Journal of Chinese Pharmaceutical Sciences

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2001, 10(2): 1-01.

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H3, An Acidic Polysaccharide from Cuscuta chinensis

Wang Zhan, Liu Cuiping, Fang Jinian^*

2001, 10(2): 57-60.

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H3, a homogeneous acidic polysaccharide was obtained from the seeds of Cuscuta chinensis Lam. Its structure was characterized for the first time by chemical and spectroscopic methods to be a highly branched heteropolysaccharide with mean molecular weight of more than 1×10⁶. It was composed of 1,6-linked-β-D Galp, 1,4-linked-β-D Galp, 1,4-linked-β-D GalA, 1,3,6-linked-β-D Galp and 1,2,4-linked Rhap, with branching points at O-2 or O-4 of 1,2,4-linked Rhap and O-3 of 1,3,6-linked-β-D Galp. Its side chains included 1-linked Araf, 1,5-linked Araf and 1,3,5-linked Araf at O-3 of 1,6-linked Galp in the main chain.

The Chemical Constituents of Diterpenoids from Kaempferia marginata Carey

Yu Jingguang, Yu Donglei, Sun Lan, Zhang Shu, Zheng Caicheng, Chen Yuheng

2001, 10(2): 61-64.

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Marginatol (1), a new isopimarene diterpenoid, and five known compounds 8(14),15-sanderacopimaradiene-1α,9α-diol (2), 8(14),15-sanderacopimaradene-1α,6β,9α-triol (3), germacrone (4), trans-ethyl p-methoxycinnamate (5) and n-pentadecane (6) were isolated from the hexane extract of Kaempferia marginata Carey. The structure of marginatol (1) was established as 8(14),15-isopimaradiene-6β-ol on the basis of spectral data (IR, MS, ¹H-¹H, ¹³C-¹H NMR, NOESY and HMBC). Compounds 2, 3 and 4 were isolated for the first time from this plant.

Chemical Constituents of Stellera chamaejasme L

Feng Baomin, Pei Yuehu^*, Hua Huiming

2001, 10(2): 65-66.

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A diterpenoid, neostellerin, was isolated from the roots of Stellera chamaejasme L together with 4 known compounds identified as β-sitosterol, scopoletin, umbelliferone and daucosterol. The structure of neostellerin, which was elucidated by NMR, especially 2D NMR analysis, was different from other daphnane type diterpenes isolated from this plant.

An Effective Procedure for the RAPD Analysis of Hemp Cannabis sativa L.

Song Shujuan, Robert. C.Clarke, Shao Hong

2001, 10(2): 67-69.

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China has a great resource of Cannabis. Research on the taxonomy and morphology of Chinese Cannabis has been carried out, but so far no molecular genetic research has been published. Random amplified polymorphic DNA (RAPD) is a suitable technique for molecular genetic research on Cannabis. In this experiment, using Cannabis herbarium specimens as a source of genetic materials, the correlative conditions of the Polymerase chain reaction (PCR), (i.e., gradient density of Mg²⁺, dNTPs, Taq DNA polymerase, anneal temperature, anneal time and reaction cycles) were examined separately. An effective procedure for the RAPD analysis of Cannabis was obtained.

Purification and Physicochemical Characteristics of Shark Hepatic Stimulator Substance

Guo Yu, Kong Yi, Li Qian, Wu Wutong^*

2001, 10(2): 70-74.

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A hepatic stimulator substance from Shark liver (sHSS) was purified and characterized. The purification procedure included homogenization, centrifugation, ultrafiltration, DEAE-sephadex A25 chromatography and FPLC mono Q chromatography. By the procedure, the stimulatory specific activity of sHSS could be increased to 9000 IU/mg, and was 750 times more than the crude extract. The purity of the final purified fraction F70 which retained the maximal activity of sHSS was checked by polyacrylamide gel electrophoresis in the presence of sodium dodecyl sulfate (SDS-PAGE) and High Performance Gel Filtration respectively, and showed only one band or one peak. Its molecular weight was measured to be 16973 Da by mass spectrometry. Its N-terminal sequence was determined to be N-Met-Arg-Thr-Gln-Glu-His-Thr-Lys- Ser-Val by PE-ABD 491A Protein N-Terminal Sequencing Meter. It was stable over a wide range of pH and temperature.

3α-Bromo-epipicropodophyllin and Its Derivatives: Novel Analogues of Podophyllotoxin with Antitumor Activities

He Yong, Ma Weiyong, Zhang Chunnian

2001, 10(2): 75-80.

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3α-bromo-epipicropodophyllin was prepared and its inhibition activities against KB cells and L1210 leukemia cells in vitro are higher than those of VP-16, a widely used drug in clinic at present. This is the first time to introduce substitution at C-3 of ring-C in the work of modifying structure of podophyllotoxin. It can be transformed easily to 4β-hydroxy-2,3-ene-apopicropodophyllin under basic condition, so that, corresponding derivatives of 2,3-ene-apopicropodophyllin with substitution on carbon-4 could be synthesized. This compound can be regarded not only as a leading compound to be modified because of its antitumor activities, but also as an intermediate for the structure transformation.

The Effects of Unsaturated Factors on Ring C to Chemical Properties of Podophyllotoxin Analogues

He Yong, Ma Weiyong, Zhang Chunnian

2001, 10(2): 81-84.

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Podophyllotoxone, 4β-hydroxy-2,3-en-apopicropodophyllin, and 4-deoxy-4β-azado-2,3-en-apopicropodophyllin can easily transform to 4-hydroxy-dehydropicropodophyllin, dehydroanhydropicropodophllyin and 4-amino-dehydropicropodophyllin respectively in different conditions. These properties remind us to be careful in handling related compounds in similar conditions.

The Preparation of Salbutamol Sulfate Controlled Release Tablets Coated with Cellulose Acetate Aqueous Dispersion

Zhang Fengyu, Wu Tao^*, Pan Weisan, Chen Jimin, Zhang Ruhua

2001, 10(2): 85-89.

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In this study, emulsion-solvent evaporation method was applied to prepare the cellulose acetate (CA) aqueous dispersion. Upon the analyzing of the character of the aqueous dispersion, a controlled release formulation of salbutamol sulfate coated with cellulose acetate aqueous dispersion was prepared through orthogonal experiment design. The factors that control the drug release character of the tablets were investigated. The drug release mechanism of the formulation was also studied. The experimental results indicated that CA aqueous dispersion had excellent film-forming ability under the effect of plasticizer. The drug release profile of the controlled release tablets coated with CA aqueous dispersion exhibited zero-order release character and the drug release rate was modulated by the osmotic pressure of the dissolution medium.

Tissue Distribution and Anti-inflammatory Activity of Dexamethasone Acetate Incorporated In Lipid Emulsion

Quan Dongqin, Cui Guanghua, Dong Huajin, Ruan Jinxiu

2001, 10(2): 90-93.

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Objective: To study the anti-inflammatory activity and tissue distribution patterns of intravenous emulsion of dexamethasone acetate in mice. Methods: The anti-inflammatory solution for injection and Limethasone (Jepanese product) given intravenously were evaluated by using the preformed carrageenan granuloma pouch method in rats. Results: The anti-inflammatory activity of dexamethasone acetate emulsion at low dose of 0.05 mg·kg^-1 was as potent as dexamethasone sodium phosphate solution at high dose of 0.3 mg·kg^-1. The distribution patterns in mice tissues of [³H]dexamethasone acetate emulsion and [³H]dexamethasone sodium phosphate solution in mice were markedly different. Dexamethasone acetate emulsion showed a much higher concentration in the liver, spleen, lung, and inflamed tissues, whereas dexamethasone sodium phosphate had a high concentration in the muscles of vastus lateralis. These results may indicate that dexamethasone incoporated in lipid emulsion was taken up by the reticuloendothelial system and inflammatory cells much more than dexamethasone sodium phosphate solution. Conclusion: When dexamethasone acetate was incorporated in emulsion, the distribution patterns in tissues were changed and they had a stronger anti-inflammatory activity.

The Effect of Electric Properties of Liposomes on SOD-like Activity of Copper Salicylate

Liu Yan, Jia Cai, Hou Xinpu

2001, 10(2): 94-96.

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The SOD-like activities of copper salicylate encapsulated in neutral, positively and negatively charged liposomes were studied with cytochrome c method. The results showed that the SOD-like activity of copper salicylate encapsulated in neutral liposomes was enhanced over 3 times more than that of copper salicylate in aqueous solution. However, the activity decreased for copper salicylate encapsulated in positively and negatively charged liposomes. It was also found that at experimental concentrations there was no regularity for the change of activity of copper salicylate encapsulated in negatively charged liposomes, and copper salicylate encapsulated in liposomes with more negative charges could promote the dismutation of superoxide anion free radicals, however, so could copper salicylate encapsulated in liposomes with fewer negative charges only in lower concentrations.

A Fast Determination of DNA Mutation Induced by Ultraviolet Radiation

Lu Feng, Liu Lili, Zhang Xiaofang, Wu Yutian

2001, 10(2): 97-100.

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Electrophoresis, chromatography, immunoassay, sequencing and other time consuming approaches have been developed to determine DNA base mismatching, oxidative lesion or strand breaks. Sometimes, however, only qualitative information is enough to decide whether mutation has happened to DNA and its extent. Convolution spectrometry (CS), a new technique to discover ultrafine difference on ultraviolet (UV) absorption of different substances, is originally employed to find out any subtle mutation of DNA induced by UV radiation. Mutative DNA is compared with ego criteria based on the spectra of the former DNA, any difference is quantitatively expressed by dispersion (δ). Visible changes cannot be observed on second -derivative spectra until the mutation gets δ up to 11.48%. Dimethyl sulfoxide is an intensifier of UV 254 nm induced DNA mutation and protector at 365 nm, which is simply confirmed by increasing and decreasing δ. Every convolution procedure takes less than 1 min. Convolution spectrometry provides a fast, simple, sensitive and inexpensive alternative to determine DNA mutation, and to screen anti-mutational medicines.

Effects of Losartan on L-type Calcium Current in Hypertrophied Rat Myocytes

Fu Liying, Li Yang, Cheng Lan, Wang Fang, Xia Guojin, Yao Weixing

2001, 10(2): 101-105.

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Objective To investigate the alterations of L-type calcium current (ICa,L) in abdominal aortic ligation-induced hypertrophied rat hearts and the effect of losartan on these alterations. Methods Cardiac hypertrophy was induced by abdominal aortic ligation in rats. To record ICa,L, whole-cell patch-clamp technique was used. Results Membrane capacitance was larger in hypertrophied cells (148±29 pF) than in sham-operated cells (102±14 pF, P<0.01) and losartan-treated cells (118±27, P<0.01). The maximal peak ICa,L was increased from -835±124 pA in sham-operated cells to -1404±417 pA in hypertrophied cells (P<0.01), the corresponding ICa,L density was increased from -7.5±1.8 pA·pF-1 to -10.5±2.2 pA·pF^-1 (P<0.01), while they were reduced to -956±170 pF (P<0.01) and -8.2±1.6 pA·pF^-1 (P<0.05) respectively in losartan-treated cells. The membrane potential of half maximal activation of the hypertrophied cells (-20.6±1.0 mV) shifted to more negative potentials than sham-operated cells (-15.6±1.6 mV, P<0.01) and lorsartan-treated cells (-17.4±1.0 mV, P<0.01). The slope of the activation curve of hypertrophied cells (5.7±0.4) was decreased slightly than sham-operated cells (6.4±0.5, P<0.05). The membrane potential of half maximal inactivation of hypertrophied cells (-27.6±1.9 mV) shifted to more positive potentials than sham-operated cells (-31.4±2.2 mV, P<0.05). The slope of inactivation curves were not different in the three groups. Conclusion Treatment with losartan (30 mg·kg^-1·d^-1, ig) prevented the cell enlargement and the alterations of ICa,L in abdominal aortic ligation-induced hypertrophied rat hearts.

Phytochemical and Bioactive Studies on Conyza blinii

Su Yanfang, Zheng Junhua, Guo Dean, Ma Junjiang

2001, 10(2): 106-108.

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Conyza blinii Lévl. (Compositae), commonly called Jin Long Dan Cao, is distributed in southwest districts of China. Its aerial parts are used in folk medicine for the treatment of chronic bronchitis, gastroenteritis and other inflammatory diseases. Preliminary pharmacological and clinical tests showed that the aerial parts of C. blinii possessed expectorant, antitussive, antiinflammatory and antibacterial effects. Although many other plants of Conyza have been studied phytochemically, there have been rare reports on the chemical constituents of C. blinii. Moreover, studies on the saponins of Conyza plants have not been observed until now. Therefore, we conducted a detailed phytochemical investigation and extensive bioassays on C. blinii.

Studies on the Syntheses and Properties of 5'-Branched-sugar Isonucleosides and the Related Oligonucleotides

Tian Xiao bing, Zhang Lihe, Min Jimei

2001, 10(2): 109-110.

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The chemistry of nucleosides and oligonucleotides is an actively investigated field in the search for new drugs. The syntheses and the properties of isonucleosides and oligonucleotides have been investigated to improve their stability, antitumor and antiviral activities, and to reduce their toxicity.

Synthesis of the Oligosaccharide Fragment of the Surface of Tumor Cell and Its Analogue

Qin Zhihui, Zhang Lihe, Li Zhongjun

2001, 10(2): 111-112.

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Selectins are a new class of carbohydrate-binding glycoproteins which have been identified on the surface of specific cell types,such as leukocytes,platelets and uascular endothelium.It is now known that the selectin-carbohydrate recognition not only play key roles at early stage of the inflammatory reaction ,but also are very important for the invasion and metastasis of tumors.These results suggested that selectin antagonists can be used as anti-adhesive therapeutics to pathological inflammatory conditions,such as reperfusion injury,storke,etc.and will be helpful to the inhibition of the matastasis of tumor cells.

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