1.Identification of andrographolide hydroxypropyl-?-cyciodextrin inclusion compound and study on its thermodynamic stability
Ke REN ; Zhi-Rong ZHANG ; Jing-Hong JU ; Yang LIU ; Tao GONG ;
Chinese Traditional and Herbal Drugs 1994;0(04):-
Objective To prepare and identify the andrographolide-hydroxypropyl-?-cyclodextrin(an- drographolide-HP-?-CD)inclusion compound.The tool ratio between andrographolide and HP-?-CD and the thermodynamic constants in inclusion were studied simultaneously.Methods The andrographolide- HP-?-CD inclusion compound was prepared with lyophilization technique.Meanwhile,the inclusion com- pound was identified by differential scanning calorimetry(DSC)methods,infrared spectrometry(IR),and X-ray diffraction(XRD),respectively.The tool ratio between host and guest moleculars and the thermo- dynamic constants during the inclusion process were also researched by phase solubility method.Results An 1:1 molar ratio inclusion complex of andrographolide with HP-?-CD could be formed at 25,35,and 45 C.The phase diagram was A_L type and the procedure of inclusion was a heat release process.Conclusion The solubility of andrographolide-HP-?-CD inclusion compound can be increased obviously by the above- mentioned preparing techniques.
2.Analysis of risk factors of skin lesion of population exposed to arsenic via drinking water in Inner Mongolia
Zhi-wei, GUO ; Ya-juan, XIA ; Ke-gong, WU ; Yan-hong, LI
Chinese Journal of Endemiology 2011;30(6):638-641
Objective To study the risk factors of skin lesion (keratosis and abnormal skin pigmentation) of population exposed to arsenic via drinking water in Inner Mongolia.Methods A cluster sampling method was used to select 902 cases from Linhe district,Hanghou and Wuyuan county in Inner Mongolia and physical examination was done.They were interviewed for information by questionnaire.The sample of fingernails and drinking water were collected.Water arsenic (As) was analyzed by inductively coupled plasma mass spectrometry (ICPMS); fingernail As and Se content were analyzed by instrumental neutron activation analysis(INAA).Data were analyzed by univariate and multivariate non-conditional Logistic regression.Results Single factor analysis showed that risk factors of keratosis were age,pesticide,arsenic in nails,smoking,years of smoking,drinking of alcohol,arsenic content in drinking water,fluorosis and duration of drinking arsenic-containing water,while occupation,nail selenium content and vitamin were protective factors.There were 10 risk factors for pigment abnormalities,which were age,pesticide,arsenic in nails,smoking,years of smoking,numbers of cigarette smoked daily,drinking of alcohol,fluorosis,the arsenic content in drinking water and duration of drinking arseniccontaining water,while sex,occupation and nails with selenium were protective factors.The multivariate factor analysis showed that the risk factors of keratosis were age,pesticide and arsenic content in drinking water(OR =1.387,1.583,1.321,all P < 0.05),while occupation and vitamin were protective factors(OR =0.307,0.260,all P < 0.05).The risk factors of abnormal skin pigmentation were age,pesticide,arsenic in nails,fluorosis and arsenic content in drinking water(OR =1.724,2.636,2.741,3.699,1.863,all P < 0.05),while sex was protective factor(OR =0.255,P < 0.01 ).Conclusions Many factors have influence on endemic arsenism and a composite measure should be implemented to prevent it such as excluding arsenic from drinking water,health education,and a reasonably intake of nutrients.
3.Research progress of anti-acute marrow leukemia drugs by targeting FLT3
Hui-ya JIA ; Bo YANG ; Xiao-meng ZHANG ; Jian-hong GONG ; Ya WU ; Yan-le ZHI
Acta Pharmaceutica Sinica 2023;57(3):605-615
Acute myeloid leukemia (AML) is a genetic heterogeneous disease in which primordial and juvenile myeloid cells proliferate or accumulate abnormally in bone marrow, peripheral blood and other tissues, resulting in damage to normal hematopoietic function. Studies have shown that about 30% of AML patients have FMS-like tyrosine kinase 3 (FLT3), FLT3 abnormal regulation is closely related to the occurrence and development of AML. At present, FLT3 has become an important target for developing small molecular targeted drugs. Currently, a variety of FLT3 inhibitors and FLT3 degraders have been developed targeting FLT3, and some compounds have exhibited good anti-AML activity. This article summarizes and sorts out the current mainstream drugs for AML therapeutic targeting FLT3, in order to provide a reference for the development and design of AML drugs.
4.Influence of arsenic exposure on menstruation
Wei-hong, YANG ; Zhi-wei, GUO ; Xiao-hong, HAN ; Ya-juan, XIA ; Ke-gong, WU ; Yan-hong, LI
Chinese Journal of Endemiology 2013;(1):27-29
Objective To study the influence of arsenic exposure on menstruation.Methods A cluster sampling method was applied to select the subjects of women aged 10 to 65 from Linhe,Hangjinhouqi and Wuyuan counties in Inner Mongolia in 2004.Drinking water samples were collected to detect arsenic levels,and menstrual related situation was surveyed.The subjects were divided into four groups according to drinking water arsenic concentration:control(≤0.01 mg/L),low(> 0.01-0.10 mg/L),moderate(> 0.10-0.20 mg/L) and high(> 0.20mag/L).Results A total of 602 women were surveyed.There were 83 subjects exposed to arsenic before menarche and their menarche age was (14.37 ± 1.54) years old.There were 90 people exposed to arsenic before menopause and the menopause age was (48.13-0.41) years old.The age of menarche and menopause were positively related to the years of arsenic exposure,and correlation coefficients were 0.268 and 0.278 (all P < 0.05).Compared to control group(14.0%,16/112),menstrual abnormality rate decreased in low(12.1%,21/173) and high dose groups(10.2%,19/186),while increased in the moderate dose group(18.2%,16/88),but the differences were not statistically significant(x2 =3.664,P > 0.05).Conclusions Long-term arsenic exposure delays the menarche and menopause age,suggesting that arsenic has certain endocrine disruption or estrogen-like effects.
5.Establishment of human lung squamous carcinoma cell line CHLH-1
Hong-Cheng LIU ; Sheng-Dong HUANG ; De-Jun GONG ; Xiao-Hong LIU ; Yang YUAN ; Zhi-Yun XU ;
Academic Journal of Second Military Medical University 1999;0(12):-
Objective:To establish a human lung squamous carcinoma cell line and to study its biological characteristics. Methods:Lung squamous carcinoma specimens were freshly resected during operation;the tissues were incubated in vitro and the cell line was named CHLH-1.The biological characteristics of the cells were studied by light microscopy,electron microsco- py,chromosome analysis and transplantation experiment.Results:Cells from the specimens of the primary tumor,the CHLC- 1 cell line and the cells from transplanted tumor possessed the characteristics of malignant squamous epithelium under light and electron microscope.The cell growth curve,doubling time and mitotic index were also observed in vitro.Nuclear chromosome analysis revealed that the tumor was a subtriploid with a mode of 60-68 per cell.Tumor nodes were observed under the skin of nude mice by heterogenic transplantation.Conclusion:The characteristics of the established cell line suggest that it is a newly established human squamous carcinoma cell line.
6.Relationship between tyrosine phosphorylation and protein expression of insulin receptor and insulin resistance in gestational diabetes mellitus.
Yong-Li, CHU ; Yu-Dian, GONG ; Zhi-Hui, SU ; Hong-Na, YU ; Qing, CUI ; Hai-Yang, JIANG ; Hong-Mei, QU
Journal of Huazhong University of Science and Technology (Medical Sciences) 2014;34(3):393-7
The relationship between tyrosine phosphorylation (TP) and protein expression of insulin receptor (InsR) and insulin resistance (IR) in patients with gestational diabetes mellitus (GDM) was investigated. The InsR expression and TP in skeleton muscle tissue were determined by Western blotting and immunoprecipitation in women with GDM (GDM group, n=22), normal pregnant women (normal pregnancy group, n=22) and normal non-pregnant women (normal non-pregnant group, n=13). Fasting plasma glucose (FPG) and fasting insulin (FINS) were measured by oxidase assay and immunoradioassay. The results showed that the levels of FPG (5.61±0.78 mmol/L), FINS (15.42±5.13 mU/L) and Homeostasis model assessment-IR (HOMA-IR) (1.21±0.52) in GDM group were significantly higher than those in normal pregnancy group (4.43±0.46 mmol/L, 10.56±3.07 mU/L and 0.80±0.31 respectively) (P<0.01). The levels of FINS and HOMA-IR in normal pregnancy group were significantly higher than those in normal non-pregnant group (7.56±2.31 mU/L and 0.47±0.26 respectively) (P<0.01). There was no significant difference in the InsR expression level among the three groups (P>0.05). TP of InsR with insulin stimulation was significantly decreased in GDM group (0.20±0.05) as compared with normal pregnancy group (0.26±0.06) (P<0.01). TP of InsR with insulin stimulation in normal pregnancy group was lower than that in normal non-pregnant group (0.31±0.06) (P<0.01). TP of InsR with insulin stimulation was negatively related with HOMA-IR in GDM group (r=-0.525, P<0.01). There was no correlation between the protein expression of InsR and HOMA-IR in GDM group (r=-0.236, P>0.05). It was suggested that there is no significant correlation between the protein expression of InsR in skeletal muscle and IR in GDM, but changes in TP of InsR are associated with IR in GDM.
7.Effect of different pacing sites on ventricular synchrony evaluated by gated blood pool SPECT
Xue, GONG ; Yan-gang, SU ; Wen-zhi, PAN ; Shu-guang, CHEN ; Hong-cheng, SHI ; Xian-hong, SHU ; Jun-bo, GE
Chinese Journal of Nuclear Medicine 2010;30(5):307-311
Objective To compare the effect of right ventricular outflow tract (RVOT) and right ventricular apex (RVA) pacing on ventricular systolic synchrony using gated blood pool SPECT (GBPS).Methods A total of 50 patients implanted with pacemaker due to high degree or complete atria-ventricular block were enrolled in the study. Twenty-three patients were RVOT paced ( Group A, n = 23) and 27 were RVA paced (Group B, n=27). Twenty-four patients with malignancy, normal echocardiographic findings and no history of cardiac diseases were scheduled for pre-chemotherapy evaluation of cardiac structure and function and were enrolled as control group ( Group C, n = 24). All patients underwent GBPS imaging and the values of phase angle (PS), mean phase of each wall, standard deviation (SD) of mean phase of each wall, lateral-septal motion delay of left ventricle ( LV Sep-Lat Delay), septal-right ventricular (RV) delay of LV ( LV Sep-RV Delay) and LV-RV Delay were acquired. The parameters of ventricular systolic synchrony among the three groups were compared using one-way ANOVA. Results The mean phase of LV lateral wall in Groups A and B were significantly higher than that in Group C: Group A (120.50 ±40.58) ms; Group B (103.23±28.34) ms; Group C (84.63 ±22.38) ms (F=7.72, P <0.05). There was no significant difference between Groups A and B ( t = 1.30, P > 0.05 ). The mean phase of RV in Group A was significantly larger than those in Groups B and C: Group A ( 137.05 ± 39.27) ms, Group B ( 100.85 ± 23.79) ms,Group C (59. 13 ±30.52) ms (F=35.55, P<0.05). PS, SD and LV Sep-Lat Delay in Groups A and B were significantly higher than those in Group C: (85.73 ± 12.00)°vs (89.85 ± 15.61 )°vs (58.95 ±9.87)°, (27.68±10.66) ms vs (26.15 ±13.02) ms vs (15.63 ±8.35) ms, (25.06±34.23) ms vs (2. 62 ± 60. 31 ) ms vs ( - 23.66 ± 31.39) ms, F = 41.54,8.55,6.81, all P < 0.01 ), however, there was no significant difference between Groups A and B ( t = 0. 68, 0.68, 1.30, all P > 0.05 ). LV Sep-RV Delay and LV-RV Delay were significantly different among the three groups ( LV Sep-RV Delay: Group A (57.60 ±56.77) ms, Group B (6.36 ±61.88) ms, Group C ( -41.89 ±35.78) ms; LV-RV Delay:Group A (47.36 ±42.59) ms, Group B ( 3.08 ± 38.81 ) ms Group C ( - 26.50 ± 20.99 ) ms, F = 20. 32,25.38, both P < 0.01 ). Conclusion Both RVA and RVOT pacing increase the segmental phases detected by GBPS, causing inter- and intra- ventricular asynchrony compared with patients without pacemakers.
8.Discussion on transmission mechanism of wild rodent plague to human in the northwestern area of Yunnan province
Mu, GUO ; Hong-ying, ZHANG ; Mei, HONG ; Zhi-zhong, SONG ; Zheng-da, GONG ; Ying-huan, LONG ; Xing-qi, DONG
Chinese Journal of Endemiology 2010;29(2):208-211
Objective To explore the relationship between wild rodent plague and human in wild rodent plague foci of the northwestern area in Yunnan to probe the possible transmission mechanism of wild rodent plague to human. Methods Data of component ratio of rodents and fleas was collected in different areas from 1985 - 1995. Activities and habits of residents regarding the way they keep cats and dogs and parasitic fleas and free fleas indoor were investigated, the dog serum was collected for detecting F1 antibody. Results Eothenomys miletus were main rodents in farmland and shrub, accounting for 48.00% (4753/9902) and 54.50% (4282/7857), Apodemus chevrieri were main rodents in garden, being 50.47% (1332/2639). The component ratio of Neopsylla specialis specialis was 13.31%(229/1720), 12.31%(1678/13 739) and 10.87%(957/8802) respectively in garden, farmland and shrub, higher than in indoor. The component ratio of Frantcpsylla spodix was 39.88% (686/1720), the highest in garden. Thirty-two per cent (32/100) of residents kept cats,in which 63% (20/32) with cat fleas, 68% (68/100) of villages kept dogs, in which 76%(52/68) with fleas. Eighteen parasitic fleas were caught from 43 dogs with a flea index of 0.119 and a rate for fleas of 11.63%, 7 pulex were collected from 17 indoor. Forty-three blood serum samples were obtained from dogs, among which 3 were positive blood serum. Conclusions Residents touch affected animals or media in different situations. The possibility of transmission for wild rodent plague to human exists in loci in a chain of wild rodent plague → fleas or predation → homebred animal plague (cats or dogs) →touching or respiratory → human.
9.Inhibition of MCP-1 mRNA expression by propylene glycol mannate sulfate in hyperlipidemic rat aorta.
Yan GAO ; Wen-gong YU ; Feng HAN ; Xin-zhi LU ; Qian-hong GONG ; Hua-shi GUAN
Acta Pharmaceutica Sinica 2003;38(8):582-585
AIMTo study the effects of prophylene glycol mannate sulfate (PGMS) on monocyte chemoattractant protein-1 (MCP-1) mRNA expression in hyperlipidemic rat aorta and to clarify the molecular mechanism of PGMS for the prevention of atherosclerosis.
METHODSPGMS (37.8 and 75.6 mg.kg-1.d-1, ig) or PGMS (37.8 and 75.6 mg.kg-1.d-1, ig) combined with diethyldithiocarbamate (DDC, an inhibitor of SOD, 200 mg.kg-1 every three days, i.p.) were given to hyperlipidemic rats for three weeks. The MDA content and SOD activity were determined after 12 h of starvation, and MCP-1 mRNA expression in aorta was detected by reverse transcription-polymerase chain reaction (RT-PCR).
RESULTSThere was significant decrease (29.46% or 58.40)% of MCP-1 mRNA expression in aortic after the therapy. The SOD activity increased markedly and the MDA content decreased at the same time. After treatment with DDC, the SOD activity was inhibited and the MDA content increased, but with no significant effect on MCP-1 mRNA expression.
CONCLUSIONPGMS inhibited MCP-1 mRNA expression with no relation to its effect on decreasing MDA content.
Animals ; Aorta, Thoracic ; drug effects ; metabolism ; Chemokine CCL2 ; biosynthesis ; genetics ; Gene Expression ; drug effects ; Hyperlipidemias ; blood ; pathology ; Hypolipidemic Agents ; pharmacology ; Male ; Malondialdehyde ; blood ; metabolism ; Propylene Glycols ; pharmacology ; RNA, Messenger ; biosynthesis ; drug effects ; Random Allocation ; Rats ; Rats, Wistar ; Superoxide Dismutase ; blood ; metabolism
10.Influence of obesity on pharmacokinetics and pharmacodynamics of isoflurane.
Zhi-yi GONG ; Tie-hu YE ; Yi-dan HUANG ; Nuo-er SANG ; He DUAN ; Hong-zhi REN
Acta Academiae Medicinae Sinicae 2003;25(5):615-618
OBJECTIVETo observe the effect of obesity on pharmacokinetics and pharmacodynamics of isoflurane.
METHODSTwenty-six patients undergoing cholecystectomy were divided into obese group (Group A, BMI > or = 27, n = 13) and normal body weight group (Group N, BMI < or = 24, n = 13) according to body mass index (BMI). All patients were given to the same isoflurane anesthesia. Inspired and end-expired concentrations of isoflurane were monitored and uptake fraction of isoflurane were calculated.
RESULTSIsoflurane concentrations of vaporizer in Group A [(1.8 +/- 0.3)%] were evidently higher than those in Group N [(1.5 +/- 0.1)%] at all observed points (P < 0.05 or P < 0.01). Uptake fraction of isoflurane in Group A were higher than those in Group N at observed points (P < 0.05, P < 0.01 or P < 0.001), but there were no differences in the time when isoflurane concentration was lowered to 50% and awake time between the two groups after discontinuing inhaling isoflurane.
CONCLUSIONSObese patients demand higher inspired concentration and uptake of isoflurane than those in normal weight patients but discharge of isoflurane was influenced by obesity within the observed period of (66 +/- 33) min.
Adult ; Aged ; Anesthesia, Inhalation ; Anesthetics, Inhalation ; administration & dosage ; pharmacokinetics ; Body Mass Index ; Cholecystectomy, Laparoscopic ; Dose-Response Relationship, Drug ; Female ; Humans ; Isoflurane ; administration & dosage ; pharmacokinetics ; Male ; Middle Aged ; Obesity ; complications ; metabolism