1.Investigation on enzymatic degradation stability of peptide drugs LXT101 and its structural modified analogs in pancreatin system
Huixian SUN ; Lei GUO ; Jianwei XIE ; Keliang LIU
Journal of International Pharmaceutical Research 2017;44(6):600-603
Objective To find the efficient modification groups of anti-proteinase hydrolyzation in polypeptide by investigat-ing and comparing the relation between the functional groups and their ability to inhibit proteinase hydrolyzation. Methods Reverse phase-high performance liquid chromatography(RP-HPLC)method was developed to investigate in vitro metabolisms of new drug LXT101 and its structural modified analogs LZN series and LMP series in pancreatin system. All the separations of peptide drugs and their digested fragments were monitored at 225 nm. Results The good linear range was 4.0-400 μg/ml(r>0.9990)for new drug LXT101 and its structural modified analogs,i.e.,LZN series and LMP series. The recoveries of all peptide drugs ranged from 95.0%to 98.7%in pancreatin systems. The relative standard derivations(RSD)of intra-day and inter-day were less than 1.5%and 2.5%,re-spectively. The revealed order of digested half-life of the peptide drugs was LZN series>LMP series>LXT101. Conclusion The study of different sites and different functional groups on the lifetime indicates that the half-lives of peptides are prolonged by introducing the functional groups in the suitable sites of peptide,which feature as proteinase inhibitors,such as carbamoyl(Cbm),acetyl(Ac),para-amino-phenylalanine(Aph)or para-uramido-phenylalanine(Uph),which work as either proton donor or acceptor. Our results can pro-vide some useful and valuable information on structural design of peptide drug with long lifetime and high activity.
2.Effects of dexmedetomidine on hemodynamics in hypertensive patients undergoing thyroid surgery with local anesthesia
Yanhong SUN ; Xiaoqian LI ; Haimei LIU ; Huixian BIAN
Journal of Chinese Physician 2013;15(7):873-877
Objective To explore the effect of dexmedetomidine on hemodynamics in hypertensive patients undergoing thyroid surgery with local anesthesia.Methods Sixty patients with preoperatively diagnosed class Ⅰ to Ⅱ hypertension undergoing selective thyroidectomy were randomly divided into D (dexmedetomidine) and M (midazolam) groups (30 patients in each group).Doses of dexmedetomidine 0.5 μg/kg were finished in 20 minutes injection in patients of D group before the start of the surgery,then sequentially maintained at the rate of 0.1 ~ 0.5 μg/ (kg · h) with decreasing speed of 0.1 μg/(kg · h) when systolic pressure kept down to 110 mmHg or heart rare down to 60 bpm or Ramsay score of 3 points.The patients in M group were injected with midazolam 0.04 mg/kg 20 minutes before the start of surgery,then maintained at the rate of 0.02 ~ 0.05 mg/(kg · h),decreasing speed of 0.1 mg/(kg · h) to keep Ramsay score of 3 points if necessary.Two groups of patients with Ramsay score of 3 points but a high blood pressure (higher than 30% of basic level) or heart rate (more than 100 bpm) were treated with drugs during operation.Record the systolic pressure,diastolic pressure,heart rate and Ramsay score at the time of before medication (T0),the injection of local anesthetics (T1),the start of surgery (T2),pain compliments required additional local anesthetics (T3),dealing with gland (T4) and the end of surgery,VAS in 8 h after operation and adverse reaction were recorded.Results In D group,the dosages of urapidil and esmolol [(10 ±5)mg and (0 ±0)mg] were significantly less than those in patients of M group [(60 ± 10) mg and (80 ±5) mg,t =14.82,t =19.78,P < 0.05].Blood pressure and heart rate were all significantly decreased at the time of T1,T2 and T5 when comparing with T0(P <0.05 orP <0.01),and only heart rate was significantly decreased at the time of T3 and T4 (P < 0.05).While in M group,blood pressure and heart rate were higher than basic levels at the time of T3 and T4 (P < 0.05).Besides,lower blood pressure and heart rate were less than those in M group at all observed time expect T0 (P < 0.05).Conclusions Good sedation effects can be produced by both dexmedetomidine and midazolam in hypertensive patients undergoing thyroid surgery with local anesthesia,but dexmedetomidine was determined more suitable in sedation and anti-hypertension in patients with light to moderate hypertension for better hemodynamic stability effect with local anesthesia.
3.Effect of topical nonsteroidal anti-inflammatory drugs and corticosteroids on ultraviolet ray-induced erythema
Huixian LIU ; Nan SUN ; Jianmei GUO ; Yan WU
Chinese Journal of Dermatology 2013;46(6):415-418
Objective To observe the suppressing effect of topical nonsteroidal anti-inflammatory drugs (NSAIDs) and corticosteroids on ultraviolet ray (UV)-induced erythema.Methods A solar simulator and an UV phototherapy device were used as light sources,respectively.Erythema reaction was induced on the back skin of 30 healthy volunteers by 1,2 and 3 minimal erythema doses (MED) of irradiation.Five preparations including butyl flufenamate 2.5% ointment,butyl flufenamate 5% ointment,the base of butyl flufenamate ointment,halometasone ointment,and diclofenac 1% ointment,were applied to the irradiation sites respectively half an hour before or immediately after the irradiation.One irradiation site remained untreated and served as the control.The degree of erythema was evaluated by a chromameter at 4,24,and 48 hours after the irradiation.Intragroup and intergroup comparisons were done by t test and analysis of variance,respectively.Results When applied half an hour before solar-simulated irradiation,both 2.5% and 5% butyl flufenamate ointment totally suppressed the erythema reaction induced by 1-3 MED of UV irradiation,with no significant increase in erythema index at all the three time points after irradiation (all P > 0.05); diclofenac 1% only inhibited the erythema induced by 1 MED of UV irradiation at 4 and 48 hours,with no difference observed in erythema index between the baseline and these time points after irradiation; however,halometasone significantly aggravated the erythema reaction (P < 0.05).Neither NSAIDs nor corticosteroids applied immediately after solar-simulated irradiation showed statistical effect on the degree of UV-induced erythema.When applied immediately after irradiation using the phototherapy device,butyl flufenamate 2.5% ointment,butyl flufenamate 5% ointment and halometasone ointment all induced a significant reduction in erythema reaction at 4 hours after 1 MED of irradiation (all P < 0.05),and diclofenac caused a statistical decrease in erythema reaction at all the time points after 1-3 MED of irradiation (all P <0.05).Conclusions Topical use of butyl flufenamate before UV irradiation can effectively inhibit erythema reaction induced by 1-3 MED of irradiation.When applied immediately after irradiation,diclofenac shows the strongest erythema-suppressive effect,followed sequentially by butyl flufenamate and halometasone.
4.Relationship Between Tongue Manifestations and Immune Function in Chronic Hepatitis B with HBsAg, HBeAg and HBcAb Positive
Xiaoyan ZHOU ; Hanlin ZHONG ; Huixian WEN ; Futai YANG ; Hongjian LIU
Journal of Guangzhou University of Traditional Chinese Medicine 2001;0(01):-
[ Objective ] To investigate the relationship between tongue manifestations and immune function in chronic hepatitis B with HBsAg, HBeAg and HBcAb positive. [Methods] Among the cases of HBsAg, HBeAg and HBcAb positive from the out - patient department and health screening survey, 200 chronic hepatitis patients and 100 asymptomatic HBV carriers with glumatic - pyruvic transaminase at normal level were included. Thirty healthy volunteers served as control. Relationship of tongue manifestations with phytohemagglutinin (PHA) skin test and the serum levels of immunoglobulin (Ig) G, IgA and IgM was analyzed. [Results] With the development of chronic hepatitis, the immune function became disordered and tongue manifestations abnormal. Reddish tongue with or without yellowish greasy fur or yellowish fur showed the hyperactivity of immune function; whitish swollen tongue with or without whitish greasy fur indicated the hypoactivity of immune function; dull purplish tongue was the sign of disordered immune function. The shape and color of tongue was superior to tongue fur in showing the condition of immune function ( P
5.Establishment of Guinea Pig Models of Allergic Rhinitis with Kidney-yang De ficiency
Huixian XU ; Yan RUAN ; Shizhen WANG ; Ye LIU
Traditional Chinese Drug Research & Clinical Pharmacology 2000;0(06):-
Objective To find a new method for the establishment of allergic rhinitis(AR) models with kidney-yang deficiency.Methods Fourty-five Hartely guinea pigs were randomized into 4 groups: hydroxycarbamide+ ovalbumin(OV); predisone+ OV;hydroxycarbamide+OV+Shenqi decoction;normal control).The general behavior and the body weight of guinea pigs were observed before and after treatment.After 3 weeks,the reaction of guinea pigs to histamine nasal drops was observed and then all animals were sacrificed to examine the pathological changes of nasal septum mucosa.Result The new model induced by hydroxycarbamide and OV was proved to be set up successfully: the manifestations of kidneyyang deficiency in the new model were more representative than those induced by predisone and OV,and the time for modeling was shorter.Conclusion Using hydr oxycarbamide and OV to set up kedney-yang deficiency AR models is an new feasible method.The result of this study will provide evidence for the further research of kidney-yang deficiency AR.
6.Morphology changes following treatment of the patients with Class Ⅱ high-angle malocclusions
Feng WANG ; Yinzhong DUAN ; Lan LIU ; Huixian BI
Journal of Practical Stomatology 1995;0(04):-
Objective: To specify what we should notice during the treatment of Class Ⅱ high-angle malocclusions.Methods: 14 patients(8 male and 6 female) with Class Ⅱ high-angle malocclusions were investigated with Tweed-Merrifield morphology analysis.Results: (1)FMIA and Z-angle were increased after treatment(P
7.Morphological changes of rat pancreatic tissue induced by ligation of thoracic duct
Haiyan HE ; Baozhi WANG ; Huixian CUI ; Li ZHANG ; Shutang SHI ; Guisheng LIU
Acta Anatomica Sinica 2009;40(4):656-659
Objective To observe the morphological changes of pancreatic tissue of thoracic duct ligated rats in fine and ultrastructural levels, and to determine whether lymph block animal model can affect pancreatic islet amyloid polypeptide(PIAP)deposit in rat pancreas. Methods At the 6th month after the operation, some pancreatic tissue sections of 16-month-old experimental rats were embedded in paraffin wax and stained with HE and Congo red;immunohistochemical staining was performed on some frozen sections, which were then observed with light microscope;transmission electron microscope (TEM) specimen preparation and observation were performed on other samples. Results HE and Congo red stained sections showed that the pancreatic glandular lobule space was widened, with significant connective tissue hyperplasia, and fat accumulation when the islet was stained indistinctly or vermeil and tissue space was broadened. The sections with immunohistochemical staining displayed the pancreatic islet as well as the tissues around it were stained into dark brown being positive with PIAP antigen. TEM observation showed the pancreatic glandular interlobule space was widened, while blood vessels and enlarged lymphatic vessels were visible;within widened pancreatic islet interstitial space, a great quantity of lipid droplets and some collagen fibril structures could be seen.Conclusion The ligation of thoracic duct can contribute to pancreatic lymph draining block, lymphagiectasis, connective tissue space and interstitial space widening, fat accumulation, and PIAP deposit in rat pancreas. These structural changes may affect the function of pancreatic islets.
8.Effects of preconditioning treadmill exercise on the dynamic changes of brain glutamate level after cerebral infarction in rats
Jie JIA ; Yongshang HU ; Yi WU ; Gang LIU ; Huixian YU ; Chunmei XIA ; Zhijuan CAO
Chinese Journal of Physical Medicine and Rehabilitation 2008;30(6):361-365
Objective To study the effects of preconditioning treadmill exercise on excitatory amino vacid changes in rats after the cerebral infarction and the protective effects against cerebral isehemia brain injury. Methods Thirty Sprague-Dawley rats were used in this study. Twenty-five rats were subject to an operation to establish the animal model of middle cerebral artery occlusion and divided into a isehemia group, an 1-week ex- ercise group (trained in the 4th week) , a 2-week exercise group (trained in the 3rd and 4th weeks) and a 4- week exercise group (trained for 4 weeks) , while the remaining 5 rats were subject to sham operation, and served as the controls. After 4 weeks of experiment, all the the rats were fixed on stereotactie apparatus for the brain microdialysis of the striatum. Then the focal middle cerebral artery ischemia and reperfusion were made with thread oeclussion in rats and microdialysis technique was used to collect extraeellular fluid in each period of pre-ischemia, ischemia (40, 80 and 120 min), and reperfusion (40, 80, 120, 160, 200 and 240 min) to detect the changes of the excitatory amino acid. At the same time the infarction volume was also measured at 24 hours after ischemia-reperfusion of the brain. Results The difference between any two groups was significant with regard to the volume of cerebral infarction (P < 0.05). Two weeks and four weeks of the preconditioning treadmill exercise couled significantly reduce concentration of Glu excessively released due to the ischemia (P < 0.01). Conclusion At least two weeks of preconditioning treadmill exercise can inhibit the excessive release of the important excitatory amino acid neurotransmitter glutamate, to some extent, in the process of the subse- quent ischemic brain injury and during reperfusion, which might be one of the protective mechanisms of move- ment against the early isehemie brain injury.
9.Performance of transfection with a complex plasmid encoding green fluorescent protein tagged cathepsin D in researches on chronic photodamaged fibroblasts
Yue ZHENG ; Haiyan CHEN ; Qingfang XU ; Congxiu YE ; Huixian LIU ; Jinling YI ; Wei LAI
Chinese Journal of Dermatology 2015;(12):876-879
Objective To evaluate the performance of transfection with a complex plasmid encoding green fluorescent protein tagged CatD (GFP-CatD)in researches on chronic photodamaged fibroblasts. Methods Human dermal fibroblasts (HSFs)were irradiated with ultraviolet A (UVA)at 25 J/cm2 once a day for 21 consecutive days to establish a chronic photodamaged cell model. A plasmid encoding GFP-CatD was constructed and transfected into some chronic photodamaged fibroblasts (experimental group). The photodamaged HSFs receiving no treatment served as the blank control group, and those transfected with the negative plasmid encoding GFP only as the negative control group. After additional culture, fluorescence microscopy and Western-blot analysis were performed to observe and measure the expression of GFP-CatD in HSFs respectively, flow cytometry and methyl thiazolyl tetrazolium (MTT)assay to evaluate the apoptosis and proliferation of chronic photodamaged fibroblasts respectively. Results Fluorescence microscopy showed the expression of GFP-CatD in cytoplasm of chronic photodamaged fibroblasts at 96 hours after transfection with the GFP-CatD-encoding plasmid. Western-blot analysis revealed that the expression of CatD in the experimental group was 1.28 times that in the blank control group. There were no significant differences in the apoptosis rate(4.29% ± 1.30%vs. 3.03% ± 1.70% , P > 0.05)or proliferative rate (45.20% ± 4.70% vs. 43.60 ± 3.90% , P > 0.05)between the experimental group and blank control group. Conclusion CatD could be traced in chronic photodamaged fibroblasts with no changes in biological activity or cell cycle after transfection with the GFP-CatD-encoding complex plasmid.
10.Analysis of clinical diagnosis of 3315 cases with pulmonary tuberculosis suspicious symptoms transferred by non-tuberculosis control institutions
Zhiqiang LIANG ; Tao SONG ; Yumei LIU ; Xiaoyan LI ; Guobiao LIU ; Xiaoying WU ; Huixian ZHOU ; Yanbin ZHANG ; Shouyong TAN ; Zhihui LIU
The Journal of Practical Medicine 2017;33(15):2505-2508
Objective To study the level of clinical diagnosis of pulmonary tuberculosis and implementa-tion of tuberculosis prevention and control policy. Methods Frequencies and percentages of pulmonary tuberculosis, other lung diseases and health among 3315 cases with pulmonary tuberculosis suspicious symptoms ,transferred by non-tuberculosis control institutions during 2010-2015,were calculated and analyzed. Results Among the 3315 suspected cases of pulmonary tuberculosis ,cases of pulmonary tuberculosis ,tuberculosis ,other lung diseases and healthy group were 2068,598 and 649 based on final diagnosis and their percentages were 62.38%,18.04% and 19.58% respectively. As to groups of elder than fifteen years ,the proportion of patients with pulmonary tubercu-losis accounts for 72.62%,61.00%and 48.58% of the total of young group(15~44 years old ),middle age group (45 ~ 64 years old)and elderly group(≥ 65 years old )respectively. Conclusions Compared with pulmonary tuberculosis suspicious symptomscases from tuberculosis control institution during the same period ,the proportion of tuberculosis patients from transferred groups is roughly the same.It indicate high levels of tuberculosis diagnosis and implementation to tuberculosis control policy.