BACKGROUND:Poor implant anchorage in osteoporotic bone impacts its stability and requires the new solutions for the treatment. The augmentation technique with bone cements or bone substitutes is one strategy for the solutions. OBJECTIVE:To evaluate the transient stability of pedicle screw augmented using calcium sulfate cement in osteoporotic vertebral body. METHODS:Fresh calf lumbar vertebrae were selected to measure bone density, and then classified into four groups:the group by pedicle screw in normal vertebral body;the group by pedicle screw augmented using calcium sulfate cement in normal vertebral body;the group by pedicle screw in osteoporotic vertebral body;the group by pedicle screw augmented using calcium sulfate cement in osteoporotic vertebral body. Pedicle screw of equal specification was twisted into the tested pedicle of vertebral arch. The maximum axial screw pul-out strength and the maximum energy required to failure were recorded so as to assess the transient stability of pedicle screw augmented using calcium sulfate cement. RESULTS AND CONCLUSION:The maximum screw pul-out strength and the maximum energy required to failure were significantly less in osteoporotic vertebral body compared with normal vertebral body (P<0.05). The maximum screw pul-out strength and the maximum energy required to failure after augmentation using calcium sulfate cement were significantly increased (P<0.05). The maximum screw pul-out strength and the maximum energy required to failure after augmentation using calcium sulfate cement were identical between normal group and osteoporosis group. These results suggested that calcium sulfate cement could effectively increase the transient stability of pedicle screw. Calcium sulfate cement is effective in augmenting fixation in osteoporotic bone, and has potential in clinical application.

OBJECTIVE: To observe the clinical efficacy of minimally invasive acupotomy-injection technique with targeted three-point in the treatment of frozen shoulder. METHODS: From March 2017 to November 2018, a total of 140 patients with frozen shoulder were randomly divided into observation group and control group. The observation group was made up of 70 patients, including 30 males and 40 females; the mean age was (59.2±11.5) years old; the mean duration of disease was (6.76±4.14) months; the observed patients were treated with acupotomy-injection technique with targeted three-point. There were also 70 patients in the control group, made up of 29 males and 41 females; the mean age was (58.9±11.8) years old; the mean duration of disease was (6.65±3.98) months; the control group was treated with the small needle knife therapy. Before treatment and one month after the treatment, the pain levels of both groups were assessed using the short-form McGill pain questionnaire, and the shoulder function was evaluated using the Constant-Murley Shoulder Outcome Scoring. The clinical efficacy of between groups was compared after treatment, and finally, the improvement rate of pain degree was used to evaluate the therapeutic effect of the patients. RESULTS: The PRI, VAS, PPI and total pain scores of frozen shoulder patients in both groups decreased significantly one month after the treatment compared with those before treatment (<0.01). Compared with the control group, the observation group exhibited a more significant decrease in pain scores (<0.01). Furthermore, the shoulder pain, muscle strength, ADL, ROM and total function scores of frozen shoulder patients in the two groups were significantly improved one month after the treatment compared with those before treatment(<0.01). The inter-group comparison indicated that the pain, ADL, ROM and total function scores were improved obviously in the observation group when compared to those in the control group(<0.01), but no remarkable difference was found between muscle strength score and the control group(>0.05). In addition, the markedly effective rate of pain improvement was 70.0% and 45.7% in the observation group and the control group, respectively, meanwhile, the corresponding total effective rate was 97.1% and 84.3%, respectively. CONCLUSIONS The application of acupotomy-injection technique with targeted three-point in the treatment of frozen shoulder shows definite efficacy, easy operation, little pain and high safety. Therefore, it is an ideal method for minimally invasive treatment.
Acupuncture Therapy ; Aged ; Bursitis ; Female ; Humans ; Male ; Middle Aged ; Shoulder ; Shoulder Joint ; Shoulder Pain ; Treatment Outcome

AIMTo establish the fundamentals for the design of scutellarin prodrug and formulation with feasible physicochemical and biopharmaceutical properties by esterifying scutellarin, an active component with poor absorption extracted from Erigeron breviscapus of Chinese medicine.

METHODSWith the method of salifying followed by esterifying, ethyl and benzyl ester of scutellarin were synthesized. Glycolamide ester of scutellarin was also synthesized with an improved method. Their structures were confirmed by MS and 1H NMR. The solubility and partition coefficient of the prodrugs were determined and their degradations were investigated in various buffers and in human plasma. The emulsion and cyclodextrin complex of glycolamide ester were prepared and the protection of the ester from degradation was compared in the intestinal tract contents. Furthermore, the degradation of glycolamide ester in the homogenates of various intestinal segments was studied. Results Three prodrugs were synthesized successfully and their structures were confirmed. Glycolamide ester of scutellarin showed better stability in the aqueous solution (t(1/2) approximately =16 d, pH 4.2) and the shortest half-life in the human serum (t(1/2) approximately =7 min). Compared with scutellarin, the solubility of glycolamide ester was increased about ten times in pH 4.0 buffer, and about thirty five times in water. Partition coefficient of the glycolamide ester increased significantly from -2.56 to 1.48. However, the ester degradation in the homogenates of intestinal mucus would be an obstacle for its absorption. The degradation rates were in the order duodenum > ileum > or = jejunum > colon. The emulsion showed a better protection of glycolamide ester from the degradation than cyclodextrin complex.

CONCLUSIONGlycolamide ester of scutellarin shows better physicochemical properties than ethyl and benzyl eater of scutellarin, but its stability in intestinal tract needs to be improved. The emulsion or / and colon-targeted delivery may be selected as one of strategies to decrease the presystemic degradation.

Animals ; Apigenin ; chemistry ; isolation & purification ; pharmacokinetics ; Emulsions ; Erigeron ; chemistry ; Esters ; Flavones ; chemical synthesis ; chemistry ; pharmacokinetics ; Glucuronates ; chemistry ; isolation & purification ; pharmacokinetics ; Glucuronides ; chemical synthesis ; chemistry ; pharmacokinetics ; Humans ; Intestinal Mucosa ; metabolism ; Intestines ; metabolism ; Male ; Plants, Medicinal ; chemistry ; Prodrugs ; chemical synthesis ; chemistry ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo observe clinical curative effect of cake-separated moxibustion on impaired glucose regulation (IGR) and explore its action mechanism.

METHODSSixty cases were randomly divided into a simple lifestyle intervention group (control group) and a cake-separated moxibustion combined with lifestyle intervention group (observation group), 30 cases in each one. The control group was treated with lifestyle intervention. Based on lifestyle intervention, cake-separated moxibustion at Pishu (BL 20), Weishu (BL 21) and Yishu (EX-B 3) was applied to the observation group. Fast plasma glucose (FPG), two hours plasma glucose after oral glucose tolerance test (OGTT2hPG), fasting insulin (FINS), homa insulin resistance index (HOMA-IR), blood lipid, body mass index (BMI) and waist circumference (WC) were observed in the two groups before and after treatment.

RESULTSAfter treatment, the OGTT2hPG and FPG were both decreased significantly (both P<0.05) in the two groups, compared between the two groups, the differences of FPG [(0.41 +/- 0.42) mmol/L vs (0.05 +/- 0.08)mmol/L] and OGTT2hPG [(0.85 +/- 0.53)mmol/L vs (0.17 +/- 0.19)mmol/L] were both statistically significant. There were no significant changes in FINS, HOMA-IR, blood lipid, BMI and WC in the control group before and after treatment (all P>0.05), but FINS, HOMA-IR levels, triglycerides (TG), total cholest-erol (TC), low density lipoprotein (LDL-C), BMI and WC in the observation group were decreased obviously after treatment (all P<0.05), which had statistical differences between the two groups (all P<0.05).

CONCLUSIONThe cake-separated moxibustion combined with lifestyle intervention can obviously control blood glucose levels, improve insulin resistance and blood lipid levels, decrease BMI and WC.

Adult ; Aged ; Female ; Glucose ; metabolism ; Glucose Intolerance ; metabolism ; physiopathology ; therapy ; Humans ; Insulin ; Male ; Middle Aged ; Moxibustion ; Waist Circumference

The target compounds were prepared from 5-aminobenzimidazolone by two steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The AChE inhibitory activity of compound 4d is the best of them, and its IC50 value is equal to 7.2 μmol·L(-1), which is better than that of rivastigmine; moreover the 4d had no inhibitory activities to BuChE. Therefore, the inhibitory activities of 5-aminobenzimidazolone derivatives to acetylcholinesterase are worth further researching.
Acetylcholinesterase ; metabolism ; Benzimidazoles ; chemical synthesis ; chemistry ; Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; Drug Design ; Phenylcarbamates ; chemistry ; Rivastigmine ; Structure-Activity Relationship

In this paper, fourteen new L-proline derivatives were designed and synthesized, and their acetlcholinesterase (AChE) inhibitory activities were also investigated in vitro. New L-proline derivatives were prepared from substituted 2-bromo-1-acetophenones through four-step reaction; and their bioactivities as AChE inhibitors were measured by Ellman spectrophotometry. The results showed that the target compounds had a certain AChE inhibitory activity to in vitro. The bioactivity of compound 8b was the best of them, and its IC50 value was 5.45 µmol.L-1, which was better than that of rivastigmine. So the acetylcholinesterase inhibitory activities of new L-proline derivatives were worth to be further studied.
Acetylcholinesterase ; Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; Drug Design ; Proline ; analogs & derivatives ; Rivastigmine ; chemistry ; Structure-Activity Relationship

The peeled stem of Syringa pinnatifolia is a Mongolia folk medicine, mainly distributed in Helan mountain, inner Mongolia and Ningxia provinces of China. It has been used for the treatment of cardiopalmus, angina pectoris, and cardiopulmonary diseases for a long history. Contemporary research revealed the presence of major lignans, sesquitepenes, and essential oils, and showed myocardial ischemia related diseases. This review summarizes the plant origins, taxonomic disputes, phytochemical and pharmacological research progress, hopefully to provide reference for full medicinal utilization, clarification of biological effective substance, and drug development.
Animals ; Drug Therapy ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Humans ; Medicine, Mongolian Traditional ; Molecular Structure ; Syringa ; chemistry

Adenocarcinoma ; metabolism ; pathology ; surgery ; Adenocarcinoma, Clear Cell ; metabolism ; pathology ; Adult ; CA-125 Antigen ; metabolism ; Carcinoembryonic Antigen ; metabolism ; Cervical Intraepithelial Neoplasia ; metabolism ; pathology ; surgery ; Cystadenocarcinoma, Serous ; metabolism ; pathology ; Diagnosis, Differential ; Female ; Follow-Up Studies ; Humans ; Hysterectomy ; Ki-67 Antigen ; metabolism ; Lymph Node Excision ; Membrane Proteins ; metabolism ; Neoplasm Invasiveness ; Uterine Cervical Neoplasms ; metabolism ; pathology ; surgery

OBJECTIVETo observe the effect of bear bile powder (BBP) on the STAT3 pathway and its downstream target genes of nude mice hepatocellular carcinoma (HCC) xenograft, and to explore its mechanism for treating HCC.

METHODSThe subcutaneous xenograft model was established using HepG2 cells. When the subcutaneous transplanted tumor was formed, naked mice were randomly divided into two groups, the BBP group and the control group. Mice in the BBP group were administered with BBP by gastrogavage, once daily for 3 consecutive weeks, while mice in the control group were administered with normal saline by gastrogavage, once daily for 3 consecutive weeks. The body weight and the tumor volume were measured once per week. By the end of medication, the tumor weight was weighed and the tumor inhibition ratio calculated. The apoptosis of the tumor tissue was detected by TdT-mediated dUTP nick end labeling (TUNEL). The expression of Bcl2-associated X protein (Bax), B cell lymphoma/eukemina-2 (Bcl-2), cyclin-dependent protein kinase (CDK4), cyclinD1 were detected by reverse transcription-polymerase chain reaction (RT-PCR). The protein expression levels of signal transducers and transcription activators 3 (p-STAT3), proliferating cell nuclear antigen (PCNA), Bax, Bcl-2, CDK4, and cyclinD1 were determined by immunohistochemistry.

RESULTSBBP could inhibit the tumor volume and tumor weight, showing statistical difference when compared with the control group (P < 0.01). Results of TUNEL showed that BBP could significantly induce the apoptosis of hepatoma carcinoma cells. Results of RT-PCR showed that BBP could up-regulate the expression of Bax and down-regulate mRNA expression of Bcl-2, CDK4, and cyclinD1. Immunohistochemical results showed that BBP could up-regulate the expression of Bax and inhibit the protein expression of p-STAT3, PCNA, Bcl-2, CDK4, and cyclinD1.

CONCLUSIONBBP could induce the apoptosis of hepatoma carcinoma cells and inhibit their proliferation by regulating STAT3 pathway.

Animals ; Bile ; Carcinoma, Hepatocellular ; metabolism ; pathology ; Cyclin D1 ; metabolism ; Cyclin-Dependent Kinase 4 ; metabolism ; Drugs, Chinese Herbal ; pharmacology ; Hep G2 Cells ; Humans ; Liver Neoplasms ; metabolism ; pathology ; Male ; Mice ; Mice, Inbred BALB C ; Mice, Nude ; Proto-Oncogene Proteins c-bcl-2 ; metabolism ; STAT3 Transcription Factor ; metabolism ; Signal Transduction ; Ursidae ; Xenograft Model Antitumor Assays ; bcl-2-Associated X Protein ; metabolism

OBJECTIVETo establish a new method for simultaneous determination of shanzhiside methyl ester, chlorogenic acid, 8-O-acetyl shanzhiside methylester, forsythiaside B, rutin, acteoside and galuteolin in Lamiophlomis rotata.

METHODSeparation was performed on a Welchrom-C18 chromatographic column with acetonitrile-0.1% orthophosphoric acid as mobile phasewith gradient elution. The flow rate was 1.0 mL x min(-1). The column temperature was 30 degrees C, and the detection wavelength was set at 238 nm, 330 nm and 350 nm.

RESULTThe seven compounds were well separated with good linear correlations. The mean recoveries of seven compounds were 96.47%-102.2% (RSD 0.70%-2.2%).

CONCLUSIONThere were good correlations among the seven compounds in the samples of aerial parts. The mean sum of shanzhiside methyl ester and 8-O-acetyl shanzhiside methylester in samples of aerial parts is 1.44%. The aerial parts have more kinds of composition and with higher content than that of underground parts in L. rotata, which was reasonable for the resonable use of the aerial part as medicinal part. The method was simple, repeatable and stable, which could be used for identification and quality evaluation of L. rotata.

Chlorogenic Acid ; chemistry ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; chemistry ; Glucosides ; chemistry ; Glycosides ; chemistry ; Lamiaceae ; chemistry ; Methyl Ethers ; chemistry ; Phenols ; chemistry ; Plant Components, Aerial ; chemistry ; Plants, Medicinal ; chemistry ; Pyrans ; chemistry ; Rutin ; chemistry