA were designed and chemically synthesized. And disorder sequences were synthesized as a negative control. These sequences were transfected with LipofectAMINE 2000 into CT-26 cells, which high-expressed APRIL gene. The transfection efficency rate of 6-FAM labelled control siRNA was detected by fluorescence microscope. The inhibition effectiveness of APRIL mRNA and protein was analyzed by FQ-RT-PCR and Western blot, respectively. Cell proliferation activity was analyzed by cell counting kit-8, cell migration capacity was detected by the repair of cell damage, and MMP-2 together with TIMP-1, two important regulatory genes in cell metastasis, were measured by RT-PCR.Results The different kinds of APRIL siRNA effectively suppressed the level of APRIL mRNA and the protein expression in CT-26 (P < 0.05 ). Cell proliferation and metastasis ability were repressed after APRIL siRNA transfection( P < 0.05 ), compared with random siRNA control and nontransfected control. The mRNA levels of MMP-2 and TIMP-1 genes wre significantly altered among APRIL siRNA groups and two control groups ( P < 0.05). Conclusion We have constructed and screened a kind of siRNA (APsi737) targeting APRIL gene in a mouse colorectal cancer cell line, CT-26. APRIL siRNA can effectively inhibit the cell growth and migration capacity, maybe be regulated by MMP-2 and TIMP-1.
6.Contents Determination of Nine Components in Guizhi Decoction and Comparison of Different Decoction Methods
Pengfei YUAN ; Huan LIU ; Mingying SHANG ; Feng XU ; Guangxue LIU ; Shaoqing CAI ; Lanfang LI ; Tingliang JIANG
China Pharmacy 2016;(6):801-804,805
OBJECTIVE:To establish a method for the contents determination of 9 components in Guizhi decoction,and com-pare the effects of traditional decoction method and the extracting machine decoction method on these contents in Guizhi decoction. METHODS:HPLC was performed on the column of Agilent Zorbax SB-C18 with mobile phaseof acetonitrile- 0.1% phosphoric ac-id(gradient elution)at a flow rate of 1.0 ml/min,the detection wavelength was 230 nm,254 nm and 280 nm,the column tempera-ture was 25℃,and the injection volume was 10μl. RESULTS:The linear range was 0.410 2-210.0μg/ml for gallic acid(r=0.999 9), 0.994 0-254.5μg/ml for albiflorin(r=0.999 9),1.636 0-1 675.0μg/ml for paeoniflorin(r=0.999 9),0.988 3-506.0μg/ml for liquiri-tin(r=0.999 6),0.987 3-31.59 μg/ml for coumarin(r=0.999 5),0.486 8-124.6 μg/ml for cinnamic acid(r=0.999 5),2.458 0-314.6μg/ml for cinnamaldehyde(r=0.999 5),0.034 3-1.096 μg/ml for 2-methoxy cinnamaldehyde(r=0.999 8),and 1.711 0-219.0 μg/ml for glycyrrdhizic acid (r=0.999 7);RSDs of precision,stability and reproducibility tests were lower than 5%,recoveries were 93.56%-103.19%(RSD=4.00%,n=9)、101.51%-107.32%(RSD=2.21%,n=9)、95.08%-103.76%(RSD=2.87%,n=9)、100.82%-105.73%(RSD=1.85%,n=9)、85.08%-89.12%(RSD=1.40%,n=9)、92.31%-99.12%(RSD=2.71%,n=9)、99.17%-102.32%(RSD=1.24%,n=9)、100.15%-103.98%(RSD=1.18%,n=9)、99.93%-102.61%(RSD=1.03%,n=9). The content of total effective components from the extracting machine decoction method was 4 565μg/g,that from the traditional decoc-tion method was 2 742 μg/g.CONCLUSIONS:The method is simple,stable and reproducible,and can be used for the simultaneous determination of 9 componentsin Guizhi decoction. The contents of gallic acid,albiflorin and 2-methoxy cinnamaldehyde are first re-ported. The total effective components from the extracting machine decoction method are higher than that from the traditional decoc-tion method.
7.Simultaneous Determination of Inulicin and Deacetylinulicin in Inulae Flos by HPLC
Liman MA ; Zhen LIU ; Mingying SHANG ; Guangxue LIU ; Feng XU ; Shaoqing CAI
China Pharmacy 2016;27(3):369-371
OBJECTIVE:To establish a method of simultaneous determination of inulicin and deacetylinulicin in Inulae Flos. METHODS:HPLC was performed on the column of Zorbax SB-C18 with mobile phase of acetonitrile-water(gradient elution)at a flow rate of 1.0 ml/min,the column temperature was 25 ℃,the detection wavelength was 210 nm,and the injection volume was 10 μl. RESULTS:The linear range was 0.000 2-0.005 μg/ml(r=0.999 8)for inulicin and 0.000 1-0.001 7 μg/ml(r=0.999 4)for deacetylinulicin;RSDs of precision,stability and reproducibility tests were lower than 2.0%;recoveries were 99.63%-103.56%(RSD=1.26%,n=9)and 95.98%-101.21%(RSD=1.84%,n=9),respectively. CONCLUSIONS:The method is simple,accurate and reliable,and can be used for the quality evaluation of Inulae Flos.
8.Biocmpatibility research of a hemostatic agent-ZSM-5 zeolite
Shaoqing FENG ; Shaozong CHEN ; Zhenqiang SITU ; Xueyong LI ; Yuejun LI ; Wangzhou LI
Chinese Medical Equipment Journal 1989;0(01):-
Objective To evaluate the biocompatibility of ZSM-5 zeolite and provide an experimental basis for developing the first-aid hemostatic agent.Methods According to Chinese evaluation standards on medical devices and biological tests,the cytotoxicity in vitro,hemolysis test,acute toxicity of system,pyrogen test,intracutaneous stimulation,sensitization and micronucleus test were studied in ZSM-5 zeolite.In order to find out the side-effect of the zeolite granules' remains left in the wounds to body,muscle implantation test was studied.Results There were no obvious cytotoxity,hemolysis reaction.Acute tocicity,pyrogen reaction,intraeutaneous stimulation,sensitization and potential mutagenesis in themicronucleus test were observed.Their results were a11 consistent with the Chinese biological evaluation of medical devices.Obvious inflammatory reaction was observed when ZSM-5 zeolite was implanted in muscle for 12 weeks.Conclusion The ZSM-5 zeo1ite has reliable biocompatibility.But zeolite can cause inflammatory reaction when it is remained in the wound surface for long term.
9.Identification and Analysis of Harpagide Metabolites in Rats in vivo
Zhen LIU ; Feng XU ; Jingzhe WANG ; Guangxue LIU ; Mingying SHANG ; Shaoqing CAI
China Pharmacy 2017;28(10):1310-1315
OBJECTIVE:To study the metabolites,distribution,metabolic type and the possible activity of harpagide which is the active component from Scrophularia ningpoensis in rats in vivo. METHODS:4 SD rats were divided into blank group (ul-tra-pure water) and administration group (harpagide reference solution),2 in each group,ig,160 mg/kg,twice a day,for 3 d. Urine and feces were collected every 12 h before administration and the first administration;sample blood 8 mL was taken after 0.5,1 h of last administration;heart,liver,spleen,lung,kidney,stomach and small intestine were taken. The blood,urine,fe-ces and other tissue solutions were prepared,HPLC-MS was conducted to detect and identify the harpagide metabolites in rats in vi-vo and presume metabolic pathways,and PharmMapper software was used to predict metabolites activity. RESULTS:12 harpagide metabolites were identified in rats in vivo,the form of prototypes and metabolites were distributed in heart,liver,spleen,lung, kidney,stomach and small intestine. The metabolic type mainly included hydrolysis,dehydration,reduction,methylation,sul-fation,glucuronic acid binding,grade A coumaric acid binding,etc. The 12 compounds may have activities in the treatment of epi-lepsy,amyotrophic lateral sclerosis,diabetes,stroke,etc. CONCLUSIONS:Harpagide may be effective in the form of prototypes and metabolites. The study has provided basis for attributing the origins of metabolite,studying the effective form of S. ningpoensis clarifying its pharmacological mechanism and processing mechanism.
10.Monitoring the post-operative lymphedema in prefabricated flap after resurfacing for facial scar
Ke LI ; Shaoqing FENG ; Hua LI ; Peiru MIN ; Wenjing XI ; Ningfei LIU ; Yixin ZHANG
Chinese Journal of Microsurgery 2015;38(5):451-455
Objective Currently, the prefabricated flap is used for reconstructing the post-burn scar in head and face.The aim is to analyze the nature of the post-op edema in the prefabricated flaps, to determine whether it is lymphedema, and to study the prognosis of the edema.Methods From January, 2011 to March, 2015, 18 cases of post-operation edema in superficial temporal fascia prefabricated flaps were studied and each case was followed for 5 months.We used ultrasound and indocyanine green (ICG) fluorescent imaging to study the nature of the edema.Apart from that, we monitored the recovery process of the post-operation edema by a) measuring the horizontal diameter of the flap by a tape, b) measuring the thickness of the flap by the ultrasound, c) monitoring the condition of edema by ICG and d) monitoring the reconstruction and recanalization of the lymphatic system by ICG.Results Pitting edema always occurred in the prefabricated flap from the first day after operation.These patients were diagnosed as mild lymphedema (7 cases), moderate lymphedema (10 cases), and severe lymphedema (1cases) by ultrasound and ICG florescent imaging.The degree of flap lymphedema improved gradually and it improved significantly from 3 days to 6 days post-op eration.The condition of flap lymphedema became stable from the 12 days post-operation.The fluorescence image of ICG showed that the stage of flap lymphedema improved from 3 weeks post-operation and the transportation capability of lymphatic vessels increased most from the 3 days to 6 days post-op eration.We also found lymphatic vessels reconnected from the 6 days post-operation and lymphatic system reconstructed following the direction to lymph nodes.We could discover the collecting lymphatic vessels from 2 months post-operation and the lymphatic system in prefabricated flap matured from 5 months post-operation.Conclusion The post-operation edema in the prefabricated flaps is lymphedema, the incidence rate of which is high.The lymphatic drainage system recovers in 6 days after the operation.It is reconstructed along the lymph nodes.The edema disappears in 2-3 weeks post-operation, the reconstructed the lymph system matures in 5 months.