Journal of Chinese Pharmaceutical Sciences

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2000, 9(3): 1-01.

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A New Alkaloid from Root of Stemona japonica Miq

Zou Changying^*, Li Jun, Lei Haimin, Fu Hongzheng, Lin Wenhan

2000, 9(3): 113-115.

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From the roots of Stemona japonica Miq., three stemona alkaloids, didehydrostemonine 1, ste-monine 2 and didehydroprotostemonine 3, were isolated by means of extensive Sil gel chromatographic separation. Their structures were identified by spectral analyses (IR, MS, ¹H, ¹³C NMR, ¹H-¹H COSY, NOESY, HMQC, HMBC) as well as 1H NMR line broadening effect. Compound 1 was a new stemona alkaloid, and 3 was a didehydroazaazu-lene alkaloid occurring in S. tuberosa, discovered in the roots of S. japonica firstly.

A New Quinazolone Alkaloid from Leaves of Dichroa febrifuga

Deng Yonghong, Xu Rensheng, Ye Yang^*

2000, 9(3): 116-118.

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A new alkaloid, neodichroine, along with several known alkaloids, a coumarin, a flavanone and vanillin were isolated from leaves of Dichroa febrifuga. Its structure was elucidated by spectral analyses and semi-synthesis from β-dichrone.

Flavone Glycosides from the Leaves of Ginkgo biloba

Tang Yuping^*, Zheng Weiping, Lou Fengchang, Li Yanfang, Wang Jinghua

2000, 9(3): 119-121.

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In addition to apigenin 7-glucoside (1), luteolin 3'- glucoside (2), luteolin 4'- glucoside (3), and chrysoeriol 7-glucoside (4), a new flavone glycoside (5) was isolated from the leaves of Ginkgo biloba. Its structure was established as tricetin 4'-methyl ether-3'-β-D-glucoside by spectroscopic analysis.

Two New Glycosides from Erigeron breviscapus

Zhang Weidong, Chen Wansheng, Wang Yonghong, HA. Thi Bang Tam, Isabella Fouraste, Kong Deyun, Li Huiting

2000, 9(3): 122-124.

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A New Triterpenoid Saponin from Albizzia julibrissin

Zou Kun, Zhao Yuying^*, Zhang Ruyi, Zheng Junhua, Tu Guangzhong

2000, 9(3): 125-127.

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A new triterpenoid saponin named Julibroside J23 was obtained by HPLC from the stem barks of Albizzia julibrissin Durazz. Its structure (1) (See Fig. 1) was elucidated on the basis of chemical and spectral analyses.

A New Phenylpropanoid and Triterpenoids from Prunella vulgaris

Wang Zhuju, Zhao Yuying^*, Wang Bin, Li Jiexiu, Ai Tiemin, Chen Yayan

2000, 9(3): 128-130.

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A new phenylpropanoid (1) together with five known triterpenoids were isolated from the spikes of Prunella vulgaris. Their structures were established on the basis of spectral analysis as 3,4,α-trihydroxy-butyl phenylpropionate (1),2α,3α,24-trihydroxyursa-12,20(30)-dien-28-oic acid (2), 2α,3α, 24-trihydroxyolean-12-en-28- oic acid (3), 2α,3α,24-trihydroxyursa-12-en-28-oic acid (4), 2α,3β-dihydroxyolean-12-en-28-oic acid (5) and 2α,3β-dihydroxyursa-12-en-28-oic acid (6). Five triterpenoids were isolated from this plant for the first time.

A New Triterpene from Rosemary (Rosmarinus officinalis)

Zhou Qunfang, Tu Pengfei^*, Chen Hongming, Xu Zhanhui, Li Gansun

2000, 9(3): 131-133.

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A new triterpene, a-amyrin hexacosoate (I) was isolated together with four known triterpenes, α-amyrenone (II), betulinic acid (III), oleanolic acid (IV) and ursolic acid (V), from the stems and leaves of rosemary (Rosmarinus officinalis L.). The structures were determined by physical and chemical methods.

Two Novel Flavonoids from Ixeris sonchifolia

Feng Xizhi, Xu Suixu, Dong Mei

2000, 9(3): 134-136.

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From the whole plants of Ixeris conchifolia Hance, two novel flavonoids, named luteolin-7-O-β-D- glucuronide methyl ester (1) and apigenin-7-O-β-D-glucuronide methyl ester (2), together with three known flavonoids luteolin (3), luteolin 7-glucoside (4) and apigenin (5) were isolated and their structures were elucidated on the basis of spectral data.

Synthesisof4(R)-(6-Amino-9H-Purine-9-yl)-2(R)-(Hydroxymethyl) tetrahydrofuran-3(R)-ol

Zhao Guisen, Vasu Nair

2000, 9(3): 137-141.

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1-Deoxyribose (5), prepared from D-ribose via methylation, silylation and reductive cleavage, was converted into cyclic sulfite(7). Reaction of 7 with NaN3 resulted in azide (8), which was converted to the isomeric deoxy adenosine, 4(R)-(6-amino-9H-purin-9-yl)-2(R)-(hydroxymethyl) tetrahy-drofuran-3(R)-ol (1) by a sequence of five high-yield reactions. Antiviral studies are in progress.

Preparation and Biodistribution In Mice of Long-circulating Liposomes with Active Carboxylic Terminals

Zhang Yufeng, Zhang Shuo, Hou Xinpu^*, Xie Shusheng, Wang Qi

2000, 9(3): 142-145.

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A new PE-PEG derivative with an active carboxylic terminal, DPPE-PEG3000-COOH, was synthesized and purified. Its incorporation into small unilamellar liposomes composed of egg phosphatidylcholine and cholesterol conferred the liposomes prolonged circulation in blood and reduced accumulation in the RES, as the traditional methoxy-PEG derivatives of PE displayed. With the active carboxylic groups on the surface, DPPE-PEG3000-COOH liposomes can be linked with some active molecules, which provide liposomes with special functions.

In Vitro Drug Release Characteristics of Gelatin Microspheres Containing Zedoary Turmeric Oil for Hepatical Arterial Embolization

Deng Rong , Chen Jimin, Gao Shengchuan

2000, 9(3): 146-150.

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The properties of gelatin microspheres Zedoary turmeric oil (GMS-ZT) in vitro release were studied by the continuous flow system (CFS), which could simulate the actual state in vivo. The effects of sterilization, different flow rates, release medium, the amount of formaldehyde, the duration of cross-linking and the size of microspheres on the drug release were investigated. The results showed that these factors except the sterilization had influences on drug release and the drug release from the microspheres was slow. Eighty percent of the drug released after 12 h, and the release profiles in vitro could be described by the first-order dynamic model, and drug release was controlled by the matrix erosion and diffusion.

Pharmacokinetics of the Enantiomers of O-Demethyltramadol, theActive Metabolite of Trans Tramadol in Healthy Subjects

Liu Huichen, Yang Yanyan, Hou Yanning, Liu Tiejun

2000, 9(3): 151-154.

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In order to investigate the pharmacokinetics of the enantiomers of O-demethyltramadol, the active metabolite of trans tramadol, twelve healthy male volunteers were given multiple oral doses of trans tramadol hydrochloride sustained-release tablets. The enantiomers of O-demethyltramadol in serum were analyzed with high-performance capillary electrophoresis (HPCE). For (+)- and (-)-O-demethyltramadol, Tmax were 3.75±1.25 h and 3.38±1.00 h, Cmax were 18.20±7.31 ng·mL^-1 and 22.80±5.55 ng×mL^-1, and AUC0~t were 162.09±64.96 ng·mL^-1×h and 178.89±46.72 ng×mL^-1×h, respectively. In each subject, the average ratio of (-)/(+)-O-demethyltramadol in the serum at all sampling time points was between 0.89 and 1.90. But at each sampling time point, the average ratio in different subjects was similar. It could be concluded that the stereoselectivity in pharmacokinetics of O-demethyltramadol was different among human subjects.

The Therapeutic Effect of Multiglycosides of Tripterygium wilfordii Hook f. on Autoimmune Syndrome Induced by Campylobacter Jejuni in Mice

Jia Yongfeng, Li Hong, Zhang Luoxiu, Zhang Jianping

2000, 9(3): 155-157.

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The effect of multiglycosides of Tripterygium wilfordii Hook f.(GTW) on autoimmune syndrome (AIS) was studied. Campylobacter fetus ssp jejuni (CF-1) 3.6×10⁹ CFU×mL^-1 was injected intradermally on d0 to induce AIS. GTW 75 and 150 mg×kg^-1×d^-1 were given ig to mice from d14 to d28. Four weeks later, hind paw swelling of mice, serum anti-dsDNA antibody, serum anti-SRBC antibody, spleen lymphocyte proliferation were tested and IL-1 and TNF-α produced from macrophages were evaluated. The results showed that GTW reduced inflammatory swelling, suppressed serum anti-dsDNA antibody, serum hemolysin and spleen lymphocyte proliferation, inhibited IL-1 and TNF-αactivity. All results indicated that GTW had a theraputic effect on AIS in mice.

Effect of Berbamine on Calcium Dynamics in Cultured Vascular Smooth Muscle Cells

Zhao Yanling, Li Xianyi, Li Baiyan

2000, 9(3): 158-161.

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The effects of berbamine (Ber) on intracellular free Ca²⁺ ([Ca²⁺]i) in single cultured aortic VSMC were studied. Cultured VSMCs derived from rabbit aorta were loaded with fluorescent probe Fluo-3/AM and [Ca²⁺]i was measured by LSCM. In the presence of extracellular 2.0 mmol·L^-1 calcium ([Ca²⁺]0), Ber blocked [Ca²⁺]i increase caused by KCl 60 mmol·L^-1, ouabain 1 mmol·L^-1, norepinephrine (NE) 30 mmol·L^-1, serotonine (5-HT) 1 mmol·L^-1 and ATP 30 mmol·L^-1 respectively, and the time before fluorescent intensity (FI) reaches the peak value was also prolonged (P<0.05 or P<0.01). In the absence of extracellular Ca²⁺, Ber had no effect on the mobilization of [Ca²⁺]i induced by caffeine 40 mmol·L^-1. The results suggested that Ber was an effective agent for blocking Ca²⁺ influx caused by opening the VDCC and activating the ROCC but had no effect on intracellular Ca²⁺ release. Ber significantly inhibited the [Ca²⁺]i elevation caused by Ouabain.

Four Stilbene Oligomers from the Roots of Caragana sinica

Luo Hongfeng, Zhang Liping, Hu Changqi^*

2000, 9(3): 162-165.

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