Currently, the herbal prescription therapy for corresponding constitutional diseases is a common constitution regulating method. This method has an obvious effect in treating and regulating constitution-related diseases. However, for people who do not have disease, they prefer to regulate constitution with dietary therapy. In this paper, the researchers came up with a design method of constitution regulating and healthcare foods based on medicinal property combination mode of clinical empirical formulas. With "Yupinfeng San", a common formula for Qi-insufficiency constitution and specific endowment constitution, as the example for constitution regulating and healthcare foods, the researchers proved the effectiveness and rationality of healthcare food schemes in terms of the efficacy of single herb and the modern pharmacological study.
Diet ; Diet Therapy ; Humans ; Plants, Medicinal ; chemistry ; metabolism ; Prescriptions

OBJECTIVETo study the antiproliferation effect on HepG2 cells and its underlying mechanism of the active chemical composition of the Viburnum Odoratissimum.

METHODS3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) reduction assay and trypan blue dye exclusion assay were used to assess the effect of vibsane-type diterpenoids on the proliferation of various tumor cells. Alterations in cell cycle and apoptosis were determined by flowcytometry. The enzymatic activity of caspase-3/7 was measured by Apo-ONE homogeneous Caspase-3/7 Assay kit.

RESULTSCompound 1 #, a vibsane-type diterpenoid, was found to significantly inhibit the growth of HepG2 cells by anticancer proliferation activity screening. It was demonstrated that the modified groups on side chain coupled to C11 site affected the cell growth-inhibition activity of compounds by structure-activity analysis. In addition, HepG2 cell line was most sensitive to compound 1 #, which induced growth arrest of HepG2 cells in a dose- and time-dependent manner. Study on the mechanisms underlying these effects indicated that compound 1 # induced significant G0/G1 phase arrest of HepG2 cells in a time- and concentration-dependent manner. Meanwhile, It was found that higher concentrations of compound (5-10 micromol/L) caused evident increase in the unmber of apoptotic cells and dose-dependent activation of caspase-3/7.

CONCLUSIONVibsane-type diterpenoids could significantly inhibit the growth of HCC HepG2 cells. Induction of cell cycle arrest and apoptosis may play important roles in their anticancer effects.

Apoptosis ; drug effects ; Cell Cycle Checkpoints ; drug effects ; Cell Proliferation ; drug effects ; Diterpenes ; pharmacology ; Hep G2 Cells ; Humans ; Viburnum ; chemistry

The aim of this study is to explore the tissue distribution of PEGylated puerarin in acute myocardial ischemia model rats. Healthy male SD rats were randomly divided into two groups (30 each). Both were given PEGylated puerarin at a dose of 488 mg x kg(-1). After 5 min of medication, one group was normal rats, another group with acute myocardial ischemia was established by peritoneal injection of 50 mg x kg(-1) isoprenaline. After administration, the animals were executed at 30, 60, 90, 120, 150 and 180 min, then heart, liver, spleen, lung, kidney were extracted. The content of puerarin in organ tissue was determined by HPLC. The results showed that the AUC of tissue distribution of PEGylated puerarin in normal rats was liver > kidney > heart ≈ spleen > lung > brain. While the AUC of tissue distribution of PEGylated puerarin in acute myocardial ischemia model rats was liver ≈ heart > kidney > lung ≈ spleen > brain. AUC(heart) of PEGylated puerarin in acute myocardial ischemia model rats was 1.7 times than that of the normal rats, and there was significant difference (P < 0.05). Thus, PEGylated puerarin had a good heart-targeting property in early myocardial infarction area, drugs could accumulate in the ischemic myocardium. It provided important information for further study and clinic use of PEGylated puerarin.
Animals ; Brain ; metabolism ; Isoflavones ; pharmacokinetics ; Kidney ; metabolism ; Liver ; metabolism ; Lung ; metabolism ; Male ; Myocardial Ischemia ; metabolism ; Myocardium ; metabolism ; Rats ; Rats, Sprague-Dawley ; Spleen ; metabolism ; Tissue Distribution

OBJECTIVETo study lymph node micrometastases (LNMM), expression of nm23-H(1), MMP(9), TIMP(2) proteins, and their relationship and clinical significance in patients with stage Dukes B colorectal cancer.

METHODSThirty patients with stage Dukes B colorectal cancer were studied. LNMM in these patients was detected by immunohistochemical anti-cytokeratin 20 (CK20) staining. The expression of nm23-H(1), MMP(9) and TIMP(2) proteins in primary tumors was examined by Strept-avidin-biotin complex method. Clinical-pathological data and survival of each patient were recorded and analyzed.

RESULTS(1) The positive dyeing of CK20 was observed in 26.7% for cases and in 7.8% for lymph nodes of 30 patients with stage Dukes B colorectal cancer. (2) Different expression of nm23-H(1) and MMP(9) proteins in the patients between stage Dukes B and stage Dukes CD was observed (P < 0.05). The decreased nm23-H(1) expression, and/or the increased MMP(9) expression in primary stage Dukes B tumors were significantly associated with LNMM (P < 0.05). Sensitivity and specificity for detection of LNMM by using nm23-H(1) or MMP(9) were respectively 62.5% and 81.8% or 75.0% and 69.8%. If by combining nm23-H(1) with MMP(9), specificity for detection of LNMM became 90.9%. The expression of TIMP(2) protein was not related with stage Dukes and LNMM. (3) The percent of tumor recurrence and/or metastasis for the stage Dukes B patients with LNMM was significantly higher than that for the patients without LNMM (P < 0.05), but the survival percent for the patients with LNMM was significantly lower than that for the patients without LNMM. The outcome for the patients with nm23-H(1) (-) LNMM (+) or MMP(9) (+) LNMM (+) was significantly worse than that for patients with nm23-H(1) (+) LNMM (-) or MMP(9) (+) LNMM (-) (P < 0.05).

CONCLUSIONSLNMM is detected by immunohistochemical anti-CK20 staining. The expression of nm23-H(1) and MMP(9) in primary stage Dukes B tumors was significantly associated with LNMM. The outcome in the LNMM patients with nm23-H(1) (-) and/or MMP(9) (+) were worse. Combining examination of CK20 for lymph nodes with expression of nm23-H(1) and MMP(9) for primary tumors is of important clinical significance for staging of Dukes, selection of adjuvant treatment and evaluation of prognosis in patients with colorectal cancer.

Colorectal Neoplasms ; metabolism ; pathology ; therapy ; Humans ; Keratins ; metabolism ; Lymph Nodes ; pathology ; Lymphatic Metastasis ; Matrix Metalloproteinase 9 ; metabolism ; NM23 Nucleoside Diphosphate Kinases ; Neoplasm Staging ; Nucleoside-Diphosphate Kinase ; metabolism ; Prognosis ; Tissue Inhibitor of Metalloproteinases ; metabolism

Objective To evaluate the clinical effect of ultrasonic location botulinum toxin A (BTX-A)injection for lower limbs spasticity in children with cerebral palsy.Methods Seventy-five children with lower limbs spasticity resulting from cerebral palsy were divided into injection group(n =37) and control group(n =38).Ultrasonography was used to located the injection of BTX-A into the spastic muscles of the legs in injection group.Then rehabilitation training was received the day after the injection.For all patients,muscle spasticity and gross motor function measure were evaluated before treatment and in the second week,the first,third and sixth month treatment using the Modified Ashworth Scale(MAS) and the Gross Motor Function Measure(GMFM) assessment.Results In the second week,the first,third and the sixth month of treatment,the improvement of muscle spasticity and GMFM in the injection group were significantly better than before(all P ＜ 0.01).And the improvement of muscle spasticity were the greatest in the second week and the first month of the injection.The average therapeutic effect in the injection group was significantly better than that in the control group(P ＜0.05).There was no statistical difference between the evaluation score of the third month and that of the sixth month for injection group.The BTX-A injection had time limit and could be reinject after 6 months.Conclusions The ultrasound located BTX-A injection to treat lower limbs spasticity in cerebral palsy has the advantages of accurate localization,safety,good child patient compliance and more effective than only rehabilitation treatment.

Searching for new antidiabetic lead compound, 4-(1-aryl-3-oxo-5-phenylpentylamino) benzenesulfonamides were designed and synthesized directly by three component one-pot condensation of 4-phenyl-2-butanone and sulfanilamide with some aromatic aldehydes at an yield of 23%-97%. The chemical structures of the twelve new Mannich bases were confirmed by 1H NMR, 13C NMR, FTIR, ESI-MS and HR-MS. The screening results of antidiabetic activity indicated that most of these title compounds possess alpha-glucosidase inhibitory activity, among which compound le is the strongest one. And compound 11 possesses good peroxisome proliferator-activated receptor response element (PPRE) agonist activity. The structure-activity relationship of these new beta-amino ketones containing benzenesulfonamide unit was also discussed preliminarily.
Drug Design ; Glycoside Hydrolase Inhibitors ; Hypoglycemic Agents ; chemical synthesis ; chemistry ; pharmacology ; Peroxisome Proliferator-Activated Receptors ; agonists ; Structure-Activity Relationship ; Sulfanilamides ; chemistry ; Sulfonamides ; chemical synthesis ; chemistry ; pharmacology ; alpha-Glucosidases ; metabolism

OBJECTIVETo analyses the clinical application of thoracodorsal artery perforator flaps (TAP).

METHODSWe used free or pedicled TAP flaps in 7 patients from Aug 2006 to April 2007, The age ranged from 7 to 42 years old, the perforator arteries was detected and labeled with a hand held Doppler flowmeter, the size of flaps ranged from 6 cm x 9 cm - 12 cm x 16 cm, the flaps designed with perforator artery included, all the flaps are based on the first perforator artery.

RESULTSAll the flaps survived well, no complication occurred with lowest donor site morbidity.

CONCLUSIONSThe thoracodorsal artery flap with latissimus dorsal muscle saved is a thin and reliable flaps with robust of blood supply, the flap can reduce significantly donor site morbidity and is a good choice for reconstructive surgery.

Adolescent ; Adult ; Back ; blood supply ; Child ; Female ; Humans ; Male ; Reconstructive Surgical Procedures ; methods ; Surgical Flaps ; blood supply ; Thoracic Arteries ; transplantation ; Young Adult

Diabetes mellitus is a common metabolic disease with a high and growing prevalence affecting 4% of the population worldwide, the development of safe and effective therapeutic drug is the major thrust for chemists and pharmacists. To search for active antidiabetic lead compound, we designed and synthesized some novel beta-amino ketone derivatives containing sulfamethoxazole moiety directly through Mannich reaction of sulfamethoxazole, 4-bromoacetophenone and some aromatic aldehydes catalyzed by concentrated hydogen chloride or iodine in the solution of ethanol at 24-40 degrees C with convenient operation, mild reaction condition and satisfactory yield (32%-90%). Their chemical structures were characterized by 1H NMR, 13C NMR, MS and HR-MS. Biological activity tests showed that, in the range of low concentration (5-10 microg x mL(-1)), these title compounds to a certain degree possess protein tyrosine phosphatase 1B (PTP1B) inhibitory activity and a-glucosidase inhibitory activity, moreover, some could activate peroxisome proliferator-activated receptor response element (PPRE) moderately. The PPRE agonist activities of seven compounds are almost 40% of that of Pioglitazone (the positive control), compound 12 shows the strongest activity (66.35%) among them. Thus, it was found that some of 4-(3-(4-bromophenyl)-3-oxo-1-arylpropylamino)-N-(5-methyl-isoxazol-3-yl) benzenesulfonamide containing sulfamethoxazole moiety exhibited antidiabetic activity for the first time.
Glycoside Hydrolase Inhibitors ; Humans ; Hypoglycemic Agents ; chemical synthesis ; chemistry ; pharmacology ; Molecular Structure ; Oxazoles ; chemistry ; Peroxisome Proliferator-Activated Receptors ; agonists ; Protein Tyrosine Phosphatase, Non-Receptor Type 1 ; antagonists & inhibitors ; Response Elements ; Structure-Activity Relationship ; Sulfonamides ; chemistry ; Thiazolidinediones ; pharmacology

AIM To establish a UPLC-MS/MS method for the simultaneous content determination of ellagic acid,gallic acid,dehydrodiisoeugenol,methyleugenol,agarotetrol,elemicin,chlorogenic acid,geniposide,rutin,ferulic acid,hydroysafflor-yellow A,deoxycholic acid,cholic acid,borneol and taurine in Zhuriheng Dropping Pills.METHODS The analysis of 50%methanol solution of this drug was performed on a 30℃thermostatic Thermo C18 column(2.1 mm×100 mm,1.9 μm),with the mobile phase comprising of acetonitrile-0.1%formic acid(containing 10 mmol/L ammonium acetate)flowing at 0.3 mL/min in a gradient elution manner,and electron spray ionization source was adopted in positive and negative ion scanning.RESULTS Fifteen constituents showed good linear relationships within their own ranges(R2>0.990 0),whose average recoveries were 75.91%-112.13%with the RSDs of 3.06%-10.66%.CONCLUSION This simple,sensitive and efficient method can be used for the quality control of Zhuriheng Dropping Pills.

Adolescent ; Busulfan ; therapeutic use ; Child ; Child, Preschool ; Cyclophosphamide ; therapeutic use ; Cyclosporine ; therapeutic use ; Female ; Hematopoietic Stem Cell Transplantation ; methods ; Humans ; Infant ; Leukemia ; drug therapy ; mortality ; therapy ; Leukemia, Myeloid, Acute ; drug therapy ; mortality ; therapy ; Male ; Mycophenolic Acid ; therapeutic use ; Precursor Cell Lymphoblastic Leukemia-Lymphoma ; drug therapy ; mortality ; therapy ; Retrospective Studies ; Treatment Outcome