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1.
Article in Chinese | WPRIM | ID: wpr-928138

ABSTRACT

Quality evaluation of Chinese medicinal decoction pieces is vital for the development of the downstream industries, and is an important channel for implementing the strategy of "higher quality, higher price, and priority for the high quality" for traditional Chinese medicine. At the moment, the quality of Chinese medicinal decoction pieces is mainly evaluated based on chemical component examination. Considering the weak preliminary research foundation and poor research conditions, traditional experience-based evaluation is undervalued in the quality rating of Chinese medicinal decoction pieces. However, traditional experience is a summary of the quality of Chinese medicinal materials based on clinical experience, which thus can be a potential basis for the quality evaluation of the decoction pieces. It is a challenge in the evaluation of Chinese medicinal decoction pieces to objectify the traditional experience-based evaluation from multiple aspects such as chemistry, effect, and characterization via modern techniques. Therefore, this study developed the "experience-ingredients-activity-electronic sensing" evaluation system for Chinese medicinal decoction pieces on the basis of experience-based assessment, chemical ingredients that can truly reflect the traditional experience, biological effect assessment, and electronic sensory evaluation, which is expected to quantify the traditional experience of quality evaluation of Chinese medicinal decoction pieces via chemistry, biology, and sensory simulation. The evaluation system can serve as a reference for clinical experience-based quality evaluation of Chinese medicinal decoction pieces.


Subject(s)
China , Drugs, Chinese Herbal , Electronics , Medicine, Chinese Traditional , Restraint, Physical
2.
Article in Chinese | WPRIM | ID: wpr-906475

ABSTRACT

Qingxin Lianzi Yin (QXLZY), as an ancient classical formula for clearing the heart and nourishing the Yin, was composed of nine herbs (Scutellariae Radix, Ophiopogonis Radix, Lycii Cortex, Plantaginis Semen, Glycyrrhizae Radix et Rhizoma Praeparata Cum Melle, Nelumbinis Semen, Poria, Astragali Radix and Ginseng Radix et Rhizoma), coming from Prescriptions of the Bureau of Taiping People's Welfare Pharmacy. It could clear away the heart-fire, promote the interaction of the heart and kidney, replenish Qi and Yin, and stop strangury-turbidity. It was used to treat gonorrhea of urination, seminal emission, restlessness, wasting-thirst and so on. At present, the usage and dosage of QXLZY and its addition and subtraction are different in clinical practice. Most of the studies just focus on its clinical efficacy, and there is few review literature reflecting its historical evolution. Based on this, this paper systematically clarified the historical evolution, composition, preparation, interpretation, function, and modern clinical application of QXLZY. This work has been explained the historical evolution of QXLZY, and found that it was wildly used in modern clinical, especially suitable for the treatment of chronic urinary system diseases. At the same time, QXLZY also had significant therapeutic effects on neurasthenia, stomatitis, diabetic nephropathy and other aspects. Through the comprehensive analysis of ancient and modern literature, this work explores the true connotation of QXLZY from the perspective of traditional Chinese medicine theory, which can point out the direction of the clinical application and positioning of this famous classical formula after it comes into the market, and also can provide reference basis for its subsequent in-depth research and development.

3.
Article in Chinese | WPRIM | ID: wpr-905868

ABSTRACT

Objective:To explore effects of different extracts and monomers of <italic>Lepidium meyenii </italic>(Maca) on the proliferation of mouse splenic lymphocytes and induction of interleukin-2 (IL-2) and tumor necrosis factor-<italic>α</italic> (TNF-<italic>α</italic>) by observing their immunomodulatory effects. Method:An octadecylsilyl (ODS) column was used to enrich the methanol extract of <italic>L. meyenii</italic> in stages to obtain six fractions and three monomers. Different groups of extracts and monomers of <italic>L. meyenii </italic>at different doses were set up. Cell counting Kit-8 (CCK-8) was used to detect the effect on the proliferation of mitogen-free, concanavalin A (Con A)-induced, and lipopolysaccharides (LPS)-induced mouse splenic lymphocytes. Enzyme-linked immunosorbent assay (ELISA) was used to determine the levels of IL-2 and TNF-<italic>α</italic>. Result:<italic>L. meyenii </italic>extracts Fr<sub>3</sub> and Fr<sub>6</sub>, and monomers <italic>N</italic>-benzyl hexadecanamide and 1,2-dihydro-4-carboxaldehyde-3-benzyl-<italic>N</italic>-hydroxypyridine slightly promoted the proliferation of Con A-induced T lymphocytes and LPS-induced B lymphocytes (<italic>P</italic><0.01) as compared with the conditions in the model group. <italic>L. meyenii</italic> extracts and monomers significantly induced the secretion of IL-2 and TNF-<italic>α</italic> by splenic lymphocytes (<italic>P</italic><0.01). Conclusion:<italic>L. meyenii</italic> extracts and monomers can achieve immunological enhancement by promoting the secretion of IL-2 and TNF-<italic>α</italic>, and facilitate the proliferation of splenic lymphocytes. The active components are presumedly macamides and pyridine alkaloids, and the specific mechanism still needs to be further explored.

4.
Article in Chinese | WPRIM | ID: wpr-921774

ABSTRACT

This study aimed to qualitatively analyze the chemical components in Xiaoer Chiqiao Qingre Granules(XRCQ) by UHPLC-LTQ-Orbitrap-MS/MS and identify its material basis. The absorbed components in plasma were combined for exploring the potential action mechanism by integrated network pharmacology. ACQUITY UPLC HSS T3(2.1 mm×100 mm, 1.8 μm) column and mobile phase system of 0.1% formic acid solution(A)-acetonitrile(B) were used for gradient elution, followed by high resolution liquid chromatography-mass spectrometry in both positive and negative ion scanning modes. According to the precise relative molecular mass and MS/MS fragment ions, a total of 124 chemical components were identified in XRCQ by the comparison with references and literature reports, among which 29 compounds were completely confirmed by comparison with reference substances. Then, the main absorbed components of XRCQ in plasma were also analyzed and clarified by UHPLC-LTQ-Orbitrap-MS/MS. BATMAN-TCM and SwissTargetPrediction were used for target prediction of absorbed components in plasma. Following the plotting of association network with Cytoscape 3.8.2, the core targets were subjected to GO and KEGG pathway enrichment analysis and a component-target-pathway network was constructed. A total of eight main targets of XRCQ against fever in children were obtained together with eight absorbed components in plasma, including glycyrhydinic acid, hesperidin, emodin, reticuline, daidzein, magnolignan C, magnolignan A, and magnolaldehyde D. It was inferred that XRCQ might improve alimentary system abnormality, inflammatory response, oxidative stress, and endocrine disorder through tumor necrosis factor, PI3 K-AKT, and other signaling pathways. The present study comprehensively expounded the chemical profiles of XRCQ and the main absorbed components in plasma and predicted the potential mechanism of XRCQ based on integrated network pharmacology, which has provided certain theoretical reference for the clinical application of XRCQ.


Subject(s)
Child , Chromatography, High Pressure Liquid , Chromatography, Liquid , Drugs, Chinese Herbal , Humans , Network Pharmacology , Tandem Mass Spectrometry
5.
Article in Chinese | WPRIM | ID: wpr-888184

ABSTRACT

Indolealkylamines(IAAs) are the main hydrophilic substances in toad skin, mainly including free N-methyl-5-hydroxytryptamine, bufotenine, bufotenidine, dehydrobufotenine, and binding bufothionine. In this study, the LPS-activated neutrophils were used to investigate the structure-activity relationship and anti-inflammatory mechanism of the above-mentioned five monomers from the toad skin in vitro. The neutrophils were divided into the control group, model group(1 μg·mL~(-1) LPS), positive drug group(100 μg·mL~(-1) indometacin), as well as the low-(50 μg·mL~(-1)), medium-(100 μg·mL~(-1)) and high-dose(200 μg·mL~(-1)) free N-methyl-5-hydroxytryptamine, bufotenine, bufotenidine, dehydrobufotenine, and binding bufothionine groups. The levels of IL-6, TNF-α and IL-1β in the neutrophil supernatant of each group was measured by enzyme-linked immunosorbent assay(ELISA) after LPS stimulation, followed by the detection of apoptosis in each group after Annexin V/PI staining. The protein expression levels of caspase-3, Bax, Bcl-2, beclin1, LC3-I, and LC3-Ⅱ were assayed by Western blot. The results showed that IAAs reduced the excessive secretion of inflammatory cytokines caused by LPS compared with the model group. Besides, the activity of each free IAAs(N-methyl-5-hydroxytryptamine, bufotenine, bufotenidine and dehydrobufotenine), especially bufotenine, was stronger than that of the binding bufothionine. As revealed by Annexin V/PI staining, LPS delayed the early apoptosis of neutrophils compared with the control group, while bufotenine promoted the apoptosis of neutrophils in a dose-dependent manner, which might be related to the elevated expression of apoptosis-related protein Bax/Bcl-2. In addition, LPS activated the autophagy pathways in neutrophils. This study confirmed the efficacy of IAAs in reducing the secretion of inflammatory cytokines in neutrophils induced by LPS for the first time. For instance, bufotenine exerts the anti-inflammatory effect possibly by inducing the apoptosis of neutrophils.


Subject(s)
Animals , Anti-Inflammatory Agents/pharmacology , Apoptosis , Bufonidae , Lipopolysaccharides/toxicity , Neutrophils , Skin
6.
Article in Chinese | WPRIM | ID: wpr-828018

ABSTRACT

UHPLC-LTQ-Orbitrap-MS was developed for the identification of chemical constituents in Qingfei Paidu Decoction, which will clarify its material basis. ACQUITY UHPLC HSS T3 chromatography column(2.1 mm×100 mm, 1.8 μm) was used with 0.1% formic acid(B)-acetonitrile(A) as the mobile phase in gradient elution. The decoction was detected by high-resolution liquid chromatography-mass spectrometry equipped with an ESI ion source in positive and negative mode. Based on the accurate mass measurements, retention time, mass fragmentation patterns combined with comparison of reference and literature reports, a total of 87 major compounds including 43 flavonoids, 9 alkaloids, 4 triterpenoid saponins, 1 sesquiterpene, 2 coumarins, 10 phenolic acids and 18 other compounds were tentatively screened and characterized. UHPLC-LTQ-Orbitrap-MS was employed to comprehensively elucidate the chemical components in Qingfei Paidu Decoction, which basically covered 20 Chinese medicines except gypsum in Qingfei Paidu Decoction. These collective results provide a scientific basis for further research on the quality control standard of Qingfei Paidu Decoction.


Subject(s)
Chromatography, High Pressure Liquid , Coumarins , Drugs, Chinese Herbal , Flavonoids , Mass Spectrometry
7.
Article in Chinese | WPRIM | ID: wpr-774519

ABSTRACT

UPLC-ESI-Orbitrap-MS/MS was used to analyze,identify and attribute the chemical constituents in Pudilan Antiphlogistic Oral Liquid. The analysis was performed on an Agilent Eclipse XDB-C18(4.6 mm × 150 mm,3.5 μm) with a gradient mobile phase of methanol-0.1% formic solution system at the flow rate of 0.5 m L·min-1. The sample volume was 2 μL. The column temperature was30 ℃. The high-resolution orbitrap mass spectrometry was used as detector,with electrospray ion source in both positive and negative models,and the MS scanning ranged between m/z 50 and 2 000. Based on the analysis of mass spectrometry and literature reports,79 compounds were confirmed,including 30 alkaloids,28 organic acids,18 flavonoids and 3 coumarins. Finally,39 compounds,such as rutin,esculetin,gallic acid,caffeic acid,cichoric acid,were identified from Taraxacum mongolicum; 11 compounds,such as baicalin,baicalein,apigenin,chrysin,oroxylin A,were identified from Scutellaria baicalensis; 13 compounds,such as arginine,proline,hypoxanthine,epigoitrin,indirubin,were identified from Isatis indigotica; and 18 compounds,such as dehydrocheilanthifoline,oxysanguinarine,corynoline,protopine,spallidamine,were identified from Corydalis bungeana. After the analysis of chemical model and attribution,the contents of some compounds were high in Pudilan Antiphlogistic Oral Liquid,such as baicalin,wogonoside,baicalein,wogonin,apigenin,chrysin,skullcapflavonⅡ,oroxylin A,cichoric acid,chlorogenic acid,caffeic acid,esculetin,dehydrocheilanthifoline,dihydrosanguinarine,protopine,corynoline and indirubin. The established method is simple,accurate,rapid,sensitive and reproducible,and thus suitable for the qualitative identification and quantitative determination of Pudilan Antiphlogistic Oral Liquid,which lays a foundation for the systematic quality control and the establishment of whole-course traceability system of active ingredients.


Subject(s)
Anti-Inflammatory Agents , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Chemistry , Phytochemicals , Tandem Mass Spectrometry
8.
Article in Chinese | WPRIM | ID: wpr-817674

ABSTRACT

@#【Objective】To explore the relationship between the miR- 132 expression in serum and cognitive deficits of OSA. 【Methods】 66 Chinese adults age 30 to 60 years old were enrolled and categorized into two groups based on Montreal Cognitive Assessment(MoCA)scores: OSA patients with cognitive impairment(OSAI,n=36),OSA patients without cognitive impairment(OSAN,n=30),and thirty adults without OSA as healthy control group(HC,n=30). Out- of- center cardiopulmonary sleep testing (OCST) and MoCA assessment were performed and the relative expression of miR-132 in serum was detected by PCR.【Results】No significant difference was observed in age,education,gender and hypertension(P>0.05). The relative expression level of miR-132 was significantly up-regulated in OSAI patient′s serum compared to the OSAN and HC patients (P<0.001),and had a positive correlation with MoCA score (r=- 0.726,P<0.001). ROC analyses showed that the areas under the curve(AUC)were statistically significant from the line of identity in OSA with cognitive impairment(AUC=0.935,95% CI:0.890- 0.981,P<0.001)and in OSA(AUC=0.787,95% CI:0.695-0.879,P<0.001).【Conclusions】Elevated serum miR-132 expression levels are closely related to the diagnosis of OSA and its cognitive dysfunction. Detection of serum miR- 132 may be a potential indicator of cognitive dysfunction and diagnosis in OSA patients.

9.
Article in Chinese | WPRIM | ID: wpr-712909

ABSTRACT

[Objective]To investigate the expression changes of miR-133b in methamphetamine(MA)-induced neuro-nal injury in PC12 cells and its regulative effects on cellular apoptosis.[Methods]PC12 cells were cultured and divided into control group and MA treated group.In MA treated group,PC12 cells were insulted with 800μmol/L MA in culture medium. The cellular injury of PC12 cells was observed under microscope. The cellular apoptosis was detected by Hoechst33342/PI double staining,and the expression level of miR-133b was examined by real-time quantitative PCR(RT-PCR). Further-more,miR-133b mimic and inhibitors were transfected into PC12 cells to analyze miR-133b's function in MA-induced cell apoptosis.[Results]The data showed that 800 μmol/L MA could induce obvious cellular injury,cause neurite shortened and increase the cell apoptosis. The RT-PCR data showed that the expression of miR-133b of PC12 cells treated with MA de-creased significantly.The apoptosis rate of PC12 cells decreased after transfection of miR-133b mimic,while increased after transfection of miR-133b inhibitors.[Conclusions]High concentration of MA causes neuron damage and induces neuronal apoptosis,and also decreases the levels of miR-133b expression. Whereas,overexpression of miR-133b can reduce the apoptosis of cultured PC12 cells.Thus,miR-133b plays a crucial role in MA mediated neurotoxicity.This study provides a theoretical basis for elucidating the mechanism of MA-induced neurotoxicity and may provide a new strategy for treating MA addiction.

10.
Article in Chinese | WPRIM | ID: wpr-687354

ABSTRACT

To study the pharmacokinetics of active ingredients (alkaloids, iridoids and flavonoids) in Huanglian Jiedu decoction (HLJDD) in Alzheimer's disease (AD) model rats, and investigate its mechanism in treatment of AD. All of rats were divided into normal control group (=6), shame operation group (=6) and model group (=12). Rats in shame operation group received daily subcutaneous injection of D-galactose (D-gal 50 mg·kg⁻¹) for a total of 45 d to induce subacute aging model. Based on the operation of shame operation group, the rats in model group were given with an injection of Aβ₂₅₋₃₅ (4.0 g·L⁻¹)-ibotenic acid (2.0 g·L⁻¹) into the nucleus basalis magnocellularis. Then rats in model group were divided into HLJDD one day administration group (=6) and HLJDD one week group (=6). The plasma concentration of alkaloids, iridoid and flavonoids was determined by liquid chromatography tandem mass spectrometry (LC-QQQ-MS) at different time points. The levels of seven inflammatory factors (MIP-2, IL-1β, IL-2, IL-8, IL-10, IL-13, TNF-α) in cerebrospinalfluid (CSF) were measured by Bio-Plex multi-factor detection technology. Iridoids in AD model rats, with high bioavailability, were easily absorbed and eliminated. The plasma concentration of alkaloid was lower, and the AUC (area under the curve) was higher in HLJDD one week group than that in HLJDD one day group. The plasma concentration-time curves of flavonoids showed obvious bimodal phenomena. After the gastric administration of HLJDD, the inflammatory factors in CSF of AD rats demonstrated a callback trend, including IL-1β/IL-10 (<0.05) with significant difference. The pharmacokinetic behaviors of iridoids, alkaloids and flavonoids (41 compounds) in AD model rats were fundamentally elucidated, and HLJDD can improve the central inflammatory status of AD rats by regulating the levels of inflammatory factors.

11.
Article in Chinese | WPRIM | ID: wpr-307088

ABSTRACT

Fifteen compounds were isolated from the toad skin by a combination of various chromatographic methods including macroporous resin, silica gel, ODS and semi-preparative HPLC. Their structures were identified as 4,5-dimethyl-1,3,4,5-tetrahydropyrrolo[4,3,2-de]quinolin-6-ol(1), serotonin(2), N-methyl serotonin(3), O-methyl bufotenine(4), 1,2,3,4-tetrahydro-6-hydroxy-β-carboline(5), O-methylserotonin(6), glycinebetaine(7), caffeine(8), bufotenine(9), shepherdine(10), tryptophan(11), (5-hydroxy-1H-indol-3-yl)acetic acid(12), 5-hydroxy tryptophol(13), 2-methyl-6-hydroxy-1,2,3,4-tetrahydro-β-carboline(14), bufothionine(15). Among them, compound 1 was a new compound,compound 5 was a new natural product. Compounds 4-8 and 10-14 were separated from toad skin for the first time.

12.
Article in Chinese | WPRIM | ID: wpr-275187

ABSTRACT

In this study, 10 samples of parasites, cursive, and the whole from six different species of Cordyceps were determined and compared by HPLC and LC-MS methods. Uridine, adenosine, and cordycepin were selected as the main evaluation index. The anti-fibrotic activity of different species Cordyceps extracts was observed using in vitro TGF-β1-induced ECM accumulation in human embryonic fibroblasts CCC-ESF-1. The results demonstrated that the number of atoms and hyphae ingredients of different species showed little difference, however, the content distribution of each component has obvious significance. The in vitro anti-fibrotic activities of different species were as follow: Cordyceps flower > Cicada Cordyceps (Cicada flower)> Silkworm Cordyceps> Tussah Cordyceps>natural Cordyceps. Our preliminary data could serve as reference for the discovery of artificial alternatives of natural Cordyceps.

13.
Article in Chinese | WPRIM | ID: wpr-337900

ABSTRACT

In this study, chemistry, biology and pharmacology were combinated to screen pseudoallergenic substances of Shuang-huanglian injection (SHLI) so that to establish a scientific and systematic approach to screen pseudoallergenic substances of traditional Chinese medicine injections. The mouse pseudoallergic reaction models were used to screen the pseudoallergic reaction of SHLI's intermediate extract and the intermediate extract's component or ingredient. Among the three intermediates of Shuanghuanglian injection (extract of Scutellaria baicalensis, extract of Lonicera japonica, extract of Forsythia suspensa) , pseudoallergic action of Forsythia suspensa was the strongest, Forsythia suspesnsa's pseudoallergic reaction mainly associated with the composition with largerchemical polarity. Further it was found that forsythiaside A and arctiin which existed in the the composition with largerchemical polarity caused obvious pseudoallergic reactions. SHLI with removal forsythoside A with the technology of HPLC-MS displayed reduced pseudoallergic reaction and a significant improved safety. This study provided a scientific basis for SHLI process improvements and also offered idea and research foundation for screening pseudoallergenic substances injections in other TCM injections.


Subject(s)
Animals , Drug Hypersensitivity , Drugs, Chinese Herbal , Furans , Glucosides , Glycosides , Injections , Male , Mice , Mice, Inbred ICR
14.
Article in Chinese | WPRIM | ID: wpr-250458

ABSTRACT

Maca as one of the star products in the international health care market in recent years, had a wide range of application value and promoted to all over the world. However, the basic research of Maca was not deep, lack of systematic and clear efficacy studies. Market products hype its aphrodisiac effect, which greatly impact more systematic in-depth research and exploration. Therefore, this paper briefly summarizes advance research in recent years including the status quo of the resources, growth cultivation, phytochemical, pharmacological effect and other aspects, which can provide reference for rational development and utilization of Maca.


Subject(s)
Animals , Biomedical Research , Humans , Lepidium , Chemistry , Classification , Plant Extracts , Chemistry , Metabolism , Pharmacology
15.
Acta Pharmaceutica Sinica ; (12): 1315-1319, 2014.
Article in Chinese | WPRIM | ID: wpr-299133

ABSTRACT

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.


Subject(s)
Animals , Chromatography, High Pressure Liquid , Dogs , Esters , Metabolism , Humans , Iridoids , Metabolism , Macaca mulatta , Microsomes, Liver , Metabolism , Rats , Spectrometry, Mass, Electrospray Ionization
16.
Acta Pharmaceutica Sinica ; (12): 1446-1450, 2014.
Article in Chinese | WPRIM | ID: wpr-299113

ABSTRACT

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.


Subject(s)
Amphibian Venoms , Chemistry , Animals , Bufanolides , Chemistry , Bufonidae , Chromatography, High Pressure Liquid , Tandem Mass Spectrometry
17.
Acta Pharmaceutica Sinica ; (12): 1574-1577, 2014.
Article in Chinese | WPRIM | ID: wpr-299095

ABSTRACT

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.


Subject(s)
Animals , Bufanolides , Chemistry , Bufo bufo , Injections , Skin , Chemistry
18.
Acta Pharmaceutica Sinica ; (12): 237-243, 2014.
Article in Chinese | WPRIM | ID: wpr-297987

ABSTRACT

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.


Subject(s)
Administration, Oral , Alkaloids , Blood , Animals , Biotransformation , Chromatography, High Pressure Liquid , Drug Combinations , Drugs, Chinese Herbal , Metabolism , Flavonoids , Blood , Iridoids , Blood , Male , Plants, Medicinal , Chemistry , Rats , Rats, Sprague-Dawley , Spectrometry, Mass, Electrospray Ionization , Tandem Mass Spectrometry
19.
Acta Pharmaceutica Sinica ; (12): 244-248, 2014.
Article in Chinese | WPRIM | ID: wpr-297986

ABSTRACT

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.


Subject(s)
Amphibian Venoms , Chemistry , Animals , Bufanolides , Chemistry , Bufo bufo , Chromatography, High Pressure Liquid , Molecular Structure , Spectrometry, Mass, Electrospray Ionization , Tandem Mass Spectrometry
20.
Acta Pharmaceutica Sinica ; (12): 822-826, 2012.
Article in Chinese | WPRIM | ID: wpr-276237

ABSTRACT

Cinobufacini is an aqueous extract of Bufo bufo gargarizans Cantor dried skin, which has been widely used for cancer therapy in China. So far, its active components are still not very clear. In previous reports, bufadienolides with low-concentration were usually studied because of their anticancer effects. However, the high polarity constituents in cinobufacini are less investigated. The present study found that more than 50% contents of cinobufacini were water-soluble peptides. Then, in vitro anticancer experiments were carried out, including human stomach cancer cell lines BGC823 and MCG803, human colon cancer cell lines DLD-1 and HT-29, and human pancreatic cancer cell line MIAPACA-2. The IC50 for these cell lines model were ranged from 25-123 microgmL(-1). The results indicated that these peptides showed similar activity with cinobufacini injection. As a conclusion, this study provides a new and further understanding of anticancer components in cinobufacini injection.


Subject(s)
Amphibian Venoms , Chemistry , Animals , Antineoplastic Agents , Pharmacology , Bufonidae , Cell Line, Tumor , Cell Proliferation , HT29 Cells , Humans , Injections , Medicine, Chinese Traditional , Peptides , Pharmacology , Skin , Chemistry
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