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1.
Chinese Journal of Rehabilitation Theory and Practice ; (12): 1247-1252, 2021.
Article in Chinese | WPRIM | ID: wpr-905135

ABSTRACT

Objective:To design a new type of assistive chopsticks for the hand disorders, such as hand weakness and poor fine movement, etc. Methods:The assistive chopsticks were palm-control operative, integrated structure designed, and bending stamping processing technology was adopted. The key parts such as the bends and joint, holding parts were improved. The prototype was tested with finite element analysis and mechanical testing, and used on trial by a three years old boy. Results:The gripping force needed was related to the bending radius, material, section size and holding position. It required less dexterity and force for particular fingers, and was not easy to drop down. They could bounce off automatically and were suitable for left hand. Conclusion:The new type of assistive chopsticks may help the patients with hand dysfunction to have meals with chopsticks, to improve the quality of life. However, it is also suitable for Westerners with less experience.

2.
Diabetes & Metabolism Journal ; : 868-879, 2021.
Article in English | WPRIM | ID: wpr-914192

ABSTRACT

Background@#Type 2 diabetes mellitus (T2DM) is characterized by elevated fasting glucagon and impaired suppression of postprandial glucagon secretion, which may participate in diabetic complications. Therefore, we investigated the associations of plasma glucagon with estimated glomerular filtration rate (eGFR), albuminuria and diabetic kidney disease (DKD) in T2DM patients. @*Methods@#Fasting glucagon and postchallenge glucagon (assessed by area under the glucagon curve [AUCgla]) levels were determined during oral glucose tolerance tests. Patients with an eGFR <60 mL/min/1.73 m2 and/or a urinary albumin-to-creatinine ratio (UACR) ≥30 mg/g who presented with diabetic retinopathy were identified as having DKD. @*Results@#Of the 2,436 recruited patients, fasting glucagon was correlated with eGFR and UACR (r=–0.112 and r=0.157, respectively; P<0.001), and AUCgla was also correlated with eGFR and UACR (r=–0.267 and r=0.234, respectively; P<0.001). Moreover, 31.7% (n=771) presented with DKD; the prevalence of DKD was 27.3%, 27.6%, 32.5%, and 39.2% in the first (Q1), second (Q2), third (Q3), and fourth quartile (Q4) of fasting glucagon, respectively; and the corresponding prevalence for AUCgla was 25.9%, 22.7%, 33.7%, and 44.4%, respectively. Furthermore, after adjusting for other clinical covariates, the adjusted odds ratios (ORs; 95% confidence intervals) for DKD in Q2, Q3, and Q4 versus Q1 of fasting glucagon were 0.946 (0.697 to 1.284), 1.209 (0.895 to 1.634), and 1.521 (1.129 to 2.049), respectively; the corresponding ORs of AUCgla were 0.825 (0.611 to 1.114), 1.323 (0.989 to 1.769), and 2.066 (1.546 to 2.760), respectively. Additionally, when we restricted our analysis in patients with glycosylated hemoglobin <7.0% (n=471), we found fasting glucagon and AUCgla were still independently associated with DKD. @*Conclusion@#Both increased fasting and postchallenge glucagon levels were independently associated with DKD in T2DM patients.

3.
Rev. Assoc. Med. Bras. (1992) ; 66(1): 74-80, Jan. 2020. tab, graf
Article in English | LILACS | ID: biblio-1091899

ABSTRACT

SUMMARY OBJECTIVE This study aims to investigate the application value of magnetic resonance (MR) hydrography of the inner ear in cochlear implantation. METHODS 146 patients were enrolled. MR hydrography and spiral CT examinations for the intracranial auditory canal were performed before surgery, and all imaging results were statistically analyzed in order to explore the application value of MR hydrography of the inner ear in cochlear implantation. RESULTS 146 patients (292 ears) were examined. Among these patients, 13 were diagnosed with abnormal vestibular aqueducts (20 ears) by MR hydrography, while five were diagnosed with this disease by CT; 15 patients were diagnosed with inner ear malformation (19 ears) by MR hydrography, while 11 were diagnosed by CT (four were misdiagnosed); five patients were diagnosed with internal acoustic canal stenosis (eight ears) by MR hydrography, while two were diagnosed by CT (three were misdiagnosed); and four patients were diagnosed with cochlear fibrosis (five ears) by MR hydrography, while four were diagnosed by CT (four ears). The correct rate of diagnosis was 77.40% (113/146) based on CT, while the rate was 93.84% (137/146) based on MR hydrography. CONCLUSIONS MR hydrography imaging technique can be applied to the preoperative evaluation of cochlear implantation, providing accurate and reliable anatomic information on the inner membranous labyrinth and nerves in the internal acoustic canal and an accurate basis for the diagnosis of cochlear fibrosis and nerve development. This has a guiding significance for the selection of treatment schemes.


RESUMO OBJETIVO Este estudo visa investigar o valor da aplicação da hidrografia por ressonância magnética (RM) do ouvido interno no implante coclear. MÉTODOS Cento e quarenta e seis pacientes foram inscritos. Os exames da hidrografia por RM e do CT espiral para o canal auditivo intracraniano foram executados antes da cirurgia, e todos os resultados da imagem foram analisados estatisticamente, a fim de explorar o valor da aplicação da hidrografia por RM do ouvido interno no implante coclear. RESULTADOS Centro e quarenta e seis pacientes (292 ouvidos) foram examinados. Dentre esses pacientes, 13 foram diagnosticados com aquedutos vestibulares anormais (20 ouvidos) pela hidrografia por RM, enquanto cinco pacientes foram diagnosticados com esta doença pelo CT; 15 pacientes foram diagnosticados com malformação do ouvido interno (19 ouvidos) pela hidrografia por RM, enquanto 11 pacientes foram diagnosticados por CT (quatro foram diagnosticados erroneamente); cinco pacientes foram diagnosticados com estenose de canal acústico interno (oito ouvidos) pela hidrografia por RM, enquanto dois pacientes foram diagnosticados por CT (três foram diagnosticados erroneamente); e quatro pacientes foram diagnosticados com fibrose coclear (cinco ouvidos) pela hidrografia por RM, enquanto quatro foram diagnosticados por CT (quatro ouvidos). A taxa correta de diagnóstico foi de 77,40% (113/146) com base no CT, enquanto a taxa foi de 93,84% (137/146) com base na hidrografia por RM. CONCLUSÕES A técnica de imagem da hidrografia por RM pode ser aplicada à avaliação pré-operatória do implante coclear, que pode fornecer informações anatômicas precisas e confiáveis sobre o labirinto membranoso interno e os nervos no canal acústico interno, além de uma base exata para o diagnóstico da fibrose coclear e do desenvolvimento do nervo. Isso tem um significado orientador para a seleção de esquemas de tratamento.


Subject(s)
Humans , Male , Female , Infant , Child, Preschool , Child , Adolescent , Adult , Young Adult , Magnetic Resonance Imaging/methods , Cochlear Implantation/methods , Ear, Inner/diagnostic imaging , Reference Values , Reproducibility of Results , Tomography, Spiral Computed/methods , Preoperative Period , Hearing Loss, Sensorineural/surgery , Hearing Loss, Sensorineural/diagnostic imaging , Ear, Inner/surgery , Labyrinth Diseases/surgery , Labyrinth Diseases/diagnostic imaging , Middle Aged
4.
China Journal of Chinese Materia Medica ; (24): 5770-5776, 2020.
Article in Chinese | WPRIM | ID: wpr-878840

ABSTRACT

Trace metals deficiency or excess are associated with the etiology and pathogenesis of rheumatoid arthritis(RA). Aconiti Radix Cocta(A) and Paeoniae Radix Alba(B) are commonly used together for the treatment of RA. In this study, we aim to determine anti-arthritic-related metal bioavailability in the compatibility of herb A and B for avoiding metal deficiency or excess, and optimize the combination ratio of herb A and B, accordingly. Anti-arthritic-related metal bioaccessibility were evaluated by in vitro simulator of all gastrointestinal tract(including mouth, stomach, small and large intestines), and the roles of gastrointestinal digestive enzymes and intestinal microflora were investigated. Anti-arthritic-related metal bioavailability was assessed by the affinity adsorption with liposomes. The results indicated that compatibility proportion of corresponding herbal plants, gastrointestinal digestion and microbial metabolic, which could affect metal digestion and absorption. The optimal compatibility proportion of 1 A∶1 B is recommended, according to the dose of anti-arthritic-related metal bioavailability, which is often chosen for clinical practice of RA therapy. Thus, anti-arthritic-related metal bioavailability might be the key active substances for RA treatment.


Subject(s)
Aconitum , Biological Availability , Drugs, Chinese Herbal , Paeonia
5.
China Journal of Chinese Materia Medica ; (24): 3790-3796, 2020.
Article in Chinese | WPRIM | ID: wpr-828384

ABSTRACT

Forskolin is a complex labdane plant diterpenoid, which has been used in the treatment of a variety of diseases based on its activity as an activator of adenosine monophosphate(cAMP) cyclase. Natural forskolin exists only in the cork layer of the root of Coleus forskohlii. Due to the complexity of the extraction and chemical synthesis processes, the yield and purity of forskolin cannot meet commercial requirements. In recent years, with the rapid development of synthetic biology and the analysis and interpretation of many diterpene biosynthetic pathways, a new approach has been provided for the green production of forskolin. In this paper, the structure, activity, biosynthetic pathway and the heterologous biosynthesis of forskolin were reviewed. The problems and solutions in the heterologous biosynthesis of forskolin were also discussed and summarized, which will provide references for the construction of high-yielding forskolin engineering strains.


Subject(s)
Biosynthetic Pathways , Colforsin
6.
Chinese Journal of Otorhinolaryngology Head and Neck Surgery ; (12): 133-138, 2020.
Article in Chinese | WPRIM | ID: wpr-787613

ABSTRACT

To research the auditory nerve transduction effects under multi-wavelength pulsed laser stimulations within a safe and acceptable signal range. The real-time detection of intracellular calcium concentration was adopted by specific fluorescent indicator staining based on calcium imager. The spiral ganglion cells of mice were cultured in vitro. After fluorescent indicating, morphologic observation under optical microscope, Fura-2 calcium ion fluorescence excitation, intact morphology cells selection, fixing the optical fiber, the spiral ganglion cells were irradiated by different wavelength laser, including visible light (450 nm) and near infrared light (808 nm,1 065 nm). The intracellular calcium concentration was monitored by calcium ion imaging. When 450 nm laser stimulated spiral ganglion cells, the intracellular calcium concentration was strongly increased, however, for other wavelength laser stimulation, there was no obvious relative response. And the sensitivity expression of the nerve cells under laser was related with the location of laser fiber. Cells closer to the fiber produced more obvious changes in calcium ion concentration, while for cells farther away from the fiber, the change amplitudes were weaker although the number of changes in calcium ion concentration was consistent. The spiral ganglion cells of mice can induce a signal transduction response under the action of laser, and the response has laser wavelength selectivity.

7.
Journal of Southern Medical University ; (12): 135-140, 2018.
Article in Chinese | WPRIM | ID: wpr-299288

ABSTRACT

<p><b>OBJECTIVE</b>To compare the medium- and long-term effect of pneumatic ballistic extracorporeal shock wave versus ultrasound-guided hormone injection in the treatment of plantar fasciitis.</p><p><b>METHODS</b>The clinical data were collected from patients with plantar fasciitis admitted to PLA General Hospital pain department from September, 2015 to February, 2017. The patients were randomly divided into ultrasound-guided drug injection group and shock wave group. The therapeutic parameters including the numerical rating scale (NRS) scores in the first step pain in the morning, American Orthopedic Foot and Ankle Society (AOFAS) Ankle Hindfoot Scale, and thickness of the plantar fascia were monitored before and at 1 week, 1 month, 3 months, and 6 months after the treatment. The recurrence rate, effectiveness, and patient satisfaction were compared between the two groups at 6 months after the treatment.</p><p><b>RESULTS</b>Thirty-nine patients were enrolled in shock wave group and 38 patients in ultrasound group. The NRS scores in the first step pain in the morning were lowered after treatment in both groups (P<0.05), and the scores were significantly lower in ultrasound group than in shock wave group at 1 week and 1 month (P<0.01), but significantly higher in ultrasound group than in shock wave group at 3 and 6 months after treatment (P<0.05). The AOFAS functional scores were increased in both groups (P<0.05) at 6 months after treatment, was significantly lower in ultrasound group than in shock wave group than group B (90.44∓13.27 vs 75.76∓21.40; P<0.05). The effective rates in shock wave group and ultrasound group were 92.31% and 76.32%, respectively (P<0.05). Recurrence was found in 1 patient (2.56%) in shock wave group and in 8 (21.05%) in ultrasound group (P<0.05). The patient satisfaction scores were significantly higher in shock wave group than in ultrasound group (8.13∓2.67 vs 6.63∓3.75, P=0.048).</p><p><b>CONCLUSION</b>Pneumatic ballistic extracorporeal shock achieves better medium- and long-term outcomes than ultrasound-guided hormone injection in the treatment of plantar fasciitis.</p>

8.
Medical Journal of Chinese People's Liberation Army ; (12): 299-302, 2018.
Article in Chinese | WPRIM | ID: wpr-694116

ABSTRACT

Objective To investigate the efficacy ofpoly (lactic acid co castor oil) microspheres containing ropivacaine for sciatic nerve block of mice.Methods A total of 150 Kunming male mice were randomly assigned into 3 groups,namely placebo microspheres (lactic acid co castor oil) group (group A,n=50),ropivacaine injection group (group B,n=50) and ropivacaine microspheres group (group C,n=50).After sevoflurane anesthesia,the mouse was fixed on the operating table and the bilateral sciatic nerve was exposed.The corresponding preparations were implanted or injected near the sciatic nerve.Five mice were randomly selected from each group for the next experiments.Paw withdrawal thermal latency,the ability to splay and flex of the hind paw and plasma ropivacaine concentration were measured 10min,30min,1h,3h,5h,7h,10h,15h,30h and 48h after drug administration.Results The anesthetic effect of group C began to work at 3h.Compared with group B,the duration of sciatic nerve sensory block of group C was significantly longer and the effect of motor block was weaker.No anesthetic effect was observed in group A.The sensory and motor block of group B reached the peak at 1h,and the pharmacodynamics subsided at 7h.Compared with group B,the concentration of ropivacaine in group C increased slowly,and the peak value at 10h after administration was gradually decreased.Conclusions Ropivacaine loading poly (lactic acid co castor oil) microspheres can significantly extend the effect of ropivacaine on sciatic nerve sensory block.Compared with ropivacaine injection,motor block effect of ropivacaine loading poly (lactic acid co castor oil) microspheres is reduced and its plasma ropivacaine concentration fluctuation range is small.

9.
Journal of Xi'an Jiaotong University(Medical Sciences) ; (6): 116-120, 2018.
Article in Chinese | WPRIM | ID: wpr-665573

ABSTRACT

Objective To explore the effects of Chinese herbal compound Qinghuayin on the pathological changes of gastric mucosa and interleukin-10 (IL-10) ,nitric oxide (NO) ,gasmn (GAS) and motilin (MTL) in the serum in the animal model of chronic atrophic gastritis (CAG ) in rats .Methods We divided 53 Wistar rats randomly into blank control group (n=8) and CAG model group (n=45) ,and the animal model of CAG in rats was replicated by combination of disease and syndrome .After confirming the sampled rat model was successful built , the other 40 CAG rats in CAG model group were divided into model group ,vitacoenzyme tablet group ,low-dosage TMC group ,medium-dosage TMC group ,and high-dosage TMC group (each group n=8) .With the corresponding drug intervention to different rats for 30 days , the rats were executed . Then their blood was drawn from the abdominal aorta and the gastric tissue was taken to analyze the changes of serum IL-10 ,NO ,GAS and MTL concentrations and gastric mucosa pathology . Results Compared with blank control group , model group had various degrees of gastric mucosa atrophy ; decreased concentrations of serum IL-10 and GAS ; increased NO and MTL ( P<0 .01 ) .Compared with model group,Qinghuayin could improve gastric mucosa pathology in different degrees and increase the concentrations of IL-10 and GAS . Decrease the concentrations of NO and MTL( P<0 .05 or P<0 .01 ) . What's more. The curative effect in high-dosage TMC group was better( P<0. 01 ). Conclusion Chinese herbal compound Qinghuayin can effectively regulate the lopsided expressions of serum IL-10 . NO .GAS and MTL and reverse the pathological and histological changes in the gastric mucosa of CAG rats .

10.
Chinese Health Economics ; (12): 28-29, 2018.
Article in Chinese | WPRIM | ID: wpr-703510

ABSTRACT

Through the investigation of the single disease policy and the local actual situation in many regions of the country, it analyzed the practical problems faced by Chinese medical institutions in the implementation of single disease payment policy. The necessity and urgency of the national unified single disease payment policy were put forward, and the system of standard quota payment for single disease standard was preferred, supporting patients to pay extra fees for differential medical services, standardize the accounting policy of single disease payment.

11.
Chinese Journal of Pathophysiology ; (12): 15-21, 2018.
Article in Chinese | WPRIM | ID: wpr-701071

ABSTRACT

AIM:To observe the effects of vitamin D on the apoptosis ,prolyl isomerase 1(Pin1)protein ex-pression and activity ,mitochondrial translocation of p 66Shc,and reactive oxygen species(ROS)production in high glu-cose-cultured human umbilical vein endothelial cells(HUVECs),and to explore the role of vitamin D receptor(VDR)in these processes.METHODS:HUVECs were treated with high glucose(33 mmol/L)in the presence or absence of vita-min D or Pin1 inhibitor juglone.The cell apoptosis was measured by flow cytometry and TUNEL staining.Intracellular ROS levels were examined by flow cytometry and fluorescence microscopy.The protein levels of Pin1,p66Shc,p-p66Shc,mito-chondria to cytoplasm ratio of p66Shc,and caspase-3 in HUVECs were measured by Western blot.Pin1 activity in HU-VECs lysate was assessed by a commercial kit.Knockdown of VDR by siRNA was conducted to evaluate the role of VDR in the regulatory effects of vitamin D on Pin 1 protein expression and activity in HUVECs under high-glucose condition.RE-SULTS:Vitamin D suppressed the apoptosis and intracellular ROS generation of HUVECs induced by high glucose(P<0.05).Vitamin D inhibited high glucose-induced upregulation of Pin1 protein expression and activity(P<0.05).Vita-min D inhibited the phosphorylation and mitochondrial translocation of p 66Shc and caspase-3 protein expression induced by high glucose(P<0.05).Knockdown of VDR by siRNA abolished the inhibitory effects of vitamin D on high glucose-in-duced upregulation of Pin 1 protein expression and activity.CONCLUSION:Vitamin D alleviates high glucose-induced endothelial cell apoptosis by inhibition of Pin 1 protein expression and activity ,and attenuation of p66Shc-mediated mito-chondrial oxidative stress ,which are dependent on VDR activation.

12.
Acta Anatomica Sinica ; (6): 199-203, 2017.
Article in Chinese | WPRIM | ID: wpr-844686

ABSTRACT

Objective: To investigate the distribution of bone strength index of adult Tibetans in Tibet and analyze the correlation between of their body composition and incidence of bone mass abnormal. Methods: The bone strength of right calcaneus, T score and body composition of 560 Tibetans in Shigatse, Tibet by using an ultrasonic bone mineral density meter and bioelectric impedance technique. Binary Logistic Regression was used to test the relationship of incidence of bone mass abnormal and body composition. Results: The bone mass index of the male and female participants reached the maximum at their 18-30 years old, and then declined with aging. The incidence of osteoporosis among male and female participants ≥50 years old were 7. 6% and 11. 7% respectively. Age(B =0. 046,OR = 1. 047,P <0. 01)and visceral fat mass (B = 0. 452, OR = 1. 572, P < 0. 05) were risk factors of incidence of bone mass abnormal whereas the subcutaneous fat mass (B = - 0. 181, OR = 0. 835, P < 0. 01) and muscle mass (B = - 0. 055, OR = 0. 947, P < 0. 05) were protective factors. Conclusion: The incidence of osteoporosis among Tibet Tibetans ≥50 years old are lower than other nationalities of China in the same age. The participants with high visceral fat mass while low subcutaneous fat mass and muscle mass are more likely to suffer from osteoporosis.

13.
Chinese Circulation Journal ; (12): 1117-1122, 2017.
Article in Chinese | WPRIM | ID: wpr-667931

ABSTRACT

Objective: To observe the effects of liraglutide on angiogenesis and myocardium protection in acute myocardial infarction (AMI) rats with its mechanisms. Methods: Rat's AMI model was established by left anterior descending of coronary ligation. AMI rats were randomly divided into 3 groups: Control group, the rats received subcutaneous injection of normal saline, Low dose (LS) group and High dose (HS) group, rats received subcutaneous injection of liraglutide 70μg/(kg?d) and 140μg/(kg?d) respectively; in addition, Sham operation group, rats received normal saline. n=6 in each group, all animals were treated for 2 weeks. 4 weeks later, cardiac structure and function were assessed by echocardiography, morphological changes of myocardium were observed by HE staining, collagen volume fraction (CVF) was calculated by Masson staining, myocardial microvessel density (MVD) and protein expression of vascular endothelial growth factor (VEGF) in marginal zone of infracted region were detected by immunohistochemistry, VEGF protein level was examined by Western blot analysis. Results: Compared with Sham operation group, Control group showed decreased LVEF, LVFS and increased LVEDd, LVESd, CVF, all P<0.01; while MVD and VEGF protein level were similar between 2 groups, P>0.05. Compared with Control group, LS group and HS group had obviously increased LVEF, LVFS, P<0.01 and decreased LVEDd, LVESd, P<0.05, obviously decreased CVF, P<0.01; obviously elevated MVD and VEGF protein level, P<0.01. Compared with LS group, HS group presented obviously increased LVEF, LVFS, P<0.01 and decreased LVEDd, LVESd, CVF, P<0.05; elevated MVD and VEGF protein level, P<0.01 or P<0.05. Conclusion: Liraglutide could improve angiogenesis in AMI rats which might be related to increased VEGF expression and reduced collagen deposition; therefore improve left ventricular systolic function for cardiac protection. The effect had certain relationship to liraglutide dosage.

14.
China Journal of Chinese Materia Medica ; (24): 3490-3495, 2016.
Article in Chinese | WPRIM | ID: wpr-307132

ABSTRACT

Based on the basic theory of thermodynamics, the thermodynamic parameters and related equations in the process of water adsorption and desorption of Chinese herbal decoction pieces were established, and their water absorption and desorption characteristics were analyzed. The physical significance of the thermodynamic parameters, such as differential adsorption enthalpy, differential adsorption entropy, integral adsorption enthalpy, integral adsorption entropy and the free energy of adsorption, were discussed in this paper to provide theoretical basis for the research on the water adsorption and desorption mechanism, optimum drying process parameters, storage conditions and packaging methods of Chinese herbal decoction pieces.

15.
Biomedical and Environmental Sciences ; (12): 356-364, 2016.
Article in English | WPRIM | ID: wpr-258812

ABSTRACT

<p><b>OBJECTIVE</b>We investigated the feasibility and efficacy of cognitive training for older adults in rural settings and with low education levels, who have mild cognitive impairment (MCI).</p><p><b>METHODS</b>Forty-five older adults (ages >65 years) with MCI were assigned to treatment or control groups, at a 2:1 ratio. Cognitive training occurred in the treatment group for 2 months. The cognitive abilities of the participants were assessed at pre-training, metaphase, and post-training time points, using the Mini-Mental State Examination (MMSE), Montreal Cognitive Assessment (MoCA), Loewenstein Occupational Therapy Cognitive Assessment (LOTCA), and Hamilton Depression Scale (HAM-D).</p><p><b>RESULTS</b>Following training, cognitive abilities improved in the treatment group, based on the total scores of all 4 measures, as well as specifically on the MoCA and LOTCA. There were differences in the main effects of group and time point on some subscales, but these differences had little, if any, effect on the overall analyses.</p><p><b>CONCLUSION</b>The present study demonstrated that cognitive training has beneficial effects on attention, language, orientation, visual perception, organization of visual movement, and logical questioning in patients with MCI. Furthermore, the observed effects are long-term changes.</p>


Subject(s)
Aged , Aged, 80 and over , Female , Humans , Male , China , Cognition , Cognitive Dysfunction , Psychology , Neuropsychological Tests
16.
Acta Pharmaceutica Sinica ; (12): 1864-2016.
Article in Chinese | WPRIM | ID: wpr-779344

ABSTRACT

Bentysrepinine (Y101), a derivative of phenyalanine dipeptide, has a novel mechanism in the treatment of hepatitis B virus (HBV) infection with a good anti-HBV effect. In the present study, a fluorometric-based high throughput method using cytochrome P450 (CYP) screening kit was adopted to evaluate in vitro inhibition potential of Y101 on CYP isoenzymes by calculating remaining enzyme activities and inhibitory potential (IC50 values) using the determined values of fluorescence intensity. The result showed that Y101 exhibited little activity in the inhibition of CYP1A2, CYP3A4, CYP2C9, CYP2C19 and CYP2D6 (IC50 > 100 μmol·L-1). Y101 was used to treat human primary hepotocytes for 72 h, and the enzyme activities of CYP1A2, CYP2B6 and CYP3A4 were determined with a cocktail of probe substrates for the three CYP isoforms. The metabolites were simultaneously determined using a LC-MS/MS method. Y101 had no activity in the induction of CYP1A2, CYP2B6 and CYP3A4 on the basis of the following results:① The ratio of enzyme activities between test and control groups were all below than 1 (varied from 0.662 to 0.928); ② The induction potential of Y101 were lower than forty percent compared with that of positive groups. The above results suggest that Y101 has little activity in the regulation of metabolic drug-drug interactions based on the CYP isoform changes following co-administration of drugs.

17.
Acta Pharmaceutica Sinica ; (12): 1233-2016.
Article in Chinese | WPRIM | ID: wpr-779301

ABSTRACT

Bentysrepinine (Y101), a derivative of phenylalanine dipeptide, is a novel drug candidate for the treatment of hepatitis B virus (HBV) infection. Our previous preclinical pharmacokinetic study showed that its in vivo absorption and distribution characteristics were probably related to transmembrane transport after Y101 was administered intragastically in rats. In this study, Caco-2 and MDCK-MDR1 cell models were used to investigate interactions between Y101 and P-gp through the apparent permeation coefficient (Papp) and efflux ratio (RE); the results showed that Y101 was a substrate of P-gp. In addition, gene-transfected cell models, HEK293-hOATP1B1, HEK293-hOATP2B1 and CHO-PEPT1 were used to evaluate the affinity to OATP1B1,

18.
Chinese journal of integrative medicine ; (12): 420-429, 2016.
Article in English | WPRIM | ID: wpr-310860

ABSTRACT

<p><b>OBJECTIVE</b>This study aimed at investigating whether notoginsenoside R1 (R1), a unique saponin found in Panax notoginseng could promote angiogenic activity on human umbilical vein endothelial cells (HUVECs) and elucidate their potential molecular mechanisms. In addition, vascular restorative activities of R1 was assessed in a chemically-induced blood vessel loss model in zebrafish.</p><p><b>METHODS</b>The in vitro angiogenic effect of R1 was compared with other previously reported angiogenic saponins Rg1 and Re. The HUVECs proliferation in the presence of R1 was determined by cell proliferation kit II (XTT) assay. R1, Rg1 and Re-induced HUVECs invasion across polycarbonate membrane was stained with Hoechst-33342 and quantified microscopically. Tube formation assay using matrigelcoated wells was performed to evaluate the pro-angiogenic actions of R1. In order to understand the mechanism underlying the pro-angiogenic effect, various pathway inhibitors such as SU5416, wortmannin (wort) or L-Nω-nitro- L-arginine methyl ester hydrochloride (L-NAME), SH-6 were used to probe the possible involvement of signaling pathway in the R1 mediated HUVECs proliferation. In in vivo assays, zebrafish embryos at 21 hpf were pre-treated with vascular endothelial growth factor (VEGF) receptor kinase inhibitor II (VRI) for 3 h only and subsequently post-treated with R1 for 48 h, respectively. The intersegmental vessels (ISVs) in zebrafish were assessed for the restorative effect of R1 on defective blood vessels.</p><p><b>RESULTS</b>R1 could stimulate the proliferation of HUVECs. In the chemoinvasion assay, R1 significantly increased the number of cross-membrane HUVECs. In addition, R1 markedly enhanced the tube formation ability of HUVECs. The proliferative effects of these saponins on HUVECs were effectively blocked by the addition of SU5416 (a VEGF-KDR/Flk-1 inhibitor). Similarly, pre-treatment with wort [a phosphatidylinositol 3-kinase (PI3K)-kinase inhibitor], L-NAME [an endothelial nitric oxide synthase (eNOS) inhibitor] or SH-6 (an Akt pathway inhibitor) significantly abrogated the R1 induced proliferation of HUVECs. In chemicallyinduced blood vessel loss model in zebrafish, R1 significantly rescue the damaged ISVs.</p><p><b>CONCLUSION</b>R1, similar to Rg1 and Re, had been showed pro-angiogenic action, possibly via the activation of the VEGF-KDR/Flk-1 and PI3K-Akt-eNOS signaling pathways. Our findings also shed light on intriguing pro-angiogenic effect of R1 under deficient angiogenesis condition in a pharmacologic-induced blood vessels loss model in zebrafish. The present study in vivo and in vitro provided scientific evidence to explain the ethnomedical use of Panax notoginseng in the treatment of cardiovascular diseases, traumatic injuries and wound healing.</p>


Subject(s)
Animals , Humans , Blood Vessels , Pathology , Cell Movement , Cell Proliferation , Collagen , Pharmacology , Disease Models, Animal , Drug Combinations , Ginsenosides , Chemistry , Pharmacology , Human Umbilical Vein Endothelial Cells , Cell Biology , Physiology , Laminin , Pharmacology , Neovascularization, Physiologic , Phosphatidylinositol 3-Kinases , Metabolism , Protein Kinase Inhibitors , Pharmacology , Proteoglycans , Pharmacology , Proto-Oncogene Proteins c-akt , Metabolism , Vascular Endothelial Growth Factor Receptor-2 , Metabolism , Zebrafish
19.
Chinese Medical Journal ; (24): 2281-2286, 2016.
Article in English | WPRIM | ID: wpr-307422

ABSTRACT

<p><b>BACKGROUND</b>Diabetes mellitus (DM) remains a major health problem worldwide. Several clinical trials have shown the superiority of the Traditional Chinese Medicine in delaying or reversing the development and progression of DM. This study aimed to evaluate the efficacy of Jinlida (JLD) granule, a Chinese herbal recipe, in the treatment of impaired glucose tolerance (IGT) and its effect on the prevention of DM.</p><p><b>METHODS</b>Sixty-five IGT patients were randomized to receive one bag of JLD granules three times daily (JLD group, n = 34) or no drug intervention (control group, n = 31) for 12 weeks. Oral glucose tolerance test, glycated hemoglobin A1c (HbA1c), body mass index, blood lipids levels, fasting insulin, and insulin resistance calculated using homeostatic model assessment (HOMA-IR) of all the patients were observed and compared before and after the treatment.</p><p><b>RESULTS</b>Sixty-one participants completed the trial (32 in JLD group and 29 in the control group). There were statistically significant decreases in HbA1c (P < 0.001), 2-h plasma glucose (P < 0.001), and HOMA-IR (P = 0.029) in JLD group compared with the control group after 12 weeks of treatment. After 12 weeks of treatment, two (6.9%) patients returned to normal blood glucose, and five (17.2%) patients turned into DM in control group, while in the JLD group, 14 (43.8%) returned to normal blood glucose and 2 (6.2%) turned into DM. There was a significant difference in the number of subjects who had normal glucose at the end of the study between two groups (P = 0.001).</p><p><b>CONCLUSIONS</b>JLD granule effectively improved glucose control, increased the conversion of IGT to normal glucose, and improved the insulin resistance in patients with IGT. This Chinese herbal medicine may have a clinical value for IGT.</p>


Subject(s)
Adult , Female , Humans , Male , Middle Aged , Blood Glucose , Body Mass Index , Drugs, Chinese Herbal , Therapeutic Uses , Glucose Intolerance , Blood , Drug Therapy , Glucose Tolerance Test , Glycated Hemoglobin , Metabolism , Hypoglycemic Agents , Therapeutic Uses , Insulin , Blood , Insulin Resistance
20.
Journal of Medical Biomechanics ; (6): E226-E232, 2015.
Article in Chinese | WPRIM | ID: wpr-804471

ABSTRACT

Objective To develop a double-gasbag weight loss equipment based on body weight support treadmill training (BWSTT),and analyze the reasonability of the structure design. Methods The mathematical model of double gasbags in the process of air inflation was established, and the 3D model of double gasbags was established and meshed using Gambit; the analog computation for gas flow of the gasbag was conducted using Fluent; normal subjects with body weight below 80 kg were selected for clinical experiments based on designing and roughing of the prototype. Results The inflation time of double gasbags was 16.9 s and the maximum weight loss percentage was 90%; the pressure inside double gasbags was 2 kPa, and the relationship between the weight loss percentage and inside pressure of the gasbag was obtained by clinical experiments, which verified the reasonability of the gasbag structure. Conclusions The double-gasbag structure can meet the requirements of weigh loss training, which provides an effective weight loss support method and a feasible structural design for patients with lower limb dysfunction during rehabilitation training.

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