Journal of Chinese Pharmaceutical Sciences

Quantitative Stucture-Activity Relationship Studies on Calmodulin Antagonists of Alkylamino 1,2-Diphenylethvl-ene Compounds

Xiao-Ping Lei^*, Chong-Hua Li, Hai-Zhen Zhong, G.Mrugacz, A.Sobieszek, R.E.Reid

1996, 5(4): 169-173.

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6-Amino-1.2-diphenylhex-1-ene is considered to be a new type of lead com-pound and structure-activity relationships for 15 calmodulin antagonists of alkylamino1.2-diphen-ylethylene compounds have been reported It has been found that the cis isomers generally show greate ractivity than the transisomers,and the reduced compound is the least active Inhibitory activity increases with the length of the alkyl chain separating the aromatic hydrophobic center from the basic center It is suggested from QSAR analysis that compounds Which have high hydrophobic parameter and with electron-donating substituents on the benzene ring may exhibit more potent in-hibitory activity.

The Antithrombotic Effects of P6A and its Derivatives

Yin-Ye Wang, Ming Zhao, Shi-Qi Peng^*, Chang-Ling Li, Qin-Lu Zhou, Qiang Li

1996, 5(4): 174-176.

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P6A was able to increase coronary blood flow and improve hemodynamics in the coronary thrombosis model of dogs In the binding of fibrinogen to GP IIb/IIIa, RGD is the key sequence In the present paper the effects of the coupling compounds of P6A and its derivatives, QP6A with RGDS, RGDV and RGDF were tested The effects of the coupling compounds so obtained on carotid thrombosis in rats were investigated At the dose of 5 μmol/kg, RGDS and RGDV exhibited no antithrombotic effects, whereas at 2.5 μmol/kg RGDF decreased the dry-weight ofthrombus significantly On the other hand, P6A(5 μmol/kg)and QP6A(2.5 μmol/kg)showed significant antithrombosis activities.All of the coupling compounds, except P6A-RGDF and QP6A-RGDF, had potent antithrombosis effects.

Isolation and Identification of Ecliptasaponin A andEcliptasaponin B from Eclipta alba (L.) Hassk

Mei Zhang^*, Ya-Yan Chen

1996, 5(4): 177-181.

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Two new triterpenoid glucosides ecliptasaponin A (3) and ecliptasaponin B (4) were isolated together with echinocystic acid (1) and oleanolic acid (2) from Eclipta alba (L.) Hassk.Their structures were deduced as 3β,16α-dihydroxy olean-12-ene-28-oic acid-3β-O-β-D-glu-copyranoside (3) and 3β-O-[β-D-glucopyranosyl(1-4)]-β-D-glucopyranosyl-16α-hydroxy olean-12-ene-28-oic acid 28-O-β-D-glucopyranoside(4), based on spectral analysis and chemical evidences as well as results ofhydrolysis.

Antioxidant Constituents from G. inflata Bat Root

Kun Zou, Yu-Ying Zhao, Nai-Wu Fu, Liang Qiao, Ru-Yi Zhang

1996, 5(4): 182-185.

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Continuing the previous report (1), seventeen compounds were isolated from the roots and rhizoma of Glycyrrhiza inflata Bat. On the basis of spectroscopic methods five of them were identified as sucrose (1), 4’,5,7-trihydroxy-8-prenyl-flavonc (2), liquiritigenin (3), formononetin (4), and glabrone (5) (1), (4) and (5) were obtained from this plant for the first time. Their antioxidant activities were observed in three oxidizing systems in vitro. (2), (3) and (5) showed remarkable activities in scavenging O2^.- (5) exhibited good activity in inhibiting hemolysis induced by H2O2 (3) and (5) displayed higher inhibitory action on (HpD+hv)-induced hemolysis than som typical antioxidants.

A Molecular Approach to Identification of the Chinese Drug“Pu Gong Ying”(Herba Taraxaci) and Six Adulterants by DNA Fingerprinting Using Random Primed PolymeraseChain Resaction (PCR)

Hui Cao, Paul Pui-Hay But, Pang-Chui Shaw

1996, 5(4): 186-194.

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DNA fingerprinting among members of the Chinese drug Pu Gong Ying (Taraxacum mongolicum Hand, -Mazz.) and six adulterants of Tu Gong Ying were demonstrated with random-primed polymerase chain reaction (PCR) including arbitrarily primed polymerase chain reaction (AP-PCR) and random amplified polymorphic DNA (RAPD). Distinctive, reproducible genomic fingerprints from DNA from 7 species belonged to Compositae were generated with two long (20 and 24 mer) and one short (10 mer) randomly chosen primers.The Pu Gong Ying can be differentiated from six species of Tu Gong Ying according to the banding pattems of their amplified DNA on agarose gels.The results showed that AP-PCR and RAPD methods can be used for identifying Chinese drugs.Moreover, the Similarity Indexes of the genomic DNA fingerprints showed that Pu Gong Ying and its adulterants are unrelated.Therefore, AP-PCR and RAPD methods can be used for identifying Chinese drugs.

Two Minor Saponins from Leaves of Panax ginseng C. A. Meyer

De-Qiang Dou, Ying-Jie Chen, Zhi-Yun Meng, Ye Wen, Yu-Ping Pei, Sui-Xu Xu, Xin-Sheng Yao, Hiroyuki Kawai, Hideaki Fukushima, Yasunobu Murakami

1996, 5(4): 195-199.

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Two minor saponins were isolated from the leaves of P. ginseng and their struc-tures were elucidated as 3β, 12β, 20(S)-trihydroxyl-dammar-24 (25)-ene-(20-O-α-L-arabinofurano-syl (1→6)-β-D-glucopyranosyl)-3-O-β-D-glucopyranoside (1), and 3β, 12β, 20(S)-trihydroxyl-dam-mar-24 (25)-ene-(20-O-α-L-arabinopyranosyl (1→6)-β-D-glucopyranosyl)-3-O-β-glucopyranoside (2), respectively The fonner corresponds to notoginsenoside-Fe which is isolated for the first time from the title plant The latter is a new natural product and named as ginsenoside-Rd2.

Mitoxantrone Ethylcellulose Microspheres for Liver Arte-rial Embolization

Zhi-Rong Zhang, Dan Wang, Fang-Yi Liao, Gong-Tie Liao

1996, 5(4): 200-206.

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Herein, the orthogonal test was used to optimize the preparation conditions and technique of mitoxantrone ethylcellulose microsphere (DHAQ-EC-MS)for liver arterial embolization.The dynamic dialysis method was used to study the drug release characteristics ofthe DRAQ-EC-MS.The suspension of DHAQ-EC-MS for clinical liver arterial embolization was prepared.The results show that the DHAQ-EC-MS is regular in morphology with a mean diameter of 110.24±38.19 μm and 86.5% of them within the range of 40-150μm, The drug loading is 12.5% and the embedding ratio is 55.6%. The release characteristics were in accordance with the single exponential model.The drug release equation is log(Y∞-Y) = -0.116t - 1.198 × 10^-3 (r = 0.9992, t50 = 2.6 h). The suspension is ofstable physical and chemical properties and is suitable for clinical use.

Effect of Fish Oil on Left Ventricular Function in Anes-thetized Rats

Fang Zhang, Jian-Zheng Zhou^*, Bao-Jie Wu, Xiu-Mei Zhang

1996, 5(4): 207-212.

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The effect of fish oil on the basal left ventricular function and changes of left ventricular function induced by isoproterenol (ISO) were demonstrated in our study. The detennina-tion of cardiac perfonnance in vivo showed that supplementation with fish oil (EPA and DHA, 70%, 1.4 ml/kg) had no significant effect on basal cardiac perfonnance, while it could significantly inhibit changes of +dp/dtmax, Vpm and HR induced by ISO (0.4 μg/ kg, 4.0 μg/ kg, 40 μg/ kg) intrave-nously.The results suggested that supplementation with fish oil perhaps affected the function of β-adrenoceptors on rat myocardial membrane.

A Pre-column Derivatization HPLC Method for the De-termination of Peimine and Peiminine in Bulbus Fritillar-iae

Wen-Yan Li, Kai-Shun Bi^*, Yan-Jiang Qiao, Li-Li Ning, Xu Luo

1996, 5(4): 213-218.

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A pre-column derivatization HPLC method for the determination of peimine(P)and peiminine(PE)in Bulbus Fritillariae has been developed. Under the derivatization conditions optimized, the calibration curve is Y1 = -3.83×10³ + 1.33×10⁵X1, r = 0.998, for P and Y2 = -7.86×10² + 6.33×10⁴X2, r = 0.995 for PE, where Y is the peak area and X is the weight of the alkaloid; the average recovery is 98.0% (n = 5, RSD = 2.1%) for P and 101.0% (n = 5, RSD = 4.1%) for PE, the linear range is from 0.504 μg to 3.126 μg for P and from 0.520 μg to 3.328 μg for PE, respectively. Results of the determination of the two alkaloids in several samples of different Fritillaria species from various parts of the country are presented. The results suggest that P and PE are two major chemical constituents in bulbs of different Fritillaria species, and that the method developed is generally applicable to the determination of the hydroxy group on aliphatic fused ring systems without steric hindrance.

Collaborative Study of Candidata National Standards for Recombinant Human Tumour Necrosis Factor Alpha (thTNF-α) Analogs

Ying lin, Hui-Lan Chang, Kang-Sen Xu, Bing Zhou, Fang Deng, Zheng-Min Zhang, Yi-Ping Chen

1996, 5(4): 219-224.

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New Tannins from Lythrum Salicaria L.

Xiu-Jing Ma^*, Chun-Ru Ji, Yu-Ming Wang, Guang-Qiang Zhang, Yan-Ze Liu

1996, 5(4): 225-225.

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