1.Recombinant in vitro tools to predict drug metabolism and safety
Haixue WANG ; Qiaolin DENG ; Duan LI ;
Chinese Pharmacological Bulletin 1986;0(06):-
Drug metabolism determines several pharmacological and toxicological properties of pharmaceuticals and is catalyzed by drug metabolizing enzymes. Predicting of drug metabolism in humans based on animal experiments is complicated by species differences in the catalytic properties of these enzymes. This review describes and evaluates the use of recombinant models that contain human drug metabolizing enzymes to facilitate the prediction of pharmacokinetical properties of candidate drugs in humans.
2.Analysis of breast cancer using low-dose thin-thickness dynamic-enhanced MDCT
Yanhui CHEN ; Jie LI ; Feng WANG ; Haixue LI ; Dongya ZHANG
Cancer Research and Clinic 2011;23(5):324-327
Objective To investigate the value of low-dose MDCT in the diagnosis of breast cancer using ROC analysis. Methods Retrospectively analyze the breast images of 105 cases that had performed both 64-row CT and pathological examinations. The case number that underwent CT examination with routinedose parameters was 48; and that with low-dose was 57. Two radiologists with clinical experiences more than 5 years evaluated the breast lesions, respectively. And ROC curve was used to test the diagnostic efficacy of breast cancer between the two groups. Results Compared with the routine-dose group, the quality of CT image was high enough to disclose the breast lesions while the exposure dose was significantly decreased. The areas under the ROC curve between the routine-dose group (0.943) and the low-dose group (0.908) did not show significant difference (P >0.05). Conclusion Low-dose thin-slice MDCT with contrast enhancement can efficiently and safely diagnose breast cancer.
3.Studies on chemical constituents of Bidens bipinnata Ⅰ
Shuai LI ; Haixue KUANG ; Yoshihito OKADA ; Tor OKUYAMA
Chinese Traditional and Herbal Drugs 1994;0(09):-
Object To study the chemical constituents in Bidens bipinnata L Methods Isolation and purifica tion were carried out on silica gel, ODS column and HPLC; the chemical constitue nts were identified by physico-chemical properties and structurally elucidated by spectral analysis Results From EtOAc extract of B bipinnata, eight compounds were obtained and identified as: salicyl i c acid (Ⅰ), 9, 12, 13-trihydroxy-10, 15-octadecadienoic acid (Ⅱ), 9, 12, 13-trihydroxy-10-octadecaenoic acid (Ⅲ), benzyl O-?-D-glucopyranoside (Ⅳ), benzen ethyl O-?-D-glucopyranoside (Ⅴ), (Z)-3-hexenyl O-?-D-glucopyranoside (Ⅵ), eugenyl O-? -D-glucopyranoside (Ⅶ), 3-methyl-2-(2-pentenyl)-4-O-?-D-glucopyranosyl-△ 2-cyclopenten-1-one (Ⅷ) Conclusion All of these compounds, with the exception of Ⅰ, are obtained from the plant for the first time
4.Chemical constituents of Bidens bipinnata (Ⅱ)
Shuai LI ; Haixue KUANG ; Okada YOSHIHITO ; Toru OKUYAMA ;
Chinese Traditional and Herbal Drugs 1994;0(09):-
Object To study the chemical constituents of Bidens bipinnata L Methods Isolation and purification were carried out on silica gel, ODS column, and Sephadex LH 20, HPLC, identified by physicochemical properties and structurally elucidated by spectral analysis Results From n BuOH extract of B bipinnata, 12 compounds were obtained and identified as: 6 O ? D glucopyranosyl 6, 7, 3′, 4′ tetrahydroxyaurone (Ⅰ), 6 O (6″ acetyl ? D glucopyranosyl) 6, 7, 3′, 4′ tetrahydroxyaurone (Ⅱ), quercetin 3 O ? D glucopyranoside (Ⅲ), quercetin 3 O ? L rhamnoside (Ⅳ), iso okanin 7 O ? D glucopyranoside (Ⅴ), esculin (Ⅵ), (E) 2 hexenyl O ? D glucopyranoside (Ⅶ), n hexyl O ? D glucopyranoside (Ⅷ), isopentyl O ? D glucopyranoside (Ⅸ), n butyl O ? D fructofuranoside (Ⅹ), n butyl O ? D fructofuranoside (Ⅺ), n butyl O ? D fructopyranoside ( ⅩⅡ ) Conclusion All of these compounds, except Ⅰ and Ⅴ, are obtained from the plant for the first time
5.Chemical constituents from the leaves of Broussonetia papyrifera
Weisheng FENG ; Hongwei LI ; Xiaoke ZHENG ; Haixue KUANG ; Suiqing CHEN ; Yanzhi WANG ; Xinyu ZANG
Acta Pharmaceutica Sinica 2008;43(2):173-180
To separate and identify the chemical constituents from the leaves of Broussonetia papyrifera (Linn.) Vent, various columns including Diaion HP-20, Toyopearl HW-40C, Sephadex LH-20, silica gel were employed for the isolation and purification of compounds from the leaves of B.papyrifera. The structures of the compounds were elucidated by their physiochemical characteristics and spectral data. Nineteen compounds were isolated from the leaves of B.papyrifera and their structures were identified as apigenin (1), apigenin-7-O-β-D-glucopyranoside (2), chrysoerid-7-O-β-D-glucopyranoside (3), apigenin-7-O-β-D-glucopyranuronide (4), vitexin-7-O-β-D-glucopyranoside (5), luteolin (6), 5,7,4′-trihydroxyl-6-C-[a-L-rhamnopyranosyl(1→2)]-β-D-glucopyranosyl flavone (7), 5,7,4′-trihydroxyl-8-C-[a-L-rhamnopyranosyl(1→2)]-β-D-glucopyranosyl flavone (8), saponaretin (9), vitexin (10), benzyl benzoate-2,6-di-O-β-D-glucopyranoside (11), (2R,3R,5R,6S,9R)-3-hydroxy-5,6-epoxy-β-ionol-2-O-β-D-glucopyranoside (12), (2R,3R,5R,6S,9R)-3-hydroxyl-5,6-epoxy-acetyl-β-ionol-2-O-β-D-glucopyranoside (13), ficustriol (14), (6S,9S)-roseoside (15), 3β-hydroxy-5α,6α-epoxy-β-ionone-2α-O-β-D-glucopyranoside (16), icariside B1 (17), sammangaoside A (18), 3-hydroxy-5α,6α-epoxy-β-ionone (19). Compounds 11, 12 and 13 are new compounds, the others are isolated from this genus Broussonetia for the first time.
6.Cloning, Sequence Analysis and Prokaryotic Expression ofGGPS Gene fromLepidium apetalum
Ligang MA ; Le ZHAO ; Yingchao LI ; Weisheng FENG ; Haixue KUANG ; Xiaoke ZHENG
World Science and Technology-Modernization of Traditional Chinese Medicine 2015;17(3):485-491
This study was aimed to clone the GGPS (geranylgeranyl pyrophosphate synthase) gene from Lepidium apetalum, to analyze its sequence, and to express the protein in E.coli expression system. Specific PCR cloning primers were designed for GGPS gene from Lepidium apetalum according to the full-length sequence from a previous transcriptome sequencing project. PCR amplification was performed with this primer pair on a leaf cDNA template. TA cloning, sequencing and sequence analysis were performed.GGPS gene from Lepidium apetalum was expressed in the E.coli expression system. The results showed that the full-lengthGGPS cDNA from Lepidium apetalum was 1 146 bp coding a protein of 381 amino acids. The LaGGPS protein had an isoprenoid synthase domain. According to a phylogenetic tree constructed with multiple alignment of GGPS protein sequences from various plant species, GGPS protein from Lepidium apetalum was the closest to Arabidopsis thaliana and Sinapis alba. The prokaryotic expression vectorpET-32a-LaGGPS was also constructed successfully. The protein was expressed in E.coli BL21 strain. It was concluded that the cloning and prokaryotic expression of LaGGPS gene provided a foundation for a follow-up research of its function with protein purification and activity analysis.
7.Effects of five processing methods on compositions and contents of fatty oils in Descurainiae Semen
Hongwei LI ; Yanbang SHI ; Lianqi TIAN ; Haixue KUANG ; Xiaoke ZHENG ; Weisheng FENG
Chinese Traditional Patent Medicine 2017;39(8):1661-1665
AIM To investigate the effects of frost-like powder,steaming,stir-frying with wine,stir-frying with salt-water and stir-frying with vinegar on compositions and contents of fatty oils in Descurainiae Semen.METHODS Descurainiae Semen was processed by five methods,respectively.The fatty oils were extracted from various processed products by petroleum ether,which were then derivatized.GC-MS was adopted in the qualitative identification and quantitative determination.RESULTS Except for frost-like powder,various processing methods could increase the extraction rate of fatty oils.Compared with raw product,the quantities of fatty oils in various processed products were decreased,together with the increased contents.The main compositions of obtained fatty oils were unsaturated fatty acids,whose contents in various processed products (except stir-frying with vinegar product) were higher than those in the raw product.CONCLUSION The effects of different processing methods on compositions and contents of fatty oils in Descurainiae Semen show obvious differences,among which the processing effect of stir-frying with vinegar is not satisfactory.
8.MRI findings of the brain after gas explosion and its relationship with post-traumatic stress disorder
Ruifeng ZHAO ; Jilong JIN ; Huabing LI ; Shufeng LI ; Shuwen TIAN ; Haixue LI ; Yanhui CHEN ; Tianliang WANG ; Lin MA ; Zijing REN
Chinese Journal of Radiology 2008;42(12):1241-1245
Objective To investigate MR findings and dynamic changes of the brain after gas explosion,and to evaluate the relationship between MR findings and post-traumatic stress disorder (PTSD).Methods Forty-nine survivors of a gas explosion (group A) were examined with brain MRI within 1 to 3 days,and serial MR follow-up examinations were also performed.Forty miners not under the ground that day were assigned as group B,and 40 staff working on the ground as group C.The signal intensity values of hippocampus and globus pallidus on T2WI were measured in the three groups and F test was performed by using SPSS 13.0.The relationship between signal intensity values of hippocampus/globns pallidus and PTSD was explored,and the relationship between ADC values of hippocampus and PTSD was also investigated.Results In group A,slight low signal on T1WI and high signal on T2WI were detected on initial MRI in hippocampus (33 cases),globus pallidus (12 cases),cortex (10 cases),and midbrain (2 cases),respectively.On follow-up MRI at 2 months,lesions in hippocampus disappeared (25 cases) or remained slight high signal on T2WI (8 cases),lesions in globus pallidus disappeared (3 cases,5 sides) or showed shrinkage and encephalomalacia (9 cases),cortical lesions resulted in encephalomalacia in 2 cases and returned normal in the others,and lesions in the midbrain showed encephalomatacia.For comparison of T2 signal intensity values in hippocampus and globus pallidus,there was significant difference between group A and group B(P <0.01),and also between group A and group C(P <0.01),but no difference was detected between group B and group C (P>0.05).In group A,the T2 signal intensities of PTSD and non-PTSD were 455±37 and 462±53 in the left hippocarnpus,and 458±36 and 460±43 in the right hippoeampus on 1 to 3 days,and the T2 signal intensities of PTSD and non-PTSD were 438±29 and 424±37 in the left hippocampns,and 442±31 and 430±32 in the right hippocampus at 2 months.The T2 signal intensities of PTSD and non-PTSD were 361 ±35 and 366±63 in the left globus pallidus,and 363 ±41 and 375±62 in the right globus pallidus on 1 to 3 days,and the T2 signal intensities of PTSD and non-PTSD were 341±24 and 337±39 in the left globns pallidus,340±26 and 332±35 in the tight glohus pallidns at 2 months.There was no difference of T2 signal intensity values in hippocampus and globus pallidus between PTSD and non-PTSD( t=0.350,0.826,0.503,0.907,P>0.05).In group A,ADC values of PTSD and nun-PTSD were (8.1±1.1)×10-4 and(8.1 ±0.9)×10-4mm2/s in the left hippocampus,and (8.2±1.0)×10-4 and(8.2±0.8)×10-4mm2/s in the tight hippocampus on 1 to 3 days,ADC values were (8.8±0.7)×10-4 and (9.0±1.0)×10-4mm2/s in the left hippocampus,and (8.5±0.9)×10-4 and (9.3±1.1)×10-4mm2/s in the tight hippocampus at 2 months.ADC values in hippocampns showed no difference between PTSD and non-PTSD(t=0.016,0.081,P>0.05)on initial MRI,but showed significant difference between PTSD and non-PTSD in tight hippocampus (t=7.407,P < 0.05) on follow-up MRI at 2 months,while no difference in left hippocampus (t =0.333,P>0.05) was observed at 2 months.Conclusion Hippocampns and globus pallidus are the most vulnerable structures in gas explosion.The occurrence of PTSD may be related to the injury of fight hippocampus,but not related to the injury of globns pallidus.
9.Study on Chemical Constituents from Chemical Split Fractions ofMori Cortex
Weisheng FENG ; Yangang CAO ; Fang LI ; Yanli ZHANG ; Chunge LI ; Xiaolan WANG ; Wenjing CHEN ; Haixue KUANG ; Xiaoke ZHENG
World Science and Technology-Modernization of Traditional Chinese Medicine 2015;17(3):492-498
This article was aimed to study the chemical constituents from the chemical split fractions of Mori Cortex. The compounds were isolated with Diaion HP-20, Toyopearl HW-40, Sephadex LH-20, MCI Gel CHP-20, Silica gel column chromatography and preparative HPLC. Structures of compounds were identified by physicochemical properties and spectral analysis. The results showed that 23 compounds were obtained. And their structures were identified. The 16 compounds were obtained from the 30% ethanol fraction as vanillic acid (1), 3,4-dimethoxyphenol (2), benzoic acid (3), syringic acid (4), kelampayoside A (5), p-hydroxyphenylpropionic acid (6), caffeic acid (7), hydroferulic acid (8), 6,7-dihydroxycoumarin (9), 5,7-dihydroxycoumarin (10), morin-7-O-β-D-glucopyranoside (11), liriodendrin (12), 2,3-trans-dihydromorin (13), 2,3-cis-dihydromorin (14), 2,3-trans-dihydroquercetin (15), 2,3-cis-dihydroquercetin (16). The 4 compounds were obtained from the 50% ethanol fraction as scopoletin (17), morin (18), kaempferol-7-O-β-D-glucopyranoside (19), umbelliferone (20). The 3 compounds were obtained from the 80% ethanol fraction as sanggenon R (21), cis-mulberroside A (22), resveratrol (23). It was concluded that compounds 2, 4-6, 11, 16, 19 were isolated from this plant for the first time.
10.Chemical Constituents from Chemical Split Fractions of Seeds ofDescurainia sophia (L.) Webb. ex Prantl.
Weisheng FENG ; Chunge LI ; Wenjing CHEN ; Yanli ZHANG ; Yangang CAO ; Jianhong GONG ; Fang LI ; Haixue KUANG ; Xiaoke ZHENG
World Science and Technology-Modernization of Traditional Chinese Medicine 2015;17(3):455-463
This article was aimed to study the chemical constituents of seeds of Descurainia Sophia (L.) Webb. ex Prantl., in order to lay the material foundation for further interpretation of seeds of D. Sophia and provide pharmacodynamic basis as well as the basis for attributing its nature and taste. The compounds were isolated and purified by Diaion HP-20, Toyopearl HW-40, MCI Gel CHP-20, ODS, Silica gel chromatography combining with Pre-HPLC. The structures were identified on the basis of spectral data and physicochemical properties. Twenty eight compounds were isolated and identified from 20% and 80% ethanol fraction. Thirteen compounds were identified from 20% ethanol fraction: kaempferol-3-O-β-D-glucopyranosyl-7-O-β-D-gentiobioside(1), quercetin-3-O-β-D-glucopyranosyl-7-O-β-D-gentiobioside (2), isorhamnetin-3-O-β-D-glucopyranosyl-7-O-β-D-gentiobioside (3), isorhamnetin-3,7-di-O-β-D-glucopyranoside (4), quercetin-3,7-di-O-β-D-glucopyranoside (5), kaempferol-3, 7-di-O-β-D-glucopyranoside (6), kaempferol-3-O-β-D-xylopyranosyl (1 → 2)-β-D-glucopyranoside (7), methyl sinapate (8), syringaldehyde (9), (S)-p- hydroxyphenyl lactate acid (10), (S)-2-hydroxy-phenylpropionic acid (11), scopoletin (12), sinapic acid (13). Fifteen compounds were identified from 80% ethanol fraction: isorhamnetin-3-O-β-D-glucopyranoside (14), quercetin-3-O-β-D-glucopyranoside (15), kaempferol-3-O-β-D-glucopyranoside (16), quercetin (17), kaempferol (18), isorhamnetin (19), syringic acids (20), quercetin-3-O-β-D-arabinopyranoside (21), quercetin-3-O-β-D-xylopyranoside (22), 6-O-[E]-Sinapoyl-(α- and β)-D-glucopyranoside (23), dimethyl (E, E)-4,4'-dihydroxy-3,3',5,5'-tetramethoxylign-7,7'-dien-9,9'-dioate (24), dimethylthomasidioate (25), 2-hydroxy-3-(1H-indol-3-yl) propanoic acid (26), 2-hydroxyl-3-(1H-indol-3-yl) propanoic acid methyl ester (27), 4'-O-methyl-dihydroquercetin (28). It was concluded that compounds 7-11 and 21-28 were isolated from seeds of D. sophia (L.) Webb. ex Prantl. for the first time.