Table of Content

15 June 1995, Volume 4 Issue 2

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Full Papers

Isolation and Identification of Eleven Tertiary Alkaloidsin Corydalis decumbens

Jing Liao^*, Wen-Zao Liang, Guo-Shi Tu

1995, 4(2):  57-61. 

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Eleven tertiary alkaloids were isolated from Corvdalis decumbens rhizome Their structures were identified as protopine (VII), allocryptopine (VIII), cryptopine (IX), muramine (XVII); (+)-tetrahydropalmatine (Ⅲ), (+)-kikemanine (IV), (-)-scoulerine (XVIII), (-)-bulbocapnine (XIX), and (-)-capnoidine (I), (-)-bicuculline(V), (+) coriumidine (XIV), respectively. Among these, cryptopine, muramine, (+)-kikemanine, (-)-scoulerine, (-)capnoidine, (-)-bicuculline were isolated for the first time from this plant.

Preparation of Liposomes with Palmitic-Antibody and Targeting in Vitro

Xin-pu Hou, Bao-Ming Ning, Xing-Zheng Gao

1995, 4(2):  62-66. 

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An anti-trichomonas vaginalis monoclonal antiboody was derivatized with palmitic acid using an activated ester of N-hydroxysuccinimide About 50% of the resulting antibody could be incorporated into liposomes. The liposomes showed specific binding to T. vaginalis by IFA and cytotoxicity tests. These results clearly demonstrated the effectiveness of targeting of liposomes modified by monoclonal antibody in vitro.

Antithrombotic Effects of BM-13505, a ThromboxaneReceptor Antagonist

Fu-Jun Wang, Shi-Ling Zhang

1995, 4(2):  67-74. 

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BM-13505 is a new type of thromboxane receptor antagonist developed first abroad and synthesized in our school, with a modifed method recently. The results of our study showed that the occlusion time of carotid artery in experimental thrombosis rats was prolonged by BM-13505, 0.45 and 0.23 mg/kg iv (P<0.00 1 and <0.01 respectively). BM-13505 2 mg/kg iv effectively prevented the cerebral thrombosis caused by AA 4 mg/kg in rats (P<0.01) BM-13505 10 mg/kg ip prevented the AA-induced pulmonary thrombosis in mice (P<0.01). Tail bleeding time of mice was prolonged by this dru.BM-13505 significantly inhibited the AA-induced rabbit platelet aggregation, with an IC50 of 0.17 μmol/L; ADP-and collagen-induced aggregations were not affected.TXB2 level in platelets and that in mice plasma were decreased by BM-13505, but cAMP level in platelets was not affected. BM-13505 may be possibly developed into a useful anti-platelet and anti-thrombotic drug.

Metabolism of Praziquantel in Erythromycin, Acetylspiramycin and Dexamethasone Induced Rat Liver Microsomes

Liang-Li Zhao^*, Wan-Yun Huang, Yu-Zhu Quan

1995, 4(2):  75-81. 

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Our results show that in liver microsomes from erythromycin, acetylspiramycin and dexamethsone pretreated rats, the rate of praziquantel (PQT)disappearence was increased as compared with control rat When microsomes from erythromycin-treated rats were exposed to PQT in the presence of potassium ferricyanide which broke down the cytochrome P-450 Fe(II)-metabolite complexes and restored the functional cytochrome P-450, PQT metabolism was further increased. Acetylspiramycin did not form the complexes, so potassium ferricyanide showed no effect on the PQT metabolism in microsomes from acetylspiramycin-treated rats. Triacetyloleandomycin, a specific inhibitor of cytochrome P-450 III Al, inhibited PQT metabolism by 53% in liver microsomes from dexamethasone-treated rats.These results indicate the cytochrome P-450 III Al seems to be involved in metabolism of PQT in rat liver microsomes.

Induction of Erythroid Differentiation of HumanErythroleukemia K-562 Cells by Mutactimycin

Qi Wu^*, Dian-Dong Li, Yong-Su Zhen

1995, 4(2):  82-88. 

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Mutactimycin, a new anthracycline antibiotic, consists of 5 components: mutac-timycin A, B, C, D and 7-deoxymutactimycinone A. Mutactimycin components differ from each other in suppressing proliferation and inducing differentiation of human erythroleukemia K-562 cells. Determined by benzidine staining, the percentage of K-562 cells with hemoglobin expression was86% by mutactimycin C. The peak percentage of benzidine positive cells appeared on day 5 or 6.The differentiated cells were partially reversed after drug removal.The induced cells lost the clonogenicity in soft-agar. The kinetics of differentiation induced by mutactimycin C, in comparison with other known anthracycline antibiotics, was similar to that by doxorubicin, epirubicin anddaunorubicin. Mutactimycin C was more active than aclarubicin A. The structure-activity relationship for mutactimycin components suggested that the substituting groups on C3, C11, and the saccharide on C7 might be important for their activities.

Protective Effect of phytolacca Acinosa Polysaccharides I(PAP-I) on Hematopoiesis in Cyclophosphamide-treated and ⁶⁰Co-irradiated Mice

Hong-Bin Wang, Qin-Yue Zheng, Sheng-Chuan Sun, Bao-Yun Liu, You-An Shen, Hui-Lan Tang, Dian-Wen Ju, Jun Fang

1995, 4(2):  89-98. 

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The protective effect of a kind of purified polysaccharides extracted from Radix of Phytolacca acinosa Roxb, with a molecular weight of 10 KDa, on hematopoiesis was investigated.Average survival time of mice treated with cyclophosphamide (CY) 300 mg/kg once alone was 13.3±7.2 d (n = 7) however, average survival time of mice treated with CY 300 mg/kg in com-bination with PAP-1 10 mg/kg, 3 times/wk was 36.7±16.4 d (n = 7, P<0.01). PAP-1, ip had benefi-cial effect on the recovery of the CY induced decrease of peripheral leukocyte number, and the nu-cleated bone marrow cell(BMC)number and [³H]TdR uptaken by BMC induced by rmGM-CSF in S180 bearing mice treated with CY, In mice, after the first ip treatment with CY 100 mg/kg on d7, the peripheral leukocyte number decreased on d9 and recovered to normal level about d13 to d15. Such recovery was accelerated by administrating PAP-1, 10 mg/kg, 3 times/wk. A significant in-crease of the activity to form colony in spleen(colony-forming unit in spleen, CFU-S8, CUF-S12 in mice irradiated with 550 rad ⁶⁰Co γ-rays and an enhancement of proliferative response of BMC to rm GM-CSF treated with PAP-1, 10 mg/kg, 3 times/wk, ip were observed.After PAP-1, 10 mg/kg, ip once, a significant increase in the number of peripheral blood leukocytes and a rise in the serum of colony stimulating factor (CSF) were also confirmed.The types of CSF in serum were M-CSF and other hematopoietic growth factors, which were confirmed by using McAb of IL-3, GM-CSF and PcAb of M-CSF. These beneficial effects of PAP-1 on hematopoiesis may be related to its activityinducing CSFs and other hematopoietic growth factors and warrant further evaluation of its use-fulness.

Hydroxylation Polymorphisms of S-mephenytoin and Debrisoquin in Native Normal Chinese Zhuang Minority Volunteers

Tang-Yong Kuang, Qi-kui Luo, Jia-Mei Zhang, An-Qing Zou, Ya-Qing Lou

1995, 4(2):  99-106. 

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S-mephenytoin and debrisoquin hydroxylation abilities were investigated in 118 normal Chinese Zhuang minority volunteers after co-administration po 100 mg racemic mephenytoin(MP)and 10 mg debrisoquin (DB). The ratio between S-and R-enantiomers of mephenytoin in urinewas determined by implication of GC-NPD and used as the measure of the drug hydroxylation. 2 ofthe 118 subjects had S/R ratios greater than 1.0 and were poor hydroxylators of S- mephenytoin. The frequency of S-mephenytoin poor metabolizers (PM) was 10.2%. No PM of debrisoquin was found in the volunteers. It indicated that there was no relationship between S-mephenytoin P(4')-hydroxylation and debrisoquin 4-hydroxylation polymorphisms in Chinese Zhuang Minority population. In addition, 16 of the 118 volunteers(4 PMs and 12 EMs of S-mephenytoin) were se-lected to conduct the elimination kinetic studies of racemic mephenytoin and debrisoquin in urine. The pharmacokinetic parameters of S-, R- mephenytoin, DB and 4-OH-DB were calculated.

Effects of Water-soluble Components Isolated from Salvia milltiorrhiza on Oxygen Free Radical Generation and Lipid Peroxidation

Ding-You Li, Li-Na Xu^*, Xiao-Guang Liu

1995, 4(2):  107-112. 

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The effects of water-soluble components isolated from Salvia miltiorrhiza on oxygen free radical prodction and lipid peroxidation were estimated. Five components (10 μmol/L)were shown to inhibit superoxide anion generation by xanthine-xanthine oxidase system. It was also demonstrated that six components (100 μmol/L) prevented H2O2-induced hemolysis and MDA fonnation in mouse erythrocytes.The effects of Sal A, Sal B, Sal C and Ros A were dose dependent. In Langendorff rat heart, pretreatment with Sal A 20 μmol/L significantly prevented MDA production induced by 30 min reoxygenation after 45 min anoxia.The results indicated that there were also other potent antioxidant componentts in Salvia milliorrhiza besides Dphl and Pal. The protection of Sal A against myocardial anoxiareoxygenation inury may be mainly ascribed to its oxygen free radical scavenging activity.