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1.
Article in Chinese | WPRIM | ID: wpr-879011

ABSTRACT

Based on the investigation of wild medicinal plant resources in Dexing city, Jiangxi province, and the collected plant specimens, which were identified by taxonomy, two new record species of geographical distribution were found, which are Meehania zheminensis A. Takano, Pan Li & G.-H. Xia and Corydalis huangshanensis L.Q.Huang & H.S.Peng. The voucher specimens are kept in Dexing museum of traditional Chinese medicine. In this paper, the new distribution species were reported, which provides valuable information for further enriching and supplementing the species diversity of medicinal plant resources in Jiangxi province.


Subject(s)
China , Corydalis , Humans , Lamiaceae , Medicine, Chinese Traditional , Museums , Plants, Medicinal
2.
Article in Chinese | WPRIM | ID: wpr-828041

ABSTRACT

Corydalis Bungeanae Herba is often used to treat a variety of inflammatory diseases in traditional Chinese medicine. In order to determine its chemical material basis, the components of Corydalis Bungeanae Herba were isolated by automated purification system. Flavonoids and alkaloids were prepared, and all such components were identified by mass spectrometry. The effects of the components on the production of inflammatory mediators and pharmacological mechanisms in the lipopolysaccharide(LPS)-induced RAW264.7 cell inflammation model were examined. Mouse macrophages(RAW264.7) were first treated with LPS. The relationship between cell viability and LPS concentration was observed. Then, the effects of flavonoids components and alkaloid components with different administration concentrations on cell viability were detected to determine the maximum administration concentration. Secondly, 2.5, 5, 10 and 20 μg·mL~(-1) flavonoids components and alkaloid components were added respectively to observe the effects and mechanism of different concentrations of flavonoids components and alkaloid components on LPS-induced inflammation of RAW264.7 macrophages. Griess reagent assay was used to detect NO content in cell supernatant. The inflammatory cytokines(TNF-α, IL-1β and IL-6) in cell supernatant were determined by ELISA method. Western blot method was used to detect the intracellular nuclear factor(NF-κB) IκBα phosphorylation(p-IκBα), p65 phosphorylation(p-p65) and protein expression of TLR4, TLR2. The results showed that the alkaloid components inhibited the production of NO, TNF-α, IL-1β and IL-6 in a dose-dependent mannerin the concentration range of 2.5-20 μg·mL~(-1). In inflammation upstream pathways, the inhibitory effect of the alkaloid components on the TLR2 expression level was weaker than that of TLR4. In inflammation downstream, alkaloid components significantly inhibited phosphorylation of IκBα and p65 in a dose-dependent manner. These data suggested that the alkaloid components were the material basis components of Corydalis Bungeanae Herba, and its anti-inflammatory mechanism might be related to inhibiting the transmission of inflammatory signals in TLRs/NF-κB signaling pathways dominated by TLR4, interfering with the activation of inflammatory genes and inhibiting their over expression, and down-regulating the secretion level of inflammatory factors.


Subject(s)
Animals , Anti-Inflammatory Agents , Therapeutic Uses , Corydalis , Inflammation , Drug Therapy , Lipopolysaccharides , Mice , NF-kappa B
3.
Article in Chinese | WPRIM | ID: wpr-827933

ABSTRACT

Two new phenylpropanoid amide glycosides and ten analogues were isolated from the CH_2Cl_2 layer of 95% ethanol extract of the whole plants of Corydalis racemosa by using various chromatographic techniques, including silica gel, Sephadex LH-20, ODS column chromatographies, and semi-preparative HPLC. Their structures were identified on the basis of physicochemical properties, MS, NMR, and IR spectroscopic data as N-cis-sinapoyltyramine-4'-O-β-glucoside(1), N-cis-sinapoyl-3-methoxytyramine-4'-O-β-glucoside(2), N-cis-sinapoyltyramine(3), N-cis-feruloyltyramine(4), N-trans-cinnamoyltyramine(5), N-trans-feruloylphenethylamine(6), N-trans-p-methoxycinnamoyl-3-hydoxyoctopamine(7), N-cis-feruloyl-3-methoxytyramine(8), N-trans-feruloyltyramine(9), N-trans-feruloyl-3-methoxytyramine(10), N-trans-sinapoyltyramine(11), and N-trans-p-coumaroyltyramine(12). Compounds 1 and 2 are new compounds. Compounds 3-7 are obtained from the plants of Papaveraceae for the first time, and compounds 8-12 are firstly isolated from C. racemosa.


Subject(s)
Amides , Chromatography, High Pressure Liquid , Corydalis , Glucosides , Glycosides
4.
Article in Chinese | WPRIM | ID: wpr-773724

ABSTRACT

To establish a DNA molecular markers method for identification of Corydalis yanhusuo,C. turtschaninovii and C. decumbens,the mat K,trn G and psb A-trn H sequences of 56 samples from 14 species of C. yanhusuo,C. turtschaninovii,C. decumbens and their related species were obtained by sequencing. The SNP loci were obtained by Bio Edit 7. 2. 2 software. The primers for AS-PCR identification were designed based on the mutation sites,and the conditions of PCR were optimized to identify C. yanhusuo,C. turtschaninovii,and C. decumbens according to the specific bands. The results showed that the amount of template( 0. 6-1 200 ng)and annealing temperature( 42-60 ℃) had little influence on the amplification results,and the number of cycles had much influence on the amplification results. When the number of cycles was 20,the specific bands of 297 bp( mat K),353 bp( trn G) and 544 bp( mat K) were amplified from C. yanhusuo,C. turtschaninovii and C. decumbens,respectively. The method established in this study had a minimum detection limit of 6 ng for C. yanhusuo,60 ng for C. decumbens and less than 0. 6 ng for C. turtschaninovii. Thus,the allelespecific PCR method established in the research can specifically identify C. yanhusuo,C. turtschaninovii,and C. decumbens.


Subject(s)
Alleles , Corydalis , Classification , Genetics , Genes, Plant , Genetic Markers , Polymerase Chain Reaction
5.
Article in Chinese | WPRIM | ID: wpr-776416

ABSTRACT

Ten phenylpropanoid amides were isolated from the whole plants of Corydalis edulis Maxim. by various of column chromatographies including silica gel, Sephadex LH-20, and ODS. Their structures were identified on the basis of physicochemical properties, MS, NMR, and IR spectroscopic data. These compounds were identified as N-trans-sinapoyl-3-methoxytyramine-4'-O-β-glucoside(1), N-trans-sinapoyl-3-methoxytyramine(2), N-trans-sinapoyltyramine(3), N-trans-p-coumaroyltyramine(4), N-trans-sinapoyl-7-hydroxytyramine(5), N-cis-feruloyltyramine(6), N-cis-p-coumaroyltyramine(7), N-trans-feruloyltyramine(8), N-trans-feruloyl-3-methoxytyramine(9), and N-trans-feruloyl-7-hydroxytyramine(10). Compound 1 is a new compound. Compounds 2-7 are obtained from the plants of Papaveraceae for the first time, while compounds 8-10 are firstly isolated from C. edulis.


Subject(s)
Amides , Corydalis , Chemistry , Glucosides , Phytochemicals , Tyramine
6.
Article in English | WPRIM | ID: wpr-110254

ABSTRACT

BACKGROUND/AIMS: Post-operative ileus (POI) is a common complication of abdominal surgery. DA-9701, an extract of Pharbitis Semen and Corydalis Tuber, is a new prokinetic agent that also alleviates visceral pain. The aim of this study was to investigate whether DA-9701 can ameliorate POI in rats. METHODS: A total of 32 rats were divided into 4 groups: no surgery/no medication (NSNM), no surgery/medication (NSM), surgery/no medication (SNM), and surgery/medication (SM). Gastrointestinal transit (GIT), which is assessed by migration of charcoal, and cumulative stool weight were measured at 24 hours after surgery. RESULTS: GIT was significantly more delayed in the SNM group than in the other groups (SNM vs NSNM, P < 0.001; SNM vs NSM, P < 0.001; SNM vs SM, P = 0.005). Cumulative stool weight in that group was also lower than in the no surgery groups (SNM vs NSNM, P = 0.007; SNM vs NSM, P = 0.033), and there was no significant difference between the SM group and the no surgery groups (SM vs NSM, P = 0.703; SM vs NSNM, P = 0.347). CONCLUSION: DA-9701 can ameliorate POI by reducing delayed GIT and improving defecation in a rat model of POI.


Subject(s)
Animals , Charcoal , Corydalis , Defecation , Gastrointestinal Transit , Ghrelin , Ileus , Models, Animal , Rats , Semen , Visceral Pain
7.
Natural Product Sciences ; : 102-106, 2016.
Article in English | WPRIM | ID: wpr-221635

ABSTRACT

A methanolic extract of Corydalis ternata having aldose reductase inhibitory activity was examined as a possible aldose reductase (ALR2) inhibitor, a key enzyme involved in diabetic complications. Seven alkaloids, tetrahydrocoptisine (1), corydaline (2), tetrahydropalmatine (3), isocorybulbine (4), corybulbine (5), dehydrocorydaline (6), and N-methyltetrahydroberbinium (7) were isolated from CHCl₃ fraction of C. ternata methanol extract. Among them, compounds 1, 5, and 7 exhibited 5.04 ± 1.97%, 5.00 ± 1.26%, and 1.80 ± 2.33% inhibitions, respectively at 40 µM. The activities of the single compounds were not comparable to that of the whole extract, suggesting that the whole combination of each single compound was responsible for the activity of the extract as shown in many cases of natural medicines. Even though this is the second report on aldose reductase inhibition activity of C. ternata, recombinant human aldose reductase was employed in this study unlike in the previous report. Furthermore, the aldose reductase inhibitory activities of isocorybulbine, corybulbine, and N-methyltetrahydroberbinium, to the best of our knowledge, were evaluated for the first time in this study. These results suggest a use of the extract of C. ternata for ameliorating diabetic complications.


Subject(s)
Aldehyde Reductase , Alkaloids , Corydalis , Diabetes Complications , Humans , Methanol
8.
Article in English | WPRIM | ID: wpr-78141

ABSTRACT

BACKGROUND/AIMS: Opioid induced bowel dysfunction (OIBD) is associated with decreased gastrointestinal (GI) propulsive activity due to intake of opioid analgesics. DA-9701, a novel prokinetic agent formulated with Pharbitis Semen and Corydalis Tuber has promising effects on GI motor function. Therefore, we aim to evaluate the prokinetic effects of DA-9701 in an OIBD model of guinea pig. METHODS: The ileal and distal colon muscle contraction in presence of different doses of DA-9701, morphine, and combination (morphine + DA-9701) was measured by tissue bath study. The prokinetic effect of DA-9701 was assessed by charcoal transit and fecal pellet output assay in an OIBD model of guinea pig. RESULTS: DA-9701 significantly increased the amplitude and area under the curve of ileal muscle contraction, while there was insignificant effect on the distal colon compared to the control. The maximal amplitude of ileal muscle contraction was acquired at a concentration of 10 μg/mL of DA-9701. In contrast, morphine significantly decreased the amplitude of ileal and distal colon muscle contraction compared to the control. Morphine delayed both upper (P < 0.01) and lower (P < 0.05) GI transit, and delayed GI transit was restored by the administration of DA-9701. Morphine induced reduction of contractility was significantly ameliorated by addition of DA-9701 in both ileal and distal colon muscles. CONCLUSIONS: DA-9701 significantly increased the amplitude of contraction of the ileal muscle, however the distal colon muscle contraction was insignificant. Additionally, it restored delayed upper and lower GI transit in an OIBD model of guinea pig, and it might prove to be a useful candidate drug in a clinical trial for OIBD.


Subject(s)
Analgesics, Opioid , Animals , Baths , Charcoal , Colon , Corydalis , Gastrointestinal Transit , Guinea Pigs , Guinea , Ileum , Morphine , Muscle Contraction , Muscles , Semen
9.
Article in Chinese | WPRIM | ID: wpr-351259

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effect of oligochitosan in promoting intestinal absorption of protoberberine alkaloids in extracts from Corydalis saxicola total alkaloids.</p><p><b>METHOD</b>The in vitro single-pass intestinal perfusion model in rats was established to study the changes in absorption kinetic parameters of dehydrocavidine, berberine hydrochloride and palmatine chloride in C. saxicola total alkaloids after the addition of different concentrations oligochitosan and evaluate the effect of oligochitosan in promoting intestinal absorption of the drugs.</p><p><b>RESULT</b>The concentration of oligochitosan had different effects on the absorption rate constant (Ka) and apparent permeability coefficient (Peff) of the three active component in rat intestines. Ka and Peff in 0.5% oligochitosan group significantly increased, indicating a stronger effect in promoting the absorption.</p><p><b>CONCLUSION</b>Oligochitosan has a certain effect in promoting the intestinal absorptions of protoberberine alkaloids in C. saxicola total alkaloids.</p>


Subject(s)
Animals , Berberine Alkaloids , Pharmacokinetics , Chitin , Corydalis , Chemistry , Drugs, Chinese Herbal , Pharmacokinetics , Intestinal Absorption , Intestines , Metabolism , Male , Rats , Rats, Sprague-Dawley
10.
Article in Chinese | WPRIM | ID: wpr-337909

ABSTRACT

Fingerprint of traditional Chinese medicine (TCM) is in the guidance of the basic theory of TCM, according to the variety and quality of TCM and using a variety of analytical methods and technology, to establish the objective, overall and multi index comprehensive evaluation system. The TCM fingerprint in one of the strategic subjects for TCM modernization. As more and more technologies have been applied to the fingerprint research of TCM, it is sure to play a much more important role in many aspects, such as the quality control of TCM, the researches of efficient components, and the mechanism in TCM, and so on. The fingerprint technology includes many modern technologies such as high-pressure liquid chromatography (HPLC). Corydalis yanhusuo is an ancient TCM, and recent years appears many researches about fingerprint of C. yanhusuo. This paper generalizes the research in progresses in research and analytical methods on fingerprint technology of C. yanhusuo, processed products (vinegar), and painkillers, to provide the scientific basis for fingerprint method and quality control of C. yanhusuo.


Subject(s)
Chromatography, High Pressure Liquid , Methods , Corydalis , Chemistry , Drugs, Chinese Herbal , Quality Control
11.
Article in Chinese | WPRIM | ID: wpr-237723

ABSTRACT

This paper established a near-infrared spectroscopy quantitative model for simultaneous quantitative analysis of coptisine hydrochloride, dehydrocorydaline, tetrahydropalmatine, corydaline and glaucine in Corydalis Rhizoma. Firstly, the chemical values of the five components in Corydalis Rhizoma were determined by the reversed-phase high performance liquid chromatography (RP-HPLC) with UV detection. Then, the quantitative calibration model was established and optimized by fourier transformation near-infrared spectroscopy (NIRS) combined with partial least square (PLS) regression. The calibration model was evaluated by correlation coefficient (r), the root-mean-square error of calibration (RMSEC) and the root mean square of cross-validation (RMSECV) of the calibration model, as well as the correlation coefficient (r) and the root mean square of prediction (RMSEP) of prediction model. For the quantitative calibration model, the r, RMSEC and RMSECV of coptisine hydrochloride, dehydrocorydaline, tetrahydropalmatine, corydaline and glaucine were 0.941 0, 0.972 7, 0.964 3, 0.978 1, 0.979 9; 0.006 7, 0.003 5, 0.005 9, 0.002 8, 0.005 9; and 0.015, 0.011, 0.020, 0.010 and 0.022, respectively. For the prediction model, the r and RMSEP of the five components were 0.916 6, 0.942 9, 0.943 6, 0.916 7, 0.914 5; and 0.009, 0.006 6, 0.007 5, 0.006 9 and 0.011, respectively. The established near-infrared spectroscopy quantitative model is relatively stable, accurate and reliable for the simultaneous quantitative analysis of the five alkaloids, and is expected to be used for the rapid determination of the five components in crude drug of Corydalis Rhizoma.


Subject(s)
Alkaloids , Chemistry , Corydalis , Chemistry , Drugs, Chinese Herbal , Chemistry , Quality Control , Rhizome , Chemistry , Spectroscopy, Near-Infrared , Methods
12.
Article in Chinese | WPRIM | ID: wpr-246079

ABSTRACT

The study is aimed to ensure the quality and safety of medicinal plants by using ITS2 DNA barcode technology to identify Corydalis boweri, Meconopsis horridula and their close related species. The DNA of 13 herb samples including C. boweri and M. horridula from Lhasa of Tibet was extracted, ITS PCR were amplified and sequenced. Both assembled and web downloaded 71 ITS2 sequences were removed of 5. 8S and 28S. Multiple sequence alignment was completed and the intraspecific and interspecific genetic distances were calculated by MEGA 5.0, while the neighbor-joining phylogenetic trees were constructed. We also predicted the ITS2 secondary structure of C. boweri, M. horridula and their close related species. The results showed that ITS2 as DNA barcode was able to identify C. boweri, M. horridula as well as well as their close related species effectively. The established based on ITS2 barcode method provides the regular and safe detection technology for identification of C. boweri, M. horridula and their close related species, adulterants and counterfeits, in order to ensure their quality control, safe medication, reasonable development and utilization.


Subject(s)
Base Sequence , China , Corydalis , Chemistry , Classification , Genetics , DNA Barcoding, Taxonomic , Methods , DNA, Plant , Chemistry , Genetics , DNA, Ribosomal Spacer , Chemistry , Genetics , Molecular Sequence Data , Nucleic Acid Conformation , Papaveraceae , Chemistry , Classification , Genetics , Phylogeny , Plants, Medicinal , Chemistry , Classification , Genetics
13.
Article in English | WPRIM | ID: wpr-186680

ABSTRACT

BACKGROUND/AIMS: Therapies of functional dyspepsia (FD) are limited. DA-9701 is a novel prokinetic agent formulated with Pharbitis semen and Corydalis Tuber. We aimed to assess the efficacy of DA-9701 compared with itopride in FD patients. METHODS: Patients with FD randomly received either itopride 50 mg or DA-9701 30 mg t.i.d after a 2-week baseline period. After 4 weeks of treatment, 2 primary efficacy endpoints were analyzed: the change from baseline in composite score of the 8 dyspeptic symptoms and the overall treatment effect. Impact on patients' quality of life was assessed using the Nepean Dyspepsia Index (NDI) questionnaire. RESULTS: We randomly assigned 464 patients with 455 having outcome data. The difference of the composite score change of the 8 symptoms between the 2 groups was 0.62, indicating that DA-9701 was not inferior to itopride. The overall treatment effect response rate was not different between the groups. When responder was defined as > or = 5 of the 7 Likert scale, responder rates were 37% of DA-9701 and 36% of itopride group. Patients receiving DA-9701 experienced similar mean percentage of days with adequate relief during the 4-week treatment period compared with those receiving itopride (56.8% vs 59.1%). Both drugs increased the NDI score of 5 domains without any difference in change of the NDI score between the groups. The safety profile of both drugs was comparable. CONCLUSIONS: DA-9701 significantly improves symptoms in patients with FD. DA-9701 showed non-inferior efficacy to itopride with comparable safety.


Subject(s)
Corydalis , Dyspepsia , Humans , Quality of Life , Surveys and Questionnaires , Semen
14.
Article in Chinese | WPRIM | ID: wpr-305332

ABSTRACT

To evaluate the efficacy and safety of compound Decumbent Corydalis Rhizome (DCR) in treating patients with knee osteoarthritis (OA). Totally 79 patients with knee osteoarthritis were selected from out-patient and inpatient departments of West China Hospital and randomly divided into the test group and the control group. The test group (n = 41) was given Compound DCR with the dosage of 1.8 g · d(-1), while the control group (n = 38) was administered with diclofenac sodium with the dosage of 75 mg · d(-1). After 12 weeks of treatment, the total efficacy rates based on patients/physicians evaluation for experimental and control groups were 68.29%, 63.41% and 71.05%, 63.16%, respectively, without significant difference between the two groups. Both of the two groups showed significant improvements in the main efficacy indexes (pain on walking 20 m) and minor indexes (tenderness on palpation, Western Ontario and McMaster Universities OA index (WOMAC) and Short-Form Health Survey (SF-36 ), but without significant difference in efficacy between them. The incidence of related adverse events was 24.39% in the test group and 47.37% in the control group, respectively, with significant differences between the two groups (P < 0.05). In the controlled study, compound DCR is as efficient as diclofenac sodium but more tolerable, with a good clinical application prospect.


Subject(s)
Adult , Aged , Corydalis , Chemistry , Diclofenac , Drugs, Chinese Herbal , Female , Humans , Male , Middle Aged , Osteoarthritis, Knee , Drug Therapy , Rhizome , Chemistry , Treatment Outcome
15.
Article in Chinese | WPRIM | ID: wpr-321340

ABSTRACT

It was estimated that about 428 species of genus Corydalis are distributed all worldwide, with about 298, especially 10 groups and 219 species being uniquely spread in China. The genus Corydalis have been widely employed as folk medicines in China, especially as traditional Tibetan medicines, for treatment of fever, hepatitis, edema, gastritis, cholecystitis, hypertension and other diseases. The phytochemical studies revealed that isoquinoline alkaloids are its major bioactive ingredients. The extensive biological researches suggested its pharmacological activities and clinic applications against cardiovascular diseases and central nervous system, antibacterial activities, analgesic effects, anti-inflammatory, anti-oxidation and anti-injury for hepatocyte, and so on. As an effort in promoting the research of pharmacodynamic ingredients, this article presents an overview focusing on the distribution, phytochemical and pharmacological results of Corydalis species that have been applied in traditional Tibetan medicinal, hopefully to provide a reference for the new Tibetan medicine development from Corydalis plant resource.


Subject(s)
Alkaloids , Chemistry , Pharmacology , Animals , Anti-Infective Agents , Chemistry , Pharmacology , Corydalis , Chemistry , Classification , Drugs, Chinese Herbal , Chemistry , Pharmacology , Humans , Mice , Molecular Structure , Phytotherapy
16.
Article in Chinese | WPRIM | ID: wpr-319661

ABSTRACT

Corydalis Rhizoma, the dried tuber of Corydalis yanhusuo (Papaveraceae) distributed traditionally mainly in south-eastern and now cultivated in northwestern and other district in China, is one of the commonly used and well-known traditional Chinese medicine. It has been widely used to treat spastic pain, abdominal pain, pain due to injury, and promote blood circulation. Its main chemical constituents were alkaloids, which were divided into the two types of protoberberines and aporphines. Among them, some alkaloids were found to elicit profound effects on the dopaminergic system in the central nervous system, which plays an important role in regulating nociception. In this article, the chemical composition and structure-types, new methods of qualitative and quantitative analysis as well as characteristics of biotransformation, absorption, distribution, metabolism, excretion, pharmacokinetic, and drug-drug interaction for the alkaloids were revealed. These results would greatly contribute to the establishment of bioactive material base of Corydalis Rhizoma.


Subject(s)
Alkaloids , Chemistry , Animals , Corydalis , Chemistry , Drug Interactions , Drugs, Chinese Herbal , Chemistry , Metabolism , Pharmacokinetics , Humans , Medicine, Chinese Traditional , Methods , Papaveraceae , Chemistry , Rats , Rhizome , Chemistry
17.
Article in English | WPRIM | ID: wpr-101966

ABSTRACT

BACKGROUND/AIMS: DA-9701 (Motilitone) is a new prokinetic agent formulated with Corydalis Tuber and Pharbitis Seed. We assessed the efficacy of DA-9701 in symptomatic patients with minimal change esophagitis. METHODS: Patients with minimal change esophagitis presenting with reflux or dyspeptic symptoms were randomly assigned to receive either DA-9701 30 mg or placebo t.i.d. (means 3 times a day). After 4 weeks of treatment, the primary efficacy end point determined by changes of the Nepean dyspepsia index questionnaire-Korean version (NDI-K) symptom scores, was analyzed. RESULTS: Forty-two and 39 patients were assigned to the treatment and control groups, respectively. After 4 weeks, NDI-K symptom scores were reduced from 35.4 to 13.5 (P < 0.001) and from 43.0 to 27.7 (P < 0.001) in the treatment and the control groups, respectively. However, changes in the symptom scores did not differ between the 2 groups (P = 0.741). Although the quality of life scores were significantly improved after 4 weeks in both groups, changes in the quality of life score between the baseline value and that at 4 weeks did not differ between the 2 groups. The reflux symptom score was significantly improved in the treatment group compared to the placebo group in patients aged 65 years or older (P = 0.035). CONCLUSIONS: Although NDI-K symptom scores and quality of life scores were improved after 4 weeks of treatment compared with baseline values in patients with minimal change esophagitis, DA-9701 did not improve the symptom scores or quality of life scores compared with the placebo.


Subject(s)
Corydalis , Dyspepsia , Esophagitis , Humans , Quality of Life
18.
Article in Chinese | WPRIM | ID: wpr-346863

ABSTRACT

<p><b>OBJECTIVE</b>To study the biotransformation by human intestinal flora, and the absorption and transportation characteristic in a model of human colon adenocarcinoma cell lines (Caco-2 cell) monolayer of d-corydaline (CDL) and tetrahydropalmatine (THP).</p><p><b>METHOD</b>CDL or THP was incubated with crude enzymes of human intestinal flora under the anaerobic environment and 37 degrees C conditions to transform CDL or THP. Caco-2 cell monolayer was used as an intestinal epithelial cell model for determination of the permeability of CDL or THP from apical side (AP side) to basolateral side (BL side) or from BL side to AP side. Transportation parameters and permeability coefficients (P(app)) were then calculated, and P(app) values were compared with the reported values for model compounds, propranolol as a well absorbed drug and atenolol as a poor absorbed drug. The concentration of CDL or THP was measured by HPLC coupled with photodiode array detector.</p><p><b>RESULT</b>CDL or THP in the human intestinal flora incubation system did not happen biotransformation. In the Caco-2 cell monolayer model, the P(app) magnitudes of both CDL and THP were 1 x 10(-5) cm x s(-1) in the bi-directional transport, which were identical with propranolol. And their transports were concentration dependent between 0-180 min.</p><p><b>CONCLUSION</b>Both CDL and THP may be stable in the human intestinal flora incubation system, and their absorption and transportation in the human Caco-2 cell monolayer model are mainly via passive diffusion mechanism.</p>


Subject(s)
Bacteria , Metabolism , Berberine Alkaloids , Metabolism , Pharmacokinetics , Biological Transport , Biotransformation , Caco-2 Cells , Corydalis , Chemistry , Drugs, Chinese Herbal , Metabolism , Pharmacokinetics , Humans , Intestinal Absorption , Intestines , Metabolism , Microbiology , Models, Biological
19.
Article in Chinese | WPRIM | ID: wpr-319677

ABSTRACT

<p><b>OBJECTIVE</b>To study and compare the effect of Corydalis yanhusuo and L-THP on dopamine neurotransmitter and D2 receptor of reward circuitry in various cerebral areas of conditioned place preference model rats and the comparison of their effects.</p><p><b>METHOD</b>The CPP model was established by injecting morphine in rats with increasing doses for 10 days. The initial dose of 10 mg x kg(-1), and the final dose of 100 mg x kg(-1), with 10 mg x kg(-1) increased each day. At 48 h after the final training, CPP was adopted to detect the successful establishment of the model. On the same day (12 d), they were orally administered with 2, 1, 0.5 g x kg(-1) C. yanhusuo (containing 0.153, 0.077 and 0.038 mg L-THP) and L-THP (3.76, 1.88, 0.94 mg x kg(-1)) for six days. On 18 d, CPP test was performed again. Next day, HPLC was adopted to determine the content of dopamine neurotransmitters of reward circuitry in VTA-NAc-PFC; Immunohistochemistry and Western blotting were adopted to detect the expression of D2 receptors.</p><p><b>RESULT</b>Compared with the physiological saline treatment group, C. yanhusuo (2, 1 g x kg(-1)) and L-THP (3.76, 1.88 mg x kg(-1)) groups showed that rats stayed in a notably shorter period in white boxes (morphine-accompanied boxes) (P < 0.01 or P < 0.05), and revealed a remarkably lower dopamine content in VTA, NAc and PFC and the significant increase in the expression of D2 receptor (P < 0.01 or P < 0.05).</p><p><b>CONCLUSION</b>The down-regulation of the increased dopamine content in reward nervous circuitry and the up-regulation of the expression of D2 receptor may be one of mechanisms of C. yanhusuo and L-THP in accelerating the recession of morphine's CPP effect Regarding the inhibition of morphine's CPP effect and the effect on dopamine system, the effect of C. yanhusuo traditional Chinese medicine containing one-fold L-THP monomer is equal to that of the independent application of around 24-fold L-THP monomer.</p>


Subject(s)
Animals , Berberine Alkaloids , Brain , Metabolism , Conditioning, Operant , Corydalis , Chemistry , Dopamine , Metabolism , Humans , Male , Morphine , Plant Extracts , Rats , Rats, Sprague-Dawley , Receptors, Dopamine D2 , Genetics , Metabolism , Substance-Related Disorders , Drug Therapy , Genetics , Metabolism , Psychology
20.
Article in English | WPRIM | ID: wpr-202366

ABSTRACT

Motilitone(R) (DA-9701) is a new herbal drug that was launched for the treatment of functional dyspepsia in December 2011 in Korea. The heterogeneous symptom pattern and multiple causes of functional dyspepsia have resulted in multiple drug target strategies for its treatment. DA-9701, a compound consisting of a combination of Corydalis Tuber and Pharbitidis Semen, has being developed for treatment of functional dyspepsia. It has multiple mechanisms of action such as fundus relaxation, visceral analgesia, and prokinetic effects. Furthermore, it was found to significantly enhance meal-induced gastric accommodation and increase gastric compliance in dogs. DA-9701 also showed an analgesic effect in rats with colorectal distension induced visceral hypersensitivity and an antinociceptive effect in beagle dogs with gastric distension-induced nociception. The pharmacological effects of DA-9701 also include conventional effects, such as enhanced gastric emptying and gastrointestinal transit. The safety profile of DA-9701 is also preferable to that of other treatments.


Subject(s)
Analgesia , Animals , Compliance , Corydalis , Dogs , Dyspepsia , Gastric Emptying , Gastrointestinal Transit , Hypersensitivity , Korea , Nociception , Pharmacology , Rats , Relaxation , Semen
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