1.Design, synthesis, and biological activities of histone deacetylase inhibitors with diketo ester as zinc binding group.
Hui LU ; Hong SU ; Bo YANG ; Qidong YOU
Acta Pharmaceutica Sinica 2011;46(3):293-8
Histone deacetylases (HDACs) inhibition causes hyperacetylation of histones leading to growth arrest, differentiation and apoptosis of tumor cells, representing a new strategy in cancer therapy. Many of previously reported HDACs inhibitors are hydroxamic acid derivatives, which could chelate the zinc ion in the active site in a bidentate fashion. However, hydroxamic acids occasionally have produced problems such as poor pharmacokinetics, severe toxicity and low selectivity. Herein we describe the identification of a new series of non-hydroxamate HDACs inhibitors bearing diketo ester moieties as zinc binding group. HDACs inhibition assay and antiproliferation assays in vitro against multiple cancer cell lines were used for evaluation. These compounds displayed low antiproliferative activity against solid tumor cells, while good antiproliferative activity against human leukemic monocyte lymphoma cell line U937. Compound CPUYS707 is the best with GI50 value of 0.31 micromol x L(-1) against U937 cells, which is more potent than SAHA and MS-275. HDACs inhibition activity of these compounds is lower than that expected, further evaluation is needed.
2.The Current Situation and Countermeasures of Sexual Education of University Students
Qi YOU ; Jianhua ZHENG ; Bai XU ; Hong BO
Chinese Journal of Medical Education Research 2003;0(04):-
Universities are cradles of leadership and full-developed specific professional.Besides specific courses,reasonable sexual health education should be set up to make the students succeed when they grow up.
3.Thinking and methods in practical assessment of TCM clinical therapeutic effect.
Hong-Cai SHANG ; Bo-Li ZHANG ; You-Ping LI
Chinese Journal of Integrated Traditional and Western Medicine 2008;28(3):266-268
Although traditional Chinese medicine (TCM) shows its effectiveness undoubtedly in clinical practice, the deficiency in objective assessment methods is yet a bottleneck which has restricted its development of modernization and internationalization. On the basis of clinical experiences, the authors discussed the title cutting from current situation and tendency, and expanded gradually. It is concluded that by aiming directly at problems and referring to the principle and methods of evidence-based medicine (EBM), using rationally the design in clinical practice and combined with individualization and standardization should be a feasible way for TCM clinical therapeutic effect assessment.
Diagnosis, Differential
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Drugs, Chinese Herbal
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therapeutic use
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Evidence-Based Medicine
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methods
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standards
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Humans
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Medicine, Chinese Traditional
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methods
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standards
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Phytotherapy
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Research Design
5.Observations on the Efficacy of Heat-sensitive Point Medicinal Moxibustion plus Percutaneous Administration of Tetrandrine in Treating Lumbar Intervertebral Disc Herniation
You-Gen SHENG ; Jian-Hong XIA ; Hai-Bo XU
Shanghai Journal of Acupuncture and Moxibustion 2018;37(3):320-323
Objective To investigate the clinical efficacy of heat-sensitive point medicinal moxibustion plus percutaneous administration of tetrandrine in treating lumbar intervertebral disc herniation. Methods One hundred and twenty patients with lumbar intervertebral disc herniation were randomized to treatment and control groups, 60 cases each. The treatment group received heat-sensitive point medicinal moxibustion plus percutaneous administration of tetrandrine and the control group, heat-sensitive point medicinal moxibustion alone. The VAS score and the JOA Score for Back Pain score were recorded in the two groups before and after treatment. The clinical therapeutic effects were compared between the two groups. Results There were statistically significant pre-/post-treatment differences in the JOA Score for Back Pain score and the VAS score in the two groups (P<0.01). There were statistically significant post-treatment differences in the JOA Score for Back Pain score and the VAS score between the treatment and control groups (P<0.01). The excellent and good rate was 80.0% in the treatment group and 55.0% in the control group; there was a statistically significant difference between the two groups (P<0.01). Conclusion Heat-sensitive point medicinal moxibustion plus percutaneous administration of tetrandrine is an effective way to treat lumbar intervertebral disc herniation.
6.External bracket fixation for tibia diaphysis complex fracture involving proximal and distal articular fractures
Chun-You WAN ; Bao-Tong MA ; Hong-Bin JIN ; Jing-Bo WANG ; Hui YAO ; Yandong LU ;
Chinese Journal of Trauma 2003;0(08):-
Objective To evaluate the clinical outcome of external bracket fixation in the treat- ment of complex tibia diaphysis fracture involving intra-articular fractures.Methods Forty-two cases of complex tibia diaphysis fracture with proximal and distal intra-articular fractures treated surgically in our hospital from January 1999 to January 2004 were analyzed.The complex tibia diaphysis fractures were categorized according to the AO classification as type C2 (multiple segments fracture) and type C3 (ir- regular fracture),proximal and distal intra-articular fractures in 23 and 19 cases,respectively.Definite operation was done within one week.Twenty-two cases were treated with simple external fixator,and 20 cases treated with screws and external fixator.Results All the 42 cases were followed-up regularly. According to AO evaluation of the knee and ankle joint movement,83% (35/42 cases) of the cases gained satisfactory functional outcome,14% (6/42 cases) had quite satisfactory results and 2% (1/42 case) had unsatisfactory functional outcome.Conclusion External bracket fixation can obtain outcome of relative length of the tibia and fibula,tube structure reconstruction,smoothness of the articular surface and the parallel and symmetric relation of knees and ankles for complex tibia diaphysis fracture with proxi- mal and distal intra-articular fracture.The arthritis resulting in pain in movement and restriction of func- tion is considered to be the most important factor affecting the joint function.Early functional exercise is important for best recovery of knee and ankle function.
7.Effect of rabbit adipose-derived stem cells transfected by adenoviral vector mediated hTGF-?_1 gene on chondrocyte differentiation in vitro
Zhong FANG ; Feng LI ; Hong-Bo YOU ; Wei XIONG ; Guang-Hui LI ;
Chinese Journal of Rheumatology 2001;0(04):-
Objective To investigate the proliferation of rabbit adipose-derived stem cell(ADSCs) transfected by adenoviral vector mediated hTGF-?_1 gene and its chondrocyte differentiation potential.Methods The Ad-hTGF-?_1 plasmid vetor which had the hTGF-?_1 gene was developed and transfected the ADSCs.The experimental group was the hTGF-?_1 transfected group.The cells enclosed by alginate were cultured in com- plete chondrogenie medium(CMM).The morphology of the cells were observed,and RT-PCR was used to measure hTGF-?_1 and collagenⅡexpression,at the same time western blot and immunohistochemistry were applied to detect the expression of collagenⅡin ADSCs before and after transfected with hTGF-?_1 gene. Results The hTGF-?_1 transfected ADSCs became the polygon and it proliferated well.The RT-PCR result of hTGF-?_1 on the transfected group was better than the control after transtected for 7 day and 21 day.The dif- ference between the two groups was significant(P
8.The mechanism of "Trichosanthis Fructus-Allii Macrostemonis Bulbus" on phlegm and blood stasis syndrome-related cardiovascular diseases based on network pharmacology and experimental verification
Bo ZHANG ; Yu-ning LIANG ; You-li BAO ; Li ZHU ; Xin SUN ; Hong-fei WU
Acta Pharmaceutica Sinica 2023;58(6):1452-1463
This study aimed to investigate the mechanism of "Trichosanthis Fructus-Allii Macrostemonis Bulbus" (GX) on phlegm and blood stasis syndrome (PBSS) rats combining the methods of network pharmacology and experimental verification. Animal experiment ethical requirements were approved by the Ethical Committee Experimental Animal Center of Anhui University of Chinese Medicine (grant number: AHUCM-rats-2021070). Based on the HPLC-Q-TOF-MS analysis and database, 69 chemical constituents of GX and 163 targets of GX for the treatment of phlegm and blood stasis-related cardiovascular diseases were obtained. Then, key targets such as serine/threonine kinase 1 (Akt1), tumor necrosis factor (TNF), interleukin 6 (IL6), vascular endothelial growth factor A (VEGFA), cellular tumor antigen p53 (Tp53) were screened. Pathway analysis showed that the targets of GX in the treatment of phlegm and blood stasis-relate cardiovascular diseases were mainly involved in PI3K/Akt signaling pathway, sphingolipid metabolism, platelet activation, hypoxia inducible factor-1 (HIF-1), ras-proximate-1 (rap1) and other signaling pathways. In addition, molecular docking analysis showed that apigenin, cucurbitacin D, linolenic acid and kaempferol and other key components had potential binding ability with Akt1, TNF, IL6, VEGFA and Tp53. In the animal experiments, compared to the phlegm and blood stasis syndrome group, GX could significantly improve the traditional Chinese medicine syndrome score, blood lipid, vascular endothelial structure disorders and reduce serum endothelin-1 (ET-1) level, increase serum nitric oxide (NO) and endothelial nitric oxide synthase (eNOS) levels, which could restore aortic endothelial function. In addition, the expression of intercellular cell adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) in aorta could be significantly reduced, which could improve the vascular endothelial injury of aorta. Western blot revealed that GX could significantly decrease the phosphorylation levels of phosphoinositide 3-kinase (PI3K) and Akt in aorta. This study revealed the mechanism of GX in treatment of phlegm and blood stasis-relate cardiovascular diseases is consistent with the characteristics of multiple ingredients, multiple targets and multiple pathways. In addition, this study also clarified that the reversal of pathological of phlegm and blood stasis syndrome rats may be related to GX inhibiting PI3K/Akt signaling pathway, which could improve vascular inflammation and vascular endothelial function injury.
9.Microsurgical resection of craniopharyngioma of the third ventricle via an improved transventricular approach.
Jian-guo XU ; Chao YOU ; Bo-wen CAI ; Shu JIANG ; Hong SUN ; Fu-you GUO ; Yong-bo YANG ; Bo WU
Chinese Medical Journal 2005;118(10):806-811
BACKGROUNDCraniopharyngioma of the third ventricle is difficult to treat and its therapeutic regimens and operative approaches have been controversial. This study was undertaken to probe indications for microsurgical resection of craniopharyngioma of the third ventricle via an improved transventricular approach, its surgical procedures and therapeutic effects, and prevention of postoperative complications.
METHODSFifty-one patients with craniopharyngioma of the third ventricle were treated from January 2000 to October 2004 by an improved transventricular approach for removing the tumor via the interventricular foramen, the intermedius of the septum pellucidum or choroid fissure. Symptoms and signs of the patients, and results of imaging, operation, and follow-up were analyzed.
RESULTSOf the 51 patients who had received the improved transventricular resection, 4 underwent a combined approach with an entrance of the pterion. Forty patients (78.43%) underwent total resection and others subtotal resection, without an operative death. Epileptic seizures were found in 3 patients (5.88%) and subdural effusion in the operative field in 4 (7.84%). All patients showed good general conditions after operation, and follow-up for an average of 27.52 months showed relapse of the tumour in 8 patients (15.69%).
CONCLUSIONSMicrosurgical resection of craniopharyngioma of the third ventricle by an improved transventricular approach has advantages of operative safety and efficacy, lower mortality and disability, and less complications.
Adolescent ; Adult ; Aged ; Cerebral Ventricle Neoplasms ; diagnosis ; pathology ; surgery ; Child ; Child, Preschool ; Craniopharyngioma ; diagnosis ; pathology ; surgery ; Female ; Humans ; Infant ; Male ; Microsurgery ; Middle Aged ; Pituitary Neoplasms ; diagnosis ; pathology ; surgery ; Third Ventricle
10.Clinical features and prognosis of gastrointestinal injury due to foreign bodies in the upper gastrointestinal tract in children: a retrospective analysis of 217 cases.
Lu-Jing TANG ; Hong ZHAO ; Jin-Gan LOU ; Ke-Rong PENG ; Jin-Dan YU ; You-You LUO ; You-Hong FANG ; Fei-Bo CHEN ; Jie CHEN
Chinese Journal of Contemporary Pediatrics 2018;20(7):567-571
OBJECTIVETo study the clinical features and prognosis of gastrointestinal injury caused by foreign bodies in the upper gastrointestinal tract in children.
METHODSA retrospective analysis was performed for the clinical data of 217 children who were diagnosed with foreign bodies in the upper gastrointestinal tract complicated by gastrointestinal injury by gastroscopy from January 2011 to December 2016, including clinical features, gastroscopic findings, complications, and prognosis.
RESULTSAmong the 217 children, 114 (52.5%) were aged 1-3 years. The most common foreign body was coin (99/217, 45.6%), followed by hard/sharp-edged food (45/217, 20.7%) and metal (35/217, 16.1%). The most common gastrointestinal mucosal injury was ulceration (43.8%), followed by erosion (33.2%). Compared with other foreign bodies, button cells were significantly more likely to cause esophageal perforation (P<0.01). The esophagus was the most commonly injured organ (207/217, 95.4%). Of all the 217 children, 24 (11.1%) experienced infection. The children with perforation caused by foreign bodies had a significantly higher incidence rate of infection than those with ulceration caused by foreign bodies (P=0.003). Of all the 217 children, 204 (94.0%) underwent successful endoscopic removal of foreign bodies. Among these children, 98 were hospitalized due to severe mucosal injury and were given anti-infective therapy, antacids, and supportive care including enteral nutrition through a nasogastric tube and/or parenteral nutrition. Of all the children, 10 left the hospital and were lost to follow-up, and all the other children were improved and discharged.
CONCLUSIONSMost cases of foreign bodies in the upper gastrointestinal tract occur at 1-3 years of age. Coin, hard/sharp-edged food, and metal are the most common foreign bodies. Button cells are more likely to cause esophageal perforation. The incidence rate of secondary infection increases with the increasing severity of gastrointestinal mucosal injury. Children undergoing endoscopic removal of foreign bodies and enteral nutrition through a nasogastric tube tend to have a good prognosis.
Female ; Food ; adverse effects ; Foreign Bodies ; diagnosis ; etiology ; therapy ; Humans ; Infant ; Male ; Metals ; adverse effects ; Prognosis ; Retrospective Studies ; Upper Gastrointestinal Tract ; injuries