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1.
J Ethnopharmacol ; 326: 117967, 2024 May 23.
Artículo en Inglés | MEDLINE | ID: mdl-38431111

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Psoraleae Fructus (PF), the dried fruit of Psoralea corylifolia L., is a commonly used traditional medicine that has contributed to the treatment of orthopedic diseases for thousands of years in China. However, recent PF-related liver injury reports have drawn widespread attention regarding its potential hepatotoxicity risks. AIM OF THE STUDY: This study was aimed to evaluate the long-term efficacy and chronic toxicity of PF using a 26-week administration experiment on rats in order to simulate the clinical usage situation. MATERIALS AND METHODS: The PF aqueous extract was consecutively administrated to rats daily at dosages of 0.7, 2.0, and 5.6 g/kg (equivalent to 1-8 times the clinical doses for humans) for as long as 26 weeks. Samples were collected after 13, 26, and 32 weeks (withdrawal for 6 weeks) since the first administration. The chronic toxicity of PF was evaluated by conventional toxicological methods, and the efficacy of PF was evaluated by osteogenic effects in the natural growth process. RESULTS: In our experiments, only the H group (5.6 g/kg) for 26-week PF treatment demonstrated liver or kidney injury, which the injuries were reversible after 6 weeks of withdrawal. Notably, the PF treatment beyond 13 weeks showed significant benefits for bone growth and development in rats, with a higher benefit-risk ratio in female rats. CONCLUSIONS: PF displayed a promising benefit-risk ratio in the treatment and prevention of osteoporosis, a disease that lacks effective medicine so far. This is the first study to elucidate the benefit-risk balance associated with clinical dosage and long-term use of PF, thereby providing valuable insights for rational clinical use and risk control of PF.


Asunto(s)
Medicamentos Herbarios Chinos , Fabaceae , Psoralea , Humanos , Ratas , Femenino , Animales , Frutas , Oportunidad Relativa , Hígado , Medicamentos Herbarios Chinos/toxicidad
2.
Front Neurol ; 14: 1163990, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37351267

RESUMEN

As radiation therapy is increasingly utilized in the treatment of cancer, neuropathic pain (NP) is a common radiotherapy-related adverse effect and has a significant impact on clinical outcomes negatively. However, despite an improved understanding of neuropathic pain management, pain is often undertreated in patients with cancer. Herein, we reported two cases with radiotherapy-related neuropathic pain (RRNP) who presented a positive reaction to acupuncture. Patient 1 (a 73-year-old woman) with gynecologic cancer complained of burning and electric shock-like pain in the lower limb after radiotherapy. With the accepted combination of acupuncture and drugs, the pain was alleviated completely in 8 weeks. Patient 2 (a 64-year-old woman) accepted acupuncture in the absence of medication because of her inability to tolerate the adverse events of anticonvulsant drugs. She achieved remission of pain 4 weeks later. The results of this study showed that acupuncture might be promising for controlling the RRNP in patients with cancer, especially who were intolerant or unresponsive to medications.

3.
J Hazard Mater ; 425: 127951, 2022 03 05.
Artículo en Inglés | MEDLINE | ID: mdl-34894515

RESUMEN

Uranium is a key element in the nuclear industry and also a global environmental contaminant with combined highly toxic and radioactive. Currently, the materials based on post-modification of amidoxime have been developed for uranium detection and adsorption. However, the affinity of amidoxime group for vanadium is stronger than that of uranium, which is the main challenge hindering the practical application of amidoxime-based adsorbents. Herein, we synthesized a fluorescent covalent organic framework (TFPPy-BDOH) through integrating biphenyl diamine and pyrene unit into the π-conjugated framework. TFPPy-BDOH has an excellent selectivity to uranium due to the synergistic effect of nitrogen atom in the imine bond and hydroxyl groups in conjugated framework. It can achieve ultra-fast fluorescence response time (2 s) and ultra-low detection limit (8.8 nM), which may be attributed to its intrinsic regular porous channel structures and excellent hydrophilicity. More excitingly, TFPPy-BDOH can chemically reduce soluble U (VI) to insoluble U (IV), and release the binding site to adsorb additional U (VI), achieving high adsorption capacity of 982.6 ± 49.1 mg g-1. Therefore, TFPPy-BDOH can overcome the challenges faced by current amidoxime-based adsorbents, making it as a potential adsorbent in practical applications.


Asunto(s)
Estructuras Metalorgánicas , Uranio , Adsorción , Colorantes , Oxidación-Reducción
4.
Oxid Med Cell Longev ; 2021: 8865813, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33968299

RESUMEN

Cassiae Semen is a widely used herbal medicine and a popular edible variety in many dietary or health beverage. Emerging evidence disclosed that improper administration of Cassiae Semen could induce obvious liver injury, which is possibly attributed to emodin, one of the bioactive anthraquinone compounds in Cassiae Semen, which caused hepatotoxicity, but the underlying mechanisms are not completely understood. Hence, the present study firstly explored the possible role of oxidative stress-mediated mitochondrial dysfunction and ER stress in emodin-cause apoptosis of L02 cells, aiming to elaborate possible toxic mechanisms involved in emodin-induced hepatotoxicity. Our results showed that emodin-induced ROS activated ER stress and the UPR via the BiP/IRE1α/CHOP signaling pathway, followed by ER Ca2+ release and cytoplasmic Ca2+ overloading. At the same time, emodin-caused redox imbalance increased mtROS while decreased MMP and mitochondrial function, resulting in the leaks of mitochondrial-related proapoptotic factors. Interestingly, blocking Ca2+ release from ER by 2-APB could inhibit emodin-induced apoptosis of L02, but the restored mitochondrial function did not reduce the apoptosis rates of emodin-treated cells. Besides, tunicamycin (TM) and doxorubicin (DOX) were used to activate ER stress and mitochondrial injury at a dosage where obvious apoptosis was not observed, respectively. We found that cotreatment with TM and DOX significantly induced apoptosis of L02 cells. Thus, all the results indicated that emodin-induced excessive ROS generation and redox imbalance promoted apoptosis, which was mainly associated with BiP/IRE1α/CHOP signaling-mediated ER stress and would be enhanced by oxidative stress-mediated mitochondrial dysfunction. Altogether, this finding has implicated that redox imbalance-mediated ER stress could be an alternative target for the treatment of Cassiae Semen or other medicine-food homologous varieties containing emodin-induced liver injury.


Asunto(s)
Emodina/uso terapéutico , Estrés del Retículo Endoplásmico/efectos de los fármacos , Mitocondrias/metabolismo , Inhibidores de Proteínas Quinasas/uso terapéutico , Animales , Apoptosis , Línea Celular Tumoral , Emodina/farmacología , Humanos , Inhibidores de Proteínas Quinasas/farmacología , Transducción de Señal , Smegmamorpha
5.
Zhen Ci Yan Jiu ; 45(6): 508-2, 2020 Jun 25.
Artículo en Chino | MEDLINE | ID: mdl-32643890

RESUMEN

Alzheimer's disease is a neurodegenerative disease closely related to age, which is characterized by cognitive and memory impairment. Extensive studies have confirmed that Wnt/ß-catenin signal pathway is involved in the occurrence and development of Alzheimer's disease. With the characteristics of holistic concept and syndrome differentiation, acupuncture is widely used in clinic. Acupuncture plays a role in the treatment of Alzheimer's disease through the regulation of each target and the whole of the pathway. The author reviewed and combed the research on acupuncture treatment of Alzheimer's disease in recent years, and reviewed the regulatory effects of acupuncture on the important components of Wnt/ß-catenin signal pathway (Wnt protein, ß-catenin, glycogen synthase kinase-3ß) and whole, ATP-binding cassette subfamily B member 1 (ABCB1), low density lipoprotein receptor associated protein-1 (LRP-1)..


Asunto(s)
Terapia por Acupuntura , Enfermedad de Alzheimer , Enfermedad de Alzheimer/terapia , Humanos , Vía de Señalización Wnt , beta Catenina
6.
J Asian Nat Prod Res ; 21(7): 652-658, 2019 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-29717884

RESUMEN

Nigakialcohol A (1), as unusual cyclization ionone derivative, together with eight known ones (2-9), were isolated from the leaves of Picrasma quassioides (D. Don) Benn (Simaroubaceae). Their structures were elucidated by extensive spectroscopic analyses and comparison with literature data. Compound 2 showed a weak inhibitory effect on NO production at non-cytotoxic concentration (100 µM) with inhibitory rate of 59%, and thus it should be regarded as potential anti-inflammatory agents.


Asunto(s)
Norisoprenoides/química , Norisoprenoides/farmacología , Picrasma/química , Hojas de la Planta/química , Animales , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/farmacología , Espectroscopía de Resonancia Magnética , Ratones , Estructura Molecular , Óxido Nítrico/antagonistas & inhibidores , Óxido Nítrico/biosíntesis , Extractos Vegetales/química , Células RAW 264.7
7.
Zhongguo Zhong Yao Za Zhi ; 43(11): 2326-2332, 2018 Jun.
Artículo en Chino | MEDLINE | ID: mdl-29945386

RESUMEN

Bear Bile Powder contains bile acids, protein, amino acids, bilirubin and microelements and other compounds. Among them, the bile acids are the most active components. Currently, there are many studies on bile acids, but few reports on other components. Therefore, the purpose of this study is to carry out a systematical analysis of multiple components in drainage Bear Bile Powder from different sources. Bilirubin and protein were quantified by microplate spectrophotometer. The contents of bile acids and amino acids were determined by liquid chromatography coupled with mass spectrometry (LC-MS). The contents of microelements were determined by inductively coupled plasma mass spectrometry (ICP-MS) The result indicated that among 20 batches of bear bile powder from different sources there is high similarity (0.922-0.977). Tauroursodeoxycholic acid (TUDCA) and taurochenodeoxycholic acid (TCDCA) were the two most abundant components. The total contents of them were 41%-59% and met the current standard for quality control of bear bile powder. However, significant differences were found in their contents among samples from different sources. Besides, bilirubin, protein, amino acids and microelements also contributed to the differentiation of samples from different sources. The main components of bear bile powder from the different sources were with satisfactory similarity. But bile acids, bilirubin, protein, amino acids and microelements all contributed to the different among samples. Our present study provided a systematical approach for the better quality control and evaluation of bear bile powder.


Asunto(s)
Ácidos y Sales Biliares/análisis , Bilis/química , Materia Medica/análisis , Ursidae , Animales , Polvos , Espectrometría de Masas en Tándem
8.
J Nat Med ; 72(2): 433-438, 2018 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-29435792

RESUMEN

Discovery of agents for oral infectious diseases is always encouraged in natural products chemistry. A bioassay-guided isolation led to the isolation of two new acetylenic acids (1, 2) along with seven known ones (3-9) from the ethanol extract of Thesium chinense Turcz, a commonly used oral anti-bacterial and anti-inflammatory herb. Their structures were elucidated on the basis of spectroscopic and chemical evidence. Exocarpic acid (3) demonstrated the most promising activity against three tested oral pathogenic bacterial strains, Porphyromonas gingivalis, Fusobacterium nucleatum, and Streptococcus mutans, with minimum inhibitory concentration values of 0.86, 3.43, and 13.70 µg/mL, respectively. Compounds 1, 2, 4, 5 and 7 also showed potential activities against periodontal bacteria (P. gingivalis, F. nucleatum).


Asunto(s)
Alquinos/metabolismo , Antibacterianos/uso terapéutico , Ácidos Grasos Insaturados/metabolismo , Enfermedades de la Boca/tratamiento farmacológico , Extractos Vegetales/química , Plantas Medicinales/química , Administración Oral , Antibacterianos/farmacología , Humanos
9.
Zhongguo Zhong Yao Za Zhi ; 42(7): 1365-1369, 2017 Apr.
Artículo en Chino | MEDLINE | ID: mdl-29052400

RESUMEN

Ginsenoside Rb1 (Rb1), which is one of the main ingredients derived from Panax ginseng, has been found to have extensive pharmacological activities including antioxidant, anti-inflammatory, anticancer properties. In this study, the effect of Rb1 on doxorubicin-induced myocardial autophagy was studied with H9c2 as the study object. CCK-8 method, transmission electron microscope observation, fluorescence staining observation and Western blot were used to detect changes in H9c2 cell proliferation and autophagy after treatment. According to the results, doxorubicin could cause cell viability decrease, significant increase in the LC3-Ⅱ/LC3-I ratio and down-regulation of the expression of p62. Pretreatment with ginsenoside Rb1 inhibited cell viability decrease and increase in doxorubicin-induced autophagic structure and LC3-Ⅱ/LC3-I ratio, and down-regulation of the expression of p62. In conclusion, doxorubicin could induce H9c2 cell death and induce autophagy, and ginsenoside Rb1 showed a protective effect on DOX-induced cardiotoxicity, which may be correlated with suppression of DOX-induced autophagy.


Asunto(s)
Autofagia/efectos de los fármacos , Ginsenósidos/farmacología , Corazón/efectos de los fármacos , Miocardio/patología , Miocitos Cardíacos/efectos de los fármacos , Animales , Línea Celular , Doxorrubicina , Corazón/fisiopatología , Ratas
10.
Zhongguo Zhong Yao Za Zhi ; 42(3): 593-599, 2017 Feb.
Artículo en Chino | MEDLINE | ID: mdl-28952270

RESUMEN

To investigate the effect of clinical dose of Realgar-Indigo Naturais formula (RIF) and large-dose of Realgar on main drug-metabolizing enzymes CYP450s of rat liver, as well as its regulatory effect on mRNA expression. Wistar rats were administrated orally with tested drugs for 14 days. A Cocktail method combined with HPLC-MS/MS was used in the determination of 4 cytochrome P450 isozymes (CYP1A2, CYP2B, CYP3A and CYP2C) in liver of the rats, and the mRNA expression levels of the above subtypes were detected by real-time fluorescent quantitative PCR. The results showed that RIF can significantly induce CYP1A2 and CYP2B enzyme activity, and inhibit CYP3A enzyme activity. This result was consistent with the mRNA expression. However, its single compound showed weaker or even contrary phenomenon. Different doses of Realgar also showed significant inconsistencies on CYP450 enzymes activity and mRNA expression. These phenomena may be relevant with RIF compatibility synergies or toxicity reduction. The results can also prompt drug interactions when RIF is combined with other medicines in application.


Asunto(s)
Arsenicales/farmacología , Sistema Enzimático del Citocromo P-450/metabolismo , Medicamentos Herbarios Chinos/farmacología , Hígado/efectos de los fármacos , Sulfuros/farmacología , Animales , Hígado/enzimología , Ratas , Ratas Wistar , Espectrometría de Masas en Tándem
11.
Artículo en Inglés | MEDLINE | ID: mdl-28421119

RESUMEN

The purpose of this work was to study the influences of Realgar-Indigo naturalis (RIF) and its principal element realgar on 4 main cytochrome P450 enzymes activities in rats. A simple and efficient cocktail method was developed to detect the four probe drugs simultaneously. In this study, Wistar rats were administered intragastric RIF and realgar for 14 days; mixed probe drugs were injected into rats by caudal vein. Through analyzing the pharmacokinetic parameter of mixed probe drugs in rats, we can calculate the CYPs activities. The results showed that RIF could inhibit CYP1A2 enzyme activity and induce CYP2C11 enzyme activity significantly. Interestingly, in realgar high dosage group, CYP3A1/2 enzyme activity was inhibited significantly, and different dosage of realgar manifested a good dose-dependent manner. The RIF results indicated that drug coadministrated with RIF may need to be paid attention in relation to drug-drug interactions (DDIs). Realgar, a toxic traditional Chinese medicine (TCM), does have curative effect on acute promyelocytic leukemia (APL). Its toxicity studies should be focused on. We found that, in realgar high dosage group, CYP3A1/2 enzymes activity was inhibited. This phenomenon may explain its potential toxicity mechanism.

12.
Zhongguo Zhong Xi Yi Jie He Za Zhi ; 37(2): 179-183, 2017 Feb.
Artículo en Chino | MEDLINE | ID: mdl-30650270

RESUMEN

Objective To evaluate the efficacy and safety of Liujin Runzao Concentrated Decoction (LRCD) for the treatment of primary Sjögren's syndrome (pSS). Methods Forty pSS patients with fluid depletion and distribution obstacles syndrome (FDDOS) were randomly assigned to the experimen- tal group and the control group according to 1:1 proportion. All patients received standard therapy: Radix Paeoniae alba total glycosides 600 mg, twice per day. Patients in the experimental group additionally took LRCD, 30 mL each time, twice per day. The therapeutic course for all was 4 weeks, and two courses for all. The improvement of dry mouth and dry eyes were comprehensively evaluated. Each outcome of composite index constitutions (integrals of dry eyes and dry mouth, salivary flow rate, Schirmer test) was respectively reported. Schirmer test and salivary flow rate were determined as well. Score of TCM syndrome, blood sedimentation,'immunoglobulin, and adverse drug reactions were observed. Results The effective rate of comprehensive effect for dry eyes and dry mouth improvement at the end of 8 weeks was 80% in the experimental group and 35% in the control group, with statistical difference (X² =8. 286, P <0. 05). As for the composition of comprehensive effect for dry eyes and dry mouth improvement: The score for dry eyes and dry mouth decreased in the two groups more after treatment than before treatment. The difference in pre-post treatment score for dry eyes and dry mouth at week 8 was higher in the experimental group than in the control group. The difference in pre-post treatment score at week 8 was 1. 71 (95% Cl: -0. 37 -3. 78) between the two groups (P <0. 05). The difference in pre-post treatment Schirmer test and salivary flow rate at week 8 was higher in the experimental group than in the control group, but with on statistical difference (P >0. 05). The difference in pre-post treatment Schirmer test and salivary flow rate at week 8 was 2. 74 mL/15 min (95% Cl: 0. 49 -4.98) and 0. 13 mm/5 min (95% Cl: 0. 92 -1. 23) between the two groups (P <0. 05). The score of TCM syndrome decreased more in the two groups, as compared with before treatment. The difference in pre-post treatment score of TCM syn- drome at week 8 was 1. 71 (95% CI: -1. 40 -4. 81) between the two groups (P >0. 05). One case of uri- nary tract infections occurred in the control group, while no obvious adverse event occurred in the exper- imental group. Conclusion Standard treatment combined LRCD showed better comprehensive effect for dry eyes and dry mouth in pSS patients with FDDOS, and was more safe.


Asunto(s)
Medicamentos Herbarios Chinos , Síndrome de Sjögren , Sedimentación Sanguínea , Medicamentos Herbarios Chinos/uso terapéutico , Humanos , Síndrome de Sjögren/terapia
13.
Planta Med ; 83(1-02): 143-150, 2017 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-27405106

RESUMEN

Sixty-three amide alkaloids, including three new, piperflaviflorine A (1), piperflaviflorine B (2), and sarmentamide D (4), and two previously synthesized ones, (1E,3S)-1-cinnamoyl-3- hydroxypyrrolidine (3) and N-[7'-(4'-methoxyphenyl)ethyl]-2-methoxybenzamide (5), were isolated from the aerial parts of Piper flaviflorum and Piper sarmentosum. Their structures were elucidated by detailed spectroscopic analysis and, in case of 3, by single-crystal X-ray diffraction. Most of the isolates were tested for their antifungal and antibacterial activities. Ten amides (6-15) showed antifungal activity against Cryptococcus neoformans ATCC 90 113 with IC50 values in the range between 4.7 and 20.0 µg/mL.


Asunto(s)
Alcaloides/farmacología , Amidas/farmacología , Antifúngicos/farmacología , Cryptococcus neoformans/efectos de los fármacos , Estructura Molecular , Piper/química , Alcaloides/química , Alcaloides/aislamiento & purificación , Amidas/química , Amidas/aislamiento & purificación , Antifúngicos/química , Antifúngicos/aislamiento & purificación , Componentes Aéreos de las Plantas/química , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Difracción de Rayos X
14.
Nat Prod Commun ; 11(6): 725-8, 2016 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-27534102

RESUMEN

Two new oleanane-type triterpenoid saponins (1 and 2) were isolated from the methanolyzed total saponins of the seeds of Momordica cochinchinensis (Lour.) Spreng, together with 16 known compounds (3-18). Their structures were elucidated on the basis of detailed spectroscopic, including 1D and 2D NMR, mass spectrometric, methanolysis and LC-MS analysis. All the isolates were tested for their cytotoxic activities against five human cancer cell lines (HL-60, SMMC-7721, PANC-1, A-549, and SW-480) and the glucose uptake activity. The known compound 6 exhibited toxic effects against HL-60 with an IC50 value of 18.1 µM, while 10 showed cytotoxicity against SMMC-7721 and A-549 cell lines, with IC50 values of 34.4 and 32.8 µM, respectively. In addition, the new compound 2 showed glucose uptake activity with a glucose consumption value of 0.29 µM at 10 µM concentration.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Medicamentos Herbarios Chinos/farmacología , Momordica/química , Ácido Oleanólico/análogos & derivados , Saponinas/farmacología , Antineoplásicos Fitogénicos/química , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Medicamentos Herbarios Chinos/química , Humanos , Estructura Molecular , Ácido Oleanólico/química , Ácido Oleanólico/farmacología , Saponinas/química
15.
Zhongguo Zhong Yao Za Zhi ; 41(7): 1313-1317, 2016 Apr.
Artículo en Chino | MEDLINE | ID: mdl-28879749

RESUMEN

3D in vitro toxicity testing model was developed by magnetic levitation method for culture of the human hepatoma cell line HepG2 and applied to evaluate the drug hepatotoxicity. After formation of stable 3D structure for HepG2 cells, their glycogen storage capacity under 2D and 3D culture conditions were detected by immunohistochemistry technology, and the mRNA expression levels of phase Ⅰ and Ⅱ drug metabolism enzymes, drug transporters, nuclear receptors and liver-specific marker albumin(ALB) were compared between 2D and 3D culture conditions by using RT-PCR method. Immunohistochemistry results showed that HepG2 cells had abundant glycogen storage capacity under 3D culture conditions, which was similar to human liver tissues. The mRNA expression levels of major drug metabolism enzymes, drug transporters, nuclear receptors and ALB in HepG2 cells under 3D culture conditions were up-regulated as compared with 2D culture conditions. For drug hepatotoxicity evaluation, the typical hepatotoxic drug acetaminophen(APAP), and most reported drugs Polygonum multiflorum Thunb.(Chinese name He-shou-wu) and Psoraleae corylifolia L.(Chinese name Bu-gu-zhi) were selected for single dose and repeated dose(7 d) exposure. In the repeated dose exposure test, 3D HepG2 cells showed higher sensitivity. This established 3D HepG2 cells model with magnetic levitation 3D culture techniques was more close to the human liver tissues both in morphology and functions, so it was a better 3D hepatotoxicity evaluation model.


Asunto(s)
Acetaminofén/toxicidad , Hepatocitos/efectos de los fármacos , Extractos Vegetales/toxicidad , Pruebas de Toxicidad , Técnicas de Cultivo de Célula , Enfermedad Hepática Inducida por Sustancias y Drogas , Células Hep G2 , Humanos
16.
Zhongguo Zhong Yao Za Zhi ; 41(8): 1504-1510, 2016 Apr.
Artículo en Chino | MEDLINE | ID: mdl-28884547

RESUMEN

To study the effect of aqueous extract of Cassiae Semen on the activity, mRNA and protein expressions of cytochrome P450(CYP450) system in rat liver microsomes, microsomes of rat liver were prepared after the oral administration with aqueous extract of Cassiae Semen for 14 days. The enzyme activity was quantified by Cocktail method. Meanwhile, the mRNA and protein expressions of CYP1A2, CYP2B1, CYP2C11, CYP2D2, CYP2E1 and CYP3A1 in the livers were detected by RT-PCR and Western blot. The result of this experiment was that aqueous extract of Cassiae Semen obviously induced the enzyme activities of CYP1A2, CYP2B1, CYP2C11, CYP2D2, CYP2E1 and CYP3A1. Low dose of aqueous extract of Cassiae Semen significantly reduced the activity of CYP2D2, but the activity of CYP2D2 was significantly induced by middle dose and high dose of aqueous extract of Cassiae Semen. These subtypes were increased in a dose-dependent manner except for CYP3A1. The mRNA levels of CYP1A2, CYP2C11, CYP2D2 and CYP2E1 were also induced in rats treated with aqueous extract of Cassiae Semen, but with no significant effect in CYP2B1 and CYP3A1 mRNA expressions. The protein levels of CYP2C11 and CYP2E1 were also induced in rats treated with aqueous extract of Cassiae Semen, but with no significant difference. Since the enzyme activity, mRNA and protein expressions of CYP450, particularly CYP2C11and2E1subtypes, were induced or inhibited by aqueous extract of Cassiae Semen to varing degrees, suggesting the potential drug-drug interactions should be concerned.


Asunto(s)
Cassia/química , Sistema Enzimático del Citocromo P-450/metabolismo , Medicamentos Herbarios Chinos/farmacología , Microsomas Hepáticos/efectos de los fármacos , Extractos Vegetales/farmacología , Animales , Isoenzimas/metabolismo , Hígado/efectos de los fármacos , Microsomas Hepáticos/enzimología , Ratas , Ratas Sprague-Dawley
17.
Zhongguo Zhong Yao Za Zhi ; 40(14): 2737-42, 2015 Jul.
Artículo en Chino | MEDLINE | ID: mdl-26666019

RESUMEN

To research the influence of Reduning injection on the activity and mRNA expression of cytochrome P450 (CYP450) system in rat liver microsomes. Rat liver microsomes were prepared after a seven-days continuous administration of Reduning injection. An HPLC-MS method was applied to determine the specific metabolites of CYP450 probe substrates in rat liver microsomal incubations. The activity of CYP450 isozymes were represented by the formation of metabolites. The Real-time quantitative polymerase chain reaction (Q-PCR) was applied to determine the mRNA expression levels of CYP450. Reduning injection significantly reduced the activity of CYP2B1, 2C12, 2C13 (P < 0.01), but did not affect CYPlA2; low dose and high dose of Reduning injection had an inhibition trend on the activity of CYP2D2, but did not statistically differ from control group; low dose of Reduning injection significantly induced the activity of CYP3A1 (P < 0.01), high dose of Reduning injection had an induce trend on the activity of CYP3A1, but did not statistically differ from control. At the mRNA level, low and high dose of Reduning injection had an induce trend on the expression of CYP1A2, 2C11, 2D1, 2E1, 3A1, but did not statistically differ from control. Reduning injection significantly induced the activity of CYP2B1. Reduning injection significantly induced the activity of CYP3A1 in mRNA expression and enzyme activity levels, which may result adverse drug reaction after being combined with macrolides antibiotics. Reduning injection significantly reduced the activity of CYP2B1, 2C12, 2C13, 2D2 in enzyme activity levels, when combined with other drugs, it should be fully taken into account of the possible drug-drug interaction in order to avoid adverse side effects.


Asunto(s)
Sistema Enzimático del Citocromo P-450/metabolismo , Medicamentos Herbarios Chinos/farmacología , Microsomas Hepáticos/efectos de los fármacos , Animales , Inyecciones , Isoenzimas/metabolismo , Masculino , Microsomas Hepáticos/enzimología , Ratas , Ratas Sprague-Dawley
18.
Zhongguo Zhong Yao Za Zhi ; 40(14): 2743-7, 2015 Jul.
Artículo en Chino | MEDLINE | ID: mdl-26666020

RESUMEN

To research the effect of Ginseng Radix et Rhizoma and Aconiti Lateralis Radix Praeparata compatibility on cardiac toxicity in rats by UPLC-Q-TOF/MS, and explore the endogenous markers and molecule mechanism. Different compatibility of Shenfu decoction were given to male Wistar rats at dosage of 20 g · kg(-1) for 7 days, collected the serum, and analyze the endogenous metabolites effected by Shenfu formulation by principal component analysis and partial least-squares analysis. Results showed that content of glutathione, phosphatidylcholine and citric acid decreased in mixed-decoction group, while ascorbic acid, uric acid, D-galactose, tryptophan, L-phenylalanine increased. The results showed cardiac toxicity of Aconiti Lateralis Radix Praeparata in Shenfu mixed-decoction. Shenfu co-decoction group showed a similar or weaker trend compared with control group, but most of them do not have a statistically significant. The results indicated the scientific basis of Shenfu compatibility by comparison of co-decoction group with mixed-decoction group. Shenfu compatibility can reduce cardiac toxicity induced by Aconiti Lateralis Radix Praeparata, and citric acid, glutathione, phosphatidyl choline, uric acid might be regarded as potential markers of cardiotoxicity.


Asunto(s)
Medicamentos Herbarios Chinos/toxicidad , Metabolómica/métodos , Animales , Biomarcadores , Cardiotoxicidad , Glutatión/sangre , Análisis de los Mínimos Cuadrados , Masculino , Análisis de Componente Principal , Ratas , Ratas Wistar
19.
Zhongguo Zhong Yao Za Zhi ; 40(14): 2748-52, 2015 Jul.
Artículo en Chino | MEDLINE | ID: mdl-26666021

RESUMEN

Dioscin has a wide range of biological effects and broad application prospects. However the studies concerning the toxicology and mechanism of dioscin is small. This article is to study the hepatotoxicity of dioscin and the effect of dioscin treatment on expression of aryl hydrocarbon receptor (AhR) mRNA and CYP1A mRNA and protein in HepG2 cells in vitro. Dioscin 0.5-32 µmol · L(-1) exposed to HepG2 cells for 12 h, cell viability was examined by CCK-8 assay and the release rate of lactate dehydrogenase (LDH) was to evaluate cell membrane damage. HepG2 cells morphologic changes were quantified by inverted Microscope, and the effect on production of reactive oxygen species (ROS) was detected by flow cytometry. The mRNA expression of CYP1A and AhR was evaluated by RT-RCR. The protein expression of CYP1A1 was detected by western blot. The cell viability was significantly inhibited after HepG2 cells were exposed to dioscin 0.5-32 µmol · L(-1). Compared with the control, the LDH release rate and ROS were significantly increased. The expression of CYPlA and AhR mRNA was increased. The expression of CYP1Al protein was increased after dioscin treatment, and resveratrol, an AhR antagonist, could downregulate the expression of CYP1A1. It follows that large doses dioscin has potential hepatotoxicity. The possible mechanism may be dioscin can active aryl hydrocarbon receptor (AhR) and induce the expression of CYP1A.


Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas/etiología , Diosgenina/análogos & derivados , Supervivencia Celular/efectos de los fármacos , Citocromo P-450 CYP1A1/genética , Diosgenina/toxicidad , Células Hep G2 , Humanos , L-Lactato Deshidrogenasa/metabolismo , ARN Mensajero/análisis , Especies Reactivas de Oxígeno/metabolismo , Receptores de Hidrocarburo de Aril/genética
20.
Artículo en Inglés | MEDLINE | ID: mdl-26273317

RESUMEN

The purpose of this study was to study the serum pharmacochemistry of SFD as well as the material basis through analyzing the constituents absorbed in blood. The SFD was orally administrated to Wistar rats at 20 g·kg(-1), and Ultra Performance Liquid Chromatography (UPLC) fingerprints of SFD were created. Serum samples were collected for analysis, and further data processing used MarkerLynx XS software. 19 ginsenosides and 16 alkaloids were detected in SFD. The absorption of alkaloids (mainly monoester diterpenoid alkaloids) increased when Aconitum carmichaeli Debx. was combined with Panax ginseng, while the ginsenosides remained stable. Diester diterpenoid alkaloids were not present in the serum samples. A suitable serum pharmacochemistry method was successfully established to study pharmacological effects and potential improvements in formulation. This may also be useful for toxicity reduction. We suspect that the increased absorption of the monoester diterpenoid alkaloids from the mixture of Panax and Radix, compared to the Panax only extract, may be the reason for the combination of the two herbs in popular medicine formulas in China.

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