Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 20 de 25
Filter
1.
Molecules ; 27(18)2022 Sep 12.
Article in English | MEDLINE | ID: mdl-36144662

ABSTRACT

We synthesized a set of small molecules using a molecular hybridization approach with good yields. The antiviral properties of the synthesized conjugates against the SAR-CoV-2 virus were investigated and their cytotoxicity was also determined. Among all the synthesized conjugates, compound 9f showed potential against SARS-CoV-2 and low cytotoxicity. The conjugates' selectivity indexes (SIs) were determined to correlate the antiviral properties and cytotoxicity. The observed biological data were further validated using computational studies.


Subject(s)
COVID-19 Drug Treatment , SARS-CoV-2 , Antiviral Agents/therapeutic use , Humans , Molecular Docking Simulation
2.
Indian J Hematol Blood Transfus ; 37(2): 302-308, 2021 Apr.
Article in English | MEDLINE | ID: mdl-33867738

ABSTRACT

Early initial massive transfusion protocol and blood transfusion can reduce patient mortality, however accurately identifying the risk of massive transfusion (MT) remains a major challenge in severe trauma patient therapy. We retrospectively analyzed clinical data of severe trauma patients with and without MT. Based on analysis results, we established a MT prediction model of clinical and laboratory data by using the decision tree algorithm in patients with multiple trauma. Our results demonstrate that shock index, injury severity score, international normalized ratio, and pelvis fracture were the most significant risk factors of MT. These four indexes were incorporated into the prediction model, and the model was validated by using the testing dataset. Moreover, the sensitivity, specificity, accuracy and area under curve values of prediction model for MT risk prediction were 60%, 92%, 90% and 0.85. Our study provides an easy and understandable classification rules for identifying risk factors associated with MT that may be useful for promoting trauma management.

3.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-882500

ABSTRACT

In recent years, with being gradually developed, three-dimensional (3D) reconstruction based on pathology and medical imaging technology has shown certain value in the diagnosis and treatment of breast cancer. And with its advantages of providing the spatial location, morphological structure and 3D structure relationships with the surrounding tissues and organs, 3D reconstruction technology has played a key role in the early diagnosis, surgical treatment, and accurate evaluation of the treatment effect after surgery of breast cancer. Although the application of 3D reconstruction technology based on pathology and medical imaging is still inadequate, with the continuous development of science and technology, 3D reconstruction technology will play an increasingly important role in the diagnosis, personalized treatment and prognosis assessment of breast cancer.

4.
Article in English | WPRIM (Western Pacific) | ID: wpr-887747

ABSTRACT

Malocclusion is one of the three most common oral diseases reported by World Health Organization(WHO). In China, its incidence rate is rising. Malocclusion seriously affects the dental and maxillofacial function, facial appearance and growth development of nearly 260 million children in China, and what is more, it affects their physical and mental health development. Malocclusion occurrence is related to genetic and environmental factors. Early treatment of malocclusion can create a good dental and maxillofacial development environment, correct abnormal growth and control the adverse effects of abnormal genetic factors. It can effectively reduce the prevalence of children's malocclusion and enhance their physical and mental health. This is an urgent need from the economic perspective of our society, so it has great practical and social significance. Experts from the project group "standard diagnose and treatment protocols for early orthodontic intervention of malocclusions of children" which initiated by China National Health Institute of Hospital Administration wrote the "China Experts' Consensus on Preventive and Interceptive Orthodontic Treatments of Malocclusions of Children", which aims to guide and popularize the clinical practice, improve the clinical theory and practice level, and accelerate the disciplinary development of early treatment of children's malocclusion in China. The consensus elaborates the harmfulness of malocclusion and the necessity of early treatment, and brings up the principles and fundamental contents. Based on the law of dental and maxillofacial development, this paper puts forward the guiding suggestions of preventive and interceptive treatments in different stages of dental development ranging from fetus to early permanent dentition. It is a systematic project to promote and standardize the early treatment of malocclusion. Through scientific and comprehensive stratified clinical practice and professional training, the clinical system of early treatment of malocclusion in China will eventually be perfected, so as to comprehensively care for children's dental and maxillofacial health, and improve their oral and physical health in China.


Subject(s)
Child , Humans , China/epidemiology , Consensus , Dental Care , Malocclusion/prevention & control , Orthodontics, Interceptive
5.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-846197

ABSTRACT

Objective: To investigate the chemical constituents from Isodon amethystoides distributed in Libo. Methods: Chemical constituents were isolated and purified by chromatography with silica gel, MCI gel CHP 20P, and Sephadex LH-20. The structures of all compounds were elucidated by physicochemical properties, comprehensive spectral data and references. Results: Eighteen known compounds were isolated from the methanol extract of I. amethystoides, which were elucidated as lophanic acid (1), rubesanolide D (2), fladin A (3), 3,4-secoisopimara-4(18),7,15-triene-3-oic acid methylester (4), 3,4-secoisopimara-4(18),7, 15-triene-3-oic acid (5), isopimara-7,15-dien-3-one (6), isopimara-7,15-dien-3β-ol (7), alpiniol (8), (-)-clovane-2,9-diol (9), ursolic acid (10), oleanolic acid (11), epimaslinic acid (12), 7α-hydroxysitosterol (13), β-sitosterol (14), stigmasterol (15), sesamin (16), paulownin acetate (17) and dibutyl phthalate (18). Conclusion: Compound 4 is a new natural product, and compounds 2-9, 15-18 are isolated from I. amethystoides for the first time.

6.
China Pharmacy ; (12): 2458-2461, 2020.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-829350

ABSTRACT

OBJECTIVE:To st udy the chemical constituents of diterpenoids from Buyi medicine Isodon coetsa ,and to provide reference for the development and utilization of the medicinal resources. METHODS :The 95% methanol extract of Buyi medicine I. coetsa were isolated and purified with silica gel column ,Sehadex LH- 20 gel column and MCI column. The structures of the compounds were obtained by spectral analysis (mass spectrum ,hydrogen spectrum and carbon spectrum ),and then compared with active components of Miao medicine “Isodon flavidus ”. RESULTS & CONCLUSIONS :Ten diterpenoids were obtained from I. coetsa,including rabdocoetsin B (Ⅰ),megathgrin B (Ⅱ),rabdocoetsin A (Ⅲ),enanderianin N (Ⅳ),rabdocoetsin D (Ⅴ), megathyrin A (Ⅵ),lophanic acid (Ⅶ),rubesanolide D (Ⅷ),excisanin D (Ⅸ),excisanin K (Ⅹ). The compounds Ⅶ,Ⅸ and Ⅹ were isolated from this specie for the first time. Compound Ⅶ(lophanic acid )is a common active component in the Buyi medicine I. coetsa and Miao medicine “I. flavidus ”.

7.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-827187

ABSTRACT

OBJECTIVE@#To evaluate the characteristics of autoimmune hemolytic anemia caused by salvianolate by antibody detection and clinical index monitoring.@*METHODS@#Micro-column gel anti-human globulin method was used for irregular antibody screening and antibody identification. Salvianolate, sodium creatine phosphate and levocarnitine were used to sensitize red blood cells that were compatible with the patient's plasma, and the RBCs were used to test drug antibody in patient plasma respectively. The patient's clinical examination of hemolysis index and blood transfusion effect were analyed retrospectively.@*RESULTS@#The patients were positive for irregular antibody screening, and there were antoanti-Ce antibodies in serum. The erythrocytes sensitized with salvianolate in the patient's serum were positive, while those sensitized with sodium creatine phosphate and levocarnitine were negative.@*CONCLUSION@#Salvianolate causes drug-induced autoimmune hemolytic anemia in this patient.


Subject(s)
Humans , Anemia, Hemolytic, Autoimmune , Blood Transfusion , Erythrocytes , Plant Extracts , Retrospective Studies
8.
Chinese Journal of Pathology ; (12): 328-333, 2018.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-809953

ABSTRACT

Objective@#To investigate the clinicopathological characteristics and prognostic factors of neuroendocrine carcinoma (NEC) of the cervix.@*Methods@#Eight-two patients diagnosed as NEC of cervix from 2008 to 2016 at West China Second University Hospital were analyzed retrospectively including HE slide review, immunohistochemistry and HPV genotyping. Survival analysis was performed using Kaplan-Meier and Cox regression model.@*Results@#The age of the patients ranged from 16 to 75 years with mean age of 43 years. According to International Federation of Gynecology and Obstetrics (FIGO) clinical stage, 52 cases were in stageⅠ, 10 cases in stageⅡ, 14 cases in stage Ⅲ and 6 cases in stage Ⅳ. The tumor size ranged from 0.5 to 6.5 cm, with an average of 3.6 cm. Upon histopathologic review, 74 tumors were classified as small cell carcinoma; 7 tumors as large cell NEC, and 1 as atypical carcinoid. Further evaluation showed 52 cases (63.4%) with deep stromal invasion, 73 cases (89.0%) with lymph-vascular invasion, and 28 cases (34.2%) with pelvic and (or) para-aortic lymph nodes involvement. Immunohistochemical staining showed neuroendocrine markers Syn, CD56, NSE, S-100 protein and CgA were positive in 93.9%, 84.2%, 74.4%, 64.6% and 51.2% of cases, respectively. The results of HPV-DNA detection were positive in 72 cases, high-risk HPV types were 70 cases and 49 cases were HPV18 positive. The median follow-up time was 37 months (range, 6-101 months). Twenty-nine cases were found recurrence or metastasis, including 23 cases of death. The univariate analysis demonstrated that the tumor size, lymph node metastasis, infiltration depth, FIGO stage and whether the lesion confined to the uterus were significant prognostic factors(P<0.05). Cox multivariate analysis showed that lymph node metastasis and FIGO stage were independent prognostic factors of NEC(P<0.05).@*Conclusions@#NEC of the cervix is a highly aggressive malignancy with poor prognosis. The tumor is associated with HPV infection, especially type 18. Small cell NEC is the most common type of cervical NEC. Diagnosis is based on histological and immunohistochemical examination. Lymph node metastasis and FIGO stage are the independent factors affecting prognosis.

9.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-772454

ABSTRACT

Obstructive sleep apnea syndrome (OSAS) is a common clinical disease with high incidence and low treating proportion, difficult evaluation, and complicated nosogenesis. OSAS can cause systematic impairments. Various treatment methods were applied in clinical setting with the tendency of cross-disciplinary promotion. Oral treatment plays an exceedingly important role in OSAS research and therapy. This study reports the oral treatment involving OSAS therapy.


Subject(s)
Humans , Sleep Apnea, Obstructive , Therapeutics
10.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-607452

ABSTRACT

Objective To analyze the influence of different factors and their relating correlation results on platelet transfusion during the bone marrow empty window period on the patients who have undergone allogeneic peripheral blood stem cell transplantation (allo-HSCT) with retrospective analysis of case-control data.Methods Clinical data of 153 cases were collected by the clinical blood management and evaluation information system with discharge diagnosis of allo-HSCT in the hematology department of The First Affiliated Hospital of Nanchang University within a time frame from January 2014 to December 2016.A total of 90 cases were considered valid for retrospective analysis according to the case exclusion criteria.The average transfusion dose for patients with allo-HSCT during the bone marrow empty window period was defined as the threshold value which divided the 90 cases into the observation group of 38 cases receiving more than 6 Units of platelet transfusion and the control group of 52 cases with less than 6Units of platelet transfusion.The amount of platelets transfused during the bone marrow empty window period,clinical indexes include Hb,ANC,Plt,SF before pretreatment,platelet engraftment time and the number of mononuclear cells implanted were compared and analyzed by Logistic regression.Results (1) There was no significant difference between the two groups in gender,age,primary diagnosis,HLA matching,Hb before pretreatment and the number of mononuclear cells implanted (P>0.05).The ANC(×109/L) (1.24±0.57 vs 3.36±1.33) and Plt(×109/L) (43.55±68.29 vs 126.62±84.73) counts before pretreatment in the observation group were significantly lower than those in the control group(P<0.05).SF(μg/L) (2351.05 ± 1 587.96 vs 1 000.96± 362.97)before pretreatment and P LT recovery time (d) (16.84± 2.47 vs 12.73 ± 1.65)was significantly higher than that in the control group(P<0.05).Donor-recipient ABO blood group typing incompatibility (15 vs 10) was significantly higher than the control group (P<0.05);(2) Single factor Logistic regression analysis showed that ABO blood group matching,clinical indexes include ANC,Plt,SF before pretreatment,PLT recovery time were statistically significant,Only ANC before pretreatment and PLT recovery time had significant effect on the platelet transfusion during bone marrow empty window period in patients with allo-HSCT in multivariate Logistic regression analysis(P<0.05).Condusion The ANC before pretreatment and PLT recovery time are independent factors for platelet transfusion of the bone marrow empty window period in patients with allo-HSCT.The PLT recovery time is an independent risk factor,which indicates that the longer the duration of PLT implantation,the greater the amount of platelet transfusion will be needed.Besides,the ANC before pretreatment is the independent protective factor,which indicates that the greater the ANC,the smaller the amount of platelet transfusion is required.

11.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-607372

ABSTRACT

Objective To evaluate the clinical value of apheresis platelets throught heanalysisof case control on the clinical efficacy and safety of cryopreserved apheresis platelets and fresh apheresis platelets.Methods 2 035 clinical cases of platelet transfusion in August 2014 to December 2016 by Using the closed loop intelligent path management and evaluation information system,456 cases were selected as control cases.Platelets were divided into the cryopreserved apheresis platelets group (group A,n=199) and fresh apheresis platelets group (group B,n=257) according to the transfused platelet type.The clinical application value of cryopreserved single platelets was evaluated by comparing the basic data,the effective indexes and safety indexes of the two groups.Results 1) The cases were 43.6% (199/456) in A groups,and 56.4% (257/456) in B groups,there were no significant difference in gender,age and medical and surgical cases between A and B group (P>0.05);2) 199 cases in group A were cryopreserved platelets of 2 275 U,including 121 medicine cases,the total amount of transfusion was about 60.9% (1 385/2 275),78 surgical cases accounted for 39.1% (890/2 275);In the distribution of diseases,the blood system diseases accounted for 49.2% (1 120/2 275),the total amount of obstetrics and gynecology disease infusion accounted for 10.6% (240/2 275),and the amount of tumor radiotherapy and chemotherapy accounted for 6.2% (140/2 275);The proportion of ABO blood type distribution was O type 25.9%,A type 22.9%,Btype 20.7%,ABtype 30.5%,respectively;3) The Plt counts of group A and B were significantly different before and after transfusion (P <0.05).But there was no significant difference between the two groups of cases before transfusion and 24h Plt count after transfusion,the Plt counts difference,and 24 h CCI (P>0.05);4) The effective rates of platelet transfusion in group A and B were 76.9% and 76.7%,respectively.Which has no significant difference between the two groups (P>0.05)).There was no significant difference between the two groups in medical and surgical cases (P>0.05),but the effective rate of surgical cases in group A (84.6%) was higher than that in B group (75.3%).The difference effect of medicine and surgery cases in B group were not statistically significant (P>0.05),but the difference effect of medicine and surgery cases in A group was statistically significant (P<0.05),platelet transfusion inefficient in surgical cases (15.4%) was significantly lower than that of cases (28.1%);5) The incidence of adverse reactions of blood transfusion was 3.5%,4.7% in group A and B,and the blood transfusion mortality rate was zero,the difference was not statistically significant (P> 0.05).Conclusion The clinical effectiveness and safety of cryopreserved apheresis platelets are similar to those of fresh apheresis platelets,and the former can be widely Used in clinic,in particular,it has certain advantages in the surgical hemostatic effect.but for repeated infusion cases or platelet transfusion ineffective cases should be given priority to fresh apheresis platelets.

12.
Article in English | WPRIM (Western Pacific) | ID: wpr-638122

ABSTRACT

Alzheimer's disease (AD) is one of the major neurodegenerative disorders of the elderly, which is characterized by the accumulation and deposition of amyloid-beta (Aβ) peptide in human brains. Oxidative streβs and neuroinflammation induced by Aβ in brain are increasingly considered to be responsible for the pathogenesis of AD. The present study aimed to determine the protective effects of walnut peptides against the neurotoxicity induced by Aβ25-35 in vivo. Briefly, the AD model was induced by injecting Aβ25-35 into bilateral hippocampi of mice. The animals were treated with distilled water or walnut peptides (200, 400 and 800 mg/kg, p.o.) for five consecutive weeks. Spatial learning and memory abilities of mice were investigated by Morris water maze test and step-down avoidance test. To further explore the underlying mechanisms of the neuroprotectivity of walnut peptides, the activities of superoxide dismutase (SOD), glutathione (GSH), acetylcholine esterase (AChE), and the content of malondialdehyde (MDA) as well as the level of nitric oxide (NO) in the hippocampus of mice were measured by spectrophotometric method. In addition, the levels of 8-hydroxy-2'-deoxyguanosine (8-OHdG), tumor necrosis factor-α (TNF-α), interleukin 1β (IL-1β) and IL-6 in the samples were determined using ELISA. The hippocampal expressions of inducible nitric oxide synthase (iNOS) and nuclear factor κB (NF-κB) were evaluated by Western blot analysis. The results showed that walnut peptides supplementation effectively ameliorated the cognitive deficits and memory impairment of mice. Meanwhile, our study also revealed effective restoration of levels of antioxidant enzymes as well as inflammatory mediators with supplementation of walnut peptides (400 or 800 mg/kg). All the above findings suggested that walnut peptides may have a protective effect on AD by reducing inflammatory responses and modulating antioxidant system.

13.
Article in English | WPRIM (Western Pacific) | ID: wpr-250312

ABSTRACT

Alzheimer's disease (AD) is one of the major neurodegenerative disorders of the elderly, which is characterized by the accumulation and deposition of amyloid-beta (Aβ) peptide in human brains. Oxidative stress and neuroinflammation induced by Aβ in brain are increasingly considered to be responsible for the pathogenesis of AD. The present study aimed to determine the protective effects of walnut peptides against the neurotoxicity induced by Aβ25-35 in vivo. Briefly, the AD model was induced by injecting Aβ25-35 into bilateral hippocampi of mice. The animals were treated with distilled water or walnut peptides (200, 400 and 800 mg/kg, p.o.) for five consecutive weeks. Spatial learning and memory abilities of mice were investigated by Morris water maze test and step-down avoidance test. To further explore the underlying mechanisms of the neuroprotectivity of walnut peptides, the activities of superoxide dismutase (SOD), glutathione (GSH), acetylcholine esterase (AChE), and the content of malondialdehyde (MDA) as well as the level of nitric oxide (NO) in the hippocampus of mice were measured by spectrophotometric method. In addition, the levels of 8-hydroxy-2'-deoxyguanosine (8-OHdG), tumor necrosis factor-α (TNF-α), interleukin 1β (IL-1β) and IL-6 in the samples were determined using ELISA. The hippocampal expressions of inducible nitric oxide synthase (iNOS) and nuclear factor κB (NF-κB) were evaluated by Western blot analysis. The results showed that walnut peptides supplementation effectively ameliorated the cognitive deficits and memory impairment of mice. Meanwhile, our study also revealed effective restoration of levels of antioxidant enzymes as well as inflammatory mediators with supplementation of walnut peptides (400 or 800 mg/kg). All the above findings suggested that walnut peptides may have a protective effect on AD by reducing inflammatory responses and modulating antioxidant system.


Subject(s)
Animals , Female , Male , Mice , Acetylcholinesterase , Metabolism , Alzheimer Disease , Drug Therapy , Amyloid beta-Peptides , Toxicity , Glutathione , Metabolism , Hippocampus , Metabolism , Interleukins , Metabolism , Juglans , Chemistry , Malondialdehyde , Metabolism , Maze Learning , Memory Disorders , Drug Therapy , NF-kappa B , Metabolism , Neuroprotective Agents , Pharmacology , Therapeutic Uses , Nitric Oxide , Metabolism , Peptide Fragments , Toxicity , Peptides , Pharmacology , Therapeutic Uses , Plant Extracts , Pharmacology , Therapeutic Uses , Superoxide Dismutase , Metabolism , Tumor Necrosis Factor-alpha , Metabolism
14.
Int J Pharm ; 454(1): 135-42, 2013 Sep 15.
Article in English | MEDLINE | ID: mdl-23871738

ABSTRACT

BACKGROUND: The organic solvent solution immersion method was often used to achieve the loading of the drugs into mesoporous silica, but the drugs that have loaded into the pores of the mesoporous silica would inevitable migrate from the inside to the external surface or near the outside surface during the process of drying. Hence, it often leads to the pores of mesoporous materials not be fully utilized, and results in a low drug loading efficiency and a fast releasing rate. OBJECTIVE: The purpose of this study was to develop a novel drug loading strategy to avoid soluble component migration during the process of drying, then, to prepare poorly water-soluble drug mesoporous silica microparticles with higher drug loading efficiency and longer sustained-release time. METHOD: Ibuprofen was used as model drug. The microparticles were prepared by a novel method based on mesoporous silica and supercritical fluid (SCF) technique. The drug-loaded mesoporous silica microparticles prepared by SCF technique were analyzed by thermogravimetric analysis (TGA), N2 adsorption/desorption, scanning electron microscopy (SEM), powder X-ray diffraction (XRD) and differential scanning calorimetry (DSC). In vitro releasing study was used to evaluate the sustained-release effect of the drug-loaded microparticles. RESULTS: By virtue of the high diffusibility and the high dissolving capacity of the supercritical carbon dioxide (SCF-CO2), the poorly water-soluble drugs, ibuprofen, entered the pores of the mesoporous silica. The amount and the depth of ibuprofen entered the pores of the mesoporous silica by SCF technique were both larger than those by the solution immersion method. It was found that ibuprofen loaded into the mesoporous silica by SCF technique was amorphous and the largest amount of the ibuprofen loaded into the mesoporous silica by SCF technique could reach 386 mg/g (w/w, ibuprofen/SiO2), it was more than that by the solution immersion method. In vitro releasing study showed that the sustained-release effect of ibuprofen in the samples prepared by SCF technique was 50% in 15 min and 90% in 60 min. It was longer than that prepared by the solution immersion method. CONCLUSION: Present study showed that sustained-release poorly water-soluble drug mesoporous silica microparticle based on SCF technique has twofold advantages. One is the larger drug loading amount in internal pores of the mesoporous silica, the other is the longer drug releasing time.


Subject(s)
Chromatography, Supercritical Fluid , Drug Carriers , Ibuprofen/chemistry , Silicon Dioxide/chemistry , Solvents/chemistry , Technology, Pharmaceutical/methods , Water/chemistry , Adsorption , Calorimetry, Differential Scanning , Chemistry, Pharmaceutical , Crystallography, X-Ray , Delayed-Action Preparations , Diffusion , Kinetics , Microscopy, Electron, Scanning , Particle Size , Porosity , Powder Diffraction , Solubility , Thermogravimetry
15.
Article in English | WPRIM (Western Pacific) | ID: wpr-636389

ABSTRACT

A rapid and highly selective liquid chromatography-tandem mass spectrometric (LC-MS/MS) method for the determination of megestrol in human plasma was described using medrysone as internal standard (IS). Blood samples were collected from 20 healthy volunteers after oral administration of 160 mg megestrol acetate dispersible tablets. The analytes were extracted by liquid-liquid extraction procedure and separated on a hanbon lichrospher column with the mobile phase of methanol and water containing 0.1% formic acid and 20 mmol/L ammonium acetate (5:1, v/v). Positive ion electrospray ionization with multiple reaction-monitoring mode (MRM) was employed by monitoring the transitions m/z 385.5-325.4 and m/z 387.5-327.4 for megestrol and medrysone, respectively. Under the isocratic separation conditions, the chromatographic run time was approximately 2.54 min for megestrol and 2.59 min for medrysone. The calibration curve range was from 0.5 to 200.0 ng/mL. The inter-batch and intra-batch precision and accuracy were less than 5.2% relative standard deviation (RSD) and 6.4% relative error (RE). The proposed method was successfully applied in the bioequivalence study of megestrol acetate dispersible tablets.

16.
Article in English | WPRIM (Western Pacific) | ID: wpr-251371

ABSTRACT

A rapid and highly selective liquid chromatography-tandem mass spectrometric (LC-MS/MS) method for the determination of megestrol in human plasma was described using medrysone as internal standard (IS). Blood samples were collected from 20 healthy volunteers after oral administration of 160 mg megestrol acetate dispersible tablets. The analytes were extracted by liquid-liquid extraction procedure and separated on a hanbon lichrospher column with the mobile phase of methanol and water containing 0.1% formic acid and 20 mmol/L ammonium acetate (5:1, v/v). Positive ion electrospray ionization with multiple reaction-monitoring mode (MRM) was employed by monitoring the transitions m/z 385.5-325.4 and m/z 387.5-327.4 for megestrol and medrysone, respectively. Under the isocratic separation conditions, the chromatographic run time was approximately 2.54 min for megestrol and 2.59 min for medrysone. The calibration curve range was from 0.5 to 200.0 ng/mL. The inter-batch and intra-batch precision and accuracy were less than 5.2% relative standard deviation (RSD) and 6.4% relative error (RE). The proposed method was successfully applied in the bioequivalence study of megestrol acetate dispersible tablets.


Subject(s)
Humans , Calibration , Gas Chromatography-Mass Spectrometry , Methods , Reference Standards , Megestrol , Blood , Chemistry , Pharmacokinetics , Therapeutic Equivalency
17.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-336804

ABSTRACT

Channels from the TRP superfamily have essential roles in a wide variety of sensory transductions, especially in mechano-sensation, such as hearing, touch and mechanical pain. TRP channels are also implicated in major channelopathies, including deafness, chronic pain, autosomal dominant polycystic kidney disease (ADPKD) and ventricular hypertrophy. As the leading candidates for mechano-sensitive channels, some TRP channels appear to be mechano-receptor, which can be activated by mechanical forces directly, such as C. elegans TRPN homolog TRP-4; whereas others may act as signal modulators, receiving and amplifying signals indirectly. This review is to introduce the function of TRPs in mechano-sensory transduction and to discuss the underlying molecular mechanisms.


Subject(s)
Animals , Humans , Neural Conduction , Sensation , Physiology , Signal Transduction , Transient Receptor Potential Channels , Metabolism , Physiology
18.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-318304

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the differences of olfactory bulb (OB) volumes between younger and older, male and female, left-side and right-side in healthy middle and old-aged persons by MRI.</p><p><b>METHODS</b>Ninety five healthy middle and old-aged volunteers (male:female = 45:50) were divided into 2 groups, group one included persons aged from 50 to 69, group two included persons elder than 70. The left-side, right-side and both-side volumes of OB, the volumes of brain and the ratio of OB/brain were measured by MRI.</p><p><b>RESULTS</b>(1) The left-side and both-side volumes of OB (x(-) +/- s), the volumes of brain [(39.89 +/- 8.7) mm(3), (81.70 +/- 16.8) mm(3) and (1281.86 +/- 140.2) cm(3)] in 50 - 69 years old group were respectively larger than those in >/= 70 years old group [(34.45 +/- 10.4) mm(3), (72.10 +/- 19.3) mm(3) and (1165.77 +/- 165.3) cm(3)], and the differences reached statistical significance (t were respectively 2.649, 2.449, 3.516, all P < 0.05). There were no significant differences of right-side OB volumes and the ratio of OB/brain between 50 - 69 years old group and >/= 70 years old group (t were respectively 1.904, 0.616, each P > 0.05). (2) The male's OB volumes of left-side, right-side and both-side, the brain volumes and the ratio of OB/brain were respectively larger than females', and the differences reached statistical significance (t were respectively 4.461, 3.630, 4.399, 3.800, 2.400, all P < 0.05). (3) The right-side OB volumes were larger than left-side's and significant differences were found in female group, 50 - 60 years old group and >/= 70 years old group (t were respectively 2.732, 2.117, 3.516, all P < 0.05). There were no significant differences of OB volumes between left-side and right-side in female (t = 2.649, P = 0.110). The ratio of right-side OB/brain were larger than the ratio of left-side's and the differences reached statistical significance (t = 3.183, P = 0.002).</p><p><b>CONCLUSIONS</b>MRI could be used to measure the volume of OB. The older the people, the smaller the OB volumes. There was no influence of age on the ratio OB/brain. The OB volumes of right-side were larger than those of left-side. The OB volumes of male were larger than those of female.</p>


Subject(s)
Humans , Magnetic Resonance Imaging , Olfactory Bulb , Smell
19.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-242998

ABSTRACT

<p><b>OBJECTIVE</b>To study the response of rat bone marrow mesenchymal stem cells (MSCs) to a single period of mechanical strain and expression patterns of transforming growth factor-beta (TGF-beta) and insulin-like growth factor-II (IGF-II) after mechanical stretch.</p><p><b>METHODS</b>Bone marrow MSCs were isolated from SD rats and cultured in vitro. A four-point bending apparatus were used to perform a single period of mechanical strain (2000 microepsilon, 40 min) on MSCs. Cellular proliferation and alkaline phosphatase (ALP) activity of MSCs were examined and gene expression patterns of TGF-beta and IGF-II were detected by SYBR green quantitative real-time RT-PCR.</p><p><b>RESULTS</b>Cell proliferation, ALP activity and expression of TGF-beta and IGF-II were all significantly up-regulated in stretched MSCs when compared with their controls. The mRNA levels of TGF-beta and IGF-II got top increase immediately after mechanical loading and increased about 51.44 and 8.92 folds, respectively, when compared with control cells. Expression of TGF-beta and IGF-II decreased with time and returned to control level at 12 h after mechanical stimulus, despite of a small increase at 6 h.</p><p><b>CONCLUSION</b>The mechanical stretch can promote MSCs proliferation, up-regulate its ALP activity and induce a time-dependent expression increase of TGF-beta and IGF-II which in turn result in osteogenic differentiation of MSCs. Mechanical stimulus is a key stimulator for osteogenic differentiation of MSCs and vital for bone formation in distraction osteogenesis.</p>


Subject(s)
Animals , Rats , Bone Marrow Cells , Cell Differentiation , Cell Proliferation , Insulin-Like Growth Factor II , Mesenchymal Stem Cells , Osteogenesis , Osteogenesis, Distraction , RNA, Messenger , Rats, Sprague-Dawley , Somatomedins , Transforming Growth Factor beta
20.
Article in English | WPRIM (Western Pacific) | ID: wpr-269709

ABSTRACT

<p><b>AIM</b>Understanding the response of mesenchymal stem cells (MSCs) to mechanical strain and their consequent gene expression patterns will broaden our knowledge of the mechanobiology of distraction osteogenesis.</p><p><b>METHODOLOGY</b>In this study, a single period of cyclic mechanical stretch (0.5 Hz, 2,000 microepsilon) was performed on rat bone marrow MSCs. Cellular proliferation and alkaline phosphatase (ALP) activity was examined. The mRNA expression of six bone-related genes (Ets-1, bFGF, IGF-II, TGF-beta, Cbfa1 and ALP) was detected using real-time quantitative RT-PCR.</p><p><b>RESULTS</b>The results showed that mechanical strain can promote MSCs proliferation, increase ALP activity, and up-regulate the expression of these genes. A significant increase in Ets-1 expression was detected immediately after mechanical stimulation, but Cbfa1 expression became elevated later. The temporal expression pattern of ALP coincided perfectly with Cbfa1.</p><p><b>CONCLUSION</b>The results of this study suggest that mechanical strain may act as a stimulator to induce differentiation of MSCs into osteoblasts, and that these bone-related genes may play different roles in the response of MSCs to mechanical stimulation.</p>


Subject(s)
Animals , Rats , Alkaline Phosphatase , Antigens, Surface , Biomechanical Phenomena , Bone Marrow Cells , Physiology , Cell Culture Techniques , Cell Differentiation , Physiology , Cell Proliferation , Core Binding Factor Alpha 1 Subunit , Fibroblast Growth Factor 2 , Insulin-Like Growth Factor II , Mesenchymal Stem Cells , Physiology , Osteoblasts , Physiology , Osteogenesis, Distraction , Pluripotent Stem Cells , Physiology , Proto-Oncogene Protein c-ets-1 , Stress, Mechanical , Transforming Growth Factor beta , Up-Regulation , Physiology
SELECTION OF CITATIONS
SEARCH DETAIL
...