Journal of Chinese Pharmaceutical Sciences

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2008, 17(3): 173-176.

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Enantioselective analytical methods in chiral drug metabolism

Yan-Jun Hong, Ling-Bo Gao, Su Zeng^*

2008, 17(3): 177-182.

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The chiral nature of biological systems enables their stereoselective interaction with chiral compounds. It has been well documented that the enantiomers of a chiral drug may show differences in drug disposition especially in metabolic behavior. As a result, it is of vital importance to separate the enantiomers of a chiral drug in metabolic studies. This paper discusses enantioselective methods (include high-performance liquid chromatography, gas chromatography, capillary electrophoresis and high-performance liquid chromatography-mass spectrometry) that applied in chiral drug metabolism, using most recent examples where possible.

Application of high-titred IgY antibodies in orthopox virus diagnostics

Xiao-Ying Zhang^*, Andreas Kurth, Diana Pauly, Georg Pauli, Rüdiger Schade, Heinz Ellerbrok

2008, 17(3): 183-191.

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Layer chickens were immunized with three species of inactivated orthopox virus (vaccinia virus, calpox virus and cowpox virus). Antibodies (IgY) were purified from egg yolks by improved polyethylene glycol precipitation. The development of IgY directed against orthopox virus antigens was followed by immunofluorescence assay, plaque reduction neutraliztion test and immunoelectron microscopy. Cross-reactivity of two IgY antibodies with cells infected by the different strains of the pox viruses was also investigated by different methods (immunofluorescence assay, plaque reduction neutraliztion test and Western blot). Even in very high dilutions in immunofluorescence assay (titres up to 1:106 and 1:105, respectively) and persisted on a plateau over 10 months after four booster injections, it was showed that anti-vaccinia virus IgY and anti-calpox virus IgY were positive. Neutralizing activity and ultra-structural detection of antigen with gold-labelled antibodies were respectively observed in plaque reduction neutralization test and immunoelectron microscopy. Western blot analysis revealed specific binding of IgY to virus proteins. Thus, there was cross-reactivity between different orthopox viruses. Finally, orthopox virus-specific IgY antibodies bounded magnetic beads (Dynabead) were used to concentration of orthopox viruses. This study suggests that anti-pox virus IgY could serve as a useful tool for orthopox viruses diagnosis.

Augmentative effect of tetrandrine on pentobarbital hypnosis mediated by 5-HT1A and 5-HT2A/2C receptors in mice

Nan Du, Li-En Wang, Xiao-Rong Shi, Xiang-Yu Cui, Su-Ying Cui, Fan Zhang, Yong-He Zhang^*

2008, 17(3): 192-196.

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It has been reported that augmentative effect of tetrandrine on pentobarbital hypnosis in mice may be related to serotonergic system. The present study was undertaken to investigate the interaction of tetrandrine and different 5-HT receptors on pentobarbital-induced sleep by using the loss-of-righting reflex method. The results showed that augmentative effect of tetrandrine on pentobarbital hypnosis in mice were potentiated by the p-MPPI (5-HT1A receptor antagonist) (1 mg/kg, i.p.) and ketanserin (5-HT2A/2C receptor antagonist) (1.5 mg/kg, i.p.), respectively. Pretreatment with either 8-OH-DPAT (5-HT1A receptor agonist) (0.1 mg/kg, s.c.) or DOI (5-HT2A/2C receptor agonist) (0.2 mg/kg, i.p.) significantly decreased pentobarbital-induced sleep time, and tetrandrine (60 mg/kg, i.g.) significantly reversed this effect. These results suggest that both the 5-HT1A and 5-HT2A/2C subfamily may be involved in the potentiating mechanism of tetrandrine’s effects on pentobarbital hypnosis.

Effects of angelica sinensis polysaccharide-iron complex on hemolytic anemia and bone marrow injury in mice

Pei-Pei Wang, Yu Zhang, Kai-Ping Wang^*, Ke Li

2008, 17(3): 197-202.

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To investigate the therapeutic effects of angelica sinensis polysaccharide-iron complex (APIC) on hemolytic anemia and bone marrow injury in mice models. The hemolytic anemia mouse model was established by i.p. of phenylhydrazine (PHZ). Changes of the indices including red blood cell count (RBC), hemoglobin (Hb) and hematocrit (HCT) were determined by blood analyzer, and reticulocytes were observed by brilliant cresol blue staining during administration. Bone marrow injured mouse model was established by i.p. of cytoxan (CY) and chloramphenicol (CH), and the therapeutic effect was observed by H-E staining. The indices of APIC treated groups with the medium and high doses were higher than those of the model group significantly. Moreover, the Hb and HCT were restored to the normal level after drug treatments. In addition, APIC can promote the proliferation and differentiation of reticulocytes obviously in the early stage of anemia mice, decrease adipose cell proliferation in bone marrow of injured mice and hasten the recuperation. In conclusion, APIC has therapeutic efficacy on hemolytic anemia and bone marrow injury caused by chemicals, which is reported for the first time.

Synthesis of nucleoside-peptide conjugate with disulfide bond as linker at C-5 of uridine

Fei-Lin Nie, Xiao-Feng Wang, Yang Liu, Zhen-Jun Yang^*, Liang-Ren Zhang, Li-He Zhang

2008, 17(3): 203-208.

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In order to prepare pyrimidine nucleoside-peptide conjugate concisely, we developed a one-pot synthetic strategy. Started from uridine, 5-S-acetyl-thiomethyl-2',3'-di-O-isopropylidene-uridine (4) was synthesized as the key intermediate in four steps. Under acidic condition, compound 4 was deprotected and reacted with PySS-R (8, 12, 15, Py = 2-pyridyl, R = amino acid or peptide) in one pot to form uridine conjugates (9, 13, 2) with disulfide bond as linker.

Synthesis of allyl 4-O-{3-deoxy-3-[4-benzylaminocarbonyl-1H-(1,2,3)-triazol-1-yl]-β-D-galactopyranosyl}-2-deoxy-2-acetamido-β-D-glucopyranoside as a potential inhibitor of galectin-3

Chen Li, Xiang-Bao Meng, Xiao-Feng Jin, Zhong-Jun Li, Qing Li^*

2008, 17(3): 209-214.

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Allyl 4-O-{3-deoxy-3-[4-benzylaminocarbonyl-1H-(1,2,3)-triazol-1-yl]-β-D-galactopyranosyl}-2-deoxy-2-acetamido-β-D-glucopyranoside, a potential inhibitor of galectin-3, was designed and synthesized using lactose as staring material. The modifications of lactose included in introducing of N-acetamino group at the C-2 position through an azidoiodoglycosylation meanwhile constructing the β-aminolactoside stereoselectively and replacing 3'-OH with substituent 1,2,3-triazolyl group to enhance the affinity toward galectin-3.

Synthesis and activity of hydroxyethylene peptidomimetic inhibitors of human β-secretase

Chao Ma, Yue-Hua Wang, Xiao-Ming Yang, Xiao-Min Zou,Yang Lü, Guan-Hua Du, Ping Xu^*

2008, 17(3): 215-220.

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A series of β-secretase peptidomimetic inhibitors with Leu*Ala hydroxyethylene dipeptide isostere were synthesized and their β-secretase inhibitory activities were measured. The most potent compound N9 showed an inhibitory rate of 59.66% (10 mg/mL). Compound N9 might be further modified by means of computational chemical methodology.

Structural elucidation of a new cembranoid diterpene from the Chinese soft coral Sarcophyton sp.

Wei Bie, Zhi-Wei Deng, Min-Juan Xu, Wen-Han Lin^*

2008, 17(3): 221-224.

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To investigate the cembranoid diterpenes from the soft coral Sarcophyton sp. collected in the South China Sea. Repeatedly column chromatography was performed for the isolation and purification. The structures were elucidated on the basis of extensive spectral data (IR, MS, 1D- and 2D-NMR) analysis by comparing with literature data. A new cembranoid diterpene namely sarcophyolide A (1), together with 7α, 8β-dihydroxydeepoxysarcophine (2) were isolated from this species. The cembranoid diterpenes with γ-lactone could be chemotaxonomic markers of Sarcophyton sp.

Chemical composition and anti-MRSA activity of the essential oil from Chinese eaglewood

Wen-Li Mei, Yan-Bo Zeng, Jiao Wu, Hai-Bin Cui, Hao-Fu Dai^*

2008, 17(3): 225-229.

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To analyze the constituents of essential oil from Chinese eaglewood [resinous wood of Aquilaria sinensis (Lour.) Gilg] and its anti-methicillin-resistant Staphylococcus aureus (MRSA) activity. The essential oil was extracted by water-steam distillation and analyzed by GC/MS method. The relative contents of the compounds were determined by normalization. The compounds were characterized by NIST05 and WILEY275L database matching and comparison of their MS spectra with those of literature data. Antibacterial activity of the oil was assayed by the filter paper disc agar diffusion method. The oil showed significant antibacterial activity against MRSA. Sixty-six chromatographic peaks were detected, among them thirty compounds comprising 59.80% of the total essential oil were characterized. Twenty-six compounds comprising 54.26% of the oil were identified as sesquiterpenes. β-Agarofuran (8.96%), kusunol (7.82%), (-)-jinkoh-eremol (5.04%), agarospirol (4.53%), baimuxifuranic acid (4.09%) were the major sesquiterpenes. Four nor-sesquiterpenes and some other sesquiterpenes, such as 10-epi-γ-eudesmol, α-agarofuran, epi-ligulyl oxide, etc. were detected in Chinese eaglewood oil for the first time. This is the first report about anti-MRSA activity of Chinese eaglewood oil from A. sinensis.

Analysis of principal isoflavone glycosides and aglycones in Radix astragali

Xin-Gang Du, Yan-Jing Bai, Bin Wang, Yu-Ying Zhao, Qing-Ying Zhang^*, Lu-Qi Huang

2008, 17(3): 230-235.

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Two major isoflavone glycosides [calycosin 7-O-β-D-glucopyranoside (1) and ononin (2)] and their aglycones [calycosin (3) and formononetin (4)] were simultaneously quantified with HPLC/DAD method. Two unknown compounds were identified as calycosin 7-O-β-D-glucopyranoside-6'''-O-malonate (U1) and formononetin 7-O-β-D-glucopyranoside-6'''-O-malonate (U2), respectively, with LC/MSn. Raw Radix astragli were shown to have higher contents of isoflavone glycosides (1, 2), but lower contents of aglycones (3, 4) than the processed herbal materials. After being moistened with water and stored up for 24 h at 35 ºC, the glycosides and their malonates were almost completely transformed to their corresponding aglycones. The different contents of the isoflavone glycosides and their aglycones in raw and processed Radix astragali materials might be due to enzymolysis of the glycosides during processing.

Determination of ganoderic acids in rat plasma after oral administration of total triterpenoids from Ganoderma lucidum

Bin-Bin Xue, Xiao-Yu Guo, Qing-Ming Che^*

2008, 17(3): 236-240.

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To investigate the absorption of total triterpenoids from Ganoderma lucidum in rats. HPLC-DAD and LC-MS methods were used to identify ganoderic acids in rat plasma after oral administration of total triterpenoids from G. lucidum by comparing their HPLC retention behaviors, UV absorption spectra, and mass spectra with authentic samples. Five ganoderic acids, ganoderic acid C2, C6, G, B and A were simultaneously detected in rat plasma. Ganoderic acids can be directly absorbed into circulation after oral administration of total triterpenoids from G. lucidum in rats.

A continued study on the bisoprolol and isosorbide dinitrate transdermal patches: cardiovascular protection in spontaneously hypertensive rats

Wei Wei, Ji-Hua Fu^*, Chang-Hai Su , Ying Shan, Yuan Wang, Shu-Jia Kong, Ji-Hui Zhao, Wan-Liang Lu^*^*, Shu-Ming Wang, Li Wang

2008, 17(3): 241-248.

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The objective of the present study is to examine cardiovascular protective action of a newly developed transdermal patch by incorporating bisoprolol and isosorbide dinitrate in spontaneously hypertensive rats. As the combination therapy with these two synergistic drugs at low doses through a suitable form of administration could provide optimal therapeutic benefit, we further evaluated the effects of a 42 d period of anti-hypertensive treatment in spontaneously hypertensive rats. Rats were divided into the following five groups: control (blank patch), bisoprolol fumarate tablets (BP-FT, 20.0 mg/kg, i.g.), bisoprolol transdermal patch (BP-TP, 20.0 mg/kg), isosorbide dinitrate transdermal patch (ISDN-TP, 20.0 mg/kg), and the combination of BP and ISDN in a transdermal patch at low doses (8 and 12 mg/kg, respectively). The effects of treatment were evaluated via biochemical indicators related to cardiovascular protection, structure and function. The combination therapy had synergistic anti-hypertensive effects and significantly reduced blood pressure with the benefit of controlling blood pressure variability compared to BP-FT and BP-TP. The combined treatment also reduced heart rate as well as BP-FT and BP-TP, while ISDN-TP had no evident effects on blood pressure, heart rate, and cardiovascular protection. Combination therapy was superior to BP-TP and BP-FT at increasing blood atrial natriuretic peptide and nitric oxide, while also reducing cardiac hydroxyproline and endothelin-1 with no difference in blood endothelin-1 and cardiac malondialdehyde levels. Cardiovascular remodeling differed among the groups, with the combination therapy reducing cardiac hypertrophy and the aortic media/lumen ratio. The consequential improvements in relaxation in response to cumulative concentrations of acetylcholine may explain the associated improvement in endothelial function. Combination treatment with a transdermal patch exhibited a synergistic therapeutic effect. Such favorable cardiovascular effects with nitric oxide donors and β-blockade combination through a transdermal patch may provide long-term cardiovascular protection during anti-hypertensive treatment.

Simultaneous determination of four active compounds in Dangguilonghui tablet by high-performance liquid chromatography

Chun-Li Hu, Dong-Mei Wang, Peng Zhang, Huai-Qing Zhao*

2008, 17(3): 249-253.

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high-performance liquid chromatography (HPLC) method has been developed for the first time to simultaneously quantify the four active ingredients, namely aloin, baicalein, aloe-emodin and wogonin, in Dangguilonghui tablet. The marker compounds were separated on the Diamonsil C18 column at a flow rate of 1.0 mL/min with a mobile phase of methanol-acetonitrile-0.3% aqueous phosphoric acid (220: 4: 200, v/v/v) and while the detection wavelength was set at 225 nm. The assay was linear over the range of 1.450 - 29.00 μg/mL (r = 0.9992) for aloin, 0.4050 - 8.100 μg/mL (r = 0.9994) for baicalein, 0.1100 - 2.200 μg/mL (r = 0.9997) for aloe-emodin, 0.2160 - 4.320 μg/mL (r = 0.9991) for wogonin, respectively. The average sample recoveries at three concentration levels were 100.7% (RSD = 0.88%), 101.0% (RSD = 0.89%), 100.0% (RSD = 1.3%) and 100.1% (RSD = 1.1%) for these constituents, respectively. This method is suitable for the quality control of Dangguilonghui tablet.

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