Journal of Chinese Pharmaceutical Sciences

Synthesis of 2-(AlkyIthio)-1,2,4-triazolo[1,5-a]pyrimidines and 3-(Alkythio)-1,2,4-triazolo[3,4-a] pyrimidines and Their Vasodilator Activity

Tian-Rui Ren^*, Fu-Heng Chen, Jia-Ju Zhou, Hong-Ming Chen, Zong-Ru Guo

1998, 7(4): 171-177.

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A series of new 2-(alkylthio)-5,7-dimethyl-l,2,4-triazolo[1,5-a] pyrimidines and 3-(alkylthio)-5,7-dimethyl-1,2,4-triazolo[3,4-a] pyrimidines have been synthesized. These derivatives were evaluated for inhibitory effects on 85.7 mmol·L^-1 K⁺and 10^-4 mol·L^-1 NE(nor-epinephrine)- induced contraction ofrat aorta strips.

2D NMR Studies on the Benzodiheteropine and its Cycloaddition Products

Yu-Xin Cui, Xiao-Feng Liu, Hai-Tao Wu, Xin-Fu Pan

1998, 7(4): 178-181.

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The signals of ¹H NMR and ¹³C NMR for benzodiheteropine 1 and its cycloaddtion products 2~5 were assigned by two dimensional NMR techniques. The characteristics of their structures were analyzed and discussed. The boat conformation of the seven-membered heteroatomic ring in these structures was interpreted on the basis of the spectrum of NOESY as well. The coupling constants of relative protons were in accord with above results.

Synthesis and Antitumor Activity of Podophyllotoxin Analogues

Kuan-Ke Lu, Fan-Ming Liu, Yao-Zu Chen^*

1998, 7(4): 182-185.

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Seven podophyllotoxin analogues were synthesized by condensation of 4’-demethyl epipodophyllotoxin 10 with 5-alkyl-4-amino-3-mercapto-1,2,4-triazoles 9(a-g) in the presence of TFA(CF3COOH). Their antitumor activities were screened in vitro against HL-60 and K562 cells.

Synthesis and Anti-inflammatory Activity of 2-(E)-(4-Hydroxy-3-methoxybenzylidene)-5-(N-Substituted aminomethyl) Cyclopentanones

Jin-Hua Dong, Li-Ying Xu, Hua-Qin, Ding-Yuan Xu, Li Li, Zhi-Zhong Ji

1998, 7(4): 186-190.

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A series of 2-(E)-(4-hydroxy-3-methoxybenzylidene)-5-(N-substituted ami-nomethyl) cyclopentanones was synthesized and evaluated for the anti-inflammatory activity. All of the target compounds were confirmed by spectral analysis and elemental analysis. Preliminary pharmacological tests showed that several compounds exerted appreciable inhibitory effect on xylene-induced ear edema in mice and that alteration of the substituents of anilines had significant influence in anti-inflammatory potency.

Study on Relative Bioavailability of Famotidine Sustained-release Tablets in Healthy Volunteers

Tao Wu, Huan-Xiang Zeng^*, Ji-Min Chen, Wei-San Pan

1998, 7(4): 191-196.

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The relative bioavailability of famotidine sustained-release (SR) tablets was studied in 16 healthy male volunteers. Famotidine plasma concentration was determined by HPLC method, and the plasma concentration-time data were processed with the method provided by USP XXIII. For single dose administration the peak plasma concentration occurring at 8.13±0.34 h was 69.52±3.00 ng/ml and the relative bioavailability was 112.4%±8.6%. For multiple dose administration the peak plasma concentration of SR tablet was 86.14±2.95 ng/ml and the degree of fluctuation (DF) was 140.6%±13.5% at steady state. Two one-sided tests were performed in bioequivalence assessment. The results showed that the sustained-release tablets were basically bioequivalent to the immediaterelease (IR) tablets on sale.

Determination of Lansoprazole by Direct Injection of Plasma and High Performance Liquid Chromatography with Column Switching

Li-Min Ye, Zhang-Wan Li, Zheng Hong, Guang-Sheng Qian

1998, 7(4): 197-200.

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High performance liquid chromatography with column switching has been developed for the determination of lansoprazole in plasma. The plasma samples were injected onto a pretreatment column packed with LiChromprep RP2 (25~40 mm) after simple dilution with distilled water. Distilled water was used to wash out protein and other polar components in plasma. After switching, the concentrated lansoprazole was eluted in the backflush mode onto a Shimpack CLC-ODS column with methanol -0.2 mol·L^-1 ammonium acetate (65:35) as mobile phase. Purge solutions were used for clean-up and for regenerating the pretreatment column. The method showed good precision and recovery. The detection limit was 0.005 mg·L^-1 plasma. The RSD’s (intra- and interday) were less than 2.5% and 5.3% respectively. The method has been successfully used to determine pharmacokinetics of lansoprazole in Chinese volunteers.

Enantioselective Determination of R-(-)- and S-(+)-Mexiletine in Microsomal Incubates by Capillary gas Chromatography

Si-Ju Wang, Hai-Qiong Mao, Su Zeng^*

1998, 7(4): 201-204.

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A method for the assay of R-(-)- and S-(+)-mexiletine in rat liver microsomal incubates was developed. The method involved extraction of mexiletine from the microsomal incubates, and formation of mexiletine diastereomeric derivatives with a chiral reagent S-(-)-N-trifluoroacetyl prolyl chloride. Separation and quantitation of the diastereomeric mexiletine derivatives were carried out by a capillary gas chromatographic system with flame ionization detection. The assay was linear from 5 to 500 μg/ml for each enantiomer. The average recoveries of analytical method were 93.31%±5.59% and 93.10%±5.11% for R-(-)- and S-(+)-mexiletine, respectively. The limits of detection and quantitation for the method were 1.0 μg/ml and 5.0 μg/ml for the R-(-)- and S-(+)-mexiletine isomers, respectively. The reproducibility in the assay was better than 16.5% (RSD). The method has been applied to the metabolism study of R-(-)- and S-(+)-mexiletine in rat liver microsomal incubates.

Effects of Rhynchophylline on L-type Calcium Channels in Isolated Rat Cortical Neurons During Acute Hypoxia

Li Kai, Zhong-Feng Wang, Chun-Sheng Xue

1998, 7(4): 205-208.

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Aim: To study the effects of rhynchophylline (Rhy) on the L-type calcium channels in freshly dissociated cortical neurons of Wistar rats during acute hypoxia. Methods: Cell-attached configuration of patch clamp technique. L-type calcium channel was activated by stepping from-40 mV to 0 mV. Results: The results showed that the L-type calcium channels of cortical neurons were activated by acute hypoxia. The mean open time of the channel was increased, the mean close time decreased and the open-state probability raised during acute hypoxia. Rhy (15 and 30 μmol·L^-1) in concentration dependent manner blocked activity of the channels. The drug shortened the mean open time of the channels from 8.87 ms to 3.03 ms and 2.23 ms (P<0.001), prolonged the mean close time from 9.23 ms to 38.84 ms and 54.43 ms (P<0.001), and decreased the open-state probability from 0.142 to 0.031 and 0.025 (P<0.001) under the hypoxia condition, respectively. The effects of Rhy were similar to but weaker than those of verapamil (15 μmol·L^-1). Conclusion: The study confirmed that Rhy has the blockade effects on L-type calcium channels in cortical neurons of rats during hypoxia, by which it protects the brain from hypoxic injury.

Mechanisms of Inhibitory Effects of Breviscapine on Lipid Peroxidation in Rat Brain Mitochondria

Xiao-Xia Chen, Bing He, Yi-Yue Chen

1998, 7(4): 209-213.

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The mechanisms by which breviscapine (Bre) inhibits the lipid preoxidation in rat brain mitochondria were investigated. The mitochondrial lipid peroxidation of rat brain induced by oxygen free radical was measured by thiobarbituric acid spectrophotometry. The chelating activities of Bre for Fe²⁺ were tested by differential spectrum. Superoxide anion (O2^·-) from xanthine-xanthine oxidase (Xan-XO) system and hydroxyl radical (·OH) from FeSO4-H2O2 system were determined with spectrophotometry. It was found that Bre could effectively inhibit the lipid peroxidation of brain mitochondria induced by free radicals driven from Xan-XO and FeSO4-H2O2 system. The IC50 of Bre were 93.01 μmol·L-1 for Xan-XO system and 62.18 μmol·L^-1 for FeSO4-H2O2 system. Bre also scavenged O2^·- and ·OH produced by Xan-XO and FeSO4-H2O2 systems. The IC50 of Bre were 32.63 μmol·L^-1 for O2^·- and 20.22 μmol·L^-1 for ·OH. Furthermore, the chelating Fe²⁺ activity of Bre was shown. It may be concluded that Bre inhibited lipid peroxidation at different stages of the reaction of oxygen free redial with the mitochondria membrane: (1) the formation of ·OH; (2) the initiation of the lipid peroxidation, by chelating Fe²⁺ and scavenging O2^·- as well as ·OH. The scavenging oxygen free radicals and chelating iron are the mechanisms of inhibitory effect of Bre on lipid peroxidation.

The Effect of Benzyltetrahydropalmatine(BTHP) on Action Potentials and the Two Components of Delayed Rectifying Potassium Currents in Guinea Pig Ventricular Myocytes

Sheng Yah, Xin-Hua Li, Wei-Xing Yao, Guo-Jin Xia, Ming-Xing Jiang, Wen-Long Huang, Zhen-Ya Huang, Si-Xun Peng

1998, 7(4): 214-217.

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The effects of BTHP on Ca²⁺-independent action potential and the two components of delayed rectifier potassium currents were studied in guinea pig single ventricular myocytes by using whole cell patch clamp technique. BTHP 30 μmol·L^{- 1} significantly prolonged APD90 from 143±16 ms to 184±21 ms (P<0.01, n = 5) without affecting either the RP or APA , and the APD prolonging effects of BTHP were independent of extracellular Ca²⁺. BTHP inhibited both Ikr (IC50 = 719μmol·L^{- 1}) and Iks (IC50 = 2214 μmol·L^{- 1}) in a concentration-dependent fashion. The results demon-strated that BTHP had no obvious selectivity for Ikr and Iks.

Chemical Constituents of the Fruit of Licium barbarum L.

Qun Wang, Yang Qiu, Shi-Peng He, Ya-Yan Chen

1998, 7(4): 218-220.

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Synthesis and Bioacticity of Xanthene-9-carboxylic Acid Derivatives

Xiao-Shen Ji, Yan Liu, Yi Miao, Tao Jin

1998, 7(4): 221-223.

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Studies on the SOD-like Activity in the Stool of Trogopterus Xanthipes Miline-Edwards

Yue-Kai Chen, Jian-Huan Ma, Ji-Kan Zhou, Yu-Ying Xi, Xin-Zhu Guo

1998, 7(4): 224-226.

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Syudies on the Phase Equilibrium of the System C6H12O6(NH4)2SO4-C2H5OH-H2O(C2H5OH/H2O=0.90) by wt at 35 ℃

Dao-Dao Hu, Dong-Qin Su, Ya-Li Cui, Yu Fang, Zong-Xun Tang

1998, 7(4): 227-229.

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Studies on the Synthesis of Tetrapyrrole Nitrogen Mustards and Their Directed Dual Anti-tumor Activities

Zhi-Long Chen^*, Wei-Qin Wan, De-Yu Xu

1998, 7(4): 230-231.

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