1.Pharmacokinetics of recombinant hirudin in rats in vivo
Yurong HUANG ; Quansheng LI ; Changxiao LIU
Chinese Traditional and Herbal Drugs 1994;0(09):-
brain and fatty. The accumulation excretion ratios within 96 h were 70.16% in urine and only 1.35% in feces after iv administration in rats, while within 24 h was 3.46% in bile. Conclusion The results of pharmacokinetics of novel r-hirudin in rats given by iv determined by RA are different from those determined by TCA-RA, but the trends indicated by the two methods are the same; urine excretion is the major excretion pathway.
2.Experiment study on antiallergic effects of norstemizole
Changxiao LIU ; Ruizhi WANG ; Ning LIU ; Jing LI ; Xiaoxiang CHENG ;
Chinese Journal of Clinical Pharmacology and Therapeutics 2000;0(01):-
AIM: To study the antiallerergic effects of norastemizole. METHODS: Antiallergic effects of norastemizole were study using rats and guinea pigs. RESULTS: Norastemizole(10 -9 -10 -8 mol?L -1 ) caused inhibition effect on the hisitamine induced contraction of isolated guinea pig ileum. Its IC 50 was 4.42 ?10 -9 mol?L -1 Norastemizole at oral doses of 0.1 , 0.5 , 1 mg?kg -1 , norastemizole caused a significant inhibition on the histamin phosphate induced shock in guinea pigs (P
3.Anti-human Cytomegalovirus Activity of Hot Water Extract from Sasa senanensis Rehder
Rie YAMADA ; Kazuhiko AKUZAWA ; Changxiao BI ; Zhuan LI ; Hidetaka SADANARI ; Keiko MATSUBARA ; Tsugiya MURAYAMA
Japanese Journal of Complementary and Alternative Medicine 2009;6(1):17-25
Objective: Anti-Human cytomegalovirus (HCMV) activity of Kumazasa (Sasa senanensis Rehder) extract were investigated in the human embryonic lung (HEL) fibroblast cell.
Method: This study examined the effect of hot water extract from Sasa senanensis Rehder on HCMV replication, viral-specific major immediate early (IE) gene expression, and protein synthesis.
Results: Treatment of HCMV-infected HEL cells with that Sasa senanensis Rehder extract inhibited the cytopathic effect and viral production in a dose-dependent manner. Further, real-time RT-PCR assay and Western blotting analysis revealed that Sasa senanensis Rehder extract decreased expression of the HCMV IE gene in virus-infected HEL cell.
Conclusion: These results suggest that Sasa senanensis Rehder extract have anti-HCMV activity by inhibitting of IE gene expression.
4.Five cases of breast reconstruction with pedicled greater omentum metastasis after mastectomy
Guangxu HAO ; Qing ZHONG ; Changxiao ZHAO ; Li DONG ; Yi REN ; Jing ZHANG
Chinese Journal of Endocrine Surgery 2021;15(2):211-214
Immediate breast reconstruction with pedicle great omentum metasasis is safe,easy to perform, and has extensive clinical indications, less postoperative complications. The shape of reconstructed breast is plump and symmetrical, which is the optimal choice for reconstruction surgery with small and medium-sized breast at present. The surgical methods and effects of breast reconstruction with pedicle great omentum metastasis in 5 patients are reported in this article. Combined with the previous literature, the feasibility and safety of surgery is discussed, which provide a reference to clinicians.
5.Early predictors of Mycoplasma pneumoniae necrotizing pneumonia in children
Shuaishuai LIU ; Jing MA ; Zhongxiao ZHANG ; Changxiao LI ; Linlin HAN ; Chen MENG
Chinese Journal of Applied Clinical Pediatrics 2021;36(8):601-604
Objective:To study the early predictors of Mycoplasma pneumoniae necrotizing pneumonia in children.Methods:Clinical data of 291 children with lobar pneumonia caused by Mycoplasma pneumoniae who were hospitalized in Department of Respiratory Intervention, Qilu Children′s Hospital of Shandong University from August 2016 to September 2018, were retrospectively analyzed.The patients were divided into necrotizing pneumonia group (154 cases) and non-necrotizing pneumonia group (137 cases). After comparing clinical characteristics, laboratory tests, and bronchoscopy findings, multivariate logistic regression analysis was carried out on the indicators with statistical significance to obtain the independent predictive indicators of Mycoplasma pneumoniae necrotizing pneumonia, and then the cutoff value with the maximum diagnostic value of each indicator was found through receiver operating characteristic (ROC) curve analysis.Results:There were no significant differences in gender and age distribution, duration before admission, and platelet count between the 2 groups(all P>0.05). Necrotizing pneumonia group manifested with 11.0(8.3-14.4)×10 9/L of white blood cell count, 0.740±0.115 of neutrophil, 44.2(21.2-72.0) mg/L of C-reactive protein(CRP), 55(35-80) mm/1 h of erythrocyte sedimentation rate, 0.19(0.08-0.60) ng/L of procalcitonin, 2.63(1.62-3.79) mg/L of plasma D-dimer, 456(340-665) U/L of serum lactate dehydrogenase, (35.6±4.3) g/L of serum albumin, 121 cases(78.6%)of bronchoscopic mucosal erosion, 75 cases(48.7%)of purulent lavage, 119 cases(77.3%)of massive secretions embolism; non-necrotizing pneumonia group manifested with 8.7(6.9-11.6)×10 9/L of white blood cell count, 0.660±0.127 of neutrophil percentage, 15.9(7.5-34.3) mg/L of CRP, 45(30-60) mm/1 h of erythrocyte sedimentation rate, 0.10(0.06-0.20) ng/L of procalcitonin, 0.69(0.46-1.24) mg/L of plasma D-dimer, 314(250-419) U/L of serum lactate dehydrogenase, (38.9±3.7) g/L of serum albumin, 53 cases(38.7%)of bronchoscopic mucosal erosion, 20 cases(14.6%)of purulent lavage, and 76 cases(55.5%)of massive secretions embolism.All the above indicators had statistical differences between the 2 groups.Erythrocyte sedimentation rate, serum lactate dehydrogenase, D-dimer, and bronchoscopic mucosal erosion were independent predictors of Mycoplasma necrotizing pneumonia.The area under the ROC curve were 0.643, 0.749, 0.858 and 0.699, respectively, with the cut off point of 53 mm/1 h, 335 U/L, and 1.36 mg/L, respectively. Conclusions:Erythrocyte sedimentation rate≥53 mm/1 h, serum lactate dehydrogenase≥335 U/L, D-dimer≥1.36 mg/L, and bronchoscopic mucosal erosion are early independent predictors of Mycoplasma necrotizing pneumonia in children, among which D-dimer has the highest value.
6.Potential synergic mechanism of Wutou-Gancao herb-pair by inhibiting efflux transporter P-glycoprotein
Yufei HE ; Zihong WEI ; Ying XIE ; Xiulin YI ; Yong ZENG ; Yazhuo LI ; Changxiao LIU
Journal of Pharmaceutical Analysis 2020;10(2):178-186
Wutou-Gancao herb-pair is extensively used to attenuate the toxicity and enhance the efficacy of aconite. In this study, potential synergic mechanism of the herb pair was investigated by utilizing multiple ap-proaches. In silico and in vitro Caco-2 cell models were applied to study the potential binding mode of bioactive ingredients existing in liquorice with P-glycoprotein (P-gp), as well as the inhibition effects on P-gp. Additionally, anti-inflammatory activity of aconitine (AC) combined with active ingredients of liquorice, as well as pharmacokinetic patterns of AC after co-administration was investigated. Anti-inflammatory effect of AC (1 mg/kg) in rats was enhanced in combination with bioactive ingredients of liquorice (10 mg/kg). In the meanwhile, the exposure of AC in vivo was altered, in terms of Cmax and AUC. For instance, the Cmax and AUC were increased to 1.9 and 1.3 folds, respectively, when used in combination with liquiritigenin. The in silico study revealed the potential binding mode with outward facing conformation of P-gp. The resulting data obtained from transport of rhodamine-123 (Rh-123) across Caco-2 cell monolayer further indicated that the function of P-gp was inhibited by chemicals in liquorice. The synergic effect was therefore proposed to be attributed to inhibition of P-gp by liquorice since AC has been demonstrated to be the substrate of P-gp. The resuls revealed that potential synergic mechanism of Wutou-Gancao herb-pair by inhibiting function of key efflux transporter P-gp to enhance the exposure of AC in systematic circulation, and further the anti-inflammatory effect, which helps clarify the compatibility rationale of these two herbs.
7.Evaluation of tolerance and pharmacodynamics of nano-micelle irinotecan formulation
Tao CUI ; Weidang WU ; Xiaoyan CI ; Wei LI ; Chuanmin GUO ; Jing XU ; Xiulin YI ; Changxiao LIU
Journal of China Pharmaceutical University 2019;50(2):175-179
This study aimed to investigate the improvement of tolance and pharmacodynamics of nano-micelle irinotecan formulation compared with irinotecan hydrochloride injection(Campto). The toxic effects of the two formulations on colorectal cancer cells COLO205, HT-29, HCT-8 and SW480 were tested in vitro. COLO205 tumor-bearing mouse model was constructed. The two preparations were given via tail vein injection to investigate the maximum tolerance dose(MTD)of tumor-bearing mice to the two preparations, and then to explore the improvement of anti-tumor efficacy of nano-micelle irinotecan formulation near the MTD. The results showed that there was no significant difference in the inhibitory effect of the two formulations on the four colorectal cancer cells in vitro. The MTD of nano-micelle irinotecan formulation and Campto was 432. 0 and 276. 5 mg/m2 respectively. Both of the two formulations showed significant anti-tumor effect in vivo, and the relative tumor proliferation rate and tumor wet weight inhibition rate of nano-micelle irinotecan formulation at high dose(345. 6 mg/m2)were significantly better than those of Campto at two doses(177. 0 and 221. 2 mg/m2)(P< 0. 05).
8.Research and development in drug innovation: reflections from the 2013 bioeconomy conference in China, lessons learned and future perspectives.
Changxiao LIU ; Panayiotis P CONSTANTINIDES ; Yazhuo LI
Acta Pharmaceutica Sinica B 2014;4(2):112-119
The enormous progress biotechnology, bioinformatics and nanotechnology made in recent years provides opportunities and scientific framework for development of biomedicine and constitutes a paradigm shift in pharmaceutical R&D and drug innovation. By analyzing the data and related information at R&D level over the past decades, developmental tendency and R&D patterns were summarized. We found that a growing number of biologics in the pipeline of pharma companies with successful products already in the market though, small molecular entities have primarily dominated drug innovation. Additionally, small/medium size companies will continue to play a key role in the development of small molecule drugs and biologics in a multi-channel integrated process. More importantly, modern and effective R&D strategies in biomedicine development to predict and evaluate efficacy and/or safety of 21st century therapeutics are urgently needed. To face new challenges, developmental strategies were proposed, in terms of molecular targeted medicine, generic drugs, new drug delivery system and protein-based drugs. Under the current circumstances, interdisciplinary cooperation mode and policy related to drug innovation in China were deeply discussed as well.
9.Nutritional literacy and influencing factors among students from Nutrition Improvement Program for Rural Compulsory Education Students in Chongqing
LI Shengping, ZENG Mao, XIE Changxiao, XU Qi, ZHAO Yong
Chinese Journal of School Health 2022;43(1):41-44
Objective:
To analyze the nutritional literacy and influencing factors among students from Nutrition Improvement Program for Rural Compulsory Education Students (NIPRCES) in Chongqing, and to provide a scientific basis for improving the nutritional literacy of middle school students in the NIPRCES.
Methods:
Using cross sectional survey, a total of 3 365 students in the grade 7 and 8 were selected from the middle schools in 12 national pilot districts and 2 Chongqing pilot districts by online survey in September 2020. Students filled out a self designed nutritional literacy questionnaire anonymously. The relative evaluation method was used to convert the nutritional literacy of scores into a percentile, and the median score was used as the criterion for qualified nutritional literacy screening.
Results:
The median score of nutritional literacy of participants was 63.5, and 64.2% achieved the qualified level. The results of multivariate Logistic regression analysis showed that boarding school ( OR =1.28, 95% CI =1.08- 1.51 ) and no parents as the primary caregiver ( OR =1.22,95% CI =1.05-1.42) were associated with poor nutritional literacy. Urban residence ( OR =0.75, 95% CI =0.63-0.90), NIPRCES local pilot ( OR =0.83, 95% CI =0.71-0.97) and high paternal education ( OR =0.70, 95% CI =0.52-0.95) were associated with higher nutritional literacy ( P <0.01). Classroom was the main channel for students to obtain nutrition information at present (65.1%) and in the future (72.8%).
Conclusion
The nutritional literacy among students in the NIPRCES in Chongqing needs to be improved. Nutritional literacy level of students can be strengthened by nutritional education in boarding schools, rural areas, national pilot areas, and primary caregivers.
10.Absolute bioavailability,dose proportionality,and tissue distribution of rotundic acid in rats based on validated LC-QqQ-MS/MS method
Haihua SHANG ; Xiaohan DAI ; Mi LI ; Yueyi KAI ; Zerong LIU ; Min WANG ; Quansheng LI ; Yuan GU ; Changxiao LIU ; Duanyun SI
Journal of Pharmaceutical Analysis 2022;12(2):278-286
Rotundic acid(RA),an ursane-type pentacyclic triterpene acid isolated from the dried barks of Ilex rotunda Thunb.(Aquifoliaceae),possesses diverse bioactivities.To further study its pharmacokinetics,a simple and sensitive liquid chromatography with triple quadrupole mass spectrometry(LC-QqQ-MS/MS)method was developed and validated to quantify RA concentration in rat plasma and tissue using etofesalamide as an internal standard(IS).Plasma and tissue samples were subjected to one-step protein precipitation.Chromatographic separation was achieved on a ZORBAX Eclipse XDB-C18 col-umn(4.6 mm×50 mm,5 μm)under gradient conditions with eluents of methanol:acetonitrile(1∶1,V/V)and 5mM ammonium formate:methanol(9∶1,V/V)at 0.5mL/min.Multiple reaction monitoring transitions were performed at m/z 487.30 → 437.30 for RA and m/z 256.10 → 227.10 for IS in the negative mode.The developed LC-QqQ-MS/MS method exhibited good linearity(2-500 ng/mL)and was fully validated in accordance with U.S.Food and Drug Administration bioanalytical guidelines.Dose proportionality and bioavailability in rats were determined by comparing pharmacokinetic data after single oral(10,20,and 40 mg/kg)and intravenous(10 mg/kg)administration of RA.Tissue distribution was studied following oral administration at 20 mg/kg.The results showed that the absolute bioavailability of RA after administration at different doses ranged from 16.1%to 19.4%.RA showed good dose proportionality over a dose range of 10-40 mg/kg.RA was rapidly absorbed in a dose-dependent manner and highly distributed in the liver.In conclusion,this study is the first to systematically elucidate the absorption and distribution characteristics of RA in rats,which can provide additional information for further development and evaluation of RA in drug metabolism and pharmacokinetic studies.