Antineoplastic Combined Chemotherapy Protocols ; therapeutic use ; Capsules ; Carcinoma, Non-Small-Cell Lung ; drug therapy ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Integrative Medicine ; Lung Neoplasms ; drug therapy ; Phytotherapy ; Small Cell Lung Carcinoma ; drug therapy

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

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

To identify the active components in Bufo melanostictus Schneider and clarify the difference between fresh and dried Venenum Bufonis, a UPLC-Orbitrap MS method has been established. The separation was performed with gradient elution of acetonitrile and water (with 0.1% formic acid) as mobile phase. By comparing their retention time and high resolution mass data of Venenum Bufonis extracts, 39 effective components were primarily identified by MS/MS analysis in positive ion mode. Twenty-six of them were bufadienolides. There were significant differences in the main composition between fresh and dried Venenum Bufonis. There are fewer bufadienolides in fresh toad venom.
Amphibian Venoms ; chemistry ; Animals ; Bufanolides ; chemistry ; Bufonidae ; Chromatography, High Pressure Liquid ; Tandem Mass Spectrometry

OBJECTIVETo determine the optimum technical parameters through controlling the different factors and the content of Dripping Pill.

METHODTime of dissolution, spherical degree and pill weight as parameters, the influential factors were investigated by orthogonal test and then to determine the content of liensinine, isoliensinine, neferine in plumula nelumbinis Alkaloid Dripping Pill.

RESULTThe optimum condition: 75% PEG4000 as matrix, methyl-silicon oil as refrigerant, 4 cm dripping distance, 10 degrees C refrigerant, 30 drippings per minute.

CONCLUSIONThe good quality pills can be produced through this process and the HPLC determination method is simple, reliable and can be used in the quality control of plumula nelumbinis Alkaloid Dripping Pill.

Alkaloids ; analysis ; chemistry ; Benzylisoquinolines ; analysis ; chemistry ; Chromatography, High Pressure Liquid ; methods ; Isoquinolines ; analysis ; chemistry ; Microspheres ; Nelumbo ; chemistry ; Particle Size ; Phenols ; analysis ; chemistry ; Plants, Medicinal ; chemistry ; Polyethylene Glycols ; chemistry ; Quality Control ; Seeds ; chemistry ; Solubility ; Technology, Pharmaceutical ; methods

In 2005, a program named "Early Detection and Early Treatment of Esophageal and Cardiac Cancer" (EDETEC) was initiated in China. A total of 8279 residents aged 40-69 years old were recruited into the EDETEC program in Linzhou of Henan Province between 2005 and 2008. Howerer, the cost-benefit of the EDETEC program is not very clear yet. We conducted herein a cost-benefit analysis of screening for esophageal and cardiac cancer. The assessed costs of the EDETEC program included screening costs for each subject, as well as direct and indirect treatment costs for esophageal and cardiac severe dysplasia and cancer detected by screening. The assessed benefits of this program included the saved treatment costs, both direct and indirect, on esophageal and cardiac cancer, as well as the value of prolonged life due to screening, as determined by the human capital approach. The results showed the screening cost of finding esophageal and cardiac severe dysplasia or cancer ranged from RMB 2707 to RMB 4512, and the total cost on screening and treatment was RMB 13 115-14 920. The cost benefit was RMB 58 944-155 110 (the saved treatment cost, RMB 17 730, plus the value of prolonged life, RMB 41 214-137 380). The ratio of benefit-to-cost (BCR) was 3.95-11.83. Our results suggest that EDETEC has a high benefit-to-cost ratio in China and could be instituted into high risk areas of China.
Adult ; Aged ; Cardia ; pathology ; China ; Cost-Benefit Analysis ; Early Detection of Cancer ; economics ; Esophageal Neoplasms ; diagnosis ; economics ; therapy ; Health Care Costs ; Humans ; Mass Screening ; economics ; Middle Aged ; Stomach Neoplasms ; diagnosis ; economics ; therapy

This study was purposed to construct a fusion DNA vaccine containing WT1 multi-epitope and stimulating epitope of mycobacterium tuberculosis heat shock protein 70 and to detect its expression and immunogenicity. On the basis of published data, a multi-epitope gene (Multi-WT1) containing three HLA *0201-restricted CTL epitopes: one HLA*2402-restricted CTL epitope, two Th epitopes and one universal Th Pan-DR epitope (PADRE) was constructed. DNA-coding sequence was modified by Computer-Aided Design (CAD) to optimize proteasome-mediated epitope processing through the introduction of different amino acid spacer sequences. The synthetic nucleotide sequence was then inserted into an eukaryotic vector to construct the plasmid pcDNA3.1-WT1.For enhancing CTL activity, HSP70 fragment including stimulatory domain P407-426 was amplified by PCR from mycobacterial HSP70 gene and cloned into pcDNA3.1(+). Then Multi-WT1 was fused to the N-terminal of pcDNA3.1-mHSP70(407-426) to make the multi-epitope fusion gene vaccine pcDNA3.1-WT1-mHSP70(407-426). HEK-293T cells were transfected with this vaccine and the expressed product was identified by RT-PCR. Enzyme-linked immunospot assay (ELISPOT) was used to evaluate the immunological responses elicited by vaccine. The results showed that the most of WT1 epitopes could be correctly cleaved which was confirmed by software Net Chop 3.1 and PAPROCIanalysis. RT-PCR showed correct expression of target gene in HEK293T cells and ELISPOT showed specific T-cell responses. It is concluded that the eukaryotic expression vector PcDNA3.1-WT1-mHSP70(407-426) fusion gene has been successfully constructed and the immunity response is also elicited, which is a good candidate for further research of DNA vaccine.
Bacterial Proteins ; genetics ; immunology ; Epitopes ; genetics ; immunology ; Genetic Vectors ; HSP70 Heat-Shock Proteins ; genetics ; immunology ; Humans ; Immunodominant Epitopes ; Vaccines, DNA ; genetics ; immunology ; WT1 Proteins ; genetics ; immunology