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This paper explored the chemical constituents of Boswellia carterii by column chromatography on silica gel, Sephadex LH-20, ODS column chromatography, and semi-preparative HPLC. The structures of the compounds were identified by physicochemical properties and spectroscopic data such as infrared radiation(IR), ultra violet(UV), mass spectrometry(MS), and nuclear magnetic resonance(NMR). Seven diterpenoids were isolated and purified from n-hexane of B. carterii. The isolates were identified as(1S,3E,7E,11R,12R)-11-hydroxy-1-isopropyl-4,8,12-trimethyl-15-oxabicyclo[10.2.1]pentadeca-3,7-dien-5-one(1),(1R,3S,4R,7E,11E)-4,8,12,15,15-pentamethyl-14-oxabicyclo[11.2.1]hexadeca-7,11-dien-4-ol(2), incensole(3),(-)-(R)-nephthenol(4), euphraticanoid F(5), dilospirane B(6), and dictyotin C(7). Among them, compounds 1 and 2 were new and their absolute configurations were determined by comparison of the calculated and experimental electronic circular dichroisms(ECDs). Compounds 6 and 7 were obtained from B. carterii for the first time.
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Estrutura Molecular , Boswellia/química , Diterpenos/química , Espectrometria de MassasRESUMO
Aim To investigate the hepatotoxic effect of aqueous extract of fructus psoraleae (WEFP) on lipopolysaccharide (LPS)-induced hepatotoxicity in SD rats under immune stress and its mechanism. Methods SD rats were divided into control (CON), LPS, WEFP, LPS+WEFP group. The LPS and LPS+WEFP groups were injected with 4 mg·kg-1 LPS via tail vein; 2 h later, the rats in WEFP group and LPS+WEFP group received the WEFP (1.1 g·kg-1·d-1) by oral gavage for seven consecutive days. Different endpoints such as body weight, liver index, bile flow rate, serum biochemical, histopathological changes, inflammatory cytokines, protein and mRNA expression levels were determined to clarify the liver toxicity and mechanism of WEFP. Results Compared with the CON group, rats in the LPS group had no significant changes in body weight, liver coefficient, serum ALT, AST, and ALP liver injury indicators; mild steatosis in the liver of the rats in the WEFP group did not cause liver damage; for rats in the LPS+WEFP group, body weight and bile excretion decreased, liver coefficient, serum ALT, AST, ALP, TBA levels significantly increased, and IL-1 and TNF-α secretion in the liver increased; at the same time, the pathological changes such as inflammatory reaction, cholestasis, and steatosis appeared in liver, RhoA mRNA and protein expression increased, and TLR4 and ICAM-1 pro-inflammatory gene expression increased, leading to acute liver injury. Conclusions The non-hepatotoxic dose of LPS can cause the same dose of psoralen to show more obvious liver toxicity, leading to the body's immunospecific response. Psoralen can cause immune stress rats to activate the expression of RhoA and other pro-inflammatory genes, further aggravate the release of inflammatory factors,and promote inflammatory reaction damage to liver cells and intrahepatic bile duct tissues,leading to obstruction of bile acid efflux and causing special effects such as heterogeneous liver injury.
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In light of related methods in Chinese Pharmacopoeia(2020 edition), this study established the quality standard for Lobeliae Chinensis Herba. The TLC identification method was established with silica gel GF_(254) thin layer plate, diosmin standard, linarin standard, and the reference material of Lobeliae Chinensis Herba. The loss on drying, total ash, acid-insoluble ash, and ethanol-soluble extracts of 18 batches of Lobeliae Chinensis Herba samples were determined according to the general principles in Chinese Pharmacopoeia. Then, HPLC was adopted in the establishment of characteristic chromatogram and content determination. The results showed that the established method can achieve good separation for diosmin, linarin, and lobetyolin. Based on the results of detection for 18 batches of Lobeliae Chinensis Herba samples, the draft quality standard was established, which was expected to provide reference for the revision of this medicinal herb in Chinese Pharmacopoeia.
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Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas/normas , Lobelia/química , Plantas Medicinais/químicaRESUMO
Eleven condensed tannins were isolated from the roots of Indigofera stachyodes by various column chromatography techniques including silica gel, octadecyl silica(ODS), Sephadex LH-20, and semi-preparative high performance liquid chromatography(HPLC). These compounds were identified on the basis of physicochemical properties, nuclear magnetic resonance(NMR) and mass spectrometry(MS) data as stachyotannin A(1), epicatechin-(2β→O→7,4β→8)-epiafzelechin-(4β→8)-catechin(2), cinnamtannin D1(3), cinnamtannin B1(4), epicatechin-(2β→O→7,4β→8)-epiafzelechin-(4α→8)-epicatechin(5), gambiriin C(6), proanthocyanidin A1(7), proanthocyanidin A2(8), aesculitannin B(9), proanthocyanidin A4(10), and procyanidin B5(11). Compound 1 is a new compound. Compounds 2-11 were isolated from Indigofera for the first time. Furthermore, compounds 1, 2, and 4-11 showed inhibitory effects on thrombin-induced ATP release in platelets.
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Cromatografia Líquida de Alta Pressão , Indigofera , Espectroscopia de Ressonância Magnética , Extratos Vegetais , ProantocianidinasRESUMO
Longxue Tongluo Capsules(LTC) has good efficacy against blood stasis syndrome during the recovery period of ischemic stroke. Its main active ingredient is the phenolic extract of Chinese dragon's blood. In our previous study, the primary mass fragmentation pathways of phenolic derivatives from LTC were clarified. Herein, the metabolites in rat plasma were characterized following the oral administration of loureirin A and loureirin C using liquid chromatography coupled with hybrid ion trap/time-of-flight mass spectro-metry(LC-IT-TOF-MS), with 18 and 55 metabolites identified, respectively. On this basis, with the help of the obtained accurate molecular weight, characteristic fragment ions, reference comparison, combined with LTC database and natural products database self-created in our group, 18 prototypes and 106 metabolites were tentatively identified in rat plasma after oral gavage of LTC at a dose of 500 mg·kg~(-1). Glucuronidation, sulfonation, and methylation were major biotransformation pathways of LTC. This study preliminarily clarified the LTC constituents absorbed into blood and laid the foundation for clarifying the effective substances of LTC.
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Animais , Ratos , Administração Oral , Cápsulas , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Medicamentos de Ervas Chinesas , Cromatografia Gasosa-Espectrometria de MassasRESUMO
This study aims to study the chemical components from the gum resin of Boswellia carterii. Five cembranoid diterpenes were isolated from the gum resin of B. carterii by various of column chromatographies including silica gel, Sephadex LH-20, and semi-preparative HPLC. Their structures were identified on the basis of physicochemical properties, mass spectrometry(MS), nuclear magnetic resonance(NMR), Ultraviolet(UV) and infrared(IR) spectroscopic data. These compounds were identified as(1S,2E,4R,5S,7E,11E)-4-methoxy-5-hydroxycembrane(1),(1R~*,4R~*,5E,8E,12E,15E)-4-hydroxycembra-5,8,12,15-tetraene(2), cembrene A(3),(3S,4S,7R)-4-hydroxycembrane(4), and pavidolide D(5). Compound 1 was a new compound. Compounds 2, 4, and 5 were obtained from the gum resin of B. carterii for the first time. Compound 2 showed weak inhibition on the human liver cancer cell line HepG2.
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Humanos , Boswellia , Linhagem Celular , Diterpenos , Estrutura Molecular , Resinas VegetaisRESUMO
Five cadinane-type sesquiterpenoids were isolated from the n-hexane extract of Commiphora myrrha by using various chromatographic techniques, including silica gel, ODS and semi-preparative HPLC. Their structures were identified by physicochemical properties and spectroscopic data. These compounds were defined as (3S,4R)-3,9-dimethoxymyrrhone (1), 9-methoxymyrrhone (2), myrrhone (3), commiterpene B (4) and comosone Ⅱ (5). Compound 1 is a new compound, of which the absolute configuration was established by single crystal X-ray crystallographic analysis. Compound 5 is firstly isolated from the Commiphora genus.
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Objective@#To study the pollution status of polybrominated diphenyl ethers (PBDEs), polychlorinated biphenyls (PCB), polychlorinated dibenzo-p-dioxins and dibenzofurans (PCDD/Fs) in cord blood of newborns in an e-waste dismantling area of Guangdong Province.@*Methods@#We recruited 20 eligible mothers and newborns who could meet the inclusion criteria in local hospitals of Guiyu in 2007. The inclusion criteria included directly engaged in dismantling e-waste during pregnancy and within 1 year before pregnancy; living in the e-waste dismantling workshops or the distance between living place and the e-waste dismantling areas was ≤200 m; the father of newborn was directly engaged in electronic waste dismantling for more than 1 year; the frequency of visiting the e-waste dismantling workshop during pregnancy was ≥3 times in a week. Questionnaires and physical examinations were performed on maternal and neonatal, and cord blood was collected from newborns to detect PCDD/Fs, PCB and PBDE. The concentration level of organic pollutants was corrected by the blood lipid content, and the total toxicity equivalent was calculated. The correlation between three compounds was analyzed by Spearman correlation.@*Results@#The mothers of the 20 newborns were (23.45±3.27) years old and lived for more than 5 years. The number of one parent engaged in e-waste dismantling, the mother or father smoking, and parent engaged in e-waste dismantling work were 3, 13, 15 and 19, respectively. The weight of newborns ranged from 2.5 to 3.6 kilogram and the Apgar score was 10 points. No adverse birth outcomes such as preterm birth, malformation or stillbirth were found. The median (maximum, minimum) concentration of PCBs, PCDD/Fs and PBDEs in cord blood were 263.22 (328.29, 244.19), 38.42 (147.49, 12.68), 39.33 (265.11, 14.81) pg/g lipid, respectively. The median (maximum, minimum) of toxic equivalence concentrations of PCDD/Fs and PCB were 3.94 (9.24, 2.69) and 15.95 (26.64, 9.28) pg TEQ/g lipid. PBDE, the proportion of PBDE, PCB and PCDD/Fs in cord blood was 50.41%, 49.25% and 0.34%, respectively. PCBs and PBDEs were positively correlated (r=0.733, P=0.039).@*Conclusion@#The high concentrations of PCDD/Fs, PCB, and PBDE were detected in the e-waste dismantling area. It is recommended that the risk of such substances on the health of local people should be assessed in a timely manner.
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Increasing e-waste has become a major problem for global environment and public health. In the process of dismantling and recycling of disordered electronic waste, heavy metals such as lead and brominated flame retardants and organic substances are released into environmental media such as air, soil, dust and water, which is harmful to the health of local residents. Taking an e-waste dismantling area in Guangdong Province as an example, this paper reviews exposure levels of heavy metals and organic matters in e-waste recycling areas in China, as well as the health effects of local residents. Previous studies have found that e-waste recycling activities led to serious environmental pollution and high exposure levels of heavy metals and organic matters in local residents, which has a certain impact on the physiological functions of various human systems. The establishment of a centralized dismantling zone can effectively reduce the load level of various pollutants.
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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.
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Amidas , Corydalis , Química , Glucosídeos , Compostos Fitoquímicos , TiraminaRESUMO
Objective To synthesize obeticholic acid and optimize the preparation process. Method Obeticholic acid was synthesized from (E) -3α-hydroxyl-6-ethylidene-7-keto-5β-cholane-24-acid via the reactions in cluding the double bound hydrogenation, inversion of α-ethyl′s configuration, and stereospecific reduction of the carbonyl group. Results The structures of the compounds were confirmed by1 H NMR, 13 C NMR and MS data. The preparation process was optimized, with the overall yield about 69%.Conclusion An industrial process for the preparation of obeticholic acid has been developed, available for the safety and quality control as well as the quality improvement of final products, which could meet the registration requiremens of Center for Drug Evalution (CDE).
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Sofosbuvir is a new type of direct-acting antiviral(DAA)drugs against hepatitis C.By competitive combination to NS5B polymerase activity sites,sofosbuvir can terminate genome synthesis of newly born virus,and finally inhibit the replication of hepatitis C virus(HCV).The research and development process of sofosbuvir is based on the principles of nucleoside antiviral drug metabolism.The subtle structure modification improves the drug′s structure stability and absorption process,which makes sofosbuvir a liver targeted anti-HCV drug.Sofosbuvir has become a clinical fundamental drug for anti-HCV infection,and then used alone or in combination with other drugs,with higher recovery rate,better safety and anti-drug resistance.This article reviews the research back?ground,development process,clinical application and synthetic methods for sofosbuvir.
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Chemical constituents from the fruits of Vitex negundo var. cannabifolia and their nitric oxide (NO) inhibitory and cytotoxic activities were investigated. The compounds were isolated and purified by various column chromatography, and their structures were identified by physiochemical properties and spectroscopic data. Thirteen lignans and six phenolic compounds were isolated from the CH2Cl2 extract of the fruits of V. negundo var. cannabifolia, respectively. Their structures were elucidated as 6-hydroxy-4-(4-hydroxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxy-3,4-dihydro-2-naphthaldehyde (1), vitedoin A (2), vitexdoin F (3), detetrahydroconidendrin (4), vitexdoin E (5), 4-oxosesamin (6), L-sesamin (7), (+)-beechenol (8), ligballinol (9), 2-(4-hydroxyphenyl)-6-(3-methoxy-4-hydroxyphenyl)-3,7-dioxabicyclo[3.3.0]octane (10), (-)-pinoresinol (11), balanophonin (12), thero-guaiacylglycerol-β-coniferyl aldehyde ether (13), trans-p-coumaryl aldehyde (14), coniferyl aldehyde (15), 5,7-dihydroxychromone (16), trans-3,5-dimethoxy-4-hydroxy-cinnamic aldehyde (17), frambinone (18), and alternariol 4-methyl ether (19). Compounds 8-10,14,18,19 were firstly isolated from Verbenaceae family, compound 13 was obtained from Vitex species, and 6,7,12,15-17 from V. negundo var. cannabifolia for the first time, respectively. The isolated compounds were evaluated for their anti-inflammatory and cytotoxic effects in vitro. Eight compounds (3,5,7,10,11,14,15,17) showed inhibition against NO production in LPS-stimulated RAW 267.4 cells (IC₅₀ in the range of 7.8-81.1 μmol•L⁻¹) and four compounds (1-4) showed cytotoxicity on HepG-2 cells (IC₅₀ in the range of 5.2-24.2 μmol•L⁻¹).
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The flavonoids were investigated from the whole plants of Lagopsis supina. The compounds were isolated and purified by various column chromatography, and their structures were identified by physiochemical properties and spectroscopic data. Two flavones were isolated from the CH2Cl2 layer of Lagopsis supina extract and identified as genkwanin (1) and 5-hydroxy-7,4'-dimethoxyflavone (2), respectively. Ten flavonoid glycosides were isolated from the water layer of Lagopsis supina and elucidated as kaempferol-3-O-6" (3-hydroxy-3-methylglutaryl) -β-D-glucoside (3), quercetin-3-O-6"-(3-hydroxy-3-methylglutaryl) -β-D-glucoside (4), quercetin-3-O-β-D-glucoside(5), kaempferol-3-Of3-D-glucoside ( 6), isorhamnetin-3-O-/-D-glycopyranoside (7), apigenin-7-O-6-D-glucoside (8), luteolin-7-O-β-D-glucoside (9), chrysoeriol-7-O-β-D-glucoside (10), rutin (11 ), and kaempferol-3-β-(6"-p-coumaroyl) -β-D-glucoside (tiliroside, 12). Compounds 3 and 4 were firstly isolated from Lamiaceae family, and compounds 1-12 were isolated from the plants of Lagopsis genus for the first time.
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Medicamentos de Ervas Chinesas , Química , Flavonoides , Química , Lamiaceae , Química , Estrutura Molecular , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
Objective To investigate the association between malnutrition parameters and serum N-terminal pro-brain natriuretic peptide (NT-proBNP) level in male patients aged ≥ 80 years with normal ejection fraction.Methods A total of 197 elderly male patients aged 80 95 years (average 85.4±9.7) were enrolled.Each patient received echocardiograms following admission,and ejection fraction was calculated.Serum concentrations of NT-proBNP were measured by electrochemiluminescence immunoassay.Multiple Logistic regression analyses and receiver operating characteristic (ROC) curves were used to assess the association between malnutrition parameters and serum level of NT-proBNP.Results Serum NT-proBNP level was higher in patients with malnutrition than in the controls [(711.9±1063.3) ng/L vs.(1375.2-±1891.7) ng/L,P=0.006].Pearson correlation analysis showed that the malnutrition parameters such as body mass index (BMI),blood hemoglobin,albumin and pre-albumin were negatively correlated with serum NT proBNP level (all P<0.05).Logistic regression analysis showed that BMI and serum pre albumin level were independently associated with serum NT-proBNP level elevation (P=0.028 and 0.006,respectively).ROC curve analysis showed that the malnutrition parameters could predict the serum NT-proBNP level elevation.The area under the ROC curves for BMI,levels of blood hemoglobin,albumin and prealbumin in predicting serum NT proBNP level elevation was 0.7 (P=0.002),0.7 (P=0.004),0.6 (P=0.036),0.6 P=0.002),the sensitivity was 75.5%,51.0%,38.8%,89.8%,and the specificity was 54.4%,70.2 %,84.2% and 31.6 %,respectively.Conclusions The malnutrition parameters including BMI,blood hemoglobin,albumin and pre-albumin can predict serum NT-proBNP level elevation.BMI and serum pre-albumin level are independently associated with serum NT-proBNP level elevation in male patients aged ≥ 80 years with normal ejection fraction.
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A new γ-alkylated-γ-butyrolactone, named melongenolide A (1), along with nine known compounds were obtained from the roots of Solanum melongena, and their structures were identified as melongenolide A (1), (+)-syringaresinol (2), (+)-lyoniresinol (3), 5,5'-dimethoxy lariciresinol (4), (+)-(7R,8R)-4-hydroxy-3,3',5'-trimethoxy-8',9'-dinor-8,4'-oxyneoligna-7, 9-diol-7'-aldehyde (5), kaempferol-3-O-(2″,6″-di-O-p-trans-coumaroyl)-β-glucoside (6), arjunolic acid (7), vanillic acid (8), scoparone (9), and β-sitosterol (10). Compounds 2, 6, and 7 showed potent inhibitory effects on nitric oxide production in lipopolysaccharide-induced RAW 264.7 macrophages, with IC50 values being 5.62 ± 0.86, 11.47 ± 0.98, and 27.75 ± 1.26 μmol·L(-1), respectively.
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Animais , Camundongos , 4-Butirolactona , Furanos , Farmacologia , Inflamação , Tratamento Farmacológico , Metabolismo , Concentração Inibidora 50 , Quempferóis , Farmacologia , Lignanas , Farmacologia , Macrófagos , Metabolismo , Óxido Nítrico , Metabolismo , Extratos Vegetais , Química , Farmacologia , Usos Terapêuticos , Raízes de Plantas , Química , Solanum melongena , Química , Triterpenos , FarmacologiaRESUMO
Acteoside (verbascoside), a phenylethanoid glycoside widely distributed in various plants, has been shown to have potential activity against Alzheimer's disease, attracting great attentions recently. The present study was designed to develop a selective and sensitive LC-MS/MS method for the determination of acteoside in biological samples and carry our a pharmacokinetic (PK) study in beagle dogs. The PK parameters were calculated using non-compartmental models. Following a single-dose oral administration, acteoside was rapidly absorbed and eliminated, with Tmax being between 30 to 45 min and terminal half-life being about 90 min. The areas under the time-concentration curve (AUC) were 47.28 ± 8.74, 87.86 ± 13.33, and 183.14 ± 28.69 mg · min · L(-1) for oral administration of 10, 20, and 40 mg · kg(-1), respectively, demonstrating that the exposure of acteoside proportionally increased with the dose level. The absolute bioavailability of acteoside was around 4%. For all the PK parameters, there were large variations between individual dogs. In conclusion, the pharmacokinetic characteristics observed in the present study can be of great value to help better understand the pharmacological properties of acteoside and to improve the outcome of its clinical use.
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Animais , Cães , Feminino , Masculino , Administração Intravenosa , Administração Oral , Doença de Alzheimer , Tratamento Farmacológico , Área Sob a Curva , Disponibilidade Biológica , Cromatografia Líquida de Alta Pressão , Glucosídeos , Farmacocinética , Absorção Intestinal , Fenóis , Farmacocinética , Extratos Vegetais , Farmacocinética , Espectrometria de Massas em Tandem , Verbenaceae , QuímicaRESUMO
<p><b>OBJECTIVE</b>To investigate the effect of acteoside on SK-N-SH nerve cell injury induced by okadaic acid (OA).</p><p><b>METHOD</b>SK-N-SH nerve cells were processed with 20 nmol * L OA to establish the Alzheimer's disease (AD) cellular model, and 5, 10, 20 mg . L-1 acteoside was used to antagonize against its effect. Cell morphology was observed under inverted microscope. The cell survival rate was detected with MTT, and the LDH release rate was measured by enzyme label kit. Western blot was applied to determine the expression of phosphorylation tau proteins in nerve cells.</p><p><b>RESULT</b>The acteoside could significantly improve SK-N-SH cell morphology, enhance the cell survival rate, decrease the cell LDH release rate and the expression of phosphorylated tau proteins at p-Ser 199/202 and p-Ser 404 sites, up-regulated the expression of at non-phosphorylated tau proteins at Ser 202 site and Ser 404 sites.</p><p><b>CONCLUSION</b>Acteoside has significant protective effect on nerve cell injury induced by OA.</p>
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Humanos , Doença de Alzheimer , Metabolismo , Linhagem Celular , Sobrevivência Celular , Glucosídeos , Farmacologia , Ácido Okadáico , Fenóis , Farmacologia , Proteínas tau , MetabolismoRESUMO
Objective: To establish the fingerprint of the extract from the rhizome of Alpinia officinarum, to investigate the effects on the proliferation, tyrosinase activity, and melanogenesis in melanoma B16 cells, and to analyze the spectrum-effect relasionship. Methods: The fingerprint of alcohol extract from the rhizome of A. officinarum (G1), water sediments of G1 (G2), macroporous resin purified extract of G2 (G3), and refined polyamide extract of G3 (G4) were established by HPLC, and the proliferation of each extract on B16 cells was measured by MTT. The tyrosinase activity and melanin content were measured by colorimetry assay. The spectrum-effect relasionship was analyzed by grey relation analysis. Results: Compared with the control group, the proliferation of B16 cells was promoted significantly after treatment with 1.00-5.00, 0.50-5.00, 0.25-5.00, and 0.25-10.00 μmol/L of G1, G2, G3, and G4, respectively. The tyrosinase activity was promoted by G1 and G2 with 0.50 μmol/L, and G3 and G4 with 0.50-1.00 μmol/L (P < 0.05, 0.01); The synthesis of melanin was promoted after the treatment with 0.5 and 5.00 μmol/L of G1, 0.50-5.00 μmol/L of G2 and G4, and 0.25-5.00 μmol/L of G3 (P < 0.01); At the same concentration, G4 had the strongest effect to promote the cell proliferation and to increase the tyrosinase activity. The galangin (peak 7) had the highest correlation with pharmacodynamics, and the contents of galangin in G1, G2, G3, and G4 were 27.61, 88.72, 348.53, and 693.35 mg/g, respectively. The proliferation, tyrosinase activity, and galangin content were promoted significantly after the treatment with galangin (0.25-10.00 μmol/L) by the verification experiment. Conclusion: The effect of the extract from the rhizome of A. officinarum on the proliferation, tyrosinase activity, and melanogenesis of B16 melanoma cells could be enhanced with the increased content of galangin, which demonstrates that the galangin is one of the efficient substances in the rhizome of A. officinarum for the treatment of vitiligo.
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<p><b>OBJECTIVE</b>To establish a HPLC method for determining acetoside in rat plasma and to investigate the pharmacokinetic characteristics of acetoside in rats.</p><p><b>METHOD</b>Six rats were orally administered with 150 mg x kg(-1) acetoside and their blood samples were collected at different time points. The plasma concentration of acetoside was determined by reserved HPLC, and the pharmacokinetic parameters were calculated by DAS 2.0 software.</p><p><b>RESULT</b>The regression equation of acetoside in rats plasma was Y = 3.509 8X-0.096 8 (r = 0.996 8), which showed a good linear relation at 0.125-2.5 mg x L(-1). The method showed a recovery of more than 85%, and both inter-day and intra-day RSDs were less than 15%. After the oral administration of 150 mg x kg(-1) acetoside, the concentration-time curves of acetoside were expressed in a open two-compartment model. The main pharmacokinetics parameters of T(max), C(max), t(1/2alpha), t(1/2beta), AUC(0-t), AUC(0-infinity), CL/F, V/F and K(a) were respectively 0.36 h, 1.126 mg x L(-1), 0.759, 4.842 h, 3.134, 3.766 mg x h x L(-), 87.089 L x h(t) x kg(-1), 207.704 L x kg(-1) and 6.345 h(-1) respectively.</p><p><b>CONCLUSION</b>It is first time to establish such a HPLC method to determine the concentration of acetoside in plasma. The method is so highly specified and sensitive that it can ble used in quantitative analysis in vivo on acetoside.</p>