2.Phage display technology and its application in antivirals discovery
Shi-qi XU ; Zi-han HE ; Bing-zhuo TAO ; Xin QIN
Acta Pharmaceutica Sinica 2022;57(7):1937-1945
The COVID-19 outbreak has drawn attention to viral infectious diseases once again, and the development of antiviral drugs for both known and potentially emerging viruses is of great significance. In recent years, peptides and protein drugs are becoming a hot spot in the field of antiviral drug research and development. Phage display technology, as a powerful tool for screening peptides and protein drugs, has been increasingly concerned in the academic and industrial fields. The present review introduced the basic principle of phage display technology, summarized phage display libraries often used in antiviral drug discovery and their applications, discussed the challenges and future direction of antiviral drug research and development based on phage display technology.
3.Pharmacognostical study on four origin plants of folk medicine Sikuaiwa.
Yong LIU ; Qi ZHANG ; Yu-jiao PENG ; Zhi-gui WU ; Gui-bing LIN ; Yan-qin XU ; Yong-ming LUO
China Journal of Chinese Materia Medica 2015;40(21):4177-4181
In order to develop characteristic folk medicine resources in Jiangxi, a pharmacognostical study was systematically performed for four different origin plants of Sikuaiwa, the result of study provides the microscopic features of powder and tissue of the crude drug. The research provided reference for the identification of Sikuaiwa, as well as a theoretical basis for the further development and the formulation of quality standards.
Magnoliopsida
;
anatomy & histology
;
chemistry
;
growth & development
;
Medicine, Traditional
;
Plants, Medicinal
;
anatomy & histology
;
chemistry
;
growth & development
4.Effect of pulchinenoside on FZD8 expression of adjuvant arthritis rats.
Cheng-gui MIAO ; Guo-liang ZHOU ; Mei-song QIN ; Jian-zhong CHEN ; Cheng-feng LI ; Hua-qi HE ; Bing ZHANG
China Journal of Chinese Materia Medica 2015;40(20):4063-4067
To study the effect of pulchinenoside (PULC) on the Frizzled (FZD) expression of adjuvant arthritis ( AA) rats. AA rats were prepared through the toe injection with complete Freund's adjuvant to culture fibroblast-like synoviocytes (FLS). The effect of the oral administration with PULC on the FZD8 expression was detected by the real time qPCR. The effect of FZD8 knockout on the expressions of IL-1, IL-6, IL-8 were detected by MTT and ELISA. The role of miR-375 in the abnomal expression of FZD8 was detected by the real time qPCR. The results showed signfiicant decrease in the FZD8 expression among AA rats, FLS proliferation ater FZD8 knockout and IL-1, IL-6, IL-8 expressions and notable increase in miR-375 expression after the oral administration with PULC. The up-regulated miR-375 expression can inhibit the FZD8 expression. PULC may inhibit the FZD8 expression by up-regulating the miR-375 expression.
Animals
;
Arthritis, Experimental
;
drug therapy
;
genetics
;
metabolism
;
Disease Models, Animal
;
Drugs, Chinese Herbal
;
administration & dosage
;
Humans
;
Male
;
Rats
;
Rats, Sprague-Dawley
;
Receptors, Cell Surface
;
genetics
;
metabolism
;
Saponins
;
administration & dosage
5.Normal sperm morphology and the outcomes of routine in vitro fertilization.
Bing HE ; Jun-ping CHENG ; Qi PAN ; Yan CHI ; Tai-shuai HUANG ; Xian-bao MAO ; Jie QIN ; Wei-hong TAN
National Journal of Andrology 2016;22(1):32-36
OBJECTIVETo explore the application value of morphology assessment of sperm from fresh semen in routine in vitro fertilization (IVF).
METHODSWe analyzed the morphology of the sperm from fresh or optimized semen samples and, based on the sperm morphology of the raw semen, allocated 908 IVF cycles due to the pure tubal factor to different groups: morphologically normal sperm (MNS) ≤ 4%, > 4% - ≤ 15%, and > 15% in Trial 1 and MNS ≤ 1%, > 1% - ≤ 2%, > 2% - ≤ 3%, and > 3%-- ≤ 4% in Trial 2. We compared the rates of fertilization, cleavage, high-quality embryo, -blastocyst formation, and pregnancy among different groups.
RESULTSThe total fertilization rate was significantly lower in the MNS ≤ 4% than in the MNS > 4% - ≤ 15% and >15% groups (74.40% vs 78.61% and 80.03%, P < 0.01). Compared with the MNS ≤ 1%, > 1% - ≤ 2%, and > 2% - ≤ 3% groups, the MNS > 3% - ≤ 4% group showed remarkably increased rates of 2PN normal fertilization (77.23%, 78.97% and 78.99% vs 85.47%, P < 0.01), cleavage (95.71%, 96.01% and 97.27% vs 98.73%, P < 0.05), and blastocyst formation (53.85%, 49.01% and 49.55% vs 63.41%, P < 0.01). No statistically significant differences were observed in the rates of clinical pregnancy, implantation, early abortion, live birth, or malformation at birth among different groups (P > 0.05).
CONCLUSIONMNS ≤ 4% affected the total rate of fertilization while MNS ≤ 3% reduced the rate of normal fertilization in IVF. However, even MNS ≤ 1% did not result in fertilization disorder or failure. Therefore, teratozoospermia alone was not an indicator of ICSI and sperm mor- phology assessment had no obvious value for predicting the rates of embryo quality, clinical pregnancy, and live birth in IVF.
Female ; Fertilization in Vitro ; Humans ; Male ; Pregnancy ; Pregnancy Outcome ; Spermatozoa ; cytology
6.Mechanism of apoptosis of NB4 cells induced by arsenic trioxide and cyclooxygenase-2 expression.
Da-Bing QIN ; Jie-Ping CHEN ; Sheng-Qi WANG
Journal of Experimental Hematology 2011;19(3):648-651
Objective of this study was to investigate the changes of cyclooxygenase-2 expression and mitochondrial membrane potential in apoptotic NB4 cells induced by arsenic trioxide (As(2)O(3)). The morphological changes in apoptosis process of NB4 cells treated by arsenic trioxide were observed under immunofluorescence microscope and DNA electrophoresis method, and the apoptosis rate of NB4 cells and the variations of mitochondrial membrane potential were detected by flow cytometry. Furthermore, the variations of expression level of cyclooxygenase-2 protein were analyzed by using Western blot method. The results indicated that after NB4 cells were treated with 2 µmol/L As(2)O(3) for 48 hours, some variations of NB4 cells were observed, such as pyknosis, chromatin segmentation, even fragmentation. Meanwhile, the typical DNA Ladder phenomenon was observed. The apoptosis rate of NB4 cells treated with 3 µmol/L As(2)O(3) for 48 hours was 33.34%, Furthermore the apoptosis rate of NB4 cells was enhanced along with the increase of concentration of As(2)O(3). After NB4 cells were treated with 0.5, 1, 2, 4 and 8 µmol/L As(2)O(3) for 48 hours, the mitochondrial membrane potential decreased by 12.8%, 21.6%, 66.9%, 83.7% and 83.8% respectively. The Western blot detection results showed that the expression level of cyclooxygenase-2 protein in NB4 cells was lower than that in control cells and decreased along with the rise of As(2)O(3) concentration, then the negative dose-dependent manner was observed between these 2 groups. It is concluded that As(2)O(3) can effectively induce NB4 cell apoptosis, and the dose-dependent manner existed in certain extent of concentrations. The decrease of mitochondrial membrane potential may be related with NB4 cell apoptosis induced by As(2)O(3). Cyclooxygenase-2 participates in the process of NB4 cell apoptosis induced by As(2)O(3).
Apoptosis
;
drug effects
;
Arsenicals
;
pharmacology
;
Cell Line, Tumor
;
Cyclooxygenase 2
;
metabolism
;
Humans
;
Leukemia, Promyelocytic, Acute
;
metabolism
;
Membrane Potential, Mitochondrial
;
Oxides
;
pharmacology
7.The analysis of drug resistance characteristics in clinical isolated Helicobacter pylori strains from different gastropathy patients and the inhibitory effect of Lactobacillus acidophilus on drug-resistant Helicobacter pylori
Qin-tu-na-la SI ; Yan LI ; Shang-wei JI ; Yong-gui ZHANG ; Wen-sai QI ; Jiang-bing WANG
Chinese Journal of Digestion 2011;31(7):465-469
Objective To analyze the drug resistant characteristics of 84 clinical isolated Helicobacter pylori (Hp) strains, and to observe the inhibitory effects of anti-Hp Lactobacillus acidophilus (La)4 and La6 on different antibiotic-resistant Hp strains. Methods Hp strains were isolated and cultured from gastric mucosa of 84 different gastropathy patients (20 patients with chronic gastritis, 24 with gastric ulcer, 19 with duodenal ulcer and 16 with gastric cancer). The minimum inhibitory concentration (MIC) of metronidazole, clarithromycin and amoxicillin were tested by E-test in order to determine the resistance of these three antibiotics in clinical isolated Hp strains. With standard La as control, the supernatant of anti-Hp La4 and La6 was added into Hp strains culture wells. Hp strains were cultured in solid media for 72 hours, and then inhibition ring were recorded. Anti-Hp Lactobacillus acidophilus liquid was also added to culture medium of different Hp strains, which were in liquid culture, culture medium were taken at different time points (4,8,12,24,48 hrs) to calculate bacteria colony number and test urease activity. Results In 84 clinical isolated Hp strains, the resistant rates of metronidazole, clarithromycin and amoxicillin resistance rates were 67.9%, 17.9% and 1.2% respectively. Of those 11 strains were mixed drug resistance, which included 10 strains of metronidazole and clarithromycin mixed drug resistance, and one of metronidazole and amoxicillin mixed drug resistance. In solid culture conditions, supernatant of anti-Hp Lactobacillus acidophilus La4 and La6 had obvious inhibitory effect on antibiotic-resistant and non-resistant Hp strains. In liquid culture conditions, anti-Hp Lactobacillu acidophilus La4 and La6 bacterium liquid could inhibit the proliferation of antibiotic-resistant and non-resistant Hp strains, the antagonistic role was significantly stronger than the standard Lactobacillus acidophilus strains (P<0.05). The urease activity of antibiotic-resistant Hp strains was inhibited since mixed cultured with anti-Hp Lactobacillu acidophilus La4 and La6 for 4 hours, the urease activity gradually decreased as culture time extended, and the inhibitory role was significantly stronger than the standard Lactobacillus acidophilus strains (P<0.05). Conclusions In 84 Hp strains, most were metronidazole resistant strains, followed by clarithromycin resistant strains, metronidazole and clarithromycin mixed resistance strains. In vitro, anti-Hp Lactobacillu acidophilus La4 and La6 had obvious inhibitory effects on antibiotic-resistant and non-resistant Hp strains.
8.Chemical constituents of Jasminum giraldii and their antioxidant activity.
Xiu-Peng ZHANG ; Hui QIN ; Fang YANG ; Jiang CHAI ; Xin WANG ; Xiao-Mei SONG ; Qi-Bing MEI ; Feng FENG ; Zheng-Gang YUE
China Journal of Chinese Materia Medica 2014;39(11):2029-2033
Ten compounds were isolated from the barks of Jasminum giraldii by means of various of chromatographic techniques such as silica gel, Sephadex LH-20 and Rp-HPLC. Their structures were identified by spectroscopic data analysis as (+)-medioresinol (1), (+) -syringaresinol (2), syringaresinol-4'-O-beta-D-glucopyranoside (3), oleanic acid (4), 3-methoxy-4-hydroxy-trans-cinnamaldehyde (5), trans-sinapaldehyde (6), syringaldehyde (7), 1-(4-methoxy -phenyl) -ethanol (8), trans-cinnamic acid (9), and 4-(1-methoxyethyl) -phenol (10). Among them, compounds 1-3, 5-8 and 10 were isolated from the J. genus for the first time and compounds 4 and 9 were obtained from J. giraldii for the first time. In the DPPH free radical scavenging assay, compound 1 exhibited significant activity (IC50 55.1 micromol x L(-1)), compared with vitamin C(IC50 59.9 micromol x L(-1)); and compound 2 showed moderate activity (IC50 79.0 micromol x L(-1)), compared with 2, 6-di-tert-butyl4-methylphenol (IC50 236 micromol x L(-1)).
Antioxidants
;
chemistry
;
isolation & purification
;
Drugs, Chinese Herbal
;
chemistry
;
isolation & purification
;
Jasminum
;
chemistry
;
Magnetic Resonance Spectroscopy
;
Molecular Structure
;
Spectrometry, Mass, Electrospray Ionization
9.Sodium tanshinone IIA sulfonate prevents postoperative peritoneal adhesions in rats by enhancing the activity of the peritoneal fibrinolytic system.
Si LIN ; Fei QIN ; Lu-Yao SONG ; Chu-Qi HOU ; Lian-Bing HOU
Journal of Southern Medical University 2016;36(2):260-264
OBJECTIVETo evaluate the effect of sodium tanshinone IIA sulfonate (STS) in preventing postoperative peritoneal adhesions in rats and explore the mechanisms.
METHODSSixty SD rats were randomized into 4 equal groups, including a blank control group, adhesion model group, and high-, moderate-, and low-dose STS-treated groups, and were subjected to injuries of the parietal peritoneum and cecum to induce peritoneal adhesions, followed by intraperitoneal administration of saline and STS at the doses of 20, 10, and 5 mg/kg for 7 consecutive days, respectively. Another 15 untreated rats served as the blank control group. The adhesion scores in each group were recorded after the treatments; the activity of tissue-type plasminogen activator (tPA) in peritoneal lavage fluid was measured, tPA/PAI-1 protein ratio in the peritoneal tissue was determined by ELISA, and the expressions of TGF-β1 and collagen I were detected by immunohistochemistry. The anastomotic healing model was used to assess the impact of STS on wound healing.
RESULTSIntraperitoneal administration of STS effectively prevented peritoneal adhesion without affecting anastomotic healing in the rats. Compared with the adhesion model group, the STS-treated groups showed increased peritoneal lavage fluid tPA activity and tPA/PAI-1 ratio in the ischemic tissues with lowered TGF-β1 and collagen I expressions in the ischemic tissues.
CONCLUSIONSIntraperitoneal administration of STS can prevent peritoneal adhesion and enhance local fibrinolysis in rats, and these effects may be mediated by TGF-β signaling pathway.
Animals ; Cecum ; injuries ; pathology ; Collagen Type I ; metabolism ; Fibrinolysis ; Injections, Intraperitoneal ; Peritoneum ; injuries ; pathology ; Phenanthrenes ; pharmacology ; Plasminogen Activator Inhibitor 1 ; metabolism ; Postoperative Complications ; prevention & control ; Rats ; Rats, Sprague-Dawley ; Tissue Adhesions ; prevention & control ; Tissue Plasminogen Activator ; metabolism ; Transforming Growth Factor beta1 ; metabolism ; Wound Healing
10.Expression of connective tissue growth factor in cardiomyocyte of young rats with heart failure and benazepril intervention.
Qin ZHANG ; Qi-jian YI ; Yong-ru QIAN ; Rong LI ; Bing DENG ; Qiao WANG
Chinese Journal of Pediatrics 2006;44(10):733-737
OBJECTIVESVentricular remodeling is an important pathologic progress in almost all end stage heart failure (HF), and it is characterized by ventricular thickening and cardiac fibrosis with poor prognosis. The connective tissue growth factor (CTGF), a new growth factor with multi-function, has an important role in fibrosis of tissue and organs. It has been demonstrated that angiotensin-converting enzyme inhibitor (ACEI) can prevent the development of cardiomyocyte from remodeling and improve cardiac function. Researchers try to test the hypothesis that cardiac function improvement attributable to ACEI is associated with inhibiting expression of CTGF in patients with HF. The aim of this study was to observe changes in CTGF expression in cardiomyocyte of young rats with HF and effect of benazepril on CTGF.
METHODSThe animal model of HF was established by constriction of abdominal aorta. Five weeks old rats were randomly divided into 3 groups after 6 weeks of operation: (1) HF group without treatment (n = 15); (2) HF group where rats were treated with benazepril (n = 15); (3) sham-operated group (n = 15) where rats were administered benazepril through direct gastric gavage. After 4 weeks of treatment, the high frequency ultrasound was performed. The expression of CTGF was detected by immunohistochemistry and semi-quantative reverse transcription-polymerase chain reaction.
RESULTSCompared with the sham-operated group, left ventricular diastolic dimension (LVEDD), left ventricular systolic dimension (LVESD), interventricular septal thickness at end-diastole (IVSTd), interventricular septal thickness at end-systole (IVSTs), left ventricular posterior wall thickness at end-diastole (LVPWTd), left ventricular posterior wall thickness at end-systole (LVPWTs), left ventricular relative weight (LVRW), and right ventricular relative weight (RVRW) were all increased (P < 0.01), but ejection fraction (EF) and fractional shortening (FS) were decreased (P < 0.01). CTGF positive cells and expression of CTGF mRNA (0.609 +/- 0.065 vs 0.117 +/- 0.011, P < 0.01) were increased in HF group without treatment. LVESD, IVSTd, IVSTs, LVPWTd, LVPWTs, LVRW and RVRW were all decreased (P < 0.01), but FS and EF were increased (P < 0.01) in cases of HF treated with benazepril when compared with HF group without treatment. LVESD, IVSTd, IVSTs, LVPWTd, LVPWTs, LVRW and RVRW were higher (P < 0.01), EF and FS were lower (P < 0.01), CTGF positive cells and expression of CTGF mRNA were higher (P < 0.01) in HF group treated with benazepril than those of sham-operated group.
CONCLUSIONThe expression of CTGF was increased in the cardiomyocyte of young rats with HF and benazepril could prevent left ventricular from remodeling partly and improve cardiac function by inhibiting the expression of CTGF in cardiomyocyte in cases of HF.
Angiotensin-Converting Enzyme Inhibitors ; pharmacology ; Animals ; Benzazepines ; pharmacology ; Connective Tissue Growth Factor ; metabolism ; Disease Models, Animal ; Heart Failure ; diagnostic imaging ; drug therapy ; metabolism ; physiopathology ; Immunohistochemistry ; Male ; Myocytes, Cardiac ; drug effects ; metabolism ; RNA, Messenger ; Rats ; Rats, Wistar ; Reverse Transcriptase Polymerase Chain Reaction ; Ultrasonography ; Ventricular Dysfunction, Left ; diagnostic imaging ; drug therapy ; physiopathology ; Ventricular Remodeling ; drug effects