Journal of Chinese Pharmaceutical Sciences

Active Constituents of Viola prionantha Bge.

Bo Qin, Qing-Ping Chen, Zhi-Cen Lou

1994, 3(2): 91-96.

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A new coumarin glucoside named prionanthoside together with esculetin and cichoriin was isolated from the whole plant of Viola prionantha Bge. (family Violaceae) for the first time. The structure of the new compound was elucidated as 6-hydroxy, 7-[(6'-O-acetyl-β-D-glucopyranosyl)- oxy-]-coumarin by means of spectral and chemical analyses.

Bovine Serum Albumin (BSA) Microspheres Containing Methotrexate II. Therapeutical Effects on Lung-bearing Sarcoma-180 in Mice

Xiao-Ping Chen, Ting-Sen Shi

1994, 3(2): 97-102.

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The mouse lung concentration of methotrexate (MTX) following the intravenous administration of MTX solution and MTX bovine serum albumin (BSA) microspheres was investigated. The therapeutic effects of the two MTX preparations on lung-bearing sarcomal-80 in mice were also studied. It was found that the AUC of the MTX microspheres group was about 7 times as much as that of the MTX solution group, and the MTX microspheres had better effects on lung-bearing sarcoma-180 than the MTX solution did.

Studies on Aclacinomycin-A Nanocapsules

Mei-Xia Zhang, Jin Hu

1994, 3(2): 103-109.

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This paper describes the conditions under which the aclacinomycin-A nanocapsules (ACM-A-NC) were prepared and lyophilized. These nanocapsules were also subjected to a redispersion test. Their size distribution and drug encapsulation efficiency were also determined. The drug concentrations in blood had shown that the aclacinomycin-A encapsulated in nanocapsules was released well after intravenous injection in rabbits. The data fit into an open two-compartment model. The rabbits given ACM-A-NC had a longer elimination half-life (t1/2(β) = 17.04 h)and a larger AUC (106.74 mg/L·h) than the group given ACM-A injection (t1/2(β) = 10.25h, AUC = 81.88 mg/L·h) Furthermore, the encapsulation of aclacinomycin-A in polybutylcyanoacrylate nanocapslues could change the drug distribution in rats, It was demonstrated that a higher level of ACM-A was found in the lung, thymus, spleen and small intestine while a lower level was found in the heart, kidney and large intestine.

Macroscopical and Microscopical Studies on Chinese Drug Baixianpi, Root-bark of Dictamnus dasycarpus and itsSubstitutes

Xuan Wang, Shao-Qing Cai, Zhi-Cen Lou, Jian-Sheng Zhang, Xi-Yuan Zhao

1994, 3(2): 110-119.

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In order to provide a method of distinguishing the Chinese traditional drug Baixianpi and its substitutes, a comparative study of the macroscopical and microscopical characters of the true Baixianpi, the root-bark of Dictamnus dasycarpus (family Rutaceae), and two substitutes, the root-barks of Cynanchum Chinese (family Asclepiadaceae) and Caragana sinica (family Leguminosae), were undertaken. The results showed that the three kinds of root-barks can be distinguished from each other macroscopically by their shape, colour and texture; and microscopically by their shape of cork cells, the type and distribution of sclerenchyma, the presence or absence of secretory cells, and the type of calcium oxalate crystals.

Effects of Siwenmycin on DNA Topoisomerases Mediated Strand Cleavage and Relaxation in Vitro

Yao Peng, Ding-Yuan Bao, Long-Gui Wang, Xiao-Mei Liu, Xiu-Juan Ji

1994, 3(2): 120-125.

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Siwenmycin, a novel anthracycline antibiotic, was first isolated from a culture of streptomyces galilaeus var. siwenesis of a piece of chinese Siwenmycin inhibited purified mammalian DNA topoisomerase II with a maximal inhibitory concentration of 25 μmol/L as assessed by the ATP-dependent relaxation of supercoiled pBR322 DNA. DNA cleavage aI1d relaxing reactions induced by DNA topoisomerase II obtained from Bel 7402 cells treated with siwenmycin, were increased by 5-fold comparing with control. In addition, siwenmycin also inhibited the catalytic activity of DNA topoisomerases I and induced single-strand DNA breakage in vitro. The results showed that topoisomerases I and II are the cellular targets of siwenmycin, the study of these targets will provide a rational basis for the structural design of aclacinomycin analogues.

Effects of Emodinon the Cytoplasmic Free Calcium in the Platelets

Xiu-Zhen Lin, Zhi-Qing Cui, Zhu-Hua Jin, De-Lu

1994, 3(2): 126-131.

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The intracellular calcium in thc rat platelets was measured with fluorescent calcium indicator fura-2, The changes in thc cytoplasmic free calcium werc also studied in the platelets treated with emodin. The results showed that the free Ca²⁺ level was 2l8.40±56.36 nmol/L (n = 13). In fura-2-loaded resting platelets. After administration of CaCl2 (l mmol/L), KCl (120 mmol/L) and thrombin (0.5 u/ml) sequentially, the free Ca²⁺ levels were 297.25±75.03 nmol/L (n = 13). 318.00±86.25 nmol/L (n = l2) and 640.59±62.49 nmol/L (n = 12) respectively. All of the levels were significantly elevated compared with that of the resting platelets (P<0.0l). After pretreatment with emodin for 20 min. the mean platelet [Ca²⁺]i in these resting platelets was 3l6.28±80.25 nmol/L (n = 16). Using above doses of CaCl2, KCl and thrombin , the free Ca²⁺ levels increased to 396.45±107.78 nmol/L (n = 16). 428.02±126.20 nmol/L (n = 5) and 698. 85±122.93 nmol/L (n = 15) respectively The results revealed an obvious increase in [Ca²⁺]i levels compared with that of the resting(P<0.05 and P<0.0l). Further- more, the Ca²⁺ levels were were significantly higher than those of the control groups(P<0.01) except for the thrombin treatment groups.It was suggested that the increase of [Ca²⁺]i induced by emodin in the platelets was due to the influx of Ca²⁺ and the release of Ca²⁺ from intracellular stores.

Effect of Pentamidine Isethionate (PI) on Fertilizing Ability of Human Spermatozoa in vitro

Ying Wang, Shu-Cheng Zhang, Jin-Song Qiu, Jing-Feng Dai, Yi-Bin Sun, Ying Zhang, Da-zhi Yang

1994, 3(2): 132-137.

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Various trations of PI(0, 0.5, 1.0and2.0mg/ml) were incubated with super-activated human spermatozoa at37 ºC for 5, 15 and 30min, then the vitality and motility of spermatozoa were examined, respectively, after which the washed spermatozoa were cultured with zone-free superovulated hamster ova for 3h. Observations were made for the presence of fertilized ova, ova attached-spermatozoa and pronuclei. The results showed that the vitality and III grade forward motility of spermatozoa were significantly reduced (P<0.05) after drug treament. There was a good negative relativity between vitality, motility and time, dose of PI treatment (P<0.05). The fertilization rate and mean attached spermatozoa/ova, the index of fertilization, were significantly reduced (P<0.01) as compared with controls. There was no pronuclei formation in the drug treated groups. It is suggested that PI may inhibit the ability of fertilization of human spermatozoa and the effect is expressed in several aspects.

Effects of Ginsenoside B on Monophasic Action Potential and His-bundle Electrogram of Rabbit Hearts

Zhu-Qiu Jin, Chong-Ming Liu

1994, 3(2): 138-140.

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The effects of ginsenoside B on His-bundle electrogram (HBE) and monophasic action potential (MAP) of rabbit hearts were studied by cardio- catheter method and suction electrode method respectively. The A-H, H-V intervals of HBE were not affected by ginsenoside B. Ginsenoside B (l mg/kg) shortened the plateau phase of MAP, but had no influence on APA, Vmax, and APD of MAP. The results suggest that ginsenoside B may exert blockage of the slow calcium channel without any apparent effect on the conduction system of the heart.

The Sensitization Models of Rabbits to Rifampicin and to two kinds of Rifampicin-Protein Conjugates and the Detectionof Rifampicin Specific IgG in these Models

Lin-Feng Li, Sun-Xi Zhang, Shi-Yin Li

1994, 3(2): 141-146.

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The Rifampicin (RFP) specific IgG in the sera of rabbits immunized with RFP or with two kinds of RFp-protein conjugates (RFP-bovine serumalbumin, RFP-BSA, and RFP-rabbit serum albumin, RFP-RSA) was measured by ennyme-linked immunosorbent assay (ELISA).The way of conjugation and the molecular cojugation rate were different between RFP-BSdA and RFP-RSA. The titre of the RFP specific IgG was l:l0-l:l00 in RFP immunized rabbits, 1:100-1:1000 in RFP-RSA immunized rabbits and overl:l000 in RFP-BSA immunized rabbits. The binding properties of the sera to RFP were demonstrated by inhibition assay. These are the first RFP sensitization models established by immunizing animals with RFP itself or RFP-protein conjugates.

Effects of Ethanolic Extract of the Stems of Kadsura heteroclita on Anhioxidative Enzymes Activity in Liver Cytosol of mice in vivo

Xiu-Wei Yang, Dao-Feng Chen, Guo-Jun Xu, Masao Hattori, Tsuneo Namba

1994, 3(2): 147-151.

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The effect of ethanolic extract of the stems of Kadeura heteroclita ( KHE) and its main constituent kadsurin, on the activities of anti-oxidative enzymes in liver cytosol of mice in vivo were studied. It is suggested that KHE and kadsurin increased the activities of superoxide dismutase (SOD) and catalase in liver cytosol of mice, but showed no statistical significance in altering the activity of GSH-peroxidase.

Study on Pharmacokinetics and Bioavailability of Terbutalinc by High-performance Liquid Chromatography with Electrochemical Detection

Yi-Sheng Yuan, Min Shen

1994, 3(2): 152-156.

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A sensitive and selective high-performance liquid chromatographic- electrochemical method using olid-phase column extraction and dual series electrode was described for the study ofpharmacokinetics and bioavailabilitv of terbutaline slow-release (SR) tablet made by SSPC (China, Bricanyl II). The erbutaline SR tablet made by Astra (Bricanyl I) was used as reference formulation The comparison of three pharmacokinetic parameters between the two SR tablets showed that the maximal serum concentration (Cmax), the time reaching Cmax (tmax) and the area under serum concentration-time profiles (AUC0→∞)were of no practical difference (P>0.05). The mean relative bioavailability of Bricanyl II compared with Bricanyl I was 105 % in 5 mg.

Separation and Quantitative Determination of Three Coumarins in the Chinese Traditional Drug Zihua Diding, Herba Violae, by High Performance Liquid Chromatography

Bo Qin, Qing-ping Chen, Lu-Wen Shi, Zhi-Cen Lou

1994, 3(2): 157-163.

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A method of separation and quantitative determination of three coumarins, i.e. cichoriin, esculetin and prionanthoside, in the Chinese traditional drug Zihua Diding, Herba Violae, by high performance liquid chromatography is developed. The results showed that among nine Viola species, only Viola prionantha Bge, V mandshurica W. Beck.and V alisoviana Kiss; contain the coumarins, the content is highest in V prionantha. These effectivc compounds exist chiefly in the aerial parts of this plant and the content varied with the growth period. June is the best time for collecting Viola prionantha.

Determination of α-Tocopherol in Human and Rabbit Plasma or Serum by High-performance Liquid Chromatography

Ke Li, Fei-Lang Zhao

1994, 3(2): 164-170.

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Studies on the Chemical Components of Panax quinquefolium L, Cultivated in JiIin Province

Ning Shen, Su-Xian Wang

1994, 3(2): 171-171.

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