1.Cultivation of Students' Innovation Ability in the Medicinal Chemistry Teaching
Chinese Journal of Medical Education Research 2006;0(12):-
In the process of chemical drugs teaching theory,we should teach the knowledge of the history of drug invention,design plan,research process and case discussion,and at the same time,try to use some new methods and interdisciplinary comprehensive experiments in the experimental teaching,so as to enhance the students'ability of combining theory with practice and achieve our cultivation goal.
2.Short-term efficacy of high-intensity ultraviolet B versus 308-nm excimer laser for the treatment of vitiligo
Dake DONG ; Lijia YANG ; Shiqin TAO ; Jiaqiang WU ; Leihong XIANG
Chinese Journal of Dermatology 2014;47(1):59-61
Objective To compare the short-term efficacy of high-intensity ultraviolet B (UVB) versus 308-nm excimer laser for the treatment of vitiligo.Methods Eighty patients with vitiligo were equally divided into two groups to be treated with high-intensity UVB twice a week or 308-nm excimer laser once a week for eight weeks.Repigmentation was evaluated at the end of the treatment.Results After eight weeks of treatment,repigmentation of different degrees was observed in 83.6% and 86.1%,and marked repigmentation in 42.1% and 50%,of the UVB-and excimer laser-treated lesions,respectively.The response rate was significantly lower in facial lesions receiving high-intensity UVB radiation than in those receiving excimer laser radiation (49.1% vs.68.4%,x2 =4.32,P < 0.05),but similar at the other body sites between the two treatment (all P > 0.05).The cumulative dosage required for initial repigmentation was similar between high-intensity UVB and 308-nm excimer laser (t =0.89,P > 0.05),while the treatment sessions and cumulative dosage required for marked or better repigmentation were significantly increased in UVB-compared with excimer laser-treated lesions (both P < 0.01).In addition,both high-intensity UVB and 308-nm excimer laser were suitable for childhood and active vitiligo.Conclusions Both high-intensity UVB and 308-nm excimer laser are safe and effective in the treatment of vitiligo with rapid onset of action,and the latter appears to be superior to the former in efficacy.
3.Design, synthesis and antitumor activities of novel E-substituted 2,3-diaryl propenoic acyloxy phosphonate derivatives.
Jiaqiang YANG ; Silan LIU ; Wanli CHE ; Maosheng ZHANG ; Xiaoqiang WAN ; Honglu JIAN ; Yongzheng CHEN
Acta Pharmaceutica Sinica 2015;50(4):464-8
According to the super-position principle of the reinforcement of biological activities, a series of novel E-substituted 2, 3-diaryl propenoic acyloxy phosphonate derivatives were designed and synthesized. And the structures of the target compounds were confirmed by IR, 1H NMR, 13C NMR and elemental analysis. Furthermore, the cytotoxicities of all compounds on A-549, SGC-7901 and EC-109 in vitro were evaluated by MTT assay, and some of them showed good antitumor activity. Among the active compounds, especially, the IC50 value of compound 3e was (12.7 ± 1.9) μmol x L(-1) against A-549 cells, similar to cisplatin [IC50 = (8.0 ± 1.5) μmol x L(-1)], compounds 3g and 3k had better inhibition effect on EC-109 cells growth, with the IC50 values of (9.5 ± 1.8) μmol x L(-1) and (11.5 ± 0.9) μmol x L(-1) respectively, and compounds 3i and 3k exhibited good cytotoxic property on A-549, SGC-7901 and EC-109, which were worth further investigation.
4.Clinical experience of changing the membranous pulmonary system during extracorporeal membrane oxygenation in infants after congenital heart disease operation
Yue CHEN ; Xiaoliang QIAN ; Weijie LIANG ; Jianchao LI ; Leiyi YANG ; Jiaqiang ZHANG ; Taibing FAN ; Zhaoyun CHENG
Chinese Pediatric Emergency Medicine 2021;28(4):297-300
Objective:To summarize the clinical experience of changing the membranous pulmonary system during extracorporeal membrane oxygenation(ECMO) in infants after congenital heart disease opration with cardiopulmonary bypass.Methods:From January to September in 2019, 6 cases of congenital heart disease with cardio-pulmonary bypass in our hospital were analyzed retrospectively, whose membrane obstruction occurred during ECMO treatment and replaced successfully.The hemodynamics and blood gas before and after replacement of ECMO system were observed, and the experience was summarized.Results:Six patients(3 males and 3 females), aging from 1 to 3 months and weighing from 3.0 to 4.9 kg, were received VA-ECMO adjuvant therapy.The ECMO system replacement process was smooth and took 175-209 s. The hemodynamic of the children was stable.The ECMO support time was 134-249 h. After the improvement of cardiac systolic function, all children were successfully withdrawn and survived.Conclusion:The improved method of liquid replacement in ECMO system can make full use of the blood components in the original system and avoid the loss of blood tangible components.According to the plan of rapid replacement, the risk of replacement will not be increased.
5.A prevalence survey of hyperlipidemia in the middle-aged and elderly people in Guangxi Hei Yi Zhuang population
Ruixing YIN ; Dezhai YANG ; Limei YAO ; Muyan LI ; Qi BI ; Tangwei LIU ; Shangling PAN ; Jing SHEN ; Yuming CHEN ; Rongshan LI ; Weixiong LIN ; Fengping HE ; Jiaqiang DENG ; Guangqing YE ; Xiuyan LONG ; Jiandong HUANG ; Zhenbiao NONG
Chinese Journal of Geriatrics 2000;0(04):-
Objective To investigate the prevalence rate of hyperlipidemia in the middle-aged and elderly in Guangxi Hei Yi Zhuang population. Methods A total of 657 people of Hei Yi Zhuang nationality aged 40 years and over were surveyed. Blood pressure, body height, body weight, serum lipid and apolipoprotein levels were measured, and both body surface areas and body mass index were calculated. The results were compared with those in 520 people of Han nationality who also live in that district. Results The prevalence of hypercholesterolemia, hypertriglyceridemia, and hyperlipidemia in Hei Yi Zhuang vs. Han population were 28.9% vs. 35.8%(P0.05), and 36.2% vs. 42.3%(P0.05) respectively. Conclusions Prevalence of hyperlipidemia of Hei Yi Zhuang is lower than that of Han ethnic group, which might results from different dietary habit, life style, physical activity, and even genetic background.
6.Effect of ulinastatin on endoplasmic reticulum stress in cardiomyocytes of patients undergoing beat-ing heart mitral valve replacement
Xiongfei RONG ; Zhibin LANG ; Yali YANG ; Fanmin MENG ; Jiaqiang ZHANG
Chinese Journal of Anesthesiology 2017;37(11):1291-1295
Objective To evaluate the effect of ulinastatin on endoplasmic reticulum stress in car-diomyocytes of patients undergoing beating heart mitral valve replacement(MVR). Methods A total of 80 patients of both sexes with rheumatic heart disease complicated with mitral valve stenosis, aged 38-59 yr, weighing 43-73 kg, with American Society of Anesthesiology physical statusⅡorⅢ, scheduled for elective MVR, were divided into ulinastatin group(UTI group, n=40)and normal saline group(NS group, n=40) using a random number table. Immediately after opening the right atrium(T0), at 30 min of cardiopulmonary bypass(T1)and while suturing the right atrium(T2), blood samples from the radial artery were collected to determine the concentrations of plasma creatine kinase-MB and cardiac troponin T by enzyme-linked immu-nosorbent assay, and the right auricle specimens were collected for determination of the expression of glucose-regulated protein 78, CCAAT∕enhancer-binding protein homologous protein, c-Jun amino-terminal kinase (JNK)protein and mRNA(by real-time polymerase chain reaction or Western blot)and phosphorylated JNK (p-JNK)expression(by Western blot). The apoptosis in cardiomyocytes was detected by TUNEL at T0,2, and the apoptosis rate was calculated. Results Compared with group NS, the concentrations of plasma crea-tine kinase-MB and cardiac troponin T at T1,2and the apoptosis rate of cardiomyocytes were significantly de-creased at T2, and the expression of glucose-regulated protein 78, CCAAT∕enhancer-binding protein homolo-gous protein and JNK protein and mRNA and p-JNK was down-regulated at T1,2in group UTI(P<0.05). Conclusion The mechanism by which ulinastatin reduces myocardial damage is related to inhibiting endo-plasmic reticulum stress in cardiomyocytes of patients undergoing beating heart MVR.
7. Effect of dexmedetomidine on pyroptosis during lung ischemia-reperfusion in rats: an in vitro experiment
Xiangyan YAO ; Jiaqiang ZHANG ; Lu LI ; Xianhui DU ; Yanyan QI ; Libin MA ; Yali YANG ; Jiangling ZHANG ; Ning LI ; Hui ZHANG
Chinese Journal of Anesthesiology 2019;39(8):915-919
Objective:
To evaluate the effect of dexmedetomidine on pyroptosis during lung ischemia-reperfusion (I/R) in rats.
Methods:
Adult male Sprague-Dawley rats, weighing 250-320 g, were used in this study.The model of isolated lung perfusion was established using an IL-2 Isolated Perfused Rat or Guinea Pig Lung System after the rats were anesthetized.Thirty lungs in which an
8.Effects of bumetanide on changes of NKCC1 and KCC2 mRNA expression in hypothalamus and anxiety in adulthood induced by multiple sevoflurane exposure in neonatal rats
Baofeng YANG ; Jie WANG ; Changhong MIAO ; Changsheng LI ; Jiaqiang ZHANG ; Xihua LU
Chinese Journal of Behavioral Medicine and Brain Science 2020;29(9):780-784
Objective:To investigate the effects of bumetanide on changes of NKCC1 and KCC2 mRNA expression in hypothalamus and anxiety in adulthood induced by multiple sevoflurane exposure in neonatal rats.Methods:Eighty-one healthy male Sprague-Dawley rats, at postnatal 5 days (P5), were randomly divided into 3 groups ( n=27 in each group): control group (group C), multiple sevoflurane group (group MS) and bumetanide group (group B). The rats were commonly reared in the cage and received no anesthesia in group C. Animals were exposed to 2.1% sevoflurane for 2 h on P5, P7, P9 in group MS and group B. In group B, animals received intraperitoneal injection of 1.82 mg/kg bumetanide(Na + -K + -2Cl - cotransporter 1 blocker, NKCC1 blocker)at 30 min before every anesthesia.The animals in group C and group MS received the same dose of dimethyl sulfoxide subcutaneously at the same time as group B. The rats were observed for 30 minutes after recovery from anesthesia, and then breastfed normally.On the 9th day after birth, six rats were taken from each group immediately at the end of anesthesia and the blood was collected by left ventricular puncture for blood gas analysis.At 30 min after anesthesia, 6 animals in each group were decapitated and the hypothalamus part of brain tissue was collected.Then the expression level of IL-6 mRNA, NKCC1 mRNA and KCC2 mRNA were detected by RT-PCR.The other rats in each group were raised to 60 days for the elevated plus maze (EPM) test. Results:Compared with group C, the expression of IL-6 mRNA and NKCC1 mRNA in hypothalamus of MS group was up-regulated (IL-6: (1.000±0.207) vs (1.782±0.231); t=6.899, P<0.01; NKCC1: (1.000±0.255) vs (1.639±0.290); t=3.518, P<0.01), the KCC2 mRNA expression was down-regulated ((1.000±0.140) vs (0.733±0.115); t=3.017, P<0.001) and the NKCC1/KCC2 mRNA ratio increased ((1.000±0.276) vs (2.054±0.521); t=5.078, P<0.001) and the differences were statistically significant.Compared with MS group, the expression of IL-6 mRNA and NKCC1 mRNA in hypothalamus of group B was down-regulated (IL-6: (1.147±0.140); t=5.635, P<0.01; NKCC1: (1.038±0.385); t=3.310, P=0.01), KCC2 mRNA expression was up-regulated((0.988±0.194); t=2.880, P<0.05), NKCC1 / KCC2 mRNA ratio was decreased((1.027±0.200); t=4.950, P<0.001), and the differences were statistically significant.EPM behavioral test showed that compared with group C, the open arm residence time in MS group was significantly shorter than that in group C ((18.4±10.1)s vs (4.3±3.1)s; P<0.01); compared with group MS, the open arm residence time in group B was significantly prolonged((16.6±7.6)s, P<0.05). Conclusion:Bumetanide can reduce the up-regulation of NKCC1 level and the down-regulation of KCC2 level in neonatal rats after sevoflurane anesthesia, and alleviate the anxiety state of adult rats.
9.Effect of sevoflurane on unfolded protein response-related cell apoptosis during acute lung injury in rats undergoing cardiopulmonary bypass
Xiangyan YAO ; Jiaqiang ZHANG ; Lu LI ; Xianhui DU ; Yanyan QI ; Libin MA ; Yali YANG ; Jian-Gling ZHANG ; Ning LI ; Hui ZHANG
Chinese Journal of Anesthesiology 2019;39(3):314-318
Objective To evaluate the effect of sevoflurane on unfolded protein response-related cell apoptosis during acute lung injury in rats undergoing cardiopulmonary bypass ( CPB) . Methods For-ty-eight clean-grade healthy adult male Sprague-Dawley rats, aged 6-8 weeks, weighing 250-300 g, were allocated into 3 groups ( n=16 each) using a random number table method: sham operation group ( Sham group) , CPB group and sevoflurane group ( Sev group) . Left common carotid artery and right internal jugu-lar vein were only cannulated in group Sham. After establishing CPB, the flow rate was gradually adjusted to the maximum (100 ml·kg-1·min-1) and maintained for 60 min in group CPB. Two percent sevoflurane was inhaled for 30 min, and 15 min later the model of CPB was established in Sev group. Rats were sacri-ficed at 1 h after the end of CPB, lungs were removed and lung tissues were obtained. The pathological changes and ultrastructure of lung tissues were examined with a light microscope and with an electron micro-scope, respectively. The wet to dry weight ratio ( W∕D ratio) , apoptosis in lung cells ( by TUNEL assay) , expression of glucose-regulated protein 78 ( GRP78) , CCAAT∕enhancer-binding protein homologous protein (CHOP), c-Jun N-terminal kinase (JNK) and caspase-12 mRNA was determined by real-time polymerase chain reaction. The expression of GRP78, CHOP, phosphorylated JNK (p-JNK) and caspase-12 was de-tected by Western blot. The index of quantitative assessment of histologic lung injury ( IQA) was measured, and apoptotic index ( AI) was calculated. Results Compared with Sham group, the W∕D ratio, IQA and AI were significantly increased, the expression of GRP78, CHOP, JNK and caspase-12 was up-regulated ( P<0. 05) , and the pathological changes of lung tissues were accentuated in CPB group. Compared with CPB group, the W∕D ratio, IQA and AI were significantly decreased, the expression of GRP78, CHOP, JNK and caspase-12 was down-regulated ( P<0. 05) , and the pathological changes of lung tissues were sig-nificantly attenuated in Sev group. Conclusion The mechanism by which sevoflurane mitigates acute lung injury induced by CPB is related to inhibiting unfolded protein response related cell apoptosis in lung tissues of rats.
10.Optimization strategy of anesthesia for liver cancer resection: serratus anterior plane block-posterior rectus sheath block-general anesthesia
Congcong LI ; Yitian YANG ; Na LI ; Mengyan HAN ; Wei ZHANG ; Jiaqiang ZHANG
Chinese Journal of Anesthesiology 2022;42(1):24-28
Objective:To evaluate the optimization strategy of anesthesia for liver cancer resection using serratus anterior plane block-posterior rectus sheath block-general anesthesia.Methods:One hundred patients, aged 30-64 yr, with body mass index of 18-30 kg/m 2, of American Society of Anesthesiologists physical status Ⅱ or Ⅲ, with liver function Child-Pugh grade A or B, scheduled for elective liver cancer resection under general anesthesia, were divided into serratus anterior plane block combined with posterior rectus sheath block group (group S, n=50) and thoracic paravertebral block group (group T, n=50) using a random number table method.Ultrasound-guided serratus anterior plane block (20 ml) combined with posterior rectus sheath block (10 ml) was performed using 0.375% ropivacaine in group S. Ultrasound-guided paravertebral block was performed at T 7 and T 9(15 ml for each site) with 0.375% ropivacaine in group T. Anesthesia was induced with intravenous midazolam, propofol, sufentanil and cisatracurium and maintained with intravenous infusion of propofol and remifentanil and intermittent intravenous boluses of cisatracurium.BIS value was maintained at 40-60 during operation.Patient-controlled intravenous analgesia (PCIA) was performed with sufentanil and flurbiprofen at the end of operation, and oxycodone 5 mg was intravenously injected as rescue analgesic when the VAS score>3.The onset time and operation time of nerve block were recorded.The intraoperative consumption of sufentanil and remifentanil and occurrence of cardiovascular events within 30 min after skin incision were recorded.The effective pressing times of PCA and requirement for rescue analgesia within 48 h after operation were recorded.The recovery quality was measured using the 40-item quality of recovery questionnaire at 24 h before surgery and 24 and 48 h after surgery.Peripheral venous blood samples were collected at 24 h before surgery and 24 h and 7 days after surgery to determine the concentrations of interleukin-17 and interferon-gamma in serum.The postoperative time to first flatus, first ambulation time, and length of hospital stay were recorded.The nausea and vomiting, respiratory depression, skin itching, puncture site infection, pneumothorax and other adverse reactions were recorded within 48 h after operation. Results:Compared with group T, the operation time of nerve block was significantly shortened, the incidence of intraoperative hypotension was decreased ( P<0.05), and no significant change was found in the onset time of nerve block, intraoperative consumption of sufentanil and remifentanil, postoperative requirement for rescue analgesia, effective pressing times of PCA, time to first flatus, first ambulation time, and length of hospital stay, and 40-item quality of recovery scores and serum concentrations of interleukin-17 and interferon-gamma at each time point in group S ( P>0.05). No postoperative adverse reactions were found in either group. Conclusions:Compared with thoracic paravertebral nerve block combined with general anesthesia, serratus anterior plane block-posterior rectus sheath block-general anesthesia has shorter operation time and lower incidence of intraoperative hypotension when used for liver cancer resection.