1.Synthesis and antimicrobial evaluation of coumarin-based benzotriazoles and their synergistic effects with chloromycin and fluconazole.
Yuan SHI ; Chenghe ZHOU ; Xiangdong ZHOU ; Rongxia GENG ; Qinggang JI
Acta Pharmaceutica Sinica 2011;46(7):798-810
A series of new coumarin-based benzotriazole derivatives were successfully synthesized via a multi-step sequence of cyclization, etherification and N-alkylation, and were confirmed by 1H NMR, IR, MS spectra as well as elemental analyses. All these synthesized coumarin compounds were evaluated for in vitro antimicrobial activities against four Gram-positive bacteria, four Gram-negative bacteria and three fungi by two fold serial dilution technique. The bioactive assay showed that all these prepared coumarin benzotriazoles could inhibit the growth of the tested bacterial and fungal strains. Title compounds 11a-11e and 13a-13c were more active than chloromycin on Proteus vulgaris ATCC 6896. Coumarin benzotriazoles 11a and 11b displayed comparable antibacterial efficacy against Staphylococcus aureus ATCC 25923 and Micrococcus luteus ATCC 4698 in comparison with reference drug chloromycin. Compared to fluconazole, compounds 11a-11d displayed stronger inhibition on Aspergillus fumigatus ATCC 96918. Moreover, coumarin-based benzotriazoles in combination with antibacterial chloromycin or antifungal fluconazole, showed notable antimicrobial efficacy with less dosage and broader antimicrobial spectrum. More importantly, fluconazole-insensitive A. fumigatus and methicillin-resistant Staphylococcus aureus N 315 (MRSA) were sensitive to these combined drugs.
2.Synthesis of 6?-butylaminocholestan-3?,5?-diol,an analogue of anti-tumoral dendrogenin
Bo FANG ; Linghui TAO ; Xiangdong ZHOU ; Chenghe ZHOU
Journal of Third Military Medical University 2003;0(10):-
Objective To synthesize 6?-butylaminocholestan-3?,5?-diol,a new analogue of anti-tumoral dendrogenin with a new method.Methods 6?-butylaminocholestan-3?,5?-diol was synthesized in 5 steps using cholesterol as the starting material,3?,5?-dihydroxyl-cholestan-6-one as the key intermediate and imidation-reduction of one-pot 2 steps as the key steps.Results The target compound was synthesized in a total yield of 62% and its structure were consistent with MS (476),HRMS (476.446 5),[?]25D(-57.0?),IR (3387),1HNMR [2.67~2.61 (1H,m,6?-H)],13CNMR spectrum and elemental analyses.Conclusion Our synthetic route to 6?-butylaminocholestan-3?,5?-diol is characterized by easily available and cheap starting material,high total yield and easy industrialization.
3.Experimental study on survival time and mortality of conscious rats immersed in different cold seawater
Lina CHEN ; Jianbo HUAN ; Chenghe SHI ; Wei DAI ; Danfeng YUAN ; Jihong ZHOU ; Zhihai HAN
Journal of Regional Anatomy and Operative Surgery 2017;26(7):469-474
Objective To observe the effects of seawater immersion at different temperatures on survival time and mortality and physiological state of non-anesthetized rats.Methods Totally 100 SD male rats(The abdominal cavity was implanted with a temperature sensor in advance)were randomly divided into five groups which were immersed in 20 ℃,17 ℃,15 ℃,13 ℃ and 10 ℃ seawater,respectively.Each group contains 20 rats.The changes of respiration,heart rate and muscle fibrillation within 2 hours were observed and the survival time and mortality of each group were counted in 24 hours.The decrease trend of intraperitoneal temperature in rats was analyzed retrospectively within 2 hours.Results Soaking for 10 minutes,the respiratory and heart rate of each group were significantly increased,but there was no significant difference among groups(P>0.05).The respiratory and heart rate decreased rapidly between 10 and 40 minutes,and the decline was slower relatively between 40 and 80 minutes.Soaking for 80 minutes,the respiration rate of rats among groups had significant difference(P<0.05).Immersing for 100 minutes,the heart rates of rats in each group were significantly different(P<0.05).Soaking for 20 minutes,the muscle fibrillation of 15 ℃,13 ℃ and 10 ℃ group reached the peak,and there were significant differences among groups(P<0.05),then disappeared.However the rats in 20 ℃ and 17 ℃ group reached the peak at 30 minutes,but there was no significant difference between two groups(P>0.05),hereafter the muscle fibrillation was maintained at a certain level.The mean survival time of 20 ℃ group,17 ℃ group,15 ℃ group,13 ℃ group and 10 ℃ group in 24 hours were(23.6±1.23)hours,(15.0±4.16)hours,(7.7±3.21)hours,(2.4±0.91)hours and (1.1±0.39)hours,respectively,and the survival curve of each group was statistically significant(P<0.05).The intraperitoneal temperature of rats showed a decline in the cliff,the lower the water temperature,the faster the descending.Soaking for 40 minutes,the difference of intraperitoneal temperature of each group was statistically significant(P<0.05).Conclusion The effects of seawater immersion at different temperatures on the physiological state and survival time and mortality of rats are significantly different.With the decrease of water temperature,the physiological state changes more obviously,the survival time is shorter and the mortality rate is higher.
4.Clinical Observation on Traditional Chinese Medicine Dietary Therapy for Improving Symptoms of Cancer Patients with Chemotherapy
Chenghe ZHAO ; Yazhi XIE ; Shaomei ZHOU ; Yufei YANG
World Science and Technology-Modernization of Traditional Chinese Medicine 2017;19(4):663-668
This study was aimed to verify the effect of traditional Chinese medicine (TCM) dietary therapy in improving symptoms induced by chemotherapy.A total of 20 patients were included in the study according to the inclusion and exclusion criteria.The randomized autocontrol double-blind method was used in the trial.In group A,the dietary therapy was used in the first chemotherapy cycle,and the control therapy was used in the second chemotherapy cycle;and vice versa for group B.There were 3 cases fell out of the study.Finally,there were 8 cases in group A and 9 cases in group B.There were all together 17 patients.Observations were given on patients from both groups for 2 cycles.So the total observed case number was 34 person-time.Observations were given on differences of quality of life (QOL) and unpleasant symptoms (including fatigue,poor appetite,dry stool,loose stool,nausea and vomiting,night sweating,spontaneous sweating,dry mouth and throat,bitter taste in the mouth,pain,restlessness and irritable,insomnia and other symptoms) by TCM dietary therapy and control therapy on cancer patients during chemotherapy.The results showed that there was significant difference on the tenth day of chemotherapy from the QOL (P<0.05).There was significant difference on the tenth day of chemotherapy from the total score of unpleasant symptoms (P<0.05).Among them,there were significant differences on fatigue and poor appetite on the tenth day of chemotherapy (P<0.05).It was concluded that TCM dietary therapy has certain effects in the improvement of patients' clinical symptoms during chemotherapy.On the tenth day of chemotherapy,the unpleasant symptoms of TCM dietary therapy group were lower than that of the control group (P<0.05);the QOL score was higher in the treatment group than that of the control group (P<0.05).After in-depth discussion,there was statistical significance on dietary therapy in improving fatigue and poor appetite in the dietary therapy group.It demonstrated that TCM dietary therapy help patients during chemotherapy.
5.Preogress in diagnosis and treatment of diabetic foot osteomyelitis
Chunhao ZHOU ; Hongan ZHANG ; Jia FANG ; Guoyun CHENG ; Rui TAO ; Chenghe QIN
Chinese Journal of Orthopaedic Trauma 2019;21(7):636-640
Diabetic foot ulcer is a major complication of diabetes which is the most expensive and the most difficult to deal with and leads to a high rate of non-traumatic amputation.Diabetic foot osteomyelitis results from aggravation of diabetic foot ulcer.Unfortunately,the current therapeutic outcomes of diabetic foot osteomyelitis are still unsatisfactory because of its difficult diagnosis and special treatment protocols which are entirely different from those for conventional soft tissue infections.This paper summarizes the latest advances achieved in diagnosis and treatment of diabetic foot osteomyelitis.
6.Proximal versus distal tibial bone transport in the treatment of chronic tibial osteomyelitis
Guoyun CHENG ; Qingrong LIN ; Chunhao ZHOU ; Xiangqing MENG ; Hongan ZHANG ; Jia FANG ; Chenghe QIN
Chinese Journal of Orthopaedic Trauma 2020;22(5):379-383
Objective:To compare the clinical effects on new bone formation and foot-ankle function between proximal tibial bone transport and distal tibial bone transport in the treatment of massive bone defects after tibial osteomyelitis debridement.Methods:From July 2012 to July 2017, 42 patients with chronic tibial osteomyelitis received bone transport surgery at Department of Orthopaedics, Nanfang Hospital.According to the Cierny-Mader classification for chronic osteomyelitis, all of them belonged to diffusive tibial osteomyelitis (type IV).Of them, 32 were treated by proximal tibial bone transport after tibial osteomyelitis debridement.In the proximal group, there were 27 males and 5 females, aged from 17 to 65 years and involving 20 left and 12 right sides. The other 10 cases received distal tibial bone transport. In the distal group, all of them were male, aged from 25 to 63 years and involving 6 left and 4 right sides. The 2 groups were compared in terms of external fixation index (EFI) and American Orthopaedic Foot & Ankle Society(AOFAS) Ankle and Hindfoot Scale.Results:There were no significant differences between the 2 groups in the preoperative general data such as gender, age or osteomyelitis site, indicating the 2 groups were comparable ( P>0.05). Both groups obtained complete follow-up. The proximal group was followed up for 590.1 d ± 287.3 d and the distal group for 615.6 d ± 130.6 d, showing no significant difference between groups ( P>0.05). In the proximal group 2 cases developed talipes equinovalgus after bone transport while in the distal group 3 cases did, and surgical intervention was needed for them. Surgical intervention was also carried out for16 cases of non-union at the docking site in the proximal group and for 2 ones in the distal group. The EFI was 76.2 d/cm±50.0 d/cm for the proximal group and 84.3 d/cm ± 59.9 d/cm for the distal group, showing no significant difference between groups ( P>0.05). The AOFAS scores were 81.4±10.1 for the proximal group and 60.0±5.9 for the distal group, showing a significant difference ( P<0.05). Conclusion:In the treatment of massive bone defects after tibial osteomyelitis debridement, no significant difference has been observed in the effect on bone formation between proximal tibial bone transport and distal tibial bone transport, but the former transport may have a less adverse effect on foot-ankle function.
7.Management of pediatric acute hematogenous osteomyelitis
Rui TAO ; Chenghe QIN ; Jia FANG ; Chunhao ZHOU ; Xiangqing MENG
Chinese Journal of Orthopaedic Trauma 2020;22(9):818-823
Acute hematogenous osteomyelitis (AHO) is the type of its kind diagnosed most frequently in pediatric patients. In the past decade, the incidence of methicillin-resistant Staphylococcus aureus infections has increased in children. The more complex situation of infections may lead additionally to deep vein thrombosis (DVT), septic pulmonary embolism, pneumonia, empyema, endocarditis, bacteremia and septic shock. Hence, hospital stays are often lengthy and patients often critically ill. Since delayed appropriate therapy can lead to chronic osteomyelitis, as well as impairments in bone growth and development, early accurate diagnosis and prompt initiation of appropriate treatment remain central principles in the evaluation and treatment of AHO. Therefore, care of children with AHO inevitably requires an organized and interdisciplinary approach to reach timely, comprehensive and accurate diagnoses so that effective treatment may be carefully planned and enacted with subsequent monitoring of the child until clinical resolution is achieved. This review is devoted exclusively to the management of AHO in children, providing an update on the current understanding of existing evidence and future directions to improve care for pediatric AHO.
8.An evidence-based clinical guideline for the treatment of infectious bone defect with induced membrane technique (version 2023)
Jie SHEN ; Lin CHEN ; Shiwu DONG ; Jingshu FU ; Jianzhong GUAN ; Hongbo HE ; Chunli HOU ; Zhiyong HOU ; Gang LI ; Hang LI ; Fengxiang LIU ; Lei LIU ; Feng MA ; Tao NIE ; Chenghe QIN ; Jian SHI ; Hengsheng SHU ; Dong SUN ; Li SUN ; Guanglin WANG ; Xiaohua WANG ; Zhiqiang WANG ; Hongri WU ; Junchao XING ; Jianzhong XU ; Yongqing XU ; Dawei YANG ; Tengbo YU ; Zhi YUAN ; Wenming ZHANG ; Feng ZHAO ; Jiazhuang ZHENG ; Dapeng ZHOU ; Chen ZHU ; Yueliang ZHU ; Zhao XIE ; Xinbao WU ; Changqing ZHANG ; Peifu TANG ; Yingze ZHANG ; Fei LUO
Chinese Journal of Trauma 2023;39(2):107-120
Infectious bone defect is bone defect with infection or as a result of treatment of bone infection. It requires surgical intervention, and the treatment processes are complex and long, which include bone infection control,bone defect repair and even complex soft tissue reconstructions in some cases. Failure to achieve the goals in any step may lead to the failure of the overall treatment. Therefore, infectious bone defect has been a worldwide challenge in the field of orthopedics. Conventionally, sequestrectomy, bone grafting, bone transport, and systemic/local antibiotic treatment are standard therapies. Radical debridement remains one of the cornerstones for the management of bone infection. However, the scale of debridement and the timing and method of bone defect reconstruction remain controversial. With the clinical application of induced membrane technique, effective infection control and rapid bone reconstruction have been achieved in the management of infectious bone defect. The induced membrane technique has attracted more interests and attention, but the lack of understanding the basic principles of infection control and technical details may hamper the clinical outcomes of induced membrane technique and complications can possibly occur. Therefore, the Chinese Orthopedic Association organized domestic orthopedic experts to formulate An evidence-based clinical guideline for the treatment of infectious bone defect with induced membrane technique ( version 2023) according to the evidence-based method and put forward recommendations on infectious bone defect from the aspects of precise diagnosis, preoperative evaluation, operation procedure, postoperative management and rehabilitation, so as to provide useful references for the treatment of infectious bone defect with induced membrane technique.
9. Identification of the long noncoding RNA_ AK096792 in cord blood as a clinical predictor for early diagnosis of bronchopulmonary dysplasia in preterm infants
Yan ZHANG ; Tianping BAO ; Xiaotong SONG ; Yunjia HAO ; Zhaofang TIAN ; Chen SONG ; Yazhou SUN ; Weiwei WANG ; Bin ZHOU ; Chenghe TANG ; Jiaqin WANG
Chinese Journal of Applied Clinical Pediatrics 2018;33(14):1075-1078
Objective:
To investigate the feasibility of long noncoding RNA (lncRNA)_AK096792 as a clinical predictor of bronchopulmonary dysplasia (BPD) in preterm infants.
Methods:
All the cord blood(2-5 mL) of very low birth weight (VLBW) preterm infants born in Huai′an First Hospital Affiliated to Nanjing Medical University were collected from December 1, 2015 to December 1, 2017.Moreover, the peripheral blood(2 mL) of those VLBW infants diagnosed with BPD was also collected.A total of 36 infants with BPD were collected.Another 36 cases of premature children with VLBW were chosen as control group according to random number table.The relative content of lncRNA_AK096792 in cord blood and peripheral blood was detected by using real-time quantitative PCR (qPCR). Additionally, the correlation of lncRNA_AK096792 levels between cord and peripheral blood of BPD infants was analyzed.The sensitivity and specificity of lncRNA_AK096792 for BPD were analyzed by using receiver operating curve test.
Results:
(1)LncRNA_AK096792 was a common, evolutionarily conserved, non-coding RNA present in both mouse and human.(2) The expression level of lncRNA_AK096792 in peripheral blood was significantly higher than that in cord blood in BPD group[(463.3±352.0)%