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

Acute Coronary Syndrome ; etiology ; Aortic Valve Insufficiency ; Female ; Heart Valve Prosthesis ; adverse effects ; Humans ; Middle Aged ; Prosthesis Failure

OBJECTIVETo investigate the apoptosis and proliferation effect of matrine on human medulloblastoma cell line D341 in vitro and the effect of the expression of the related caspase 3 and caspase 9 proteins.

METHODSThe D341 cells were cultivated successfully in vitro. Then the cells were divided into 5 groups according to the concentration of matrine (0.5 mg/mI group, 1.0 mg/ml group, 1.5 mg/ml group, 2.0 mg/ml group and the control group was 0 mg/ml). All the experiments were repeated three times. The cell morphologic and structure change was observed with the optical microscope and the transmission electron microscope. The proliferation of D341 cell was analyzed using Cell Counting Kit-8 assay. Apoptosis was detected by Annexin V-FITC/PI double staining. The expression of Caspase3 and Caspase9 was detected by Western blot.

RESULTSWith the effect of matrine, the proliferation inhibition rate gradually increased with drug concentrations increasing, and there was a significant difference (P < 0.01). The inhibitory effect of matrine on cell proliferation was different with the different treatment time, there was a significant difference between the 24 h to 72 h groups (P < 0.01). The apoptotic rate increased with matrine concentrations increasing. There were significant differences between the group of 0.5 mg/mI or 1.0 mg/mI to the group of 1.5 mg/mI or 2.0 mg/mI (P < 0.05). The apoptotic rate increased with the prolonged treatment time. There were significant differences between the group of 24 h or 48 h to the group of 72 h ( P < 0.05). With the increase of matrine concentration, the expression of Caspase 3 and Caspase 9 increased (P < 0.01).

CONCLUSIONMatrine induces the apoptosis, and inhibits the proliferation of human medulloblastoma D341 cells in vitro by up-regulation of the expression level of Caspase3, Caspase9.

Alkaloids ; pharmacology ; Apoptosis ; Caspase 3 ; metabolism ; Caspase 9 ; metabolism ; Cell Line, Tumor ; Cell Proliferation ; Cerebellar Neoplasms ; metabolism ; pathology ; Humans ; Medulloblastoma ; metabolism ; pathology ; Quinolizines ; pharmacology ; Up-Regulation

Female ; Humans ; Infant ; Mitochondrial Proton-Translocating ATPases ; deficiency ; genetics ; Mutation

Humans ; Sinus of Valsalva ; Death, Sudden, Cardiac/etiology* ; Coronary Stenosis/complications*

In order to study the contraindications of the compatibility of Flos Genkwa-Radix et Rhizoma Glycyrrhizae, in this study, the solubilizing and poisoning essence were explored. In this experiment, chromatographic assay, field emission scanning electron microscopy, MTT cytotoxicity evaluation, and other methods were used to study the main chemical components, morphology and toxicity of the ethyl acetate part of Flos Genkwa and its co-decoction with glycyrrhizic acid, in order to clarify Flos Genkwa-Radix et Rhizoma Glycyrrhizae incompatibility provides a new idea for the research on incompatibility of Flos Genkwa-Radix et Rhizoma Glycyrrhizae. The results showed that after co-decoction of the ethyl acetate part of Flos Genkwa with glycyrrhizic acid, high performance liquid chromatography (HPLC) detected the dissolution of the toxic component yuanhuacine of 54.8%, while yuanhuacine chromatographic peak was not detected in the Flos Genkwa ethyl acetate part of the single decoction. The increase of co-decoction dissolution rate was observed by scanning electron microscopy, and it was found that glycyrrhizic acid uniformly dispersed the fat-soluble components of Flos Genkwa into nano-scale particles, which improved the solubility and stability in the solution. Furthermore, the results of cytotoxicity evaluation showed that the survival rate of cells decreased after co-decoction, 4',6-diamidino-2-phenylindole (DAPI) staining also gave the same results. In summary, the co-decoction of the ethyl acetate part of Flos Genkwa with glycyrrhizic acid promotes the dissolution of the toxic component yuanhuacine, and makes the part form uniformly distributed nanoparticles, which is conducive to the absorption of the ingredient and increases the toxicity.

BACKGROUNDHamstring (HS) autograft and bone-patellar tendon-bone allograft are the most common choice for reconstruction of anterior cruciate ligament (ACL). There was a little report about the clinical outcome and difference of arthroscopic ACL reconstruction using allograft and autograft. This study aimed to compare the clinical outcome of autograft and allograft reconstruction for ACL tears.

METHODSA total of 106 patients who underwent surgery because of ACL tear were included in this study. The patients were randomly divided into two groups, including 53 patients in each group. The patients in group I underwent standard ACL reconstruction with HS tendon autografts, while others in group II underwent reconstruction with bone-patellar tendon-bone allograft. All the patients were followed up and analyzed; the mean follow-up was 81 months (range: 28-86 months). Clinical outcomes were evaluated using the International Knee Documentation Committee (IKDC), Lysholm scores, physical instability tests, and patient satisfaction questionnaires. The complication rates of both groups were compared. Tibial and femoral tunnel widening were assessed using lateral and anteroposterior radiographs.

RESULTSAt the end of follow-up, no significant differences were found between the groups in terms of IKDC, Lysholm scores, physical instability tests, patient satisfaction questionnaires, and incidences of arthrofibrosis. Tibial and femoral tunnel widening was less in the HS tendon autografts. This difference was more significant on the tibial side.

CONCLUSIONSIn the repair of ACL tears, allograft reconstruction is as effective as the autograft reconstruction, but the allograft can lead to more tunnel widening evidently in the tibial tunnel, particularly.

Adolescent ; Adult ; Anterior Cruciate Ligament Injuries ; surgery ; Anterior Cruciate Ligament Reconstruction ; methods ; Female ; Humans ; Male ; Patellar Ligament ; surgery ; Transplantation, Autologous ; methods ; Transplantation, Homologous ; methods ; Treatment Outcome ; Young Adult

Objective To investigate the effect of 620 nm red light on chondrogenic differentiation in rat precartilaginous stem cells (PSCs). Methods Rats' PSCs were isolated and purified using magnetically activated cell sorting and cultured in vitro.The PSCs were exposed once to 620 nm wavelength red light from a light-emitting diode (LED) with an irradiation energy of 0.5 J/cm2,1 J/cm2,2 J/cm2 or 4 J/cm2.Any effect was confirmed by Alcian blue staining,immunohistochemistry and observing histomorphological changes under a light microscope,as well as detection using a reverse transcription polymerase chain reaction (RT-PCR). Results After being induced for 14 d,the PSCs exhibited polygonal and round shapes. Alcian blue and type Ⅱ collagen immunohistoehemistry staining showed positive results,but the control group had no significant change.RT-PCR showed that the mRNA expression of Sox9 and type Ⅱ collagen increased significantly compared with the control group. Conclusion Low energy 620 nm red light can enhance chondrogenic differentiation in PSCs significantly.

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.