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1.
China Tropical Medicine ; (12): 277-2023.
Article in Chinese | WPRIM | ID: wpr-979630

ABSTRACT

@#Abstract: Objective To investigate the species distribution and the antifungal susceptibility of fungi originating from positive blood cultures in Guangdong, so as to provide a basis for the rational use of antifungal drugs in clinical fungal bloodstream infections. Methods All data were collected for retrospective study from monitoring units of the Guangdong Fungal Disease Surveillance Network between 2019-2021, including clinical characteristics, species distribution and antifungal susceptibility. Results A total of 3 589 fungi strains were isolated, most of which were Candida spp. (86.5%, 3 105/3 589). The most common species was Candida albicans (36.6%, 1 315/3 589), followed by Candida tropicalis (17.4%, 1 626/3 589) and Candida parapsilosis (14.5%, 520/3 589). There were 42.1%(1 512/3 589) of strains isolated from ICU. The proportions of Candida albicans strains were 40.0%-50.0% among ICU, general surgery, organ transplantation and emergency department. Candida tropicalis (60.0%, 144/240) was the most common species in hematology department. Both Cryptococcus neoformans (35.4%, 69/195) and Talaromyces marneffei (35.9%,70/195) were common in infection department. All of the Candida isolates were of wild-type (WT) phenotype to amphotericin B. Resistance rates of caspofungin and micafungin for Candida spp. ranged from 0.0% to 4.2%. The resistance rates of Candida tropicalis to fluconazole and voriconazole were 42.3% and 38.9%, which were significantly higher than other common Candida spp. The cryptococcus neoformans strains were totally of WT phenotype to fluconazole and voriconazole. Conclusions Candida albicans is the most common species originating from positive blood cultures in Guangdong Province. Common Candida strains are highly sensitive to echinocandins and amphotericin B. Candida tropicalis has a high resistance rate to triazole drugs.

2.
Article in Chinese | WPRIM | ID: wpr-906342

ABSTRACT

Objective:To simulate the occupancy rates of baicalein, quercetin and galangin on the target sites of xanthine oxidase <italic>in vivo</italic>. Method:In this experiment, the half inhibitory concentration (IC<sub>50</sub>) of febuxostat, baicalein, quercetin and galangin against xanthine oxidase were determined by <italic>in vitro</italic> enzymatic reaction. Binding free energy was predicted by molecular docking technology and their association rate constant (k<sub>on</sub>) and dissociation rate constant (k<sub>off</sub>) were determined by surface plasmon resonance technology. Based on measured binding kinetic parameters (k<sub>on</sub> and k<sub>off</sub>) and extracted pharmacokinetic data, the target occupancy model <italic>in vivo</italic> was established. Result:The IC<sub>50 </sub>values of febuxostat, baicalein, quercetin and galangin were 0.002 7, 1.63, 0.38, 1.59 µmol·L<sup>-1</sup>, respectively. The IC<sub>50</sub> of febuxostat was very close to that reported in the literature. The predicted curve of target occupancy rate <italic>in vivo</italic> of febuxostat was consistent with its duration of clinical efficacy. When single intragastric administration of long-circulating liposomes of quercetin with dose of 100 mg·kg<sup>-1</sup> in rats, the time of target occupancy rate >70% <italic>in vivo</italic> lasted for about 3.9 h. When rats were orally administered baicalein and galangin with dose of 200 mg·kg<sup>-1</sup>, the time of target occupancy rate >50% <italic>in vivo </italic>lasted for about 10 h and 1.7 h, respectively. Conclusion:The prediction model of xanthine oxidase target occupancy constructed by drug target binding kinetics and <italic>in vivo</italic> pharmacokinetic curves can effectively evaluate the <italic>in vivo</italic> inhibitory activity of compounds against the target.

3.
Zhongguo Zhong Yao Za Zhi ; (24): 1822-1831, 2021.
Article in Chinese | WPRIM | ID: wpr-879097

ABSTRACT

Based on the target occupancy mathematical model, the binding kinetic process of potential active ingredients of lowering uric acid in Chrysanthemum morifolium with xanthine oxidase(XOD) was evaluated. The potential active ingredients of lowering uric acid in Ch. morifolium were screened by UPLC-Q-Exactivems MS technology, reference substance identification and in vitro enzymatic kinetics experiments. The binding kinetic parameters of xanthine oxidase and potential inhibitor in Ch. morifolium were determined by surface plasma resonance(SPR). The verified mathematical model of the XOD target occupancy evaluated the kinetic binding process of inhibitors and xanthine oxidase in vivo. According to UPLC-Q-Exactive MS and reference substance identification, 39 potential uric acid-lowering active ingredients in Ch. morifolium extracts were identified and the inhibitory activities of 23 compounds were determined. Three potential xanthine oxidase inhibitors were screened, namely genistein, luteolin, and apigenin. whose IC_(50 )were 1.23, 1.47 and 1.59 μmol·L~(-1), respectively. And the binding rate constants(K_(on)) were 1.26×10~6, 5.23×10~5 and 6.36×10~5 mol·L~(-1)·s~(-1), respectively. The dissociation rate constants(K_(off)) were 10.93×10~(-2), 1.59×10~(-2), and 5.3×10~(-2 )s~(-1), respectively. After evaluation by different administration methods, the three selected compounds can perform rapid and sustained inhibition of xanthine oxidase in vivo under combined administration. This study comprehensively evaluated the target occupancy process of three effective components in different ways of administration in vivo by UPLC-MS, concentration-response method, SPR technology and xanthine oxidase target occupancy model, which would provide a new research idea and method for screening active ingredients in traditional Chinese medicine.


Subject(s)
Chromatography, Liquid , Chrysanthemum , Flavonoids , Kinetics , Pharmaceutical Preparations , Tandem Mass Spectrometry , Xanthine Oxidase/metabolism
4.
Article in Chinese | WPRIM | ID: wpr-793227

ABSTRACT

@#Objective: To investigate whether long non-coding RNA (lncRNA) FOXD2-AS1 targets miR-506-5p to regulate proliferation and apoptosis of cervical cancer cells. Methods: Human normal cervical cells Ect1/E6E7 and cervical cancer cell lines (HeLa, Siha and Caski) were cultured in vitro, and the expression levels of FOXD2-AS1 and miR-506-5p in cells were detected by qPCR. The cervical cancer cells with FOXD2-AS1 knockdown and miR-506-5p over-expression were constructed by liposome transfection technology, and the proliferation and apoptosis of cells were detected by MTT assay and flow cytometry respectively, the expression of proliferation-related proteins CyclinD1, p21, p27 and apoptosis-related proteins Bcl-2, BAX, cleaved-capase-3 were detected by WB. Dual luciferase reporter assay was used to verify whether FOXD2-AS1 would target miR-506-5p; and the effects of simultaneous inhibition of FOXD2-AS1 and miR-506-5p on proliferation and apoptosis of cervical cancer cells were also analyzed. Results: Compared with Ect1/E6E7 cells, the expression of FOXD2-AS1 significantly increased while the expression of miR-506-5p significantly decreased in cervical cancer HeLa, Siha and Caski cells (all P<0.01). FOXD2-AS1 knockdown significantly inhibited the protein expressions of CyclinD1, Bcl-2 and cell proliferationin cervical cancer cells, but promoted the protein expressions of p21, p27, BAX, cleavedcapase-3, and cell apoptosis (all P<0.01). miR-506-5p over-expression significantly inhibited the protein expressions of CyclinD1, Bcl2 and cell proliferation in cervical cancer cells, but promoted the protein expressions of p21, BAX, and cell apoptosis (all P<0.01). Dual luciferase reporter gene assay confirmed that FOXD2-AS1 negatively regulated the expression of miR-506-5p in cervical cancer cells (P<0.01). Inhibition of miR-506-5p expression reversed the effect of FOXD2-AS1 knockdown on proliferation and apoptosis of cervical cancer cell (P<0.01). Conclusion: FOXD2-AS1 modulates proliferation and apoptosis of cervical cancer cells by negatively regulating the expression of miR-506-5p.

5.
Rev. bras. farmacogn ; 28(4): 468-473, July-Aug. 2018. graf
Article in English | LILACS | ID: biblio-958887

ABSTRACT

Abstract Flavones have the potential of being used as a dietary supplement for bone health promotion beyond calcium and vitamin D. Recent studies have showed that flavones enhanced bone formation and inhibited bone resorption by affecting osteoblast and osteoclast differentiation through various cell signaling pathways. In this study, we investigated the effects of a new flavone (2R,3S)-pinobanksin-3-cinnamate, isolated from the metabolites of the endophytic fungus Penicillium sp. FJ-1 of Acanthus ilicifolius L., Acanthaceae, on osteoblast differentiation by using MC3T3-E1 cells. It was observed that (2R,3S)-pinobanksin-3-cinnamate promoted osteoblast differentiation, as evidenced by increased mineralization process and alkaline phosphatase activity, as well as expression of genes encoding the bone differentiation. Moreover (2R,3S)-pinobanksin-3-cinnamate treatment upregulated the gene expression of wingless-type MMTV integration site family, bone morphogenetic protein and runt-related transcription factor 2, and protein expression of phosphor-Smad1/5/8, β-catenin and runt-related transcription factor 2 in MC3T3-E1 cells. The osteoblast differentiation effects induced by (2R,3S)-pinobanksin-3-cinnamate were attenuated by the bone morphogenetic protein antagonist Noggin, and wingless-type MMTV integration site family signaling pathway inhibitors Dickkopf-1. Co-treatment with adenosine 30,50-cyclic monophosphate and guanosine 30,50-cyclic monophosphate pathway inhibitors, H89 and KT5823, respectively, reversed the (2R,3S)-pinobanksin-3-cinnamate-induced activations of p-Smad1/5/8, β-catenin, and runt-related transcription factor 2. Our data demonstrated that (2R,3S)-pinobanksin-3-cinnamate promoted the osteoblast differentiation of MC3T3-E1 cells, at least partially through the adenosine 30,50-cyclic monophosphate and guanosine 30,50-cyclic monophosphate signaling pathways, providing the scientific rational to develop (2R,3S)-pinobanksin-3-cinnamate against bone loss-associated diseases.

6.
Chinese Medical Equipment Journal ; (6): 89-91,108, 2018.
Article in Chinese | WPRIM | ID: wpr-700026

ABSTRACT

Objective To improve the teaching effects of medical image processing.Methods Teaching content was reformed considering the problems encountered during clinical practice and research. Modern teaching methods such as problem-based learning and flipped classroom were adopted. In addition, professors from world famous Universities were invited to teach lessons.A website was also built for this course.Moreover,the students were encouraged to participate in after-class research.Finally,a new practice-based teaching mode with characteristic content and modern methods was developed.By adopting information technology,all-round students could be gifted with international vision.Results The students'interest was stimulated and their problem solving skills were improved.Conclusion The teaching effects of medical image processing can be largely improved by research,so that the students can not only master the course content well but also develop skills to solve practical problems.

10.
Article in Chinese | WPRIM | ID: wpr-666879

ABSTRACT

Objective To understand the present situation of the chronic schistosomiasis patients'knowledge,attitude and practice on schistosomiasis control in Nanchang City. Methods The knowledge,attitude and values on schistosomiasis control of 523 chronic schistosomiasis patients in Nanchang County,Jinxian County and Xinjian District in the Poyang Lake District were investigated with questionnaires. And the accuracy rates of the knowledge,attitude and practice among the patient groups of different counties,genders,age groups,occupations and educational levels were analyzed. Results The accuracy rates of the knowledge,attitude and practice of patients on schistosomiasis control were 95.76%,82.80%,and 81.73% in Nanchang County;91.37%,93.32%,and 76.48%in Jinxian County;88.25%,67.56%,and 49.40%in Xinjian District. In the accuracy rates of knowledge,attitude and practice,the differences among the three counties (districts) were statistically significant (χ2=57.511-301.378,all P<0.05). Conclusions The accuracy rates of chronic schistosomiasis patients'attitude and prac-tice on schistosomiasis control in Nanchang City remain low. Therefore,the intensity of attitude and practice intervention should be strengthened in the Poyang Lake District in order to enhance the self-protection awareness of the patients.

12.
Chinese Journal of Rheumatology ; (12): 680-685, 2016.
Article in Chinese | WPRIM | ID: wpr-502016

ABSTRACT

Objective To analyze the clinical manifestations,immunological characteristics,pathological changes and prognosis in primary Sj(o)gren's syndrome complicated with renal involvement.Methods Three hundred and eighty-seven patients with pSS were enrolled in this retrospective study.Among these patients,198 patients were complicated with renal involvement and 189 patients without renal involvement.The data of the two groups were analyzed for clinical manifestations,blood tests,urine tests and immunological characteristics by independent sample t test,x2 test,Fisher exact probability and Logistic regression model respectively.Seventy-two patients in the group with renal involvement had kidney biopsies.Results The average of these 387 patients (female/male 345/42 cases) were (55.3±13.2) years old.The average age of 198 patients with renal involvement (female/male 168/30 cases) was (55.3±13.2) years old.The serum RF and IgG of the group with renal volvement was significantly higher than the patients without renal involvement.In the 198 patients with renal involvement;102 patients (51.5%) developed type Ⅰ renal tubular acidosis (RTA Ⅰ).Among these RTA Ⅰ patients,54 patients presented hypokalemia;12 patients developed hypokalemic plegia,30 patients with urolithiasis,6 patients with osteoporosis;69 patients presented with overt renal glomerulus impairment,36 cases had nephrotic syndrome (NS),and 33 cases had chronic glomerulonephritis;In 81 patients with renal failure,including 27 were stage 1 CKD,18 were stage 2 CKD,9 were stage 3 CKD,15 were stage 4 CKD,12 were stage 5 CKD.Among these patients with renal biopsie,light microscopy showed chronic interstitial nephritis (IN,69/72),mesangial proliferative glomerulonephritis (36/72),hyperplastic and sclerosing glomerulonephritis (9/72),partly sclerosing glomerulonephritis (9/72) and membranous nephropathy (6/72).Immunofluorescent examination revealed:IgG deposition in 21 patients (29.1%),IgA in 21(29.1%),IgM in 33(45.8%),C3 in 12(16.6%),C4 in 18(25%) and C1q in 15(20.8%).Sixty-six cases with renal biopsies were followed for (8-30)months,except the patient died of cerebral bemorrhage,all the other patients survived,and renal functions were steady or improved.Conclusion ① The pSS patients with renal involvement mainly shows interstitial nephritis.However,the occurrence of glomerulonephritis is not rare.② Rheumatoid factor (RF) or IgG is significantly associated with renal involvement in patients with pSS.③ When renal involvement is presents,renal biopsies is a necessary for patients with pSS.

13.
Asian j. androl ; Asian j. androl;(6): 633-638, 2016.
Article in Chinese | WPRIM | ID: wpr-842869

ABSTRACT

The [-2]proPSA (p2PSA) and its derivatives, the p2PSA-to-free PSA ratio (%p2PSA), and the Prostate Health Index (PHI) have greatly improved discrimination between men with and without prostate cancer (PCa) in prostate biopsies. However, little is known about their performance in cases where a digital rectal examination (DRE) and transrectal ultrasonography (TRUS) are negative. A prospective cohort of 261 consecutive patients in China with negative DRE and TRUS were recruited and underwent prostate biopsies. A serum sample had collected before the biopsy was used to measure various PSA derivatives, including total prostate-specific antigen (tPSA), free PSA, and p2PSA. For each patient, the free-to-total PSA ratio (%fPSA), PSA density (PSAD), p2PSA-to-free PSA ratio (%p2PSA), and PHI were calculated. Discriminative performance was assessed using the area under the receiver operating characteristic curve (AUC) and the biopsy rate at 91% sensitivity. The AUC scores within the entire cohort with respect to age, tPSA, %fPSA, PSAD, p2PSA, %p2PSA, and PHI were 0.598, 0.751, 0.646, 0.789, 0.814, 0.808, and 0.853, respectively. PHI was the best predictor of prostate biopsy results, especially in patients with a tPSA of 10.1-20 ng ml-1. Compared with other markers, at a sensitivity of 91%, PHI was the most useful for determining which men did not need to undergo biopsy, thereby avoiding unnecessary procedures. The use of PHI could improve the accuracy of PCa detection by predicting prostate biopsy outcomes among men with a negative DRE and TRUS in China.

14.
Article in Chinese | WPRIM | ID: wpr-849969

ABSTRACT

Objective The aim of the study was to explore the long-term benefits of coronary artery bypass grafting (CABG). Methods From January 2007 to November 2014, 240 patients (187 males and 53 females, average age 59 years) received robotic off-pump CABG assisted with da Vinci Surgical System (Intuitive Surgical, USA) in our center. Totally endoscopic coronary artery bypass (totally robot-assisted TECAB, n=100) or mini-thoracotomy direct coronary artery bypass (free of internal mammary artery, IMA, by robot, MIDCAB, n=140) grafting was performed. Patients were followed-up regularly, and their graft patency was assessed every 6 months by coronary angiography or 64-multi-slide CT angiography. Results All the procedures were completed successfully without conversion to median sternotomy or cardiopulmonary bypass, there was no operative mortality. 237 unilateral IMA grafts (98.7%) and 3 bilateral IMA grafts (1.3%) were used. Hybrid revascularization of non-left anterior descending vessels was performed in 24 patients (10%). In the follow-up of 41.1±12.9 months, no death, stroke or myocardial infarction occurred. All grafts were patent before discharge. The IMA graft patency was 97.1% in TECAB and 96.4 % in MIDCAB over 3 years (up to 91 months) after surgery. Conclusions Robotic off-pump CABG using IMA grafts is a safe and effective surgery method in selected patients. The long-term outcome and patency of IMA grafts are excellent.

15.
International Eye Science ; (12): 2088-2090, 2016.
Article in Chinese | WPRIM | ID: wpr-638062

ABSTRACT

AIM: To observe the efficacy and safety of intravitreal injection of Conbercept for the treatment of wet age-related macular degeneration( AMD) . METHODS:Retrospective analysis. A total of 20 patients involving 22 eyes were diagnosed of wet AMD and confirmed by routine ophthalmic examination, fundus fluorescein angiography ( FFA ) and optical coherence tomography. All these affected eyes received intravitreal injection of 10 mg/ml of 0. 5mg Conbercept, once monthly, for 3 successive times during the initial treatment. The need for repeated treatment was determined according to patients'disease conditions. The patients were followed up once monthly for ≥6mo. The changes in best corrected visual acuity ( BCVA ) , central retinal thickness ( CRT ) and choroidal neovascularization ( CNV) lesion leakage of the affected eyes before and after treatment were compared and analyzed. RESULTS:Within 1, 3 and 6mo after treatment, the mean BCVA ( logMAR ) of the affected eyes increased when compared with before treatment;the difference was statistically significant(PCONCLUSION: Clinically, intravitreal injection of Conbercept for the treatment of wet AMD can increase visual acuity of the affected eyes. It also can decrease CRT of the affected eyes, and inhibit neovascular leakage. There are no treatment-related adverse reactions.

16.
Rev. bras. farmacogn ; 25(2): 117-123, Mar-Apr/2015. tab, graf
Article in English | LILACS | ID: lil-749857

ABSTRACT

Abstract The effects of allelochemicals and aqueous extracts from different Pogostemon cablin (Blanco) Benth., Lamiaceae, parts and rhizosphere soil on growth parameters, leaf membrane peroxidation and leaf antioxidant enzymes were investigated in patchouli. P. cablin seedlings were incubated in solutions containing allelochemicals and aqueous extracts from different patchouli parts and its rhizosphere soil at several concentrations. Firstly, the growth parameters were significantly reduced by the highest concentration of leaves, roots and stems extracts (p < 0.05). As compared to the control, plant height was reduced by 99.8% in the treatment with leaves extracts (1:10). The malondialdehyde content increased greatly when patchouli seedlings were subject to different concentrations of leaves, roots and stems extracts; meanwhile, the superoxide dismutase and peroxidase activities showed an increase trend at the low concentration, followed by a decline phase at the high concentration of roots and leaves extracts (1:10). What's more, leaves and roots extracts had a more negative effect on patchouli growth than stems extracts at the same concentrations. Secondly, the total fresh mass, root length and plant height were greatly reduced by the highest strength of soil extracts. Their decrements were 22.7, 74.9, and 33.1%, respectively. Thirdly, growth parameters and enzymatic activities varied considerably with the kinds of allelochemicals and with the different concentrations. Plant height, root length and total fresh weight of patchouli were greatly reduced by p-hydroxybenzoic acid (200 μM), and their decrements were 77.0, 42.0 and 70.0%, respectively. Finally, three useful measures on reducing the autotoxicity during the sustainable patchouli production were proposed.

17.
Chin. med. j ; Chin. med. j;(24): 1490-1495, 2015.
Article in English | WPRIM | ID: wpr-231749

ABSTRACT

<p><b>BACKGROUND</b>Superior semicircular canal dehiscence (SSCD) is gradually recognized by otologists in recent years. The patients with SSCD have a syndrome comprising a series of vestibular symptoms and hearing function disorders which can be cured by the operation. In this study, we evaluated the characteristics of patients with SSCD and determined the effectiveness of treating this syndrome by resurfacing the canal via the transmastoid approach using a dumpling structure.</p><p><b>METHODS</b>Patients with SSCD, confirmed by high-resolution computed tomography and hospitalized at Beijing Tongren Hospital between November 2009 and October 2012, were included in the study. All of the patients underwent the unilateral transmastoid approach for resurfacing the canal, and received regular follow-up after surgery. Data from preoperative medical records and postoperative follow-up were comparatively analyzed to evaluate the effect of surgery.</p><p><b>RESULTS</b>In total, 10 patients and 13 ears (three left ears, four right ears, three bilateral ears) were evaluated in the study, which included 7 men and 3 women. Different symptoms and distinctive manifestations of vestibular evoked myogenic potential were found in these patients. After surgery, 4 patients had complete resolution, 5 had partial resolution, and 1 patient, with bilateral SSCD, had aggravation. None of the patients suffered from serious complications such as sensorineural hearing loss, facial paralysis, cerebrospinal fluid leakage, or intracranial hypertension.</p><p><b>CONCLUSIONS</b>In patients with unilateral SSCD, resurfacing the canal via the transmastoid approach using a dumpling structure is an effective and safe technique. However, more consideration is needed for patients with bilateral SSCD.</p>


Subject(s)
Adult , Female , Humans , Male , Middle Aged , Otologic Surgical Procedures , Methods , Retrospective Studies , Semicircular Canals , Congenital Abnormalities , General Surgery
18.
Rev. bras. farmacogn ; 24(6): 626-634, Nov-Dec/2014. tab, graf
Article in English | LILACS | ID: lil-741836

ABSTRACT

Sesquiterpenes Essential oil produced by patchouli was one of the most important naturally occurring base materials used in the perfume industry, containing various sesquiterpenes. Three different parts (leaves, stems and roots) of Pogostemon cablin (Blanco) Benth., Lamiaceae, were profiled in relation to different maturation phases in this paper, evaluating the variations in content of the major sesquiterpenes in the essential oil. Twelve sesquiterpenes were analyzed by GC-MS throughout the maturity of P. cablin. Patchouli alcohol (37.54%-51.02% in leaves, 28.24%-41.96% in stems and 14.55%-35.12% in roots) was the major sesquiterpene during the maturation of the plant. The average content of several other sesquiterpenes (α-bulnesene, α-guaiene, seychellene, β-humulene and caryophyllene) were higher than 3% among leaves, stems and roots. The content of essential oil, patchouli alcohol, α-bulnesene and several other compounds were highly accumulated at 210 days of maturation after cultivation of P. cablin. Thus, this period was the best moment to exploit the maximum level of these high value-added compounds in P. cablin. Furthermore, our results indicated that the essential oil extracted from leaves of P. cablin has the highest potential to be used in the perfume industry.

19.
Yao Xue Xue Bao ; (12): 977-984, 2014.
Article in Chinese | WPRIM | ID: wpr-299180

ABSTRACT

Previous studies proposed that the synergistic effect of fibroblast growth factor-21 (FGF-21) and insulin may be due to the improvement of insulin sensitivity by FGF-21. However, there is no experimental evidence to support this. This study was designed to elucidate the mechanism of synergistic effect of FGF-21 and insulin in the regulation of glucose metabolism. The synergistic effect of FGF-21 and insulin on regulating glucose metabolism was demonstrated by investigating the glucose absorption rate by insulin resistance HepG2 cell model and the blood glucose chances in type 2 diabetic db/db mice after treatments with different concentrations of FGF-21 or/and insulin; The synergistic metabolism was revealed through detecting GLUT1 and GLUT4 transcription levels in the liver by real-time PCR method. The experimental results showed that FGF-21 and insulin have a synergistic effect on the regulation of glucose metabolism. The results of real-time PCR showed that the effective dose of FGF-21 could up-regulate the transcription level of GLUT1 in a dose-dependent manner, but had no effect on the transcription level of GLUT4. Insulin (4 u) alone could up-regulate the transcription level of GLUT4, yet had no effect on that of GLUT1. Ineffective dose 0.1 mg kg(-1) FGF-21 alone could not change the transcription level of GLUT1 or GLUT4. However, when the ineffective dose 0.1 mg x kg(-1) FGF-21 was used in combination with insulin (4 u) significantly increased the transcription levels of both GLUT1 and GLUT4, the transcription level of GLUT1 was similar to that treated with 5 time concentration of FGF-21 alone; the transcription level of GLUT4 is higher than that treated with insulin (4 u) alone. In summary, in the presence of FGF-21, insulin increases the sensitivity of FGF-21 through enhancing GLUT1 transcription. Vice versa, FGF-21 increases the sensitivity of insulin by stimulating GLUT4 transcription in the presence of insulin. FGF-21 and insulin exert a synergistic effect on glucose metabolism through mutual sensitization.


Subject(s)
Animals , Humans , Mice , Blood Glucose , Diabetes Mellitus, Experimental , Metabolism , Drug Synergism , Fibroblast Growth Factors , Pharmacology , Glucose , Metabolism , Glucose Transporter Type 1 , Metabolism , Glucose Transporter Type 4 , Metabolism , Hep G2 Cells , Insulin , Pharmacology , Insulin Resistance , Liver , Metabolism
20.
Zhongguo Zhong Yao Za Zhi ; (24): 4499-4504, 2014.
Article in Chinese | WPRIM | ID: wpr-341790

ABSTRACT

To illustrate the solubility involved in biopharmaceutics classification system of Chinese materia medica (CMMBCS) , the influences of artificial multicomponent environment on solubility were investigated in this study. Mathematical model was built to describe the variation trend of their influence on the solubility of puerarin. Carried out with progressive levels, single component environment: baicalin, berberine and glycyrrhizic acid; double-component environment: baicalin and glycyrrhizic acid, baicalin and berberine and glycyrrhizic acid and berberine; and treble-component environment: baicalin, berberin, glycyrrhizic acid were used to describe the variation tendency of their influences on the solubility of puerarin, respectively. And then, the mathematical regression equation model was established to characterize the solubility of puerarin under multicomponent environment.


Subject(s)
Berberine , Chemistry , Biopharmaceutics , Drugs, Chinese Herbal , Chemistry , Flavonoids , Chemistry , Glycyrrhizic Acid , Chemistry , Isoflavones , Chemistry , Materia Medica , Chemistry , Solubility
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