[Interpretation of Chinese guideline for the clinical management of patients with ruptured intracranial aneurysms (2024)].

Aneurysmal subarachnoid hemorrhage (aSAH) is a life-threatening neurological emergency with high mortality, and even patients receiving optimal medical care may develop long-term disability, which seriously affects their quality of life and increases the heavy medical burden on society and families. To provide comprehensive clinical management advice, the Society of Neurosurgery of the Chinese Medical Association, the Society of the Chinese Stroke Association of the National Medical Center for Neurological Diseases, and the National Clinical Research Center for Neurological Diseases jointly formulate "Chinese Guidelines for the Clinical Management of Patients With Ruptured Intracranial Aneurysms in 2024". The evidence sources are divided into the Chinese population and other populations, using a modular format to provide recommendations, summaries of relevant opinions, and future research directions on epidemiology, clinical imaging diagnosis, prognosis evaluation, treatment strategies and choices, anesthesia management, perioperative care, and recommendations for the management of aSAH in special populations. It provides practical clinical guidance and recommendations for doctors and related professionals.

[Preliminary experience of transcatheter pulmonary valve replacement using domestic balloon-expandable valve].

Objectives: To evaluate the feasibility and preliminary clinical results of transcatheter pulmonary valve replacement (TPVR) with the domestically-produced balloon-expandable Prizvalve system. Methods: This is a prospective single-center observational study. Patients with postoperative right ventricular outflow tract (RVOT) dysfunction, who were admitted to West China Hospital of Sichuan University from September 2021 to March 2023 and deemed anatomically suitable for TPVR with balloon-expandable valve, were included. Clinical, imaging, procedural and follow-up data were analyzed. The immediate procedural results were evaluated by clinical implant success rate, which is defined as successful valve implantation with echocardiography-assessed pulmonary regurgitation

[Prediction on the cardio-cerebrovascular death and probability of premature death caused by common risk factors in China in 2030].

Objective: Predictive models were used to evaluate the impact of common risk factors on the number of cardio-cerebrovascular deaths and the probability of premature death. Methods: Using the data for China estimated by the Global Burden of Disease study 2015 (GBD 2015), we calculated the population attribution fraction (PAF) of risk factors. The proportional change model was used to estimate the number of unattributable deaths by 2030, and to predict the number of deaths, mortality, standardized mortality and probability of premature death by 2030. Results: According to the natural change trend of risk factors from 1990 to 2015, the number of deaths and mortality would reach 6.12 million and 428.53/100 000 by 2030, with an increase of 59.92% and 52.87%. By 2030, the probability of premature death from cardio-cerebrovascular diseases among Chinese aged 30-70 years old would continue to decline, from 11.43% to 11.28% for men, and from 5.79% to 4.43% for women. If the goals of all included risk factors were reached by 2030, 2 289 200 cardio-cerebrovascular deaths would be avoided. If only the exposure to a single risk factor was achieved by 2030, blood pressure, total cholesterol, and fine particulate matter exposure were the three most important factors affecting cardio-cerebrovascular deaths, which would reduce 1 332 800, 609 100 and 306 800 deaths, respectively. Among the involved risk factors, the control of blood pressure would mostly decrease the number of deaths due to ischemic heart disease and hemorrhagic stroke, about 677 300 and 391 100 deaths, accordingly. Conclusion: The control of risk factors is of great significance in reducing deaths and probability of premature death due to cardio-cerebrovascular diseases. If the control targets of all risk factors could be achieved by 2030, the burden of cardio-cerebrovascular diseases would be reduced greatly.

[Clinicopathological and molecular genetic characteristics of nodular fasciitis in unusual sites].

Objective: To study the clinicopathological, immunophenotypic and molecular genetic characteristics of nodular fasciitis (NF) in unusual sites. Methods: A total of 50 cases of NF diagnosed between January 2015 and January 2021 were reviewed in the Department of Pathology, Henan Provincial People's Hospital, and the clinical and pathologic data were analyzed. Among them, 14 cases from unusual sites were included in this study. Immunohistochemical (IHC) staining was used to detect the expression of related proteins, and fluorescence in situ hybridization (FISH) was used to detect the breakage of the USP6 gene. Results: There were seven males and seven females in the 14 NF respectively. The lesions were located in the extremities, perineum, breast, wrist joints, the gap between lumbar vertebra 4/5, and in eight cases there was involvement of unusual tissues (six cases in skeletal muscle, one case in nerve root, and one case was intravascular). The tumor boundary was unclear with infiltrating growth. Spindle-shaped myofibroblasts were arranged in bundles or chaotically, with mild pleomorphic, small nucleoli and various mitotic figures. The tumor stroma showed collagenization to myxoid degeneration with erythrocyte extravasation and infiltration of inflammatory cells. IHC staining showed that the spindle cells expressed SMA focally or partially, and p16 diffusely and strongly. FISH showed that 12 of 14 cases had USP6 gene breakage, and two of them occurred in the intrathoracic skeletal muscle with the red signal amplification of USP6 gene. Conclusions: NF in unusual sites shows similar clinicopathological and genetic characteristics to classic NF, but the tumor mostly has infiltrating borders, non-specific and strong expression of p16, and USP6 red signal amplification. The pathological diagnosis of NF in rare sites should be highly vigilant.

[Prognostic analysis of gastrointestinal stromal tumors complicated with gastrointestinal bleeding].

OBJECTIVE: To study the relationship between clinicopathological characteristics, prognosis and gastrointestinal bleeding in primary gastrointestinal stromal tumors (GIST). METHODS: The clinicopathological and follow-up data of 200 patients with gastrointestinal stromal tumors treated in our hospital from April 2008 to December 2014 were retrospectively reviewed. The correlation of gastrointestinal bleeding with gastrointestinal stromal tumor clinicopathological characteristics and prognosis were analyzed. RESULTS: The 200 GIST patients were divided into two groups according to the bleeding in the digestive tract, including 57 gastrointestinal bleeding patients and 143 non-bleeding patients. The mean tumor diameter was 6.5 cm (range 1.8-22 cm) in the bleeding group and 2.5 cm (range 0.4-18 cm) in the non-bleeding group (P<0.05). Of the 57 bleeding patients, 31 located in the stomach, 25 in the small intestine, and one had colorectal bleeding. Fifty patients had mitotic index (MI) ≤ 5/50 HPF, other 6 patients ranged between 5 and 10/50 HPF and one patient had MI >10/50 HPF. Six GIST patients were complicated with tumor rapture. But in the non-bleeding group, 125 patients had gastric GIST, 8 in the small intestine, one colorectum, and 9 had esophageal or other GIST. 141 patients had MI ≤5/50 HPF, 1 patients ranged between 5 and 10/50 HPF and one patient had MI >10/50 HPF. Only 1 GIST patients was complicated with tumor rapture. The gastrointestinal bleeding was closely associated with tumor size, mitotic index, tumor location, risk classifications, tumor rapture and tumor recurrence (P<0.05 for all). The 3-year and 5-year survival rates of the 200 patients were 96.5% and 86.8%, respectively. 16 patients developed recurrence or metastasis, and 11 died of GIST. The 5-year survival rate of patients with gastrointestinal bleeding was 76.2%, significantly lower than that of patients without gastrointestinal bleeding (91.6%, P<0.05). CONCLUSIONS: GIST patients complicated with gastrointestinal bleeding have poor prognosis, and attention should be paid to stratifying patients for therapy.

[Forecasting the burden of disease from diabetes under the scenarios of specific risk factors control in China in 2030].

Objective: To forecast mortality, age-standardized mortality, and probability of premature mortality from diabetes, and to simulate the impact of controlling risk factors by 2030 in China. Methods: We simulated the burden of disease from diabetes in six scenarios according to the development goals of risk factors control by the WHO and Chinese government. Based on the theory of comparative risk assessment and the estimates of the burden of disease for China from the Global Burden of Disease Study 2015, we used the proportional change model to project the number of deaths, age-standardized mortality, and probability of premature mortality from diabetes under different scenarios of risk factors control in 2030. Results: If the trends in exposures to risk factors from 1990 to 2015 continued. Mortality, age-standardized mortality, and probability of premature mortality from diabetes would increase to 32.57/100 000, 17.32/100 000, and 0.84% by 2030, respectively. During that time, mortality, age-standardized mortality and probability of premature mortality for males would all be higher than for females. If the goals of controlling risk factors were all achieved, the number of deaths from diabetes in 2030 would decrease by 62.10% compared to the predicted numbers based on the historical trends in exposure to risk factors, and the probability of premature mortality would drop to 0.29%. If only the exposure to a single risk factor were achieved by 2030, high fasting plasma glucose control would have the greatest impact on diabetes, resulting in a 56.00% reduction in deaths compared to the predicted numbers based on the historical trends, followed by high BMI (4.92%), smoking (0.65%), and low physical activity (0.53%). Conclusions: Risk factors control plays an important role in reducing the number of deaths, age-standardized mortality rate, and probability of premature mortality from diabetes. We suggest taking comprehensive measures to control relevant risk factors for certain populations and regions, to achieve the goal of reducing the burden of disease from diabetes as expected.

[Prediction of disease burden caused by malignant cancer in the context of risk factor control in China, 2030].

Objective: To predict the number of deaths, standardized mortality and probability of premature mortality caused by malignant cancer in the context of risk factor control at different levels in China in 2030, and assess the possibility of achieving the target of reducing the probability of premature mortality of malignant cancer. Methods: According to the risk factor control standard for malignant cancer used both at home and abroad, the results of China from Global Burden of Disease Study 2015 were used to calculate the population attributable fraction of the risk factors. Based on the comparative risk assessment theory, the deaths of malignant cancer were classified as attributable deaths and un-attributable deaths. Proportional change model was used to predict risk factor exposure and un-attributable deaths of malignant cancer in the future, then the number of deaths, standardized mortality rate and probability of premature mortality of malignant cancer in 2030 was estimated. Data analyses were performed by using software R 3.6.1. Results: If the risk factor exposure level during 1990-2015 remains, the number of deaths, standardized mortality rate, and probability of premature mortality of malignant cancer would increase to 3.62 million, 153.96/100 000 and 8.92% by 2030, respectively. If the risk factor exposure control level meets the requirement, the probability of premature mortality from cancer in people aged 30-70 years would drop to 7.57% by 2030. Conclusions: The control of risk factor exposure will play an important role in reducing deaths, standardized mortality rate and probability of premature mortality of malignant cancer. But more efforts are needed to achieve the goals of Health China Action.

[Prediction on the burden of disease of chronic obstructive pulmonary disease and simulation of the effectiveness of controlling risk factors in China by 2030].

Objective: To forecast the burden of chronic obstructive pulmonary disease (COPD) in China by 2030 and evaluate the effectiveness of controlling risk factors based on the predictive model. Methods: Based on the relationship between the death of COPD and exposure to risk factors and the theory of comparative risk assessment, we used the estimates of the Global Burden of Disease Study 2015 (GBD2015) for China, targets for controlling risk factors, and proportion change model to project the number of deaths, standardized mortality rate, and probability of premature mortality from chronic respiratory diseases by 2030 in different scenarios and to evaluate the impact of controlling the included risk factors to the disease burden of COPD in 2030. Results: If the trends in exposure to risk factors from 1990 to 2015 continued, the number of deaths and the mortality for COPD would be 1.06 million and 73.85 per 100 000 population in China by 2030, respectively, with an increase of 15.81% and 10.69% compared to those in 2015. Compared to 2015, the age-standardized mortality rate would decrease by 38.88%, and the premature mortality would reduce by 52.73% by 2030. If the smoking rate and fine particulate matter (PM2.5) concentration separately achieve their control targets by 2030, there would be 0.34 and 0.27 million deaths that could be avoided compared to the predicted numbers based on the natural trends in exposure to risk factors and the probability of premature death would reduce to 0.59% and 0.52%, respectively. If the control targets of all included risk factors were achieved by 2030, a total of 0.53 million deaths would be averted, and the probability of premature death would decrease to 0.44%. Conclusions: If the exposures to risk factors continued as showed from 1990 to 2015, the number of deaths and mortality for COPD would increase by 2030 compared to 2015, and the standardized mortality and the probability of premature death would decrease significantly, which would achieve the targets of preventing and controlling COPD. If the exposure to the included risk factors all achieved the targets by 2030, the burden of COPD would be reduced, suggesting that the control of tobacco use and air pollution should be enhanced to prevent and control COPD.

[Review on the progress regarding the intervention mapping protocol].

Along with the significant development on both theory and practice of health promotion programs, the application of behavioral and social science theories has also been advanced in the fields of design and evaluation regarding the intervention-related studies. Intervention mapping is a new planning protocol, efficiently used to develop, implement, and evaluate health promotion related intervention programs. In this article, we are briefly introducing the basic concepts, implementation steps, specific requirements, as well as reviewing the current progress in methodologies, application that are related to intervention mapping, so as to provide reference for health intervention research studies, domestically.

Influences of LncRNA SNHG20 on proliferation and apoptosis of glioma cells through regulating the PTEN/PI3K/AKT signaling pathway.

OBJECTIVE:   To investigate the influences of long non-coding ribonucleic acid (lncRNA) small nucleolar RNA host gene 20 (SNHG20) on proliferation and apoptosis of glioma cells, and further explore the mechanism of SNHG20 in the incidence and development of glioma. PATIENTS AND METHODS: A total of 80 cases of glioma specimens and 80 cases of para-carcinoma specimens were collected, and the expression level of SNHG20 was detected via reverse transcription-polymerase chain reaction (RT-PCR). The human glioma U118 and U251 cell lines with the stable knockout of SNHG20 were constructed using the small-interfering RNA (siRNA). The influence of SNHG20 on proliferation of human glioma cells was detected via cell counting kit-8 (CCK-8), and the protein expression levels of apoptosis-related genes, B-cell lymphoma-2 (Bcl-2) and Bcl-2 associated X protein (Bax), were also detected. The apoptosis level of glioma cells was detected in blank control group and SNHG20 siRNA group using the terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) technique. At the same time, the expression levels of proteins related to the phosphatase and tensin homolog deleted on chromosome ten/phosphatidylinositol 3-hydroxy kinase/protein kinase B (PTEN/PI3K/AKT) signaling pathway were detected via Western blotting. RESULTS: The expression level of SNHG20 messenger RNA (mRNA) in glioma tissues was significantly higher than that in para-carcinoma tissues (p<0.05). After the inhibition of siRNA on SNHG20, the proliferation of U118 and U251 cells was significantly inhibited, and the expression of Bax was significantly up-regulated, while that of Bcl-2 was down-regulated. The TUNEL results showed that the number of apoptotic cells in SNHG20 siRNA group was about 12 times that in control group (p<0.05). After SNHG20 knockout, the protein expressions in the PTEN/PI3K/AKT signaling pathway were inhibited (p<0.05). CONCLUSIONS: Inhibiting the SNHG20 expression in glioma cells can increase the apoptosis of glioma cells, and the mechanism may be related to the SNHG20-mediated PTEN/PI3K/AKT signaling pathway.

Clinical significance of epithelial-mesenchymal transition-related molecules in lung adenocarcinoma.

Background: Epithelial-mesenchymal transition (emt) refers to the biologic process in which epithelial cells are transformed into interstitial phenotypes by specific pathways. This transition plays an important biologic role in the process by which epithelium-derived malignant tumour cells acquire the ability to migrate and invade. We explored the relationship between emt-associated molecules and patient-related clinical factors to determine whether any clinical characteristics could be used as biomarkers for emt-related protein alterations in lung cancer-especially lung adenocarcinoma. Methods: Tumour specimens were collected from 80 patients with lung adenocarcinoma who underwent surgery or lung biopsy, with 4 patients being evaluated a 2nd time after re-biopsy. Expression of emt-related proteins, including E-cadherin and vimentin, was evaluated by immunohistochemistry. We analyzed the relationship between clinicopathologic characteristics and expression level of the emt markers. Results: Positive expression of E-cadherin was observed in 63 patients (79%), and vimentin, in 46 patients (57.5%). No significant relationships between E-cadherin or vimentin expression and smoking history, sex, age, driving gene mutations, or cell differentiation were identified. A significant correlation was observed between vimentin expression and pathologic stage. Of the 4 patients who were evaluated a 2nd time after re-biopsy, 3 showed the same emt-related protein expression status as in the first analysis. In the remaining patient, E-cadherin had changed completely. Conclusions: Clinicopathologic factors in cancer patients did not help to diagnose emt status in lung adenocarcinoma; however, TNM stage might be associated with vimentin expression.

Increase in G protein-coupled receptor autoantibodies with decline of cardiac function in hypercholesterolemic rats.

OBJECTIVE: This study aimed to explore the effects of diet-induced hypercholesterolemia (HC) on the production of G protein-coupled receptor autoantibodies and to elucidate the potential mechanisms involved. MATERIALS AND METHODS: Male Wistar rats were fed a normal or high-cholesterol diet for 8 weeks. Cardiac function, autoantibodies against G protein-coupled receptors, the beat frequency of neonatal cardiomyocytes, the CD4+/CD8+ T-lymphocyte ratio and lymph leukocyte counts in the spleen were determined. RESULTS: Diet-induced hypercholesterolemia significantly increased the levels of autoantibodies against α1- and ß1-adrenergic receptors and the angiotensin II type 1 receptor in sera, as well as the CD4+/CD8+ T-lymphocyte ratio and lymph leukocyte count in the spleen, and decreased cardiac function. There were strong negative correlations between the levels of autoantibodies and cardiac injury. CONCLUSIONS: The present study demonstrates, for the first time, that G protein-coupled receptor autoantibodies exist in the sera of hypercholesterolemic rats and that the levels of these autoantibodies are related to cardiac function, which implies that these cardiac receptor autoantibodies may play a role in cardiac dysfunction in hypercholesterolemic rats.

Efficacy of pressure topical anaesthesia in punctal occlusion by diathermy.

AIMS: To prospectively compare the efficacy and safety of pressure topical anaesthesia in punctal occlusion by using cautery in the treatment of dry eye syndrome (DES) with that of conventional treatment by using needle injection of anaesthetic agents. METHODS: In a randomised controlled trial, 18 consecutive adult patients with DES requiring punctal occlusion were recruited over a 10 month period. Consenting patients were randomised into two groups. Group A patients received pressure topical anaesthesia in the right eye followed by injection anaesthesia in the left eye. Group B was vice versa. Punctal occlusion using cautery was performed in each eye after a specified time following the application of anaesthesia. The main outcome measures were the pain experienced during application of anaesthesia and that during punctal occlusion. RESULTS: 36 eyes of 18 patients were randomised to receive injection anaesthesia in one eye and pressure topical anaesthesia in the other. Nine patients (nine females) were in group A and nine patients (seven females, two males) in group B. The mean age of group A patients was 45.3 (SD 13.5) years, and that of group B patients was 55.6 (12.6) years. The two groups were comparable in terms of mean age (p=0.117) and mean pain score for pressure topical anaesthesia application (p=0.612), injection anaesthesia application (p=0.454), diathermy in pressure anaesthetised eyes (p=0.113), and diathermy in injection anaesthetised eyes (p=0.289). Paired t test was used to compare the mean pain score for pressure topical anaesthesia application (16.8 (24.8)) with those for injection anaesthesia application (56.7 (30.0)). 18 eyes of 18 patients were compared with the fellow eye of the same 18 patients. The mean pain score for injection anaesthesia was greater than for pressure topical anaesthesia application (p<0.0001) (statistical power=0.87). No statistically significant difference was found in the mean pain score for diathermy for eyes that received pressure topical anaesthesia (20.5 (27.5)) compared with eyes that received injection anaesthesia (23.1 (26.3)) (p=0.760) (statistical power=0.96). All 18 patients preferred pressure topical anaesthesia to injection anaesthesia. CONCLUSION: Injection anaesthesia for punctal occlusion is more painful than pressure topical anaesthesia application. However, the pain experienced during diathermy application for punctal occlusion is similar between pressure anaesthetised eyes and injection anaesthetised eyes. Pressure topical anaesthesia is a less painful (in terms of anaesthesia application) but equally effective alternative to conventional injection anaesthesia when used for punctal occlusion.

Autogenous palmaris longus tendon as frontalis suspension material for ptosis correction in children.

PURPOSE: To determine the safety and efficacy of autogenous palmaris longus tendon as a sling material in frontalis suspension surgery for ptosis correction in children. METHODS: In a prospective study, the authors evaluated 15 frontalis sling suspension surgeries using palmaris longus tendon in 14 consecutive children with congenital ptosis. The method of harvesting the palmaris longus tendon is described in detail. RESULTS: The mean age of the patients was 4.7 years (range, 2 to 7 years). At a mean follow-up of 30 months (range, 20 to 40 months), all ptotic eyelids were successfully corrected with good final lid position. No recurrence of ptosis was encountered. In one eye, knot slippage of the sling was related to upper eyelid trauma, which was readily repaired. Otherwise, no exposure keratitis, wound infection, eyelid contour abnormality, or ptosis overcorrection occurred. There were no complications associated with the palmaris longus tendon donor site. CONCLUSION: Frontalis suspension with autogenous palmaris longus tendon appears to be an effective treatment for congenital ptosis with poor levator function in children. Its use as an alternative material to fascia lata for sling surgery in children can be considered.

Efficacy of lignocaine 2% gel in chalazion surgery.

BACKGROUND/AIMS: To determine whether topical 2% lignocaine (lidocaine) gel is an effective anaesthetic agent for chalazion surgery. METHODS: In a randomised controlled clinical trial, 57 subjects aged 12 years or over requiring incision and curettage for chalazion were recruited over an 8 month period. Patients were randomised into two groups. One group received 1.5 ml of lignocaine 2% injection and the other 1.5 ml of lignocaine 2% gel topically. Standard incision and curettage was then performed. The primary outcome of interest was the total pain experienced during the entire procedure including anaesthetic administration as well as incision and curettage. The pain from the local anaesthetic administration and during incision and curettage was assessed independently using a visual analogue scale (0-100). The sum of these two scores would be the total pain score out of 200. "Fear of injection" score (0-100) was also assessed. RESULTS: There was a statistically significant difference in the mean total pain scores between the injection and the gel groups (95.6 v 57.0) (p <0.001) (alpha = 0.05) (1 - beta = 0.9394). There was a statistically significant difference in the mean scores on "pain of anaesthetic administration" (47.0 v 5.5) (p <0.000). There was no statistically significant differences in the mean scores on "fear of injection" (43.9 v 47.7) (p = 0.668) and "pain during incision and curettage" (48.28 v 51.4) (p=0.679). CONCLUSIONS: Lignocaine 2% gel is effective in chalazion surgery especially in lowering the pain caused by anaesthetic administration.

Epidemiology of acute primary angle-closure glaucoma in the Hong Kong Chinese population: prospective study.

OBJECTIVES: To determine the incidence of acute primary angle-closure glaucoma in the Hong Kong Chinese population, and to identify risk factors for this condition. DESIGN: Prospective study. SETTING: University teaching hospital, Hong Kong. PARTICIPANTS: Patients with acute primary angle-closure glaucoma presenting between 1 March 1998 and 29 February 2000. MAIN OUTCOME MEASURES: Demographic data, presenting symptoms and signs, temporal details of the presentation, and precipitating factors. The crude regional incidence was calculated according to the Hong Kong population census of 1991 and the age-specific incidence was calculated. RESULTS: Seventy-two cases (72 eyes of 72 patients) of acute primary angle-closure glaucoma were recruited. The crude incidence was 10.4 per 100,000 per year in the population aged 30 years and older. Patients at higher risk of attacks were those aged 70 years or older (age-specific incidence, 58.7 per 100,000 per year) and females, who had a relative risk of 3.8 compared with males (95% confidence interval, 1.7-8.4). Only four (5.6%) patients had a positive family history of acute primary angle-closure glaucoma. Seventeen (23.6%) patients were noted to have an upper respiratory tract infection before the attack, and 25 (34.7%) patients had taken antitussive agents. There was a statistically significant inverse correlation between the monthly attack rate and the monthly rate of influenza (Spearman's rank correlation coefficient = -0.388; P=0.031). CONCLUSION: There is a high incidence of acute primary angle-closure glaucoma among Chinese residents of Hong Kong, with elderly females at highest risk. A significant proportion of patients reported upper respiratory tract infection or the use of antitussive medication prior to attacks.

[Studies on antitumor drugs: the synthesis of N',N"-dispirotripiperaziniums].

In order to search for new antitumor drugs, sixteen N',N"-dispirotripiperazine derivatives were synthesized from N',N"-dispirotripiperazinium dichloride dihydrochloride by substitution, acylation and Mannich reaction. Six compounds were selected for preliminary pharmacological test. The result showed that five compounds possess inhibitory action against carcinoma S37 in rats. The inhibitory activity of compounds VI and X was 55.0% and 41.9% respectively.

[Synthesis and anti-tumor activities of 1,4-bis[3-(amino-dithiocarboxy)propionyl] piperazine derivatives].

AIM: To synthesize piperazine derivatives and screen anti-tumor compounds with higher activity and lower toxicity. METHODS: Selecting 1,4-bis(3-bromopropionyl)piperazine as leading compound, a series of 1,4-bis[3-(amino-dithiocarboxy)propionyl] piperazine derivatives (4a-j) were synthesized through the use of aminodithiocarboxylate. All the synthetic compounds (4a-j) were tested for their anti-tumor activity against eight kinds of tumor cells. RESULTS: Compounds (4a-j) are new compounds, among them, compounds 4c, 4d and 4e showed anti-tumor activity against HL-60. The inhibition of compounds 4c, 4d and 4e against HL-60 are 44%, 90% and 70% respectively, at the concentration of 10 mumol.L-1. However, the inhibition of the other kinds of anti-tumor cells are not distinctive. CONCLUSION: These results suggest that this may be one of the effective routes to improve the anti-tumor activity and reduce the toxicity of 1,4-bis(3-bromopropionyl)piperazine.