2.Synthesis of podo-and epipodo-11C-podophyllotoxin and their biodistribution in mouse bearing EMT6 tumor
Xi LIU ; Xiaojun ZHANG ; Jinming ZHANG ; Peng LI ; Jiahe TIAN ; Boli LIU
Chinese Journal of Nuclear Medicine and Molecular Imaging 2014;34(5):370-373
Objective To synthesize podo-and epipodo-podophyllotoxin labeled with 11C and investigate their biodistribution in mice bearing EMT6 tumor by microPET.Methods 11 C-podo-or epipodopodophyllotoxin was synthesized by 11 C-CH3-Triflate mixed with 4'-methyl-demethmyl-podophyllotoxin (podo-and epipodo-) and purified using HPLC.The radiochemical purity (RCP) was analyzed by HPLC.Thirty mice bearing EMT6 tumor were divided into 2 groups and injected with 3.7 MBq 11C-podo-or epipodo-podophyllotoxin.The biodistribution of 11C-podo-or epipodo-podophyllotoxin was evaluated with microPET.The ID%/g was calculated.Paired t test was used to analyze the data.Results The yields of 11C-podo-and epipodo-podophyllotoxin were both >90%.The RCP was >99%.The biodistribution of 11C-podo-and epipodo-podophyllotoxin was similar with slow blood clearance and high uptake in abdomen.The tumor uptake of 11C-epipodophyllotoxin and 11C-podophyllotoxin at 30 min was (3.63±0.98) %ID/g and (3.16±0.27) %ID/g,respectively.The uptake ratio of tumor to blood and to muscle was 0.68 vs 0.62 and 1.52 vs 1.22,respectively.There was no significant difference between the tumor uptake of the two agents (t=0.47,P>0.05).The result of microPET imaging was consistent with that of mice experiment.Conclusion 11C-podophyllotoxin has limited clinical value for tumor imaging.
5.A Comparative Study on the Mutagenicity of Natural Borneol and Synthetic Borneol
Yang LIU ; Limin HU ; Yilan LI ; Xiang FAN ; Rong DU ; Boli ZHANG
Traditional Chinese Drug Research & Clinical Pharmacology 1993;0(04):-
Objective&Methods The mutagenicity of natural Borneol and synthetic Borneol was studied by using Ames test.Results Natural Borneol and Synthetic Borneol in the dose range of 0.4~250.0 ?g/plate had no effect in reducing the reversion frequencies of Salmonella Typhimurium histidine auxotrophic mutant(TA97,TA98,TA100,TA102)whether if metabolic activation system(S9mix)existed or not.Moreover,the backward mutant colony had normal background.Conclusion Natural Borneol and Synthetic Borneol do not possess evident mutagenicity under experimental condition.
6.Strategies of the study on herb genome program
Shilin CHEN ; Yongzhen SUN ; Jiang XU ; Hongmei LUO ; Chao SUN ; Liu HE ; Xianglin CHENG ; Boli ZHANG ; Peigen XIAO
Acta Pharmaceutica Sinica 2010;45(7):807-12
Herb Genome Program (HerbGP) includes a series of projects on whole genome sequencing (WGS) and post-genomics research of medicinal plants with unique secondary metabolism pathways or/and those of great medical and pharmaceutical importance. In this paper, we systematically discussed the strategy of HerbGP, from species selection, whole-genome sequencing, assembly and bioinformatics analysis, to postgenomics research. HerbGP will push study on Chinese traditional medicines into the front field of life science, by selecting a series of plants with unique secondary metabolism pathways as models and introducing "omics" methods into the research of these medicinal plants. HerbGP will provide great opportunities for China to be the leader in the basic research field of traditional Chinese medicine. HerbGP shall also have significant impacts on the R&D of natural medicines and the development of medicinal farming by analysis of secondary metabolic pathways and selection of cultivars with good agricultural traits.
7.Extending the CONSORT Statement to moxibustion.
Chungwah CHENG ; Shufei FU ; Qinghui ZHOU ; Taixiang WU ; Hongcai SHANG ; Xudong TANG ; Zhishun LIU ; Jia LIU ; Zhixiu LIN ; Lixing LAO ; Aiping Lü ; Boli ZHANG ; Baoyan LIU ; Zhaoxiang BIAN
Journal of Integrative Medicine 2013;11(1):54-63
The STandards for Reporting Interventions in Clinical Trials Of Moxibustion (STRICTOM), in the form of a checklist and descriptions of checklist items, were designed to improve reporting of moxibustion trials, and thereby facilitating their interpretation and replication. The STRICTOM checklist included 7 items and 16 sub-items. These set out reporting guidelines for the moxibustion rationale, details of moxibustion, treatment regimen, other components of treatment, treatment provider background, control and comparator interventions, and precaution measures. In addition, there were descriptions of each item and examples of good reporting. It is intended that the STRICTOM can be used in conjunction with the main CONSORT Statement, extensions for nonpharmacologic treatment and pragmatic trials, and thereby raise the quality of reporting of clinical trials of moxibustion. Further comments will be solicited from the experts of the CONSORT Group, the STRICTA Group, acupuncture and moxibustion societies, and clinical trial authors for optimizing the STRICTOM.
8.Screening of pregnane X receptor activation from ginsenosides.
Yuguang WANG ; Haosheng LIU ; Xianxie ZHANG ; Yong XIAO ; Beibei LU ; Zengchun MA ; Qiande LIANG ; Xianglin TANG ; Chengrong XIAO ; Hongling TAN ; Boli ZHANG ; Yue GAO
Acta Pharmaceutica Sinica 2013;48(1):144-8
In order to study effects of ginseng on the metabolism of drug belong to CYP3A4 substrate, screening of pregnane X receptor activation from ginsenosides was performed by reporter assay. Based on PXR-CYP3A stable translation cell lines, 13 ginsenosides were screened for pregnane X receptor activation by reporter assays, and RIF as the positive control. The effect of ginsenosides Rg1 onCYP3A4 mRNA expression was also investigated by RT-PCR. The PXR-CYP3A stable translation cell lines had good response to RIF, and the EC50 is 2.51 micro mol x L(-1). When the condition of final concentration was 10 micromol x L(-1), ginsenoside F2 and protopanaxatriol had moderate inductive effects on PXR. Panaxotriol, Rg2, pseudoginsenoside F11, Rg1, ginsenoside and Rb3 had inhibitory effects on PXR. Ginsenoside Rf1, Rg3, Rh2 and protopanaxdiol had no obvious effects on PXR. Rg1 down-regulated CYP3A4 mRNA expression in a concentration-dependent manner. Activation of pregnane X receptor by ginsenosides may influence the metabolism of drug belong to CYP3A4 substrate, and cause ginseng-drug interactions.
9.Effect of three penetration enhancers on corneal permeability of mangiferin in vitro.
Rui LIU ; Zhidong LIU ; Lexin SHU ; Chengui ZHANG ; Boli ZHANG
China Journal of Chinese Materia Medica 2010;35(23):3131-3135
OBJECTIVETo investigate the effects of labrasol, solutol HS 15 and transcutol P on the corneal permeability of mangiferin in vitro.
METHODThe effects of three penetration enhancers on the corneal permeability of mangiferin were investigated in vitro by using isolated rabbit corneas.
RESULTThe apparent Papp enhancements were increased 1.80, 3.27, 3.41 and 4.76-folds with Lab at 1.0%, 1.5%, 2.0% and 3.0% (P < 0.01), respectively. The apparent Papp increased 1.98 and 3.07-folds with Sol at 0.2% and 0.4% (P < 0.01), respectively, but reduced with 0.010%-0.03% Trans.
CONCLUSIONThe Papp value of mangiferin is significantly enhanced by 1.0%-3.0% Lab, 0.2% and 0.4% Sol, however the Papp value of mangiferin is reduced by 0.01%-0.03% Trans.
Animals ; Cornea ; drug effects ; metabolism ; Drug Carriers ; chemistry ; Ethylene Glycols ; chemistry ; Glycerides ; In Vitro Techniques ; Organic Chemicals ; chemistry ; Permeability ; Plant Extracts ; pharmacokinetics ; Polyethylene Glycols ; chemistry ; Rabbits ; Stearic Acids ; chemistry ; Xanthones ; pharmacokinetics
10.Clinical significances of additional chromosome abnormalities and t (15;17) in acute promyelocytic leukemia
Yingying LIU ; Tingting FU ; Chunting ZHAO ; Boli CUI ; Lingjie SUN ; Zhan SU ; Xiaodan LIU ; Tianlan LI
Journal of Leukemia & Lymphoma 2019;28(2):100-103
Objective To investigate the clinical significances of additional chromosome abnormalities and t(15;17) in acute promyelocytic leukemia (APL). Methods A total of 90 newly diagnosed APL patients in the Affiliated Hospital of Qingdao University from January 2007 to June 2014 were analyzed retrospectively. Patients with different chromosome karyotypes were divided into four groups: additional chromosome number abnormalities group (16 cases), additional chromosome structural abnormalities group (14 cases), additional chromosome number and structural abnormalities group (4 cases) and typical chromosome group (56 cases). According to whether the patient contained t(15;17), the patients were divided into group with t (15;17) and group without t (15;17). The short-term efficacy and survival of each group were analyzed and compared. Results The rate of complete remission in additional chromosome number abnormalities group, additional chromosome structural abnormalities group, additional chromosome number and structural abnormalities group and typical t(15;17) chromosome changes group were 56.3%(9/16), 100.0%(14/14), 25.0%(1/4) and 82.1%(46/56), the early mortality rates were 25.0%(4/16), 0 (0/14), 75.0%(3/4) and 8.9% (5/56) respectively. Among them, the additional number and structural abnormalities group had lower complete remission rate and higher early mortality rate, and compared with other groups, the differences were statistically significant (all P< 0.05). The complete remission rates of the group with t (15;17) and the group without t (15;17) were 80.5% (66/82) and 50.0% (4/8), respectively, and the difference was not statistically significant (P= 0.070). Conclusions APL patients with karyotypes with additional number and structural changes have low complete remission rate, high early mortality rate and poor prognosis. Patients with t(15;17)have a high rate of complete remission.