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Studies on the Non-isothermal Decomposition Kinetics of Vitamin B6

Donghua CHEN ; Jian ZHANG ; Wang ZOU ; Wanjun TANG

Journal of China Pharmaceutical University.2001;(3):203-205.

AIM　The purpose is to study the non-isothermal decomposition process and mechanics of vitamin B6. METHOD　The TG technique was used to observe between 30～700℃. RESULTS　The decomposition of vitamin B6 was performed by two stages. Vitamin B6 loses HCl at the first stage together with losing H2O. The kinetic equation obtained was dα/dt=A*e-E/RT*1/2(1-α)3; activation energy obtained was 325.27 kJ/mol; and preexponential factor A obtained was 7.22×1032/s as well. CONCLUSION　Vitamin B6 is rather thermal stable, and it loses HCl together with losing H2O at temperature range of 173℃～271℃.

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Chemical Constituents of Dendrobium fimbriatum Hook.(Ⅰ)

Zhiming BI ; Yisheng YANG ; Zhengtao WANG ; Yanqing GONG ; Juxiu HE ; Tani TADATO

Journal of China Pharmaceutical University.2001;(3):200-202.

AIM　Bio-active constituents were expected to be obtained from Dendrobium fimbriatum Hook. METHODS　It was extracted with 95% alcohol, distributed by petrol, isolated via column chromatography on silica gel and purified by crystallization. RESULTS　Nine compounds were isolated from the stems of Dendrobium fimbriatum Hook., On the basis of spectral analyses, six compounds of them were identified as chrysophanol(3), n-dotriacodtanoic acid(5), defuscin(6), n-triacontyl cis-p-coumarate(7), β-sitosterol(8) and chrysotobibenzyl(9). CONCLUSION　Chrysophanol(3) was firstly isolated from Genus dendrobium and chrysotobibenzyl(9) was found from this species for the first time.

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Studies on the Constituents of Belamcanda chinensis(Ⅰ)

Wenliang JI ; Minjian QIN ; Zhengtao WANG

Journal of China Pharmaceutical University.2001;(3):197-199.

AIM　The aim is to investigate the chemical constituents of Belamcanda chinensis. METHODS　The chemical constituents were isolated and purified by solvent extraction together with various chromatographic techniques. The stuctures was elucidated on the basis of chemical evidence and spectral data. RESULTS　Eight compounds were isolated from the ethanol extract of the rhizome of Belamcanda chinensis (L.)DC..Among them,six isoflavones were elucidated as irilone(Ⅰ)、genistein(Ⅱ)、tectorigenin(Ⅲ)、 irigenin(Ⅳ)、dimethyltectorigenin(Ⅴ)、irisflorentin(Ⅵ). CONCULSION　 ⅠandⅡ were isolated from this medicinal plant for the first time.

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Improved Synthesis of 2-(3-benzoylphenyl) propionitrile

Min YU

Journal of China Pharmaceutical University.2001;(3):185-186.

2-(3-benzoylphenyl)propionitrile which is an important intermediate of ketoprofen was synthesized through phase-transfer catalytic by four steps, involving Friedel-crafts reaction, bromination and cyanation. Pure compound was obtained, and the content of crystal was about 98%.AIM　The content of 2-(3-benzoylphenyl)propionitrile was improved. METHODS　Phase-transfer catalytic methylation and suitable method of aftertreatment were used. RESULTS　The yield and content was both improved. CONCLUSION　Phase-transfer catalytic methylation was the best method, and suitable method of aftertreatment was essential.

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Synthesis and Antihypertensive Activity of 1-Phenylethyl(or 3,4-Dimethyloxyphenylethyl)-4-substituted Aryloxypiperidines

Weifang TANG ; Peizhou NI ; Lin XIA ; Jihua FU

Journal of China Pharmaceutical University.2001;(3):180-184.

AIM　The purpose is to make a search for new antihypertensive agents with higher activity and lower side effect. METHODS　As DDPH a lead compound, ten 1-Phenylethyl (or 3,4-dimethyloxyphenylethyl)-4-substituted aryloxypiperidine compounds were designed and synthesized, keeping the two structural fragments of DDPH: phenylethylamine and aryloxyalkylamine. Their structures were confirmed by Elemental Analysis, IR, 1H-NMR and Mass Spectrum. RESULTS　The majority of the compounds possessed potent antihypertensive activity and the antihypertensive effect of I3 and I4 was stronger than that of DDPH. CONCLUSION　The experimental results were accordant with designed thought and provided useful information for modifying the structure of DDPH deeply.

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Determination of Baicalin in Scutellaria baicalensis Georgi. in the Different Parts by HPLC

Jiwen XU ; Suxiang LUO

Journal of China Pharmaceutical University.2001;(3):235-236.

AIM　The content of baicalin in Scutellalria baicalensis Georgi. in the different parts was determined by RP-HPLC. METHODS　The mobile phase was a mixed liquid with MeOH-Water-H3PO4(60∶40∶0.2). Standard curve showed a linearity within the range of 0.36～0.84 μg/ml(r=0.9995), the average recovery was 99.28%, and RSD=1.4%(n=5). RESULTS　The results showed that the content of baicalin is highest in the bark (cortex) part of Scutellalria baicalensis Georgi.

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Effect of Nerve Regeneration Factor on GAP-43 and NF-L Gene Expression in Dorsal Roots Ganglia Cell

Fei DING ; Mei LU ; Xiaosong GU

Journal of China Pharmaceutical University.2001;(3):231-234.

AIM　To Detect the varying of gene expression in cultured dorsal root ganglion cells treated by Nerve Regeneration Factor and explore its molecular mechanism promoting to nerve growth. METHODS　By RT-PCR, the change of gene expression in GAP-43 and NF-L on the cultured DRG cells with Nerve Regeneration Factor were studied during 4 h, 12 h, 24 h. RESULTS　The expression of GAP-43 and NF-L were increased by Nerve Regeneration Factor on DRG′s culture. CONCLUSION　This study indicated Nerve Regeneration Factor may up-regulate the gene expression associated nerve growth on cultured nervous cells.

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Cloning of D-hydantoinase Gene from Pseudomonas and Its Expression in E.coli

Zhiqiang LI ; Jingjing LIU ; Zhuoyi HU ; Zhenghua WANG ; Xin MING

Journal of China Pharmaceutical University.2001;(3):227-230.

AIM　The purpose is to construct D-hydantoinase genetic engineering strain for the purpose of the industrial production of D-p-hydroxyphenylglycine. METHODS　D-hydantoinase gene was created from Pseudomonas putida 9801 by PCR technique and inserted into pMD18-T vector. The recombinant plasmid was transformed into several Escherichia coli strains. The positive transformants with D-hydantoinase activity were obtained by the two step screening, digoxigenin DNA labeling in situ hybridization and D-hydantoinase activity assay. RESULTS　The D-hydantoinase activity of the genetic engineering strain E.coli BL21/pMD-dht was 1700 U*L-1 and increased as high as 8 times compared with those of wild-type strain Pseudomonas putida 9801. The subunit molecular weight of recombinant D-hydantoinase was about 53 kDa measured by SDS-PAGE. The amount of the recombinant D-hydantoinase was about 20 percent of total bacterial soluble proteins. CONCLUSION　The genetic engineering strain E.coli BL21/pMD-dht possesses the initial industrial production prospects.

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Study on the Anti-inflammatory Effect of Biota orientalis

Tong LIANG ; Yanmei QIN ; Nianci LIANG

Journal of China Pharmaceutical University.2001;(3):224-226.

AIM　The purpose is to investigate the Anti-inflammatory mechanism of Biota orientalis. METHODS　Using rat leukocytes and rabbit platelets as experimental material the biosynthesis of leukotriene, 12-hydroxyheptadecatrienoic acid(12-HHT) and 12-hydroxyeicosatetraenoic acid(12-HETE) in the cells was determined with HPLC. RESULTS　Biota orientalis was shown to inhibit the biosynthesis of leukotriene B4(LTB4) and 5-hydroxyeicosatetraenoic acid(5-HETE) with IC50 of 0.40 and 0.41　mg/ml crude herb, respectively. It was also displayed to inhibit biosynthesis of 12-HHT in the platelets. CONCLUSION　Biota orientalis leaves contain anti-inflammatory components and the anti-inflammatory mechanism was related with inhibiting metabolism of arachidonic acid.

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Antagonistic Effects of Extracts from Cultural Mycelium of Cordyceps sinensis on Arrhythmia

Xiaojian GONG ; Hui JI ; Qi CAO ; Shaoping LI ; Ping LI

Journal of China Pharmaceutical University.2001;(3):221-223.

AIM　The purpose is to study the anti-arrhythmic effects of extracts from cultured Cordyceps sinensis. METHODS　Aconitine and barium chloride were used to induce experimental arrhythmia models in rats. RESULTS　The results showed that PE was more potent than other ingredients. Pretreatment with PE by oral administration significantly antagonized arrhythmia induced by aconitine. PE significantly prolonged the onset of arrhythmia, decreased the duration and diminished the degree of severity. And in barium chloride-induced arrhythmia model, PE had some anti-arrhythmia effect，which could diminish the degree of severity effectively to some extent. CONCLUSION　PE is an active component to antagonize arrhythmia induced by aconitine and barium chloride.

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