Referring to the rapid developed life science and the higher requirements for the approval of innovative Chinese drugs in recent years, this paper described systematically the discovery, research and development (R&D) approaches for the innovative Chinese drugs under the new situation from the following five aspects, i. e., active components discovered from TCMs, the discovery of effective fractions of TCMs and their formulae, the R&D of TCM innovative drugs based on famous classic prescriptions and famous Chinese patent drugs, and the transformation of clinical effective prescriptions, on the basis of analysing the advantages of innovative drugs derived from natural products based on TCM theories and the problems existed in current R&D of new TCM drugs. Moreover, five suggestions are also given for the rapid development of TCM innovative drugs in China. All these will provide reference for the R&D of TCM innovative drugs.
China ; Drug Discovery ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Humans ; Medicine, Chinese Traditional ; trends ; Research

Objective:To make a preliminary application of the assessment system for cancer pain management and find insuffi-ciency in the clinical practice of cancer pain diagnosis and treatment. Methods:Data from 41 doctor questionnaires, 43 nurse question-naires, 50 patient questionnaires, and 12 ward questionnaires from the tumor departments of 3 hospitals were analyzed, and the insuffi-ciency in cancer pain management was determined. The wards in the tumor and non-tumor departments related to oncology were as-sessed using rank test, and differences between the 2 wards were investigated. Results:The average scores of doctor, nurse, and wards were 85.41±5.93, 88.46±5.09 and 83.75±3.11, respectively, whereas patient score was 68.67±7.14. To further analyze the patient subsys-tem by converting into a hundred-mark system, the effectiveness and safety scores for the pain management was 81.69±7.71. However, patients' opinion score on pain treatment was only 55.78±11.37. The score of tumor departments was 82.22±2.03, whereas related non-tumor departments had a score of 39.27 ± 3.58. Wilcoxon W value was at 120.0 with P<0.01 after rank test. Conclusion:Education on patients' opinion on cancer pain management should be promoted in the tumor wards, and continuous education on cancer pain diagno-sis and treatment is needed in the non-tumor departments relative to oncology.

The high performance liquid chromatography-fluorescence micelle assay (HPLC-FMA) method for the content determination of polysorbate 80 in monoclonal antibody drugs was validated to study its applicability and transferability between various laboratories, and the feasibility to be included in the Chinese Pharmacopoeia. Both J.T. Baker and Nanjing Well-sourced polysorbate 80 was used in the collaborative validation of polysorbate 80 content analysis in seven different laboratories. The results show that when the protein concentration was no more than 20 mg·mL^-1 and the concentration of polysorbate 80 ranged from 0.05 to 0.5 mg·mL^-1, the method had good specificity. The recovery rates of the spiked samples ranged from 92.20% to 117.70% for J.T.Baker and from 93.90% to 117.20% for Nanjing Well. The intra-laboratory precision (%RSD) was less than 4.30% for J.T. Baker, and less than 2.60% for Nanjing Well, while the overall precision was less than 5.45% for J.T. Baker, and less than 6.70% for Nanjing Well. The linear correlation coefficient was more than 0.98 for J.T. Baker and more than 0.99 for Nanjing Well. The results of the collaborative validation prove that the HPLC-FMA method has good accuracy, precision, linearity, and specificity, and could be used for release control analysis of polysorbate 80 content in monoclonal antibodies across different laboratories.

A new steroidal ester, beta-rosaterol palmitate (1) along with ten known compounds, uvaol(2), 3-epi-ursolic acid (3), 2alpha, 3beta, 24-trihydroxyolean-12-en-28-oic acid (4), 2alpha, 3alpha, 24-trihydroxyurs-12-en-28-oic acid (5), 2alpha, 3alpha, 24-trihydroxyolean-12-en-28-oic acid (6), 2alpha, 3alpha, 24-trihydroxyolean-12-en-28-oic acid-28-O-beta-D-glucopyranosyl ester (7), (Z)-9-hexadecenoic acid (8), octacosyl alcohol (9), beta-sitosterol (10) and beta-daucosterol (11), has been isolated from the stems and leaves of Vitex trifolia. Their structures were elucidated using a combination of 1D and 2D NMR techniques (COSY, HMQC, and HMBC)and HR-ESI-MS analyses. Compounds 2-7 were isolated from this plant for the first time.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Vitex ; chemistry

Objective To evaluate early and dynamic changes of the left ventricular systolic function of patients with septic shock by two-dimensional speckle tracking imaging (2D-STI), and to provide guidance for treatment and prognosis.Methods Fifty-eight septic shock patients admitted to intensive care unit (ICU) of Subei People's Hospital from January 2016 to April 2017 were enrolled. The septic shock patients were given early fluid resuscitation. The left ventricular end-diastolic volume (LVEDV), left ventricular end-systolic volume (LVESV), left ventricular ejection fraction (LVEF), early diastolic mitral flow velocity/early diastolic mitral annular peak velocity (E/Em) were obtained by conventional echocardiography, and the left ventricular global longitudinal strain (GLS), global circumferential strain (GCS), global radial strain (GRS) were obtained by 2D-STI before fluid resuscitation and 1, 3, 7, 14 days after fluid resuscitation. According to the 28-day survival, the septic shock patients were divided into survival group (38 cases) and death group (20 cases). Thirty normal subjects with age and sex matched were selected as control group.Results① Compared with control group, heart rate (HR) and LVESV were increased [HR (bpm): 92.71±12.51 vs. 73.07±5.52, LVESV (mL): 42.50±7.89 vs. 38.73±4.23, bothP < 0.05], while LVEF, GLS, GCS were decreased [LVEF: 0.57±0.06 vs. 0.61±0.03, GLS: (-17.72±1.35)% vs. (-22.07±1.95)%, GCS: (-17.08±1.49)% vs. (-22.98±1.97)%] in septic shock group (allP < 0.01). ② Compared with the data before fluid resuscitation, heart rate was declined (bpm: 87.83±11.50vs. 92.71±12.51,P < 0.01), while LVEDV and LVEF were increased [LVEDV (mL): 102.32±9.23 vs. 99.24±8.86, LVEF: 0.59±0.05 vs. 0.56±0.06] in patients of the septic shock after fluid resuscitation (allP <0.01). ③ With the extension of treatment time, HR, LVEDV, LVESV, E/Em were increased gradually, and LVEF, GLS, GCS, GRS were decreased gradually in dead patients. In septic shock patients, compared with survival group, GCS was significantly different on day 1 [(-15.98±1.41)% vs. (-17.66±1.22)%,P < 0.05], HR, LVEDV, LVESV, GLS were significantly different on the 3rd day [HR (bpm): 104.60±10.94 vs. 88.71±5.06, LVEDV (mL): 109.69±10.00 vs. 103.99±5.74, LVESV (mL): 47.78±7.21 vs. 42.29±5.13, GLS: (-14.44±0.92)% vs. (-16.36±1.00)%, allP < 0.05], LVEF, GRS were significantly different on the 7th day [LVEF: 0.47±0.07 vs. 0.58±0.04, GRS: (28.27±3.23)% vs. (31.48±3.12)%, bothP < 0.05], and E/Em was significantly different on the 14th day (12.81±1.56 vs. 10.61±1.27) in dead group (P < 0.05).Conclusions Our study demonstrates myocardial dysfunction at the early phase in septic shock patients, and 2D-STI GCS can be more sensitive than the conventional echocardiography to determine prognosis. 2D-STI GCS, GLS, GRS were not volume-load dependent parameter. Low levels of GLS, GCS might suggest a poor prognosis.

Objective To study the effects of electromagnetic field (EMF) exposure on osteoporosis in ovariectomized mice. Methods Sixty 8-week-old female Kunming mice were divided into four groups at random: a sham operation group (group A), an ovariectomized group (group B), an EMF and ovariectomized group (group C) and a nilestriol and ovariectomized group (group D). Bilateral ovariectomies were performed on all mice except those in group A. The mice of group C were exposured to a 15 Hz, 1.0 mT electromagnetic field. The mice of group D were given at nilestriol 1.5 mg/kg/week. The bone mineral density (BMD) of the lumbar vertebrae was measured before the mice were sacrificed at the 12th week. Blood specimens were collected every two weeks to measure the ac-tivity of alkaline phosphatase (ALP) and the concentration of bone gamma-carboxyglutamic-acid-containing proteins (BGP), calcium and estradiol in the serum. Histological sections were taken to examine and analyze the changes in bone trabeculae in the lumbar vertebrae after 6 and 12 weeks. Results EMF at 15 Hz and 1.0 mT intensity signifi-cantly increased the activity of ALP and the concentrations of BGP and calcium in the serum. In addition, the absorp-tion of bone trabeculae in the lumbar vertebrae was significantly restrained. Conclusions EMF at 15 Hz and 1.0 mT can restrain the development of osteoporosis in ovariectomized mice.

Objective To study the effects of an electromagnetic field (EMF) on the expression of fibro-blast growth factor (FGF-2) and it' s receptor (FGFR-2) mRNA in rat bone marrow mesenchymal stem cells (BMSCs) in vitro. Methods Rat BMSCs were isolated and cultured in vitro. The subcultured cells were divided into different groups to be EMF stimulated at 1.0 mT. The expression of FGF-2 and FGFR-2 mRNA were detected by reverse transcription-polymerase chain reaction (RT-PCR). Results Different frequencies and durations of 1.0 mT EMF exposure induced FGF-2 and FGFR-2 mRNA expression in comparison to blank controls. The expression of FGF-2 mRNA reached a peak after stimulation at 15 Hz for 10 min, 50 Hz for 60 min and 75 Hz for 30 min. And the expression of FGFR-2 mRNA reached a peak after 30 minutes at all frequencies. At 1.0 mT with 30 min exposure, the expression of FGF-2 mRNA peaked after 50 Hz stimulation, and the expression of FGFR-2 mRNA peaked after stimulation at 75 Hz. Conclusions Moderate EMF stimulation can significantly increase the expression of FGF-2 and FGFR-2 mRNA in rat BMSCs in vitro.

OBJECTIVETo evaluate biomechanical properties in different methods of internal fixation combined with distal tibiofibular syndesmosis injury, in order to provide a theoretical basis for clinical choice.

METHODSSix lower limbs specimens were collected and divided into 5 groups, including normal group, distal tibiofibular syndesmosis injury (injury group), 3 cortexes group, 4 cortexes group and hook-plate fixation group. Neutral position, plantar flexion position (30°), dorsiflexion (20°) supination external rotation position of foot movement were simulated on universal materials tester. Strength, stiffness and stability of ankle joint in 4 kinds of motion conditions were measured.

RESULTSThere was significant differences in strength and stiffness of ankle joint between injury group and normal group in 4 different kinds of motion conditions (P<0.05). Strength and stiffness of ankle joint in 3 cortexes group, 4 cortexes group and hook-plate fixation group were improved obviously in 4 different kinds of motion conditions, and biomechanical indexes were recovered normally or better than normal group. Stiffness of the three fixation groups were better than normal group,but there was no significant differences among three groups (P > 0.05), while stiffness of hook-plate fixation group was closed to normal group.

CONCLUSIONFor distal tibiofibular syndesmosis injury, 1 screw with 3 cortexes, 4 cortexes and hook-plate had a positive impact on strength, stiffness and stability of distal tibiofibular syndesmosis injury stress,and could restore the normal stabllity of ankle joint after reconstruction. While fixing by screw fixation would limit the rototary motion of ankle joint,ankle mortise could not adapt to changes of talus bone, thus induces screw breakage and traumatic arthritis. Hook-plate fixation is more suitable than 3 cortexes or 4 cortexes fixation for bilmechanical properties,and its' stress is more balance and can reduce postoperative complcations.

Ankle Injuries ; physiopathology ; surgery ; Biomechanical Phenomena ; Fibula ; injuries ; surgery ; Fracture Fixation, Internal ; methods ; Humans ; Joint Instability ; physiopathology ; prevention & control ; Reconstructive Surgical Procedures ; methods ; Tibia ; injuries ; surgery

OBJECTIVETo search for an optimum method for testicular prothesis implantation in the treatment of testis loss.

METHODSWe retrospectively analyzed the surgical methods and outcomes of 53 cases of terminal prostate cancer and 4 cases of unilateral testicular torsion treated by implantation of testicular prothesis with the polypropylene mesh.

RESULTSThe 57 male patients all received testicular prothesis with the polypropylene mesh. All the patients were satisfied with the appearance and size of the scrotum after surgery. No scrotal hematoma, prosthesis infection, or autoimmune disease occurred postoperatively.

CONCLUSIONTestis loss is not a rare condition clinically, for the treatment of which surgical implantation of testicular prothesis with the polypropylene mesh can achieve both a fine tissue compatibility and a desirable scrotal appearance.

Humans ; Male ; Polypropylenes ; Prostatic Neoplasms ; surgery ; Prostheses and Implants ; Retrospective Studies ; Scrotum ; Spermatic Cord Torsion ; surgery ; Surgical Mesh ; Testis

Objective To investigate the effects of heart displacement on hemodynamics during off-pump coronary artery bypass grafting (OP-CABG) while the sites for anastomosis were being exposed. Methods Forty-seven patients of both sexes (36 male, 11 female) aged 50-82 years undergoing OP-CABG were enrolled in the study. Preoperative cardiac function was assessed : class Ⅱ in 22 patients; Ⅲ in 23 and Ⅳ in 2 according to NYHA classification.The mean ejection fraction was 0.55?0.14 before surgery.They received on average 3.2 grafts. Premedication consisted of intramuscular morphine 10 mg, midazolam 3-5 mg and scopolamine 0.3 mg.Before induction of anesthesia ECG and SpO2 were monitored and radial artery was cannulated for continuous direct BP monitoring. Anesthesia was induced with midazolam 0.1 nig?kg-1 , fentanyl 4?g?kg-1 and pancuronium 0.1 mg?g-1 iv.The patients were mechanically ventilated after tracheal intubation and PETCO2 was maintained at about 40 mm Hg. Anesthesia was maintained with isoflurane and 50%-60% N2O in O2 and intermittent intravenous boluses of fentanyl and pancuronium. Swan-Ganz catheter which can continuously monitor mixed venous blood O2 saturation (SvO2) was placed in pulmonary artery via right internal jugular vein. SvO2, cardiac output (CO), BP, pulmonary arterial pressure (PAP) and HR were continuously monitored. Right atrial pressure (RAP) and PAWP were measured intermittently. Cardiac index (CI),stroke index (SI),systemic vascular resistance index (SVRI),PVRI, left and right ventricular work index (LVWI,RVWI) and left and right ventricular stroke work index (LVSWI,RVSWI) were calculated. The hemodynamic parameters were recorded after induction of anesthesia before surgery (T1,baseline),before heart displacement (T2), while anastomosis to anterior descending branch was being made (T3), while anastonosis to right coronary artery or posterior descending branch (T4) and to left circumflex artery or diagonal branch (T5) was being made, after normal heart position was resumed (T6) and at the end of operation (T7). Results While anastomosis to the anterior descending branch was being made (T3) SI and LVSWI significantly decreased as compared with the baseline (P