Cinobufacino injection is a significant anti-tumor medicine for the treatment of various tumors in clinic, which was made from water extraction of the skin of Bufo bufo gargarizans. In present paper, HPLC-DAD-FT-ICR-MS method was used to identify the major bufadienolides in cinobufacino for the first time. Solid-phase extraction with dichloromethane and silica was used to enrich the total bufadienolides in cinobufacino. Based on the UV and high resolution MS/MS data, 33 bufadienolides were analyzed and characterized. Among them, eight compounds were identified by comparing with standard references unambiguously. This study elucidated the major bufadienolides in cinobufacino, which provided material foundation of cinobufacino and will be benefit for the further pharmacological research.
Amphibian Venoms ; chemistry ; Animals ; Bufanolides ; analysis ; chemistry ; Bufo bufo ; Chromatography, High Pressure Liquid ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry

To obtain chemical constituent information of rat plasma after oral administration of Huang-Lian-Jie-Du Decoction (HLJDD), a LC-FT-ICR-MS method has been established, and both positive and negative ions scan modes were include in the analysis. By comparing their retention time, high resolution mass data of HLJDD extracts, blank plasma and dosed plasma, 38 constituents, including 22 prototype compounds and 16 metabolites, were detected in rat plasma after oral administration of HLJDD. In the 22 prototype compounds, 16 constituents were determined unambiguously by comparing with references. In the analysis of metabolites, phase II reactions like glucuronidation and sulfation were the major biotransformation pathways of HLJDD. M11 was observed as the only phase I metabolite in present experiment. The results will be beneficial for the further pharmacokinetics and pharmacological evaluations of HLJDD.
Administration, Oral ; Alkaloids ; blood ; Animals ; Biotransformation ; Chromatography, High Pressure Liquid ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; metabolism ; Flavonoids ; blood ; Iridoids ; blood ; Male ; Plants, Medicinal ; chemistry ; Rats ; Rats, Sprague-Dawley ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry

Autophagy is a common phenomenon which widely ex-ists in eukaryotic cells. Researches have shown that autophagy plays a critical role in maintaining cellular hemostasis, cell com-ponents update and keeping a normal physiological state. In re-cent years, the study has found that autophagy is closely related to the growth, the development of cardiovascular diseases and tumors. Further studies show that in different pathological condi-tions, autophagy could both promote angiogenesis and inhibit the formation of blood vessels. Therefore, it is particularly critical to elucidate the mechanisms of autophagy in the regulation of angio-genesis in different pathological conditions. The role of autophagy in cardiovascular diseases especially in the regulation of angio-genesis is discussed in this paper. Besides, the paper also in-cludes the discussion about the mechanisms of autophagy in the regulation angiogenesis, which may provide references for follow-up research and clinical treatment.

Objective To investigate and evaluate the changes of T lymphocytes and red cell immunity of peripheral blood in patients with primary hepatocyte carcinoma (PHCC) after radiofrequency ablation(RFA) treatment. Methods The pre- and post- RFA(3d,7d,14d) peripheral blood T lymphocyte subsets(T3,T4,T8,T4/T8) and red cell immunity (RBC C3 receptor flower and RBC-immuocomplex formation rate) were investigated in 120 patients with PHCC treated by RFA. Results On 7d, 14d after RFA, T3, T4 lymphocytes and T4/T8 were higher than those on preoperative day significantly(P

OBJECTIVETo compare the solubilities of ephedrine and d-pseudo-ephdrine in the compound of traditional Chinese drugs--Maxing Shigan decoction with and without ultramicro-pulverizations using a RP-HPLC procedure.

METHODThe analytical column was a YMC ODS-C18(4.6 mm x 150 mm,4 microm). A mixture of water-acetonitrile-sodium dodecyl sulfate-phosphorous acid (650:350:5:1) was used as the mobile phase at flow rate of 1.5 mL x min(-1). The column temperature was 50 degrees C and the wavelength was 210 nm.

RESULTIn this way, ephedrine and d-pseudo-ephedrine of the compound samples can be separated well and showed significant differences before and after the ultramicro-pulverizations.

CONCLUSIONFor the Maxing Shigan decoction, the dissolution rates and solubilites of ephedrine and d-pseudo-ephedrine ultramicro-pulverization were greatly improved.

Calcium Sulfate ; chemistry ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; isolation & purification ; Ephedra ; chemistry ; Ephedrine ; analysis ; chemistry ; Glycyrrhiza uralensis ; chemistry ; Particle Size ; Plants, Medicinal ; chemistry ; Powders ; Prunus ; chemistry ; Solubility ; Technology, Pharmaceutical ; methods

Cinobufacino injection is purified from water extraction of the skin of Bufo bufo gargarizans, which has been widely used for various cancers in clinic with significant anti-tumor effects. Bufadienolides were regarded as the main active constituents of cinobufacino injection in previous reports. In present study, 6 bufadienolides were isolated and purified from Cinobufacino injection. Their structures were identified as 3-epi-ψ-bufarenogin (1), ψ-bufarenogin (2), 3-epi-arenobufagin (3), arenobufagin (4), 3-epi-gamabufotalin (5), and 3-oxo-arenobufagin (6), separately. Among them, 1 and 3 were new compounds, 5 and 6 were new natural products. Compounds 1, 2 and compounds 3, 4 were two pairs configuration isomers at C-3, separately.
Animals ; Bufanolides ; chemistry ; isolation & purification ; Bufo bufo ; Injections ; Skin ; chemistry

In order to clarify the metabolism pathways of scandoside methyl ester, the analysis of metabolites profiling in four kinds of liver microsomes was performed by using an ultra-performance liquid chromatography/ electrospray-tandem mass spectrometry (UPLC-ESI-MS). The data obtained from the 0 h-incubation and the 2 h-incubation were compared and analyzed. After incubation, 5 metabolites of scandoside methyl ester were found in rat, Beagles, rhesus monkey and human liver microsome. The results showed that scandoside methyl ester's major metabolic pathway in the liver microsomes is hydrolysis, oxidation and reduction reactions, and there are certain kinds differences between species. The study provides a research base for further research about iridoid compounds in vivo metabolic pathways.
Animals ; Chromatography, High Pressure Liquid ; Dogs ; Esters ; metabolism ; Humans ; Iridoids ; metabolism ; Macaca mulatta ; Microsomes, Liver ; metabolism ; Rats ; Spectrometry, Mass, Electrospray Ionization

OBJECTIVETo optimize the molding formula of refined Xiong-gui sustained release pills, types and assorted dosages of water-soluble and non water-soluble drug carrier were studied.

METHODAn orthogonal design was performed to sift the pill formulation. The processing conditions were determining in terms of roundness, hardness, viscosity, fluidity, easily drop.

RESULT AND CONCLUSIONAccording to the final optimal formula, the amount of drug release can be detected instantly, while remaining over 80% at 10 h.

4-Butyrolactone ; analogs & derivatives ; analysis ; Angelica sinensis ; chemistry ; Delayed-Action Preparations ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; isolation & purification ; Ligusticum ; chemistry ; Plants, Medicinal ; chemistry ; Technology, Pharmaceutical ; methods

OBJECTIVETo observe the protective effects of the Huanglian Jiedu decoction aqueous extract and its active fraction, which consists of total alkaloids, total flavonoids and total iridoid, on the thalamus of cerebral ischemia in rats.

METHODThe rat model of middle cerebral artery occlusion (MCAO) was chosen. Male SD rats were randomly divided into sham-operation group, model group, aqueous extract group (800 mg x kg(-1)), total alkaloids group(44 mg x kg(-1)), total flavonoids group (50 mg x kg(-1)) and the total iridoid group (80 mg x kg(-1)). The rats were administered the appropriate drugs intragastrically once a day, for 7 days after surgery. An equivalent volume of saline was given in the sham surgery and model groups. The HE staining was adopted to observe the pathological changes. Determination of Glu and gamma-GABA in thalamus were detected by HPLC with fluorescence detection. The expression of GAD65 was examined with immunohistochemistry and double staining with uorescent-conjugated antibodies against GFAP and Cx43 was chosen in this study.

RESULTThe neurons degenerated in MCAO rats after cerebral ischemia 7 d. The content of Glu, gamma-GABA decreased (P < 0.05), the expression of GAD65 reduced (P < 0.05) and the expression of GFAP and Cx43 increased (P < 0.01) in thalamus of rats compared with sham-operation group. Huanglian Jiedu decoction aqueous extract, total alkaloids, total flavonoids and total iridoid reduced the degeneration of neurons. Total flavonoids could promote the expression of GAD65 (P < 0.05) and decrease the expression of GFAP and Cx43 (P < 0.01) in thalamus compared with model group while it could also increased the content of Glu,gamma-GA BA to normal levels. Compared with model group, Huanglian Jiedu decoction aqueous extract, total alkaloids and total iridoid could raise the expression of Cx43, and Huanglian Jiedu decoction aqueous extract could also increase the expression of GAD65 (P < 0.05). The expression of GFAP in Huanglian Jiedu decoction aqueous extract group, total alkaloids group and total iridoid group were not different compared with model group while the content of gamma-GABA decreased (P < 0.05) compared with sham-operation group.

CONCLUSIONThe degeneration of nerve cells, the reduction of neurotransmitter amino acids content, the aberrant activation of astrocytes and the abnormal expression of GFAP and Cx43 will appear in thalamus of MCAO rats after ischemia. Huanglian Jiedu decoction total flavonoids could relieve the injury of nerve cell through inhibiting the abnormal activation of astrocytes and regulating the expression of GFAP and GAD65.

Animals ; Astrocytes ; drug effects ; Disease Models, Animal ; Drugs, Chinese Herbal ; pharmacology ; Infarction, Middle Cerebral Artery ; drug therapy ; Male ; Protective Agents ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Thalamus ; drug effects

OBJECTIVETo isolate and identify the chemical constitutents in roots of Jasminum sambac.

METHODThe compounds were isolated by means of chromatography and the structures were identified on the basis of physical and spectral data.

RESULTDotriacontanoic acid, dotriacontanol, oleanolic acid, daucosterol and hesperidin were elucidated.

CONCLUSIONAll compounds were found in this plant for the first time.

Hesperidin ; chemistry ; isolation & purification ; Jasminum ; chemistry ; Oleanolic Acid ; chemistry ; isolation & purification ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Sitosterols ; chemistry ; isolation & purification