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1.
Article in Chinese | WPRIM | ID: wpr-909572

ABSTRACT

OBJECTIVE Compound Kushen injection (CKI) is a bis-herbal formulation extracted from Kushen (Radix Sophorae Flavescentis) and Baituling (Rhizoma Heterosmilacis Japonicae). Clinically, it is used as the adjuvant treat?ment of cancer. However, with the increased application, the cases of immediate hypersensitivity reactions (IHRs) also gradually rise. In this study, we investigated the underlying mechanism(s) and active constituent(s) for CKI-induced IHRs in experimental models. METHODS T helper 2 (Th2) immunity-amplified mice were prepared by aluminum adjuvant. Anaphylactic shock was detected by measuring rectal thermometry in propranolol pretreated mice. For evaluating micro?vascular permeability, Evans blue extravasation assay was used. Platelet-activating factor (PAF), serum total IgE (tIgE) and mouse mast cell protease 1 (MMCP1) were measured by ELISA. RESULTS The obtained results showed that CKI did not elevate serum tIgE and MMCP1 after consecutive immunization for five weeks, but could induce Evans blue extravasation (local) and cause obvious hypothermia (systemic) after a single injection. Further study showed that alka?loids in Kushen, especially matrine, were responsible for CKI-induced IHRs. Mechanism study showed that various PAF receptor antagonists could significantly counter CKI-induced IHRs locally or systemically. In cell system, CKI was able to promote PAF production in a non-cell-selective manner. In cell lysate, the effect of CKI on PAF production became stron?ger and could be abolished by blocking de novo pathway. CONCLUSION In conclusion, our study identifies, for the first time, that CKI is a PAF inducer. It causes non-immunologic IHRs, rather than IgE-dependent IHRs, by promoting PAF production through de novo pathway. Alkaloids in Kushen, especially matrine, are the prime culprits for IHRs. Our find?ings may provide a potential approach for preventing and treating CKI-induced IHRs.

2.
Article in Chinese | WPRIM | ID: wpr-879135

ABSTRACT

The absorption is the key to the resulted efficacy of orally administered drugs and the small intestine is the main site to absorb the orally administered drug. In this paper, internationally recognized human colon adenocarcinoma cell line(Caco-2) monola-yer model which can simulate small intestinal epithelial cell was used to comparatively study the absorption and transportation diffe-rences of total coumarins and main individual coumarin in Angelica dahurica 'Yubaizhi' by separately using 6-and 12-well plates. It was found that apparent permeability coefficient(P_(app)) values of oxypeucedanin hydrate, byakangelicin and phellopterin were at the quantitative degree of 1 × 10~(-5) cm·s~(-1) when the individual administration was conducted independently, indicating that they were well-absorbed compounds. P_(app) ratio of their bi-directional transportation was close to 1, indicating that they can be absorbed across Caco-2 monolayer by passive diffusion mechanism without carrier mediation during the transportation. The similar trend of transportation was also observed for imperatorin, isoimperatorin and bergapten. The P_(app) values of oxypeucedanin hydrate, byakangelicin and bergapten were at quantitative degree of 1 × 10~(-5) cm·s~(-1) when the administration of total coumarins in Angelica dahurica 'Yubaizhi' was conducted, indicating that they were well-absorbed compounds. The results were consistent with those of independent administration of individual coumarins. Whereas, the P_(app) values of imperatorin, phellopterin and isoimperatorin in the total coumarins decreased, indicating that the interaction between compounds may exist although the P_(app) value ratio of bi-directional transportation was between 0.5 and 1.5. The results laid the foundation for intestinal absorption study of Angelica dahurica 'Yubaizhi' coumarins in compound Chinese medicine.


Subject(s)
Angelica , Caco-2 Cells , Coumarins , Drugs, Chinese Herbal , Humans , Intestinal Absorption , Plant Roots
3.
Article in Chinese | WPRIM | ID: wpr-774520

ABSTRACT

To establish an HPLC characteristic fingerprint method of Fuke Qianjin Capsules,and determine the contents of its main components. The analysis was carried out on a Kromasil 100-5-C18 analytical column(4. 6 mm ×250 mm,5 μm) with gradient elution by acetonitrile(A)-0. 1% phosphoric acid aqueous solution(B),a flow rate at 1. 0 m L·min-1 and the detection wavelength of 254 nm.The column temperature was 30 ℃,and the injection volume was 10 μL. The determination method of genistin,jatrorrhizine,andrographolide and 14-deoxy-11,12-didehydroandrographolide index components were studied methodologically. The common mode of the characteristic fingerprint of Fuke Qianjin Capsules was set up with 8 common peaks,which were identified as genistin,jatrorrhizine,palmatine,berberine,andrographolide,14-deoxy-11,12-didehydroandrographolide,Z-ligustilide,and Z-3-butylidenephthalide,respectively,in comparison with the references. The similarities of 20 batches of Fuke Qianjin Capsules samples were above 0. 95. All of the above-mentioned 4 analytes could be well separated under the optimized chromatographic conditions. RSD of precision and repeatability experiment were both less than 1. 5%,and the sample solution was stable during 72 h. All of the compounds had a good linearity and linear range. The contents of genistin,jatrorrhizine,andrographolide,and 14-deoxy-11,12-didehydroandrographolide in 20 batches of Fuke Qianjin Capsules samples were 28. 66-56. 04,94. 77-197. 92,1 705. 33-4 148. 93 and 462. 16-1 225. 96 μg in each capsule,respectively. The developed HPLC characteristic fingerprint and quantitative analysis methods were reliable,accurate and sensitive,and could be used effectively evaluate the quality of Fuke Qianjin Capsules samples.


Subject(s)
Capsules , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Chemistry , Phytochemicals
4.
Article in Chinese | WPRIM | ID: wpr-690495

ABSTRACT

Fukeqianjin formula, a traditional Chinese medicine compound, consists of eight Chinese medicinal materials including roots of Moghania macrophylla, roots of Rosa laevigata, aerial parts of Andrographis paniculata, caulis of Mahonia fortunei, roots of Zanthoxylum dissitum, roots of Angelica sinensis, caulis of Spatholobus suberectus, and roots of Codonopsis pilosula. The chemical constituents from Fukeqianjin formula were studied in this paper. The compounds were separated and purified by repeated column chromatographic methods including silica gel, Sephadex LH-20, macroporous adsorptive resin, and reverse phase high performance liquid chromatography. And their chemical structures were determined by spectral data analyses. Thirty-eight compounds were obtained and identified as Z-3-butylidenephthalide (1), Z-ligustilide (2), senkyunolide I (3), senkyunolide H (4), vanillin (5), 7-O-methylwogonin (6), wogonin (7), panicolin (8), 19-hydroxy-8(17),13-labdadien-15,16-olide (9), andrograpanin (3,14-dideoxyandrographolide; 10), andrographolide (11), 14-deoxy-11,12-didehydroandrographolide (12), isoandrographolide (13), andrographin (2'-O-methylskullcapflavone, 14), biochanin A (15), 5-hydroxy-7,8,2',5'-tetramethoxyflavone (16), formononetin (17), daidzein (18), genistein (19), benzoic acid (20), vanillic acid (21), trans-ferulic acid (22), salicylic acid (23), daidzin (24), genistein-7-O-β-D-apiofuranosyl-(1→6)-O-β-D-glucopyranoside (25), apigenin-7-O-β-D-glucuronide (26), andrographidin C (27), apigenin-7-O-β-D-(6"-methyl)glucuronide (28), neoandrographolide (29), genistin (30), andrographiside (31), 14-deoxy-11,12-didehydroandrographiside (32), lobetyolin (33), epicatechin (34), catechin (35), palmatine (36), berberine (37), and jatrorrhizine (38), respectively. From the results of an individual medicinal material studies, it can be judged that compounds 17, 19, 24 and 30 as flavonoids came from the roots of M. macrophylla, compounds 36-38 as alkaloids came from the caulis of M. fortunei, compounds 6-8, 14, 16, and 27 as flavonoids as well as 9-13, 29, 31, and 32 as diterpenes came from the aerial parts of A. paniculata, compound 5 as phenols came from the roots of Z. dissitum, compounds 1-4 as phthalides as well as compound 22 as phenylpropanoids came from the roots of A. sinensis, compound 33 as alkynes came from the roots of C. pilosula, compounds 15, 17-19 as flavonoids as well as compound 21 as phenolic acids came from the caulis of S. suberectus. While compounds 34 and 35 as flavanoids could come from both the caulis of S. suberectus and roots of R. laevigata. The chemical composition of traditional Chinese medicine compound can be tracked from the original sources. This work provides a demonstration for the material basis study of traditional Chinese medicine compound. Compounds 25, 26 and 28 have not so far been isolated and identified from the above-mentioned single herb.

5.
Article in Chinese | WPRIM | ID: wpr-335873

ABSTRACT

Tongmai formula (TMF) is a drug combination of three components including Puerariae Lobatae Radix [roots of Pueraria lobata], Salviae Miltiorrhizae Radix (roots of Salvia miltiorrhiza) and Chuanxiong Rhizoma (rhizomes of Ligusticum chuanxiong) in a weight ratio of 1∶1∶1. The absorption and transport of isoflavonoid compounds from Tongmai formula across human intestinal epithelial (Caco-2) cells in vitro were studied in this paper. The assay isoflavonoid compounds include daidzein, formononetin, 5-hydroxylononin, ononin, daidzin, 3'-methoxypuerarin, genistin, puerarin, formononetin-8-C-β-D-apiofuranosyl-(1→6)-O-β-D-glucopyranoside, formononetin-7-O-β-D-apiofuranosyl-(1→6)-O-β-D-glucopyranoside, lanceolarin, kakkanin, daidzein-7,4'-di-O-β-D-glucopyranoside, mirificin, 3'-hydroxypuerarin, 3'-methoxydaidzin, formononetin-8-C-β-D-xylopyranosyl-(1→6)-O-β-D-glucopyranoside, genistein-8-C-β-D-apiofuranosyl-(1→6)-O-β-D-glucopyranoside, genistein-7-O-β-D-apiofuranosyl-(1→6)-O-β-D-glucopyranoside (ambocin), 3'-hydroxymirificin, 6″-O-β-D-xylosylpuerarin, biochanin A-8-C-β-D-apiofuranosyl-(1→6)-O-β-D-glucopyranoside, 3'-methoxydaidzein-7,4'-di-O-β-D-glucopyranoside, daidzein-7-O-β-D-glucopyranosyl-(1→4)-O-β-D-glucopyranoside, and daidzein-7-O-α-D-glucopyranosyl-(1→4)-O-β-D-glucopyranoside. By using human Caco-2 monolayer as an intestinal epithelial cell model in vitro, the permeability of above-mentioned 25 isoflavonoids in TMF were studied from the apical (AP) side to basolateral (BL) side or from the BL side to AP side. The assay compounds were determined by reversed phased high-performance liquid chromatography (HPLC) coupled with UV detector. Transport parameters and apparent permeability coefficients (Papp) were then calculated and and compared with those of propranolol and atenolol, which are the transcellular transport marker and as a control substance for high and poor permeability, respectively. The Papp values of daidzein and formononetin were (2.55±0.03) ×10⁻⁵,(3.06±0.01) ×10⁻⁵ cm•s⁻¹ from AP side to BL side, respectively, and (2.62±0.00) ×10⁻⁵, (2.65±0.11) ×10⁻⁵ cm•s⁻¹ from BL side to AP side, respectively. Under the condition of this experiment, the Papp value was (2.66±0.32) ×10⁻⁵ cm•s⁻¹ for propranolol and (2.34±0.10) ×10⁻⁷ cm•s⁻¹ for atenolol. The Papp values of daidzein and formononetin were at a same magnitude with those of propranolol. And the Papp values of other 23 isoflavonoid compounds were at a same magnitude with those of atenolol. On the other hand, the rats of Papp AP→BL/Papp BL→AP of daidzein and formononetin on the influx transport were 0.97 and 1.15, respectively. It can be predicted that daidzein and formononetin can be absorbed across intestinal epithelial cells to go to the body circulation by the passive diffusion mechanism and they were assigned to the well-absorbed compounds. Other 23 isoflavonoid compounds were assigned to the poorly absorbed compounds. Because of the rats of Papp AP→BL/Papp BL→AP of 5-hydroxylononin, genistin, lanceolarin, kakkanin, and genistein-7-O-β-D-apiofuranosyl-(1→6)-O-β-D-glucopyranoside were 0.18, 0.28, 0.45, 0.38, 0.49, they may have been involved in the efflux mechanism in Caco-2 cells monolayer model from the BL side to AP side direction.

6.
Article in Chinese | WPRIM | ID: wpr-275162

ABSTRACT

The chemical constituents from lipophilic parts in the roots of Angelica dahurica cv. Yubaizhi were studied in this paper. The compounds were separated and purified by repeated column chromatographic methods on silica gel and HPLC, and the chemical structures of compounds were determined by spectral data analyses. Thirty-three compounds were obtained and identified as isoimperatorin (1), imperatorin (2), stigmasterol (3), isooxypeucedanin (4), pabulenol (5), psoralen (6), bergapten (7), isodemethylfuropinarine (8), phellopterin (9), osthenol (10), alloimperatorin (11), xanthotoxin (12), xanthotoxol (13), isopimpinellin (14), alloisoimperatorin (15), β-sitosterol (16), oxyalloimperatorin (17), pabularinone (18), 5-hydroxy-8-methoxypsoralen (19), columbianetin (20), heracol (21), isogosferol (22), 2″R-neobyakangelicol (23), byakangelicin ethoxide (24), byakangelicin (25), oxypeucedanin hydrate (26), uracil (27), umbelliferone (28), bergaptol (29), demethylfuropinarine (30), isobyakangelicol (31), oxypeucedanin ethanolate (32), heraclenol (33). Among them, compounds 8, 10, 17, 21, and 30 were obtained from the roots of title plant for the first time.

7.
Article in Chinese | WPRIM | ID: wpr-304864

ABSTRACT

The chemical constituents of the Chinese red ginseng were systematically investigated by using various column chromatographic methods including D-101 macroporous adsorptive resins and open silica gel column chromatographies as well as high-performance liquid chromatography.Their chemical structures were identified by physico-chemical properties and spectral analyses.Fifty-two compounds were isolated from Chinese red ginseng decoction and identified as 20(S)-ginsenoside Rh₁ (1), 20(R)-ginsenoside Rh₁ (2), ginsenoside Rg₆ (3), 20(22) E-ginsenoside F₄ (4), ginsenoside Rk₃ (5), 20(22) E-ginsenoside Rh₄ (6), ginsenoside Rg₁ (7), 20(S)-ginsenoside Rf-1a(8), 20(S)-ginsenoside Rf(9), 20(R)-ginsenoside Rf(10),20(S)-notoginsenoside R₂ (11),20(R)-notoginsenoside R₂ (12), 20(S)-ginsenoside Rg₂ (13), 20(R)-ginsenoside Rg₂ (14), ginsenoside Rs₂ (15),ginsenoside Rs₁ (16),ginsenoside Rd(17),notoginsenoside R₁ (18),ginsenoside Re₂ (19), ginsenoside Re(20), 20-gluco-ginsenoside Rf(21),quinquenoside-R₁ (22),ginsenoside Ro methyl ester(23),ginsenoside Ro(24),ginsenoside Rb₁ (25),ginsenoside Rc(26),ginsenoside Rb₂ (27),ginsenoside Ra₂ (28),ginsenoside Ra₃ (29),ginsenoside Rb₃ (30),20(22)Z-ginsenoside Rh₄ (31),chikusetsusaponin IVa butyl ester(32), 20(22)Z-ginsenoside Rs₄ (33),ginsenoside Rs₅ (34),20(22)E-ginsenoside Rs₄ (35),zingibroside R1-6'-butyl ester(36), chikusetsusaponin IVa methyl ester(37),20(S)-ginsenoside Rs₃ (38),20(R)-ginsenoside Rs₃ (39),zingibroside R1-6'-methyl ester(40),ginsenoside Rz₁ (41),ginsenoside Rk₁ (42),ginsenoside Rg₅ (43),23-O-methylginsenoside-Rg₁ ₁ (44),12β,25-dihydroxydammar-20(22)E-ene-3-O-β-D-glucopyranosyl-(1→2)-O-β-D-glucopyranoside(45), 20(22)Z-ginsenoside F₄ (46),3β,12β-dihydroxydammar-20(22)E,24-diene-6-O-β-D-xylopyranosyl-(1→2)-O-β-D-glucopyranoside(47), 20(S)-ginsenoside Rg₃ (48),20(R)-ginsenoside Rg₃ (49),20(22)E-ginsenoside Rg₉ (50),ginsenoside-Ro-6'-butyl ester(51), and polyacetyleneginsenoside Ro(52). Compounds 8, 12, 31-33, 36, 37, 44, 45, 47 and 51 were isolated from the P. ginseng, and compounds 19, 23 and 46 were isolated from Chinese red ginseng for the first time.

8.
Article in Chinese | WPRIM | ID: wpr-275181

ABSTRACT

To establish MDCK-pHaMDR cell model and standard operation procedure for assessing the blood-brain barrier permeability of chemical components of traditional Chinese medicine. MDCK-pHaMDR cell model was evaluated by determining the morphology features, transepithelial electrical resistance, bidirectional transport and intracellular accumulation of Rhodamine 123 and the apparent permeability of positive control drugs caffeine and atenolol. The MDCK-pHaMDR cell model had satisfactory integrity and tightness, and stable expression of P-gp. In addition, the transport results of the positive control drugs were consistent with the reported values in literature. All the parameters tested of the MDCK-pHaMDR cell model were consistent with the requirements, so the model can be used to study the blood-brain barrier permeability of chemical components of traditional Chinese medicine.

9.
Article in Chinese | WPRIM | ID: wpr-230086

ABSTRACT

Tongmai granule (TM) is composed of Puerariae Lobatae Radix (Gegen), Salviae Miltiorrhizae Radix et Rhizoma(Danshen) and Chuanxiong Rhizoma(Chuanxiong). It has been used to treat ischemic cardio-cerebrovascular diseases for decades. For the purpose of elucidating its pharmacodynamic material foundation, the absorption and pharmacokinetic property of TM were investigated in acute myocardial ischemic model beagles. All serum samples were extracted before analysis with ethyl acetate after being acidified by hydrochloric acid. Under negative ESI detection mode, the chromatographic separation was carried out with monolithic C₁₈ column for gradient elution. A simultaneous quantitative analysis was made on 15 polyphenols, including 8 from Gegen, 5 from Danshen and 2 from Chuanxiong, in 8.5 min. The validation result demonstrated the specificity, accuracy and precision of the method in line with the bioanalysis requirements. After TM solution was administrated to acute myocardial ischemic model beagles through duodenum injection, serum samples were collected after 6 h. The quantitative detection proved the prompt absorption of TM, all of the components were detectable in the blood samples 5 min later, and reached peak respectively at 0.18-3.83 h after administration. The components presented large variabilities. The most components were exposed in serum with puerarin and salvianic acid A, followed by 3'-methoxypuerarin, mirificin, and 3'-hydroxypuerarin. The study proves puerarin and salvianic acid A are dominating active components of TM in acute myocardial ischemic model beagles.

10.
Article in English | WPRIM | ID: wpr-812582

ABSTRACT

Angelica dahurica (A. dahurica) is a traditional Chinese medicinal plant being used in clinical practice. The present study demonstrated that A. dahurica could reduce white-fat weight in high-fat-diet hyperlipidemic mice, decrease total cholesterol and triglyceride concentrations in the livers of both high-fat-diet and Triton WR1339 induced hyperlipidemic mice, and enhance the total hepatic lipase activities of them. These findings were further supported by the results derived from the experiments with HepG2 cells in vitro. In addition, the proteins related to lipids metabolism were investigated using LC-MS/MS, indicating that genes of lipid metabolism and lipid transport were regulated by A. dhurica. The results from LC-MS/MS were further conformed by Western blot and real time PCR assays. A. dahurica could down-regulate the expression of catalase (CAT) and sterol carrier protein2 (SCP2) and up-regulate the expression of lipid metabolism related genes-lipase member C (LIPC) and peroxisome proliferator-activated receptor gamma (PPARγ). In the Triton WR1339 mouse liver and HepG2 cells in vitro, A. dahurica was able to increase the expression of LIPC and PPARγ, confirming the results from in vivo experiments. Imperatorin showed the same activity as A. dahurica, suggesting it was one of the major active ingredients of the herb. In conclusion, our work represented a first investigation demonstrating that A. dahurica was able to regulate lipid metabolism and could be developed as a novel approach to fighting against fatty liver and obesity.


Subject(s)
Angelica , Chemistry , Animals , Carrier Proteins , Genetics , Metabolism , Cholesterol , Metabolism , Drugs, Chinese Herbal , Fatty Liver , Drug Therapy , Genetics , Metabolism , Humans , Liver , Metabolism , Male , Mice , Mice, Inbred ICR , Obesity , Drug Therapy , Genetics , Metabolism , PPAR gamma , Genetics , Metabolism , Triglycerides , Metabolism
11.
Article in Chinese | WPRIM | ID: wpr-337968

ABSTRACT

The chemical constituents from lipophilic parts in the roots of Angelica dahurica var. formosana cv. Chuanbaizhi were studied in this paper. The compounds were separated and purified by repeated column chromatographic methods on silica gel and HPLC, and the chemical structures of compounds were determined by spectral data analyses. Twenty-nine compounds were obtained and identified as isoimperatorin (1), β-sitosterol (2), imperatorin (3), bergapten (4), osthenol (5), xanthotoxin (6), isoimpinellin (7), dehydrogeijerin (8), phellopterin (9), isodemethylfuropinarine (10), 7-demethylsuberosin (11), alloimperatorin (12), xanthotoxol (13), isooxypeucedanin (14), alloisoimperatorin (15), demethylfuropinarine (16), 5-hydroxy-8-methoxypsoralen (17), oxypeucedanin methanolate (18), pabulenol (19), byakangelicin (20), marmesin (21), (+) -decursinol (22), heraclenol (23), oxypeucedanin hydrate (24), marmesinin (25), ulopterol (26), erythro-guaiacylglycerol-β-ferulic acid ether (27), threo-guaiacylglycerol-β-ferulic acid ether (28), and uracil (29). Compounds 5, 8, 11, 18, 21-23, and 26-28 were obtained from the roots of title plant for the first time.


Subject(s)
Angelica , Chemistry , Coumarins , Chemistry , Furocoumarins , Chemistry , Methoxsalen , Chemistry , Phytochemicals , Chemistry , Plant Roots , Chemistry
12.
Article in Chinese | WPRIM | ID: wpr-853881

ABSTRACT

Objective: To study the chemical constituents of saponins in the stems and leaves of Panax ginseng. Methods: The chemical constituents were isolated and purified by various chromatographic methods, and the chemical structures were identified by NMR and MS data analyses. Results: A total of 39 compounds were isolated and identified. Among them, 17 compounds were determined as ginsenoside Re (1), 20(S)-ginsenoside Rh1 (2), 20(R)-ginsenoside Rh1 (3), ginsenoside Rh5 (4), 20(E)-ginsenoside F4 (5), ginsenoside F2 (6), 20(S)-ginsenoside Rg3 (7), 20(R)-ginsenoside Rg3 (8), 20(S)-ginsenoside Rf2 (9), 20(R)-ginsenoside Rf2 (10), 20(S)- protopanaxadiol (11), 20(R)-protopanaxadiol (12), 20(S)-ginsenoside Rh2 (13), 20(R)-ginsenoside Rh2 (14), 20(S)-protopanaxatriol (15), 20(R)-protopanaxatriol (16), and ginsenoside Rd (17). Conclusion: Compound 9 is a new saponin. Compounds 2-10, 13, and 14 are rare ginsenosides.

13.
Article in Chinese | WPRIM | ID: wpr-237727

ABSTRACT

The chemical constituents from polarity part in the roots of Angelica dahurica var. formosana cv. Chuanbaizhi were studied in this paper. The compounds were separated and purified by repeated column chromatographic methods on silica gel and HPLC, and the chemical structures of compounds were determined by spectral data analyses. Fourteen compounds were obtained and identified as tert-O-β-D-glucopyranosyl-(R)-byakangelicin (1), (2"S) -3"-O-β-D-glucopyranosyl-oxypeucedanin hydrate (2), marmesinin (3), sec-O-β-D-glucopyranosyl-byakangelicin (4), isofraxidin-7-O-β-D-glucopyranoside (5), benzyl-O-β-D-glucopyranoside (6), 8-O-β-D-glycopyranosylxanthotoxol (7), prenyl-O-β-D-glucopyranoside (8), scopolin (9), (2' R) -5'-hydroxymarmesin-5'-O-β-D-glucopyranoside (10), (2'S,3'R) -3'-hydroxymarmesinin (11), skimmin (12), benzyl-O-β-D-apiofuranosyl-(1"--> 6')-β-D-glucopyranoside (13), and decuroside IV (14). Among them, compounds 2, 5, 6, 8, and 10-13 were obtained from the roots of title plant for the first time.


Subject(s)
Angelica , Chemistry , Drugs, Chinese Herbal , Chemistry , Mass Spectrometry , Molecular Structure , Plant Roots , Chemistry
14.
Article in Chinese | WPRIM | ID: wpr-237693

ABSTRACT

The compound Chinese materia medica is the medication pattern of the traditional Chinese medicine for the disease prevention and treatment. The single Chinese materia medica (mostly in decoction pieces) is the prescription composition of the compound Chinese materia medica. The study of the effective substance basis of Chinese materia medica should be based on the chemical compositions of the compound Chinese materia medica as an entry point considering the different status of "Monarch, Minister, Assistant, and Guide" for a certain single Chinese materia medica in the different compound Chinese materia medica while substance basis research of a certain single Chinese materia medica should be a full component analysis as well as both stable and controllable quality. Substance basis research on Chinese materia medica is one of key scientific problems of inheriting, development and innovation of Chinese materia medica.


Subject(s)
China , Drug Discovery , Drugs, Chinese Herbal , Chemistry , Pharmacology , Humans , Materia Medica , Chemistry , Pharmacology , Medicine, Chinese Traditional
15.
Article in Chinese | WPRIM | ID: wpr-321394

ABSTRACT

Caco-2 cell monolayer model is widely utilized in drug absorption study and 12-well transwellTM plates were commonly used to study the absorption of different kinds of natural products. To establish a stable method for the study of traditional Chinese medicine prescription, 6-well plates were chosen because of the larger well volumes than 12-well plates. To study the impacts of collagen kinds, coating density as well as coating time on the cell culture, the transepithelial electrical resistance of Caco-2 cell monolayers grown on different collagen coating transwells was determined, and the permeations of propranolol and atenolol as standard markers were detected with HPLC. The results showed that the kinds of collagen, the different coating densities and coating time of rat tail collagen had no significant influences on the Caco-2 cell monolayer integrality and absorption capacity. 6-well plates coated with 2 micro g Scm-2 rat tail collagen for 1 hour were enough reliable and suitable for the study of traditional Chinese medicine prescription in vitro.


Subject(s)
Adsorption , Animals , Caco-2 Cells , Cell Culture Techniques , Methods , Collagen , Chemistry , Drug Prescriptions , Humans , Medicine, Chinese Traditional , Rats , Time Factors
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 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
18.
Article in Chinese | WPRIM | ID: wpr-855206

ABSTRACT

Objective: To study the absorption and transport characteristic of paeoniflorin (PF), oxypaeoniflorin (OP), benzoylpaeoniflorin (BP), tetraacetylpaeoniflorin (TP), pentaacetylpaeoniflorin (PP), and pentacacetylalbiflorin (PA) in human colon adenocarcinoma cell line Caco-2 cell monolayer model. Methods: The Caco-2 cell monolayers were used as an intestinal epithelial cell model. The permeability of the tested compounds from apical (AP) side to basolateral (BL) side or from BL side to AP side was evaluated. The concentration of the tested compounds was measured by HPLC coupled with UV detector. The transport parameters and apparent permeability coefficients (Papp) were calculated, and the Papp values were compared with the reported values for model compounds, Propranolol and Atenolol. Results: The Papp values of PF in the bi-directional transport and atenolol were at the quantitative degree of 10-7 cm/s. Whereas those of OP, BP, TP, PP, and PA were between atenolol and propranolol used as a control substance for low and high permeability, respectively. The absorption and transport of the tested compounds were concentration-dependent at the concentration range of 10-200 μmol/L for PF, OP, and BP, 10-150 μmol/L for TP and PA, and 10-100 μmol/L for PP. Conclusion: The six tested compounds could be absorbed across the intestinal epithelial cells by passive diffusion mechanism. PF is poorly absorbed compound and OP, BP, TP, PP, and PA are moderately absorbed compounds. BP has a role to promote atenolol uptake transporters in Caco-2 cell monolayer model.

19.
Article in English | WPRIM | ID: wpr-812638

ABSTRACT

Flos Trollii, the flowers of Trollius chinensis Bunge, has been widely used in Chinese and Mongolian medicine for its efficacy of heat-clearing and detoxification. This drug has both medicinal and edible applications, and has led to various pharmacognosy, natural product chemistry, and pharmacology studies. As a result, its chemical constituents and bioactivities have been well-characterized in recent years. Nevertheless, a couple of critical issues, such as the major effective components, are still unresolved. The present review summarizes research progress on this drug regarding the constituents and bioactivities based on investigations in these laboratories and the results reported in recent publications. In addition, the pending issues are discussed and constructive suggestions for further investigation are proposed.


Subject(s)
Animals , Drug Therapy , Drugs, Chinese Herbal , Chemistry , Pharmacology , Flowers , Chemistry , Humans , Ranunculaceae , Chemistry
20.
Article in Chinese | WPRIM | ID: wpr-291335

ABSTRACT

To study the chemical constituents in Tongmai formula (TMF) after biotransformation by human intestinal flora (HIF), water extract of TMF was anaerobically incubated with HIF at 37 degrees C. Column chromatographic methods over silica gel, Sephadex LH-20 and semi-preparative high-performance liquid chromatography as well as recrystallization were used to isolate and purify the chemical constituents in TMF after biotransformation by HIF. The chemical structures of isolated compounds were identified on the basis of MS and NMR data. Twenty-six compounds were obtained and identified as phenylpropionic acid (1), 6"-O-acetylpuerarin (2), formononetin(3), daidzein(4), p-hydroxyphenylpropionic acid (5), 3-indolepropionic acid (6), genistein (7), isoformononetin (8), isoononin (9), a mixture of (-)-puerol B-2"-O-glucopyranoside (10a) and (+) -puerol B-2"-O-glucopyranoside (10b), 8-hydroxydaidzein (11), puerol A (12), 3'-methoxy-6"-O-acetylpuerarin (13), 6"-O-acetyldaidzin (14), 3'-methoxydaidzin (15), puerol B (16), 3-methyluracil (17), genistin (18), daidzin (19), 3'-methoxypuerarin (20), mirificin (21), swertiamarin (22) , daidzein-7, 4'-O-glucoside (23), adenine (24), 3'-hydroxypuerarin (25), and puerarin (26). After biotransformation by HIF, the glycosides in TMF were transformed into aglycone and/or less glycosyl compounds along with some hydroxylation and demethylation reactions. Therefore, the glycosides in the TMF are the pro-drug.


Subject(s)
Bacteria , Metabolism , Biotransformation , Drugs, Chinese Herbal , Chemistry , Metabolism , Humans , Intestines , Metabolism , Microbiology , Microbiota , Molecular Structure
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