2.Research progress on local anesthetic drug delivery systems based on covalent modification strategies
Jia-xing YAO ; Zi-fu LIU ; Yue-qin ZHENG
Acta Pharmaceutica Sinica 2024;59(12):3215-3221
This review introduced the research progress of covalent modification strategies in local anesthetic drug delivery systems. As a commonly used and multimodal analgesic drug, local anesthetics have limited duration of action and potential toxicity in clinical application. In order to prolong the analgesic effect and reduce systemic toxicity, researchers are committed to the development of sustained-release local anesthetics with long-lasting dose-controlled-release functions. When it comes to the delivery of local anesthetics, the covalent modification strategy is a key approach. By covalently binding drugs to large molecule carriers, covalent modification strategies can improve drug stability, targeting and delivery efficiency. Macromolecular prodrugs can modulate the kinetic process of the drug, so that the drug is released in the form of the active ingredient and achieve better therapeutic effects. In recent years, stimulus-responsive macromolecular prodrugs have become a research hotpot for local anesthetic drug delivery systems, and the stimulus-responsive performance of macromolecular prodrugs can rapidly release drugs under internal and external stimulus conditions, and maintain low toxicity and high efficiency in blood circulation and normal tissues. These emerging research directions provide important guidance for prolonging the analgesic effect of local anesthetics and reducing systemic toxicity, and provide new idea for the development of more effective drug delivery systems in the future.
3.Assessment of overall function after percutaneous coronary intervention by cardiopulmonary exercise testing in patients with stable coronary heart disease.
Hong-chao ZHENG ; Yue-you DING ; Xing-guo SUN ; Jian YANG ; Qing LI ; Fang LIU
Chinese Journal of Applied Physiology 2015;31(4):378-382
UNLABELLEDObjective: In order to assess the integrative cardiopulmonary function after percutaneous coronary intervention (PCI) in patients with stable coronary artery disease (CAD), we used symptom limited maximum cardiopulmonary exercise testing (CPET).
METHODSAll 59 patients diagnosed stable CAD by coronary angiography and echocardiography from August to December of 2014 in our hospital, were divided two groups. PCI group, 31 patients received PCI and drugs. Control group, 28 patients received drugs therapy only. All patients performed CPET before and after the treatment.
RESULTSAll patients safely completed CPET without any complications. The control group, all functional parameters were unchanged (P > 0.05). PCI group, the anaerobic threshold, peak oxygen uptake and peak oxygen pulse increased significantly (P < 0.05) from baseline,but not for others (P > 0.05). For individual analysis, PCI group had higher rates of increase (≥ 10% of baseline) in both peak oxygen uptake and peak oxygen pulse than those of control group (P < 0.05).
CONCLUSIONCPET is an objective, quantitative, safe and effective method to evaluate the clinical therapeutic efficiency. PCI can improve the integrative cardiopulmonary function in CAD patients.
Anaerobic Threshold ; Coronary Angiography ; Coronary Artery Disease ; surgery ; Exercise Test ; Heart Rate ; Humans ; Oxygen ; Oxygen Consumption ; Percutaneous Coronary Intervention
4.Influence of Asphyxia on Nitric Oxide and Nitric Oxide Synthase Levels in Renal of Neonatal Rats
juan, YU ; zheng-yue, CHEN ; ling, YANG ; lu-wei, XING ; hong-chang, GUO ; jing-bin, CUI
Journal of Applied Clinical Pediatrics 1994;0(04):-
Objective To study the effects of nitric oxide synthase(NOS) and nitric oxide(NO) in post-asphyxial renal injury in neonatal rats.Methods Forty-eight Wistar neonatal rats were randomly divided into 4 groups:controls,2 h,24 h and 48 h post-asphyxia groups (12 in each group).The rats were decapitated in different times(2 h,24 h and 48 h) after asphyxia for 30 minutes.The renals were dissected to determined the concentrations of NO and NOS.And the scores of renal tubules were measured under light microscope.Results Compared with control group,the levels of NO and NOS significantly increased at 2 h and 24 h after asphyxia.The scores of renal tubules were significant difference at 24 h and 48 h after asphyxia compared to controls.Conclusion These findings suggest NOS and NO may play an important role in the development of post-asphyxia renal injury.
5.Hepatoprotective Effects of Silybin-Phosphatidylcholine Complex in Septic Rats
xing-xia, LIU ; pei-yong, QIU ; jian-zhi, GAO ; zheng-yue, CHEN
Journal of Applied Clinical Pediatrics 2004;0(09):-
Objective To investigate the hepatoprotective effect of silybin-phosphatidylcholine complex(SPC) in sepsis rats.Me-(thods) Fifty Wistar immature rats were randomly divided into 3 groups:normal control(10 cases),septic group(30 cases) and interfe-(rence) group(10 cases).In septic group and interference group,rats were treated by cecal ligation and puncture(CLP).Meanwhile,the interference group was given SPC before 2 hours of CLP and after 2 hours of CLP.Blood of rats was taken from all groups to determine the levels of serum tumor necrosis factor-?(TNF-?),interleukin-1(IL-1),alanine aminotransferase(ALT) and aspartate aminotransferase(AST) at varying intervals.Results The levels of serum TNF-?,IL-1,ALT and AST after CLP were significantly elevated in septic group compared with the normal control group(P
6.Arthroscopic treatment of symptomatic anterior cruciate ligament cysts of the knee.
Hua-chen YU ; Hong WEN ; Yu ZHANG ; Yue-zheng HU ; Xiao-yun PAN ; Cheng-wang CHEW ; En-xing XUE
China Journal of Orthopaedics and Traumatology 2014;27(8):638-641
OBJECTIVETo explore the clinical symptom and effect of arthroscopic treatment of symptomatic anterior cruciate ligament (ACL) cysts of the knee.
METHODSClinical data from 12 symptomatic ACL cysts patients from January 2005 to December 2010 were retrospectively analyzed,including 8 males and 4 females,with an average age of (33.7±9.5) years old (ranged, 19 to 53 years old). The locations were the left knee in 5 cases and the right knee in 7 cases. The disease duration ranged from 3 to 48 months,with a mean of (15.8±13.2) months. All cysts were arthroscopically resected. Range of motion was measured preoperatively and postoperatively, and Lysholm scoring system was used to evaluate the knee function.
RESULTSAll the incisions healed by first intention, and no complications occurred. Twelve patients were followed up for an average of (32.3±6.6) months(ranged, 24 to 48 months). The symptoms of arthralgia,swelling and interlocking of the affected knees disappeared. There was no recurrence during the follow-up. There were significant differences in the range of motion and Lysholm score between pre-operation and post-operation.
CONCLUSIONArthroscopic surgery, showing its advantages of minimal invasion and rapid recovery,is an effective measure in the treatment of ACL cysts.
Adult ; Anterior Cruciate Ligament ; physiopathology ; surgery ; Arthroscopy ; methods ; Cysts ; physiopathology ; surgery ; Female ; Humans ; Magnetic Resonance Imaging ; Male ; Middle Aged ; Range of Motion, Articular
7.β-elemene combined with pemetrexed inhibits the proliferation and increases the apoptosis of HeLa cells
Yang BAI ; Lu LI ; Litian MA ; Yi ZHANG ; Liting MAO ; Rui MA ; Qinyou REN ; Yue HU ; Jinsong XING ; Jin ZHENG
Journal of Medical Postgraduates 2015;(1):7-10
Objective Pemetrexed and β-elemene can inhibit the growth of tumor cells .This study was to investigate the effect of pemetrexed combined with β-elemene on the proliferation and apoptosis of cervical cancer HeLa cells. Methods Cervical cancer HeLa cells were treated with pemetrexed at the concentrations of 38, 76, 152, 228, and 304μg/mL, and at 24 and 48 hours of treatment subjected to MTT for detection of their proliferation .The experiment included four groups , with the cells treated with β-elemene ( 125μg/mL) , pemetrexed ( 76 μg/mL ) , β-elemene ( 125 μg/mL ) +pemetrexed (76μg/mL), and nothing (blank control) for 24 hours, followed by determination of their proliferation and apoptosis by MTT and flow cytometry, respectively. Results Pemetrexed at 38, 76, 152 and 228μg/mL inhibited the proliferation of the HeLa cells in a concentration-dependent manner, with the inhibition rates of (7.24 ±3.78), (7.94 ±4.37), (11.10 ±2.86) and (15.88 ± 3.38)%at 24 hours, and (16.69 ±0.95), (22.54 ±1.53), (24.48 ±0.92) and (25.54 ±3.61)%at 48 hours, both with statis-tically significant differences between any two groups (P<0.05).Significant differences were also found in the proliferation rate of the same concentration of pemetrexed at the two time points (P<0.05).The combination of pemetrexed and β-elemene showed an inhibi-tion rate of (49.95 ±5.76)%at 24 hours, remarkably higher than (24.36 ±5.59)%in theβ-elemene group and (10.69 ±1.37)%in the pemetrexed group (P<0.01). Conclusion Pemetrexed combined with β-elemene can significantly inhibit the proliferation and synergistically accelerate the apoptosis of HeLa cells .
8.Pioglitazone administration combined with bone marrow mesenchymal stem cells transplantation improved the heart function of rats with myocardial infarction
Quanhua WU ; Jingying HOU ; Tianzhu GUO ; Tingting ZHONG ; Huibao LONG ; Yue XING ; Changqing ZHOU ; Shaoxin ZHENG ; Tong WANG
Chinese Journal of Tissue Engineering Research 2015;(23):3698-3704
BACKGROUND:Our previous work has demonstrated that bone marrow mesenchymal stem cels (BMSCs) transplantation can improve the heart function of rats with myocardial infarction. However, the overal efficacy is not satisfactory. OBJECTIVE: To adopt pioglitazone as a peroxisome proliferator-activated receptor gamma (PPAR-γ) agonist combined with BMSCs transplantation therapy, thereby further improving cardiac function of rats with myocardial infarction as wel as investigating the relevant mechanisms. METHODS:Twenty Sprague-Dawley rats with myocardial infarction were induced by the left anterior descending coronary artery ligation. The animals were randomized into two groups: BMSCs and BMSCs+pioglitazone. Two weeks later, al the animals received the injection of BMSCs labeled with PKH26 in PBS into the local infarct zone, and then pioglitazone (3 mg/kg/d) was given by the oral gavage for 2 weeks in the BMSCs+pioglitazone group after the cel transplantation. After 2 weeks of cel transplantation, cardiac functions were evaluated by echocardiography. The expressions of PPAR-γ, Connexin 43 and molecules in TGF-β1/SMAD signaling pathway were examined in different areas of the left ventricle from each harvested heart using immunofluorescent staining, western blot assay and qRT-PCR. RESULTS AND CONCLUSION:There were no differences in the baseline parameters of cardiac function between the two groups. At 2 weeks after cel transplantation, the left ventricular internal diameter at end-diastole, left ventricular internal diameter at end-systole and left ventricular ejection fraction were significantly improved in the BMSCs+ pioglitazone group; the expressions of PPAR-γ and Connexin 43 were distinctly increased in different zones of the left ventricle; the levels of TGF-β1, SMAD2 and SMAD3 were obviously attenuated in the infarct zone and border zone. The above-mentioned findings suggest that pioglitazone, a PPAR-γ agonist, can enhance BMSCs potential in improvingthe heart function after myocardial infarction, and PPAR-γ may elevate the expression of Connexin 43via the blockade of the TGF-β1/SMAD signaling pathway in the procedure.
9.Rejuvenation of the forehead/temple by limited incision.
Xing-yue ZHENG ; Zhi-hong ZHENG ; Wei-zhong LIANG ; Hai-ming ZHANG ; Jia-qi WANG ; Ye-guang SONG
Chinese Journal of Plastic Surgery 2005;21(3):184-186
OBJECTIVETo utilize multiplane, subcutaneous and subperiosteal, dissection through small incisions in scalp to rejuvenate aging signs of forehead/temple.
METHODSForehead: We make four small incisions in scalp, widely separate tissues between subperiosteum skin and frontal muscle to form galea frontal muscle-periosteum flap, the flap is tightened and sutured with the galea at the posterior border of the incision. This method avoid to excise scalp. Temple: there are two small incisions in the scalp of temple at each side. Superficial temple fascia and orbicularis oculi muscle as well is dissected from deep temporal fascia and skin respectively, then tightened and sutured with the superficial part of deep temporal fascia, excising scalp is not necessary.
RESULTSTwenty patients have received this treatment, the effects are satisfying.
CONCLUSIONSMultiplane dissection through small incisions can remove wrinkles of skin, correct the prolapse of eyebrow and avoid the complications of coronary incision. This approach brings more rapid recovery of patients, it is safe and affective.
Adult ; Female ; Follow-Up Studies ; Forehead ; surgery ; Humans ; Male ; Middle Aged ; Rejuvenation ; Rhytidoplasty ; methods
10.Levels of environmental endocrine disruptors in umbilical cord blood and maternal blood of low-birth-weight infants.
Ling LIN ; Li-Xing ZHENG ; Yue-Ping GU ; Jie-Yun WANG ; Yun-Hui ZHANG ; Wei-Min SONG
Chinese Journal of Preventive Medicine 2008;42(3):177-180
OBJECTIVETo monitor the biological levels of environmental endocrine disruptors (EDs, phthalates and surfactants) in the umbilical cord blood and maternal blood of low-birth-weight infants.
METHODSAll 30 umbilical cord blood samples and 21 maternal blood samples were collected from low-birth-weight infants. The concentration of four kinds of phthalates (di-2-ethylhexyl phthalate, DEHP; mono-2-ethylhexyl phthalate, MEHP; di-ethyl phthalate, DEP; di-n-butyl phthalate, DBP) and two kinds of surfactants (4-nonylphenol, 4-NP; octylphenol, OP) in these blood samples were measured by using reversed-phase high performance liquid chromatography.
RESULTSThe mean birth weight and birth length of low-birth-weight infants were (2158.48 +/- 125.06) g and (45.36 +/- 2.52) cm, respectively. The concentrations of DEP, MEHP, DBP, DEHP, 4-NP and OP were 18.90, 11.87, 7.67, 8.84, 1.51 and 2. 86 mg/L in maternal blood, and the detective rates were 86.7%, 63.3%, 60.0%, 63.3%, 56.7% and 66.7%, respectively. In umbilical cord blood, the concentrations of those EDs were 11.92, 9.94, 5.71, 5.20, 1.12 and 1.19 mg/L; the detective rates were 86.7%, 63.3%, 60.0%, 63.3%, 56.7% and 66.7%. No matter in maternal blood or in umbilical cord blood, the contents and detective rates of phthalates were higher than the surfactants. The concentration of MEHP was higher than its primer, DEHP. The contents of the target EDs in umbilical cord blood were less than those in the matched maternal blood. The percentages were 47.82% -84.05%.
CONCLUSIONPeople could be exposed to EDs from embryo period. And this should be paid attention by the related departments.
Diethylhexyl Phthalate ; blood ; Endocrine Disruptors ; blood ; Fetal Blood ; chemistry ; Humans ; Infant ; Infant, Low Birth Weight ; blood ; Infant, Newborn ; Mothers ; Surface-Active Agents