3.Studies on the chemical constituents of Cirsium japonicum DC.
Fei ZHI ; Ling-yi KONG ; Si-xun PENG
Acta Pharmaceutica Sinica 2003;38(6):442-447
AIMIn order to look for new bioactive compounds, investigation on the chemical constituents, especially on the typical polyacetylenes from the rhizomes of Cirsium japonicum DC. was carried out.
METHODSChromatographic techniques including silica column chromatography and preparative silica thin-layer chromatography were used to separate and purify the constituents. Their structures were elucidated by physicochemical properties and spectral analyses including UV, IR, 1HNMR, 13CNMR, HMQC, HMBC and HREIMS.
RESULTSTwelve compounds were isolated from the rhizomes of Cirsium japonicum DC., and their structures were identified as cis-8, 9-epoxy-heptadeca-1-ene-11, 13-diyne-10-ol (1), ciryneol A (2), 8,9,10-triacetoxyheptadeca-1-ene-11,13-diyne (3), ciryneone F (4), cireneol G (5), ciryneol H (6), ciryneol C (7), p-coumaric acid (8), syringin (9), linarin (10), beta-sitosterol (11) and daucosterol (12).
CONCLUSIONCompounds 4, 5 and 6 are new compounds, compound 3 is a new natural product and compound 8 was isolated from this plant for the first time.
Cirsium ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Molecular Conformation ; Molecular Structure ; Plants, Medicinal ; chemistry ; Rhizome ; chemistry
4.Studies on structure modification of (+)-praeruptorin A.
Xian-li WU ; Ling-yi KONG ; Zhi-da MIN
Acta Pharmaceutica Sinica 2002;37(7):527-534
AIMIn order to look for new active compounds, the structure of (+)-praeruptorin A is modified.
METHODS(+)-Praeruptorin A was isolated from the root of Peucedanum praeruptorum, basic hydrolysis of (+)-praeruptorin A and acyled reactions of hydrolysis product of (+)-praeruptorin A were carried out.
RESULTSEighteen compounds were semi-synthesized from (+)-praeruptorin A.
CONCLUSIONFourteen compounds (5-18) among them are new compounds. Preliminary bioactivity assay indicated that the new compounds show calcium antagonist activity, but they are not as strong as (+)-praeruptorin A.
Animals ; Aorta, Thoracic ; drug effects ; Apiaceae ; chemistry ; Calcium Channel Blockers ; chemical synthesis ; isolation & purification ; pharmacology ; Coumarins ; chemical synthesis ; isolation & purification ; pharmacology ; Drugs, Chinese Herbal ; chemical synthesis ; isolation & purification ; pharmacology ; Molecular Structure ; Muscle Contraction ; drug effects ; Muscle, Smooth, Vascular ; drug effects ; Plants, Medicinal ; chemistry ; Rats
5.Economic burden of coronary heart disease and stroke attributable to hypertension in China.
Yi ZHAI ; Jian-Ping HU ; Ling-Zhi KONG ; Wen-Hua ZHAO ; Chun-Ming CHEN
Chinese Journal of Epidemiology 2006;27(9):744-747
OBJECTIVE1) To estimate annual direct medical costs of coronary heart disease (CHD) and stroke attributable to hypertension among Chinese adults aged 35-74 years in China, 2) to analyze the correlation between the hypertension awareness and hypertension treatment rate.
METHODS2003 National Health Services Survey (n = 93 018) was used to derive direct medical costs including costs for outpatient visits, physician services, inpatient stays, rehabilitation services, nurses fees, and medications. The medical costs of CHD and stroke attributable to hypertension were estimated by multiplying population attributable risk proportion by corresponding disease costs. Using 2002 National Nutrition and Health Survey (n = 148 804), the prevalence of hypertension awareness and hypertension treatment rate in 132 survey sites were calculated. Correlation was used to analyze the correlation between the two variables.
RESULTSThe direct medical costs of hypertension, CHD and stroke were 20.2, 15.7 and 24.3 billion Yuan, respectively. The medical costs attributable to hypertension were estimated at 19.1 billion Yuan (RMB), accounting for 47.7% of the total medical costs of the two chronic diseases. The prevalence of hypertension awareness is highly correlated with hypertension treatment rate (r = 0.9777, P < 0.0001).
CONCLUSIONThe economic burden of CHD and stroke attributable to hypertension is very high, reaching about 50% of the total medical costs of the two diseases. The prevalence of hypertension awareness could be used as an important indicator to evaluate the effectiveness of hypertension prevention and control at community level.
China ; Coronary Disease ; economics ; etiology ; Cost of Illness ; Data Collection ; Health Care Costs ; statistics & numerical data ; Humans ; Hypertension ; complications ; Stroke ; economics ; etiology
6.The role of dietary factors in chronic disease control in China.
Chun-Ming CHEN ; Wen-Hua ZHAO ; Zheng-Xiong YANG ; Yi ZHAI ; Yang-Feng WU ; Ling-Zhi KONG
Chinese Journal of Epidemiology 2006;27(9):739-743
OBJECTIVETo examine the association of dietary patterns with chronic diseases and their indicators.
METHODSUsing the data from 2002 National Nutrition and Health Survey, we divided the subjects into clusters according to their dietary patterns classified by different percentage of energy intake from cereal foods, carbohydrate and fat, respectively. The analysis of variance was used to identify the difference in chronic disease prevalence across clusters of subjects while controlling for age, gender and geographic regions. Logistic regression analysis was applied to calculate the odd ratios (OR) for association of chronic disease and each dietary pattern, after adjusted for age, gender, region, energy intake, leisure time.
RESULTSThe higher percentage of energy intake from cereals was significantly associated with lower body mass index (BMI), lower total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C). While it was significantly associated with lower risk for overweight/obesity, hypertension, high total cholesterol, high triglyceride (TG) and high LDL-C, but the prevalence of underweight was significantly higher in the cluster of subjects with cereal energy share more than 75%. The higher percentage of energy intake from fat was significantly associated with higher BMI, higher total cholesterol and higher LDL-C, which accordingly, was significantly associated with higher risk for overweight/obesity, hypertension, high total cholesterol, triglyceride and high LDL-C.
CONCLUSIONOur study confirmed the important role of dietary pattern in chronic disease control; in particular, appropriate percentage of energy intake from fat and cereals/carbohydrates are beneficial to control and prevention of chronic diseases.
China ; epidemiology ; Chronic Disease ; epidemiology ; prevention & control ; Diet ; Dietary Carbohydrates ; Dietary Fats ; Humans ; Nutrition Surveys ; Odds Ratio
7.Effect of nutritional status during infancy and childhood on the risk of overweight and obesity in adulthood.
Wen-hua ZHAO ; Zheng-xiong YANG ; Yi ZHAI ; Ling-zhi KONG ; Chun-ming CHEN
Chinese Journal of Epidemiology 2006;27(8):647-650
OBJECTIVETo examine the association between fetal nutritional status and overweight and obesity in their adulthood and to provide evidence for formulation of the strategy on preventing low birth weight.
METHODSUsing data from 2002 Nationwide Nutrition and Health Survey to set up a case-control method in order to compare body mass index(BMI), prevalence of overweight and obesity as well as to calculate odds ratio of overweight and obesity of case group compared with control group. Three case groups were selected from those who were born in 1959, 1960,1961 respectively, and the controls were those who were born in 1964.
RESULTSThe health consequence of being famines on adulthood was evident in women. Means of BMI in women were significantly higher in three case groups than that in control group(P<0.01). After adjustment on geographic regions, the prevalence of overweight in women was significantly higher in three case groups than that in control group(P< 0.01). The prevalence rates of obesity were significantly higher in 1959, 1960 groups than 1964 group(P< 0.05). The odds ratios of overweight of women in three case groups were 28.9% (95% CI:1.063-1.565), 37.2% (95% CI:1. 136-1.658) and 35.2% (95% CI: 1. 103-1.657) respectively, all higher than that in the control group. The odds ratios of obesity of women born in 1959, 1960 groups were 46.5% (95% CI: 1.088-1.972) and 39.6% (95% CI: 1.039- 1.876) respectively, higher than that in the 1964 group. However, such differences were not found in men.
CONCLUSIONHigher risks of overweight and obesity in women were caused by malnutrition during their fetal lives. A strategy on preventing low birth weight should be formulated by the government to prevent the chronic disease in adulthood.
Adult ; Case-Control Studies ; China ; epidemiology ; Female ; Humans ; Infant Nutritional Physiological Phenomena ; Infant, Low Birth Weight ; Infant, Newborn ; Male ; Nutritional Status ; Obesity ; epidemiology ; Overweight ; epidemiology ; Prevalence ; Risk
8.Screening of antidepressant fractions of banxia houpu decoction.
Ye-min WANG ; Ling-dong KONG ; Zhi-qi HUANG
China Journal of Chinese Materia Medica 2002;27(12):932-936
OBJECTIVETo screen the antidepressant fractions of Banxia Houpu Decoction.
METHODBehavioral despair models in mice were used to evaluate antidepressant activities and the levels of monoamine neurotransmitters in regions of animal brains were determined with spectrophotofluoremetry method.
RESULTThe extract of Banxia Houpu Decoction (AE) and its four fractions were able to elicit time-dependent reducing of duration of immobility in the tail suspension test and the forced swimming test in mice. Among these test samples, AE, petrol fraction (AE-1) and water soluble fraction (AE-4) were more potent, but there was no significant difference between them. AE significantly increased 5-HT level in mice striatum and NE level in mice cortex, respectively, and did not affect any monoamine neurotransmitters in other regions of animal brain. AE-1 elevated 5-HT level in the striatum and the NE and DA level in the cortex, chloroform fraction (AE-2) only significantly increased DA level in cortex.
CONCLUSIONBanxia Houpu Decoction has antidepressant effect. The active parts are in AE-1 and AE-4. The antidepressant action of Banxia Houpu Decoction is probably by mediated in part through many monoamine neurotransmitter systems.
Animals ; Antidepressive Agents ; pharmacology ; Behavior, Animal ; drug effects ; Brain ; metabolism ; Chloroform ; chemistry ; Dopamine ; metabolism ; Drugs, Chinese Herbal ; pharmacology ; Ethanol ; chemistry ; Magnolia ; chemistry ; Male ; Mice ; Mice, Inbred ICR ; Pinellia ; chemistry ; Plants, Medicinal ; chemistry ; Serotonin ; metabolism
9.Semi-synthesis of derivatives with C-3' and C-4' trans-configuration from (+)-praeruptorin A.
Ling-yi KONG ; Xian-li WU ; Zhi-da MIN
Acta Pharmaceutica Sinica 2003;38(5):358-363
AIMIn order to compare the calcium antagonist activity between the derivatives of (+)-praeruptorin A with C-3' and C-4' cis-configuration and trans-configuration, and to look for new active compounds, some derivatives with C-3', C-4' trans-configuration of (+)-praeruptorin A were semi-synthsized.
METHODS(+)-Praeruptorin A was isolated from the root of Peucedanum praeruptorum. Basic hydrolysis of (+)-praeruptorin A was carried out. From the alkaline hydrolysis product (2), eight new products (5-12) with C-3', C-4' trans-configuration were semi-synthsized whose C-3' was linked to angeloyloxy and C-4' was linked to various acyloxy, using respective acids as acylating agents, DCC as a dehydrant, DMAP as catalyst. From the alkaline hydrolysis product (4), five new products (13-17) with C-3', C-4' trans-configuration were obtained whose C-3', C-4' is linked to various same acyloxys, using respective acids as acylating agents, DCC as dehydrant, DMAP as catalyst. Also from the alkaline hydrolysis product (4), using respective acyl chlorides as acylating agents, anhydrous dichloromethane containing minor pyridine as a solvent, the improved Schotten-Baumann reactions were carried out, two new products (18, 20) with C-3', C-4' trans-configuration were obtained whose only C-3' linked to acyloxy and two other new products (19, 21) with C-3', C-4' trans-configuration were obtained whose C-3' and C-4' linked two acyloxys. The structures of all the products were elucidated by spectral analyses including IR, 1HNMR and EIMS. The calcium antagonist activity of all of the products were tested by inhibition of the systole of rat artery ring.
RESULTSSeventeen compounds with C-3', C-4' trans-configuration were semi-synthesized from (+)-praeruptorin A for the first time and their calcium antagonist activity were evaluated.
CONCLUSIONAll of the derivatives were new compounds. Bioactivity assay indicated that some new compounds with C-3', C-4' trans-configuration showed obvious calcium antagonist activity, but they are not as strong as (+)-praeruptorin A. The activity of some products was shown to be similar to that of the derivatives with C-3', C-4' cis-configuration for the first time.
Animals ; Aorta, Thoracic ; drug effects ; Calcium Channel Blockers ; chemical synthesis ; pharmacology ; Coumarins ; chemical synthesis ; chemistry ; pharmacology ; Drugs, Chinese Herbal ; chemical synthesis ; chemistry ; pharmacology ; Molecular Structure ; Muscle Contraction ; drug effects ; Muscle, Smooth, Vascular ; drug effects ; Rats ; Stereoisomerism
10.Clinical significance of STMN1 expression in cervical cancer and effect of inhibition of its expression on viability and apoptosis of cervical cancer Si-Ha cells
Zhi-Hong CHAI ; Ling-Xiao YING ; Yi-Hong PAN ; Xian-Li CAI ; Wei-Min KONG
Chinese Journal of Pathophysiology 2018;34(6):1119-1123,1128
AIM:To investigate the clinical significance of stathmin 1 (STMN1) expression in cervical cancer and the influence of its expression on the viability and apoptosis of cervical cancer cells. METHODS:Western blot was used to detect the protein expression of STMN1 in cervical cancer tissues, and the relationship between the expression and clinical characteristics of cervical cancer was analyzed. STMN1-siRNA was transfected into cervical squamous-cell carcino-ma SiHa cells. The protein levels of STMN1, STAT3, p-STAT3 and survivin were determined by Western blot after trans-fection for 48 h. The cell viability was measured by MTT assay. The apoptosis was analyzed by flow cytometry. DCFH-DA probe was used to detect the level of reactive oxygen species (ROS). RESULTS:The protein expression of STMN1 in cer-vical cancer tissues was significantly higher than that in paracancerous tissues (P<0.01). The STMN1 protein expression level was not correlated with age and histological types of cervical cancer patients, but was related to clinical stage, histo-logical differentiation and lymph node metastasis ( P<0.01). Transfection with STMN1-siRNA significantly reduced the expression of STMN1 in SiHa cells. Compared with control group, the cell viability in STMN1-siRNA group was significant-ly decreased, the apoptotic rate and ROS content were increased, and the protein levels of p-STAT3 and survivin were down-regulated (P<0.01). However, no significant difference of the STAT3 protein level was observed between STMN1- siRNA group and control group. CONCLUSION:STMN1 is highly expressed in cervical cancer, and its expression is re-lated to clinical stage, histological differentiation and lymph node metastasis. Inhibition of STMN1 expression reduces the viability and promotes apoptosis of cancer cells by down-regulating STAT3 signaling pathway.